ПРИМЕНЕНИЕ НЕСТЕРОИДНЫХ ПРОТИВОВОСПАЛИТЕЛЬНЫХ СРЕДСТВ ПОСРЕДСТВОМ ИНГАЛЯЦИИ В ЛЕЧЕНИИ ОСТРОГО И ХРОНИЧЕСКОГО БРОНХИТОВ

Предложено применение нестероидного противовоспалительного средства лизина ацетилсалицилата, введенного путем ингаляции с помощью небулайзера, пригодного для аэрозольной терапии, для лечения хронической обструктивной болезни легких или эмфиземы. Показано, что такое введение не только положительно влияет на кашель больных, но также улучшает функцию дыхательной системы (снижает выраженность симптомов бронхообструкции), поскольку препарат больше абсорбируется и накапливается легочными структурами, задействованными при заболевании. 3 з.п. ф-лы.

КОМПОЗИЦИИ И СПОСОБЫ ПРИМЕНЕНИЯ ФОРБОЛОВЫХ ЭФИРОВ ДЛЯ ЛЕЧЕНИЯ ИНСУЛЬТА

Настоящая группа изобретений относится к медицине, а именно к терапии и неврологии, и касается применения форболового эфира для лечения инсульта. Для этого вводят эффективное количество форболового эфира формулыЭто обеспечивает эффективное лечение инсульта и его неврологических осложнений за счет модулирования фактора NF-kB и активности цитокинов Th1. 4 н. и 14 з.п. ф-лы, 1 табл., 10 пр.

СОЕДИНЕНИЯ, ПРИМЕНЯЕМЫЕ В ЛЕЧЕНИИ НЕОПЛАСТИЧЕСКИХ ЗАБОЛЕВАНИЙ

Настоящее изобретение относится к соединениям и их фармацевтически приемлемым солям, которые применяются в лечении неопластических заболеваний или расстройств, фармацевтической композиции, содержащей такое соединение, и способу получения этого соединения. Лекарственное средство для лечения неопластического заболевания или (дис)пролиферативного расстройства, содержащее соединение, выбранное из группы, состоящей из:,,,,. Лекарственное средство для лечения злокачественной опухоли, содержащее соединение. 7 н. и 7 з.п. ф-лы, 9 ил., 2 табл., 8 пр.

НОВОЕ СОЕДИНЕНИЕ И ЕГО ПРИМЕНЕНИЕ В МЕДИЦИНЕ

Изобретение относится к (2S)-2-амино-3-(3,4-бис((2-(бензоилокси)-2-метилпропаноил)окси)фенил)пропановой кислоте, ее соли, выбранной из кислотно-аддитивных солей, солей щелочных металлов, солей щелочноземельных металлов, солей аммония, солей тетраметиламмония, солей тетрабутиламмония, солей фармацевтически приемлемых органических аминов и солей природных основных аминокислот, или ее низкотоксичному и растворимому в воде сольвату, которые могут найти применение для профилактики и/или лечения болезни Паркинсона и/или синдрома Паркинсона. Предлагаемая (2S)-2-амино-3-(3,4-бис((2-(бензоилокси)-2-метилпропаноил)окси)фенил)пропановая кислота, ее соль или сольват является пролекарством леводопы, которое позволяет обеспечить эффективную концентрацию леводопы в крови при небольшом числе доз. Изобретение относится также к фармацевтической композиции и лекарственному средству, содержащим (2S)-2-амино-3-(3,4-бис((2-(бензоилокси)-2-метилпропаноил)окси)фенил)пропановую кислоту, ее соль или сольват. 3 н ...

КОМПОЗИЦИИ ГЕЛЯ С БРИМОНИДИНОМ И СПОСОБЫ ПРИМЕНЕНИЯ

Группа изобретений относится к фармацевтической промышленности, а именно к композиции геля для местного применения, содержащей от 0,05 до 0,20 % мас. метилпарабена в качестве консерванта; один или более дополнительных консервантов; от 0,80 до 1,50 % мас. карбомера; от 9,0 до 13,0 % мас. общего содержания многоатомных спиртов, в частности пропиленгликоль и глицерин; активный ингредиент, содержащий агонист альфа-адренергических рецепторов или его фармацевтически приемлемую соль, в частности бримонидин тартрат, и очищенную воду, в которой общее количество всех ингредиентов равно 100%, pH композиции составляет от 4,5 до 7,5, и где при концентрации метилпарабена более 0,15 % мас. концентрация карбомера составляет менее 1,25 % мас., и способу лечения или предотвращения заболевания кожи у пациента. Группа изобретений обеспечивает создание улучшенной композиции геля для местного применения, которая по существу не содержит кристаллов метилпарабена и обладает микробиологической чистотой. 4 н. и 11 ...

ИСПОЛЬЗОВАНИЕ ПРОИЗВОДНЫХ (3-ТРИГАЛОМЕТИЛФЕНОКСИ)-(4-ГАЛОФЕНИЛ) УКСУСНОЙ КИСЛОТЫ ДЛЯ ЛЕЧЕНИЯ РЕЗИСТЕНТНОСТИ К ИНСУЛИНУ, ДИАБЕТА II ТИПА, ГИПЕРЛИПИДЕМИИ И ГИПЕРУРИКЕМИИ

Изобретение относится к усовершенствованным способам модулирования диабета II типа у млекопитающего и модулирования резистентности к инсулину, включающим введение указанному млекопитающему, нуждающемуся в этом, (-)стереоизомера соединения формулы I, в которой R выбран из группы, состоящей из гидрокси, низшего аралкокси, ди-низшего алкиламино-низшего алкокси, низшего алканамидо низшего алкокси, бензамидо-низшего алкокси, уреидо-низшего алкокси, N'-низшего алкил-уреидо-низшего алкокси, карбамоил-низшего алкокси, галофеноксизамещенного низшего алкокси, карбамоилзамещенного фенокси, или R представляет собой гидролизуемую сложноэфирную группировку; каждый Х независимо представляет собой галоген; или его фармацевтически приемлемой соли, причем (-)стереоизомер по существу не содержит (+)стереоизомера соединения. Изобретение также относится к фармацевтическим композициям, содержащим (-)стереоизомер соединения формулы I и где композиции обладают существенно сниженным ингибирующим эффектом на цитохром ...

Композиции, полезные для предупреждения и/или лечения костно-суставного воспаления и боли и повреждения хряща

Настоящее изобретение относится к фармацевтической промышлености, а именно к композиции, обладающей анальгетической и противовоспалительной активностью. Композиция, обладающая анальгетической и противовоспалительной активностью, которая содержит на единицу дозировки: а) 250,00 мг экстракта Vitis vinifera в форме комплекса с фосфолипидами, б) 50,00 мг липофильного экстракта Zingiber officinale, содержащего 25% масс./масс. гингеролов, в) 20,00 мг липофильного экстракта Zanthoxylum piperitum, полученного путем экстрагирования CO2, стандартизированного до 25% масс./масс. изобутиламидов, и г) 50,00 мг диацереина. Вышеописанная композиция обладает синергетической анальгетической и противовоспалительной активностью. 4 з.п. ф-лы, 2 табл., 7 пр.

Композиция для повышения качества спермы у субъекта мужского пола

Настоящее изобретение относится к фармацевтической промышленности, а именно к композиции для улучшения качества спермы у субъекта мужского пола. Композиция для улучшения качества спермы у субъекта мужского пола, содержащая i) сухой препарат I из корневищ Alpinia galanga или Alpinia conchigera, содержащий по меньшей мере 2% по массе 1'S-1'-ацетоксихавиколацетата, и ii) растительный экстракт II, содержащий соединения с антиоксидантной активностью, получаемые из Punica granatum, где отношение (вес./вес.) между сухим препаратом I и экстрактом II находится в диапазоне от 10:1 до 1:10. Способ лечения мужского бесплодия, обусловленного низким числом сперматозоидов и/или низкой подвижностью сперматозоидов. Набор для улучшения качества спермы у субъекта мужского пола. Вышеописанная композиция эффективна для улучшения качества спермы у субъекта мужского пола. 3 н. и 15 з.п. ф-лы, 4 ил., 8 табл., 6 пр.

ИНГИБИТОРЫ МЕТАЛЛО-β-ЛАКТАМАЗЫ

Изобретение относится к новому ингибитору металло-β-лактамазы, который действует как лекарственное средство для ингибирования инактивации β-лактамовых антибиотиков и восстановления антибактериальных активностей. Производные малеиновой кислоты, имеющие общую формулу (I), имеют металло-β-лактамаза-ингибирующую активность. Возможно восстанавливать антибактериальные активности β-лактамовых антибиотиков в отношении бактерий, продуцирующих металло-β-лактамазу, комбинируя соединение общей формулы (I) с β-лактамовыми антибиотиками. Ингибитор металло-β-лактамазы представляет собой соединение формулы (I) или его фармацевтически приемлемую соль, в которой R1 обозначает С2-6-алкил; С3-7-циклоалкил, где указанный цикл может быть замещен гидроксильной группой или может быть конденсирован с арилом; гидроксиметил; - С1-3-алкиленфенил, где указанная фенильная группа может быть замещена гидроксильной группой, С1-6-алкильной группой, гидроксиметильной группой, группой -СООМ, где М обозначает атом водорода ...

СИСТЕМА ДОСТАВКИ ДЛЯ ДОСТАВКИ ПЕРВОЙ И ВТОРОЙ КОМПОЗИЦИЙ, СОСТАВЛЕННЫХ ДЛЯ ПРИМЕНЕНИЯ К РАЗЛИЧНЫМ ИНДИВИДУУМАМ И ДЛЯ ВЗАИМОДЕЙСТВИЯ ДРУГ С ДРУГОМ ПРИ ФИЗИЧЕСКОМ ВЗАИМОДЕЙСТВИИ ИНДИВИДУУМОВ ДРУГ С ДРУГОМ

... 1. Система доставки для доставки первой и второй композиций, составленных для применения к различным индивидуумам и для взаимодействия друг с другом при физическом взаимодействии индивидуумов друг с другом, причем указанная система доставки содержит:первый контейнер (100), содержащий первую композицию; ивторой контейнер (100), содержащий вторую композицию, составленную для взаимодействия с первой композицией, когда первая и вторая композиции нанесены на участки нанесения первого и второго индивидуумов соответственно, а участки нанесения контактируют друг с другом;где указанные первый и второй контейнеры связаны друг с другом, по меньшей мере, одним из факторов: цветом, формой или физическим соединением для указания индивидуумам, что контейнеры предназначены к использованию в сочетании друг с другом; при этом система дополнительно содержит держатель (200, 300), сконфигурированный для удерживания как первого, так и второго контейнеров; причем первый и второй контейнеры представлены в форме ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, АКТИВНАЯ В ОТНОШЕНИИ РЕЦЕПТОРА КАЛЬЦИЯ, СПОСОБ ЛЕЧЕНИЯ ПАЦИЕНТА, СПОСОБ АНАЛИЗА СОЕДИНЕНИЯ ОКАЗЫВАТЬ ВЛИЯНИЕ НА АКТИВНОСТЬ РЕЦЕПТОРА НЕОРГАНИЧЕСКОГО ИОНА, НУКЛЕИНОВАЯ КИСЛОТА, КОДИРУЮЩАЯ РЕЦЕПТОР, РЕЦЕПТОР КАЛЬЦИЯ

Изобретение относится к медицине, точнее препаратам и способам лечения и исследования, связанным с рецепторами кальция и др. неорганических ионов. Предпочтительно молекула способна воздействовать как селективный агонист или антагонист на Са+2-рецептор одной или более, но не всех клеток, выбранных из группы, состоящей из паратироидных клеток, костных остеокластов, окологломерулярных почечных клеток, проксимальных канальцевых почечных клеток, периферических канальцевых почечных клеток, клеток толстой восходящей ветви петли Хенля и/или собирающей протоки, кератиноцита в эпидермисе, парафолликулярной клетки в тироиде (С-клеток), интестинальных клеток, трофобласта в плаценте, тромбоцита, клетки сосудов гладкой мышцы, клетки сердечного предсердия, клеток, секретирующих гастрин и глюкагон, почечной, мезангиальной клетки и клетки грудной железы. Изобретение расширяет арсенал средств, способных блокировать активность внеклеточных ионов кальция, при различных патологиях. 6 с. и. 50 з.п. ф-лы, 47 ...

ИНГИБИТОРЫ КИНУРЕНИН 3-ГИДРОКСИЛАЗЫ ДЛЯ ЛЕЧЕНИЯ ДИАБЕТА

... 1. Применение, по крайней мере, одного соединения, которое ингибирует кинуренин 3-гидроксилазу для получения лекарственного средства для профилактики и/или лечения диабета и его осложнений путем ингибирования кинуренин 3-гидроксилазы. 2. Применение по п.1, отличающееся тем, что лекарственное средство предназначено для профилактики и/или лечения инсулинонезависимого диабета и его осложнений. 3. Применение по п.1 или 2, отличающееся тем, что соединение соответствует общей формуле (I) или общей формуле (II) где W представляет собой двухвалентный радикал, выбранный из следующих радикалов: R1представляет собой радикал, выбранный из линейной или разветвленной алкильной группы, которая содержит от 1 до 14 атомов углерода, и является необязательно замещенной, алкенил, алкинил, циклоалкил, циклоалкенил, гетероциклический радикал, арилрадикал и гетероарилрадикал; R2выбран из группы, которая включает водород, атом галогена, гидроксил, тиол, карбоксил, алкил, алкенил, алкинил, алкокси, алкилтио, алкилкарбонил ...

ДОПОЛНЯЮЩИЕ ПЕРСОНАЛЬНЫЕ СМАЗЫВАЮЩИЕ КОМПОЗИЦИИ

... 1. Система доставки для доставки первой и второй композиций, составленных для применения к различным индивидуумам и для взаимодействия друг с другом при физическом взаимодействии индивидуумов друг с другом, причем указанная система доставки содержит: ! первый контейнер, содержащий первую композицию; и ! второй контейнер, содержащий вторую композицию, составленную для взаимодействия с первой композицией, когда первая и вторая композиции нанесены на участки нанесения первого и второго индивидуумов соответственно, а участки нанесения контактируют друг с другом; ! где указанные первый и второй контейнеры связаны друг с другом, по меньшей мере, одним из факторов: цветом, формой или физическим соединением для указания индивидуумам, что контейнеры предназначены к использованию в сочетании друг с другом. ! 2. Система доставки по п.1, где указанные первый и второй контейнеры имеют, по существу, одну и ту же форму. ! 3. Система доставки по п.2, где указанные первый и второй контейнеры имеют различный ...

СТАБИЛЬНАЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ОСНОВЕ ПРАВАСТАТИНА

... 1. Фармацевтическая композиция, которая является стабильной и подходит для перорального введения, включающая эффективное количество правастатина или его фармацевтически приемлемых солей и носитель, причем указанный носитель включает по меньшей мере один разбавитель и по меньшей мере одно смазывающее вещество для придания водной дисперсии указанной композиции значения рН между 6,5 и 8,5. 2. Фармацевтическая композиция по п. 1, отличающаяся тем, что разбавителем может быть водорастворимый разбавитель, диспергируемый в воде разбавитель или их смеси. 3. Фармацевтическая композиция по п. 2, отличающаяся тем, что водорастворимый разбавитель выбирают из группы, состоящей из карбоната кальция, фосфата кальция, гидрофосфата кальция, трехосновного фосфата кальция, сульфата кальция, сгущаемого сахара, лактозы, сахарозы, сорбита, маннита, декстранов, декстрина, декстрозы, мальтодекстрина и их смесей. 4. Фармацевтическая композиция по п. 2, отличающаяся тем, что диспергируемый в воде разбавитель выбирают ...

ИММУНОПОТЕНЦИИРУЮЩИЕ АГЕНТЫ, СПОСОБЫ ЛЕЧЕНИЯ ИММУНОДЕФИЦИТНЫХ МЛЕКОПИТАЮЩИХ, А ТАКЖЕ ВИРУСНЫХ ИНФЕКЦИЙ И РАКА У МЛЕКОПИТАЮЩИХ

Изобретение относится к использованию класса соединений в качестве иммунопотенциаторов, композициям, содержащим такие соединения, и к их получению, сочетаниям этих соединений с противоопухолевыми и противоинфекционными лекарствами и к применению этих сочетаний при профилактике или лечении таких заболеваний, которые связаны с опухолями или заражениями.

КОМПЛЕКС ТАННАТА СИТАГЛИПТИНА

УЗКО ПОЛИ- И МОНОДИСПЕРСНЫЙ ВОДОРАСТВОРИМЫЙ ОЛИГОМЕР, ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ, СПОСОБ ПОЛУЧЕНИЯ ОЛИГОМЕРА, СПОСОБ ДИАГНОСТИКИ И/ИЛИ ЛЕЧЕНИЯ ВИРУСНЫХ ИНФЕКЦИЙ

Узко поли- и монодисперсные олигомеры настоящего изобретения являются полимочевинами, поликарбонатами, полиэфирами или полиамидами, имеющими довторность единицы от 3 до 50. Эти олигомеры являются водорастворимыми, предпочтительно имеют жесткий каркас, имеют повторяющиеся единицы, соединенные карбонильными связывающими составляющими, которые обладают анионными группами, проявляют преимущественно линейную геометрию, так что в водной среде между анионными группами существуют постоянные расстояния, и являются фармацевтически приемлемыми. Узко поли- и монодисперсные олигомеры применимы для лечения и/или диагностики СПИД и/или КСС или HSV инфекций.

ПЕРОРАЛЬНО ВВОДИМАЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ДЛЯ ЛЕЧЕНИЯ СИНДРОМА РАЗДРАЖЕННОГО КИШЕЧНИКА, СОДЕРЖАЩАЯ РЕГУЛЯТОР ПЕРИСТАЛЬТИКИ КИШЕЧНИКА, СРЕДСТВО, КОТОРОЕ ПРЕДОТВРАЩАЕТ ЗАДЕРЖКУ ГАЗОВ, И ПИЩЕВАРИТЕЛЬНЫЕ ФЕРМЕНТЫ, И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

... 1. Фармацевтическая композиция или состав, адаптированный для перорального введения, в форме таблетки, покрытой оболочкой таблетки или капсулы для предотвращения или лечения кишечных нарушений, где состав состоит из регулятора перистальтики кишечника, средства, которое предотвращает задержку газов, пищеварительного фермента, связующего средства, разбавителя, абсорбирующего средства, дезинтегрирующего средства, смазывающего средства и средства, способствующего скольжению.2. Фармацевтический состав по п. 1, где регулятор перистальтики кишечника выбран из группы, которая состоит из тримебутина, феноверина, мебеверина, дицикловерина, этилбромида, алосетрона, тегасерода, лоперамида, флороглюцинола, триметилфлороглюцинола, бутилскополамина и паргеверина.3. Фармацевтический состав по п.2, где регулятор перистальтики кишечника представляет собой тримебутин и его фармацевтически приемлемые соли.4. Фармацевтический состав по п.2, где регулятор перистальтики кишечника представляет собой феноверин ...

КОМПОЗИЦИИ И СПОСОБЫ ПРИМЕНЕНИЯ ФОРБОЛОВЫХ СЛОЖНЫХ ЭФИРОВ

СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ МЕТАБОЛИЧЕСКИХ ЗАБОЛЕВАНИЙ

... 1. Соединение формулы ! ! где m равно 1; n равно 1 или 2; t равно 0 или 1; и A представляет собой фенил, замещенный 2 группами, выбранными из галогена, алкила, содержащего 1 или 2 атома углерода, перфторметила и перфторметокси. ! 2. Соединение формулы ! ! где m равно 1; n равно 1 или 2; t равно 0 или 1; и A представляет собой фенил, замещенный 2 группами, выбранными из: галогена, алкила, содержащего 1 или 2 атома углерода, перфторметила и перфторметокси.

ПОЛИМОРФЫ 4-[2-ДИМЕТИЛАМИНО-1-(1-ГИДРОКСИЦИКЛОГЕКСИЛ)ЭТИЛ]ФЕНИЛ 4-МЕТИЛБЕНЗОАТА ГИДРОХЛОРИДА, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ИСПОЛЬЗОВАНИЕ

... 1. Кристаллическая форма II [4-[2-диметиламино-1-(1-гидроксициклогексил)этил]фенил 4-метилбензоата гидрохлорида], характеризующаяся, по меньшей мере, одной из следующих характеристик:порошковой рентгенограммой, полученной с использованием излучения CuKи с характерными пиками при углах 2θ (±0.2°): 5.899°, 11.799°, 14.481°, 15.440°, 18.420°, 19.800° и 23.620°, или 5.899°, 11.799°, 13.779°, 14.481°, 15.039°, 15.440°, 17.701°, 18.420°, 19.800°, 23.620° и 25.220°, или 5.899°, 10.280°, 11.799°, 13.779°, 14.481°, 15.039°, 15.440°, 15.920°, 16.901°, 17.701°, 17.900°, 18.420°, 19.800°, 20.679°, 20.938°, 21.819°, 22.761°, 23.242°, 23.620°, 24.799°, 25.220°, 26.001°, 26.440°, 26.717°, 27.241°, 27.780°, 28.160°, 28.719°, 29.279°, 29.796°, 30.604°, 31.340°, 31.723°, 31.901°, 32.425°, 32.939°, 33.880°, 34.282°, 34.460°, 35.141°, 36.400°, 37.225°, 38.377° и 39.501° или как показано на фиг.3;точкой плавления 209.5-210.2°С;спектром ДСК как показано на фиг.4.2. Способ получения кристаллической формы II, ...

Композиция для повышения качества спермы у субъекта мужского пола

3-АЦИЛИНГЕНОЛЫ II

... 1. Соединение общей формулы Iгде R представляет собой арил, замещенный одним или несколькими заместителями, независимо выбранными из R3;или R представляет собой (С-C)-циклоалкил, (С-C)-циклоалкенил или (С-C)-циклоалкинил, каждый из которых может быть необязательно замещен одним или несколькими заместителями, независимо выбранными из R4;R3 представляет собой галоген, циано, гидроксил;или R3 представляет собой (С-С)-алкил, (С-С)-алкенил, (С-С)-алкинил, (С-С)-циклоалкил, гетероциклоалкил, арил, гетероарил, каждый из которых может быть необязательно замещен одним или несколькими заместителями, независимо выбранными из R5;или R3 представляет собой -NRaCORb, -CONRaRb, -COORc, -OCORa,-ORa, -OCONRaRb, -NRaCOORb, -NRaCONRaRb, -NRaSONRaRb, -NRaSORb, -SONRaRb, -SORa, -S(О)Ra, -SRa или -NRdRe;R5 представляет собой галоген, циано, гидрокси, (С-С)-алкил, галоген(С-С)-алкилили R5 представляет собой -NRaCORb, -COORc, -OCORa, -CONRaRb, -OCONRaRb, -NRaCOORb, -NRaCONRaRb, -NRaSONRaRb, -NRaSORb,-SONRaRb, - ...

КОМПОЗИЦИИ И СПОСОБЫ ПРИМЕНЕНИЯ ФОРБОЛОВЫХ ЭФИРОВ ДЛЯ ЛЕЧЕНИЯ ИНСУЛЬТА

... 1. Способ профилактики или лечения одного или более последствий инсульта у млекопитающего, включающий введение эффективного количества форболового эфира формулы I или его фармацевтически приемлемой соли, изомера или энантиомера указанному млекопитающему,где Rи Rвыбраны из группы, состоящей из водорода, гидроксила,и их замещенных производных; и Rявляется водородом,и их замещенными производными.2. Способ по п. 1, где Rили Rявляетсяа оставшийся из Rили Rявляетсяи Rявляется водородом.3. Способ по п. 1, где форболовый эфир является форбол 13-бутиратом, форбол 12-деканоатом, форбол 13-деканоатом, форбол 12,13-диацетатом, форбол 13,20-диацетатом, форбол 12,13-дибензоатом, форбол 12,13-дибутиратом, форбол 12,13-дидеканоатом, форбол 12,13-дигексаноатом, форбол 12,13-дипропионатом, форбол 12-миристатом, форбол 13-миристатом, форбол 12,13,20-триацетатом, 12-дезоксифорбол 13-ангелатом, 12-дезоксифорбол 13-ангелат 20-ацетатом, 12-дезоксифорбол 13-изобутиратом, 12-дезоксифорбол 13-изобутират-20-ацетатом ...

