КОМБИНИРОВАННЫЙ ПРЕПАРАТ ДЛЯ ЛЕЧЕНИЯ СЛАБОУМИЯ

Изобретение относится к медицине, конкретно к средствам терапии слабоумия. Сущность изобретения заключается в создании комбинированного препарата на основе активных компонентов, содержащего соединение, обладающее эффектом торможения ацетилхолинэстеразы или обнаруживающее мускаринергическое действие, и соединение, которое повышает эндогенный внеклеточный уровень аденозина. Технический результат заключается в повышении эффективности препарата за счет эффекта потенцирования. 2 с. и 4 з.п. ф-лы, 4 табл., 3 ил.

ЛЕКАРСТВЕННАЯ КОМБИНАЦИЯ С ТЕОБРОМИНОМ И ЕЕ ИСПОЛЬЗОВАНИЕ В ЛЕЧЕНИИ

Предложена группа из 7 изобретений для лечения кашля. Она включает комбинированное средство для лечения кашля, содержащее теобромин и кодеин для введения кодеина в дозе 3 мг/кг/сутки, фармацевтическую композицию, содержащую указанное комбинированное средство, применение средства или композиции для лечения кашля; применение средства или композиции для получения препарата для лечения кашля, способ лечения кашля, применение теобромина в сочетании с кодеином для получения препарата для лечения кашля (варианты) и применение теобромина в сочетании с кодеином для лечения кашля (варианты). Технический результат состоит в повышении эффективности заявленной комбинации против монотерапии теобромином и монотерапии кодеином. 7 н. и 7 з.п. ф-лы, 1 ил.

СПОСОБ УЛУЧШЕНИЯ ФУНКЦИИ МОЧЕВОГО ПУЗЫРЯ

Группа изобретений относится к медицине и фармации. Предложено применение i) уридина и/или эквивалента, выбранного из группы, состоящей из дезоксиуридина, уридин фосфатов, нуклеинового основания урацила и/или ацилированных производных уридина и/или сложных эфиров и (ii) n-3 полиненасыщенных жирных кислот (PUFA) для производства композиции для восстановления или улучшения функции мочевого пузыря у субъекта, имеющего нарушенную функцию мочевого пузыря и где субъектом является пациент, который страдает, выздоравливает от, и/или страдал неврологическим нарушением и соответствующий способ лечения указанного нарушения. Технический результат состоит в сокращении (с 12 до 2 дней) сроков восстановления рефлекторной способности мочевого пузыря к опорожнению на модели статистического сдавливания спинного мозга на уровне Т12 грудного отдела позвоночника. 2 н. и 19 з.п. ф-лы, 2 табл., 2 пр.

СОЕДИНЕНИЯ С КОНДЕНСИРОВАННЫМ КОЛЬЦОМ И ИХ ИСПОЛЬЗОВАНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Изобретение относится к области медицины и органической химии и касается терапевтического средства против гепатита С, содержащего соединения формулы I, фармкомпозиции, содержащей указанные соединения, и ингибитора полимеразы вируса гепатита С. Соединения обладают существенно более высокой активностью, чем известные. 9 с. и 24 з.п.ф-лы, 218 табл.

СУЛЬФОНАМИДНОЕ ПРОИЗВОДНОЕ И ЕГО МЕДИЦИНСКОЕ ПРИМЕНЕНИЕ

Изобретение относится к новым сульфонамидным производным общей формулы (1) или их фармацевтически приемлемым солям, обладающим свойствами ингибитора интегрина α4β7. Соединения могут найти применение для лечения или профилактики воспалительного заболевания, в котором патологическое состояние связано с опосредованным интегринами α4β7 процессом адгезии. В общей формуле (1)А обозначает группу, представленную общей формулой (2-1) или (2-2)где Arm представляет собой 5- или 6-членное ароматическое кольцо, содержащее 0, 1 или 2 гетероатома, выбранных из атомов азота, Rи R, каждый, независимо, представляет собой любой заместитель из атома водорода, атома галогена, низшей алкильной группы, низшей алкокси группы, моно- или ди-низшей алкиламино группы, R, Rи R, каждый, независимо, представляет собой любой заместитель из атома водорода, низшей алкильной группы, низшей алкокси группы, амино группы, низшей алкиламино группы, низшей ди(алкил)амино группы или (низший алкиламино)низшей алкильной группы, ...

ПРЕПАРАТ В ФОРМЕ ПЕЛЛЕТ С ЗАМЕДЛЕННЫМ ВЫСВОБОЖДЕНИЕМ ДЛЯ ВЕРТИГО

Изобретение относится к фармацевтической промышленности. Фармацевтическая композиция в форме пеллет для лечения головокружения, содержащая циннаризин и дименгидринат, в которой высвобождение активных ингредиентов замедлено и композиция также содержит связующий агент, замедляющий высвобождение средство, наполнитель, дополнительный вспомогательный агент, взятые в определенном соотношении. Применение фармацевтической композиции для лечения головокружения любого происхождения. Вышеописанная композиция с замедленным высвобождением активных ингредиентов эффективна для лечения головокружения. 2 н. и 4 з.п. ф-лы, 4 ил., 3 табл.

ПРИМЕНЕНИЕ ПРОИЗВОДНЫХ ТЕОФИЛЛИНА ДЛЯ ЛЕЧЕНИЯ И ПРОФИЛАКТИКИ СОСТОЯНИЙ ШОКА, НОВЫЕ СОЕДИНЕНИЯ КСАНТИНА

Изобретение относится к области медицины и касается лекарственного средства для лечения шоковых заболеваний, содержащего соединение формулы I, а также к новым соединениям общей формулы I. Средство обладает повышенной антишоковой активностью. 2 с. и 4 з.п. ф-лы, 4 табл.

КОМПОЗИЦИИ И СПОСОБЫ МОДУЛИРОВАНИЯ МЕТАБОЛИЧЕСКИХ ПУТЕЙ

Группа изобретений относится к медицине, а именно к эндокринологии, и может быть использована для лечения метаболических нарушений. Композиция по изобретению содержит по меньшей мере 500 мг лейцина и/или, по меньшей мере, 200 мг одного или более его метаболитов, где один или более метаболитов лейцина, выбраны из группы, состоящей из кетоизокапроновой кислоты (KIC), альфагидроксиизокапроновой кислоты и гидроксиметилбутирата (НМВ), и противодиабетическое средство, включающее метформин. Способы по изобретению включают введение композиции субъекту. Использование изобретения позволяет снизить дозу метформина при лечении метаболических нарушений за счет синергического действия компонентов композиции. 3 н. и 24 з.п. ф-лы, 3 табл., 76 ил., 10 пр.

КОМПОЗИЦИЯ, ВКЛЮЧАЮЩАЯ АЦЕТАМИНОФЕН, КОФЕИН И НЕОБЯЗАТЕЛЬНО АСПИРИН В СМЕСИ СО ЩЕЛОЧНЫМ АГЕНТОМ ДЛЯ УВЕЛИЧЕНИЯ АБСОРБЦИИ

Изобретение относится к химико-фармацевтической промышленности и касается способа снижения времени проявления активности обезболивающей/жаропонижающей композиции, содержащей эффективное количество обезболивающего/жаропонижающего средства, включающего ацетилсалициловую кислоту, ацетаминофен, кофеин и щелочной агент, причем указанный способ включает добавление в композицию, по крайней мере, одного щелочного агента, снижающего время проявления активности обезболивающей/жаропонижающей композиции. Композиция характеризуется быстрым проявлением обезболивающего/жаропонижающего эффекта, не токсична. 2 н. и 7 з.п. ф-лы, 4 табл., 4 ил.

СПОСОБЫ ИЗГОТОВЛЕНИЯ ЛЕКАРСТВЕННЫХ СОСТАВОВ АЦИКЛОВИРА

Настоящее изобретение относится к химико-фармацевтической промышленности и касается способа изготовления лекарственных составов ацикловира с улучшенной биологической доступностью. Изобретение также относится к единичной дозированной форме ацикловира, способу ее введения, способу лечения вирусного заболевания и способу улучшения биологической доступности ацикловира. Изобретение обеспечивает повышенную эффективность лечения вирусных инфекционных заболеваний у пациента и сокращение числа приема лекарственного средства пациентом. 9 н. и 7 з.п. ф-лы, 2 табл., 10 ил.

ПРОИЗВОДНЫЕ КСАНТИНА С КОНЦЕВЫМИ АМИНИРОВАННЫМИ АЛКИНОЛЬНЫМИ БОКОВЫМИ ЦЕПЯМИ И ЛЕКАРСТВЕННОЕ СРЕДСТВО

Изобретение относится к новым производным ксантина с концевыми аминированными алкинольными боковыми цепями формулы I в форме индивидуальных стереоизомеров или в виде смесей стереоизомеров, обладающим нейрозащитным действием. Указанные соединения обладают большим терапевтическим потенциалом. В соединениях общей формулы I R1 и R3 означают алкинольный остаток формулы (Ia), R2 означает а) линейный или разветвленный (С1 -C5)-алкил, б) (С3-C6)-циклоалкил, в) (С4-C8)-циклоалкил-алкил, R4 означает водород или (C1-C3)-алкил, R5 и R6 независимо друг от друга означают а) атом водорода, б) (С1-C6)-алкил, в) фенил(С1-C5)-алкил, или R5 и R6 вместе с атомом азота, с которым они связаны, образуют 5-6-членный насыщенный цикл, или R5 и R6 вместе с атомом азота, с которым они связаны, образуют 5-6-членный насыщенный цикл, где одна -СН2-группа цикла заменена остатком из группы О, NR13, причем R13 означает атом водорода, (C1-C3)-алкилкарбонил, (С1-C4)-алкил, А означает неразветвленный или разветвленный (С1- ...

ТАБЛЕТИРОВАННЫЙ ПРЕПАРАТ С ЗАМЕДЛЕННЫМ ВЫСВОБОЖДЕНИЕМ ДЛЯ ВЕРТИГО

Изобретение относится к фармацевтической промышленности, в частности к средству для лечения головокружения. Фармацевтическая композиция для лечения головокружения, в которой высвобождение активных ингредиентов замедлено, содержащая циннаризин, дименгидринат, связующий агент, замедляющее высвобождение средство и наполнитель, взятые в определенном соотношении. Вышеописанная композиция с замедленным высвобождением активных ингредиентов эффективна для лечения головокружения. 8 з.п. ф-лы, 4 ил., 3 табл.

