ТИОЛСУЛЬФОНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРА МАТРИКСНОЙ МЕТАЛЛОПРОТЕАЗЫ И СПОСОБЫ ЛЕЧЕНИЯ

Изобретение относится к тиолсульфоновым соединениям общей формулы Iа, которые могут быть использованы в качестве ингибиторов матриксных металлопротеаз-13 (ММП-13). В формуле Ia R1 представляет собой замещенный фенил, R2 и R3 представляют собой радикал, выбранный из группы, состоящей из атома водорода, C1-С6 алкила, аралкила с одним кольцом, имеющего 1-3 атома углерода в алкильной цепи, или R2 и R6 вместе с атомами углерода, с которыми они связаны, образуют 5- или 6-членное кольцо; R6 представляет собой радикал, выбранный из группы, состоящей из C1-С6 алкила, карбоксила, C1-С6 алкоксикарбонила. Изобретение также относится к способам лечения патологических состояний, связанных с патологической активностью матриксных металлопротеаз, относящихся к ММП-13. 5 с. и 15 з.п. ф-лы, 51 табл.

ПРОИЗВОДНЫЕ, ПРИМЕНЯЕМЫЕ ДЛЯ ЛЕЧЕНИЯ МЫШЕЧНОЙ АТРОФИИ

Изобретение относится к применению производного общей формулы Iгде Rи Rнезависимо друг от друга представляют собой водород, n представляет собой целое число между 1 и 2, Rпредставляет собой группу -OH или группу -O(C-Cалкил), Rпредставляет собой C-Cалкильную группу, Rи Rпредставляют собой независимо друг от друга атом галогена, или его фармацевтически приемлемой соли в качестве лекарственного средства для лечения и/или предотвращения мышечной атрофии у млекопитающих, и/или для ограничения мышечной атрофии у млекопитающих, и/или для стимуляции мышечного роста у тренирующихся млекопитающих, стремящихся увеличить массу и качество мышц, предотвращая появление симптомов саркопении, связанных с возрастом или реабилитацией после потери мышц, возрастной мышечной атрофии и/или последствий лекарственного лечения, и/или иммобилизации, и/или кахексии. 11 з.п. ф-лы, 1 ил., 3 табл.

ПРИМЕНЕНИЕ АНТАГОНИСТОВ SMOOTHENED ДЛЯ ЛЕЧЕНИЯ СВЯЗАННЫХ С ПУТЕМ HEDGEHOG НАРУШЕНИЙ

Группа изобретений основана на модуляции путей трансдукции сигналов Hedgehog. Более подробно группа изобретений относится к способам лечения, связанным с Hedgehog раков. В частности, в заявке описаны способы ингибирования состояний аномального роста, которые обусловлены такими фенотипами, как потеря функции Ptch, усиление по доминантно-негативному типу функции Hedgehog, усиление по доминантно-негативному типу функции Smoothened или усиление по доминантно-негативному типу функции Gli, заключающиеся во введении млекопитающему комбинации, включающей ингибиторы Smoothened и ингибиторы Gli или ингибиторы фосфатидилинозитол-3-киназы (PI3K). Группа изобретений позволяет эффективно лечить раки, связанные с Hedgehog. 2 н. и 4 з.п. ф-лы, 4 табл., 2 пр., 9 ил.

НОВАЯ АНТИРЕТРОВИРУСНАЯ КОМБИНАЦИЯ

Предложенная группа изобретений относится к области медицины. Предложена фармацевтическая композиция, представляющая собой таблеточный состав, содержащий ритонавир в первом слое и атазанавир во втором слое и полимер. Предложен способ получения указанной фармацевтической композиции, в котором выполняют экструзию горячего расплава ритонавира, получая экструдат, помещают данный экструдат в первый таблеточный слой, атазанавир - во второй слой и объединяют первый и второй слои, обеспечивая получение одной единичной многослойной таблетки. Предложена композиция, полученная вышеуказанным способом, для применения в лечении ВИЧ или СПИДа и способ лечения ВИЧ или СПИДа. Предложенная группа изобретений является эффективной в создании многослойной таблетки, обеспечивающей хорошую биодоступность для ритонавира. где атазанавир не разрушается во время приготовления. 4 н. и 15 з.п. ф-лы. 5 табл.. 4 пр.

ДИКЕТОНЫ И ГИДРОКСИКЕТОНЫ В КАЧЕСТВЕ АКТИВАТОРА СИГНАЛЬНОГО ПУТИ КАТЕНИНА

Данное изобретение относится к соединениям или их фармацевтически приемлемым солям общей формулы I, где Rпредставляет собой;Rвыбирают из группы, состоящей из замещенного или незамещенного фенила и,и; иR, R, Rи Rвсе представляют собой Н, также к соединениям II и III. Изобретение также относится к фармацевтическим композициям на основе этих соединений, способу активации передачи сигнала Wnt, способам лечения заболеваний, связанных с сигнальной трансдукцией, и применению их для лечения таких заболеваний, как остеопороз и остеоартропатия; несовершенный остеогенез, дефекты костей, переломы костей, пародонтоз, отосклероз, заживление раны, черепно-лицевые дефекты, онколитическое заболевание костей, травматические повреждения мозга, относящиеся к дифференцировке и развитию центральной нервной системы, включающие болезнь Паркинсона, удар, ишемическое церебральное заболевание, эпилепсию, болезнь Альцгеймера, депрессивное состояние, биполярное расстройство, шизофрению; глазные заболевания, такие как ...

ПРОИЗВОДНОЕ БЕНЗИЛФЕНИЛОВОГО ЭФИРА, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ЕГО ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И ПРИМЕНЕНИЕ

Настоящее изобретение относится к производному бензилфенилового эфира, представленному формулой (IA-1), или его фармацевтически приемлемой соли или стереоизомеру, а также к конкретным производным бензилфенилового эфира, структуры которых представлены в формуле изобретения, или их фармацевтически приемлемой соли или стереоизомеру, ингибирующим взаимодействие PD-1/PD-L1. Также изобретение относится к способу получения заявленных соединений, фармацевтической композиции и применению заявленных соединений.В формуле IA-1 R2выбран из циано и метилсульфонила; R3выбран из;X выбран из водорода и хлора. 6 н. и 4 з.п. ф-лы, 1 табл., 28 пр.

ПРОИЗВОДНЫЕ БЕНЗАМИДОВ И ГЕТЕРОАРЕНОВ

Настоящее изобретение относится к новым соединениям формулы I: ! , ! а также к их фармацевтически приемлемым солям, обладающим ингибирующей активностью в отношении белка-переносчика холестерилового эфира (БПХЭ), к способу их получения, фармацевтической композиции на их основе и к их применению для приготовления лекарственных средств. Значения заместителей R1, R2, R4, R5, а также А, В, D и n указаны в формуле изобретения. 4 н. и 10 з.п. ф-лы.

Способ профилактики ажитационного синдрома у детей с онкологической патологией

Изобретение относится к медицине, а именно к детской анестезиологии, и может быть использовано для профилактики ажитационного синдрома у детей с онкологической патологией, возникающего при высокопотоковой ингаляционной масочной анестезии севофлураном. Способ включает однократное интраназальное введение препарата дексмедетомидин в дозе 2 мкг/кг перед наркозом севофлураном по полуоткрытому контуру с сохраненным спонтанным дыханием. Использование изобретения позволяет достичь преднаркозной седации уровня R3-R5 по шкале Рамсей без угнетения дыхания, развития анальгезирующего эффекта, что позволяет уменьшить МАК севофлурана, удлинения времени постнаркозного сна, снижения внутричерепного давления, уровня мозгового кровотока и потребления мозгом кислорода. 2 табл., 2 пр.

КОМПОЗИЦИЯ И ПРОИЗВОДНЫЕ ЗАМЕЩЕННОГО АЗАИНДОЛОКСОАЦЕТАПИПЕРАЗИНА, ОБЛАДАЮЩИЕ ПРОТИВОВИРУСНОЙ АКТИВНОСТЬЮ

... 1. Соединение формулы I, включая его фармацевтически приемлемые соли, где Q выбран из группы, состоящей из R1, R2, R3, и R4, независимо выбраны из группы, состоящей из водорода, галогена, циано, нитро, COOR56, XR57, C(O)R7, C(O)NR55R56, В, D, и Е при условии, что по крайней мере один из R1-R4 выбран из В или Е; где ― представляет собой углерод-углеродную связь или отсутствует; m имеет значение 1 или 2; R5 представляет собой водород или (СН2)nCH3, -С(O)(СН2)nСН3, -С(O)O(СН2)nСН3, -С(O)(СН2)nN(СН3)2, где n имеет значение 0-5; R6 представляет собой О или отсутствует; А выбран из группы, состоящей из C1-6алкокси, арила и гетероарила; в которой указанный арил представляет собой фенил или нафтил; указанный гетероарил выбран из группы, состоящей из пиридинила, пиримидинила, пиразинила, триазинила, фуранила, тиенила, пирролила, имидазолила, тиазолила, изотиазолила, оксазолила, изоксазолила, хинолинила, изохинолинила, бензофуранила, бензотиенила, бензоимидазолила и бензотиазолила; и указанный арил ...

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 ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ПРОИЗВОДНОЕ ВЕРБЕНОЛА, ДЛЯ ЛЕЧЕНИЯ ИЛИ ПРОФИЛАКТИКИ НЕЙРОДЕГЕНЕРАТИВНОГО ЗАБОЛЕВАНИЯ

... 1. Фармацевтическая композиция для профилактики или лечения дегенеративного заболевания мозга, содержащая в качестве действующего вещества производное вербенона, представленное изображенной ниже формулой 1, или его фармацевтически приемлемую соль:где R, R, R, Rи Rкаждый независимо представляют собой по меньшей мере один заместитель, выбранный из группы, состоящей из атома водорода, атома галогена, выбранного из F, О, Br и I, гидроксильной группы, С-Салкильной группы, С-Салкокси-группы, амино-группы, С-Салкиламино-группы, С-Салкилдиамино-группы, С-Сароматического цикла, C-Cциклического кольца и C-Cгетероароматического цикла;X, Y и Z каждый независимо представляют собой атом углерода или по меньшей мере один гетероатом, выбранный из группы, состоящей из атомов N, О S; иозначает двойную связь или одинарную связь.2. Фармацевтическая композиция по п. 1, в которой R, R, R, Rи Rкаждый независимо представляют собой по меньшей мере один заместитель, выбранный из группы, состоящей из атома водорода ...

СПОСОБ ИНГИБИРОВАНИЯ ПРОДУЦИРОВАНИЯ ОСТАТОЧНЫХ ЛИПОПРОТЕИНОВ

... 1. Способ ингибирования продуцирования остаточных липопротеинов, включающий введение соединения, обладающего CETP-ингибирующей активностью, субъекту, нуждающемуся в таком введении. 2. Ингибитор продуцирования остаточных липопротеинов, содержащий соединение, обладающее CETP-ингибирующей активностью, в качестве активного ингредиента. 3. Способ ингибирования переноса холестерилового эфира, находящегося в HDL, в хиломикрон и/или VLDL, включающий введение соединения, обладающего CETP-ингибирующей активностью, субъекту, нуждающемуся в таком введении. 4. Ингибитор переноса холестерилового эфира, находящегося в HDL, в хиломикрон и/или VLDL, содержащий соединение, обладающее CETP-ингибирующей активностью, в качестве активного ингредиента. 5. СЕТР-ингибитор, имеющий ингибирующую активность в отношении переноса холестерилового эфира, находящегося в HDL, в хиломикрон и/или VLDL. 6. Способ по п.1, где ингибирование продуцирования остаточных липопротеинов достигается ингибированием переноса холестерилового ...

PPAR-ПОДДЕРЖИВАЮЩИЕ СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ МЕТАБОЛИЧЕСКИХ ЗАБОЛЕВАНИЙ

ПРИМЕНЕНИЕ АТАЗАНАВИРА ДЛЯ УЛУЧШЕНИЯ ФАРМАКОКИНЕТИКИ ЛЕКАРСТВЕННЫХ СРЕДСТВ, МЕТАБОЛИЗИРУЕМЫХ UGT1A1

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

КОМБИНАЦИИ ЛЕКАРСТВЕННЫХ СРЕДСТВ И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ СОСТОЯНИЯ, СОПРОВОЖДАЮЩЕГОСЯ КАШЛЕМ

5-МЕТИЛ-1-(ЗАМЕЩЕННЫЙ ФЕНИЛ)-2-(1Н)-ПИРИДОН ДЛЯ ПРОИЗВОДСТВА МЕДИКАМЕНТОВ ДЛЯ ЛЕЧЕНИЯ ФИБРОЗА В ОРГАНАХ И ТКАНЯХ

... 1. Применение соединений 5-метил-1-(замещенный фенил)-2(1Н)-пиридонов общей структурной формулы (I) ! ! для производства медикаментов для лечения фиброза органа или ткани, где, когда п=1, заместитель R представляет собой F, Cl, Br, I, нитро, алкильную группу, алкоксигруппу, галогенированную алкильную группу; когда n=2, заместитель R представляет собой F, Cl, Br, I, алкильную группу, алкоксигруппу, галогенированную алкильную группу. ! 2. Применение по п.1, при котором, когда n=1, R может быть F, или Br, или I; если n равно 2, то R может быть F, или Cl, или Br, или I, или насыщенной алкильной группой с прямой цепью, или насыщенной алкоксигруппой с прямой цепью, или насыщенной галогенированной алкильной группой с прямой цепью, и относительное положение R групп может быть орто или мета или пара. ! 3. Применение по п.2, при котором указанные соединения 5- метил-1-(замещенный фенил)-2(1Н)-пиридоны (общей структурной формулы I) выбирают из группы, содержащей: ! когда n=1, R=Br, соединениями являются ...

ИММУНОРЕГУЛИРУЮЩИЕ СРЕДСТВА

Твердые композиции на основе бетагистина для перорального применения с непульсирующим пролонгированным высвобождением

ИНГИБИТОРЫ ВАСЕ ДЛЯ ПРИМЕНЕНИЯ В ЛЕЧЕНИИ ДИАБЕТА

... 1. Соединение формулы I,,гдеRвыбран из группы, состоящей изi) арила иii) гетероарила,Rвыбран из группы, состоящей изi) H,ii) C-алкила иiii) -N(R,R);Rвыбран из группы, состоящей изi) H иii) C-алкила,Rвыбран из группы, состоящей изi) -CH-арила иii) -CH-гетероарила;или Rи Rвместе с азотом, к которому они присоединены, образуют пятичленный гетероциклил, возможно замещенный Z, или 3-аза-бицикло[3.2.1]октан-3-ил, возможно замещенный C-алкилом;Rвыбран из группы, состоящей изi) H иii) C-алкила;Rпредставляет собой -SO-C-алкил;n представляет собой 0, 1 или 2;m представляет собой 0, 1 или 2;А независимо выбран из группы, состоящей изi) ацетамидила,ii) ацетила,iii) амидо,iv) амино,v) C-алкокси,vi) C-алкила,vii) карбокси,viii) циано,ix) галогена,x) галоген-C-алкокси,xi) галоген-C-алкила,xii) гидрокси,xiii) -N(C-алкил, C-алкил) иxiv) -N(H, C-алкил),xv) -SO-C-алкила, представляет собой C-алкил;Z независимо выбран из группы, состоящей изi) арила, возможно замещенного 1 или 2 заместителями, независимо выбранными ...

АГОНИСТЫ GPR40

... 1. Соединение формулы (I):где кольцо А представляет собой возможно замещенную фенильную группу;кольцо В представляет собой возможно замещенную фенильную группу;Х представляет собой связь или линкерный фрагмент, содержащий от 1 до 8 атомов в линейной цепи;Y представляет собой связь или линкерный фрагмент, содержащий от 1 до 8 атомов в линейной цепи;Z представляет собой связь или выбран из группы, состоящей из возможно замещенного C-Cарила и возможно замещенного C-Cгетероарила, -С(=O)-, -C(=NR)-, -(CRR)-, -(CRR)O-, -(CRR)S-, -(CRR)NR'-, или представляет собой гетероатомную группу, выбранную из группы, состоящей из S, О, Р и NR'', где R'' выбран из группы, состоящей из Н, возможно замещенного C-Cалкила, возможно замещенного С-Сгетероалкила, возможно замещенного С-Сциклоалкила, возможно замещенного С-Cарила и возможно замещенного C-Cгетероарила;L представляет собой группу, способную высвобождать катион, или ее соль;Rвыбран из группы, состоящей из Н, OR, возможно замещенного C-Cалкила, возможно ...

СПОСОБЫ ПРИМЕНЕНИЯ АНТИТЕЛ К LGR5

ПРОИЗВОДНЫЕ, ПРИМЕНЯЕМЫЕ ДЛЯ ЛЕЧЕНИЯ МЫШЕЧНОЙ АТРОФИИ

ПРОИЗВОДНЫЕ ИНДОЛИН-2-ОНА ИЛИ ПИРРОЛОПИРИДИН/ПИРИМИДИН-2-ОНА

КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ РЕВМАТОИДНОГО АРТРИТА И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

... 1. Способ лечения ревматоидного артрита у пациента, получавшего ранее лечение метотрексатом, лефлуномидом, сульфасалазином и/или гидроксихлорохином, включающий введение пациенту эффективного количества сарилумаба (SAR153191), где сарилумаб вводят в дозе 150 мг раз в две недели или 200 мг раз в две недели.2. Способ по п. 1, где пациента ранее неэффективно лечили от ревматоидного артрита путем введения метотрексата, лефлуномида, сульфасалазина и/или гидроксихлорохина.3. Способ по п. 2, где метотрексат, лефлуномид, сульфасалазин и/или гидроксихлорохин вводят вместе с сарилумабом.4. Способ по п. 3, где сарилумаб и метотрексат вводят вместе.5. Способ по п. 4, где метотрексат вводят в дозе от 6 до 25 мг в неделю.6. Способ по п. 1, где сарилумаб вводят в дозе 150 мг раз в две недели.7. Способ по п. 1, где сарилумаб вводят в дозе 200 мг раз в две недели.8. Способ по п. 1, где пациент достигает 20%-ного улучшения по критериям основного заболевания Американской Коллегии ревматологов после 12 недель ...

МОНОГИДРАТ МЕЗИЛАТА N-[5-(АМИНОСУЛЬФОНИЛ)-4-МЕТИЛ-1,3-ТИАЗОЛ-2-ИЛ]-N-МЕТИЛ-2-[4-(2-ПИРИДИНИЛ)ФЕНИЛ]АЦЕТАМИДА

... 1. Способ получения N-[5-(аминосульфонил)-4-метил-1,3-тиазол-2-ил]-N-метил-2-[4-(2-пиридинил)фенил]ацетамида в соответствии со следующими стадиями:Стадия А:Взаимодействие соединения А следующей общей формулы А*гдеRпредставляет собой уходящую группу иRпредставляет собой алкильный остаток, содержащий от 1 до 6 атомов углерода, или циклоалкильный остаток, содержащий от 3 до 6 атомов углерода,с производным бороновой кислоты, бороланом, боринаном или реагентом дибороновой кислоты при удалении R-H или R-B(OR)и образовании промежуточного производного бороновой кислоты соединения А,в котором промежуточное производное бороновой кислоты затем подвергают взаимодействию с пиридином соединения В следующей общей формулы В*гдеRпредставляет собой уходящую группупри основных условиях для непосредственного получения (4-пиридин-2-илфенил)уксусной кислоты, которую затем очищают.Стадия В:Взаимодействие (4-пиридин-2-илфенил)уксусной кислоты, полученной на стадии А, с 4-метил-2-(метиламино)-1,3-тиазол-5-сульфонамидомдля ...

МОДУЛЯТОРЫ ROR ГАММА(RORy)

ПРОИЗВОДНЫЕ 2-БЕНЗОИЛАМИНОБЕНЗАМИДА В КАЧЕСТВЕ ИНГИБИТОРОВ BCL-3

КОМБИНАЦИИ ЛЕКАРСТВЕННЫХ СРЕДСТВ И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ СОСТОЯНИЯ, СОПРОВОЖДАЮЩЕГОСЯ КАШЛЕМ

... 1. Пероральная композиция, содержащая терапевтически эффективное количество теобромина и множество дополнительных терапевтических соединений, обладающих противокашлевой активностью.2. Пероральная композиция по п. 1, где множество терапевтических соединений, обладающих противокашлевой активностью, включает неопиоидное средство против кашля, опиоидное средство против кашля, антиконгестант, отхаркивающее средство, муколитическое средство, антигистаминное средство, нестероидное противовоспалительное лекарственное средство (НПВС), средство против нейропатической боли, терпен, ингибитор АПФ, антагонист рецептора ангиотензина II или любую их комбинацию.3. Пероральная композиция по п. 1, где противокашлевая активность подавляет функцию блуждающего нерва, ассоциированную с кашлем, подавляет функцию центральной нервной системы, ассоциированную с кашлем, и/или подавляет функцию периферической нервной системы, ассоциированную с кашлем.4. Пероральная композиция по любому из п.п. 1-3, где противокашлевая ...

