СПОСОБЫ И КОМПОЗИЦИИ ДЛЯ ИНГИБИРОВАНИЯ ПОЛИМЕРАЗЫ

Группа изобретений относится к медицине, а именно к способам и композициям для лечения вирусной инфекции. Для ингибирования вирусных полимераз нуклеиновых кислот субъекту вводят терапевтически эффективное количество соединения формулы I или его фармацевтически приемлемой соли или гидрата. Группа изобретений относится также к способу лечения, подавления и предотвращения вирусной инфекции. Группа изобретений позволяет ингибировать вирусную РНК-полимеразу с подавлением синтеза РНК. 4 н. и 80 з.п. ф-лы, 15 пр., 14 ил., 8 табл.

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ОСЕЛЬТАМИВИР

Группа изобретений относится к области фармацевтики, а именно к гранулированной композиции, содержащей осельтамивир или его фармацевтически приемлемую соль, к способу получения указанной композиции, к способу профилактики или лечения инфекции, вызванной вирусом гриппа A или гриппа B, включающему введение указанной композиции, и к применениям указанной композиции в изготовлении лекарственного средства против инфекции, вызванной вирусом гриппа A или гриппа B, и для лечения инфекции, вызванной указанными вирусами. Гранулированная композиция, содержащая осельтамивир или его фармацевтически приемлемую соль, при этом гранулированная композиция содержит гранулу, включающую ядро, слой лекарственного средства, окружающий ядро и содержащий осельтамивир или его фармацевтически приемлемую соль, и слой покрытия, окружающий слой лекарственного средства и содержащий водорастворимый полимер и плохо растворимый в воде полимер, в которой ядро имеет средний размер частиц (D50) от 150 до 250 мкм. Способ получения ...

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.

АНТИТЕЛА ЧЕЛОВЕКА К PCSK9 ДЛЯ ПРИМЕНЕНИЯ В СПОСОБАХ ЛЕЧЕНИЯ КОНКРЕТНЫХ ГРУПП ИНДИВИДУУМОВ

Настоящая группа изобретений относится к медицине, а именно к терапии, и касается лечения заболеваний, опосредованных экспрессией конвертазы пробелков типа субтилизина/кексина 9 (PCSK9). Для этого вводят фармацевтическую композицию, содержащую антитело, которое специфически связывается с пропротеином конвертазы hPCSK9, или его антигенсвязывающий фрагмент. Фармацевтическая композиция содержит указанное антитело в фиксированных дозах – 75, 150 или 300 мг. Введение композиции осуществляют раз в две или четыре недели. Такой режим введения обеспечивает эффективное лечение указанных заболеваний или патологических состояний при минимальных побочных эффектах. 4 н. и 20 з.п. ф-лы, 6 ил., 2 табл., 4 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.

КОМПОЗИЦИЯ, ВКЛЮЧАЮЩАЯ ДИИНДОЛИЛМЕТАН И РЕТИНОИД ДЛЯ ЛЕЧЕНИЯ КОЖНОЙ ПАТОЛОГИИ

Изобретение относится к способу лечения акне у субъекта, нуждающегося в этом, включающему введение композиции, включающей: (а) первый компонент, включающий 3,3' дииндолилметан, имеющий следующую структуру,и (b) второй компонент, включающий соединение витамина А. Изобретение оказывает синергетическое действие при лечении и предотвращении кожных патологий. 21 з.п. ф-лы, 4 ил., 2 табл.

СЛОЖНЫЕ ЭФИРЫ ДЛЯ ЛЕЧЕНИЯ ОФТАЛЬМОЛОГИЧЕСКИХ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ

Настоящее изобретение относится к офтальмологическим композициям и способам лечения синдрома сухого глаза и других воспалительных офтальмологических заболеваний. В частности, настоящее изобретение относится к композиции, содержащей этерифицированный противовоспалительный липоидный медиатор, который представляет собой эфир противовоспалительного липоидного медиатора, который представляет собой продукт реакции противовоспалительного липоидного медиатора и одноатомного спирта или амида, причем большая часть противовоспалительного липоидного медиатора присутствует в форме эфира. Таким образом, композиции содержат 10% по весу или менее кислотной формы противовоспалительного липоидного медиатора. Противовоспалительные липоидные медиаторы могут быть выбраны из группы, состоящей из полиненасыщенных жирных кислот (например, жирные кислоты Омега-3 и Омега-6), ресольвинов или метаболически стабильного аналога, протектинов или метаболически стабильного аналога, липоксинов или метаболически стабильного ...

ФАРМАЦЕВТИЧЕСКАЯ ФЕНОФИБРАТНАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ВЫСОКИМ БИОЛОГИЧЕСКИМ ПОТЕНЦИАЛОМ, И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

Фармацевтическая композиция фенофибрата немедленного высвобождения для перорального введения содержит гранулы, состоящие из изолированных или агломерированных между собой частиц водорастворимой инертной основы, связанных с частицами микронизированного фенофибрата с размером частиц менее 20 μм в смеси с гидрофильным полимером. Гидрофильный полимер нанесен на поверхность частиц водорастворимой инертной основы. Указанные гранулы могут иметь одну или несколько внешних фаз или слоев или могут быть агломерированными. Способ получения фармацевтической композиции осуществляется путем приготовления суспензии фенофибрата в микронизированной форме в растворе гидрофильного полимера и нанесения суспензии на водорастворимую инертную основу. Фармацевтическая композиция и способ ее получения обеспечивают повышенный биологический потенциал благодаря улучшенному профилю растворения по сравнению с известными композициями. 2 н. и 29 з.п. ф-лы, 2 ил., 1 табл.

ЛЕЧЕБНАЯ СХЕМА И СПОСОБЫ ЛЕЧЕНИЯ ИЛИ УМЕНЬШЕНИЯ НАРУШЕНИЙ ЗРЕНИЯ, СВЯЗАННЫХ С ДЕФИЦИТОМ ЭНДОГЕННЫХ РЕТИНОИДОВ

Группа изобретений относится к медицине, а именно к офтальмологии, и может быть использована для лечения или улучшения нарушения зрения, связанного с дефицитом у субъекта ретиноидов. Для этого вводят терапевтически эффективное количество синтетического производного ретиналя в виде разделенной дозы в течение периода до двух недель с периодом отдыха в течение по меньшей мере месяц с последующим введением дополнительной дозы синтетического производного ретиналя. Это позволяет значимо улучшить или восстановить зрение при минимизации токсичности. 5 н. и 92 з.п. ф-лы, 12 ил., 6 пр.

АРИЛАМИДЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ TNα-АКТИВИРОВАННОЙ РЕПЛИКАЦИИ РЕТРОВИРУСА

Описываются новые соединения общей формулы I Y-C(=O)-NH-CH(R2)-CH2-C(= O)-Z, в которой R2 представляет 3,4-дизамещенный фенил, в котором каждый заместитель выбран независимо из группы, состоящей из нитро, циано, трифторметила, карбэтокси, карбометокси, карбопропокси, ацетила, карбамоила, ацетокси, карбокси, гидрокси, амино, алкила с 1 - 10 атомами углерода, алкокси с 1 - 10 атомами углерода и галогена; Z представляет алкокси с 1 - 10 атомами углерода, бензилокси, амино или алкиламино с 1 - 10 атомами углерода; Y представляет (i) фенил, незамещенный или замещенный одним или более заместителями, каждый из которых независимо друг от друга выбран из группы, состоящей из нитро, циано, трифторметила, карбэтокси, карбометокси, карбопропокси, ацетила, карбамоила, ацетокси, карбокси, гидрокси, амино, алкила с 1 - 10 атомами углерода, алкокси с 1 - 10 атомами углерода и галогена, или (ii) нафтил. Ариламиды общей формулы I являются ингибиторами фактора некроза опухолевых клеток α и могут использоваться ...

КОМПОЗИЦИИ ЛИПИДОВ

Изобретение относится к пищевой промышленности. Обессоленная композиция липидов криля, содержащая: от 30 до 50% масс./масс. фосфолипидов; от 32 до 52% масс./масс. триглицеридов; при этом указанная композиция характеризуется следующими свойствами: содержит менее 0,2% масс./масс. неорганических солей; содержит менее 2 ppm Cu; содержит менее 3 ppm общего мышьяка и содержит от 0,01 до 1% масс./масс. этиловых эфиров. Композиция концентрата фосфолипидов криля, содержащая: от 50 до 85% масс./масс. фосфолипидов; от 5 до 35% масс./масс. триглицеридов; и при этом указанная композиция обладает следующими свойствами: содержит менее 0,2% масс./масс. неорганических солей; содержит менее 2 ppm Cu; содержит менее 3 ppm общего мышьяка и содержит от 0,01 до 1% масс./масс. этиловых эфиров. Композиция липидов криля, содержащая: от 70 до 95% масс./масс. триглицеридов; от 2 до 20% масс./масс. фосфолипидов; при этом указанная композиция обладает следующими свойствами: содержит менее 0,2% масс./масс. неорганических ...

ЛЕЧЕНИЕ ОСТЕОПОРОЗА

Настоящее изобретение относится к применению соединения формулы (I), или его фармацевтически приемлемой соли, или его N-ацильного производного, или его основания Манниха для лечения остеопороза и/или остеопении, а также к фармацевтической композиции, фармацевтическому препарату, комбинированному продукту и вариантам набора, включающим соединение формулы (I). Кроме того, изобретение относится к применению соединения формулы (I) или содержащей его фармацевтической композиции для приготовления лекарственного средства, а также к способу лечения остеопороза и/или остеопении.В формуле (I) Rпредставляет собой алкильную группу, включающую алкильные группы с неразветвленной или разветвленной цепью, содержащие от 1 до 9 атомов углерода; Rпредставляет собой водород; Rпредставлен следующей формулой (II):где неприсоединенная связь представляет собой точку присоединения структурного фрагмента формулы (II) к остатку соединения формулы (I). R, R, R, R, r, s,и n имеют значения, указанные в формуле изобретения ...

ЦЕЛАСТРОЛ И ЕГО ПРОИЗВОДНЫЕ ДЛЯ ЛЕЧЕНИЯ ОЖИРЕНИЯ

Изобретение относится к области медицины и фармацевтики, а именно к применению фармацевтической композиции для индуцирования снижения массы тела и/или снижения содержания жира в организме пациента с предожирением, ожирением или патологическим ожирением, где фармацевтическая композиция содержит эффективное количество соединения следующей структуры:,,,,,илиили его фармацевтически приемлемой соли и фармацевтически приемлемый носитель. Изобретение обеспечивает расширение арсенала средств для снижения массы тела и/или снижения содержания жира в организме. 12 з.п. ф-лы, 47 ил., 1 табл., 8 пр.

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 ...

ЗАМЕЩЕННЫЕ ЦИКЛОАЛКЕНОВЫЕ ПРОИЗВОДНЫЕ

Изобретение относится к новым замещенным циклоалкеновым производным формулы (I) ! ! в которой X и Y представляют собой группу, в которой Х и Y вместе с атомом углерода кольца В, к которому они присоединены, образуют кольцо А, Х и Y вместе представляют заместитель кольца В или Х и Y каждый представляет собой атом водорода. ! Изобретение также относится к лекарственному средству на основе этих соединений, обладающему подавляющим действием в отношении внутриклеточной сигнальной трансдукции или активации клеток, индуцируемой эндотоксином. 2 н. и 19 з.п. ф-лы., 3 табл.

ПРЕБИОТИЧЕСКИЕ КОМПОЗИЦИИ ДЛЯ УХОДА ЗА ПОЛОСТЬЮ РТА, СОДЕРЖАЩИЕ КАРБОНОВЫЕ КИСЛОТЫ

Группа изобретений относится к области применения композиций для ухода за полостью рта для предупреждения заболеваний в ротовой полости. Предлагается применение композиции для ухода за полостью рта, содержащей карбоновую кислоту, где кислота представляет собой монометилсукцинат, для предупреждения одного или нескольких заболеваний пародонта, выбранных из группы, состоящей из гингивита, пародонтита, пери-имплантита, пери-имплантного мукозита, некротизирующего гингивита, некротизирующего пародонтита и кариеса. Также предлагается способ предупреждения одного или более заболеваний пародонта, выбранных из группы, состоящей из гингивита, пародонтита, пери-имплантита, пери-имплантного мукозита, некротизирующего гингивита, некротизирующего пародонтита и кариеса у субъекта, причем способ включает приведение полости рта субъекта в контакт с композицией для ухода за полостью рта, содержащей эффективное количество карбоновой кислоты, где карбоновая кислота представляет собой монометилсукцинат. Показано ...

НЕЙТРАЛИЗУЮЩИЕ АНТИТЕЛА К ВИРУСУ ГРИППА А И ПУТИ ИХ ПРИМЕНЕНИЯ

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ИМПЛАНТАНТЫ НАЗОЛАКРИМАЛЬНОЙ ДРЕНАЖНОЙ СИСТЕМЫ ДЛЯ МЕДИКАМЕНТОЗНОЙ ТЕРАПИИ

... 1. Глазной имплантант, вставляемый в глазную полость, где глазной имплантат включает: ! центрально расположенный элемент, простирающийся вдоль продольной оси, от части проксимального конца к части дистального конца и имеющий промежуточную часть между ними; и ! способную к расширению, не способный к набуханию в жидкости удерживающую структуру, сцепленную с или располагающуюся вокруг части центрально расположенного элемента, причем удерживающая структура сконфигурована так, что когда она имплантирована в окулярный просвет, удерживающая структура расширяется для смещения, по крайней мере, части удерживающей структуры, расположенной рядом с промежуточной частью или частью дистального конца центрально расположенного элемента против, по крайней мере, части стенки окулярного просвета. ! 2. Глазной имплантат по п.1, где удерживающая структура расширяется из конфигурации с первым сечением, пригодной для вставления в глазную полость до конфигурации со вторым сечением большего диаметра для смещения ...

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... 1. Композиция для применения при лечении кожной патологии, композиция, включающая:(a) первый компонент, включающий замещенное или незамещенное соединение дииндолилметана; и(b) второй компонент, включающий замещенное или незамещенное ретиноидное соединение.2. Композиция по п.1, в котором композиция включает дополнительный компонент, выбранный из одного или более из следующих: дополнительное замещенное или незамещенное ретиноидное соединение, антибиотическое соединение, замещенное или незамещенное соединение азелаиновой кислоты, противозачаточное соединение для перорального введения, сера, серосодержащее соединение, замещенное или незамещенное соединение салициловой кислоты, замещенное или незамещенное соединение резорцина, растительный продукт, минерал, витамин и нутрицевтический продукт.3. Композиция по п.1 или 2, в котором первый компонент включает соединение дииндолилметана, обладающее следующей структурой:,в которой группы R могут одинаковыми или различными и выбранными из атомов водорода ...

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КОМПОЗИЦИИ И СПОСОБЫ ПРИМЕНЕНИЯ ФОРБОЛОВЫХ СЛОЖНЫХ ЭФИРОВ

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СЛОЖНЫЕ ЭФИРЫ ДЛЯ ЛЕЧЕНИЯ ОФТАЛЬМОЛОГИЧЕСКИХ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ

АНТИКОАГУЛЯНТНЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ

... 1. Применение соединения формулы (I):в которойRпредставляет собой водород, галоген, циано, трифторметил, нитро, -OR, SR, SOR, -SOR, -SONRR, -NRR, -NRCOR, -NRCOR, -COR, -COR, -CONRRили углеводородную группу, содержащую линейный, разветвленный либо циклический фрагмент, каждый содержащий до 18 атомов углерода, либо гетероциклическую группу, содержащую до 18 атомов углерода и по меньшей мере один гетероатом;R, независимо в каждом случае, представляет собой водород, галоген, циано, трифторметил, нитро, -OR, SR, SOR, -SOR, SONRR, -NRR, -NRCOR, -NRCOR, -COR, -COR, -CONRRили углеводородную группу, содержащую линейный, разветвленный либо циклический фрагмент, каждый содержащий до 18 атомов углерода, либо гетероциклическую группу, содержащую до 18 атомов углерода и по меньшей мере один гетероатом;Rпредставляет собой углеводородную группу, содержащую линейный, разветвленный или циклический фрагмент, каждый содержащий до 18 атомов углерода и замещенный по меньшей мере одним заместителем, включая заместитель ...

ФАРМАЦЕВТИЧЕСКАЯ ФЕНОФИБРАТНАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ВЫСОКИМ БИОЛОГИЧЕСКИМ ПОТЕНЦИАЛОМ, И СПОСОБ ЕЕ ПОЛУЧЕНИЯ

... 1. Композиция фенофибрата немедленного высвобождения, содержащая водорастворимую инертную основу и фенофибрат в микронизированной форме с размером частиц менее или равным 20 μм, обладающий растворимостью по меньшей мере 10% за 5 мин, 20% за 10 мин, 50% за 20 мин и 75% за 30 мин, измеренной с помощью способа вращающейся лопасти со скоростью вращения 75 об/мин в соответствии с Европейской Фармакопеей, в растворяющей среде, состоящей из воды с 2 мас.% полисорбата 80 или 0,025 М лаурилсульфата натрия. 2. Композиция по п.1, в которой фенофибрат обладает размером частиц меньшим или равным 10 μ м. 3. Композиция по п.1 или 2, в которой фенофибрат присутствует в количестве от 5 до 50 мас.%. 4. Композиция по п.3, в которой фенофибрат присутствует в количестве от 20 до 45 мас.%. 5. Композиция по одному из пп.1-4, содержащая дополнительно гидрофильный полимер. 6. Композиция по п.5, в которой гидрофильный полимер выбран из: поливинилпирролидона, поливинилового спирта, гидроксипропилцеллюлозы, гидроксиметилцеллюлозы ...

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 ...

OXYBUTYNINFORMULIERUNGEN MIT GESTEUERTER FREISETZUNG

VERFAHREN ZUR VERHINDERUNG DER FREISETZUNG VON HISTAMIN

TETRAHYDRONAPHTALINDERIVATE, VERFAHREN UND ZWISCHENPRODUKTE ZU DEREN HERSTELLUNG SOWIE DIESE ENTHALTENDE ARZNEIMITTEL.

ESTER VON CYCLOPROPANCARBONSAEURE UND 2,3-DIHYDRO-4-PHENYL-1H-INDEN-2-OL, IHRE HERSTELLUNG, IHRE VERWENDUNG ALS PARASITIZIDE UND SIE ENTHALTENDE ZUSAMMENSETZUNGEN.

Verfahren zur Herstellung von 3-trans-Dimethylamino-4-phenyl-4-trans-carbaethoxycyclohexen-(1) neben 3-cis-Dimethylamino-4-phenyl-4-cis-carbaethoxy-cyclohexen-(1)

Alkanolaminderivate

SYNTHESE UND VERWENDUNG VON RETINOID-VERBINDUNGEN MIT NEGATIVER HORMON UND/ODER ANTAGONISTAKTIVITÄT

EIN KRÄUTERMOLEKÜL ALS POTENTIELLES ANTI-LEUKÄMISCHES ARZNEIMITTEL

STABILE EMULSIONSZUBEREITUNGEN

Kosmetische und/oder dermatologische Wirkstoffkombination

Kosmetische und/oder dermatologische O/W-Emulsion mit einem Gehalt an Retinoiden, Glycerylstearat und Cyclodextrinen.

Verwendung von Boswelliasäure zur Behandlung von Hirntumoren

The invention concerns the use of pure boswellic acid, a physiologically acceptable salt, a derivative, a salt of this derivative or a plant preparation containing boswellic acid to produce a medicament for the treatment of brain tumours.

