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Применить Всего найдено 10367. Отображено 200.
24-05-2023 дата публикации

АНТИБАКТЕРИАЛЬНЫЕ КОМПОЗИЦИИ

Номер: RU2796503C2
Принадлежит: ВОКХАРДТ ЛИМИТЕД (IN)

Изобретение относится к области фармацевтики и может быть использовано для лечения, контроля или предупреждения бактериальной инфекции. Антибактериальная фармацевтическая композиция представлена в форме раствора объемом 100 мл с pH в диапазоне от 9 до 10,5 и осмолярностью в диапазоне от приблизительно 250 до приблизительно 350 мосмоль/л, который содержит: (а) 1186,7 мг S-(-)-9-фтор-6,7-дигидро-8-(4-гидроксипиперидин-1-ил)-5-метил-1-оксо-1H,5H-бензо[i,j]хинолизин-2-карбоновой кислоты, соль L-аргинина, (b) 1333 мг L-аргинина или его фармацевтически приемлемой соли, и (c) 580 мг хлорида натрия. Обеспечивается повышение стабильности композиции. 8 з.п. ф-лы, 3 табл., 1 пр.

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27-11-2011 дата публикации

ПРОИЗВОДНЫЕ БЕНЗОХИНОЛИЗИН-2-КАРБОНОВОЙ КИСЛОТЫ

Номер: RU2434867C2
Принадлежит: ВОКХАРДТ ЛТД (IN)

Настоящее изобретение относится к новым производным бензохинолизин-2-карбоновой кислоты формулы I и их фармацевтически приемлемым сольватам, в которой R обозначает СН3 или СН(СН3)2 и R1 обозначает С1-С6 алкил или фенил, в случае необходимости замещенный одним или более заместителями, выбранными из C1-С6 алкила или нитро. Также изобретение относится к способу получения соединения формулы I, к фармацевтической композиции на основе соединения формулы I и применению соединения формулы I. Технический результат: получены новые производные бензохинолизин-2-карбоновой кислоты, обладающие улучшенной растворимостью в воде широком диапазоне рН, которые могут использоваться для лечения бактериальных грамположительных, грамотрицательных и анаэробных инфекций. 4 н. и 14 з.п. ф-лы, 2 табл.

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20-07-2016 дата публикации

СПОСОБЫ ПРИМЕНЕНИЯ (+)-1,4-ДИГИДРО-7-[(3S, 4S)-3-МЕТОКСИ-4-(МЕТИЛАМИНО)-1-ПИРРОЛИДИНИЛ]-4-ОКСО-1-(2-ТИАЗОЛИЛ)-1,8-НАФТИРИДИН-3-КАРБОНОВОЙ КИСЛОТЫ ДЛЯ ЛЕЧЕНИЯ РАКА

Номер: RU2592231C2

Группа изобретений относится к медицине, а именно к онкологии, и может быть использована для лечения острого миелогенного лейкоза. Для этого пациенту, страдающему острым миелогенным лейкозом, вводят (+)-1,4-дигидро-7-[(3S,4S)-3-метокси-4-(метиламино)-1-пирролидинил]-4-оксо-1-(2-тиазолил)-1,8-нафтиридин-3-карбоновую кислоту в дозах от приблизительно 30 мг/мдо менее чем 50 мг/ми от более чем 90 до 100 мг/м. Группа изобретений обеспечивает лечение острого миелогенного лейкоза при введении указанного соединения в эффективных и безопасных дозах. 2 н. и 9 з.п. ф-лы, 20 ил., 16 табл., 11 пр.

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23-05-2018 дата публикации

НОВЫЕ СОЕДИНЕНИЯ

Номер: RU2654857C2

Изобретение относится к новым соединениям формулы (I-A) или (I-B):или, а также к фармацевтическим композициям, содержащим указанные соединения. Технический результат: получены новые соединения, пригодные для применения в профилактике или лечении заболевания или состояния, опосредованного FGFR киназой, например рака. 5 н. и 16 з.п. ф-лы, 1 табл., 43 пр.

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29-05-2018 дата публикации

АЗОТСОДЕРЖАЩЕЕ ГЕТЕРОЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ ИЛИ ЕГО СОЛЬ

Номер: RU2655604C2

Изобретение относится к азотсодержащему гетероциклическому соединению, представленному следующей формулой [1], или к его фармацевтически приемлемым солям:в которой Zпредставляет собой N или CR; Xпредставляет собой NRили S; Rпредставляет собой атом водорода или атом галогена; Rпредставляет собой атом водорода или атом галогена; Rпредставляет собой атом водорода, атом галогена, аминогруппу или Салкоксигруппу; значения остальных заместителей указаны в формуле изобретения. Изобретение также относится к азотсодержащему гетероциклическому соединению формулы [1а], к средству для лечения заболевания, при котором ингибирование PI3K и/или ERK является эффективным, к ингибитору PI3K и/или ERK и к индивидуальным азотсодержащим гетероциклическим соединениям. Технический результат: получены новые соединения, обладающие ингибиторной активностью в отношении PI3K и/или ERK. 5 н. и 14 з.п. ф-лы, 10 табл., 955 пр.

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25-03-2020 дата публикации

ФАРМАЦЕВТИЧЕСКИЙ СОСТАВ ПОЛИМЕРНОГО ПРОИЗВОДНОГО, СОДЕРЖАЩЕГО КАМПТОТЕЦИН

Номер: RU2717690C2

Изобретение относится к фармацевтической промышленности, а именно к фармацевтическому противоопухолевому лиофилизированному составу, включающему рН регулирующий агент и блок-сополимер формулы (1), содержащий звено глутаминовой кислоты, связанное с производным камптотецина:,где R, R, R– H или (C-C) алкильная группа; А – (С-С) алкиленовая группа; R– H, (С-С) ацильная группа или (С-С) алкоксикарбонильная группа; R– -ОН и/или -N(R)CONH(R); Rи R– (C-C) алкильная группа; каждый из t, d, e - целое число; t=45-450; (d+e)=6-60; доля d и e относительно (d+e) соответственно 1-100% и 0-99%; доля звеньев глутаминовой кислоты, когда R-ОН и когда R-N(R)CONH(R), составляет соответственно 15-60% и 0-50% относительно (d+e). При этом рН водного раствора предложенного состава при концентрации блок-сополимера формулы (1) 1 мг/мл в пересчете на производное камптотецина составляет от 3,0 до 6,5. Изобретение обеспечивает улучшение стабильности состава при хранении, сохраняя свойства блок-сополимера образовывать ...

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12-10-2018 дата публикации

ПРЕПАРАТ ДЛИТЕЛЬНОГО ВЫСВОБОЖДЕНИЯ ДЛЯ СНИЖЕНИЯ ЧАСТОТЫ МОЧЕИСПУСКАНИЯ И СПОСОБ ЕГО ПРИМЕНЕНИЯ

Номер: RU2669565C2

Группа изобретений относится к медицине, а именно к урологии, и может быть использована для снижения частоты мочеиспускания. Для этого субъекту вводят фармацевтическую композицию, состоящую из эффективных количеств золпидема, составленного для немедленного высвобождения, и одного или более анальгетических средств, составленных для длительного или отсроченного высвобождения. Также предложена фармацевтическая композиция, состоящая из эффективных количеств золпидема, составленного для немедленного высвобождения, и одного или более анальгетических средств, составленных для длительного или отсроченного высвобождения. Группа изобретений обеспечивает эффективное подавление сокращений гладкой мускулатуры мочевого пузыря. 2 н.п. ф-лы, 9 табл., 8 пр., 1 ил.

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27-10-2005 дата публикации

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ЦЕРЕБРОВАЗОДИЛАТИРУЮЩЕЙ И НООТРОПНОЙ АКТИВНОСТЬЮ

Номер: RU2262931C2
Автор:

Изобретение относится к химико-фармацевтической промышленности и касается фармацевтической композиции в виде твердой лекарственной формы, обладающей церебровазодилатирующей и ноотропной активностью, включающей в качестве активных компонентов винпоцетин и пирацетам. Композиция обладает высокой эффективностью при более низких дозах за счет синергетического эффекта и обладает высокой биодоступностью. 2 з.п. ф-лы, 9 табл.

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13-08-2020 дата публикации

СПОСОБ ПОЛУЧЕНИЯ (4S)-4-(4-ЦИАНО-2-МЕТОКСИФЕНИЛ)-5-ЭТОКСИ-2,8-ДИМЕТИЛ-1-4-ДИГИДРО-1,6-НАФТИРИДИН-3-КАРБОКСАМИДА И ЕГО ОЧИСТКИ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ФАРМАЦЕВТИЧЕСКОГО АКТИВНОГО ИНГРЕДИЕНТА

Номер: RU2729998C2

Изобретение относится к области органической химии, а именно к способу получения (4S)-4-(4-циано-2-метоксифенил)-5-этокси-2,8-диметил-1,4-дигидро-1,6-нафтиридин-3-карбоксамида формулы (I), который включает взаимодействие соединения формулы (XIV) или (XIVa) с диметилсульфатом с получением соединения формулы (XV) или (XVa), которые без выделения направляют на восстановление с помощью 1.21 экв. REDAL (натрия бис(2-метоксиэтокси)алюминия дигидрида) и 1.28 экв. N-метилпиперазина с получением альдегида формулы (XVI) или (XVIa), который вводят далее в реакцию без выделения с получением нитрила формулы (VI), которое растворяют в 3-7-кратном количестве изопропанола, 5-10 мол. % пиперидина и 5-10 мол. % ледяной уксусной кислоты при 30°С, вводят далее в реакцию с соединением формулы (VII) с получением соединения (VIIIa+b), которое затем реагирует с 4-амино-5-метилпиридоном с получением соединения (X), которое вводят в реакцию при перемешивании с 2.5-5 экв. триэтилортоацетата в диметилацетамиде при ...

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25-12-2018 дата публикации

КОМБИНИРОВАННЫЕ ТЕРАПЕВТИЧЕСКИЕ СРЕДСТВА, СОДЕРЖАЩИЕ ОКСАЗОЛИДИНОН-ХИНОЛОНЫ, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ЛЕЧЕНИЯ БАКТЕРИАЛЬНЫХ ИНФЕКЦИЙ

Номер: RU2675847C2

Изобретение относится к фармацевтической промышленности, а именно к комбинации для лечения и/или профилактики бактериальных инфекций. Предложены комбинация для лечения и/или профилактики бактериальных инфекций, включающая по меньшей мере одно гибридное соединение оксазолидинон-хинолона или его фармакологически приемлемую соль, сольват или гидрат и по меньшей мере одно дополнительное антибактериальное соединение, выбранное из следующих соединений: цефтриаксон, ампициллин, фосфомицин, полипептиды, линезолид и моксифлоксацин; фармацевтическая композиция для лечения и/или профилактики бактериальных инфекций; набор компонентов для лечения и/или профилактики бактериальных инфекций; способ лечения субъекта, страдающего от бактериальной инфекции или подверженного бактериальной инфекции. Предложенная комбинация для лечения и/или профилактики бактериальных инфекций, содержащая гибридное средство оксазолидинон-хинолона с антибактериальным соединением, вследствие синергического воздействия повышает ...

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21-05-2020 дата публикации

Производные хинолона как ингибиторы рецептора фактора роста фибробластов

Номер: RU2721723C2

Изобретение относится к области органической химии, а именно к гетероциклическому соединению формулы (III) и/или к его фармацевтически приемлемой соли, где J представляет собой N; J’ представляет собой CR, где Rпредставляет собой водород; Ar представляет собой фенил, замещенный тремя или четырьмя заместителями, независимо выбранными из С-Салкокси и галогена; Rпредставляет собой С-С алкил, С-С алкинил, галоген-С-С алкил, С-С циклоалкил, необязательно замещенный гидрокси-группой; С-С циклоалкил-Салкил, гидрокси-С-С алкил, С-С алкокси-С-С алкил, С-С гетероциклил, содержащий один гетероатом, выбранный из O; или С-С гетероциклил-С-С алкил, содержащий один или два гетероатома, выбранных из N или O; Q представляет собой С-С алкилен или С-С алкилен замещенный двумя метилами; и X представляет собой группу формулы (a), где Rпредставляет собой водород или С-С алкил; и Rпредставляет собой водород или С-С алкил; Y представляет собой –CO-; Rпредставляет собой водород или С-С алкил; и Rпредставляет собой ...

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14-08-2018 дата публикации

ДИГИДРОНАФТИРИДИНЫ И РОДСТВЕННЫЕ СОЕДИНЕНИЯ, ПОДХОДЯЩИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗ ДЛЯ ЛЕЧЕНИЯ ПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ

Номер: RU2664055C2

Изобретение относится к дигидронафтиридинам и родственным соединениям. В настоящем изобретении предложено применение соединений, ингибирующих cKIT киназу с широким диапазоном мутаций с-KIT, включая комплексные проявления первичных мутаций (эксоны KIT 9 или 11) и вторичных мутаций KIT (эксоны 13, 14, 17 и 18), которые могут возникать в клеточной линии опухолей с резистентными GIST. 7 з.п. ф-лы, 3 табл., 115 пр.

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08-10-2019 дата публикации

ГИБРИДНЫЕ АНТИБАКТЕРИАЛЬНЫЕ СРЕДСТВА ОКСАЗОЛИДИНОН-ХИНОЛОН, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ПАРЕНТЕРАЛЬНОГО ВВЕДЕНИЯ ДЛЯ ЛЕЧЕНИЯ ИЛИ ПРОФИЛАКТИКИ БАКТЕРИАЛЬНЫХ ЗАБОЛЕВАНИЙ

Номер: RU2702364C2

Группа изобретений относится к медицине и может быть использована для лечения или профилактики бактериальных заболеваний у пациента. Для этого парентерально вводят гибридное средство оксазолидинон-хинолон. Также предложены фармацевтическая композиция, способ лечения, применение гибридного средства оксазолидинон-хинолон. Группа изобретений обеспечивает парентеральное лечение или профилактику кишечных заболеваний, вызванных грамположительными бактериями. 4 н. и 15 з.п. ф-лы, 2 табл., 2 пр.

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06-05-2019 дата публикации

АНТИТЕЛА ПРОТИВ СТЕНОЧНОЙ ТЕЙХОЕВОЙ КИСЛОТЫ И ИХ КОНЪЮГАТЫ

Номер: RU2687044C2
Принадлежит: ДЖЕНЕНТЕК, ИНК. (US)

Изобретение относится к области биохимии, в частности к конъюгату анти-WTA (стеночная тейхоевая кислота) антитело-антибиотик для лечения бактериальной инфекции, вызванной Staphylococcus aureus, а также к фармацевтической композиции, его содержащей. Также раскрыт способ получения конъюгата анти-WTA антитело-антибиотик, включающий конъюгирование промежуточного соединения антибиотик-линкер с анти-WTA антителом. Изобретение позволяет эффективно осуществлять лечение бактериальной инфекции, вызванной Staphylococcus aureus. 3 н. и 20 з.п. ф-лы, 22 ил., 5 табл., 24 пр.

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14-10-2021 дата публикации

КОМБИНИРОВАННАЯ ТЕРАПИЯ ПРОТИВООПУХОЛЕВЫМ АЛКАЛОИДОМ

Номер: RU2757373C2
Принадлежит: ФАРМА МАР, С.А. (ES)

Настоящее изобретение относится к фармацевтической синергической комбинации для лечения рака, содержащей терапевтически эффективное количество РМ01183 или его фармацевтически приемлемой соли и терапевтически эффективное количество ингибитора митоза, где ингибитор митоза выбран из паклитаксела, доцетаксела, винкристина и винорелбина, при этом рак, подлежащий лечению, выбран из рака легкого, саркомы, рака предстательной железы, рака желудка, рака яичника, гепатомы, рака молочной железы, колоректального рака, рака почки и рака головного мозга. Техническим результатом изобретения является увеличение или потенцирование терапевтической эффективности противораковых лекарственных средств. 3 н. и 12 з.п. ф-лы, 296 ил., 26 табл., 21 пр.

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01-03-2021 дата публикации

ПИРАНОДИПИРИДИНОВОЕ СОЕДИНЕНИЕ

Номер: RU2743998C2

Изобретение относится к соединениям, представленным формулами (I)-(XXII), или их фармацевтически приемлемым солям:Изобретение также относится к фармацевтической композиции, обладающей ингибирующим действием в отношении рецептора α-амино-3-гидрокси-5-метил-4-изоксазолпропионовой кислоты (AMPA), на основе указанных соединений. Технический результат – получены новые соединения и фармацевтическая композиция на их основе, которые могут найти применение в медицине для лечения эпилепсии. 12 н. и 4 з.п. ф-лы, 4 табл., 2 ил., 22 пр.

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18-02-2021 дата публикации

СПОСОБ ПОЛУЧЕНИЯ (4S)-4-(4-ЦИАНО-2-МЕТОКСИФЕНИЛ)-5-ЭТОКСИ-2,8-ДИМЕТИЛ-1,4-ДИГИДРО-1,6-НАФТИРИДИН-3-КАРБОКСАМИДА И ЕГО ОЧИСТКА ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ФАРМАЦЕВТИЧЕСКОГО БИОЛОГИЧЕСКИ АКТИВНОГО ВЕЩЕСТВА

Номер: RU2743429C2

Изобретение относится к области органической химии, а именно к способу получения соединения (4S)-4-(4-циано-2-метоксифенил)-5-этокси-2,8-диметил-1,4-дигидро-1,6-нафтиридин-3-кар-боксамида формулы (I), отличающийся тем, что рацемическое соединение формулы (XIII) разделяют на соответствующие энантиомеры, причем соединение формулы (XIII) получают путем взаимодействия соединения формулы (XVIII) со сложным ортоэфиром формулы (XX), в которой R означает водород или метил, при кислотном катализе и температуре 100-120°С. Также изобретение относится к соединениям формул (XVIII) и (XVI a,b), их применению в способе получения соединения формулы (I), способам получения соединений формул (XVIII), (XVI a,b) и (XIII). Технический результат: разработан новый способ получения соединения формулы (I), полезного в качестве нестероидного антагониста минералокортикоидного рецептора, отличающийся высоким общим выходом и чистотой целевого соединения и низкими производственными расходами. 10 н. и 2 з.п. ф-лы, 8 ...

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23-07-2018 дата публикации

КОМБИНИРОВАННАЯ ТЕРАПИЯ С ИСПОЛЬЗОВАНИЕМ АНТИТЕЛ К КЛАУДИНУ 18.2 ДЛЯ ЛЕЧЕНИЯ РАКА

Номер: RU2662066C2

Группа изобретений относится к медицине и касается способа лечения или предотвращения ракового заболевания, где раковые клетки экспрессируют CLDN18.2, включающего введение пациенту антитела, обладающего способностью связываться с CLDN18.2, в комбинации со средством, стимулирующим γδ Т-клетки и интерлейкин-2, где средство, стимулирующее γδ Т-клетки, представляет собой бисфосфонат. Группа изобретений также касается медицинского препарата для лечения или предотвращения ракового заболевания, содержащего указанные вещества; набора для лечения или предотвращения ракового заболевания. Группа изобретений обеспечивает значительное увеличение общей ADCC-активности. 3 н. и 32 з.п. ф-лы, 26 ил., 1 табл., 17 пр.

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28-03-2019 дата публикации

АЗАСПИРОПРОИЗВОДНЫЕ В КАЧЕСТВЕ АНТАГОНИСТОВ TRPM8

Номер: RU2683309C2

Изобретение относится к соединению формулы (I) или его фармацевтически приемлемым солям. В формуле (I) A обозначает фенил, 5-6-членный гетероарил, содержащий от 1 до 3 гетероатомов, выбранных из группы, состоящей из азота, кислорода и серы, или 9-членный бициклический гетероарил, содержащий один гетероатом, выбранный из азота и кислорода; B обозначает фенил, инданил, 5-6-членный гетероарил, содержащий от 1 до 4 гетероатомов, выбранных из группы, состоящей из азота, кислорода и серы, или 9-11-членный бициклический гетероарил, содержащий от 1 до 4 гетероатомов, выбранных из группы, состоящей из азота и кислорода; L независимо выбран из группы, состоящей из химической связи, кислорода, серы, -NR-, -(CRR)-, -O(CRR)-, -(CRR)O-, -N(R)(CRR)O- и -O(CRR)N(R)-; X независимо выбран из группы, состоящей из -CH-, кислорода и NH; значения остальных радикалов указаны в формуле изобретения. Изобретение также относится к индивидуальным соединениям, к применению соединения, к способу лечения состояния или ...

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10-02-2013 дата публикации

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ (ВАРИАНТЫ) И СПОСОБ ЕЕ СТЕРИЛИЗАЦИИ

Номер: RU2474425C2
Принадлежит: МЕДА АБ (SE)

Изобретение относится к фармацевтической композиции для местного применения, включающей лекарственное соединение модификатора иммунного ответа, которое устойчиво к стерилизации и пригодно для локального нанесения непосредственно на участки тканей с нарушением кожного покрова, где указанная композиция подвергнута стерилизации посредством облучения электронным пучком, а лекарственное соединение представляет собой 1-(2-метилпропил)-1Н-имидазо[4,5-с]хинолин-4-амин (имиквимод). Изобретение также относится к композиции для местного применения в упакованном виде, включающей упаковочный материал и указанную выше фармацевтическую композицию. Настоящее изобретение обеспечивает устойчивую к стерилизации фармацевтическую композицию. 2 н. и 24 з.п. ф-лы, 5 табл., 1 пр.

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15-02-2018 дата публикации

ИНГИБИТОРЫ СЕРИН/ТРЕОНИН КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ

Номер: RU2644947C2

Изобретение относится к области органической химии, а именно к гетероциклическому соединению формулы (I) или к его стереоизомеру или фармацевтически приемлемой соли, гдепредставляет собой CH или N;представляет собой (i) NH(CH)CH, гдеравно 0 или 1, или (ii) 1-алкил-4-арил-пирролидин-3-иламин, где алкил представляет собой Cалкил, необязательно замещенный фенильным кольцом, и арил представляет собой фенил, замещенный метокси;представляет собой (а) водород, (b) C-Cалкил, необязательно замещенный гидроксильной группой, (c) 4-5-членный гетероцикл, содержащий 1 гетероатом, выбранный из N, где гетероцикл необязательно замещен одной группой, выбранной из группы, состоящей из галогена, или (d) 5-членный гетероарил, содержащий 1 или 2 гетероатома, выбранных из N, где гетероарил необязательно замещен одной группой, выбранной из Cалкила;представляет собой фенил, пиридинил или индолил, необязательно замещенный 1-2 группами, независимо выбранными из (а) Cалкокси, (b) галогена, (c) Cгалогеналкокси, (d) ...

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11-10-2021 дата публикации

ЛИПОСОМНЫЕ КОМПОЗИЦИИ, ИСПОЛЬЗУЕМЫЕ ДЛЯ ДОСТАВКИ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Номер: RU2757110C2
Принадлежит: ИПСЕН БИОФАРМ ЛТД. (GB)

Группа изобретений относится к области медицины, а именно к противоопухолевой иринотекановой липосомной композиции, содержащей иринотекан сахарозооктасульфат, инкапсулированный в липидные везикулы, содержащие один или более фосфолипидов, причем липосомная композиция содержит суммарное количество в диапазоне от 150 до 550 мг основания иринотекана на ммоль суммарных фосфолипидов, а также относится к противоопухолевой иринотекановой липосомной композиции, содержащей липосомы, в которых инкапсулирован иринотекан в форме соли, выбранной из пирофосфата, трифосфата и инозитгексафосфата, причем указанная композиция содержит лецитин, холестерин и амфипатический полимер, и указанная композиция имеет от около 0,15 до около 1,5 моль иринотекана на моль суммарного липида, также относится к противоопухолевой иринотекановой липосомной композиции, содержащей липидные везикулы, в виде липосомной дисперсии, где в липидных везикулах инкапсулирован иринотекан и сахарозооктасульфат, так что иринотекан и сахарозооктасульфат ...

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19-06-2017 дата публикации

Способ лечения морфометрических изменений макулярной области при полиморбидных соматических состояниях

Номер: RU2622759C1

Изобретение относится к области медицины, а именно к офтальмологии, и предназначено для лечения морфометрических изменений макулярной области при полиморбидных соматических состояниях. Для исследований используют оптическую когерентную томографию сетчатки. При уплощении рельефа макулярной области и увеличении средней центральной толщины сетчатки свыше 300 мкм диагностируют диабетический макулярный отек. При наличии кистозных полостей в ядерных и плексиформных слоях сетчатки - кистозный макулярный отек. Назначают лечение 2,0% раствором дорзопта утром и вечером в глаз непрерывно. При наличии неравномерных контуров сетчатки и складок сетчатки неправильной формы дополнительно диагностируют эпиретинальность мембраны и дополнительно назначают закапывание 0,1% раствора диклофенака три раза в день в исследуемый глаз в течение месяца. Затем отдых в течение месяца и повтор лечения раствором диклофенака по описанной выше схеме. Повторно назначают курс препаратами: винпоцетином, пирацетамом, детралексом ...

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21-01-2020 дата публикации

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01-06-2020 дата публикации

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28-04-2018 дата публикации

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26-07-2019 дата публикации

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16-01-2020 дата публикации

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16-03-2018 дата публикации

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06-03-2018 дата публикации

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20-01-2021 дата публикации

Номер: RU2019114665A3
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14-01-2021 дата публикации

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02-11-2021 дата публикации

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21-02-2019 дата публикации

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14-11-2022 дата публикации

Ингибиторы цитохрома 11В2 человека

Номер: RU2783521C1

Изобретение относится к соединению общей формулы (I) или его фармацевтически приемлемой соли, где R1 выбирается независимо и представляет собой: (С1-С5)-алкил, который замещен нитрильной группой, (С3-С7)-циклоалкил, 5-6-членный гетероцикл, содержащий 1 атом кислорода и/или 1 атом азота и необязательно замещенный 1-2 заместителями R2, 5-6-членный гетероарил, содержащий 1 атом серы и/или 1-2 атома азота и необязательно замещенный 1-2 заместителями R3, С6-арил, необязательно замещенный 1-4 заместителями R4, бицикл, состоящий из фенильного кольца, соединенного с 5-членным гетероциклом, содержащим -С(=О)-, 1 атом азота и необязательно замещенный 1-3 заместителями R5; R2 выбирается независимо и представляет собой водород, -С(=О)-СН3; R3 выбирается независимо и представляет собой водород, (С1-С3)-алкил или частично или полностью галогенированный (С1-С3)-алкил; R4 выбирается независимо представляет собой водород, галоген, (С1-С3)-алкил, -О(С1-С3)-алкил, -CONR6''R7''; R5 выбирается независимо и ...