Способ получения гидрохлорида 1,3-бис-(диметиламино)-2-пропил-4-хлорфеноксиацетата

Изобретение касается ариловых эфиров и, в частности, получения гидрохлорида 1,З-бис-(диметиламино)- -2-пропил-4-хлорфеноксиацетата (ГХ), который обладает нейроэнергетической активностью. Цель - разработка способа получения новых, более активных соединений. Получение ГХ ведут взаимодействием производного 4-хлорД)е- ноксй-уксусной кислоты формулы CICH ...

VERBINDUNGEN ZUR BEHANDLUNG VON ERKRANKUNGEN,DIE MIT DES VASCULOGENESE UND/ODER ANGIOGENESE IN VERBUNDEN STEHEN.

Artikel für die weibliche Hygiene mit antifibrinolytischem oder hämostatischem Wirkstoff und pharmazeutische Zusammensetzung

Mit Arzneimittel versehener Artikel für die weibliche Hygiene, umfassend eine therapeutisch wirksame Menge eines antifibrinolytischen oder hämostatischen Wirkstoffs zur Reduktion von Menstruationsblutverlust.

METHODEN ZUR HEMMUNG DER AKTIVITÄT DER OSTEOKLASTEN

ANTIVIRALE VERWENDUNG EINER IN POSITION-4 SUBSTITUIERTEN 2,6-DI-T-BUTYLPHENOLVERBINDUNG, BESONDERS GEGEN HERPES- UND PAPILLOMAVIREN

Microbially stable cosmetic or dermatological light-protective skin care preparations, containing taurine and paraben, sorbic acid or (3-iodo-2-propynyl) N-butylcarbamate

New cosmetic or dermatological preparations (I) contain (A) taurine and (B) a paraben, sorbic acid (or its alkali metal salt) or (3-iodo-2-propynyl) N-butylcarbamate (IPBC).

Pharmaceutical composition for in situ treatment of inflammatory and infective injuries at all positions comprises antibiotics, antifungal antibiotic in saccharose, and optionally dexamethasone, starch, preservative and filler

A pharmaceutical composition comprises at least an antibiotic, antifungal antibiotic in saccharose, optionally in combination with dexamethasone, starch, preservative, and filler for keeping pH stable at injuries. ACTIVITY : Antiinflammatory; Vulnerary; Antibacterial; Fungicide.

POLYCYCLISCHE DIANTHRACHINONE ALS ANTIKREBSMITTEL UND ANTIANGIOGENESEMITTEL

EIN KRÄUTERMOLEKÜL ALS POTENTIELLES ANTI-LEUKÄMISCHES ARZNEIMITTEL

ZUSAMMENSETZUNGEN ZUR MODULIERUNG DER SCHLEIMSEKRETION

STABILE EMULSIONSZUBEREITUNGEN

Neuropeptid Y Antagonisten

Verfahren zur Herstellung von in 5-Stellung substituierten 2-(N, N-Dialkyl- bzw. N-Alkyl-N-alkoxy-carbamoyl-methoxy)-benzoesaeureestern

ANTIDIABETISCHE MITTEL

MEDIZINISCHE ZUSAMMENSETZUNG ZUR BEHANDLUNG VON INFEKTIONEN MIT ARZNEIMITTELRESISTENTEM STAPHYLOCOCCUS AUREUS

Therapeutic agents

Drug composition and its use in therapy

Prodrugs

Styrax benzoin rejuvenating cosmetic preparation

INJECTABLE LOCAL ANAESTHETIC

... 1360820 An injectable local anaesthetic ESPE FABRIK PHARMAZEUTISCHER PRAPARATE GmbH 19 Nov 1971 [20 Nov 1970] 53795/71 Heading A5B Injectable local anaesthetics contain in aqueous solution a local anaesthetic active agent, a vasoconstrictor, and as a beta-receptor blocking agent, 3-t-butylamino-1-(6'-chloro-3'- methyl-phenoxy)-propan-2-ol in the form of a physiologically acceptable salt such as the hydrochloride, tartrate or lactate. The solution preferably contains 0.2 to 4% by weight of the local anaesthetic, 10 to 100 p.p.m. of the vasoconstrictor and at least 50 p.p.m. of the beta receptor blocking agent. The local anaesthetic active agent may be procaine, #-diethylamino-2,6-dimethyl-acetanilide (lidocaine), #- butyl amino-2-methyl-6-ohloro-acetanilide, rac. N - methyl - hexahydropicolinyl - 2,6 - di methyl - anilide, 3 - methyl - 2 - (diethylamino)- acetylamino benzoic acid methyl ester and/or -(n - propylamino) - propionic acid - (2 - methyl - anilide) (Prilocaine) in free base or ...

Improved use of ß2-bronchodilator drugs

COMPOSITIONS FOR TREATING GLAUCOMA

The use of serine protease inhibitors

Wound-healing promoters containing polyprenyl derivatives

Compounds of formula (I): (I) (wherein: R1 represents a hydroxy group, a C1-C8 alkoxy group, an aliphatic acyloxy group, a benzoyloxy group or a cinnamoyloxy group; p1 R2 represents a hydrogen atom, a C1-C8 alkyl group, an aliphatic acyl group, a benzoyl group or a cinnamoyl group; and n represents an integer from 1 to 3) when applied topically have been found to promote wound-healing and exuberant granulation; they are preferably formulated with a pharmaceutical topical base.

LOUSE REPELLENT COMPOSITIONS

Antagonists of prostaglandin D2 receptors

1,8-DIACYLOXY-10-ACYLANTHRONES

Substituted benzaldehyde compounds and methods fortheir use in increasing tissue oxygenation

Narrow poly- and mono-dispersed anionic oligomers, and their uses formulations and process.

The narroe poly- or mono dispersed oligomers of the present invention are polyureas, polycarbonates, polyesters or polyamides having a recurring unit of from 3 to 50. These oligomers are water-soluble, preferably have a rigid backbone, have recurring units coupled by carbonyl linking moieties which have anionic groups, display predominantly linear geometry such that regular spacing between anionic groups exists in an aqueous medium, and are pharmaceutically-acceptable. The narrow poly- or mono-dispersed oligomers are useful for the treatment and/or diagnosis of aids and/or arc or hsv.

Substituted benzaldehyde compounds and methods fortheir use in increasing tissue oxygenation

NARROW POLY-AND MONO-DISPERSED ANIONIC OLIGOMERS AND THEIR USES,FORMULATIONS AND PROCESS

Substituted benzaldehyde compounds and methods fortheir use in increasing tissue oxygenation

Method of preparation of new secondary amines and tertiary sectors carrying a group benzonyloxylic.

Aids prophylactic lubricating composition and devices for its use

Narrow poly- and mono-dispersed anionic oligomers and their uses formulations and process

NARROW POLY-AND MONO-DISPERSED ANIONIC OLIGOMERS AND THEIR USES,FORMULATIONS AND PROCESS

PHARMAZEUTISCHES PRÄPARAT IN FORM VON TABLETTEN AUF DER BASIS VON TRIMEBUTIN MIT VERLÄNGERTER WIRKSTOFFFREISETZUNG UND VERFAHREN ZU DEREN HERSTELLUNG

ORAL, PHARMACEUTICAL DARREICHUNGSFORMEN OF LIQUID MEDICINES OF MITVERBESSERTER BIO-AVAILABILITY

VERFAHREN ZUR HERSTELLUNG VON NEUEN HYDOXYAMINOESTERN

aTOMIZATION DEVICE FOR USE IN THE iNHALATION THERAPY

PROCEDURE FOR THE PRODUCTION STABLE THYMOSINFRAKTION 5

PROCEDURE FOR the PRODUCTION OF NEW ONE 1-BENZOYLOXYPHENYL-2-AMINOATHANOLEN (1)

PROCEDURE FOR the PRODUCTION OF NEW ONE 2-AMINO-3 (HALOGENBENZOYL) - METHYLPHENYLESSIGSAEUREDERIVATEN AND FROM PHAMRAZEUTI PREPARATIONS, WHICH THIS CONTAINING

MEDICAL COMPOSITION FOR THE TREATMENT OF INFECTIONS WITH DRUG-RESISTANT STAPHYLOCOCCUS AUREUS

COMPOSITIONS FOR THE INHIBITION OF THE PROTEIN KINASE C ALPHA FOR THE TREATMENT OF DIABETES MELLITUS

TUCARESOL AS MEANS TO IMMUNOPOTENTIERUNG

ANTI-INFLAMMATORY MEANS.

POLYETHYLENGLYKOL- UND KONSERVIERUNGSMITTEL- AUFWEISENDE ELEKTROLYTLÖSUNGEN

A solution in mater comprises N x (70 to 130) g/L polyethylene glycol (PEG) having an average molecular weight of 2500 to 4500; N x (1.6 to 4.0) g/L sodium chloride; N x (0.2 to 0.6) g/L potassium chloride; N x (0.6 to 2.2) g/L sodium bicarbonate; and N x an amount of preservative where N is in the range 2 to 8. Preferably, the preservative is selected from the group including sodium propyl paraben, methyl paraben, ethyl paraben, propyl paraben, benzyl alcohol, phenoxyethanol, propylene glycol, glyceryl triacetate and blends of two or more thereof and is preferably present in an amount of N x (0.3 to 1.4) g/L. The formulation may optionally include N x (0.02 to 0.2) g/L sweeteners including acesulfame and/or sucralose and N x (0.2 to 2) g/L flavourings. The solution is a concentrate for dilution and is diluted N-fold with water to provide a solution for use in the treatment of constipation or faecal impaction. Also outlined are solutions, kits and unit doses comprising the formulation, ...

PHARMACEUTICAL PREPARATIONS, THE ESTERS OR AMIDES AS ACTIVE SUBSTANCES CONTAINING.

TETRALIN ESTER OF PHENOLEN OR BENZOIC ACIDS WITH RETINOIDAEHNLICHER ACTIVITY.

COMPLEX CONNECTIONS, ON CYCLODEXTRINENBASIEREND.

COMPOSITION FOR TREATMENT OF MALIGNANT TUMORE AND YOUR METASTASE

LOUSE-REJECTING COMPOSITIONS

ANTIDIABETI MEANS

NEUROPEPTID Y ANTAGONIST

PREPARATION AND USE OF RSR ANTAGONIST FOR DEMAND THE CHONDROGENESE

USE FROM BENZONAPHTALENE DERIVATIVES TO THE PRODUCTION OF A DRUG FOR THE TREATMENT OF DISEASES OF THE NERVOUS SYSTEM

Compounds for the treatment of acute brain injury

The invention relates to a compound according to formula I wherein when R ...

NOVEL COMPOUND CONTAINED IN MANUKA HONEY AND USE OF SAME

The present description discloses a novel biologically active ingredient of manuka honey. Specially, the present description discloses a compound represented by the following formula. In this formula, each of R 1, R2 and R3 independently represents a hydrogen atom or optionally substituted C 1 .4 alkyl group, m represents an integer from 1 to 3, each of R4-m, R-m and R6-m independently represents a hydrogen atom or optionally substituted C1-4 alkyl group, and each of R7, R8, R9 and Rio independently represents a hydrogen atom or optionally substituted C1 .4 alkyl group. [C7] i OR7 CH2 R R 5-mR OR4-m 0 ...

Methods of assessing and treating hepatic encephalopathy

The present disclosure relates to methods of treating or ameliorating hepatic encephalopathy (HE), including assessing the severity of HE in a patient suffering from HE, or the determining the presence or occurrence of an overt hepatic encephalopathy (OHE) event. In particular, some aspects of the methods use a novel Hepatic Encephalopathy Staging Tool (HEST), which includes a set of criteria to categorize the HE into different stages and provide guidance on effective treatments based on the severity of the HE. Other aspects of the methods use an Overt Hepatic Encephalopathy Screening Tool (O-HEST) to determine whether an OHE event is occurring or has occurred and provide guidance on proper medical attention and change in treatment.

Anti-Bacterial Siderophore-Aminopenicillin Conjugates

NIH 0 NH HN 0 N N I. Amid linkage H Hu- R R R 1l. Unsubstituted metal binding enterobachn I triscatecholate sideropohre 2 (R= H or Ac) oran Trarsaportdiated Dug D9eivery C IiV ~)OI~t dd(~II~ Am#001Ad snd AmaxkUiln Affdn~p@WrIJIn Cooqiupaieo Ahfi'psuadomomi V10,f 00 MRl And-psadimww KMCm4O54JO p Figure 1 An artificial tris-catecolate siderophore with a tripodal backbone and its conjugates with ampicillin and amoxicillin were synthesized. Both conjugates exhibited significantly enhanced in vitro antibacterial activities against Gram-negative species compared to the parent drugs, especially against P. aeruginosa. The conjugates appear to be assimilated by an induced bacterial iron transport process as their activities were inversely related to iron concentration. The easily synthesized tris catecolate siderophores can be used with a variety of drugs as conjugates to target antibiotic-resistant Gram-negative bacteria.

AMINOTETRALIN COMPOSITIONS FOR TREATING GLAUCOMA

ANTIMICROBIAL COMPOSITIONS CONTAINING BENZOIC ACID DERIVATIVES AND USE AS DISINFECTANTS AND PRESERVATIVES

COMPOSITIONS FOR TREATING GLAUCOMA

TREATING AGENT FOR OSTEOARTHRITIS

TREATING AGENT FOR OSTEOARTHRITIS

Treatment of cardiac abnormalities with aryloxy propanolamines

Proteasome inhibitors and uses thereof

The invention relates to methods and compositions for inhibiting proteasome activity using cinnamate compounds. These cinnamate compounds can be formulated for topical or systemic use for skin disorders such as psoriasis.

Compounds for the treatment of metabolic disorders

Using selective antagonists of persistent sodium current to treat neurological disorders and pain

Antiviral compounds and method of treating viral infections

Pharmaceutical combinations including anti-inflammatory and antioxidant conjugates useful for treating metabolic disorders

One aspect of the present invention is a pharmaceutical combination comprising (a) an anti-inflammatory agent/anti-oxidant agent conjugate; and (b) an insulin secretogogue, an insulin sensitizer, an alpha-glucosidase inhibitor, a peptide analog, or a combination thereof. Another aspect of the invention relates to methods of treating metabolic disorders with such conjugates.

Theobromine in combination with an expectorant or a mucolytic for use in therapy

An agent comprises theobromine and an expectorant, or an agent comprises theobromine and a mucolytic. The agents of the invention may be used as a combined preparation for simultaneous, sequential or separate use in the therapy of cough.

Complementary personal lubricant compositions

This invention relates to novel compositions and methods of use by which the compositions of this invention are applied topically to one or more body parts of at least two individuals who bring said body parts into contact with the other individual and, when said body parts come into contact with each other, permit the formulations to interact and thereby achieve an unexpected sensation to each individual. Also disclosed is a delivery system for said compositions, consisting of two containers (100) associated with each other, and preferably a holder (200, 300) for said containers.

Metallo-beta-lactamase inhibitors

A new metallo-β-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of β-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-β-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of β-lactam antibiotics against metallo-β-lactamase producing bacteria by combining the compound of the general formula (I) with β-lactam antibiotics.

Methods for treating inflammation

The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands.

Topical pharmaceutical formulations containing a low concentration of benzoyl peroxide in suspension in water and a water-miscible organic solvent

An aqueous formulation for topical application to the skin comprising water, a water-miscible organic solvent, and benzoyl peroxide, wherein the concentration of the organic solvent is sufficient to provide a stable suspension of benzoyl peroxide in the aqueous formulation without the inclusion of a surfactant in the formulation, wherein the ratio of concentrations of water and organic solvent in the formulation is sufficient to maintain the benzoyl peroxide in saturated solubility in the formulation following, application to the skin, and wherein the concentration of benzoyl peroxide in the formulation is less than 5.0% and at least 1.0% w/w. The formulation may further contain a chemical compound in addition to benzoyl peroxide that is effective in the treatment of acne. The aqueous formulations of the invention are useful in the treatment of acne and acne rosacea.

Anti-Viral Compounds

Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.

CHEMICAL AGENTS FOR THE PREVENTION OF INHIBITION OR TUMOR METASTASIS

The present invention provides methods of preventing or inhibiting tumor metastasis in a subject by administering a therapeutically effective amount of (1) a compound from a group of enumerated compounds, or a pharmaceutically acceptable salt thereof; (2) an agent that covalently modifies at least one cysteine residue of S100A4 protein; or (3) an agent that inhibits the interaction between S100A4 and myosin-IIA. 2. The method of claim 1 , wherein the compound is the compound of formula (I).5. The method of claim 1 , wherein the compound is the compound of formula (III).8. The method of claim 1 , wherein the compound comprises 2 claim 1 ,3-dihydrobenzo[g][1 claim 1 ,4]benzodithiine-5 claim 1 ,10-dione claim 1 , 2 claim 1 ,3-bis(2-hydroxyethylsulfanyl)naphthalene-1 claim 1 ,4-dione claim 1 , 2-(2-hydroxyethylsulfanyl)naphthalene-1 claim 1 ,4-dione claim 1 , 3-(1 claim 1 ,4-dioxonaphthalen-2-yl)sulfanylpropanoic acid claim 1 , 2-ethylsulfanylnaphthalene-1 claim 1 ,4-dione claim 1 , 4 claim 1 ,11-diaminonaphtho[2 claim 1 ,3-f]isoindole-1 claim 1 ,3 claim 1 ,5 claim 1 ,10-tetrone claim 1 , 2-(3-methyl-1 claim 1 ,4-dioxonaphthalen-2-yl)sulfanylacetic acid claim 1 , 2-butylsulfanylnaphthalene-1 claim 1 ,4-dione claim 1 , 2-ethylsulfanyl-3-methylnaphthalene-1 claim 1 ,4-dione claim 1 , 2-(2-hydroxyethylsulfanyl)-3-methylnaphthalene-1 claim 1 ,4-dione claim 1 , 2-methyl-3-methylsulfanylnaphthalene-1 claim 1 ,4-dione claim 1 , (1 claim 1 ,4-dioxonaphthalen-2-yl) 4-methylbenzoate claim 1 , N-[3-(4-chlorophenyl)sulfanyl-1 claim 1 ,4-dioxonaphthalen-2-yl]acetamide claim 1 , 2-benzylsulfanyl-3-methylnaphthalene-1 claim 1 ,4-dione claim 1 , N-(3-chloro-1 claim 1 ,4-dioxonaphthalen-2-yl)-N-(4-fluorophenyl)acetamide claim 1 , 2-methylquinoline-5 claim 1 ,8-dione claim 1 , N-(7-chloro-5 claim 1 ,8-dioxoquinolin-6-yl)acetamide claim 1 , 6-amino-7-chloroquinoline-5 claim 1 ,8-dione claim 1 , 7-amino-6-methoxyquinoline-5 claim 1 ,8-dione claim 1 , 6 claim 1 ,7-dichloroquinoline-5 claim ...

Cyclohexylamines

The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.

METHODS AND USES OF NUR77 AND NUR77 AGONISTS TO MODULATE MACROPHAGES AND MONOCYTES, AND TREAT INFLAMMATION, INFLAMMATORY DISEASE AND CARDIOVASCULAR DISEASE

Methods of decreasing, reducing, inhibiting, suppressing, limiting or controlling an undesirable or aberrant immune response, immune disorder, inflammatory response, or inflammation in a subject; decreasing, reducing, inhibiting, suppressing, limiting or controlling an autoimmune response, disorder or disease in a subject; and decreasing, reducing, inhibiting, suppressing, limiting or controlling an adverse cardiovascular event or cardiovascular disease in a subject, are provided. Methods include, for example, administering a Nur77 polypeptide or subsequence thereof, a Nur77 agonist, or CD14CD16monocytes or CD14CD16(CD115CD11bGR1 (Ly6C−)) monocytes or macrophages to a subject to decrease, reduce, inhibit, suppress, limit or control the underlying condition or an adverse symptom or pathology of the condition. 1. A method of decreasing , reducing , inhibiting , suppressing , limiting or controlling an undesirable or aberrant immune response , immune disorder , inflammatory response , inflammation autoimmune response , autoimmune disease , adverse cardiovascular event or cardiovascular disease in a subject , comprising administering a Nur77 polypeptide or subsequence thereof , a Nur77 agonist , or CD14CD16 monocytes and/or CD14CD16(CD115CD11bGR1 (Ly6C−)) monocytes or macrophages to a subject in an amount to decrease , reduce , inhibit , suppress , limit or control the undesirable or aberrant immune response , immune disorder , inflammatory response , inflammation , autoimmune response , autoimmune disease , adverse cardiovascular event or cardiovascular disease in the subject.23-. (canceled)4. The method of claim 1 , wherein the adverse cardiovascular event or cardiovascular disease comprises coronary artery or heart disease claim 1 , atherosclerosis claim 1 , peripheral artery disease claim 1 , cerebrovascular disease claim 1 , renal artery disease claim 1 , stroke claim 1 , myocardial infarction (heart attack) claim 1 , ischemic heart failure claim 1 , transient ...

ALLOSTERIC BINDING COMPOUNDS

The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds. 2. The method according to claim 1 , comprising administering the compound of formula (I) wherein A is an aryl ring.35.-. (canceled)6. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 6-membered cycloalkyl claim 1 , aryl claim 1 , or heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.78.-. (canceled)9. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein B is a 5-membered heteroaryl ring claim 1 , which ring together with A forms an annulated ring system.1011.-. (canceled)14. (canceled)15. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Lis selected from the group consisting of —O— claim 1 , —NH— claim 1 , and —NR—.16. The method according to claim 15 , wherein Ris Calkyl.17. The method according to claim 16 , wherein Ris selected from the group consisting of methyl claim 16 , ethyl claim 16 , propyl claim 16 , isopropyl claim 16 , butyl claim 16 , iso-butyl claim 16 , sec-butyl claim 16 , and tert-butyl.1821.-. (canceled)22. The method according to claim 1 , comprising administering the compound of formula (I) claim 1 , wherein Ris selected from the group consisting of Calkyl claim 1 , Calkoxy claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , and —NH—Calkyl claim 1 , where any of these optionally is substituted with one or more substituents.23. (canceled)24. The method according to claim 22 , wherein Ris Calkyl claim 22 , wherein the alkyl optionally is substituted with one or more substituents.2527.-. (canceled)29. The method according to claim 28 , wherein Lis selected from the group consisting of —O— and —S—.3038.-. (canceled)39. The method ...

Topical pharmaceutical composition comprising flurbiprofen

The invention provides topical pharmaceutical compositions comprising flurbiprofen, or a pharmaceutically acceptable derivative thereof, in combination with a solubilising system which comprises at least one glycol ether and at least one glycol ester. These are suitable for treating any condition associated with pain, inflammation and/or stiffness, for example sub-dermal pain in the joints or soft tissue.

Sympathetic inhibitor, and cosmetic composition, food, and sundry article containing the same

Disclosed are a sympathetic inhibitor allowing more effective inhibition of activity of a sympathetic nerve, as well as a cosmetic composition, a food, and a sundry article containing the same. Ethyl 4-methoxybenzoate is efficacious for quieting down the activity of the sympathetic nerve. The sympathetic inhibitor, the cosmetic composition, the food and the sundry article containing the same enable more effective inhibition of the activity of the sympathetic nerve.