Sustained release oral pharmaceutical compositions of dicycloverine

Anti-Adherent Formulation Including a Cationic or Nonionic Acrylate Co-Polymer

HYDRATROPIC ACID DERIVATIVES AND PREPARATION THEREOF

... 1435050 Hydratropic acid derivatives MERCK PATENT GmbH 25 Nov 1974 [26 Nov 1973] 50946/74 Heading C2C Novel compounds I in which R1 is H, C 1-4 alkyl, 2-acetamidoethyl, 1 - methyl - 4 - piperidyl or 2,3 - dihydroxypropyl, R2 is Hal, phenyl, 4-Hal-phenyl, 4-Halphenoxy, 4 - Hal - phenoxymethyl, 1,2,3,4- tetrahydro - 1 - naphthyl, 1 - pyrryl, piperidino, isoindolino, 1,2,3,4-tetrahydroquinolino, 1,2,3,4 - tetrahydro - 4 - quinolyl or 1 - methyll,2,3,4-tetrahydro-4-quinolyl and Hal is F, Cl or Br, and their physiologically acceptable salts with acids or bases, are prepared by (a) condensing a phenol II or a salt thereof, with a compound III in which X is Cl, Br, I, OH or esterified OH, or (b) methylating a compound IV or a metal derivative thereof, or (c) treating a compound V in which Z is a functionally modified carboxyl group but is different from COOR1, with a solvolysing agent. The resulting compound I may be treated to convert the R1 radical thereof ...

Pharmaceutical and cleaning compositions and their use in treatment

Composition

Foodstuff additive

A foodstuff additive contains as active ingredient proadifen and/or lysolecithin which on administration is incorporated into stomach cell membranes to increase the porosity of the membrane. This said increase has the effect of increasing the nutrient absorption into the blood supply and is of particular use to body builders and athletes for the purposes of weight gain and of altering the ratio in the body of fat to muscle. The additive can also enhance the yield of milk when taken by lactating women.

A combination composition comprising paracetamol and ibuprofen

A combination composition comprising paracetamol and ibuprofen

Polyprenyl compounds, processes for the production thereof and medicines containing same

Non-steroidal, anti-inflammatory drugs are disclosed which are polyprenyl alcohol esters of indolyl lower carboxylic acids, phenyl lower carboxylic acids, acetyl salicylic acid, anthranilic acid and derivatives thereof.

PREPARATION OF ESTERS OF DIETHYLENE GLYCOL

1,4-Dihydro-1,4-dioxonaphtalene derivatives for the treatment of osteoporosis

Stabilization of pleuromutilin derivatives against oxidation by sodium hypochlorite in aqueous solution

A composition and method which provides a compound of the formula I: (I) wherein either R1 is ethyl or vinyl. n is an integer from 2 to 5 and each of R2 and R3 is alkyl of 1 to 10 carbon atoms. Also provided is a hypochlorite scavenger in solution with the formula I compound which stabilizes the compound against oxidation by sodium hypochlorite. A preferred solution contains the compound of formula I wherein R1 is vinyl, R2 and R3 are ethyl as a salt of hydrogen fumarate i.e. tiamulin hydrogen fumarate. The solution is added to drinking water which is fed to farm animals as treatment for mycoplasma infection.

Synergistic antibiotic composition and process for its preparation

The invention relates to a synergistic antibiotic composition useful for the treatment of respiratory, gastrointestinal or urinary infections and septicaemia of domestic animals. The composition comprises tiamulin hydrogen fumarate and an aminoglycoside antibiotic or a pharmaceutically acceptable salt thereof in a weight ratio of 5:1 to 1:5. The active components are admixed or diluted with a carrier, used in veterinary therapy, in a weight ratio of 1:1 to 1:50 and formulated for oral or parenteral application.

SYNERGISTIC ANTIBIOTIC COMPOSITION

1,4-Dihydro-1,4-dioxonaphtalene derivatives as anticoagulants

A compound of formula (I), or a pharmaceutically acceptable salt, tautomer or prodrug thereof, for use as an anticoagulant. R1or R2represents hydrogen, halogen, cyano, trifluoromethyl, nitro, ORa, SRa, SORa, SO2Ra, SO2NRaRb, NRaRb, NRaCORb, NRaCO2Rb, CORa, CO2Ra, CONRaRb, Ak or Het. n = 1-4. R3represents a hydrocarbon group comprising a straight chain, branched or cyclic group each containing up to 18 carbon atoms, and being substituted by at least one moiety including a CO2Rasubstituent. Raand Rbindependently represent hydrogen, Ak or Het. Ak represents a hydrocarbon group comprising a straight chain, branched or cyclic group each containing u to 18 carbon atoms. Het represents a heterocyclic group containing up to 18 carbon atoms and at least one heteroatom. Preferred are (4E)-6-(1,4-dihydro-2-methyl-1,4-dioxonaphthalen-3-yl)-4-methylhex-4-enoic acid; (2E)-6-(1,4-dihydro-2-methyl-1,4-dioxonaphthalen-3-yl)-2-methylbut-2-enoic acid; 8-(1,4-dihydro-2-methyl-1,4-dioxonaphthalen-3-yl)octanoic ...

Stable prostaglandin-containing compositions

A-HALOMETHYLAMINO COMPOUNDS AND THEIR PREPARATION

MEDICAMENTS

TOXIC AGENT PROTECTIVE COMPOUNDS

A topical parasiticide composition

Inhibitors of influenza viruses replication

Topical compositions comprising fipronil and permethrin and methods of use

Synthetic excitatory amino acids

Synthetic excitatory amino acids.

The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.

Process for combatting the protozoa responsible for illness of vertebrates and compositions intended for putting the process to work.

A process for combatting illnesses and endemics transmitted to living beings by protozoa. The process consists in applying a sufficient quantity of a compound of the pyrethrinoid type in the place where the protozoa are foundin order to prevent the development of protozoa. The invention is also concerned with compositions intended for putting the process into operation.

Use of hydroxybenzoic acid ester and analogues forthe manufacture of a mendicament for the preventi on and treatment of virus infection

A topical parasiticide composition

PROCESS FOR COMBATING THE PROTOZOA RESPONSIBLE FOR ILLNESS OF VERTEBRATES AND COMPOSITION INTENDED FOR PUTTING THE PROCESS TO WORK

Synthetic excitatory amino acids

Inhibitors of influenza viruses replication

Topical compositions comprising fipronil and permethrin and methods of use

Diclofenac composition

A topical parasiticide composition.

Compounds and methods for treating influenza.

Inhibitors of influenza viruses replication

Parasiticidal compositions comprising an isoxazoline active agent, methods and uses thereof

Compounds and methods for treating influenza.

New compositions intended for the fight against the parasites of the warm-blooded animals.

Process of fight against the protozoa responsible for diseases for vertebrate and compositions intended for the implementation of this process.

New use of pyrethrinoid esters like agent of fight against the parasites of the warm-blooded animals.

Potentiation of pyrethrinoid by the useful crotamiton in the treatment of the pediculosis

Method of preparation of pharmaceutical compositions containing of the pyrethrinoid ones.

Topical compositions comprising fipronil and permethrin and methods of use

Diclofenac composition

Compounds and methods for treating influenza.

Use of glycyrrhetinic acid, glycyrrhizic acid and related compounds for prevention and/or treatment of pulmonary fibrosis

The present invention pertains to novel uses of glycyrrhetinic acid (GA), glycyrrhizic acid (GLA) and related compounds for prevention and/or treatment of pulmonary fibrosis, in particular, irradiation-induced pulmonary fibrosis. Also embodied are therapeutic uses of prodrugs, metabolites, derivatives (e.g., acids, esters and ethers), and salts of glycyrrhetinic acid (GA) and glycyrrhizic acid (GLA). The present invention also provides for therapeutic or pharmaceutical compositions comprising a compound of the invention in a form that can be combined with a pharmaceutically acceptable carrier.

(R)-(-)-1,2-propanediol compositions and methods

Short-chain 2- to 3-carbon alcohols are used as solvents for cooling agents in the preparation of topical therapeutic and cosmetic formulations. Some of these alcohols, especially ethanol, inhibit the ability of the cooling agent to activate its target receptor. In one embodiment of this invention, (R)-1,2-propanediol is used as an alcoholic solvent for the topical delivery of cooling agents to biological surfaces. This propanediol enantiomer has a minimum inhibitory effect on cooling with respect to standard 2- to 3-carbon alcoholic solvents, and functions to substantially protect the agent's cooling activity from inhibition when in the presence of a short-chain alcohol.

Antiviral treatments

The invention provides unit dosage forms, kits, and methods useful for treating viral infections.

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 of Treating Fragile X Syndrome

Subjects having fragile X syndrome are treated with a composition that includes gamma-aminobutyric acid agonists. The gamma-aminobutyric acid agonist (GABA) can be a GABA(B) agonist, such as baclofen, including racemic and R-baclofen.

Treatment of eye discomfort by topical administration of a cooling agent to the external surface of the eyelid

The present invention pertains generally to the field of ocular treatment, and more specifically to the use of a liquid cooling agent composition comprising a cooling agent for the treatment of (e.g., the alleviation of symptoms of; the amelioration of) eye discomfort. The preferred cooling agent is (1R,2S,5R)-2-isopropyl-5-methyl-cyclohexanecarboxylic acid 2,3-dihydroxy-propyl ester (referred to herein as CPS-030). The liquid cooling agent composition is topically administered to at least a portion of the external surface of the eyelid (preferably the closed eyelid) of the eye to be treated. Preferably, the liquid cooling agent composition is carried on or in a wipe, pad, or towelette, for example, an eye wipe.

Compositions and methods relating to proliferative diseases

Anti-cancer compositions and methods are described herein. In particular, compositions including one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described. Methods for treatment of pathological conditions particularly cancer, in a subject using one or more of leelamine, a leelamine derivative, abietylamine, an abietylamine derivative, and an abietic acid derivative are described herein.

Use of jasmonate to treat bladder dysfunction

A formulation or composition contractility comprising jasmonate for modulating bladder and/or treating bladder dysfunction, particularly an overactive bladder in a mammal, particularly a human and use of jasmonate for treating bladder dysfunction is provided.

Compositions and improved soft tissue replacement methods

The specification discloses compositions and methods for treating a soft tissue defect of an individual.

Pharmaceutical composition including sunflower extract, preparative method and use thereof

A pharmaceutical composition containing sunflower extract comprises the extract of total flavonoids from leaves, heads or stems of sunflower ( Helianthus annuus L.), in which the content of total flavonoids is 50-90%. Preferably, the pharmaceutical composition comprises the extract of total terpenes and/or the extract of total organic acids. The pharmaceutical composition is used as an active ingredient in manufacture of foods, functional foods or medicaments for preventing or treating hypertension.

Compositions and methods for lowering triglycerides without raising ldl-c levels in a subject on concomitant statin therapy

In various embodiments, the present invention provides compositions and methods for treating and/or preventing cardiovascular-related diseases in subject in need thereof.

COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISEASES

In one aspect of the present invention, a pharmaceutical composition for treating a metabolic disease in a mammalian subject includes a therapeutically effective amount of (R)-all-trans-13,14-dihydroretinol and a pharmaceutically acceptable carrier or diluent. In another aspect of the present invention, pharmaceutical composition for treating a metabolic disease in a mammalian subject includes a therapeutically effective amount of (S)-all-trans-13,14-dihydroretinol and a pharmaceutically acceptable carrier or diluent. In a further aspect of the present invention, a method is provided for treating a metabolic disease in a mammalian subject. The method includes administering to the subject a pharmaceutical composition comprising at least one all-trans-13,14-dihydroretinoid, all-trans-13,14-dihydroretinoid derivative, or agent capable of modulating the level of at least one all-trans-13,14-dihydroretinoid or all-trans-13,14-dihydroretinoid derivative in the subject. 123-. (canceled)24. A method of treating obesity or an obesity related condition in a mammalian subject , the method comprising administering to the subject a therapeutically effective amount of a pharmaceutical composition comprising at least one all-trans-13 ,14-dihydroretinoid , all-trans-13 ,14-dihydroretinoid derivative , all-trans-retinol:all-trans-13 ,14-dihydroretinol saturase or a compound that modulates the level and/or activity of all-trans-retinol:all-trans-13 ,14-dihydroretinol saturase , wherein the obesity or obesity related condition is associated with improved glucose tolerance , abnormal fasting response manifested by visceral fat retention , or decreased hepatic triglyceride levels.25. The method of claim 24 , the pharmaceutical composition being administered to at least one cell expressing G-protein-coupled receptor 40 (GPR40) and/or a polynucleotide encoding GPR40.26. The method of claim 24 , the pharmaceutical composition promoting lipolysis in the subject.27. The method of claim 24 , ...

METHODS FOR THE TREATMENT AND PREVENTION OF AGE-RELATED RETINAL DYSFUNCTION

A method of treating or preventing age-related retinal dysfunction involves administering to a patient a pharmaceutically effective amount of a synthetic retinal derivative repeatedly over a duration of at least about 3 months. Effective synthetic retinal derivatives include 9-cis-retinyl esters, 11-cis-retinyl esters, derivatives and congeners thereof, and combinations thereof. Suitable ester substituents include carboxylates of C-Cmonocarboxylic acids and C-Cpolycarboxylic acids. 144-. (canceled)45. A method of treating age-related retinal dysfunction in a human subject , comprising:administering a synthetic retinal derivative to an eye of the human subject, wherein the synthetic retinal derivative supplements or replaces endogenous 11-cis retinal in the eye, and wherein the synthetic retinal derivative is a cis-retinoid administered as a long term dosage regimen.46. The method of claim 45 , wherein the long term dosage regimen is about once a month over a period of at least four months.47. The method of claim 45 , wherein the long term dosage regimen is administered intermittently for about 3 months or longer.48. The method of claim 45 , wherein the long term dosage regimen is administered intermittently for about 6 months or longer.49. The method of claim 45 , wherein the long term dosage regimen is administered intermittently about once a day to about once every two months.50. The method of claim 45 , wherein the age-related retinal dysfunction is age-related macular degeneration.51. The method of claim 45 , wherein the age-related retinal dysfunction comprises impairment in rod-mediated dark adaptation after light exposure claim 45 , impairment in night vision claim 45 , impairment in contrast sensitivity or age-related macular degeneration.52. The method of claim 45 , wherein the synthetic retinal derivative is an 11-cis-retinal or a 9-cis-retinal that has a formula according to one of formulae I claim 45 , II claim 45 , III claim 45 , IV claim 45 , V claim ...

RETINAL DERIVATIVES AND METHODS FOR THE USE THEREOF FOR THE TREATMENT OF VISUAL DISORDERS

Compositions of and methods for using synthetic retinal derivatives as retinoid replacements and opsin agonists are provided. 184-. (canceled)85. A pharmaceutical ophthalmological composition for use in treating a visual disorder due to a deficiency of 11-cis retinal in an eye of a human subject , comprising:a synthetic retinyl ester, wherein when the synthetic retinyl ester is administered to the human subject a functional opsin/chromophore complex is formed in the eye; and, a pharmaceutically acceptable vehicle.86. The pharmaceutical ophthalmological composition of claim 85 , wherein the endogenous 11-cis retinal deficiency is associated with Retinitis Pigmentosa (RP) claim 85 , Leber Congenital Amaurosis (LCA) claim 85 , Retinitis Punctata Albesciens claim 85 , Congenital Stationary Night Blindness claim 85 , Fundus Albipunctatus claim 85 , Age-Related Macular Degeneration claim 85 , loss of night vision or contrast sensitivity.87. The pharmaceutical ophthalmological composition of claim 85 , wherein the human subject has a mutation selected from an RPE65 mutation and an LRAT mutation.88. The pharmaceutical ophthalmological composition of claim 85 , wherein the composition is formulated for local administration to an eye of a human subject.89. The pharmaceutical ophthalmological composition of claim 85 , wherein the composition is formulated for oral administration claim 85 , systemic administration claim 85 , time release administration claim 85 , controlled release administration or prophylactic administration.90. The pharmaceutical ophthalmological composition of claim 85 , wherein the composition is formulated for oral administration and the pharmaceutical acceptable vehicle is canola oil.91. The pharmaceutical ophthalmological composition of claim 89 , wherein the oral administration is in a unit dosage of about 1.0 to about 1000 mg or about 10 to about 250 mg of the retinyl ester.92. The pharmaceutical ophthalmological composition of claim 88 , wherein the ...

INDUCING INACTIVATION OF FIBROGENIC MYOFIBROBLASTS

Provided are methods of treating fibrotic conditions in a subject and diagnostic methods for determining fibrosis and appropriate treatments for the fibrosis by the identification of specific subsets of fibrogenic myofibroblasts. 1. A method for reducing one or more symptoms of fibrosis in a subject , comprising administering to said subject a therapeutic amount of one or more compounds that upregulate one or more of Hspa1a/b gene , PPARα , PPARγ , HSP70 , HSP40 , Hyaluronan synthase 1 , GATA2 , C/EBPa , BMPS , septin 4 , Bambi , cathepsin S and H , neural proteins: synaptogyrin 1 , synaptotagmin XIII , GFAP , transcription factors: Spi-C transcription factor (spi/PU.1 related) , Spi-B transcription factor (spi-1/PU.related) , PU.1-IRF , IRF-1 and 3 and 5 , ISRE , Stat1 , Pax5 , Mafk2 , ISGF3-g1; BL34 regulator of G-protein signaling 1 , or Rnd1-Rho family GTPase , in an activated fibrogenic myofibroblast cell or fibrogenic myofibroblast-like cell in an amount sufficient to decrease or inhibit the fibrosis.2. The method of wherein the one or more compounds upregulate PPARγ claim 1 , PPARα and/or Hspa1a/b genes.3. The method of claim 1 , wherein the fibrotic condition is a fibrotic condition of the lung claim 1 , liver claim 1 , heart claim 1 , kidney claim 1 , skin claim 1 , gastrointestinal tract or a combination thereof.4. The method according to claim 3 , wherein the fibrotic condition of the liver is chosen from fatty liver disease claim 3 , steatohepatitis claim 3 , primary and secondary biliary cirrhosis claim 3 , cirrhosis claim 3 , alcohol induced liver fibrosis claim 3 , biliary duct injury claim 3 , biliary fibrosis claim 3 , hepatic fibrosis associated with hepatitis infection claim 3 , autoimmune hepatitis claim 3 , non-alcoholic fatty liver disease or progressive massive fibrosis.5. The method according to claim 1 , wherein the compound is selected from one or more of PPARα agonist claim 1 , PPARγ agonist claim 1 , Hsp70 upregulator claim 1 , HSP40 ...

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.

Topical Composition and Use Thereof for the Prophylaxis and the Treatment of Defects Connected to Inflammatory Dermopathies

A topical composition and its use for the prophylaxis and the treatment of defects connected to inflammatory dermopathies. Particularly, a topical composition including at least an alum, 18-β-glycyrrhetic acid and/or one derivative thereof, and vitamin A and/or one derivative thereof, and the use of such composition for the prophylaxis and the treatment of inflammatory dermopathies, preferably of the seborrhoeic dermatitis and of those affections in which the presence of an excess of sebum occurs. 1. A topical composition comprising:a) at least an alum selected among the group consisting of aluminium and an alkaline metal or ammonium double sulfates;b) 18-β-glycyrrhetic acid and/or one salt and/or organic or inorganic derivative thereof;c) vitamin A and/or one derivative thereof; andd) at least a cosmetically acceptable excipient or vehicle.2. A composition according to claim 1 , comprising:a) 0.1-97.0% by weight of at least an alum;b) 0.1-1.0% by weight of 18-β-glycyrrhetic acid and/or one salt and/or organic or inorganic derivative thereof;c) 0.1-1.0% by weight of vitamin A and/or one derivative thereof, simple and/or hydrogenated and/or a retinoic acid ester or derivatives thereof and/or mixtures obtained by reacting retinol and saccharomycetes polypeptides; andd) at least the cosmetically acceptable excipient or vehicle.3. A composition according to claim 1 , comprising:a) 0.3-80.0% by weight of at least an alum;b) 0.2-0.8% by weight of 18-β-glycyrrhetic acid and/or one salt and/or organic or inorganic derivative thereof;c) 0.2-0.8% by weight of vitamin A and/or one derivative thereof, simple and/or hydrogenated and/or a retinoic acid ester or derivatives thereof and/or mixtures obtained by reacting retinol and saccharomycetes polypeptides; andd) at least the cosmetically acceptable excipient or vehicle.4. A composition according to claim 1 , comprising:a) 0.5-60.0% by weight of at least an alum;b) 0.3-0.6% by weight of 18-β-glycyrrhetic acid and/or one salt and ...

