ПЕРОРАЛЬНАЯ ДОЗИРОВАННАЯ ФОРМА, СОДЕРЖАЩАЯ НАРУЖНОЕ ПОКРЫТИЕ ДЛЯ БЫСТРОГО ВЫСВОБОЖДЕНИЯ

Группа изобретений относится к области фармацевтики и медицины. Изобретения представляют собой пероральную дозированную форму с покрытием, обеспечивающим чувственное ощущение в полости рта потребителя, содержащую: сердцевину, содержащую ацетаминофен, фенилэфрин и декстрометорфан или дифенгидрамин; наружное покрытие для быстрого высвобождения, содержащее гидроксипропилметилцеллюлозу, в частности, дополнительно полиэтиленгликоль, а также мальтодекстрин и согревающее ощущаемое вещество; и промежуточное покрытие, содержащее гидроксипропилметилцеллюлозу, в частности, дополнительно полиэтиленгликоль. Изобретения также представляют собой способ лечения симптомов простуды и/или гриппа, и/или аллергии, включающий введение человеку, нуждающемуся в этом, пероральной дозированной формы с покрытием. Технический результат заключается в обеспечении вкусовой добавки и, в частности, ощущаемого вещества, способных быстро высвобождаться из наружного покрытия, что обеспечивает пользу для потребителей, нуждающихся ...

РЕЖИМЫ ДОЗИРОВАНИЯ ТРАНС-КЛОМИФЕНА

Предложено применение композиции, по существу состоящей из транс-кломифена или его фармацевтически приемлемой соли, для применения при получении лекарственного средства, которое вводится пациенту мужчине один раз каждые 3-30 суток для лечения гипогонадизма, липодистрофии, доброкачественной гипертрофии простаты или рака простаты (варианты). Показано: продукт устойчиво повышает общий уровень тестостерона до нормального диапазона без аномально высоких пиков. При этом компенсируется один из побочных эффектов воздействия экзогенного тестостерона - снижение уровня биосинтеза ФСГ, вызывающего понижение формирования спермы. Наоборот, продукт применяют для лечения нарушения, связанного с мужским гипогонадизмом и связанными с ним нарушениями, включая уменьшение мышечной массы, ограничение физических возможностей организма, снижение плотности костей, снижение полового влечения, снижение потенции, редукцию доброкачественной гиперплазии простаты и бесплодие. 2 н. и 16 з.п. ф-лы, 7 ил., 1 табл.

АКТИВАЦИЯ ПРОКАСПАЗЫ-3 С ПОМОЩЬЮ КОМБИНИРОВАННОЙ ТЕРАПИИ

Группа изобретений относится к химико-фармацевтической промышленности и представляет собой композицию для терапии рака путем активации прокаспазы, содержащую соединение РАС-1:; второе активное средство, выбранное из: бортезомиб, ставроспорин, доксорубицин, тамоксифен, цисплатин, карбоплатин или паклитаксел; и фармацевтически приемлемый разбавитель, наполнитель и/или носитель, где концентрация РАС-1 составляет от 2 мкМ до 50 мкМ, а концентрация второго активного средства составляет от 1 нМ до 1 мМ. Также изобретения включают в себя способы индукции апоптоза в раковых клетках и подавления роста и/или пролиферации раковых клеток для лечения рака путем активации прокаспазы, включающие в себя воздействие на эти раковые клетки эффективным количеством композиции, описанной выше. Группа изобретений обеспечивает синергетический эффект активных агентов в композиции, что приводит к индуцированию апоптотической смерти раковых клеток, и проявляет более слабые нейротоксические эффекты, чем другие соединения ...

КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ НЕЙРОДЕГЕНЕРАТИВНЫХ ЗАБОЛЕВАНИЙ

Настоящее изобретение относится к новым соединениям общей Формулы (А), их стереоизомерам или фармацевтически приемлемым солям, обладающим способностью ингибировать активность изомеразы, участвующей в зрительном цикле. Соединения ингибируют дегенерацию ретинальной клетки, в частности нейрональной клетки, такой как фоторецепторная клетка, в сетчатке пациента. Соединения могут найти применение для лечения офтальмологического заболевания или нарушения, такого как возрастная макулярная дегенерация или макулярная дистрофия Штаргардта. В общей формуле (А)Z представляет собой -С(R)(R)-C(R)(R)-; Rи Rкаждый, независимо друг от друга, является выбранным из водорода, галогена, С-Салкила, или -OR; или Rи Rвместе образуют оксо; Rи Rкаждый, независимо друг от друга, является выбранным из водорода; Rвыбран из а) С-Салкила, необязательно замещенного гидрокси, C-Cалкокси; или б) С-Скарбоциклилалкила, в котором карбоцикл является 4-, 5-, 6-, 7- или 8-членным неароматическим карбоциклом, необязательно замещенным ...

АНТИТЕЛА К FcRH5, ИХ ИММУНОКОНЪЮГАТЫ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Данное изобретение относится к области иммунологии. Предложено выделенное моноклональное антитело к FcRH5 человека, охарактеризованное последовательностями гипервариабельных участков (HVR), и его антигенсвязывающий фрагмент. Кроме того, рассмотрен полинуклеотид, кодирующий антитело по изобретению, экспрессирующий вектор и клетка-хозяин для получения антитела по изобретению. Описаны иммуноконъюгаты, содержащие антитело по изобретению и предназначенные для ингибирования роста клеток, для определения присутствия FcRH5 человека в образце, для лечения пролиферативного расстройства, а также для ингибирования пролиферации клетки. Также предложена фармацевтическая композиция для ингибирования роста клеток, которые экспрессируют FcRH5 человека, содержащая эффективное количество иммуноконъюгата; применение иммуноконъюгата для получения лекарственных средств для ингибирования жизнеспособности клетки, которая экспрессирует FcRH5 человека, и для лечения пролиферативного расстройства, опосредованного ...

УСТРОЙСТВО ДЛЯ ТРАНСДЕРМАЛЬНОГО ВВЕДЕНИЯ БИСОПРОЛОЛА

Настоящее изобретение относится к медицине, конкретно к устройству для трансдермального введения бисопролола, которое включает в себя основу и слой чувствительного к давлению адгезива, содержащий бисопролол, который наслаивают на одну поверхность основы, где максимальное значение скорости высвобождения бисопролола в период времени непосредственно от нанесения на кожу до истечения 24 часов составляет 30 мкг/см2/час или меньше и где скорость высвобождения бисопролола через 24 часа после нанесения на кожу составляет 10 мкг/см2/час или меньше. Устройство для трансдермального введения снижает раздражение кожи, особенно при отслаивании, и может постоянно вводить в живой организм терапевтически или профилактически эффективное количество бисопролола. 4 з.п. ф-лы, 3 табл., 3 ил.

СПОСОБЫ ЛЕЧЕНИЯ ЛЕЙКОПЕНИИ И ТРОМБОЦИТОПЕНИИ

Изобретение относится к медицине и может быть использовано для приготовления медикамента для лечения индуцированной химиотерапией нейтропенией и/или тромбоцитопенией у человека, страдающего раком. При этом у человека общее количество нейтрофилов не снижается менее чем до 500/мкл или количество тромбоцитов не снижается менее чем до 25000/мкл. Для лечения вводят соединение моноацетилдиацилглицерина, описанное структурной формулой 2. Изобретение позволяет уменьшить индуцированную химиотерапией нейтропению и/или тромбоцитопению у человека, страдающего раком. 29 з.п. ф-лы, 9 ил., 10 табл., 10 пр.

СТАБИЛЬНАЯ КОМБИНИРОВАННАЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Изобретение относится к области медицины, а именно к упакованному фармацевтическому продукту, включающему стабильную твердую фармацевтическую композицию и влагонепроницаемую упаковку, где указанная композиция содержит гомогенную смесь основания амлодипина или амлодипина безилата и бисопролола фумарата и фармацевтически приемлемых эксципиентов, упакована в указанную влагонепроницаемую упаковку и дополнительно содержит меньше чем 0,5% от массы активных ингредиентов соединения формулы (3), и где указанная влагонепроницаемая упаковка представляет собой блистерную упаковку холодного формования из композитной фольги OPA/AL/PVC (фольга из ориентированного полиамида/алюминия/поливинилхлорида), покрытой алюминиевой мембранной фольгой. Изобретение обеспечивает получение упакованного фармацевтического продукта, где количество примеси не превышает 0,5% во время приготовления или во время хранения до окончания срока годности композиции, по меньшей мере в течение двух лет. 7 з.п. ф-лы, 2 табл., 2 пр.

ОРГАНИЧЕСКИЕ СОЕДИНЕНИЯ

Изобретение относится к области фармацевтики и касается твердой фармацевтической композиции, пригодной для орального введения, которая содержит: (а) агонист рецептора S1P и (б) сахарный спирт. Изобретение обеспечивает однородное распределение активного компонента в твердой композиции и ее высокую стабильность. 17 з.п. ф-лы, 2 табл.

ОПТИЧЕСКИ АКТИВНЫЕ ПРОИЗВОДНЫЕ БЕНЗОПИРАНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБ ЛЕЧЕНИЯ ЧУВСТВИТЕЛЬНЫХ К ЭСТРОГЕНАМ ЗАБОЛЕВАНИЙ

Изобретение относится к новым оптически активным производньм бензопирана формулы где R и R независимо выбраны из группы, состоящей из гидроксила и радикала, который может преобразовываться in vivo в гидроксил, такой как ацилокси, -OR4, -OC(O)R7 или -OC(O)OR4 (где R4 представляет собой алкил, алкенил, алкинил или арил; и R7 представляет собой амино, алкиламино, аминоалкил и алкилсульфанил); и R3 представляет собой -СН2- или -СН2СН2-; или его фармацевтически приемлемая соль, где указанное соединение или соль являются оптически активными, поскольку содержат более 50% (по массе относительно всех стереоизомеров) 2S стереоизомеров. Эти соединения обладают ингибирующей активностью в отношении полового стероида и могут использоваться при лечении чувствительных к эстрогенам заболеваний, таких как рак молочной железы и рак эндометрия. Изобретение относится также к фармацевтической композиции на основе этих соединений и способу лечения чувствительных к эстрогенам заболеваний. Технический результат ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ БЕТА-БЛОКАТОР И ИНГИБИТОР АНГИОТЕНЗИНПРЕВРАЩАЮЩЕГО ФЕРМЕНТА

Описана фармацевтическая форма для лечения или профилактики сердечно-сосудистых заболеваний. Фармацевтическая форма содержит бисопролол и/или его фармацевтически приемлемую соль и периндоприл и/или его фармацевтически приемлемую соль в комбинации с одним или несколькими фармацевтически приемлемыми наполнителями. В фармацевтической форме по изобретению бисопролол и периндоприл разделены физически. Дозы бисопролола составляют 1,05 и 8,50 мг в пересчете на основание бисопролола или между 1,25 и 10 мг в пересчете на фумарат бисопролола. Дозы периндоприла составляют 1,65 и 6,80 мг в пересчете на основание периндоприла или между 2,5 и 10 мг в пересчете на аргинин периндоприла. Фармацевтическая форма по изобретению представляет собой двухслойную таблетку или трехслойную таблетку или желатиновую капсулу, содержащую гранулы и/или таблетки бисопролола и гранулы и/или таблетки периндоприла. Фармацевтическая форма по изобретению в виде двухслойной таблетки является стабильной в течение 6 месяцев. 2 ...

АДГЕЗИВНЫЙ ПЛАСТЫРЬ, СОДЕРЖАЩИЙ БИСОПРОЛОЛ

Изобретение относится к медицине. Описан адгезивный пластырь, где каждый из элементов подложки, защитной пленки и адгезивного слоя имеет прямоугольную плоскую форму, и выступающая часть образована на поверхности со стороны подложки адгезивного пластыря по его углу. Кроме того, адгезивный пластырь может быть образован, чтобы иметь среднюю часть и периферийную часть, и выступающая часть может быть образована по углу прямоугольной средней части. Дополнительно, между смежными, по меньшей мере, двумя выступающими частями может быть предоставлена соединительная составная часть, в которой толщина адгезивного пластыря является меньшей, чем толщина адгезивного пластыря в выступающей части. Пластырь предотвращает просачивание наружу бисопролола или его соли из адгезивного слоя, предотвращая посредством этого снижение содержания лекарственного средства. 5 з.п. ф-лы, 6 ил., 4 табл., 8 пр.

ПРЕДНАЗНАЧЕННАЯ ДЛЯ ПЕРОРАЛЬНОГО ПРИМЕНЕНИЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Фармацевтическая композиция, пригодная для перорального введения, содержит агонист рецептора S1P и маннит, причем эта композиция представляет собой твердую дозированную форму. Маннит имеет удельную площадь поверхности одной частицы от 1 до 7 м/г, а агонист рецептора S1P выбирают из 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диола (FTY720), его фармацевтически приемлемой соли и РТУ720-фосфата. Композиции по изобретению характеризуются высоким уровнем однородности распределения указанного агониста рецептора S1P и хорошо приспособлены для орального введения в твердой форме, например в форме таблетки или капсулы. 13 з.п. ф-лы, 39 пр.

СПОСОБЫ И МАТЕРИАЛЫ ДЛЯ ЛЕЧЕНИЯ ТЕСТОСТЕРОНОВОЙ НЕДОСТАТОЧНОСТИ У МУЖЧИН

Изобретение относится к медицине, к способу использования композиций, содержащих транс-кломифен и цис-кломифен в соотношении по массе, большем или равном 71/29, для повышения уровня тестостерона в сыворотке крови у млекопитающего мужского пола. Использование практически чистого транс-кломифена по данному изобретению обеспечивает повышение уровня тестостерона как при снижении, так и при достаточном содержании этого гормона, в случае необходимости или желательности такого повышения для млекопитающего, при уменьшении побочных эффектов от лечения кломифеном. 3 н. и 1 з.п. ф-лы, 1 табл., 3 ил.

СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ НЕДЕРЖАНИЯ МОЧИ

Изобретение относится к области медицины. Недержание мочи у людей лечат посредством применения венлафаксина или соединения, выбранного из ряда арилоксипропиламинов. Предложенное средство не имеет нежелательных побочных результатов. 8 з.п.ф-лы, 5 ил.

СПОСОБ СЕНСИБИЛИЗАЦИИ РАКОВЫХ КЛЕТОК К ЛИЗИСУ, ОПОСРЕДОВАННОМУ КЛЕТКАМИ-КИЛЛЕРАМИ

Изобретение относится к медицине, а именно к способу сенсибилизации раковых клеток к лизису, опосредованному клетками-киллерами, и продукту. Способ включает в себя введение пациенту эффективного количества антиэстрогена и клеток-киллеров совместно или последовательно, причем клетки-киллеры выбирают из группы клеток ЕКК, ЛАКК и ЦТЛ, а антиэстроген выбирают из группы антиэстрогенов класса трифенилэтилена, таких как тамоксифен, или торемифен, или их фармацевтически приемлемые соли. Способ позволяет замедлить рост опухоли. 3 с. и 10 з.п. ф-лы, 3 табл., 10 ил.

Применение ксенона, иммобилизированного в носителе в средстве для повышения резистентности организма к гипоксии

Изобретение относится к неотложной медицине, и может быть использовано для для повышения резистентности организма к гипоксии. Для этого используют средство в форме газа ксенона, иммобилизированного в носителе, причем указанное средство дополнительно содержит смесь препаратов, состоящую из: бета-блокатора пропранолола 0,099 мас.%, симпатолитика резерпина 0,020 мас.%, антагониста H1 гистаминовых рецепторов дифенгидрамина 0,099 мас.%, антиангинального препарата с противоишемическим эффектом ивабрадина 0,099 мас.%, серотонинергического средства серотонина гидрохлорида 0,099 мас.%, нейролептического средства с гипотермическим эффектом перициазина 0,079 мас.%, антитиреоидного средства пропицила 0,099 мас.%, препарата, содержащего ионы магния-магния сульфата 0,593 мас.%, остальное - фармацевтически приемлемый растворитель. Носитель представляет собой 20% жировую эмульсию липофундина, при этом в 1 мл липофундина содержится от 0,54 до 2,2 мл ксенона. Применение средства позволяет продлить стабильное ...

Способ лечения острого послеродового эндометрита у коров

Изобретение относится к медицине, а именно к ветеринарии, и касается лечения острого послеродового эндометрита у коров. Для этого осуществляют комплексное лечение, включающее внутримышечное введение в 1, 2 и 3 дни иммунокорригирующих средств - α, γ-интерферонов и аминоселетона - с интервалом 24 часа в дозе 5,0 мл каждого в сочетании с миотропным препаратом утеротон внутримышечно в 1-4 дни в дозе 10 мл/животное с 24-часовым интервалом и этиотропным препаратом ниокситил внутриматочно в дозе 10-15 мл/100 кг массы тела с 48-часовым интервалом. Такое комплексное фармакологическое воздействие в указанном режиме обеспечивает эффективное лечение эндометрита и снижение продолжительности бесплодия за счет повышения общей неспецифической резистентности организма и уменьшения микробной контаминации матки. 2 пр., 3 табл.

ОРГАНИЧЕСКИЕ СОЕДИНЕНИЯ

... 1. Твердая фармацевтическая композиция, пригодная для орального введения, которая содержит (а) агонист рецептора S1P; и (б) сахарный спирт, в которой агонист рецептора S1P выбран из соединения формулы I в которой R1 обозначает прямую или разветвленную (С12-С22)-углеродную цепь, причем указанная цепь может нести связь или гетероатом, выбранные из двойной связи, тройной связи, О, S, NR6, где R6 обозначает Н, алкил, аралкил, ацил или алкоксикарбонил, и карбонила, и/или может иметь в качестве заместителя алкоксигруппу, алкенилоксигруппу, алкинилоксигруппу, аралкилоксигруппу, ацил, алкиламиногруппу, алкилтиогруппу, ациламиногруппу, алкоксикарбонил, алкоксикарбониламиногруппу, ацидоксигруппу, алкилкарбамоил, нитрогруппу, галоген, аминогруппу, гидроксииминогруппу, гидроксигруппу или карбоксигруппу; или R1 обозначает фенилалкил, в котором алкил обозначает прямую или разветвленную (С6-С20)-углеродную цепь; или фенилалкил, в котором алкил обозначает прямую или разветвленную (C1-С30)-углеродную цепь ...

ПИЩЕВОЕ ВОЛОКНО ДЛЯ ПРИМЕНЕНИЯ ПРИ ЛЕЧЕНИИ ПОБОЧНОГО ЭФФЕКТА ПИТАНИЯ ИЛИ ЛЕКАРСТВЕННОГО СРЕДСТВА В ОТНОШЕНИИ ЖЕЛУДОЧНО-КИШЕЧНОГО ТРАКТА

... 1. Применение пищевого волокна при замедлении или ином уменьшении насыщающего эффекта лечебного питания или лекарственного средства, где пищевое волокно является зерновым пищевым волокном, а лечебное питание или лекарственное средство предназначены для перорального или гастроэнтерального введения человеку.2. Применение по п. 1, где пищевое волокно содержит волокно из злаков, выбранное из немодифицированных и модифицированных рисовых волокон.3. Применение по п. 2, где волокно из злаков является рисовым волокном, обеспеченным в виде рисовых отрубей, предпочтительно рисовых отрубей в комбинации с рисовым зародышем.4. Применение по п. 1, где лекарственное средство является лекарством, оказывающим ингибирующее действие на обратный захват серотонина, ингибирующее действие на окисление моноаминов или опиатом.5. Применение по п. 1, где пищевое волокно состоит по меньшей мере на 15 мас.% из неацетогенных сахаридных единиц, предпочтительно по меньшей мере на 60 мас.% состоит из неацетогенных сахаридных ...

КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ РАКА

... 1. Соединение (5,6-дигидро-4H-пирроло[3,2,1-ij]хинолин-1-ил)пиррол-2,5-диона, выбранное из группы, состоящей ...

КОМПОЗИЦИИ И СПОСОБЫ ЛЕЧЕНИЯ ИЛИ ПРЕДУПРЕЖДЕНИЯ ВОСПАЛИТЕЛЬНЫХ ЗАБОЛЕВАНИЙ

... 1. Способ лечения или предупреждения рассеянного склероза, включающий введение пациенту терапевтически эффективного количества антимикротрубочкового агента таким образом, что рассеянный склероз лечится или предупреждается. 2. Способ по п.1, в котором вышеуказанный антимикротрубочковый агент выбран из группы, состоящей из эпотилона А или В, дискодермолида, оксида дейтерия (D2 O), гексиленгликоля, туберцидина, LY290181, фторида алюминия, бис(сукцинимидилсукцината)этиленгликоля, этилового эфира глицина, а также их аналогов или производных. 3. Способ по п.1, в котором вышеуказанный антимикротрубочковый агент является паклитакселом или его аналогом или производным. 4. Способ лечения или предупреждения псориаза, включающий введение пациенту терапевтически эффективного количества антимикротрубочкового агента таким образом, что псориаз лечится или предупреждается. 5. Способ по п.4, в котором вышеуказанный антимикротрубочковый агент выбран из группы, состоящей из эпотилона А или В, дискодермолида ...

СЕЛЕКТИВНЫЕ ОБРАТНЫЕ АГОНИСТЫ СЕРОТОНИНОВЫХ РЕЦЕПТОРОВ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ ПРИ ЗАБОЛЕВАНИИ

... 1. Фармацевтическая композиция, включающая: первое соединение, выбранное из группы, состоящей из обратного агониста серотонинового рецептора, антагониста серотонинового рецептора и их фармацевтически приемлемых солей; и второе соединение, выбранное из группы, состоящей из SSRI, SNRI, МАО-I, ТСА, антипсихотического средства, ингибитора обратного захвата норэпинефрина, допаминового агониста, лекарственного средства от бессонницы, антиманиакального лекарственного средства, антифобийного лекарственного средства, соединения, имеющего формулу (II) и их фармацевтически приемлемых солей. 2. Фармацевтическая композиция по п.1, где серотониновый рецептор является 5НТ2А-рецептором. 3. Фармацевтическая композиция по п.2, в котором первое соединение является соединением, имеющим формулу (I): 4. Фармацевтическая композиция по п.2, в котором первое соединение является соединением, имеющим формулу (II): а второе соединение выбрано из группы, состоящей из SSRI, SNRI, МАО-I, ТСА, антипсихотического средства ...