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10-03-2014 дата публикации

СТАБИЛИЗИРОВАННЫЕ АНТИТЕЛА ПРОТИВ АНГИОПОЭТИНА-2 И ИХ ПРИМЕНЕНИЕ

Номер: RU2509085C2
Принадлежит: МЕДИММУН ЛИМИТЕД (GB)

Изобретение относится к области иммунологии. Представлено антитело против ангиопоэтина-2 (Ang-2), причем указанное антитело включает вариабельную область тяжелой цепи SEQ ID No:7 (MEDI5) и вариабельную область легкой цепи, выбранную из SEQ ID No:3 (MEDI1); SEQ ID No:4 (MEDI2); SEQ ID No:5 (MEDI3); и SEQ ID No:6 (MEDI4). Раскрыта выделенная нуклеиновая кислота, кодирующая указанное антитело. Описана композиция для применения в ингибировании ангиогенеза раковой опухоли у животного, нуждающегося в этом, содержащая указанное выделенное антитело в терапевтически эффективном количестве и эксципиент. Предложенные вариантные антитела обладают повышенной стабильностью при хранении по сравнению с исходным антителом 3.19.3, из которого они получены, и способны конкурировать с Tie-2 за связывание с Ang-2. 3 н. и 9 з.п. ф-лы, 17 ил., 15 табл., 13 пр.

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24-01-2022 дата публикации

Способ комбинированного лечения метастатического колоректального рака у больных с резектабельными метастазами в печени и при отсутствии мутаций в генах KRAS и BRAF

Номер: RU2764955C1

Изобретение относится к медицине, а именно к онкологии, и может быть использовано для комбинированного лечения метастатического колоректального рака у больных с резектабельными метастазами в печени и при отсутствии мутаций в генах KRAS и BRAF. Способ включает введение цетуксимаба 500 мг/м2 внутривенно капельно в 1 день, иринотекана внутривенно капельно в 1 день, оксалиплатина 85 мг/м2 внутривенно капельно в 1 день, инфузию лейковорина 200 мг/м2 внутривенно капельно в 1 день и 5-фторурацила внутривенно капельно. Проводят три курса предоперационного лечения, при этом инфузию лейковорина проводят в 1 и 2 дни по 200 мг/м2, доза иринотекана составляет 165 мг/м2, инфузию 5-фторурацила в дозе 3200 мг/м2 проводят в течение 46 часов, перерыв между курсами составляет 12 дней. После завершения предоперационного лечения при наличии объективного ответа опухоли выполняют симультанную радикальную операцию на первичной опухоли и на метастатических очагах в печени R0, в послеоперационном периоде проводят ...

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19-12-2023 дата публикации

СОЕДИНЕНИЕ НА ОСНОВЕ ДИГИДРОНАФТИРИДИНОНА, И СПОСОБ ЕГО ПОЛУЧЕНИЯ, И ЕГО ПРИМЕНЕНИЕ В МЕДИЦИНЕ

Номер: RU2809869C1

Изобретение относится к соединению на основе дигидронафтиридинона формулы (I), где A, B, R1-R6 определены в формуле изобретения, его фармацевтически приемлемой соли и стереоизомерам. Соединение обладает селективным ингибирующим эффектом в отношении RIPK1. Также предложена фармацевтическая композиция, содержащая соединение формулы (I), и ее применение в получении лекарственного средства для лечения заболеваний или состояний, связанных с RIPK1. 5 н. и 11 з.п. ф-лы, 3 табл., 90 пр. (I) ...

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08-04-2019 дата публикации

Бициклические конденсированные гетероарильные или арильные соединения в качестве модуляторов IRAK4

Номер: RU2684324C1
Принадлежит: ПФАЙЗЕР ИНК. (US)

Изобретение относится к гетероциклическому соединению формул IIс или IIе, где Rпредставляет собой C-Салкил; Rпредставляет собой водород; Rпредставляет собой водород; каждый из Rи Rнезависимо представляет собой водород или фтор; Rи Rнезависимо представляют собой водород или C-Салкил; и Rпредставляет собой водород. Также изобретение относится к конкретным соединениям и фармацевтической композиции на основе указанных соединений. Технический результат: получены новые гетероциклические соединения, обладающие IRAK4-ингибирующей активностью. 3 н.п. ф-лы, 1 табл., 33 пр.

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22-05-2024 дата публикации

Способ комбинированного лечения метастатического колоректального рака у больных с резектабельными метастазами в печени при отсутствии мутаций в генах KRAS

Номер: RU2819653C1

Изобретение относится к области медицины, а именно к онкологии, и может быть использовано для комбинированного лечения метастатического колоректального рака у больных с резектабельными метастазами в печени при отсутствии мутаций в генах KRAS. Способ включает проведение курсов противоопухолевой лекарственной терапии, в первый день внутривенно капельно вводят: иринотекан в дозе 165 мг/м2, оксалиплатин в дозе 85 мг/м2, цетуксимаб в дозе 500 мг/м2, капецитабин перорально ежедневно в два приема в дозе 2500 мг/м2 с 1 по 14 дни. Перерыв между курсами составляет 7 дней, проводят 3 курса предоперационного лечения, радикальную операцию и 3 курса адъювантного лечения. Использование изобретения позволяет достичь улучшения результатов комбинированного лечения метастатического колоректального рака у больных с резектабельными метастазами в печени при отсутствии мутаций в генах KRAS за счет повышения частоты объективных ответов опухоли и снижения количества нежелательных явлений при проведении лекарственного ...

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12-02-2024 дата публикации

Способ комбинированного лечения метастатического колоректального рака у больных с резектабельными метастазами в печени

Номер: RU2813334C1

Изобретение относится к медицине, а именно к онкологии, и может быть использовано для комбинированного лечения метастатического колоректального рака (мКРР) у больных с резектабельными метастазами в печени. Способ включает проведение курсов противоопухолевой лекарственной терапии с использованием иринотекана в дозе 165 мг/м2 внутривенно капельно в 1 день, оксалиплатина в дозе 85 мг/м2 внутривенно капельно в 1 день, капецитабина перорально ежедневно в два приема, применяют 3 курса предоперационного лечения по вышеуказанной схеме, радикальную операцию и 3 курса адъювантного лечения, при этом прием капецитабина в дозе 2500 мг/м2 проводят с 1 по 14 дни, перерыв между курсами составляет 7 дней. Использование изобретения позволяет достичь улучшения результатов комбинированного лечения мКРР у больных с резектабельными метастазами в печени за счет повышения частоты объективных ответов опухоли и снижения количества нежелательных явлений при проведении лекарственного противоопухолевого лечения, увеличения ...

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27-01-2008 дата публикации

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ВИНФЛУНИНА, ПРЕДНАЗНАЧЕННАЯ ДЛЯ ПАРЕНТЕРАЛЬНОГО ВВЕДЕНИЯ, СПОСОБ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

Номер: RU2006126708A
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... 1. Фармацевтическая композиция винфлунина, отличающаяся тем, что она имеет форму стабильного и стерильного водного раствора водорастворимой соли винфлунина с рН от 3 до 4. 2. Композиция по п.1, отличающаяся тем, что соль винфлунина является дитартратом винфлунина. 3. Композиция по п.2, отличающаяся тем, что композиция состоит из дитартрата винфлунина и воды для получения препарата для инъекций. 4. Композиция по п. 1, отличающаяся тем, что она содержит буферную систему рН для поддержания значения рН от 3 до 4. 5. Композиция по п.4, отличающаяся тем, что молярность буферной системы рН составляет от 0,002 до 0,2М. 6. Композиция по п.4, отличающаяся тем, что буферная система рН состоит из буфера уксусная кислота/ацетат натрия или буфера лимонная кислота/цитрат натрия. 7. Композиция по п.2, отличающаяся тем, что композиция содержит дитартрат винфлунина с концентрацией основного винфлунина от 1 до 50 мг/мл, предпочтительно от 25 до 30 мг/мл, в частности 25 мг/мл. 8. Композиция по п.2, отличающаяся ...

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10-02-2011 дата публикации

ЛИОФИЛИЗИРОВАННАЯ ИНЪЕЦИРУЕМАЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ПОЛУСИНТЕТИЧЕСКИХ АЛКАЛОИДОВ VINCA И УГЛЕВОДА, СТАБИЛЬНАЯ ПРИ КОМНАТНОЙ ТЕМПЕРАТУРЕ

Номер: RU2009128327A
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... 1. Фармацевтическая композиция, состоящая из полусинтетического водорастворимого производного алкалоида vinca, стабильного при комнатной температуре, где указанное производное находится в лиофилизированной форме, полученной в присутствии по меньшей мере одного углевода. ! 2. Композиция по п.1, где полусинтетическое водорастворимое производное алкалоида vinca находится в форме водорастворимой соли. ! 3. Композиция по п.2, где водорастворимая соль полусинтетического производного алкалоида vinca представляет собой винфлунин или винорелбин. ! 4. Композиция по п.1, содержащая, в дополнение к углеводу(ам) в качестве эксципиентов для лиофилизации, по меньшей мере одну буферную систему. ! 5. Композиция по п.1, где углевод(ы) выбран(ы) из моносахаридов, восстановленных или невосстановленных, олигосахаридов или полисахаридов, таких как инулин, в частности, дисахаридов. ! 6. Композиция по п.5, где углевод(ы) выбран(ы) из сахарозы, трегалозы и лактозы. ! 7. Композиция по п.4, где буферная система, ...

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27-10-2016 дата публикации

ИНГИБИТОРНЫЕ СОЕДИНЕНИЯ

Номер: RU2015112580A
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... 1. Соединение формулы I, показанное ниже:,где:группа W представляет N или C-R;группа X представляет СН или N;группа Z представляет N или С-Н;группа Rвыбрана из хлор-, (1-6С)алкила, (1-8С)гетероалкила, арила, арил(1-2С)алкила, гетероарила, гетероарил(1-2С)алкила, гетероциклила, гетероциклил(1-2С)алкила, (3-8С)циклоалкила, (3-8С)циклоалкил(1-2С)алкила, NRR, OR, C(O)R, C(O)OR, OC(O)R, N(R)OR, N(R)С(О)OR, С(О)N(R)R, N(R)C(O)R, S(O)R(где p=0, 1 или 2), SON(R)R, N(R)SOR, N(R)SORили SON(R)R;и где группа Rнеобязательно замещена одной или несколькими группами заместителей, выбранных из фтор-, хлор-, трифторметила, трифторметокси, циано, нитро, гидрокси, амино, карбокси, карбамоила, сульфамоила, (1-4С)алкила, (1-4С)алкокси, S(O)CH(где q=0, 1 или 2), метиламино или диметиламино, арила, арил(1-2С)алкила, гетероарила, гетероарил(1-2С)алкила, гетероциклила, гетероциклил(1-2С)алкила, (3-8С)циклоалкила или (3-8С)циклоалкил(1-2С)алкила,и где любая (1-4С)алкильная, (1-4С)алкокси, арильная, гетероарильная ...

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19-12-2019 дата публикации

ДИАЗАБЕНЗОФТОРАНТРЕНОВЫЕ СОЕДИНЕНИЯ

Номер: RU2697513C9

Изобретение относится к соединению формулы (I), к его фармацевтически приемлемым солям или таутомерам, где Rнезависимо выбран из H или необязательно замещенного RS(=O)NH; Rнезависимо выбран из Cалкила; Rвыбран из,,,,,,,,,,или; где от нуля до двух Tпредставляют собой N, а остальные представляют собой C(R); Dвыбран из -C(R)(R)-, -N(R)-, -O-, -S- или -C(=O)-; Tвыбран из N или C(R); каждый из Dнезависимо выбран из -C(R)(R)-, -O-, -S- или -C(=O)-; до двух Tпредставляют собой N, а остальные представляют собой C(R); необязательно любые два из Rи Rсвязаны вместе с общим атомом или группой атомов с образованием одного 5-6-членного кольца; каждый из R, Rи Rнезависимо выбран из H, CN, NH, C(=O)NHC(=O)N(CH); или Rнезависимо выбран из группы, состоящей из необязательно замещенных RCалкила, Cгетероалкила, тетрагидропиранила, тетрагидропиридинила, морфолинила, пиридинила,,,, CFCHCF, CHCHFили фенила; Rвыбран из OH или R; Rвыбран из Cалкила, Cгетероалкила, Cциклоалкила, гетероциклического Cалкила, который ...

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10-07-2016 дата публикации

КОМБИНИРОВАННАЯ ТЕРАПИЯ С ИСПОЛЬЗОВАНИЕМ АНТИТЕЛ К КЛАУДИНУ 18.2 ДЛЯ ЛЕЧЕНИЯ РАКА

Номер: RU2014152107A
Принадлежит:

... 1. Способ лечения или предотвращения ракового заболевания, включающий введение пациенту антитела, обладающего способностью связываться с CLDN18.2, в комбинации со средством, стимулирующим γδ Т-клетки.2. Способ по п. 1, согласно которому γδ Т-клетки являются Vγ9Vδ2 Т-клетками.3. Способ по п. 1 или 2, согласно которому средство, стимулирующее γδ Т-клетки, является бисфосфонатом.4. Способ по п. 1 или 2, согласно которому средство, стимулирующее γδ Т-клетки, является азотсодержащим бисфосфонатом (аминобисфосфонатом).5. Способ по п. 1 или 2, согласно которому средство, стимулирующее γδ Т-клетки, выбирают из группы, состоящей из золедроновой кислоты, клодроновой кислоты, ибандроновой кислоты, памидроновой кислоты, ризедроновой кислоты, минодроновой кислоты, олпадроновой кислоты, алендроновой кислоты, инкадроновой кислоты и их солей.6. Способ по п. 1 или 2, согласно которому средство, стимулирующее γδ Т-клетки, вводится в комбинации с интерлейкином-2.7. Способ по п. 1 или 2, согласно которому ...

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13-11-2017 дата публикации

КОМБИНАЦИЯ

Номер: RU2016116915A
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21-02-2018 дата публикации

ПРОИЗВОДНЫЕ 1,5-НАФТИРИДИНА И ИНГИБИТОРЫ MELK, СОДЕРЖАЩИЕ ИХ

Номер: RU2645339C1

Изобретение относится к области органической химии, а именно к гетероциклическому соединению формулы (I) или к его фармацевтически приемлемой соли, где Xвыбирают из прямой связи или -NН; Qвыбирают из группы, включающей C-Cциклоалкил, фенил, пиридил, пиразолил, пиримидинил, пиперидил, (C-Cциклоалкил)-C-Cалкил и (3-10-членный неароматический гетероциклил)-C-Cалкил; где Qнеобязательно замещен одним A; Xвыбирают из -CO- и -SO-; Rвыбирают из группы, включающей C-Cалкил и C-Cциклоалкил, которые необязательно замещены одной гидроксильной группой; Rвыбирают из группы, включающей атом галогена, C-Cарил, 5-10-членный гетероарил и 3-10-членный неароматический гетероциклил; где арил, гетероарил и гетероциклил необязательно замещены 1-3 заместителями A; R, Rи Rпредставляют собой атом водорода; Aвыбирают из группы, включающей C-Cалкил, -NRR, -OR, 3-10-членный неароматический гетероциклил и (CD)N-C-Cалкил; где алкил и гетероциклил необязательно замещены одним Aи где гетероциклил необязательно замещен ...

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10-01-2009 дата публикации

ПРИМЕНЕНИЕ АТАЗАНАВИРА ДЛЯ УЛУЧШЕНИЯ ФАРМАКОКИНЕТИКИ ЛЕКАРСТВЕННЫХ СРЕДСТВ, МЕТАБОЛИЗИРУЕМЫХ UGT1A1

Номер: RU2007125130A
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... 1. Способ улучшения фармакокинетических характеристик перорального лекарственного средства, непосредственно метаболизируемого UGT1A1, который предусматривает пероральное введение млекопитающему, нуждающемуся в лечении лекарственным средством, эффективного количества комбинации лекарственного средства, или его фармацевтически приемлемой соли, и атазанавира, или его фармацевтически приемлемой соли. 2. Способ по п.1, где лекарственное средство, непосредственно метаболизируемое UGT1A1, представляет соединение формулы I, или его фармацевтически приемлемую соль где R1 означает C1-6алкил, замещенный: (1) N(RA)-C(=O)-N(RC)RD, (2) N(RA)-C(=O)-C1-6алкилен-N(RC)RD, (3) N(RA)SO2RB, (4) N(RA)SO2N(RC)RD, (5) N(RA)-C(=O)-C1-6алкилен-SO2RB, (6) N(RA)-C(=O)-C1-6алкилен-SO2N(RC)RD, (7) N(RA)C(=O)C(=O)N(RC)RD, (8) N(RA)-C(=O)-HetA, (9) N(RA)C(=O)C(=O)-HetA или (10) HetB; R2 означает -C1-6алкил; или, альтернативно, R1 и R2 соединены вместе так, что соединение формулы I представляет соединение формулы II R3 ...

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20-07-2012 дата публикации

ДИАЗАКАРБАЗОЛЫ И СПОСОБЫ ПРИМЕНЕНИЯ

Номер: RU2010154105A
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... 1. Соединение формулы (I), (I-a) или (I-b) или его сольват, гидрат или соль: ! ! X представляет собой CR2 или N; ! Y представляет собой CR4 или N; ! Z представляет собой CR8 или N; при условии, что не более чем один из X, Y и Z представляет собой N одновременно; ! R2 представляет собой H, галоген, CN, CF3, -OCF3, OH, -NO2, C1-C5алкил, -О(C1-C5алкил), -S(C1-C5алкил) или N(R22)2; ! R3 представляет собой H, галоген, CN, -O-R9, -N(R22)-R9, -S(O)P-R9 или R9; ! p равен 0, 1 или 2; ! R4 представляет собой H, галоген, CN, CF3, -OCF3, OH, -NO2, ! -(CR14R15)nC(=Y')OR11, -(CR14R15)nC(=Y')NR11R12, -(CR14R15)nNR11R12, ! -(CR14R15)nOR11, -(CR14R15)nS(O)pR11, -(CR14R15)nNR12C(=Y')R11, ! -(CR14R15)nNR12C(=Y')OR11, -(CR14R15)nNR12C(=Y')NR11R12, ! -(CR14R15)nNR12SO2R11, -(CR14R15)nOC(=Y')R11, ! -(CR14R15)nOC(=Y')NR11R12, -(CR14R15)nS(O)2NR11R12, алкил, алкенил, алкинил, циклоалкил, гетероциклил, арил или гетероарил, где указанный алкил, алкенил, алкинил, циклоалкил, гетероциклил, арил и гетероарил необязательно ...

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10-07-2010 дата публикации

НОВОЕ ГЕТЕРОЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ ИЛИ ЕГО ПРОМЕЖУТОЧНОЕ СОЕДИНЕНИЕ

Номер: RU2008151754A
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... 1. Соединение, представленное общей формулой ! [Формула 1] ! ! где R1 обозначает необязательно замещенную C2-C12 алкильную, арильную или гетероциклическую группу; X1 обозначает необязательно замещенную C2-C4 алкиленовую группу; X2 обозначает группу, представленную общей формулой NR2 (где R2 обозначает атом водорода, необязательно замещенную низшую алкильную группу или имино-защитную группу), или связь; X3 обозначает группу, представленную общей формулой NR3 или CR4R5NR3 (где R3 обозначает атом водорода, необязательно замещенную низшую алкильную группу или имино-защитную группу; и R4 и R5 являются одинаковыми или различными, и каждый из них представляет собой атом водорода или необязательно замещенную низшую алкильную группу, или R4 и R5 вместе образуют оксо группу), или связь; X4 обозначает необязательно замещенную низшую алкиленовую, низшую алкениленовую или низшую алкиниленовую группу или связь; X5 обозначает атом кислорода, атом серы, сульфинильную группу, сульфонильную группу, группу ...

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10-02-2009 дата публикации

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ (ВАРИАНТЫ) И СПОСОБ ЕЕ СТЕРИЛИЗАЦИИ

Номер: RU2007129104A
Принадлежит:

... 1. Фармацевтическая композиция местного применения, включающая лекарственное соединение модификатора иммунного ответа, которое устойчиво к стерилизации и пригодно для локального нанесения непосредственно на участки тканей с нарушением кожного покрова, отличающаяся тем, что она подвергнута стериализации, а лекарственное соединение выбрано из группы, состоящей из 1-(2-метилпропил)-1Н-имидазо[4,5-с]хинолин-4-амина (имиквимод), 2-метил-1-(2-метилпропил)-1Н-имидазо[4,5-с][1,5]нафтиридин-4-амина (сотиримод) и 4-амино-альфа,альфа-диметил-2-этоксиметил-1Н-имидазо[4,5-с]хинолин-1-этанола (резиквимод). 2. Композиция по п.1, отличающаяся тем, что композиция была стерилизована облучением, предпочтительно облучением электронным пучком. 3. Композиция по п.1, отличающаяся тем, что она содержит лекарственные примеси, каждая из которых в отдельности составляет в количестве не выше 0,3 мас.% от веса соединения, выбираемого из группы, состоящей из имиквимода, сотиримода и резиквимода, при этом общий вес лекарственных ...

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10-02-2012 дата публикации

КОМПОЗИЦИИ, ВКЛЮЧАЮЩИЕ НЕНАСЫЩЕННЫЕ ЖИРНЫЕ КИСЛОТЫ И СОЕДИНЕНИЯ, ВЫСБОЖДАЮЩИЕ ОКСИД АЗОТА, И ИХ ПРИМЕНЕНИЕ ДЛЯ УСИЛЕНИЯ КОГНИТИВНОЙ ФУНКЦИИ И СВЯЗАННЫХ С НЕЙ ФУНКЦИЕЙ

Номер: RU2010132637A
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... 1. Композиция, пригодная для усиления когнитивной функции и связанных с ней функций у животного, включающая одну или более ненасыщенных жирных кислот (НЖК) и одно или более соединений, высвобождающих оксид азота (NO-ВС), в количестве, эффективном для усиления когнитивной функции и связанных с ней функций у животного. ! 2. Композиция по п.1, где животное является человеком или домашним животным. ! 3. Композиция по п.2, где домашнее животное является собакой или кошкой. ! 4. Композиция по п.1, где животное является стареющим животным. ! 5. Композиция по п.1, в которой НЖК включает одно или более из природного рыбьего жира, АЛК, ЭПК, ДПК, ДГК или другой n-3 жирной кислоты из любого источника. ! 6. Композиция по п.1, в которой НЖК является рыбьим жиром. ! 7. Композиция по п.1, включающая от примерно 0,1% до примерно 50% НЖК. ! 8. Композиция по п.1, в которой NO-ВС является аргинином или его производным, высвобождающим оксид азота. ! 9. Композиция по п.1, в которой NO-ВС является цитруллином ...

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20-12-2013 дата публикации

КОМПОЗИЦИИ {3-[5-(4-ХЛОРФЕНИЛ)-1Н-ПИРРОЛО[2, 3]ПИРИДИН-3-КАРБОНИЛ]-2,4-ДИФТОРФЕНИЛ}АМИДА ПРОПАН-1-СУЛЬФОНОВОЙ КИСЛОТЫ И ИХ ПРИМЕНЕНИЕ

Номер: RU2012123958A
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... 1. Способ получения твердой дисперсии, содержащей аморфную форму соединения формулы 1и HPMCAS, включающий следующие стадии:(a) растворение соединения формулы 1 и HPMCAS в том же самом органическом растворителе, при этом получают одну органическую фазу,(b) непрерывное добавление органической фазы, полученной на стадии (а), в водную фазу, которая присутствует в смесительной камере, причем указанная смесительная камера оборудована смесительным устройством с высоким сдвигом и двумя дополнительными отверстиями, которые соединяют указанную смесительную камеру с замкнутой системой, через которую указанная водная фаза циркулирует и проходит через смесительную камеру,(c) высаживание смеси, включающей аморфную форму соединения формулы 1 и HPMCAS, из водной фазы, указанной в стадии (b), при включенном смесителе с высоким сдвигом, а указанная водная фаза циркулирует через смесительную камеру и замкнутую систему, при этом образуется водная суспензия осадка,(d) непрерывная циркуляция водной суспензии ...

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27-08-2013 дата публикации

КОМБИНИРОВАННАЯ ТЕРАПИЯ, ВКЛЮЧАЮЩАЯ МОДУЛЯТОРЫ СК2

Номер: RU2012106518A
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... 1. Способ лечения или облегчения неопластического расстройства, включающий введение субъекту, нуждающемуся в таком лечении или облегчении, терапевтически эффективного количества соединения Формулы Iили его фармацевтически приемлемой соли или эфира,где Zпредставляет собой N или CR;каждый RR, Rи Rнезависимо представляет собой Н или необязательно замещенный С1-С8 алкил, С2-С8 гетероалкил, С2-С8 алкенил, С2-С8 гетероалкенил, С2-С8 алкинил, С2-С8 гетероалкинил, С1-С8 ацил, С2-С8 гетероацил, С6-С10 арил, С5-С12 гетероарил, С7-С12 арилалкил или С6-С12 гетероарилалкильную группу,или каждый RR, Rи Rнезависимо представляет собой галоген, CF, CFN, OR, NR, NROR, NRNR, SR, SOR, SOR, SONR, NRSOR, NRCONR, NRCOOR, NRCOR, CN, COOR, карбокси биоизостеру, CONR, OOCR, COR или NO,каждый Rнезависимо представляет собой необязательно замещенный С1-С8 алкил, С2-С8 гетероалкил, С2-С8 алкенил, С2-С8 гетероалкенил, С2-С8 алкинил, С2-С8 гетероалкинил, С1-С8 ацил, С2-С8 гетероацил, С6-С10 арил, С5-С12 гетероарил, С7 ...