ANTIMICROBIAL COMPOSITION

An antimicrobial composition containing coniferous resin acids and/or their derivates, an antimicrobial polymer composition including coniferous resin acids and/or their derivates and processes for preparing thereof, and the use of the derivates of coniferous resin acids as an antimicrobial agent. 1. A process for manufacturing a polymer composition , comprising impregnation of coniferous resin acids and/or their derivates in a solution into a polymer composition matrix for a sufficient time to render the polymer composition antimicrobial.2. The process of claim 1 , wherein the amount of coniferous resin acids and/or their derivates is 0.1 to 20% w/w or w/v of the polymer composition.3. The process of claim 1 , wherein the polymer composition is natural or synthetic fibre or fabric claim 1 , thermosetting plastic or thermoplast claim 1 , rubber claim 1 , or silicone.4. The process of claim 3 , wherein the polymer composition is polypropylene fibre.5. The process of claim 3 , wherein the polymer composition is epoxy resin.6. The process of claim 3 , wherein the polymer composition isa paint,a plastic cloth for protection of surgical sites, such as skin, and injuries,coatings to be spread onto the skin or tissues,a coating for suture thread, hooks and clamps,a protective glove, hair cover, apron and coatings thereof,a plaster, wound dressing,a biomedical device, like a plastic catheter such as an urinary catheter and drain, hose, cannula and coatings thereof,a bandage for surgical wounds and skin openings made during operations, e.g. colostomy, ileostomy,artificial plastic parts for the body or body cavities like prostheses and artificial transplants, oral prostheses, dental bridges, implants, tubes, nails, and coatings thereof,coatings for artificial parts to be placed into the body and made of metal or material other than plastic, plasters, splints, supporting prostheses, protective bandages, shoes, insoles and coatings thereof.7. The process of claim 6 , wherein ...

TREATING CANCER WITH STATINS AND COMPOUNDS HAVING DIPYRIDAMOLE ACTIVITY

The disclosure pertains to methods of treating a cancer comprising administering to a subject in need thereof an effective amount of a statin in combination with an effective amount of a dipyridamole and/or a compound that has dipyridamole activity. 1. A method of treating a cancer or precancerous disorder comprising administering to a subject in need thereof: 1) a statin , and 2) a compound that increases cAMP levels.23.-. (canceled)4. The method of claim 1 , wherein the statin is selected from a compound of Formula Ia or Ib and/or mixtures thereof claim 1 , optionally selected from lovastatin claim 1 , simvastatin claim 1 , atorvastatin claim 1 , fluvastatin claim 1 , rosuvastatin claim 1 , pravastatin claim 1 , and pitavastatin.5. The method of claim 1 , comprising administering:lovastatin in combination with dipyridamole and/or a dipyridamole analogue;atorvastatin in combination with dipyridamole and/or a dipyridamole analogue;fluvastatin in combination with dipyridamole and/or a dipyridamole analogue; and/orsimvastatin in combination with dipyridamole and/or a dipyridamole analogue.68.-. (canceled)9. The method of claim 1 , wherein the compound that increases cAMP levels is selected from dipyridamole claim 1 , a dipyridamole analogue claim 1 , a phophodiester (PDE inhibitor and an adenyl cyclase activator.10. (canceled)11. The method of claim 9 , wherein the compound is selected from dipyridamole claim 9 , cilostazol claim 9 , forskolin and/or a cell permeable cAMP analogue.1214.-. (canceled)15. The method of claim 11 , wherein the cell permeable cAMP analogue is db-cAMP16. The method of claim 1 , wherein the cancer is selected from a hematological cancer or a solid tumor claim 1 , such as colorectal claim 1 , prostate claim 1 , skin claim 1 , HCC claim 1 , breast or lung cancer and/or the precancerous disorder is a hematological precancerous disorder.17. (canceled)18. The method of claim 16 , wherein the hematological cancer is a leukemia claim 16 , myeloma or ...

Compound Used to Prevent Diseases Caused by Aquaporin Deficiency

A compound used to prevent diseases caused by aquaporin deficiency, which is 18β-Glycyrrhetinic acid derivative. Said compound can not only prevent diseases caused aquaporin deficiency, but be able to prevent aquaporin (AQP) production and enhance skin function. Since AQPs have many advantages in skin cells, e.g. promoting water and glycerine molecular transportation, increasing skin elasticity and cuticle moisture, increasing the cell proliferation and cell migration, aquaporin can promote skin bather function and wound cicatrization. Therefore, said compound can be applied potentially as a medicinal cosmetic in skin medicine cosmetology, or as a new medical composition to treat diseases caused by AQP abnormality, such as urine concentration defect, wound healing slow down, corneal re-epithelialization slow down and etc. 1. A method for preventing diseases caused by aquaporin deficiency with a novel compound , wherein the novel compound is a 18β-glycyrrhetinic acid derivative , the chemical structure of which is shown in , wherein R is selected from one of the following functional groups: H , CH , CH(CH) , and CHPh.2. The method as claimed in claim 1 , wherein the 18β-glycyrrhetinic acid derivative is a pharmaceutically-acceptable salt of 18β-glycyrrhetinic acid.3. The method as claimed in claim 1 , wherein the 18β-glycyrrhetinic acid derivative is a solvate of 18β-glycyrrhetinic acid.4. The method as claimed in claim 1 , wherein the 18β-glycyrrhetinic acid derivative is a pharmaceutically active derivative of 18β-glycyrrhetinic acid.5. The method as claimed in claim 1 , wherein the novel compound can increase AQP-3 expression in fibroblasts.6. The method as claimed in claim 1 , wherein the novel compound can increase AQP-3 expression in human keratinocytes.7. The method as claimed in claim 1 , wherein the novel compound is used for glycerol transport.8. The method as claimed in claim 1 , wherein the novel compound is used to increase the number of fibroblast.9. ...

COMPOSITION AND USES FOR INFLUENCING HAIR GROWTH

The invention describes a combination of at least one aromatase inhibitor selected from the group of chemical-synthetic aromatase inhibitors and aromatase inhibition exhibiting extracts of soya beans and rapeseed, respectively, and at least one plant extract that contains one or more active ingredient substance(s) extracted from the plant, which is(are) selected from the group of 5α reductase type I and/or type II inhibitors and androgen receptor blockers, said combination being contained for example in a composition and having special properties for influencing hair growth. Uses of this combination are also described. 119-. (canceled)20. A method for cosmetic treatment of a person , the method comprising applying to the person a cosmetic treatment effective amount of a composition comprising:(i) at least one aromatase inhibitor, selected from the group of chemical-synthetic aromatase inhibitors and aromatase inhibition exhibiting extracts of soya beans and rapeseed, respectively, and(ii) at least one plant extract that contains one or more active ingredient substance(s) extracted from the plant, which is(are) selected from the group consisting of 5α reductase type I and/or type II inhibitors and androgen receptor blockers.21. The method according to claim 20 , wherein the aromatase inhibitor inhibits 5α reductase.22. The method according to claim 20 , wherein component (ii) comprises a plant extract with a mixture of active ingredients of 5α reductase type I and/or type II inhibitors and/or androgen receptor blockers.23. The method according to claim 22 , wherein the aromatase inhibitor inhibits 5α reductase.24. The method according to claim 20 , wherein component (i) consists of (a) an extract of soya beans and/or of rapeseed or (b) a chemical-synthetic aromatase inhibitor.25. The method according to claim 20 , wherein component (i) is a combination of (a) the extract of soya beans and/or of rapeseed with (b) a chemical-synthetic aromatase inhibitor.26Serenoa ...

ANTI-VIRAL CARBAMIMIDOTHIOIC ACID ESTERS

Carbamimidothioic acid esters of formula (I) and 2-nitro-N-[4-(pyridin-4-ylamino)phenyl]-4-(quinolin-4-ylamino)benzamide are used for the treatment of influenza, and for the inhibition of a viral RNA-dependent RNA polymerase. Formulae (I), (II). 3. The compound according to claim 1 , consisting of a compound shown in Table 2.4. A pharmaceutical composition comprising the compound of claim 1 , in admixture with a suitable pharmaceutically acceptable diluent or carrier.5. The pharmaceutical composition of claim 4 , in admixture with a medication for the treatment of influenza.6. The pharmaceutical composition of claim 5 , wherein the medication for the treatment of influenza is oseltamivir claim 5 , zanamivir claim 5 , amantadine claim 5 , or rimantadine.7. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering the compound of to a patient.8. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering carbamimidothioic acid claim 1 , phenyl- claim 1 , 1 claim 1 ,3-propanediyl ester or a pharmaceutically acceptable salt claim 1 , solvent claim 1 , or hydrate thereof to a patient.9. A method for the treatment or prophylaxis of influenza claim 1 , comprising administering carbamimidothioic acid claim 1 , phenyl- claim 1 , 1 claim 1 ,3-propanediyl ester claim 1 , dihydrobromide or 2-nitro-N-[4-(pyridin-4-ylamino)phenyl]-4-(quinolin-4-ylamino)benzamide to a patient.10. The method according to claim 8 , wherein the influenza is influenza A.11. The method according to claim 8 , wherein the influenza is influenza type B or C.12. The method according to claim 10 , wherein the influenza is type A group-1.13. The method according to claim 10 , wherein the influenza is type A group-2.14. The method according to claim 10 , wherein the influenza is H1N1 claim 10 , H1N2 claim 10 , H3N2 claim 10 , H5N1 claim 10 , H9N2 claim 10 , H7N3 claim 10 , or H7N7.15. The method according to claim 8 , for treatment or prophylaxis ...

METHOD OF DRUG DETOXIFICATION

A method of detoxifying a patient addicted to at least one drug comprises the step of administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient. The method further comprises the step of administering an anesthetic component to the patient for putting the patient in a sedated state. The method further comprises the step of administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state. The detoxification component can comprise naloxone. The method further comprises the step of administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state. The second-medication component can comprise naltrexone. The method further comprises the step of terminating administration of the anesthetic component to the patient for reviving the patient from the sedated state. 1. A method of detoxifying a patient addicted to at least one drug , said method comprising the steps of:administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient;administering an anesthetic component to the patient for putting the patient in a sedated state;administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state;administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state; andterminating administration of the anesthetic component to the patient for reviving the patient from the sedated state;wherein the first-medication component comprises gabapentin, ropinirole, citric acid sodium citrate, famotidine, glycopyrrolate, ondansetron, dexamethasone, midazolam, or combinations thereof.2. A method as set forth in wherein the patient is in the sedated state ...

LIPOSOMAL FORMULATION FOR OCULAR DRUG DELIVERY

The present invention is directed to a liposomal formulation for ocular drug delivery comprising (i) liposomes comprising at least one lipid bilayer, and (ii) a prostaglandin drug and/or a prostaglandin derivative associated in the liposomes, wherein the liposomes have a mean diameter of less than 2μπι. The present invention is also directed to a pharmaceutical comprising the liposomal formulation and a method of producing the liposomal formulation for ocular drug delivery. Additionally, the present invention is directed to a method of treating or preventing an ocular disease, comprising administering the liposomal formulation or the pharmaceutical composition to a subject in need thereof. 1. A liposomal formulation for ocular drug delivery comprising:(i) liposomes comprising at least one lipid bilayer; and wherein the liposomes have a mean diameter of less than 2 μm; and', 'wherein the liposomes comprise phosphatidylcholines., '(ii) a prostaglandin drug and/or a prostaglandin derivative encapsulated in the liposomes,'}2. The liposomal formulation as claimed in claim 1 , wherein the liposomes comprise mixtures of phosphatidylcholines and at least one of sphingolipids claim 1 , sterol lipids claim 1 , saccharolipids claim 1 , or polyketide lipids.35.-. (canceled)6. The liposomal formulation as claimed in claim 1 , wherein the phosphatidylcholines each comprises at least one unsaturated fatty acid moiety.7. The liposomal formulation as claimed in claim 6 , wherein the phosphatidylcholines each comprises L-α-phosphatidylcholine or 95% Egg phosphatidylcholines (EPC).8. The liposomal formulation as claimed in claim 2 , wherein the sphingolipids each comprises at least one unsaturated fatty acid moiety.9. The liposomal formulation as claimed in claim 8 , wherein the sphingolipids each comprises hexadecanoylsphingomyelin or Egg Sphingomyelin.1011.-. (canceled)12. The liposomal formulation as claimed in claim 1 , wherein the prostaglandin drug comprises latanoprost.1316.-. ...

TOPICAL COMPOSITIONS COMPRISING FIPRONIL AND PERMETHRIN AND METHODS OF USE

The subject matter disclosed herein is directed to stable, highly-effective topical formulations comprising permethrin, fipronil and a solvent system that is sufficient to solubilize these two active ingredients and limit degradation of fipronil to its sulfone, and their uses in topical applications on animals and the environment. Useful formulations comprise from about 30% to about 55% (w/w) permethrin and about 2 to 15% (w/w) fipronil and a solvent system that comprises N-methylpyrrolidone and a glycol, glycol ether, glycol ester, fatty acid ester or neutral oil, wherein the N-methylpyrrolidone and glycol, glycol ether, glycol ester, fatty acid ester or neutral oil are present in a weight:weight ratio of from about 1:2.0 to about 1:3.5, glycol, glycol ether, glycol ester, fatty acid ester or neutral oil to n-methylpyrrolidone. These two actives when combined in the described amounts have been found to have unexpected enhanced repellent activity against stable fly. However, it is the formulations described herein that provide solvency and stability that maintain synergistic concentrations after application on an animal. 1. A topical composition for the treatment and prevention of an ectoparasitic infestation comprising:from about 2% (w/w) to about 15% (w/w) fipronil;from about 30% (w/w) to about 55% (w/w) permethrin; anda neutral oil(s) and N-methylpyrrolidone, wherein said neutral oil(s) and N-methylpyrrolidone are present in a weight:weight ratio of from about 1:2.0 to about 1:3.5, neutral oil(s) to N-methylpyrrolidone.2. The composition of claim 1 , wherein said fipronil is present in a concentration of from about 4% (w/w) to about 8% (w/w).3. The composition of claim 1 , wherein said fipronil is present at a concentration of about 6% (w/w).4. The composition of claim 1 , wherein said permethrin is present in a concentration of from about 35% (w/w) to about 50% (w/w).5. The composition of claim 1 , wherein said permethrin is present in a concentration of from ...

THERAPEUTIC COMPOSITIONS

Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer. 146.-. (canceled)47. A method of treating skin cancer in a subject in need thereof , the method comprising topically administering a therapeutically effective amount of a pharmaceutical formulation of ingenol angelate to the skin of the subject , wherein the pharmaceutical formulation comprises ingenol angelate in an amount from about 0.001% to about 0.15% w/w , and wherein at least about 95% of the ingenol angelate is ingenol-3-angelate (isoform ‘b’) and the pharmaceutical formulation has a pH of less than 4.48. The method of claim 47 , wherein the pharmaceutical formulation has a pH of about 3.5 or less.49. The method of claim 47 , wherein the pharmaceutical formulation has a pH of about 3.0.50. The method of claim 47 , wherein the pharmaceutical formulation has a pH within the range of about 2.5 to less than 4.0.51. The method of claim 47 , wherein the skin cancer is a squamous cell carcinoma.52. The method of claim 47 , wherein the skin cancer is a basal cell carcinoma.53. The method of claim 47 , wherein the skin cancer is a malignant melanoma.54. The method of claim 47 , wherein the pharmaceutical formulation is a gel.55. The method of claim 48 , wherein the skin cancer is a squamous cell carcinoma.56. The method of claim 48 , wherein the skin cancer is a basal cell carcinoma.57. The method of claim 48 , wherein the skin cancer is a malignant melanoma.58. The method of claim 48 , wherein the pharmaceutical formulation is a gel.59. A method of treating a cancerous skin condition in a subject in need thereof claim 48 , the method comprising topically administering a therapeutically effective amount of a pharmaceutical formulation of ingenol angelate to a skin lesion of the subject selected from the group consisting of squamous cell carcinoma claim 48 , basal cell carcinoma claim 48 , malignant melanoma claim 48 , and ...

THERAPEUTIC COMPOSITIONS

Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer. 146.-. (canceled)47. A method of treating skin cancer in a subject in need thereof , the method comprising topically administering a therapeutically effective amount of a pharmaceutical formulation of ingenol angelate to the skin of the subject , wherein the pharmaceutical formulation comprises ingenol angelate in an amount from about 0.001% to about 0.15% w/w , and wherein at least about 97.5% of the ingenol angelate is ingenol-3-angelate (isoform ‘b’) and the pharmaceutical formulation has a pH of less than 4.48. The method of claim 47 , wherein the pharmaceutical formulation has a pH of about 3.5 or less.49. The method of claim 47 , wherein the pharmaceutical formulation has a pH of about 3.0.50. The method of claim 47 , wherein the pharmaceutical formulation has a pH within the range of about 2.5 to less than 4.0.51. The method of claim 47 , wherein the skin cancer is a squamous cell carcinoma.52. The method of claim 47 , wherein the skin cancer is a basal cell carcinoma.53. The method of claim 47 , wherein the skin cancer is a malignant melanoma.54. The method of claim 47 , wherein the pharmaceutical formulation is a gel.55. The method of claim 48 , wherein the skin cancer is a squamous cell carcinoma.56. The method of claim 48 , wherein the skin cancer is a basal cell carcinoma.57. The method of claim 48 , wherein the skin cancer is a malignant melanoma.58. The method of claim 48 , wherein the pharmaceutical formulation is a gel.59. A method of treating a cancerous skin condition in a subject in need thereof claim 48 , the method comprising topically administering a therapeutically effective amount of a pharmaceutical formulation of ingenol angelate to a skin lesion of the subject selected from the group consisting of squamous cell carcinoma claim 48 , basal cell carcinoma claim 48 , malignant melanoma claim 48 , and ...

ROS-Activated Compounds as Selective Anti-Cancer Therapeutics

Provided are compounds according to the following Formula I: 2. The compound according to claim 1 , wherein said alkyl claim 1 , aryl claim 1 , and aralkyl substitutions are selected from the group consisting of alkoxyl claim 1 , halo claim 1 , OH claim 1 , CN claim 1 , carboxyl claim 1 , carboxyl ester claim 1 , and substituted or unsubstituted alkyl.3. The compound according to claim 1 , wherein Ris H or alkyl when Ris aryl or aralkyl claim 1 , and wherein Ris H or alkyl when Ris aryl or aralkyl.4. The compound according to claim 1 , wherein Rand Rare each independently selected from the group consisting of H claim 1 , substituted or unsubstituted C-Calkyl claim 1 , and substituted or unsubstituted phenyl; and Ris OH.5. The compound according to claim 1 , wherein the cancer is associated with production of elevated reactive oxygen species.6. The compound according to claim 5 , wherein the cancer is selected from the group consisting of leukemia claim 5 , renal cancer claim 5 , and cancers of the central nervous system.7. The compound according to claim 6 , wherein the leukemia is selected from the group consisting of acute myeloid leukemia claim 6 , acute lymphoblastic leukemia claim 6 , plasmacytoma claim 6 , myeloma claim 6 , myelogenous leukemia claim 6 , acute lymphocytic leukemia claim 6 , acute promyelocytic leukemia claim 6 , and multiple myeloma.9. A method of reducing proliferative capacity in a cell claim 1 , the method comprising contacting the cell with an effective amount of a compound according to .10. The method according to claim 9 , wherein the cell is a mammalian cell.11. The method according to claim 10 , wherein the cell is a cancer cell.12. A method of treating a cancer associated with elevated ROS comprising administering to a subject in need thereof an effective amount of a compound according to .13. The method according to claim 12 , wherein the subject is a mammal.14. The method according to claim 13 , wherein the cancer is selected from ...