ПРИМЕНЕНИЕ РАНОЛАЗИНА В КОМБИНАЦИИ С ПО МЕНЬШЕЙ МЕРЕ ОДНИМ АГЕНТОМ СОВМЕСТНОГО РЕМОДЕЛИРОВАНИЯ ПРИ ЛЕЧЕНИИ СЕРДЕЧНОЙ НЕДОСТАТОЧНОСТИ

... 1. Способ реверсии вредного ремоделирования левого желудочка, включающий введение нуждающемуся в этом млекопитающему терапевтически эффективного количества ранолазина и терапевтически эффективного количества, по меньшей мере, одного агента совместного ремоделирования.2. Способ по п.1, в котором агент совместного ремоделирования включает ACE-ингибитор, ARB или бета-блокатор.3. Способ по п.2, в котором агент совместного ремоделирования включает ACE-ингибитор.4. Способ по п.3, в котором ACE-ингибитор выбран из группы, включающей беназеприл, каптоприл, силазаприл, эналаприл, фозиноприл, имидаприл, лизиноприл, периндоприл, гуинаприл, рамиприл, темокаприл и трандолаприл.5. Способ по п.2, в котором агент совместного ремоделирования включает ARB.6. Способ по п.5, в котором ARB выбран из группы, включающей кандесартан, силексетил, эпросартан, ирбесартан, лосартан, олмесартан, медоксомил, телмисартан, валсартан, золасартин и тасосартан.7. Способ по п.2, в котором агент совместного ремоделирования ...

ПРОИЗВОДНЫЕ АМИНА И ИХ ПРИМЕНЕНИЕ ДЛЯ ЛЕЧЕНИЯ ОФТАЛЬМОЛОГИЧЕСКИХ ЗАБОЛЕВАНИЙ И РАССТРОЙСТВ

... 1. Соединение Формулы (А) или его таутомер, стереоизомер, геометрический изомер или фармацевтически приемлемый сольват, гидрат, соль, N-оксид или их пролекарства: ! ! в которой Z представляет собой связь, -C(R1)(R2)-, -C(R9)(R10)-C(R1)(R2)-, -X-C(R31)(R32)-, -C(R9)(R10)-C(R1)(R2)-C(R36)(R37)- или X-C(R31)(R32)-C(R1)(R2)-; ! X представляет собой -O-, -S-, -S(=O)-, -S(=O)2-, -N(R30)-, -C(=O)-, -C(=CH2)-, -C(=N-NR35)- или -C(=N-OR35)-; ! G является выбранным из -C(R41)2-C(R41)2-R40, -C(R42)2-S-R40, -C(R42)2-SO-R40, -C(R42)2-SO2-R40, -C(R42)2-O-R40, -C(R42)2-N(R42)-R40, -C(=O)-N(R42)-R40; ! R40 является выбранным из -C(R16)(R17)(R18), арила или гетероарила; ! каждый R41 является независимо выбранным из водорода, гидрокси, OR6, алкила или две R41 группы вместе могут формировать оксо; ! каждый R42 является независимо выбранным из водорода или алкила; ! R1 и R2 каждый, независимо друг от друга, является выбранным из водорода, галогена, C1-C5 алкила, фторалкила, -OR6 или NR7R8; или R1 и R2 вместе ...

ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ НА ОСНОВЕ ГЕНОТИПА ИЛИ ФЕНОТИПА

... 1. Фармацевтическая композиция комбинированного препарата с фиксированными дозами, содержащая исходное вещество, действие которого зависит от количества или активности экспрессируемых вариантов белков, вариантов ферментов, вариантов рецепторов или вариантов транспортеров, и по меньшей мере его метаболит.2. Композиция по п. 1, доза которой определяется в зависимости от генотипа или фенотипа.3. Композиция по п. 1 и 2, отличающаяся тем, что включает тамоксифен и эндоксифен.4. Композиция по п. 3, отличающаяся тем, что включает 15-25 мг тамоксифена и 0,25-5,0 мг эндоксифена.5. Композиция по п. 4 для пациентов с CYP2D6 IM, включающая 15-25 мг тамоксифена и 0,25-2,00 мг эндоксифена.6. Композиция по п. 4 для пациентов с CYP2D6 РМ, включающая 15-25 мг тамоксифена и 1,0-5,0 мг эндоксифена.7. Способ получения фармацевтической композиции комбинированного препарата с фиксированными дозами по любому из пп. 1-4, включающий следующие этапы:а) ввод организма, его генотипа или фенотипа, исходного вещества ...

ОРАЛЬНЫЕ КОНТРАЦЕПТИВЫ ДЛЯ ПРЕДОТВРАЩЕНИЯ БЕРЕМЕННОСТИ И УМЕНЬШЕНИЯ ПРЕДМЕНСТРУАЛЬНОЙ СИМПТОМАТИКИ

... 1. Комплект, включающий: (a) от 60 до 110 лекарственных форм, содержащих эстроген и прогестин; и (b) от 2 до 10 лекарственных форм, содержащих эстроген; в которых от 60 до 110 лекарственных форм, содержащих эстроген и прогестин согласно (а), или от 2 до 10 лекарственных форм, содержащих эстроген согласно (b), или как в (а), так и в (b), находятся в сочетании с антидепрессантом. 2. Комплект, включающий: (a) от 21 до 26 лекарственных форм, содержащих эстроген и прогестин; и (b) от 2 до 10 лекарственных форм, содержащих эстроген; в которых от 21 до 26 лекарственных форм, содержащих эстроген и прогестин, в (а), или от 2 до 10 лекарственных форм, содержащих эстроген, в (b), или как в (а), так и в (b), находятся в сочетании с антидепрессантом. 3. Комплект по п.1 или 2, в котором лекарственные формы являются таблетками. 4. Комплект по п.1, включающий: (a) от 81 до 89 таблеток, содержащих эстроген и прогестин; и (b) от 2 до 7 таблеток, содержащих эстроген. 5. Комплект по п.2, включающий: (a) от ...

АГОНИЗМ 5HT2А-РЕЦЕПТОРА ДЛЯ ЛЕЧЕНИЯ НАРУШЕНИЯ ФУНКЦИИ ТЕРМОРЕГУЛЯЦИИ

... 1. Продукт, содержащий ингибитор повторного поглощения серотонина (SRI) и антагонист 5НТ1а-рецептора в виде комбинированного препарата для одновременного, раздельного либо последовательного применения при лечении и/или профилактике вазомоторной нестабильности. 2. Продукт по п.1, отличающийся тем, что упомянутый ингибитор повторного поглощения серотонина выбран из группы, которую составляют флуоксетин, пароксетин, сертралин, флувоксамин, дулоксетин, амоксапин, доксепин, бупропион, циталопром и амитриптилин. 3. Продукт по п.1 или 2, отличающийся тем, что упомянутый антагонист 5НТ1а-рецептора выбран из группы, которую составляют N-[2-[4-(2-метоксифенил)-1-пиперазинил]этил]-N-2-пиридинилциклогексанкарбоксамид, (R)-N-(2-метил-(4-индолил-1-пиперазинил)этил)-N-(2-пиридинил)циклогексанкарбоксамид и NAD-299. 4. Применение агониста 5НТ2а-рецептора при изготовлении лекарственного средства для лечения и/или профилактики вазомоторной нестабильности. 5. Применение по п.4, отличающееся тем, что упомянутый ...

ТАБЛЕТКИ МЕТОПРОЛОЛА СУКЦИНАТА ПРОЛОНГИРОВАННОГО ДЕЙСТВИЯ И СПОСОБЫ ИХ ПРИГОТОВЛЕНИЯ

... 1. Фармацевтическая композиция пролонгированного действия, содержащая пеллеты, каждая из которых покрыта слоем активного фармацевтического ингредиента и включает ! а) инертное ядро, содержащее по меньшей мере приблизительно 50% (вес./вес.) растворимого вещества, ! б) слой лекарственного вещества, содержащий активный фармацевтический ингредиент, нанесенный на инертное ядро, и ! в) на нем - слой контролируемого высвобождения. ! 2. Фармацевтическая композиция по п.1, в которой активный фармацевтический ингредиент представляет собой метопролол или его фармацевтически приемлемую соль. ! 3. Фармацевтическая композиция по п.2, в которой фармацевтически приемлемой солью метопролола является метопролол сукцинат. ! 4. Фармацевтическая композиция по п.1, в которой инертное ядро содержит от приблизительно 70 вес.% до приблизительно 90 вес.% растворимых веществ. ! 5. Фармацевтическая композиция по п.1, в которой вес инертного ядра составляет от приблизительно 20% до приблизительно 35% от веса каждой ...

Средство, его применение и способ повышения устойчивости организма млекопитающих к переохлаждению

Группа изобретений относится к созданию лекарственного средства для повышения устойчивости млекопитающих к переохлаждению. Средство содержит фармацевтическую композицию препаратов, содержащую 0,78-1,18 мас.% пропранолола, 0,015-0,024 мас.% резерпина, 0,078-0,12 мас.% ивабрадина, 0,098-0,18 мас.% дифенгидрамина, 0,025-0,035 мас.% перициазина, 0,25-0,35 мас.% серотонина гидрохлорид, 0,07-0,12 мас.% пропицила, 0,07-0,16 мас.% сульфата магния, 98-98,61 мас.% фармацевтически приемлемого растворителя. Также предлагается способ повышения устойчивости организма млекопитающих к переохлаждению, заключающийся в введении терапевтически эффективного количества средства. Техническим результатом является повышение резистентности клеток жизненно важных органов и тканей к переохлаждению. 3 н.п. ф-лы, 2 ил., 2 пр.

РЕЖИМЫ ДОЗИРОВАНИЯ ТРАНС-КЛОМИФЕНА

... 1. Композиция, включающая от 0 до примерно 29 мас.% цис-кломифена и примерно от 100 до примерно 71 мас.% транс-кломифена или его аналогов для использования при получении лекарственного средства для введения пациенту в качестве однократной дозы для достижения фармакологически эффективной концентрации тестостерона в крови пациента на перед 3-30 суток. ! 2. Применение по п.1, в котором композиция состоит преимущественно из транс-кломифена или его аналога. ! 3. Применение по п.1, в котором однократная доза составляет примерно от 5 до примерно 100 мг. ! 4. Применение по п.3, в котором однократная доза составляет примерно он 12,5 до примерно 50 мг. ! 5. Применение по п.4, в котором однократная доза составляет 12,5, 25 или 50 мг. ! 6. Применение по п.1, в котором время составляет примерно от 7 до примерно 15 суток. ! 7. Применение по п.6, в котором период времени составляет примерно от 10 до примерно 12 суток. ! 8. Применение по п.1, в котором лекарственное средство предназначено для повышения ...

СПОСОБ КРИСТАЛЛИЗАЦИИ ГИДРОХЛОРИДА 2-АМИНО-2-[2-[4-(3-БЕНЗИЛОКСИФЕНИЛТИО)-2-ХЛОРФЕНИЛ]ЭТИЛ]-1,3-ПРОПАНДИОЛА

... 1. Способ кристаллизации гидрохлорида 2-амино-2-[2-[4-(3-бензилоксифенилтио)-2-хлорфенил]этил]-1,3-пропандиола, включающий стадии: ! (1) растворения 2-амино-2-[2-[4-(3-бензилоксифенилтио)-2-хлорфенил]этил]-1,3-пропандиола в смешанном растворителе, содержащем растворитель, в котором соединение в форме его гидрохлорида имеет высокую растворимость, и растворитель, в котором гидрохлорид меньше растворим, для того, чтобы таким образом получить раствор 2-амино-2-[2-[4-(3-бензилоксифенилтио)-2-хлорфенил]этил]-1,3-пропандиола; и затем ! (2) добавления хлористоводородной кислоты к указанному выше раствору при перемешивании для того, чтобы таким образом кристаллизовать гидрохлорид 2-амино-2-[2-[4-(3-бензилоксифенилтио)-2-хлорфенил]этил]-1,3-пропандиола. ! 2. Способ по п.1, дополнительно включающий стадию (3), стадию охлаждения указанного раствора, полученного на стадии (2), при перемешивании. ! 3. Способ по п.1 или 2, где растворитель, в котором гидрохлорид соединения высоко растворим, выбран из ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ДЛЯ ЛЕЧЕНИЯ ПРЕЖДЕВРЕМЕННОЙ ЭЯКУЛЯЦИИ

... 1. Фармацевтическая композиция для лечения преждевременной эякуляции, содержащая в качестве активных ингредиентов кломипрамин или его фармацевтически приемлемую соль, сертралин или его фармацевтически приемлемую соль и флуоксетин или его фармацевтически приемлемую соль. ! 2. Композиция по п.1, в которой соотношение по массе кломипрамина или его фармацевтически приемлемой соли, сертралина или его фармацевтически приемлемой соли и флуоксетина или его фармацевтически приемлемой соли составляет 1:1-2:0,5-1. ! 3. Композиция по п.1, в которой фармацевтически приемлемая соль является гидрохлоридом. ! 4. Композиция по п.1, которая дополнительно содержит фармацевтически приемлемый носитель. ! 5. Композиция по п.4, в которой фармацевтически приемлемый носитель выбран из группы, состоящей из наполнителей, разрыхлителей, связывающих веществ, смазывающих веществ, эмульгаторов, суспендирующих средств, стабилизаторов, подсластителей, ароматизаторов и их комбинации. ! 6. Композиция по п.1, которая дополнительно ...

ИСПОЛЬЗОВАНИЕ СОЕДИНЕНИЙ РЯДА 3-АРОЛОКСИПРОПИЛАМИНОВ В ЛЕЧЕНИИ НЕДЕРЖАНИЯ

Недержание мочи у людей лечат посредством применения венлафаксина или соединения, выбранного из ряда арилоксипропиламинов.

ИСПОЛЬЗОВАНИЕ МОДУЛЯТОРА РЕЦЕПТОРА S1P

... 1. Способ предотвращения, подавления или лечения депрессии, обусловленной продуцированием нейротрофического фактора головного мозга (НФГМ), у пациента, нуждающегося в этом, состоящий из введения указанному пациенту терапевтически эффективного количества модулятора рецептора S1P, выбранного из группы, состоящей из 2-амино-2-[4-(3-бензилоксифенилтио)-2-хлорфенил]-2-этил-пропан-1,3-диола, 1-{4-[1-(4-циклогексил-3-трифторметил-бензилоксиимино)-этил]-2-этил-бензил}-азетидин-3-карбоксильной кислоты и 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диол или в каждом случае их фармацевтически приемлемых солей и/или их фосфорилированных форм. ! 2. Способ по п.1, в котором модулятор рецептора S1P представляет собой 2-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диол или его фармацевтически приемлемую соль. ! 3. Способ по п.1, в котором модулятор рецептора S1P представляет собой 1-амино-2-[2-(4-октилфенил)этил]пропан-1,3-диол гидрохлорид. ! 4. Способ по п.1, в котором модулятор рецептора S1P представляет собой ...

СПОСОБ ПОЛУЧЕНИЯ ФАРМАЦЕВТИЧЕСКОЙ КОМПОЗИЦИИ

... 1. Способ получения фармацевтической композиции, заключающийся в том, что: ! (а) смешивают агонист рецептора S1P с сахарным спиртом; ! (б) размалывают и/или гранулируют смесь, полученную на стадии (а); и ! (в) смешивают размолотую и/или гранулированную смесь, полученную на стадии (б), с замасливателем. ! 2. Способ по п.1, в котором агонист рецептора S1P тонко измельчают и/или предварительно просеивают до стадии (а). ! 3. Способ по п.1 или 2, где стадия смешения (а) включает перемешение агониста рецептора S1P и сахарного спирта в любом пригодном смесителе или миксере в течение, например 100-400 оборотов. ! 4. Способ по п.1 или 2, в котором компоненты смешивают путем сухого смешения. ! 5. Способ по п.4, где стадия смешения (б) предусматривает пропуск полученной на стадии (а) смеси через сито. ! 6. Способ по п.1 или 2, при котором на стадии (а) осуществляют стадию смешения всего количества агониста рецептора S1P сначала с небольшим количеством сахарного спирта для приготовления премикса. !

КОМБИНАЦИИ, СОДЕРЖАЩИЕ АНТИМУСКАРИНОВЫЕ СРЕДСТВА И БЕТА-АДРЕНЕРГИЧЕСКИЕ АГОНИСТЫ

... 1. Комбинация, содержащая (а) β2-агонист и (b) антагонист мускариновых рецепторов М3, который представляет собой 3(R)-(2-гидрокси-2,2-дитиен-2-илацетокси)-1-(3-феноксипропил)-1-азонийбицикло[2.2.2]октан в форме соли с анионом X, который представляет собой фармацевтически приемлемый анион моно- или поливалентной кислоты. ! 2. Комбинация по п.1, где антагонист мускариновых рецепторов М3 (b) представляет собой бромид 3(R)-(2-гидрокси-2,2-дитиен-2-илацетокси)-1-(3-феноксипропил)-1-азонийбицикло[2.2.2]октана. ! 3. Комбинация по п.1 или 2, где β2-агонист выбран из группы, состоящей из арформотерола, бамбутерола, битолтерола, броксатерола, карбутерола, кленбутерола, допексамина, фенотерола, формотерола, гексопреналина, ибутерола, изопреналина, мабутерола, мелуадрина, ноломирола, орципреналина, пирбутерола, прокатерола, репротерола, ритодрина, римотерола, сальбутамола, салметерола, сибенадета, сульфонтерола, тербуталина, тулобутерола, GSK-597901, GSK-159797, KUL-1248, ТА-2005 и QAB-1491 необязательно ...

Новая терапия транстиретин-ассоциированного амилоидоза

СПОСОБЫ ЛЕЧЕНИЯ РАКА ЯИЧНИКА

ЛЕЧЕНИЕ ОСЛОЖНЕНИЙ ХРОНИЧЕСКОГО ЗАБОЛЕВАНИЯ ПЕЧЕНИ

СПОСОБ ЛЕЧЕНИЯ ПЕРВИЧНОГО ГОРМОНОРЕЗИСТЕНТНОГО ЭНДОМЕТРИАЛЬНОГО РАКА И РАКА ГРУДИ

ЛЕЧЕНИЕ РАКА/ИНГИБИРОВАНИЕ МЕТАСТАЗИРОВАНИЯ

... 1. Композиция для применения в(а) способе уменьшения метастатического поведения или(б) способе предотвращения метастатического поведения у пациента, страдающего от ракового заболевания, связанного с экспрессией потенциалзависимых натриевых каналов (VGSC), причем указанную композицию применяют в дозировке, которая по меньшей мере уменьшает незатухающую часть тока VGSC без устранения переходной части.2. Композиция для применения в способе уменьшения или предотвращения метастатического поведения по п.1, обладающая указанным эффектом без уничтожения клеток.3. Композиция для применения в способе уменьшения или предотвращения метастатического поведения по п.1, обладающая указанным эффектом без существенного влияния на пролиферацию.4. Композиция для применения в способе уменьшения или предотвращения метастатического поведения по п.1, отличающаяся тем, что метастатическое поведение представляет собой по меньшей мере одно из следующих:(i) адгезивность, причем композиция увеличивает адгезивность ...

ВЫБОР АНТИАРИТМИЧЕСКОЙ ТЕРАПИИ У ПАЦИЕНТОВ С ФИБРИЛЛЯЦИЕЙ ПРЕДСЕРДИЙ

СПОСОБЫ И МАТЕРИАЛЫ С ТРАНС-КЛОМИФЕНОМ ДЛЯ ЛЕЧЕНИЯ МУЖСКОГО БЕСПЛОДИЯ

... 1. Композиция, включающая эффективное количество транс-кломифена или его фармацевтически приемлемой соли или сольвата и необязательно один или несколько фармацевтически приемлемых разбавителей, адъювантов, носителей или эксципиентов и используемая для получения лекарственного средства для лечения мужского бесплодия, отличающаяся тем, что: (а) отношение транс-кломифена к цис-кломифену превышает 71/29, или (б) композиция включает от 0% до примерно 29 мас.% цис-кломифена и примерно от 100% до примерно 71% транс-кломифена. 2. Применение по п.1, в котором композиция состоит в значительной степени из эффективного количества транс-кломифена или его фармацевтически приемлемой соли или сольвата. 3. Применение по п.1, в котором лекарственное средство предназначено для введения в дозе 1-200 мг транс-кломифена в сутки. 4. Применение по п.3, в котором лекарственное средство предназначено для введения в дозе примерно 50 мг транс-кломифена в сутки. 5. Применение по п.3, в котором лекарственное средство ...

ФАРМАЦЕВТИЧЕСКИЕ СОЕДИНЕНИЯ

... 1. Соединение формулы (1):или соль, N-оксид, таутомер или стереоизомер указанного соединения, где:А представляет собой СН или азот;Е представляет собой СН или азот;Rвыбран из следующего:- ациклическая Cуглеводородная группа, возможно содержащая один или два заместителя R, причем один атом углерода в ациклической Cуглеводородной группе может быть необязательно заменен гетероатомом или группой, выбранными из О, S, NR, S(O) и SO, или два соседних атома углерода в ациклической d.углеводородной группе могут быть необязательно заменены группой, выбранной из CONR, NRCO, NRSOи SONR, при условии, что в каждом случае в ациклической Cуглеводородной группе сохраняется по меньшей мере один атом углерода; и- моноциклическая карбоциклическая или гетероциклическая группа, содержащая от 3 до 7 членов кольца, из которых 0, 1, 2, 3 или 4 членов кольца являются гетероатомами, выбранными из О, N и S, причем указанная карбоциклическая или гетероциклическая группа возможно содержит один или два заместителя R; ...

КОМБИНАЦИИ СОЕДИНЕНИЙ, ИНГИБИРУЮЩИХ АКТ, И ХИМИОТЕРАПЕВТИЧЕСКИХ АГЕНТОВ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

... 1. Комбинация а) соединения формулы I:или его фармацевтически приемлемой соли; и b) одного или нескольких средств, выбранных из 5-FU, платинового агента, лейковорина, иринотекана, доцетаксела, доксорубицина, гемцитабина, SN-38, капецитабина, темозоломида, паклитаксела, бевацизумаба, пертузумаба, тамоксифена, рапамицина и лапатиниба, или его фармацевтически приемлемой соли для профилактики или терапевтического лечения гиперпролиферативного нарушения.2. Комбинация по п.1, где гиперпролиферативным нарушением является злокачественное новообразование.3. Комбинация по п.2, где злокачественное новообразование связано с мутацией PTEN.4. Комбинация по п.2, где злокачественное новообразование связано с мутацией AKT, сверхэкспрессией или амплификацией.5. Комбинация по п.2, где злокачественное новообразование связано с мутацией PI3K.6. Комбинация по п.2, где злокачественное новообразование связано с мутацией или амплификацией Her2/ErbB2.7. Комбинация по п.1, где комбинация обеспечивает синергетический ...

КОМБИНАЦИИ СОЕДИНЕНИЙ-ИНГИБИТОРОВ АКТ И АБИРАТЕРОНА И СПОСОБЫ ПРИМЕНЕНИЯ

... 1. Комбинация a) соединения формулы Ia:или его фармацевтически приемлемой соли и b) абиратерона или его фармацевтически приемлемой соли для профилактического или терапевтического лечения гиперпролиферативного нарушения.2. Комбинация по п.1, где гиперпролиферативным нарушением является рак.3. Комбинация по п.2, где рак ассоциирован с мутацией PTEN.4. Комбинация по п.2, где рак ассоциирован с мутацией, оверэкспрессией или амплификацией AKT.5. Комбинация по п.2, где рак ассоциирован с мутацией PI3K.6. Комбинация по п.2, где рак ассоциирован с мутацией Her2/ErbB2.7. Комбинация по любому из пп.2-6, где рак выбран из рака молочной железы, легкого, яичников, предстательной железы, меланомы, рака желудка, толстой кишки, почки, головы и шеи, и глиомы.8. Комбинация по любому из пп.1-6, где комбинация обеспечивает синергический эффект при лечении гиперпролиферативного нарушения.9. Комбинация по п.8, где значение комбинаторного индекса синергического эффекта составляет менее чем приблизительно 0,8.10 ...