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27-01-2014 дата публикации

1,7-ДИАЗАКАРБАЗОЛЫ И ИХ ПРИМЕНЕНИЕ ПРИ ЛЕЧЕНИИ РАКА

Номер: RU2012127877A
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... 1. Соединение формулы (I), (I-a) или (I-b) или его сольват, гидрат или соль:Х представляет собой CRили N;Y представляет собой CRили N;Z представляет собой CRили N, притом, что не более чем один из X, Y и Z представляет собой N одновременно;Rпредставляет собой Н, гало, CN, CF, -OCF, ОН, -NO, C-Cалкил, -O(C-Cалкил), -S(C-Cалкил) или N(R);Rпредставляет собой Н, гало, CN, -O-R, -N(R)-R, -S(O)-Rили R;p представляет собой 0, 1 или 2;Rпредставляет собой Н, галоген, CN, CF, -OCF, ОН, -NO, -(CRR)C(=Y')OR, -(CRR)C(=Y')NRR, -(CRR)NRR, -(CRR)OR, -(CRR)S(O)R, -(CRR)NRC(=Y')R, -(CRR)NRC(=Y')OR, -(CRR)NRC(=Y')NRR, -(CRR)NRSOR, -(CRR)OC(=Y')R, -(CRR)OC(=Y')NRR, -(CRR)S(O)NRR, алкил, алкенил, алкинил, циклоалкил, гетероциклил, арил или гетероарил, где указанные алкил, алкенил, алкинил, циклоалкил, гетероциклил, арил и гетероарил необязательно замещены от одной до четырех групп R;каждое n независимо представляет собой 0-5;Rпредставляет собой Н, гало, CN, CF, -OCF, ОН, -NO, -(CRR)C(=Y')OR, -(CRR)C(=Y')NRR ...

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27-02-2013 дата публикации

ЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ, СОДЕРЖАЩЕЕ ГЕТЕРОАТОМ

Номер: RU2011134637A
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... 1. Соединение, имеющее общую формулу (I), или его фармакологически приемлемая соль:в которой каждый заместитель определяется следующим образом:А представляет собой 3-10-членную гетероциклильную группу, необязательно замещенную группой (группами), выбранной(ыми) из A1, и 3-10-членная гетероциклильная группа представляет собой группу, выбранную из группы, состоящей из азетидинильной, пирролидинильной, пиперидинильной, морфолинильной, 1,4-диоксанильной, пиперазинильной, азепанильной, 1,4-диазепанильной, пирролильной, тиазоильной, пиридильной, тетрагидропиридильной, тетрагидропиранильной, тетрагидрофуранильной, тетрагидроизохинолинильной и декагидроизохинолинильной группы,A1:гидроксильная группа, атом галогена, цианогруппа, нитрогруппа, карбамоильная группа, ди-С1-С6-алкилкарбамоильная группа, С1-С6-алкильная группа, необязательно замещенная группой (группами), выбранной(ыми) из А2,С1-С6-алкоксигруппа, необязательно замещенная группой (группами), выбранной(ыми) из А2,С1-С6-алкилкарбонильная ...

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20-09-2015 дата публикации

ТРИЦИКЛИЧЕСКИЕ ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И ИНГИБИТОРЫ JAK

Номер: RU2014109363A
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... 1. Соединение, представленное формулой (I):[где кольцо Aпредставлено следующей формулой (II-1) или формулой (II-2):(где Tявляется атомом азота или CR, Uявляется атомом азота или CR, Tявляется одинарной связью или CRR, и Eявляется атомом кислорода или атомом серы),Xявляется атомом азота или CR,Yявляется CR,Rявляется атомом водорода, атомом галогена, Cалкильной группой илиCгалоалкильной группой,кольцо BявляетсяCциклоалканом, Cциклоалкеном (составляющая кольцо метиленовая группа Cциклоалкана и Cциклоалкена может быть заменена карбонильной группой), 3 - 14-членным неароматическим гетероциклом, Cароматическим карбоциклом или 5 - 10-членным ароматическим гетероциклом,Lявляется одинарной связью, Cалкиленовой группой, Cалкениленовой группой или Cалкиниленовой группой (Cалкиленовая группа, Cалкениленовая группа и Cалкиниленовая группа не замещены или замещены одним или более одинаковыми или различными заместителями, независимо выбранными из группы, состоящей из атомов галогенов, гидроксигрупп, аминогрупп ...

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20-06-2015 дата публикации

СОЕДИНЕНИЯ ПИРРОЛИДИНИЛМОЧЕВИНЫ И ПИРРОЛИДИНИЛТИОМОЧЕВИНЫ КАК ИНГИБИТОРЫ КИНАЗЫ TRKA

Номер: RU2013155456A
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... 1. Соединение Формулы I:или его стереоизомеры, таутомеры или фармацевтически приемлемые соли, сольваты или пролекарства, где:фрагмент Y-B и фрагмент NH-C(=X)-NH находятся в транс-конфигурации;R, R, Rи Rнезависимо выбраны из Н и (1-3С)алкила;X представляет собой О, S или NH;Rпредставляет собой (1-3С алкокси)(1-6С)алкил, (трифторметокси)(1-6С)алкил, (1-3С сульфанил)(1-6С)алкил, монофтор(1-6С)алкил, дифтор(1-6С)алкил, трифтор(1-6С)алкил, тетрафтор(2-6С)алкил, пентафтор(2-6С)алкил, циано(1-6С)алкил, аминокарбонил(1-6С)алкил, гидрокси(1-6С)алкил, дигидрокси(2-6С)алкил, (1-6С)алкил, (1-3С алкиламино)(1-3С)алкил, (1-4С алкоксикарбонил)(1-6С)алкил, амино(1-6С)алкил, гидрокси(1-3С алкокси)(1-6С)алкил, ди(1-3С алкокси)(1-6С)алкил, (1-3С алкокси)трифтор(1-6С)алкил, гидрокситрифтор(1-6С)алкил, (1-4С алкоксикарбонил)(1-3С алкокси)(1-6С)алкил, гидроксикарбонил(1-3С алкокси)(1-6С)алкил, гетAr(СН)или Ar(СН);Rпредставляет собой Н, F или ОН;Y представляет собой связь, -O- или -ОСН-;В представляет собой Ar ...

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20-02-2015 дата публикации

НОВОЕ БИЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ ИЛИ ЕГО СОЛЬ

Номер: RU2013136895A
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... 1. Соединение, представленное следующей общей формулой (I), или его соль:где по меньшей мере один из X, X, Xи Xпредставляет собой N или N-оксид, и остальные одинаковы или различны, и каждый представляет собой C-R;любой один или два из Y, Y, Yи Yпредставляют собой C-R, и остальные одинаковы или различны, и каждый представляет собой CH или N;Rпредставляет собой необязательно замещенную моноциклическую или бициклическую ненасыщенную гетероциклическую группу, содержащую от 1 до 4 гетероатомов, выбранных из N, S и О;Rпредставляет собой атом водорода, необязательно замещенную алкильную группу, содержащую от 1 до 6 атомов углерода, необязательно замещенную циклоалкильную группу, содержащую от 3 до 7 атомов углерода, или необязательно замещенную алкенильную группу, содержащую от 2 до 6 атомов углерода;Rпредставляет собой цианогруппу или -CO-R;Rпредставляет собой атом водорода, атом галогена, алкильную группу, содержащую от 1 до 6 атомов углерода, алкоксигруппу, содержащую от 1 до 6 атомов углерода ...

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20-02-2015 дата публикации

КОМБИНАЦИЯ СИРОСИНГОПИНА И МИТОХОНДРИАЛЬНЫХ ИНГИБИТОРОВ ДЛЯ ЛЕЧЕНИЯ РАКА И ДЛЯ ИММУНОСУПРЕССИИ

Номер: RU2013137380A
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... 1. Фармацевтическая композиция, содержащая сиросингопин и митохондриальный ингибитор.2. Фармацевтическая композиция по п.1, содержащая сиросингопин и метформин или фенформин.3. Фармацевтическая композиция по п.1, содержащая сиросингопин и метформин.4. Фармацевтическая композиция по п.1, содержащая сиросингопин и митохондриальный ингибитор, выбранный из ротенона, пиерицидина A, эпиберберина, 2-теноилтрифторацетона (TTFA), антимицина A, олигомицина, карбонилцианид-пара-трифторметоксифенилгидразона (FCCP) и ставудина.5. Фармацевтическая композиция по п.1, содержащая сиросингопин и олигомицин.6. Фармацевтическая композиция по одному из пп.1-5, в которой соотношение количеств (мас./мас.) сиросингопина и митохондриального ингибитора составляет от 1 к 10 до 1 к 1000.7. Фармацевтическая композиция по п.3, в которой соотношение количеств (мас./мас.) сиросингопина и метформин составляет от 1 к 10 до 1 к 200.8. Фармацевтическая композиция по п.5, в которой соотношение количеств (мас./мас.) сиросингопина ...

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27-08-2015 дата публикации

ПРОИЗВОДНЫЕ N-(ИМИДАЗОЛИДИН-2-ИЛИДИН)ХИНОЛИНА КАК МОДУЛЯТОРЫ АДРЕНЕРГИЧЕСКИХ РЕЦЕПТОРОВ АЛЬФА-2

Номер: RU2014106364A
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... 1. Соединение Формулы I, его энантиомеры, диастереомеры, таутомеры или их фармацевтически приемлемая сольв котором:Rпредставляет собой водород, замещенный или незамещенный Салкил или галоген;Y представляет собой СН или N;Х представляет собой СН или N; исоединение N-(имидазолидин-2-илидин)хинолин-4-амина;кроме N-(4,5-дигидро-1Н-имидазол-2-ил)-3-хинолинамина.2. Соединение по п.1, отличающееся тем, что:Rпредставляет собой водород, метил, бром или хлор;Y представляет собой СН или N;Х представляет собой СН или N; икроме соединения N-(4,5-дигидро-1Н-имидазол-2-ил)-3-хинолинамин.3. Соединение по п.1, отличающееся тем, что:Rпредставляет собой метил, бром или хлор;Y представляет собой СН или N; иХ представляет собой СН или N.4. Соединение по п.1, отличающееся тем, что:Rпредставляет собой метил;Y представляет собой СН или N; иХ представляет собой СН или N.5. Соединение по п.1, отличающееся тем, что:Rпредставляет собой бром;Y представляет собой СH или N; иХ представляет собой СН или N.6. Соединение ...

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27-10-2008 дата публикации

СПОСОБЫ И КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ ГИПЕРЛИПИДЕМИИ

Номер: RU2007114290A
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... 1. Способ предупреждения или лечения гиперлипидемии у субъекта-млекопитающего, включающий введение эффективного в анти-гиперлипидемическом отношении количества берберина или родственного берберину соединения, или производного соединения формулы I, или их фармацевтически приемлемых соли, изомера, энантиомера, сольвата, гидрата, полиморфа или пролекарства указанному субъектуФормула Iгде каждый из R, R, R, R, R, R, R, Rи/или Rобозначает независимо, в совокупности или в любом сочетании группу, выбранную из водорода, галогена, гидрокси, алкила, алкокси, нитро, амино, трифторметила, циклоалкила, (циклоалкил)алкила, алканоила, алканоилокси, арила, ароила, аралкила, нитрила, диалкиламино, алкенила, алкинила, гидроксиалкила, аминоалкила, алкиламиноалкила, диалкиламиноалкила, галогеналкила, карбоксиалкила, алкоксиалкила, карбокси, алканоиламино, карбамоила, карбамила, карбониламино, алкилсульфониламино или гетероциклической групп.2. Способ по п.1, в котором Rвыбирают из метила, этила, гидрокси или ...

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20-07-2016 дата публикации

НОВЫЕ СОЕДИНЕНИЯ

Номер: RU2014153591A
Принадлежит:

... 1. Соединение формулы (I-A) или (I-B):иливключая его любую таутомерную или стереохимически изомерную форму, гдедля (I-A)Xявляется N, Хявляется N, и Хявляется СН; илиXявляется CR, Хявляется N, и Хявляется СН; илиХявляется CR, Хявляется CR, и Хявляется N;для (I-B)Хявляется N или CR;каждый Rнезависимо выбран из гидроксила, галогена, цианогруппы, Салкила, Салкенила, Салкинила, Салкокси, гидроксиСалкила, гидроксиСалкокси, галогенСалкила, галогенСалкокси, гидроксигалогенСалкила, гидроксигалогенСалкокси, СалкоксиСалкила, галогенСалкоксиСалкила, СалкоксиСалкила, где каждый Салкил необязательно может быть замещен одной или двумя гидроксильными группами, гидроксигалогенСалкоксиСалкила, R, Салкила, который замещен R, Салкила, который замещен -C(=O)-R, Салкокси, который замещен R, Салкокси, который замещен -C(=O)-R, -C(=O)-R, Салкила, который замещен -NRR, Салкила, который замещен -С(=O)-NRR, Салкокси, который замещен -NRR, Салкокси, который замещен -С(=O)-NRR, -NRRи -С(=O)-NRR; или когда две группы ...

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29-03-2001 дата публикации

Use of gemifloxacin compounds, which can be active against bacterial strains resistant to other antibiotics, in treatment of infections caused by respiratory tract pathogenic bacteria

Номер: DE0019945885A1
Автор: NACHTRÄGLICH
Принадлежит:

Gemifloxacin compounds are used to modulate the metabolism of respiratory tract pathogenic bacteria, and to treat and prevent infection by such bacteria. Independent claims are included for: (1) modulating metabolism of respiratory tract pathogenic bacteria, comprising contacting the bacteria with a composition comprising a gemifloxacin compound, or derivative of this; and (2) treating or preventing infection by respiratory tract pathogenic bacteria, comprising administering a gemifloxacin compound to a mammal.

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26-12-2018 дата публикации

Small molecule modulators of human STING

Номер: GB0002563642A
Принадлежит:

... (I) A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof, for use in therapy is provided, wherein X is CR9R10, O, S, S=O or SO2; X1 is CR1 or N; X2 is CR2 or N; X3 is CR3 or N; the or each Z is independently CR11R12 or NR11; n is 1 or 2; Q is C=O, S=O, SO2, C=S or CR4R5; L is optionally substituted C1-C6alkyl, C1-C3polyfluoroalkyl, optionally substituted C3-C6cycloalkyl, optionally substituted C2-C6alkenyl, optionally substituted C2-C6alkynyl, C=O, S=O, SO2, -CH2C(O)-, -CH2CONH- or -CONH-; Y is an optionally substituted C1-C6alkyl, C1-C3polyfluoroalkyl, an optionally substituted C2-C6alkenyl, an optionally substituted C2-C6alkynyl, an optionally substituted C3-C6cycloalkyl, an optionally substituted mono or bicyclic 3 to 8 membered heterocycle; R6 is mono or bicyclic optionally substituted C5-C10aryl, mono or bicyclic optionally substituted 5 to 10 membered heteroaryl, optionally substituted C3-C6cycloalkyl or an optionally substituted mono or bicyclic 3 to ...

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29-08-2012 дата публикации

Vascular remodelling

Номер: GB0201212773D0
Автор:
Принадлежит:

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01-04-2020 дата публикации

Therapeutic mentods

Номер: GB0202001980D0
Автор:
Принадлежит:

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31-08-2015 дата публикации

Pyridinyl and fused pyridinyl triazolone derivatives

Номер: AP0201508646A0
Принадлежит:

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30-09-2001 дата публикации

Tricyclic inhibitors of ply (adp-robose) polymerases

Номер: AP0200102211A0
Автор:
Принадлежит:

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31-10-2008 дата публикации

Use of cantffln-6-one and its analogues in the treatment of pathologies linked to mycobacteria

Номер: AP0200804644D0
Принадлежит:

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31-10-2011 дата публикации

Thienopyridine derivatives for the treatment and prevention of dengue virus infections.

Номер: AP0201105901D0
Принадлежит:

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19-07-2005 дата публикации

Tricyclic inhibitors of poly(adp-ribose)polymerases.

Номер: OA0000011749A
Принадлежит:

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31-10-2016 дата публикации

NOVEL MACROCYCLIC COMPOUNDS

Номер: AP0201609483D0
Принадлежит:

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10-01-2006 дата публикации

Tricyclic inhibitors of poly (ADP-RIBOSE) polymerases.

Номер: AP0000001538A
Принадлежит:

Compounds of formula (I) are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.

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26-11-2004 дата публикации

Salt of naphthyridine carboxylic acid derivative.

Номер: AP0000001331A
Принадлежит:

... 7-(3-aminomethyl-4-methoxyiminopyrrolidin-1-yl) -1-cyclopropyl-6-fluoro -4-oxo-1,4-dihydro-1,8 -naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositons comprising them, and their use in antibacterial therapy.

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28-09-2000 дата публикации

Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use.

Номер: AP0000000872A
Принадлежит:

Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof: in which: R.1 is vinyl or ethyl; and R2 is a group R3, R4CH2~, or R5R6C=CH-; wherein each of R3 and R4 is an azabicyclic ring system or R5 and R^ together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

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19-08-2002 дата публикации

Trovafloxacin mesylate tablet.

Номер: AP0000001094A
Принадлежит:

Compositions, especially in the form of tablets containing the polymorph ii form of trovafloxacin mesylate, a lubricant, and microcrystalline cellulose (mc)as the diluent. Such compositions employing mc as a diluent exhibit good storage stability properties and dissolution.

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03-12-1999 дата публикации

Novel crystal form of anhydrous 7-(1a, 5a, 6a)-6-Amino-3-Azabicyclo(3.1.0) hex-3-YI)-6-Fluoro-1-(2,4- Difluorophenyl)-1,4-Dihydro-4-Oxo-1, 8-Naphthyridine-3-Carboxylic Acid, Methanesulfonic acid salt.

Номер: AP0000000788A
Принадлежит:

Theanhydrateof7-([1a,5a,6a]-6-amino-3-azabicyGlo[3.1.0]hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt has advantageous stability for formulation as an antibacterial agent.

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31-08-2015 дата публикации

Pyridinyl and fused pyridinyl triazolone derivatives

Номер: AP2015008646A0
Принадлежит:

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30-04-2016 дата публикации

NOVEL HETEROCYCLIC COMPOUNDS

Номер: AP2016009176A0
Принадлежит:

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30-11-2016 дата публикации

NAPHTHYRIDINEDIONE DERIVATIVES

Номер: AP2016009545A0
Принадлежит:

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19-01-2012 дата публикации

Compounds for the prevention and treatment of cardiovascular diseases

Номер: US20120015905A1
Автор: Henrik C. Hansen
Принадлежит: Resverlogix Corp

The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.

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19-04-2012 дата публикации

Mangiferin-Berberine Salt, Manufacturing Method and Use Thereof

Номер: US20120094941A1
Автор: Houlei Teng, Wei Wu
Принадлежит: Hainan Deze Drug Research Co Ltd

The present invention provides a mangiferin-berberine salt and manufacturing method thereof. Otherwise, the present invention also provides the use of mangiferin-berberine salt as AMPK activator.

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13-09-2012 дата публикации

Block Copolymer For Intraperitoneal Administration Containing Anti-Cancer Agent, Micelle Preparation Thereof, And Cancer Therapeutic Agent Comprising The Micelle Preparation As Active Ingredient

Номер: US20120231053A1
Принадлежит: Nippon Kayaku Co Ltd

To provide a therapeutic method using a water soluble, high molecular weight block polymer to enable that an intraperitoneally administered anti-cancer agent may maintain for a long-term retention in the abdominal cavity to enoughly exert the effect of the anti-cancer agent and reduce adverse side-effects thereof. A therapeutic agent as a micelle preparation, comprising a copolymer having a hydrophilic polymeric moiety and a polycarboxylic acid derivative moiety; and an anti-cancer agent bonding to or encapsulated in the copolymer, wherein the micelle preparation may exhibit sustained drug release capability, and enables an extension of a retention time period of the anti-cancer agent in an abdominal cavity, is provided. A superior life-prolonging effect was found in an intraperitoneal administration mouse model compared with a case in which only an encapsulated drug is administered, and thus the present invention was completed accordingly.

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11-10-2012 дата публикации

Pharmaceutical compositions providing enhanced drug concentrations

Номер: US20120259022A1
Принадлежит: Bend Research Inc

A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.

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01-11-2012 дата публикации

Novel heterocyclic acrylamides and their use as pharmaceuticals

Номер: US20120277207A1
Принадлежит: FAB PHARMA Sas

The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.

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15-11-2012 дата публикации

Kinase inhibitors useful for the treatment of proliferative diseases

Номер: US20120289540A1
Принадлежит: Deciphera Pharmaceuticals LLC

The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

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17-01-2013 дата публикации

Composition, and Method of Using the Composition, Effective for Minimizing the Harmful Effects Associated with Individuals Suffering from Alcohol Intoxication

Номер: US20130017276A1
Автор: Gregory Blackman

The present invention relates to a composition, and methods of using the composition, for minimizing the harmful effects associated with alcohol consumption. The composition includes a plurality of ingredients, which when combined, have the unexpected effect of increasing one or more metabolic pathways in the individual. As the metabolic rate is increased, alcohol is burned off, or utilized as energy source, and occurs at a considerably much faster rate than under normal physiological means. It is believed that the composition may have an effect on the brain causing it to increase metabolic rates. By administering the composition to an inebriated individual, the rate at which a person sobers up, occurs at a faster rate than would occur under normal physiological time frames.

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17-01-2013 дата публикации

Aminomethyl quinolone compounds

Номер: US20130018043A1
Принадлежит: Individual

The invention relates to JNK inhibitors and corresponding methods, formulations, and compositions for inhibiting JNK and treating JNK-mediated disorders. The application discloses JNK inhibitors, as described below in Formula I: wherein the variables are as defined herein. The compounds and compositions disclosed herein are useful to modulate the activity of JNK and treat diseases associated with JNK activity. Disclosed are methods and formulations for inhibiting JNK and treating JNK-mediated disorders, and the like, with the compounds, and processes for making said compounds, and corresponding compositions, disclosed herein.

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07-02-2013 дата публикации

Biaryl compounds and methods of use thereof

Номер: US20130035326A1
Принадлежит: Ambit Bioscience Corp

Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.

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14-03-2013 дата публикации

Salt of naphthyridine carboxylic acid derivative

Номер: US20130065917A1
Принадлежит: LG Chemical Co Ltd

7-(3-Aminomethyl-4-methoxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid methanesulfonate and hydrates thereof, processes for their preparation, pharmaceutical compositions comprising them, and their use in antibacterial therapy.

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21-03-2013 дата публикации

Combination

Номер: US20130072507A1
Принадлежит: GlaxoSmithKline LLC

The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.

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11-04-2013 дата публикации

Heterocyclic compounds and their uses

Номер: US20130090323A1
Принадлежит: AMGEN INC

Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer.

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25-04-2013 дата публикации

METHODS OF USING (+)-1,4-DIHYDRO-7-[(3S,4S)-3-METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OXO-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID FOR TREATMENT OF ANTECEDENT HEMATOLOGIC DISORDERS

Номер: US20130102559A1
Автор: Michelson Glenn
Принадлежит:

Methods of treating, preventing or managing antecedent hematologic disorders, such as myelodysplastic syndrome, including chronic myelomonocytic leukemia are disclosed. The methods encompass the administration of SNS-595. Also provided are methods of treatment using this compound with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy. In certain embodiments, the method of treatment comprise administering SNS-595 in combination with cytarabine. Pharmaceutical compositions and single unit dosage forms suitable for use in the methods are also disclosed. 1. A method of treating an antecedent hematological disorder comprising administering to a mammal in need thereof a therapeutically effective amount of an enantiomerically pure (+)-1 ,4-dihydro-7-[(3S ,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1 ,8-naphthyridine-3-carboxylic acid.2. The method of claim 1 , wherein the antecedent hematological disorder is a myelodysplastic syndrome.3. The method of claim 1 , wherein the myelodysplastic syndrome is characterized by ineffective blood cell production claim 1 , progressive cytopenia claim 1 , risk of progression to acute leukemia or cellular marrow with impaired morphology.4. The method of claim 2 , wherein the myelodysplastic syndrome is selected from group consisting of refractory anemia claim 2 , refractory anemia with ringed sideroblasts claim 2 , refractory anemia with excess blasts claim 2 , refractory anemia with excess blasts in transformation claim 2 , and chronic myelomonocytic leukemia.5. The method of claim 2 , wherein the myelodysplastic syndrome is chronic myelomonocytic leukemia.6. The method of claim 5 , wherein the chronic myelomonocytic leukemia is relapsed claim 5 , refractory claim 5 , or resistant to conventional therapy.7. The method of claim 1 , further comprising administering a therapeutically effective amount of a second active agent.8. The method of claim 7 , wherein the second active ...

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25-04-2013 дата публикации

2,4-DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER

Номер: US20130102603A1

The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors. 2. Compound according to claim 1 , with the further proviso that Wdenotes N and/or Z excludes N═C claim 1 , i.e. Z denotes C═C claim 1 , N(R)CO claim 1 , NR claim 1 , C═N claim 1 , O claim 1 , CON(R) claim 1 , S claim 1 , CH or N═N claim 1 ,and the physiologically acceptable salts, solvates, stereoisomers and tautomers thereof, including mixtures thereof in all ratios.3. Compound according to claim 1 , wherein Z is selected from the group consisting of:(a) C═C, or{'sup': '4', '(b) N(R)CO, or'}{'sup': '4', '(c) NR, or'}(d) C═N, or(e) O, or{'sup': '4', '(f) CON(R),'}and preferably is C═C,and the physiologically acceptable salts, solvates, stereoisomers and tautomers thereof, including mixtures thereof in all ratios.6. Compound according to claim 1 , wherein{'sup': '2', 'sub': n', '2', 'n', 'n', 'n', 'n', 'n', 'n', '3, 'Ris absent or denotes H, A, Hal, —(CYY)—OY, NO, —(CYY)—NYY, —(CYY)-Het, —O—(CYY)-Het, —O—(CYY)—OY, —O—(CYY)—NYY, NY—(CYY)—NYY, NY—COY or a monocyclic heteroaryl having 5, 6, 7, 8, 9, 10, 11, 12, 13 or 14 C atoms and 1, 2, 3, 4 or 5 N, O and/or S atoms, where the monocyclic heteroaryl can be independently substituted by at least one substituent selected from the group consisting of Y, Hal, CN, CFor OY, and the physiologically acceptable salts, solvates, stereoisomers and tautomers thereof, including mixtures thereof in all ratios.'}10. A method for inhibiting ATP consuming proteins claim 1 , preferably TGF-beta receptor kinase claim 1 , RON claim 1 , TAK1 claim 1 , PKD1 claim 1 , MINK1 claim 1 , SAPK2-alpha claim 1 , SAPK2-beta and/or ...

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25-04-2013 дата публикации

Artemisinin with Berberine Compositions and Methods of Making

Номер: US20130102625A1
Принадлежит: U.S. PHYTOTHERAPY, INC.