КОМБИНИРОВАННОЕ ЛЕЧЕНИЕ АГОНИСТОМ ТОЛЛ-ПОДОБНОГО РЕЦЕПТОРА (TLR7) И ИНГИБИТОРОМ СБОРКИ КАПСИДА ВИРУСА ГЕПАТИТА В

Группа изобретений относится к области медицины и фармацевтики, а именно к фармацевтической композиции, включающей агонист TLR7, выбранный из [(1S)-1-[(2S,4R,5R)-5-(5-амино-2-оксо-тиазоло[4,5-d]пиримидин-3-ил)-4-гидрокси-тетрагидрофуран-2-ил]пропил]ацетата и 5-амино-3-[(2R,3R,5S)-3-гидрокси-5-[(1S)-1-гидроксипропил]тетрагидрофуран-2-ил]-6Н-тиазоло[4,5-d]пиримидин-2,7-диона, и ингибитор сборки капсида HBV, выбранный из 3-[(8aS)-7-[[(4R)-4-(2-хлор-3-фтор-фенил)-5-этоксикарбонил-2-тиазол-2-ил-1,4-дигидропиримидин-6-ил]метил]-3-оксо-5,6,8,8а-тетрагидро-1H-имидазо[1,5-а]пиразин-2-ил]-2,2-диметил-пропановой кислоты и 3-[(8aS)-7-[[(4S)-5-этоксикарбонил-4-(3-фтор-2-метил-фенил)-2-тиазол-2-ил-1,4-дигидропиримидин-6-ил]метил]-3-оксо-5,6,8,8а-тетрагидро-1Н-имидазо[1,5-а]пиразин-2-ил]-2,2-диметил-пропановой кислоты, в фармацевтически приемлемом носителе. Остальные объекты относятся к способу изготовления лекарственного средства, способу, набору и применению фармацевтической композиции для лечения или ...

АНТИТЕЛА К ТЕОФИЛЛИНУ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Изобретение относится к области биохимии, в частности к антителу, специфически связывающемуся с теофиллином, или его фрагменту, специфически связывающемуся с теофиллином. Изобретение позволяет эффективно получать антитело, специфически связывающееся с теофиллином. 2 н. и 8 з.п. ф-лы, 5 ил., 2 табл., 6 пр.

КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ДИАМИНОКСИДАЗУ, ДЛЯ ПРИМЕНЕНИЯ ДЛЯ ЛЕЧЕНИЯ ИЛИ ПРЕДОТВРАЩЕНИЯ ФИБРОМИАЛГИИ ИЛИ СИНДРОМА ХРОНИЧЕСКОЙ УСТАЛОСТИ

Настоящее изобретение относится к фармакологии и медицине. Предложено применение диаминоксидазы для получения композиции для лечения фибромиалгии или синдрома хронической усталости у субъектов с дефицитом диаминоксидазы. Технический результат: улучшение состояния и качества жизни пациентов за счёт снижения сильной головной боли и усталости. 10 з.п. ф-лы, 3 табл., 8 пр.

ПРОИЗВОДНОЕ КСАНТИНА

Изобретение относится к производному ксантина, представленному формулой (I),формула (I),гдеR выбран из;Rвыбран из метоксикарбонила; Rвыбран из водорода и атомов галогена; каждый из X и Y независимо выбран из C или N; n равняется 0, 1, 2, 3 или 4, для лечения заболеваний, связанных с дипептидилпептидазой IV. 3 н. и 5 з.п. ф-лы, 6 ил., 7 табл.

ИНГИБИТОРЫ РЕПАРАЦИИ ПОВРЕЖДЕНИЙ ДНК ДЛЯ ЛЕЧЕНИЯ РАКА

Предложенная группа изобретений относится к области медицины. Предложено применение ингибитора поли(АДФ-рибоза)-полимеразы (PARP) для получения медикамента, предназначенного для лечения у индивидуума рака, который является дефектным по пути репарации двухнитевого разрыва (ДНР) ДНК, зависимой от гомологической рекомбинации. Предложены способы лечения рака у индивидуума, включающие введение ингибитора PARP указанному индивидууму, при этом указанный рак является дефектным по пути репарации ДНР ДНК, зависимой от гомологической рекомбинации. Предложенная группа изобретений обеспечивает селективную индукцию летальности раковых клеток, дефектных по репарации ДНР ДНК, зависимой от гомологической рекомбинации. 3 н. и 26 з.п. ф-лы, 18 ил., 1 пр.

КОМПОЗИЦИИ И СПОСОБЫ ДЛЯ ИНГИБИРОВАНИЯ СЕКРЕЦИИ ЖЕЛУДОЧНОЙ КИСЛОТЫ С ИСПОЛЬЗОВАНИЕМ ПРОИЗВОДНЫХ МАЛЫХ ДИКАРБОНОВЫХ КИСЛОТ В СОЧЕТАНИИ С PPI

Настоящее изобретение относится к новым пероральным композициям, содержащим необратимый желудочный ингибитор Н/K-АТФазы протонной помпы (PPI) в качестве ингибитора секреции желудочной кислоты и одну или несколько молекул производных алифатических карбоновых кислот, которые активируют париетальные клетки, где производные вызывают отсроченный или длительный эффект усиления в отношении активности PPI по сравнению с немодифицированными молекулами кислоты. Настоящее изобретение дополнительно относится к способу применения таких композиций для снижения секреции желудочной кислоты у млекопитающего. 3 н. и 14 з.п. ф-лы, 3 пр., 2 ил.

СПОСОБ ПРОФИЛАКТИКИ РЕПЕРФУЗИОННОГО СИНДРОМА ПРИ РЕКОНСТРУКТИВНЫХ ОПЕРАЦИЯХ НА ПРЕЦЕРЕБРАЛЬНЫХ СОСУДАХ

Изобретение относится к медицине, а именно к хирургии и касается профилактики реперфузионного синдрома при реконструктивных операциях на прецеребральных сосудах. Для этого вводят раствор эуфиллина 2,4% при соотношении 10 мл эуфиллина на 200 мл физраствора. Введение лекарственного препарата начинают за 5 минут до снятия зажима с общей сонной артерии и восстановления кровотока по эндартерэктомированной сонной артерии и продолжают в течение еще 25 минут после снятия зажима с общей сонной артерии. Такой режим введения эуфиллина обеспечивает эффективное предупреждение ишемии головного мозга и реперфузионных осложнений при реконструктивных операциях на прецеребральных сосудах. 3 пр.

СПОСОБ ЛЕЧЕНИЯ СИСТЕМНОЙ КРАСНОЙ ВОЛЧАНКИ ЧЕЛОВЕКА

Изобретение относится к медицине, а именно к терапии и иммунологии, и касается лечения системной красной волчанки. Для этого осуществляют комплексное лечение, состоящее из двух десятидневных этапов. Первый этап включает внутримышечное введение препаратов интерферона, антиагрегантов и/или дезинтоксикационную терапию в сочетании аутогемотерапией в виде смеси в одном шприце аутокрови в количестве 2 мл и иммуноглобулина человеческого нормального в количестве 1,5 мл в течение последующих 5 дней. Второй этап включает пероральное введение индукторов интерферона и проведение внутривенной инфузионной терапии гепатопротекторами. Такие курсы лечения проводят один раз в три месяца. Терапевтические курсы повторяют до нормализации иммунологических, лабораторных показателей и улучшения клинической картины пациента. Способ обеспечивает наступление стойкой ремиссии при снижении зависимости от цитостатиков и глюкокортикостероидов. 2 з.п. ф-лы, 2 пр.

СРЕДСТВО ДЛЯ НАРУЖНОЙ ТЕРАПИИ ПСОРИАЗА И СПОСОБ ЕГО ИЗГОТОВЛЕНИЯ

Средство для наружной терапии псориаза включает в качестве активных веществ препараты группы метилксантинов 0,01-0,1 и препараты селена 0,00001-0,0003 (г на 1 г готового продукта). В качестве вспомогательных веществ средство содержит жировую основу, растительное рафинированное масло и воду. Средство применяют в липосомальной форме в виде крема. Для образования липидной пленки используют пищевую добавку - соевый фосфатидный концентрат "Лецитин", представляющий собой смесь фосфолипидов, включающих фосфатидилхолин. Указанную пищевую добавку смешивают с холестерином в соотношении 1:1 по отношению к фосфатидилхолину. Липосомальную эмульсию получают добавлением раствора с указанными активными веществами. Готовый продукт в виде крема получают добавлением к липосомальной эмульсии жировой основы и растительного рафинированного масла. Новое средство обеспечивает высокую эффективность наружной терапии сложных форм псориаза. Средство эффективно при экссудативном псориазе и псориазе волосистой части ...

СПОСОБ ЛЕЧЕНИЯ ПАЦИЕНТОВ С ЛИЦЕВОЙ БОЛЬЮ С ПОСТГЕРПЕТИЧЕСКИМИ ГАНГЛИОНИТАМИ ГОЛОВЫ

Изобретение относится к медицине и предназначено для лечения пациентов с лицевой болью с постгерпетическими ганглионитами головы. Определяют содержание специфических антител класса G к вирусу простого герпеса (ВПГ) 1 типа и цитомегаловирусу, содержание в крови интерферонов альфа и гамма, сывороточного и спонтанного интерферона, в ротовой жидкости: концентрации секреторного иммунноглобулина А, интерферона альфа и уровня лактоферрина. Вычисляют показатель реакции адсорбции микроорганизмов (РАМ). Если показатели сывороточного и спонтанного интерферона не превышают 2 ед./мл, содержание специфических антител класса G к ВПГ 1 типа - от 1:2973,75 и выше, к цитомегаловирусу - от 1:2916,91 и выше, интерферона альфа - от 194,78 ед./мл и ниже, интерферона гамма - от 16,87 ед./мл и ниже, а в ротовой жидкости: концентрация секреторного иммуноглобулина - от 225,11 мг/мл и ниже, концентрация интерферона альфа - от 8,6 пг/мл и ниже, уровень лактоферрина - от 9613,3 нг/мл и ниже, показатель РАМ - от 6,5 ...