СЕЛЕКТИВНОСТЬ В ОТНОШЕНИИ МУТАНТНЫХ ФОРМ И КОМБИНАЦИИ СОЕДИНЕНИЯ, ПРЕДСТАВЛЯЮЩЕГО СОБОЙ ИНГИБИТОР ФОСФОИНОЗИТИД-3-КИНАЗЫ, И ХИМИОТЕРАПЕВТИЧЕСКИХ АГЕНТОВ ДЛЯ ЛЕЧЕНИЯ РАКА

... 1. Способ лечения рака, выбранного из рака молочной железы, шейки матки, толстой кишки, эндометрия, желудка, глиомы, рака легкого, меланомы, рака яичников, поджелудочной и предстательной железы, включающий введение млекопитающему терапевтической комбинации в виде объединенной композиции или путем чередования, где терапевтическая комбинация содержит терапевтически эффективное количество GDC-0032, имеющего структуру:,и терапевтически эффективное количество химиотерапевтического агента, выбранного из 5-фторурацила (5-FU), доцетаксела, эрибулина, гемцитабина, GDC-0973, GDC-0623, паклитаксела, фулвестранта, пертузумаба, трастузумаба эмтанзина и трастузумаба.2. Способ по п. 1, где химиотерапевтический агент представляет собой 5-FU.3. Способ по п. 1, где химиотерапевтический агент представляет собой доцетаксел.4. Способ по п. 1, где химиотерапевтический агент представляет собой эрибулин.5. Способ по п. 1, где химиотерапевтический агент представляет собой гемцитабин.6. Способ по п. 1, где химиотерапевтический ...

КОМПОЗИЦИИ И СПОСОБЫ СЕЛЕКТИВНОЙ ДЕГРАДАЦИИ БЕЛКА

Настоящее изобретение относится к области биотехнологии и может быть применимо в медицине. Изобретение раскрывает слитый полипептид, содержащий связывающий цереблон (CRBN) фрагмент и фрагмент специфичного к опухолевому антигену химерного антигенного рецептора (CAR). Изобретение может быть использовано в медицине при лечении злокачественных опухолей в качестве модулирующего экспрессию терапевтических белков агента. Изобретение позволяет регулировать экспрессию белков путем стимулирования их протеасомной и/или убиквитинзависимой деградации. Изобретение также раскрывает способ устранения побочных эффектов, возникающих при терапии рака с использованием CAR. 13 н. и 31 з.п. ф-лы, 18 пр., 34 табл., 40 ил.

VERWENDUNG VON NOREPINEPHRINWIEDERAUFNAHMEHEMMERN ZUR BEHANDLUNG VON TICKS

VERWENDUNG VON TOREMIFENE FÜR DIE BEHANDLUNG VON SLE

VERWENDUNG VON NIEDERMOLEKULAREN AMINOALKOHOLEN IN OPHTHALMOLOGISCHEN PRÄPARATEN

LÖSLICHE ZUSAMMENSETZUNGEN VON TOREMIFENE

Retardmikrotablette von beta-Phenylpropiophenonderivaten

PHENOXYHYDROXYPROPYLAMINES AND THEIR PREPARATION

... 1308106 Substituted phenoxy-hydroxy propylamines HASSLE AB 19 April 1971 [18 Feb 1970] 21994/71 Heading C2C Novel compounds of the Formula IV wherein R1 is isopropyl or t-butyl, A is a straight or branched C 1-4 alkylene chain and Z is -OR2, -SO 2 R2, -SOR2, -SR2, NR 3 -COR2, NR 3 SO 2 R2 or NR3COOR2 wherein R2 is straight or branched C 1-3 alkyl and R3 is hydrogen or a straight or branched alkyl radioal and pharmaceutically acceptable acid addition salts thereof may be prepared by (i) reacting a compound V wherein X is an unsubstituted ethylene oxide ring or -CHOHCH 2 -halogen with a compound R1NHCONHR1 or R1NH 2 ; (ii) reductively alkylating IV wherein R1 is H with acetone to produce IV, R1 = iPr; (iii) alkylating IV R1 = H with Hal-CH(CH 3 ) 2 where Hal is a halogen atom; (iv) hydrolysing a compound wherein R4 is a hydrolytioally ...

Means and methods to treat torsin related neurologicl diseases

Estrogen receptor

Improved use of ß2-bronchodilator drugs

Compositions

There is described a composition comprising an effective amount of a combination of two or more components selected from a NAD precursor; a NAMPT upregulator; a NQO1 upregulator and a NNMT (nicotinamide N-methyltransferase) downregulator.

Metered dose inhaler with vortex device

The present invention relates to metered dose inhalers for the administration of active medicaments/propellants and excipients. The invention provides a pMDI inhaler comprising a pMDI canister 22, a vortex device, an integral horn and a breath-activated mechanism 26, 28, 34 wherein the canister contains a formulation comprising a combination of two or more active ingredients. Proposed active ingredients include beta agonists, inhaled corticosteroids and anticholinergics. The integral horn may have a shape which widens towards the mouthpiece, thus reducing the aerosol flow velocity.

Pharmaceutical combination

Alkoxy compounds for disease treatment

Starch-based release modifying excipients and pharmaceutical compositions derived therefrom

An extended release dosage form (ERDF) comprising a release modifying excipient comprising a high amylose starch, a cross-linked hydroxypropylated amylopectin and a pre-gelatinized common starch; wherein the release modifying excipient is substantially free of crosslinks between amylose and amylopectin and substantially free of crosslinks between amylose and amylose. In an embodiment, the dosage form is formulated into an extended release tablet using tramadol as the active ingredient. In a preferred embodiment the ERDF is used in a bi-layer tablet containing both immediate and extended release layers where both layers contain the active acetaminophen. The extended release properties of conventional cross-linked high amylose starches can be reproduced by intimately mixing i) cross-linked chemically modified amylopectin; ii) a high amylose, non-chemically modified starch and; iii) a pre-gelatinized common starch. Producing a release modifying excipient in this way means that no chemical ...

Treatment of heart failure

Novel system

Gynecomastia treatment

A selective estrogen receptor modulator and/or an aromatase inhibitor (A) for use in the treatment or prevention of gynecomastia, wherein said selective estrogen receptor modulator and/or aromatase inhibitor is/are administered combination with (B) an estrogen modulator, wherein said estrogen modulator is different to said selective estrogen receptor modulator.

The process for manufacturing formulation of topical beta blockers with improved efficiency

Pharmaceutical compositions comprising a proton pump inhibitor and a prokinetic agent

Antibodies to insulin-like growth factor i receptor

Aerosol formulations containing salmeterol, salbutamol or fluticasone.

This invention relates to aerosol formulations of use for the ...

Antibodies to insulin-like growth factor i receptor

MEDICAMENTS

The process for manufacturing formulation of topical beta blockers with improved efficacy.

Beta blockers are used as topical ophthalmic preparation for reducing intra ocular pressure. B-blocker used for this purpose include timolol, levobunolol, carteolol, metipranalol. They reduce the aqueous produ tion and thereby reduce i.O.p. They are commonly used as drops. Efficacy of topical b-blockers is dependent on concentration of drug in formulation. However, increasing the concentration of drug beyond approved dosage forms does not increase the efficacy significantly e.G. timolol 0.5 has indentical pressure lowering capacity as 1 timolol. The attempts to improve pressure reduction efficiency of b-blockers has not met with success so far. The sustained lease formulation of timolol (timolol xf)has resulted in amount of drug to achieve same therapeutic effect. However, none of the formulation has improved efficacy of drug for reducing i.O.p. The present invention relates to the process of manufacturing such formulation of b-blocker which improves its i.O.p. Lowering effect. The formulation ...

New pharmaceuticals combinations for nos inhibitors.

The present invention relates to new pharmaceutical uses for compounds that exhibit activity as nitric oxide synthase (nos)inhibitors. Specifically, it relates to the use of nos inhibitors, particularly selective neuronal nos (nnos)inhibitors, alone or in combination with another active agent, in particular, either an ssri or an nk-1 receptor antagonist, for the treatment of disorders or conditions the treatment which can be effected or facilitated by altering circadian rhythms. Examples of such disorders and conditions are blindness, obesity, seasonal affective disorder, bipolar disorder, jet lag, circadian sleep rhythms disorder, sleep deprivation, parasomnias, rem sleep disorders, hypersomnia, sleep-wake cycle disorders, narcolepsy and sleep disorders associated with shift work or irregular work schedules; nocturnal enuresis, and restless-legs syndrome.

Pharmaceutical compositions comprising a proton pump inhibitor and a prokinetic agent

Stable preservative-free mydriatic and anti-inflammatory solutions for injection

FORMULATION COMPRISING GLYCOPYRROLATE, METHOD AND APPARATUS

Antibodies to insulin-like growth factor i receptor

Rapid dissolve tablet compositions for vaginal administration

New pharmaceutical combinations for nos inhibitors

Antibodies to insulin-like growth factor I receptor

The present invention relates to antibodies and antigen-binding portions thereof that specifically bind to insulin-like growth factor I receptor (IGF-IR), which is preferably human IGF-IR. The invention also relates to human anti-IGF-IR antibodies, including chimeric, bispecific, derivatized, single chain antibodies or portions of fusion protein. The invention also relates to isolated heavy and light chain immunoglobulin molecules derived from anti-IGF-IR antibodies and nucleic acid molecules encoding such molecules. The present invention also relates to methods of making anti-IGF-IR antibodies, pharmaceutical compositions comprising these antibodies and methods of using the antibodies and compositions thereof for diagnosis and treatment. The invention also provides gene therapy methods using nucleic acid molecules encoding the heavy and/or light immunoglobulin molecules that comprise the human anti-IGF-IR antibodies. The invention also relates to gene therapy methods and transgenic animals ...

New pharmacetical combinations for nos inhibitors

Antibodies to insulin-like growth factor i receptor.

Medicaments

Stable preservative-free mydriatic and anti-inflammatory solutions for injection

MEDICAMENTS

Rapid dissolve tablet compositions for vaginal administration

FORMULATION COMPRISING GLYCOPYRROLATE, METHOD AND APPARATUS

Stable preservative-free mydriatic and anti-inflammatory solutions for injection

Pharmaceutical compositions comprising a proton pump inhibitor and a prokinetic agent

IDENTIFICATION OF MATERIAL FROM THE MILK CHANNEL OF THE CHEST

4-HYDROXYTAMOXIFEN FOR TREATMENT AND PROPHYLAXIS OF BENIGNEN BREAST ILLNESSES

PREVENTION AND TREATMENT OF OSTEOPOROSIS INDUCED BY LACK OF ANDROGEN

VERFAHREN ZUR HERSTELLUNG NEUER BASISCHER ATHER

Genetic markers and diagnostic methods for resistance of breast cancer to hormonal therapies

This application provides a method to identify genetic markers associated with increased sensitivity or resistance to hormonal therapies using an outlier analysis. More specifically, this application discloses that amplifications on chromosomes 8 and 17 are associated with increased proliferation and poor outcome in ER-positive breast cancer, and amplicons 17q21.33-q25.1, 8p11.2 and 8q24.3 may be responsible for higher proliferation and poor outcome in the setting of antiestrogen, in particular Tamoxifen, treatment clinically observed in a subset of ER-positive, HER2-negative breast cancers. The invention also provides use of the identified genetic markers in the development of targeted treatments for antiestrogen-resistant ER-positive breast cancers as well as in improving current methods of drug response prediction.

Treatment of cutaneous hemangioma

This invention concerns a method of treating hemangiomas with a beta blocker by applying the beta blocker onto the hemangiomas directly. The invention also concerns a combination therapy by using a beta blocker along with a corticosteroid or an alpha adrenergic receptor agonist for the treatment of hemangiomas.

Transdermal Preparation

Provided is a transdermal preparation, which is capable of long-term (1-day to 7-day) release of a basic drug from a preparation, continuously and at a consistent concentration; shows little reduction over time in the drug content, even if multiple drugs are contained in the preparation; and is produced by a simple process. The transdermal preparation comprises a substrate, and an adhesive layer containing a basic drug and a water-soluble polymer.

Combinations comprising antimuscarinic agents and pde4 inhibitors

A combination which comprises (a) a PDE4 inhibitor and (b) an antagonist of M3 muscarinic receptors which is (3R)-1-phenethyl-3-(9H-xanthene-9carbonyloxy)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid.

Anti-estrogen and immune modulator combinations for treating breast cancer

Compositions for treating cancers of mucosal tissues including breast, prostate, ovary, colon are disclosed which include various combinations of new or conventional anti-estrogen compounds, aromatase inhibitors, immune modulators, immune inhibitors, immune inhibitor mimicking compounds and steroid or thyroid hormones. Methods of predicting susceptibility of a cancer of mucosal origin to treatment with a composition containing an immune inhibitor or an immune inhibitor mimicking compound are also disclosed. Preferred methods include identifying in a specimen of cancer cells the presence of a Poly-Ig (Fe) receptor or Poly-Ig-like (Fc) receptor capable of binding to an immune inhibitor or an immune inhibitor mimicking compound and of mediating immune inhibition of cancer cell growth.

Combination of a sedative and a neurotransmitter modulator, and methods for treating depression

One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., insomnia and/or depression. The first component of the pharmaceutical composition is a GABA receptor modulating compound. The second component of the pharmaceutical composition is a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a 5-HT 2A modulator, or dopamine reuptake inhibitor. In certain embodiments, the pharmaceutical composition comprises eszopiclone. In a preferred embodiment, the pharmaceutical composition comprises eszopiclone and fluoxetine. The present invention also relates to a method of treating a sleep abnormality, treating insomnia, treating depression, augmenting antidepressant therapy, eliciting a dose-sparing effect, reducing depression relapse, improving the efficacy of antidepressant therapy or improving the tolerability of antidepressant therapy, comprising co-administering to a patient in need thereof a GABA-receptor-modulating compound; and a SRI, NRI, 5-HT 2A modulator or DRI.

Nuclear receptor binding agents

The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

Therapeutic Inhibitor of Vascular Smooth Muscle Cells

Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associates in a specific manner with a cell surface of the vascular smooth muscle cell, coupled to a therapeutic agent dosage form that inhibits a cellular activity of the muscle cell. Methods are also provided for the direct and/or targeted delivery of therapeutic agents to vascular smooth muscle cells that cause a dilation and fixation of the vascular lumen by inhibiting smooth muscle cell contraction, thereby constituting a biological stent.

Methods of treating hyperacidic disorders

The present invention relates to methods for treating or preventing hyperacidic disorders such as GERD or NERD using calcium receptor active compounds.

Dosage regimen of an s1p receptor modulator

S1P receptor modulators are administered following a dosage regimen providing a positive benefit-risk profile.

Methods and compositions for the treatment of proliferative vascular disorders

The technology described herein is directed to methods and compositions for the treatment of proliferative vascular disorders, e.g. hemangioma. In some aspects, the methods and compositions described herein related to a mTOR inhibitor or nifedipine.

Oral drug delivery system

An oral drug delivery system comprising a coated tablet having one or more surfaces. The coated tablet further comprises a core and a coating surrounding the core. The core comprises an active ingredient composition comprising at least one active ingredient and a pharmaceutically acceptable excipient and a reactive composition located in an immediate vicinity of one or more preselected surfaces. The coating is operable to be reliably removed fully from the one or more of the preselected surfaces of the tablet upon contact with an aqueous environment, but not removed from at least one of the surfaces.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF ASTHMA AND ASSOCIATED DISORDERS

This disclosure provides methods for treating asthma or an associated disorder in a patient in need thereof, by administering to the patient an effective amount of an autophagy inducing agent, thereby treating the asthma or the associated disorder. Disorders that can be treated include, allergic asthma, chronic obstructive pulmonary disease, lung inflammation, respiratory tolerance and a lung infection or disorder. 1. A method for treating asthma or an associated disorder in a patient in need thereof , comprising administering to the patient an effective amount of an autophagy inducing agent , thereby treating the asthma or the associated disorder.2. The method of claim 1 , wherein the asthma is allergic asthma.3. The method of claim 1 , wherein the related disorder is one or more of chronic obstructive pulmonary disease claim 1 , lung inflammation claim 1 , respiratory tolerance and a lung infection or disorder.4. The method of claim 1 , wherein autophagy inducing agent is one or more of carbomezepine claim 1 , tamoxifen claim 1 , minoxidil claim 1 , erapumil claim 1 , clonidine claim 1 , and an autophagy inducing FLIP peptide.5. The method of claim 4 , wherein the autophagy inducing FLIP peptide is of the group of peptides identified by SEQ ID NO.: 1-8 or 14-28 claim 4 , a variant or an equivalent thereof6. The method of claim 5 , wherein the equivalent is a peptide having at least 70% sequence identity to the reference FLIP peptide and having the ability to induce autophagy.7. The method of claim 5 , wherein the equivalent is a peptide coded by a polynucleotide that hybridizes to the coding or non-coding strand of a polypeptide that encodes peptides identified by SEQ ID NO.: 1-8 or 14-28 under conditions of moderate or high stringency.8. The method of claim 7 , wherein the conditions of high stringency are at about 60° C. in about 1×SSC and moderate stringency are performed at about 50° C. in about 6×SSC.9. The method of claim 1 , wherein the autophagy inducing ...

USE OF A BETA BLOCKER FOR THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF HEMANGIOMAS

The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroids, interferon or vincristine, generally used for the treatment of hemangiomas. 119-. (canceled)20. A method for treating an infant or small child having an infantile hemangioma , the method comprising administering to the infant or small child a medicament comprising a pharmaceutically acceptable and efficient dose a beta blocker.21. The method of claim 20 , wherein the beta blocker is selected from the group consisting of non-selective beta blockers claim 20 , beta-1-selective beta blockers claim 20 , mixtures of alpha-1/beta-adrenergic antagonists claim 20 , beta-2-selective beta blockers claim 20 , and mixtures of two or more beta-blockers.22. The method of claim 20 , wherein the beta blocker is a non-selective beta blocker.23. The method of claim 20 , wherein the beta blocker is a beta-1 selective beta blocker.24. The method of claim 20 , wherein the beta blocker has an intrinsic sympathomimetic activity.25. The method of claim 20 , wherein the medicament is for oral or topical administration.26. A method for treating a hemangioma comprising administering to a patient in need thereof a pharmaceutically acceptable and efficient dose of a beta blocker.27. The method of claim 26 , wherein the beta blocker is selected from the group consisting of non-selective beta blockers claim 26 , beta-1-selective beta blockers claim 26 , mixtures of alpha-1/beta-adrenergic antagonists claim 26 , beta-2-selective beta blockers claim 26 , and mixtures of two or more beta-blockers.28. The method of claim 26 , wherein the beta blocker is a non-selective beta blocker.29. The method of claim 28 , wherein the non-selective beta blocker is selected from the ...

Baclofen and acamprosate based therapy of neurological disorders

The present invention relates to combinations and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid β toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorder, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury, based on Baclofen and Acamprosate combination.

ANTI-FcRH5 ANTIBODIES AND IMMUNOCONJUGATES AND METHODS OF USE

The present invention is directed to compositions of matter useful for the treatment of hematopoietic tumor in mammals and to methods of using those compositions of matter for the same.

TIME-DELAYED SUSTAINED RELEASE PHARMACEUTICAL COMPOSITION COMPRISING DAPOXETINE FOR ORAL ADMINISTRATION

The present invention relates to a time-delayed sustained release pharmaceutical composition for oral administration, which comprises an immediate release phase and a prolonged sustained release phase, wherein said immediate release phase and prolonged sustained release phase respectively comprise Dapoxetine therein as an active ingredient. The pharmaceutical composition of the present invention comprises Dapoxetine, which is an agent for treating premature ejaculation, in both the immediate release phase and the prolonged sustained release phase thereof, to thereby immediately exhibit the effectiveness of the pharmaceutical composition of the present invention in order to enable a patient to achieve sexual satisfaction during the early stage of administration, as well as to reduce side effects by means of the time-delayed sustained release of the prolonged sustained release phase during the early stage of administration and enable a continuous in vivo absorption of Dapoxetines, to thereby lengthen the duration of the effectiveness of the pharmaceutical composition of the present invention. Further, agents for treating erectile dysfunction, such as sildenafil, tadalifil or the like can be added to the immediate release phase so as to allow for a coincidence of the durations of the effectiveness of a premature ejaculation treatment agent and erectile dysfunction treatment agents, even though a half-life difference exists between the two types of treatment agents, thus maximizing patient satisfaction. 1. A time-delayed sustained release pharmaceutical composition for oral administration , which is comprised of an immediate release phase and a prolonged sustained release phase ,wherein said immediate release phase and prolonged sustained release phase respectively contain Dapoxetine therein as an active ingredient;characterized in that Dapoxetine contained in said immediate release phase is eluted 80 wt % or more from an eluate in 30 minutes, and Dapoxetine contained ...

METHOD FOR ENHANCING LEARNING AND MEMORY IMPAIRED BY NEURODEGENERATIVE DISORDERS AND COMPOUNDS AND COMPOSITIONS FOR EFFECTING THE SAME

A method for enhancing learning or memory of both in a mammal having impaired learning or emory of both from a neuro-degenerative disorder, which entails the step of administering at least one compound or a salt thereof which is a β-adrenergic receptor agonist, partial agonist or receptor ligand in an amount effective to improve the learning or memory or both of said mammal. 1) A method for enhancing learning or memory or both in a mammal having impaired learning or memory or both from a neuro-degenerative disorder , which comprises the step of administering at least one compound or a salt thereof which is a β-adrenergic receptor agonist , partial agonist or receptor ligand in an amount effective to improve said learning or memory or both of said mammal.2) The method of claim 1 , wherein said at least one compound is xamoterol or a pharmaceutically-acceptable salt thereof.3) The method of claim 1 , wherein said at least one compound is noradrenalin or a pharmaceutically-acceptable salt thereof.4) The method of claim 1 , wherein said at least one compound is isoprenaline or a pharmaceutically-acceptable salt thereof.5) The method of claim 1 , wherein said at least one compound is dobutamine or a pharmaceutically-acceptable salt thereof.6) The method of claim 1 , wherein said at least one compound is dopamine or a pharmaceutically-acceptable salt thereof.7) The method of claim 1 , wherein the mammal is a human.8. The method of claim 1 , wherein the impaired learning or memory is caused by Alzheimer's disease.9. The method of claim 1 , wherein the impaired learning or memory is caused by Down Syndrome.10. A method of comprehensively phenotyping Ts65Dn mice to identify behavioral abnormalities in learning claim 1 , memory and social behavior claim 1 , which comprises subjecting Ts65Dn mice to tests in order to correlate behavioral phenotypic traits with trisomy 16.11. The method of claim 10 , which identifies hippocampus-mediated learning and memory to be a severely- ...