Pharmaceutical Compositions Containing Diacerein

A once-daily controlled-release formulation of diacerein for treating inflammatory or autoimmune diseases or their complications, with reduced adverse side effects and methods of treating such diseases are disclosed. 1. A once-daily controlled-release formulation of diacerein for treating inflammatory diseases , autoimmune diseases or their complications with reduced adverse side effects , comprising an active layer , a sustained-release film layer , and a delayed-release film layer , wherein said sustained-release film layer comprises an ethyl cellulose polymer , povidone , triethyl citrate and talc , and wherein said delayed-release film layer comprises an Eudragit® polymer , triethyl citrate and talc.2. The controlled-release formulation according to claim 1 , wherein the formulation is a membrane-controlled formulation claim 1 , matrix formulation or osmotic pump formulation.3. The controlled-release formulation according to claim 1 , wherein the formulation comprises a surfactant claim 1 , acidifying agent or a buffering agent.4. The controlled-release formulation according to claim 1 , wherein the particle size of diacerein is less than 2000 μm.5. The controlled-release formulation according to claim 1 , wherein the diacerein is presented as an amorphous state in a solid carrier.6. The controlled-release formulation according to claim 1 , wherein the diacerein is formed as a complex with cyclodextrins.7. The controlled-release formulation according to claim 1 , wherein the diacerein is crystalline.8. The controlled release formulation according to wherein a formulation containing 50 mg diacerein maintains the plasma concentration of rhein above the concentration of 1 mg/L for more than 12 hours in humans claim 1 , when orally administered to a human patient who has reached the steady state condition9. The controlled release formulation according to wherein a formulation containing 100 mg diacerein maintains the plasma concentration of rhein above the ...

METHOD FOR PREVENTION OR TREATMENT OF DEGENERATIVE NEUROLOGIAL BRAIN DISORDERS

The present invention relates to a method for the prevention or treatment of degenerative neurological brain disorders and, more specifically, relates to a method for the prevention or treatment of degenerative neurological brain disorders, such as Parkinson's disease, Alzheimer's dementia (senile dementia), stroke, Lou Gehrig's disease, Pick's disease, Creutzfeldt-Jakob disease, Huntington's disease, progressive supranuclear palsy, spinocerebellar degeneration, cerebellar atrophy, multiple sclerosis, post-traumatic stress disorder, and amnesia. The method includes administering to a subject in need thereof a therapeutically effective amount of a composition, wherein the composition contains a paraben compound as an active ingredient having effects that are useful in combating oxidation to remove active oxygen, suppressing cell-death, improving impaired movement, and enhancing declining memory. 2. The method according to claim 1 , wherein the compound represented by Formula 1 is at least one selected from a group consisting of methylparaben claim 1 , ethylparaben claim 1 , propylparaben claim 1 , butylparaben claim 1 , isopropylparaben claim 1 , and isobutylparaben.3. The method according to claim 2 , wherein the compound represented by Formula 1 is methylparaben.4. The method according to claim 1 , wherein the compound represented by Formula 1 is prepared by esterifying a reactant of phenol and carbon dioxide with alcohol.5Epimedium KoreanumVaccinium corymbosum. The method according to claim 1 , wherein the compound represented by Formula 1 is isolated from horny goat weed (Nakai) extract or blueberry () extract.6. The method according to claim 1 , wherein the degenerative neurological brain disorer is selected from a group consisting of Parkinson's disease claim 1 , Alzheimer's dementia (senile dementia) claim 1 , stroke claim 1 , Lou Gehrig's disease claim 1 , Pick's disease claim 1 , Creutzfeldt-Jakob disease claim 1 , Huntington's disease claim 1 , progressive ...

OLIGO-BENZAMIDE COMPOUNDS FOR USE IN TREATING CANCERS

The present invention provides bis- and tris-benzamide compounds in the treatment of breast, brain and ovarian cancers. 2. The method of claim 1 , wherein X is —NO.3. The method of claim 1 , wherein Y is —C(O)NH4. The method of claim 2 , wherein A claim 2 , A′ and A″ are each O.5. The method of claim 2 , wherein R claim 2 , Rand Rare independently Calkyl claim 2 , Chydroxyalkyl claim 2 , or Calkenyl.6. The method of claim 4 , wherein R claim 4 , Rand Rare independently Calkyl claim 4 , Chydroxyalkyl claim 4 , or Calkenyl.7. The method of claim 2 , wherein R claim 2 , Rand Rare independently Calkyl or Chydroxyalkyl.8. The method of claim 4 , wherein R claim 4 , Rand Rare independently Calkyl or Chydroxyalkyl.9. The method of claim 1 , wherein Y is COOCH.10. The method of claim 1 , wherein A claim 1 , A′ and A″ are each NH.11. The method of claim 9 , wherein A claim 9 , A′ and A″ are each NH.12. The method of claim 9 , wherein R claim 9 , Rand Rare independently Calkyl claim 9 , Chydroxyalkyl claim 9 , or Calkenyl.13. The method of claim 11 , wherein R claim 11 , Rand Rare independently Calkyl or Chydroxyalkyl.14. The method of claim 1 , wherein X is —NOand Y is —C(O)NH15. The method of claim 14 , wherein A claim 14 , A′ and A″ are each O.16. The method of claim 14 , wherein R claim 14 , Rand Rare independently Calkyl claim 14 , Chydroxyalkyl claim 14 , or Calkenyl.17. The method of claim 15 , wherein R claim 15 , Rand Rare independently Calkyl claim 15 , Chydroxyalkyl claim 15 , or Calkenyl.18. The method of claim 14 , wherein R claim 14 , Rand Rare independently Calkyl or Chydroxyalkyl.19. The method of claim 15 , wherein R claim 15 , Rand Rare independently Calkyl or Chydroxyalkyl.21. The method of claim 1 , wherein the tumor cell is an androgen receptor (AR)-positive tumor cell.22. The method of claim 1 , wherein the tumor cell is an estrogen receptor (ER)-positive tumor cell.23. The method of claim 1 , tumor cell is a carcinoma cell.24. The method of claim 23 , ...

USE OF CARBON NANOTUBES FOR PREVENTING OR TREATING BRAIN DISEASE

A method for preventing or treating a brain nervous disease includes administering to a subject in need thereof a therapeutically effective amount of a carbon nanotube, wherein the nervous disease is a brain disease or a traumatic central nervous system injury. The composition of the present invention enables patients to recover from physical damage to the brain, exhibits superior efficacy for inhibiting the onset of Parkinson's disease and strokes in animal models for Parkinson's disease and strokes, and the cytotoxic effects of beta amyloid in beta amyloid toxicity tests. Therefore, the composition of the present invention can be effectively used in the preparation of medicine for protecting cranial nerves, therapeutic agents for preventing or treating brain disease, or therapeutic agents for treating traumatic injuries to the central nervous system. 116-. (canceled)17. A method for preventing or treating a brain disease or a traumatic central nervous system injury , comprising administering to a subject in need thereof a therapeutically effective amount of a carbon nanotube.18. (canceled)19. (canceled)20. The method according to claim 17 , wherein the method is for preventing or treating the brain disease claim 17 , and the subject is in need of preventing or treating the brain disease.21. The method according to claim 20 , wherein the brain disease is a degenerative brain disease or an ischemic brain disease.22. The method according to claim 21 , wherein the brain disease is the degenerative brain disease selected from the group consisting of Alzheimer's disease claim 21 , Parkinson's disease claim 21 , dementia claim 21 , progressive supranuclear palsy claim 21 , multiple system strophy claim 21 , Olivopontocerebellar atrophy (OPCA) claim 21 , Shy-Drager syndrome claim 21 , Striatonigral degeneration claim 21 , Huntington's disease claim 21 , amyotrophic lateral sclerosis (ALS) claim 21 , essential tremor) claim 21 , cortico-basal ganlionic degeneration claim ...

EXTENDED-RELEASE FORMULATION FOR REDUCING THE FREQUENCY OF URINATION AND METHOD OF USE THEREOF

Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in an extended-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients formulated for extended-release. 1. A method for reducing the frequency of urination in a subject , comprising:administering to a subject in need thereof a pharmaceutical composition comprising:an active ingredient comprising one or more analgesic agents in an amount of 50-400 mg per agent, wherein said one or more analgesic agents are selected from the group consisting of aspirin, ibuprofen, naproxen, naproxen sodium, indomethacin, nabumetone, and acetaminophen,wherein said pharmaceutical composition is formulated for extended-release such that said active ingredient is released continuously over a period of 5-24 hours.2. The method of claim 1 , wherein said one or more analgesic agents comprises acetaminophen.3. The method of claim 1 , wherein said active ingredient further comprises an antimuscarinic agent.4. The method of claim 1 , wherein said active ingredient further comprises an antidiuretic agent.5. The method of claim 1 , wherein said active ingredient further comprises a spasmolytic.6. The method of claim 1 , wherein said active ingredient further comprises zolpidem.7. The method of claim 1 , wherein said an active ingredient further comprises two additional agents selected from the group consisting of an antimuscarinic agent claim 1 , an antidiuretic agent claim 1 , a spasmolytic and zolpidem.8. The method of claim 1 , wherein said pharmaceutical composition is formulated for extended-release such that said active ingredient is released continuously over a period of 5-8 hours.9. The method of claim 1 , wherein said pharmaceutical ...

Novel compound and medical use thereof

Provided is a levodopa prodrug that overcomes the problems attributed to the blood kinetics of levodopa such as large number of doses and the incidence of side effects due to frequent dosing. (2S)-2-Amino-3-(3,4-bis((2-(benzoyloxy)-2-methylpropanoyl)oxy)phenyl)propanoic acid, a salt thereof, or a solvate thereof is a levodopa prodrug, and provides a flat blood concentration-time profile of levodopa through oral administration, and therefore is useful as a preventive and/or therapeutic agent for Parkinson's disease and/or Parkinson's syndrome that overcomes the problems associated with pharmaceutical preparations of levodopa.

Compounds and methods for delivery of prostacyclin analogs

This invention pertains generally to prostacyclin analogs and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. Generally, the compounds and methods of the present invention increase the oral bioavailability and circulating concentrations of treprostinil when administered orally. Compounds of the present invention have the following formula:

Compounds for the treatment of metabolic disorders

Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis, are disclosed.

Acne Vulgaris Treatment Regimen

A kit for treatment of acne vulgaris, said formulation of the kit effectively inhibiting or killing without antibiotics. A preferred formulation alleviates the four pathogenic factors of acne. 1. A kit for use in the treatment of acne , comprising:a. a first container containing a face wash formulation comprising from about 1.0% to about 2.5% zinc pyrithione suspended in a topical carrier; andb. a second container containing a leave-on formulation comprising at least 0.25% zinc pyrithione.2. The kit according to claim 1 , further comprising instructions for using said face wash formulation and said leave-on composition claim 1 , which instructions are that a user should first apply said face wash formulation topically to skin for at least one minute claim 1 , then remove said face wash formulation from said skin claim 1 , and thereafter apply said leave on formulation to said skin.3. The kit according to claim 2 , wherein said instructions for using said face wash formulation are that a user should first apply said face wash formulation to said skin for up to thirty minutes.4. The kit of claim 1 , wherein said leave-on composition further comprises linoleic acid.5. The kit of wherein said leave-on composition further comprises salicylic acid.6. The kit of wherein said leave-on composition further comprises retinaldehyde.7. The kit of claim 1 , wherein said leave-on composition further comprises an inhibitor of 5 alpha-reductase.8. The kit according to wherein said inhibitor comprises unsaturated aliphatic fatty acids.9. The kit according to wherein the unsaturated aliphatic fatty acid is selected from gamma-linolenic acid claim 8 , linoleic acid and combinations thereof.10. The kit according to claim 8 , wherein said aliphatic unsaturated fatty acid is selected from gamma-linolenic acid claim 8 , cis 4 claim 8 ,7 claim 8 ,10 claim 8 ,13 claim 8 ,16 claim 8 ,19-docosahexaenoic acid claim 8 , cis-6 claim 8 ,9 claim 8 ,12 claim 8 ,15-octatetraenoic acid claim 8 , ...

Anti-microbial composition

This invention pertains to an anti-microbial, in particular anti-bacterial and/or anti-fungal composition comprising cinnamaldehyde, trans-2-methoxy cinnamaldehyde, cinnamyl acetate and linalool. In particular this composition is intended for preventing and/or treating microbial infection in an animal.

TERNARY MIXTURE FORMULATIONS

The invention relates to a novel free-flowing powder pharmaceutical formulation for the delivery of a poorly-water-soluble drug substance that increases the solubility and bioavailability of the poorly- water soluble drug substance, as well as to a method of making the free-flowing powder pharmaceutical formulation. The invention also relates to dispersed particles that disperse instantaneously from the free-flowing powder formulation when the formulation is added to water, aqueous solvent, or organic solvent, wherein the bulk distribution of the poorly-water soluble drug substance of the free-flowing powder formulation in the dispersed particles is uniform. Such dispersed particles increase the bioavailable surface area of the poorly water-soluble drug substance and facilitate the drug substance's dissolution. 1. A free-flowing powder formulation comprising a homogenous mixture of: a lipid or mixture of lipids; a poorly water-soluble drug substance or a combination of poorly water-soluble drug substances; a surfactant or a combination of surfactants; and a solubilizing aid , or a combination of solubilizing aids.2. The free-flowing powder formulation according to claim 1 , wherein at least one lipid is a phospholipid.3. The free-flowing powder formulation according to claim 2 , wherein the at least one phospholipid is selected from soy phosphatidyl choline claim 2 , egg phosphatidyl choline claim 2 , dimyristoyl-phosphocholine claim 2 , dimyristoyl-phosphoglycerol claim 2 , distearoyl-phosphatidylcholine claim 2 , distearoyl-phosphatidylglycerol claim 2 , Dipalmitoyl-phosphocholine claim 2 , or combinations thereof.4. The free-flowing powder formulation according to claim 1 , wherein at least one poorly water-soluble drug substance is a BCS II drug claim 1 , a BCS IV drug claim 1 , or a combination BCS II and BCS IV drugs.5. The free-flowing powder formulation according to claim 1 , wherein the at least one surfactant is selected from Vitamin E d-α-tocopheryl ...

GPR35 Ligands And Uses Thereof

A pharmaceutical composition including at least one compound of the Formulas (I), (II), or (III), or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, as defined herein. Also disclosed is a method of treatment of diseases which are pathophysiologically related to GPR35, the GPR35-hERG signaling complex, or both, as defined herein. 2. The method of claim 1 , wherein R′ is a covalent carbon-carbon single bond claim 1 , —CH— claim 1 , —CH═CH— claim 1 , —CHCH(CN)— claim 1 , —CHCH(OH)— claim 1 , —CHC(═O)— claim 1 , —N═N— claim 1 , —NH—NH— claim 1 , —C(CH)— claim 1 , —C(═CCl)— claim 1 , —CHCH(NH)— claim 1 , —CHC(CH)(NH)— claim 1 , —(CHCHO)— or —(CHCH(CH)O)— where n is from 1 to 10.3. The method of claim 2 , where R′ is —(CHCHO)— n is 1 to 7.4. The method of claim 1 , wherein the compound of Formula (I) has Rand Rtaken together is a heterocyclyl.5. The method of claim 1 , wherein the compound of Formula (II) has Rand Rtaken together is a heterocyclyl.9. The method of claim 1 , wherein the compound of the Formula (I) claim 1 , (II) claim 1 , or (III) claim 1 , is a GPR35 modulator.10. The method of claim 1 , wherein the disease is inflammation claim 1 , metabolic disorder claim 1 , inflammatory bowel disorder claim 1 , congestive heart failure claim 1 , or cancer.11. The method of claim 10 , wherein the metabolic disorder is diabetes claim 10 , Type I diabetes claim 10 , Type II diabetes claim 10 , inadequate glucose tolerance claim 10 , insulin resistance claim 10 , hyperglycemia claim 10 , hyperinsulinemia claim 10 , hyperlipidemia claim 10 , hypertriglyceridemia claim 10 , hypercholesterolemia claim 10 , dyslipidemia claim 10 , obesity claim 10 , premature or accelerated aging claim 10 , Syndrome X claim 10 , atherosclerosis claim 10 , heart disease claim 10 , stroke claim 10 , hypertension claim 10 , and peripheral vascular disease.12. The method of claim 10 , wherein the cancer is selected from prostate claim 10 , leukemia claim 10 , hormone ...

Methods For Enhancing The Release And Absorption of Water Insoluble Active Agents

Methods for enhancing the release and/or absorption of poorly water soluble active agents are described herein. The method involves dissolving, melting, or suspending a poorly water soluble active agent in one or more molten fatty acids, conjugated fatty acids, (semi-) solid surfactants of high HLB value, and/or hydrophilic polymers. The molten active agent mixture is then suspended and homogenized in a hydrophilic or lipophilic carrier to form microparticles suspended in the hydrophilic or lipophilic carrier. The particles suspended in the hydrophilic or lipophilic carrier can be encapsulated in a hard or soft gelatin or non-gelatin capsule. It is believed that the microparticles produced by the method described above will exhibit enhanced dissolution profiles. In vitro release studies of formulations containing cilostazol and fenofibrate showed 100% dissolution of cilostazol in 15 minutes and over 90% dissolution of fenofibrate in 35 minutes. 134-. (canceled)35. Microparticles comprising fenofibrate and one or more coatings materials selected from the group consisting of fatty acid , conjugated fatty acid , surfactant , and hydrophilic polymer , wherein the microparticles release at least 85% of the fenofibrate after 30 minutes using a USP dissolution apparatus II (paddles) at 75 rpm and 37.0±0.5° C. in 0.05 M sodium dodecyl sulfate.36. The particles of claim 35 , wherein when the active agent is fenofibrate claim 35 , the percent dissolution of fenofibrate is about 95% after 45 minutes.37. The particles of claim 35 , wherein when the active agent is fenofibrate claim 35 , the percent dissolution of fenofibrate is about 100% after 60 minutes.38. The microparticles of claim 35 , wherein the one or more coating materials are one ore more fatty acids claim 35 , conjugated fatty acids claim 35 , or combinations thereof.39. The microparticles of claim 38 , wherein the one or more fatty acids are selected from the group consisting of dodecanoic (lauric) acid claim 38 , ...

NOVEL FORMULATIONS FOR DERMAL, TRANSDERMAL AND MUCOSAL USE 1

A dermal, transdermal and/or mucosal formulation for topical application on skin, comprising an active pharmaceutical ingredient and a pharmaceutically acceptable solvent, and an anti-solvent; wherein the active pharmaceutical ingredient is soluble in the solvent in the absence of the anti-solvent, and wherein the active pharmaceutical ingredient is substantially in the solid state in the presence of the anti-solvent. A method for increasing the stability of an active pharmaceutical ingredient. 1. A dermal , transdermal , and/or mucosal formulation comprising:at least one active pharmaceutical ingredient selected from aciclovir, benzoyl peroxide, mometasone, piracetam, salicylic acid and spironolactone;a pharmaceutically acceptable solvent and/or solvent system; and (a) the active pharmaceutical ingredient is substantially in the solid state in said formulation in the presence of said anti-solvent;', '(b) the active pharmaceutical ingredient is soluble in the solvent and/or solvent system in the absence of said anti-solvent,', '(c) the solvent and/or solvent system includes a dihydric or polyhydric alcohol, and', '(d) the anti-solvent comprises an ester or water or mixtures thereof., 'a pharmaceutically acceptable anti-solvent, characterized in that'}2. (canceled)3. (canceled)4. The formulation according to claim 1 , wherein the pharmaceutically acceptable solvent and/or solvent system includes an unsaturated aliphatic dihydric or trihydric alcohol.5. The formulation according to claim 1 , wherein the pharmaceutically acceptable solvent and/or solvent system includes an unsaturated dihydric or trihydric alicyclic alcohol.6. The formulation according to claim 1 , wherein the pharmaceutically acceptable solvent and/or solvent system includes an alcohol chosen from 1 claim 1 ,2-propanediol claim 1 , butanediol claim 1 , pentanediol claim 1 , hexanediol claim 1 , polyethylene glycol claim 1 , glycerol and mixtures thereof.7. The formulation according to claim 1 , ...

PHARMACEUTICAL COMPOSITION COMPRISING TRANS-CINNAMALDEHYDE AND ITS USE IN THE TREATMENT OF INFECTIONS

This invention pertains to an anti-microbial, in particular anti-bacterial, more particularly against Gram−bacteria, and/or anti-fungal composition comprising as active blend trans-cinnamaldehyde and a potentiating agent, and to the potentiating agent. In particular this composition is intended for preventing and/or treating microbial infection in an animal. 1. Composition comprising: trans-cinnamaldehyde', at least one terpenoïd, chosen from mono and sesquiterpenoïds and/or', 'at least one derivate from trans-cinnamaldehyde, belonging to the group of phenylpropanoïds, with a molecular weight below 200 g/mol,', 'optionally phenylpropane derivative, 'a potentiating agent comprising or consisting of, 'optionally a drug, in particular an antibiotic or an antiviral drug,', 'optionally a carrier., 'a synergistic active blend comprising, or consisting of2. Composition according to claim 1 , wherein the composition is free of coumarin or safrole claim 1 , or is free of coumarin and safrole.3. Composition according to claim 1 , wherein the terpenoïd is chosen from menthanes claim 1 , acyclic monoterpenoïds and caryophyllanes.4. Composition according to claim 1 , wherein phenylpropane derivative is selected from the group consisting of apiole claim 1 , coniferyl benzoate claim 1 , chavicol claim 1 , cinnamein claim 1 , vanillin and benzyle benzoate.6. Composition according to claim 5 , wherein the trans-cinnamaldehyde derivate is chosen from trans-2-methoxycinnamaldehyde and cinnamyl acetate.7. Composition according to claim 1 , wherein the potentiating agent comprises claim 1 , or consists of:at least one terpenoïd and phenylpropane derivative in an amount ranging from 1 to 50% by weight compared to the total weight of the active blend,at least one derivate from trans-cinnamaldehyde in an amount ranging from 1 to 50% by weight compared to the total weight of the active blend.8. Composition according to claim 1 , wherein it comprises at least one antibiotic.912-. (canceled) ...

3-ACYL-INGENOLS II

The invention relates to compounds of general formula I, (I), wherein R is wherein R is aryl substituted by R3; or R is (C3-Ci3)-cycloalkyl, (C3-Ci3)-cycloalkenyl or (C7-Ci3)-cycloalkynyl optionally substituted by R4; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis. 2. A compound according to , wherein Rd and Re independently represents hydrogen , (C-C)-alkyl , (C-C)-alkenyl , (C-C)-alkynyl , aryl , heteroaryl , cycloalkyl , heterocycloalkyl , arylalkyl , heteroarylalkyl , cycloalkylalkyl , heterocycloalkylalkyl , halo(C-C)-alkyl , (C-C)-alkoxy(C-C)-alkyl , hydroxy(C-C)-alkyl or cyano(C-C)-alkyl , said (C-C)-alkyl , (C-C)-alkenyl , (C-C)-alkynyl , aryl , heteroaryl , cycloalkyl , heterocycloalkyl , arylalkyl , heteroarylalkyl , cycloalkylalkyl or heterocycloalkylalkyl optionally being substituted by one or more substituents selected from R7 , wherein R7 is as defined in ,{'sub': 1', '4, 'or Rd and Re may form a heterocyclic ring together with the nitrogen to which they are attached, said heterocyclic ring comprising up to two heteroatoms chosen from O, N or S, said heterocyclic ring optionally being substituted with (C-C)-alkyl.'}3. A compound according to , wherein R is aryl substituted by two or more substituents independently selected from R3; wherein R3 is as defined in ;{'sub': 3', '13', '3', '13', '7', '13, 'or R is (C-C)-cycloalkyl, (C-C)-cycloalkenyl or (C-C)-cycloalkynyl each of which may optionally be substituted by one or more substituents independently selected from R4; wherein'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'R4 is as defined in .'}4. A compound according to claim 1 , wherein R is aryl substituted by ...