КОМПОЗИЦИИ ДЛЯ СУПРЕССИИ ЭКСПРЕССИИ ССR5 И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

... 1. Фармацевтическая композиция для уменьшения экспрессии поверхностных рецепторов CRR5 на мононуклеарных клетках, где композиция содержит терапевтически эффективное количество по меньшей мере одного соединения, блокирующего фазу G1. 2. Фармацевтическая композиция по п.1, дополнительно содержащая по меньшей мере одно противовирусное средство. 3. Фармацевтическая композиция по п.1, где соединение, блокирующее фазу G1, является представителем, выбранным из группы, включающей бутират натрия, афидиколин, гидроксимочевину (HU), оломуцин, росковитин, токоферолы и рапамицин (RAPA). 4. Фармацевтическая композиция по п.2, где противовирусное средство представляет собой противовирусное средство против ВИЧ. 5. Фармацевтическая композиция по п.4, где противовирусное средство против ВИЧ представляет собой ингибитор нуклеозида RT, ингибитор/антагонист CCR5, ингибитор вирусного вхождения и их функциональные эквиваленты. 6. Фармацевтическая композиция по п.2, где противовирусное средство представляет собой ...

СПОСОБЫ И КОМПОЗИЦИИ ДЛЯ УЛУЧШЕНИЯ ПИАЛЬНОГО КОЛЛАТЕРАЛЬНОГО КРОВООБРАЩЕНИЯ И ЛЕЧЕНИЯ КОАГУЛОПАТИЙ

... 1. Способ улучшения пиального коллатерального кровообращения и защиты ишемизированной ткани, включающий стадии:a) введение композиции, содержащей, по меньшей мере, одну форму токотриенола в количестве от около 10 мг до около 1000 мг в день субъекту, нуждающемуся в улучшении пиального коллатерального кровообращения и защите ишемизированной ткани; иb) улучшение пиального коллатерального кровообращения и защиты ишемизированной ткани в объекте.2. Способ улучшения артериогенеза в субъекте, включающий стадии:a) введение композиции, содержащей, по меньшей мере, одну форму токотриенола в количестве от около 10 мг до около 1000 мг в день субъекту, нуждающемуся в стимуляции артериогенеза; иb) стимуляция артериогенеза в объекте.3. Способ повышения тканевого ингибитора металлопротеиназ-металлопептидаз-1 (TIMP1) в сосудах цереброваскулярного коллатерального кровообращения и ослабления активности матриксной металлопротеиназы-2 (ММР2) у нуждающегося в этом субъекта, включающий стадии:a) введение композиции ...

ПРОИЗВОДНЫЕ ПУРИНА, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ ПРИМЕНЕНИЯ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЙ, СВЯЗАННЫХ С БАФ (БЕЛОК-АКТИВАТОР ФИБРОБЛАСТОВ)

... 1. Применение соединения ! формулы (I) ! ! формулы (II), ! ! формулы (III), ! ! или формулы (IV), ! ! в которой R1 обозначает пиридинилметил, пиримидинилметил, хинолинилметил, (2-оксо-1,2-дигидрохинолинил)метил, изохинолинилметил, хиназолинилметил, (4-оксо-3,4-дигидрохиназолинил)метил, хиноксалинилметил, [1,5]нафтиридинилметил, (1H-пиридинил)метил, фенантридинилметил, (11Н-дибензо[b,е]азепинил)метил, (дибензо[b,f[1,4]оксазепинил)метил, (5Н-дибензо[b,е][1,4]диазепинил)метил или (имидазо[1,2-а]хинолинил)метил и гетероциклические группы указанных выше групп могут быть моно- или дизамещены с помощью Ra, где заместители могут быть одинаковыми или разными и Ra обозначает фтор, хлор, бром, цианогруппу, метил, этил, пропил, изопропил, циклопропил, фенил, метоксигруппу, этилоксигруппу, аминогруппу, метиламиногруппу, диметиламиногруппу, пирролидиновую группу, пиперидиновую группу, морфолиновую группу, пиперазиновую группу или N-метилпиперазиновую группу, ! R2 обозначает метил, этил, пропил, изопропил ...

КСАНТИНОВЫЕ СОЕДИНЕНИЯ, ОБЛАДАЮЩИЕ ПОЛОЖИТЕЛЬНЫМ АЛЛОСТЕРИЧЕСКИМ МОДУЛЯТОРНЫМ ДЕЙСТВИЕМ В ОТНОШЕНИИ GABAB

... 1. Соединение общей формулы (I) ! ! а также его фармацевтически приемлемые соли; !где R1 выбран из галогена; C1-С10алкила; C1-С10алкокси; гидрокси-C1-С10алкила; C1-С10алкокси-C1-С10алкила; С3-С10циклоалкила; амино, замещенного одним или более чем одним C1-С10алкилом и C1-С10алкокси-C1-С10алкилом; и гетероциклила, незамещенного или замещенного одним или более чем одним C1-С10алкилом, C1-С10алкокси, C1-С10алкокси-C1-С10алкилом, ди-C1-С10алкиламино, оксо и гетероциклил-C1-С10алкилом; ! R2 выбран из бензила, замещенного одним или более чем одним галогеном; циано; C1-С10алкилом; C1-С10алкокси; ароилом; галогено-C1-С10алкилом; арил-C1-С10алкокси и C1-С10алкоксикарбонилом; 2-нафтилметила; 1-(4-хлорфенил)-5-(трифторметил)-1Н-пиразол-4-илметила; 2-(4-хлорфенил)этила; 2,1,3-бензотиадиазол-5-илметила; и 1-[5-(трифторметил)]-1,3-бензотиазол-2-илметила; ! R3 выбран из C1-С10алкила и арила, замещенного одним или более чем одним галогеном; ! R4 выбран из этила; изобутила; пропила; 3,3-диметилбутила; C1 ...

КОНДИТЕРСКИЙ ПРОДУКТ, СОДЕРЖАЩИЙ АКТИВНЫЕ И/ИЛИ РЕАКЦИОННЫЕ КОМПОНЕНТЫ, И СПОСОБЫ ЕГО ПОЛУЧЕНИЯ

... 1. Кондитерский продукт, содержащий экструдированную корпусную часть, причем корпусная часть имеет множество расположенных в ней капилляров, и содержит первое создающее ощущение вещество и второе создающее ощущение вещество, которое отличается от указанного первого создающего ощущение вещества, размещенные в отдельных и ограниченных областях указанного продукта и предназначенные для создания профилей последовательного высвобождения.2. Кондитерский продукт по п.1, содержащий от 5 до 50 указанных капилляров.3. Кондитерский продукт по п.2, содержащий от 10 до 40 указанных капилляров.4. Кондитерский продукт по п.3, содержащий от 20 до 30 указанных капилляров.5. Кондитерский продукт по любому из пп.1-4, содержащий первую группу указанных капилляров и вторую группу указанных капилляров, причем указанная первая группа капилляров, по меньшей мере частично, заполнена первым материалом начинки, содержащим указанное первое создающее ощущение вещество, и указанная вторая группа капилляров, по меньшей ...

ФАРМАЦЕВТИЧЕСКАЯ КОМБИНАЦИЯ, ВКЛЮЧАЮЩАЯ 3-(3-ДИМЕТИЛАМИНО-1-ЭТИЛ-2-МЕТИЛПРОПИЛ)ФЕНОЛ Т НЕСТЕРОИДНЫЙ ПРОТИВОВОСПАЛИТЕЛЬНЫЙ ПРЕПАРАТ

... 1. Комбинация, включающая в качестве компонентов: ! (а) по крайней мере один 3-(3-диметиламино-1-этил-2-метилпропил)фенол формулы (I), ! ! необязательно в форме одного из индивидуальных стереоизомеров, прежде всего, ! энантиометра или диастереомера, рацемата или в форме смеси стереоизомеров, прежде всего, энантиомеров и/или диастереомеров, в любом соотношении, или в форме любой кислотно-аддитивной соли, или любых сольватов указанных соединений, и ! (б) один или более нестероидных противовоспалительных препаратов (НПВП). ! 2. Комбинация по п.1, отличающаяся тем, что компонент (а) выбирают из группы, включающей ! (1R,2R)-3-(3-диметиламино-1-этил-2-метилпропил)фенол, ! (1S,2S)-3-(3-диметиламино-1-этил-2-метилпропил)фенол, ! (1R,2S)-3-(3-диметиламино-1-этил-2-метилпропил)фенол, ! (1S,2R)-3-(3-диметиламино-1-этил-2-метилпропил)фенол, или любую смесь указанных соединений. ! 3. Комбинация по п.2, отличающаяся тем, что компонент (а) выбирают из группы, включающей !(1R,2R)-3-(3-диметиламино-1-этил ...

СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ И ПРОФИЛАКТИКИ ТРОМБОЗА

Изобретение относится к фармацевтической промышленности и медицине и представляет собой применение 3-метил-8-(пиперазин-1-ил)-7-(тиетан-3-ил)-1-этил-1H-пурин-2,6(3H,7H)-диона гидрохлорида в качестве средства для лечения и профилактики тромбоза посредством блокирования рецептора тромбоцитов ГП IIb-IIIa. Изобретение обеспечивает расширение арсенала средств, обладающих терапевтической и профилактической активностями в отношении тромбоза посредством блокирования рецептора тромбоцитов ГП IIb-IIIa. 5 табл.

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 ...

ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ ДЛЯ ЛЕЧЕНИЯ ХРОНИЧЕСКИХ ОБСТРУКТИВНЫХ ЗАБОЛЕВАНИЙ ЛЕГКИХ

ПУРИНОВЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ АКТИВАТОРА АДЕНОЗИНОВОГО РЕЦЕПТОРА

... 1. Соединение формулы (I) !! в свободной форме или в форме соли, ! где R1, R2 и R3 указаны ниже ! R1 R2 R3 ! R1 R2 R3 ! R1 R2 R3 ! 2. Соединение по п.1 для применения в качестве лекарства. ! 3. Соединение по п.1 в комбинации с противовоспалительной, бронхорасширяющей, антигистаминной или противокашлевой лекарственной субстанцией, причем указанное соединение и указанная лекарственная субстанция могут находиться в одной и той же или в разной фармацевтической композиции. ! 4. Фармацевтическая композиция, включающая соединение по п.1 в качестве активного ингредиента, необязательно вместе с фармацевтически приемлемым разбавителем или носителем. ! 5. Фармацевтическая композиция по п.4, содержащая, кроме того, противовоспалительную, бронхорасширяющую, антигистаминную или противокашлевую лекарственную субстанцию. ! 6. Применение соединения по п.1 для получения медикамента для лечения состояния, опосредованного активацией аденозинового А2а рецептора. ! 7. Применение соединения по п.1 для получения ...