Control of Cardiac Growth, Differentiation and Hypertrophy

Methods and compositions are provided for the diagnosis and treatment of heart diseases relating to cardiac hypertrophy, and for the regulation of proliferation and differentiation of cardiomyocyte progenitors in vitro. The detection of expression of components of the BAF complex, including, without limitation, detection of expression of Brg1, provides useful methods for early detection, diagnosis, staging, and monitoring of conditions leading to hypertrophy and enlargement of the heart. Manipulation of Brg1 activity provides for therapeutic intervention in the development of cardiac hypertrophy, where methods of decreasing Brg1 activity, e.g. through inhibition of binding, decreasing expression, and the like, reduces cardiac hypertrophy. 1. A method to suppress cardiac hypertrophy or prevent onset of cardiac hypertrophy in a patient , the method comprising:administering to said patient an effective amount of an agent that suppresses functional activity or expression of Brg1 or other BAF subunit proteins in cardiomyocytes and/or cardiac endothelial cells.2. The method according to claim 1 , wherein said agent inhibits the expression of Brg1 or other BAF subunit proteins in cardiomyocytes and/or cardiac endothelial cells.3. The method according to claim 2 , wherein said agent is a nucleic acid having a sequence complementary to Brg1 or other BAF subunits genetic sequence4. The method according to claim 3 , wherein said substance is an antisense molecule or RNAi effector.5. The method according to claim 1 , wherein said agent is a small molecule inhibitor.6. A method for the diagnosis of cardiac hypertrophy in the heart claim 1 , the method comprising:determining the differential expression Brg1 or other BAF subunits in cardiomyocytes and/or cardiac endothelial cells.7. The method according to claim 6 , wherein said determining comprises:contacting a biological sample comprising protein from a patient suspected of suffering from cardiac hypertrophy with an antibody ...

ALLOSTERIC BINDING COMPOUNDS

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

Glycoproteins Having Lipid Mobilizing Properties an Therapeutic Uses Thereof

The invention provides formulations and methods for ameliorating symptoms associated with metabolic disorders, such as cachexia, hypoglycemia, obesity, diabetes, and the like by administering Zn-α-glycoproteins or a functional fragment thereof, alone or in combination with additional agents, such as β adrenergin receptor agonists, β adrenergin receptor antagonists, and/or glycemic control agents. 1145-. (canceled)146. A formulation comprising a zinc-α-glycoprotein (ZAG) , a ZAG variant , a modified ZAG , or a functional fragment thereof.147. The formulation of claim 146 , wherein the ZAG is mammalian.148. The formulation of claim 147 , wherein the ZAG is human.149. The formulation of claim 148 , wherein the ZAG consists of the amino acid sequence set forth in SEQ ID NO: 1.150. The formulation of claim 149 , wherein the ZAG is conjugated to a non-protein polymer.151. The formulation of claim 150 , wherein the ZAG is sialylated claim 150 , PEGylated or modified to increase solubility or stability.152. The formulation of claim 146 , wherein the ZAG is recombinant or synthetic.153. The formulation of claim 146 , wherein the modified ZAG consists of the wild-type ZAG amino acid sequence with one or more mutations to the amino acid sequence selected from deletions claim 146 , additions or conservative substitutions.154. The formulation of claim 146 , wherein the ZAG further comprises one or more of a leader sequence and a trailing sequence.155. The formulation of claim 150 , wherein the ZAG is glycosylated.156. The formulation of claim 155 , wherein the ZAG is glycosylated as a result of a posttranslational modification.157. The formulation of claim 146 , wherein the functional fragment is generated by proteolysis chemical degradation claim 146 , or folding-domain-preserving fragmentation.158. The formulation of claim 146 , wherein the formulation comprises at least 5 claim 146 , 10 claim 146 , 25 claim 146 , 50 claim 146 , 100 mg of ZAG.159. The formulation of claim 146 ...

Respirably dry powder comprising calcium lactate, sodium chloride and leucine

The present invention relates to respirable dry powders that contain respirable dry particles that comprise about 20% (w/w) leucine, about 75% (w/w) calcium lactate, and about 5% (w/w) sodium chloride, or about 37.5% (w/w) leucine, about 58.6% (w/w) calcium lactate, and about 3.9% (w/w) sodium chloride, and methods for treating a subject using the respirable dry powders.

Compositions and Methods for Treatment of Cancer

The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent. 115-. (canceled)1716. The pharmaceutical composition of , wherein said second chemotherapeutic agent is selected from the group consisting of tamoxifen , raloxifene , anastrozole , exemestane , letrozole , trastuzumab , imatinib , paclitaxel , cyclophosphamide , lovastatin , mimosine , gemcitabine , araC , 5-fluorouracil , methotrexate , docetaxel , goserelin , vinctristine , vinblastine , nocodazole , teniposide , etoposide , gemcitabine , epothilone , navelbine , camptothecin , daunorubicin , dactinomycin , mitoxantrone , amsacrine , doxorubicin , epirubicin or idarubicin.1826-. (canceled)28. The method of claim 27 , wherein said second chemotherapeutic agent is selected from the group consisting of tamoxifen claim 27 , raloxifene claim 27 , anastrozole claim 27 , exemestane claim 27 , letrozole claim 27 , trastuzumab claim 27 , imatinib claim 27 , paclitaxel claim 27 , cyclophosphamide claim 27 , lovastatin claim 27 , mimosine claim 27 , gemcitabine claim 27 , araC claim 27 , 5-fluorouracil claim 27 , methotrexate claim 27 , docetaxel claim 27 , goserelin claim 27 , vinctristine claim 27 , vinblastine claim 27 , nocodazole claim 27 , teniposide claim 27 , etoposide claim 27 , gemcitabine claim 27 , epothilone claim 27 , navelbine claim 27 , camptothecin claim 27 , daunorubicin claim 27 , dactinomycin claim 27 , mitoxantrone claim 27 , amsacrine claim 27 , doxorubicin claim 27 , epirubicin or idarubicin.29. The method of wherein said treating said cell proliferative ...

ALCOHOL-RESISTANT EXTENDED RELEASE DOSAGE FORMS COMPRISING VENLAFAXINE

This disclosure relates to an extended release oral dosage form comprising a matrix containing a viscosity modifier (but no lipid) and coated granules containing venlafaxine or a pharmaceutically acceptable salt or solvate thereof. The dosage form has alcohol resistance and may also have crush resistance. 1. An extended release oral dosage form comprising:a matrix, wherein the matrix comprises a viscosity modifier in an amount from about 1 to about 60 percent by weight of the dosage form; andcoated granules comprising venlafaxine or a pharmaceutically acceptable salt or solvate thereof;wherein the matrix does not contain a lipid.2. An extended release oral dosage form comprising:a matrix, wherein the matrix comprises a viscosity modifier in an amount from about 1 to about 60 percent by weight of the dosage form; andcoated granules comprising venlafaxine or a pharmaceutically acceptable salt or solvate thereof;wherein the matrix does not contain a lipid;in which the percent of venlafaxine released after 2 hours in a solution of 0.1N hydrochloric acid and 40% alcohol is no more than 10 percentage points greater than the percent of said venlafaxine released in a solution of 0.1N hydrochloric acid in the absence of alcohol.3. An extended release oral dosage form comprising:a matrix, wherein the matrix comprises a viscosity modifier in an amount from about 1 to about 60 percent by weight of the dosage form; andcoated granules comprising venlafaxine or a pharmaceutically acceptable salt or solvate thereof;wherein the matrix does not contain a lipid;in which the release of venlafaxine from the dosage form 6 hours after testing is less than about 80 percent when tested in 500 ml of 0.1N hydrochloric acid solution using USP dissolution apparatus.4. The dosage form of or or , wherein the viscosity modifier is selected from the group consisting of: sodium alginate , hydroxypropylmethylcellulose , hydroxyethylcellulose , hydroxypropylcellulose , methylcellulose , ...

Methods of nourishing animals

The present invention relates to methods of maintaining, and methods of restoring, a desired calcium homeostasis in a non-human terrestrial animal by administering an effective amount of one or more Calcium-Sensing Receptor modulators (CaSRs) to the animal. The invention further provides methods of reducing foot lesions in chickens. The invention also relates to food compositions useful in the methods of the invention.

USE OF ADRENERGIC BETA-3-RECEPTOR AGONISTS IN ANTI-AGING

A method for treating an aging-related disease is disclosed comprising administering to a subject a pharmaceutical composition comprising an adrenergic beta-3-receptor agonist. 1. A method for treating an aging-related disease , comprising administering to a subject in need of the treatment a pharmaceutical composition comprising an adrenergic beta-3-receptor agonist.23. The method of claim 1 , wherein the adrenergic beta--receptor agonist is selected from the group consisting of CL316243 claim 1 , N-5984 claim 1 , BMS-194449 claim 1 , BMS-196085 claim 1 , CP114271 claim 1 , CP80625 claim 1 , BRL 37344 claim 1 , SR58611A claim 1 , TAK2677 claim 1 , and N25984.3. The method of claim 1 , wherein the adrenergic beta-3-receptor agonist is selected from the group consisting of BRL 37344 claim 1 , SR58611A claim 1 , TAK2677 claim 1 , and N25984.4. The method of claim 1 , wherein the aging-related disease is selected from a group consisting of Alzheimer's disease claim 1 , myocardial fibrosis claim 1 , renal failure claim 1 , therioma claim 1 , and lipofuscin.5. The method of claim 4 , wherein the aging-related disease is lipofuscin.6. The method of claim 4 , wherein the aging-related disease is myocardial fibrosis. The present invention claims priority from Chinese application number 201210020843.9 filed on Jan. 30, 2012, the disclosure of which is incorporated herein by reference.The present invention relates to a new usage of adrenergic beta-3-receptor (ADRB 3) agonists, and in particular to its usage in anti-aging or preparation of anti-aging medicaments.Adrenergic beta-3-receptor, also known as beta-3 adrenergic receptor or beta-3 adrenoreceptor, a beta-adrenergic receptor, is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. ADRB 3 activating drugs could theoretically be used as weight-loss agents, but are limited by the side effect of tremors. Some ADRB 3 agonists have demonstrated antistress effects in animal studies ...

USE OF ADRENERGIC BETA-E-RECEPTOR BLOCKERS IN CANCER TREATMENT

A method for treating an cancer disease is disclosed comprising administering to a subject a pharmaceutical composition comprising an adrenergic beta-3-receptor blocker. 1. A method for treating a cancer disease , comprising administering to a subject in need of the treatment a pharmaceutical composition comprising an adrenergic beta-3-receptor blocker.2. The method of claim 1 , wherein the adrenergic beta-3-receptor agonist is SR59230A or its derivatives.3. The method of claim 1 , wherein the cancer disease is selected from a group consisting of breast carcinomas claim 1 , leukemia claim 1 , pulmonary carcinomas claim 1 , hepatocarcinomas claim 1 , colon cancers claim 1 , pancreatic cancers claim 1 , prostate cancers.4. The method of claim 3 , wherein the cancer disease is breast carcinomas.5. The method of claim 3 , wherein the cancer disease is leukemia. The present invention claims priority from Chinese application number 201210020844.3 filed on Jan. 30, 2012, the disclosure of which is incorporated herein by reference.The present invention relates to a new usage of adrenergic beta-3-receptor (ADRB 3) blockers, and in particular to its usage in treatment of cancers or other diseases.Adrenergic beta-3-receptor, also known as beta-3 adrenergic receptor or beta-3 adrenoreceptor, a beta-adrenergic receptor, is located mainly in adipose tissue and is involved in the regulation of lipolysis and thermogenesis. ADRB 3 activating drugs could theoretically be used as weight-loss agents, but are limited by the side effect of tremors. Some ADRB 3 agonists have demonstrated antistress effects in animal studies, suggesting they also have a role in the CNS. Beta-3 receptors are found in gallbladder, urinary bladder, and in brown adipose tissue. Their role in gallbladder physiology is unknown, but they are thought to play a role in lipolysis and thermogenesis in brown fat. Our search did not reveal any reports about potential effect of beta-3 receptors in genesis and ...

Flibanserin for the Treatment of Urinary Incontinence and Related Diseases

The invention relates to the use of Flibanserin for the treatment or prevention of urinary incontinence and related diseases. In a further embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment or prevention of urinary incontinence and related diseases. 1. A method for treating or preventing urinary incontinence comprising administering a therapeutically effective amount of Flibanserin 1 , or a pharmacologically acceptable acid addition salt , hydrate , or solvate thereof.2. The method for treating or preventing urinary incontinence according to claim 1 , further comprising administering and an active ingredient 2 claim 1 , or a pharmaceutically acceptable salts claim 1 , hydrate claim 1 , or solvate thereof claim 1 ,3. The method for treating or preventing urinary incontinence according to claim 1 , wherein the urinary incontinence is overactive bladder syndrome4. The method for treating or preventing urinary incontinence according to claim 2 , wherein the urinary incontinence is overactive bladder syndrome.5. The method for treating or preventing urinary incontinence according to claim 1 , wherein the urinary incontinence is urgency.6. The method for treating or preventing urinary incontinence according to claim 1 , wherein the urinary incontinence is urge urinary incontinence.7. The method for treating or preventing urinary incontinence according to claim 1 , wherein the urinary incontinence is stress urinary incontinence.8. The method for treating or preventing urinary incontinence according to claim 1 , wherein the urinary incontinence is mixed urinary incontinence.9. The method for treating or preventing urinary incontinence according to claim 2 , wherein the active ingredient 2 is an antimuscarinic agent 2a claim 2 , vasopressin agonist 2b claim 2 , Serotonin/Noradrenaline modulator 2c claim 2 , or B3 agonist ...

Compositions of small molecule therapeutics

Compositions containing a small molecule therapeutic and an alkyl N,N-disubstituted amino acetate are disclosed. Inclusion of the alkyl N,N-disubstituted amino acetate enhances the pharmacokinetic properties of the small molecule therapeutic.

TREATMENT OF L-DOPA, DOPAMINE AGONIST AND/OR DOPAMINE ENHANCER INDUCED DISORDERS

One or more agent selected from A/B-cis furostane, furostene, spirostane and spirostene steroidal sapogenins and ester, ether, ketone or glycosylated forms thereof, including E and/or F ring opened derivatives thereof, is used to treat or prevent L-DOPA, dopamine agonist and/or dopamine enhancer induced disorders, such as L-DOPA induced dyskinesia (LID), which is a side effect of L-DOPA, dopamine agonist and/or dopamine enhancer therapies, e.g., for Parkinson's disease. The agent according to the invention may be administered in association with the therapeutic agent for the treatment of the Parkinson's disease or another dopamine-responsive disorder. 1. A method of treating or preventing L-DOPA , dopamine agonist and/or dopamine enhancer induced disorders in a subject in need thereof , comprising administering to the subject an effective amount of one or more agent selected from A/B-cis furostane , furostene , spirostane and spirostene steroidal sapogenins and ester , ether , ketone and glycosylated forms thereof , including E and/or F ring opened derivatives thereof , wherein the L-DOPA , dopamine agonist and/or dopamine enhancer induced disorder is selected from dyskinesia , hypotension , arrhythmias , nausea , disturbed respiration , sleep disorders (for example , somnolence , insomnia and vivid dreams) , dopamine dysregulation syndrome , hallucinations , and neuropsychiatric problems such as risk-taking , gambling tendency , impulse control disorders , anxiety , disorientation and confusion , psychosis and any combination thereof.2. (canceled)3. The method according to claim 1 , wherein the L-DOPA claim 1 , dopamine agonist and/or dopamine enhancer induced disorder is dyskinesia.4. The method according to claim 1 , wherein the L-DOPA claim 1 , dopamine agonist and/or dopamine enhancer induced disorder is L-DOPA-induced dyskinesia and the subject is a human undergoing L-DOPA claim 1 , dopamine agonist and/or dopamine enhancer treatment for Parkinson's disease ...

Method and composition for weight-gain management

Presented herein is a methodology for reducing weight in obese subjects and in patients receiving various medical treatments that are accompanied with weight gain. The methodology allows for management of weight gain, management of triglyceride levels and weight reduction in obese subjects.

Tamper-resistant pharmaceutical dosage form comprising nonionic surfactant

The invention relates to a pharmaceutical dosage form having a breaking strength of at least 500 N and comprising a pharmacologically active compound, a polyalkylene oxide having an average molecular weight of at least 200,000 g/mol, and a nonionic surfactant; wherein the content of the polyalkylene oxide is within the range of from 20 to 75 wt.-%, based on the total weight of the pharmaceutical dosage form.

COMPOSITIONS AND METHODS FOR THE TREATMENT OF SOMATOSENSORY DISORDERS

A method of combating a somatosensory disorder in a subject, comprising administering to the subject an effective amount of a composition comprising bupranolol and/or pharmaceutically acceptable derivative(s) thereof. Compositions useful for such administration are described, including salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine, in which such salt, ester, solvate, etc. compound is in enantiomeric excess or homoenantiomeric in the R isomer thereof, or is formulated with racemic mixtures of the R and S stereoisomers of the salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine. Combination therapy compositions of opioid receptor agonists and such compounds are also described. A method is disclosed of referential genotypic screening of candidate subjects in connection with therapeutic intervention using the compositions of the disclosure to combat the somatosensory disorder. 1. A bupranolol composition formulated for non-ophthalmic administration , comprising tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine , or a salt , ester , solvate or other pharmaceutically acceptable derivative thereof , in an enantiomeric excess of the R stereoisomer or homoenantiomeric in the R stereoisomer , and a pharmaceutically acceptable non-ophthalmic administration carrier.2. The bupranolol composition of claim 1 , wherein the tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine claim 1 , or a salt claim 1 , ester claim 1 , solvate or other pharmaceutically acceptable derivative thereof is homoenantiomeric in the R stereoisomer.3. The bupranolol composition of claim 2 , wherein the tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine claim 2 , or a salt claim 2 , ester claim 2 , solvate or other pharmaceutically acceptable derivative thereof is R-tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine.4. The bupranolol composition of claim 1 , wherein the tert- ...

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 ...

Drug Combination Comprising a Selective Serotonin Reuptake Inhibitor and a Glucocorticoid Receptor Antagonist for the Treatment of Depression

The invention provides for a combination comprising an amount of an SSRI, or a pharmaceutically acceptable salt or solvate thereof, and an amount of a GR antagonist, or a pharmaceutically acceptable salt or solvate thereof, optionally in association with one or more pharmaceutically acceptable carriers for use as therapy for depression and related disorders 1. A combination comprising an amount of an SSRI , or a pharmaceutically acceptable salt or solvate thereof , and an amount of a GR antagonist , or a pharmaceutically acceptable salt or solvate thereof , optionally in association with one or more pharmaceutically acceptable carriers.2. The combination according to for therapy3. The combination according to wherein the therapy is for depression and related disorders4. The combination according to wherein the therapy is for treatment-resistant depression5. The use of an SSRI in the manufacture of a medicament comprising a GR antagonist for the treatment of depression and related disorders.6. The use of a GR antagonist in the manufacture of a medicament comprising an SSRI for the treatment of depression and related disorders.7. A method for the treatment of an individual of a vertebrate species suffering from depression or a related disorder claim 3 , which method of treatment comprises administering an effective amount of an SSRI in combination with a GR antagonist. The invention relates to a drug combination for the treatment of depression and related disorders comprising a specific serotonin reuptake inhibitor.A recent clinical study has demonstrated that in patients with hypothalamic-pituitary-adrenal (HPA) axis disturbances, the anti-depressant efficacy of a selective serotonin reuptake inhibitor (SSRI) was less in patients with high stress hormone levels (Young et al.; HPA axis activation in major depression and response to fluoxetine: a pilot study, Psychoneuroendocrinology, 2004, vol 29, pp 1198-1204). It was suggested that those patients might be treated ...

4-SUBSTITUTED-3-BENZYLOXY-BICYCLO[3.1.0]HEXANE COMPOUNDS AS mGluR 2/3 ANTAGONISTS

A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.

Acamprosate formulations, methods of using the same, and combinations comprising the same

Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.

METHODS FOR TREATING TRIPLE NEGATIVE BREAST CANCER USING BIFUNCTIONAL SRC 3 shRNA

The present invention includes compositions and methods treating triple negative breast cancer comprising administering a therapeutically effective amount of a formulation that includes vector that expresses an SRC-1-specific bifunctional shRNA, an SRC-3-specific bifunctional shRNA, or both, to impair triple negative breast cancer cell growth. 1. A method for treating triple negative breast cancer comprising administering a therapeutically effective amount of a formulation that includes vector that expresses an SRC-1-specific bifunctional shRNA , an SRC-3-specific bifunctional shRNA , or both , to impair triple negative breast cancer cell growth.2. The method of claim 1 , wherein the formulation further comprises a cationic liposomal preparation.3. The method of claim 2 , wherein the cationic liposomal preparation comprises a single vector that encodes the SRC-1-specific bifunctional shRNA claim 2 , the SRC-3-specific bifunctional shRNA claim 2 , or both the SRC-1-specific bifunctional shRNA and the SRC-3-specific bifunctional shRNA.4. The method of claim 1 , wherein the one or more shRNA's is comprises a sequence selected from SEQ ID NO: 2 claim 1 , SEQ ID NO: 3 claim 1 , SEQ. ID NO: 4 claim 1 , SEQ ID NO: 5 claim 1 , SEQ ID NO: 6 claim 1 , SEQ ID NO: 7 claim 1 , SEQ ID NO: 8 claim 1 , SEQ ID NO: 9 claim 1 , SEQ ID NO: 10 claim 1 , SEQ ID NO: 11 claim 1 , or combinations or modifications thereof.5. The method of claim 1 , wherein a sequence arrangement for the shRNA comprises a 5′ stem arm-19 nucleotide target (SRC-3 gene)-TA-15 nucleotide loop-19 nucleotide target complementary sequence-3′ stem arm-Spacer-5′ stem arm-19 nucleotide target variant-TA-15 nucleotide loop-19 nucleotide target complementary sequence-3′ stem arm.6. The method of claim 1 , wherein the one or more polycations is a 10 kDA polyethylene glycol (PEG)-substituted cysteine-lysine 3-mer peptide (CK30PEG10k).7. The method of claim 1 , wherein the compacted DNA nanoparticles are further ...