NEURONAL CIRCUIT-DEPENDENT NEUROPROTECTION BY INTERACTION BETWEEN NICOTINIC RECEPTORS

A method of inhibiting excitotoxicity by indirectly activating α4β2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed. Inhibitors of α7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate α4β2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis. 1. A method of treating or preventing neuronal damage in a subject comprising: administering to the subject at least one macrocyclic diterpenoid , or a biologically active fragment , analog , or derivative thereof.2. The method of wherein at least one macrocyclic diterpenoid is administered in an amount sufficient to achieve a concentration between about 200 nM to about 20 μM.3. The method of wherein the subject has suffered claim 1 , suffers from claim 1 , or is at risk for at least one neurodegenerative disease selected from the group consisting of:(a) Alzheimer's Disease;(b) Parkinson's Disease;(c) Frontotemporal Dementia;(d) Amyotrophic Lateral Sclerosis (ALS);(e) Motor Neuron Disease;(f) delayed effects of stroke;(g) delayed effects of traumatic brain injury; and(h) AIDS-related dementia.4. The method of wherein the subject has suffered claim 1 , suffers from claim 1 , or is at risk for developing a disease associated with neuronal impairment selected from the group consisting of:(a) glaucoma caused by optical nerve damage;(b) delayed effects of epilepsy; and(c) multiple sclerosis.5. The method of wherein the macrocyclic diterpenoid is administered during prenatal or postnatal treatment.6. The method of wherein the macrocyclic diterpenoid is selected from the ...

NOVEL INHIBITORS OF BACTERIAL BIOFILMS AND RELATED METHODS

Certain multi-cyclic compounds and compositions thereof are useful for reducing or inhibiting the growth of bacterial biofilms and for controlling bacterial biofilm infections. Such compounds and compositions are also useful in methods for reducing or inhibiting the growth of biofilms and for controlling bacterial biofilm infections involving biofilms. 162-. (canceled)65. A compound according to wherein Ris selected from the group consisting of methyl claim 63 , halide claim 63 , lower haloalkyl claim 63 , nitrile claim 63 , lower alkyl nitrile claim 63 , lower alkyl claim 63 , substituted lower alkyl claim 63 , lower alkenyl claim 63 , substituted lower alkenyl claim 63 , lower alkynyl claim 63 , substituted lower alkynyl claim 63 , lower cycloalkyl claim 63 , lower cycloalkenyl claim 63 , aryl claim 63 , substituted aryl claim 63 , heteroaryl claim 63 , and substituted heteroaryl claim 63 , preferably Ris selected from the group consisting of pyrrolyl claim 63 , pyrazolyl claim 63 , imidazolyl claim 63 , oxazolyl claim 63 , isoxazolyl claim 63 , oxadiazolyl claim 63 , thiazolyl claim 63 , isothiazolyl claim 63 , thienyl claim 63 , furanyl claim 63 , furazanyl claim 63 , pyridinyl claim 63 , pyrimidinyl claim 63 , pyridazinyl claim 63 , indolyl claim 63 , 3H-indolyl claim 63 , isoindolyl claim 63 , indolinyl claim 63 , indolizinyl claim 63 , indazolyl claim 63 , dihydroindolyl claim 63 , tetrahydroindolyl claim 63 , purinyl claim 63 , pyrazinyl claim 63 , quinolinyl claim 63 , isoquinolinyl claim 63 , tetrahydroisoquinolinyl claim 63 , quinoxalinyl claim 63 , quinazolinyl claim 63 , cinnolinyl claim 63 , pteridinyl claim 63 , benzimidazolyl claim 63 , benzopyranyl claim 63 , benzoxazolyl claim 63 , benzisoxazolyl claim 63 , benzofuranyl claim 63 , isobenzofuranyl claim 63 , benzothiazolyl claim 63 , benzisothiazolyl claim 63 , benzothienyl claim 63 , furopyridinyl claim 63 , phthalazinyl claim 63 , napthyridinyl claim 63 , pyrazolopyridyl claim 63 , ...

COMBINATION OF AN HMG-COA REDUCTASE INHIBITOR AND A FARNESYL-PYROPHOSPHATASE SYNTHASE INHIBITOR FOR THE TREATMENT OF DISEASES RELATED TO THE PERSISTENCE AND/OR ACCUMULATION OF PRENYLATED PROTEINS

The invention relates to the use of a hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor and of a farnesyl-pyrophosphate synthase inhibitor, or of one of their associated physiologically acceptable salts, in the preparation of a composition, particularly a pharmaceutical composition, for use in the treatment of human or animal, pathological or nonpathological situations related to the accumulation and/or the persistence of prenylated proteins in cells, such as during progeria (Hutchinson-Gilford syndrome), restrictive dermopathy or physiological ageing. 1. A method of treating of conditions , pathological or not , relating to the accumulation and/or persistence in cells of prenylated proteins , the method comprising administering to a subject in need thereof an effective amount of an inhibitor of hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase and an inhibitor of farnesylpyrophosphate synthase , or one of their physiologically acceptable salts.2. The method according to claim 1 , characterised in that the conditions claim 1 , pathological or not claim 1 , are related to the accumulation and/or persistence in cells of farnesylated and/or geranylgeranylated proteins.3. The method according to claim 1 , characterised in that the conditions claim 1 , pathological or not claim 1 , are related to the accumulation and/or persistence in cells of progerin.4. The method according to claim 1 , characterised in that the conditions claim 1 , pathological or not claim 1 , are related to the accumulation and/or persistence in cells of farnesylated prelamin A.5. The method according to claim 4 , characterised in that the farnesylated prelamin A can also be truncated.6. The method according to claim 1 , characterised in that the inhibitor of farnesyl-pyrophosphate synthase is a molecule in the family of aminobisphosphonates (NBP) or one of its physiological acceptable salts.7. The method according to claim 6 , characterised in that the aminobisphosphonate is ...

EYE DROP PREPARATION COMPRISING LATANOPROST

It is intended to provide an eye drop preparation capable of preventing not only degradation of latanoprost in water but also adsorption of latanoprost onto a plastic container so that a decrease in latanoprost content thereof is satisfactorily prevented. The eye drop preparation contains an ophthalmic solution composition containing components (A) and (B) and packed in a plastic container: (A) latanoprost; and (B) a nonionic surfactant. 116.-. (canceled)17. An eye drop preparation comprising an ophthalmic solution composition comprising components (A) to (D) and packed in a plastic container , which is storable at room temperature and substantially does not require refrigerated storage:(A) latanoprost;(B) a nonionic surfactant;(C) one or more compounds selected from the group consisting of a tricarboxylic acid and a tetracarboxylic acid, or a pharmaceutically acceptable salt thereof; and(D) a sugar or one or more organic amines selected from the group consisting of trometamol and monoethanolamine.18. An eye drop preparation comprising an ophthalmic solution composition comprising components (A) , (B) , (D) , and (E) and packed in a plastic container , which is storable at room temperature and substantially does not require refrigerated storage:(A) latanoprost;(B) a nonionic surfactant;(D) a sugar or one or more organic amines selected from the group consisting of trometamol and monoethanolamine; and(E) boric acid and/or phosphoric acid or a salt form thereof19. The eye drop preparation according to claim 17 , wherein the component (B) is polyoxyethylene sorbitan fatty acid ester claim 17 , polyoxyethylene hydrogenated castor oil claim 17 , or polyoxyl stearate.20. The eye drop preparation according to claim 17 , wherein the component (C) is citric acid claim 17 , edetic acid claim 17 , or a pharmaceutically acceptable salt thereof.21. The eye drop preparation according to claim 18 , wherein the organic amine of the component (D) is trometamol and/or ...

LOW TOXICITY TOPICAL ACTIVE AGENT DELIVERY SYSTEM

An active agent delivery composition is provided that allows topical delivery of active agents including vitamin A and its derivatives. A volatile vehicle serves as a coupler for an active agent and an organosiloxane carrier so as to allow full solubilization of active agents not normally miscible in silicones and providing a non-irritating, targeted evaporating composition. 1. An active agent topical delivery composition comprising:a volatile organosiloxane carrier;an active agent selected from the group consisting of vitamin A or vitamin A derivatives, hydroxy acids, benzoyl peroxide, and combinations thereof; anda volatile vehicle,said composition having less than 15% organic hydrocarbon solvent of 6 carbon atoms or fewer.2. The composition of having an evaporation rate in air of 10 to 200 mg/cm/minute at 25° C. and atmospheric pressure of 760 mmHg.3. The composition of with an irritancy value of 2 or less.4. The composition of that is a clear solution of said active agent.5. The composition of wherein said composition has less than 5% organic hydrocarbon solvent of 6 carbon atoms or fewer.6. The composition of wherein said agent is vitamin A or its derivatives wherein said vitamin A or its derivatives are present at between 0.001 to 2 weight percent.7. The composition of wherein said active agent is a vitamin A derivative selected from the group consisting of: retinal; retinoic acid; retinyl ester; retinol; tretinoin claim 1 , isotretinoin claim 1 , or esters thereof; an ester or amide of 13-trans retinoic acid; adapalene; tazarotene; or combinations thereof.8. The composition of wherein said hydroxy acid is salicylic acid claim 1 , acetylsalicylic acid claim 1 , or combinations thereof.9. The composition of wherein said agent is benzoyl peroxide present from about 1 to about 10 weight percent.10. The composition of wherein said organosiloxane carrier is a linear aliphatic polyorganosiloxane.11. The composition of wherein said organosiloxane carrier is ethyl ...

Drug delivery devices for delivery of ocular therapeutic agents

Drug delivery devices comprising a non-bioabsorbable polymer structure configured to support a composition comprising an active agent. The devices include a plurality of portions fused together and a recess configured to support the composition. At least one of the portions includes an impermeable polymer and at least one other portion includes a rate-limiting water-permeable polymer. The rate-limiting water-permeable polymer allows for transportation of the active agent to an exterior of the device.

METHODS AND COMPOSITIONS FOR PREVENTING AND TREATING AUDITORY DYSFUNCTIONS

The invention provides methods for treating auditory impairments in a subject in need of treatment comprising administering to said subject an effective amount of a composition comprising, as an active agent, one or more of a carboxy alkyl ester, a quinic acid derivative, a caffeic acid derivative, a ferulic acid derivative, or a quinic acid lactone or derivative thereof or pharmaceutically acceptable salt thereof and an acceptable carrier or excipient, so as to treat auditory impairments in the subject. 1. A method of treating an auditory impairment in a subject comprising administering to said subject an effective amount of a composition comprising , as an active agent , one or more of a carboxy alkyl ester , a quinic acid derivative , a caffeic acid derivative , a ferulic acid derivative , or a quinic acid lactone or derivative thereof or pharmaceutically acceptable salt thereof so as to treat the auditory impairment in the subject.2. (cancel)3. The method of or , wherein the carboxy alkyl ester is any ofa. 3,4-O-dicaffeoylquinic acid,b. 3,5-O-dicaffeoylquinic acid,c. 1,3-O-dicaffeoylquinic acid,d. 4,5-O-dicaffeoylquinic acid,e. 1,5-O-dicaffeoylquinic acid,f. 3-O-feruloylquinic acid,g. 4-O-feruloylquinic acid, '1-O-caffeoylquinic acid', 'h. 5-O-feruloylquinic acid,'}i. 3-O-caffeoylquinic acid,j. 4-O-caffeoylquinic acid,k. 5-O-caffeoylquinic acid,l. (1S ,3R,4R,5R)-3-[3-(3,4-dihydroxyphenyl)-3R-hydroxypropanoyl]1,4,5-trihydroxycyclohexanecarboxylic acid,m. (1S,3R,4R,5R)-3-[3-(3,4 dihydroxyphenyl)-3S-hydroxypropanoyl]-1,4,5-trihydroxycyclohexanecarboxylic acid,n. (1S,3R,4R,5R)-5-[3-(3,4-dihydroxyphenyl)-3R-hydroxypropanoyl]-1,3,4-trihydroxycyclohexanecarboxylic acid,o. (1S,3R,4R,5R)-5-[3-(3,4-dihydroxyphenyl)-3S-hydroxypropanoyl]-1,3,4-trihydroxycyclohexanecarboxylic acid,p. (1S,3R,4R,5R)-4-[3-(3,4-dihydroxyphenyl)-3R-hydroxypropanoyl]-1,3,5-trihydroxycyclohexanecarboxylic acid,q. (1S,3R,4R,5R)-4-[3-(3,4-dihydroxyphenyl)-3S-hydroxypropanoyl]-1,3,5- ...

Methods and Compositions for Inhibition of Polymerase

The present invention is directed to methods and compositions for inhibition of viral nucleic acid polymerases, such as RNA and DNA polymerases, and methods and compositions that are useful for treating viral infections in subjects. The methods comprise administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier. The composition or method may optionally comprise one or more additional anti-viral agents.

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 ...

INGENOLS FOR TREATING SEBORRHEIC KERATOSIS

The invention provides ingenol compounds for treating seborrheic keratosis. 110.-. (canceled)11. A method for the treatment of seborrheic keratosis in a subject , the method comprising administering an ingenol compound to the subject such that seborrheic keratosis is treated.12. The method of claim 11 , wherein said ingenol compound is ingenol-3-angelate.13. The method of claim 11 , wherein the ingenol compound is applied to the skin of the subject.14. The method of claim 11 , wherein the ingenol compound is administered in the form of an isopropyl alcohol based gel.15. The method of claim 11 , wherein the ingenol compound is present in a concentration of about 0.05%.16. A topical composition for use in the treatment of seborrheic keratosis in a subject claim 11 , the topical composition comprising an ingenol compound together with a pharmaceutically acceptable carrier.17. The topical composition of claim 16 , wherein said ingenol compound is ingenol-3-angelate.18. The topical composition of claim 16 , wherein the ingenol compound is administered in the form of an isopropyl alcohol based gel.19. The topical composition of claim 16 , wherein the ingenol compound is present in a concentration of about 0.05%. Ingenol compounds are previously described for treatment of cancer and actinic keratosis in WO99/08994, WO01/93884, WO06/063382 and WO02/11743. Treatment of other lesions of the skin are described in WO2007/059584, WO2008/131491 and WO2010/091472.seborrheic keratosis is as such a benign skin condition. However, treatment of the condition is often pursued for cosmetic purposes. Treatment of the condition by removing the growth is typically by cryosurgery. Small lesions can be treated with light electrocautery. Larger lesions can be treated with electrodessication and curettage, shave excision, or cryotherapy. Removal of seborrheic keratoses will cause some visible scarring especially in persons with dark skin tones. Also the removal of the growths are performed at ...

STABLE COMPOSITION COMPRISING CHOLESTEROL-LOWERING AGENTS, ANTIHYPERTENSIVE AGENTS AND ANTIPLATLET AGENTS

The present invention relates to a stable composition for providing substances with different types of activity, such as cholesterol lowering agents, antihypertensive agents and antiplatelet agents, which substantially reduce the dosage required to prevent cardiovascular events. 1. A stable composition of cholesterol-lowering agents , antihypertensives agents and antiplatelet agents containing granules with 30-50 mg of cholesterol-lowering agents , 30-60 mg of antihypertensive agents and 70-100 mg of antiplatelet agents wherein said composition comprises 400-700 mg of a diluting agent; 30-60 mg of a disintegrating agent , 5-15 mg of an anti-adherent , 90-120 mg of lubricant and 25-55 mg of protective agents.2. The stable composition according to claim 1 , wherein said cholesterol lowering agent is preferably pravastatin sodium.3. The stable composition according to claim 1 , wherein said antihypertensive agent is preferably losartan potassium.4. The stable composition according to claim 1 , wherein said antiplatelet agent is acetylsalicylic acid.5. The stable composition according to claim 1 , wherein said protective agents are selected from the group consisting of: calcium carbonate claim 1 , aluminum hydroxide claim 1 , magnesium hydroxide claim 1 , magnesium oxide claim 1 , propyl gallate claim 1 , ascorbyl palmitate claim 1 , sodium metabisulfite claim 1 , butylhydroxyanisole claim 1 , butylhydroxytoluene claim 1 , and combinations thereof.6. The stable composition according to claim 1 , wherein said cholesterol-lowering agents claim 1 , antihypertensives agents claim 1 , antiplatelet agents claim 1 , diluting agents claim 1 , disintegrating agents claim 1 , anti-adherents claim 1 , lubricants and protective agents are present in a single phase. The present invention relates to a stable composition which immediately delivers various drugs having different types of activity such as cholesterol-lowering agents, antihypertensive agents and antiplatelet agents that ...

AGENT FOR DELAYING DIGESTION AND ABSORPTION OF LIPID

An object is to achieve a big effect about an agent for delaying digestion and absorption of lipid or a lipase inhibitor which is composed of specific triacylglycerol and fat-soluble and which exerts the effect more mildly with small used amount. An oil-in-water emulsion having 2 μm or less of average particle diameter, in which a melting point of a fat composition which composes an oil phase of the emulsion is 37° C. or less and the fat composition includes 30% by weight or more of BX2 triacylglycerol (B represents Behenic acid and X represents fatty acid having 4 to 24 carbon atoms) is simultaneously ingested with ingesting fat-containing food. An amount of the BX2 triacylglycerol with respect to fat amount derived from fat-containing food ingested simultaneously is preferably 0.5 to 20% by weight. 1. An agent for delaying digestion and absorption of lipid , comprising an oil-in-water emulsion having 2 μm or less of average particle diameter as an active substance , wherein a melting point of a fat composition which composes an oil phase of the emulsion is 37° C. or less , and wherein the fat composition comprises 30% by weight or more of BX2 triacylglycerol wherein B represents Behenic acid and X represents fatty acid having 4 to 24 carbon atoms.2. The agent for delaying digestion and absorption of lipid according to claim 1 , wherein an amount of the BX2 triacylglycerol with respect to fat amount derived from fat-containing food ingested simultaneously with the agent is 0.5 to 20% by weight.3. The agent for delaying digestion and absorption of lipid according to claim 1 , wherein the oil-in-water emulsion is used in dried form.4. A method for enhancing a lipase inhibitor claim 1 , comprising preparing an oil-in-water emulsion having 2 μm or less of average particle diameter and administering the oil-in-water emulsion claim 1 , wherein a melting point of a fat composition which composes an oil phase of the emulsion is 37° C. or less claim 1 , and wherein the fat ...

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: ...

COMBINATION OF SULFONAMIDE COMPOUND AND TAFLUPROST

The object of the present invention is to discover a combination of preventive or therapeutic drugs for glaucoma or ocular hypertension, which is useful as a preventive or therapeutic agent for glaucoma or ocular hypertension. By combining isopropyl(6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate with tafluprost, their intraocular pressure lowering effects are complemented and/or enhanced each other. As for the administration form, these drugs may be administered concomitantly or may be administered as a combination drug. 1. A preventive or therapeutic agent for glaucoma or ocular hypertension , comprising a combination of isopropyl(6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate with tafluprost.2. An intraocular pressure lowering agent , comprising a combination of isopropyl(6-{[4-(pyrazol-1-yl)benzyl](pyridin-3-ylsulfonyl)aminomethyl}pyridin-2-ylamino)acetate with tafluprost.3. The preventive or therapeutic agent or the intraocular pressure lowering agent according to or , which is further combined with other preventive or therapeutic drug for glaucoma or ocular hypertension.4. The preventive or therapeutic agent or the intraocular pressure lowering agent according to claim 3 , wherein the other preventive or therapeutic drug for glaucoma or ocular hypertension is one or more preventive or therapeutic agents selected from the group consisting of a nonselective sympathomimetic drug claim 3 , an α-receptor agonist claim 3 , an α-receptor antagonist claim 3 , a β-receptor antagonist claim 3 , a parasympathomimetic drug claim 3 , a carbonic anhydrase inhibitor claim 3 , a prostaglandin and a Rho-kinase inhibitor.5. The preventive or therapeutic agent or the intraocular pressure lowering agent according to claim 4 , wherein the nonselective sympathomimetic drug is dipivefrin.6. The preventive or therapeutic agent or the intraocular pressure lowering agent according to claim 4 , wherein the α- ...