КОМПОЗИЦИИ ДЛЯ МЕСТНОГО ПРИМЕНЕНИЯ, СОДЕРЖАЩИЕ ПРОТИВОГРИБКОВОЕ И ПРОТИВОВИРУСНОЕ СРЕДСТВО

... 1. Фармацевтическая композиция, содержащая противогрибковое средство и противовирусное средство, необязательно в сочетании с одним или более фармацевтически приемлемыми вспомогательными веществами. ! 2. Фармацевтическая композиция по п.1, в которой противогрибковое средство представляет собой кетоконазол, итраконазол, флюконазол, равуконазол, посаконазол, вориконазол, каспофунгин или производное гидроксипиридона, такое как Циклопирокс, мимозин или деферипон, и противовирусное средство представляет собой Тенофовир, Ацикловир и/или Ганцикловир. ! 3. Фармацевтическая композиция по п.1, в которой предпочтительное противогрибковое средство представляет собой Циклопирокс и предпочтительное противовирусное средство представляет собой Тенофовир. ! 4. Фармацевтическая композиция по любому из предшествующих пунктов, которая представлена в форме геля, спрея, пены, крема, промывки, пессария, свечи овальной формы, лосьона, мази, пленки, вспенивающейся таблетки, тампона, вагинального спрея, раствора, ...

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

СПОСОБ СТИМУЛЯЦИИ НЕЙРОГЕНЕЗА В ГИППОКАМПЕ

КОМПОЗИЦИИ ТВЕРДЫХ РАСТВОРОВ И ИХ ПРИМЕНЕНИЕ ПРИ СИЛЬНОЙ БОЛИ

ПРОИЗВОДНЫЕ 2-ТИОКСАНТИНА, ДЕЙСТВУЮЩИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ МРО

... 1. Соединение формулы (I) !! где R1 выбран из С1-С6алкила, и указанный С1-С6алкил замещен С1-С6алкокси; ! и по меньшей мере один указанный С1-С6алкил или указанный C1-С6алкокси является разветвленным; ! или его фармацевтически приемлемая соль, сольват или сольват его соли. ! 2. Соединение по п.1, где С1-С6алкил в R1 представляет собой С2-4алкил. ! 3. Соединение по п.1, где указанный алкил выбран из изобутила, этила и пропила. ! 4. Соединение по п.1, где указанный алкил замещен C1-3алкокси. ! 5. Соединение по п.1, где указанный алкил замещен С1-алкокси. ! 6. Соединение по п.1, где указанный алкил замещен С2-алкокси. ! 7. Соединение по п.1, где указанный алкил замещен пропокси или изопропокси. ! 8. Соединение, представляющее собой: ! 3-(2-этокси-2-метилпропил)-2-тиоксантин; ! 3-(2-пропокси-2-метилпропил)-2-тиоксантин; ! 3-(2-метокси-2-метилпропил)-2-тиоксантин; ! 3-(2-изопропоксиэтил)-2-тиоксантин; ! 3-(2-этоксипропил)-2-тиоксантин; ! 3-(2S-этоксипропил)-2-тиоксантин; ! 3-(2R-этоксипропил ...

НОВЫЕ (ГЕТЕРО)АРИЛ-ЗАМЕЩЕННЫЕ ПИПЕРИДИНИЛЬНЫЕ ПРОИЗВОДНЫЕ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ИХ

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

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

ИНГИБИТОРЫ РЕПАРАЦИИ ПОВРЕЖДЕНИЙ ДНК ДЛЯ ЛЕЧЕНИЯ РАКА

ПОКРЫВАЮЩАЯ КОМПОЗИЦИЯ, ПОДХОДЯЩАЯ ДЛЯ ФАРМАЦЕВТИЧЕСКИХ ИЛИ НУТРИЦЕВТИЧЕСКИХ ЛЕКАРСТВЕННЫХ ФОРМ

... 1. Покрывающая композиция, подходящая для покрытия фармацевтической или нутрицевтической лекарственной формы, содержащей ядро, которое содержит один или более фармацевтических или нутрицевтических активных ингредиентов, причем покрывающая композиция содержит по меньшей мере 20% мас. кишечнорастворимой полимерной композиции типа ядро/оболочка, полученной в процессе эмульсионной полимеризации, где ядро полимерной композиции типа ядро/оболочка образовано нерастворимым в воде сшитым полимером или сополимером, а оболочка полимерной композиции типа ядро/оболочка образована анионным полимером или сополимером.2. Покрывающая композиция по п.1, содержащая вплоть до 80% мас. фармацевтических или нутрицевтических наполнителей, выбираемых из группы антиоксидантов, осветлителей, связующих агентов, ароматизаторов, агентов для повышения текучести, отдушек, скользящих агентов, улучшающих пенетрацию агентов, пигментов, пластификаторов, несшитых полимеров, порообразователей или стабилизаторов.3. Покрывающая ...

КОМПОЗИЦИИ НА ОСНОВЕ ФЛАВОНОИДОВ И СПОСОБЫ ПРИМЕНЕНИЯ

ЛЕКАРСТВЕННАЯ КОМБИНАЦИЯ С ТЕОБРОМИНОМ И ЕЕ ИСПОЛЬЗОВАНИЕ В ЛЕЧЕНИИ

... 1. Средство (медикамент), содержащее теобромин и опиат, в виде комбинированного препарата для применения в терапии.2. Средство по п.1, где терапия является лечением кашля.3. Средство по п.1 или 2, в котором опиат выбран из кодеина, морфина, диаморфина, тебаина, папаверина, носкапина, орипавина, фентанила, альфаметилфентанила, алфентанила, суфентанила, ремифентанила, карфентанила, пропоксифена, оксиморфона, оксикодона, гидроморфона, петидина, дигидрокодеина, бупренорфина, эторфина, этилморфина, лоперамида и гидрокодона, пентазоцина, трамадола, типепидина и носкапина.4. Средство по любому из пп.1 или 2, в котором опиатом является кодеин.5. Средство или теобромин по любому из пп.1 или 2, в котором опиат вводится в дозе от 0,1 до 30 мг/кг/сут.6. Средство по п.4, в котором кодеин вводится в дозе до 3 мг/кг/сут.7. Применение теобромина в сочетании с опиатом для лечения кашля.8. Применение по п.7, где опиат выбран из кодеина, морфина, диаморфина, тебаина, папаверина, носкапина, орипавина, фентанила ...

ТОПИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИБУПРОФЕН

... 1. Композиция для топической доставки к коже субъекта, содержащаядонор оксида азота, выбранный из L-аргинина или его производного;неблагоприятную биофизическую среду, включающую ионную соль;полимер для стабилизации, включающий ксантановую камедь;пропиленгликоль;полисорбатное поверхностно-активное вещество, включающее полисорбат 20; иибупрофен и/или соль ибупрофена.2. Композиция по п.1, где композиция является стабильной при воздействии температуры 40ºС в течение времени, выбранного из, по меньшей мере, приблизительно одного дня, по меньшей мере, приблизительно одной недели, и, по меньшей мере, приблизительно 4 недель.3. Композиция по п.1, где композиция представляет собой крем, гель, примочку или трансдермальный пластырь.4. Композиция по п.1, где донор оксида азота присутствует в концентрации, выбранной из группы, включающей, по меньшей мере, приблизительно 0,5 мас.% из расчета на композицию, по меньшей мере, приблизительно 5 мас.% из расчета на композицию, и, по меньшей мере, приблизительно ...

СПОСОБ УЛУЧШЕНИЯ ФУНКЦИИ МОЧЕВОГО ПУЗЫРЯ

КОМБИНИРОВАННОЕ ЛЕЧЕНИЕ АГОНИСТОМ ТОЛЛ-ПОДОБНОГО РЕЦЕПТОРА (TLR7) И ИНГИБИТОРОМ СБОРКИ КАПСИДА ВИРУСА ГЕПАТИТА В

ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ПРОПЕНОНОВЫЕ ПРОИЗВОДНЫЕ

... 1. Антиретровирусная композиция, содержащая в качестве действующих веществ соединение, представленное формулой (I): А-С(=O)-СН=С(ОН)-В, где А обозначает необязательно замещенный гетероарил; В обозначает необязательно замещенный гетероарил или необязательно замещенный арил; при условии, что исключаются варианты, когда А и/или В обозначают необязательно замещенный индол-3-ил; его таутомер, пролекарство, фармацевтически приемлемую соль или сольват и одно или несколько антиретровирусных действующих веществ другого типа. 2. Антиретровирусная композиция по п.1, где антиретровирусное действующее вещество в сочетании с соединением, представленным формулой (I), его таутомером, пролекарством, фармацевтически приемлемой солью или сольватом обладает синергетическим действием. 3. Антиретровирусная композиция по п.1 или 2, где антиретровирусное действующее вещество не является ингибитором интегразы. 4. Антиретровирусная композиция по любому из пп.1-3, где антиретровирусное действующее вещество представляет ...

ПРЕПАРАТ В ФОРМЕ ПЕЛЛЕТ С ЗАМЕДЛЕННЫМ ВЫСВОБОЖДЕНИЕМ ДЛЯ ВЕРТИГО

... 1. Фармацевтическая композиция, содержащая циннаризин и дименгидринат, характеризующаяся тем, что высвобождение активных ингредиентов замедлено и препарат находится в форме пеллет. ! 2. Фармацевтическая композиция по п.1, характеризующаяся тем, что она дополнительно содержит связующий агент, замедляющий высвобождение средства и наполнители. ! 3. Фармацевтическая композиция по п.1, характеризующаяся тем, что она содержит дополнительные вспомогательные агенты. ! 4. Фармацевтическая композиция по п.1, характеризующаяся тем, что весовое соотношение связующий агент/наполнитель в ядре находится между 50/1 и 5/1, в то время как весовое соотношение замедляющее высвобождение средство/дополнительные вспомогательные агенты в лаке находится между 4/1 и 1,5/1. ! 5. Фармацевтическая композиция по п.3, характеризующаяся тем, что весовое соотношение связующий агент: наполнитель в ядре находится между 33,12/1 и 6,25/1 и весовое соотношение замедляющее высвобождение средство/дополнительные вспомогательные ...