НОВАЯ АНТИРЕТРОВИРУСНАЯ КОМБИНАЦИЯ

... 1. Фармацевтическая композиция, включающая твердую дозированную форму, содержащую: ! (i) ритонавир или его фармацевтически приемлемую соль; ! (ii) атазанавир или его фармацевтически приемлемую соль. ! 2. Фармацевтическая композиция по п.1, которая представляет собой таблеточный состав, содержащий упомянутый ритонавир в первом слое состава и упомянутый атазанавир во втором слое состава. ! 3. Фармацевтическая композиция по любому из предыдущих пунктов, дополнительно содержащая нерастворимый в воде полимер и/или растворимый в воде полимер. ! 4. Фармацевтическая композиция по п.3, в которой отношение массы ритонавира или атазанавира к массе полимера составляет от 1:1 до 1:6. ! 5. Фармацевтическая композиция по п.3, в которой полимер присутствует, по меньшей мере, в слое, содержащем ритонавир. !6. Фармацевтическая композиция по любому из пп.1, 2, 4 или 5, дополнительно содержащая, по меньшей мере, один фармацевтически приемлемый эксципиент. ! 7. Фармацевтическая композиция по п.6, в которой ...

ANTHRANILSÄUREAMID DERIVATE UND DEREN VERWENDUNG ALS VEGF-REZEPTOR TYROSIN KINASE INHIBITOREN

HEMMUNG DER p38 KINASE UNTER VERWENDUNG VON SYMMETRISCHEN UND ASYMMETRISCHEN DIPHENYLHARNSTOFFEN

Metalloproteinase inhibitors

The compound N1-[2,2-dimethyl-1S-(pyridin-2-ylcarbamoyl)-propyl]-N4-hydroxy-2R-isobutyl-3S- methoxy-succinamide is a matrix metalloproteinase inhibitor.

Amide derivatives

Drugs for potentiating the therapeutic effect against cancers, the mechanisms of action of which drugs involve DNA damage, containing compounds represented by the general formula (I) or salts thereof as the active ingredient: (I) wherein one of R<1> and R<2> is hydrogen and the other is -X-A (wherein A is hydrogen or acyl; and X is oxygen or NH); and one of R<3> and R<4> is hydrogen and the other is a group represented by the general formula (II): (II) (wherein Y is sulfonyl or carbonyl; R<5> is a cyclic group; Z is a single bond or C1-4 alkylene; and R<6> is hydrogen or C1-6 alkyl).

Organic compounds

Antibacterial agents

Potassium ion channel modulators & uses thereof

Use of 2-Amino-Heterocycles

Novel compounds, methods for their manufacture, and uses thereof

Synthetic cannabinoid analogue compounds of formula (I), wherein X is a group as defined herein. Also provided is a pharmaceutical composition of compounds of formula (I). Also provided is a compound of formula (I), or pharmaceutical composition, for use in a method of treatment, or for use as a medicament; which may be for use in the treatment of, or for use as a medicament for treating, epilepsy, generalised seizure, tonic-clonic seizure. Also provided is a method of preparing a compound of formula (I), comprising reacting a compound of formula (II) with a compound of formula (III), both defined herein. The method may use a palladium catalyst. Also provided is a method of preparing compounds of formula (I), comprising reacting a compound of formula (II) with bis(pinacolato)diboron (B2pin2), and reacting the product of that with a compound of formula (IV). The steps of the method may use a palladium catalyst. Also provided is an intermediate compound of formula (II), for use in the preparation ...

Topical compositions comprising fipronil and permethrin and methods of use

Therapeutic compositions and the use thereof

Compositions of non-steroidal antiinflammatory drugs and decongestants or anti-histamines

Substituted 4-hydroxy-phenylalcanoic acid derivatives with agonist activity to ppar-gamma

Substituted 4-hydroxy-phenylalcanoic acid derivatives with agonist to PPAR-gamma.

A compound having formula (I), wherein A is selected from the group consisting of: (i) phenyl, wherein said phenyl is optionally substituted by one or more halogen atoms, C1-6alkyl, C1-3alkoxy, C1-3fluoroalkoxy, nitrile, or -NR7R8 where R7 and R8 are independently hydrogen or C1-3alkyl; (ii) a 5- or 6-membered heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulfur; and (iii) a fused bicyclic ring (a), wherein ring C represents a heterocyclic group as defined in point (ii) above, which bicyclic ring is attached to group B via a ring atom of ring C; B is selected from the group consisting of: (iv) C1-6alkylene; (v) -MC1-6alkyiene or C1-6alkyleneMC1-6alkylene, wherein M is O, S, or-NR2 wherein R2 represents hydrogen or C1-3 alkyi; (vi) a 5-or 6-membered heterocyclic group containing at least one nitrogen heteroatom and optionally at least one further heteroatom selected from oxygen, nitrogen and sulfur and optionally substituted by C1-3 alkyl; and ( ...

Inhibition of the replication of HIV and related viruses using thiourea derivative compounds or salts thereof.

Method of aids, inhibition of the replication of hiv by contacting hiv with a compound of the formula-(see file) ...

Aerosol formulations containing salmeterol, salbutamol or fluticasone.

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

Inhibition of the replicateion of HIV and related viruses using thiourea derivative compounds or salts thereof.

Method for inhibiting the replication of hiv by contacting hiv with a compound of the formula: ...

COMPOSITIONS FOR THE TREATMENT OF HYPERTENSION AND/OR FIBROSIS

SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS

Use of an antagonist of ppar-alpha and ppr-gamma for the treatment of syndrom X.

A method for the treatment and/or prophylaxis of syndrome x in a human or non-human mammal, which method comprises the administration of an effective, non toxic and pharmaceutically effective amount of an agonist of ppar and ppar r, or a pharmaceutically acceptable derivative thereof, to a human ornon-human mammal in need of such treatment, and certain compounnd for use in such method.

MEDICAMENTS

Novel antiretroviral combination

Therapeutic compositions and the use thereof

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

Inhihition of the replication of hiv and related viruses using thiourea derivative compounds or salts thereof

Chemical compounds

Improvements of implantation rates after in vitro fertilization.

A method is provided for the improvement of implantation rates and/or pregnancy rates in a female mammal, comprising administering to a female mammal in whom prganancy is desired an effective amount of: a nitric oxide synthase substrate, a nitric oxide donor, or both, optionally in combination with, (b)a progestin, and, (c)optionally, in further combination with an estrogen. A method is also provided for fertility control for a female mammal, comprising administering to a female mammal in whom pregnancy is not desired and at risk of becoming pregnant an effective amount of nitric oxide synthase inhibitor in combination with an antiprogestin. Pharmaceutical compositions are also provided ...

Therapeutic compositions and the use thereof

Compositions of non-steroidal antiinflammatory drugs and decongestants or anti-histamines

Pyridine derivatives

Modulators of pharmacokinetic properties of therapeutics

Cxcr4 antagonists for the treatment of hiv infection

Benzenesulfonylamino-pyridin-2-yl derivatives and related compounds as inhibitors of 11-BETA-hydroxysteroid dehydrogenase type 1 (11-BETA-HSD-1) for the treatment of diabetes and obesity

Modulators of pharmacokinetic properties of therapeutics

Topical compositions comprising fipronil and permethrin and methods of use

Novel antiretroviral combination

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

Benzyl sulfonamide derivatives useful as mogat-2 inhibitors

Use of an antagonist of ppar-alpha and ppar-gamma for the treatment of syndrom x.

Inhibitors of metazoan parasite proteases

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

Medicaments

Topical compositions comprising fipronil and permethrin and methods of use

Cxcr4 antagonists for the treatment of hiv infection

SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS

Therapeutic compositions and the use thereof

Novel antiretroviral combination

Chemical compounds

MEDICAMENTS

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

Inhihition of the replication of hiv and related viruses using thiourea derivative compounds or salts thereof

COMPOUNDS AND METHODS FOR INHIBITION OF HIV AND RELATED VIRUSES

SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS

Benzyl sulfonamide derivatives useful as mogat-2 inhibitors

Modulators of pharmacokinetic properties of therapeutics

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

Cxcr4 antagonists for the treatment of hiv infection

Novel antiretroviral combination

BETAHISTINEZUBEREITUNGEN WITH CONTROLLED RELEASE

BICYCLI CONNECTIONS AS H3 RECEPTOR LIGAND

CARBAMATE OF 2-HETEROZYKLISCHEN 1,2-ETHANDIOLEN

PROCEDURE FOR THE INTESTINE CLEANING

CHEMICAL COMPOUNDS AND YOUR USE TO THE INCREASE OF THE PYRUVAT DEHYDROGENASE ACTIVITY

PROCEDURE FOR THE TREATMENT OF CHRONIC VIRALER HEPATITIS C ASSISTANCE OF RO 113-0830

AEROSOL PREPARATIONS

PHARMACEUTICAL COMPOSITIONS WITH MALONAMID DERIVATIVES FOR THE DECREASE OF TALLOW PRODUCTION

PHARMACEUTICAL ONE AEROSOLFORMULIERUNG.

DRUG

SIMETHICON CONTAINING EXHAUSTING MEANS

DOSING PATTERN FOR PPAR GAMMA ACTIVATORS

Modified release formulations containing drug-ion exchange resin complexes

A solid dose composition containing a mixture of a cured, modified release-barrier coated methylphenidate-ion exchange resin complex-matrix and an uncoated methylphenidate-ion exchange resin complex is described. The barrier coated methylphenidate-ion exchange resin complex-matrix comprises methylphenidate complexed with a pharmaceutically acceptable ion-exchange resin to form the complex which is admixed with a polymer to form a methylphenidate-ion exchange resin complex-matrix, which is subsequently coated with a modified release coating. The modified coating contains polyvinyl acetate polymer and a plasticizer and is cured.

Ethanamine Compounds and Methods of Using the Same

(S)-2-methyl- 1 -phenyl-2-(pyridin-2-yl)propan-1-amine, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, uses of said compound or salt for therapy of depression and other conditions, and methods of treating depression and other conditions by administering said compound or salt.

Combination Therapy Comprising A CCR5 Antagonist, A HIV-1 Protease Inhibtior and a Pharmacokinetic Enhancer

The present invention discloses a novel combination therapy for HIV-1 treatment relying on a combination of at least one CCR5 antagonist, at least one HIV-1 protease inhibitor and at least one pharmacokinetic enhancer of said at least one CCR5 antagonist and/or at least one HIV-1 protease inhibitor. The combination is intended for use in oral treatment of a disorder selected from the group consisting of HIV-1 infection, retroviral infections genetically related to HIV and AIDS, in a treatment-naïve patient infected with CCR5 tropic HIV-1 virus.

ArylSulfonamide Based Matrix Metalloprotease Inhibitors

The present invention provides a compound of formula (I): 2. The compound of claim 1 , wherein Ris selected from (C-C) aryl claim 1 , (5-14) membered heteroaryl claim 1 , and (4-14) membered heterocycloalkyl claim 1 , each of which is optionally substituted by one to three substituents selected from the group consisting of HC(O)— claim 1 , (5-9) membered heteroaryl claim 1 , and (4-9) membered heterocycloalkyl claim 1 , (C-C) alkyl claim 1 , (C-C) cycloakyl claim 1 , R—O— claim 1 , R—C(O)— claim 1 , R—SO— claim 1 , (R)NH—C(O)— claim 1 , and (R)(R)N— claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently (C-C) alkyl or (C-C) aryl claim 1 , each of which is further optionally substituted by one to two substituents selected from the group consisting of (C-C) alkyl claim 1 , halo claim 1 , hydroxy claim 1 , (C-C) alkoxy claim 1 , (C-C) aryl claim 1 , (C-C) dialkylamino claim 1 , and (4-9) membered heterocycloalkyl; Rand Rare independently hydrogen claim 1 , or (C-C) alkyl; X is selected from hydrogen claim 1 , amine claim 1 , cyano claim 1 , halogen claim 1 , nitro claim 1 , alkyl-S— claim 1 , alkyl-SO— claim 1 , alkyl-SO— claim 1 , HN—SO— claim 1 , R—C(O)— claim 1 , alkyl claim 1 , and R—O claim 1 , wherein Rand Rare defined above; ora pharmaceutically acceptable salt thereof, or an optical isomer thereof; or a mixture of optical isomers.4. The compound of claim 3 , wherein R′ claim 3 , is selected from (C-C) alkyl claim 3 , (C-C) cycloalkyl claim 3 , (C-C) alkoxy claim 3 , HC(O)— claim 3 , (5-9) membered heteroaryl claim 3 , and (4-9) membered heterocycloalkyl claim 3 , or (C-C) aryl claim 3 , said (C-C) aryl claim 3 , (5-9) membered heteroaryl claim 3 , and (4-9) membered heterocycloalkyl are optionally substituted by one or two substituents selected from hydroxy claim 3 , halo claim 3 , (C-C) alkyl claim 3 , carboxyl claim 3 , (C-C) alkoxycarbonyl claim 3 , and HC(O)—;{'sub': 2', '3, 'Rand Rare hydrogen;'}{'sub': 1', '7, 'X is ...

Methods for treating atrial fibrillation

The subject invention provides methods for reducing stroke rate, methods for preventing atrial remodeling, and methods for reversing atrial remodeling by administering budiodarone to reduce atrial fibrillation (AF) episode duration and an anticoagulant (AC). According to some methods of the invention, the average AF episode duration can be reduced to less than about 24, 5, 3 or 1 hour(s), and the maximum AF episode duration may be reduced to less than about 20, 10 or 5 hours. According to some methods of the invention, the reduced stroke rate upon administration of budiodarone and AC is less than the age-adjusted overall stroke rate. Further, some methods provide that patients who were refractory to one or more anti-arrhythmic drugs prior to administration of budiodarone may also be treated. Some methods provide for prevention of atrial remodeling and others provide for the reversal of atrial remodeling, including methods to quantify the reversal of atrial remodeling. In some methods of the invention, budiodarone is administered 400 mg BID or more preferably 600 mg BID.

Novel trpv3 modulators

Disclosed herein are modulators of TRPV3 of formula (I) wherein G 1 , X 1 , X 2 , X 3 , X 4 , X 5 , G 2 , Z 1 , R a , R b , u, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also presented.

Methods for Detecting and Treating Rhinovirus Infection

The invention provides a method for evaluating the activity of an agent for treating rhinovirus infection or a symptom thereof, a method of detecting or monitoring rhinovirus infection, and a method of treating rhinovirus infection or a symptom thereof. Various embodiments comprise measuring expression of (i) one or more genes selected from the group consisting of CRY2, B3GAT3, C10ORF95, and BATF3, and (ii) one or more genes selected from the group consisting of RNFT2, BTG4, PSD3, CAPN9, SULT1E1, HEY1, LRRC36, RAB3B, ALDH3B1, FAM134B, FAS, PLSCR1, CLEC2B, HAS2, MX1, SP110, GBP1, IFIT3, IFIT1, CXCL9, CXCL10, and CXCL11, from at least one biological sample to produce a gene expression profile, and comparing the gene expression profile to a reference gene expression profile. Systems, computer readable media, compositions, and methods for maintaining or improving respiratory health also are provided.

METHOD FOR DECREASING SEBUM PRODUCTION

The present invention is directed to the topical application of the malonamide ACAT inhibitors described by Formula I. Other aspects of the invention are directed to topical formulations of these diamides, their use to treat sebaceous gland disorders and their use to alleviate oily skin. 123-. (canceled)26. A method of claim 24 , wherein said compound is selected from the group consisting of: N′-[2 claim 24 ,6-bis(1-methylethyl)phenyl]-N-(1-methylethyl)-N-[[4-(methylthio)phenyl]methyl]-propanediamide or pharmaceutically acceptable salt thereof claim 24 , and N-[2 claim 24 ,6-bis(1-methylethyl)phenyl]-]β-[[(4-methoxyphenyl)methyl](2-pyridinyl)amino]-]β]-oxo-propanamide or pharmaceutically acceptable salt thereof.27. A method for treating a dermal disease comprising the topical administration of an effective amount of N-benzyl-N′-(2 claim 24 ,6-diisopropyl-phenyl)-N-isopropyl-malonamide claim 24 , or a pharmaceutically acceptable salt thereof claim 24 , to a patient in need thereof. This application claims the benefit of U.S. Provisional Application 60/509,984 filed Oct. 9, 2003.The present invention is directed to the topical application of a class of diamide ACAT inhibitors. Other aspects of the invention are directed to topical formulations of these diamides, their use to treat sebaceous gland disorders and their use to alleviate oily skin.Human skin is composed of three primary layers, the stratum corneum, the epidermis, and the dermis. The outer layer is the stratum corneum. Its primary function is to serve as a barrier to the external environment. Lipids are secreted to the surface of the stratum corneum. These lipids decrease the stratum corneum's water permeability. Sebum typically constitutes 95% of these lipids. Abramovits et al, Dermatologic Clinics, Vol 18, Number 4, Oct. 2000.Sebum is produced in the sebaceous glands. These glands are present over most of the surface of the body. The highest concentration of these glands occurs on the scalp, the forehead ...

GABR-A2 DIAGNOSTIC

The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sites known as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence at these GABR-A2 SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs. 1. A method for selecting a patient for treatment with an NMDA antagonist drug , comprising determining in a nucleic acid containing sample from said patient the nucleotide at single nucleotide polymorphism (SNP) position rs3756007 (SEQ ID NO: 9) and/or , rs11503016 (SEQ ID NO: 10) , and/or rs17537359 (SEQ ID NO: 11) , and/or rs1372472 (SEQ ID NO: 12) in GABR-A2 gene , wherein if there is a cytosine at rs3756007 (SEQ ID NO: 9) , or a thymine at rs11503016 (SEQ ID NO: 10) , or a thymine at rs11503016 (SEQ ID NO: 10) , or a thymine at rs1372472 (SEQ ID NO: 12) , said patient is selected for treatment with an NMDA antagonist drug.2. A method of recommending a treatment , the method comprising(a) selecting a patient in need of treatment for depression and/or anxiety, the patient's genome having been identified as bearing a minor allele at any one rs3756007 (SEQ ID NO: 9), rs11503016 (SEQ ID NO: 10), rs17537359 (SEQ ID NO: 11) or rs1372472 (SEQ ID NO: 12) in GABR-A2 gene; and(b) recommending that the patient be treated with an NMDA antagonist.3. The method as claimed in or , wherein the NMDA antagonist drug is selected from the group consisting of: (S)-1-phenyl-2-(pyridin-2-yl)ethanamine and ketamine.4. The method as claimed in or , wherein the NMDA antagonist drug is (S)-1-phenyl-2-(pyridin-2-yl)ethanamine.5. The ...

SUBSTITUTED 8-ALKOXY-2-AMINOTETRALIN DERIVATIVES, AND USE THEREOF

The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. 5. (canceled)6. A method for the treatment and/or prevention of heart failure claim 1 , angina pectoris claim 1 , hypertension claim 1 , pulmonary hypertension claim 1 , ischemias claim 1 , vascular disorders claim 1 , thromboembolic disorders and arteriosclerosis comprising administering and effective amount of a compound of to a human or animal in need thereof.7. (canceled)8. A pharmaceutical composition comprising a compound of in combination with one or more inert claim 1 , non-toxic claim 1 , pharmaceutically suitable excipients.9. The pharmaceutical composition of claim 8 , further comprising an at least one active ingredients selected from the group consisting of an organic nitrate claim 8 , an NO donors claim 8 , a cGMP-PDE inhibitor claim 8 , a stimulator of guanylate cyclase claim 8 , an agent having antithrombotic activity claim 8 , an agent lowering blood pressure claim 8 , and an agent altering lipid metabolism.10. (canceled) The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.One of the most important cellular transmission systems in mammalian cells is cyclic guanosine monophosphate (cGMP). Together with nitric oxide (NO), which is released from the endothelium and transmits hormonal and mechanical signals, it forms the NO/cGMP system. Guanylate cyclases catalyze the biosynthesis of cGMP from ...

PHARMACEUTICAL COMPOSITIONS

A composition of an antitussive, a decongestant, or an antihistamine to treat respiratory and oral pharyngeal congestion and related symptoms in a patient. 1. A pharmaceutical composition for alleviating symptoms of upper respiratory and oral-pharyngeal congestion in a subject , the composition comprising a first active ingredient selected from the group consisting of chlophedianol hydrochloride , chlorcyclizine hydrochloride , thonzylamine hydrochloride and dextromethorphan hydrogen bromide.2. The pharmaceutical composition of claim 1 , further comprising a second active ingredient selected from the group consisting of Pseudoephedrine Hydrochloride claim 1 , Guaifenesin claim 1 , Codeine phosphate claim 1 , Dexbrompheniramine claim 1 , Phenylephrine HC1 and thonzylamine hydrochloride.3. The pharmaceutical composition of claim 2 , further comprising a third active ingredient selected from the group consisting of Dexchlorpheniramine Maleate claim 2 , Chlorpheniramine Maleate claim 2 , dextromethorphan hydrogen bromide claim 2 , Pyrilamine maleate claim 2 , Diphenhydramine HCl claim 2 , Phenylephrine claim 2 , Codeine phosphate claim 2 , Doxylamine Succinate claim 2 , and Guaifenesin.4. The pharmaceutical composition of claim 1 , wherein the first active ingredient is present at a range of 9.375 mg to 100 mg.5. The pharmaceutical composition of claim 2 , wherein the second active ingredient is present at a range of 1 mg to 100 mg.6. The pharmaceutical composition of claim 3 , wherein third active ingredient is present at a range of 2 mg to 500 mg. This application claims priority from U.S. Provisional Patent Application No. 61/354,053 filed Jun. 11, 2010, U.S. Provisional Patent Application No. 61/354,057 filed Jun. 11, 2010, and U.S. 61/354,061 filed Jun. 11, 2010, all of which are hereby incorporated by reference as if fully set forth herein.The present invention relates to the treatment and relief of various symptoms of upper respiratory and oral pharyngeal ...

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.

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 ...