Composition Comprising Retinol, a Precursor or a Reaction Product of it and a Plant Extract from at least one Chamomilla Plant for the Treatment of Cancer

The invention relates to a (i) Vitamin A, a reaction product, a metabolite or a precursor of it and (ii) a plant extract of chamomile or an active component thereof, preferably for use in the treatment of cancer. The inventive composition may be provided as a medicament or a pharmaceutical composition. The at least one Chamomilla plant typically contained in the inventive compositions preferably comprises , more preferably fibres tubiformis of . Esters of Retinol typically contained in the inventive compositions typically comprise e.g. Retinyl acetate and a plant extract from the plant 1. A composition comprising(i) Vitamin A, a reaction product, a metabolite or a precursor of it, selected from Vitamin A, retinioic acid, all-trans-retinoic acid, 13-cis-retinoic acid, esters of Vitamin A, retinyl palmitate, retinol, retinal, retinyl acetate, alitretinoin, beta-carotene, alpha-carotene, gamma-carotene, beta-cryptoxanthine and provitamin A, and(ii) a plant extract of chamomile selected from an aqueous extract, an ethanolic liquid extract and a waterfree ethanolic liquid extract,wherein components (i) and (ii) represent the only active ingredients.2. (canceled)3. A composition according to claim 1 , wherein the plant extract is a volatile oil of chamomile.4Matricaria recutita. A composition according to claim 1 , wherein the plant extract is a chamomile extract prepared from tubular flowers of L.5Matricaria recutita. A composition according to claim 1 , wherein the composition comprises about 50 mg to about 1500 mg of the chamomile extract from tubular flowers of L. claim 1 , and about 3 mg to about 90 mg of Vitamin A or any of the Vitamin A reaction products claim 1 , metabolites claim 1 , or precursors as defined in .6. A composition according to claim 1 , wherein the plant extract prior to preparing the composition has been purified by contacting it with crosspovidone (crosslinked povidone) and sodiumsulfate.7. A method according to claim 13 , wherein the cancer or ...

Method for Treating Overactive Bladders and a Device for Storage and Administration of Topical Oxybutynin Compositions

The invention relates to a method for treating overactive bladders and a device for storing and administering non-occluded oxybutynin topical compositions.

METHOD FOR PREVENTING OR TREATING ARRHYTHMIA, METHOD FOR PREVENTING OR TREATING ATRIAL FIBRILLATION, MODEL OF SUSTAINED ATRIAL FIBRILLATION, METHOD FOR PRODUCING THE MODEL, AND METHOD FOR SCREENING FOR ATRIAL FIBRILLATION INHIBITOR

A method for preventing or treating atrial fibrillation, including: 2. The method according to claim 1 , wherein the atrial fibrillation is idiopathic atrial fibrillation or chronic atrial fibrillation.3. A method for producing a model of sustained atrial fibrillation claim 1 , comprising:inserting an electrode catheter into a region of a dog containing an atrioventricular node and applying high-frequency current to the region from the electrode catheter to break the atrioventricular node and block atrioventricular conduction, to thereby dilate and enlarge the atrium thereof, andpacing the atrium which has been dilated and enlarged.4. The method for producing a model of sustained atrial fibrillation according to claim 3 , wherein the pacing is pacing the atrium at 500 bpm to 700 bpm for 4 weeks or more.5. A model of sustained atrial fibrillation claim 3 , wherein the model of sustained atrial fibrillation is produced by a method for producing a model of sustained atrial fibrillation claim 3 , which comprises:inserting an electrode catheter into a region of a dog containing an atrioventricular node and applying high-frequency current to the region from the electrode catheter to break the atrioventricular node and block atrioventricular conduction, to thereby dilate and enlarge the atrium thereof; andpacing the atrium which has been dilated and enlarged.6. The model of sustained atrial fibrillation according to claim 5 , wherein atrial fibrillation is sustained for at least one week.7. A method for screening for an atrial fibrillation inhibitor claim 5 , comprising:administering a test substance to a model of sustained atrial fibrillation; andscreening for, as an atrial fibrillation inhibitor, the test substance that inhibits atrial fibrillation in the model of sustained atrial fibrillation after the administering,wherein the model of sustained atrial fibrillation is produced by a method for producing a model of sustained atrial fibrillation, which comprises:inserting ...

Oral Dosage Forms of Methyl Hydrogen Fumarate and Prodrugs Thereof

Improved oral dosage forms of methyl hydrogen fumarate and prodrugs thereof are disclosed. Methods of treating diseases such as multiple sclerosis and psoriasis using such dosage forms are also disclosed. 1. An oral pharmaceutical tablet , comprising:(A) a tablet core comprising (i) a compound selected from (a) methyl hydrogen fumarate (MHF), (b) a prodrug of MHF, (c) pharmaceutically acceptable salts of (a) or (b), and (d) combinations of any of the foregoing, and (ii) one or more core tableting excipients; and(B) a compressed coating layer surrounding said tablet core, the coating layer comprising a material that is either (i) a proton-donating acidic material having a pKa of greater than 8, (ii) a proton-accepting basic material having a pKa of less than 2, (iii) a natural gum or polysaccharide, (iv) a neutral polymer salt, or (v) a lipid,the coating layer releasing no more than 20% of the compound over a period of 2 hours after the tablet is placed in an aqueous solution free of the compound.2. The oral pharmaceutical tablet of claim 1 , wherein the coating layer material is a non-ionizable polymer substantially free of carboxylic acid moieties.3. The oral pharmaceutical tablet of claim 1 , wherein the coating layer material is selected from non-ionizable cellulosic polymers claim 1 , non-ionizable vinyl polymers claim 1 , and non-ionizable polyvinyl alcohol polymers.4. The oral pharmaceutical tablet of claim 1 , wherein the tablet core comprises an immediate release formulation.5. The oral pharmaceutical tablet of claim 1 , wherein the tablet core comprises a sustained release formulation.6. The oral pharmaceutical tablet of claim 1 , wherein at least one of the tablet core and the coating layer comprises a sustained release agent.7. The oral pharmaceutical tablet of claim 6 , wherein the sustained release agent is selected from hydroxypropylmethyl cellulose and ethyl cellulose.8. The oral pharmaceutical tablet of claim 1 , the tablet having a core weight to: ...

NITRIC OXIDE RELEASING AMINO ACID ESTER COMPOUND, COMPOSITION AND METHOD OF USE

There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: 7. (canceled)9. (canceled)10. A composition comprising the compound of and a pharmaceutically acceptable carrier.11. The composition of claim 10 , further comprising (i) at least one other therapeutic agent; (ii) at least one other nitric oxide donor compound; or (iii) at least one other therapeutic agent and at least one other nitric oxide donor compound.12. The composition of claim 11 , wherein the therapeutic agent is an aldosterone antagonist claim 11 , an alpha-adrenergic receptor antagonist claim 11 , an angiotensin II antagonist claim 11 , an angiotensin-converting enzyme inhibitor claim 11 , an antidiabetic compound claim 11 , an anti-hyperlipidemic compound claim 11 , an antioxidant claim 11 , an antithrombotic and vasodilator compound claim 11 , a β-adrenergic antagonist claim 11 , a calcium channel blocker claim 11 , a digitalis claim 11 , a diuretic claim 11 , an endothelin antagonist claim 11 , a hydralazine compound claim 11 , a Hreceptor antagonist claim 11 , a neutral endopeptidase inhibitor claim 11 , a nonsteroidal antiinflammatory compound claim 11 , a phosphodiesterase inhibitor claim 11 , a potassium channel blocker claim 11 , a platelet reducing agent claim 11 , a proton pump inhibitor claim 11 , a renin inhibitor claim 11 , a selective cyclooxygenase-2 inhibitor claim 11 , or a combination of two or more thereof.13. The composition of claim 12 , wherein the therapeutic agent is at least one compound selected from the group consisting of an aldosterone antagonist claim 12 , an angiotensin II antagonist claim 12 , an angiotensin-converting enzyme inhibitor claim 12 , a β-adrenergic antagonist claim 12 , a diuretic and a ...

INTRACELLULAR CALCIUM MODULATION FOR CANCER TREATMENT

Tumor cells exhibit consistent abnormalities in calcium regulation. The present disclosure teaches methods by which such differences are exploited to induce Apoptosis selectively in tumor/cancer cells while sparing normal cells. These methods are based upon employing drugs that, acting in synergistic combinations, trigger selective killing of malignant cells. Since the invention is based upon fundamental cell cycle requirements, to the extent that calcium handling abnormalities are a general characteristic of the malignant state, the methods presented here are widely applicable regardless of tissue of origin and degree of cellular de-differentiation. 1. A method for treating a cancer in a patient comprising administering to said patient effective amounts of two or more drugs at concentrations which interact synergistically , that stimulate an increase in the Ca burden of smooth endoplasmic reticulum and mitochondria.2. The method of wherein at least one of said drugs stimulates Smooth-Endoplasmic-Reticulum Ca-ATPase (SERCA) and wherein at least one of said drugs is an antagonist of SER Ca gates.3. The method of wherein at least one of said drugs is selected from the group consisting of inhibitors of SER IP3-sensitive Ca gates and SERCA agonists claim 1 , and one of said drugs are selected from the group consisting of drugs which are stimulators of particulate guanylate cyclase.4. The method of wherein at least one of said drugs is selected from the group consisting of inhibitors of SER IP3-sensitive Ca gates and agonists of SERCA and wherein at least one of said drugs is an effective elevator of cGMP levels including activators of particulate guanylate cyclases and inhibitors of cGMP phosphodiesterases.5. The method of wherein at least one of said drugs is a calmodulin antagonist claim 1 , including antagonists of the CAM targets calcineurin/protein phosphatase 2B and CAM-dependent protein kinase II and wherein at least one of said drugs is a Protein Kinase C ...

Pyrimidinone compounds and methods for preventing and treating influenza

In one aspect, the invention relates to novel, broad-spectrum anti-viral, pyrimidinone compounds, methods of use, compositions and kits useful in treating and/or preventing influenza. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

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.

Neuronal circuit-dependent neuroprotection by interaction between nicotinic receptors

A method of inhibiting excitotoxicity by indirectly activating α4β2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed Inhibitors of α7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate α4β2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis.

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. 120-. (canceled)23. The method of claim 21 , wherein the phorbol ester is phorbol 13-butyrate claim 21 , phorbol 12-decanoate claim 21 , phorbol 13-decanoate claim 21 , phorbol 12 claim 21 ,13-diacetate claim 21 , phorbol 13 claim 21 ,20-diacetate claim 21 , phorbol 12 claim 21 ,13-dibenzoate claim 21 , phorbol 12 claim 21 ,13-dibutyrate claim 21 , phorbol 12 claim 21 ,13-didecanoate claim 21 , phorbol 12 claim 21 ,13-dihexanoate claim 21 , phorbol 12 claim 21 ,13-dipropionate claim 21 , phorbol 12-myristate claim 21 , phorbol 13-myristate claim 21 , phorbol 12 claim 21 ,13 claim 21 ,20-triacetate claim 21 , 12-deoxyphorbol 13 -angelate claim 21 , 12-deoxyphorbol 13 -angelate 20-acetate claim 21 , 12-deoxyphorbol 13-isobutyrate claim 21 , 12-deoxyphorbol 13-isobutyrate-20-acetate claim 21 , 12-deoxyphorbol 13-phenyl acetate claim 21 , 12-deoxyphorbol 13 -phenylacetate 20-acetate claim 21 , 12-deoxyphorbol 13-tetradecanoate claim 21 , phorbol 12-tigliate 13-decanoate claim 21 , 12-deoxyphorbol 13-acetate claim 21 , phorbol 12-acetate claim 21 , or phorbol 13-acetate.24. The method of claim 21 , wherein the phorbol ester is 12-O-tetradecanoylphorbol-13-acetate.25. The method of claim 21 , wherein the phorbol ester of Formula I is administered parenterally.26. The method of claim 21 , wherein said phorbol ester of Formula I is administered at least 30 times.27. The method of claim 21 , wherein said effective amount is between about 100 μg to about 300 μg.28. The method of claim 21 , further comprising administering at least one ...

Pharmaceutical composition for oral administration comprising high concentration taxane

The present invention provides a pharmaceutical composition for oral administration, comprising (a) 4 to 40% by weight of a taxane, (b) 10 to 30% by weight of a medium chain triglyceride, (c) 30 to 70% by weight of monooleoyl glycerol, (d) 5 to 30% by weight of a surfactant, and (e) 10 to 30% by weight of polyoxyl glyceryl fatty acid ester and a process for preparing the same.

COMPOSITION COMPRISING A DIINDOLYLMETHANE AND A RETINOID TO TREAT A SKIN CONDITION

Provided is a composition for use in treating a skin condition, the composition comprising: 134-. (canceled)36. The dosage form of claim 35 , wherein the ratio (mg:μg) of the first and the second component is from about 10:3000 to about 500:200.37. The dosage form of claim 35 , wherein the ratio (mg:μg) of the first and the second component is from about 75:800 to about 300:200.38. The dosage form of claim 35 , wherein the ratio (mg:IU) of the first and the second component is from about 75:10000 to about 300:2500.39. The dosage form of claim 35 , wherein the ratio (mg:mg) of the first and the second component is from about 75:5.3 to about 300:1.3.40. The dosage form of claim 35 , wherein the dosage form comprises a first capsule comprising the first component and a second capsule comprising the second component.41. The dosage form of claim 35 , wherein the dosage form comprises a capsule comprising the first component and the second component claim 35 , wherein the first and the second component are provided in a single formulation.42. The dosage form of claim 41 , wherein the single formulation comprises a blended powder comprising the first and the second component.43. The dosage form of claim 35 , wherein the dosage form comprises a first tablet comprising the first component and a second tablet comprising the second component.44. The dosage form of claim 35 , wherein the dosage form comprises a tablet comprising the first component and the second component claim 35 , wherein the first and the second component are provided in a single formulation.45. The dosage form of claim 35 , wherein the first component is in a microencapsulated form.46. The dosage form of claim 35 , further comprising at least one excipient selected from the group consisting of: tricalcium phosphate claim 35 , cellulose fiber claim 35 , ascorbic acid claim 35 , silicon dioxide claim 35 , magnesium stearate claim 35 , and any combination thereof.47. The dosage form of claim 35 , wherein a ...

Compositions and Methods for Treating Cardiovascular Diseases

The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a cardiovascular disease in an individual using such pharmaceutical compositions. 2. The pharmaceutical composition according to claim 1 , wherein the fibrate comprises Bezafibrate claim 1 , Ciprofibrate claim 1 , Clofibrate claim 1 , Fenofibrate claim 1 , Gemfibrozil claim 1 , or a combination thereof.3. The pharmaceutical composition according to claim 1 , wherein the concentration of the fibrate is at least 50 mg/mL.4. The pharmaceutical composition according to claim 1 , wherein the pharmaceutically-acceptable lipid-adjuvant is in an amount of about 80% to about 97%.5. The pharmaceutical composition according to claim 1 , wherein the pharmaceutically-acceptable lipid-adjuvant is in an amount of about 80% to about 93%.6. The pharmaceutical composition according to claim 5 , wherein the pharmaceutically-acceptable lipid-adjuvant is in an amount of about 85% to about 93%.7. The pharmaceutical composition according to claim 1 , wherein the pharmaceutically-acceptable lipid-adjuvant comprises at least 55% of the pharmaceutically-acceptable lipid-adjuvant.8. The pharmaceutical composition according to claim 7 , wherein the pharmaceutically-acceptable lipid-adjuvant comprises at least 60% of the pharmaceutically-acceptable lipid-adjuvant.9. The pharmaceutical composition according to claim 8 , wherein the pharmaceutically-acceptable lipid-adjuvant comprises at least 65% of the pharmaceutically-acceptable lipid-adjuvant.10. The pharmaceutical composition according to claim 1 , wherein the one or more glycerolipids comprises a monoglyceride claim 1 , an acetylated monoglyceride claim 1 , a diglyceride claim 1 , an acetylated diglyceride claim 1 , a triglyceride claim 1 , an acetylated triglyceride claim 1 , or any combination thereof.11. The pharmaceutical composition according to claim 10 , wherein the one or more ...

NASOLACRIMAL DRAINAGE SYSTEM IMPLANTS FOR DRUG THERAPY

An implant for insertion through a punctum and into a canalicular lumen of a patient. The implant includes a matrix of material, a therapeutic agent dispersed in the matrix of material, a sheath disposed over a portion of the matrix of material and configured to inhibit the therapeutic agent from being released from the matrix of material into the canalicular lumen and to allow the therapeutic agent to be released from a surface of the matrix of material to a tear film, and a retention structure configured to retain the implant within the canalicular lumen. 1. An implant for insertion into a punctum of a patient , the implant comprising:a drug core having a distal end and a proximal end, the distal end of the drug core having a cross section suitable for insertion through a punctum, the drug core comprising a therapeutic agent deliverable into the eye; anda sheath disposed over a portion of the drug core to define at least one exposed surface of the drug core, the at least one exposed surface of the drug core located near the proximal end to contact a tear or tear film fluid and release the therapeutic agent at therapeutic levels over a sustained period when the implant is implanted for use.2. The implant of further comprising a retention structure attached to the drug core to retain the drug core near and/or in the punctum.3. The implant of wherein the retention structure is attached to the drug core via the sheath.4. The implant of wherein the retention structure comprises a hydrogel adapted to expand when the retention structure is placed in the punctum.5. The implant of wherein the retention structure comprises an attachment member having an axially oriented surface claim 4 , the hydrogel capable of expansion to urge against the axially oriented surface to retain the hydrogel while the hydrogel is hydrated.6. The implant of wherein the attachment member comprises at least one of a protrusion claim 5 , a flange claim 5 , a rim claim 5 , or an opening through a ...

Method for treating overactive bladders and a device for storage and administration of topical oxybutynin compositions

The invention relates to a method for treating overactive bladders; a device for storing and administering non-occluded oxybutynin topical compositions and a method for preparing the device for storing and administering non-occluded oxybutynin topical compositions.

COMPOSITIONS AND METHODS FOR AGONIZING THE CB2 RECEPTOR

Disclosed herein are new compositions comprising a purified cannabinoid and a purified terpene. In one embodiment, the compositions comprise one or more purified cannabinoids. In one embodiment, the compositions comprise one or more purified cannabinoids in combination with one or more purified terpenes. In one embodiment, the compositions comprise unnaturally occurring ratios. In one embodiment, the compositions comprise unnaturally occurring concentrations. In one embodiment, the compositions comprise unexpected and/or synergistic effects. 1. A composition comprising:purified CBC;wherein the composition is substantially free from cellulose; andwherein the purified CBC makes up greater than 50% of the total cannabinoids present in the composition.2. The composition of claim 1 , further comprising a compound chosen from a second purified cannabinoid claim 1 , a purified terpene claim 1 , and an analgesic.3. The composition of claim 2 , further comprising a purified terpene chosen from Linalool claim 2 , Borneol claim 2 , Elemene claim 2 , Beta-Myrcene claim 2 , Nerolidol claim 2 , Phytol claim 2 , Terpinolene claim 2 , Bornyl Acetate claim 2 , and Terpineol claim 2 , alpha bisabolol.4. The composition of claim 2 , further comprising an analgesic.5. The composition of claim 4 , wherein the analgesic is chosen from Morphine claim 4 , Thebaine claim 4 , Buprenorphine claim 4 , Fentanyl claim 4 , Acetylfentanyl claim 4 , Norfentanyl claim 4 , 3-Methylfentanyl claim 4 , Carfentanil claim 4 , Alfentanil claim 4 , Oxymorphone claim 4 , Noroxymorphone claim 4 , Hydromorphone claim 4 , Tapentadol claim 4 , Oxycodone claim 4 , Hydrocodone claim 4 , eroin claim 4 , Diacetylmorphine claim 4 , Codeine claim 4 , Meperidine claim 4 , Dextropropoxyphene claim 4 , Papaverine claim 4 , Levacetylmethado claim 4 , Tramadol claim 4 , Levorphanol claim 4 , Methadone claim 4 , Butorphanol claim 4 , Pentazocine claim 4 , and Nalbuphine.6. A method of agonizing the CB2 receptor comprising ...