СПОСОБЫ ЛЕЧЕНИЯ ИНФЕКЦИИ ГЕПАТИТА В

КОМПОЗИЦИЯ ДЛЯ ДОСТАВКИ ЛЕКАРСТВ, СОДЕРЖАЩАЯ СИЛИЛЬНЫЕ ПОЛИМЕРЫ

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 ...

КОНДИТЕРСКИЙ ПРОДУКТ, СОДЕРЖАЩИЙ АКТИВНЫЕ И/ИЛИ РЕАКЦИОННЫЕ КОМПОНЕНТЫ, И СПОСОБЫ ЕГО ПОЛУЧЕНИЯ

... 1. Кондитерский продукт, содержащий экструдированную корпусную часть, причем корпусная часть имеет множество расположенных в ней капилляров, причем один или более из указанных капилляров, по меньшей мере, частично заполнены материалом начинки, содержащим активный и/или реакционный компонент, который является летучим при температурах 35°C и выше, и при этом указанная экструдированная корпусная часть не содержит указанного летучего активного и/или реакционного компонента, причем указанный летучий активный и/или реакционный компонент выбран из вкусо-ароматических добавок, активных компонентов для ухода за полостью рта; подсластителей; физиологических охлаждающих агентов; согревающих агентов; покалывающих агентов; окрашивающих добавок; шипучих добавок, фармацевтических агентов, нутрицевтиков, растительных экстрактов, средств для отбеливания зубов и их комбинаций.2. Способ изготовления кондитерского продукта, содержащего экструдированную корпусную часть, имеющую множество расположенных в ней ...

СПОСОБ УЛУЧШЕНИЯ УПРАВЛЯЮЩИХ ФУНКЦИЙ

... 1. Применение композиции для изготовления продукта для улучшения управляющих функций у субъекта, нуждающегося в этом, причем указанная композиция содержит:i) один или несколько из уридина и цитидина или их солей, фосфатов, ацильных производных или сложных эфиров; иii) липидную фракцию, содержащую по меньшей мере одну из докозагексаеновой кислоты (22:6; DHA), эйкозапентаеновой кислоты (20:5; ЕРА) и докозапентаеновой кислоты (22:5; DPA) или их сложных эфиров.2. Применение композиции для изготовления продукта для лечения субъекта, нуждающегося в этом, причем указанная композиция содержит:i) один или несколько из уридина и цитидина или их солей, фосфатов, ацильных производных или сложных эфиров; иii) липидную фракцию, содержащую по меньшей мере одну из докозагексаеновой кислоты (22:6; DHA), эйкозапентаеновой кислоты (20:5; ЕРА) и докозапентаеновой кислоты (22:5; DPA) или их сложных эфиров,причем указанный субъект проходит тестирование на управляющие функции.3. Применение по п. 2, в котором ...

СПОСОБ НОРМАЛИЗАЦИИ МОЧЕИСПУСКАНИЯ ПРИ НАРУШЕНИИ ФУНКЦИИ ПОЧЕК

... 1. Фармацевтический состав, содержащий терапевтически эффективное количество KW-3902, или его фармацевтически приемлемой соли, эфира, амида, метаболита или пролекарства, и аденозин-неблокирующий проксимальный или дистальный диуретик. 2. Состав по п.1, где диуретик представляет собой проксимальный диуретик. 3. Состав по п.1, где диуретик представляет собой дистальный диуретик. 4. Состав по п.1, где диуретик выбирают из группы, состоящей из гидрохлоротиазидов, норсемида, спиронолактона, триамтерена и амилорид - тиазидов. 5. Способ индуцирования диуретического эффекта у нуждающегося в этом человека-пациента, поддержания или восстановления диуретического эффекта аденозин-неблокирующего диуретика у нуждающегося в этом пациента, поддержания или восстановления почечной функции у нуждающегося в этом пациента, предотвращения или замедления начала нарушения почечной функции у пациента с повышенным содержанием жидкости в организме или хронической сердечной недостаточностью, лечения пациента, страдающего ...

ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, ВКЛЮЧАЮЩИЕ АГОНИСТЫ В-2-АДРЕНЕРГИЧЕСКИХ РЕЦЕПТОРОВ И КСАНТИНЫ

... 1. Фармацевтическая композиция в виде таблетки, включающая (i) слой с замедленным высвобождением, включающий по меньшей мере один ксантин, и (ii) слой с немедленным высвобождением, включающий по меньшей мере один агонист β-2-адренергических рецепторов, выбранный из группы, состоящей из агонистов β-2-адренергических рецепторов пролонгированного действия и кратковременного действия. 2. Фармацевтическая композиция по п.1, где указанный агонист β -2-адренергических рецепторов пролонгированного действия выбран из группы, включающей сальметерол, бамбутерол и формотерол или их фармацевтически приемлемую соль, сольват или физиологически функциональное производное. 3. Фармацевтическая композиция по п.2, где указанный агонист β-2-адренергических рецепторов пролонгированного действия представляет собой бамбутерол гидрохлорид. 4. Фармацевтическая композиция по п.1, где указанный агонист β-2-адренергических рецепторов кратковременного действия выбран из группы, включающей пирбутерол ацетат, битолтерол ...

СОДЕРЖАЩИЕ ВАРДЕНАФИЛ ЛЕКАРСТВЕННЫЕ ФОРМЫ С РЕГУЛИРУЕМЫМ ВЫСВОБОЖДЕНИЕМ ДЕЙСТВУЮЩЕГО ВЕЩЕСТВА

... 1. Галеновая форма применения с регулируемым высвобождением действующего вещества, которая в качестве действующего вещества содержит ингибитор фосфодиэстеразы 5 варденафил и/или его фармацевтически совместимые соли, гидраты и/или сольваты, и которая характеризуется средней скоростью высвобождения, определяемой временем высвобождения 80% действующего вещества, от 2 до 24 ч.2. Галеновая форма применения по п.1 со средней скоростью высвобождения, определяемой временем высвобождения 80% действующего вещества, от 3 до 20 ч.3. Галеновая форма применения по п.1 со средней скоростью высвобождения, определяемой временем высвобождения 80% действующего вещества, от 3 до 18 ч и начальным высвобождением, определяемым количеством высвобождающегося в течение первых 30 мин действующего вещества, менее 65%.4. Галеновая форма применения по п.1, отличающаяся тем, что начальное высвобождение, определяемое количеством высвобождающегося в течение первых 30 мин действующего вещества, составляет от 0 до 30%.5.

СПОСОБЫ ИЗГОТОВЛЕНИЯ ЛЕКАРСТВЕННЫХ СОСТАВОВ АЦИКЛОВИРА

... 1. Фармацевтический состав, включающий (а) ацикловир и (б) агент доставки формулы или его соль, где Ar представляет собой фенил или нафтил при этом Ar возможно замещен одним или более из -ОН, галогена, C1-C4алкила, С1-С4алкенила, C1-C4алкокси или C1-C4галоалкокси; R7 представляет собой C4-C20алкил, С4-С20алкенил, фенил, нафтил, (С1-С10алкил)фенил, (C1-С10алкенил)фенил, (C1-С10алкил)нафтил, (С1-С10алкенил)нафтил, фенил(С1-С10алеил), фенил(С1 -С10алкенил), нафтил(С1-С10алкил), или нафтил(С1-С10алкенил); R8 представляет собой водород, C1 до С4 алкил, С2 до C4 алкенил, C1 до С4 алкокси, или C1-C4 галоалкокси; при этом R7 возможно замещен C1 до C4 алкилом, C2 до С4 алкенилом, C1 до C4 алкокси, C1-C4 галоалкокси, -ОН, -SH, -CO2R9 или их любой комбинацией; R9 представляет собой водород, C1 до C4 алкил, или C2 до C4 алкенил; причем R7 может быть прерван кислородом, азотом, серой или любой их комбинацией. 2. Фармацевтический состав, включающий (а) ацикловир и (б) агент доставки формулы или его соль ...

Formulierungen mit kontrollierter Abgabe überzogen mit wässrigen Dispersionen von Ethylcellulose

Stabilisiertes Substrat für kontrollierte Freigabe mit von einer wässerigen Dispersion eines hydrophobischen Polymers abgeleitete Beschichtung

New topical composition for treating herpes family viruses, reduces treatment-related erythema but maintains high activity

Topical pharmaceutical formulation comprising aciclovir, dimethicone and at least 30 w/w % of a water miscible polyhydric alcohol, is new. Independent claims are also included for: (1) an oil-in-water pharmaceutical formulation comprising water, solubilized aciclovir, dimethicone and at least 30 w/w % of a water-miscible polyhydric alcohol, as well as a continuous aqueous phase in which is dispersed an oil phase; (2) use of aciclovir, dimethicone and at least 30 w/w % of a water miscible polyhydric alcohol in the preparation of a topical medicament for treating herpes family viral infections; (3) use of dimethicone in decreasing irritancy of topical oil-in-water formulations comprising at least 30 w/w % of a water-miscible polyhydric alcohol. ACTIVITY : Antiviral. MECHANISM OF ACTION : None given.

Kosmetische oder dermatologische Zusammensetzung, die schlankmachend oder gegen Zellulitis wirkt, mit Liposomen Kolaextrakten.

Mikro- oder Nanoemulsion zur ophthalmologischen Anwendung

Mikro- oder Nanoemulsion zur ophthalmologischen Anwendung, enthaltend oder bestehend aus a) hydrophilen Komponenten, enthaltend oder bestehend aus Hyaluronsäure und/oder Chondroitinsulfat und/oder Dexpanthenol sowie mindestens ein Purinalkaloid, b) lipophilen Komponenten, enthaltend oder bestehend aus mittelkettigen Triglyceriden mit einer Kettenlänge der Fettsäuren von 6 bis 18 Kohlenstoffatomen, sowie c) ad 100 Gew.-% Wasser.

Antitumormittel enthaltend einen Komplex einer Oxidoreduktase und eines Polymers und ein Substrat des Enzyms

Verwendung von Theophyllinderivaten zur Behandlung und Propylaxe von Schockzuständen, neue Xanthinverbindungen und Verfahren zu deren Herstellung

Pharmazeutische Formulierungen, die ß-2-Adrenorezeptor-Agonisten und Xantine enthalten

Pharmazeutische Tablettenformulierung, die umfasst (i) eine anhaltende Freisetzungsschicht, die mindestens ein Xanthin umfasst, und (ii) eine sofortige Freisetzungsschicht, die mindestens einen ß-2-Adrenorezeptor-Agonisten umfasst, aufgewählt aus der Gruppe, die besteht aus ß-2-Adrenorezeptor-Agonisten mit langer Wirkungsdauer und solchen mit kurzer Wirkungsdauer.