GASTRIC AND COLONIC FORMULATIONS AND METHODS FOR MAKING AND USING THEM

In alternative embodiments, the invention provides compositions, e.g., formulations, used for gastric, gastrointestinal and/or colonic treatments or lavage, e.g., orthostatic lavage, e.g., for inducing the purgation (e.g., cleansing) of a gastrointestinal (GI) tract, including a colon; and methods for making and using them. In alternative embodiments, compositions and methods of the invention are used for the amelioration, treatment and/or prevention of constipation, for the treatment of abdominal pain, particularly non-specific abdominal pain, and diarrhea, including diarrhea caused by a drug side effect, a psychological condition, a disease or a condition such as Crohn's Disease, a poison, a toxin or an infection, e.g., a toxin-mediated traveler's diarrhea. In alternative embodiments, the invention provides pharmaceuticals and products (articles) of manufacture for delivering these compositions and formulations to an individual, e.g., a human or an animal. 1: A composition comprising: 'a bisoxatin (or 2,2-bis(4-hydroxyphenyl)-2H-benzo[b][1,4]oxazin-3(4H)-one), or bisoxatin acetate, or equivalent,', '(i) a bisacodyl, or pyridin-2-ylmethanediyl)dibenzene-4,1-diyl diacetate, or 4,4′-(pyridin-2-ylmethylene) bis(4,1-phenylene) diacetate, or bioequivalent diphenylmethane or equivalent, or'}(ii) an erythritol, or (2R,3S)-butane-1,2,3,4-tetraol, or equivalent isomers or sugar or polyol substitute isoforms, and(III) a pharmaceutically acceptable salt.2: The composition of claim 1 , wherein the composition comprises:(a) between about 1, 5, 10, 15, 20, 25, 30, 35, 40, 45 to 50 milligram (mg) to about 100, 150, 200, 250, 300, 350, 400, 450, 500, 550, 600, 650, 700, 750, 800, 850, 900, 950 or 1000 or more milligrams (mg), or between about 5 milligrams (mg) to about 15 milligrams (mg), or the composition comprises about 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 45, 50, ...

Diphenyl-amine derivatives: uses, process of synthesis and pharmaceutical compositions

The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, prodrug or solvate thereof, a method of synthesis of said compounds, pharmaceutical compositions comprising them and their use as a medicament for treating inflammatory diseases.

Chemosensory Receptor Ligand-Based Therapies

Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention. 2. (canceled)5. (canceled)9. (canceled)14. (canceled)20. A composition comprising a chemosensory receptor ligand comprising an extract or a combination of extracts selected from the following: a) the fruit of one or more plants of the Cucurbitaceae family consisting of between 20 wt % and 100 wt % , based on the total weight of the extract , of Mogroside V , b) the fruit of the Katemfe plant , and c) an optional glycyrrhizinate; and wherein the composition is adapted to release a therapeutically effective amount of the ligand to one or more regions of the intestine of a subject.28. A composition according to claim 27 , wherein the tripeptide is selected from the following: Glu-Asp-Ile claim 27 , Glu-Asp-Phe claim 27 , Leu-Glu-Glu claim 27 , Glu-Glu-Leu claim 27 , Asp-Glu-Ile claim 27 , γGlu-Glu-Leu claim 27 , Glu-Glu-Val claim 27 , Glu-Leu-Glu claim 27 , Lys-Asp-Ile and Glu-Ile-Gly.35. (canceled)36. (canceled)37. A composition according to claim 1 , wherein the composition further releases at least some of the chemosensory receptor ligand in the stomach.38. A composition according to claim 1 , wherein one or more regions of the intestine are the duodenum claim 1 , jejunum claim 1 , ileum claim 1 , caecum claim 1 , colon and/or rectum.39. (canceled)40. A composition according to claim 1 , wherein the composition releases at an onset of about 5 to about 45 minutes claim 1 , about 105 to about 135 minutes claim 1 , about 165 to about 195 minutes claim 1 , about 225 to about 255 minutes or a combination of times thereof following administration to a subject.41. A ...

Methods for Preventing Flea Allergy Dermatitis in Companion Animals

Methods for reducing the incidence of flea allergy dermatitis (FAD) in a companion animal are disclosed, the methods directed to inhibiting blood feeding by ectoparasites on a companion animal. The methods of the present invention involve administering a pesticide composition comprising cyphenothrin to a companion animal, specifically dogs and cats, in doses and proportions which are parasiticidally effective against a variety of ectoparasites, and in formulations which are convenient for topical application to the animal's skin, preferably localized over a small surface area. Such methods are useful in preventing and/or reducing the incidence of flea allergy dermatitis.

Treatments for cellular proliferative disorders and identification thereof

This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.

B- and y -diketones and y -hydroxyketones as wnt/ b -catenin signaling pathway activators

The present invention discloses β-diketones, γ-diketones or γ-hydroxyketones or analogs thereof, that activate Wnt/β-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.

Ophthalmic formulation and method for ameliorating presbyopia

An ophthalmic formulation having an effective amount of a parasympathomimetic agent comprising pilocarpine, or a pharmaceutically acceptable salt thereof, and one or more α1 adrenergic agonists or antagonists is disclosed. The ophthalmic formulation may enable treatment of conditions adversely affecting the visual acuity of a patient, including presbyopia. A method of using the disclosed ophthalmic formulation to treat or ameliorate symptoms of presbyopia is also disclosed.

Modified Release Formulations Containing Drug-Ion Exchange Resin Complexes

An aqueous liquid suspension containing a coated drug-ion exchange resin complex comprising a core composed of an amphetamine complexed with a pharmaceutically acceptable ion-exchange resin and an uncoated amphetamine-ion exchange resin complex is provided. The coated amphetamine-ion exchange resin complex is in admixture with a polymer to form a matrix. Methods of making the coated complex and the liquid suspension are described.

Methods of treating muscular dystrophy

Disclosed herein are α7β1 integrin modulatory agents and methods of using such to treat conditions associated with decreased α7β1 integrin expression or activity, including muscular dystrophy. In one example, methods for treating a subject with muscular dystrophy are disclosed. The methods include administering an effective amount of an α7β1 integrin modulatory agent to the subject with muscular dystrophy, wherein the α7β1 integrin modulatory agent increases α7β1 integrin expression or activity as compared to α7β1 integrin expression or activity prior to treatment, thereby treating the subject with muscular dystrophy. Also disclosed are methods of enhancing muscle regeneration, repair, or maintenance in a subject and methods of enhancing α7β1 integrin expression by use of the disclosed α7β1 integrin modulatory agents. Methods of prospectively preventing or reducing muscle injury or damage in a subject are also disclosed.

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 ...

COMPOSITIONS AND METHODS FOR THE TREATMENT OF PAIN

The claimed invention relates to compositions that may be in a form of a liquid, solid, gel, cream or gel capsule comprising an analgesic, and methods for administering these compositions for treatment of patients suffering from various forms of pain. 1. A composition comprising an analgesic/antipyretic compound.2. The composition of claim 1 , wherein said analgesic/antipyretic is selected from one or more of the group consisting of acetaminophen claim 1 , buprenorphine claim 1 , butorphanol claim 1 , codeine claim 1 , dextropropoxyphene claim 1 , dihydrocodeine claim 1 , fentanyl claim 1 , diamorphine claim 1 , hydrocodone claim 1 , hydromorphone claim 1 , ketobemidone claim 1 , morphine claim 1 , nalbuphine claim 1 , oxycodone claim 1 , oxymorphone. pentazocine claim 1 , pethidine claim 1 , tramadol claim 1 , acetylsalicylic acid claim 1 , diflunisal ethenzamide claim 1 , aminophenazone claim 1 , metamizole claim 1 , phenazone claim 1 , phenacetin claim 1 , ziconotide claim 1 , tetrahydrocannabinol claim 1 , acetylsalicylic acid claim 1 , choline salicylate claim 1 , magnesium salicylate claim 1 , sodium salicylate claim 1 , ibuprofen claim 1 , naproxen and ketoprofen.3. The composition of further comprising an analgesic adjunct.4. The composition of claim 3 , wherein said analgesic adjunct is selected from one or more of the group consisting of S (+)-ketamine claim 3 , metoclopramide claim 3 , ciramadol claim 3 , sufentanil claim 3 , caffeine and remifentanil.5. The composition of further comprising an antihistamine.6. The composition of claim 5 , wherein said antihistamine is selected from the group consisting of diphenhydramine claim 5 , cyproheptadine hydrochloride claim 5 , brompheneramine claim 5 , hydroxyzine claim 5 , chloropheniramine claim 5 , pyrilamine maleate claim 5 , pyrilamine tannate claim 5 , acepromazine claim 5 , aceprometazine claim 5 , alimemazine claim 5 , alimemazine tartrate claim 5 , amoxydramine camsilate claim 5 , antazoline ...

Aquaporin modulators and methods of using them for the treatment of edema and fluid imbalance

Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.

MATERIALS AND METHODS FOR TREATING VALVULAR HEART DISEASES

Methods of treating a valvular heart disease are provided. Methods for treating valvular heard disease include administering to a subject a therapeutically effective amount of at least one hedgehog pathway inhibitor. Also provided are methods for reducing fibrosis in a subject, which comprise administering to the subject a therapeutically effective amount of at least one hedgehog pathway inhibitor. 1. A method of treating a valvular heart disease in a subject , the method comprising:administering to the subject a therapeutically effective amount of at least one hedgehog pathway inhibitor.2. The method according to claim 1 , wherein the at least one hedgehog pathway inhibitor is selected from: at least one smoothened (SMO) antagonist; at least one antagonist of GLI1 claim 1 , GLI2 claim 1 , and/or GLI3; at least one agonist of PTCH1 and/or PTCH2; or any combination thereof.3. The method according to claim 1 , wherein the at least one hedgehog pathway inhibitor comprises at least one of: vismodegib claim 1 , sonidegib claim 1 , BMS-833923 claim 1 , TAK-441 claim 1 , glasdegib claim 1 , taladegib claim 1 , saridegib claim 1 , arsenic trioxide claim 1 , PF-5274857 claim 1 , MRT-92 claim 1 , GANT-58 claim 1 , GANT-61 claim 1 , RU-SKI 43 claim 1 , sonic hedgehog (Shh) monoclonal antibody 5E1 claim 1 , itraconazole claim 1 , and robotnikinin.4. The method according to claim 1 , further including the step of:identifying a subject at risk of having a valvular heart disease and/or identifying a subject having a valvular heart disease or a symptom related to the valvular heart disease.5. The method according to claim 1 , wherein the valvular heart disease comprises at least one disease process involving one or more of the four valves of the heart.6. The method according to claim 1 , wherein the valvular heart disease comprises at least one disease selected from: aortic valve stenosis claim 1 , mitral valve stenosis claim 1 , tricuspid valve stenosis claim 1 , pulmonary valve ...

COMPOSITIONS USEFUL FOR THE TREATMENT OF GASTROINTESTINAL DISORDERS

This invention provides novel peptides and methods to prevent, control, and treat an inflammation, cancer and other disorders, particularly of the gastrointestinal tract and the lung by administering at least one agonist of guanalyte cyclase receptor either alone or in combination with a compound selected from i) 5-aminosalicyclic acid (5-ASA) or a derivative or a pharmaceutically acceptable salt thereof; ii) mercaptopurine; or iii) an anti-TNF therapy. 1. A composition comprising a guanylate cyclase receptor agonist (GCRA) peptide consisting essentially of the sequence of any one of Tables 1-8 and a compound selected from i) 5-aminosailcyclic acid (5-ASA) or a derivative or a pharmaceutically acceptable salt thereof: ii) mercaptopurine; iii) an anti-TNF therapy; or iv) an antibiotic.2. The composition of claim 1 , wherein said 5-ASA or derivative or pharmaceutically acceptable salt thereof is covalently linked to the N terminus and/or the C terminus of said peptide.4. The composition of claim 1 , further comprising a pharmaceutical carrier claim 1 , excipient or diluent.5. The composition of claim 1 , wherein said derivative is sulfasalazine.6. The composition of claim 1 , wherein said peptide is a bicyclic peptide comprising the sequence of any one of Tables 1 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , and 8.7. A formulation comprising an inert carrier coated with composition of and an enteric coating which releases said composition at pH5 or pH7.8. The formulation of claim 7 , wherein said inert carrier is a selected from mannitol claim 7 , lactose claim 7 , a microcrystalline cellulose claim 7 , or starch.9. A method for treating a condition that responds to enhanced cGMP levels in a subject in need thereof comprising administering to said subject a therapeutically effective amount of a composition of claim 1 , wherein said composition is administered in an amount sufficient to increase water transport in the gastrointestinal tract and induce cGMP production ...

MODIFIED RELEASE FORMULATIONS CONTAINING DRUG-ION EXCHANGE RESIN COMPLEXES

A particulate, modified release barrier coated drug-cation exchange resin complex comprising a core composed of a drug complexed with a pharmaceutically acceptable ion-exchange resin is provided. Methods of making and products containing this coated complex are described. 1. An orally ingestible aqueous liquid suspension comprising: (i) a particulate drug-cation exchange resin complex comprising at least one drug bound to a pharmaceutically acceptable water insoluble cation exchange resin, and further comprising a water insoluble polymer or copolymer, or hydrophilic polymer which forms a matrix with the drug-cation exchange resin complex, which particulate drug-cation exchange resin complex-(water insoluble polymer or copolymer or a hydrophilic polymer) matrix is capable of passing through a number 40 mesh screen, and', '(ii) about 25% w/w to about 50% w/w of a water permeable, water insoluble, non-ionic, modified release polymeric diffusion barrier coating which provides a modified release profile to the drug in said drug-cation exchange resin complex-(water insoluble polymer or copolymer or hydrophilic polymer) matrix, wherein said at least one drug is methylphenidate, said barrier coating having an elongation factor of about 125% to about 400% and comprising a water insoluble polymer and about 2.5% w/w to about 20% w/w plasticizer based on the weight of the barrier coating; and, '(A) barrier coated particulates which provide a modified release profile which comprise (iiia) an uncoated particulate methylphenidate-cation exchange resin complex of a size capable of passing through a number 40 mesh screen, wherein said uncoated methylphenidate-cation exchange resin complex is methylphenidate bound to a pharmaceutically acceptable water insoluble cation exchange resin and/or', '(iiib) methylphenidate or a pharmaceutically acceptable salt thereof which is not complexed with an ion exchange resin; and, '(B) at least one of (iiia) and/or (iiib)(C) a pharmaceutically ...

Purgative Composition

The present invention relates to a purgative composition containing polyethylene glycol and sodium picosulfate, wherein the stability of sodium picosulfate is improved by adding a pH controller. According to the present invention, the purgative composition ensures the stability of medicinal ingredients and has a great advantage of having a small dose even while showing a bowel cleansing rate greater than or equal to a commercial preparation, which should be taken in a large dose. In addition, according to the present invention, the composition has high compliance due to a good taste. 1. A purgative composition comprising polyethylene glycol and sodium picosulfate , further comprising a pH controller in order to improve the stability of sodium picosulfate.2. The purgative composition of claim 1 , wherein the pH controller is an alkalizer.3. The purgative composition of claim 2 , wherein the alkalizer is sodium hydroxide claim 2 , sodium phosphate claim 2 , sodium hydrogencarbonate claim 2 , sodium citrate claim 2 , potassium citrate claim 2 , potassium hydroxide claim 2 , potassium phosphate claim 2 , magnesium carbonate claim 2 , sodium carbonate claim 2 , ammonium carbonate claim 2 , or a mixture thereof.4. The purgative composition of claim 3 , wherein the alkalizer is sodium hydrogencarbonate.5. The purgative composition of claim 1 , wherein the composition is liquid and its pH is 7 to 12.6. The purgative composition of claim 1 , wherein the composition is dissolved in purified water to make its total volume 300 ml and the pH of the prepared solution is 7 to 12.7. A method for cleansing bowel claim 1 , using a liquid purgative composition comprising 100-200 g of polyethylene glycol having number average molecular weight of 3000-5000 claim 1 , 40-70 g of sorbitol claim 1 , 0.005-0.03 g of sodium picosulfate claim 1 , 0.1-0.4 g of alkalizer claim 1 , and a suitable amount of sweetener in 300 ml of solution claim 1 ,wherein the method comprises (1) administering 100 ...

COMPOUNDS FOR TREATMENT OF PD-L1 DISEASES

Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris -A-Z.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris —O—X—Y.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris -A-Z claim 1 , A is a bond claim 1 , and Z is phenyl claim 1 , optionally substituted with one to three R.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Xis —CH—.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein R claim 1 , Rand Rare H claim 1 , and Ris selected from the group consisting of F claim 1 , Cl claim 1 , CH claim 1 , CFand OCH.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein a ring is formed between one pair of Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , or Rand R.8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris -A-Z claim 1 , and Z is selected from the group consisting of piperidinyl claim 1 , imidazolyl and pyridinyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein n is 0.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Ris selected from the group consisting of F claim 1 , Cl claim 1 , CH claim 1 , CFand OCH.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein the group Ris OCHand Ris F.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Rand Rare each H.13. The compound of claim 1 , or a pharmaceutically acceptable salt thereof wherein Rand Rare combined to form a 4- to 8-membered ring or spirocyclic ring claim 1 , optionally having one or two additional ring vertices selected from O claim 1 , N or S; wherein said ring or spirocyclic ring is substituted with 0 to 4 substituents independently selected from the group ...

COMPOSITIONS AND METHODS OF MAKING RAPIDLY DISSOLVING IONICALLY MASKED FORMULATIONS

The present invention includes compositions and methods for reduce the taste of the drug in the drug resin complex. The composition may include one or more drug-resin complexes and a highly compressible, free-flowing pharmaceutical excipient. The resin is present in an amount effective to reduce the taste of the drug in the drug resin complex relative to an otherwise identical pharmaceutical composition without the resin; and wherein the highly compressible, free-flowing pharmaceutical excipient causes release of the drug-resin complex in the mouth. 1. A taste-masked pharmaceutical composition comprising:a drug-resin complex and a highly compressible, free-flowing pharmaceutical excipient, wherein the resin is present in an amount effective to reduce the taste of the drug in the drug resin complex by more than about 15 percent relative to an otherwise identical pharmaceutical composition without the resin; and wherein the highly compressible, free-flowing pharmaceutical excipient aids release of the drug-resin complex in the mouth.2. The composition of claim 1 , wherein the composition comprises a chewable tablet claim 1 , a solid claim 1 , a dissolvable or disintegrating tablet claim 1 , a liquid claim 1 , a gel claim 1 , a tab claim 1 , a capsule claim 1 , a powder claim 1 , a lotion claim 1 , a cream claim 1 , a gum claim 1 , a lozenge and combinations thereof.3. The composition of claim 1 , wherein the drug in the drug-resin complex comprises dextromethorphan claim 1 , codeine claim 1 , morphine claim 1 , hydrocodone claim 1 , hyoscyamine claim 1 , moguisteine claim 1 , pseudoephedrine claim 1 , chlorpheniramine claim 1 , phenylpropanolamine claim 1 , pharmaceutically acceptable salts of the same and combinations thereof.4. The composition of claim 1 , wherein the pharmaceutical composition is suitable for oral administration.5. The composition of claim 1 , further comprising one or more flavorants claim 1 , sweeteners claim 1 , coolants claim 1 , dyes claim 1 , ...

COMPOSITIONS AND METHODS FOR TREATING ALZHEIMER'S DISEASE

Provided are methods for treating Alzheimer's disease (AD), which in some embodiments can include administering to a subject in need thereof a composition that includes an inhibitor of an Aβ oligomer (AβO) biological activity. Also provided are methods for inhibiting development and/or progression of at least one symptom associated with AD, methods for inhibiting neuronal cell cycle re-entry (CRR), methods for inhibiting Aβ oligomer (AβO) biological activity, methods for inhibiting Aβ oligomer (AβO)-stimulated activation of calcium-calmodulin-dependent protein kinase II (CaMKII) biological activity, and methods for inhibiting calcium influx-induced excitotoxic neuronal death. In some embodiments, the inhibitor of the AβO biological activity or the inhibitor of N-methyl-D-aspartate receptor (NMDAR) signaling includes a small molecule inhibitor, an inhibitory nucleic acid, a calcium chelator, or any combination thereof. Also provided are methods for treating subjects who are pre-symptomatic for AD with inhibitors of AβO and/or NMDAR biological activities. 1. (canceled)2. A method for inhibiting development and/or progression of at least one symptom associated with Alzheimer's disease (AD) , the method comprising , consisting essentially of , or consisting of administering to a subject in need thereof a composition comprising , consisting essentially of , or consisting of an effective amount of an inhibitor of an Aβ oligomer (AβO) biological activity.3. (canceled)4. A method for inhibiting Aβ oligomer (AβO) biological activity , the method comprising , consisting essentially of , or consisting of administering to a subject in need thereof a composition comprising , consisting essentially of , or consisting of an effective amount of an inhibitor of N-methyl-D-aspartate receptor (NMDAR) signaling.5. (canceled)6. A method for inhibiting calcium influx-induced excitotoxic neuronal death , the method comprising , consisting essentially of , or consisting of administering to ...