An all-natural herbal composition and methods of preparing the same are provided. The novel Artemisinin Combination Therapy (ACT) consists of artemisinin and its derivatives and berberine, the two active substances mixed with various selected excipient compounds to form a single pill, tablet or capsule for treatment and prevention of malaria, dengue fever, yellow fever, dysentery, Lyme disease, babesiosis, progressive multifocal leukoencephalopathy, , and colitis, in adults and children. A tablet or pill for children is formulated to be chewable. 1. An artemisinin and berberine treatment composition for treating a patient in a single pill , tablet or capsule consisting essentially of , in combination:artemisinin;berberine; and{'i': 'Helicobacter Pylori', 'at least one binding or delivery component, wherein the composition is useful for treating an adult in a single pill, tablet or capsule, for at least one illness selected from the group comprising malaria, dengue fever, dysentery, yellow fever, Lyme disease and babesiosis, progressive multifocal leukoencephalopathy, , and colitis.'}2. The composition of claim 1 , wherein the composition is adaptable for an adult patient and includes:50 mg-120 mg artemisinin; and350 mg-1000 mg berberine.3. The composition of claim 2 , wherein the composition is adaptable for an adult patient and includes:90 mg-110 mg artemisinin; and600 mg-900 mg berberine.4. The composition of claim 3 , wherein the composition is adaptable for an adult patient and includes:approximately 100 mg artemisinin; andapproximately 800 mg berberine.5. The composition of claim 2 , wherein the composition is adaptable for an adult patient and the at least one binding or delivery component is selected from the group comprising: microcrystalline cellulose claim 2 , stearic acid claim 2 , silicon dioxide claim 2 , calcium carbonate claim 2 , magnesium stearate claim 2 , and croscarmellose sodium.6. The composition of claim 1 , wherein the composition is ...

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02-05-2013 дата публикации

TREATMENT OF MITOCHONDRIA-RELATED DISEASES AND IMPROVEMENT OF AGE-RELATED METABOLIC DEFICITS

Номер: US20130108709A1
Принадлежит:

Pharmaceutical compositions and methods for the treatment of subjects, including humans, who have or are at risk for various disease, disorders and conditions, including, mitochondria-associated diseases, disorders, and conditions, including respiratory chain disorders, and diseases, disorders and conditions associated with or characterized at least in part by mitochondria swelling, mitochondria dysfunction, mitochondria leaking, oxidative stress, increased mitochondria number, increased mitochondria and mitochondria-related protein mass, and increased mitochondria and related-related proteins expression. 1. A method for improving age-related physiological deficits and increasing longevity in a mammal comprising administering to a subject in need thereof a composition comprising a therapeutically effective amount of a pharmaceutically acceptable copper (II) antagonist and a pharmaceutically acceptable carrier.2. The method of wherein said copper antagonist is a linear or branched tetramine capable of binding copper (II).3. The method of wherein said linear or branched tetramine is a copper (II) chelator.4. The method of wherein said linear or branched tetramine is selected from the group consisting of 2 claim 3 ,3 claim 3 ,2 tetramine claim 3 , 2 claim 3 ,2 claim 3 ,2 tetramine claim 3 , and 3 claim 3 ,3 claim 3 ,3 tetramine.5. The method of wherein said copper (II) antagonist is triethylenetetramine.6. The method of wherein said copper (II) antagonist is a triethylenetetramine salt.7. The method of wherein said triethylenetetramine salt is a succinate salt.8. The method of wherein said triethylenetetramine succinate salt is triethylenetetramine disuccinate.9. The method of wherein said composition is a tablet or capsule for oral administration.10. The method of wherein said composition is a long-acting tablet or capsule for oral administration.11. The method of wherein said copper antagonist is selected from the group consisting penicillamine claim 1 , N- ...

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02-05-2013 дата публикации

TETRAHYDROCARBOLINE DERIVATIVE

Номер: US20130109699A1
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. 3. The compound according to , wherein Y is a straight C1-3 alkylene group optionally substituted with one or two Rs wherein Ris as defined in .4. The compound according to claim 3 , wherein X is a nitrogen atom.5. The compound according to claim 3 , wherein X is a carbon atom.6. The compound according to claim 4 , wherein Ris a hydrogen atom.8. The compound according to claim 7 , wherein Yis an unsubstituted methylene group claim 7 , and Tis a bond or an unsubstituted methylene group.9. The compound according to claim 7 , wherein the C5-10 bridged carbon ring in the C5-10 bridged carbon ring optionally substituted with one to five Rs is bicyclo[2.2.1]heptane or bicyclo[2.2.2]octane.10. The compound according to claim 7 , wherein the 5- to 7-membered monocycle in the 5- to 7-membered monocycle optionally substituted with one to five Rs is (i) a C5-7 monocyclic carbon ring or (ii) a 5- to 7-membered monocyclic heterocyclic ring containing one to four heteroatoms selected from an oxygen atom claim 7 , a nitrogen atom and a sulfur atom.11. The compound according to claim 10 , wherein the C5-7 monocyclic carbon ring is benzene claim 10 , cyclopentane or cyclohexane.14. The compound according to claim 7 , wherein the ring A is a C5-6 monocyclic carbon ring or a C9-10 bicyclic carbon ring.15. The compound according to claim 7 , wherein the ring A is (i) a 5- to 6-membered monocyclic heterocyclic ring containing one to four heteroatoms selected from an oxygen atom claim 7 , a nitrogen atom and a sulfur atom or (ii) a 9- to 10-membered bicyclic heterocyclic ring containing one to four heteroatoms selected from an oxygen atom claim 7 , a nitrogen atom and a sulfur atom.16. The compound according to claim ...

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09-05-2013 дата публикации

Hepatitis C Virus Inhibitors

Номер: US20130115193A1
Принадлежит: Bristol Myers Squibb Co

The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.

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09-05-2013 дата публикации

Therapeutic combinations containing riluzole

Номер: US20130116274A1
Автор: Suzie Chen
Принадлежит: Rutgers State University of New Jersey

Disclosed is a method of treating melanoma in a mammal comprising administering (a) a therapeutically effective amount of an inhibitor of metabotropic glutamate receptor 1 (GRM1); and (b) a therapeutically effective amount of an inhibitor of at least one downstream signaling target of GRM1. Also disclosed are compositions and kits for treating melanoma comprising (a) a therapeutically effective amount of an inhibitor of GRM1; and (b) a therapeutically effective amount of an inhibitor of at least one downstream signaling target of GRM1.

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16-05-2013 дата публикации

Hetero-Bicyclic Derivatives as HCV Inhibitors

Номер: US20130123244A1
Принадлежит: JANSSEN R&D IRELAND

Inhibitors of HCV replication of formula I 4. The compound of claim 1 , wherein ZCY is CH═C—NH.5. The compound of claim 1 , wherein R and R′ are the same.6. The compound of claim 1 , wherein Ris hydroxyl claim 1 , amino claim 1 , mono- or di-Calkylamino claim 1 , Calkyl-carbonylamino claim 1 , Calkyloxy-carbonylamino.7. The compound of claim 1 , wherein Ris selected from Calkyl; Calkyl substituted with methoxy or hydroxyl; phenyl; and phenyl substituted with 1 or 2 substituents independently selected from halo and methyl.9. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.10. (canceled)11. A product containing (a) a compound of claim 1 , and (b) another HCV inhibitor claim 1 , as a combined preparation for simultaneous claim 1 , separate or sequential use in the treatment of HCV infections.12. A method for the prevention or treatment of an HCV infection comprising administering the pharmaceutical composition of to a patient in need thereof. This invention relates to hetero-bicyclic derivatives, in particular quinolinone derivatives, which are inhibitors of the hepatitis C virus (HCV), their synthesis and their use, alone or in combination with other HCV inhibitors, in the treatment or prophylaxis of HCV.HCV is a single stranded, positive-sense RNA virus belonging to the Flaviviridae family of viruses in the hepacivirus genus. The viral genome translates into a single open reading frame that encodes for multiple structural and nonstructural proteins.Following the initial acute infection, a majority of infected individuals develop chronic hepatitis because HCV replicates preferentially in hepatocytes but is not directly cytopathic. In particular, the lack of a vigorous T-lymphocyte response and the high propensity of the virus to mutate appear to promote a high rate of chronic infection. Chronic hepatitis can progress to liver fibrosis, leading to cirrhosis, end-stage liver disease, and HCC (hepatocellular carcinoma), ...

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23-05-2013 дата публикации

Thienopyridine Derivatives for the Treatment and Prevention of Dengue Virus Infections

Номер: US20130129677A1
Принадлежит: Siga Technologies Inc

Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.

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23-05-2013 дата публикации

TETRACYCLIC COMPOUNDS

Номер: US20130131054A1
Принадлежит: MEDIVATION TECHNOLOGIES, INC.

This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder. 112-. (canceled)1422-. (canceled)25. The method of claim 13 , wherein the compound claim 13 , or a pharmaceutically acceptable salt thereof claim 13 , modulates at least one of the following receptors: adrenergic receptor claim 13 , serotonin receptor claim 13 , dopamine receptor and histamine receptor.26. The method of claim 13 , wherein the compound claim 13 , or a pharmaceutically acceptable salt thereof claim 13 , has X claim 13 , Xand Xare each CRwhere Ris H and Xis CRwhere Ris substituted or unsubstituted C-Calkyl or halo.27. The method of claim 26 , wherein the compound claim 26 , or a pharmaceutically acceptable salt thereof claim 26 , has Xis CRwhere Ris methyl claim 26 , chloro or fluoro.28. The method of claim 13 , wherein the compound claim 13 , or a pharmaceutically acceptable salt thereof claim 13 , has at least one of X claim 13 , X claim 13 , Xand Xis N.29. The method of claim 13 , wherein the compound claim 13 , or a pharmaceutically acceptable salt thereof claim 13 , has one of R-Ris hydroxyl and its geminal R-Ris C-Calkyl or C-Cperhaloalkyl.30. The method of claim 13 , wherein the compound claim 13 , or a pharmaceutically acceptable salt thereof claim 13 , has one of R claim 13 , R claim 13 , Rand Ris hydroxyl and its geminal R claim 13 , R claim 13 , Rand Ris C-Calkyl or C-Cperhaloalkyl; X claim 13 , Xand Xare each CRwhere Ris H; Xis CRwhere Ris substituted or unsubstituted C-Calkyl or halo and Ris substituted or unsubstituted C-Calkyl.31. The method of claim 13 , wherein the compound ...

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23-05-2013 дата публикации

TETRAHYDROPYRIDOETHERS FOR TREATMENT OF AMD

Номер: US20130131101A1
Автор: Schraermeyer Ulrich
Принадлежит:

A medication comprising tetrahydropyridoethers for use in the treatment of AMD. 1. A method of treatment of AMD or dry AMD in a subject , comprising administering to the subject in need of such treatment a medication comprising tetrahydropyridoethers in a suitable amount.3. The method of claim 2 , wherein R1 is methyl claim 2 , one of the substituents R2a and R2b is hydrogen and the other is methoxy claim 2 , ethoxy claim 2 , isopropoxy claim 2 , methoxyethoxy or methoxypropoxy claim 2 , one of the substituents R3a and R3b is hydrogen and the other is hydroxy claim 2 , and its salts.4. The method according to claim 2 , wherein R1 is methyl claim 2 , one of the substituents R2a and R2b is hydrogen and the other is methoxy claim 2 , ethoxy claim 2 , isopropoxy claim 2 , methoxyethoxy or methoxypropoxy claim 2 , one of the substituents R3a and R3b is hydrogen and the other is methoxy claim 2 , ethoxy claim 2 , isopropoxy claim 2 , methoxyethoxy or methoxypropoxy claim 2 , and its salts.5. The method according to claim 2 , wherein R3b is hydrogen.6. The method according to claim 2 , wherein R2a and R3b are hydrogen.7. The method according to claim 2 , wherein R2a is hydrogen and R2b is methoxy claim 2 , ethoxy claim 2 , isopropoxy claim 2 , methoxyethoxy or methoxypropoxy claim 2 , and its salts.9. The method according to claim 8 , wherein R1 is methyl claim 8 , one of the substituents R2a and R2b is hydrogen and the other is methoxy claim 8 , ethoxy claim 8 , isopropoxy claim 8 , methoxyethoxy or methoxypropoxy claim 8 , one of the substituents R3a and R3b is hydrogen and the other is hydroxy claim 8 , and its salts.10. The method according to claim 8 , wherein R1 is methyl claim 8 , one of the substituents R2a and R2b is hydrogen and the other is methoxy claim 8 , ethoxy claim 8 , isopropoxy claim 8 , methoxyethoxy or methoxypropoxy claim 8 , one of the substituents R3a and R3b is hydrogen and the other is methoxy claim 8 , ethoxy claim 8 , isopropoxy claim 8 , ...

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27-06-2013 дата публикации

HETEROARYLS AND USES THEREOF

Номер: US20130165472A1
Принадлежит: Millennium Pharmaceuticals, Inc.

This invention provides compounds of formula IA: 4. The compound of claim 3 , wherein Yis carbon claim 3 , Xis nitrogen claim 3 , Gis N(R) claim 3 , and Xand X claim 3 , are CH.5. The compound of claim 3 , wherein Yis carbon claim 3 , Xand Xare nitrogen claim 3 , Gis N(R) claim 3 , and Xis CH.6. The compound of claim 3 , wherein Yis carbon claim 3 , Xand Gare nitrogen claim 3 , Xis N(R) claim 3 , and Xis CH.7. The compound of claim 3 , wherein Yis carbon claim 3 , Xand Xare nitrogen claim 3 , Gis N(R) claim 3 , and Xis CH.8. The compound of claim 3 , wherein Yis carbon claim 3 , Gis N(R) claim 3 , Xis nitrogen claim 3 , and Xand XCH.9. The compound of claim 3 , wherein Yis carbon claim 3 , Gis nitrogen claim 3 , Xis N(R) claim 3 , and Xand Xare CH.10. The compound of claim 3 , wherein Yis carbon claim 3 , Xis nitrogen claim 3 , Xis N(R) claim 3 , and Xand Gare CH.11. The compound of claim 3 , wherein Yis carbon claim 3 , Xis nitrogen claim 3 , Gis N(R) claim 3 , and Xand X claim 3 , are CH.12. The compound of claim 3 , wherein Yis carbon claim 3 , Xis N(R) claim 3 , Gis nitrogen claim 3 , and Xand X claim 3 , are CH.13. The compound of claim 1 , wherein Ris Cy claim 1 , and Cy is an optionally substituted 5- to 6-membered heteroaryl or heterocyclyl ring.15. The compound of claim 1 , wherein Ris Cy claim 1 , and Cy is an optionally substituted 6-membered aryl ring.16. The compound of claim 1 , wherein Ris —CON(R) claim 1 , —C(O)OR claim 1 , —NHCOR claim 1 , or —CHOR.19. The compound of claim 1 , wherein Ris Caliphatic substituted with a 5-10-membered heteroaryl having 1-5 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , or sulfur.23. The compound of claim 22 , wherein R is hydrogen claim 22 , methyl claim 22 , or chloro.24. The compound of claim 22 , wherein R is methyl claim 22 , and Ris —NHCOR.25. The compound of claim 1 , wherein Ris —NHR claim 1 , wherein Ris an optionally substituted 5- to 10-membered heteroaryl having 1-5 heteroatoms ...

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27-06-2013 дата публикации

Azaquinolinone Derivatives and Uses Thereof

Номер: US20130165473A1
Автор: Duggan Mark E.
Принадлежит: AstraZeneca AB

The present invention provides compounds and methods for treating or preventing the development of a disease, disorder, or condition in a subject or patient. 2. The method of claim 1 , wherein Vis N.4. The method of claim 1 , wherein is a double bond.5. The method of claim 1 , wherein Ris phenyl claim 1 , and wherein Ris optionally substituted with 0-5 —R.6. The method of claim 1 , wherein Ris a 5 membered monocyclic heteroaryl ring having 1-3 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , and sulfur claim 1 , and optionally substituted with 1-2 Rgroups.7. The method of claim 1 , wherein Ris phenyl substituted with 0-3 Rgroups.9. The method of claim 1 , wherein at least one Rgroup is independently selected from the group consisting of R claim 1 , halogen claim 1 , —OR claim 1 , —N(R′) claim 1 , and —C(R).10. The method of claim 1 , wherein Ris selected from the group consisting of —OR claim 1 , halogen claim 1 , and —N(R′).11. The method of claim 1 , wherein Ris an acyclic Caliphatic moiety.13. The method of claim 1 , wherein the proteinopathy is selected from neurodegenerative disease claim 1 , proliferative disease claim 1 , inflammatory disease claim 1 , and cardiovascular disease.14. The method of claim 1 , wherein the proteinopathy is a synucleinopathy claim 1 , an amyloidopathy claim 1 , or a taupathy.19. The compound of claim 18 , wherein Vis N. This application is a divisional application of U.S. application Ser. No. 12/618,336, filed Nov. 13, 2009 (i.e., U.S. Pat. No. 8,343,996), which claims priority to, and the benefit of U.S. Provisional Application No. 61/114,303, filed Nov. 13, 2008 and U.S. Provisional Application No. 61/231,434, filed Aug. 5, 2009. The entire contents of each of the above-identified applications are herein incorporated by reference in their entireties.A variety of disorders are associated with abnormal protein folding and/or aggregation. For example, several neurodegenerative diseases and/or conditions ...

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04-07-2013 дата публикации

4-oxoquinoline compound and use thereof as hiv integrase inhibitor

Номер: US20130172344A1
Принадлежит: Japan Tobacco Inc

An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.

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11-07-2013 дата публикации

2,4,5-TRISUBSTITUTED IMIDAZOLES AND THEIR USE AS ANTI-MICROBIAL AGENTS

Номер: US20130177632A1
Принадлежит:

The present invention provides therapeutically effective 2,4,5-trisubstituted imidazole compounds, methods of preparing the same, and compositions comprising the compounds alone or in combination with other agents. The present invention further provides for the use of the compounds as anti-microbial agents. The anti-microbial properties of the compounds include anti-bacterial and/or anti-fungal activity. 2. The compound according to claim 1 , wherein R2 and R3 are independently phenyl claim 1 , substituted phenyl claim 1 , naphthyl claim 1 , substituted naphthyl claim 1 , pyridyl claim 1 , thienyl claim 1 , substituted pyridyl claim 1 , or substituted thienyl5. The compound according to claim 4 , wherein said compound is selected from compounds: 5 claim 4 , 6 claim 4 , 7 claim 4 , 8 claim 4 , 9 claim 4 , 10 claim 4 , 11 claim 4 , 13 claim 4 , 17 claim 4 , 19 claim 4 , 20 claim 4 , 21 claim 4 , 23 claim 4 , 25 claim 4 , 26 claim 4 , 27 claim 4 , 28 claim 4 , 29 claim 4 , 31 claim 4 , 32 claim 4 , 33 claim 4 , 34 claim 4 , 35 claim 4 , 36 claim 4 , 42 claim 4 , 43 claim 4 , 48 claim 4 , 49 claim 4 , 51 claim 4 , 54 claim 4 , 55 claim 4 , 56 claim 4 , 75 claim 4 , 83 or 84.6. The compound according to claim 5 , wherein said compound is: 8.7. The compound according to claim 5 , wherein said compound is: 30.9. The anti-microbial composition according to claim 8 , wherein said anti-microbial composition is for inhibiting the growth and/or proliferation of a drug-resistant bacterium and said one or more compounds have anti-bacterial activity.10Staphylococcus aureusEnterococcus.. The anti-microbial composition according to claim 9 , wherein said drug-resistant bacterium is methicillin-resistant cell or vancomycin-resistant11. The anti-microbial composition according to claim 8 , wherein said composition is a liposomal formulation.12. The anti-microbial composition according to claim 8 , wherein said composition is a pharmaceutical formulation.13. The anti-microbial ...

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11-07-2013 дата публикации

ARYLSULFONAMIDE PYRIDINE-PYRIDINONE DERIVATIVES, PREPARATION OF SAME, AND THERAPEUTIC USE THEREOF

Номер: US20130178472A1
Принадлежит: SANOFI

The invention relates to pyridine-pyridinone derivatives general formula (I): 2. The compound according to claim 1 , wherein:R1 represents a —(C1-C4)alkyl group,in the form of a base or addition salts with an acid.3. The compound according to claim 1 , wherein:R2 represents a —(C1-C4)alkyl group,in the form of a base or addition salts with an acid.4. The compound according to claim 1 , wherein:n′ represents 1,in the form of a base or addition salts with an acid.5. The compound according to claim 1 , wherein:R3 represents a hydrogen atom,in the form of a base or addition salts with an acid.6. The compound according to claim 1 , wherein:Ar represents a phenyl,in the form of a base or addition salts with an acid.7. The compound according to claim 1 , wherein: an alkyl group;', 'a group —NRR′, with R and R′, which may be identical or different, representing, independently of each other, a hydrogen atom, an alkyl group or a —(C3-C6)cycloalkyl group,', 'an alkenyl group,', 'an aryl group, said group being optionally substituted with at least one halogen atom, and/or with at least one group chosen from alkoxy groups and the groups —NRR′, with R and R′ as defined above,', 'it being understood that, when said heteroaryl group is chosen from pyrrolyl, imidazolyl, pyrazolyl and triazolyls, at least one of the nitrogen atoms of said heteroaryl may be optionally substituted with a group R6, with R6 representing a group chosen from an alkyl group.', 'a heteroaryl group, said heteroaryl group being optionally substituted with at least one group chosen from alkyl groups and heterocycloalkyl groups comprising at least one heteroatom chosen from the nitrogen and oxygen atoms;'}], 'R4 represents a group chosen from8. The compound according to claim 1 , wherein R4 represents a group chosen from phenyl claim 1 , pyridinyl and imidazolyl groups.9. The compound according to claim 1 , wherein Y claim 1 , Z claim 1 , V and W each represents a ═CH group or a ═C(R5)-group claim 1 , and R5 ...

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11-07-2013 дата публикации

Use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment and/or prevention of serious depression and sleep/waking cycle disorders

Номер: US20130178493A1
Принадлежит: Biocortech SpA

The invention relates to a novel therapeutic use of 14,15-dihydro-20,21-dinoreburnamenin-14-ol for the treatment of serious depression in humans, particularly for the treatment of a patients resistant to conventional anti-depressant treatments and for treatment of sleep/waking cycle disorders.

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11-07-2013 дата публикации

Modulators of cystic fibrosis transmembrane conductance regulator

Номер: US20130178496A1
Принадлежит: Vertex Pharmaceuticals Inc

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.

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18-07-2013 дата публикации

DIHYDROPYRROLONAPHTHYRIDINONE COMPOUNDS AS INHIBITORS OF JAK

Номер: US20130184252A1
Принадлежит: Takeda Pharmaceutical Company Limited

Disclosed are JAK inhibitors of formula I 2. A method according to claim 1 , wherein each of Rand Rare hydrogen.3. A method according to claim 1 , wherein G is CR.4. A method according to claim 3 , wherein G is CRand Ris selected from hydrogen claim 3 , halo claim 3 , and optionally substituted Calkyl.5. A method according to claim 4 , wherein G is CRand Ris selected from hydrogen claim 4 , halo claim 4 , and Calkyl.6. A method according to claim 1 , wherein G is N.7. A method according to claim 1 , wherein Ris optionally substituted Ccycloalkyl.8. A method according to claim 1 , wherein Ris optionally substituted Cheterocycloalkyl.9. A method according to claim 1 , wherein Ris optionally substituted Caryl.10. A method according to claim 1 , wherein Ris optionally substituted Cheteroaryl.11. A method according to claim 1 , wherein Ris optionally substituted Calkyl.12. A method according to claim 1 , wherein R claim 1 , R claim 1 , and the carbon atom to which they are attached form a carbonyl.13. A method according to claim 12 , wherein each of Rand Ris hydrogen.14. A method according to claim 1 , wherein R claim 1 , R claim 1 , and the carbon atom to which they are attached form a carbonyl.15. A method according to claim 14 , wherein each of Rand Ris hydrogen.16. A method according to claim 1 , in which the compound is selected from:tert-butyl 4-(5-oxopyrrolo[4,3,2-de][2,6]naphthyridin-4(1H,3H,5H)-yl)piperidine-1-carboxylate;4-(piperidin-4-yl)-3,4-dihydropyrrolo[4,3,2-de][2,6]naphthyridin-5(1H)-one;3-oxo-3-(4-(5-oxopyrrolo[4,3,2-de][2,6]naphthyridin-4(1H,3H,5H)-yl)piperidin-1-yl)propanenitrile;tert-butyl 4-methyl-4-(5-oxopyrrolo[4,3,2-de][2,6]naphthyridin-4(1H,3H,5H)-yl)piperidine-1-carboxylate;4-(4-methylpiperidin-4-yl)-3,4-dihydropyrrolo[4,3,2-de][2,6]naphthyridin-5(1H)-one;3-(4-methyl-4-(5-oxopyrrolo[4,3,2-de][2,6]naphthyridin-4(1H,3H,5H)-yl)piperidin-1-yl)-3-oxopropanenitrile;tert-butyl 4-ethyl-4-(5-oxopyrrolo[4,3,2-de][2,6]naphthyridin-4(1H,3H,5H)-yl) ...

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25-07-2013 дата публикации

TREATMENT OF SYMPTOMS ASSOCIATED WITH MENOPAUSE

Номер: US20130191934A1

A method for treating symptoms associated with a dramatic reduction in reproductive hormone levels is provided, particularly in menopausal women and breast cancer survivors undergoing aromatase inhibitor therapy. The method comprises administered to a subject an inhibitor of orexin activity in an amount sufficient to reduce or decrease onset, progression, severity, frequency, duration or probability of one or more such symptoms. A method of detecting compounds having activity for relieving menopausal symptoms is also provided. 1. A method of treating a female patient for menopausal symptoms , said method comprising the step ofadministering to said patient a composition comprising an inhibitor of orexin activity, in an amount sufficient to prevent the onset, or reduce the severity, frequency or duration of said menopausal symptoms.2. The method of further comprising the step of identifying women with below average estrogen levels claims 1 , wherein such women are administered said composition prophylactically or in response to symptoms.3. The method of wherein the composition comprises an ORX1 receptor antagonist.4. The method of wherein the composition comprises an ORX2 receptor antagonist.5. The method of wherein the composition comprises ORX1 and ORX2 receptor antagonist activity.6. The method of wherein the composition comprises an orexin inhibitor selected from the group consisting of SB334867 claim 1 , MK4305 and Almorexant.7. The method of wherein the patient is receiving aromatase inhibitor therapy.8. The method of wherein the patient is menopausal.9. A method of treating a woman to prevent or reduce the severity claim 1 , frequency or duration of hot flashes claim 1 , said method comprising the steps ofidentifying women that have below average estrogen levels;administering to woman having below average estrogen levels a composition comprising an orexin inhibitor.10. The method of wherein the orexin inhibitor interferes with ORX receptor activity.11. The ...