KALLIKREIN 7 INHIBITORS

The present invention relates to methods for inhibiting the activity of human kallikrein 7 (KLK7) (also known as serine protease stratum corneum chymotryptic enzyme, SCCE). The invention further relates to the use of KLK7 inhibitors of Formula I for the treatment and prevention of diseases, more specifically for the treatment and prevention of skin diseases. The invention also provides new compounds demonstrated to be inhibitors of KLK7. 2. The compound according to{'sub': '1', 'wherein Ris selected from phenyl, substituted phenyl, isoxazolyl, substituted isoxazolyl;'}{'sub': 2', '1', '6', '1', '3', '1', '6, 'Ris selected from hydrogen, —C-C-alkyl, C-C-alkyloxy-C-C-alkyl, and phenyl;'}{'sub': 3', '1', '3', '5', '5, 'Ris selected from alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, and —C-C-alkyl-R, wherein Ris selected from cycloalkyl, substituted cycloalkyl, aryl, substituted aryl;'}{'sub': 4', '6, 'Ris selected from hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, and —NH—CO—R,'}{'sub': '6', 'wherein Ris selected from aryl, and substituted aryl;'}or a pharmaceutical acceptable salt thereof,for use in the prophylaxis, prevention, or treatment of a skin disease.3. The compound according to claim 1 , or a pharmaceutical acceptable salt thereof claim 1 , for use in the prophylaxis claim 1 , prevention claim 1 , or treatment of an inflammatory skin disease.4. The compound according to claim 1 , or a pharmaceutical acceptable salt thereof claim 1 , for use in the prophylaxis claim 1 , prevention claim 1 , or treatment of a skin disease claim 1 , wherein the skin disease is selected from Netherton syndrome claim 1 , atopic dermatitis claim 1 , contact dermatitis claim 1 , eczema claim 1 , psoriasis claim 1 , acne claim 1 , epidermal hyperkeratosis claim 1 , acanthosis claim 1 , epidermal inflammation claim 1 , dermal inflammation and pruritus.5. A method for the prophylaxis claim 1 , prevention claim 1 , or treatment of a ...

Synergistic Compositions and Devices for Gynecological Procedures

Synergistic compositions and medical devices for use in treatment during gynecological procedures are provided. A gynecological device for treatment of cervical blockages without general anesthesia thereby suitable for out-patient service, saving time and money to the patients is provided. Synergistic compositions that enable the practioners to perform gynecological procedures without pain or bleeding to the patients are provided. 1. A dilating device for unblocking cervix pathway , comprising the following parts;(a) a shaft with a head at one end and a threaded part at the other end,(b) a tubular structure as middle or connecting part covering the shaft,(c) a base or handle part,(d) a taper part to precede the middle part with provision(s) on its external surface to connect with a patch and{'i': 'Plantago ovato', '(e) a cone or patch.'}2. The device of claim 1 , wherein the central part of the shaft of the device between the head and the threaded part is unthreaded.3. The device of claim 1 , wherein the central part of the shaft comprises a plurality of bores.4. The device of claim 1 , wherein said central part of the shaft comprises means for fluid transmission claim 1 , a light source claim 1 , a fluorescent probe claim 1 , camera connectivity claim 1 , a surgical probe claim 1 , a drain provision to remove any undesired liquid claim 1 , during the procedure.5. The device of claim 2 , wherein said central part of the shaft is covered by a tubular structure claim 2 , to connect the taper part and base or handle part of the device having a smooth external surface and the tubular part is provided with a horizontal bore sufficient enough to allow the shaft to pass through.6. The device of claim 1 , wherein said base or handle part is tubular inside with a threaded part and an unthreaded part claim 1 , having external side tapered towards the head of the shaft claim 1 , with wider portion at the end to hold the device externally.7. The device of claim 5 , wherein said ...

METHODS FOR TREATMENT OF ATHEROSCLEROSIS

Disclosed herein are methods and compositions for preventing or treating atherosclerosis in a mammalian subject. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide and, in some applications, a second active agent, to subjects in need thereof. The present technology relates to the treatment or prevention of atherosclerosis in mammals through the administration of a therapeutically effective amount of aromatic cationic peptides and, in some embodiments, a second active agent. 130.-. (canceled)31. A method for delaying onset , ameliorating or eliminating statin side effects in a subject in need thereof , the method comprising administering simultaneously , separately or sequentially with the statin , an effective amount of a peptide D-Arg-2′6′-Dmt-Lys-Phe-NHor a pharmaceutically acceptable salt thereof , wherein the statin side effect comprises mitochondrial dysfunction.32. The method of claim 31 , wherein the statin is selected from the group consisting of: atorvastatin claim 31 , simvastatin claim 31 , pravastatin claim 31 , fluvastatin claim 31 , lovastatin claim 31 , pitavastatin claim 31 , rosuvastatin claim 31 , niacin extended-release/lovastatin claim 31 , lovastatin extended-release claim 31 , amlodipine claim 31 , atorvastatin claim 31 , rosuvastatin claim 31 , sitagliptin/simvastatin claim 31 , fluvastatin claim 31 , fluvastatin extended-release claim 31 , atorvastatin claim 31 , pitavastatin claim 31 , lovastatin claim 31 , pravastatin claim 31 , niacin extended-release/simvastatin claim 31 , ezetimibe/simvastatin claim 31 , and simvastatin.33. The method of claim 31 , wherein the peptide and statin are administered sequentially in either order.34. The method of claim 31 , wherein the pharmaceutically acceptable salt comprises acetate salt or trifluoroacetate salt.35. The method of claim 31 , wherein the statin comprises rosuvastatin or atorvastatin. This application claims the benefit of and priority to U.S ...

COMPOSITIONS OF JASMONATE COMPOUNDS AND METHODS OF USE

The disclosure describes nanocarried and/or microcarried jasmonate compounds and their pharmaceutical compositions, as well as use thereof for treating or preventing angiogenesis-related or NF-κB-related disorders. Also disclosed are methods of making the nanocarried and/or microcarried compounds and their compositions. 1. A pharmaceutical composition comprising a pharmaceutically acceptable solvent and a plurality of nanocarriers or microcarriers that contain a jasmonate compound , whereinthe nanocarriers or microcarriers are formed of a cyclodextrin or a dendrimer, or are synthetic nanoemulsion particles (LDEs) comprising a cholesteryl ester core surrounded by a phospholipid layer;the nanocarriers have a size ranging from 1 nanometer (nm) to 900 nm; orthe microcarriers have a size ranging from 1 micron to 50 micron; andthe pharmaceutical composition has a concentration of the jasmonate compound ranging from 1 nM to 1 M.2. The pharmaceutical composition of claim 1 , wherein the jasmonate compound is selected from the group consisting of jasmonic acid claim 1 , 7-iso -jasmonic acid claim 1 , 9 claim 1 ,10-dihydrojasmonic acid claim 1 , 9 claim 1 ,10-dihydro-isojasmonic acid claim 1 , 2 claim 1 ,3-didehydrojasmonic acid claim 1 , 3 claim 1 ,4-didehydrojasmonic acid claim 1 , 3 claim 1 ,7-didehydrojasmonic acid claim 1 , 4 claim 1 ,5-didehydrojasmonic acid claim 1 , 4 claim 1 ,5-didehydro-7-isojasmonic acid claim 1 , cucurbic acid claim 1 , 6-epi-cucurbic acid claim 1 , 6-epi-cucurbic acid-lactone claim 1 , 12-hydroxy-jasmonic acid claim 1 , 12-hydroxy-jasmonic acid-lactone claim 1 , 11-hydroxy-jasmonic acid claim 1 , 8-hydroxy-jasmonic acid claim 1 , homo-jasmonic acid claim 1 , dihomo-jasmonic acid claim 1 , 11-hydroxy-dihomo-jasmonic acid claim 1 , 8-hydroxy-dihomo-jasmonic acid claim 1 , tuberonic acid claim 1 , tuberonic acid-O-β-glucopyranoside claim 1 , cucurbic acid-O-β-glucopyranoside claim 1 , 5 claim 1 ,6-didehydro-jasmonic acid claim 1 , 6 claim 1 ,7- ...

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.

Prodrug derivatives of protein kinase c modulators

Embodiments of prodrugs of PKC modulators that show efficacy coupled with low levels of toxicity and improved stability are provided. The prodrug compounds are useful in academic research (animal studies), as candidates for preclinical research, and as therapeutic agents. By taking advantage of a pharmacophore-based strategy, this design strategy provides access to prodrugs of PKC modulators of diverse scaffolds including tigliane diterpenes, ingenane diterpenes, daphnane diterpene orthoesters, diacylglycerols, and bryostatins, and analogs thereof. In particular, embodiments of the prodrug ingenane esters having substitutions at C20 and their use as therapeutic agents are provided.

METHODS FOR ASSESSING RESPONSIVENESS TO ASTHMA TREATMENT BASED ON VNN-1 EXPRESSION AND PROMOTER METHYLATION

Provided herein are methods and kits related to use of vanin-1 (VNN1) expression for assessing responsiveness to steroid treatment in subjects with asthma and for treating subjects with asthma. 126-. (canceled)27. A method of treating a subject with asthma , the method comprising:administering an effective amount of cysteamine or a pharmaceutically acceptable salt thereof to a subject having asthma, wherein the subject does not respond to a steroid treatment.2831-. (canceled)32. The method of claim 27 , wherein the pharmaceutically acceptable salt of cysteamine is cysteamine bitartrate or cysteamine hydrochloride.33. The method of claim 27 , wherein the cysteamine is in disulfide form.34. The method of claim 27 , further comprising applying to the subject a non-steroid treatment for asthma.35. The method of claim 34 , wherein the non-steroid treatment involves a mast cell stabilizer claim 34 , a leukotriene modifier claim 34 , an immunomodulator claim 34 , or a combination thereof.36. The method of claim 27 , wherein the subject is a human patient free of steroid treatment.37. The method of claim 27 , wherein the cysteamine or the pharmaceutically acceptable salt thereof is administered to the subject orally or by injection.38. The method of claim 27 , wherein the cysteamine or the pharmaceutically acceptable salt thereof is formulated in a pharmaceutical formulation claim 27 , which is in an enteric-coated solid form or in a sustained-release form.39. The method of claim 27 , wherein the subject is a human adult.40. The method of claim 27 , wherein the subject is a human child who is 18 years old or younger. This application is a national stage filing under 35 U.S.C. § 371 of PCT International Application No. PCT/US2015/030984, which has an international filing date of May 15, 2015, and claims the benefit under 35 U.S.C. § 119(e) of U.S. provisional application No. 61/994,477, filed May 16, 2014, the contents of each of which are incorporated by reference herein in ...

MISOPROSTOL DISPERSIBLE TABLET

The present invention relates to a solid pharmaceutical formulation comprising misoprostol or a pharmaceutically acceptable salt thereof. In particular, the invention relates to a dispersible tablet comprising misoprostol or a pharmaceutically acceptable salt thereof. 1. A pharmaceutical dosage form comprising misoprostol or a pharmaceutically acceptable salt thereof as the sole active ingredient , wherein said dosage form is suitable for both sublingual and oral administration.2. (canceled)3. The pharmaceutical dosage form according to claim 1 , further comprising cross-linked polyvinylpyrrolidone as a disintegrant.4. The pharmaceutical dosage form according to claim 1 , further comprising at least two disintegrants.5. The pharmaceutical dosage form according to claim 4 , wherein at least one of said disintegrants is a cross-linked carboxymethylcellulose.6. The pharmaceutical dosage form according to claim 4 , wherein said disintegrants use at least two different mechanisms of disintegration.7. The pharmaceutical dosage form according to claim 6 , wherein said mechanisms of disintegration are selected from the group consisting of swelling claim 6 , porosity and capillary action claim 6 , and deformation.8. The pharmaceutical dosage form according to claim 4 , wherein said disintegrants are superdisintegrants.9. The pharmaceutical dosage form according to claim 1 , further comprising a starch as a disintegrant.10. The pharmaceutical dosage form according to claim 9 , further comprising at least one superdisintegrant.11. The pharmaceutical dosage form according to claim 1 , further comprising an excipient selected from the group consisting of maize starch claim 1 , potato starch claim 1 , pea starch claim 1 , rice starch claim 1 , tapioca starch claim 1 , wheat starch claim 1 , and modified starch.12. The pharmaceutical dosage form according to claim 11 , wherein said excipient is maize starch.13. The pharmaceutical dosage form according to claim 1 , further ...

Neuronal circuit-dependent neuroprotection by interaction between nicotinic receptors

A method of inhibiting excitotoxicity by indirectly activating α4β2 nicotinic acetylcholine receptors (nAChRs) which indirectly activate synaptic AMPA and NMDA receptors is disclosed. Inhibitors of α7 nACHRs, such as macrocyclic diterpenoids, more specifically cembranoids or methyllycaconitine (MLA), indirectly activate α4β2 nAChRs and can be used to treat neurodegenerative diseases, including, but not limited to, Alzheimer's Disease, Parkinson Disease, AIDS related dementia and the delayed effects of stroke. They can also be used to treat diseases associated with neuronal impairment, including, but not limited to glaucoma caused by optical nerve damage, delayed effects of epilepsy; and multiple sclerosis.

LOCAL TOPICAL ADMINISTRATION FORMULATIONS CONTAINING INDOXACARB

The present invention provides formulations and methods useful in the control of ectoparasites on a domestic animal, using a formulation comprising Indoxacarb and a veterinarily acceptable carrier that is applied topically to 10% or less of the total surface area of a domestic animal. Other embodiments include these formulations also including one or more additional pesticides such as fipronil. 2: The formulation of claim 1 , wherein said ectoparasite is an Arthropod.3: The formulation of claim 2 , wherein said Arthropod is an Insecta.4: The formulation of claim 3 , wherein said Insecta is a flea claim 3 , fly claim 3 , or louse.5: The formulation of claim 2 , wherein said Arthropod is an Arachnida.68-. (canceled)9: The formulation of claim 1 , wherein said veterinarily acceptable carrier further comprises one or more of a crystallization inhibitor claim 1 , adjuvant claim 1 , co-solvent claim 1 , colorant claim 1 , surfactant claim 1 , spreading oil claim 1 , antioxidant claim 1 , light stabilizer or tackifier.10. (canceled)11: The formulation of claim 1 , wherein said solvent comprises propylene glycol monomethyl ether.12. (canceled)13: The formulation of claim 1 , wherein said solvent comprises ethyl acetoacetate.14: The formulation of claim 9 , wherein said crystallization inhibitor is triacetin.15: The formulation of claim 1 , wherein said domestic animal is a mammal.16: The formulation of claim 15 , wherein said mammal is a canine.1724-. (canceled)25: A method for the control of ectoparasites on a domestic animal comprising topically applying to a localized region having a surface area of less than or equal to 10% of the total surface area of said domestic animal the formulation of .26: The method of claim 25 , wherein said localized region has a surface area less than or equal to 5% of the total surface area of said domestic animal.27: The method of claim 25 , wherein said domestic animal is a canine and said localized region of said canine is less than 10 cm ...

Pharmaceutical composition for neuropathic pain

The present application describes a pharmaceutical composition/formulation for use in controlling neuropathic pain. The composition/formulation includes Palmitoylethanolamide (PEA) and one or more natural ingredients. The application also provides various formulations and methods of preparing the same.

Compositions and Methods for Treating Chronic Inflammation and Inflammatory Diseases

The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions. 1. A pharmaceutical composition comprising:a) a therapeutically effective amount of a pharmaceutically-acceptable form of a propionic acid derived non-steroidal anti-inflammatory drug (NSAID);b) less than about 20% by weight of the composition of a pharmaceutically-acceptable liquid polyethylene glycol (PEG) polymer; andc) at least 50% by weight of the composition of pharmaceutically-acceptable glycerolipids comprising monoglycerides, diglycerides, and triglycerides;wherein the pharmaceutical composition is formulated to have a melting point temperature of about 30° C. or higher.2. The pharmaceutical composition according to claim 1 , wherein the concentration of the propionic acid derived NSAID is at least 50 mg/mL.3. The pharmaceutical composition according to claim 2 , wherein the concentration of the propionic acid derived NSAID is about 100 mg/mL to about 750 mg/mL.4. The pharmaceutical composition according to claim 1 , wherein the propionic acid derived NSAID is a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or solvate of a salt thereof.5. The pharmaceutical composition according to claim 1 , wherein the propionic acid derived NSAID comprises an Alminoprofen claim 1 , a Benoxaprofen claim 1 , a Dexketoprofen claim 1 , a Fenoprofen claim 1 , a Flurbiprofen claim 1 , an Ibuprofen claim 1 , an Indoprofen claim 1 , a Ketoprofen claim 1 , a Loxoprofen claim 1 , a Naproxen claim 1 , an Oxaprozin claim 1 , a Pranoprofen claim 1 , or a Suprofen.6. The pharmaceutical composition according to claim 1 , wherein the propionic acid derived NSAID is an ester thereof.7. The pharmaceutical composition according to claim 1 , wherein the liquid PEG polymer is in an amount of less than about 15% by ...

SELF-EMULSIFYING FORMULATIONS OF DIM-RELATED INDOLES

Disclosed herein are self-emulsifying compositions and formulations of Diindolylmethane (“DIM”) and certain derivatives of DIM, their uses and methods of making. In particular, the disclosed compositions comprise a DIM-related indole as an active agent and a carrier, wherein the carrier comprises a solvent, one or more surfactants with an HLB of greater than 7, and one or more co-surfactants with an HLB equal to or less than 7. In certain aspects of the invention, the compositions disclosed herein show improved bioavailability. 1. A composition comprising a DIM-related indole having log P from 3 to 5.5 as the biologically active agent and a carrier of said active agent , wherein the carrier comprises:(i) a carrier solvent, wherein the carrier solvent is caprylocaproyl polyoxyl-8 glyceride, a diethylene glycol monoethyl ether, propylene glycol, or an essential oil;(ii) one or more surfactants comprising at least one of: Polysorbate 80, a lauroyl polyoxyl-32 glyceride, and a polyoxyethyl hydroxyl stearate; and(iii) one or more co-surfactants comprising at least one of: a lecithin, Propylene Glycol Caprylate, a phosphatidic acid derivative of Propylene Glycol Caprylate, and Oleoyl polyoxyl-6 glyceride.2. The composition of claim 1 , wherein the carrier is a solution or a suspension.3. The composition of or claim 1 , wherein the DIM-related indole is dissolved in the carrier claim 1 , and/or wherein the DIM-related indole has more than 10% solubility in the solvent.4. The composition of claim 1 , wherein the one or more co-surfactants comprise a lecithin.5. The composition of claim 4 , wherein the lecithin is phosphatidyl choline or lysophosphatidyl choline.6. The composition of claim 5 , wherein the lecithin is phosphatidyl choline.7. The composition of claim 1 , wherein the one or more co-surfactants comprise Propylene Glycol Caprylate or a phosphatidic acid derivative thereof.8. The composition of claim 1 , which comprises at least two co-surfactants claim 1 , and at ...