ORALLY ADMINISTERED PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME, COMPRISING AN INTESTINAL MOTILITY MODIFIER, AN AGENT THAT PREVENTS GAS RETENTION, AND DIGESTIVE ENZYMES, AND PREPARATION METHOD THEREOF

A pharmaceutical composition or formulation adapted for oral administration in tablet, coated tablet, capsule or reconstitutable powder form for the prevention or treatment of intestinal disorders such irritable bowel syndrome, also known as irritable colon syndrome, based on an intestinal motility modifier, an agent that prevents gas retention, of digestive enzymes, a binding agent, a diluting agent, an absorbent agent, a lubricant, aglidant, and an disintegrating agent or suspending agent, effective in the normalization of intestinal disorders, to achieve an analgesic activity, to achieve an anti-spasmic activity and to reduce the symptoms associated with intestinal gas such as distention, abdominal pain and flatulence. 1. A pharmaceutical composition or formulation adapted for oral administration in tablet , coated tablet or capsule form for the prevention or treatment of intestinal disorders , the formulation is composed of: an intestinal motility modifier , an agent , which prevents the retention of gases , a digestive enzyme , a binding agent , a diluting agent , an absorbing agent , a disintegrating agent , a lubricating agent and a gliding agent.2. The pharmaceutical formulation in accordance with claim 1 , wherein the intestinal motility modifier is selected from a group which consists of: trimebutine claim 1 , fenoverine claim 1 , mebeverine claim 1 , dicycloverine claim 1 , ethyl bromide claim 1 , alosetron claim 1 , tegaserod claim 1 , loperamide claim 1 , phloroglucinol claim 1 , Trimethylphloroglucinol claim 1 , Butylscopolamine claim 1 , and pargeverine.3. The pharmaceutical formulation in accordance with claim 2 , wherein the intestinal motility modifier is trimebutine and its acceptable pharmaceutical salts.4. The pharmaceutical formulation in accordance with claim 2 , wherein the intestinal motility modifier is fenoverine and its acceptable pharmaceutical salts.5. The pharmaceutical formulation in accordance with claim 2 , wherein the intestinal ...

Use Of 2,5-Dihydroxybenzene Compounds And Derivatives For The Treatment Of Rosacea

The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea.

ANTI-CHOLESTEROLEMIC COMPOUNDS AND METHODS OF USE

The present invention provides novel compounds with hypocholesteremic activity from crude (EO) extracts and methods of use. The invention also provides nutraceuticals. 1. (canceled)2. A method for preventing or treating inflammation in a subject comprising administering to the subject an effective amount of one or more gallic acid derivatives , thereby preventing or treating inflammation in the subject.3. A method for preventing or treating a stress response in a subject comprising administering to the subject an effective amount of one or more gallic acid derivatives , thereby preventing or treating a stress response in the subject.4. The method of claim 2 , wherein the one or more gallic acid derivatives is administered as a nutraceutical.5. The method of claim 2 , wherein the one or more gallic acid derivatives are selected from the group consisting of: methyl gallate claim 2 , ethyl gallate claim 2 , glycerol-1-gallate claim 2 , glucose-1-gallate (GG1) claim 2 , glucose-6-gallate (GG6) claim 2 , glucose-1 claim 2 ,6-digallate (DGG16) claim 2 , mucic acid-2-gallate claim 2 , 1-methyl mucate-2-gallate claim 2 , mucic acid 1 claim 2 ,4-lactone 5-gallate claim 2 , geraniin claim 2 , corilagin claim 2 , chebilc acid claim 2 , and m-digallic acid with minor p-digallic acid.6. The method of claim 5 , wherein the one or more gallic acid derivatives are selected from the group consisting of: Compound 4+Compound 5+Compound 2a claim 5 , Compound 4+Compound 8+Compound 2a claim 5 , Compound 4+Compound 5+Compound 7 claim 5 , Compound 4+Compound 2a claim 5 , Compound 4+Compound 2b claim 5 , Compound 7+Compound 2b claim 5 , Compound 5+Compound 8 claim 5 , and Compound 5+Compound 7.714.-. (canceled)15. The method of claim 2 , wherein the at least one gallic acid derivative is present in an amount from about 10 mg-500 mg.16. The method of claim 15 , wherein the at least one gallic acid derivative is present in an amount from about 40 mg-200 mg.17. The method of claim 2 , further ...

TOPICAL PHARMACEUTICAL FORMULATIONS CONTAINING A LOW CONCENTRATION OF BENZOYL PEROXIDE IN SUSPENSION IN WATER AND A WATER-MISCIBLE ORGANIC SOLVENT

An aqueous formulation for topical application to the skin comprising water, a water-miscible organic solvent, and benzoyl peroxide, wherein the concentration of the organic solvent is sufficient to provide a stable suspension of benzoyl peroxide in the aqueous formulation without the inclusion of a surfactant in the formulation, wherein the ratio of concentrations of water and organic solvent in the formulation is sufficient to maintain the benzoyl peroxide in saturated solubility in the formulation following application to the skin, and wherein the concentration of benzoyl peroxide in the formulation is less than 5.0% and at least 1.0% w/w. The formulation may further contain a chemical compound in addition to benzoyl peroxide that is effective in the treatment of acne. The aqueous formulations of the invention are useful in the treatment of acne and acne rosacea. 1. A formulation for topical application to the skin comprising water , a water-miscible organic solvent , and benzoyl peroxide , wherein the concentration of the water-miscible organic solvent is sufficient to provide a stable suspension of benzoyl peroxide in the aqueous gel without the inclusion of a surfactant in the formulation , and wherein the concentration of benzoyl peroxide in the gel is less than 5.0% w/w and at least 1.0% w/w.2. The formulation of claim 1 , wherein the formulation is an aqueous gel that further comprises a gelling agent.3. The aqueous gel of claim 2 , wherein the organic solvent is a polyol.4. The aqueous gel of claim 3 , wherein the polyol is propylene glycol.5. The aqueous gel of claim 2 , wherein the concentration of the organic solvent is lower than that which will dissolve all of the benzoyl peroxide in the gel following the removal of all of the water from the gel.6. The aqueous gel of claim 2 , wherein the concentration of the organic solvent is 1 to 4 times the concentration of the benzoyl peroxide in the gel.7. The aqueous gel of claim 2 , wherein the ratio of water ...

Aerosol Forming Device For Use In Inhalation Therapy

The present invention relates to the inhalation delivery of aerosols containing small particles. Specifically, it relates to a device that forms drug containing aerosols for use in inhalation therapy. In a device aspect of the present invention, a device for delivering drug containing aerosols for inhalation therapy is provided. The device includes a housing and an airway that has a gas/vapor mixing airway. The airway further includes a subassembly, which has a metallic substrate coated on its surface with a composition comprising a drug.

Small molecule inhibitors of trpa1

The present invention relates to the use of compounds which are capable of attenuating skin irritation when they are applied to the skin. Skin irritation can be caused, inter alia, by ingredients of cosmetic or pharmaceutical compositions and/or environmental irritants. In particular, the present invention relates to compounds having the property of antagonizing the activation of the transient receptor potential (TRP) ankyrin 1 (TRPA1) ion channel and the use of said compounds as soothing agents. Such compounds can be used in many fields, particularly in personal-care products, cosmetics, textile and packaging products, pharmaceutical compositions, medical devices, and foodstuffs. The present invention further relates to products and/or pharmaceutical compositions containing said compounds. The present invention also relates to the use of the compounds described herein for the modulation of the taste of a food product.

Compositions Comprising Siloxane Polymer

Compositions comprising siloxane polymers are disclosed. The compositions are useful as thixotropic bases for a variety of components, such as antimicrobial agents, sterilants, medicaments, antibiotics, analgesics, essential oils, preservatives, colorants, fragrances, and the like. Methods for preparing the compositions are also disclosed. 1. A composition , comprising: [ i. organic compounds;', 'ii. compounds containing a silicon atom;', 'iii. mixtures of organic compounds;', 'iv. mixtures of compounds containing a silicon atom; and', 'v. mixtures of organic compounds and compounds containing a silicon atom;, 'a. a first solvent selected from the group consisting of, [ [{'sub': 3', '2', 'a', 'b', '3, '(a) RSiO(R′SiO)(R″HSiO)SiR;'}, {'sub': 2', '2', 'c', '2, '(b) HRSiO(R′SiO)SiRH; and'}, {'sub': 2', '2', 'a', 'b', '2, '(c) HRSiO(R′SiO)(R″HSiO)SiRH;'}, 'wherein:', {'sub': 1', '6, 'R, R′, R″ are, each independently, C-Calkyl;'}, 'a is about 0 to about 250;', 'b is about 1 to about 250; and', 'c is about 0 to about 250; and, 'i. an hydridopolysiloxane selected from the group consisting of, [{'br': None, 'sub': 2', '2', 'x', '2, 'CH═CH(CH)CH═CH'}, 'wherein:', 'x is about 1 to about 20;, 'ii. an α,ω-diene having the general formula], 'b. a siloxane copolymer comprising a reaction product of], 'A. a siloxane gel comprising a. organic compounds;', 'b. compounds containing a silicon atom;', 'c. mixtures of organic compounds;', 'd. mixtures of compounds containing a silicon atom; and', 'e. mixtures of organic compounds and compounds containing a silicon atom;, 'B. a first additional solvent selected from the group consisting of a. organic compounds;', 'b. compounds containing a silicon atom;', 'c. mixtures of organic compounds;', 'd. mixtures of compounds containing a silicon atom; and', 'e. mixtures of organic compounds and compounds containing a silicon atom., 'C. a second additional solvent selected from the group consisting of2. A composition of claim 1 , further ...

Use of a feed composition for reducing methane emission in ruminants, and/or to improve ruminant performance

The present invention relates to the field of reduction of methane emission in ruminants. Particularly, it relates to the use of a feed composition or a feed additive comprising at least one antibiotic and at least one organic molecule substituted at any position with at least one nitrooxy group for reducing the production of methane emanating from the digestive activities of ruminants, and/or to improve the ruminant performance.

VIRAL INHIBITOR COMPOSITION FOR IN VIVO THERAPEUTIC USE

The present invention concerns a pharmaceutical composition comprising a compound of formula A being (2,3(dihydroxy), 5[3(1,2)butadiene], 1(3hydroxy,3methyl,4pentene)benzene) and/or a compound of formula B being (2,3(dihydroxy), 5[3(1,2)butadiene], 2[2methylbutane]benzenal) and/or a compound of formula C being (2,3(dihydroxy), 5[3(1,2)butadiene], 2hydroxy,3butene benzoate) or a combination thereof for use as a medicament or for in vivo use in treatment and prevention of diseases caused by DNA enveloped viruses, DNA non-enveloped viruses, RNA enveloped viruses and RNA non-enveloped viruses. 3. Composition according to or composition for use according to , wherein the compounds are selected from the group consisting in:the compound of formula A alone, orthe compound of formula B alone, orthe compound of formula C alone, orthe compound of formula A and the compound of formula B, orthe compound of formula A and the compound of formula C, orthe compound of formula B and the compound of formula C, orthe compound of formula A and the compound of formula B and the compound of formula C.4. Composition according to or composition for use according to , wherein each compound is administered at a dose higher than or equal to 0.1 mg per administering.5. Composition according to or composition for use according to , wherein each compound is administered at a dose comprised between 0.1 mg and 5000 mg per administering.6. Composition according to or , wherein the dose is administered at least one time per day.7macadamia. Composition according to or composition for use according to or composition according to , wherein a base oil such as olive oil , or oil is added.8. Composition according to or composition for use according to , wherein the composition is used as a prophylactic.9. Composition according to or composition for use according to , wherein the composition is used as a viral inhibitor within the body.10. Composition according to or composition for use according to , ...

Combinations of Oral Medicaments Bonded by a Wrapping

An oral pharmaceutical dosage form is provided which contains at least two medicaments, in which form the medicaments on the one hand are brought together in a leakproof and in-vivo water soluble wrapping and on the other hand are separated so that the active principle of the combined medicaments cannot come into contact with one another. At least one of the medicaments can be chosen from the following therapeutic classes: non-steroidal anti-inflammatory drug (NSAID), proton pump inhibitor (PPI), beta-blocker, statin, conversion enzyme inhibitor (CEI), biguanide, myorelaxant, calcium inhibitor, corticoid, antidepressant, benzodiazepine, non-atropine-like intestinal transit retarder, intestinal antibacterial, and the following therapeutic molecules: spironolactone, propranolol, clarithromycin, amoxycillin, low-dose acetylsalicylic acid, potassium, and clopidogrel. 1. An oral pharmaceutical dosage form comprising at least two medicaments , wherein the medicaments are in the form of separately preconstituted tablets , wherein the preconstituted tablets are film coated and the film coating is present over the entire outer surface of the preconstituted tablets and wherein the preconstituted tablets are bonded together.2. The pharmaceutical dosage form according to claim 1 , wherein the medicaments comprise commercial galenical forms and/or galenical forms having the same qualitative and quantitative composition as commercial galenical forms but a different geometric form.3. The pharmaceutical dosage form according to claim 1 , wherein the film coating comprises a material that is water-soluble at the pH of the mouth claim 1 , at the pH of the stomach or at the pH of the intestine.4. The pharmaceutical dosage form according to claim 1 , comprising two claim 1 , three or four medicaments.5. The pharmaceutical dosage form according to claim 1 , wherein the total weight of medicament is less than or equal to 1500 mg.6. The pharmaceutical dosage form according to claim 1 , ...

METHODS OF THERAPEUTIC MONITORING OF NITROGEN SCAVENGING DRUGS

The present disclosure provides methods for evaluating daily ammonia exposure based on a single fasting ammonia blood level measurement, as well as methods that utilize this technique to adjust the dosage of a nitrogen scavenging drug, determine whether to administer a nitrogen scavenging drug, and treat nitrogen retention disorders. 111.-. (canceled)12. A method of predicting ammonia exposure for a patient having a urea cycle disorder (UCD) comprising measuring a fasting blood ammonia level for the subject wherein increasing fasting ammonia being associated with higher AUCand maximum observed ammonia.13. The method of claim 12 , wherein ammonia exposure is chosen from daily ammonia burden claim 12 , average daily ammonia level claim 12 , and/or highest daily ammonia value.14. The method of claim 12 , wherein the blood sample used for measuring fasting blood ammonia levels is a venous blood sample.15. The method of claim 12 , wherein the blood sample used for measuring fasting blood ammonia levels is a plasma blood sample.16. The method of claim 12 , wherein the fasting blood ammonia level is measured from a fasting morning blood draw.17. The method of claim 12 , wherein the fasting period for obtaining a fasting blood ammonia level is 4 hours or more claim 12 , 5 hours or more claim 12 , 6 hours or more claim 12 , 7 hours or more claim 12 , 8 hours or more claim 12 , 9 hours or more claim 12 , 10 hours or more claim 12 , 11 hours or more claim 12 , or 12 hours or more.18. The method of claim 12 , wherein the fasting period for obtaining a fasting blood ammonia level is 4-8 hours claim 12 , 6-8 hours claim 12 , or 8-12 hours.19. The method of claim 12 , wherein the fasting period for obtaining a fasting blood ammonia level is overnight.20. The method of claim 12 , wherein the upper limit of normal for blood ammonia level is 35 μmol/L.21. The method of claim 12 , further comprising comparing the fasting blood ammonia level for the subject with the upper limit of ...

Modified Alginate Hydrogels for Therapeutic Agents, their Preparation and Methods Thereof

A novel chemically modified alginate hydrogel has been developed which combines an aromatic compound with a carbohydrate, where the aromatic compound is one or more amines combined with an alginate. The chemical structure of alginate is modified using different amines and different methods, including: (1) covalently bonding aminoethyl benzoic acid to the alginate backbone, and (2) oxidizing the vicinal diol in the alginate chain to an aldehyde before coupling to aminoethyl benzoic acid. Alternatively, the combined aromatic compound and carbohydrate can be a dopamine combined with the alginate. The chemically modified alginate and the methods used can be utilized to encapsulate a variety of bioactive substances for oral delivery in humans and animals, including, but not limited to: (i) drugs, medicines, enzymes, proteins, hormones, and vaccines, (ii) vitamins, minerals, micronutrients and/or other dietary supplements, (iii) probiotics and/or other microorganisms, (iv) cells, cell parts, and/or other biological materials, and/or (v) other bioactive substances. 1. A composition comprising a substance wherein said substance comprises one or more (i) drugs , medicines , enzymes , proteins , hormones , vaccines , vitamins , minerals , micronutrients and/or other dietary supplements , (ii) probiotics and/or other microorganisms , (ii) cells , cell parts , and/or other biological materials , and/or (iii) other bioactive compounds or substances ,in combination with a modified alginate, wherein said modified alginate comprises an alginate backbone that has been modified by the addition of an aromatic compound substituent.2. The composition of wherein the aromatic substituent comprises one or more of a dopaminic substituent claim 1 , a phenolic substituent claim 1 , a benzoic acid substituent claim 1 , an anilinic substituent claim 1 , a toluenic substituent claim 1 , an amino sulfonamidic benzene substituent and/or mixtures thereof.3. The composition of claim 2 , wherein the ...

ANTI-MICROBIAL COMPOSITION

This invention pertains to an anti-microbial, in particular anti-bacterial and/or anti-fungal composition comprising cinnamaldehyde, trans-2-methoxycinnamaldehyde, cinnamyl acetate and linalool. In particular this composition is intended for preventing and/or treating microbial infection in an animal. 1. A method for antimicrobial prevention or treatment , said method comprising: [ trans-cinnamaldehyde, trans-2-methoxycinnamaldehyde, cinnamyl acetate, and linalool,', 'optionally cineole, beta-caryophyllene, and/or benzyl benzoate,, 'an active blend comprising, or consisting of, 'optionally a drug,', 'optionally a carrier,', 'wherein the total amount of coumarin and/or safrole is below 1% by weight compared to the total weight of the composition, and', 'wherein the composition comprises at least one pharmaceutical acceptable excipient., 'administering to a patient in need thereof a composition comprising2. A method for preventing or treating infections resulting from resistant bacteria or fungi or viruses , said method comprising: [ trans-cinnamaldehyde, trans-2-methoxycinnamaldehyde, cinnamyl acetate, and linalool,', 'optionally cineole, beta-caryophyllene, and/or benzyl benzoate,, 'an active blend comprising, or consisting of, 'optionally a drug,', 'optionally a carrier,', 'wherein the total amount of coumarin and/or safrole is below 1% by weight compared to the total weight of the composition,', 'wherein the composition comprises at least one pharmaceutical acceptable excipient., 'administering to a patient in need thereof a composition comprising3. Method according to claim 1 , wherein the bacteria involved in the infection are Gram − bacteria.4. Method according to claim 1 , wherein the bacteria involved in the infection is active toward drug-resistant Gram − bacteria strains to at least 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 or 7 bacteria belonging to strains:{'i': Pseudomonas', 'P. aeruginosa;, ', and more particularly'}{'i': ...

Formulations and carrier systems including farnesylthiosalicylic moieties

A formulation includes a carrier agent formed by conjugating at least one biologically active hydrophobic compound with at least one hydrophilic compound, the at least one biologically active hydrophobic compound selected from the group of farnesylthiosalicylic acid and a derivative of farnesylthiosalicylic acid which is biologically active as an RAS antagonist, wherein a plurality of the carrier agents are adapted to assemble into a structure and the at least one biologically active hydrophobic compound is conjugated with the at least one hydrophilic compound via a linkage which is labile in vivo, and a biologically active compound associated with the carrier agent.

Compositions and methods of use of phorbol esters in the treatment of neoplasms

Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms, treatments, or sequelae of disease. The phorbol esters described are particularly useful in the treatment of neoplastic diseases and/or managing the side effects of chemotherapeutic and radiotherapeutic treatments of neoplastic diseases.

Dermal Delivery Compositions Comprising Active Agent-Calcium Phosphate Particle Complexes and Methods of Using the Same

Dermal delivery compositions are provided. Aspects of the dermal delivery compositions include the presence of active agent-calcium phosphate particle complexes, where these complexes include uniform, rigid, spherical nanoporous calcium phosphate particles associated with one or more active agents. Also provided are methods of using the compositions in active agent delivery applications. 1. A composition comprising uniform , rigid , spherical nanoporous calcium phosphate calcium phosphate particles , wherein the particles have an average particle diameter of 2 microns or less and are complexed with an active agent.2. The composition according to claim 1 , wherein the particles have a pore volume ranging from 30 to 85%.3. The composition according to claim 2 , wherein the particles have a pore size ranging from 2 nm to 100 nm.4. The composition according to claim 1 , wherein the particles are produced by:preparing a fluid composition of calcium phosphate crystals;drying the fluid composition in a manner sufficient to produce precursor particles; andsubjecting the precursor particles to elevated temperature and pressure in a manner sufficient to produce uniform, rigid, spherical nanoporous calcium phosphate calcium phosphate particles.5. The composition according to claim 4 , wherein the drying comprises spray-drying.6. The composition according to claim 1 , wherein the composition is a topical formulation.7. The composition according to claim 1 , wherein the amount of active agent complexed with the particles ranges from 0.01 to 300 mg active agent per gram of particles.8. A method of delivering an active agent to a subject claim 1 , the method comprising: 'uniform, rigid, spherical nanoporous calcium phosphate calcium phosphate particles, wherein the particles have an average particle diameter of 2 microns or less and are complexed with an active agent;', 'applying a composition comprisingto a topical region of the subject to deliver the active agent to the subject. ...

COMPOUNDS AND METHODS FOR DELIVERY OF PROSTACYCLIN ANALOGS

This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis. 1. A method of treating pulmonary hypertension comprising intravenously administering to a human suffering from pulmonary hypertension a formulation for intravenous administration comprising a therapeutically effective amount of treprostinil or a pharmaceutically acceptable salt or ester thereof and a carrier selected from the group consisting of sterile water , isotonic aqueous saline solution , and 5% dextrose solution.2. The method of claim 1 , wherein the therapeutically effective amount of treprostinil in the formulation is in the form of an ester.4. The method of claim 1 , wherein the therapeutically effective amount of treprostinil in the formulation is in the form of a salt of treprostinil.5. The method of claim 4 , wherein the therapeutically effective amount of treprostinil in the formulation is in the form of a polymorph of a salt of treprostinil.6. The method of claim 5 , wherein the polymorph is a polymorph of a diethanolamine salt of treprostinil. This application is a continuation of U.S. application Ser. No. 13/906,585, filed May 31, 2013, which is a divisional of U.S. application Ser. No. 13/558,757, filed Jul. 26, 2012, which is a continuation of U.S. application Ser. No. 12/078,955, filed Apr. 8, 2008, which is a divisional of U.S. application Ser. No. 11/603,124, filed Nov. 22, 2006, which is a continuation of U.S. application Ser. No. 10/851,481, filed May 24, 2004, which claims benefit of U.S. Provisional Application Ser. No. 60/472,407, filed on May 22, 2003, the entire contents of which applications are incorporated by reference herein.This invention pertains generally to prostacyclin analogs and methods for ...