Purin-Derivate zur Behandlung allergischer Erkrankungen und systemischem Lupus erythematodes

Tablettenförmige Retardzubereitung gegen Schwindel

Pharmazeutische Zusammensetzung mit retardierter Wirkstofffreisetzung, enthaltend Cinnarizin und Dimenhydrinat, Bindemittel, Retardierungsmittel und Füllstoffe, dadurch gekennzeichnet, dass das Gewichts-Verhältnis von Bindemittel/Retardierungsmittel/Füllstoff zwischen 1:0,5:6 und 1:10:50 liegt.

Drug composition and its use in therapy

Purine diones as WNT pathway modulators

Preparations for treatment of recurrent herpetic lesions

Pharmaceutical compositions

The use of a compound of formula I in which R1, R2 and R3 are N or CH, X1 and X2 are hydrogen, hydroxy, or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclyl group and Z1 and Z2 are hydrogen, hydroxy, keto (=O), or an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclyl group or one of Z1 and X1 and Z2 and X2 form a second bond of a double bond at the 1,6 or 2,3 positions with the proviso that at least one of the groupings R1 Z1 X1 R2 Z2 X2 and R1 X1 Z2 form a hydroxamate moiety (-N(OH)C(=O)- and B is a 5 or 6 membered ring of formula II or III in which R4, R5, R6, R7, R8, R9 and R10 are CH or N with the proviso that ring B cannot contain more than 3 ring members which are nitrogen and the ring B may optionally be substituted by one or more of hydroxy, keto (=O), and an optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl or heterocyclyl group or a salt thereof formed with a physiologically acceptable ...

Wound Composition

A composition for the treatment of acute wounds comprises one or more of i) an adenylyl cyclase agonist, ii) cyclic 3', 5'-adenosine monophoshate (CAMP) or a salt or derivative thereof and iii) a phosphodiesterase (PDE) inhibitor. The composition, which can be topically applied, is thought to prevent scarring by elevating CAMP levels in the wound. Preferred examples of suitable substances are i) forskolin, ii) dibutyryl cAMP and iii) isobutyl methyl xanthine (IBMX).

Methods for making active crystalline materials

Method for preparing pharmaceutical formulations

A pharmaceutical formulation may be prepared by a method comprising providing the active ingredient in solution in a pharmacologically-acceptable base and mixing the resulting solution with a pharmacologically-acceptable acid in an amount such that the formulation attains a pH in the range of from about 3.5 to about 8.5 to thereby precipitate out the active ingredients, a viscosity-enhancing agent having been incorporated in the formulation prior to or during the mixing with acid. The formulation is suitable for administration of a pharmacologically active ingredient which is sparingly soluble in water at a pH acceptable for administration, for example to the eye of the patient. Exemplified formulations comprise the antivirals aciclovir, ganciclovir or penciclovir.

Free radical scavenging wound powder

Uric acid as monovalent urate is a potent endogenous antioxidant protecting against free radical damage in man and other animals. The free radical peroxynitrite is implicated in non-healing chronic wounds. Urate is a most efficient scavenger of peroxynitrite forming a reduced radical capable of regeneration back into urate in the presence of ascorbate or thiols. Uricase a ubiquitous enzyme, although absent in human tissues, converts urate to allantoin the latter having potent angiogenic wound healing properties. Persistent bacteria, common in chronic non-healing wounds, would generate allantoin from topically applied urate. Synthetic urate spheres formed in a cation rich aqueous solution at ambient temperature, are extracted in ethanol and air-dried to the wound powder. These spheres show stability in various physiological media and added to the low solubility of urate, ensures prolonged local tissue activity; also precluding the risk of systemic absorption causing gout, although excessive ...