NEUTRALIZING ANTI-INFLUENZA A ANTIBODIES AND USES THEREOF

The invention relates to antibodies and binding fragments thereof that are capable of binding to influenza A virus hemagglutinin and neutralizing at least one group 1 subtype and at least 1 group 2 subtype of influenza A virus. 1. An isolated antibody or a binding fragment thereof that is capable of binding to influenza A virus hemagglutinin and neutralizing at least one group 1 subtype and at least 1 group 2 subtype of influenza A virus.2. An antibody or binding fragment according to claim 1 , wherein the antibody or binding fragment is capable of neutralizing one or more influenza A virus group 1 subtype selected from: H1 claim 1 , H2 claim 1 , H5 claim 1 , H6 claim 1 , H8 claim 1 , H9 claim 1 , H11 claim 1 , H12 claim 1 , H13 claim 1 , H16 and variants thereof; and one or more influenza A virus group 2 subtypes selected from: H3 claim 1 , H4 claim 1 , H7 claim 1 , H10 claim 1 , H14 and H15 and variants thereof.3. An antibody or binding fragment thereof according to any one of the preceding claims claim 1 , wherein the antibody or binding fragment is capable of neutralizing group 1 subtypes: H1 claim 1 , H2 claim 1 , H5 claim 1 , H6 and H9 and group 2 subtypes H3 and H7; or wherein the antibody or binding fragment is capable of neutralizing group 1 subtypes: H1 claim 1 , H2 claim 1 , H5 and H6 and group 2 subtypes H3 and H7.4. An antibody or binding fragment thereof according to any one of the preceding claims claim 1 , wherein the antibody or binding fragment has high neutralizing potency expressed as 50% inhibitory concentration (ICug/ml) in the range of from about 0.01 ug/ml to about 50 ug/ml of antibody for neutralization of influenza A virus in a microneutralization assay.5. An antibody or binding fragment thereof according to according to any one of the preceding claims claim 1 , wherein the antibody or fragment thereof includes a set of six CDRs: HCDR1 claim 1 , HCDR2 claim 1 , HCDR3 claim 1 , LCDR1 claim 1 , LCDR2 claim 1 , LCDR3 in which the set of six ...

ANTIVIRAL TREATMENTS

The invention provides unit dosage forms, kits, and methods useful for treating viral infections. 3. The method of claim 1 , wherein the viral infection is an influenza infection.4. The method of claim 3 , wherein the influenza infection is an influenza type A or type B infection.5. The method of claim 1 , wherein the viral infection is caused by a strain of virus represented by the formula HNwherein X is an integer from 1-16 and Y is an integer from 1-9.6. The method of claim 3 , wherein the influenza is an: H3N2 claim 3 , H1N1 claim 3 , H5N1 claim 3 , avian claim 3 , or seasonal influenza.7. The method of claim 1 , wherein the effective anti-viral amount is up to 800 mg.8. The method of claim 1 , wherein the effective anti-viral amount is up to 600 mg.9. The method of claim 1 , wherein the effective anti-viral amount is up to 400 mg.10. The method of claim 1 , wherein the effective anti-viral amount is up to 200 mg.11. The method of claim 1 , wherein the effective anti-viral amount is up to 100 mg.12. The method of claim 1 , wherein the effective anti-viral amount is up to 75 mg.13. The method of claim 1 , wherein the entire effective anti-viral amount is administered in one intravenous administration.14. The method of claim 1 , wherein the entire effective anti-viral amount is administered in multiple intravenous administrations.15. The method of claim 2 , wherein a compound or formula Ia claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , is administered.16. The method claim 1 , wherein the plasma concentration of the compound is higher than the ICof the virus causing the viral infection 48 hours following administration of the compound.17. The method of claim 1 , further comprising orally administering a neuraminidase inhibitor to the human.20. The method of claim 18 , further comprising orally administering a neuraminidase inhibitor to the human. This application is a continuation of U.S. patent application Ser. No. 14/313,738, filed Jun. 24, ...

RECOVERY AND PROCESSING OF HUMAN EMBRYOS FORMED IN VIVO

A kit having instructions for use for performing uterine lavage in a female patient includes a uterine lavage catheter configured for insertion into a woman's uterus to remove viable blastocysts from the uterus, and one or more first containers having a sufficient dosage amount of a GnRH antagonist to cause desynchronization of the endometrium of the patient prior to, during and/or following recovery of viable blastocysts from the uterus. 1. A method comprising:providing a fluid delivery and collection device; andprogramming a controller to deliver lavage liquid from the fluid delivery and collection device to the uterus to assist with the recovery of blastocysts from the uterus at a flow of fluid supply that substantially limits or prevents leakage of fluid into the fallopian tubes by limiting the total volume of liquid in the uterus at any given time to not exceed 10 mL.2. The method of claim 1 , further comprising programming the controller to control the flow of fluid supply such that it does not exceed a maximum pressure of the device of between about 2 ounces per square inch and 50 pounds of pressure per square inch.3. The method of claim 1 , further comprising programming the controller to control the flow of fluid supply such that it does not exceed a maximum pressure of the device of between about 2 ounces per square inch and 20 pounds of pressure per square inch.4. The method of claim 1 , further comprising programming the controller to control the delivery of the fluid through the fluid delivery and collection device into the uterus in a series of pulses at a pre-determined pulse rate.5. The method of claim 4 , wherein the pulse rate has a preset frequency in the range of one pulse per 0.5 to 4 seconds.6. The method of claim 1 , wherein the controller is programmed to automatically control the delivery of the fluid through the fluid delivery and collection device into the uterus.7. A method comprising:providing a fluid delivery and collection device; ...

Method of treating influenza a

Provided herein are methods for treating, reducing or preventing influenza A virus infection in a patient, as well as compositions and articles of manufacture for treating, reducing or preventing influenza A virus infection in a patient.

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.

Compositions and Methods For Targeting Cancers

In various aspects and embodiments the invention provides a method of treating or preventing a cancer in a mammalian subject in need thereof, the method comprising administering to the subject a therapeutically effective amount of at least one compound selected from the group consisting of a DNA repair inhibitor, a DNA strand break repair inhibitor, and a homologous recombination (HR) repair inhibitor, wherein cells in the cancer comprise a fumarate hydratase (FH) and/or succinate dehydrogenase (SDH) mutation.

Human antibodies to influenza hemagglutinin

The present invention provides monoclonal antibodies, or antigen-binding fragments thereof, that bind to the influenza hemagglutinin (HA) protein, pharmaceutical compositions comprising the antibodies and methods of use. The antibodies of the invention are useful for inhibiting or neutralizing influenza virus activity, thus providing a means of treating or preventing influenza infection in humans. In some embodiments, the invention provides for use of one or more antibodies that bind to the influenza HA for preventing viral attachment and/or entry into host cells. The antibodies of the invention may be used prophylactically or therapeutically and may be used alone or in combination with one or more other anti-viral agents or vaccines.

Parasiticidal compositions comprising an isoxazoline active agent, methods and uses thereof

This invention relates to topical compositions for combating ectoparasites and endoparasites in animals, comprising at least one isoxazoline active agent and a pharmaceutically acceptable carrier, optionally in combination with one or more additional active agents. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof.

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: ...

ANTIVIRAL TREATMENTS

The invention provides unit dosage forms, kits, and methods useful for treating viral infections. 3. The method of claim 1 , wherein the effective anti-viral amount is less than or equal to 500 mg.4. The method of claim 1 , wherein the effective anti-viral amount is less than or equal to 400 mg.5. The method of claim 1 , wherein the effective anti-viral amount is less than or equal to 300 mg.6. The method of claim 1 , wherein the effective anti-viral amount is less than or equal to 200 mg.7. The method of claim 1 , wherein the effective anti-viral amount is less than or equal to 150 mg.8. The method of claim 1 , wherein the effective anti-viral amount is less than or equal to 75 mg.9. The method of claim 1 , wherein the effective anti-viral amount is 600 mg.10. The method of claim 1 , wherein the effective anti-viral amount is 300 mg.11. The method of claim 1 , wherein the influenza viral infection is the type A influenza viral infection.12. The method of claim 1 , wherein the influenza viral infection is the type B influenza viral infection.13. The method of claim 1 , wherein the influenza viral infection is the seasonal influenza viral infection.14. The method of claim 1 , further comprising orally administering a neuraminidase inhibitor to the human.15. The method of claim 14 , wherein the neuraminidase inhibitor that is administered orally is oseltamivir carboxylate.19. The method of claim 14 , wherein the neuraminidase inhibitor that is administered orally is administered for up to 20 days.20. The method of claim 14 , wherein the neuraminidase inhibitor that is administered orally is administered for up to 10 days.21. The method of claim 14 , wherein the neuraminidase inhibitor that is administered orally is administered for up to 5 days.22. The method of claim 1 , wherein the effective anti-viral amount is less than or equal to 800 mg.23. The method of claim 1 , wherein the effective anti-viral amount is less than or equal to 600 mg. This application is a ...

Methods and Compositions for Inhibition of Polymerase

The present invention is directed to methods and compositions for inhibition of viral nucleic acid polymerases, such as RNA and DNA polymerases, and methods and compositions that are useful for treating viral infections in subjects. The methods comprise administering to the subject a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, or a composition comprising a compound of formula I, or a pharmaceutically acceptable salt or hydrate thereof, and a pharmaceutically acceptable carrier. The composition or method may optionally comprise one or more additional anti-viral agents. 2. The method of claim 1 , wherein the virus is selected from the group consisting of Ebola and Marburg viruses.3. The method of claim 2 , wherein the virus is Ebola virus.4. The method of claim 2 , wherein the virus is Marburg virus.5. The method of claim 2 , further comprising co-administering to the human subject an effective amount of an anti-viral agent.6. The method of claim 5 , wherein the anti-viral agent is a neuraminidase inhibitor.7. The method of claim 5 , wherein the anti-viral agent is selected from the group consisting of laninamivir claim 5 , oseltamivir claim 5 , zanamivir claim 5 , and peramivir.8. The method of claim 5 , wherein the anti-viral agent is peramivir.9. The method of claim 2 , wherein the compound is administered intravenously claim 2 , intraperitoneally claim 2 , intramuscularly claim 2 , or orally.11. The method of claim 10 , wherein the virus is selected from the group consisting of Ebola and Marburg viruses.12. The method of claim 11 , wherein the virus is Ebola virus.13. The method of claim 11 , wherein the virus is Marburg virus.14. The method of claim 11 , further comprising co-administering to the human subject an effective amount of an anti-viral agent.15. The method of claim 14 , wherein the anti-viral agent is a neuraminidase inhibitor.16. The method of claim 14 , wherein the anti-viral ...

MARINE ORGANISM-DERIVED EXTRACT, COMPOUND, AND MEDICAL COMPOSITION HAVING NICHE FORMATION SUPPRESSING ACTIVITY OF LEUKEMIC STEM CELLS

Using the cobblestone area (CA) formation inhibitory activity of human leukemic stem cell-like cells as an indicator, a fraction having the activity has been extracted from the fat-soluble fraction of Porifera, then, a compound having the activity has been isolated and purified from the aforementioned fraction, and then, the structure thereof has been determined, so that a Stelliferin compound comprising a novel compound has been identified. Moreover, it has been found that the isolated and purified Stelliferin compound significantly suppresses the niche formation of leukemic stem cell-like cells derived from human chronic myelogenous leukemia (CML) having resistance to existing antitumor agents and enhances the effects of antitumor agents on the cells. The present invention provides a pharmaceutical composition having inhibitory or suppressive activity against the niche formation of leukemic stem cells, a prophylactic agent against the recurrence of malignant tumor, which involves the combined use of other antitumor drugs, and the like. 2. The extract of claim 1 , wherein the Stelliferin compound is selected from the group consisting of Stelliferin A claim 1 , Stelliferin B claim 1 , a diastereomer of Stelliferin A claim 1 , a diastereomer of Stelliferin B claim 1 , an enantiomer of Stelliferin A claim 1 , and an enantiomer of Stelliferin B.5. An inhibitor of a niche formation of a tumor cell claim 1 , the inhibitor comprising the extract of .6. An inhibitor of a niche formation of a tumor cell claim 3 , the inhibitor comprising the compound of .7. The inhibitor of claim 5 , wherein the tumor cell is a cancer stem cell claim 5 , a leukemic stem cell claim 5 , or a chronic myelogenous leukemic cell.8. An antitumor pharmaceutical composition claim 1 , comprising the extract of and at least one antitumor agent.9. The antitumor pharmaceutical composition of claim 8 , wherein each antitumor agent is independently selected from the group consisting of ibritumomab ...

WATER-SWELLABLE POLYMERS

A water-swellable linear polyurethane polymer is formed by reacting a polyethylene oxide (e.g. PEG 4000 to 35,000), a difunctional compound (e.g. a diamine or diol such as 1,10-decanediol) with a diisocyanate. The ratio of the three components is generally in the range 0.1-1.5 to 1 to 1.1-2.5. The polyurethane is water-swellable in the range 300 to 1700% and soluble in certain organic solvents such as dichloromethane. It can be loaded with pharmaceutically active agents, particularly of high molecular weight, to produce controlled release compositions, such as pessaries etc. 120-. (canceled)21. A controlled release composition , comprising a cross-linked polyurethane polymer loaded with misoprostol;wherein the cross-linked polyurethane polymer is formed from a polyethylene glycol, a triol and a diisocyanate, and at least about 80% of the misoprostol is released when the composition is immersed in water at 37° C. for 480 minutes.22. The composition of claim 21 , wherein the cross-linked polyurethane polymer is formed from PEG8000 claim 21 , hexanetriol and dicyclohexylmethane-4 claim 21 ,4-diisocyanate.23. The composition of claim 22 , wherein the ratio of PEG8000:hexanetriol:dicyclohexylmethane-4 claim 22 ,4-diisocyanate is in the range of 0.8-1.0:1.0-1.2:2.3-2.8.24. The composition of claim 23 , wherein the ratio of PEG8000:hexanetriol:dicyclohexylmethane-4 claim 23 ,4-diisocyanate is 1.0:1.2:2.8.25. The composition of claim 23 , wherein the ratio of PEG8000:hexanetriol:dicyclohexylmethane-4 claim 23 ,4-diisocyanate is 0.8:1.0:2.3.2620. The composition of claim claim 23 , wherein the misoprostol content is 200 μg.2720. The composition of claim claim 23 , wherein the composition is in the form of a pessary.28. The composition of claim 27 , wherein the composition has been dried in a vacuum oven at room temperature for at least 24 hours.29. The composition of claim 27 , wherein the composition has a misoprostol release rate of 4.507 minute.3020. The composition of ...

METHODS AND COMPOSITIONS COMPRISING A NITRITE-REDUCTASE PROMOTER FOR TREATMENT OF MEDICAL DISORDERS AND PRESERVATION OF BLOOD PRODUCTS

The invention provides methods, compositions, and medical kits comprising a nitrite-reductase promoter, such as an allosteric modulator of hemoglobin, for use in treating medical disorders and preservation of blood products. In one aspect, the invention provides methods, compositions, and medical kits comprising an inorganic nitrite salt and a nitrite-reductase promoter, such as an allosteric modulator of hemoglobin, for use in treating medical disorders, such as cancer, cardiovascular disorders, ischemic conditions, hemolytic conditions, and bacterial infections. Exemplary inorganic nitrite salts include sodium nitrite and arginine nitrite. Exemplary allosteric modulators of hemoglobin described herein include alkyl-substituted and acyl-substituted di-nitroheterocycles. 137-. (canceled)39. (canceled)41. The method of claim 40 , wherein the blood product comprises erythrocyte cells.42. The method of claim 41 , wherein the blood product comprises blood plasma.43. (canceled)44. (canceled)45. (canceled)46. The method of claim 40 , further comprising administering an alkali metal nitrite to the patient.47. The method of claim 40 , further comprising administering sodium nitrite to the patient.4856-. (canceled)57. The method of claim 40 , wherein the therapeutic agent is an organonitro compound of Formula I.58. The method of claim 40 , wherein the therapeutic agent is an erythrocyte cell that has been exposed to an organonitro compound of Formula I claim 40 , and said therapeutic agent is administered by injection.59. (canceled)60. The method of claim 57 , wherein Ris bromo.61. The method of claim 60 , wherein n is 0 claim 60 , and m is 2.63. The method of claim 40 , wherein the therapeutic agent is a hemoglobin conjugate of Formula III claim 40 , and said therapeutic agent is administered by injection.64. (canceled)65. (canceled)67106-. (canceled)109. The method of claim 107 , wherein the blood product comprises erythrocyte cells.110. The method of claim 108 , wherein ...

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 ...

CONTROLLED RELEASE PHARMACEUTICAL COMPOSITIONS COMPRISING A FUMARIC ACID ESTER

The present invention relates to controlled release pharmaceutical compositions comprising fumaric acid ester(s) as active substance(s). The compositions are suitable for use in the treatment of e.g. psoriasis or other hyperproliferative, inflammatory or autoimmune disorders and are designated to release the fumaric acid ester in a controlled manner so that local high concentrations of the active substance within the gastrointestinal tract upon oral administration can be avoided and, thereby, enabling a reduction in gastro-intestinal related side-effects. 1. A pharmaceutical composition comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid , or a pharmaceutically acceptable salt thereof , which—upon oral administration and in comparison to that obtained after oral administration of Fumaderm® tablets in an equivalent dosage—gives a reduction in GI related side effects.2. The pharmaceutical composition according to in the form of a controlled release composition.3. A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of fumaric acid claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the release of the fumaric acid ester—when subjected to an in vitro dissolution test employing 0.1 N hydrochloric acid as dissolution medium during the first 2 hours of the test and then 0.05 M phosphate buffer pH 6.5 as dissolution medium—is as follows:within the first 3 hours after start of the test at the most about 70% w/w of the total amount of the fumaric acid ester contained in the composition is released.4. A controlled release pharmaceutical composition for oral use comprising as an active substance one or more fumaric acid esters selected from di-(C-C)alkylesters of fumaric acid and mono-(C-C)alkylesters of ...

METHODS OF PREVENTING SECONDARY INFECTIONS

A method of treating or preventing a disease associated with a secondary infection in a subject infected with a pathogen is provided. The method comprises administering to the subject a therapeutically effective amount of an anti-pathogenic agent directed towards the pathogen and a therapeutically effective amount of an agent which down-regulates at least one extracellular matrix-associated polypeptide. 117-. (canceled)18. A method of preventing a disease associated with a secondary infection in a subject infected with a pathogen comprising administering to the subject a therapeutically effective amount of an anti-pathogenic agent directed towards said pathogen and a therapeutically effective amount of an agent which down-regulates at least one extracellular matrix-associated polypeptide , thereby preventing the disease associated with a secondary infection in the subject.19. A method of treating a subject infected with a pathogen comprising administering to the subject a therapeutically effective amount of an anti-pathogenic agent directed towards said pathogen and a therapeutically effective amount of an agent which down-regulates membrane type 1-matrix metalloproteinase 1 (MT1-MMP1) , thereby treating the subject.20. The method of claim 18 , wherein said extracellular matrix-associated polypeptide is set forth in Table 1.21. The method of claim 18 , wherein said secondary infection is a blood infection.22. The method of claim 18 , wherein said disease is sepsis.2324-. (canceled)25. The method of claim 18 , wherein said extracellular matrix-associated polypeptide is selected from the group consisting of membrane type 1-matrix metalloproteinase 1 (MT1-MMP1) claim 18 , MMP-9 claim 18 , MMP-8 and MMP-3.2628-. (canceled)29. The method of claim 18 , wherein said virus is a respiratory virus.30. The method of claim 29 , wherein said respiratory virus is influenza.31. The method of claim 18 , wherein said anti-pathogenic agent is a neuraminidase inhibitor (NAI).32. The ...

THERAPEUTIC REGIMEN AND METHODS FOR TREATING OR AMELIORATING VISUAL DISORDERS ASSOCIATED WITH AN ENDOGENOUS RETINOID DEFICIENCY

Disclosed herein are therapeutic regimens for treating or ameliorating a visual disorder associate with an endogenous retinoid deficiency in a subject by administering a therapeutically effective amount of a synthetic retinal derivative or a pharmaceutically acceptable composition comprising a synthetic retinal derivative according to the therapeutic regimen which leads to local recovery of visual functions such as visual fields, visual acuity and retinal sensitivity, among others. 1. A method for treating a patient suffering from the loss or impairment of vision caused by a retinoid deficiency disorder , comprising the steps of:a) administering to the patient an initial therapeutically effective dose of a synthetic retinal derivative that provides replacement for endogenously produced 11-cis-retinal,b) refraining from administering to the patient an additional therapeutically effective dose of synthetic retinal derivative for a resting interval of at least 1 month,c) administering to the patient an additional therapeutically effective dose of a synthetic retinal derivative.233-. (canceled)34. A kit for use in the treatment or amelioration of a visual disorder associated with an endogenous retinoid deficiency in a subject , the kit comprising:(i) a therapeutic effective amount of a synthetic retinal derivative, or a therapeutic effective amount of a pharmaceutically acceptable composition comprising a synthetic retinal derivative; and(ii) instructions for administering the synthetic retinal derivative or the pharmaceutically acceptable composition to the subject35. A method of preparing a medicament for administration to a subject having an endogenous retinoid deficiency , the method comprising formulating a synthetic retinal derivative with a pharmaceutically acceptable vehicle. This application is a continuation of Ser. No. 14/875,342 filed Oct. 5, 2015, now U.S. Pat. No. 9,987,245, which is a continuation of Ser. No. 13/090,215 filed Apr. 19, 2011, now U.S. Pat. ...