ANIMAL MODELS, SCREENING METHODS, AND TREATMENT METHODS FOR INTRAOCULAR DISEASES OR DISORDERS

Provided herein are screening methods and animal models related to intraocular diseases such as age-related macular degeneration (AMD), for example, for identifying candidate therapeutics for treating or preventing eye diseases, such as AMD. Also provided herein are compounds/compositions that are useful for killing or inhibiting the growth of a microorganism, such as . Further provided herein are methods of using the compounds/compositions for treating infections with a microorganism, such as and for treating or preventing diseases or disorders associated with such infections, such as AMD. 1. A screening method comprising:a) Culturing a microorganism in a suitable culture medium in the presence of a test compound;b) Measuring the growth of the microorganism in the culture medium in the presence of the test compound; and optionallyc) Identifying a candidate therapeutics that inhibits the growth of the microorganism compared to a control,wherein the microorganism comprises a species that is enriched in the intraocular space (e.g., aqueous humor in anterior chamber, a suspensory ligament, ciliary body, ciliary body and muscle, vitreous humor in posterior chamber, retina, choroid, optic nerve, lens, or iris) in a subject having age-related macular degeneration (AMD) compared to a healthy subject.2Staphylococcus epidermidis, Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus haemolyticus, Pseudomonas putida, Stenotrophomonas maltophilia, Bacillus cereus, Bacillus megaterium, Lactobacillus reuteri, Gardnerella vaginalis, Enterococcus faecium, Cytophaga hutchinsonii, Bacillus licheniformisXanthomonas oryzae.. The screening method of claim 1 , wherein the microorganism comprises one or more species selected from claim 1 , and3Bacillus megateriumPseudomonas putida.. The screening method of claim 1 , wherein the microorganism comprises and/or4. The screening method of claim 1 , wherein the microorganism comprises a mixture of microbial species substantially ...

Composition to Mitigate Spikes in Blood Sugar

Compositions comprising therapeutically effective amounts of quercetin, myricetin and chlorogenic acid are improved by the addition of one or multiple additional components, for mitigating blood sugar spikes in general and for treating diabetes specifically. Certain other additives produce additional benefits. 1. A composition comprising therapeutically effective amounts of quercetin , myricetin and chlorogenic acid in combination with curcumin.2. The composition according to claim 1 , wherein the curcumin is in an amount no greater than 12 g.3. The composition according to claim 2 , wherein the amount of curcumin is greater than 50 mg.4. The composition according to claim 1 , wherein the curcumin is in the form of an extract of turmeric root.5. The composition according to claim 1 , further comprising an agent that increases bioavailability of the curcumin in humans by at least 50%.6. The composition according to claim 5 , wherein the agent includes piperine.7. The composition according to claim 6 , wherein the piperine is in an amount greater than 20 mg.8. The composition according to claim 1 , wherein the agent is in the form of black pepper.9. The composition according to claim 1 , in combination with dried tea leaves.10. The composition according to claim 9 , wherein the composition and the dried tea leaves are combined in a flow through tea bag.11. The composition according to claim 9 , wherein content of the tea bag is characterized by no more than a trace amount of an agent that increases bioavailability of the curcumin in humans.12. A composition comprising therapeutically effective amounts of quercetin claim 9 , myricetin and chlorogenic acid in combination with capsicum.13. The composition according to claim 12 , wherein the capsicum is in an amount no greater than 8 g.14. The composition according to claim 13 , wherein the amount of capsicum is greater than 2 g.15. The composition according to claim 12 , wherein the capsicum is in the form of an extract ...

Methods for Treating Mucopolysaccharidosis

The present invention provides methods and compositions for the treatment of mucopolysaccharidoses (MPS). 1. A method of treating mucopolysaccharidosis (MPS) in a subject in need thereof , comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising a stilbene or stilbenoid compound or a pharmaceutically acceptable salt , ester , or prodrug thereof.2. The method of claim 1 , wherein the MPS is MPS I-H.3. The method of claim 1 , wherein the MPS is MPS I-S.4. The method of claim 1 , wherein the MPS is MPS I-H/S5. The method of claim 1 , wherein the MPS is MPS II.6. The method of claim 1 , wherein the MPS is MPS III A.7. The method of claim 1 , wherein the MPS is MPS III B.8. The method of claim 1 , wherein the MPS is MPS III C.9. The method of claim 1 , wherein the MPS is MPS III D.10. The method of claim 1 , wherein the MPS is MPS IV A.11. The method of claim 1 , wherein the MPS is MPS IV B.12. The method of claim 1 , wherein the MPS is MPS VI.13. The method of claim 1 , wherein the MPS is MPS VII.14. The method of claim 1 , wherein the MPS is MPS IX.15. The method of any one of to claim 1 , wherein the compound is a modified stilbene having from one to ten substituents.16. The method of claim 15 , wherein the substituents are independently selected from hydroxyl claim 15 , alkyl claim 15 , alkenyl claim 15 , carboxyl claim 15 , alkyloxy claim 15 , amino claim 15 , amido claim 15 , aryl claim 15 , or halogen.18. The method of claim 17 , wherein from 2 to 5 of R-Rare not hydrogen.19. The method of any one of - claim 17 , wherein the stilbene or stilbenoid compound is trans-resveratrol.20. The method of claim 1 , wherein the stilbene or stilbenoid compound is piceatannol.21. The method of claim 1 , wherein the stilbene or stilbenoid compound is CTI-110.22. The method of claim 1 , wherein the stilbene or stilbenoid compound is CTI-111.23. The method of claim 1 , wherein the stilbene or stilbenoid compound is CTI- ...

ANTISEPTIC COMPOSITION COMPRISING UNITHIOL AND DIMETHYLSULFOXIDE, USE OF THE COMPOSITION AND METHOD OF WOUND TREATMENT WITH ITS USE

Colloidal antiseptic compositions for treating wounds and/or for use in surgical operations are provided. The compositions form an elastic air- and water-permeable biodegradable film on the wound surface and have antiseptic, hemostatic, anti-inflammatory, wound-healing, and especially anesthetic and antitoxic effects. The compositions include a collagen hydrolysate, one or more salts of alginic acid and one or more antiseptics, and additionally include unithiol and dimethylsulfoxide. The compositions may also optionally include one or more anesthetics. 1. An antiseptic composition comprising a collagen hydrolysate , one or more pharmaceutically acceptable salts of alginic acid , one or more antiseptics , unithiol , dimethylsulfoxide , and a pharmaceutically acceptable aqueous carrier.2. The composition according to claim 1 , wherein the amount of unithiol is about 0.1 to about 10 wt % based on the total weight of the composition.3. The composition according to claim 1 , wherein the amount of dimethylsulfoxide is about 0.05 to about 5 wt % based on the total weight of the composition.4. The composition according to claims 1 , further comprising one or more anesthetics.5. The composition according to claim 4 , wherein one or more of the anesthetics is selected from the group consisting of lidocaine claim 4 , trimecaine claim 4 , tetracaine claim 4 , novocaine and a combination thereof.6. The composition according to claim 4 , wherein the amount of one or more anesthetics is about 0.01 to about 10 wt % based on the total weight of the composition.7. (canceled)8. The composition according to claim 1 , wherein the pharmaceutically acceptable carrier includes an aqueous solution of sodium hypochlorite.9. The composition according to claim 1 , wherein said one or more antiseptics are selected from the group consisting of oxyquinoline derivatives claim 1 , quaternary ammonium compounds claim 1 , silver-based antiseptics claim 1 , biguanides claim 1 , bisphenols claim 1 , ...

Carotenoid Formulation For Increased Bioavailability

A composition including a xanthophyll carotenoid diacetate, a transition metal salt, and phospholipids is provided. The composition does not include micelles and is not an emulsion. Methods of supporting eye health in subjects in need thereof using the composition are also provided. 1. A composition comprising:a xanthophyll carotenoid diacetate;a transition metal salt; andphospholipids,wherein the composition does not comprise micelles, andwherein the composition is not an emulsion.2. The composition according to claim 1 , wherein the phospholipids are selected from the group consisting of phosphatidylcholines claim 1 , lysophosphatidylcholines claim 1 , phosphatidic acids claim 1 , phosphatidylethanolamines claim 1 , phosphatidylglycerols claim 1 , phosphatidylserines claim 1 , phosphoinositides claim 1 , phosphosphingolipids claim 1 , and combinations thereof.3. The composition according to claim 1 , wherein the xanthophyll carotenoid diacetate comprises meso-zeaxanthin diacetate.4. The composition according to claim 3 , further comprising:(3R,3′R)-zeaxanthin diacetate, (3R,3′R,6R)-lutein diacetate, or a combination thereof.5. The composition according to claim 1 , further comprising:(3R,3′R,6R)-lutein, (3R,3′R)-zeaxanthin, meso-zeaxanthin, esters thereof, and combinations thereof.6. The composition according to claim 1 , wherein the composition is configured such that micelles encapsulating the xanthophyll carotenoid in free form are formed in a digestive tract of a subject after the composition is orally administered to the subject.7. The composition according to claim 1 , further comprising:an antioxidant.8. The composition according to claim 1 , wherein the transition metal salt comprises zinc oxide claim 1 , cupric oxide claim 1 , cuprous oxide claim 1 , or combinations thereof.9. A soft gel capsule comprising the composition according to .10. A method of supporting good eye health in a subject in need thereof claim 1 , the method comprising: a xanthophyll ...

METHODS AND PHARMACEUTICAL COMPOSITIONS FOR MODULATING AUTOPHAGY IN A SUBJECT IN NEED THEREOF

The present invention provides novel methods for the modulation of autophagy and the treatment of autophagy-re lated diseases, including cancer, neurodegenerative diseases, liver diseases, muscle diseases and pancreatitis. 120-. (canceled)21. A method of treating cancer in a subject in need thereof , comprising administering to the subject at least one acetyl CoA (AcCoA) depleting agent and at least one chemotherapeutic agent , wherein the AcCoA depleting agent is an inhibitor of ATP-citrate lyase (ACLY).22. The method according to claim 21 , wherein the inhibitor of ACLY is selected from the group consisting of hydroxycitrate claim 21 , (R claim 21 ,S)—S-(3 claim 21 ,4-dicarboxy-3-hydroxy-3-methyl-butyl)-CoA claim 21 , S-carboxymethyl-CoA claim 21 , (3R claim 21 ,5S)-rel-5-[6-(2 claim 21 ,4-Dichlorophenyl)hexyl]tetrahydro-3-hydroxy-2-oxo-3-furanacetic acid and 3 claim 21 ,5-Dichloro-2-hydroxy-N-(4-methoxy[1 claim 21 ,1′-biphenyl]-3-yl)-benzenesulfonamide.23. The method according to claim 21 , wherein the chemotherapeutic agent is selected from the group consisting of danurobicin claim 21 , doxorubidin claim 21 , epirubicin claim 21 , idarubicin claim 21 , mitoxantrone claim 21 , paclitaxel and docetaxel.24. The method according to claim 21 , wherein the cancer is selected from the group consisting of cancer cells from the bladder claim 21 , blood claim 21 , bone claim 21 , bone marrow claim 21 , brain claim 21 , breast claim 21 , colon claim 21 , esophagus claim 21 , gastrointestine claim 21 , gum claim 21 , head claim 21 , kidney claim 21 , liver claim 21 , lung claim 21 , nasopharynx claim 21 , neck claim 21 , ovary claim 21 , prostate claim 21 , skin claim 21 , stomach claim 21 , testis claim 21 , tongue claim 21 , or uterus.25coli. The method according to claim 21 , wherein the cancer is selected from the group consisting of malignant; carcinoma; carcinoma claim 21 , undifferentiated; giant and spindle cell carcinoma; small cell carcinoma; papillary carcinoma; ...

PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITORS AND METHODS OF USE THEREOF TO MODULATE LIPID METABOLISM

The invention relates to plasminogen activator-1 (PAI-1) inhibitor compounds and uses thereof in the treatment of any disease or condition associated with elevated PAI-1. The invention includes, but is not limited to, the use of such compounds to modulate lipid metabolism and treat conditions associated with elevated PAI-1, cholesterol, or lipid levels. 139.-. (canceled)44. A method of increasing circulating high density lipoprotein (HDL) in a subject claim 40 , comprising administering to said subject a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to increase HDL.45. A method of decreasing circulating very low density lipoprotein (VLDL) in a subject claim 40 , comprising administering to said subject a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to decrease VLDL.46. The method of claim 44 , wherein the subject is human.47. The method of claim 44 , wherein the PAI-1 inhibitor decreases PAI-1 binding to apolipoprotein E (ApoE) claim 44 , apolipoprotein A (ApoA) claim 44 , and/or VLDL.48. (canceled)49. (canceled)50. The method of claim 44 , wherein the PAI-1 inhibitor binds to PAI-1 in the presence of vitronectin.51. The method of claim 44 , wherein the PAI-1 inhibitor binds to PAI-1 in the presence of urokinase type plasminogen activator (uPA).52. A method of modulating cholesterol and/or lipid uptake comprising the step of administering a PAI-1 inhibitor compound according to in an amount effective to modulate cholesterol and/or lipid uptake.53. A method of modulating cholesterol and/or lipid clearance comprising the step of administering a plasminogen activator inhibitor-1 (PAI-1) inhibitor compound according to in an amount effective to inhibit very low density lipoprotein (VLDL) or apolipoprotein E (ApoE) or apolipoprotein A (ApoA) binding to VLDL-R and modulate cholesterol and/or lipid clearance.54. A method of modulating cholesterol and/or lipid clearance ...

Methods and compounds for modulating the secretion or expression of adhesion proteins or angiopoietins of cells

This invention provides methods, processes, compounds and compositions for modulating the gene expression or secretion of adhesion proteins, angiopoietins or their receptors to cure diseases, for anti-angiogenesis and for treating parasites, wherein the adhesion proteins or receptors comprise fibronectin, integrins family, myosin, vitronectin, collagen, laminin, glycosylation cell surface proteins, polyglycans, cadherin, heparin, tenascin, CD 54, CAM, elastin and FAK; wherein the angiopoietins comprise angiopoietin 1, angiopoietin 2, angiopoietin 3, angiopoietin 4, angiopoietin 5, angiopoietin 6, angiopoietin 7, angiopoietin-like 1, angiopoietin-like 2, angiopoietin-like 3, angiopoietin-like 4, angiopoietin-like 5, angiopoietin-like 6, and angiopoietin-like 7; wherein the cancers comprise breast cancer, leukocyte cancer, liver cancer, ovarian cancer, bladder cancer, prostate cancer, skin cancer, bone cancer, brain cancer, leukemia cancer, lung cancer, colon cancer, CNS cancer, melanoma cancer, renal cancer, cervical cancer, esophageal cancer, testicular cancer, spleenic cancer, kidney cancer, lymphatic cancer, pancreas cancer, stomach cancer and thyroid cancer.

Methods of treating and preventing diseases and disorders of the central nervous system

Disclosed is a method of treating or preventing a disease or disorder of the central nervous system (CNS) in a patient comprising administering transcranially, for example, directly to the skull, an effective amount of an anti-inflammatory agent to the patient. Examples of the anti-inflammatory agent include glutathione and inhibitors of purinergic receptors such as P2X 4 ,P2X 7 , P2Y 6 , and P2Y 12 receptors. Examples of disease or disorder of the CNS include brain injury, particularly traumatic brain injury, inflammation, infection, degeneration of brain cells, stroke, brain edema, tumor, Alzheimer's disease, Parkinson's disease, and multiple sclerosis. Also disclosed is a kit comprising at least one anti-inflammatory agent and printed materials containing instructions for transcranially administering the anti-inflammatory agent to the patient having a disease or disorder of the CNS, disorder of the CNS.

Urea derivative and use therefor

A compound has inhibitory activity on Discoidin Domain Receptor 1. The compound includes a urea derivative represented by the formula below or a pharmaceutically acceptable salt thereof.

ANTI-CHOLESTEROLEMIC COMPOUNDS AND METHODS OF USE

The present invention provides novel compounds with hypocholesteremic activity from crude (EO) extracts and methods of use. The invention also provides nutraceuticals. 147.-. (canceled)48. A pharmaceutical composition for the treatment or prevention of an elevated blood lipid level-related disease or disorder comprising one or more gallic acid derivatives and a pharmaceutically acceptable excipient.49. The pharmaceutical composition of claim 48 , wherein the gallic acid derivative is derived from EuMil.50. The pharmaceutical composition of claim 48 , wherein the one or more gallic acid derivatives is selected from the group comprising: methyl gallate claim 48 , ethyl gallate claim 48 , glycerol-1-gallate claim 48 , glucose-1-gallate (GG1) claim 48 , glucose-6-gallate (GG6) claim 48 , glucose-1 claim 48 ,6-digallate (DGG16) claim 48 , mucic acid-2-gallate claim 48 , 1-methyl mucate-2-gallate claim 48 , mucic acid 1 claim 48 ,4-lactone 5-gallate claim 48 , geraniin claim 48 , corilagin claim 48 , chebilc acid claim 48 , and m-digallic acid with minor p-digallic acid.51. The pharmaceutical composition of claim 48 , comprising a combination of gallic acid derivatives selected from the group consisting of: Compound 4+Compound 5+Compound 2a claim 48 , Compound 4+Compound 8+Compound 2a claim 48 , Compound 4+Compound 5+Compound 7 claim 48 , Compound 4+Compound 2a claim 48 , Compound 4+Compound 2b claim 48 , Compound 7+Compound 2b claim 48 , Compound 5+Compound 8 claim 48 , and Compound 5+Compound 7.52. The pharmaceutical composition of claim 48 , wherein the at least one gallic acid derivative is present in an amount from about 10 mg-500 mg.53. The pharmaceutical composition of claim 52 , wherein the at least one gallic acid derivative is present in an amount from about 40 mg-200 mg.54. The pharmaceutical composition of claim 48 , further comprising a one or more second agents.55. The pharmaceutical composition of claim 54 , wherein the one or more second agents is a ...

Compositions, Methods, and Medical Compositions for Treatment of and Maintaining the Health of the Liver

Compositions and methods for treatment of and maintaining the health of the liver are disclosed that include a mixture of plant extracts, wherein the plant extracts comprise at least one extract, at least one gel powder, and at least one extract. Compositions and methods for treatment of and maintaining the health of the liver are disclosed that include a mixture of plant extracts, wherein the plant extracts comprise at least one extract enriched for at least one polymer or biopolymer, at least one gel powder enriched for at least one chromone, and at least one extract enriched for at least one lignan and organic acid. 1ArtemisiaAloeSchizandra. A composition for treatment of and maintaining the health of the liver , comprising a mixture of plant extracts , wherein the plant extracts comprise at least one extract , at least one gel powder , and at least one extract.2ArtemisiaAloeSchizandra. A composition for treatment of and maintaining the health of the liver , comprising a mixture of plant extracts from an extract enriched for at least one polymer or biopolymer , an gel powder enriched for at least one chromone , and a extract enriched for at least one lignan and organic acid.3ArtemisiaSchizandra. The composition of claim 1 , wherein the extract and the extract are blended in a weight ratio from 4:1 to 1:4.4AloeArtemisiaSchizandra. The composition of claim 1 , wherein the gel powder are further blended with a mixture of and extracts in a weight percentage of about 5% to about 50%.5Artemisia, SchizandraAloe. The composition of claim 1 , wherein the mixture of and leaf gel powder is in a ratio of 8:4:3.6Artemisia. The composition of claim 2 , wherein the extract comprises 0.01% to 99.9% of biopolymers with molecular weight higher than 500.7ArtemisiaArtemisia absinthium, Artemisia abrotanumArtemisia afra, Artemisia annuaArtemisia arborescens, Artemisia asiatica, Artemisia campestris, Artemisia deserti, Artemisia iwayomogi, Artemisia ludoviciana, Artemisia vulgaris, ...

METHODS OF THERAPEUTIC MONITORING OF NITROGEN SCAVENGING DRUGS

The present disclosure provides methods for evaluating daily ammonia exposure based on a single fasting ammonia blood level measurement, as well as methods that utilize this technique to adjust the dosage of a nitrogen scavenging drug, determine whether to administer a nitrogen scavenging drug, and treat nitrogen retention disorders. 111-. (canceled)12. A method of treating a subject with a urea cycle disorder (UCD) who has a fasting morning plasma ammonia level less than the upper limit of normal , the method comprising:a) administering an initial dosage of glyceryl tri-[4-phenylbutyrate];b) after a time period sufficient for the glyceryl tri-[4-phenylbutyrate] to reach steady state, measuring a fasting morning plasma ammonia level for the subject;c) comparing the fasting morning plasma ammonia level to the upper limit of normal; andd) administering an adjusted dosage of glyceryl tri-[4-phenylbutyrate], wherein the adjusted dosage is greater than the initial dosage if the fasting morning plasma ammonia level is greater than half the upper limit of normal for plasma ammonia level.13. The method of claim 12 , wherein the time period sufficient for the glyceryl tri-[4-phenylbutyrate] to reach steady state is 48 hours.14. The method of claim 12 , wherein the time period sufficient for the glyceryl tri-[4-phenylbutyrate] to reach steady state is 48 to 72 hours.15. The method of claim 12 , wherein the time period sufficient for the glyceryl tri-[4-phenylbutyrate] to reach steady state is 72 hours to 1 week.16. The method of claim 12 , wherein the time period sufficient for the glyceryl tri-[4-phenylbutyrate] to reach steady state is 1 week to 2 weeks.17. The method of claim 12 , wherein the time period sufficient for the glyceryl tri-[4-phenylbutyrate] to reach steady state is greater than 2 weeks.18. The method of claim 12 , further comprising repeating steps (b) to (d) until the subject exhibits a fasting morning plasma ammonia level at or below half the upper limit of ...

METHODS OF TREATING UREA CYCLE DISORDERS

The present disclosure provides novel methods for determining an effective dosage of a PAA prodrug and for treating a UCD that incorporate body surface area and urinary PAGN concentration. The disclosure further provides novel methods for assessing compliance with PAA prodrug administration that incorporate urinary PAGN concentration, and the subject's current dosing regimen, BSA, or age. The disclosure further provides novel methods of treating a UCD in a subject in need thereof that incorporate urinary PAGN concentration, and the subject's current dosing regimen, BSA, and/or age. 120-. (canceled)21. A method of treating a urea cycle disorder (UCD) in a subject in need thereof who is less than two years of age comprising:a) administering glyceryl tri-[4-phenylbutyrate] to the subject whose urinary PAGN level is above 9000 μg/ml at the previously administered dosage, orb) administering an adjusted dosage of the glyceryl tri-[4-phenylbutyrate] to the subject whose urinary PAGN level is below 9000 μg/ml.22. The method of claim 21 , wherein the dosage of glyceryl tri-[4-phenylbutyrate] is administered orally.23. The method of claim 21 , wherein the effective dosage is 5 to 12.4 g/m/day.24. The method of claim 23 , wherein the effective dosage is at or about 7 to 9.5 g/m/day claim 23 , 7.5 to 9 g/m/day claim 23 , 8.0 to 8.5 g/m/day claim 23 , or 8.3 to 8.5 g/m/day.25. The method of claim 24 , wherein the effective dosage is at or about 8.02 or 8.35 g/m/day.26. The method of claim 21 , wherein the subject has not previously been administered one or more dosages of glyceryl tri-[4-phenylbutyrate].27. The method of claim 21 , wherein the subject in need thereof lacks systemic control of endogenous blood ammonia levels.28. A method of assessing compliance in a subject suffering from a urea cycle disorder (UCD) who is less than two years of age comprising:a) testing urinary PAGN level of the subject; andb) administering glyceryl tri-[4-phenylbutyrate] to the subject whose ...

Effects of a decaffeinated green coffee extract on body weight control by regulation of glucose metabolism

A method of controlling body weight in humans by administering an amount of decaffeinated green coffee extract effective to treat a subject. A preferred green coffee extract contains a ratio of 4-caffeoylquinic acid (4-CQA) to total chlorogenic acids (tCGA) (5-CQA/tCGA) of from about 0.1 to about 0.2. More preferably, the green coffee extract comprises from about 6% to about 8% of 4-caffeoylquinic acid and has a total chlorogenic acid concentration that exceeds about 45%. A preferred method of administration consists of administering the green coffee extracts is a dosage of about 200 mg twice a day prior to meals on an empty stomach.