Therapeutic method

Pharmaceutically active 1-Methylxanthine Derivatives

N-3,7 substituted 1-Methylxanthine derivatives of formula I and II,
wherein
```R1 is a linear or branched C1-C4 alkyl group, in particular methyl, ethyl, propyl, butyl, iso-propyl and iso-butyl;
```R2 is a group consisting of:
```R4 is a member consisting of H, -(CH2)nCH3, X, -NH2, -OH, -O(CH2)nCH3 and -NO2;
```R5 is a member consisting of H, -CONH2,
```R3 is a member consisting of halogen, hydroxyl group (OH), saturated 1-3 straight chain carbon atoms, or having a group substituting one H; and n is 0, 1, 2, or 3. In vivo or in vitro experiments prove the carvernosal relaxation induced by these compounds.

Prevention of scarring

Ethynylxanthines, preparation and use as calcium ion channel modulators

The present invention relates to novel pharmaceutical compounds, which exhibit ability to act as calcium ion channel modulators, methods for their synthesis and the treatment and/or prevention of various diseases and disorders including deregulated calcium ion channel activity.

A method for improving farrowing performance

PHARMACEUTICAL TREATMENT

Pharmaceutical formulations comprising -2 adrenoreceptor agonists and xanthines

Promoter of the healing and/or repair and/or regeneration and/or rejuvenation of damaged skin/or body tissue and/or muscles and/or organs of the body

Method for preparing pharmaceutical formulations

Therapeutic mentods

Adenosine receptor modulators for the treatment of circadian rhythm disorders

COMPOSITIONS AND METHODS FOR ALTERING SECOND MESSENGER SIGNALING

Antiviral drugs for treatment or prevention of dengue infection

Method for improving the pharmacokinetic of HIV integrase inhibitors

Valaciclovir tablets containing colloidal silicon dioxide

Derivatives of purine or deazapurine useful for the treatment of inter, alia viral, infections.

Spirocyclic quinazoline derivatives as pde7 inhibitors

Dpp iv inhibitor formulations

The present invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus.

Methods of using a methylxanthine compound

The invention relates to compositions and methods for treating various diseases or medical conditions by administering a methylxanthine compound. Specifically, the invention relates to compositions and methods for treating cytochrome oxidase (CcOX) mediated diseases or medical conditions by administering compositions comprising a methyl xanthine compound.

Enhanced Natural Colors

A natural color is concentrated to intensify color range and to provide useful amounts of one or more of anti-oxidant, nutritional, and anti-inflammatory compounds derived from one or more pigment sources. In a preferred embodiment, the pigment source is a fruit, a vegetable, a legume, a spice, algae, or a combination thereof.

Compositions, use and method for the use of surface active proteins in topical drug delivery across keratin

The present invention provides the use of surface active proteins, especially class I and class II hydrophobins, in topically applied pharmaceutical formulations. The invention is particularly directed to topically applied pharmaceutical products for enhancing the penetration to achieve a transungual delivery of a prophylactically and/or therapeutically effective amount of an active ingredient (drug) to a patient (including animals and humans) into and/or through a nail, of the animal or human body, in order to treat one or more of a variety of diseases or disorders. Related embodiments of the invention are also disclosed.

Novel kinase modulators

The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.

Easily administrable solid preparation

It is an object to provide a coating composition, which is used for an orally-administered preparation, the administering property of which has been improved, and/or an easily administrable preparation that does not affect dissolution property. The aforementioned object can be achieved using a coating composition comprising a first thickener selected from the group consisting of a carboxyvinyl polymer and sodium alginate, a polyvalent metal compound, and at least one type of a second thickener selected from the group consisting of xanthan gum, guar gum and sodium alginate, with the proviso that when the first thickener is sodium alginate the second thickener is not sodium alginate, or using a coating composition comprising, as thickeners, hydroxypropylmethylcellulose and sugar or sugar alcohol having a solubility at 20° C. of 30 or more.

Compounds and compositions for treating chemical warfare agent-induced injuries

Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols as phosphodiesterase inhibitors

Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.

Combination Preparation Against Vertigo

The use of cinnarizine and dimenhydrinate or their physiologically compatible salts in combination is described for the treatment of vertigo of any genesis.

Theophylline Derivative Inhibits Osteoporosis

The theophylline derivative disclosed in the present invention is characterized by having the pharmaceutical functions of osteoporosis. The theophylline derivative protects against bone resorption and inflammatory mediator infiltration.

Method of treatment of cancer patients

This invention may be used in human and veterinary medicine in combination with traditional methods of treatment of oncological illnesses for the purpose of increasing their effectiveness. It is a method of treating patients with oncological diseases that is distinct in that an antiviral drug is used as an additional component of standard treatment before the beginning of and in parallel with standard treatment, in which Acyclovir, Valacyclovir, alpha interferon, a specific antiviral immunoglobulin or a combination of these substances are used as an antiviral drug, which may be used for inclusion in the standard surgical, radiological, or chemotherapeutic treatment plan for cancer patients. The proposed method allows us to significantly improve the results of the treatment of cancer patients, decrease the number of relapses, improve patients' quality of life, and significantly extend their lives. Because the proposed drugs are already approved for use, there are no technical difficulties facing their inclusion in cancer patients' treatment plans.

Composition comprising a pde4 inhibitor and a pde5 inhibitor

The claimed subject matter relates to pharmaceutical compositions comprising a PDE4 inhibitor and a PDE5 inhibitor and the treatment of a disease in which phosphodiesterase 4 (PDE4) and/or phosphodiesterase 5 (PDE5) is detrimental.

Methods of optimizing drug therapeutic efficacy for treatment of immune-mediated gastrointestinal disorders

The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.

Pharmaceutical Compositions

Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.

Pyrrolopyrimidine compounds and their uses

The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrrolopyrimidine compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.

Hsp90 Inhibitors

The present application provides compounds useful in the inhibition of Hsp90, and hence in the treatment of disease.

Method of treating an anxiety disorder

Anxiety disorders, such as panic disorder, agoraphobia, obsessive-compulsive disorder, social phobia, post-traumatic stress disorder, generalized anxiety disorder, specific phobia, or the like, are treated by administering an effective amount of at least one adenosine A 2A receptor antagonist to a patient in need thereof, optionally in combination with an anxiolytic(s) other than the adenosine A 2A receptor antagonist.

Compositions, methods and kits for repressing virulence in gram positive bacteria

Bacterial virulence is repressed by compositions and methods for activating permanently a repressor of virulence factors. Compositions provided contain at least one non-metabolizable analog of guanine, guanosine, isoleucine and valine.

Lipid depot formulations

The present invention relates to pre-formulations comprising low viscosity, non-liquid crystalline, mixtures of: a) at least one neutral diacyl lipid and/or at least one tocopherol; b) at least one phospholipid; c) at least one biocompatible, oxygen containing, low viscosity organic solvent; wherein at least one bioactive agent is dissolved or dispersed in the low viscosity mixture and wherein the pre-formulation forms, or is capable of forming, at least one liquid crystalline phase structure upon contact with an aqueous fluid. The preformulations are suitable for generating parenteral, non-parenteral and topical depot compositions for sustained release of active agents. The invention additionally relates to a method of delivery of an active agent comprising administration of a preformulation of the invention, a method of treatment comprising administration of a preformulation of the invention and the use of a preformulation of the invention in a method for the manufacture of a medicament.

Aqueous solution comprising 3 - quinuclidinones for the treatment hyperproliferative, autoimmune and heart disease

A liquid composition that is an aqueous solution of a compound of formula (I), wherein the aqueous solution has a pH from about 3.0 to about 5.0. The liquid composition may be used in the treatment of a disorder selected from hyperproliferative diseases, autoimmune diseases and heart diseases.

Methods for regulating blood glucose levels

The invention relates to methods and compositions for reducing blood glucose levels in hyperglycaemic subjects. The methods and compositions may therefore be suitable for treating a disease or condition associated with hyperglycaemia such as, for example, obesity (particularly diet induced obesity (DIO)), weight gain, Type II diabetes mellitus, insulin sensitivity, impaired glucose tolerance and inflammation. In some embodiments, the methods comprise administering a melanocortin-5 receptor (MC5R) agonist to one or more skeletal muscle cells of the subject. Preferred MC5R agonists are those that specifically activate MC5R and/or enhance expression of MC5R, such as the melanocortin analogue, Ac-Nle-c[Asp-Pro-D-Nal(2′)-Arg-Trp-Lys]-NH 2 .

Analgesic composition and method of making the same

A soluble aspirin composition, comprising: (i) granules including aspirin, heat-treated bicarbonate salt, pharmaceutically-acceptable resin and surfactant, in mixture with: (ii) crystalline particles of pharmaceutically-acceptable acid; and (iii) crystalline particles of heat-treated bicarbonate salt; wherein the soluble aspirin composition when introduced to water undergoes reaction of the crystalline particles of pharmaceutically-acceptable acid with the heat-treated bicarbonate salt and the aspirin to effect effervescing action and disintegration of the granules with conversion of the aspirin to an acetylsalicylate compound of the bicarbonate salt cation so that the composition rapidly dissolves in the water without occurrence of undissolved residue. The composition is solublizable within 30 seconds in cool to cold water to provide an effervescent analgesic solution that can be readily orally administered to an individual in need of analgesia.

Crosslinked Hydrogels and Related Method of Preparation

The present invention provides a method of manufacturing a hydrogel comprising the step of crosslinking a biopolymer using a carbodiimide crosslinker of Formula I wherein at least one of R 1 and R 2 is a functional group that is a bulky organic functional group. R 1 and R 2 can each independently be an optionally substituted saturated or unsaturated functional group selected from the group consisting of an alkyl, a cycloalkyl, a heterocyclic, and an aryl. The bulky organic functional group will slow down the crosslinking reaction of carbodiimide due to the steric effects and/or electronic effects, in comparison to a crosslinking reaction using EDC. Also provided are the hydrogels and ophthalmic devices prepared using the method of the invention and uses thereof.

Mucosal bioadhesive slow release carrier for delivering active principles

A mucosal bioadhesive slow release carrier comprising an active principle and devoid of starch, lactose, which can release the active principal for a duration of longer than 20 hours. This bioadhesive carrier contains a diluent, an alkali metal alkylsulfate, a binding agent, at least one bioadhesive polymer and at least one sustained release polymer, as well as a method for its preparation.

Famciclovir for the treatment of recurrent herpes labialis using a one-day treatment

A method for the treatment of recurrent herpes labialis in mammals, including humans, which method comprises administering to the mammal in need of such treatment, an effective amount of penciclovir or famciclovir, or a pharmaceutically acceptable salt thereof for a period of one day.

Taste masked pharmaceutical composition

This application relates to taste masked multi-layered particles an inert core, one or more coating layer(s) comprising a pharmaceutically active ingredient and a binder, an intermediate coating layer (seal coating) free from a low molecular weight water-soluble ionic compound and comprising a water-soluble pharmaceutical film-forming compound selected from (i) HPMC and PEG or (ii) PVP, and an outer coating layer (final or taste masking coating) free from a low molecular weight water-soluble ionic compound and comprising (i) a poly(meth)acrylate or (ii) a mixture comprising 60-90% (w/w) EC and 10-40% (w/w) HPMC, wherein the pharmaceutically active ingredient is water-soluble and comprises either at least one basic group and/or a bitter taste. Further disclosed are methods for the production of such particles and pharmaceutical compositions comprising them.

Heteroaryl imidazolone derivatives as jak inhibitors

New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed, as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).

INHALED NO DONOR KMUPS DERIVATIVE PREVENTING ALLERGIC PULMONARY VASCULAR AND BRONCHIAL INFLAMMATION VIA SUPPRESSED CYTOKINES, INOS AND INFLAMMATORY CELL COUNTS IN ASTHMA MODEL