NOVEL FORMULATIONS TO INHIBIT CYCLOOXYGENASE AND PRO-INFLAMMATORY CYTOKINE MEDIATED DISEASES

The invention provides method and composition for alleviating one or more symptoms associated with a medical condition mediated by one or more of a cyclooxygenase, a pro-inflammatory cytokine, and a pro-inflammatory enzyme. The method includes administering an effective amount of a composition to a person suffering from the medical condition. The composition essentially includes a set of plant extracts. The set of plant extracts include an extract of , an extract of , an extract of , and an extract of . Wherein, one or more extracts of the set of plant extracts includes one or more desired active ingredient in an amount greater than an amount of other active ingredients present in the one or more extracts. The composition can also be used as combination therapy with any other known anti-inflammatory agents. 1. A method for alleviating at least one symptom associated with a medical condition mediated by at least one of a cyclooxygenase , a pro-inflammatory cytokine , and a pro-inflammatory enzyme , the method comprising:administering to a person suffering from the medical condition a therapeutic dose of an agent selected from the group consisting of celecoxib, dexamethasone, and sulfasalazine; and{'i': Withania somnifera', 'Boswellia serrata', 'Curcuma longa', 'Zingiber officinale., 'administering to the person suffering from the medical condition a composition comprising a set of plant extracts, wherein the set of plant extracts comprises an extract of , an extract of , an extract of , and an extract of'}2. (canceled)3Withania somniferaWithania somniferaWithania somnifera.. The method of claim 1 , wherein the at least one extract comprises the extract of claim 1 , wherein the at least one desired active ingredient comprises Withanolide-D claim 1 , and wherein an amount of Withanolide-D present in the extract of is greater than an amount of other active ingredients present in the extract of4Withania somnifera,Boswellia serrata,Curcuma longaZingiber officinale.. The ...

Preparations for the Treatment of Sleep-Related Respiratory Disorders

The present invention is directed to combinations of sedating antihistamines and at least one, and preferably two or more dietary supplements, which can be indole-based, such as tryptophan, 5-hydroxytryptophan, serotonin, N-acetyl-5-hydroxytryptamine and melatonin, and to their use for treating and thereby improving the health and quality of life of those suffering from sleep-related respiratory disorders, characterized by abnormal breathing during sleep. These include snoring, sleep disordered breathing, sleep apneas, upper airway resistance syndrome, obstructive sleep apnea, central sleep apnea and obesity hypoventilation syndrome and associated ailments. 1. A pharmaceutical composition for the treatment of sleep-related respiratory disorders comprising a mixture of at least one antihistamine drug and at least one dietary supplement.2. The pharmaceutical composition according to wherein the antihistamine drug is selected from a group consisting of Cetirizine claim 1 , Chlorpheniramine claim 1 , Clemastine claim 1 , Desloratadine claim 1 , Dexchlorpheniramine claim 1 , Dimenhydrinate claim 1 , Dimetindene claim 1 , Diphenhydramine claim 1 , Doxylamine claim 1 , Ebastine claim 1 , Embramine claim 1 , Fexofenadine claim 1 , Levocetirizine claim 1 , Loratadine claim 1 , Meclozine claim 1 , Olopatadine claim 1 , Pheniramine claim 1 , Promethazine claim 1 , Triprolidine claim 1 , and pharmaceutically-acceptable salts thereof.3. The pharmaceutical composition according to wherein the dietary supplement is an indole-based compound.4. The composition according to further includes at least one vitamin and pharmaceutically acceptable minerals to enhance the effect of the indole-based compounds.5. The pharmaceutical composition of wherein the indole-based compound is L-tryptophan or a derivative of L-tryptophan.6. The pharmaceutical composition of further comprising melatonin and its pharmaceutically acceptable salts.7. The composition according to further includes ...

Antihistamines Combined with Dietary Supplements for Improved Health

The present invention provides combinations comprising a sedating antihistamine and selected indole-based natural products such as L-tryptophan, 5-hydroxytryptophan and melatonin, along with pharmaceutically acceptable calcium and magnesium salts and selected B vitamins. These combinations are useful in providing a medicament for improving sleep in mammals, especially humans. 1. A method of inducing restorative sleep function comprising administering a pharmaceutical composition comprising a tablet , capsule or beverage for ingestion containing a mixture of an antihistamine drug and two or more indole-based dietary supplements.2. The method of claim 1 , wherein the antihistamine drug is selected from a group consisting of Cetirizine claim 1 , Chlorpheniramine claim 1 , Clemastine claim 1 , Desloratadine claim 1 , Dexchlorpheniramine claim 1 , Dimenhydrinate claim 1 , Dimetindene claim 1 , Diphenhydramine claim 1 , Doxylamine claim 1 , Ebastine claim 1 , Embramine claim 1 , Fexofenadine claim 1 , Levocetirizine claim 1 , Loratadine claim 1 , Meclozine claim 1 , Olopatadine claim 1 , Pheniramine claim 1 , Promethazine Triprolidine claim 1 , and pharmaceutically-acceptable salts thereof.3. The method of wherein one of the indole-based dietary supplement is L-tryptophan or a derivative of L-tryptophan.4. The method of wherein the pharmaceutical composition further comprises melatonin and its pharmaceutically acceptable salts.5. The method of wherein the composition further includes at least one vitamin and pharmaceutically acceptable minerals to enhance the effect of the indole-based compounds.6. The method of wherein the composition further includes pharmaceutically acceptable calcium salts claim 1 , magnesium salts claim 1 , and at least one pyridine-based vitamin.7. The method of wherein inducing restorative sleep function comprises preventing or ameliorating a sleep related breathing disorder.8. The method of wherein sleep related breathing disorder is selected from ...

COMPOSITIONS AND METHODS FOR THE TREATMENTOF NEURODEGENERATIVE AND OTHER DISEASES

In one embodiment, the present application discloses methods of treating diseases and disorders with sulfasalazine, an ABCG2 inhibitor and pharmaceutical formulations of sulfasalazine where the bioavailability of the sulfasalazine is increased. In another embodiment, the present application also provides dosing regimens for treating neurodegenerative diseases and disorders with compositions comprising sulfasalazine and an ABCG2 inhibitor. 117.-. (canceled)18. A method for the treatment of neurodegenerative disease selected from P-MS , ALS , Parkinson's disease , Alzheimer's disease , epilepsy and other seizure disorders , neuropathic pain , traumatic brain injury , Huntington's disease , ischemic stroke , Rett Syndrome , Frontotemporal Dementia , HIV-associated Dementia and Alexander disease , the method comprising:administering to a patient a pharmaceutical composition comprising a therapeutically effective amount of 2-hydroxy-5-[[4-[(2-pyridinylamino)sulfonyl]phenyl]azo]benzoic acid (sulfasalazine), an ATP-binding cassette sub-family G member 2 inhibitor (ABCG2 inhibitor); and a pharmaceutically acceptable excipient;wherein the administration of the pharmaceutical composition provides an increase of at least 200% in the bioavailability of sulfasalazine when compared to an RLD.19. The method of claim 18 , wherein the ABCG2 inhibitor is TPGS or Tween-20.20. The method of claim 18 , wherein the pharmaceutically acceptable excipient is PVP-VA64.2128.-. (canceled) This application claims the priority under 35 U.S.C. 119(e) of U.S. Application No. 62/411,512, filed Oct. 21, 2016, which is incorporated into this application by reference.The invention relates generally to the field of pharmaceuticals, pharmaceutical formulations, methods of treatment using such formulations, formulations for use in treating patients and in particularly compositions, formulations, uses and methods for treating patients with neurological diseases wherein the formulation comprises an ...

Medicament for suppressing malignant tumor metastasis

Provided are a novel medicament for suppressing or preventing the metastasis of a malignant tumor such as carcinoma, a novel treatment or prevention method for suppressing or preventing the metastasis of a malignant tumor, etc. The medicament comprises a non-peptidic angiotensin type 2 receptor agonist as an active ingredient. In the medicament, the non-peptidic angiotensin type 2 receptor agonist may be, for example, a sulfonyl malonamide compound. The medicament may be a medicament for use in combination with an anticancer agent and/or an antitumor agent.

STABILIZED LIQUID FORMULATIONS CONTAINING PICOSULFATE

Stable liquid formulations containing picosulfate and magnesium citrate are provided. The formulations are useful to treat constipation or for the clearance of the bowel prior to X-ray examination, endoscopy or surgery. 1. A liquid formulation comprising:picosulfate; magnesium citrate, and an antioxidant.2. The liquid formulation of claim 1 , wherein the picosulfate is sodium picosulfate.3. The liquid formulation of claim 1 , wherein the picosulfate is present in the formulation at a concentration in the range from about 0.10 mM to about 0.15 mM.4. The liquid formulation claim 3 , wherein the picosulfate is present in the formulation at a concentration in the range from about 0.12 mM to about 0.14 mM.5. The liquid formulation of claim 1 , wherein the antioxidant is chosen from ascorbic acid or a salt or ester thereof claim 1 , butylated hydroxyanisole claim 1 , butylated hydroxytoluene claim 1 , histidine claim 1 , D-mannose claim 1 , propionic acid claim 1 , potassium metabisulfite claim 1 , propyl gallate claim 1 , sodium metabisulfite claim 1 , sodium sulfite claim 1 , sodium thiosulfate claim 1 , sulfur dioxide claim 1 , and α-tocopherol.6. The liquid formulation of claim 1 , wherein the antioxidant is chosen from ascorbic acid claim 1 , sodium ascorbate claim 1 , sodium metabisulfite claim 1 , potassium metabisulfite claim 1 , sodium sulfite claim 1 , sodium thiosulfate claim 1 , and sulfur dioxide.7. The liquid formulation of claim 1 , wherein the antioxidant is sodium metabisulfite.8. The liquid formulation of claim 1 , wherein the antioxidant is chosen from butylated hydroxyanisole claim 1 , butylated hydroxytoluene claim 1 , propyl gallate claim 1 , and α-tocopherol.9. The liquid formulation of claim 1 , wherein the antioxidant is present in the formulation at a concentration in the range from about 0.002 M to about 0.1 M.10. The liquid formulation of claim 9 , wherein the antioxidant is present in the formulation at a concentration in the range from about ...

Methods of Treating Meniere's Disease

Methods of treating a human patient suffering from Eustachian tube malfunctions are provided. A nasal spray or pharmaceutical composition containing a therapeutically effective amount of betahistine is administered to the patient. The nasal spray or pharmaceutical composition has particular applicability to alleviate the symptoms of Meniere's disease in persons suffering from abnormal Eustachian tube function, but also has an applicability to beneficially improve vascular oxygenation of the inner ear. 1. A nasal spray for treating Meniere's disease in a patient , comprising:a solution of betahistine or an acceptable pharmaceutical salt thereof formulated such that each spray of the solution contains a therapeutically effective amount of the betahistine or the acceptable pharmaceutical salt thereof to treat the secondary Meniere's disease.2. The nasal spray according to claim 1 , wherein the solution is formulated with the betahistine or the acceptable pharmaceutical salt thereof in a concentration in the range of 4.0 mg/ml to 8.0 mg/ml at pH 5.0.3. The nasal spray according to claim 2 , wherein the therapeutically effective amount of the betahistine or the acceptable pharmaceutical salt thereof is in a range of 0.2 mg to 5.0 mg.4. The nasal spray according to claim 3 , wherein the therapeutically effective amount of the betahistine or the acceptable pharmaceutical salt thereof is in a range of range 0.5 mg to 2.0 mg.5. A pharmaceutical composition comprising the nasal spray of and a pharmaceutically acceptable carrier.6. A method of treating a human patient suffering from Meniere's disease due to Eustachian tube malfunction where an imbalance exists of the autonomic nervous system whereby the cervical sympathetic is activated claim 1 , the method comprising administering to the patient the nasal spray of .7. The method according to claim 6 , wherein said administering step is performed by spraying the nasal spray into each nostril of the patient.8. A method of ...

NON-MUCOADHESIVE FILM DOSAGE FORMS

Orally disintegrating film dosage forms for delivering active pharmaceutical agents, methods of formulating the dosage forms to retard absorption through the oral mucosa, and methods of using the dosage forms for the treatment of various medical conditions are provided. 1) A non-mucoadhesive orally disintegrating film , able to disintegrate upon contact with saliva in the buccal cavity within about sixty seconds , comprising donepezil or a pharmaceutically acceptable salt thereof in combination with a hydrophilic binder and a water-soluble diluent , wherein:a) said film is characterized predominantly by gastrointestinal absorption when placed on the tongue, allowed to disintegrate, and subsequently swallowed;b) said film comprises from about 2.5 to about 20 mg of donepezil or a pharmaceutically acceptable salt thereof;c) said donepezil hydrochloride is present in an amount of from about 0.05% to about 50% (w/w), based on the total weight of the film,{'sub': 'max', 'd) said film has a Tof from about 3 to about 4 hours, and'}e) said donepezil or pharmaceutically acceptable salt thereof has an absolute bioavailability in said film of about 100%.2) The film of wherein said donepezil is present as amorphous donepezil hydrochloride.3) The film of characterized by greater than 95% gastrointestinal absorption.4) The film of wherein said film comprises from about 40% to about 80% (w/w) of one or more ingredients that constitute a hydrophilic binder and a water soluble diluent.5) The film of claim 1 , further comprising from about 5 to about 25 wt. % of an aminoalkyl methacrylate copolymer claim 1 , having a molecular weight of from about 120 claim 1 ,000 to about 180 claim 1 ,000.6) The film of further comprising from about 10 to about 40 wt. % of a cyclodextrin or derivative thereof.7) The film of comprising from about 0.5 to about 2.0 wt. % citric acid.8) The film of comprising amorphous donepezil hydrochloride claim 1 , made by a process comprising:a) dissolving donepezil ...

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

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

PHARMACEUTICAL COMPOSITIONS

A composition of an antitussive, a decongestant, or an antihistamine to treat upper respiratory and oral pharyngeal congestion and related symptoms in a patient. 1. A pharmaceutical composition for alleviating symptoms of upper respiratory and oral-pharyngeal congestion in a subject , the composition comprising:a first active ingredient selected from the group consisting of chlophedianol hydrochloride, chlorcyclizine hydrochloride, phenylephrine hydrochloride, dextromethorphan hydrobromide and thonzylamine hydrochloride; anda second active ingredient selected from the group consisting of pyrilamine maleate, Pseudoephedrine Hydrochloride, chlorcyclizine hydrochloride, dexbrompheniramine maleate, diphenhydramine hydrochloride, diphenhydramine citrate, chlorpheniramine maleate, dexchlorpheniramine maleate, doxylamine succinate, triprolidine hydrochloride, dextromethorphan hydrobromide, bromopheniramine maleate, Guaifenesin, Codeine phosphate, and thonzylamine hydrochloride.2. The pharmaceutical composition of claim 1 , further comprising a third active ingredient selected from the group consisting of pyrilamine maleate claim 1 , Pseudoephedrine Hydrochloride claim 1 , chlorcyclizine hydrochloride claim 1 , dexbrompheniramine maleate claim 1 , diphenhydramine hydrochloride claim 1 , diphenhydramine citrate claim 1 , chlorpheniramine maleate claim 1 , dexchlorpheniramine maleate claim 1 , doxylamine succinate claim 1 , triprolidine hydrochloride claim 1 , dextromethorphan hydrobromide claim 1 , bromopheniramine maleate claim 1 , Guaifenesin claim 1 , Codeine phosphate claim 1 , and thonzylamine hydrochloride.3. The pharmaceutical composition of claim 1 , wherein the first active ingredient is present at a range of 9.375 mg to 100 mg.4. The pharmaceutical composition of claim 1 , wherein the second active ingredient is present at a range of 1 mg to 100 mg.5. The pharmaceutical composition of claim 2 , wherein third active ingredient is present at a range of 1 mg to 500 mg ...

MICRO- AND NANO-QUANTITY SLEEP ENHANCING NUTRIENT COMPOSITION AND METHOD OF ENHANCING CENTRAL NERVOUS SYSTEM PROTEIN CLEARANCE USING SAME

The present invention relates to a dietary supplement, composition, nutraceutical, and/or system for inducing or treating biological responses or conditions (namely sleep or sleep disorders) which utilize ultra-low dosage amounts of vitamins, minerals, amino acids, co-enzymes, stimulants, and/or similar ingredients in a highly bio-active delivery system which bypasses first pass metabolism. In particular, the present invention relates to a nutraceutical composition/formulation which substantially bypasses first pass metabolism and such as, but not limited to, activation of the glymphatic system to facilitate clearance of neuronal metabolites from the CSF and interstitial fluids in the brain. 1. A nutraceutical composition comprising micro- or nano-quantities of the following ingredients in an oral preparation suitable for oral administration to a person in need thereof , the ingredients comprising , in combination at least one mineral or salts thereof selected from the group consisting of magnesium , sodium , potassium , calcium , chromium , copper , iron and zinc , at least one vitamin selected from the group consisting of A , B1 , B2 , B3 , B6 , B12 , folic acid , C , D3 , E and H , at least one antioxidant , and at least one amino acid.2. The nutraceutical composition of claim 1 , wherein the at least one mineral further comprises a chloride salt claim 1 , a carbonate claim 1 , an ascorbate claim 1 , a nitrite claim 1 , a picolinate claim 1 , a polynicotinate claim 1 , a benzoate or an iodide.3. The nutraceutical composition of claim 1 , wherein the at least one mineral further comprises claim 1 , in combination claim 1 , magnesium chloride claim 1 , sodium ascorbate claim 1 , sodium nitrite claim 1 , potassium carbonate claim 1 , calcium ascorbate claim 1 , potassium benzoate claim 1 , chromium picolinate claim 1 , chromium polynicotinate claim 1 , potassium sorbate claim 1 , potassium iodide claim 1 , calcium carbonate claim 1 , iron claim 1 , copper and zinc.4 ...

Pharmaceutical Compositions

The invention relates to aqueous suspension pharmaceutical compositions of poorly water soluble drugs, wherein said drugs are selected from compounds of formula I 2. The process of claim 1 , further comprising reducing the particle size of the active ingredient.3. The process of claim 2 , wherein the particle size of the active ingredient is reduced in the aqueous vehicle.4. The process of claim 3 , wherein the particle size is reduced using precipitation claim 3 , wet ball milling claim 3 , or high pressure homogenisation.5. The process of claim 3 , wherein the particle size is reduced using high shear fluid processing.6. The process of claim 2 , wherein the particle size of the active ingredient is reduced in the dry form prior to suspension in the aqueous vehicle.7. The process of claim 6 , wherein the particle size is reduced using ball milling claim 6 , jet milling claim 6 , or roller milling.8. The process of claim 1 , wherein the active ingredient is:(S)—N-(4-Aminomethyl-benzyl)-2-[(R)-3-(4-ethoxy-phenyl)-2-propionylamino-propionylamino]-3-phenyl-propionamide;N—[(R)-1-[(S)-1-(4-Aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide;{(R)-1-[(S)-1-(4-Aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-cyclohexyl-ethylamino}-acetic acid;(S)—N-(4-Aminomethyl-3-fluoro-benzyl)-2-[(R)-3-(4-ethoxy-phenyl)-2-propionylamino-propionylamino]-3-phenyl-propionamide;(S)—N-(4-Aminomethyl-2-chloro-benzyl)-2-[(R)-3-(4-ethoxy-phenyl)-2-propionylamino-propionylamino]-3-phenyl-propionamide;(S)—N-(4-Aminomethyl-benzyl)-3-(3,4-dichloro-phenyl)-2-[(R)-3-(4-ethoxy-phenyl)-2-propionylamino-propionylamino]-propionamide;(S)—N-(4-Aminomethyl-3-chloro-benzyl)-2-[(R)-3-(4-ethoxy-phenyl)-2-propionylamino-propionylamino]-3-phenyl-propionamide;(S)—N-(4-Aminomethyl-benzyl)-2-{[(R)-3-(4-ethoxy-phenyl)-2-propionylamino-propionyl]-methyl-amino}-3-phenyl-propionamide;({(R)-1-[(S)-1-(4-Aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-cyclohexyl-ethyl}- ...

ATAZANAVIR SULFATE FORMULATIONS WITH IMPROVED Ph EFFECT

Disclosed are compressed tablets containing atazanavir sulfate and an acidifying agent, optionally with another active agent, e.g., anti-HIV agents, and optionally with precipitation retardant agents. Also disclosed are processes for making the tablets, and methods of treating HIV. 1. A compressed tablet comprising atazanavir sulfate and an acidifying agent selected from citric acid , tartaric acid , fumaric acid , ascorbic acid and mixtures thereof.2. A compressed tablet according to further comprising a precipitation retardant agent.3. A compressed tablet according to wherein the precipitation retardant agent is selected from the group consisting of polyvinylpyrrolidone claim 1 , polyvinylpyrrolidone-vinyl acetate claim 1 , hydroxypropyl cellulose claim 1 , hydoxypropyl methylcellulose claim 1 , and hydroxypropylmethylcellulose acetate succinate and mixtures thereof.4. A compressed tablet according to comprising at least one other agent having anti-HIV activity or the ability to enhance the pharmacokinetics of the atazanavir.5. A compressed tablet according to wherein the other agent is ritonavir.6. A compressed tablet according to wherein the other agent is cobicistat.7. A compressed tablet comprising atazanavir sulphate claim 4 , cobicistat claim 4 , an acidifying agent and a precipitation retardant agent.8. A compressed tablet according to wherein the acidifying agent is selected from citric acid claim 7 , tartaric acid claim 7 , fumaric acid claim 7 , ascorbic acid and mixtures thereof.9. A compressed tablet according to wherein the acidifying agent is present in an amount of 10-30 w/w %.10. A compressed tablet according to further comprising a precipitation retardation agent selected from polyvinylpyrrolidone claim 8 , polyvinylpyrrolidone-vinyl acetate claim 8 , hydroxypropyl cellulose claim 8 , hydoxypropyl methylcellulose claim 8 , and hydroxypropylmethylcellulose acetate succinate and mixtures thereof.11. A compressed tablet according to wherein the ...