ANTIPARASITIC COMPOSITIONS AND METHODS

Compositions and methods for treating parasitic infections are provided. The compositions can include two or more of alpha-pinene, linalyl acetate, para-cymene, and thymol octanoate. The compositions and methods can be effective against, for example, protozoan parasites, helminthic parasites, nematodes, trematodes, flukes, cestodes, and the like. Formulations made from the composition are also provided, including formulations in which the composition is combined with a carrier to form a food product and/or a drink. The formulation can be, for example, a suspension, a solution, or an emulsion in an oily or an aqueous carrier; like-wise, the composition can be provided in an encapsulated or microencapsulated form. 1106-. (canceled)107. A method of treating a parasitic infection comprising:administering to a subject or a host an effective amount of an antiparasitic composition comprising:thymol acetate;linalyl acetate;para-cymene;alpha-pinene; andan artificial additive.108. The method of claim 107 , wherein the antiparasitic composition comprises claim 107 , by weight of the composition claim 107 , 10% to 50% para-cymene.109. The method of claim 107 , wherein the antiparasitic composition comprises claim 107 , by weight of the composition claim 107 , 10% to 30% para-cymene.110. The method of claim 107 , wherein the antiparasitic composition comprises claim 107 , by weight of the composition claim 107 , 10% to 50% linalyl acetate.111. The method of claim 107 , wherein the antiparasitic composition comprises claim 107 , by weight of the composition claim 107 , 10% to 30% linalyl acetate.112. The method of claim 107 , wherein the antiparasitic composition further comprises a carrier.113. The method of claim 107 , wherein the subject or host is a human.114. The method of claim 107 , wherein the subject or host is a non-human animal.115. The method of claim 107 , wherein the subject or host is a mammal.116. The method of claim 107 , wherein the subject or host is selected ...

BICYCLIC ANALGESIC COMPOUNDS

Analgesic compounds for treatment of pain or fever that include a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering a compound described herein.

Fumarate compounds, pharmaceutical compositions thereof, and methods of use

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed.

METHOD FOR PROMOTING WOUND HEALING BY ADMINISTERING A COMPOUND WHICH BINDS LDL-RECEPTOR-RELATED PROTEIN (LRP) LIGAND BINDING DOMAIN

The present invention relates to the field of therapeutic methods, compositions and uses thereof, that affect, directly or indirectly, the behavior of LRP receptors. These compositions and methods result in the treatment of inflammatory, immunological and metabolic conditions. More particularly, the methods and compositions of the invention are directed to the identification of small molecules, drugs and/or pharmacological agents that affect the Wnt pathway by affecting normal complex formation among various signaling receptors, the LRP5 and LRP6 receptor, and related ligands. 2. The method of claim 1 , wherein the human patient has Diabetes mellitus.4. The method of claim 3 , wherein the human patient has Diabetes mellitus.6. The method of claim 5 , wherein the human patient has Diabetes mellitus.8. The method of claim 7 , wherein the human patient has Diabetes mellitus. This application is a Continuation of Ser. No. 14/680,547, filed Apr. 7, 2015, which is a Divisional of application Ser. No. 12/221,863, filed Aug. 7, 2008 (now U.S. Pat. No. 9,046,537), which is a Continuation-in-Part of application Ser. No. 11/598,916, filed Nov. 14, 2006 (now U.S. Pat. No. 8,367,822), which is a Continuation-in-Part of application Ser. No. 11/097,518, filed Apr. 1,2005 (abandoned), which is a Continuation-in-Part of application Ser. No. 11/084,668, filed Mar. 18, 2005 (now U.S. Pat. No. 8,461,155), which is a Continuation-in-Part of application Ser. No. 10/849,067, filed May 19, 2004 (now U.S. Pat. No. 8,637,506), which claims the benefit of U.S. Provisional Patent Application No. 60/504,860, filed Sep. 22, 2003, each of which is hereby incorporated by reference in its entirety.Receptors which are binding sites for proteins and small molecules are attractive targets for pharmacological intervention in disease-related processes. One group that fits this category of receptors is comprised of members of the LRP family. The term LRP is an abbreviation for LDL-Receptor-related ...

COMPOSITIONS AND METHODS TO TREAT DISEASE CHARACTERIZED BY CELLULAR PROLIFERATION AND ANGIOGENESIS

Described herein are compositions and methods for preventing and/or treating diseases involving aberrant angiogenesis employing one or more benzo[c]chromen-6-one derivatives. 24-. (canceled)5. The composition of claim 1 , wherein said composition is one or more compositions selected from the group consisting of Table I.6. The composition of claim 5 , wherein said Table I comprises benzo(c)chromen-6-one derivatives SG00272 claim 5 , SG00273 claim 5 , SG00373 claim 5 , SG00477 claim 5 , SG00519 claim 5 , SG00526 claim 5 , SG00527 claim 5 , SG00528 claim 5 , SG00529 claim 5 , SG00530 claim 5 , SG00531 claim 5 , SG00532 claim 5 , SG00533 claim 5 , SG00535 claim 5 , SG00536 claim 5 , SG00537 claim 5 , SG00538 claim 5 , SG00539 claim 5 , SG00540 claim 5 , SG00541 claim 5 , SG00542 claim 5 , SG00543 claim 5 , SG00544 claim 5 , SG00545 claim 5 , SG00546 claim 5 , SG00547 claim 5 , SG00548 claim 5 , SG00549 claim 5 , SG00550 claim 5 , SG00551 claim 5 , SG00552 claim 5 , SG00553 claim 5 , SG00554 claim 5 , SG00555 claim 5 , SG00556 claim 5 , SG00557 claim 5 , SG00558 claim 5 , SG00559 claim 5 , SG00560 claim 5 , SG00561 claim 5 , SG00562 claim 5 , SG00563 claim 5 , SG00564 claim 5 , SG00565 claim 5 , SG00566 claim 5 , SG00567 claim 5 , SG00568 claim 5 , SG00569 claim 5 , SG00570 claim 5 , SG00571 claim 5 , SG00572 claim 5 , SG00573 claim 5 , SG00574 claim 5 , SG00575 claim 5 , SG00576 claim 5 , SG00577 claim 5 , SG00579 claim 5 , SG00580 claim 5 , SG00581 claim 5 , SG00582 claim 5 , SG00583 claim 5 , SG00584 claim 5 , SG00585 claim 5 , SG00586 claim 5 , SG00587 claim 5 , SG00588 claim 5 , SG00589 claim 5 , SG00590 claim 5 , SG00591 claim 5 , SG00592 claim 5 , SG00593 claim 5 , SG00594 claim 5 , SG00595 claim 5 , SG00596 claim 5 , SG00597 claim 5 , SG00598 claim 5 , SG00599 claim 5 , SG00600 claim 5 , SG00601 claim 5 , SG00602 claim 5 , SG00603 claim 5 , SG00604 claim 5 , SG00605 claim 5 , SG00606 claim 5 , SG00607 claim 5 , SG00608 claim 5 , SG00609 claim 5 , SG00610 claim 5 ...

Compositions And Methods Of Use Of Phorbol Esters In The Treatment Of Neoplasms

Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms, treatments, or sequelae of disease. The phorbol esters described are particularly useful in the treatment of neoplastic diseases and/or managing the side effects of chemotherapeutic and radiotherapeutic treatments of neoplastic diseases. 3. The method of claim 1 , wherein the phorbol ester is phorbol 13-butyrate claim 1 , phorbol 12-decanoate claim 1 , phorbol 13-decanoate claim 1 , phorbol 12 claim 1 ,13-diacetate claim 1 , phorbol 13 claim 1 ,20-diacetate claim 1 , phorbol 12 claim 1 ,13-dibenzoate claim 1 , phorbol 12 claim 1 ,13-dibutyrate claim 1 , phorbol 12 claim 1 ,13-didecanoate claim 1 , phorbol 12 claim 1 ,13-dihexanoate claim 1 , phorbol 12 claim 1 ,13-dipropionate claim 1 , phorbol 12-myristate claim 1 , phorbol 13-myristate claim 1 , phorbol 12 claim 1 ,13 claim 1 ,20-triacetate claim 1 , 12-deoxyphorbol 13-angelate claim 1 , 12-deoxyphorbol 13-angelate 20-acetate claim 1 , 12-deoxyphorbol 13-isobutyrate claim 1 , 12-deoxyphorbol 13-isobutyrate-20-acetate claim 1 , 12-deoxyphorbol 13-phenylacetate claim 1 , 12-deoxyphorbol 13-phenylacetate 20-acetate claim 1 , 12-deoxyphorbol 13-tetradecanoate claim 1 , phorbol 12-tigliate 13-decanoate claim 1 , 12-deoxyphorbol 13-acetate claim 1 , phorbol 12-acetate. claim 1 , or phorbol 13-acetate.4. The method of claim 1 , wherein the phorbol ester is 12-O-tetradecanoylphorbol-13-acetate.5. The method of claim 1 , wherein the at least one secondary or adjunctive therapeutic agent is administered to said subject in a coordinate administration protocol claim 1 , simultaneously with claim 1 , prior to claim 1 , or after claim 1 , administration of said phorbol ester to said subject.6. The method of claim 1 , wherein the at least one secondary or adjunctive therapeutic agent is selected from the group consisting of: ...

ANTI-VIRULENCE COMPOSITIONS AND METHODS

A method of treating a bacterial infection in a subject in need thereof includes administering to the subject an AgrA antagonist. 2. The method of claim 1 , wherein Ris selected from the group consisting of 5-Pr claim 1 , and 5-Hexyl; Ris selected from the group consisting of F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , NO claim 1 , Me claim 1 , i-Pr claim 1 , Ph claim 1 , COOH claim 1 , t-Bu claim 1 , OCH claim 1 , and COOCH; wherein p is an integer from 0-5; and pharmaceutically acceptable salts thereof.3. The method of claim 1 , wherein the compound is provided in a topical composition with a pharmaceutically acceptable carrier and administered to the bacterial infection of the subject topically.4. The method of claim 1 , further comprising administering an antibiotic to the bacteria.5. The method of claim 1 , wherein the compound is administered at an amount to effective to inhibit biofilm formation of the bacteria.9Staphylococcus aureus.. The method of claim 1 , wherein the bacteria is methicillin-resistant11. The method of claim 10 , wherein Ris selected from the group consisting of 5-Pr claim 10 , and 5-Hexyl; Ris selected from the group consisting of F claim 10 , Cl claim 10 , Br claim 10 , I claim 10 , NO claim 10 , Me claim 10 , i-Pr claim 10 , Ph claim 10 , COOH claim 10 , t-Bu claim 10 , OCH claim 10 , and COOCH; wherein p is an integer from 0-5; and pharmaceutically acceptable salts thereof.12. The method of claim 10 , wherein the compound is provided in a topical composition with a pharmaceutically acceptable carrier and administered to the bacteria topically.13. The method of claim 10 , further comprising administering an antibiotic to the bacteria.17Staphylococcus aureus.. The method of claim 10 , wherein the bacteria is methicillin-resistant This application is a Continuation-in-Part of U.S. patent application Ser. No. 14/435,387, filed Apr. 13, 2017, which is a National Phase Filing of PCT/US2013/064800, filed Oct. 14, 2013, which claims ...

DIACEREIN OR RHEIN TOPICAL FORMULATIONS AND USES THEREOF

A topical pharmaceutical composition containing diacerein and/or its analogs is provided. Also provided is a method for treating various diseases using this topical pharmaceutical composition. 1. A topical pharmaceutical composition comprising a therapeutically effective amount of a compound selected from the group consisting of diacerein , rhein , monoacetylrhein , and salts or esters or prodrugs thereof , and one or more pharmaceutically acceptable excipients , wherein the composition is in the form of ointment , and at least about 90% by volume of the compound has a particle size of about 0.5 to about 35 μm.2. The composition of claim 1 , wherein at least about 90% by volume of the compound has a particle size of about 10 to about 30 μm.3. The composition of claim 1 , wherein at least about 90% by volume of the compound has a particle size of about 12 to about 25 μm.4. The composition of claim 1 , wherein the pharmaceutically acceptable excipient comprises an ointment base claim 1 , an ointment base modifier claim 1 , and a surfactant.5. The composition of claim 1 , wherein the compound is present in an amount between about 0.1% to about 10.0% w/w of the total composition.6. The composition of claim 1 , wherein the compound is present in an amount between about 0.1% to 5.0% w/w of the total composition.7. The composition of claim 1 , wherein the compound is present in an amount between about 0.5% to about 2.0% w/w of the total composition.8. The composition of claim 1 , comprising about 0.1% to about 10% w/w of the compound claim 1 , about 15% to about 99% w/w of an ointment base claim 1 , about 0% to about 60% w/w of an ointment base modifier claim 1 , and about 0% to about 10% w/w of a surfactant claim 1 , based on the total weight of the composition.9. The composition of claim 1 , comprising about 1% w/w of the compound claim 1 , about 84.5% w/w of an ointment base claim 1 , about 12% w/w of an ointment base modifier claim 1 , and about 2% w/w of a surfactant ...

METHODS OF THERAPEUTIC MONITORING OF NITROGEN SCAVENGING DRUGS

The present disclosure provides methods for evaluating daily ammonia exposure based on a single fasting ammonia blood level measurement, as well as methods that utilize this technique to adjust the dosage of a nitrogen scavenging drug, determine whether to administer a nitrogen scavenging drug, and treat nitrogen retention disorders. 111-. (canceled)12. A method of treating impaired neurocognitive executive function in a subject suffering from a urea cycle disorder (UCD) comprising administering a therapeutically-effective amount of glyceryl tri-[4-phenylbutyrate] (HPN-100).13. The method of claim 12 , wherein administration of HPN-100 reduces total ammonia burden.14. The method of claim 12 , wherein the method reverses neurocognitive impairment.15. The method of claim 12 , wherein the subject is a pediatric patient.16. The method of claim 15 , wherein the pediatric patient is from 6 to 17 years old.17. The method of claim 12 , wherein neurocognitive function is assessed by BRIEF (Behavior Rating Inventory of Executive Function).18. The method of claim 12 , wherein the therapeutically-effective amount of HPN-100 maintains a monthly average fasting ammonia level at about half the upper limit of normal (ULN). The present application is a divisional of U.S. patent application Ser. No. 13/417,137, filed Mar. 9, 2012 and now pending, which claims the benefit of U.S. Provisional Application No. 61/564,668, filed Nov. 29, 2011, and U.S. Provisional Application No. 61/542,100, filed Sep. 30, 2011, the disclosures of which are incorporated by reference herein in their entirety, including drawings.Nitrogen retention disorders associated with elevated ammonia levels include urea cycle disorders (UCDs) and hepatic encephalopathy (HE).UCDs include several inherited deficiencies of enzymes or transporters necessary for the synthesis of urea from ammonia, including enzymes involved in the urea cycle. The urea cycle is depicted in , which also illustrates how certain ammonia- ...

METHODS OF TREATING UREA CYCLE DISORDERS

The present disclosure provides novel methods for determining an effective dosage of a PAA prodrug and for treating a UCD that incorporate body surface area and urinary PAGN concentration. The disclosure further provides novel methods for assessing compliance with PAA prodrug administration that incorporate urinary PAGN concentration, and the subject's current dosing regimen, BSA, or age. The disclosure further provides novel methods of treating a UCD in a subject in need thereof that incorporate urinary PAGN concentration, and the subject's current dosing regimen, BSA, and/or age. 120.-. (canceled)21. A method for determining or adjusting an effective dosage of a phenylacetic acid (PAA) prodrug to be administered to a subject with a urea cycle disorder , comprising:calculating the body surface area (BSA) of the subject; and{'sup': 2', '2, 'administering an effective dosage of the PAA prodrug to the subject wherein the effective dosage of the PAA prodrug is a first dosage if the BSA is at or above 1.3 mor a second dosage if the BSA is below 1.3 m, and wherein the second dosage is higher than the first dosage.'}22. The method of claim 21 , wherein the PAA prodrug is glyceryl tri-[4-phenylbutyrate].23. The method of claim 21 , wherein the subject has previously been administered an initial dosage of an initial PAA prodrug.24. The method of claim 23 , wherein the initial PAA prodrug is glyceryl tri-[4-phenylbutyrate].25. The method of claim 23 , wherein the initial dosage of the glyceryl tri-[4-phenylbutyrate] is 5 to 12.4 g/m/day.26. The method of claim 25 , wherein the effective dosage of the PAA prodrug is 5.33 to 8.79 g/m/day.27. The method of claim 26 , wherein the PAA prodrug is glyceryl tri-[4-phenylbutyrate].28. The method of claim 25 , wherein the effective dosage of the PAA prodrug is 6.25 to 9.9 g/m/day.29. The method of claim 28 , wherein the PAA prodrug is glyceryl tri-[4-phenylbutyrate].30. The method of claim 21 , wherein the subject is under the age of ...

METHODS OF THERAPEUTIC MONITORING OF NITROGEN SCAVENGING DRUGS

The present disclosure provides methods for evaluating daily ammonia exposure based on a single fasting ammonia blood level measurement, as well as methods that utilize this technique to adjust the dosage of a nitrogen scavenging drug, determine whether to administer a nitrogen scavenging drug, and treat nitrogen retention disorders. 111-. (canceled)12. A method of predicting the maximum daily blood ammonia value for a patient in need thereof , consisting of:measuring the patient's fasting morning blood ammonia level,wherein if the fasting morning blood ammonia level is less than or equal to half the upper limit of normal for blood ammonia for the laboratory which performed the fasting morning blood ammonia level measurement, the patient has an average likelihood of about 70% to 80% within a 95% confidence interval that the patient's maximum daily blood ammonia level will not exceed 1.5 times the upper limit of normal for blood ammonia.13. The method of claim 12 , wherein the average likelihood is about 75% with 95% confidence that the true probability is between 58% and 86%.14. The method of claim 12 , further comprising administering a therapeutically effective amount of glycerol triphenylbutyrate to said patient if the fasting morning blood ammonia level is greater than half the upper limit of normal.15. A method of predicting the maximum daily blood ammonia value for a patient in need thereof claim 12 , consisting of:measuring the patient's fasting morning blood ammonia level,wherein if the fasting morning blood ammonia level is less than or equal to half the upper limit of normal for blood ammonia for the laboratory which performed the fasting morning blood ammonia level measurement, the patient has an average likelihood of about 84% within a 95% confidence interval that the patient's maximum daily blood ammonia level will not exceed 1.5 times the upper limit of normal for blood ammonia.16. The method of claim 15 , wherein the average likelihood is about 84% ...

INHIBITORS OF MICROBIALLY INDUCED AMYLOID

The present disclosure provides methods and compositions for the prevention, amelioration, or alleviation of one or more neurological disorders associated with microbially-induced amyloid formation. Methods of inhibiting, ameliorating, reducing the likelihood, delaying the onset of, treating, or preventing an amyloid disorder are disclosed. Methods of identifying compounds capable of inhibiting the formation of microbially-induced amyloid fibrils are disclosed. 1. A method of inhibiting , ameliorating , reducing the likelihood , delaying the onset of , or treating a microbially induced amyloid disorder , the method comprising administering to a subject in need thereof a composition comprising a compound selected from the group consisting of: epigallocatechin gallate , quercetin , morin , rosmarinic acid , gallic acid , lauryl gallate , methoxyhydroquinone , curcumin , resveratrol , apigenin , nordihydroguaiaretic acid , phloretin and genistein; or pharmaceutically acceptable salts thereof.2. The method of claim 1 , wherein the microbially induced amyloid disorder is α-synucleinopathy claim 1 , Parkinson's Disease claim 1 , Lewy Body Dementia claim 1 , incidental Lewy body disease claim 1 , Lewy body variant of Alzheimer's disease claim 1 , multiple system atrophy claim 1 , pure autonomic failure claim 1 , intestinal dysbiosis claim 1 , intestinal hyperpermeability claim 1 , irritable bowel syndrome (IBS) claim 1 , inflammatory bowel disease (IBD) claim 1 , ulcerative colitis claim 1 , or Crohn's disease or any combination thereof.3. The method of claim 1 , wherein the subject suffers from gastrointestinal symptoms comprising one or more of dysphagia claim 1 , reduced gut motility claim 1 , gastroparesis claim 1 , constipation claim 1 , small intestine bacterial overgrowth (SIBO) claim 1 , diarrhea claim 1 , abdominal pain and/or cramping claim 1 , bloating claim 1 , flatulence claim 1 , and nausea.4. The method of claim 3 , wherein the gastrointestinal symptoms are ...

FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. 2. The compound according to claim 1 , wherein each Ris independently chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , n-pentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , cyclohexylmethyl claim 1 , phenyl claim 1 , benzyl claim 1 , and substituted methyl.3. The compound according to claim 1 , wherein each Ris independently chosen from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , cyclohexyl claim 1 , and phenyl.4. The compound according to claim 1 , wherein each Ris independently chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , and n-butyl.5. The compound according to claim 1 , wherein each Xis independently chosen from methane-diyl claim 1 , ethane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,3-diyl claim 1 , substituted methane-diyl claim 1 , substituted ethane-1 claim 1 ,2-diyl claim 1 , and substituted propane-1 claim 1 ,3-diyl.6. The compound according to claim 1 , wherein each Xis independently chosen from methane-diyl claim 1 , ethane-1 claim 1 ,1-diyl claim 1 , ethane-1 claim 1 ,2-diyl claim 1 , 2-phenylethane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,3-diyl claim 1 , 2-methylpropane-1 claim 1 ,1-diyl claim 1 , 2-methylpropane-1 claim 1 ,2-diyl claim 1 , 2 claim 1 ,2-dimethylpropane-1 claim 1 ,3-diyl claim 1 , butane-1 claim 1 ,2-diyl claim 1 , butane-1 claim 1 ,3- ...

FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. 2. The compound according to claim 1 , wherein Ris chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , and isopropyl.3. The compound according to claim 1 , wherein Ris chosen from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , n-pentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , cyclohexylmethyl claim 1 , phenyl claim 1 , benzyl claim 1 , substituted methyl claim 1 , substituted ethyl claim 1 , substituted n-propyl claim 1 , substituted isopropyl claim 1 , substituted n-butyl claim 1 , substituted isobutyl claim 1 , substituted tert-butyl claim 1 , substituted n-pentyl claim 1 , and substituted n-hexyl.4. The compound according to claim 1 , wherein Ris chosen from methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , isobutyl claim 1 , tert-butyl claim 1 , n-pentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , cyclohexylmethyl claim 1 , phenyl claim 1 , and benzyl.5. The compound according to claim 1 , wherein Xis chosen from methane-diyl claim 1 , ethane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,3-diyl claim 1 , substituted methane-diyl claim 1 , substituted ethane-1 claim 1 ,2-diyl claim 1 , and substituted propane-1 claim 1 ,3-diyl.6. The compound according to claim 1 , wherein Xis chosen from methane-diyl claim 1 , ethane-1 claim 1 ,1-diyl claim 1 , ethane-1 claim 1 ,2-diyl claim 1 , 2-phenylethane-1 claim 1 ,2-diyl claim 1 , propane-1 claim 1 ,2- ...