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01-08-2013 дата публикации

COMBINATION COMPRISING CNDAC (2'-CYANO-2'-DEOXY-N4-PALMITOYL-1-BETA-D-ARABINOFURANOSYL-CYTOSINE) AND A CYTOTOXIC AGENT

Номер: US20130196938A1
Принадлежит: CYCLACEL LIMITED

A first aspect of the invention relates to a combination comprising 2′-cyano-2′-deoxy-N-palmitoyl-1-β-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof. A second aspect relates to a pharmaceutical product comprising (i) 2′-cyano-2′-deoxy-N-palmitoyl-1-β-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and (ii) a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect relates to a method of treating a proliferative disorder, said method comprising simultaneously, separately or sequentially administering to a subject 2′-cyano-2′-deoxy-N-palmitoyl-1-β-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, and a cytotoxic agent selected from: (a) a HDAC inhibitor; and (b) a topoisomerase inhibitor selected from etoposide, topotecan and SN-38, or a prodrug thereof. A fourth aspect of the invention relates to the use of a subject 2′-cyano-2′-deoxy-N-palmitoyl-1-β-D-arabinofuranosyl-cytosine, or a metabolite thereof, or a pharmaceutically acceptable salt thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL). 1. A combination comprising 2-cyano-2′-deoxy-N-palmitoyl-1-β-D-arabinofuranosyl-cytosine , or a metabolite or pharmaceutically acceptable salt thereof , and a cytotoxic agent , wherein the cytotoxic agent is either selected an HDAC inhibitor or a topoisomerase inhibitor selected from the group consisting of etoposide , topotecan , irinotecan , SN-38 , and a prodrug thereof.28-. (canceled)9. A combination according to wherein the ...

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08-08-2013 дата публикации

Autotaxin pathway modulation and uses thereof

Номер: US20130202614A1
Автор: Vassilios Aidinis
Принадлежит: B S R C "ALEXANDER FLEMING"

Disclosed are methods for preventing, treating, or reducing symptoms of a disorder involving the autotaxin (ATX) pathway. In one embodiment, the method features administering to a mammal a sufficient amount of an autotaxin (ATX) or lysophosphatidic acid (LPA) signaling inhibitor, to prevent, treat or reduce symptoms of an inflammatory disorder, autoimmune disorder, fibrosis or malignancy of the lung. Further disclosed are methods for diagnosing an autotaxin-related disorder as well as kits for performing the methods of the invention.

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08-08-2013 дата публикации

Tetracyclic compounds

Номер: US20130203746A1
Принадлежит: Medivation Technologies LLC

This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

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08-08-2013 дата публикации

INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Номер: US20130203747A1
Принадлежит: Gilead Sciences, Inc.

Compounds of formula I: 6. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris (C)alkyl claim 1 , —CN claim 1 , halo or (C)haloalkyl.7. A compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CH.11. A pharmaceutical composition comprising a compound of formula (I) according to any one of to claim 1 , or a pharmaceutically acceptable salt thereof; and one or more pharmaceutically acceptable carriers.12. A method of treating HIV infection which comprises administering to a host infected by HIV a therapeutically effective amount of a compound of formula (I) according to any one of to claim 1 , or a pharmaceutically acceptable salt thereof. This application claims benefit of U.S. Ser. No. 61/178,551, filed May 15, 2009, and U.S. Ser. No. 61/285,766, filed Dec. 11, 2009, which are herein incorporated by reference.The present invention relates to compounds, compositions and methods for the treatment of human immunodeficiency virus (HIV) infection. In particular, the present invention provides novel inhibitors of the HIV integrase enzyme, pharmaceutical compositions containing such compounds and methods for using these compounds to reduce HIV replication and in the treatment of HIV infection.Acquired immune deficiency syndrome (AIDS) is caused by the human immunodeficiency virus (HIV), particularly the HIV-1 strain. Most currently approved therapies for HIV infection target the viral reverse transcriptase and protease enzymes. There are also two approved drugs targeting HIV entry and one approved drug targeting the integrase enzyme. Within the reverse transcriptase inhibitor and protease inhibitor classes, resistance of HIV to existing drugs is a problem. Therefore, it is important to discover and develop new antiretroviral compounds.International patent application WO 2007/131350 and United States published patent application US 2006/0106070 describe compounds which are active ...

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15-08-2013 дата публикации

Synergistic Effects Between Auristatin-Based Antibody Drug Conjugates And Inhibitors Of The PI3K-AKT mTOR Pathway

Номер: US20130209496A1
Принадлежит: Seattle Genetics Inc

The present invention is directed to methods for treating cancer comprising administering to a subject in need thereof an auristatin-based antibody drug conjugate and an inhibitor of the PI3K-AKT-mTOR pathway.

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15-08-2013 дата публикации

Inhibitors of Human Immunodeficiency Virus Replication

Номер: US20130210857A1
Принадлежит: Bristol Myers Squibb Co

The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

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22-08-2013 дата публикации

Pyrido [4,3-b] indole and pyrido [3,4-b] indole derivatives and methods of use

Номер: US20130217675A1
Принадлежит: Medivation LLC, Medivation Technologies LLC

This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

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12-09-2013 дата публикации

TREATMENT

Номер: US20130237557A1
Принадлежит: UCL Business PLC

The present invention derives from the finding that increased levels of alpha 2a adrenergic receptors (ADRA2a) are associated with chronic liver disease and that by decreasing ADRA2a levels in vivo, a number of symptoms and consequences of chronic liver disease may be reduced. Accordingly, the invention provides ADRA2a antagonists for use in a method of treating an individual suffering from liver disease. 1. A method of treating liver disease in an individual in need thereof , said method comprising a step of administering an antagonist of an alpha 2a adrenergic receptor (ADRA2a).2. The method according to claim 1 , wherein said individual is suffering from chronic liver disease.3. The method according to claim 1 , wherein said individual is suffering from liver cirrhosis.4. The method according to claim 1 , wherein said method is for treating or preventing liver failure.5. The method according to claim 1 , wherein the individual is suffering from claim 1 , or is at risk of one or more of the following claim 1 , when compared to a subject not suffering from liver disease: (a) splanchnic vasodilation and normal claim 1 , reduced or increased cardiac output; (b) portal hypertension; (c) reduced mean arterial pressure; (d) reduced hepatic arterial blood flow; (e) increased intra-hepatic resistance; (f) increased plasma ammonia; (g) hepato-renal dysfunction; (h) increased brain water; (i) increased plasma creatinine; (j) increased plasma lactate; (k) alcoholic cirrhosis; and/or (l) non-alcoholic fatty liver disease.6. The method according to claim 1 , wherein either or both of: (i) the individual is not suffering from active hepatitis claim 1 , and (ii) the individual has no significant inflammation of the liver.7. The method according to claim 1 , wherein said antagonist leads to one or more of:(a) decreased expression of ADRA2a in the liver of the individual;(b) decreased levels of ADRA2a in the liver of the individual;(c) decreased activity of ADRA2a in the liver of ...

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19-09-2013 дата публикации

SNS-595 AND METHODS OF USING THE SAME

Номер: US20130244967A1
Принадлежит: SUNESIS PHARMACEUTICALS, INC.

The present invention relates to SNS-595 and methods of treating cancer using the same. 125-. (canceled)26. A method for treating cancer comprising administering to a human patient having cancer (+)-1 ,4-dihydro-7-[(3S ,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1 ,8-naphthyridine-3-carboxylic acid in a dose of about 10 mg/m-100 mg/ma therapeutically effective amount of cytarabine.27. The method of claim 26 , wherein the dose is about 30 mg/m-75 mg/m.28. The method of claim 26 , wherein the dose is about 40 mg/m-80 mg/m.29. The method of claim 26 , wherein the dose is about 50 mg/m-90 mg/m.30. The method of claim 26 , wherein the amount of cytarabine administered to the patient is at least 100 mg/m.31. The method of claim 27 , wherein the amount of cytarabine administered to the patient is at least 100 mg/m.32. The method of claim 28 , wherein the amount of cytarabine administered to the patient is at least 100 mg/m.33. The method of claim 29 , wherein the amount of cytarabine administered to the patient is at least 100 mg/m.34. The method of claim 26 , wherein the cancer is leukemia.35. The method of claim 29 , wherein the cancer is leukemia.36. The method of claim 26 , wherein cytarabine is administered intravenously. This application claims priority to U.S. Ser. No. 60/553,578 filed Mar. 15, 2004 and is incorporated herein by reference.SNS-595 is novel naphthyridine cytotoxic agent that was previously known as AG-7352 (see e.g., Tsuzuki et al., Tetrahedron-Asymmetry 12: 1793-1799 (2001) and U.S. Pat. No. 5,817,669). The chemical name of SNS-595 is (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazoyl)-1,8-naphthyridine-3-carboxylic acid and has the structure shown below 1The present invention relates to SNS-595 and methods for maximizing its therapeutic potential to treat cancer.Proliferating cells undergo four phases of the cell cycle: G, S, G, and M. These phases were first identified by observing ...

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19-09-2013 дата публикации

Stabilization of Hypoxia Inducible Factor (HIF) Alpha

Номер: US20130245037A1
Принадлежит: FibroGen, Inc.

The present invention relates to methods of stabilizing the alpha subunit of hypoxia inducible factor (HIF). The invention further relates to methods of preventing, pretreating, or treating conditions associated with HIF, including ischemic and hypoxic conditions. Compounds for use in these methods are also provided. 1. A method for treating a disorder associated with hypoxia or ischemia in a subject , the method comprising administering to the subject an effective amount of a compound that stabilizes the alpha subunit of hypoxia inducible factor (HIFα).2. The method of claim 1 , wherein the compound is a compound that inhibits HIF prolyl hydroxlase enzyme activity and is selected from the group consisting of a heterocyclic carboxamide claim 1 , a phenanthroline claim 1 , or a hydroxamate.3. The method of claim 1 , wherein the disorder is associated with an ischemic event.4. The method of claim 3 , wherein the ischemic event is acute.5. The method of claim 3 , wherein the ischemic event is associated with surgery claim 3 , organ transplantation claim 3 , infarction claim 3 , trauma claim 3 , or injury.6. The method of claim 3 , wherein the ischemic event is chronic.7. The method of claim 3 , wherein the ischemic event is associated with ischemic reperfusion injury in a subject.8. The method of claim 1 , wherein the administering is oral administration.9. A method for stabilizing the alpha subunit of hypoxia inducible factor (HIFα) in a subject claim 1 , the method comprising administering to the subject an effective amount of a compound that inhibits HIF prolyl hydroxylase enzyme activity claim 1 , wherein the compound is selected from the group consisting of a heterocyclic carboxamide claim 1 , a phenanthroline claim 1 , or a hydroxamate. This application is a continuation of U.S. application Ser. No. 12/928,119, filed 2 Dec. 2010, which is a continuation of U.S. application Ser. No. 11/494,978, filed 28 Jul. 2006, now abandoned, which is a continuation of U.S. ...

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26-09-2013 дата публикации

ANTIMICROBIAL 4-OXOQUINOLIZINES

Номер: US20130252882A1
Принадлежит: EVOLVA SA

This invention provides novel 4-oxoquinolizine compounds and their uses for a series of broad-spectrum antibiotics having no cross-resistance to existing or emerging classes of antibiotics. In addition the novel 4-oxoquinolizine compounds are useful against CDC Category A and B pathogens The invention also provides pharmaceutical compositions comprising certain 4-oxoquinolizines in combination with subinhibitory concentrations of polymyxin B against clinical isolates which are resistant to quinolones, carbapenems and other antimicrobial agents. 2. (canceled)67-. (canceled)8. The pharmaceutical composition according to claim 5 , wherein Ris hydrogen or halogen.9. The pharmaceutical composition according to claim 5 , wherein Y is aryl optionally substituted by one to five groups that are each independently halogen claim 5 , Calkyl claim 5 , Chaloalkyl claim 5 , Ccycloalkyl claim 5 , heterocyclyl claim 5 , aryl claim 5 , heteroaryl claim 5 , Ccycloalkyl(C) alkyl claim 5 , heterocyclyl(C)alkyl claim 5 , aryl(C)alkyl claim 5 , heteroaryl(C)alkyl claim 5 , —R claim 5 , C(O)R claim 5 , or —Calkyl-R.10. The pharmaceutical composition according to claim 5 , wherein Y is phenyl substituted with one group which is halogen claim 5 , cyano claim 5 , —OR claim 5 , —SR claim 5 , —N(R) claim 5 , Calkyl claim 5 , —Calkyl-N(R) claim 5 , or —Calkyl-OR claim 5 , and optionally substituted by one to two groups that are each independently halogen claim 5 , Calkyl claim 5 , Chaloalkyl claim 5 , Ccycloalkyl claim 5 , heterocyclyl claim 5 , aryl claim 5 , heteroaryl claim 5 , Ccycloalkyl(C) alkyl claim 5 , heterocyclyl(C)alkyl claim 5 , aryl(C)alkyl claim 5 , heteroaryl(C)alkyl claim 5 , —R claim 5 , or —Calkyl-R.1116-. (canceled)17. The pharmaceutical composition according to claim 5 , wherein Y is a 5-membered or 6-membered heteroaryl optionally substituted by one to five groups that are each independently halogen claim 5 , Calkyl claim 5 , Chaloalkyl claim 5 , Ccycloalkyl claim 5 , ...

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26-09-2013 дата публикации

TRICYCLIC COMPOUND AND USE THEREOF

Номер: US20130252993A1
Принадлежит: ONO PHARMACEUTICAL CO., LTD.

The present invention relates to the compound represented by formula (I): 2. The compound according to claim 1 , wherein Rand Rform a cyclic group which may have a substituent(s) together with their binding carbon atom claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , a solvate thereof claim 1 , or a prodrug thereof.3. The compound according to claim 1 , wherein ring Ais a monocyclic heterocyclic ring claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , a solvate thereof claim 1 , or a prodrug thereof.4. The compound according to claim 1 , wherein ring Ais a monocyclic carbocyclic ring claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , a solvate thereof claim 1 , or a prodrug thereof.5. The compound according to claim 1 , wherein X is a bond claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , a solvate thereof claim 1 , or a prodrug thereof.6. The compound according to claim 1 , wherein Y is —C(═O)— or —C(═O)NR— wherein X binds to a left side of each group claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , a solvate thereof claim 1 , or a prodrug thereof.7. The compound according to claim 1 , wherein Z is a bond or C1-3 alkylene which may have a substituent(s) claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , a solvate thereof claim 1 , or a prodrug thereof.8. The compound according to claim 1 , wherein B is C1-8 alkyl which may have a substituent(s) claim 1 , C3-10 monocyclic or bicyclic aromatic carbocyclic which may have a substituent(s) claim 1 , a carbocyclic ring which is partially or fully saturated claim 1 , or 3-10 membered monocyclic or bicyclic aromatic heterocyclic ring which may be partially or fully saturated claim 1 , and which contains 1 to 4 hetero atom(s) selected from an oxygen atom claim 1 , a nitrogen atom and/or a sulfur atom claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , a solvate thereof claim 1 , or a prodrug thereof.15. The compound according to ...

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03-10-2013 дата публикации

METHODS OF USE OF DIAZACARBAZOLES FOR TREATING CANCER

Номер: US20130261104A1
Принадлежит: Genentech, Inc.

Methods of use of compounds of formula (I) for treating cancer: 2. The method of claim 1 , wherein the compounds of formula (I) are those wherein X is CR.3. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris H.4. The method of claim 1 , wherein the compounds of formula (I) are those wherein Y is CR.5. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris H.6. The method of claim 1 , wherein the compounds of formula (I) are those wherein Z is CR.7. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris H.8. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris Br.9. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris H.10. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris R.11. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris C-Calkyl claim 1 , C-Calkynyl claim 1 , Caryl claim 1 , or 5-6 membered monocyclic or 8-10-membered bicyclic heteroaryl having 1 to 2 ring atoms selected from N claim 1 , O and S; and wherein each member of Ris independently substituted with one to two Rgroups.12. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris isopropyl claim 1 , propynyl claim 1 , phenyl claim 1 , pyrazolyl claim 1 , furanyl claim 1 , thienyl claim 1 , pyridyl claim 1 , imidazolyl claim 1 , pyrimidinyl claim 1 , benzothienyl claim 1 , thiazolyl claim 1 , tetrahydrothienopyridinyl claim 1 , tetrahydrothiazolopyridinyl claim 1 , isothiazolyl claim 1 , tetrahydropyridinyl claim 1 , tetrahydroisoquinolinyl claim 1 , triazolyl claim 1 , dihydrobenzodioxinyl claim 1 , dihydroindolyl claim 1 , oxazolyl claim 1 , or tetrahydrobenzothienyl claim 1 , wherein each member of Ris independently substituted with one to two Rgroups.13. The method of claim 1 , wherein the compounds of formula (I) are those wherein Ris halo claim 1 , R claim 1 , — ...

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10-10-2013 дата публикации

Combination Therapy with an Antitumor Alkaloid

Номер: US20130266666A1
Принадлежит: PHARMA MAR, S.A.

The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and/or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer. 1. A method of treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of PM01183 , or a pharmaceutically acceptable salt thereof , and a therapeutically effective amount of another anticancer drug selected from antimetabolites , proteasome inhibitors , nonclassical alkylating agents , mTOR inhibitors , tyrosine kinase inhibitors , histone deacetylase inhibitors , anticancer antibiotics , antitumor platinum coordination complexes , mitotic inhibitors , topoisomerase I and/or II inhibitors , nitrogen mustard alkylating agents , nitrosourea alkylating agents , estrogen antagonists , androgen antagonists , and other agents selected from aplidine , ET-743 , PM02734 and PM00104.2. A method of increasing the therapeutic efficacy of an anticancer drug selected from antimetabolites , proteasome inhibitors , nonclassical alkylating agents , mTOR inhibitors , tyrosine kinase inhibitors , histone deacetylase inhibitors , anticancer antibiotics , antitumor platinum coordination complexes , mitotic inhibitors , topoisomerase I and/or II inhibitors , nitrogen mustard alkylating agents , nitrosourea alkylating agents , estrogen antagonists , androgen antagonists , and other agents selected from aplidine , ET-743 , PM02734 and PM00104 in the treatment of cancer , which ...

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10-10-2013 дата публикации

PHARMACEUTICAL COMPOSITIONS FOR COMBINATION THERAPY

Номер: US20130267552A1
Принадлежит: IVAX INTERNATIONAL GMBH

This invention relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a dopaminergic stabilizer known as Pridopidine, and an inhibitor of the vesicular monoamine transporter type 2 (VMAT) known as Tetrabenazine. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for improving the symptomatic therapeutic effects, and for reducing the adverse effects, of Tetrabenazine in the treatment of movement disorders, and in particular movement disorders associated with Huntington's disease, Gilles de la Tourette's syndrome, or tardive dyskinesia. 1. A method of treating a subject afflicted with a movement disorder comprising periodically administering to the subject an amount of Tetrabenazine or a pharmaceutically acceptable salt thereof , and an amount of Pridopidine or a pharmaceutically acceptable salt thereof.2. A method of treating a subject afflicted with obesity , an obesity associated disorder , or a cardiovascular side effect of Pridopidine comprising administering to the subject an amount of Pridopidine or a pharmaceutically acceptable salt thereof , and an amount of Tetrabenazine or a pharmaceutically acceptable salt thereof.3. The method of claim 1 , wherein the amounts when taken together are more effective to treat the subject than when each agent at the same amount is administered alone.4. The method of claim 1 , wherein either the amount of Tetrabenazine or a pharmaceutically acceptable salt thereof when taken alone claim 1 , and the amount of Pridopidine or a pharmaceutically acceptable salt thereof when taken alone claim 1 , or each such amount when taken alone is not effective to treat the subject.5. A method of reducing or preventing one or more side effects of periodic administration of an amount of Tetrabenazine or a pharmaceutically acceptable salt thereof to a subject claim 1 , comprising periodically administering to the subject an amount of Pridopidine or a ...

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17-10-2013 дата публикации

Pharmaceutical compositions to treat fibrosis

Номер: US20130274215A1
Принадлежит: Fate Therapeutics Inc

The present invention provides methods for the prevention, treatment and/or amelioration of fibrosis or fibrotic conditions. The present invention further provides small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling to prevent, treat and/or ameliorate fibrosis or fibrotic conditions. Kits comprising small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling and methods of identifying small molecule inhibitors of Wnt- and TGF-p-mediated β-catenin signaling are also provided.

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24-10-2013 дата публикации

CBP/CATENIN ANTAGONISTS FOR ENHANCING ASYMMETRIC DIVISION OF SOMATIC STEM CELLS

Номер: US20130280233A1
Принадлежит:

Provided are: methods for treating aging or an age-related condition, symptom or disease; methods for stimulating hair growth, regrowth or pigmentation (or preventing hair loss); methods for increasing the expression of an adenosine receptor in dermal cells (in combination with hair growth); methods for treating a condition or disease of the skin or at least one symptom thereof, including cosmetic treatment (e.g., wrinkles, hyperpigmentation, redness, rosacea, dryness, cracking, loss of firmness, loss of elasticity, thinning, and loss of vibrance). The methods comprise administering a sufficient amount of a CBP/catenin (e.g., CBP/β-catenin) antagonist as disclosed, and particularly wherein administration is in an amount and manner sufficient to provide for increasing the number of asymmetric renewing divisions relative to, or at the expense of symmetric divisions in relevant somatic stem cell population. In particular aspects, the CBP/catenin (e.g., CBP/β-catenin) antagonist comprises an alkyl and/or fatty acid ester derivative thereof as disclosed herein. 1. A method for treating aging or an age-related condition , symptom or disease , comprising:identifying a mammalian subject having somatic stem cells for least one tissue compartment or type having an age-related condition, symptom or disease; andadministering to the subject a CBP/catenin antagonist in a manner and amount sufficient to provide for increasing the number of asymmetric renewing divisions relative to, or at the expense of symmetric divisions of the somatic stem cells for the at least one tissue compartment or type, wherein the age related condition, symptom or disease of the tissue compartment or type is decreased or ameliorated, wherein a method for treating aging or an age-related condition, symptom or disease is afforded.2. The method of claim 1 , wherein the somatic stem cells for the at least one tissue compartment or type comprise quiescent somatic stem cells claim 1 , and wherein administering ...

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24-10-2013 дата публикации

Stabilized Angiopoietin-2 Antibodies And Uses Thereof

Номер: US20130280251A1
Принадлежит: MedImmune Limited

Stabilized antibodies directed to Angiopoeitin-2 and uses of such antibodies are described. Nucleic acid and amino acid sequences, hybridomas or other cell lines for expressing such antibodies are also provided. 1. An isolated antibody that binds to Ang-2 , wherein said antibody comprises a variable light chain , said light chain comprising a sequence selected from the group consisting of SEQ ID No:3 (MEDI1); SEQ ID No:4 (MEDI2); SEQ ID No:5 (MEDI3); SEQ ID No:6 (MEDI4); and SEQ ID No:8 (MEDI6).2. The antibody of claim 1 , wherein said antibody is an IgG1 or an IgG2 isotype antibody.3. The antibody of or claim 1 , wherein said antibody further comprises a variable heavy chain region comprising SEQ ID No:7 (MEDI5).43. The antibody of any of - claims 1 , wherein said antibody claims 1 , when produced claims 1 , exhibits a production efficiency in a mammalian host cell equal to or greater than 2 times the production efficiency of the Ang-2 antibody 3.19.3.5. The antibody of claim 4 , wherein said production efficiency is equal to or greater than 3 times the production efficiency of the Ang-2 antibody 3.19.3.6. The antibody of claim 4 , wherein said production efficiency is equal to or greater than 5 times the production efficiency of the Ang-2 antibody 3.19.3.76. A nucleic acid encoding the antibody of any of -.8. A vector comprising the nucleic acid of9. A host cell comprising the vector of .106. A pharmaceutical composition comprising the antibody of any of - and an excipient.11. A method of preventing claim 10 , treating claim 10 , or managing cancer in an animal in need thereof claim 10 , said method comprising administering to said animal a dose of an effective amount of the composition of .12. A method of preventing metastasis of cancer in an animal in need thereof claim 10 , said method comprising administering to said animal a dose of an effective amount of the composition of .13. A method of preventing recurrences of cancer in an animal in need thereof claim ...

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24-10-2013 дата публикации

TREATMENT OF DISEASES BY EPIGENETIC REGULATION

Номер: US20130281397A1
Принадлежит: RVX Therapeutics Inc.

The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis. 3. The method according to claim 1 , wherein X is selected from CH and N.4. The method according to claim 1 , wherein the compound of Formula I is selected from:3-(4-hydroxy-3,5-dimethylphenyl)-6,8-dimethoxy-7-(morpholinomethyl)isoquinolin-1(2H)-one;2-(4-(bis(2-hydroxyethyl)amino)phenyl)-6,7-dimethoxyquinazolin-4(3H)-one;2-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-6,7-dimethoxyquinazolin-4(3H)-one;2-(2-chloro-6-methylpyridin-4-yl)-5,7-dimethoxyquinazolin-4(3H)-one;3-(4-Hydroxyphenyl)-2H-isoquinolin-1-one;4-(1-Oxo-1,2-dihydroisoquinolin-3-yl)phenyl 2-amino-5-guanidino-pentanoate trihydrochloride;3-(4-hydroxy-3,5-dimethylphenyl)-6,8-dimethoxy-2-methylisoquinolin-1(2H)-one;3-(4-hydroxy-3,5-dimethylphenyl)-6,8-dimethoxy-2,7-dimethylisoquinolin-1(2H)-one;3-(4-hydroxy-3,5-dimethylphenyl)-6,8-dimethoxy-2-methyl-7-(morpholino-methyl)isoquinolin-1(2H)-one;5,7-dimethoxy-2-(pyridin-2-yl)quinazolin-4(3H)-one;5,7-dimethoxy-2-(pyridin-3-yl)quinazolin-4(3H)-one;5,7-dimethoxy-2-(pyridin-4-yl)quinazolin-4(3H)-one;2-(3,5-dimethyl-4-(2-morpholinoethoxy)phenyl)quinazolin-4(3H)-one;2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)quinazolin-4(3H)-one;2-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)quinazolin-4(3H)-one;2-(4-(4-oxo-3,4-dihydroquinazolin-2-yl)phenoxy)acetic acid;2-(4-(dimethylamino)pyridinon-1-yl)quinazolin-4(3H)-one;2-(4-(4-oxo-3,4-dihydroquinazolin-2-yl)phenoxy)acetamide;2-(4-(dimethylamino)pyridinon-1-yl)-6,7-dimethoxyquinazolin-4(3H)-one;2-(4-(bis(2-hydroxyethyl)amino)phenyl)quinazolin-4(3H)-one;2-(4-hydroxy-3,5-dimethylphenyl)-6,7-dimethoxyquinazolin-4(3H)-one;N-(2-(4-hydroxy-3,5- ...