Modified Release Formulations Containing Drug - Ion Exchange Resin Complexes

An aqueous liquid suspension containing a coated drug-ion exchange resin complex comprising a core composed of an amphetamine complexed with a pharmaceutically acceptable ion-exchange resin and an uncoated amphetamine-ion exchange resin complex is provided. The coated amphetamine-ion exchange resin complex is in admixture with a polymer to form a matrix. Methods of making the coated complex and the liquid suspension are described. 1. A product comprising an aqueous pharmaceutical liquid suspension suitable for oral ingestion comprising:(i) a particulate drug-ion exchange resin complex-matrix comprising a pharmaceutically acceptable drug bound to a pharmaceutically acceptable water insoluble ion exchange resin to form said particulate drug-ion exchange resin complex, said particulate drug-ion exchange resin complex being in a matrix with a water insoluble polymer or copolymer or a hydrophilic polymer, which polymer or copolymer is present in an amount of about 3% to about 30% by weight, based on the weight of said particulate drug-ion exchange resin complex-matrix, and (a) about 75% w/w to about 90% w/w polyvinylacetate polymer;', '(b) a stabilizer comprising polyvinylpyrrolidone, and', '(c) about 2.5% w/w to about 20% w/w of plasticizer effective to enhance the tensile strength of said cured barrier coating, whereby said barrier coating is over the particulate drug-ion exchange resin complex-matrix and provides a modified release profile to said pharmaceutically acceptable drug in said particulate drug-ion exchange resin complex-matrix., '(ii) a cured, high tensile strength, water permeable, water insoluble, non-ionic polymeric diffusion modified release barrier coating over said particulate drug-ion exchange resin complex defined in (i), said cured barrier coating applied as an aqueous dispersion, wherein said cured barrier coating comprises2. The product according to claim 1 , wherein said cured modified release barrier coating has an elongation factor of between ...

COMPOUNDS AFFECTING PIGMENT PRODUCTION AND METHODS FOR TREATMENT OF BACTERIAL DISEASES

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II): 3. A composition comprising the compound according to claim 1 , the derivatives thereof claim 1 , and a pharmaceutical carrier salt claim 1 , ester claim 1 , expicient claim 1 , vehicle claim 1 , prodrug claim 1 , solvent claim 1 , and diluent claim 1 , or any combination thereof.4. A composition comprising the compound according to claim 2 , the derivatives thereof claim 2 , and a pharmaceutical carrier salt claim 2 , ester claim 2 , excipient claim 2 , vehicle claim 2 , prodrug claim 2 , solvent claim 2 , and diluent claim 2 , or any combination thereof.7. The method of claim 5 , wherein the microbial infections comprise staphylococcal infection.8Staphylococcus aureus.. The method of claim 5 , wherein the method reduces the production of pigment in9. The method of claim 5 , wherein the microbial infections and/or related diseases or conditions comprise infections of the skin and soft tissue claim 5 , bone and joint claim 5 , surgical wound claim 5 , indwelling devices claim 5 , lung and heart valves.10. The method of claim 5 , wherein said subject is a mammal.11. The method of claim 5 , wherein said subject is human. The present application claims priority from a U.S. provisional patent application Ser. No. 62/535,540 filed Jul. 21, 2017, and the disclosure of which is incorporated by reference in its entirety.The present invention relates to compounds and derivatives thereof, composition comprising said compounds and/or derivatives, and methods for treating microbial infections and/or related diseases or conditions. More specifically, the present compounds, derivatives, composition comprising thereof, and methods are for bacterial infections.is a major ...

Composition for the management of nausea and vomiting

A pharmaceutical dosage system comprising (a) an effective amount of one or more of Doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof; (b) an effective amount of one or more of (i) Pyridoxine, (ii) an analog thereof, (iii) a derivative thereof, (iv) a prodrug thereof, (v) a metabolite thereof and (vi) a salt of any of (i)-(v); and (c) an effective amount of one or more compounds of formula (I) 2. The system of claim 1 , wherein R is a hydroxyl group.3. The system of claim 1 , wherein R is a phosphate group.5. The system of claim 1 , wherein said system comprises from about 5 to about 35 mg of Doxylamine and/or a pharmaceutically acceptable salt thereof.6. The system of claim 5 , wherein said system comprises from about 5 to about 30 mg of Doxylamine and/or a pharmaceutically acceptable salt thereof.7. The system of claim 6 , wherein said system comprises from about 5 to about 20 mg of Doxylamine and/or a pharmaceutically acceptable salt thereof.8. The system of claim 7 , wherein said system comprises about 20 mg of Doxylamine and/or a salt thereof.9. The system of claim 1 , wherein said system comprises Doxylamine succinate.10. The system of claim 1 , wherein said system comprises from about 5 to about 70 mg of (i) Pyridoxine (ii) a metabolite thereof and/or (iii) a pharmaceutically acceptable salt of (i) or (ii).11. The system of claim 10 , wherein said system comprises from about 5 to about 50 mg of (i) Pyridoxine (ii) a metabolite thereof and/or (iii) a pharmaceutically acceptable salt of (i) or (ii).12. The system of claim 11 , wherein said system comprises from about 5 to about 30 mg of (i) Pyridoxine (ii) a metabolite thereof and/or (iii) a pharmaceutically acceptable salt of (i) or (ii).13. The system of claim 12 , wherein said system comprises from about 5 mg to about 20 mg of (i) Pyridoxine (ii) a metabolite thereof and/or (iii) a pharmaceutically acceptable salt of (i) or (ii).14. The system ...

Composition for the management of nausea and vomiting

A pharmaceutical dosage system comprising (a) an effective amount of one or more of Doxylamine, an analog thereof, a derivative thereof, a prodrug thereof, a metabolite thereof and/or a salt thereof; (b) an effective amount of one or more of (i) Pyridoxine, (ii) an analog thereof, (iii) a derivative thereof, (iv) a prodrug thereof, (v) a metabolite thereof and (vi) a salt of any of (i)-(v); and (c) an effective amount of one or more compounds of formula (I) 130-. (canceled)32. The method of claim 31 , wherein said subject is a pregnant female and said method is for alleviating the symptoms of nausea and vomiting of human pregnancy (NVP) in said subject.33. The method of claim 31 , wherein R is a hydroxyl group.34. The method of claim 31 , wherein R is a phosphate group.36. The method of claim 31 , wherein said system comprises from about 5 to about 35 mg of Doxylamine and/or a pharmaceutically acceptable salt thereof.37. The method of claim 36 , wherein said system comprises from about 5 to about 30 mg of Doxylamine and/or a pharmaceutically acceptable salt thereof.38. The method of claim 37 , wherein said system comprises from about 5 to about 20 mg of Doxylamine and/or a pharmaceutically acceptable salt thereof.39. The method of claim 38 , wherein said system comprises about 20 mg of Doxylamine and/or a salt thereof.40. The method of claim 31 , wherein said system comprises Doxylamine succinate.41. The method of claim 31 , wherein said system comprises from about 5 to about 70 mg of (i) Pyridoxine (ii) a metabolite thereof and/or (iii) a pharmaceutically acceptable salt of (i) or (ii).42. The method of claim 41 , wherein said system comprises from about 5 to about 50 mg of (i) Pyridoxine (ii) a metabolite thereof and/or (iii) a pharmaceutically acceptable salt of (i) or (ii).43. The method of claim 42 , wherein said system comprises from about 5 to about 30 mg of (i) Pyridoxine (ii) a metabolite thereof and/or (iii) a pharmaceutically acceptable salt of (i) or (ii ...

ORAL LIQUID CONCENTRATE COMPRISING BROMPHENIRAMINE, PSEUDOEPHEDRINE AND DEXTROMETHORPHAN

There is provided a liquid oral concentrate comprising combination of dextromethorphan, bromrpheniramine and pseudoephedrine or pharmaceutically acceptable salts thereof. The invention further provides process for preparation of such compositions. 1. An oral ready-to-use pharmaceutical liquid composition comprising more than 0.04% w/v of brompheniramine , 0.60% w/v of pseudoephedrine and 0.20% w/v of dextromethorphan or pharmaceutically acceptable salts thereof.2. The oral ready-to-use pharmaceutical liquid composition of claim 1 , wherein the composition is free of alcohol.3. The oral ready-to-use pharmaceutical liquid composition of claim 1 , wherein the composition is free of sugar.4. The oral ready-to-use pharmaceutical liquid composition of claim 1 , wherein the composition is in the form of a liquid concentrate.5. The oral ready-to-use pharmaceutical liquid composition of claim 1 , wherein the composition comprises hydrobromide salt of dextromethorphan claim 1 , maleate salt of brompheniramine claim 1 , and hydrochloride salt of pseudoephedrine.6. The oral ready-to-use pharmaceutical liquid composition of claim 1 , wherein the composition is taste-masked.7. The oral ready-to-use pharmaceutical liquid composition of claim 1 , wherein the composition is in the form of solution claim 1 , syrup claim 1 , suspension claim 1 , or emulsion.8. The oral ready-to-use pharmaceutical liquid composition of claim 1 , wherein the composition retains at least 90% w/w of total potency of brompheniramine claim 1 , pseudoephedrine claim 1 , and dextromethorphan or pharmaceutically acceptable salts thereof after storage at 25° C. and 40% relative humidity or 25° C. and 40% relative humidity for at least 3 months.9. An oral ready-to-use pharmaceutical liquid concentrate comprising about 0.05% w/v of brompheniramine claim 1 , 0.75% w/v of pseudoephedrine and 0.25% w/v of dextromethorphan or pharmaceutically acceptable salts thereof claim 1 , wherein the composition is free of ...

PHARMACEUTICAL COMPOSITION COMPRISING BETAHISTINE

The present disclosure relates to a pharmaceutical composition comprising as active substance betahistine or a pharmaceutically acceptable salt thereof, for use in the treatment of otological or neurological disorders in a human subject by intranasal application. 159-. (canceled)60. A pharmaceutical composition for intranasal delivery to a human patient , comprising a solution or suspension of therapeutically effective amount of betahistine dihydrochloride and hydroxypropyl methylcellulose as a viscosity enhancing agent.61. The pharmaceutical composition of claim 60 , wherein after a single intranasal administration to a human claim 60 , the Cof betahistine ranges from 80-125% of about 3000 pg/mL for a 5 mg betahistine dihydrochloride dose.62. The pharmaceutical composition of claim 60 , wherein after a single intranasal administration to a human claim 60 , the Cof betahistine ranges from 80-125% of about 8000 pg/mL for a 10 mg betahistine dihydrochloride dose.63. The pharmaceutical composition of claim 60 , wherein after a single intranasal administration to a human claim 60 , the AUCof betahistine ranges from about 80%-125% of about 1300 pg*hr/mL for a 5 mg betahistine dihydrochloride dose.64. The pharmaceutical composition of claim 60 , wherein after a single intranasal administration to a human claim 60 , the AUCof betahistine ranges from about 80%-125% of about 3000 pg*hr/mL for a 20 mg betahistine dihydrochloride dose.65. The pharmaceutical composition of claim 60 , wherein the tof betahistine in human plasma after single intranasal dose of the composition is about 0.08 h or greater.66. The pharmaceutical composition of claim 60 , further comprising one or more moisturizing agent.67. The pharmaceutical composition of claim 60 , wherein the one or more moisturizing agent is selected from the group consisting of glycerin claim 60 , ethylene glycol claim 60 , propylene glycol claim 60 , propylene glycol 400 claim 60 , hexalene glycol claim 60 , butylene glycol ...

Amphiphilic thiol compounds and uses thereof

Provided herein are, inter alia, amphiphilic thiol compounds and methods of using the same for the purpose of depalmitoylating proteins in cellular membranes (e.g., plasma membranes). The compounds provided herein include an amphiphilic tail, which enables them to associate with a cellular membrane and depalmitoylate (cleave native S-palmitoyl groups from) a protein in said membrane by native chemical ligation thereby triggering the protein's release from the plasma membrane. The compounds (amphiphilic thiol compounds of formula (I), (II), (III)) are, inter alia, useful for the treatment of diseases caused or associated with aberrant depalmitoylation of certain proteins (e.g., HRas, EGFR).

SUBSTITUTED DIHYDROINDENE-4-CARBOXAMIDES AND ANALOGS THEREOF, AND METHODS USING SAME

The present invention includes novel substituted bicyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infections in a patient. In certain embodiments, the compounds and compositions of the invention are capsid inhibitors. 2. The compound of claim 1 , wherein each occurrence of Ror Ris independently selected from the group consisting of —(CH)-(optionally substituted heteroaryl) claim 1 , —(CH)-(optionally substituted heterocyclyl) claim 1 , and —(CH)-(optionally substituted aryl).3. The compound of claim 1 , wherein each occurrence of optionally substituted alkyl claim 1 , optionally substituted heterocyclyl claim 1 , or optionally substituted cycloalkyl is independently optionally substituted with at least one substituent selected from the group consisting of C-Calkyl claim 1 , halo claim 1 , —OR claim 1 , optionally substituted phenyl claim 1 , optionally substituted heteroaryl claim 1 , optionally substituted heterocyclyl claim 1 , —N(R)C(═O)R claim 1 , —C(═O)NRR claim 1 , and —N(R)(R) claim 1 , wherein each occurrence of Ris independently H claim 1 , optionally substituted C-Calkyl claim 1 , optionally substituted C-Ccycloalkyl claim 1 , optionally substituted aryl claim 1 , or optionally substituted heteroaryl claim 1 , or two Rgroups combine with the N to which they are bound to form a heterocycle.4. The compound of claim 1 , wherein each occurrence of optionally substituted aryl or optionally substituted heteroaryl is independently optionally substituted with at least one substituent selected from the group consisting of C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Chaloalkoxy claim 1 , halo claim 1 , —CN claim 1 , —OR claim 1 , —N(R)(R) claim 1 , —NO claim 1 , —S(═O)N(R)(R) claim 1 , acyl claim 1 , and C-Calkoxycarbonyl claim 1 , wherein each occurrence of Ris independently H claim 1 , C-Calkyl claim 1 , or C-Ccycloalkyl.5. The compound of claim 1 , wherein each occurrence of optionally ...

Pharmaceutical depot for n-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl)-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide

A pharmaceutical depot comprising (i) N-{5-[(cyclopropylamino)carbonyl]-2-methylphenyl}-3-fluoro-4-(pyridin-2-ylmethoxy)benzamide, or a pharmaceutically-acceptable salt thereof, as a pharmaceutical agent (PA) and (ii) a polymer which degrades to create an acidic microclimate, wherein the PA is released from the polymer upon polymer degradation.

PROTEASE INHIBITORS HAVING ENHANCED FEATURES

Provided herein (among other things) are protease inhibitor compounds having enhanced features, along with methods for administering such compounds. For example, the subject compounds can be administered without concomitant administration of a CYP3A4 inhibitor, have increased therapeutic index and/or increased potency, and are low-resistance inducing in nature. 1. A method comprising administering an HIV protease inhibitor conjugate to an individual infected with HIV , wherein the HIV protease inhibitor conjugate has an increased therapeutic index and/or increased potency relative to the HIV protease inhibitor in unconjugated form.2. The method of claim 1 , wherein the dose administered is (i) different than the dose of the corresponding HIV protease inhibitor in unconjugated form claim 1 , when compared on a molar basis claim 1 , and (ii) retains at least the same (or substantially the same) HIV protease inhibitor activity on a molar basis claim 1 , when evaluated in a suitable model or individual.3. The method of claim 2 , wherein the dose administered is less than the dose of the corresponding HIV protease inhibitor in unconjugated form.4. A method of increasing the potency of a small drug molecule by covalently attaching to the small molecule drug one or more water-soluble oligomers.5. The method of claim 4 , wherein the small molecule drug is an HIV protease inhibitor.6. A method of administering a potent protease inhibitor therapy to an individual infected with a virus claim 4 , wherein the potent protease inhibitor therapy does not include co-administration of a CYP3A4 inhibitor.7. The method of claim 6 , wherein the potent protease inhibitor is administered in a CYP3A4-competent biological system.8. A method comprising administering an HIV protease inhibitor conjugate as a protease inhibitor monotherapy to a biological system infected with HIV claim 6 , wherein: (i) in a biological model in which the HIV protease inhibitor conjugate is periodically added in ...

SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS

The present invention relates to Substituted Quinolizine Derivatives of Formula (I): 115.-. (canceled)17. A pharmaceutical composition comprising an effective amount of a compound according to claim 16 , or a pharmaceutically acceptable salt thereof claim 16 , and a pharmaceutically acceptable carrier.18. A method for the inhibition of HIV integrase in a subject in need thereof which comprises administering to the subject an effective amount of the compound according claim 16 , or a pharmaceutically acceptable salt thereof.19. A method for the treatment of infection by HIV or for the treatment of AIDS in a subject in need thereof claim 16 , which comprises administering to the subject an effective amount of the compound according to claim 16 , or a pharmaceutically acceptable salt thereof.20. (canceled)21. The pharmaceutical composition of claim 17 , further comprising one or more additional therapeutic agents selected from claim 17 , lamivudine claim 17 , abacavir claim 17 , ritonavir claim 17 , darunavir claim 17 , atazanavir claim 17 , emtricitabine claim 17 , tenofovir claim 17 , rilpivirine and lopinavir.22. The method of claim 17 , further comprising administering to the subject one or more additional therapeutic agents selected from claim 17 , abacavir claim 17 , lamivudine claim 17 , ritonavir and lopinavir claim 17 , wherein the amounts administered of the compound of . The present invention relates to Substituted Quinolizine Derivatives, compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.A retrovirus designated human immunodeficiency virus (HIV), particularly the strains known as HIV type-1 (HIV-1) virus and type-2 (HIV-2) virus, is the etiological agent of the complex disease that includes progressive destruction of the immune system (acquired immune deficiency syndrome; AIDS) and degeneration of the central and ...

Combined herbal and pharmaceutical composition and method

An herbal combination composition can include, herbal extracts, including combinations of: , and ; pharmaceutical compositions, including combinations of: Brompheniramine Maleate, Pseudoephedrine, dextromethorphan, guaifenesin, acetaminophen, phenylephrine, diphenhydramine. The herbal combination composition can further include: polyethylene glycol; propylene glycol; poloxamer 407; ethylenediaminetetraacetic acid; methyl paraben; potassium sorbate; propyl paraben; xanthan gum; sodium citrate, citric acid; anhydrous citric acid; and purified acetate buffered water. Also disclosed is a method for manufacture of an herbal combination composition, including dissolving herbal extracts, adding poloxamer, adding pharmaceutical compositions, adding acetate buffer, adding xanthan gum gel, adding acetate buffer. 1. An herbal combination composition , comprising: [{'i': 'Viola odorata;'}, {'i': 'Chamomile', '; and'}, {'i': 'Ocimum tenuiflorum', '; and'}], 'a) an herbal extract combination, comprising Guaifenesin in a range of 200-1200 mg; and', 'Dextromethorphan in a range of a 5-80 mg., 'b) a pharmaceutical combination composition, comprising2. The herbal combination composition of claim 1 , wherein the pharmaceutical combination composition further comprises:Brompheniramine maleate in a range of 1 to 12 mg.3. The herbal combination composition of claim 1 , wherein the pharmaceutical combination composition further comprises:Pseudoephedrine in a range of 15-120 mg.4. The herbal combination composition of claim 1 , wherein the herbal extract combination further comprises:{'i': 'Centella asiatica.'}5. The herbal combination composition of claim 4 , wherein the herbal extract combination comprises:{'i': 'Centella asiatica', 'a) the in a range of 0.25% to 1.5% by weight of the herbal combination composition;'}{'i': 'Viola odorata', 'b) the in a range of 0.25%-1.5% by weight of the herbal combination composition;'}{'i': 'Chamomile', 'c) the in a range of 0.25% to 1.0% by weight of ...

2-BENZOYLAMINOBENZAMIDE DERIVATIVES AS BCL-3 INHIBITORS

The invention relates to a compound of general formula (I): 2. A method according to claim 1 , wherein Ris halo claim 1 , nitro claim 1 , Calkyl claim 1 , Chaloalkyl or OR.3. A method according to claim 1 , wherein Ris hydrogen claim 1 , or methyl or ethyl claim 1 , either of which may optionally be substituted by one or more halo substituents.4. A method according to claim 1 , wherein Ris halo claim 1 , nitro claim 1 , methyl claim 1 , trifluoromethyl claim 1 , OH claim 1 , methoxy or trifluoromethoxy.5. A method according to claim 1 , wherein m is 1 or 2.6. A method according to claim 1 , wherein at least one Ris fluoro.7. A method according to claim 6 , wherein Ris 2-fluoro.8. A method according to claim 1 , wherein at least one Ris OR.9. A method according to claim 8 , wherein Ris Calkyl.10. A method according to claim 9 , wherein Ris methyl.11. A method according to claim 1 , wherein Ris morpholinyl.12. A method according to claim 1 , wherein p is 2 or 3.13. A method according to claim 1 , wherein Ris Calkyl or OR.14. A method according to claim 13 , wherein Ris methyl or methoxy.15. A method according to claim 1 , wherein n is 0 or 1.17. The method of claim 1 , wherein the cancer is leukaemia or lymphoma.18. The method of claim 1 , wherein the cancer is anaplastic large cell lymphoma (ALCLs) claim 1 , classic Hodgkin lymphoma (cHL) claim 1 , non-Hodgkin's lymphoma or solid tumour cancer.19. The method of claim 18 , wherein the cancer is a solid tumour cancer selected from the group consisting of: breast cancer claim 18 , melanoma claim 18 , lung cancer claim 18 , pancreatic cancer claim 18 , oesophageal cancer claim 18 , colorectal cancer claim 18 , nasopharyngeal carcinoma or hepatocarcinoma.20. The method according to claim 1 , wherein the treatment comprises the treatment or prevention of metastasis in cancers.21. The method according to claim 19 , wherein the cancer is breast cancer.22. The method according to claim 21 , wherein the cancer is triple ...