LONG ACTING DUAL RELEASE PRODUCT CONTAINING CARBINOXAMINE AND PSEUDOEPHEDRINE

Provided are oral dosage forms that contain carbinoxamine in an immediate release format, and pseudoephedrine in a prolonged release format. The biphasic oral dosage forms may also contain other active ingredients in combination with carbinoxamine, including other decongestants, antitussives, analgesics and expectorants. 116-. (canceled)16. An orally administered pharmaceutical dosage form comprising:a) a therapeutically effective amount of carbinoxamine or pharmaceutically acceptable salt thereof in an immediate release format adapted to release at least 80% of said carbinoxamine or carbinoxamine salt in 60 minutes or less when measured in a type II dissolution apparatus according to the U.S. Pharmacopoeia in 0.1N hydrochloric acid buffer (pH=2) at 37° C.; andb) a therapeutically effective amount of pseudoephedrine or a pharmaceutically acceptable salt thereof in a prolonged release format adapted to release no more than 50% of said pseudoephedrine or pseudoephedrine salt in 60 minutes or less, and at least 75% of said pseudoephedrine or pseudoephedrine salt in eight hours or less, when measured in a type II dissolution apparatus according to the U.S. Pharmacopoeia in 0.1N hydrochloric acid buffer (pH=2) at 37° C.17. The dosage form of in the form of capsule claim 16 , tablet claim 16 , multilayer tablet or multicoated tablet.18. The dosage form of in the form of a tablet comprising first and second layers claim 16 , wherein said first later comprises from about 2 mg to about 8 mg of carbinoxamine maleate and said second layer comprises from about 60 to about 240 mg of pseudoephedrine hydrochloride.19. The dosage form of wherein said carbinoxamine or carbinoxamine salt is present in an amount sufficient to provide decongestant relief for at least about twelve hours.20. The dosage form of wherein said pseudoephedrine or pseudoephedrine salt is present in an amount sufficient to provide decongestant relief for at least about twelve hours.21. The dosage form of ...

SOX9 INHIBITORS

Methods for treating a condition associated with proteoglycan production in a mammal are provided. The methods comprise the administration of at least one of a calmodulin antagonist, a transient receptor potential (TRP) channel inhibitor and a calmodulin-binding peptide to the mammal. 1. A method of treating a pathological condition associated with proteoglycan production or modulation in a mammal comprising administering to the mammal an agent selected from the group of a calmodulin antagonist and a transient receptor potential (TRP) channel inhibitor.2. The method as defined in claim 1 , wherein the pathological condition is a condition involving inhibition of neuronal growth or neuronal plasticity.3. The method of claim 2 , wherein the condition is selected from the group consisting of spinal cord injury claim 2 , traumatic brain injury claim 2 , neurodegenerative disease claim 2 , Friedreich's ataxia claim 2 , spinocerebellar ataxia claim 2 , Alzheimer's disease claim 2 , Parkinson's Disease claim 2 , Lou Gehrig's Disease (ALS) claim 2 , demyelinative disease claim 2 , multiple sclerosis claim 2 , transverse myelitis resulting from spinal cord injury claim 2 , inflammation claim 2 , and disease associated with retinal neuronal degeneration.4. The method of claim 1 , wherein the calmodulin antagonist is selected from the group consisting of alpha-adrenergic blockers claim 1 , phenothiazines claim 1 , naphthalenesulfonamides claim 1 , ACE inhibitors claim 1 , alkaloids and pharmaceutically acceptable salts thereof.5. The method of claim 1 , wherein the calmodulin antagonist is selected from the group consisting of phenoxybenzamine claim 1 , Prazosin claim 1 , Terazosin claim 1 , Doxazosin claim 1 , Tamsulosin claim 1 , chlorpromazine claim 1 , calmidazolium claim 1 , E6 Berbamine claim 1 , CGS 9343B claim 1 , trifluoperazine claim 1 , fluphenazine claim 1 , cyclosporine claim 1 , rapamycin claim 1 , FK506 claim 1 , A7 claim 1 , J8 claim 1 , W-5 claim 1 , W-7 claim ...

Cholesterol Efflux Assay Probe Formulations, Methods of Making and Using

A cholesterol efflux assay probe formulation having a core comprised of a biocompatible hydrophobic material at least partially coated with a sphingomyelin/cholesterol layer, methods of making and methods of using are described. 1. A cholesterol efflux assay probe formulation , comprising at least one nanoparticle having a biocompatible hydrophobic core at least partially coated with a lipid-cholesterol mixture.2. The formulation of claim 1 , wherein the lipid-cholesterol mixture comprises a phospholipid and cholesterol.3. The formulation of claim 2 , wherein the phospholipid consists of sphingomyelin.4. The formulation of claim 1 , wherein the lipid-cholesterol mixture comprises cholesterol esters claim 1 , triglycerides claim 1 , or sphingolipids.5. The formulation of claim 1 , wherein the core comprises polystyrene.6. The formulation of claim 1 , wherein the at least one nanoparticle has a diameter in the range of about 25 nm to about 50 nm.7. The formulation of claim 1 , wherein the at least one nanoparticle has a diameter of about 31 nm.8. The formulation of claim 1 , wherein the core is at least partially porous to allow for passive adsorption of lipids and hydrophobic molecules on the surface of the formulation.9. The formulation of claim 1 , further including at least one of: a therapeutic agent claim 1 , a diagnostic agent claim 1 , or a contrast agent claim 1 , at least partially encapsulated in the formulation.10. The formulation of claim 1 , wherein the formulation has a Zeta potential in the range of from about −10 mV to about −100 mV.11. The formulation of claim 1 , wherein the formulation is stable at cell culture conditions.12. The formulation of claim 1 , wherein the formulation comprises nanoparticles loaded with a drug selected from the group consisting of: cholesterol drugs claim 1 , anticancer agents claim 1 , antibacterial agents claim 1 , antiviral agents claim 1 , autoimmune agents claim 1 , anti-inflammatory agents claim 1 , cardiovascular ...

Soft Elastic Capsules Containing Tablets and Liquid or Semisolid Fills and Methods for Their Manufacture

Disclosed herein is a soft elastic capsule that includes an acid resistant, capsule shell that defines an encapsulated space having a predetermined volume, a liquid or semisolid fill comprising a first active ingredient located within the encapsulated space, and a first compressed tablet a having a minimal dimension of 2 mm, being located within the encapsulated space, unanchored to the capsule shell, and surrounded by the fill, said tablet comprising a second active ingredient that is substantially insoluble in the fill. A method of manufacturing a soft elastic capsule is also disclosed.

PROSTAGLANDIN AND VASOCONSTRICTOR PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE

Compositions containing a prostaglandin agent and a vasoconstrictor agent for ophthalmic applications are provided as well as methods of treating ophthalmic diseases using the same. In certain embodiments, the compositions and methods are useful for treating glaucoma without causing conjunctival hyperemia. 1. A composition comprising a prostaglandin agent and a vasoconstrictor agent.2. The composition of claim 1 , wherein said composition is an ophthalmic pharmaceutical formulation further comprising an ophthalmically acceptable excipient.3. The composition of claim 1 , wherein said prostaglandin agent is present in a therapeutically effective amount.4. The composition of claim 1 , wherein said vasoconstrictor agent is present in a sub-therapeutic amount.5. The composition of claim 2 , wherein said prostaglandin agent and said vasoconstrictor agent are present in a combined amount effective to treat an ophthalmic disease.6. The composition of claim 2 , wherein said ophthalmic pharmaceutical formulation is a gel formulation.7. The composition of claim 2 , wherein said ophthalmic pharmaceutical formulation is an aqueous solution.8. The composition of claim 2 , wherein said prostaglandin agent is bimatoprost.9. The composition of claim 8 , wherein said bimatoprost is present in an amount approximately equal to or less than about 0.1% w/w.10. The composition of claim 8 , wherein said bimatoprost is present in an amount of about 0.03% w/w.11. The composition of claim 2 , wherein said prostaglandin agent is travoprost.12. The composition of claim 11 , wherein said travoprost is present in an amount approximately equal to or less than about 0.1% w/w.13. The composition of claim 11 , wherein said travoprost is present in an amount of about 0.004% w/w.14. The composition of claim 2 , wherein said prostaglandin agent is latanoprost.15. The composition of claim 14 , wherein said latanoprost is present in an amount approximately equal to or less than about 0.1% w/w.16. The ...

USE OF BETA-ADRENERGIC INVERSE AGONISTS FOR SMOKING CESSATION

The chronic use of p-adrenergic inverse agonists such as nadolol, carvedilol, and ICI-118,551 provides an improved method for the treatment of mucus hypersecretion in subjects with such mucus hypersecretion. One aspect of a method according to the present invention is a method of preventing or controlling mucus hypersecretion in the respiratory tract comprising administering a therapeutically effective quantity of a p-adrenergic inverse agonist to a subject with mucus hypersecretion or at risk of mucus hypersecretion. The invention further encompasses pharmaceutical compositions comprising the p-adrenergic inverse agonist and the additional compound. 1. A method of preventing or controlling mucus hypersecretion in the respiratory tract comprising administering a therapeutically effective quantity of a β-adrenergic inverse agonist to a subject with mucus hypersecretion or at risk of mucus hypersecretion.2. The method of wherein the mucus hypersecretion is associated with smoking cessation and the subject is attempting smoking cessation or is about to cease smoking.34.-. (canceled)5. The method of wherein the β-adrenergic inverse agonist is selected from the group consisting of β-selective inverse agonists claim 1 , and non-selective inverse agonists having inverse agonist activity against both β- and β-adrenergic receptors.6. The method of wherein the β-adrenergic inverse agonist is a β-selective inverse agonist.7. The method of wherein the β-adrenergic inverse agonist is selected from the group consisting of nadolol claim 1 , bupranolol claim 1 , butoxamine claim 1 , carazolol claim 1 , carvedilol claim 1 , ICI-118 claim 1 ,551 claim 1 , levobunolol claim 1 , metoprolol claim 1 , propranolol claim 1 , sotalol claim 1 , and timolol.9. The method of wherein the β-adrenergic inverse agonist is nadolol.11. The method of wherein the β-adrenergic inverse agonist is carvedilol.1218.-. (canceled)19. The method of wherein the method exerts a therapeutic effect that is an ...

Use of selective estrogen receptor modulator for joint fusion and other repair or healing of connective tissue

Methods for facilitating joint immobilization or fusion using selective estrogen receptor modulator (SERM) such as raloxifene are disclosed. The SERM may be administered systemically or locally. In conjunction with SERM, other therapeutic agents such as calcium, vitamin D, bone morphogenetic protein may be administered simultaneously. The method can similarly be applied to facilitate bone repair, bone healing, and connective tissue healing processes in a patient.

Selective inhibition of beta1- adrenergic receptors for the treatment of pediatric heart failure

Provided are methods of treating heart failure in children using B1-selective adrenergic receptor antagonists, alone or in combination with other agents, including B-2-selective adrenergic receptor agonists.

COMBINATIONS COMPRISING ANTIMUSCARINIC AGENTS AND BETA-ADRENERGIC AGONISTS

Combinations comprising (a) a β2 agonist and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane, in the form of a salt having an anion X, which is a pharmaceutically acceptable anion of a mono or polyvalent acid are useful, e.g., for the treatment of respiratory disease, e.g., asthma or chronic obstructive pulmonary disease. 1. A combination which comprises (a) a β2 agonist and (b) an antagonist of M3 muscarinic receptors which is 3(R)-(2-hydroxy-2 ,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane , in the form of a salt having an anion X , which is a pharmaceutically acceptable anion of a mono or polyvalent acid.2. The combination according to wherein the antagonist of M3 muscarinic receptors (b) is 3(R)-(2-hydroxy-2 claim 1 ,2-dithien-2-ylacetoxy)-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide.3. The combination according to characterised in that the active ingredients (a) and (b) form part of a single pharmaceutical composition.4. The combination according to wherein the active ingredients (a) and (b) are provided together with instructions for simultaneous claim 1 , concurrent claim 1 , separate or sequential administration claim 1 , in a kit of parts for the treatment of a patient suffering from or susceptible to a respiratory disease which responds to M3 antagonism.5. The combination according to wherein the respiratory disease is asthma or chronic obstructive pulmonary disease (COPD).6. The combination according wherein the β2 agonist is selected from the group consisting of arformoterol claim 1 , bambuterol claim 1 , bitolterol claim 1 , broxaterol claim 1 , carbuterol claim 1 , clenbuterol claim 1 , dopexamine claim 1 , fenoterol claim 1 , formoterol claim 1 , hexoprenaline claim 1 , ibuterol claim 1 , isoprenaline claim 1 , mabuterol claim 1 , meluadrine claim 1 , nolomirole claim 1 , orciprenaline claim 1 , pirbuterol claim 1 , ...

Pharmaceutical Compositions

A pharmaceutical composition for inhalation comprising R (+) budesonide and one or more bronchodilators, and, optionally, one or more pharmaceutically acceptable excipients is described.

METHODS AND COMPOSITIONS FOR CANCER PREVENTION AND TREATMENT

The present invention provides methods of preventing or delaying the development of cancer (e.g., breast cancer) in BRCA1 mutation positive patients by beginning progesterone receptor antagonist treatment at an early age (e.g., by age 35, 30, or 25). In certain embodiment, such early treatment is long-term treatment, which may substitute or delay a preventative ovariectomy, single or double mastectomy (e.g., in patients wishing to delay or avoid a mastectomy, or patients that cannot afford a mastectomy). 1. A method for preventing progesterone receptor related cancers comprising:a) providing a subject with a breast cancer gene 1 (BRCA1) mutation that is progesterone receptor related, wherein said subject is less than 35 years old and does not have detectable progesterone receptor related cancer;b) providing a progesterone receptor antagonist, andc) treating said subject with said progesterone receptor antagonist thereby preventing, or delaying the onset of, said progesterone receptor related cancer.2. The method of claim 1 , wherein said subject has been diagnosed as possessing said BRCA 1 mutation.3. The method of claim 1 , wherein said subject has been diagnosed as likely to have said BRCA1 mutation based on family history.4. The method of claim 1 , wherein said subject is less than 30 years old and does not have detectable progesterone receptor related cancer.5. The method of claim 1 , wherein said subject is less than 25 years old and does not have detectable progesterone receptor related cancer.6. The method of claim 1 , wherein said antagonist of the progesterone receptor is a selective progesterone receptor modulator.7. The method of claim 6 , wherein said selective progesterone receptor modulator comprises mifepristone.8. The method of claim 6 , wherein said selective progesterone receptor modulator comprises 17α-acetoxy-11β-(4-N claim 6 ,N-dimethylaminophenyl)-19-norpregna-4 claim 6 ,9-diene-3 claim 6 ,20-dione (CDB-2914).9. The method of claim 1 , further ...

PHARMACEUTICAL COMPOSITIONS FOR SLEEP APNEA

Pharmaceutical compositions are provided for the pharmacological treatment of breathing disorders and, more specifically, to compositions containing agents having serotonin receptor modulating activity for the alleviation of sleep apnea (central and obstructive) and other sleep-related breathing disorders wherein the active ingredients are released such as to extend effective blood plasma concentrations across the period of sleep. 1. An orally administrable pharmaceutical composition for providing modified release of a serotonin receptor antagonist wherein the release of antagonist provides a therapeutically effective level of antagonist in the blood plasma of a subject over a continuous period in excess of 4 hours ,wherein the composition further comprises an SNRI.2. A composition as claimed in wherein the period extends to between 6 and 14 hours from administration of the composition.3. (canceled)4. (canceled)5. The composition as claimed in which provides a therapeutically effective level for a continuous period initiated at from 0 to 2 hours from administration of the composition and extending to between 6 and 14 hours from administration of the composition.6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. The composition as claimed in wherein the antagonist is ondansetron.11. A pharmaceutical formulation comprising a composition as claimed in claim 1 , wherein the antagonist is released in two or more pulses claim 1 , wherein a first pulse of antagonist is released within 30 minutes of oral administration and a second pulse is released between 1 hour and 4 hours of administration.12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. The composition according to claim 1 , wherein the SNRI is a member selected from the group consisting of venlafaxine claim 1 , duloxetine claim 1 , and milnacipran.19. The composition according to claim 1 , wherein the serotonin receptor antagonist is ondansetron and the SNRI is milnacipran. ...

Combination breast cancer therapy with hsp90 inhibitory compounds

Methods for treating breast cancer, comprising administering to the subject an effective amount of a selective estrogen receptor modulator and an effective amount of a compound represented by the following structural formula: (I) (Ia) a tautomer, or a pharmaceutically acceptable salt thereof. The variables depicted in the structural formula are defined herein.

Composition and Method for Treatment of Depression and Psychosis in Humans

Compositions and methods tor the treatment of depression and psychoses in humans are disclosed. More particularly, the invention is directed to formulations containing antipsychotic and/or antidepressant medications and also containing an NMPAR antagonist. The present invention is also directed to methods for the treatment of humans suffering from depression and other psychoses, including, schizophrenia, by administration of the inventive compositions in antidepressant and/or antipsychotic effective amounts.

Transdermal Delivery of Therapeutic Agents Using Poly (Amidoamine) Dendrimers

The invention provides for compositions for transdermal delivery of a therapeutic agent associated with a surface modified poly(amidoamine) PAMAM dendrimer, wherein the surface modified dendrimer increased skin penetration of the therapeutic agent. The invention particularly provides for compositions and methods for transdermal delivery of anticancer and chemo-preventive agents.

METHODS FOR INDUCING MITOCHONDRIAL BIOGENESIS

Methods and compositions for inducing mitochondrial biogenesis are provided. In some aspects, methods for the treatment of diseases such as acute kidney disease (AKI) or a muscle wasting disease by administering tomoxetine, nisoxetine, fenoterol, formoterol, or procaterol to an individual are provided. 1. A method of inducing mitochondrial biogenesis , comprising administering to a subject , identified as in need of increased mitochondrial biogenesis , a pharmacologically effective dose of a beta-2 adrenergic receptor agonist , wherein the beta-2 adrenergic receptor agonist is tomoxetine , nisoxetine , fenoterol , formoterol , or procaterol.2. The method of claim 1 , wherein a pharmacologically effective dose of tomoxetine claim 1 , nisoxetine claim 1 , fenoterol claim 1 , or procaterol is administered to the subject.3. The method of claim 1 , wherein the compound is administered to the subject orally claim 1 , intravenously claim 1 , intramuscularly claim 1 , intraperitoneally claim 1 , topically claim 1 , or via inhalation.4. The method of claim 1 , wherein the compound is comprised in a pharmaceutically acceptable formulation.5. The method of claim 1 , wherein the subject is a human.6. The method of claim 1 , wherein the subject has been identified as having deficient mitochondrial biogenesis by a muscle biopsy test claim 1 , a metabolic test claim 1 , or a genetic test.7. The method of claim 1 , wherein the subject has a mitochondrial injury.8. The method of claim 7 , wherein the mitochondrial injury resulted from an acute kidney injury (AKI) claim 7 , neurodegeneration claim 7 , a heart disease claim 7 , heart attack claim 7 , a stroke claim 7 , renal dysfunction claim 7 , type 2 diabetes claim 7 , a central nervous system disorder claim 7 , Alzheimer's disease claim 7 , Parkinson's disease claim 7 , Huntington's disease claim 7 , ischemia/reperfusion claim 7 , trauma claim 7 , a drug/toxicant-induced organ injury claim 7 , chronic traumatic encephalopathy (CTE ...

Chloride channel and chloride transporter modulators for therapy in smooth muscle diseases

The present invention provides, inter alia, methods and pharmaceutical compositions for preventing, treating, or ameliorating the effects of a disease characterized by altered smooth muscle contractility, such as e.g., asthma and chronic obstructive pulmonary disease.

COMPOUND COMPOSITION FOR INHALATION USED FOR TREATING ASTHMA

A compound composition for inhalation comprising β2 receptor agonist and corticosteriod is provided in the present invention. The composition is used as a reliever for a patient with asthma or chronic obstructive pulmonary disease, or a controller in eccentric way, and can reduce drug acute resistance of β2 receptor agonist. 110-. (canceled)11. An inhaled composition , characterized by comprising:an effective amount of beta-2 agonist; andan effective amount of corticosteroid.12. The composition as claimed in claim 11 , further comprising a pharmaceutically acceptable carrier.13. The composition as claimed in claim 11 , wherein the composition is an inhaled aerosol composition.14. The composition as claimed in claim 11 , wherein the composition is configured to be used as a reliever for a patient with asthma or obstructive respiratory disorder.15. The composition as claimed in claim 11 , further characterized by being used as a controller in eccentric way such as before sleeping or after waking up.16. The composition as claimed in claim 11 , wherein the beta-2 agonist is one selected from a group consisting of Albuterol claim 11 , Fenoterol claim 11 , Procaterol claim 11 , Terbutaline claim 11 , Albuterol sulfate claim 11 , Procaterol HCl claim 11 , Fenoterol hydrobromide claim 11 , Terbutaline sulphate and a combination thereof.17. The composition as claimed in claim 11 , wherein the corticosteroid is one selected from a group consisting of Budesonide claim 11 , Fluticasone claim 11 , Mometasone claim 11 , Ciclesonide claim 11 , Beclomethasone claim 11 , Triamcinolone claim 11 , Fluticasone propionate claim 11 , Beclomethasone dipropionate claim 11 , Triamcinolone Acetonide and a combination thereof.18. The composition as claimed in claim 11 , wherein the ratio of the beta-2 agonist and the corticosteroid is 1:2 w/w % to 1:70 w/w %.19. A preparation method of an inhaled aerosol composition comprising:mixing an effective amount of beta-2 agonist with an effective ...

COMPOSITIONS FOR TREATING NEUROLOGICAL DISORDERS

The present invention relates to compositions and methods for the treatment of neurological disorders related to glutamate excitotoxicity and Amyloid β toxicity. More specifically, the present invention relates to novel combinatorial therapies of Multiple Sclerosis, Alzheimer's disease, Alzheimer's disease related disorders, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, neuropathic pain, alcoholic neuropathy, alcoholism or alcohol withdrawal, or spinal cord injury. 1. A method of treating of a neurological disorder in a subject in need thereof comprising administering to said subject a compound selected from Torasemide , Trimetazidine , Mexiletine , Ifenprodil , Moxifloxacin or Bromocriptine , or a salt , prodrug , derivative , or sustained release formulation thereof.2. The method of claim 1 , further comprising administering to the subject at least one further distinct compound selected from Sulfisoxazole claim 1 , Methimazole claim 1 , Prilocalne claim 1 , Dyphylline claim 1 , Quinacrine claim 1 , Carbenoxolone claim 1 , Acamprosate claim 1 , Aminocaproic acid claim 1 , Baclofen claim 1 , Cabergoline claim 1 , Diethylcarbamazine claim 1 , Cinacalcet claim 1 , Cinnarizine claim 1 , Eplerenone claim 1 , Fenoldopam claim 1 , Leflunomide claim 1 , Levosimendan claim 1 , Sulodexide claim 1 , Terbinafine claim 1 , Zonisamide claim 1 , Etomidate claim 1 , Phenformin claim 1 , Trimetazidine claim 1 , Mexiletine claim 1 , Ifenprodil claim 1 , Moxifloxacin claim 1 , Bromocriptine or Torasemide claim 1 , or a salt claim 1 , prodrug claim 1 , derivative claim 1 , or sustained release formulation thereof.3. The method of claim 2 , comprising administering at least one of the following combinations of compounds:Baclofen and Torasemide,Sulfisoxazole and Torasemide,Eplerenone and Torasemide,Acamprosate and Ifenprodil,Baclofen and Mexiletine,Baclofen and Trimetazidine,Bromocriptine and Sulfisoxazole,Cinacalcet and Mexiletine,Cinnarizine and ...