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24-10-2013 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20130281433A1
Принадлежит:

Compounds disclosed herein including compounds of formula I′: 2. The compound of wherein the configuration of the —OC(CH)group as shown in formula I′ is the (S) stereochemistry.3. The compound of wherein Ris selected from aryl claim 1 , heterocycle and heteroaryl claim 1 , wherein any aryl claim 1 , heterocycle and heteroaryl of Ris optionally substituted with one or more halo or (C-C)alkyl.4. The compound wherein Ris selected from aryl and heterocycle claim 1 , wherein any aryl and heterocycle of Ris optionally substituted with one or more chloro claim 1 , fluoro or methyl.7. The compound of wherein A is phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle claim 1 , wherein any phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.8. The compound of wherein A is monocyclic N-heteroaryl claim 1 , wherein monocyclic N-heteroaryl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.9. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl or pyrazinyl claim 1 , wherein pyridinyl claim 1 , pyrimidinyl or pyrazinyl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.10. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl or pyrazinyl and B is aryl claim 1 , heteroaryl or heterocycle claim 1 , wherein any aryl claim 1 , heteroaryl or heterocycle of B is optionally substituted with one or more Zgroups.11. The compound of wherein A and B together form a ...

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24-10-2013 дата публикации

COMBINATION OF SYROSINGOPINE AND MITOCHONDRIAL INHIBITORS FOR THE TREATMENT OF CANCER AND IMMUNOSUPPRESSION

Номер: US20130281478A1
Принадлежит:

The invention relates to a combination of syrosingopine and a mitochondrial inhibitor, e.g. metformin or oligomycin, and the use of the combination of syrosingopine and a mitochondrial inhibitor for the treatment of cancer and for achieving immunosuppression. The invention also relates to a fluorescence-based method for predicting syrosingopine sensitivity of a cancer cell. 1. A pharmaceutical composition comprising syrosingopine and a mitochondrial inhibitor.2. The pharmaceutical composition of wherein the mitochondrial inhibitor is metformin or phenformin.3. The pharmaceutical composition of wherein the mitochondrial inhibitor is metformin.4. The pharmaceutical composition of wherein the mitochondrial inhibitor is selected from the group consisting of rotenone claim 1 , piericidin A claim 1 , epiberberine claim 1 , 2-thenoyltrifluoroacetone (TTFA) claim 1 , antimycin A claim 1 , oligomycin claim 1 , carbonyl cyanide-p-trifluoromethoxyphenylhydrazone (FCCP) claim 1 , and stavudine.5. The pharmaceutical composition of wherein the mitochondrial inhibitor is oligomycin.6. The pharmaceutical composition of wherein the relative amount (weight per weight) of syrosingopine and the mitochondrial inhibitor is between 1 to 10 and 1 to 1′000.7. The pharmaceutical composition of wherein the relative amount (weight per weight) of syrosingopine and metformin is between 1 to 10 and 1 to 200.8. The pharmaceutical composition of wherein the relative amount (weight per weight) of syrosingopine and oligomycin is between 1′000 to 1 and 10′000 to 1.9. A combination of syrosingopine and a mitochondrial inhibitor for use in the treatment of cancer or autoimmune diseases.10. The method of wherein the mitochondrial inhibitor is metformin.11. The method of wherein the mitochondrial inhibitor is oligomycin.12. The method of wherein the cancer is selected from the group consisting of carcinoma claim 19 , sarcoma claim 19 , leukemia claim 19 , myeloma claim 19 , lymphoma claim 19 , and cancers ...

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31-10-2013 дата публикации

COMBINATION THERAPY FOR TREATING CANCER COMPRISING AN IGF-1R INHIBITOR AND AN AKT INHIBITOR

Номер: US20130287763A1
Принадлежит: Merck Sharp & Dohme Corp.

The present invention relates to a method of treating cancer by administering an IGF-1R specific antibody in combination with an anti-cancer agent exemplified by an Akt pathway inhibitor. The first and second amounts together comprise a therapeutically effective amount. 1. A method of treating a hyper-proliferative disorder in a patient suffering from the disorder comprising administering , to the patient , a combination comprising an isolated antibody or antigen-binding fragment thereof that specifically binds to human Insulin-like growth factor-1 receptor and an Atk inhibitor , wherein administration of the combination results in enhanced therapeutic efficacy in the treatment of the disorder relative to administration of the antibody or antigen-binding fragment alone , wherein the antibody or antigen-binding fragment comprises CDR1 , CDR2 and CDR3 of a light chain immunoglobulin comprising an amino acid sequence set forth in SEQ ID NO: 7; and CDR1 , CDR2 and CDR3 of a heavy chain immunoglobulin comprising an amino acid sequence set forth in SEQ ID NO: 8.2. The method of where the antibody or antigen-binding fragment thereof comprises a light chain immunoglobulin comprising the amino acid sequence set forth in SEQ ID NO: 7; and a heavy chain immunoglobulin comprising the amino acid sequence set forth in SEQ ID NO: 8.3. The method of wherein the antibody or fragment is an antibody which is dalotuzumab4. The method according to claim 1 , wherein said Akt inhibitor is MK-2206.5. The method of wherein the antibody or fragment is an antibody which is dalotuzumab and said Akt inhibitor is MK-2206.6. The method of wherein the patient is human.7. The method of wherein the disorder is cancer.8. The method of wherein the cancer is:acute lymphocytic leukemia;acute nonlymphocytic leukemia;adrenal cancer;adult T-cell leukemia/lymphoma;basal cell carcinoma;bladder cancer;bone cancer;brain cancer;breast cancer;chronic lymphocytic leukemia;chronic myelogenous leukemia;colon cancer ...

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07-11-2013 дата публикации

EFFLUX PUMP INHIBITORS

Номер: US20130296228A1
Принадлежит:

Novel compositions and methods of reducing microbial resistance to antimicrobial agents and treating infections are disclosed. In particular, compositions and methods of inhibiting efflux pump activity, treating infection and methods of enhancing antimicrobial activity of antimicrobial agents are provided. 1. A method of inhibiting efflux pump activity in a microorganism , comprising contacting said microorganism with an effective amount of an efflux-pump inhibitor , wherein said efflux-pump inhibitor is a β-lactam compound.2. (canceled)3. A method of treating infection caused by a microorganism in a subject , comprising administering to the subject in need thereof , a therapeutically effective amount of an efflux-pump inhibitor in combination with at least one antimicrobial agent , wherein said efflux-pump inhibitor is a β-lactam compound.4. A method for prophylactic treatment of a subject , comprising administering to a subject at risk of infection caused by microorganism , a prophylactically effective amount of an efflux-pump inhibitor , wherein said efflux-pump inhibitor is a β-lactam compound.5. A method for prophylactic treatment of a subject , comprising administering to a subject at risk of infection by microorganism , a prophylactically effective amount of an efflux-pump inhibitor in combination with at least one antimicrobial agent , wherein said efflux-pump inhibitor is a β-lactam compound.6. (canceled)7. (canceled)8. A method according to claim 1 , wherein the microorganism at least one microorganism selected from a bacteria claim 1 , fungi claim 1 , protozoa claim 1 , yeast claim 1 , mold claim 1 , or mildew.9. A method according to claim 1 , wherein the β-lactam compound is at least one selected from Cefazolin claim 1 , Cefacetrile claim 1 , Cefadroxil claim 1 , Cefalexin claim 1 , Cefaloglycin claim 1 , Cefalonium claim 1 , Cefaloridine claim 1 , Cefalotin claim 1 , Cefapirin claim 1 , Cefatrizine claim 1 , Cefazedone claim 1 , Cefazaflur claim 1 , ...

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07-11-2013 дата публикации

QUINOLINES AND AZA-QUINOLINES AS CRTH2 RECEPTOR MODULATORS

Номер: US20130296300A1
Принадлежит:

The invention provides certain quinolines and aza-quinolines of the Formula (I), and their pharmaceutically acceptable salts, wherein E, J, J, J, R, R, R, R, R, R, R, X, Y, b, n, and q are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions associated with uncontrolled or inappropriate stimulation of CRTHfunction. 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein E is —N(R)(R).4. The compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein{'sup': '6a', 'claim-text': {'sup': 6b', 'AH', 'HC, 'Ris -Q-Ror -Q-R; or'}, '(i) Ris H and'}{'sup': 6a', '6b', '6H, '(ii) Rand Rtogether with the N atom to which they are attached form R.'}5. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein{'sup': '6a', 'Ris H and'}{'sup': 6b', 'AH', 'HC, 'Ris -Q-Ror -Q-R.'}7. The compound of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , wherein Rand Rtogether with the N atom to which they are attached form R.13. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound is selected from the group consisting of:(1) 2-phenyl-6-[[[[4-(trifluoromethoxy)phenyl]methyl]amino]carbonyl]-3-quinolinepentanoic acid;(1D 6-[[[(3-chlorophenyl)methyl]amino]carbonyl]-2-phenyl-3-quinolinepentanoic acid;(1E) 6-[[[(4-methylphenyl)methyl]amino]carbonyl]-2-phenyl-3-quinolinepentanoic acid;(1L) 2-phenyl-6-[(3(R)-phenyl-1-piperidinyl)carbonyl]-3-quinolinepentanoic acid;(1T) 2-phenyl-6-[[(1(S)-phenylethyl)amino]carbonyl]-3-quinolinepentanoic acid;(1AD) 6-[[[1(R)-(4-chlorophenyl)ethyl]amino]carbonyl]-2-phenyl-3-quinolinepentanoic acid;(1AE) 6-[[[1(S)-(4-chlorophenyl)ethyl]amino]carbonyl]-2-phenyl-3-quinolinepentanoic acid;(1AF) 6-[[[1(R)-(4-chlorophenyl)-2,2,2-trifluoroethyl]amino]carbonyl]-2-phenyl-3-quinolinepentanoic acid;(1AG) 6-[[[1(S ...

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14-11-2013 дата публикации

INDOLE ALKALOID COMPOUNDS AS MELANOGENESIS PROMOTERS AND USES THEREOF

Номер: US20130302264A1
Принадлежит: New York University

Provided are indole alkaloid compounds of formula I, for example, pubescine, and the use of such compounds and compositions thereof to promote (e.g., enhance) melanogenesis and pigmentation. 1. (canceled)2. (canceled)4. (canceled)6. The method according to claim 3 , wherein Ris H claim 3 , OH claim 3 , substituted or unsubstituted (C-C) alkoxy claim 3 , or OCOR; and Ris OH claim 3 , substituted or unsubstituted (C-C) alkyl claim 3 , substituted or unsubstituted aryl claim 3 , or substituted or unsubstituted heteroaryl.7. The method according to claim 3 , wherein Ris H claim 3 , OH claim 3 , OMe claim 3 , OCOPh claim 3 , OC(O)-(3 claim 3 ,4 claim 3 ,5-trimethoxyphen-1-yl) claim 3 , OCOMe claim 3 , or OCOCHCOMe.8. (canceled)10. (canceled)11. The method according to claim 3 , wherein Ris H claim 3 , OH claim 3 , OMe claim 3 , Me claim 3 , or Et.12. (canceled)13. The method according to claim 3 , wherein Ris H claim 3 , OH claim 3 , substituted or unsubstituted acyloxy claim 3 , and substituted or unsubstituted (C-C) alkoxy.14. (canceled)15. (canceled)16. (canceled)17. The method according to claim 3 , wherein Ris COH claim 3 , COMe claim 3 , COEt claim 3 , C(O)OCHCHNH claim 3 , C(O)OCHCHNMe claim 3 , CONH claim 3 , CONHMe claim 3 , CONHPh claim 3 , CONMe claim 3 , or C(O)NHCHCHNH.18. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. The method according to claim 3 , wherein n is 1 or 2; and each Ris independently F claim 3 , Cl claim 3 , Me claim 3 , OMe or OEt.27. (canceled)28. The method of claim 3 , wherein the compound is reserpic acid claim 3 , reserpic acid analog claim 3 , pubescine or pubescine analog.29. (canceled)30. (canceled)31. A method for increasing the melanin content in a mammalian subject in need thereof claim 3 , comprising administering to said mammal a melanin content-increasing amount of a compound; wherein the compound is selected from the group consisting of the compounds set forth in Table 1 or in Table 2; or a ...

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14-11-2013 дата публикации

Use of modulators of CCR5 in the treatment of Cancer and cancer metastasis

Номер: US20130303512A1
Автор: Richard G. Pestell
Принадлежит: Individual

This disclosure is directed, in part, to a method of determining whether a subject having cancer is at risk for developing metastasis of the cancer. In one embodiment, the method comprises (a) obtaining a biological sample from the subject having cancer; (b) determining CCR5 expression level and/or expression level of at least one of CCR5 ligands in the biological sample; and (c) if the expression level of CCR5 and/or of at least one of CCR5 ligands determined in step (b) is increased compared to CCR5 expression level and/or expression level of at least one of CCR5 ligands in a control sample, then the subject is identified as likely at risk for developing metastasis of the cancer.

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21-11-2013 дата публикации

Azolyl Urea Compounds and Methods of Use Thereof

Номер: US20130310357A1
Автор: Liu Gang
Принадлежит: AMBIT BIOSCIENCES CORPORATION

Provided herein are azolyl urea compounds for treatment of CSF-1R kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. 3. The compound of claim 1 , wherein A is optionally substituted isoxazolyl or optionally substituted pyrazolyl claim 1 , wherein substituents when present are selected from one claim 1 , two or three Rgroups claim 1 , each independently selected from hydrogen claim 1 , halo claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , alkoxy claim 1 , hydroxyl claim 1 , haloalkoxy claim 1 , cycloalkyl claim 1 , cycloalkylalkyl claim 1 , hydroxyalkyl claim 1 , haloalkyl claim 1 , aryl claim 1 , arylalkyl claim 1 , heterocyclyl claim 1 , heterocyclylalkyl claim 1 , heteroaryl claim 1 , and heteroarylalkyl claim 1 , where the alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , alkoxy claim 1 , haloalkoxy claim 1 , cycloalkyl claim 1 , cycloalkylalkyl claim 1 , hydroxyalkyl claim 1 , haloalkyl claim 1 , aryl claim 1 , heterocyclyl claim 1 , and heteroaryl groups are optionally substituted with 1 to 5 groups selected from halo claim 1 , hydroxy claim 1 , alkoxy claim 1 , cycloalkyl claim 1 , cyano claim 1 , and —RN(R)(R) claim 1 , where Ris independently alkylene or a direct bond claim 1 , R claim 1 , and Rare each independently hydrogen or alkyl.9. The compound of claim 1 , where Ris hydrogen claim 1 , alkyl or alkoxy.10. The compound of claim 1 , where Ris hydrogen claim 1 , cycloalkyl claim 1 , heterocyclyl or heterocyclylalkyl claim 1 , where the cycloalkyl claim 1 , heterocyclyl and heterocyclylalkyl are optionally substituted with one or two alkyl groups.13. The compound of claim 1 , wherein each Qis independently selected from —CH claim 1 , —CH—CH claim 1 , —CHCF claim 1 , —CH—(CH) claim 1 , —C(O)O(CH) claim 1 , —(CH)S(O)CH claim 1 , —CHC(O)N(CH) claim 1 , —C(CH) claim 1 , cyclopropyl and oxetanyl.15. The compound of claim 1 , wherein the compound is ...

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28-11-2013 дата публикации

Aldosterone synthase inhibitors

Номер: US20130317057A1
Принадлежит: Individual

The invention involves compounds of structural Formula (I) and the pharmaceutically acceptable salts thereof. The compounds of the invention are effective at selectively inhibiting CYP11B2, and are therefore useful for the treatment or prophylaxis of disorders that are associated with elevated aldosterone levels, including, but not limited to, hypertension and heart failure.

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05-12-2013 дата публикации

THERAPEUTIC COMPOSITION FOR TREATMENT OF GLIOBLASTOMA

Номер: US20130323300A1
Принадлежит: Regents of the University of Minnesota

The present invention is directed to compositions and methods for treating an animal diagnosed with Glioblastoma multiforme (GBM). 1. An anti-tumor composition comprising a purified glioblastoma GBM6-AD stem cell.2. The anti-tumor composition of claim 1 , wherein the purified GBM6-AD stem cell is an adherent cell.3. The anti-tumor composition of claim 2 , wherein the purified adherent glioblastoma GBM6-AD stem cell is ATCC® Patent Deposit Designation PTA-11498.4. The anti-tumor composition of claim 1 , wherein the GBM6-AD cells are lysed or irradiated.5. (canceled)6. The anti-tumor composition of claim 1 , further comprising a physiologically-acceptable claim 1 , non-toxic vehicle.7. The anti-tumor composition of claim 1 , further comprising an adjuvant.8. The anti-tumor composition of claim 7 , wherein the adjuvant is a CpG ODN claim 7 , Poly ICLC claim 7 , Annexin A2 claim 7 , a TLR ligand claim 7 , Imiquimod claim 7 , or a non-TLR ligand that stimulates an immune response.9. The anti-tumor composition of claim 8 , wherein the adjuvant is a TLR ligand claim 8 , and the TLR Ligand is a TLR7 claim 8 , TLR8 or TLR7/8 ligand.1011-. (canceled)12. The anti-tumor composition of claim 1 , wherein the cell or cell lysate is conjugated to a carrier.13. The anti-tumor composition of claim 12 , wherein the carrier is a dendritic cell or a macrophage.14. The anti-tumor composition of claim 1 , wherein the composition is contained in a non-cell carrier.15. The anti-tumor composition of claim 1 , wherein the composition is contained in a liposome.16. A method of eliciting an immune response in an animal in need thereof claim 1 , comprising administering to the animal the anti-tumor composition of .17. The method of claim 16 , further comprising administering Imiquimod to the animal.18. (canceled)19. The method of claim 16 , wherein the anti-tumor composition is administered parenterally claim 16 , orally or intranasally.2021-. (canceled)22. The method of claim 16 , wherein the ...

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26-12-2013 дата публикации

CONCENTRATION AND MENTAL PERFORMANCE AMPLIFYING FORMULATION

Номер: US20130344141A1
Автор: BUCKLEY Michael Scott
Принадлежит:

A concentration and mental performance amplifying formulation comprising and geranium oil, together with at least one of vinpocetine, phosphatidylcholine, caffeine and (White Willow Bark). In another aspect, there is disclosed a concentration and mental performance amplifying formulation comprising: geranium oil, and at least one of anhydrous caffeine and nicotine. In yet another aspect, there is disclosed a concentration and mental performance amplifying formulation as last described which further comprises: Vinpocetine, or Vincamine together with Huperzine-A, or (Periwinkle) together with Huperzine-A; PhosphatidylCholine or (Brahmi) or Nicotinamide Adenine Dinucleotide Hydrate; and (White Willow Bark). Also described is a method of amplifying concentration and mental performance in a human subject by administering such formulations to such a subject. 1rhodiola rosea,Salix alba. A method for amplifying concentration and mental performance in a human subject in need of such amplification , which comprises administering to said subject a formulation comprising a concentration and mental performance amplifying formulation comprising geranium oil , vinpocetine , phosphatidylcholine , caffeine and (White Willow Bark).2. A method as claimed in wherein the formulation comprises a concentration and mental performance amplifying formulation comprising: rhodiola rosea claim 1 , geranium oil claim 1 , and at least one of anhydrous caffeine and nicotine.3Vinca minorBacopa monnieriMucuna pruriens;Salix alba. A method as claimed in wherein the formulation comprises the concentration and mental performance amplifying formulation further comprising: Vinpocetine claim 1 , or Vincamine together with Huperzine-A claim 1 , or (Periwinkle) together with Huperzine-A; PhosphatidylCholine or (Brahmi) or Nicotinamide Adenine Dinucleotide Hydrate; and (White Willow Bark).4. A method as claimed in wherein the formulation comprises the concentration and mental performance amplifying ...

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02-01-2014 дата публикации

POLYCYCLIC AGENTS FOR THE TREATMENT OF RESPIRATORY SYNCYTIAL VIRUS INFECTIONS

Номер: US20140004111A1
Принадлежит: Biota Scientific Management Pty Ltd.

The present invention relates to polycyclic antiviral compounds, and salts thereof, methods for their preparation and compositions containing them, and the use of the compounds and composition in the treatment of viral infections. 2. (canceled)3. A compound according to wherein ring A is an optionally substituted heteroaryl ring selected from a pyridyl claim 1 , pyridazinyl claim 1 , pyrimidinyl or pyrazinyl ring.4. (canceled)5. A compound according to wherein ring A is an optionally substituted pyridyl ring.614-. (canceled)15. A compound according to wherein Rrepresents an optionally substituted aryl claim 1 , optionally substituted alkyl or optionally substituted heterocyclyl.16. A compound according to wherein Rrepresents an optionally substituted phenyl claim 15 , optionally substituted thienyl claim 15 , optionally substituted pyrrolyl or optionally substituted pyridyl.17. A compound according to wherein Rrepresents an optionally substituted phenyl ring.18. A compound according to claim 1 , wherein Ris optionally substituted phenyl where the substituents are each independently selected from halo claim 1 , hydroxy or alkoxy; cycloalkyl; or optionally substituted pyridyl or an N-oxide thereof where the substituents are each independently selected from halo.19. A compound according to claim 18 , wherein Ris optionally substituted phenyl where the substituents are each independently selected from chloro claim 18 , hydroxy or methoxy; lower cycloalkyl; or optionally substituted pyridyl or an N-oxide thereof where the substituents are each independently selected from chloro.20. A compound according to claim 18 , wherein Ris phenyl claim 18 , 4-chlorophenyl claim 18 , 4-methoxyphenyl claim 18 , 4-hydroxyphenyl claim 18 , 5-chloro-2-pyridyl claim 18 , 4-pyridyl or 4-pyridyl N-oxide.21. A compound according to claim 1 , wherein Ris selected from O claim 1 , —CHR claim 1 , —C(═Y)R claim 1 , —C(═Y)OR claim 1 , —C(═Y)N(R)R claim 1 , —C(═Y)CHN(R)R claim 1 , —C(═Y)CHSRand —S ...

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09-01-2014 дата публикации

1,2-disubstituted heterocyclic compounds

Номер: US20140011808A1
Принадлежит: Envivo Phamaceuticals Inc

1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.

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16-01-2014 дата публикации

ADJUVANT NANOEMULSIONS WITH CRYSTALLISATION INHIBITORS

Номер: US20140017279A1
Принадлежит: NOVARTIS AG

High loading of lipophilic pharmacological agents (in particular, lipophilic immunopotentiators) in oil-in-water emulsions can result in crystallisation of the lipophilic agent. To overcome this problem the invention uses an oil-in-water emulsion in combination with a crystallisation inhibitor, and this combination provides emulsions which can be loaded with high levels of lipophilic pharmacological agents. 1. An oil-in-water emulsion comprising an aqueous phase , an oil phase , a surfactant , and a crystallisation inhibitor , wherein the average droplet size in the emulsion is less than 250 nm.2. The emulsion of claim 1 , including a lipophilic small molecule immune potentiator (SMIP).3. The emulsion of claim 2 , wherein the SMIP is a TLR agonist.4. The emulsion of claim 3 , wherein the SMIP is a naphthyridine agonist of TLR7.5. The emulsion of claim 2 , wherein >80% of the SMIP is present in the emulsion's oil droplets.6. The emulsion of claim 2 , wherein crystallisation inhibitor is a polyvinylpyrrolidone.7. The emulsion of claim 2 , wherein the oil phase comprises squalene.8. The emulsion of claim 2 , wherein the aqueous phase comprises a buffer.9. The emulsion of claim 2 , wherein surfactant comprises polysorbate 80.10. The emulsion of claim 2 , comprising 2-20% (by volume) oil and 0.001%-8% (by weight) surfactant.11. The emulsion of claim 2 , wherein the weight ratio of oil to surfactant is between 4:1 and 5:1.12. The emulsion of claim 2 , comprising squalene claim 2 , polysorbate 80 and a polyvinylpyrrolidone claim 2 , wherein the average diameter of the emulsion's droplets is between 80 nm and 180 nm.13. An immunogenic composition comprising (a) the emulsion and (b) an immunogen.14. The composition of claim 13 , wherein the immunogen elicits an immune response in vivo against a bacterium or a virus.15Neisseria meningitidis.. The composition of claim 14 , wherein the bacterium is16. The composition of claim 14 , wherein the virus is an influenza virus.17. A ...

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16-01-2014 дата публикации

QUINOLINONE DERIVATIVES FOR USE IN THE TREATMENT OF AN AUTOIMMUNE DISEASE AND/OR AN INFLAMMATORY DISEASE

Номер: US20140018384A1
Принадлежит: PRONOXIS AB

There is provided compounds of formula I, wherein Xto X, Rto R, Y, Yand L are as defined in the description, and pharmaceutically-acceptable salts thereof, which may be useful in the treatment and/or prophylaxis of autoimmune diseases, inflammatory (e.g. chronic inflammatory) diseases and/or other diseases that may benefit from production of ROS (reactive oxygen species) by a NADPH oxidase complex. 2. A compound as claimed in claim 1 , wherein:{'sup': 6', '7', 'n, 'at least one of Rand Ris present and represents —OR, or'}{'sup': 6', '7, 'sub': 1-4', '1-4', '1-3, 'Rand Rare both present and are linked together to form a —O—Calkylene-, —Calkylene-O— or —O—Calkylene-O— group.'}3. A compound as claimed in claim 2 , wherein:{'sup': 6', '7, 'sub': '1-3', 'Rand Rare both present and are linked together to form a —O—Calkylene-O— group.'}4. A compound as claimed in claim 1 , wherein:{'sup': 1', '2', '3', '4', '5', '6', '7', '8', '1', '4, 'X, X, Xand Xeach represents CR, CR, CR, CRrespectively or any one of Xto X, alternatively and independently represents N;'}{'sup': 1', '2', 'a', 'c', 'd', 'f', 'g', 'h', 'i', 'j', 'k', 'l', 'm', 'n', 'q', 'r', 's, 'sub': 2', '2', 'm', '2, 'Eand Eeach independently represent halogen, —R, —CN, C(O)N(R)R, —N(R)R, —N(R)C(O)R, —N(R)C(O)OR, NO, —N(R)S(O)—R, —OR, —S(O)Ror S(O)N(R)R; or'}{'sup': 1', '2, 'sub': 1-5', '1-4', '1-4', '1-3', '1-3, 'any two Eor Esubstituents, when adjacent to one another, may be linked to form a —Calkylene-, O—Calkylene-, —Calkylene-O— or a O—Calkylene-O— group, which groups are optionally substituted by one or more substituent selected from —F, Calkyl, optionally substituted by one or more —F, and ═O;'}{'sup': '1', 'sub': 2', '2', '3, 'Rrepresents hydrogen, -Me, -Et, —CHF, —CHFor —CF;'}{'sup': '2', 'Rrepresents hydrogen, -Me or -Et;'}{'sup': 3', '4', '3', '4, 'Rand Reach independently represents hydrogen or -Me, or Rand Rmay be linked to form a further 3- to 4-membered ring;'}{'sup': 5', '6', '7', '8', 'a', 'c', 'd', 'f ...