PARASITE CONTROL AGENT FOR PARASITICIDE

A parasite-control or parasiticide agent that exhibits excellent effects of controlling or expelling parasites, particularly endoparasites and that can be used safely contains at least one selected from the group consisting of compounds represented by formula (I) and salts thereof as an active ingredient thereof 2. The parasite-control or parasiticide agent according to claim 1 , wherein Rand Reach indenpendently represents an unsubstituted or substituted C1-6 alkyl group claim 1 , and{'sup': '5', 'Rrepresents an unsubstituted or substituted C6-10 aryl group, an unsubstituted or substituted heteroaryl group, or an unsubstituted or substituted C1-6 alkylaminocarbonyl group.'}3. The parasite-control or parasiticide agent according to claim 1 , wherein Rrepresents an unsubstituted or substituted C1-6 alkyl group claim 1 , and Rrepresents a hydrogen atom.4. The parasite-control or parasiticide agent according to claim 1 , wherein A represents a nitrogen atom.5. The parasite-control or parasiticide agent according to claim 1 , wherein A represents a group represented by CR claim 1 , and Rrepresents a hydrogen atom.6. The parasite-control or parasiticide agent according to claim 1 , wherein the parasite-control or parasiticide agent targets an endoparasite.7. A method for controlling or expelling an endoparasite that is parasitic in warm-blooded animals or fishes claim 6 , comprising administering a parasite-control or parasiticide agent of to the warm-blooded animals or the fishes at an effective dose.8. The parasite-control or parasiticide agent according to claim 6 , wherein the parasite-control or parasiticide agent targets nematodes.9. A method for controlling or expelling nematodes that are parasitic in warm-blooded animals or fishes claim 8 , comprising administering a parasite-control or parasiticide agent of to the warm-blooded animals or the fishes at an effective dose. The present invention relates to a composition useful as a medicine or an animal drug, and ...

Nmda antagonist prodrugs

Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.

ANTIMICROBIAL COMPOUNDS AND NANOSTRUCTURES

The present disclosure provides compounds and nanostructures having one or more quaternary ammonium salts, compositions including the compounds and nanostructures, and methods useful for treating conditions using the compounds, nanostructures, and compositions. In at least one aspect, a compound is represented by formula (I): 3. The nanorod of claim 1 , wherein the second compound comprises a pyridyl disulfide moiety.5. The nanorod of claim 1 , wherein Q is chloro.8. The nanorod of claim 1 , wherein the first compound is a pharmaceutically acceptable salt of a halide.9. The nanorod of claim 8 , wherein the salt is an iodo salt.10. The nanorod of claim 1 , wherein a ratio of the integer n to the integer m is from 5:1 to 15:1.11. The nanorod of claim 1 , wherein the nanorod has a diameter from about 10 nm to about 20 nm.12. The nanorod of claim 1 , wherein the nanorod has a length from about 1 micron to about 2 microns.14. A gel comprising the nanorod of .15. The gel of claim 14 , wherein the gel is an aqueous gel and the gel comprises from 2 wt % to 16 wt % nanorod claim 14 , based on the total weight of the gel.18. The nanoworm of claim 16 , wherein the second compound comprises a pyridyl disulfide moiety.20. The nanoworm of claim 16 , wherein Q is chloro.23. The nanoworm of claim 16 , wherein the first compound is a pharmaceutically acceptable salt of a halide.24. The nanoworm of claim 23 , wherein the salt is an iodo salt.25. The nanoworm of claim 16 , wherein a ratio of the integer n to the integer m is from 5:1 to 15:1.26. A gel comprising the nanoworm of .27. The gel of claim 26 , wherein the gel is an aqueous gel and the gel comprises from 1 wt % to 8 wt % nanoworm claim 26 , based on the total weight of the gel. This application is continuation application of U.S. non-provisional patent application Ser. No. 15/838,751, filed Dec. 12, 2017, which claims priority to and the benefit of U.S. provisional patent application Ser. No. 62/521,040 filed Jun. 16, 2017. ...

Phenylcyclopropylamine derivatives and their medical use

The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.

Methods for Detecting and Treating Rhinovirus Infection

The invention provides a method for evaluating the activity of an agent for treating rhinovirus infection or a symptom thereof, a method of detecting or monitoring rhinovirus infection, and a method of treating rhinovirus infection or a symptom thereof. Various embodiments comprise measuring expression of (i) one or more genes selected from the group consisting of CRY2, B3GAT3, C10ORF95, and BATF3, and (ii) one or more genes selected from the group consisting of RNFT2, BTG4, PSD3, CAPN9, SULT1E1, HEY1, LRRC36, RAB3B, ALDH3B1, FAM134B, FAS, PLSCR1, CLEC2B, HAS2, MX1, SP110, GBP1, IFIT3, IFIT1, CXCL9, CXCL10, and CXCL11, from at least one biological sample to produce a gene expression profile, and comparing the gene expression profile to a reference gene expression profile. Systems, computer readable media, compositions, and methods for maintaining or improving respiratory health also are provided.

METHODS AND COMPOSITIONS FOR TREATING VIRAL OR VIRALLY-INDUCED CONDITIONS

Provided are methods and compositions for the prevention and/or treatment of viral conditions, virally-induced conditions and inflammatory conditions. The methods can comprise administering to a subject a viral inducing agent with an antiviral agent, and optionally an additional agent. The viral inducing agent can be a HDAC inhibitor administered orally. 1. A method for treating and/or preventing a viral or virally-induced condition comprising administering a HDAC inhibitor and an antiviral agent wherein the viral or virally-induced condition is caused by a DNA virus and the HDAC inhibitor is administered at dose of less than 2 mg/kg per dose.2. The method of claim 1 , wherein the HDAC inhibitor is CHR-3996.3. The method of claim 1 , wherein the DNA virus is a herpesvirus.4. The method of claim 1 , wherein the DNA virus is an Epstein-Barr virus.5. The method of claim 1 , wherein the DNA virus is a cytomegalovirus.6. The method of claim 1 , wherein the DNA virus is a varicella zoster virus.7. The method of claim 1 , wherein the virally-induced condition is a lymphoma claim 1 , chronic lymphocytic leukemia claim 1 , nasopharyngeal carcinoma claim 1 , gastric cancer claim 1 , Kaposi's sarcoma claim 1 , rheumatoid arthritis claim 1 , systemic lupus erythematosus claim 1 , or multiple sclerosis.8. The method of claim 1 , wherein the antiviral agent is acyclovir (ACV) claim 1 , ganciclovir (GCV) claim 1 , valganciclovir claim 1 , famciclovir claim 1 , foscarnet claim 1 , ribavirin claim 1 , zalcitabine (ddC) claim 1 , zidovudine (AZT) claim 1 , stavudine (D4T) claim 1 , lamivudine (3TC) claim 1 , didanosine (ddI) claim 1 , cytarabine claim 1 , dideoxyadenosine claim 1 , edoxudine claim 1 , floxuridine claim 1 , idozuridine claim 1 , inosine pranobex claim 1 , 2′-deoxy-5-(methylamino)uridine claim 1 , trifluridine and vidarabine.9. The method of claim 1 , wherein the antiviral agent is ganciclovir (GCV).10. A method for treating and/or preventing a viral or virally-induced ...

SUBSTITUTED BICYCLIC COMPOUNDS

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): 111-. (canceled)13. The method according to wherein said autoimmune disease or chronic inflammatory disease is selected from systemic lupus erythematosis claim 12 , multiple sclerosis claim 12 , inflammatory bowel disease claim 12 , ulcerative colitis claim 12 , Crohn's disease claim 12 , rheumatoid arthritis claim 12 , scleroderma claim 12 , giant cell arteritis claim 12 , and Sjögren's syndrome.17. The method according to wherein said autoimmune disease or chronic inflammatory disease is systemic lupus erythematosis.18. The method according to wherein said autoimmune disease or chronic inflammatory disease is ulcerative colitis.19. The method according to wherein said autoimmune disease or chronic inflammatory disease is multiple sclerosis.20. The method according to wherein said autoimmune disease or chronic inflammatory disease is inflammatory bowel disease.21. The method according to wherein said autoimmune disease or chronic inflammatory disease is rheumatoid arthritis.22. The method according to wherein said autoimmune disease or chronic inflammatory disease is Crohn's disease.23. The method according to wherein said autoimmune disease or chronic inflammatory disease is Sjögren's syndrome.24. The method according to wherein said autoimmune disease or chronic inflammatory disease is systemic lupus erythematosis.25. The method according to wherein said autoimmune disease or chronic inflammatory disease is ulcerative colitis.26. The method according to wherein said autoimmune disease or chronic inflammatory disease is multiple sclerosis.27. The method according to wherein said autoimmune disease or chronic inflammatory disease is inflammatory bowel disease.28. The method according to wherein said autoimmune disease or chronic inflammatory disease is rheumatoid arthritis.29. The method according to wherein said autoimmune disease or chronic inflammatory disease is Crohn's disease.30. The method ...

N-hydroxymethanesulfonamide nitroxyl donors

The disclosed subject matter provides N-hydroxymethanesulfonamide compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.

PRESERVATIVE CONTAINING COMPOSITIONS

The present invention relates to compositions providing improved preservative efficacy. The present invention further relates to polyquaternium compound containing compositions having improved the antifungal activity. In certain embodiments, the present invention relates to ophthalmic compositions comprising a polyquaternium compound, a polyol or combination of polyols, borate compound, and an antimicrobial mixture comprising electrolytes and nutrients.

LIPOSOMES FOR MODULATING WISKOTT-ALDRICH SYNDROME PROTEIN

Embodiments of the invention relate to liposomes comprising: a lipid bilayer having an internal cavity; a therapeutic agent within the internal cavity configured to modify expression or degradation of WASp in a cell; and a targeting moiety external to the lipid bilayer configured to target an extracellular domain of a cell. Embodiments of the invention relate to methods of treatment of disease comprising administering the liposomes. Novel pharmaceutical compositions are also disclosed. 1. A liposome comprising:a lipid bilayer having an internal cavity;a therapeutic agent within the internal cavity configured to modify expression or degradation of WASp in a cell; anda targeting moiety external to the lipid bilayer configured to target an extracellular domain of a cell;wherein said therapeutic agent is any one of:(a) an siRNA, shRNA or miRNA molecule that decreases the expression of WASp or increase the degradation of WASp in a cell; or(b) a peptide that increases the expression of WASp or decreases WASp degradation in a cell.2. The liposome according to claim 1 , wherein the targeting moiety comprises an agent which binds a molecule preferentially or uniquely expressed on the surface of a hematopoietic cell.3. The liposome according to claim 2 , wherein the molecule expressed on the surface of a hematopoietic cell is integrin claim 2 , said integrin being an active conformation of lymphocyte-function-associated antigen-1 (LFA-1).4. The liposome according to claim 3 , comprising an siRNA that claim 3 , when contacted with a cell claim 3 , reduces the expression of WASp or increases WASp degradation in said cell.5. The liposome according to claim 4 , wherein said siRNA comprises an oligonucleotide comprising a sequence selected from the group consisting of SEQ ID NO. 1 claim 4 , SEQ ID NO. 2 claim 4 , SEQ ID NO. 3 claim 4 , SEQ ID NO. 4 claim 4 , SEQ ID NO. 5 claim 4 , SEQ ID NO. 6 or SEQ ID NO. 7 claim 4 , or any mixture thereof and a complementary strand associated ...

PARASITICIDAL COMPOSITIONS COMPRISING AN ISOXAZOLINE ACTIVE AGENT, METHODS AND USES THEREOF

This invention relates to topical compositions for combating ectoparasites and endoparasites in animals, comprising at least one isoxazoline active agent and a pharmaceutically acceptable carrier, optionally in combination with one or more additional active agents. This invention also provides for an improved methods for eradicating, controlling, and preventing parasite infections and infestations in an animal comprising administering the compositions of the invention to the animal in need thereof. 118-. (canceled)20. The method of claim 19 , wherein the isoxazoline is 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4 claim 19 ,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[2-oxo-2-[(2 claim 19 ,2 claim 19 ,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide.21. (canceled)22. The method of claim 19 , wherein:W is O;{'sup': '4', 'sub': 1', '6, 'Ris H or C-Calkyl;'}{'sup': '5', 'sub': 2', '2', '3, 'Ris —CHC(O)NHCHCF;'}{'sup': 1', '2', '3', '4', '5', '6, 'each of A, A, A, A, Aand Ais CH;'}{'sup': 1', '6, 'sub': 1', '6, 'Ris C-Calkyl each optionally substituted with one or more substituents independently selected from R;'}{'sup': '6', 'sub': 1', '6, 'Ris halogen or C-Calkyl; and'}{'sup': 1', '2', '3, 'sub': 1', '6', '1', '6', '1', '6, 'B, B, and Bare independently CH, C-halogen, C—C-Calkyl, C—C-Chaloalkyl, or C—C-Calkoxy.'}23. The method of claim 19 , wherein the pharmaceutically acceptable carrier comprises a diester of a dicarboxylic acid claim 19 , a glycol ester claim 19 , a glycol ether claim 19 , a fatty acid ester claim 19 , a polyethylene glycol claim 19 , or polyethylene glycol ester claim 19 , an oil claim 19 , an alcohol claim 19 , a glycerol ester claim 19 , a glycerol ether claim 19 , propylene glycol claim 19 , ethylene glycol claim 19 , a glycol carbonate claim 19 , dimethyl isosorbide claim 19 , N-methylpyrrolidone claim 19 , or a mixture thereof.24. The method of claim 23 , wherein the diester of a dicarboxylic acid is a diester of a C-Cdicarboxylic acid. ...

METHOD OF TREATING OR PREVENTING NEURODEGENERATION

The invention relates to a compound which is effective in inhibiting the function of the TRPM4 ion channel and the use of such compound in treating or preventing a neurodegenerative disease, such as Multiple Sclerosis, Parkinson's disease, Alzheimer's disease, or amyotrophic lateral sclerosis, in a subject. The invention also provides a pharmaceutical composition comprising a TRPM4 inhibitory compound. The invention further relates to in vitro methods for identifying pharmaceutically active compounds that are useful for treating or preventing a neurodegenerative disease. 117-. (canceled)18. A method of treating multiple sclerosis in a subject in need of treatment thereof , the method comprising administering to the subject a therapeutically effective amount of gliclazide or a pharmaceutically acceptable salt , solvate , tautamer or ester thereof.19. The method of claim 18 , wherein the multiple sclerosis is relapsing remitting multiple sclerosis or secondary progressive multiple sclerosis.20. The method of claim 19 , wherein the gliclazide is administered at a dose of between about 10 ug/kg to about 2000 ug/kg.21. The method of claim 20 , wherein the administration begins after the first clinical symptoms occur.22. The method of claim 20 , wherein the gliclazide is administered once daily.23. The method of claim 22 , wherein the dose of gliclazide is administered orally to the subject. The instant application contains a Sequence Listing file entitled 058223-502D01US SL.txt, with a file size of about 20,391 bytes in size and created on our about Oct. 26, 2020, has been submitted electronically in ASCII format and is hereby incorporated by reference in its entirety.Neurodegenerative diseases of the central nervous system (CNS) which cause progressive loss of neuronal structure and function are particularly devastating diseases for the affected patients and their families. Among these neurodegenerative diseases are, for example, Multiple Sclerosis (MS), Parkinson's ...

Modified Release Formulations Containing Drug-Ion Exchange Resin Complexes

An aqueous liquid suspension containing a coated drug-ion exchange resin complex comprising a core composed of an amphetamine complexed with a pharmaceutically acceptable ion-exchange resin and an uncoated amphetamine-ion exchange resin complex is provided. The coated amphetamine-ion exchange resin complex is in admixture with a polymer to form a matrix. Methods of making the coated complex and the liquid suspension are described.

LIQUID FORMULATIONS CONTAINING PICOSULFATE AND MAGNESIUM CITRATE

Liquid formulations containing picosulfate and magnesium citrate are provided. The formulations are useful to treat constipation or for the clearance of the bowel prior to X-ray examination, endoscopy or surgery. 1. A liquid formulation comprising:sodium picosulfate;magnesium citrate; andat least one precipitation inhibitor, wherein the precipitation inhibitor is a carboxylic acid, an ammonium salt or a soluble anionic polymer;wherein the precipitation inhibitor is malonic acid or tartaric acid if the formulation does not comprise an ammonium salt or a soluble anionic polymer;wherein the formulation is in the form of an aqueous solution having a pH in the range from about 4.0 to about 6.5.2. The liquid formulation of claim 1 , wherein the sodium picosulfate is present at a concentration in the range from about 0.10 mM to about 0.15 mM claim 1 , the magnesium citrate comprises magnesium and citrate in a molar ratio in the range from about 1:1 to about 1.5:1 claim 1 , and wherein the magnesium citrate is present at a concentration of magnesium in the range from about 0.2 to about 0.8 M.3. The liquid formulation of claim 2 , wherein the sodium picosulfate is present at a concentration in the range from about 0.12 mM to about 0.14 mM claim 2 , the magnesium citrate comprises magnesium and citrate in a molar ratio of about 1.4:1 claim 2 , and wherein the magnesium citrate is present at a concentration of magnesium in the range from about 0.5 to about 0.6 M.47-. (canceled)8. The liquid formulation of claim 1 , wherein the magnesium citrate is formed from magnesium oxide and citric acid.9. The liquid formulation of claim 1 , comprising a carboxylic acid.10. The liquid formulation of claim 9 , wherein the carboxylic acid is selected from the group consisting of malonic acid claim 9 , tartaric acid claim 9 , acetic acid claim 9 , arginine claim 9 , ascorbic acid claim 9 , asparagine claim 9 , aspartic acid claim 9 , citric acid claim 9 , cysteine claim 9 , fumaric acid claim ...

Transdermal and/or topical delivery systems composed of doxylamine succinate and pyridoxine hydrochloride in combination, or alone

Pharmaceutical compositions for simultaneous transdermal delivery of Doxylamine and Pyridoxine comprising Doxylamine or its salts, Pyridoxine or its salts or its active metabolites and a vehicle system wherein pharmaceutical compositions are liquid formulations, semisolid formulations and polymer matrices. Further pharmaceutical compositions can be incorporated into transdermal delivery systems or transdermal patches. The invention provides a method for treatment of nausea and vomiting in general, and for pregnant women in particular by continuous and simultaneous transdermal delivery of Doxylamine and Pyridoxine. This is to be accomplished through topical application of pharmaceutical compositions or by application of a transdermal delivery system or transdermal patch to the surface of the skin wherein the duration of application is once in a day, once every two days, once every three days, once every four days, once every five days, once every six days, or once in a week.

MOLECULAR ACTIVATORS OF THE WNT/BETA-CATENIN PATHWAY

The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/β-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/β-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/β-catenin pathway in a subject is also discussed. 1. A method of treating a subject for a condition mediated by aberrant Wnt/β-catenin signaling , said method comprising:selecting a subject with a condition mediated by aberrant Wnt/β-catenin signaling andadministering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein the subject is human.3. The method of claim 1 , wherein a compound of Table 1 or a pharmaceutically acceptable salt thereof is administered.4. The method of claim 1 , wherein a compound of Table 2 or a pharmaceutically acceptable salt thereof is administered.5. The method of claim 1 , wherein the condition is selected from the group consisting of cancer claim 1 , bone mass diseases claim 1 , fracture repair claim 1 , FEVR claim 1 , diabetes mellitus claim 1 , cord blood transplants claim 1 , psychiatric disease claim 1 , neurodegenerative disease claim 1 , hair loss claim 1 , diseases linked to loss of stem/progenitor cells claim 1 , conditions improved by increasing stem/progenitor cell populations claim 1 , HIV claim 1 , and tooth agenesis.6. A method of activating the Wnt/β-catenin pathway in a subject comprising:selecting a subject in need of Wnt/β-catenin pathway activating andadministering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof.7. The method of claim 6 , wherein a ...

KETONE INHIBITORS OF LYSINE GINGIPAIN

The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium . Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of Ccycloalkyl claim 1 , Calkyl claim 1 , Caryl claim 1 , and 5- to 12-membered heteroaryl each of which is optionally substituted with one or more Rsubstituents claim 1 , and each Ris independently selected from the group consisting of halogen claim 1 , —N claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , Chaloalkoxy claim 1 , —N(R) claim 1 , —N(R) claim 1 , and —NRC(O)R.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl substituted with Calkoxy.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.67-. (canceled)8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O—R claim 1 , and Ris Chaloalkyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O—R claim 1 , and Ris 5- to 12-membered heteroaryl claim 1 , which is optionally substituted with one or more members independently selected from the group consisting of halogen and Calkyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of —N(R) claim 1 , 5- to 12-membered heteroaryl claim 1 , and 3- to 12-membered heterocyclyl claim 1 , wherein:{'sub': 1-3', '1-3, '5- to 12-membered heteroaryl is optionally substituted with one or more members ...