DIRECTED DIFFERENTIATION OF OLIGODENDROCYTE PRECURSOR CELLS TO A MYELINATING CELL FATE

The present invention provides methods of inducing differentiation of oligodendrocyte progenitor cells to a mature myelinating cell fate with a neurotransmitter receptor modulating agent. The present invention also provides methods of stimulating increased myelination in a subject in need thereof by administering said neurotransmitter receptor modulating agent. Methods of treating a subject having a demyelinating disease using a neurotransmitter receptor modulating agent are also provided. 1. A method of stimulating increased myelination of nerves in a human subject having a demyelinating disease , the method comprising:administering to the subject a therapeutically effective dose of a neurotransmitter receptor modulating agent selected from a muscarinic receptor antagonist, a dopamine receptor antagonist, a histamine receptor antagonist, a beta adrenergic receptor modulator, and an opioid receptor modulator; thereby stimulating increased myelination of nerves in the subject.2. The method of claim 1 , wherein the neurotransmitter receptor modulating agent is a muscarinic receptor antagonist.3. (canceled)4. The method of claim 2 , wherein the muscarinic receptor antagonist is selected from benztropine claim 2 , carbetapentane claim 2 , clemastine claim 2 , ipratropium claim 2 , atropine claim 2 , and salts thereof.5. The method of claim 1 , wherein the neurotransmitter receptor modulating agent is a dopamine receptor antagonist.6. (canceled)7. The method of claim 5 , wherein the dopamine receptor antagonist is selected from benztropine claim 5 , GBR12935 claim 5 , trifluoperazine claim 5 , and salts thereof.8. The method of claim 1 , wherein the neurotransmitter receptor modulating agent is a histamine receptor antagonist.9. (canceled)10. The method of claim 8 , wherein the histamine receptor antagonist is clemastine or a salt thereof.11. The method of claim 1 , wherein the neurotransmitter receptor modulating agent is a beta adrenergic receptor antagonist.12. ( ...

Controlled release pharmaceutical compositions

The present application discloses a sustained release composition in pellet form, wherein the core of the pellet comprises: (a) a therapeutically effective amount of a medicament; (b) 0.5 to 50% by weight of a water-soluble polymer; and (c) 1 to 25% by weight of a water-insoluble polymer applied as an aqueous latex dispersion and subsequently the water is removed, wherein the sum of the percentages of the medicament, the water-insoluble polymer and the water-soluble polymer is equal to or less than 100%. It also discloses methods of making this composition.

Pramipexole transdermal delivery for severe headaches

The present invention relates to a method for the treatment and prevention of cluster headaches and migraines using the transdermal administration of pramipexole.

TREATMENT FOR CEREBRAL PALSY IMPAIRED SPEECH IN CHILDREN

Cerebral palsy impaired speech in children and adolescents are effectively treated by administration of a psychostimulant. Low doses of the psychostimulant significantly increases the percentage of correctly pronounced intelligible syllables or words and the ability to more intelligibly communicate. The improvement in speech persists after cessation of or prior to continued psychostimulant treatment. 1. A method for treating a speech impairment secondary to cerebral palsy in a subject in need of such treatment , said method comprises:(a) providing a psychostimulant;(b) administering the psychostimulant in a therapeutically effective dose to the subject;whereby the speech impairment is diminished.2. The method of claim 1 , wherein the subject has a chronological age is greater than the speech-language age equivalence prior to step (a) and the difference between the chronological age and speech language age equivalence is diminished after step (b).3. The method of claim 1 , wherein there is a diminished difference in chronological age to speech-language age equivalence that persists after the psychostimulant is no longer efficaciously active in the subject.4. The method of claim 1 , wherein the subject is unable to pronounce one or more of the bilabial consonants prior to step (a) and is able to pronounce the one or more bilabial consonants after step (b).5. The method of claim 1 , wherein steps (a) and (b) are repeated periodically over a period of time and wherein the diminishment in the impaired speech continues over the period of time.6. The method of claim 1 , wherein further comprising prior to step (a) determining the cognitive functional age of the subject through non-verbal means claim 1 , and wherein the cognitive functional age is at least about two years.7. The method of claim 1 , wherein the diminished speech impairment comprises a percentage increase in correctly pronounced syllables and words of from at least about 20% to several hundred percent.8. The ...

COMBINATION THERAPIES COMPRISING ANTI-ERBB3 AGENTS

Disclosed are methods and compositions for inhibiting the growth of a tumor (e.g., a malignant tumor) in a subject. In particular, combination therapies for treating a tumor in a subject by co-administering either i) an effective amount of an anti-estrogen agent or ii) an effective amount of a receptor tyrosine kinase inhibitor and an effective amount of a bispecific anti-ErbB2/anti-ErbB3 antibody, and optionally an effective amount trastuzumab. Also disclosed is a bispecific anti-ErbB2/anti-ErbB3 antibody for use in the therapy of a tumor in combination with either i) an anti-estrogen agent or ii) a receptor tyrosine kinase inhibitor, and optionally in use with trastuzumab. 1. A method of treating a subject with a malignant tumor , the method comprising co-administering to the subject:eitheri) an effective amount of an anti-estrogen agent, orii) an effective amount of a receptor tyrosine kinase inhibitor; andeitheriii) an effective amount of a bispecific anti-ErbB2/anti-ErbB3 antibody, oriv) an effective amount of a bispecific anti-ErbB2/anti-ErbB3 antibody and an effective amount of trastuzumab.25.-. (canceled)6. The method of claim 1 , wherein all effective amounts are either mouse effective amounts or human effective amounts.78.-. (canceled)9. The method of claim 1 , wherein the co-administration to the subject does not create a drug-drug interaction-mediated toxicity in the subject.10. The method of claim 1 , wherein the co-administration to the subject creates a substantially additive or superadditive effect.11. The method of claim 1 , wherein the anti-estrogen agent is an estrogen receptor antagonist or an aromatase inhibitor.12. The method of claim 11 , wherein the estrogen receptor antagonist is fulvestrant or tamoxifen.13. The method of claim 11 , wherein the aromatase inhibitor is letrozole claim 11 , exemestane claim 11 , anastrozole claim 11 , aminoglutethimide claim 11 , testolactone claim 11 , vorozole claim 11 , formestane claim 11 , or fadrozole.14. ...

TREATMENT OF ACUTE EXACERBATION OF ASTHMA AND REDUCTION OF LIKELIHOOD OF HOSPITALIZATION OF PATIENTS SUFFERING THEREFROM

The invention provides a method of improving one or more clinical outcomes of an individual experiencing an acute respiratory attack. The acute respiratory attack may include acute reversible bronchospasm, severe acute bronchospasm, or acute exacerbation of asthma. The method includes administering to an individual suffering from an acute respiratory attack an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen. 1. A method of improving one or more clinical outcomes of an individual experiencing an acute exacerbation of asthma , comprising administering to an individual suffering from an acute exacerbation of asthma an effective amount of bedoradrine or a pharmaceutically acceptable salt thereof in combination with a standard of care (SOC) treatment regimen.2. The method of in which the bedoradrine or a pharmaceutically acceptable salt thereof is administered after administration of the SOC treatment regimen.3. The method of in which the bedoradrine or a pharmaceutically acceptable salt thereof is administered contemporaneously with the SOC treatment regimen.4. The method of in which the bedoradrine or a pharmaceutically acceptable salt thereof is administered before administration of the SOC treatment regimen.5. The method of in which the SOC treatment regimen comprises administration of one or more 3-agonist bronchodilators claim 1 , one or more anti-cholinergic drugs claim 1 , one or more corticosteroids claim 1 , or combinations thereof.6. The method of in which the SOC treatment regimen includes the administration of magnesium.7. The method of in which the one or more n-agonist bronchodilators claim 5 , or one or more anti-cholinergic drugs are administered by inhalation claim 5 , injection claim 5 , or intravenous infusion.8. The method of in which the one or more β-agonist bronchodilators are selected from albuterol claim 5 , bitolterol claim 5 , levalbuterol claim 5 , ...

METHODS AND COMPOSITIONS FOR THE "BROWNING" OF WHITE FAT

Methods for increasing the amount of brown adipose tissue in a subject, of increasing the ratio of brown fat to white fat in a subject, or for effecting a change in white adipose tissue to become brown adipose tissue in a subject include the administration of one or more agents. The agent can increase or induce hypothalamic expression of BDNF, can be a TrkB receptor agonist or a beta-3 adrenergic receptor agonist, or encode an agonist that modulates a hypothalamic-adipocyte axis. 1. A method for increasing the amount of brown adipose tissue in a subject having a low amount of brown adipose tissue , the method comprising administering a TrkB receptor agonist or a nucleotide sequence encoding the TrkB receptor agonist to a subject having a low amount of brown adipose tissue to white adipose tissue , wherein the TrkB receptor agonist or expression of the TrkB receptor agonist increases the amount of brown adipose tissue in the subject.2. The method of claim 1 , wherein the TrkB receptor agonist is administered as a peptide.3. The method of claim 2 , wherein the peptide is selected from the group consisting of BDNF claim 2 , Neurotrophin-4 claim 2 , and Neurotrophin-3.4. The method of claim 3 , wherein the peptide is BDNF.5. The method of claim 1 , wherein the nucleotide sequence is administered encoding BDNF claim 1 , Neurotrophin-4 claim 1 , Neurotrophin-3 claim 1 , or a combination thereof.6. The method of claim 5 , wherein the nucleotide sequence encodes BDNF.7. The method of claim 1 , wherein the TrkB receptor agonist or the nucleotide sequence encoding the TrkB receptor agonist is administered systemically claim 1 , centrally claim 1 , directly into a brain claim 1 , or a combination thereof in an amount sufficient to activate the TrkB receptor.8. The method of claim 1 , wherein the TrkB receptor agonist or expression of the TrkB receptor agonist modulates sympathetic nervous system activity claim 1 , thereby increasing the amount of brown adipose tissue in the ...

ANTCIN DERIVATIVES IN COMBINATION WITH ANTI-CANCER DRUGS IN THE TREATMENT AND/OR PREVENTION OF TUMORS

The invention surprisingly found that antcin or an ester derivative, salt or a composition thereof in combination with an anti-tumor drug provides unexpected efficacy in inhibiting tumors, while retaining normal cells at high viability. In addition, the amount of the anti-tumor drug in chemotherapy can be reduced by combinatorially using antcin or an ester derivative, salt or a composition thereof in view of the fact that they play a role in adjuvant therapy. 2. The combination of claim 1 , wherein the antcin is selected from the group consisting of: antcin A claim 1 , antcin B claim 1 , antcin C claim 1 , antcin D claim 1 , antcin E claim 1 , antcin F claim 1 , antcin H claim 1 , and antcin K.3. The combination of claim 1 , wherein the antcin is antcin A.4. The combination of claim 1 , wherein the salt of antcin includes base addition and acid addition salts.5. The combination of claim 1 , wherein the ester derivative of antcin is selected from the group consisting of: alkyl actcin claim 1 , alkynyl actcin claim 1 , and alkeny antcin.6. The combination of claim 1 , wherein the ester derivative of antcin is selected from the group consisting of: methyl antcinate A claim 1 , methyl antcinate B claim 1 , methyl antcinate C claim 1 , methyl antcinate G claim 1 , methyl antcinate H claim 1 , ethyl antcinate A claim 1 , and ethyl antcinate B.7Taiwanofungus camphoratus.. The combination of claim 1 , wherein the composition of antcin is an extract of8Taiwanofungus camphoratusTaiwanofungus camphoratus. The combination of claim 7 , wherein the extract of is the low polar fraction of ethanol extract.9. The combination of claim 1 , wherein the anti-tumor drug is an antimitotic drug claim 1 , an antimetabolite drug claim 1 , an alkyling agent claim 1 , a nitrogen mustard claim 1 , a drug that targets DNA claim 1 , a topoisomerase inhibitor claim 1 , a hormone antagonist claim 1 , or a tyrosine kinase inhibitor.10. The combination of claim 9 , wherein the antimitotic drug is ...

MULTILAYER TABLET

A multilayer oral dosage form that provides controlled release of an active compound includes a non-erodible core containing a pharmaceutically active compound and/or a nutritionally active compound, and at least one release-modulating layer laminated to each side of the core layer. The dosage form can be prepared using simple, inexpensive tablet compression techniques. 1. A trilayer tablet , comprising:a porous, non-erodible core layer containing at least one pharmaceutically active compound and/or at least one nutritionally active compound; andat least one erodible layer laminated to each side of the non-erodible core layer;wherein the porous, non-erodible core layer comprises at least one insoluble polymer defining a matrix.2. The trilayer tablet of claim 1 , wherein the active compound is soluble in a gastrointestinal fluid.3. The trilayer tablet of claim 1 , wherein the active compound is selected from Tramadol HCl claim 1 , Bupropion and Propanolol.4. The trilayer tablet of claim 1 , in which the porous claim 1 , non-erodible core layer further comprises a pore-forming material.5. The trilayer tablet of claim 1 , in which at least one insoluble polymer in the porous non-erodible core layer is a swellable insoluble polymer.6. The trilayer tablet of claim 1 , wherein the layers laminated to each side of the core layer are comprised of at least one swellable erodible polymer.7. The trilayer tablet of claim 1 , wherein at least one of the erodible layers comprises at least one polymer that is permeable to water.8. The trilayer tablet of claim 1 , wherein at least one of the erodible layers comprises at least one insoluble polymer.9. The trilayer tablet of claim 1 , wherein at least one of the erodible layers comprises from about 10% to about 30% by weight of at least one insoluble polymer.10. The trilayer tablet of claim 1 , wherein at least one of the erodible layers comprises from about 15% to about 25% by weight of at least one insoluble polymer. This ...

DOSAGE REGIMEN FOR A S1P RECEPTOR AGONIST

S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial days of treatment the daily dosage is lower than the standard daily dosage 1. A kit comprising units of medication of a S1P receptor modulator or agonist , comprising one or more low-dose units of a dose strength below the standard daily dose of the S1P receptor agonist , whereby the unit is to be administered during the initial period of treatment , and wherein the S1P receptor modulator or agonist is 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1 ,3-diol (FTY720) , or a pharmaceutically acceptable salt thereof.2. A kit containing daily units of medication of an S1P receptor modulator or agonist of varying daily dosage , whereby the daily dosage of S1P receptor modulator or agonist is ⅕ and 1/2.5; or ¼ and ½ , of the standard dose of the S1P receptor modulator or agonist , respectively , and optionally units for the standard daily dosage of the S1P receptor modulator or agonist , wherein the S1P receptor modulator or agonist is 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1 ,3-diol (FTY720) , or a pharmaceutically acceptable salt thereof.3. A kit containing daily units of medication of an S1P receptor modulator or agonist of varying daily dosage , whereby said kit contains a) one or more of the following: 1/10 , ⅛ , ⅕ , ¼ , ⅓ , 1/2.5 , ½ , 1/1.5 , of the standard dose of the S1P receptor modulator or agonist , respectively , and b) units for the standard daily dosage of the S1P receptor modulator or agonist , wherein the S1P receptor modulator or agonist is 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1 ,3-diol (FTY720) , or a pharmaceutically acceptable salt thereof.4. A Kit according to claim 1 , wherein the unit for the standard daily dosage of the S1P receptor modulator of agonist contains 0.5 mg of said S1P receptor modulator or agonist.5. A Kit according to claim 2 , wherein the unit for the standard daily dosage of the S1P receptor modulator of agonist contains ...

METHODS FOR DRUG SCREEN USING ZEBRAFISH MODEL AND THE COMPOUNDS SCREENED THEREFROM

The disclosure relates to a platform of using zebrafish in screening candidates for treating and/or preventing myopia and keratoconus disease. The disclosure is mainly based on that Lumican, one of several SLRPs, plays an important role in the regulation of fibrillogenesis or the genes affecting the size of eyeballs in zebrafish, in addition to playing an important role in clinical myopia. Therefore, the disclosure uses the established zebrafish model to further identify the drugs affecting the expression of lumican and collagen fibrillogenesis, and/or the regulation of eyeball size. These drugs are potential candidates for treating myopia and/or keratoconus disease. 1. A method for treating a disease mediated by expression of lumican and/or collagen fibrillogenesis , and/or treating myopia and/or keratoconus disease , comprising administering to the subject a therapeutically effective amount of a MMP inhibitor.6. The method of claim 5 , wherein the compound is CL-82198 claim 5 , Marimastat claim 5 , or Batimastat.8. The method of claim 7 , wherein Ris H; Ris H claim 7 , —CH-pyrrolyl claim 7 , —CH—NH—CH—CH—CH—CH—CH(NH2)-COOH; Ris H or oxo; Ris H or OH; Ris H or OH and Ris NH claim 7 , N(CH)or halogen.10. The method of claim 9 , wherein the compound is Minocycline claim 9 , Tetracycline or doxycycline.17. A method for treating a disease medicated by expression of lumican and/or collagen fibrillogenesis claim 9 , and/or treating myopia and/or keratoconus disease claim 9 , comprising administering to the subject a therapeutically effective amount of a TGF-beta inhibitor.19. The method of claim 18 , wherein the TGF-beta inhibitor is Losartan claim 18 , N-acetylcysteine claim 18 , Propofol and Captopril.20. The method of claim 1 , wherein the method is for treating myopia.21. The method of claim 17 , wherein the method is for treating myopia. This application claims priority to U.S. Provisional Patent Application No. 61/649,611, filed on May 21, 2012, the disclosure of ...

COMBINATION THERAPIES COMPRISING ANTI-ERBB3 AGENTS

Disclosed are methods and compositions for inhibiting the growth of a tumor (e.g., a malignant tumor) in a subject. In particular, combination therapies for treating a tumor in a subject by co-administering an agent selected from i) an effective amount of an anti-estrogen agent; ii) an effective amount of a receptor tyrosine kinase inhibitor; iii) an effective amount of a MEK/PI3 kinase/AKT inhibitor; iv) an effective amount of MM-151; v) an effective amount of an mTOR inhibitor; and/or vi) an effective amount of trastuzumab or TMD1, and/or combinations thereof; and an effective amount of a bispecific anti-ErbB2/anti-ErbB3 antibody. Also disclosed is a bispecific anti-ErbB2/anti-ErbB3 antibody for use in the therapy of a tumor in combination with an agent selected from i) an effective amount of an anti-estrogen agent; ii) an effective amount of a receptor tyrosine kinase inhibitor; iii) an effective amount of a MEK/PI3 kinase/AKT inhibitor; iv) an effective amount of MM-151; v) an effective amount of an mTOR inhibitor; and/or vi) an effective amount of trastuzumab or TMD1, and/or combinations thereof. 1. A method of treating a subject with a malignant tumor , the method comprising co-administering to the subject an agent selected from one or more of i) an effective amount of an anti-estrogen agent; ii) an effective amount of a receptor tyrosine kinase inhibitor; iii) an effective amount of a MEK/PI3 kinase/AKT inhibitor; iv) an effective amount of MM-151; v) an effective amount of an mTOR inhibitor; and/or vi) an effective amount of trastuzumab or ado-trastuzumab emtanstine; and an effective amount of a bispecific anti-ErbB2/anti-ErbB3 antibody.28.-. (canceled)9. The method of claim 1 , wherein the co-administration to the subject does not create a drug-drug interaction-mediated toxicity in the subject.10. The method of claim 1 , wherein the co-administration to the subject creates a substantially additive or superadditive effect.11. (canceled)12. The method of ...

Treatment of cerebral ischemia

The present invention relates to new compositions and methods for protecting neuronal cells from ischemic or hypoxic events. More precisely, this invention provides new combinatorial therapies that efficiently protect neuronal cells from ischemia or hypoxia.

Compositions and Methods for Localized Drug Delivery through Mammary Papillae

The invention provides compositions and methods for the prevention, diagnosis, or treatment of conditions affecting breast tissue. The compositions can include one or more therapeutic agents or diagnostic agents, and an effective carrier. The composition can be specifically adapted for transdermal permeation through the mammary papilla, areola, or a combination thereof, and into underlying breast tissue. 1. A composition for the prevention , diagnosis , or treatment of a condition affecting breast tissue comprising an alcoholic component , a therapeutic agent or a diagnostic agent , and an effective carrier , the composition being adapted for transdermal permeation through the mammary papilla , areola , or a combination thereof , and into underlying breast tissue , wherein said carrier is an extract of sandalwood oil.2. The composition of wherein the agent is chemopreventive agent claim 1 , a diagnostic agent claim 1 , or a chemotherapeutic agent.3. The composition of claim 1 , wherein the agent is hydrophilic agent claim 1 , a lipophilic agent claim 1 , or a macromolecular agent.4. The composition of any one of claims 1 , wherein the agent is 5-fluorouracil claims 1 , cyclophosphamide claims 1 , tamoxifen claims 1 , adriamycin claims 1 , danazol claims 1 , progesterone claims 1 , doxorubicin claims 1 , paclitaxel claims 1 , cisplatin claims 1 , docetaxel claims 1 , or a diagnostic agent.5. The composition of claim 1 , wherein the carrier is α-santalol.6. The composition of claim 1 , wherein the composition is substantially a microemulsion.7. The composition of claim 1 , wherein the composition is substantially a hydroalcoholic solution.8. The composition of claim 5 , wherein the composition comprises at least 5% α-santalol (v/v).9. The composition of claim 5 , wherein the composition comprises between about 5% to about 25% α-santalol (v/v).10. The composition of claim 1 , wherein the therapeutic agent or a diagnostic agent has a molecular weight of between about ...

METHODS AND MATERIALS FOR THE TREATMENT OF TESTOSTERONE DEFICIENCY IN MEN

The present invention relates to the use of compositions comprising trans-clomiphene for treating men with hypogonadism. The invention is also directed to methods for treating males with hypogonadism. 1. A method for treating a condition associated with testosterone deficiency in a human male , comprising administering to said male an effective amount of a composition consisting essentially of trans-clomiphene or pharmaceutically acceptable salts thereof and one optionally one or more pharmaceutically acceptable diluents , adjuvants , carriers or excipients , wherein the condition associated with testosterone deficiency is oligospermia of azoospermia.2. The method of claim 1 , wherein the trans-clomiphene is in a dosage of 1-200 mg per day.3. The method of claim 2 , wherein the trans-clomiphene is in a dosage of 50 mg per day.4. The method of wherein the trans-clomiphene is administered in a dosage of 1.5 mg/kg per day.5. The method of claim 1 , wherein the composition consists essentially of 12.5 mg of trans-clomiphene or a pharmaceutically acceptable salt thereof6. The method of claim 1 , wherein the composition is in the form of a filled capsule for oral use.7. The method of claim 1 , wherein the composition is in the form of a tablet for oral use.8. The method of claim 1 , wherein the human male is a human male with secondary hypogonadism. This application is a divisional of U.S. application Ser. No. 10/483,458, filed Jul. 2, 2004, which is the U.S. National Stage of International Application Number PCT/US02/21524, filed Jul. 9, 2002, and which claims the benefit of U.S. Provisional Patent Application No. 60/304,313, filed on Jul. 9, 2001, the contents of each of which is incorporated herein by reference in its entirety.The present invention relates to the compositions and methods for increasing testosterone levels. More specifically, the present invention relates to a composition comprising clomiphene enriched for trans-clomiphene. The present invention also ...