ANTI-CANCER LEAD MOLECULE

Derivatives of plumbagin can be selectively cytotoxic to breast cancer cells. Derivative ‘A’ (Acetyl Plumbagin) has emerged as a lead molecule for testing against estrogen positive breast cancer and has shown low hepatotoxicity as well as overall lower toxicity in nude mice model. The toxicity of derivative ‘A’ was determined to be even lower than vehicle control (ALT and AST markers). The possible mechanism of action identified based on the microarray experiments and pathway mapping shows that derivative ‘A’ could be acting by altering the cholesterol-related mechanisms. The low toxicity profile of derivative ‘A’ highlights its possible role'as future anti-cancer drug and/or as an adjuvant drug to reduce the toxicity of highly toxic chemotherapeutic'drugs. 2. The method of claim 1 , wherein Ris H.3. The method of claim 1 , wherein Ris R—C(O)—O— claim 1 , in which Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , propenyl claim 1 , isopropyl claim 1 , butyl claim 1 , isobutyl claim 1 , sec-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , aryl or heteroaryl.4. The method of claim 1 , wherein Ris H.5. The method of claim 1 , wherein Ris H claim 1 , —O—R′ claim 1 , or C-Calkyl.6. The method of claim 1 , wherein Ris phenyl.7. The method of claim 1 , wherein Ris H claim 1 , OH claim 1 , or methyl.8. The method of claim 1 , wherein each group R-R claim 1 , for each occurrence claim 1 , is claim 1 , independently claim 1 , optionally substituted with halo claim 1 , carboxylic acid claim 1 , cyano claim 1 , or nitro.10. The pharmaceutical composition of claim 9 , wherein Ris H.11. The pharmaceutical composition of claim 9 , wherein Ris R—C(O)—O— claim 9 , in which Ris methyl claim 9 , ethyl claim 9 , propyl claim 9 , propenyl claim 9 , isopropyl claim 9 , butyl claim 9 , isobutyl claim 9 , sec-butyl claim 9 , pentyl claim 9 , hexyl claim 9 , aryl or heteroaryl.12. The pharmaceutical composition of claim 9 , wherein Ris H.13. The pharmaceutical composition of claim 9 , ...

Compositions comprising S-Adenosylmethionine and a gallic acid ester

Provided herein are compositions and formulations comprising S-adenosyl-L-methionine (“SAM-e” or “SAMe”) and one or more gallic acid esters. Also provided herein are methods for improving the delivery of SAMe. Compositions and formulations provided herein increase SAMe plasma concentrations and area under the curve (AUC) values. Also provided herein are methods of treating a disease or disorder in a subject by administering compositions or formulations comprising exogenous SAMe and one or more gallic acid esters. 1. A method of treating a disease or disorder comprising administering a composition comprising exogenous S-adenosylmethionine and at least one gallic acid ester to a patient in need thereof.2. The method of claim 1 , wherein the at least one gallic acid ester is selected from the group consisting of ethyl gallate claim 1 , propyl gallate and octyl gallate. This application is a continuation of U.S. patent application Ser. No. 14/628,623, filed Feb. 23, 2015, entitled “COMPOSITIONS COMPRISING S-ADENOSYLETHIONINE AND A GALLIC ACID ESTER”, which is a continuation of U.S. patent application Ser. No. 14/247,061, filed Apr. 7, 2014, now U.S. Pat. No. 8,975,238, Issue Date Mar. 10, 2015, which is a continuation of International Patent Application No. PCT/CA2013/000876, filed Oct. 16, 2013, which claims the benefit of U.S. Provisional Application No. 61/715,138, filed Oct. 17, 2012, both of which are incorporated herein by reference in their entireties.S-adenosyl-L-methionine (“SAM-e” or “SAMe”) is a naturally occurring compound that is present in almost every tissue throughout the body. Aside from water, SAMe is considered the second most common metabolic molecule—adenosine triphosphate (ATP) being the most common. SAMe is available as an over-the-counter dietary supplement in a number of countries and by prescription in Europe. Supplementation with exogenous SAMe has been tested and showed efficacious for the treatment of various ailments, including arthritis, ...

ANTI-HEMAGGLUTININ ANTIBODIES AND METHODS OF USE

The present invention provides anti-hemagglutinin antibodies, compositions comprising anti-hemagglutinin antibodies, and methods of using the same. 153.-. (canceled)54. An isolated nucleic acid encoding an anti-hemagglutinin antibody comprising three heavy chain hypervariable regions (HVR-H1 , HVR-H2 , and HVR-H3) and three light chain hypervariable regions (HVR-L1 , HVR-L2 , and HVR-L3) , wherein:(a) HVR-H1 comprises the amino acid sequence of SEQ ID NO:178;(b) HVR-H2 comprises the amino acid sequence of SEQ ID NO:179;(c) HVR-H3 comprises an amino acid sequence selected from the group consisting of SEQ ID NOs:180 and 181;(d) HVR-L1 comprises an amino acid sequence selected from the group consisting of SEQ ID NOs:182, 183, 184, 185, and 186;(e) HVR-L2 comprises the amino acid sequence of SEQ ID NO:187; and(f) HVR-L3 comprises an amino acid sequence selected from the group consisting of SEQ ID NOs:188, 189, and 190.55. The isolated nucleic acid of claim 54 , wherein the antibody comprises a light chain variable region comprising an amino acid sequence selected from the group consisting of SEQ ID NOs:113 claim 54 , 117 claim 54 , 119 claim 54 , 122 claim 54 , 124 claim 54 , 126 claim 54 , 128 claim 54 , 130 claim 54 , and 132.56. The isolated nucleic acid of claim 54 , wherein the antibody comprises a heavy chain variable region comprising an amino acid sequence selected from the group consisting of SEQ ID NOs:111 and 115.57. The isolated nucleic acid of claim 54 , wherein the antibody comprises a heavy chain variable region and a light chain variable region claim 54 , wherein the heavy chain variable region comprises an amino acid sequence selected from the group consisting of SEQ ID NOs:111 and 115 claim 54 , and the light chain variable region comprises an amino acid sequence selected from the group consisting of SEQ ID NOs:113 claim 54 , 117 claim 54 , 119 claim 54 , 122 claim 54 , 124 claim 54 , 126 claim 54 , 128 claim 54 , 130 claim 54 , and 132.58. The ...

NUTRACEUTICAL SUPPLEMENT WITH LACTOBACILLUS RHAMNOSUS

Compositions and uses thereof include an admixture of a probiotic and natural phytochemicals that can affect an individual's stem cells and the inflammatory process to reduce underlying symptoms of various health issues, including arthritis, aging, and physical or athletic injuries, thereby facilitating healing and repair of tissues. 1. A dietary supplement , comprising a composition including a synergistic combination of:{'i': 'Lactobacillus rhamnosus;'}ginger; andvitamin D.2Lactobacillus rhamnosusLactobacillus rhamnosus.. The dietary supplement of claim 1 , wherein the comprises about 10 billion CFU of3. The dietary supplement of claim 1 , wherein the ginger comprises about 500 mg ginger.4. The dietary supplement of claim 1 , wherein the vitamin D comprises about 1 claim 1 ,000 IU of vitamin D.5. The dietary supplement of claim 1 , further comprising curcumin.6. The dietary supplement of claim 6 , wherein the curcumin comprises about 350 mg tumeric root extract.7Boswellia. The dietary supplement of claim 1 , further comprising extract.8BoswelliaBoswellia serrata. The dietary supplement of claim 7 , wherein the extract comprises about 500 mg extract.9Boswellia. The dietary supplement of claim 1 , further comprising curcumin and extract.10. The dietary supplement of claim 1 , further comprising green tea extract.11Camellia sinensis. The dietary supplement of claim 10 , wherein the green tea extract comprises about 500 mg of green tea leaf extract of standardized to about 98% polyphenols claim 10 , 80% catechins claim 10 , and 50% epigallocatechin gallate.12Boswellia. The dietary supplement of claim 1 , further comprising extract and green tea extract.13Epidmedium. The dietary supplement of claim 1 , further comprising extract.14EpidmediumEpimedium sagittatum. The dietary supplement of claim 13 , wherein the extract comprises about 500 mg of extract standardized to about 10% icariin.15Epimedium. The dietary supplement of claim 1 , further comprising curcumin and ...

Stabilization Of Moisture-Sensitive Drugs

Described are stability-enhancing formulations of drugs that are sensitive to moisture. The formulations comprise co-granulates containing a moisture-sensitive drug and an excipient selected from fructose, xylitol, maltitol, and mixtures thereof. Also described are methods of producing a pharmaceutical tablet. The method comprises forming a blend of a moisture-sensitive drug and a first excipient selected from fructose, xylitol, maltitol, and mixtures thereof; spraying the blend with water to produce granules; drying and milling the granules; mixing a second excipient with the granules; and compressing into tablets.

USE OF BIOCOMPATIBLE MICRODROPLETS FOR THE TREATMENT OF ATHEROSCLEROSIS, HEART DISEASE AND STROKE

A pharmacologically acceptable emulsion of biocompatible solvent microdroplets is provided for treating atherosclerosis, heart disease and stroke. Intravenous administration of the biocompatible solvent microdroplets enables the microdroplets to bind and dissolve free cholesterol, cholesterol esters or other fatty compounds within the plaque. A high level of selectivity is ensured from energy principals, by designing the microdroplets to have a low interfacial surface energy when binding to free cholesterol or cholesterol esters in arterial plaque and a high interfacial surface energy when coming into contact with blood cells or endothelial cells along the walls of blood vessels. A review of many compounds which may form the basis of the biocompatible solvent from which the microdroplets are fabricated, as well as their solubility parameters are provided. Furthermore, a specially designed catheter with a micromachined tip is also provided to allow the microdroplets to be generated directly within a blood vessel, as an alternative to emulsification. 1. A method of treating atherosclerosis comprising of administering microdroplets of a biocompatible solvent means intravenously where the said microdroplets are comprised of a hydrophobic water insoluble solution and have a diameter which is sufficiently small to circulate through the cardiovascular system without causing embolisms2. A method of treating atherosclerosis according to where the said microdroplets have solubility properties which are suitable for dissolving one of cholesterol claim 1 , cholesterol esters or a component of arterial plaque.3. A method of treating atherosclerosis according to where the said microdroplets have a relative energy difference (RED) as defined by Hansen Solubility Theory with one of cholesterol claim 2 , cholesterol esters or another component of arterial plaque of less than 1.0.4. A method of treating atherosclerosis according to where the said microdroplets have a relative energy ...

Use Of 2,5-Dihydroxybenzene Compounds And Derivatives For The Treatment Of Rosacea

The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, rosacea. 2. The method of claim 1 , wherein Ris —(CH)aY or —CH═CH—(CH)Y.3. The method of claim 2 , wherein Y is selected from —SOH claim 2 , —SO.X claim 2 , —SOR.4. The method of claim 2 , wherein Ris selected from methyl and ethyl.5. The method of claim 1 , wherein Rand R claim 1 , are claim 1 , independently claim 1 , a substituted or unsubstituted alkylsulfonyloxy group claim 1 , a substituted or unsubstituted arylsulfonyloxy group claim 1 , a substituted or unsubstituted alkylcarbonyloxy group or a substituted or unsubstituted arylcarbonyloxy group.6. The method of claim 1 , wherein Ris selected from methylcarbonyl claim 1 , phenylsulfonyl claim 1 , 4-methylphenylsulfonyl claim 1 , benzylsulfonyl claim 1 , benzyl and phenyl.7. The method of claim 1 , wherein the compound of Formula (I) is selected from the group consisting of:5-hydroxy-2-{[(4-methylphenyl)sulfonyl]oxy}benzenesulfonic acid;2-hydroxy-5-{[(4-methylphenyl)sulfonyl]oxy}benzenesulfonic acid;2,5-bis{[(4-methylphenyl)sulfonyl]oxy}benzenesulfonic acid;2-(acetyloxy)-5-hydroxybenzenesulfonic acid;5-(acetyloxy)-2-hydroxybenzenesulfonic acid;2,5-bis(acetyloxy)benzenesulfonic acid;5-hydroxy-2-{[(4-methylphenyl)sulfonyl]oxy}benzenehomosulfonic acid;2-hydroxy-5-{[(4-methylphenyl)sulfonyl]oxy}benzenehomosulfonic acid;2,5-bis{[(4-methylphenyl)sulfonyl]oxy}benzenehomosulfonic acid;2-(acetyloxy)-5-hydroxybenzenehomosulfonic acid;5-(acetyloxy)-2-hydroxybenzenehomosulfonic acid;2,5-bis(acetyloxy)benzenehomosulfonic acid;5-hydroxy-2-{[(4-methylphenyl)sulfonyl]oxy}benzoic acid;2-hydroxy-5-{[(4-methylphenyl)sulfonyl]oxy}benzoic acid;2,5-bis{[(4-methylphenyl)sulfonyl]oxy}benzoic acid;2-(acetyloxy)-5-hydroxybenzoic acid;5-(acetyloxy)-2-hydroxybenzoic acid;2,5-bis(acetyloxy)benzoic acid;5-hydroxy-2-{[(4- ...

Antimicrobial compounds

Disclosed herein are compounds for use as antimicrobial agents, having a structure of formula (I):

TREATMENT OF STAPHYLOCOCCAL DISORDERS

Materials and methods are provided for treatment and/or prevention of Staphylococcal diseases and disorders such as infection and dermal inflammation. 1Staphylococcus. A method for treating or preventing skin inflammation comprising the step of administering to an individual a prophylactically or therapeutically effective amount of a compound that inhibits delta toxin.2StaphylococcusS. aureus, S. epidermidis, S. saprophyticus, S epidermidis, S. warneriS. intermedius. The method of wherein the delta toxin is a claim 1 , or delta toxin.3. The method of claim 1 , wherein the skin inflammation arises from mast cell-mediated cytokine release.4. The method of claim 1 , wherein the skin inflammation arises from mast cell degranulation.5. The method of any one of claim 1 , claim 1 , or wherein the inflammation is dermatitis.6. The method of wherein dermatitis is atopic dermatitis.76. The method of any one of - wherein the compound inhibits delta toxin activity.8. The method of wherein the compound binds delta toxin.9. The method of wherein the compound inhibits delta toxin interaction with mast cells.10. The method of wherein the compound inhibits delta toxin secretion.11. The method of wherein the compound inhibits delta toxin expression.12. The method of wherein the compound inhibits delta toxin transcription.13. The method of wherein the compound inhibits delta toxin translation.149. The method of any one of - claims 1 , wherein the compound is a polypeptide.15. The method of claim 14 , wherein the compound is an antibody or antigen binding fragment thereof.16. The method of wherein the antibody or antigen binding fragment thereof is isolated from a polyclonal sera.17. The method of wherein the antibody or antigen binding fragment thereof is a monoclonal antibody claim 15 , or fragment thereof.18. The method of claim 15 , wherein the antibody or antigen binding fragment thereof is a humanized antibody claim 15 , a chimeric antibody claim 15 , a hybrid antibody claim 15 , ...

TREATMENT OF STAPHYLOCOCCAL DISORDERS

Materials and methods are provided for treatment and/or prevention of Staphylococcal diseases and disorders such as infection and dermal inflammation. 152-. (canceled)53Staphylococcus aureusS. aureus. A method for inhibiting agr virulence comprising the step of administering to an individual a therapeutically effective amount of a compound that inhibits delta toxin activity.54S. aureusS. aureus. The method of wherein the compound inhibits delta toxin secretion or delta toxin expression.55. The method of wherein the compound binds delta toxin.56. The method of claim 54 , wherein the compound is an anti-delta toxin antibody or antigen binding fragment thereof.57. The method of claim 56 , wherein the antibody or antigen binding fragment thereof is a polyclonal antibody claim 56 , a monoclonal antibody claim 56 , a humanized antibody claim 56 , a chimeric antibody claim 56 , a hybrid antibody claim 56 , a single-chain antibody claim 56 , a single chain Fv antibody claim 56 , an Fab antibody claim 56 , an Fab′ antibody claim 56 , an (Fab′) claim 56 , a diabody claim 56 , or an antigen-binding fragment of a monoclonal antibody.58S. aureus. The method of wherein the delta toxin comprises the sequence set forth in SEQ ID NO:1.59S. aureusS. aureus. The method of claim 53 , wherein the compound specifically binds a carboxy terminal region of the delta toxin (SEQ ID NO:3) or an amino terminal region of the delta toxin (SEQ ID NO:2).60S. aureus. The method of claim 53 , wherein the compound that inhibits agr virulence is an delta toxin inhibitory RNA (RNAi) selected from the group consisting of an antisense RNA claim 53 , a short hairpin RNA (shRNA) claim 53 , a small interfering RNA (siRNA) claim 53 , a microRNA (miRNA) and a ribozyme.61. The method of wherein the compound is selected from the group consisting of HEXESTROL; SR 2640; OCTOCRYLENE|EUSOLEX; ROBUSTIC ACID; CARNOSIC ACID; SODIUM MECLOFENAMATE; DIENESTROL; DICHLOROEVERNIC ACID; TPCK; CPD000466278_1H-Indole-2- ...

ASCORBATE IN THE PREVENTION OF STATIN INDUCED VASCULAR CALCIFICATION

A method of treating or preventing vascular calcification in a patient by administering L-ascorbic acid or ascorbate to the patient and a pharmaceutical composition containing at least one statin and L-ascorbic acid or ascorbate in a dosage form that allows for the concomitant administering of the at least one statin and L-ascorbic acid or ascorbate to a patient. 1. A method of treating or preventing vascular calcification in a patient by administering L-ascorbic acid or ascorbate to the patient.2. The method as claimed in including treating or preventing vascular calcification in a patient treated with statins by administering L-ascorbic acid or ascorbate to the patient.3. A method of treating a patient with L-ascorbic acid or ascorbate claim 1 , wherein the patient is concomitantly treated with at least one statin.4. The method as claimed in including concomitantly administering at least one statin and L-ascorbic acid or ascorbate to a patient for treating or preventing cardiovascular disease.5. (canceled)6. A pharmaceutical composition containing at least one statin and L-ascorbic acid or ascorbate in a dosage form that allows for the concomitant administering of the at least one statin and L-ascorbic acid or ascorbate to a patient.7. The pharmaceutical composition according to claim 6 , wherein the at least one statin and L-ascorbic acid or ascorbate are present as a physical mixture or as separate pharmaceutical compositions intended for concomitant administration to a patient.8. The pharmaceutical composition according to for the prevention or treatment of cardiovascular disease.9. The pharmaceutical composition according to claim 8 , wherein the cardiovascular disease is coronary artery disease claim 8 , cerebrovascular disease or peripheral vascular disease.10. The pharmaceutical composition according to claim 6 , wherein the statin is selected from the group consisting of atorvastatin claim 6 , cerivastatin claim 6 , fluvastatin claim 6 , lovastatin claim 6 ...

GLUCOCORTICOID-RESISTANT LEUKOCYTES AND THEIR USE IN THE TREATMENT OF CANCERS AND VIRUSES

A composition including genetically modified leukocytes is provided, where the genetically modified leukocytes contains a gene or expresses a protein that confers reversible resistance to glucocorticoids. In various aspects, the gene that confers resistance to glucocorticoids encodes 11-beta-dehydrogenase. Administering such genetically modified leukocytes provides leukocyte functions in treating one or more auto-immune, inflammatory, infectious or cancerous diseases or disorders, where the leukocytes are resistant to the effects of glucocorticoids such as alterations of numerous gene transcriptions in the leukocytes. Methods of reversing the glucocorticoid resistance in such genetically modified leukocytes are also provided by administering inhibitors of 11-beta-hydroxysteroid dehydrogenase. Methods of modifying the growth of these genetically modified leukocytes, or identification of candidate inhibitors of glucocorticoid resistance based on these genetically modified leukocytes, are also provided. 1. A population of genetically modified leukocytes wherein at least ten percent of the genetically modified leukocytes express a gene that confers resistance to a glucocorticoid.2. The population of genetically modified leukocytes of claim 1 , wherein the gene that confers resistant to a glucocorticoid is selected from a group consisting of 11-beta-hydroxysteroid dehydrogenase type II (HSD11B2) claim 1 , 11-beta-hydroxysteroid dehydrogenase type I (HSD11B1) claim 1 , and a combination thereof.3. The population of genetically modified leukocytes of claim 1 , wherein the gene encodes corticosteroid 11-beta-dehydrogenase isozyme 2 or the gene comprises a polynucleotide sequence set forth in any one of SEQ ID Nos.: 31 claim 1 , 18 and 32 claim 1 , wherein the 11-beta-dehydrogenase isozyme 2 comprises a polypeptide sequence set forth in any one of SEQ ID Nos.: 3 claim 1 , 33 and 38.4. (canceled)5. (canceled)6. The population of genetically modified leukocytes of claim 2 , ...

Composition Containing Extracts of the Fruit of Hovenia Dulcis THUNB as an Active Ingredient for Preventing and Treating Bone Diseases

The invention relates to a composition containing extracts of the fruit of ., gallocatechin, and methyl vanillate as active ingredients for preventing and treating bone disease. The extracts of the fruit of ., the gallocatechin, and the methyl vanillate according to the present invention are natural materials and thus cause no side effects, and may activate the Wnt/β-catenin pathway to promote bone formation rather than inhibiting bone decomposition, and therefore may be effective in treating osteoporosis and related diseases. In addition, the extracts of the fruit of ., the gallocatechin, and the methyl vanillate according to the present invention may have the effects regrowing hair and preventing and treating wounds and metabolic diseases related to the activation of Wnt/β-catenin pathway. 1Hoveniadulcis Thunb. A composition for the prevention and/or treatment of bone disease comprising . extract as an active ingredient.2. The composition for the prevention and/or treatment of bone disease according to claim 1 , characterized in that the bone disease is any one selected from the group consisting of osteoporosis claim 1 , osteomalacia claim 1 , rickets claim 1 , fibrous osteitis claim 1 , aplastic bone disease and metabolic bone disease.3. The composition for the prevention and/or treatment of bone disease according to claim 1 , characterized in that the extract promotes activity of a Wnt/β-catenin signaling pathway.4. The composition for the prevention and/or treatment of bone disease according to claim 1 , characterized in that the extract promotes bone formation by activating a Wnt/β-catenin signaling pathway.5. The composition for the prevention and/or treatment of bone disease according to claim 1 , characterized in that the bone disease is osteoporosis.6. The composition for the prevention and/or treatment of bone disease according to claim 1 , characterized in that a dosage for the extract ranges from 0.1 to 10 g/kg.7. The composition for the prevention and/ ...

PAIN-RELIEVING TOPICAL COMPOSITIONS

Described herein are compositions for topical use comprising active agents to provide pain relief. The compositions comprise a magnesium salt, a cannabinoid and at least one additional topical analgesic agent. Additionally described herein are methods for treating pain comprising administering to a person in need thereof a composition comprising a pharmaceutically effective amount of a cannabinoid, a magnesium salt and at least one of: methyl salicylate, and menthol. 1. A topical pharmaceutical composition comprising a magnesium salt , a cannabinoid and at least one additional topical analgesic agent , wherein magnesium ion in the composition is present in an amount of 1% to 6% of the composition.2Impatiens biflora. The composition according to wherein the at least one additional topical analgesic agent is selected from the group consisting of: alcohol claim 1 , ethoxylated alkyl alcohol claim 1 , allantoin claim 1 , allyl isothiocyanate claim 1 , aluminum acetate claim 1 , aluminum chloride hexahydrate claim 1 , aluminum hydroxide claim 1 , ammonia solution claim 1 , aspirin claim 1 , benzalkonium chloride claim 1 , benzethonium chloride claim 1 , benzocaine claim 1 , benzyl alcohol claim 1 , bismuth sodium tartrate claim 1 , bithionol claim 1 , butamben picrate claim 1 , calamine claim 1 , camphor claim 1 , camphorated metacresol claim 1 , capsaicin claim 1 , capsicum claim 1 , capsicum oleoresin claim 1 , cetalkonium chloride claim 1 , chloral hydrate claim 1 , chlorobutanol claim 1 , chlorpheniramine maleate claim 1 , creosote claim 1 , cupric sulfate claim 1 , cyclomethycaine sulfate claim 1 , dexpanthenol claim 1 , dibucaine claim 1 , dimethisoquin hydrochloride claim 1 , diperodon hydrochloride claim 1 , diphenhydramine hydrochloride claim 1 , dyclonine hydrochloride claim 1 , ephedrine hydrochloride claim 1 , ergot fluid extract claim 1 , eucalyptus oil claim 1 , eugenol claim 1 , ferric chloride claim 1 , glycerin claim 1 , glycol salicylate claim 1 , ...