THERAPEUTIC AURONES

Substituted aurones were found to have antitrypanosomal, antifungal and immunomodulatory activity. The invention provides novel aurone compounds, pharmaceutical compositions, and methods encompassing medical and veterinary applications. 213-. (canceled)14. The method of claim 1 , wherein the composition further comprises a pharmaceutically acceptable carrier.15. The method of claim 1 , wherein the subject is a human.16. The method of claim 1 , wherein the subject is an animal.1718-. (canceled)2031-. (canceled)33. The method of claim 1 , wherein the compound of Formula I is selected from the group consisting of compounds 4001 claim 1 , 2014 claim 1 , 9087 claim 1 , 9019 claim 1 , 9024 claim 1 , 9030 claim 1 , 9028 claim 1 , 7000 claim 1 , 9065 claim 1 , 9084 claim 1 , 9070 claim 1 , AA8 claim 1 , 9006 claim 1 , 9057 claim 1 , 3001 claim 1 , 9312 claim 1 , 9063 claim 1 , 6003 claim 1 , 2015 claim 1 , AA11 claim 1 , 9086 claim 1 , 7002 claim 1 , 3009 claim 1 , 9076 claim 1 , 3011 claim 1 , 8002 claim 1 , 3008 claim 1 , 2909 claim 1 , 9064 claim 1 , 9085 claim 1 , 5006 claim 1 , 2904 claim 1 , 9051 claim 1 , 8001 claim 1 , 2018 claim 1 , 6001 claim 1 , 6000 claim 1 , 4006 claim 1 , 9007 claim 1 , 2008 claim 1 , and 9026 as in Table 1.3440-. (canceled)42. (canceled)43. The kit of further comprising at least one second active agent which can be co-administered with the compound of Formula I.4454-. (canceled)55. The method of claim 32 , wherein a is 0 claim 32 , b is 1 claim 32 , and R1 is Cl.57. The kit of claim 56 , wherein a is 0 claim 56 , b is 1 claim 56 , and R1 is Cl.58Trypanosoma bruceiTrypanosoma cruziLeishmania. The method of claim 1 , wherein the trypanosomatid infection comprises at least one of a infection claim 1 , a infection claim 1 , or a infection.59. The method of claim 1 , further comprising administering to the subject an effective amount of at least one second compound comprising an antiprotozoan compound claim 1 , an antiparasitic compound claim 1 , ...

System for Preparing Medicinal Beverages Using Cartridge-Type Beverage Brewers

A system for brewing medicinal beverages, using a cartridge-based beverage formation apparatus, comprises a cartridge containing a beverage composition comprising a mixture of one or more water-soluble active pharmacological treatment agents, such as pain relievers, cold medications, sleeping aids, laxatives, stimulants, or vitamins, and one or more water-soluble non-pharmacological constituents, which can include water-soluble carbohydrates, proteins, alcohols, sweetening, flavoring and coloring agents, anti-caking agents, buffering and acidifying agents, surfactants, thickening and stabilizing agents, antioxidants and/or preservatives. 1. A system for brewing medicinal beverages using a cartridge-based beverage formation apparatus , the system comprising:a cartridge, adapted for use with the cartridge-based beverage formation apparatus; andcontained within the cartridge, a beverage composition comprising a mixture of one or more water-soluble active pharmacological treatment agents and one or more water-soluble non-pharmacological constituents.2. The system of claim 1 , wherein the beverage composition comprises 0.001 to 6.0 grams of the one or more water-soluble active pharmacological treatment agents claim 1 , mixed with 0.1 to 20 grams of the one or more water-soluble non-pharmacological constituents claim 1 , in powdered or agglomerated form claim 1 , and wherein the one or more water-soluble non-pharmacological constituents are selected from the group consisting of carbohydrates claim 1 , alcohols and proteins.3. The system of claim 2 , wherein the one or more water-soluble non-pharmacological constituents are selected from the group of carbohydrates claim 2 , alcohols and proteins claim 2 , consisting of dextrose claim 2 , fructose claim 2 , sucrose claim 2 , sorbitol claim 2 , mannitol claim 2 , allulose claim 2 , polydextrose claim 2 , soluble dextrins claim 2 , maltodextrins claim 2 , corn syrup solids claim 2 , spray dried or agglomerated natural honey ...

INHIBITORS OF CREATINE TRANSPORT AND USES THEREOF

This invention relates to compounds that inhibit creatine transport and/or creatine kinase, pharmaceutical compositions including such compounds, and methods of utilizing such compounds and compositions for the treatment of cancer. 2. The compound of claim 1 , wherein Ris hydrogen.4. The compound of any one of to claim 1 , wherein Rcombines with Rwith the atoms to which they are attached to form an optionally substituted C-Ccycloalkyl ring.7. The compound of any one of to claim 1 , wherein Ris hydrogen claim 1 , hydroxyl claim 1 , or NH.8. The compound of any one of to claim 1 , wherein Ris hydrogen.9. The compound of any one of to claim 1 , wherein m is 1 and Ris deuterium claim 1 , optionally substituted C-Calkyl claim 1 , optionally substituted C-Calkenyl claim 1 , optionally substituted C-Calkynyl claim 1 , or Rand Rcombine with the atoms to which they are attached to form an optionally substituted C-Ccycloalkyl ring.10. The compound of claim 9 , wherein Ris deuterium.11. The compound of claim 10 , wherein Ris deuterium.12. The compound of or claim 10 , wherein Rand Rare both deuterium.13. The compound of claim 9 , wherein Ris optionally substituted C-Calkyl claim 9 , optionally substituted C-Calkenyl claim 9 , optionally substituted C-Calkynyl.14. The compound of claim 13 , wherein Ris methyl claim 13 , ethyl claim 13 , n-propyl claim 13 , iso-propyl claim 13 , —CD claim 13 , —CF claim 13 , —CHF claim 13 , —CHF claim 13 , —CH═CH claim 13 , or —C≡CH.15. The compound of or claim 13 , wherein Ris hydrogen or methyl.16. The compound of any one of to claim 13 , wherein Ris hydrogen.17. The compound of any one of to claim 13 , wherein Ris hydrogen claim 13 , NH claim 13 , or methyl.18. The compound of claim 9 , wherein Rand Rcombine with the atoms to which they are attached to form an optionally substituted C-Ccycloalkyl ring.19. The compound of claim 18 , wherein said optionally substituted C-Ccycloalkyl ring is an optionally substituted C-Ccycloalkyl ring.20. The ...

MODIFIED RELEASE LIQUID PHARMACEUTICAL COMPOSITION COMPRISING BROMOPHENIRAMINE, PSEUDOEPHEDRINE AND DEXTROMETHORPHAN

There is provided a modified release liquid pharmaceutical composition comprising combination of dextromethorphan, bromrpheniramine and pseudoephedrine or pharmaceutically acceptable salts thereof. The invention further provides process for preparation of such compositions. 2. The modified release liquid pharmaceutical composition of claim 1 , wherein pseudoephedrine or salt thereof is complexed or coated with one or more an ion exchange resins.3. The modified release liquid pharmaceutical composition of claim 1 , wherein dextromethorphan or salt thereof is complexed or coated with one or more an ion exchange resins.43. The modified release liquid pharmaceutical composition of claim 1 , claim 1 , or claim 1 , wherein the ion exchange resin comprises one or more organic claim 1 , inorganic claim 1 , anionic claim 1 , and cationic exchange resins.5. The modified release liquid pharmaceutical composition of claim 4 , wherein the ion exchange resin comprises polistirex claim 4 , sodium polystyrene sulphonate claim 4 , and mixture thereof.6. The modified release liquid pharmaceutical composition of claim 1 , wherein the composition comprises one or more rate-controlling polymers.7. The modified release liquid pharmaceutical composition of claim 6 , wherein the rate-controlling polymers comprises one or more hydrophilic polymers claim 6 , hydrophobic polymers claim 6 , or mixture thereof.9. A method of treating one or more symptoms selected from upper respiratory tract infection claim 6 , common cold claim 6 , and allergic rhinitis claim 6 , which method comprises of administering the modified release liquid pharmaceutical composition 1 or 8 to a patient in need thereof. The present invention relates to a modified release liquid pharmaceutical composition comprising combination of brompheniramine, pseudoephedrine and dextromethorphan or pharmaceutically acceptable salts thereof. The invention further provides process for preparation of such compositions.Upper respiratory ...

GABR-A2 DIAGNOSTIC

The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sites known as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence at these GABR-A2 SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs. 1. A method for selecting a patient for treatment with an NMDA antagonist drug , comprising determining in a nucleic acid containing sample from said patient the nucleotide at single nucleotide polymorphism (SNP) position rs3756007 and/or , rs11503016 , and/or rs17537359 , and/or rs1372472 in GABR-A2 gene , wherein if there is a cytosine at rs3756007 , or a thymine at rs11503016 , or a thymine at rs11503016 , or a thymine at rs1372472 , said patient is selected for treatment with an NMDA antagonist drug.2. A method of recommending a treatment , the method comprising(a) selecting a patient in need of treatment for depression and/or anxiety, the patient's genome having been identified as bearing a minor allele at any one rs3756007, rs11503016, rs17537359 or rs1372472 in GABR-A2 gene; and(b) recommending that the patient be treated with an NMDA antagonist.3. The method as claimed in or , wherein the NMDA antagonist drug is selected from the group consisting of: (S)-1-phenyl-2-(pyridin-2-yl)ethanamine and ketamine.4. The method as claimed in or , wherein the NMDA antagonist drug is (S)-1-phenyl-2-(pyridin-2-yl)ethanamine.5. The method as claimed in any of the preceding claims wherein the depression and/or anxiety is selected from: major depressive disorder (MDD) , single or recurrent depressive episodes , treatment- ...

Immediate Release Abuse-Deterrent Granulated Dosage Forms

Described are immediate release oral dosage forms that contain abuse-deterrent features. In particular, the disclosed dosage forms provide deterrence of abuse by ingestion of multiple individual doses. In addition, the disclosed dosage forms provide protection from overdose in the event of accidental or intentional ingestion of multiple individual doses. 1. An immediate release compressed tablet comprising:a disintegrant;more than one gelling polymers; and,an active pharmaceutical ingredient (API) selected from ketamine, esketamine and pharmaceutically acceptable salts thereof,wherein at least one of the gelling polymers is present within a matrix.2. The tablet according to claim 1 , wherein the gelling polymers are independently selected from the group consisting of a natural starch claim 1 , a synthetic starch claim 1 , a natural cellulose claim 1 , a synthetic cellulose claim 1 , an acrylate claim 1 , a polyalkylene oxide claim 1 , a carbomer and combinations thereof.3. The tablet according to claim 1 , wherein the gelling polymers are independently selected from the group consisting of polyethylene oxide claim 1 , polyvinyl alcohol claim 1 , hydroxypropyl methyl cellulose claim 1 , hydroxypropyl cellulose claim 1 , methyl cellulose claim 1 , hydroxyethylmethylcellulose claim 1 , sodium carboxymethylcellulose claim 1 , hydroxyethylcellulose claim 1 , polyacrylic acid and polyvinyl carboxy polymers claim 1 , carbomer polymers and combinations thereof.4. The tablet according to claim 3 , wherein the gelling polymers comprise hydroxypropyl methyl cellulose (HPMC) and a carbomer.5. The tablet according to claim 1 , wherein the gelling polymer present within the matrix comprises a carbomer.6. The tablet according to claim 1 , wherein the gelling polymer present within the matrix comprises polyethylene oxide.7. The tablet according to claim 1 , wherein the total amount of gelling polymers is about 0.7 to about 20 weight percent based on total weight of the tablet.8. ...

ANTIMICROBIAL COMPOUNDS AND NANOSTRUCTURES

The present disclosure provides compounds and nanostructures having one or more quaternary ammonium salts, compositions including the compounds and nanostructures, and methods useful for treating conditions using the compounds, nanostructures, and compositions. In at least one aspect, a compound is represented by formula (I): 2. The method of claim 1 , wherein depositing is performed using an aqueous solution comprising the nanorod.3. The method of claim 1 , further comprising evaporating water of the aqueous solution after depositing the aqueous solution onto the surface.4. The method of claim 1 , wherein depositing the nanorod on the surface is performed by painting the surface claim 1 , dipping the surface claim 1 , spraying the surface claim 1 , taping the surface claim 1 , brush coating the surface claim 1 , spin coating the surface claim 1 , roll coating the surface claim 1 , doctor-blade coating the surface claim 1 , or combination(s) thereof with the nanorod.5. The method of claim 1 , wherein the surface is an interior surface of an aircraft claim 1 , spacecraft claim 1 , or boat.6. The method of claim 1 , wherein the surface is a surface of an air filter of a vehicle.7. The method of claim 1 , wherein the surface is selected from the group consisting of a floor surface claim 1 , a seat surface claim 1 , an overhead bin surface claim 1 , a ceiling surface claim 1 , a door surface claim 1 , a door handle surface claim 1 , and combination(s) thereof.8. The method of claim 1 , wherein Ris pyridyl disulfide.9. The method of claim 1 , wherein Q is chloro.12. The method of claim 1 , wherein the first compound is a pharmaceutically acceptable salt of a halide.13. The method of claim 12 , wherein the salt is an iodo salt.14. The method of claim 1 , wherein a ratio of the integer n to the integer m is about 5:1 to about 15:1.15. The method of claim 1 , wherein the nanorod has a diameter of about 10 nm to about 20 nm.16. The method of claim 1 , wherein the nanorod has ...

PLURIMODAL RELEASE FORMULATION OF DOXYLAMINE AND PYRIDOXINE AND/OR METABOLITES OR SALTS THEREOF

A solid oral dosage form comprising a core comprising a doxylamine component and a pyridoxine component coated with an enteric coating is disclosed. The solid oral dosage form further comprises two active ingredient-containing coatings surrounding the enteric coating, the active ingredient-containing coatings being separated from one another by an intermediate coating, and one of the two active ingredient-containing coatings comprising a doxylamine component and being free of a pyridoxine component, and the other of the two active ingredient-containing coatings comprising a pyridoxine component and being free of doxylamine component. Uses of the solid oral dosage form for the alleviation of the symptoms of nausea and vomiting, for example in the case of nausea and vomiting of pregnancy (NVP), are also disclosed. 2. The solid oral dosage form of claim 1 , wherein said core comprises about 10 mg of said doxylamine or pharmaceutically acceptable salt thereof.3. The solid oral dosage form of claim 1 , wherein said core comprises doxylamine succinate.4. The solid oral dosage form of claim 1 , wherein said core comprises about 10 mg of said pyridoxine or pharmaceutically acceptable salt thereof.5. The solid oral dosage form of claim 1 , wherein said core comprises pyridoxine hydrochloride.6. The solid oral dosage form of claim 1 , wherein said first or second active ingredient-containing coating comprises about 10 mg of said doxylamine or pharmaceutically acceptable salt thereof.7. The solid oral dosage form of claim 1 , wherein said first or second active ingredient-containing coating comprises doxylamine succinate.8. The solid oral dosage form of claim 1 , wherein said first or second active ingredient-containing coating comprises about 10 mg of said pyridoxine or pharmaceutically acceptable salt thereof.9. The solid oral dosage form of claim 1 , wherein said first or second active ingredient-containing coating comprises pyridoxine hydrochloride.10. The solid oral ...

IMMEDIATE RELEASE ORAL GUAIFENESIN SOLUTION

Disclosed is a method of treating or ameliorating a condition which can be treated or ameliorated by the administration of guaifenesin, which method comprises orally administering to a subject in need thereof an effective amount of an an immediate release solution for oral administration of guaifenesin and at least one additional drug. In addition to water the solution comprises as solvents propylene glycol and glycerol in a concentration which significantly increases the bioavailability of guaifenesin in the human body. 1. A method of treating or ameliorating a condition which can be treated or ameliorated by the administration of guaifenesin , wherein the method comprises orally administering to a subject in need thereof an effective amount of an immediate release solution for oral administration of guaifenesin and one or more additional drugs which comprise at least one of an antitussive , a decongestant , an antihistsamine or an analgesic , which solution comprises as solvents water and a total of from 48% to 72% by weight , relative to a total weight of the solution , of propylene glycol and glycerol , and , when orally administered to an adult human subject as a single dose in an amount which affords 200 mg of guaifenesin , provides (i) a Cof at least 3600 ng/mL of guaifenesin and/or an AUCof guaifenesin of at least 3700 ng.hr/mL and (ii) a therapeutically effective plasma concentration of guaifenesin for at least 4 hours.2. The method of claim 1 , wherein the solution comprises a total of from 54% to 66% by weight of propylene glycol and glycerol.3. The method of claim 1 , wherein a weight ratio of glycerol to propylene glycol is from 1.7:1 to 2.5:1.4. The method of claim 1 , wherein the solution comprises from 15% to 23% by of propylene glycol.5. The method of claim 1 , wherein the solution comprises from 33% to 49% by weight of glycerol.6. The method of claim 1 , wherein the solution provides a Cof at least 3800 ng/mL of guaifenesin.7. The method of claim 1 ...

COMPOSITIONS AND METHODS FOR TREATING OCULAR CONDITIONS

Disclosed herein are methods for treating an ocular pathology in a subject, comprising administering to the subject an ENPP1 inhibitor. Also disclosed are methods of inhibiting ATP hydrolysis in ocular tissue, the method comprising contacting the ocular tissue with an ENPP1 inhibitor. Also provided herein are ectonucleotide pyrophosphatase/phosphodiesterase-1 (ENPP1) inhibitors and compositions comprising the same. 1. A method of treating an ocular pathology characterized by ectopic calcification in a subject , comprising administering to the subject an ENPP1 inhibitor.2. The method of claim 1 , wherein the ocular pathology is pseudoxanthoma elasticum (PXE) claim 1 , sclero-choroidal calcification or choroidocalcinosis.3. The method of or claim 1 , wherein the ocular pathology is pseudoxanthoma elasticum (PXE) or sclero-choroidal calcification.4. The method of claim 2 , wherein the ocular pathology is PXE.5. The method of claim 2 , wherein the ocular pathology is sclero-choroidal calcification.6. The method of claim 3 , wherein the ocular pathology is choroidocalcinosis.7. The method of any one of - claim 3 , comprising administering the ENPP1 inhibitor ocularly.8. The method of claim 7 , wherein the ocular administration is topically (e.g. claim 7 , as eyedrops).9. The method of claim 7 , wherein the ocular administration is by intraocular injection.10. The method of claim 7 , wherein the ocular administration is via implantation of a device comprising the ENPP1 inhibitor to an eye of the subject.11. The method of any one of - claim 7 , wherein the subject is an elderly subject.12. The method of any one of - claim 7 , wherein the subject is a pediatric subject.13. The method of any one of - claim 7 , wherein the subject is an adult.19. The method of any one of - claim 7 , further comprising conjointly administering a bisphosphonate with the ENPP1 inhibitor.20. The method of claim 19 , wherein the bisphosphonate is selected from clondrate claim 19 , tiludronate ...

COMPOSITIONS AND METHODS FOR TREATING CARDIAC INJURY

Disclosed herein are methods for treating cardiac injury in a subject, comprising administering an ENPP1 inhibitor. Also disclosed are methods of promoting healing of cardiac tissue in a subject having a cardiac injury, comprising administering an ENPP1 inhibitor. Also disclosed are methods of inhibiting ATP hydrolysis in a cardiac fibroblast the method comprising contacting the cardiac fibroblast with an ENPP1 inhibitor. Also provided herein are ectonucleotide pyrophosphatase/phosphodiesterase-1 (ENPP1) inhibitors. 1. A method of treating cardiac injury in a subject , comprising administering an ENPP1 inhibitor.2. A method of promoting healing of cardiac tissue in a subject having a cardiac injury , comprising administering an ENPP1 inhibitor.3. The method of any one of - , wherein the cardiac injury is a myocardial injury.4. The method of claim 3 , wherein the myocardial injury is a myocardial infarction claim 3 , cardiac hypertrophy claim 3 , or myocarditis.5. The method of claim 4 , wherein the myocardial injury is a myocardial infarction.6. The method of any one of - claim 4 , wherein the ENPP1 inhibitor is administered to the subject within about 3 weeks of the cardiac injury.7. The method of claim 6 , wherein the ENPP1 inhibitor is administered to the subject within about 2 weeks of the cardiac injury.8. The method of claim 6 , wherein the ENPP1 inhibitor is administered to the subject within about 1 week of the cardiac injury.9. The method of claim 6 , wherein the ENPP1 inhibitor is administered to the subject within about 48 hours of the cardiac injury.10. The method of claim 6 , wherein the ENPP1 inhibitor is administered to the subject within about 24 hours of the cardiac injury.11. The method of claim 6 , wherein the ENPP1 inhibitor is administered to the subject within about 12 hours of the cardiac injury.12. The method of claim 6 , wherein the ENPP1 inhibitor is administered to the subject within about 8 hours of the cardiac injury.13. The method of ...