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23-01-2014 дата публикации

SUBSTITUTED FUSED TRICYCLIC COMPOUNDS, COMPOSITIONS AND MEDICINAL APPLICATIONS THEREOF

Номер: US20140023614A1
Принадлежит:

The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity. Such conditions include, but not limited to, arthritis, Alzheimer's disease, autoimmune thyroid disorders, cancer, diabetes, leukemia, T-cell prolymphocytic leukemia, lymphoma, myleoproliferation disorders, lupus, multiple myeloma, multiple sclerosis, osteoarthritis, sepsis, psoriatic arthritis, prostate cancer, T-cell autoimmune disease, inflammatory diseases, chronic and acute allograft transplant rejection, bone marrow transplant, stroke, asthma, chronic obstructive pulmonary disease, allergy, bronchitis, viral diseases, or Type I diabetes, complications from diabetes, rheumatoid arthritis, asthma, Crohn's disease, dry eye, uveitis, inflammatory bowel disease, organ transplant rejection, psoriasis and ulcerative colitis. The present disclosure also relates to process for the preparation of such compounds, and to pharmaceutical compositions containing them. 3. The compound of formula (Ia) as claimed in claim 2 , wherein claim 2 ,{'sup': '1', 'Yrepresents N or CR′ wherein R′ is H or alkyl;'}A represents a six membered ring which is saturated, unsaturated or partially unsaturated optionally having up to three heteroatoms selected from O, N or S;{'sup': '1', 'Ris selected from hydrogen or alkyl;'}{'sup': '2', 'Ris selected from the group consisting of hydrogen, halogen, hydroxyl, cyano and alkyl;'}{'sup': '3', 'Ris selected from the group consisting of hydrogen, hydroxyalkyl, amino, monoalkylamino, dialkylamino, halogen, perhaloalkyl, cyano, nitro, alkoxyalkyl, carboxy, carboxyalkyl, acyl, ...

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30-01-2014 дата публикации

TRI - AND TETRACYCLIC PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS AS ANTINEOPLASTIC AGENT

Номер: US20140031362A1
Принадлежит: PIERRE FABRE MEDICAMENT

The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent. 119.-. (canceled)22. The compound according to claim 20 , wherein Rand Rtogether form claim 20 , with the carbon atoms that carry them claim 20 , a ring selected from an aryl claim 20 , a heteroaryl claim 20 , a carbocycle and a heterocycle claim 20 ,{'sub': 2', '26', '27', '28', '29', 'N', '2', '31', '2', '32', '33', '34', '35', '36', '37', '2', '38', '2', '39', '40', '2', '41', '42', '1', '6', '1', '6', '43', '44', '45', '1', '6', '1', '6, 'said ring being optionally substituted by one or more groups selected from a halogen atom, a CN, NO, OR, SR, NRR, COR, COR, OCOR, CONRR, NRCOR, NRSOR, SONRR, SOR, SOR, (C-C)alkyl, aryl, heteroaryl, carbocycle and heterocycle group, the (C-C)alkyl chains as well as the rings of the whole being optionally substituted by one or more groups selected from OR, NRR, —C(O)O—(C-C)-alkyl, heterocycle and (C-C)-alkyl.'}23. The compound according to claim 20 , wherein Rand Reach represent claim 20 , independently of each other claim 20 , a hydrogen atom claim 20 , a halogen atom claim 20 , or a (C-C)alkenyl claim 20 , (C-C)alkynyl claim 20 , aralkyl claim 20 , (C-C)alkyl claim 20 , aryl claim 20 , heteroaryl claim 20 , carbocycle or heterocycle group claim 20 , the (C-C)alkenyl and (C-C)alkynyl chains as well as the aromatic or non-aromatic rings of the whole being optionally substituted by one or more groups selected from a halogen atom claim 20 , a CN claim 20 , NO claim 20 , OR claim 20 , SR claim 20 , NRR claim 20 , COR claim 20 , COR claim 20 , OCOR claim 20 , CONRR claim 20 , NRCOR claim 20 , NRSOR claim 20 , SONRR claim 20 , SOR claim 20 , SOR claim 20 , ( ...

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06-02-2014 дата публикации

TFEB PHOSPHORYLATION INHIBITORS AND USES THEREOF

Номер: US20140038920A1
Принадлежит: FONDAZIONE TELETHON

The invention refers to TFEB phosphorylation inhibitors. Such molecules have a therapeutic applicability in all disorders that need induction of the cell authophagic/lysosomal system, such as lysosomal storage disorders, neurodegenerative diseases, hepatic diseases, muscle diseases and metabolic diseases. 134-. (canceled)35. A method of producing lysosomal endogeneous or recombinant enzymes comprising:(1) contacting an inhibitor of TFEB phosphorylation with the autophagic/lysosomal system in a cell;(2) inducing said autophagic/lysosomal system; and(3) increasing production of said lysosomal enzymes.36. A method of treating a disorder alleviated comprising administering to a subject in need thereof a therapeutically effective amount of an inhibitor of TFEB phosphorylation.37. (canceled)38. The method according to wherein the disorder is selected from the group consisting of lysosomal storage disorders claim 36 , neurodegenerative diseases claim 36 , hepatic diseases claim 36 , muscle diseases and metabolic diseases.39. The method according to wherein the disorder is a metabolic disease wherein the metabolic disease is hypercholesterolemy or fatty liver disease.40. The method according to wherein the disorder is a neurodegenerative disease and the neurodegenerative disease is selected from the group consisting of Alzheimer's disease claim 38 , Parkinson's disease claim 38 , Huntington's disease claim 38 , Creutzfeldt-Jakob disease claim 38 , and spinocerebellar ataxia.41. The method according to wherein the disorder is a lysosomal storage disorder and wherein the lysosomal disorder is selected from the group consisting of: activator deficiency/GM2 gangliosidosis claim 38 , alpha-mannosidosis claim 38 , aspartylglucosaminuria claim 38 , cholesteryl ester storage disease claim 38 , chronic hexosaminidase A deficiency claim 38 , cystinosis claim 38 , Danon disease claim 38 , Fabry disease claim 38 , Farber disease claim 38 , fucosidosis claim 38 , galactosialidosis claim ...

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06-02-2014 дата публикации

Serotonin receptor modulator

Номер: US20140038943A1
Принадлежит: Janssen Pharmaceutica NV

Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.

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06-02-2014 дата публикации

Treatment of glaucoma

Номер: US20140039003A1

A method is provided for treating patients suffering from elevated intraocular pressure or fluctuation in intraocular pressure, including for example glaucoma patients. The method comprises administering to the patient an inhibitor of orexin activity in an amount sufficient to reduce intraocular pressure or intraocular pressure fluctuation in one or both eyes of the patient.

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13-02-2014 дата публикации

METHOD OF TREATMENT USING CHECKPOINT KINASE 1 INHIBITORS

Номер: US20140045782A1
Принадлежит:

Methods of treating cancer by administering a DNA damaging agent and a CHK1 Inhibitor on a dosing regimen are provided. 1. A method for treating cancer comprising administering a DNA damaging agent followed by four doses of a CHK1 inhibitor , wherein the first two doses of the CHK1 inhibitor are administered one day after the DNA damaging agent , and the third and fourth doses of the CHK1 inhibitor are administered two days after the DNA damaging agent , and wherein said CHK1 inhibitor is selected from the group consisting of: (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 ,3-b]pyridin-3-yl)nicotinamide; (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 ,3-b]pyridin-3-yl)isobutyramide; (R)—N-(5-bromo-4-(3-(methylamino)piperidin-1-yl)-1H-pyrrolo[2 ,3-b]pyridin-3-yl)nicotinamide; (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 ,3-b]pyridin-3-yl)-5-methylnicotinamide; (R)—N-4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 ,3-b]pyridin-3-yl)cyclopropanecarboxamide; (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 ,3-b]pyridin-3-yl)-3-methylbutanamide; and (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 ,3-b]pyridin-3-yl)-2-cyclopropylacetamide.2. The method of claim 1 , wherein the CHK1 inhibitor is (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 claim 1 ,3-b]pyridin-3-yl)nicotinamide.3. The method of claim 1 , wherein the CHK1 inhibitor is (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 claim 1 ,3-b]pyridin-3-yl)isobutyramide.4. The method of claim 1 , wherein the CHK1 inhibitor is (R)—N-(5-bromo-4-(3-(methylamino)piperidin-1-yl)-1H-pyrrolo[2 claim 1 ,3-b]pyridin-3-yl)nicotinamide.5. The method of claim 1 , wherein the CHK1 inhibitor is (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 claim 1 ,3-b]pyridin-3-yl)-5-methylnicotinamide.6. The method of claim 1 , wherein the CHK1 inhibitor is (R)—N-(4-(3-aminopiperidin-1-yl)-5-bromo-1H-pyrrolo[2 claim 1 ,3-b]pyridin-3-yl)cyclopropanecarboxamide.7. The method of claim 1 , wherein ...

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20-02-2014 дата публикации

Methods of treating a disease or condition of the central nervous system

Номер: US20140051701A1
Принадлежит: Bionomics Ltd

The present invention provides methods of treating central nervous system disorders, such as mood disorders (e.g., depression) and neurodegenerative diseases using compounds of formula (I). The subject disclosure enables the manufacture of medicaments as well as compositions containing same for use in methods of therapy and prophylaxis of central nervous system disorders.

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13-03-2014 дата публикации

Block Copolymer For Intraperitoneal Administration Containing Anti-Cancer Agent, Micelle Preparation Thereof, And Cancer Therapeutic Agent Comprising The Micelle Preparation As Active Ingredient

Номер: US20140072604A1
Принадлежит: Nippon Kayaku Co Ltd

To provide a therapeutic method using a water soluble, high molecular weight block polymer to enable that an intraperitoneally administered anti-cancer agent may maintain for a long-term retention in the abdominal cavity to enoughly exert the effect of the anti-cancer agent and reduce adverse side-effects thereof. A therapeutic agent as a micelle preparation, comprising a copolymer having a hydrophilic polymeric moiety and a polycarboxylic acid derivative moiety; and an anti-cancer agent bonding to or encapsulated in the copolymer, wherein the micelle preparation may exhibit sustained drug release capability, and enables an extension of a retention time period of the anti-cancer agent in an abdominal cavity, is provided. A superior life-prolonging effect was found in an intraperitoneal administration mouse model compared with a case in which only an encapsulated drug is administered, and thus the present invention was completed accordingly.

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13-03-2014 дата публикации

Ladder-Frame Polyether Conjugates

Номер: US20140073604A1

Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes. 1. A conjugate comprising a ladder frame polyether compound and at least one of the group consisting of biologically active compounds and research compounds , or a salt , solvate , hydrate or coordination compound thereof.2. The conjugate of claim 1 , wherein the at least one compound is a biologically active compound.3. The conjugate of claim 1 , wherein the at least one compound is a research compound.4. The conjugate of claim 2 , wherein the at least one biologically active compound is a drug or pro-drug.5. The conjugate of claim 2 , wherein the at least one biologically active compound is a pesticide.6. (canceled)7. The conjugate of claim 1 , wherein the ladder frame polyether compound is a brevisin compound.8. The conjugate of claim 1 , further comprising one or more linkers connecting one or more of A to L.9. (canceled)10. (canceled)11. A pharmaceutical formulation comprising a pharmaceutically effective amount of the conjugate of and at least one pharmaceutically acceptable carrier.12. (canceled)13. A formulation for use on non-animal target species comprising an effective amount of the conjugate of and at least one adjuvant.14. (canceled)15. A formulation for the control of insects comprising an effective amount of the conjugate of and at least one adjuvant.16. (canceled)17. A method of improving the cellular uptake of a compound selected from the group consisting of one or more biologically active compound and research compound comprising administering the conjugate according to to a target species.18. (canceled)19. (canceled)20. A method of improving the cellular uptake of a compound selected from the group consisting of one or more biologically active compound and research compound comprising ...

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27-03-2014 дата публикации

Method of Inhibiting Constitutively Active Phosphorylated FLT3 Kinase

Номер: US20140088143A1
Автор: Vinay K. Jain
Принадлежит: Arog Pharmaceuticals LLC

The present invention includes a method of inhibiting or reducing deregulated FLT3 tyrosine kinase activity or FLT3 tyrosine kinase expression in a subject with a proliferative disease by administering to the subject having or suspected to have the proliferative disease, a therapeutically or prophylactically effective amount of the compound of Formula I: or pharmaceutically acceptable salt thereof.

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27-03-2014 дата публикации

Method of inhibiting mutant c-kit

Номер: US20140088147A1
Автор: Vinay K. Jain
Принадлежит: Arog Pharmaceuticals LLC

The present invention includes a method of reducing or inhibiting the kinase activity of C-KIT mutant tyrosine kinase activity in a cell or a subject, and the use of such compound for treating mutant C-KIT driven cell proliferative disorder(s) in a subject related to using a compound of the present invention: or pharmaceutically acceptable salt thereof.

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03-04-2014 дата публикации

Pyridonaphthyridine PI3K/MTOR Dual Inhibitors and Preparation and Use Thereof

Номер: US20140093505A1
Автор: Wu Frank, Zhang Yan
Принадлежит: XUANZHU PHARMA CO., LTD.

The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R, R, R, R, R, R, Rand X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease. 2. The compound of claim 1 , and its pharmaceutically acceptable salt claim 1 , stereoisomer or deuteride thereof claim 1 , wherein{'sup': 1', '8, 'Ris 3-14-membered cycloalkyl, 6-14-membered aryl, 3-14-membered heterocyclyl, 7-12-membered spiro ring group or 7-12-membered bridged ring group, all of which are unsubstituted or substituted by 1-3 R;'}{'sup': 2', '8′, 'Ris 3-14-membered cycloalkyl, 6-14-membered aryl or 3-14-membered heterocyclyl, all of which are unsubstituted or substituted by 1-3 R;'}{'sup': 3', '4, 'each of Rand Ris independently selected from the group consisting of hydrogen, halogen, cyano, amino, hydroxy, trifluoromethyl and trifluoromethoxy;'}{'sup': '5', 'Ris hydrogen, cyano or amino;'}{'sup': 6', '7, 'sub': '1-6', 'each of Rand Ris independently selected from the group consisting of hydrogen, hydroxy, halogen, amino, and Calkyl;'}{'sup': 8', '8′, 'each of Rand R is independently selected from the group consisting of'}{'sub': 2', 'n', '2', 'n', '2', 'n', 'm', '2', 'n', 'm', '2', 'n', 'm', '2', 'n', '2', 'n', '2', 'n', '2', 'n', '2', 'n, 'sup': c', 'a', 'b', 'c', 'a', 'b', 'a', 'c', 'a', 'b', 'c', 'a', 'c', 'a', 'a', 'b, '(1) hydroxy, halogen, amino, cyano, —(CH)C(O)R, —(CH)NRR, —(CH)S(O)R, —(CH)S(O)NRR, —(CH)NRS(O)R, —(CH)C(O)(CH)NRR, —(CH)OC(O)R, —(CH)NRC(O)Rand —(CH)NRC(O)NRR,'}{'sub': 1-6', '1-6, '(2) Calkyl and ...

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03-04-2014 дата публикации

2-AMINO-3-(IMIDAZOL-2-YL)-PYRIDIN-4-ONE DERIVATIVES AND THEIR USE AS VEGF RECEPTOR KINASE INHIBITORS

Номер: US20140094488A1
Принадлежит: SANOFI

The invention relates to the compounds of general formula (I): Preparation process and therapeutic use. 2. The compound according to claim 1 , wherein W represents a nitrogen atom or a group CH claim 1 , in the form of the base or of an acid-addition salt.3. The compound according to claim 1 , wherein W represents a nitrogen atom claim 1 , in the form of the base or of an acid-addition salt.4. The compound according to claim 1 , wherein Y represents a group C-C-alkynylene in the form of the base or of an acid-addition salt.5. The compound according to claim 1 , wherein{'sub': 1', '2, 'Z represents a bond, a group CRR;'}{'sub': 1', '1', '6', '2', 'n', '6', '3', '7, 'Rrepresents a group chosen from a hydrogen atom, a group C-C-alkyl, a group (CH)OR, C-C-cycloalkyl, an aryl or a 5- or 6-membered-heteroaryl;'}{'sub': 2', '1', '6, 'Rrepresents a group chosen from a hydrogen atom, a group C-C-alkyl or a trifluoromethyl;'}{'sub': 6', '1', '6, 'Rrepresents a group chosen from a hydrogen atom or a group C-C-alkyl;'}n is equal to 1, 2 or 3;in the form of the base or of an acid-addition salt.6. The compound according to claim 1 , wherein{'sub': 1', '2, 'Z represents a group CRR;'}{'sub': 1', '1', '6', '2', 'n', '6', '3', '7, 'Rrepresents a group chosen from a hydrogen atom, a group C-C-alkyl, a group (CH)OR, C-C-cycloalkyl, an aryl or a 5- or 6-membered-heteroaryl;'}{'sub': 2', '1', '6, 'Rrepresents a group chosen from a hydrogen atom, a group C-C-alkyl or a trifluoromethyl;'}{'sub': 6', '1', '6, 'Rrepresents a group chosen from a hydrogen atom or a group C-C-alkyl; and'}n is equal to 1, 2 or 3;in the form of the base or of an acid-addition salt.7. The compound according to claim 1 , wherein Rrepresents a group chosen from a group C-C-alkyl claim 1 , a group (CH)OR claim 1 , C-C-cycloalkyl or C-C-alkyl optionally substituted by a C-C-cycloalkyl claim 1 , in the form of the base or of an acid-addition salt.8. The compound according to claim 1 , wherein Rrepresents a group C-C- ...

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07-01-2021 дата публикации

EPILEPSY TREATMENT AGENT

Номер: US20210000771A1
Принадлежит: Eisai R&D Management Co., Ltd.

Provided is a combination agent that combines N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide with an AMPA-type glutamate receptor antagonist such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one or 2-fluoro-6-(3-fluoro-8-oxo-7-(pyridin-3-yl)-7,8-dihydro-6H-pyrano[3,2-b:5,4-b′]dipyridin-9-yl)benzonitrile, and it has potential for use as a therapeutic agent for epilepsy. 17.-. (canceled)9. The method according to claim 8 , wherein N-[(1S)-2 claim 8 ,2 claim 8 ,5 claim 8 ,7-tetrafluoro-2 claim 8 ,3-dihydro-1H-inden-1-yl]sulfamide or the pharmaceutically acceptable salt thereof claim 8 , and the AMPA-type glutamate receptor antagonist are administered simultaneously.10. The method according to claim 8 , wherein N-[(1S)-2 claim 8 ,2 claim 8 ,5 claim 8 ,7-tetrafluoro-2 claim 8 ,3-dihydro-1H-inden-1-yl]sulfamide or the pharmaceutically acceptable salt thereof claim 8 , and the AMPA-type glutamate receptor antagonist are administered separately. The present invention relates to a therapeutic agent for epilepsy that combines an indan-1-ylsulfamide derivative and an AMPA-type glutamate receptor antagonist. More specifically, it relates to a therapeutic agent for epilepsy that combines N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide (or a pharmaceutically acceptable salt thereof) and an AMPA-type glutamate receptor antagonist.Epilepsy is one of the most common central nervous system diseases, affecting over 50,000,000 or more persons throughout the world. The WHO defines it as “chronic disease of the brain of various causes, characterized by recurrent seizures (epileptic seizures) due to excessive discharge of cerebral neurons, accompanied by highly variable clinical and laboratory findings”.Examples of known types of epileptic seizures include partial seizures such as simple partial seizures, complex partial seizures and secondary generalized seizures, as well as absent seizures, myoclonic seizures, clonic seizures, tonic ...

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03-01-2019 дата публикации

Tumor therapeutic agent

Номер: US20190000797A1
Принадлежит: Eisai R&D Management Co Ltd

A novel tumor therapeutic agent for a combination therapy is disclosed. More specifically, a tumor therapeutic agent used for a combination therapy of lenvatinib, ifosfamide, and etoposide is disclosed.

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02-01-2020 дата публикации

THERAPEUTIC COMPOSITIONS CONTAINING HARMINE AND ISOVANILLIN COMPONENTS, AND METHODS OF USE THEREOF

Номер: US20200000779A1
Принадлежит: Ankh Life Sciences Limited

Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers. 1. A method of killing or inhibiting the growth of cancer cells comprising the step of administering to a patient a composition comprising a quantity of a harmine component selected from the group consisting of harmine , and the esters , metal complexes , and pharmaceutically acceptable salts thereof , with a quantity of a isovanillin component selected from the group consisting of vanillin , isovanillin , and mixtures thereof , and the esters , metal complexes , and pharmaceutically acceptable salts of the foregoing , said harmine component and said isovanillin component being selected and present in amounts to provide anti-cancer synergy for the composition.2. The method of claim 1 , including the step of co-administering a composition in accordance with said composition together with one or more other chemotherapeutic agents.3. The method of claim 1 , said administering step comprising oral claim 1 , rectal claim 1 ,nasal, ophthalmic, parenteral, cutaneous, and subcutaneous administration.4. The method of claim 1 , including the step of administering said composition at a level of from about 5-2000 mg per day.5. The method of claim 1 , including the step of administering said composition as a single administration per day claim 1 , or multiple administrations per day.6. The method of claim 1 , said composition exhibiting anti-cancer activity against ovarian claim 1 , lung claim 1 , prostate claim 1 , lymphoma claim 1 , leukemia claim 1 , and head and neck cancer cells.7. The method of claim 6 , said composition exhibiting anti-cancer activity against lung cancer cells claim 6 , H358 claim 6 , lymphoma cells claim 6 , MO205 claim 6 , and leukemia cells claim 6 , Jurkat-E6-1. This application a ...

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02-01-2020 дата публикации

PHARMACEUTICAL COMPOSITIONS FOR COMBINATION THERAPY

Номер: US20200000785A1
Принадлежит: PRILENIA NEUROTHERAPEUTICS LTD.

This invention relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a dopaminergic stabilizer known as Pridopidine, and an inhibitor of the vesicular monoamine transporter type 2 (VMAT) known as Tetrabenazine. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for improving the symptomatic therapeutic effects, and for reducing the adverse effects, of Tetrabenazine in the treatment of movement disorders, and in particular movement disorders associated with Huntington's disease, Gilles de la Tourette's syndrome, or tardive dyskinesia. 1. A method of treating a subject afflicted with a movement disorder , obesity , an obesity associated disorder , or a cardiovascular side effect of Pridopidine comprising administering to the subject an amount of Tetrabenazine or a pharmaceutically acceptable salt thereof , and an amount of Pridopidine or a pharmaceutically acceptable salt thereof.2. (canceled)3. The method of claim 1 , wherein the amounts when taken together are more effective to treat the subject than when each agent at the same amount is administered alone.4. The method of claim 1 , wherein either the amount of Tetrabenazine or a pharmaceutically acceptable salt thereof when taken alone claim 1 , and the amount of Pridopidine or a pharmaceutically acceptable salt thereof when taken alone claim 1 , or each such amount when taken alone is not effective to treat the subject.5. A method of reducing or preventing one or more side effects of periodic administration of an amount of Tetrabenazine or a pharmaceutically acceptable salt thereof to a subject claim 1 , comprising periodically administering to the subject an amount of Pridopidine or a pharmaceutically acceptable salt thereof.6. The method of claim 5 , wherein the one or more side effects are selected from depression claim 5 , suicidality claim 5 , akathisia claim 5 , restlessness claim 5 , agitation claim 5 , ...

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03-01-2019 дата публикации

FUSED TRICYCLIC COMPOUNDS AS RAF KINASE INHIBITORS

Номер: US20190000857A1
Принадлежит:

Provided are certain fused tricyclic compounds and salts thereof, compositions thereof and methods of use therefor. 110.-. (canceled)13. The method of claim 12 , wherein X is O.14. The method of claim 12 , wherein R claim 12 , R claim 12 , Rand R claim 12 , which may be the same or different claim 12 , are each selected from hydrogen claim 12 , halogen claim 12 , C1-C4 alkyl claim 12 , C1-C4 haloalkyl claim 12 , —CN claim 12 , —OCH claim 12 , —OCF3 claim 12 , —OH claim 12 , or phenyl.15. The method of claim 12 , wherein R claim 12 , R claim 12 , Rand R claim 12 , which may be the same or different claim 12 , are each selected from hydrogen or —CF.16. The method of claim 12 , wherein Ris —CF.17. The method of claim 12 , wherein R claim 12 , R claim 12 , and Rare each hydrogen.18. The method of claim 11 , wherein the cancer is selected from one or more of the group consisting of melanoma claim 11 , colorectal cancer claim 11 , and thyroid cancer.19. The method of claim 11 , wherein the B-Raf mutation is a B-Raf V600E mutation.24. The method of claim 20 , wherein the cancer is selected from selected from one or more of the group consisting of melanoma claim 20 , colorectal cancer claim 20 , and thyroid cancer.25. The method of claim 20 , wherein the B-Raf mutation is a B-Raf V600E mutation. Disclosed herein are fused tricyclic compounds, pharmaceutical compositions comprising at least one such fused tricyclic compound*processes for the preparation thereof, and the use thereof in therapy. Disclosed herein are certain tricyclic compounds that can be useful for inhibiting Raf kinase and for treating disorders mediated thereby.The Raf/MEK/ERK pathway is of interest for cell survival, growth, proliferation and tumorigenesis (Zebisch et al., Curr Med Chem. 14(5): 601-623, 2007; Roberts and Der, Oncogene 26 (22): 3291-3310, 2007; Montagut and Seltleman, Cancer Lett. 283(2): 125-134, 2009). Stimulation of the Raf/MEK/ERK signal transduction pathway may occur after binding of a ...