Synaptojanin-2 inhibitors for use in the treatment of cancer

Disclosed herein are synaptojanin-2 inhibitors, and novel methods and uses utilizing same for preventing tumor metastasis, treating cancer or inhibiting synaptojanin-2. Compounds disclosed herein include chlorhexidine and pyrvinium, the compound having the formula: and compounds characterized by the general formula: X-L-[(Y)i-(Z)j]-(L-X)k and/or by the general formula: wherein L, X, Y, Z, D, E, i, j and k are as defined herein.

BICYCLIC ANALGESIC COMPOUNDS

Analgesic compounds for treatment of pain or fever that include a bicyclopentane moiety linked to an amine, combinations of the compounds with opioid analgesic drugs, and methods for treating pain or fever by administering a compound described herein. 2. The method of claim 1 , further comprising administering an opioid analgesic.3. The method of claim 2 , wherein the opioid analgesic is selected from the group consisting of morphine claim 2 , codeine claim 2 , hydrocodone claim 2 , oxycodone claim 2 , fentanyl claim 2 , pethidine claim 2 , methadone claim 2 , pentazocine claim 2 , sufentanil claim 2 , levorphanol claim 2 , dihydrocodeine claim 2 , nalbuphine claim 2 , butorphanol claim 2 , tramadol claim 2 , meptazinol claim 2 , buprenorphine claim 2 , dipipanone claim 2 , alfentanil claim 2 , remifentanil claim 2 , oxymorphone claim 2 , tapentadol claim 2 , propoxyphene and hydromorphone.4. The method of claim 1 , wherein the administration is intravenous or topical.5. (canceled)6. The method of claim 1 , wherein the pain is post-operative pain.7. The method of claim 1 , wherein Ris —C(═Y)R; and Ris H.8. (canceled)9. (canceled)10. (canceled)11. The method of claim 1 , wherein Ris H; and Ris H.12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. The method of claim 1 , wherein Ris H.17. (canceled)18. (canceled)19. The method of claim 1 , wherein Ris hydroxy or an unsubstituted (Cto C) alkoxy.20. (canceled)21. (canceled)22. The method of claim 1 , wherein Ris an unsubstituted (Cto C)alkyl.23. (canceled)24. (canceled)25. The method of claim 1 , wherein Ris an unsubstituted mono-cyclic (Cto C) cycloalkyl.26. (canceled)27. (canceled)28. (canceled)29. (canceled)30. (canceled)31. (canceled)32. (canceled)33. The method of claim 1 , wherein Ris NHor an unsubstituted —NC(═O)—Calkyl.34. (canceled)36. (canceled)37. (canceled)38. (canceled)39. (canceled)40. (canceled)41. (canceled)43. The compound of claim 42 , wherein Ris —C(═Y)R; and Ris H.44. (canceled)45. (canceled) ...

INHIBITORS TO TARGET HIV-1 NEF-CD80/CD86 INTERACTIONS FOR THERAPEUTIC INTERVENTION

The compounds of Formula I, II, and III along with their stereoisomers, pharmaceutically acceptable salts, polymorphs, solvates and hydrates thereof are described in the present disclosure. The said compounds restore immune activation in case of infections or a disease associated with an HIV infection in a subject in need thereof.

COMPOSITIONS TO ALLEVIATE PRESYSTEMIC METABOLISM OF OPIOIDS

Compositions comprising one or more opioids and one or more inhibitors of uridine diphosphate glucuronosyl transferases (UGTs) are provided. The inhibitors decrease the presystemic metabolism of the one or more opioids, thereby increasing their bioavailability. The inhibitors are compounds that are designated as Generally Regarded as Safe (GRAS) and/or “Everything Added to Food” (EAF) and/or are dietary supplements. Methods of alleviating pain and of treating opiate addiction in a subject by administering the compositions are also provided. 1. A method of providing one or more opioids to a subject in need thereof so as to enhance systemic bioavailiability of said one or more opioids , comprising the step ofproviding said one or more opioids to said subject in combination with one or more inhibitors of one or more uridine diphosphate glucuronosyl transferases (UGTs), wherein said one or more inhibitors of one or more UGTs are classified as Generally Regarded as Safe (GRAS), “Everything Added to Food” (EAF) and/or as a dietary supplement.2. The method of claim 1 , wherein said one or more opioids includes buprenorphine.3. The method of claim 1 , wherein said one or more opioids includes buprenorphine and naloxone.4. The method of claim 1 , wherein said one or more inhibitors of one or more UGTs inhibits at least one of UGT1A1 claim 1 , UGT1A3 claim 1 , UGT1A4 claim 1 , UGT1A5 claim 1 , UGT1A6 claim 1 , UGT1A7 claim 1 , UGT1A8 claim 1 , UGT1A9 claim 1 , UGT1A10 claim 1 , UGT2A1 claim 1 , UGT2A2 claim 1 , UGT2A3 claim 1 , UGT2B4 claim 1 , UGT2B7 claim 1 , UGT2B10 claim 1 , UGT2B11 claim 1 , UGT2B15 claim 1 , UGT2B17 and UGT2B28.5. The method of claim 1 , further comprising providing said subject with one or both of:i) one or more inhibitors of at least one cytochrome P450 monooxygenase (CYP) selected from the group consisting of CYP1A1, CYP1A2, CYP2A6, CYP2D6, CYP2C9, CYP2C8, CYP2C18, CYP2C19, CYP3A4, CYP3A5 and CYP3A7; andii) one or more inhibitors of at least one ...

PROPOLIS AND CAFFEIC ACID PHENETHYL ESTER AND USES THEREOF

Methods for treating a subject with cancer using a combined therapeutic regimen comprising administering propolis or caffeic acid phenethyl ester (CAPE) in conjunction with other cancer therapeutics are described herein. More particularly, methods for treating subjects with breast cancer using the combined therapeutic regimen are embodied herein. The present methods are particularly useful for treating cancer patients (e.g., breast cancer patients) who are refractory to or who have become refractory to the cancer therapeutic/s used in combination with propolis or CAPE. Propolis or CAPE for use in a combined treatment with other cancer therapeutics for treating cancer patients and compositions comprising propolis or CAPE and other cancer therapeutics are also encompassed herein wherein the ability of propolis or CAPE to act as a histone deacetylase (HDAC) inhibitor is used to advantage. Also encompassed herein are methods and compositions for the treatment of diseases caused by or associated with viral infections. In particular embodiments, methods and compositions for the treatment of viral infections caused by or associated with retroviruses are envisioned, wherein the ability of propolis or CAPE to act as a histone deacetylase (HDAC) inhibitor is also used to advantage. Also encompassed herein are methods and compositions for the treatment of diseases caused by or associated with viral infections. 1. A method for treating a patient with cancer , the method comprising administering to the patient a therapeutically effective amount of propolis or CAPE in combination with an agent used in hormonal therapy of cancer , wherein administration of the propolis or CAPE and the agent reduces the number of cancer cells or the tumor burden in the patient , thereby treating the patient.2. The method of claim 1 , wherein the cancer is breast cancer or prostate cancer.3. The method of claim 2 , wherein the breast cancer is a triple negative breast cancer (TNBC).4. The method of ...

Kung Fu Gu

Kung Fu GU: a topical balm, circulatory, emollient, that helps accelerate the healing of Bruises, reduces swelling and pain as well as increasing circulation. Comprised of Grape seed oil, Bees wax, Rhubarb, Phellodendron, Safflower, Dandelion, Gardenia fruit, Skullcaps, Arnica Montana, Comfrey, Devil's claw, Frankincense, Myrrh, Dragon's Blood resin, Menthol crystals, Wintergreen oil, Birch oil, Lavender oil, Cajuput oil, Clove oil, and the method of preparing same said circulatory emollient balm. 1. Kung Fu GU a topical balm circulatory , emollient that helps accelerate the healing of bruises , and if used in a timely manner will help to prevent the manifestation of a bruise. As well as reduces swelling and pain of strained or sprained tendon and ligaments , as well as increases circulation further more expediting the healing process. Said balm comprising of Grape seed oil , Bees wax Rhubarb , Dandelion , Phellodendron , Safflower , Gardenia fruit , Skullcaps , Arnica Montana , Comfrey , Devil's claw Frankincense , Myrrh , Dragon's Blood , Menthol crystals Wintergreen oil , Birch oil , Lavender oil , Cajuput oil , Clove oil.2. A method for making Kung Fu GU balm , circulatory , emollient comprised of Grape seed oil , Bees wax , Rhubarb , Phellodendron , Safflower , Dandelion , Gardenia fruit , Skullcaps , Arnica Montana , Comfrey , Devil's claw , Frankincense , Myrrh , Dragon's Blood , Menthol crystals , Wintergreen oil , Birch oil , Lavender oil , Cajuput oil , Clove oil. The present invention relates to the recovery and healing of bruises strained or sprained tendon and ligaments more particularly pertains to a new invention that accelerates the healing of bruises and if used in a timely manner will help to prevent the manifestation of a bruise. As well as reducing pain and inflammation of strained or sprained tendon and ligaments, further more increases circulation which also expedites the healing process, additionally serving as an all-purpose massage ...

ROSACEA TREATMENTS USING POLYMETAL COMPLEXES

Described herein are novel methods for the treatment of rosacea which include the step of applying of a composition containing a polymetal complex to an area of the skin afflicted with rosacea and novel regimens using such compounds. 1. A treatment regimen comprising:cleansing at least a portion of an area of skin afflicted with rosacea with an antimicrobial or cleanser;applying a composition containing a polymetal complex to at least a portion of the cleansed area; andapplying a protective composition to at least a portion of the cleansed, and polymetal complex-treated area.2. A treatment regimen as in further comprising the step of applying a composition containing metronidazole to at least a portion of the afflicted area.3. A treatment regimen as in further comprising the step of applying an anti-redness composition to at least a portion of the afflicted area.4. A treatment regimen as in further comprising the step of applying an anti-parasitic compound to at least a portion of the afflicted area.5. The treatment regimen of wherein the anti parasitic product is selected from the group consisting of benzyl benzoate claim 4 , salicylic acid and combinations thereof.6. A treatment regimen as in wherein the polymetal complex comprises a Cu/Zn malonate complex.7. A treatment regimen as in wherein the protective composition comprises a sunscreen.8. A treatment regimen as in wherein the protective composition comprises a compound selected from the group consisting of ZnO claim 1 , Vitamin A claim 1 , Vitamin D and combinations thereof.9. A treatment regimen as in further comprising the step of applying a benzoyl peroxide containing composition to at least a portion of the cleansed claim 1 , and moisturized area of skin.10. A treatment regimen as in further comprising the step of applying a retinoid containing composition to at least a portion of the cleansed claim 1 , area of skin.11. A treatment regimen as in further comprising the step of applying an antibiotic ...

Methods of therapeutic monitoring of nitrogen scavenging drugs

The present disclosure provides methods for evaluating daily ammonia exposure based on a single fasting ammonia blood level measurement, as well as methods that utilize this technique to adjust the dosage of a nitrogen scavenging drug, determine whether to administer a nitrogen scavenging drug, and treat nitrogen retention disorders.

Compositions and Methods for Oral Administration of Cannabinoids and Terpenoids

The present invention relates to oral administration of water soluble cannabinoid and terpenoid concentrates on a flavored fibrous carrier. The compositions described herein provide an alternative to smoked cannabis that also avoid the slow action and unpredictable dosing of edible cannabis preparations. Water soluble concentrates of cannabinoids and terpenoids may be produced by derivatization reactions which are known in the art. Such water soluble concentrates enjoy significantly increased absorption by mucosal membranes of the mouth and may therefore be experienced by the consumer more quickly. Water soluble cannabinoid and terpenoid concentrates may be used in combination with each other and in combination with non-derivatized molecules which provides the user with fast and slow acting components in a single delivery vehicle. 1. An edible cannabis composition comprising:a. water soluble cannabinoids;b. A fibrous carrier;c. A pouch.2. The edible cannabis composition of wherein the water soluble cannabinoids are derivatized carbon 1 phenolic esters.3. The edible cannabis composition of wherein the water soluble cannabinoids are derivatized carbon 3 pentyl side chains.4. The edible cannabis composition of wherein the water soluble cannabinoids may be one or a mixture of cannabinoids.5. The edible cannabis composition of further comprising water soluble terpenes and terpenoids.6. The edible cannabis composition of wherein the water soluble terpenes and terpenoids may be derivatized by reduction to alcohols.7. The edible cannabis composition of wherein the water soluble terpenes and terpenoids may be ester derivatized.8. The edible cannabis composition of wherein the water soluble terpenes and terpenoids may be one or a mixture of terpenes and terpenoids.9. The edible cannabis composition of further comprising non water soluble cannabinoids.10. The edible cannabis composition of further comprising non water soluble terpenes and terpenoids11. The edible cannabis ...

COMPOSITIONS COMPRISING BETA-GLUCOGALLIN AND THERAPEUTIC APPLICATIONS THEREOF IN CONTROLLED KINETICS OF CARBOHYDRATE BREAKDOWN AND MONOSACCHARIDE ABSORPTION

Disclosed are the compositions for the effective regulation of carbohydrate breakdown and absorption. More specifically, the invention discloses compositions containing at least 10% w/w or above of 1-O-galloyl-β-D-glucose (β-glucogallin) and additionally comprising of about 10% w/w to greater than 60% w/w total mucic acid gallates for the effective regulation of carbohydrate breakdown and absorption by the inhibition of enzymes amylase, glucosidase and dipeptidyl peptidase. 1. A method of inhibiting key enzymes involved in carbohydrate metabolism , said method comprising steps of:i) Bringing into contact one of the key enzymes in carbohydrate metabolism with a suitable substrate;ii) Incubating with an effective concentration of a composition containing at least 10% w/w of 1-O-galloyl-β-D-glucose-(β-glucogallin) and 10% w/w to 60% w/w mucic acid gallates under optimal conditions;iii) Reading the change in absorbance using spectrophotometric and fluorimetric methods{'sub': '50', 'claim-text': {'br': None, '% Inhibition=[(absorbance of control−absorbance of inhibitor)/absorbance of control]×100.'}, 'iv) Comparing the absorbance with a control blank and determining the percentage enzyme inhibition (IC) by the said composition containing at least 10% w/w of 1-O-galloyl-β-D-glucose (β-glucogallin) and 10% w/w to 60% w/w mucic acid gallates using the formula2. The method as in claim 1 , wherein the mucic acid gallates are selected from the group consisting of mucic acid 1 claim 1 ,4-lactone 5-O-gallate claim 1 , mucic acid 2-O-gallate claim 1 , mucic acid 6-Methyl ester 2-O-gallate claim 1 , mucic acid 1-Methyl ester 2-O-gallate and ellagic acid.3. The method as in claim 1 , wherein the enzymes are selected from the list consisting of pancreatic α-amylase claim 1 , salivary α-amylase claim 1 , α-glucosidase and dipeptidylpeptidase-4.4. A composition containing at least 10% w/w of 1-O-galloyl-β-D-glucose (β-glucogallin) and 10% w/w to 60% w/w mucic acid gallates for the ...

Compositions And Methods Of Use of Phorbol Esters For Treatment of Stroke

Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment and prevention of stroke and the sequelae of stroke. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools to treat or prevent stroke and the long term effects of stroke in mammalian subjects. 3. The method of claim 1 , wherein the phorbol ester is phorbol 13-butyrate claim 1 , phorbol 12-decanoate claim 1 , phorbol 13-decanoate claim 1 , phorbol 12 claim 1 ,13-diacetate claim 1 , phorbol 13 claim 1 ,20-diacetate claim 1 , phorbol 12 claim 1 ,13-dibenzoate claim 1 , phorbol 12 claim 1 ,13-dibutyrate claim 1 , phorbol 12 claim 1 ,13-didecanoate claim 1 , phorbol 12 claim 1 ,13-dihexanoate claim 1 , phorbol 12 claim 1 ,13-dipropionate claim 1 , phorbol 12-myristate claim 1 , phorbol 13-myristate claim 1 , phorbol 12 claim 1 ,13 claim 1 ,20-tri acetate claim 1 , 12-deoxyphorbol 13-angelate claim 1 , 12-deoxyphorbol 13-angelate 20-acetate claim 1 , 12-deoxyphorbol 13-isobutyrate claim 1 , 12-deoxyphorbol 13-isobutyrate-20-acetate claim 1 , 12-deoxyphorbol 13-phenylacetate claim 1 , 12-deoxyphorbol 13-phenylacetate 20-acetate claim 1 , 12-deoxyphorbol 13-tetradecanoate claim 1 , phorbol 12-tigliate 13-decanoate claim 1 , 12-deoxyphorbol 13-acetate claim 1 , phorbol 12-acetate claim 1 , or phorbol 13-acetate.4. The method of claim 1 , further comprising administering at least one secondary or adjunctive therapeutic agent that is effective in a combinatorial formulation or coordinate treatment regimen with said phorbol ester of Formula I to treat or prevent effects of stroke in said subject.5. The method of claim 4 , wherein the at least one secondary or adjunctive therapeutic agent is administered to said subject in a coordinate administration protocol claim 4 , simultaneously with claim 4 , prior to claim 4 , or after ...

ORAL AND DENTAL HYGIENE AND CLEANING AGENTS WITH IMPROVED ANTI-BACTERIAL ACTION

The anti-inflammatory and preventive action of antimicrobial substances can surprisingly be enhanced by the use of polylactic acid particles. Corresponding advantageous products are in particular oral and dental care and cleaning products that—based on the weight thereof—comprise 0.001 to 25 wt. % polylactic acid particles and 0.00001 to 5 wt. % of at least one antibacterial compound from the groups consisting of the benzoates and/or the parabens and/or the Cu salts and/or the Ag salts and/or triclosan and/or hexetidine. 1. An oral and dental care and cleaning product , comprising , based on the weight thereof ,a) 0.001 to 25 wt. % polylactic acid particles, and a. of the benzoates and/or', 'b. of the parabens and/or', 'c. of the Cu salts and/or', 'd. of the Ag salts and/or', 'e. triclosan and/or', 'f. hexetidine., 'b) 0.00001 to 5 wt. % of at least one antibacterial compound from the groups consisting'}2. The oral and dental care and cleaning product according to claim 1 , wherein the product comprises claim 1 , based on the weight thereof claim 1 , 0.002 to 20 wt. % of polylactic acid particles.3. The oral and dental care and cleaning product according to claim 1 , wherein the product comprises claim 1 , based on the weight thereof claim 1 , 0.004 to 15 wt. % polylactic acid particles.4. The oral and dental care and cleaning product according to claim 1 , wherein the product comprises claim 1 , based on the weight thereof claim 1 , 0.005 to 12.5 wt. % polylactic acid particles.5. The oral and dental care and cleaning product according to claim 1 , wherein the polylactic acid particles have particle sizes of 1 to 1000 μm.6. The oral and dental care and cleaning product according to claim 1 , wherein the polylactic acid particles have particle sizes of 2 to 750 μm.7. The oral and dental care and cleaning product according to claim 1 , wherein the polylactic acid particles have particle sizes of 10 to 500 μm.8. The oral and dental care and cleaning product according ...

Compositions And Methods Of Use Of Phorbol Esters For the Treatment Of Stroke

Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment and prevention of stroke and the sequelae of stroke. Additional compositions and methods are provided which employ a phorbol ester or derivative compound in combination with at least one additional agent to yield more effective treatment tools to treat or prevent stroke and the long term effects of stroke in mammalian subjects. 3. The method of claim 1 , wherein the phorbol ester is phorbol 13-butyrate claim 1 , phorbol 12-decanoate claim 1 , phorbol 13-decanoate claim 1 , phorbol 12 claim 1 ,13-diacetate claim 1 , phorbol 13 claim 1 ,20-diacetate claim 1 , phorbol 12 claim 1 ,13-dibenzoate claim 1 , phorbol 12 claim 1 ,13-dibutyrate claim 1 , phorbol 12 claim 1 ,13-didecanoate claim 1 , phorbol 12 claim 1 ,13-dihexanoate claim 1 , phorbol 12 claim 1 ,13-dipropionate claim 1 , phorbol 12-myristate claim 1 , phorbol 13-myristate claim 1 , phorbol 12 claim 1 ,13 claim 1 ,20-triacetate claim 1 , 12-deoxyphorbol 13-angelate claim 1 , 12-deoxyphorbol 13-angelate 20-acetate claim 1 , 12-deoxyphorbol 13-isobutyrate claim 1 , 12-deoxyphorbol 13-isobutyrate-20-acetate claim 1 , 12-deoxyphorbol 13-phenylacetate claim 1 , 12-deoxyphorbol 13-phenylacetate 20-acetate claim 1 , 12-deoxyphorbol 13-tetradecanoate claim 1 , phorbol 12-tigliate 13-decanoate claim 1 , 12-deoxyphorbol 13-acetate claim 1 , phorbol 12-acetate claim 1 , or phorbol 13-acetate.4. The method of claim 1 , further comprising administering at least one secondary or adjunctive therapeutic agent that is effective in a combinatorial formulation or coordinate treatment regimen with said phorbol ester of Formula I to treat or prevent effects of stroke in said subject.5. The method of claim 4 , wherein the at least one secondary or adjunctive therapeutic agent is administered to said subject in a coordinate administration protocol claim 4 , simultaneously with claim 4 , prior to claim 4 , or after ...

Compositions And Methods Of Use Of Phorbol Esters In The Treatment Of Neoplasms

Methods and compositions containing a phorbol ester or a derivative of a phorbol ester are provided for the treatment of chronic and acute conditions. Such conditions may be caused by disease, be symptoms, treatments, or sequelae of disease. The phorbol esters described are particularly useful in the treatment of neoplastic diseases and/or managing the side effects of chemotherapeutic and radiotherapeutic treatments of neoplastic diseases. 3. The method of claim 1 , wherein the phorbol ester is phorbol 13-butyrate claim 1 , phorbol 12-decanoate claim 1 , phorbol 13-decanoate claim 1 , phorbol 12 claim 1 ,13-diacetate claim 1 , phorbol 13 claim 1 ,20-diacetate claim 1 , phorbol 12 claim 1 ,13-dibenzoate claim 1 , phorbol 12 claim 1 ,13-dibutyrate claim 1 , phorbol 12 claim 1 ,13-didecanoate claim 1 , phorbol 12 claim 1 ,13-dihexanoate claim 1 , phorbol 12 claim 1 ,13-dipropionate claim 1 , phorbol 12-myristate claim 1 , phorbol 13-myristate claim 1 , phorbol 12 claim 1 ,13 claim 1 ,20-triacetate claim 1 , 12-deoxyphorbol 13-angelate claim 1 , 12-deoxyphorbol 13-angelate 20-acetate claim 1 , 12-deoxyphorbol 13-isobutyrate claim 1 , 12-deoxyphorbol 13-isobutyrate-20-acetate claim 1 , 12-deoxyphorbol 13-phenylacetate claim 1 , 12-deoxyphorbol 13-phenylacetate 20-acetate claim 1 , 12-deoxyphorbol 13-tetradecanoate claim 1 , phorbol 12-tigliate 13-decanoate claim 1 , 12-deoxyphorbol 13-acetate claim 1 , phorbol 12-acetate claim 1 , or phorbol 13-acetate.4. The method of claim 1 , wherein the phorbol ester is 12-O-tetradecanoylphorbol-13-acetate.5. The method of claim 1 , wherein the at least one secondary or adjunctive therapeutic agent is administered to said subject in a coordinate administration protocol claim 1 , simultaneously with claim 1 , prior to claim 1 , or after claim 1 , administration of said phorbol ester to said subject.6. The method of claim 1 , wherein the at least one secondary or adjunctive therapeutic agent is selected from the group consisting of: ...