CENTRAL ADMINISTRATION OF STABLE FORMULATIONS OF THERAPEUTIC AGENTS FOR CNS CONDITIONS

The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS. 1. A method for treating a CNS-related condition or disorder in a subject in need thereof , the method comprising intracerebroventricularly administering to the subject a pharmaceutical composition comprising (i) a CNS therapeutic agent effective to treat the CNS-related condition or disorder and (ii) a solubility enhancing agent; wherein the solubility enhancing agent allows an effective amount of the CNS therapeutic agent to be intracerebroventricularly administered to the subject; and wherein the CNS therapeutic agent maintains solubility in the composition for at least two months at physiological temperature and pH.2. The method of claim 1 , wherein the CNS-related condition or disorder is selected from the group consisting of epilepsy claim 1 , schizophrenia claim 1 , closed head injury spectrum claim 1 , Alzheimer's disease spectrum claim 1 , sleep disorders spectrum claim 1 , depression claim 1 , anxiety spectrum claim 1 , bipolar disorder claim 1 , and multiple sclerosis.3. The method of claim 1 , wherein the pharmaceutical composition is chronically administered over at least two months via ...

METHODS AND APPARATUS FOR TREATING A WOUND

Methods for treating a wound or promote wound healing are provided, comprising the step of administering a composition including an effective amount of β-1 adrenergic receptor antagonist to a subject in need thereof. Also provided is apparatus for wound healing, comprising a dressing and a composition including an effective amount of β-1 adrenergic receptor antagonist. 1. A method for treating a deep fissure in a patient comprising the step of administering a composition comprising an effective amount of a β-1 adrenergic receptor antagonist to the patient in need thereof.2. The method of claim 1 , wherein said deep fissure is induced by targeted therapy.3. The method of claim 2 , wherein the β-1 adrenergic receptor antagonist is atenolol claim 2 , betaxolol claim 2 , bisoprolol claim 2 , esmolol claim 2 , acebutolol claim 2 , metoprolol claim 2 , nebivolol or any combination thereof.4. The method of claim 1 , wherein the β-1 adrenergic receptor antagonist is atenolol claim 1 , betaxolol claim 1 , bisoprolol claim 1 , esmolol claim 1 , acebutolol claim 1 , metoprolol claim 1 , nebivolol or any combination thereof.5. The method of claim 1 , further comprising administering an additional therapeutic agent for wound healing.6. The method of claim 5 , wherein the additional therapeutic agent for wound healing is growth factors claim 5 , cytokines claim 5 , chemokines claim 5 , antibodies claim 5 , antibiotics claim 5 , immunosuppressive agents claim 5 , steroids claim 5 , zinc claim 5 , hyperbaric oxygen claim 5 , anti-fungal agents claim 5 , anti-viral agents claim 5 , stem cells claim 5 , bioengineered skin claim 5 , debriding agents or any combination thereof. This application is a Divisional of U.S. patent application Ser. No. 16/234,867, filed Dec. 28, 2018, the entire disclosure of which is hereby incorporated by reference.Wound healing, initiated by whatever aetiology, is a dynamic process encompassing a number of overlapping phases, including inflammation, ...

Combinations of Oral Medicaments Bonded by a Wrapping

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

COMPOSITIONS FOR SMALL MOLECULE THERAPEUTIC AGENT COMPOUNDS

A composition comprising a small molecule therapeutic agent and an organic acid compound is described. The small molecule therapeutic agent (i) has a water solubility at room temperature of less than about 1.0 g/L and (ii) is a base. The organic acid is one that (i) has a water solubility at room temperature of between 0.1 and 10 or of less than about 20 g/L, (ii) has a molar mass of less than 500 grams per mole, and/or (iii) maintains a pH of the composition when hydrated in its environment of use of between 3.0-6.5 for a period of at least about 30 days. The organic acid, particularly when it is present in the composition in stoichiometric excess, improves solubility of the small molecule therapeutic agent to provide a composition that delivers the therapeutic agent for a sustained period of time. 1. A composition , comprising:a therapeutic agent that (i) has a water solubility at room temperature of less than 1.0 g/L and (ii) is an organic base, and an organic acid that (i) has a water solubility at room temperature between 0.1 and 10 g/L, (ii) has a molar mass of less than 500 grams per mole, (iii) is present in a stoichiometric (molar) excess relative to the therapeutic agent, and (iv) maintains a pH of the composition when hydrated to form a solution or a suspension in its environment of use of between 3.0-6.5 for a period of at least about 30 days, wherein the therapeutic agent is not risperidone, olanzapine, paliperidone, aripiprazole, brexpiprazole, or asenapine.2. The composition of claim 1 , wherein a saturated aqueous solution of the organic acid has a pH value approximately equal to or less than the pKa of the protonated therapeutic agent.3. The composition of claim 1 , wherein the organic acid is present in an amount approximately equal to or above its saturation concentration at the end of the period.4. The composition of claim 1 , wherein the organic acid is present in a stoichiometric excess of 105% to 1000% relative to the therapeutic agent.5. The ...

BUPROPION AS A MODULATOR OF DRUG ACTIVITY

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan. 1. A method of treating major depressive disorder , comprising administering a drug combination to a human being in need thereof , wherein the drug combination comprises:a bupropion, in an amount that is about 105 mg of bupropion hydrochloride, or a molar equivalent amount of a bupropion in the free base form or another salt form, wherein the bupropion is administered once a day for the first three days and twice a day thereafter for at least 11 days; anda dextromethorphan, in an amount that is about 45 mg of dextromethorphan hydrobromide, or a molar equivalent amount of a dextromethorphan in the free base form or another salt form, wherein the dextromethorphan is administered once a day for the first three days and twice a day thereafter for at least 11 days;wherein the human being is selected for being male; andwherein the human being experiences a greater reduction in Montgomery-Asberg Depression Rating Scale (MADRS) score after receiving the drug combination, as compared to what would be experienced from receiving the same amount of the bupropion alone.2. The method of claim 1 , wherein administering the drug combination of the bupropion and the dextromethorphan is more effective in treating major depressive disorder than administering the same amount of the dextromethorphan alone.3. The method of claim 1 , wherein the drug combination comprising about 105 mg of bupropion hydrochloride and about 45 mg of dextromethorphan hydrobromide is administered once a day for the first three days and twice a day thereafter for at least 11 days to the human being.4. The method of claim 3 , wherein administering the drug combination is more effective in treating major depressive disorder than ...

PARTICULATE DELIVERY SYSTEMS

The present invention provides particulate delivery systems comprising plurality of particles comprising fenugreek gum and at least one pharmaceutically acceptable excipient. The particulate delivery systems of the present invention are used for the delivery of therapeutic, immunologic or diagnostic agents, and the like. 131-. (canceled)32. A particulate delivery system comprising plurality of particles comprising fenugreek gum and at least one pharmaceutically acceptable excipient.33. The delivery system of claim 32 , wherein the particles are of nanoscale or microscale size.34. The delivery system of claim 32 , wherein the particles are of a size of about 0.1 nm to about 1000 μm.35. The delivery system of claim 32 , wherein the particles are in the form of nanoparticles claim 32 , nanospheres claim 32 , nanocapsules claim 32 , microparticles claim 32 , microspheres claim 32 , microcapsules claim 32 , liposomes claim 32 , nanoemulsions claim 32 , solid lipid nanoparticles claim 32 , or mixtures thereof.36. The delivery system of claim 35 , wherein the particles are in the form of nanoparticles claim 35 , nanospheres claim 35 , microparticles claim 35 , microspheres claim 35 , or mixtures thereof.37. The delivery system of claim 32 , wherein the fenugreek gum comprises not less than about 15% by weight of galactomannan.38. The delivery system of claim 32 , wherein the fenugreek gum comprises not less than about 15% by weight of galactomannan claim 32 , not more than about 80% by weight of insoluble fibers and not more than about 5% by weight of proteins.39. The delivery system of claim 32 , wherein the pharmaceutically acceptable excipient is a surfactant claim 32 , a synthetic polymer claim 32 , a natural polymer claim 32 , a surface modifier claim 32 , a crosslinking agent claim 32 , solvent claim 32 , a complexing agent claim 32 , a lipid claim 32 , a pH modifier or a mixture thereof.40. The delivery system of claim 39 , wherein the synthetic polymer is selected ...

BUPROPION AS A MODULATOR OF DRUG ACTIVITY

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan. 1. A method of enhancing dextromethorphan plasma levels in a human being , comprising co-administering a bupropion with a dextromethorphan , to the human being , twice daily for at least eight consecutive days , wherein the human being is an extensive metabolizer of dextromethorphan in need of treatment with dextromethorphan , wherein the weight ratio of the dextromethorphan to the bupropion is about 0.4 to about 0.7 , wherein , on the eighth day that the bupropion and the dextromethorphan are co-administered , the AUCof dextromethorphan is at least about 15 times the AUCof dextromethorphan that would result from administering the same amount of the dextromethorphan twice daily without the bupropion for eight consecutive days , and wherein the AUCof dextromethorphan is at least about 800 ng·hr/mL.2. The method of claim 1 , wherein the bupropion and the dextromethorphan are administered in a single dosage form.3. The method of claim 2 , wherein the single dosage form is a solid.4. The method of claim 2 , wherein about 40 mg to about 50 mg of the dextromethorphan is administered in the single dosage form.5. The method of claim 2 , wherein about 30 mg to about 40 mg of the dextromethorphan is administered in the single dosage form.6. The method of claim 2 , wherein about 30 mg to about 60 mg of the dextromethorphan is administered in the single dosage form.7. The method of claim 2 , wherein a daily dose of about 150 mg to about 200 mg of the bupropion is administered.8. The method of claim 2 , wherein a daily dose of about 200 mg to about 250 mg of the bupropion is administered.9. The method of claim 1 , wherein the weight ratio of the dextromethorphan to the bupropion is about 0.4 to ...

COMPOSITIONS, METHODS & SYSTEMS FOR RESPIRATORY DELIVERY OF TWO OR MORE ACTIVE AGENTS

Compositions, methods and systems are provided for pulmonary or nasal delivery of two or more active agents via a metered dose inhaler. In one embodiment, the compositions include a suspension medium, active agent particles, and suspending particles, in which the active agent particles and suspending particles form a co-suspension within the suspension medium. 161.-. (canceled)62. A pharmaceutical composition deliverable from a metered dose inhaler , the composition comprising:a suspension medium comprising a pharmaceutically acceptable propellant;one or more species of respirable active agent particles comprising two or more active agents; anda plurality of respirable suspending particles different than the active agent particles and comprising a particulate phospholipid material that is substantially insoluble in the suspension medium, wherein the active agent particles and suspending particles are included in the suspension medium at a weight ratio of total mass of the suspending particles to total mass of the one or more species of active agent particles that ranges from above 1:1 and up to 200:1.63. The pharmaceutical composition of claim 62 , wherein the two or more active agents are selected from short-acting beta agonist claim 62 , long-acting and ultra long-acting βadrenergic receptor agonist (LABA) claim 62 , corticosteroid claim 62 , anti-inflammatory claim 62 , anti-tussive claim 62 , bronchodilator claim 62 , muscarinic antagonist claim 62 , and long-acting muscarinic antagonist (LAMA) active agents claim 62 , including any pharmaceutically acceptable salts claim 62 , esters claim 62 , or isomers thereof64. The pharmaceutical composition of claim 63 , wherein the one or more species of respirable active agent particles comprises two or more different species of respirable active agent particles claim 63 , each of the two or more different species of respirable active agent particles comprises a different active agent claim 63 , and the different active ...

DRUG COMBINATION PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USING THEM

The invention provides preparations, formulations, kits and other products of manufacture (e.g., blister packs) comprising combinations of beneficial ingredients that are serviceable as therapies for improving states and disease symptoms such as involving inflammation, excessive sympathoneural drive, cachexia, anorexia, and anorexia-cachexia, as well as stress or anxiety related thereto, and methods of making and using them. The invention provides compositions and therapies comprising use of a beta adrenergic antagonist (also called “beta blockers”, e.g., propranolol) in combination with an anti-inflammatory agent, e.g., a nonsteroidal anti-inflammatory drug (NSAID), an angiotensin-converting enzyme (ACE) inhibitor, an angiotensin receptor blocker (ARB), an anabolic steroid, a natural oil or fatty acid or any combination thereof. 135-. (canceled)37: The method of claim 36 , wherein the condition or disease comprises a maladaptive nutritional state secondary to the SIRS; anorexia; insulin resistance; anxiety; sleep disturbances; weakness; fatigue; lethargy; depression; malaise; or any combination thereof.38: The method of claim 36 , wherein the maladaptive nutritional state comprises cachexia or anorexia.39: The method of claim 38 , wherein the cachexia comprises cachexia secondary to cancer.40: The method of claim 38 , wherein the cachexia is defined as at least two of the symptoms selected from the group consisting of: 1) a hyper-inflammatory state claim 38 , 2) altered hormone levels and cytokine levels; 3) increased heart rate variability; 4) weight loss claim 38 , and 5) increased heart rate claim 38 , wherein optionally the increased heart rate is having a sustained elevated heart rate of at least about 6 bpm.4160-. (canceled)61: The method of claim 36 , wherein the therapeutic combination or the pharmaceutical composition further comprises a nutritional supplement.62: The method of claim 36 , wherein the member of the first drug group and member of the second ...

INHIBITORS OF THE FKBP51 PROTEIN FROM A HIGH-THROUGHPUT DRUG SCREEN AND METHODS OF USE

The subject invention concerns materials and methods for treating depression, stress disorders, such as PTSD, anxiety disorders, and/or a neurodegenerative disease or condition in a person or animal. In one embodiment, a person or animal in need of treatment is administered one or more compounds or drugs, or a composition comprising the one or more compounds or drugs, that inhibit FKBP51 activity or function. The subject invention also concerns a method for inhibiting activity of the FKBP51 protein in a cell. The subject invention also concerns methods of screening for compounds or drugs that inhibit the FKBP51 protein. 1. A method for treating a person or animal having a neurodegenerative disease or condition , or depression , a stress disorder , and/or an anxiety disorder , the method comprising administering to the person or animal a therapeutically effective amount of one or more compounds or drugs , or a composition comprising said one or more compounds or drugs , that inhibits FKBP51 activity or function.2. The method according to claim 1 , wherein the person or animal exhibits increased levels of FKBP51 protein relative to a control.3. The method according to claim 1 , wherein the compound or drug is one that lessens or attenuates the suppressive effect of FKBP51 on glucocorticoid receptor (GR) activity.4. The method according to claim 1 , wherein the compound or drug is benztropine claim 1 , clonidine claim 1 , pimozide claim 1 , thioridazine claim 1 , trifluoperazine claim 1 , or triflupromazine claim 1 , or a pharmaceutically or physiologically acceptable salt thereof.5. The method according to claim 1 , wherein the person or animal exhibits one or more single nucleotide polymorphisms (SNPs) in the FKBP5 gene claim 1 , and wherein said one or more SNPs are associated with elevated levels of FKBP51 protein.6. The method according to claim 1 , wherein said compound or drug is provided in the form of a pharmaceutically or physiologically acceptable salt.7. ...

BUPROPION AS A MODULATOR OF DRUG ACTIVITY

Dosage forms, drug delivery systems, and methods related to sustained release of dextromethorphan or improved therapeutic effects are disclosed. Typically, bupropion or a related compound is orally administered to a human being to be treated with, or being treated with, dextromethorphan. 1. A method , comprising orally administering a dosage form to a human being twice daily for at least eight consecutive days , wherein the dosage form comprises a bupropion and a dextromethorphan , wherein the human being is an extensive metabolizer of dextromethorphan in need of treatment with dextromethorphan , and wherein on the eighth day that the dosage form is administered twice daily , the method results in a Cof dextromethorphan , that is: 1) at least about 40 ng/mL , and 2) at least about 15 times the Cof dextromethorphan that would be achieved by administering the same amount of the dextromethorphan without the bupropion twice daily for eight consecutive days.2. The method of claim 1 , wherein the dosage form is a solid.3. The method of claim 2 , wherein the solid oral dosage form further comprises a binder.4. The method of claim 2 , wherein the solid oral dosage form further comprises a disintegrating agent.5. The method of claim 2 , wherein the solid oral dosage form further comprises a lubricant.6. The method of claim 1 , wherein the dosage form is effective for immediate release of the dextromethorphan.7. The method of claim 1 , wherein the dosage form is effective for sustained release of the bupropion.8. The method of claim 1 , wherein the Cof dextromethorphan on the eighth day that the dosage form is administered twice daily is about 45 ng/mL to about 70 ng/mL.9. The method of claim 1 , wherein the Cof dextromethorphan on the eighth day that the dosage form is administered twice daily is about 50 ng/mL to about 60 ng/mL.10. The method of claim 1 , wherein the AUCof dextromethorphan on the eighth day that the dosage form is administered twice daily is about 400 ng·hr ...

COMPOSITIONS AND METHODS FOR TREATING PARKINSON'S DISEASE

Described herein are methods for treating a subject having or at risk of developing Parkinson's disease, by administering pluripotent cells that express glucocerebrosidase (GBA) or pluripotent cells that express GBA and one or more M2-promoting agents to the subject. Also disclosed are compositions comprising pluripotent cells expressing GBA, such as pluripotent cells expressing GBA and one or more M2-promoting agents. 1. A method of treating Parkinson's disease in a subject , the method comprising administering to the subject a composition comprising a population of pluripotent cells that express a transgene encoding glucocerebrosidase (GBA).2. The method of claim 1 , wherein the GBA is full-length GBA.3. The method of claim 1 , wherein the GBA is a catalytic domain of GBA.4. The method of any one of - claim 1 , wherein the GBA has an amino acid sequence that is at least 85% identical to the amino acid sequence of SEQ ID NO. 1.5. The method of claim 4 , wherein the GBA has an amino acid sequence that is at least 90% identical to the amino acid sequence of SEQ ID NO. 1.6. The method of claim 5 , wherein the GBA has an amino acid sequence that is at least 95% identical to the amino acid sequence of SEQ ID NO. 1.7. The method of claim 6 , wherein the GBA has an amino acid sequence that is at least 95% identical to the amino acid sequence of SEQ ID NO. 1.8. The method of any one of - claim 6 , wherein the GBA has an amino acid sequence that is at least 85% identical to the amino acid sequence of SEQ ID NO. 5.9. The method of claim 8 , wherein the GBA has an amino acid sequence that is at least 90% identical to the amino acid sequence of SEQ ID NO. 5.10. The method of claim 9 , wherein the GBA has an amino acid sequence that is at least 95% identical to the amino acid sequence of SEQ ID NO. 5.11. The method of claim 10 , wherein the GBA has the amino acid sequence of SEQ ID NO. 5.12. The method of any one of - claim 10 , wherein the transgene encoding GBA has a nucleic ...

CANCER VACCINE COMPOSITIONS AND METHODS OF USE THEREOF

The disclosure provides a cancer vaccine composition comprising inactivated cancer cells and an adjuvant, wherein the inactivated cancer cells are incapable of replication. Also provided is a method for producing a cancer vaccine composition, the method comprising contacting cancer cells with light (e.g., UV light) in the presence of a photosensitizer (e.g., riboflavin). 1. A cancer vaccine composition , the composition comprising inactivated cancer cells , wherein the inactivated cancer cells are incapable of replication.2. The cancer vaccine composition of claim 1 , wherein the cancer cells are from a patient suffering from one or more types of cancer.3. The cancer vaccine composition of claim 2 , wherein the patent is suffering from one or more of breast cancer claim 2 , lung cancer claim 2 , liver cancer claim 2 , bladder cancer claim 2 , gynecological cancer claim 2 , brain cancer claim 2 , stomach cancer claim 2 , prostate cancer claim 2 , skin cancer claim 2 , thyroid cancer claim 2 , pancreatic cancer claim 2 , colon cancer claim 2 , and blood cancer.4. The cancer vaccine composition of claim 3 , wherein the skin cancer is a melanoma.5. The cancer vaccine composition of claim 3 , wherein the blood cancer is a leukemia claim 3 , a lymphoma claim 3 , or a myeloma.6. The cancer vaccine composition of claim 5 , wherein the leukemia is Acute Lymphocytic Leukemia or Acute Myeloid Leukemia.7. The cancer vaccine composition of claim 5 , wherein the lymphoma is Hodgkin's Lymphoma or Non-Hodgkin's Lymphoma.8. The cancer vaccine composition of claim 5 , wherein the myeloma is multiple myeloma.9. The cancer vaccine composition of claim 2 , wherein the patent is suffering from a benign tumor.10. The cancer vaccine composition of claim 2 , wherein the cancer is metastatic cancer.11. The cancer vaccine composition of any one of - claim 2 , wherein the cancer cells are derived from an immortalized cell line.12. The cancer vaccine composition of any one of to claim 2 , ...

METHODS FOR TREATING OR PREVENTING ASTHMA BY ADMINISTERING AN IL-33 ANTAGONIST

The invention provides methods for treating or preventing asthma and associated conditions in a patient. The methods featured in the invention comprise administering to a subject in need thereof a therapeutic composition comprising an interleukin-33 (IL-33) antagonist, such as an anti-IL-33 antibody. The methods featured in the invention further comprise administering to a subject in need thereof a first therapeutic composition comprising an interleukin-33 (IL-33) antagonist, such as an anti-IL-33 antibody, and a second therapeutic composition comprising an interleukin-4 receptor (IL-4R) antagonist, such as an anti-IL-4R antibody. 1. A method for treating asthma in a subject in need thereof comprising administering to the subject:an initial dose of about 300 mg of a first antibody or antigen-binding fragment thereof that specifically binds interleukin-33 (IL-33) and comprises three heavy chain complementary determining region (HCDR) sequences comprising SEQ ID NOs: 4, 5 and 6, and three light chain complementary determining region (LCDR) sequences comprising SEQ ID NOs: 12, 14 and 16; andone or more maintenance doses of about 300 mg of the antibody or antigen-binding fragment thereof, and optionally administering to the subject:an initial dose of about 300 mg of a second antibody or antigen-binding fragment thereof that specifically binds interleukin-4 receptor (IL-4R) and comprises three heavy chain complementary determining region (HCDR) sequences comprising SEQ ID NOs: 21, 22 and 23, and three light chain complementary determining region (LCDR) sequences comprising SEQ ID NOs: 24, 25 and 26; andone or more maintenance doses of about 300 mg of the second antibody or antigen-binding fragment thereof.2. The method of claim 1 , wherein:(a) loss of asthma control (LOAC) is reduced in the subject; optionally selected from the group consisting of forced expiratory volume in 1 second (FEV1), peak expiratory flow (PEF), forced vital capacity (FVC), forced expiratory flow ...