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04-01-2018 дата публикации

Therapeutic Nanoparticles With High Molecular Weight Copolymers

Номер: US20180000885A1
Принадлежит: PFIZER INC.

The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 0.1 to about 40 weight percent of a therapeutic agent and about 10 to about 90 weight percent a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic) acid having a number average molecule weight of about 30 kDa to about 90 kDa or the diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer comprises poly(lactic)-co-poly(glycolic) acid having a number average molecule weight of about 30 kDa to about 90 kDa. 1. A biocompatible , therapeutic polymeric nanoparticle comprising: 'about 10 to about 95 weight percent biocompatible polymer, wherein the biocompatible polymer is selected from the group consisting of:', 'about 0.1 to about 40 weight percent of a therapeutic agent; and'}a) a diblock poly(lactic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic) acid having a number average molecule weight of about 30 kDa to about 90 kDa; andb) a diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer comprises poly(lactic)-co-poly(glycolic) acid having a number average molecule weight of about 30 kDa to about 90 kDa.2. The biocompatible claim 1 , therapeutic polymeric nanoparticle of claim 1 , wherein the biocompatible polymer is selected from the group consisting of:a) a diblock poly(lactic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic) acid having a number average molecule weight of about 40 kDa to about 90 kDa; andb) a diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer, ...

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02-01-2020 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF LYSOSOMAL STORAGE DISORDERS AND DISORDERS CHARACTERIZED BY LYSOSOMAL DYSFUNCTION

Номер: US20200000832A1
Автор: Sardiello Marco
Принадлежит:

The present invention relates to compositions and methods of treating lysosomal storage diseases and methods of using trehalose. 1. A method of treating Sanfilippo B disease (MPS IIIB) in a subject in need thereof , the method comprising administering a therapeutically effective amount of a composition comprising a protein kinase B inhibitor and miglustat.2. The method of claim 1 , wherein the protein kinase B inhibitor is trehalose.3. The method of claim 2 , wherein the composition is administered parenterally.4. The method of claim 3 , wherein the administration is completed within less than 120 minutes.5. The method of claim 4 , wherein the trehalose is administered at a dosage range of from about 0.1 g/kg to about 1 g/kg.6. The method of claim 5 , wherein the miglustat is administered at a dosage range of from about 30 to about 100 mg/Kg claim 5 , about 100 to about 300 mg/Kg claim 5 , or about 100 to about 150 mg/Kg.7. The method of claim 6 , wherein the composition is administered parenterally at a per administration dose of between 0.1 g/kg to 1 g/kg trehalose and a per administration dose of the miglustat ranging from about 30 to about 100 mg/Kg claim 6 , about 100 to about 300 mg/Kg claim 6 , or about 100 to about 150 mg/Kg.8. The method of claim 1 , wherein the protein kinase B inhibitor is a trehalose analog.9. The method of claim 8 , wherein the trehalose analog is selected from lentztrehalose A claim 8 , lentztrehalose B claim 8 , and lentztrehalose C.10. The method of claim 2 , wherein the composition is administered orally.11. The method of claim 10 , wherein the trehalose is administered at a dosage range of from about 0.1 g/kg to about 1 g/kg.12. The method of claim 10 , wherein the composition is administered at a per administration dose of miglustat ranging from about 30 to about 100 mg/Kg claim 10 , about 100 to about 300 mg/Kg claim 10 , or about 100 to about 150 mg/Kg.13. The method of claim 2 , wherein the composition is administered orally at ...

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05-01-2017 дата публикации

Azaspiro derivatives as trpm8 antagonists

Номер: US20170002016A1
Принадлежит: Raqualia Pharma Inc

The present invention relates to azaspiro derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

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03-01-2019 дата публикации

IMMUNOREGULATORY AGENTS

Номер: US20190002472A1
Принадлежит:

Compounds that modulate the oxidoreductase enzyme indoleamine 2,3-dioxygenase, and compositions containing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by indoleamine 2,3-dioxygenase is also provided. 1. A compound having the formula (I): the subscript n is 1; the subscript p is 1;', {'sub': '5', 'the ring designated as A is phenyl, 5- or 6-membered heteroaryl, or C-7 cycloalkyl;'}, 'Z is O;', {'sup': '3a', 'B is C(R);'}, {'sup': 5', '5a, 'each X is independently, CHR, C(O), or CH(OR);'}, {'sup': '6', 'Q is N, C(CN), or CR;'}, {'sup': 5', '5a, 'sub': '2', 'D is a bond, O, C(R), or NR;'}, 'E is a substituted 9- or 10-membered fused bicyclic heteroaryl, optionally substituted with halogen;', {'sup': 1', '2, 'Rand Rare independently hydrogen or halogen;'}, {'sup': 3', '3a', '4, 'sub': 1', '6, 'R, Rand Rare independently hydrogen or C-Calkyl;'}, {'sup': '5', 'sub': 1', '6, 'each Ris independently H, F, OH, or C-Calkyl;'}, {'sup': '5a', 'sub': 1', '6, 'each Ris independently H, or C-Calkyl;'}, {'sup': '6', 'sub': 1', '6', '1', '6', '5a', '2, 'Ris H, OH, F, C-Calkyl, —O—C-Calkyl, or —N(R);'}, 'and each m is independently 1, 2, or 3., 'or a pharmaceutically acceptable salt, hydrate or solvate thereof, wherein,'}2. A combination comprising a compound of or a pharmaceutically acceptable salt claim 1 , hydrate or solvate thereof claim 1 , and at least one additional therapeutic agent.3. The combination of claim 2 , wherein said additional therapeutic agent is an immuno-oncology agent.4. The combination of claim 3 , wherein said immuno-oncology agent is selected from a CTLA-4 antagonist claim 3 , a PD-1 antagonist claim 3 , a PD-L1 antagonist claim 3 , a LAG-3 antagonist claim 3 , a CD137 agonist claim 3 , a GITR agonist claim 3 , an OX40 agonist claim 3 , an OX40L antagonist claim 3 , ...

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02-01-2020 дата публикации

HETEROARYL ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Номер: US20200002353A1
Принадлежит: Genentech, Inc.

Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: 2. The compound of claim 1 , wherein A claim 1 , B claim 1 , C claim 1 , and D are each CR.3. The compound of having Formula II claim 1 , wherein Zis CR.4. The compound of having Formula III claim 1 , wherein Zis O or S.5. The compound of having Formula III claim 1 , wherein Zis NR.6. The compound of claim 1 , wherein Cy is phenyldiyl substituted with one or more halo groups.7. The compound of claim 1 , wherein Zis O or NR.8. The compound of claim 7 , wherein Zis NH.9. The compound of claim 1 , wherein Zis O—(C-Calkyldiyl) claim 1 , Yis N claim 1 , and Yis C(R).10. The compound of claim 9 , wherein Yis CH(CHF).11. The compound of claim 1 , wherein Yis CRand Yis NR.12. The compound of claim 11 , wherein Yis NCHCHCHF.13. The compound of claim 1 , wherein Ris C-Calkyl substituted with one or more F.16. A pharmaceutical composition comprising a compound of and at least one pharmaceutically acceptable excipient.17. A method of treating breast cancer claim 1 , lung cancer claim 1 , ovarian cancer claim 1 , endometrial cancer claim 1 , prostate cancer claim 1 , or uterine cancer in a patient having such cancer claim 1 , the method comprising administering a therapeutically effective amount of a compound of .18. The method of claim 17 , further comprising administering an additional therapeutic agent selected from the group consisting of an anti-inflammatory agent claim 17 , an immunomodulatory agent claim 17 , a chemotherapeutic agent claim 17 , an apoptosis-enhancer claim 17 , a neurotropic factor claim 17 , an agent for treating cardiovascular disease claim 17 , an agent for treating liver disease claim 17 , an anti-viral agent claim 17 , an agent for treating blood disorders claim 17 , an agent for treating diabetes claim 17 , and an agent for treating immunodeficiency disorders.19. The method of claim 18 , wherein the additional ...

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04-01-2018 дата публикации

HETEROARYL ESTROGEN RECEPTOR MODULATORS AND USES THEREOF

Номер: US20180002344A1
Принадлежит: Genentech, Inc.

Described herein are heteroaryl compounds with estrogen receptor modulation activity or function having the Formula I, II, and III structures: 2. The compound of wherein A claim 1 , B claim 1 , C claim 1 , and D are each CR.3. The compound of wherein one or two of A claim 1 , B claim 1 , C claim 1 , and D are N.4. The compound of having Formula I wherein Zis O.5. The compound of having Formula I wherein Zis S.6. The compound of having Formula I wherein Zis NR.7. The compound of having Formula II wherein Zis CR.8. The compound of having Formula II wherein Zis N.9. The compound of having Formula III wherein Zis O.10. The compound of having Formula III wherein Zis S.11. The compound of having Formula III wherein Zis NR.12. The compound of wherein Cy is phenyldiyl claim 1 , substituted with one or more F.13. The compound of wherein Zis O or NR.14. The compound of wherein Zis NH.15. The compound of wherein Zis O—(C-Cis N claim 1 , Yis —(CH)— claim 1 , and Yis C(R).16. The compound of wherein Yis CH(CHF).17. The compound of wherein Yis CR claim 1 , Yis —(CH)— claim 1 , and Yis NR.18. The compound of wherein Yis NCHCHCHF.19. The compound of wherein Ris C-Calkyl claim 1 , substituted with one or more F.20. The compound of selected from Tables 1a and 1b.21. A pharmaceutical composition comprised of a compound of and a pharmaceutically acceptable carrier claim 1 , glidant claim 1 , diluent claim 1 , or excipient.22. The pharmaceutical composition according to claim 21 , further comprising a therapeutic agent.23. A process for making a pharmaceutical composition which comprises combining a compound of with a pharmaceutically acceptable carrier claim 1 , glidant claim 1 , diluent claim 1 , or excipient.24. A method of treating an ER-related disease or disorder in a patient comprising administering a therapeutically effective amount of the pharmaceutical composition of to a patient with an ER-related disease or condition.25. The method of wherein the ER-related disease or ...

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13-01-2022 дата публикации

INHIBITORS OF POSITIVE STRAND RNA VIRUSES

Номер: US20220008399A1
Принадлежит:

Methods of treating a disease caused by a positive strand RNA virus. The methods include administering to a subject in need thereof an effective amount of a compound of Formula I or Formula II. 2. The method of claim 1 , wherein the positive strand RNA virus is a flavivirus or a coronavirus.3. The method of claim 1 , wherein the positive strand RNA virus is a SARS-CoV-2 virus claim 1 , a Zika virus claim 1 , a Dengue virus claim 1 , a HCoV-OC43 virus claim 1 , or a HCoV-229E virus.4. The method of claim 2 , wherein the positive strand RNA virus is a Zika virus or a Dengue virus.5. The method of claim 2 , wherein the positive strand RNA virus is a SARS-CoV-2 virus.6. The method of claim 1 , wherein each of R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Ris H; each of R claim 1 , R claim 1 , R claim 1 , and R claim 1 , independently claim 1 , is alkoxy; Ris H or alkoxy; Rand Rtogether are a single bond; X is CH; and Y is N or N+→O−; each of and is a single bond; and n is 1 or 2.8. The method of claim 7 , wherein the positive strand RNA virus is a SARS-CoV-2 virus claim 7 , a Zika virus claim 7 , a Dengue virus claim 7 , a HCoV-OC43 virus claim 7 , or a HCoV-229E virus.9. The method of claim 7 , wherein the positive strand RNA virus is a Zika virus or a Dengue virus.10. The method of claim 7 , wherein the positive strand RNA virus is a SARS-CoV-2 virus.12. The method of claim 11 , wherein the positive strand RNA virus is a flavivirus or a coronavirus.13. The method of claim 11 , wherein the positive strand RNA virus is a SARS-CoV-2 virus claim 11 , a Zika virus claim 11 , a Dengue virus claim 11 , a HCoV-OC43 virus claim 11 , or a HCoV-229E virus.14. The method of claim 12 , wherein the positive strand RNA virus is a Zika virus or a Dengue virus.15. The method of claim 12 , wherein the positive strand RNA virus is a SARS-CoV-2 virus.16. The method of claim 1 , wherein each of R claim 1 , R claim 1 , R ...

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01-01-2015 дата публикации

Tris(hydroxymethyl)Aminomethane Salts of a Small-Molecule GLP1R Agonist and Pharmaceutical Compositions and Uses Thereof

Номер: US20150005339A1
Принадлежит: Trans Tech Pharma Inc

The invention provides tris(hydroxymethyl)aminomethane salts of a small-molecule GLP1R agonist. The invention further provides solid compositions comprising tris(hydroxymethyl)aminomethane salts of a small-molecule GLP1R agonist. The invention further provides uses of tris(hydroxymethyl)aminomethane salts of a small-molecule GLP1R agonist, e.g., for treating type 1 diabetes, type 2 diabetes, or obesity.

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12-01-2017 дата публикации

Adoptive Cellular Therapy Using an Agonist of Retinoic Acid Receptor-Related Orphan Receptor Gamma & Related Therapeutic Methods

Номер: US20170007686A1
Принадлежит:

The invention relates to medical therapy using an agonist of the retinoic acid receptor-related orphan receptor gamma (RORγ) and provides adoptive cellular therapies using an agonist of RORγ, populations of lymphocyte cells that have been exposed to an agonist of RORγ, populations of dendritic cells that have been exposed to an agonist of RORγ, pharmaceutical compositions, and methods for enhancing therapeutic effects of lymphocyte cells and/or dendritic cells in a patient by administering an agonist of RORγ to a patient. 1. A method of delivering to a patient a RORγ agonist treated cell selected from the group consisting of a lymphocyte cell and dendritic cell , comprising administering to a patient in need thereof a pharmaceutical composition comprising said cell that has been exposed ex vivo to an agonist of RORγ.2. The method of claim 1 , further comprising culturing a cell selected from the group consisting of a lymphocyte cell and dendritic cell with an agonist of RORγ to provide the cell that has been exposed ex vivo to an agonist of RORγ.3. The method of claim 2 , wherein the culturing comprises exposing the cell to a cytokine.4. The method of claim 3 , wherein the cytokine is IL-1β claim 3 , IL-2 claim 3 , IL-6 claim 3 , IL-7 claim 3 , IL-10 claim 3 , IL-12 claim 3 , IL-15 claim 3 , IL-18 claim 3 , IL-21 claim 3 , IL-23 claim 3 , or transforming growth factor beta.5. The method of any one of - claim 3 , wherein the culturing comprises exposing the cell to an antigen associated with a medical disorder.6. The method of claim 5 , wherein the antigen comprises cancer tissue.7. The method of any one of - claim 5 , further comprising obtaining a lymphocyte cell or dendritic cell from said patient for use in the culturing step.8. The method of any one of - claim 5 , further comprising obtaining a lymphocyte cell or dendritic cell from a subject that produces cells allogenic to cells of the patient claim 5 , for use in the culturing step.9. The method of any one of ...

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14-01-2016 дата публикации

Compounds, compositions, and methods for preventing metasasis of cancer cells

Номер: US20160008327A1
Принадлежит: Aerpio Therapeutics LLC

Disclosed are methods for preventing metastasis of cancer cells. The disclosed compounds can be used to prevent the spread of tumor or other types of cancer cells.

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14-01-2016 дата публикации

PROPHYLACTIC OR THERAPEUTIC AGENT FOR POSTERIOR OCULAR DISEASE CONTAINING TETRAHYDROPYRANYLAMINOCYCLOPENTYLCARBONYLTETRAHYDROPYRIDOPYRIDINE DERIVATIVE AS EFFECTIVE INGREDIENT

Номер: US20160008333A1
Принадлежит: SANTEN PHARMACEUTICAL CO., LTD.

The present invention relates to a prophylactic or therapeutic agent for a posterior ocular disease containing the compound represented by a formula (1), its enantiomer or diastereomer, or their pharmaceutically acceptable salt thereof as an active ingredient. 3. The prophylactic or therapeutic agent according to claim 1 , wherein the pharmaceutically acceptable salt of the compound represented by the formula (1) or the formula (1a) is a succinate.4. The prophylactic or therapeutic agent according to claim 1 , wherein the posterior ocular disease is a disease at a vitreous body claim 1 , a retina claim 1 , a choroid claim 1 , a sclera or an optic nerve.5. The prophylactic or therapeutic agent according to claim 1 , wherein the posterior ocular disease is a posterior ocular disease to which a CCR2 receptor pertains.6. The prophylactic or therapeutic agent according to claim 1 , wherein the posterior ocular disease is at least one selected from the group consisting of age-related macular degeneration claim 1 , diabetic retinopathy claim 1 , diabetic macular edema claim 1 , retinal pigmentary degeneration claim 1 , proliferative vitreoretinopathy claim 1 , retinal artery occlusion claim 1 , retinal vein occlusion claim 1 , uveitis claim 1 , Leber's disease claim 1 , retinopathy of prematurity claim 1 , retinal detachment claim 1 , retinal pigment epithelial detachment claim 1 , central serous chorioretinopathy claim 1 , central exudative chorioretinopathy claim 1 , polypoidal choroidal vasculopathy claim 1 , multiple choroiditis claim 1 , neovascular maculopathy claim 1 , retinal aneurysm claim 1 , retinal angiomatous proliferation claim 1 , ophthalmic nerve disorder caused by these diseases claim 1 , ophthalmic nerve disorder caused by glaucoma and ischemic ophthalmic nerve disorder.7. The prophylactic or therapeutic agent according to claim 1 , wherein the posterior ocular disease is at least one selected from the group consisting of age-related macular degeneration ...

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11-01-2018 дата публикации

METHOD FOR MANUFACTURING NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF AND MANUFACTURING INTERMEDIATE OF NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF

Номер: US20180008583A1
Принадлежит: FUJIFILM Corporation

Provided are a method for efficiently manufacturing a nitrogen-containing compound, which is used for manufacturing a treatment agent for integrin-related diseases, or a salt thereof and a manufacturing intermediate of the compound or a salt thereof. 2. The manufacturing method according to claim 1 ,{'sup': '2', 'sub': '1-6', 'wherein Ris a Calkyl group which may be substituted or a benzyl group which may be substituted.'}6. The manufacturing method according to claim 1 ,{'sup': '1', 'sub': '1-6', 'wherein Ris a hydrogen atom, a Calkoxycarbonyl group which may be substituted, an arylsulfonyl group which may be substituted, or a heterocyclic sulfonyl group which may be substituted.'}7. The manufacturing method according to claim 1 ,{'sup': '7', 'sub': '1-6', 'wherein Ris a Calkyl group which may be substituted or a benzyl group which may be substituted.'}8. The manufacturing method according to claim 1 ,wherein the step of deprotecting is a step of deprotecting by using an acid.9. A method for manufacturing a metal complex claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a step of reacting the compound represented by Formula [11] or a salt thereof obtained by the manufacturing method according to with a metal ion.'}11. The compound according to or a salt thereof claim 10 ,{'sup': '8', 'sub': '2-6', 'wherein Ris a Calkyl group which may be substituted.'}15. The compound according to or a salt thereof claim 10 ,{'sup': '1', 'sub': '1-6', 'wherein Ris a hydrogen atom, a Calkoxycarbonyl group which may be substituted, an arylsulfonyl group which may be substituted, or a heterocyclic sulfonyl group which may be substituted.'}16. The compound according to or a salt thereof claim 10 ,{'sup': '7', 'sub': '1-6', 'wherein Ris a Calkyl group which may be substituted or a benzyl group which may be substituted.'}18. The compound according to or a salt thereof claim 17 ,{'sup': '7', 'sub': '1-6', 'wherein Ris a Calkyl group which may be substituted or a ...

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11-01-2018 дата публикации

Combination therapy with an antitumor alkaloid

Номер: US20180008602A1
Принадлежит: Pharmamar SA

The present invention relates to the combination of PM01183 with several anticancer drugs, in particular other anticancer drugs selected from antitumor platinum coordination complexes, antimetabolites, mitotic inhibitors, anticancer antibiotics, topoisomerase I and/or II inhibitors, proteasome inhibitors, histone deacetylase inhibitors, nitrogen mustard alkylating agents, nitrosourea alkylating agents, nonclassical alkylating agents, estrogen antagonists, androgen antagonists, mTOR inhibitors, tyrosine kinase inhibitors, and other agents selected from aplidine, ET-743, PM02734 and PM00104, and the use of these combinations in the treatment of cancer.

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11-01-2018 дата публикации

BICYCLIC HETEROCYCLES AS FGFR4 INHIBITORS

Номер: US20180008610A1
Принадлежит:

The present disclosure relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of the FGFR4 enzyme and are useful in the treatment of FGFR4-associated diseases such as cancer. 3. (canceled)5. (canceled)6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is C-Carylene.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is 1 claim 1 ,3-phenylene.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is 5-membered heteroarylene.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring A is a 5-membered heteroarylene selected from pyrrol-2 claim 1 ,5-diyl claim 1 , pyrrol-1 claim 1 ,2-diyl claim 1 , pyrrol-3 claim 1 ,4-diyl claim 1 , pyrrol-2 claim 1 ,3-diyl claim 1 , pyrrol-1 claim 1 ,3-diyl claim 1 , pyrrol-1 claim 1 ,4-diyl claim 1 , pyrazol-1 claim 1 ,3-diyl claim 1 , pyrazol-1 claim 1 ,4-diyl claim 1 , pyrazol-1 claim 1 ,5-diyl claim 1 , pyrazol-3 claim 1 ,4-diyl claim 1 , pyrazol-4 claim 1 ,5-diyl claim 1 , pyrazol-3 claim 1 ,5-diyl claim 1 , imidazol-1 claim 1 ,2-diyl claim 1 , imidazol-1 claim 1 ,4-diyl claim 1 , imidazol-1 claim 1 ,5-diyl claim 1 , imidazol-2 claim 1 ,4-yl claim 1 , imidazol-2 claim 1 ,5-diyl claim 1 , triazol-diyl claim 1 , tetrazol-diyl claim 1 , oxazol-2 claim 1 ,5-diyl claim 1 , oxazol-2 claim 1 ,4-diyl claim 1 , thiophen-2 claim 1 ,3-diyl claim 1 , thiophen-2 claim 1 ,4-diyl claim 1 , thiophen-2 claim 1 ,5-diyl claim 1 , thiazol-2 claim 1 ,4-diyl claim 1 , thiazol-2 claim 1 ,5-diyl claim 1 , isoxazol-3 claim 1 ,4-diyl claim 1 , isoxazol-3 claim 1 ,5-diyl claim 1 , isothiazol-3 claim 1 ,4-diyl claim 1 , isothiazol-3 claim 1 ,5-diyl claim 1 , furan-2 claim 1 ,3-diyl claim 1 , furan-2 claim 1 ,4-diyl or furan-2 claim 1 ,5-diyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ...

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14-01-2021 дата публикации

PARTICULATE SUBSTANCE MIXTURE, PREFERABLY FOR USE IN THE PROPHYLAXIS AND/OR TREATMENT OF A RESPIRATORY DISORDER

Номер: US20210008090A1
Принадлежит:

A particulate substance mixture, preferably for use in the prophylaxis and/or treatment of a respiratory disorder includes a mucolytic substance and amorphous silicon dioxide. The mixture may also have the following characteristics: the amorphous silicon dioxide is hydrophilic silicon dioxide, the amorphous silicon dioxide has a mean particle diameter ≤20 μm, and an amount of the amorphous silicon dioxide is 0.1% by weight to 10% by weight, based on the total weight of the particulate substance mixture. 120-. (canceled)21. A method for preventing and/or treating a respiratory disorder , comprising the step of administering a particulate substance mixture to a human or non-human mammal , wherein the particulate substance mixture comprises a mucolytic substance and amorphous silicon dioxide , wherein the amorphous silicon dioxide is present in the form of particles having a mean particle diameter <20 μm and wherein the mucolytic substance is present in the form of particles having a mean particle diameter <20 μm.22. The method as claimed in claim 21 , wherein the amorphous silicon dioxide is hydrophilic silicon dioxide.23. (canceled)24. The method as claimed in claim 21 , wherein an amount of the amorphous silicon dioxide is 0.1% by weight to 10% by weight claim 21 , based on the total weight of the particulate substance mixture.25. The method as claimed in claim 21 , wherein the mucolytic substance is a secretolytically claim 21 , mucolytically or secretomotorically active substance.26. The method as claimed in claim 21 , wherein the mucolytic substance is an organic compound selected from the group consisting of emetine claim 21 , saponins claim 21 , acetylcysteine claim 21 , bromhexine claim 21 , ambroxol claim 21 , clenbuterol and mixtures of at least two of said organic compounds.27. The method as claimed in claim 21 , wherein the mucolytic substance is an inorganic salt.28. The method as claimed in claim 21 , wherein the mucolytic substance is selected from the ...

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09-01-2020 дата публикации

METHODS FOR TREATING PULMONARY NON-TUBERCULOUS MYCOBACTERIAL INFECTIONS

Номер: US20200009171A1
Автор: EAGLE Gina, Gupta Renu
Принадлежит:

Provided herein are methods for treating a pulmonary infection in a patient in need thereof, for example, a nontuberculous mycobacterial pulmonary infection for at least one treatment cycle. The method comprises administering to the lungs of the patient a pharmaceutical composition comprising a liposomal complexed aminoglycoside comprising a lipid component comprising electrically neutral lipids and an aminoglycoside. Administration comprises aerosolizing the pharmaceutical composition to provide an aerosolized pharmaceutical composition comprising a mixture of free aminoglycoside and liposomal complexed aminoglycoside, and administering the aerosolized pharmaceutical composition via a nebulizer to the lungs of the patient. The methods provided herein result in a change from baseline on the semi-quantitative scale for mycobacterial culture for a treated patient, and/or NTM culture conversion to negative during or after the administration period. 189.-. (canceled)90Mycobacterium avium. A method for treating a complex (MAC) lung infection , comprising:administering to the patient a macrolide antibiotic; andadministering to the lungs of the patient for an administration period of at least six months, a pharmaceutical composition comprising amikacin, or a pharmaceutically acceptable salt thereof, encapsulated in a plurality of liposomes, wherein the lipid component of the plurality of liposomes consists of an electrically neutral phospholipid and cholesterol,wherein administering to the lungs of the patient comprises aerosolizing the pharmaceutical composition via a nebulizer to provide an aerosolized pharmaceutical composition comprising a mixture of free amikacin, or a pharmaceutically acceptable salt thereof, and liposomal complexed amikacin, or a pharmaceutically acceptable salt thereof, and administering the aerosolized pharmaceutical composition via the nebulizer to the lungs of the patient once daily in a single dosing session during the administration period; ...

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