COMPOSITIONS AND METHODS FOR TREATING ACNE VULGARIS

Disclosed are compositions, methods of treatment using the compositions and methods of preparing the compositions for the treatment of acne vulgaris. The compositions include succinic acid and an API selected from the group consisting of salicylic acid, azelaic acid, picolinic acid, benzoyl peroxide, antibiotic, retinoid and combinations thereof in a pharmaceutically acceptable preparation. The compositions that include the combination of succinic acid and another API produce improved efficacy in treating acne vulgaris. 1Propionibacterium acnesP. acnesP. acnes. A method of killing a () that is resistant to an antibiotic , the method comprising treating the with a composition comprising succinic acid , wherein the succinic acid is at a concentration of at least 15 mM.231P. acnes. The method of claim , wherein the is on skin of a subject having acne vulgaris and the composition is a topical composition.331P. acnes. The method of claim , wherein the is resistant to erythromycin , clindamycin , minocycline , doxycycline , or any combination thereof.431P. acnes. The method of claim , wherein the is resistant to erythromycin , clindamycin , minocycline and doxycycline.531. The method of claim , wherein the composition further comprises azelaic acid.631. The method of claim , wherein the composition further comprises picolinic acid.731. The method of claim , wherein the composition further comprises benzoyl peroxide.831. The method of claim , wherein the composition further comprises an antibiotic.931. The method of claim , wherein the composition further comprises salicylic acid.1039. The method of claim , wherein the salicylic acid is present at concentration from 0.1 to 5%.1139. The method of claim , wherein the succinic acid is present at concentration from 0.1 to 10%.1239. The method of claim , wherein the salicylic acid and succinic acid present in a 1:2 ratio.1332. The method of claim , wherein the topical composition further comprises aloe vera , propanediol , ...

SEMI-SOLID CHEWABLE DOSAGE FORM FOR OVER-THE-COUNTER MEDICATIONS AND METHOD FOR PRODUCING SAME

The invention provides a semi-solid chewable dosage form for use as an over-the-counter medication that contains an active pharmaceutical ingredient to treat symptoms associated with allergies, colds, coughs, fever, pain, gastrointestinal disorders, sleep, and other common conditions. The invention further provides a semi-solid chewable dosage form that contains an active pharmaceutical ingredient, a gelling agent, gelatin, sugar, a polyol, and a pH adjusting agent. The invention also provides a semi-solid chewable dosage form that contains a gelling agent, sugar, a polyol, glycerin, and a pH adjusting agent. 1. A semi-solid chewable dosage form comprising an active pharmaceutical ingredient , a gelling agent , gelatin , sugar , a polyol , and a pH adjusting agent.2. The semi-solid chewable dosage form of claim 1 , wherein the gelling agent is pectin claim 1 , the gelatin is hydrolyzed gelatin claim 1 , and the polyol is hydrolyzed starch hydrolysate.3. The semi-solid dosage form of claim 2 , wherein pectin is present in an amount from about 0.5% by weight to about 7% by weight claim 2 , hydrolyzed gelatin is present in an amount from about 0.5% by weight to about 8% by weight claim 2 , and hydrolyzed starch hydrolysate is present in an amount from about 40% by weight to about 90% by weight.4. The semi-solid chewable dosage form of claim 1 , wherein the active pharmaceutical ingredient is diphenhydramine hydrochloride.5. The semi-solid chewable dosage form of claim 4 , wherein the gelling agent is pectin.6. The semi-solid chewable dosage form of claim 4 , wherein the gelatin is hydrolyzed gelatin.7. The semi-solid chewable dosage form of claim 4 , wherein the polyol is hydrolyzed starch hydrolysate.8. The semi-solid dosage form of claim 4 , wherein the gelling agent is pectin present in an amount from about 0.5% by weight to about 7% by weight claim 4 , the gelatin is hydrolyzed gelatin present in an amount from about 0.5% by weight to about 8% by weight claim 4 , ...

SEMI-SOLID CHEWABLE DOSAGE FORM FOR OVER-THE-COUNTER MEDICATIONS AND METHOD FOR PRODUCING SAME

The invention provides a semi-solid chewable dosage form that contains one or more active pharmaceutical ingredients that are generally available as over-the-counter medications including, for example, chlorpheniramine maleate, phenylephrine hydrochloride, guaifenesin, dextromethorphan hydrobromide, loratadine, or a combination thereof. The invention further provides a semi-solid chewable dosage form that contains chlorpheniramine maleate, phenylephrine hydrochloride or a combination thereof, a gelling agent, gelatin, sugar, a polyol, and a pH adjusting agent. The invention further provides a semi-solid chewable dosage form that contains the active pharmaceutical ingredient chlorpheniramine maleate, phenylephrine hydrochloride or a combination thereof, a gelling agent, gelatin, sugar, corn syrup, and a pH adjusting agent. The semi-solid chewable dosage form is useful for administration to individuals to treat symptoms from allergies, colds, congestion, and the like. 1. A semi-solid chewable dosage form comprising an active pharmaceutical ingredient selected from the group consisting of chlorpheniramine maleate , phenylephrine hydrochloride , and a combination thereof , a gelling agent , gelatin , sugar , a polyol , and a pH adjusting agent.2. The semi-solid chewable dosage form of claim 1 , wherein the active pharmaceutical ingredient is a combination of chlorpheniramine maleate and phenylephrine hydrochloride.3. The semi-solid chewable dosage form of claim 2 , wherein the gelling agent is pectin.4. The semi-solid chewable dosage form of claim 2 , wherein the gelatin is hydrolyzed gelatin.5. The semi-solid chewable dosage form of claim 2 , wherein the polyol is hydrolyzed starch hydrolysate.6. The semi-solid chewable dosage form of claim 2 , wherein the pH adjusting agent is sodium citrate and citric acid.7. The semi-solid chewable dosage of claim 1 , wherein the gelling agent is pectin in an amount from about 0.5% by weight to about 7% by weight claim 1 , the ...

Anise Flavored Medication

An anise flavored liquid medication. The liquid medication contains phenylephrine and an anethole analog that is substantially free of aldehyde groups. In one example, the anethole analog can be 1-methoxy-4-n-propylbenzene. 1. A liquid medication comprising:a. from about 0.01% to about 0.04% phenylephrine, by weight of the composition;b. from about 1% to about 3% of a pain reliever, by weight of the composition, wherein the pain reliever is selected from the group consisting of acetaminophen, ibuprofen, ketoprofen, naproxen, aspirin, and combinations thereof; andc. from about 2 ppm to about 5 ppm of an anethole analog, by weight of the composition, wherein the anethole analog is selected from the group consisting of 1-methoxy-4-n-propylbenzene, methyl anisate, anisole, 2-chloroanethole, 2,6-dichloroanethole, 3-nitroanethole, 3,5-dinitroanethole, 3-cyanoanethole, 3,5-dicyanoanethole, 1-methoxy-3-(1-propenyl)benzene, and combinations thereof.2. The liquid medication of wherein the phenylephrine is phenylephrine hydrochloride.3. The liquid medication of further comprising from about 0.01% to about 0.2% of an antitussive claim 2 , by weight of the composition claim 2 , wherein the antitussive is selected from the group consisting of dextromethorphan HBr claim 2 , chlophedianol claim 2 , levodropropizine claim 2 , and combinations thereof.4. The liquid medication of further comprising from about 3% to about 15% ethanol claim 3 , by weight of the composition.5. The liquid medication of further comprising from about 3% to about 15% glycerin claim 4 , by weight of the composition.6. The liquid medication of further comprising doxylamine succinate.7. The liquid medication of comprising from about 0.03% to about 0.05% doxylamine succinate claim 6 , by weight of the composition.8. The liquid medication of further comprising guaifenesin.9. The liquid medication of wherein the anethole analog is 1-methoxy-4-n-propylbenzene.10. The liquid medication of wherein the anethole analog ...

Methods of treating lactose intolerance

Disclosed herein are methods for treating lactose intolerance, including compounds that may be specific or modulate PPARγ receptors.

Pharmaceutical Suspension Composition

An aqueous oral liquid pharmaceutical composition system with reduced propensity for agglomeration and phase separation which is particularly amendable to the suspension of one or more pharmaceutical actives that are substantially insoluble in water. The oral liquid pharmaceutical composition may further comprise pharmaceutical actives that are soluble in water and dissolve in the aqueous medium. In the composition of the invention both suspended and any dissolved active agents are distributed homogeneously. 124.-. (canceled)25. A method of preparing an oral liquid pharmaceutical composition comprising:a. preparing a suspending system, including suspended components in an aqueous medium;b. suspending at least one substantially insoluble first pharmaceutical active in the suspending system; andc. matching the true density of the at least one substantially insoluble first pharmaceutical active and the suspended components of the suspending system with the specific gravity of the aqueous medium.26. The method of further comprising de-aerating the composition by subjecting it to vacuum.27. The method of further comprising dissolving in the aqueous medium at least one second pharmaceutical active soluble in the aqueous medium.28. The method of further comprising adding a surface modifying agent to the pharmaceutical composition.29. A method for treatment of pain and discomfort associated with at least one of headache claim 25 , body ache claim 25 , cold symptoms claim 25 , flu symptoms claim 25 , and allergy symptoms in humans comprising the administration to a human of a safe and effective amount of the pharmaceutical composition of .30. A method for treatment of pain and discomfort associated with at least one of headache claim 27 , body ache claim 27 , cold symptoms claim 27 , flu symptoms claim 27 , and allergy symptoms in humans comprising the administration to a human of a safe and effective amount of the pharmaceutical composition of . This is a divisional ...

SYNERGISTIC DRUG COMBINATIONS PREDICTED FROM GENOMIC FEATURES AND SINGLE-AGENT RESPONSE PROFILES

The present disclosure relates to discovery of specific synergistic drug combinations and mechanisms of drug resistance. Compositions involving newly-identified drug combinations as well as diagnostic and therapeutic methods related to such discoveries are provided. 1. A pharmaceutical composition for treating a cancer in a subject comprising a KDM6A/KDM6B inhibitor and a MGLL inhibitory agent , and a pharmaceutically acceptable carrier.2. The pharmaceutical composition of claim 1 , wherein the KDM6A/B inhibitor is selected from the group consisting of GSK-J4 claim 1 , IOX1 claim 1 , GSK-J1 and caffeic acid.3. The pharmaceutical composition of claim 1 , wherein the MGLL inhibitory agent is selected from the group consisting of JZL 184 claim 1 , URB602 claim 1 , pristimerin claim 1 , an 0-hexafluorosiopropyl carbamate claim 1 , and an oligonucleotide inhibitor ofMGLL.4. The pharmaceutical composition of claim 1 ,wherein the cancer is selected from the group consisting of AML, ALL and prostate cancer.5. A pharmaceutical composition for treating a cancer in a subject selected from the group consisting of:A pharmaceutical composition comprising a STAT3 signaling inhibitor and a UGTJAJO inhibitory agent, and a pharmaceutically acceptable carrier;A pharmaceutical composition comprising a CDK4/6 inhibitor and a CCNE1 inhibitory agent, and a pharmaceutically acceptable carrier;A pharmaceutical composition comprising an AKT1/2 inhibitor and an AKT3 inhibitory agent, and a pharmaceutically acceptable carrier;A pharmaceutical composition comprising a topoisomerase II inhibitor and a BCL2L1 inhibitory agent, and a pharmaceutically acceptable carrier;A pharmaceutical composition comprising a PI3 kinase inhibitor and an IRS2 inhibitory agent, and a pharmaceutically acceptable carrier;A pharmaceutical composition comprising a GPX4 inhibitor and an AIFM2 inhibitory agent, and a pharmaceutically acceptable carrier;A pharmaceutical composition comprising an inducer of reactive oxygen ...

Pharmaceutical Compositions of Sodium Picosulfate, Magnesium Oxide and Citric Acid

The present invention relates to pharmaceutical compositions of sodium picosulfate, magnesium oxide and citric acid. In particular, the invention relates to pharmaceutical compositions comprise granules having a layer of sodium picosulfate on neutral carrier/s. The invention also relates to processes for the preparation of such compositions and use thereof for bowel cleansing. 1. A pharmaceutical composition comprising:a) granules of sodium picosulfate and a neutral carrier, andb) a mixture comprising citric acid, magnesium oxide, an alkaline agent and one or more pharmaceutically acceptable excipients,2. The pharmaceutical composition according to claim 1 , wherein the neutral carrier comprising one or more of saccharides claim 1 , sugar alcohols and cellulose derivatives.3. The pharmaceutical composition according to claim 1 , wherein the neutral carrier is lactose.4. The pharmaceutical composition according to claim 1 , wherein the alkaline is agent comprising one or more of sodium bicarbonate claim 1 , potassium bicarbonate claim 1 , calcium carbonate claim 1 , sodium carbonate and lithium carbonate.5. The pharmaceutical composition according to claim 1 , wherein the composition is in the form of capsules or sachets.6. The pharmaceutical composition according to retains at least 80% of the potency of active ingredients in the pharmaceutical composition after storage at 40° C. and 75% relative humidity for three months.7. A process for preparing a pharmaceutical composition comprising:i) preparing granules of sodium picosulfate and a neutral carrier;ii) drying the granules;iii) mixing citric acid, magnesium oxide, an alkaline agent and one or more pharmaceutically acceptable excipient; andiv) mixing the granules of step ii) with the mixture of step iii) to prepare the final composition.8. The process according to claim 7 , wherein the granules are prepared by applying solution or suspension of sodium picosulfate onto the neutral carrier.9. The process according ...

Dexanabinol or a Derivative Thereof for Use in the Treatment of Cancer in Dose Ranges of 2-30 mg/kg

There is described a method of treating cancer in a patient wherein the method comprises the administration of dexanabinol, or a derivative thereof, in an amount of from about 2 mg/kg to about 30 mg/kg, based on the weight of the patient. 1. A method of treating cancer in a patient wherein the method comprises the administration of dexanabinol , or a derivative thereof , in an amount of from about 2 mg/kg to about 30 mg/kg , based on the weight of the patient.2. (canceled)3. A method of treating cancer in a patient wherein the method comprises the administration of dexanabinol , or a derivative thereof , in an amount sufficient to achieve a plasma concentration of dexanabinol from about 10 to about 100 μM.4. (canceled)5. (canceled)6. A method according to wherein the dosage of dexanabinol claim 1 , or a derivative thereof claim 1 , is sufficient to achieve a plasma concentration of dexanabinol claim 1 , or a derivative thereof claim 1 , that is maintained for at least 2 hours in the patient.7. A method according to wherein the dose regime comprises administration once weekly claim 1 , twice weekly claim 1 , three times weekly claim 1 , four times weekly claim 1 , five times weekly claim 1 , six times weekly claim 1 , or every day; for one week in a 3 week cycle.8. (canceled)9. (canceled)10. A method according to wherein the dose regime comprises administration once weekly claim 1 , twice weekly claim 1 , three times weekly claim 1 , four times weekly claim 1 , five times weekly claim 1 , six times weekly claim 1 , or every day; for one week in a 4 week cycle.11. (canceled)12. (canceled)13. A method according to wherein the dose regime comprises administration once weekly claim 1 , twice weekly claim 1 , three times weekly claim 1 , four times weekly claim 1 , five times weekly claim 1 , six times weekly claim 1 , or every day.14. A method according to wherein the dose regime comprises administration a course of treatment comprising of 1 claim 7 , 2 claim 7 , 3 claim ...

A method for treating swi/snf complex-deficient cancers comprising glutathione (gsh) metabolic pathway inhibitor

The present invention provides a method for treating SWI/SNF complex-deficient cancers comprising a glutathione (GSH) metabolic pathway inhibitor, a pharmaceutical composition comprising a glutathione (GSH) metabolic pathway inhibitor for therapy in SWI/SNF complex-deficient cancers, and a glutathione (GSH) metabolic pathway inhibitor for use in treating SWI/SNF complex-deficient cancers. The present invention also provides a method for detecting and/or selecting a susceptible patient to a glutathione (GSH) metabolic pathway inhibitor.

COMPOUNDS AND METHODS OF TREATING RETINAL DEGENERATION

A method of treating retinal degeneration in a subject includes administering to the subject a therapeutically effective amount of a compound of formula (I). 7. The method of claim 1 , the retinal degeneration comprising inherited retinal degeneration associated with rhodopsin mutations.8. The method of claim 1 , wherein the retinal degeneration is selected from the group consisting of Leber congenital amaurosis claim 1 , Stargardt disease claim 1 , and retinitis pigmentosa.9. The method of claim 8 , the retinitis pigmentosa comprising autosomal dominate retinitis pigmentosa associated with a P23H RHO mutation.10. The method of claim 1 , the therapeutically effective amount of the compound is an amount required to inhibit photoreceptor cell death in the subject.11. The method of claim 1 , the therapeutically effective amount of the compound is an amount effective to inhibit bright light-induced retinal degeneration in a Rdh8Abca4 mouse.12. The method of claim 1 , wherein the compound stabilizes P23H rod opsin mutant proteins.13. The method of claim 1 , wherein the compound promotes rod photoreceptor cell homeostasis in the subject.14. The method of claim 1 , wherein the compound upon administration to the subject mobilizes the P23H opsin from the endoplasmic reticulum to the plasma membrane of photoreceptor cells.15. The method of claim 1 , wherein the compound inhibits early endoplasmic reticulum associated protein degradation (ERAD) pathway in the subject.16. The method of claim 1 , the compound being delivered to the subject by at least one of topical administration claim 1 , systemic administration claim 1 , intravitreal injection claim 1 , and intraocular delivery.17. The method of claim 16 , wherein the compound is administered to the subject systemically.18. The method of claim 1 , wherein the activity of the compound is not affected negatively when photoreceptor cells of the subject are exposed to light.19. The method of claim 1 , further comprising ...

Oral dosage forms for oxygen-containing active agents and oxyl-containing polymer

The disclosed invention is drawn to pharmaceutical tablets that provide delivery of active agents having at least three oxygen-containing groups, a tri-oxy active agent, as well as a second active ingredient. Non-limiting examples of three oxygen-containing group active agents include guaifenesin, codeine, hydrocodone, and their pharmaceutically acceptable salts. In one embodiment, a pharmaceutical tablet for oral administration once every 12 hours is provided. The tablet includes a first active agent that is a tri-oxy active agent, a second active agent, and a release rate controlling non-ionic oxyl-containing hydrophilic polymer. The total oxyl content of the hydrophilic polymer in the tablet is from about 4×10 −4 moles to about 2.0×10 −3 moles. The tablet is a matrix tablet and a single-dose administration of one or more tablets to a subject under fasted conditions provides a mean C max for each of the first active agent and the second active agent that is 70% to 135% of a respective mean C max provided by administering an immediate release oral dosage form to a subject under fasted conditions every 4 to 6 hours over a 12 hour time period, wherein cumulative dosage amounts administered over the 12 hour time period of each active agent is equivalent to the respective amount of each active agent in the pharmaceutical tablet.

Phenoxy Acetic Acids and Phenyl Propionic Acids as PPAR Delta Agonists

Phenoxy acetic acids and phenyl propionic acids and their use in improving mitochondrial energy output in a subject are provided herein. The present compounds are activators of PPARδ and may be useful for treating conditions mediated by the same. 2. The method of claim 1 , wherein Xis morpholin-4-ylmethyl.3. A method of improving mitochondrial energy output in a subject claim 1 , the method comprising administering to a subject in need thereof an effective amount of a compound selected from the group consisting of:(E)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methylphenoxy]acetic acid; andZ)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methylphenoxy]acetic acid; ora pharmaceutically acceptable salt thereof.4. The method of claim 3 , wherein the compound is (E)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof.5. The method of claim 3 , wherein the compound is (Z)-[4-[3-(4-Fluorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methyl-phenoxy]acetic acid or a pharmaceutically acceptable salt thereof.7. The method of claim 6 , wherein Xis morpholin-4-ylmethyl.8. The method of claim 6 , wherein the compound is (E)-[4-[3-(4-Chlorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methylphenyl]-propionic acid or a pharmaceutically acceptable salt thereof.9. The method of claim 6 , wherein the compound is (Z)-[4-[3-(4-Chlorophenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl]allyloxy]-2-methylphenyl]-propionic acid or a pharmaceutically acceptable salt thereof.10. A method of improving mitochondrial energy output in a subject claim 6 , the method comprising administering to a subject in need thereof an effective amount of a compound of selected from the group consisting of:(Z)-[2-Methyl-4-[3-(4-methylphenyl)-3-[4-[3-(morpholin-4-yl)propynyl]phenyl] allyloxy]-phenoxy]acetic acid;(E)-[2-Methyl-4-[3-[4 ...

INJECTION COMPOSITION COMPRISING HYALURONIDASE FOR REMOVAL OF TOPICAL FAT

The present invention relates to an injection composition comprising hyaluronidase for topical fat reduction. More particularly, the present invention relates to an injection composition comprising 300 IU to 600 IU of hyaluronidase and a local anesthetic, an antihistamine, a lipolysis stimulator and a collagen production stimulator. The present invention promotes the reduction of topical fat tissue, thereby improving obesity and helping weight loss and maintenance of body shape while preventing side effects or skin imbalance by the even removal of fat. Further, at the same time, the present invention can achieve a skin lifting effect where skin resilience is maintained by the stimulation of collagen production. 1. An injection composition for topical fat removal comprising 300 IU to 600 IU of hyaluronidase and, based on the weight of the total composition, 0.08 to 0.4% by weight of lidocaine as local anesthetic, 0.01 to 0.02% by weight of pheniramin as antihistamine, 0.01 to 4.0% by weight of L-carnitine as lipolysis stimulator, and 0.1 to 2.0% by weight of vitamin C as collagen production stimulator, with the remainder being saline solution, wherein the composition is characterized as being injected at a unit volume of 0.5 to 2 cc with an interval between injection points of 0.5 to 1.5 cm. The present application claims priority from Korean Patent Applications No. 10-2016-0116462 filed on Sep. 9, 2016, the entire subject matter of which is incorporated herein by reference.The present invention relates to an injection composition comprising hyaluronidase for the removal of topical fat. More specifically, the present invention relates to an injection composition comprising 300 IU to 600 IU of hyaluronidase and one or more local anesthetics, antihistamines, lipolysis stimulators and collagen production stimulators. Further, the present invention relates to a method for a reduction of topical fat by injecting an injection composition comprising 300 IU to 600 IU of ...