CENTRAL ADMINISTRATION OF STABLE FORMULATIONS OF THERAPEUTIC AGENTS FOR CNS CONDITIONS

The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS. 1. A pharmaceutical composition comprising a central nervous system (CNS) therapeutic agent and a solubility enhancing agent , wherein the CNS therapeutic agent maintains solubility in said composition for at least two months at physiological temperature and pH.2. The pharmaceutical composition of claim 1 , wherein the CNS therapeutic agent is active in the treatment of a CNS condition or disorder selected from the group consisting of epilepsy claim 1 , schizophrenia claim 1 , Closed Head Injury Spectrum claim 1 , Alzheimer's Spectrum claim 1 , sleep disorders spectrum claim 1 , depression claim 1 , anxiety spectrum claim 1 , bipolar disorder and multiple sclerosis.3. The pharmaceutical composition of claim 1 , wherein the CNS therapeutic agent is active in the treatment of epilepsy.4. The pharmaceutical composition of claim 3 , wherein the CNS therapeutic agent is an anti-epilepsy agent that acts on the GABA system claim 3 , a Sodium Channel claim 3 , and/or a Calcium Channel.5. The pharmaceutical composition of claim 3 , wherein the CNS therapeutic agent is selected from the group consisting of: ...

GLYCOPROTEINS HAVING LIPID MOBILIZING PROPERTIES AND THERAPEUTIC USES THEREOF

The invention provides formulations and methods for ameliorating symptoms associated with metabolic disorders, such as cachexia, hypoglycemia, obesity, diabetes, and the like by administering Zn-α-glycoproteins or a functional fragment thereof, alone or in combination with additional agents, such as β adrenergin receptor agonists, β adrenergin receptor antagonists, and/or glycemic control agents. 1. A formulation comprising a zinc-α-glycoprotein (ZAG) , a ZAG variant , a modified ZAG , or a functional fragment thereof.2. The formulation of claim 1 , wherein the ZAG is mammalian.3. The formulation of claim 2 , wherein the ZAG is human.4. The formulation of claim 3 , wherein the ZAG consists of the amino acid sequence set forth in SEQ ID NO: 1.5. The formulation of claim 4 , wherein the ZAG is conjugated to a non-protein polymer.6. The formulation of claim 5 , wherein the ZAG is sialylated claim 5 , PEGylated or modified to increase solubility or stability.7. The formulation of claim 1 , wherein the ZAG is recombinant or synthetic.8. The formulation of claim 1 , wherein the modified ZAG consists of the wild-type ZAG amino acid sequence with one or more mutations to the amino acid sequence selected from deletions claim 1 , additions or conservative substitutions.9. The formulation of claim 5 , wherein the ZAG is glycosylated.10. The formulation of claim 1 , wherein the formulation comprises at least 5 claim 1 , 10 claim 1 , 25 claim 1 , 50 claim 1 , 100 mg of ZAG.11. The formulation of claim 1 , further comprising one or more agents selected from the group consisting of a β3 agonist and β-adrenergic receptor (β-AR) antagonist.12. The formulation of claim 11 , wherein the β-AR antagonist is selected from the group consisting of a β2-adrenergic receptor (β2-AR) antagonist claim 11 , a β1-adrenergic receptor (β1-AR) antagonist claim 11 , and a β3-adrenergic receptor (β3-AR) antagonist.13. The formulation of claim 11 , wherein the β3 agonist is selected from the group ...

RESPIRABLY DRY POWDER COMPRISING CALCIUM LACTATE, SODIUM CHLORIDE AND LEUCINE

The present invention relates to respirable dry powders that contain respirable dry particles that comprise about 20%-37.5% (w/w) leucine, about 58.6-about 75% (w/w) calcium lactate, and about 3.9-about 5% (w/w) sodium chloride, and methods for treating a subject using the respirable dry powders. 134-. (canceled)35. A respirable dry powder , comprising:respirable dry particles that comprise calcium lactate, sodium chloride, leucine, and one or more additional therapeutic agents;wherein the ratio of calcium cation to sodium cation is about 4:1 (mole:mole); and,wherein the calcium lactate is about 58.6% (w/w) to about 75% (w/w), and the sodium chloride is about 3.9% (w/w) to about 5% (w/w), and the leucine is about 20% (w/w) to about 37.5% (w/w), where all weights are on a dry basis.36. The respirable dry powder of claim 35 , wherein the one or more additional therapeutic agents are selected from group consisting of corticosteroids and bronchodilators claim 35 , and wherein said bronchodilators are one or more bronchodilators selected from the group consisting of long-acting betaagonists and long-acting muscarinic anagonists.37. The respirable dry powder of claim 36 , wherein said long-acting betaagonists are selected from the group consisting of salmeterol claim 36 , formoterol claim 36 , arformoterol claim 36 , clenbuterol claim 36 , tulobuterol claim 36 , vilanterol claim 36 , indacaterol claim 36 , carmoterol claim 36 , isoproterenol claim 36 , procaterol claim 36 , bambuterol claim 36 , and milveterol.38. The respirable dry powder of claim 36 , wherein the long-acting muscarinic anagonists are selected from the group consisting of tiotroprium claim 36 , trospium chloride claim 36 , glycopyrrolate claim 36 , aclidinium claim 36 , and ipratropium.39. The respirable dry powder of claim 36 , wherein the corticosteroids are selected from the group consisting of budesonide claim 36 , fluticasone claim 36 , flunisolide claim 36 , triamcinolone claim 36 , beclomethasone ...

TREATMENT AND PREVENTION OF GLIOBLASTOMA

The invention relates to the use of a selective βadrenergic receptor antagonist for treating glioma. In particular, the invention relates to the use of an alkanolamine derivative or a pharmaceutically acceptable acid-addition salt thereof for treating a glioblastoma in a patient. 118-. (canceled)19. A method of treatment and/or prevention of glioma in a patient comprising administering to said patient a therapeutically effective amount of a selective antagonist of the β-adrenergic receptor.20. The method according to claim 19 , wherein the glioma is characterized by having increased expression of the β-adrenergic receptor compared to a reference value.22. The method according to claim 19 , wherein the antagonist is administered together with an antitumor compound selected from temozolomide claim 19 , leptomycin B claim 19 , capecitabine and an alkylating claim 19 , intercalating or DNA damaging agent.23. The method according to claim 22 , wherein the antitumor compound is propranolol.24. The method according to claim 19 , wherein the glioma comprises a subpopulation of cancer stem cells.25. The method according to claim 19 , wherein the glioma is a high-grade glioma.26. The method according to claim 19 , wherein the glioma is a non-recurrent glioma.27. The method according to claim 19 , wherein the glioma is astrocytoma.28. The method according to claim 27 , wherein the astrocytoma is glioblastoma.29. The method according to claim 19 , wherein n is 1.30. The method according to claim 19 , wherein Ris isopropyl claim 19 , Ris methyl and/or Ris methyl.32. The method according to claim 21 , wherein the pharmaceutically acceptable acid-addition salt is hydrochloride.33. The method according to claim 19 , wherein the alkanolamine derivative or pharmaceutically acceptable acid-addition salt thereof is administered at a dose between 1 mg/Kg body/day and 4.5 mg/kg body/day.34. The method according to claim 33 , wherein the alkanolamine derivative or pharmaceutically ...

Methods for treating cancer in models harboring esr1 mutations

Disclosed herein are methods of treating a drug resistant estrogen receptor alpha-positive cancer in a subject having a mutant estrogen receptor alpha, the method comprising administering to the subject a therapeutically effective amount of elacestrant, or a pharmaceutically acceptable salt or solvate thereof, wherein the mutant estrogen receptor alpha comprises one or more mutations selected from the group consisting of D538G, Y537X1, L536X2, P535H, V534E, S463P, V392I, E380Q and combinations thereof, wherein: X1 is S, N, or C; and X2 is R or Q. In some embodiments, the drug resistant estrogen receptor alpha-positive cancer is selected from the group consisting of breast cancer, uterine cancer, ovarian cancer, and pituitary cancer.

Pharmaceutical Compositions For Combination Therapy

This invention relates to the use of pharmaceutical compositions comprising a therapeutically effective combination of Tesofensine and Metoprolol for preventing the cardiovascular side effects of Tesofensine, while leaving the robust inhibitory efficacy on food intake and body weight loss unaffected. 1. A method of inducing hypophagia in a human comprising:administering 0.1 mg to 1 mg of Tesofensine, or a pharmaceutically acceptable salt thereof, to the human, daily;in combination with 25 mg to 200 mg of Metoprolol, or a pharmaceutically acceptable salt thereof, daily,wherein the combination is effective in inducing hypophagia and wherein the combination is effective in preventing or alleviating drug-induced cardiovascular side-effects.2. The method of claim 1 , wherein the Tesofensine claim 1 , or pharmaceutically acceptable salt thereof claim 1 , is administered at a dosage of 0.1 mg to about 0.5 mg daily claim 1 , based on the amount of free base.3. The method of claim 1 , wherein the Metoprolol claim 1 , or pharmaceutically acceptable salt thereof claim 1 , is administered at a dosage of 25 mg to 100 mg daily claim 1 , based on the amount of free base.4. The method of claim 1 , wherein the human is a pre-obese human claim 1 , an obese human claim 1 , or a morbidly obese human.5. The method of claim 1 , wherein the human suffers from over-eating disorders claim 1 , bulimia nervosa claim 1 , binge eating disorder claim 1 , compulsive over-eating claim 1 , impaired appetite regulation claim 1 , metabolic syndrome claim 1 , type 2 diabetes claim 1 , dyslipidemia claim 1 , atherosclerosis claim 1 , or drug-induced obesity.6. The method of claim 1 , wherein the human suffers from an over-eating disorder claim 1 , bulimia nervosa claim 1 , binge eating disorder claim 1 , or compulsive over-eating.7. The method of claim 1 , wherein the drug-induced cardiovascular side effects are increased heart rate claim 1 , increased diastolic blood pressure claim 1 , or increased ...

UNIT ORAL DOSE COMPOSITIONS COMPOSED OF IBUPROFEN AND FAMOTIDINE FOR THE TREATMENT OF ACUTE PAIN AND THE REDUCTION OF THE SEVERITY AND/OR RISK OF HEARTBURN

Described herein are unit oral dose compositions that reduce the severity of heartburn and/or the risk of the occurrence of heartburn in a human in need of taking ibuprofen for the OTC treatment of acute pain wherein the human is not experiencing heartburn prior to the oral administration of the unit oral dose composition comprising orally administering to the human of a unit oral dose composition comprising (i) ibuprofen at a dosage from about 50 mg to about 400 mg per unit oral dose composition and (ii) famotidine at a dosage from about 3 mg to about 20 mg per unit oral dose composition, wherein the dissolution rate of famotidine in the unit oral dose composition in said human at a specified time within 45 minutes of administration of said unit oral dose composition to said human is greater than the dissolution rate of ibuprofen in the unit oral dose composition in said human at the same specified time. 1. A method for reducing the severity of heartburn and/or the risk of the occurrence of heartburn in a human in need of taking ibuprofen for the treatment of acute pain wherein the human is not experiencing heartburn prior to the oral administration of the unit oral dose composition comprising orally administering to the human of a unit oral dose composition comprising (i) ibuprofen at a dosage from about 50 mg to about 400 mg per unit oral dose composition and (ii) famotidine at a dosage from about 3 mg to about 20 mg per unit oral dose composition ,wherein the dissolution rate of famotidine in the unit oral dose composition in said human at a specified time within 45 minutes of administration of said unit oral dose composition to said human is greater than the dissolution rate of ibuprofen in the unit oral dose composition in said human at the same specified time.2. The method of claim 1 , wherein the famotidine in the unit oral dose composition has a dissolution rate that is about 10% to about 30% greater than the dissolution rate of ibuprofen at about 5 minutes ...

Methods of treating depression, anxiety and sexual dysfunction using the compound pimavanserin

The disclosure provides, in part, a method of treating anxious distress with major depressive disorder in a patient in need thereof, comprising administering to the patient N-(4-fluorophenylmethyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide or a pharmaceutically acceptable salt thereof. Also provided herein is a method of treating depression in a patient in need thereof, wherein the patient is also suffering from Parkinson's disease, comprising orally administering to the patient 34 mg of N-(4-fluorophenylmethyl)-N-1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide once daily, as well as methods for the treatment of a SSRI or SNRI-induced sexual dysfunction in a human subject.

PHARMACEUTICAL COMPOSITIONS FOR COMBINATION THERAPY

This invention relates to the use of pharmaceutical compositions comprising a therapeutically effective combination of Tesofensine and Metoprolol for preventing the cardiovascular side effects of Tesofensine, while leaving the robust inhibitory efficacy on food intake and body weight loss unaffected. 1. A method of treating type 2 diabetes in a human comprising:administering Tesofensine, or a pharmaceutically acceptable salt thereof, to the human;in combination with Metoprolol, or a pharmaceutically acceptable salt thereof,wherein the combination is effective in treating the type 2 diabetes and wherein the combination is effective in preventing or alleviating drug-induced cardiovascular side-effects.2. The method of claim 1 , wherein 0.1 mg to 1 mg of Tesofensine is administered daily daily.3. The method of claim 1 , wherein 0.1 mg to about 0.5 mg of Tesofensine is administered daily daily.4. The method of claim 1 , wherein 0.25 mg to 200 mg of the Metoprolol is administered daily.5. The method of claim 1 , wherein 25 mg to 100 mg of the Metoprolol is administered daily.6. The method of claim 1 , wherein the human is a pre-obese human claim 1 , an obese human claim 1 , or a morbid obese human.7. The method of claim 1 , wherein the drug-induced cardiovascular side effects are increased heart rate claim 1 , increased diastolic blood pressure claim 1 , or increased systolic blood pressure claim 1 , or a combination thereof.8. A method of treating metabolic syndrome in a human comprising:administering Tesofensine, or a pharmaceutically acceptable salt thereof, to the human;in combination with Metoprolol, or a pharmaceutically acceptable salt thereof,wherein the combination is effective in treating the metabolic syndrome and wherein the combination is effective in preventing or alleviating drug-induced cardiovascular side-effects.9. The method of claim 8 , wherein 0.1 mg to 1 mg of the Tesofensine is administered daily daily.10. The method of claim 8 , wherein 0.1 mg to ...

HYDROXYBUPROPION AND RELATED COMPOUNDS AS MODULATORS OF DRUG PLASMA LEVELS

This disclosure relates to methods administering bupropion in conjunction with dextromethorphan to a human being. Dosage forms, drug delivery systems, and methods related to dextromethorphan or dextrorphan and bupropion are also disclosed. 1. A method of decreasing seizure risk associated with use of a bupropion comprising co-administering to a human being the bupropion with a dextromethorphan once or twice daily for at least four weeks; wherein co-administering the bupropion with the dextromethorphan results in a decreased risk of seizure while maintaining efficacy as compared administering 150 mg of the bupropion twice daily for at least four weeks without the dextromethorphan.2. The method of claim 1 , wherein the combination is administered twice a day.3. The method of claim 1 , wherein at least about 40 mg of the dextromethorphan is administered twice a day.4. The method of claim 1 , wherein about 50 mg to about 140 mg of the bupropion is administered twice a day.5. The method of claim 1 , wherein 44 mg to 46 mg of the dextromethorphan is administered twice a day.6. The method of claim 1 , wherein 100 mg to about 105 mg of the bupropion is administered twice a day.7. The method of claim 3 , wherein 100 mg to about 105 mg of the bupropion is administered twice a day.8. The method of claim 2 , wherein the dextromethorphan Con the eighth day that the combination is administered claim 2 , is at least about 40 ng/mL.9. The method of claim 1 , wherein the Cof the dextromethorphan on the eighth day is about 45 ng/mL to about 50 ng/mL.10. The method of claim 1 , wherein the Cof the dextromethorphan on the eighth day is about 50 ng/mL to about 60 ng/mL.11. The method of claim 1 , wherein the Cof the dextromethorphan on the eighth day is about 60 ng/mL to about 70 ng/mL.12. The method of claim 1 , wherein the Cof the dextromethorphan on the eighth day is about 70 ng/mL to about 90 ng/mL.13. The method of claim 7 , wherein the Cof the dextromethorphan on the eighth day is ...

COMPOSITIONS FOR AFFECTING WEIGHT LOSS

Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity. 1. A composition for affecting weight loss comprising a first compound and a second compound , wherein said first compound is an opioid antagonist and said second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions.2. The composition of claim 1 , wherein said opioid antagonist antagonizes an opioid receptor selected from a μ-opioid receptor (MOP-R) claim 1 , a κ-opioid receptor claim 1 , and a δ-opioid receptor.3. The composition of claim 1 , wherein said opioid antagonist is selected from the group consisting of alvimopan claim 1 , norbinaltorphimine claim 1 , nalmefene claim 1 , naloxone claim 1 , naltrexone claim 1 , methylnaltrexone claim 1 , and nalorphine claim 1 , and pharmaceutically acceptable salts or prodrugs thereof.4. The composition of claim 1 , wherein said second compound triggers the release of α-melanocyte stimulating hormone (α-MSH).5. The composition of claim 4 , wherein said second compound increases the extracellular serotonin concentrations in the hypothalamus.6. The composition of claim 5 , wherein said second compound is selected from the group consisting of a selective serotonin reuptake inhibitor (S SRI) claim 5 , a serotonin 2C agonist claim 5 , and a serotonin 1B agonist.7. The composition of claim 6 , wherein ...

Transdermal Drug Delivery Using Amphiphilic Dendron-Coil Micelles

The invention generally relates to the field of drug delivery. In particular, the invention relates to amphiphilic dendron-coils, micelles thereof and their use for the transdermal delivery of drugs. 1. A method of transdermal delivery of a drug to a patient comprising administering to the patient a topical composition comprising a micelle and a pharmaceutically acceptable excipient ,wherein the drug has a molecular weight over 500 g/mol, a 1-octanol/PBS partition coefficient (log P) less than 1 or greater than 3, or both, andwherein the micelle comprises amphiphilic dendron-coils and encapsulates the drug, andwherein each amphiphilic dendron-coil comprises a hydrophobic core-forming block, a polyester dendron and a poly(ethylene) glycol (PEG) moiety.2. The method of wherein the hydrophobic core-forming block comprises polycaprolactone (PCL) claim 1 , poly(lactic acid) (PLA) claim 1 , poly(glycolic acid) (PGA) or poly(lactic-co-glycolic acid) (PLGA); wherein the polyester dendron is a generation 3 to generation 5 polyester dendron with either an acetylene or carboxylate core; and wherein the PEG moiety is a methoxy PEG (mPEG) moiety claim 1 , amine-terminated PEG (PEG-NH) moiety claim 1 , acetylated PEG (PEG-Ac) moiety claim 1 , carboxylated PEG (PEG-COOH) moiety claim 1 , thiol-terminated PEG (PEG-SH) moiety claim 1 , N-hydroxysuccinimide-actived PEG (PEG-NHS) moiety claim 1 , NH-PEG-NHmoiety or NH-PEG-COOH moiety.3. The method of wherein the hydrophobic core-forming block comprises polycaprolactone (PCL) claim 2 , poly(lactic acid) (PLA) claim 2 , poly(glycolic acid) (PGA) or poly(lactic-co-glycolic acid) (PLGA).4. The method of wherein the hydrophobic core-forming block comprises PCL.5. The method of wherein the hydrophobic core-forming block comprises PLA.6. The method of wherein the hydrophobic core-forming block comprises PGA.7. The method of wherein the hydrophobic core-forming block comprises PLG.8. The method of wherein the PCL is poly(ε-caprolactone).9. ...

BUPROPION AS A MODULATOR OF DRUG ACTIVITY

This disclosure relates to methods administering bupropion or a prodrug thereof in conjunction with dextromethorphan to a human being. Dosage forms, drug delivery systems, and methods related to dextromethorphan or dextrorphan and bupropion or a prodrug of bupropion are also disclosed 1. A method of increasing dextromethorphan plasma levels in a human being , comprising co-administering bupropion with about 40 mg per day to about 500 mg per day of dextromethorphan to the human being , wherein the human being is an extensive metabolizer of dextromethorphan in need of treatment with dextromethorphan , wherein bupropion and dextromethorphan are co-administered once or twice a day , and wherein on the eighth day that bupropion and dextromethorphan are co-administered , the co-administration results in an AUCof dextromethorphan that is at least about 20 times the AUCthat would be achieved by administering the same amount of dextromethorphan without bupropion for eight consecutive days.2. The method of claim 1 , wherein the AUCof dextromethorphan claim 1 , on the eighth day that bupropion and dextromethorphan are co-administered claim 1 , is at least about 500 ng·hr/mL.3. The method of claim 1 , wherein the AUCof dextromethorphan claim 1 , on the eighth day that bupropion and dextromethorphan are co-administered claim 1 , is about 800 ng·hr/mL to about 900 ng·hr/mL.4. The method of claim 1 , wherein the AUCof dextromethorphan claim 1 , on the eighth day that bupropion and dextromethorphan are co-administered claim 1 , is at least about 600 ng·hr/mL.5. The method of claim 1 , wherein the AUCof dextromethorphan claim 1 , on the eighth day that bupropion and dextromethorphan are co-administered claim 1 , is at least about 1000 ng·hr/mL.6. The method of claim 1 , wherein the AUCof dextromethorphan claim 1 , on the eighth day that bupropion and dextromethorphan are co-administered is at least about 2000 ng·hr/mL.7. The method of claim 1 , wherein the Cof dextromethorphan on ...

Oral Dosage Form Containing a Fast Release Exterior Coating

Aspects of the present invention are directed to an oral dosage form comprising a core containing one more active ingredients and a fast-release exterior coating. The fast release exterior coating includes a water soluble polymer; a saccharide or sugar alcohol, or a combination thereof, and a flavoring. The flavoring may be a warming sensate that is released in the oral cavity of the user after inserting the dosage form in his or her mouth. 1. An oral dosage form comprising:a core containing one or more active ingredients; and a water soluble polymer;', 'a saccharide or sugar alcohol or combination thereof; and', 'a flavoring., 'a fast-release, exterior coating comprising2. The oral dosage form of claim 1 , wherein the water-soluble polymer is present in the coating in an amount from about 10% (w/w) to about 90% (w/w).3. The oral dosage form of claim 1 , wherein the water soluble polymer is an alkylcellulose or an hydroxyalkylcellulose.4. The oral dosage form of claim 3 , wherein the water soluble polymer is an hydroxyalkylcellulose.5. The oral dosage form of claim 1 , wherein the water soluble polymer is a combination of hydroxypropylmethylcellulose and polyethylene glycol.6. The oral dosage form of claim 1 , wherein the saccharide or sugar alcohol or combination thereof is present in the coating in a total amount from about 1% (w/w) to about 50% (w/w).7. The oral dosage form of claim 1 , wherein the saccharide is a monosaccharide claim 1 , disaccharide claim 1 , polysaccharide claim 1 , or mixtures thereof.8. The oral dosage form of claim 7 , wherein the saccharide is maltodextrin.9. The oral dosage form of claim 1 , wherein the flavor includes a warming sensate or cooling sensate.10. The oral dosage form of claim 9 , wherein the warming sensate or cooling sensate provides a sensorial effect in the oral cavity of a user.11. The oral dosage form of claim 1 , wherein the flavoring further comprises a flavor selected from the group consisting of menthol claim 1 , ...