AZA-PYRIDONE COMPOUNDS AND USES THEREOF

Disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection, with an aza-pyridone compounds. Examples of an orthomyxovirus viral infection include an influenza infection. 184-. (canceled) Any and all applications for which a foreign or domestic priority claim is identified, for example, in the Application Data Sheet or Request as filed with the present application, are hereby incorporated by reference under 37 CFR 1.57, and Rules 4.18 and 20.6.The present application is being filed along with a Sequence Listing in electronic format. The Sequence Listing is provided as a file entitled ALIOS078, created Apr. 28, 2016, which is 4 kb bytes in size. The information in the electronic format of the Sequence Listing is incorporated herein by reference in its entirety.The present application relates to the fields of chemistry, biochemistry and medicine. More particularly, disclosed herein are aza-pyridone compounds, pharmaceutical compositions that include one or more aza-pyridone compounds, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating an orthomyxovirus viral infection with one or more aza-pyridone compounds.The viruses of the Orthomyxoviridae family are negative-sense, single-stranded RNA viruses. The Orthomyxoviridae family contains several genera including Influenzavirus A, Influenzavirus B, Influenzavirus C, Isavirus and Thogotovirus. Influenzaviruses can cause respiratory viral infections, including upper and lower respiratory tract viral infections. Respiratory viral infections are a leading cause of death of millions of people each year. Upper respiratory tract viral infections involve the nose, sinuses, pharynx and/or larynx. Lower respiratory tract viral infections involve the ...

PLEUROMUTILIN DERIVATIVES FOR THE TREATMENT OF DISEASES MEDIATED BY MICROBES

A compound of formula (I) wherein n is 0 to 4; m is 0 or 1 with the proviso that the sulphur atom and Rare in vicinal position (if m=0 then Ris in position 2′, and if m=1 then Ris on position 1′); R is ethyl or vinyl; Ris hydrogen or (C1-6)alkyl; Ris hydrogen or —(C)cycloalkyl, or —unsubstituted (C)alkyl, or —(C)alkyl substituted by one or more of —hydroxy; preferably one or two, —methoxy, —halogen, —(C)cycloalkyl, or Rand Rtogether with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring containing at least 1 nitrogen atom or 1 nitrogen and 1 additional heteroatome e.g. selected from N or O, or Ris hydroxy and Ris formyl; Ris OH, OR, a halogen atom, or —with the proviso that Ris bound to 2′ Rrepresents —O—(CH)P—O— with p is 2 or 3; Ris unsubstituted (C)alkyl or (C)cycloalkyl. 8. The compound according to any of to in the form of a salt and/or solvate.9. A compound according to any of to for use as a pharmaceutical drug substance.10. A method of treatment of diseases mediated by microbes which comprises administering to a subject in need of such treatment an effective amount of a compound of any one of to .11. A pharmaceutical drug composition comprising a compound of anyone of to , in association with at least one pharmaceutical excipient.12. A pharmaceutical drug composition according to claim 11 , further comprising another pharmaceutically active agent. The present invention relates to organic compounds, namely pleuromutilins.Pleuromutilin, a compound of formula Ais a naturally occurring antibiotic, e.g. produced by the basidomycetes and , see e.g. The Merck Index, 13th edition, item 7617. A number of further pleuromutilins having the principle ring structure of pleuromutilin and being substituted at the hydroxy group have been developed, e.g. as antimicrobials.From WO 02/04414 A1 pleuromutilin derivatives, e.g. 14-O-[(Aminocyclohexan-2-yl (and -3-yl)-sulfanyl)-acetyl]-mutilins; from WO 07/014409 A1e.g. 14-O-[((Mono- or ...

FORMULATIONS AND USES OF RETINOIC ACID RECEPTOR SELECTIVE AGONISTS

The invention provides retinoic acid receptor (RAR) selective agonists and formulations thereof for the treatment of disease or for inducing a medically beneficial effect. 130.-. (canceled)32. The method of claim 31 , wherein the RAR selective agonist is administered by applying a cream claim 31 , by applying an ointment claim 31 , by applying a lotion claim 31 , by applying a liquid claim 31 , by foam claim 31 , orally or intravenously comprising the RAR selective agonist.33. The method of claim 31 , wherein the disease or disease condition is selected from the group consisting of a metabolic disease or condition associated with a metabolic disease and a carcinoma.34. The method of claim 33 , wherein the condition associated with the metabolic disease is selected from hyperglycemia claim 33 , hyperinsulinemia claim 33 , hyperlipidemia claim 33 , impaired glucose metabolism claim 33 , diabetic retinopathy claim 33 , macular degeneration claim 33 , cataracts claim 33 , diabetic nephropathy claim 33 , glomeruloscerosis claim 33 , diabetic neuropathy claim 33 , erectile dysfunction claim 33 , premenstrual syndrome claim 33 , vascular restenosis claim 33 , ulcerative colitis claim 33 , angina pectoris claim 33 , myocardial infarction claim 33 , stroke claim 33 , skin or connective tissue disorders claim 33 , scar tissue repair claim 33 , wrinkle treatment claim 33 , psoriasis claim 33 , UV-damage skin claim 33 , rosacea claim 33 , metabolic acidosis claim 33 , arthritis claim 33 , osteoporosis claim 33 , conditions of impaired glucose tolerance claim 33 , diabetic ulcer claim 33 , diabetes and cardiovascular disease.35. The method of claim 33 , wherein the carcinoma is selected from the group consisting of basal cell carcinoma claim 33 , squamous cell carcinoma and leukemia.36. The method of claim 31 , wherein Rand Rare H.37. The method of claim 31 , wherein R claim 31 , R claim 31 , Rand Rare alkyl.38. The method of claim 31 , wherein{'sub': 1', '2', '3', '4, 'R, R, R, ...

THERAPEUTIC REGIMENS AND METHODS FOR IMPROVING VISUAL FUNCTION IN VISUAL DISORDERS ASSOCIATED WITH AN ENDOGENOUS RETINOID DEFICIENCY

Therapeutic regimes for improving visual function in a subject having a deficiency in endogenously produced 11-cis retinal comprising administering the synthetic retinal derivative as a divided dose over 2-7 days then providing a resting period of 7-28 days after which the second dose of the synthetic retinal derivative is administered. Preferred synthetic retinal derivatives are 9- or 11-cis-retinyl esters. Disorders associated with deficiency in endogenously produced 11-cis retinal include retinitis pigmentosa and Leber congenital amaurosis. 1. A method of improving visual function in a subject having a deficiency in endogenously produced 11-cis retinal comprising:a. administering a first therapeutic dose of a synthetic retinal derivative to a subject in need thereof, wherein the first therapeutic dose is administered as a divided dose over a period of from about 2 to about 7 days;b. providing a resting period of from about 7 to about 28 days; andc. administering a second therapeutic dose of the synthetic retinal derivative to said subject following the end of the resting period.2. The method of claim 1 , wherein the subject has retinitis pigmentosa (RP).3. The method of claim 2 , wherein the subject has moderate to severe RP.4. The method of claim 2 , wherein the subject has mild RP.5. The method of claim 2 , wherein the subject has early onset or juvenile RP.6. The method of claim 1 , wherein the subject has Leber congenital amaurosis (LCA)7. The method of claim 1 , wherein the subject has a LRAT gene mutation.8. The method of claim 1 , wherein the subject has a RPE65 gene mutation.98. The method of any of - claims 1 , wherein the synthetic retinal derivative provides replacement of endogenously produced 11-cis-retinal.109. The method of any of - claims 1 , wherein the method further comprises repeating steps b and c one or more times.1110. The method of any of - claims 1 , wherein the first therapeutic dose is administered as a divided dose over a period of 7 ...

METHOD FOR PROMOTING INSULIN SECRETION BY USING COMPOUNDS AND EXTRACTS ISOLATED FROM ANTRODIA CAMPHORATA

The present invention discloses a method for promoting insulin secretion by using compounds and extracts isolated from in manufacturing medicaments for promoting insulin secretion, wherein the compounds is represented by formula (I): 6Antrodia camphorataAntrodia camphorataAntrodia camphorataAntrodia camphorata.. A method for promoting insulin secretion by using extracts from , comprising administering to a subject in need thereof an effective amount of extracts isolated from , wherein the extracts are extracted and then obtained by following steps: the mycelium , fruiting body or mixture of both taken from are extracted twice by ten-fold ethanol; and then the ethanol solutions were merged to concentrate to a crude product; and then the crude product is operated triple by partition extraction with dichloromethane/water (1:1) to form a dichloromethane layer and a water layer , wherein the dichloromethane layer and the water layer are the extracts from This application claims the priority of Taiwanese patent application No. 103127486, filed on Aug. 11, 2014 and Taiwanese patent application No. 103140521, filed on Nov. 21, 2014, which are incorporated herewith by reference.1. Field of the InventionThe present invention relates to a medical use of compounds and extracts isolated from , especially a method for promoting insulin secretion by using the compounds and extracts isolated from2. The Prior Artsis also called Chang-Zhi, Niu Chang-Gu, red camphor mushroom and the like, which is a perennial mushroom belonging to the order Aphyllophorales, the family Polyporaceae. is a unique Formosan fungal growing on the inner wall of the rotten cavity of wood of Hay. Hay is rarely distributed and overcut unlawfully, which makes parasitizing inside the tree in the wild become even rare. The price of is very expensive due to the extremely slow growth rate of the fruiting body that only grows between June to October.Triterpenoids are the most studied components among the numerous ...

USE OF MEDIUM CHAIN TRIGLYCERIDES FOR THE TREATMENT AND PREVENTION OF ALZHEIMER'S DISEASE AND OTHER DISEASES RESULTING FROM REDUCED NEURONAL METABOLISM II

Methods and compositions for treating or preventing, the occurrence of senile dementia of the Alzheimer's type, or other conditions arising from reduced neuronal metabolism and leading to lessened cognitive function are described. In a preferred embodiment the administration of triglycerides or fatty acids with chain lengths between 5 and 12, to said patient at a level to produce an improvement in cognitive ability. 1. A method of treating loss of cognitive function caused by Alzheimer's disease or Mild Cognitive Impairment , wherein said treatment comprises oral administration of a dosage unit of medium chain triglyceride to a patient such that the blood level of D-beta-hydroxybutyrate in the patient is raised to about 0.1 to 50 mM causing hyperketonemia in the patient , wherein the patient has a diet wherein carbohydrate intake is not restricted , resulting in ketone bodies being utilized for energy in the brain , wherein the dosage unit is given in a single dose.2. The method of claim 1 , wherein the blood level of D-beta-hydroxybutyrate is raised to about 0.2 to 20 mM.3. The method of claim 1 , wherein the blood level of D-beta-hydroxybutyrate is raised to about 0.3 to 5 mM.4. The method of claim 1 , wherein the blood level of D-beta-hydroxybutyrate is raised to about 0.5 to 2 mM.5. The method of claim 1 , wherein the blood level of D-beta-hydroxybutyrate is raised to about 1 to 10 mM.6. The method of claim 1 , wherein the loss of cognitive function is caused by Alzheimer's Disease.7. The method of claim 1 , wherein the patient's apolipoprotein E genotype is ApoE4(−).8. A method of treating loss of cognitive function caused by Alzheimer's disease or mild cognitive impairment claim 1 , wherein said treatment comprises oral administration of a dosage unit of medium chain triglyceride to a patient such that the blood level of D-beta-hydroxybutyrate in the patient is raised to about 0.2 to 20 mM causing hyperketonemia in the patient claim 1 , wherein the patient has ...

NOVEL CLASS OF COMPOUNDS FOR THE TREATMENT OF CARDIOVASCULAR DISEASE

The present invention relates to the field of medicine, specifically the field of treatment and prevention of cardiovascular diseases. 3. The compound according to , wherein the compound is derived from a compound selected from the group consisting of simvastatin , atorvastatin , cerivastatin , fluvastatin , lovastatin , mevastatin , pitavastatin , pravastatin , and rosuvastatin , wherein the carboxylic acid moiety has been replaced by a substituted or non-substituted moiety R as defined in .4. A pharmaceutical composition comprising a compound according to claim 1 , further comprising a pharmaceutically acceptable excipient.5. The pharmaceutical composition according to claim 4 , in the form of a tablet claim 4 , soft or hard capsule claim 4 , ampoule claim 4 , solution for injection claim 4 , emulsion for injection claim 4 , suspension for injection claim 4 , solution for inhalation claim 4 , emulsion for inhalation claim 4 , suspension for inhalation claim 4 , cream claim 4 , or ointment.614-. (canceled)15. The compound according to claim 1 , wherein Z″ and Z′″ are each individually O or S.16. The compound according to claim 2 , wherein Q is a bond.18. The compound according to claim 17 , wherein the compound has the general formula Ie.19. A method for the treatment claim 1 , prevention claim 1 , or delay of a cardiovascular disease claim 1 , hypercholesterolemia claim 1 , hypertriglyceridemia claim 1 , a metabolic disorder claim 1 , inflammation claim 1 , nephropathy claim 1 , and/or Alzheimer's disease in a subject claim 1 , said method comprising administering to the subject an effective amount of the compound of .20. The method of treatment according to claim 19 , wherein R is hydroxamic acid. The present invention relates to the field of medicine, specifically the field of treatment and prevention of cardiovascular diseases.Cardiovascular diseases are still one the most frequent causes of mortality. Multiple risk factors have been identified. Reduction of ...

DEVICE AND METHOD FOR ADMINISTERING AN ACTIVE INGREDIENT

This disclosure pertains to devices and methods for administering one or more active ingredients, e.g., cannabinoids, terpenes, etc. In particular, the devices and methods disclosed herein administer one or more cannabinoids in a mist for transmucosal and transdermal absorption. In one embodiment, the device contains compositions comprising purified active ingredients (e.g., cannabinoids, terpenes, etc.) and/or unique combinations thereof for delivery via a mist for transmucosal and transdermal adsorption. In one embodiment, the device contains two separate compositions in separate chambers, wherein each composition comprises one or more of the active ingredients. In one embodiment, a composition in one chamber comprises a purified cannabinoid and the composition in the other chamber comprises a purified terpene. In an embodiment, the device operates without heating the active ingredients. 2. (canceled)3. The device of claim 1 , wherein the cannabinoid is purified.4. The device of claim 3 , wherein the purified cannabinoid is THC claim 3 , Δ9-THC claim 3 , Δ8-THC claim 3 , THCA claim 3 , THCV claim 3 , Δ8-THCV claim 3 , Δ9-THCV claim 3 , THCVA claim 3 , CBD claim 3 , CBDA claim 3 , CBDV claim 3 , CBDVA claim 3 , CBC claim 3 , CBCA claim 3 , CBCV claim 3 , CBCVA claim 3 , CBG claim 3 , CBGA claim 3 , CBGV claim 3 , CBGVA claim 3 , CBN claim 3 , CBNA claim 3 , CBNV claim 3 , CBNVA claim 3 , CBND claim 3 , CBNDA claim 3 , CBNDV claim 3 , CBNDVA claim 3 , CBE claim 3 , CBEA claim 3 , CBEV claim 3 , CBEVA claim 3 , CBL claim 3 , CBLA claim 3 , CBLV claim 3 , or CBLVA.5. (canceled)6. (canceled)7. (canceled)8. The device of claim 1 , wherein the first composition comprises a first active ingredient and the second composition comprises a second active ingredient claim 1 , wherein at least one of the first active ingredient and the second active ingredient is the cannabinoid.9. The device of claim 8 , wherein the first active ingredient and the second active ingredient are ...

SELF-EMULSIFYING FORMULATIONS OF DIM-RELATED INDOLES

Disclosed herein are self-emulsifying compositions and formulations of Dimdolylmethane (“DIM”) and certain derivatives of DIM, their uses and methods of making. In particular, the disclosed compositions comprise a DIM-related indole as an active agent and a carrier, wherein the carrier comprises a solvent, one or more surfactants with an HLB of greater than 7, and one or more co-surfactants with an HLB equal to or less than 7. In certain aspects of the invention, the compositions disclosed herein show improved bioavailability. 3. The composition of which is formulated as an oral capsule.4. A method of promoting sleep claim 2 , reducing sleep latency claim 2 , improving sleep quality claim 2 , or reducing the number of night-time awakenings in a subject claim 2 , comprising administering to the subject the composition of .6. The composition of claim 5 , which is formulated as an oral capsule.7. A method of treating prostate cancer in a subject claim 5 , comprising administering to the subject the composition of .10. The composition of claim 9 , which is formulated as an oral capsule.11. A method of treating cancer in a subject claim 9 , comprising administering to the subject the composition of .14. The method of claim 13 , wherein the composition is formulated for oral or rectal administration.16. The composition of which is formulated as an oral capsule.17. A method of treating osteoporosis in a subject claim 15 , comprising administering to the subject the composition of .18. A method of treating cardiovascular disease and/or heart disease in a subject claim 15 , comprising administering to the subject the composition of . This application is a continuation of U.S. application Ser. No. 15/565,381, filed Jun. 19, 2018; which is a 371 of International Application No. PCT/US2016/026715, filed Apr. 8, 2016; which claims the benefit of U.S. provisional application No. 62/146,216, filed Apr. 10, 2015, each of which is incorporated by reference herein in its entirety.The ...

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) ...

Micronutrient formulation in electronic cigarettes

An antioxidant formulation for use with electronic cigarettes is provided and the formulation comprises: Vitamin A, Vitamin E, Trans-Resveratrol, polyphenol, and tertiary butyl hydroquinone 1. An antioxidant formulation for supporting health in human beings comprising: Vitamin A , Vitamin E , Trans-Resveratrol , polyphenol , and tertiary butyl hydroquinone (TBHQ).2. The formulation of is to be used in a liquid form for electronic cigarettes.3. The formulation of is composed of lipid soluble components.4. The formulation of is designed to be inhaled by human beings.5. The formulation of wherein Vitamin A is chosen from a group comprising retinyl palmitate claim 1 , fish oil claim 1 , natural mixed carotenoids claim 1 , and mixtures thereof.6. The formulation of claim 1 , wherein Vitamin E is chosen from a group comprising: alpha-tocopherol claim 1 , d-alpha tocopheryl succinate claim 1 , d-alpha tocopheryl acetate claim 1 , vegetable products claim 1 , natural tocopheryl claim 1 , or wheat germ products and mixtures thereof.7. The formulation of claim 1 , wherein polyphenols are chosen from a group comprising: green teas claim 1 , black teas claim 1 , berries claim 1 , flavonoids claim 1 , curcumin claim 1 , resveratrol claim 1 , and mixtures thereof.8. The formulation of claim 1 , wherein additional ingredients are chosen from a group comprising: Vitamin A claim 1 , Vitamin E claim 1 , Vitamin C claim 1 , Calcium claim 1 , Niacin claim 1 , Vitamin D claim 1 , Vitamin B claim 1 , Folic Acid claim 1 , Biotin claim 1 , Pantothenic Acid claim 1 , Co-enzyme Q10 claim 1 , N-acetyl cysteine claim 1 , and Alpha Lipoic Acid.9. The formulation of is to be supplemented with a secondary antioxidant formulation.10. The secondary antioxidant formulation of is selected from a group comprising: Vitamin A claim 10 , Vitamin E claim 10 , Natural mixed carotenoids claim 10 , Vitamin C claim 10 , Vitamin D claim 10 , B-vitamins claim 10 , Selenium claim 10 , Co-enzyme Q10 claim 10 , ...