A method for treating a disease is provided. The method includes steps of: providing a subject in need thereof; and administering one selected from a group consisting of KMUPS compound represented by formula I, a pharmaceutically acceptable salts thereof; and a pharmaceutical composition thereof to the subject in a dosage from 1 to 2.5 milligram per kilogram of body weight, 2. A method as claimed in claim 1 , wherein the KMUPS compound comprising is one selected from a group consisting of KMUP-1 claim 1 , KMUP-2 claim 1 , KMUP-3 and KMUP-4.3. A method as claimed in claim 2 , wherein KMUP-1 is 7-[2-[4-(2-chlorobenzene) piperazinyl]ethyl]-1 claim 2 ,3-dimethylxanthine claim 2 , KMUP-2 is 7-[2-[4-(2-methoxybenzene)piperazinyl]ethyl]-1 claim 2 ,3-dimethylxanthine claim 2 , KMUP-3 is 7-[2-[4-(4-nitrobenzene)piperazinyl]ethyl]-1 claim 2 ,3-dimethylxanthine and KMUP-4 is 7-[2-[4-(2-nitrobenzene)piperazinyl]ethyl]-1 claim 2 ,3-dimethylxanthine.4. A method as claimed in claim 1 , wherein the pulmonary inflammation comprising one selected from a group consisting of an obstructive pulmonary disease claim 1 , a pulmonary artery hypertension claim 1 , pulmonary artery proliferation claim 1 , an allergic pulmonary vascular inflammation claim 1 , a physiological activity of a lung cell claim 1 , a vascular remodeling inhibiting disease and a combination thereof.5. A method as claimed in claim 1 , wherein the administering steps is performed by an oral administration.7. A method as claimed in claim 6 , wherein the KMUPS complex compound is one selected from a group consisting of KMUP-1-Atorvastatin complex claim 6 , KMUP-2-Atorvastatin complex claim 6 , KMUP-3-Atorvastatin complex claim 6 , KMUP-4-Atorvastatin complex claim 6 , KMUP-1-Cerivastatin complex claim 6 , KMUP-2-Cerivastatin complex claim 6 , KMUP-3-Cerivastatin complex claim 6 , KMUP-4-Cerivastatin complex; KMUP-1-Fluvastatin complex claim 6 , KMUP-2-Fluvastatin complex claim 6 , KMUP-3-Fluvastatin complex claim 6 , KMUP ...

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

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

COMPOSITION FOR PREVENTION, AMELIORATION OR TREATMENT OF METABOLIC SYNDROME

A composition comprising (a) and (b), and a food or drink or a medicine comprising the composition, wherein 1. A composition for the prevention , amelioration , or treatment of metabolic syndrome , the composition comprising (a) and (b):(a) at least a kind of polyphenols selected from the group consisting of a polyphenol containing 15 mass % or more of proanthocyanidin having a polymerization degree of 1 to 3, hesperidin, a hesperidin derivative, and hesperetin; and(b) at least a kind of xanthine derivatives, the mass ratio of (a):(b) in the composition being 1:(0.001 to 5).2. The composition according to claim 1 , wherein the mass ratio of (a):(b) is 1:(0.01 to 0.5).3. The composition according to claim 1 , wherein the xanthine derivative is caffeine claim 1 , theophylline claim 1 , or theobromine.4. A medicine claim 1 , a food or drink claim 1 , or a feed comprising the composition according to .5. A food or drink comprising the composition according to claim 1 , the food or drink being labeled as at least one selected from the group consisting of improving lipid metabolism; promoting basal metabolism; reducing body weight; reducing visceral fat or subcutaneous fat; having a slimming effect; preventing or treating obesity claim 1 , or ameliorating a symptom thereof; and preventing or treating metabolic syndrome claim 1 , or ameliorating a symptom thereof. The present invention relates to a composition for the prevention, amelioration, or treatment of metabolic syndrome. More specifically, the present invention relates to a composition comprising a polyphenol and a xanthine derivative, for the prevention, amelioration, or treatment of metabolic syndrome.In recent years, with steadily increasing obesity, the World Health Organization (WHO) is warning countries around the world of an increased risk of lifestyle-related diseases, which are associated with obesity and include diabetes, hyperlipidemia, hypertension, arteriosclerosis, and fatty liver. Metabolic syndrome ...

PHARMACEUTICAL COMPOSITION COMPRISING A SGLT2 INHIBITOR IN COMBINATION WITH A DPP-IV INHIBITOR

The invention relates to a pharmaceutical composition according to claim comprising a SGLT2 inhibitor in combination with a DPP IV inhibitor which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions. 2. The pharmaceutical composition according to wherein the DPP IV inhibitor is selected from the group consisting of1-[4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-amino-piperidin-1-yl)-xanthine,1-[([1,5]naphthyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine,1-[(quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine,2-((R)-3-amino-piperidin-1-yl)-3-(but-2-ynyl)-5-(4-methyl-quinazolin-2-ylmethyl)-3,5-dihydro-imidazo[4,5-d]pyridazin-4-one,1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[(2-amino-2-methyl-propyl)-methylamino]-xanthine,1-[(3-cyano-quinolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine,1-(2-cyano-benzyl)-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine,1-[(4-methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-[(S)-(2-amino-propyl)-methylamino]-xanthine,1-[(3-cyano-pyridin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine,1-[(4-methyl-pyrimidin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine,1-[(4,6-dimethyl-pyrimidin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine and1-[(quinoxalin-6-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-((R)-3-amino-piperidin-1-yl)-xanthine,or a pharmaceutically acceptable salt thereof.3. The pharmaceutical composition according to characterized in that the composition is suitable for combined or simultaneous or sequential use of the ...

Combination of a GPR119 Agonist and the DPP-IV Inhibitor Linagliptin for Use in the Treatment of Diabetes and Related Conditions

The present invention relates to combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto. 2. The pharmaceutical combination according to wherein the GPR119 agonist is selected from the following compounds:2-Fluoro-N—((R)-2-hydroxy-1-methylethyl)-4-{3-[1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}benzamide;4-{3-[1-(3-tert-Butyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}-2-fluoro-N—((R)-2-hydroxy-1-methylethyl)benzamide;4-{3-[1-(3-tert-Butyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}-N—((R)-2-hydroxy-1-methyl-ethyl)-2-methylbenzamide;4-{3-[1-(3-tert-Butyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}-N-ethy-l-2-fluorobenzamide;4-{3-[1-(3-tert-Butyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}-2-fluoro-N-(2-hydroxyethyl)benzamide;4-{3-[1-(5-tert-Butyl-[1,2,4]oxadiazol-3-yl)piperidin-4-yl]propoxy}-2-fluoro-N—((R)-2-hydroxy-1-methylethyl)benzamide;2-Fluoro-N—((R)-2-hydroxy-1-methylethyl)-4-{3-[1-(5-isopropyl-[1,2,4]oxadiazol-3-yl)piperidin-4-yl]propoxy}benzamide;N—((R)-2-Hydroxy-1-methylethyl)-4-{3-[1-(5-isopropyl-[1,2,4]oxadiazol-3-yl)piperidin-4-yl]propoxy}-2-methylbenzamide;2-Fluoro-N-(2-hydroxyethyl)-4-{3-[1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}benzamide;N—((R)-2-Hydroxy-1-methyl-ethyl)-4-{3-[1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]propoxy}-2-methylbenzamide;N—((R)-2-Hydroxy-1-methylethyl)-4-{(R)-3-[1-(3-isopropyl-[1,2,4]oxadiazol-5-yl)piperidin-4-yl]butoxy}-2-methylbenzamide;2-Fluoro-N—((R)-2-hydroxy-1-methylethyl)-4-{(R)-3-[1-(5-isopropyl-[1,2,4]oxadiazol-3-yl)piperidin-4-yl]butoxy}benzamide;N-(2-Hydroxyethyl)-4-{3-[1-(5-isopropyl-[1,2,4]oxadiazol-3-yl)piperidin-4-yl]propoxy}-2-methylbenzamide;2-Fluoro-N-(2-hydroxyethyl)-4-{3-[1-(5-isopropyl-[1,2,4]oxadiazol-3-yl)piperidin-4-yl]propoxy}benzamide;2-Fluoro-N—((R)-2-hydroxy-1- ...

TRANSMUCOSAL COMPOSITION CONTAINING ANTHOCYANINS FOR ALLEVIATING A VISUAL DISCOMFORT

The present invention relates to a composition comprising a natural extract containing anthocyanins and an agent for enhancing vigilance, and to a method for alleviating visual discomfort related to or caused by oxidative stress comprising administering via transmucosal route the composition of the invention, said composition being in a form adapted to transmucosal administration, said form preferably being a chewing gum, an orodispersible/orodisintegrating tablet or film or a buccal spray. 1. A composition comprising a natural extract containing anthocyanins , an agent for enhancing vigilance , and optionally at least one of lutein , zeaxanthin , meso-zeaxanthin and asthaxanthin; said composition being in an unitary dosage form adapted to transmucosal administration , said unitary dosage form preferably being a chewing gum , an orodispersible/orodisintegrating tablet or film or a buccal spray.2. A composition according to claim 1 , wherein said composition is a nutraceutical composition claim 1 , a food or dietary supplement claim 1 , a functional food or a pharmaceutical composition.3. A composition according to or claim 1 , wherein said transmucosal administration is a buccal administration.4. A composition according to anyone of to claim 1 , wherein said agent for enhancing vigilance is at least one of caffeine claim 1 , taurin and vitamin C claim 1 , preferably caffeine.5. A composition according to anyone of to claim 1 , wherein said unitary dosage form comprises an amount of natural extract containing anthocyanins ranging from 0.1 to 200 mg.6Vaccinium MyrtillusRubusRubus occidentalisVaccinium corymbosumVaccinium macrocarponVaccinium oxycoccusRubus idaeusFragaria X ananassaPrunus virginianaViburnum trilobumAmelanchier alnifoliaShepherdia argenteaRubus articusRibes nigrumRubus chamaemorusEmpetrum nigrum, Empetrum hermaphroditumSambucusRibes uvacrispaVaccinium vitisidaeaRubus loganobaccusSorbusHippophae rhamnoidesPunica granatumLycium barbarumGarcinia ...

THEOBROMINE FOR INCREASING HDL-CHOLESTEROL

Theobromine for use in the treatment of increasing HDL-cholesterol and/or increasing the ratio HDL-cholesterol:LDL-cholesterol in humans and the use of theobromine for increasing HDL-cholesterol in humans, and/or for increasing the ratio HDL-C/LDL-C, and compositions comprising theobromine. 1. Theobromine for use in the treatment of improving blood lipids.2. Theobromine for use in the treatment of increasing HDL-cholesterol in humans.3. Theobromine for use in the treatment of increasing the ratio HDL-cholesterol/LDL-cholesterol in humans.4. Theobromine for use in the treatment of increasing the ratio HDL-cholesterol/non-HDL-cholesterol in humans.5. Theobromine for use in the treatment according to any of to , wherein the treatment comprises ingestion by a human of from 300 to 2000 mg theobromine per day.6. Theobromine for use in the treatment according to claim 4 , wherein the treatment comprises ingestion from 400 to 1800 mg theobromine per day claim 4 , preferably from 500 to 1500 theobromine mg per day claim 4 , more preferably from 600 to 1400 mg theobromine per day claim 4 , even more preferably from 700 to 1300 mg theobromine per day claim 4 , most preferably from 750 to 1250 mg theobromine per day.7. Theobromine for use in the treatment according to any of to claim 4 , wherein the theobromine is ingested for at least 5 days per week for at least 3 weeks claim 4 , preferably for at least 5 days per week for at least 4 weeks.8. Theobromine for use in the treatment according to any of to claim 4 , wherein theobromine is ingested in the form of encapsulates.9. Edible composition comprising theobromine and plant sterols claim 4 , wherein the amount of theobromine is between 500 and 2000 mg per daily dosing and the amount of plant sterols is 1 to 3 g per daily dosing.10. Edible composition comprising theobromine and plant sterols claim 4 , wherein the amount of theobromine is between 300 and 2000 mg per daily dosing and the amount of plant sterols more than 1.8 g ...

COMPOSITIONS AND METHODS FOR TREATING DIABETES USING LISOFYLLINE ANALOGS AND ISLET NEOGENESIS ASSOCIATED PEPTIDE

Pharmaceutical compositions and methods are provided for treating diabetes and/or restoring β-cell mass and function in a mammal in need thereof. Type 1 diabetes mellitus (T1 DM) is an autoimmune disorder characterized by immune damage to pancreatic beta-cells. Lisofylline analogs (LSF analogs) are immunomodulators that reduce interlukin 12 signaling and reduce the onset of T1 DM in non-obese diabetic (NOD) mice. A combination therapy with both LSF analog (pretreatment) and INGAP provides protection from autoimmune destruction. The concomitant or combination of an LSF analog and INGAP after pre-treatment with an LSF analog is an effective therapy for a disease or condition resulting from the loss of pancreatic islet cells or insulin production in a mammal. 1. A method for treating diabetes in a mammal , comprising a first step of administering to the mammal a therapeutically-effective amount of a pharmaceutical composition comprising biological response modifier in admixture with a pharmaceutically acceptable carrier , diluent , excipient , adjuvant or vehicle followed by a second step of administering a therapeutically-effective amount of a pharmaceutical composition comprising INGAP in admixture with a pharmaceutically acceptable carrier , diluent , excipient , adjuvant or vehicle.2. The method of claim 1 , wherein the biological response modifier is an immunomodulator including pharmaceutically acceptable enantiomers claim 1 , diastereomers claim 1 , tautomers claim 1 , salts and solvates thereof.4. The method of claim 3 , wherein Ris substituted with a member of the group consisting of N—OH claim 3 , acylamino claim 3 , cyano group claim 3 , sulfo claim 3 , sulfonyl claim 3 , sulfinyl claim 3 , sulfhydryl (mercapto) claim 3 , sulfeno claim 3 , sulfanilyl claim 3 , sulfamyl claim 3 , sulfamino claim 3 , and phosphino claim 3 , phosphinyl claim 3 , phospho claim 3 , phosphono and —NRR claim 3 , wherein each of Rand Rmay be the same or different and each is ...

DPP IV INHIBITOR FORMULATIONS

The present invention relates to pharmaceutical compositions of DPP IV inhibitors with an amino group, their preparation and their use to treat diabetes mellitus. 2. The pharmaceutical composition of further comprising an additional disintegrant.3. The pharmaceutical composition of claim 2 , wherein the additional disintegrant is crospovidone.4. The pharmaceutical composition of further comprising a glidant.5. The pharmaceutical composition of claim 4 , wherein the glidant is colloidal silicon dioxide.8. The pharmaceutical composition according to in the dosage form of a capsule claim 1 , a tablet claim 1 , or a film-coated tablet.9. The pharmaceutical composition of comprising 2-4% film coat.10. The pharmaceutical composition of claim 9 , wherein the film coat comprises a film-forming agent claim 9 , a plasticizer claim 9 , a glidant and optionally one or more pigments.11. The pharmaceutical composition of claim 10 , wherein the film coat comprises hydroxypropylmethylcellulose (HPMC) claim 10 , polyethylene glycol (PEG) claim 10 , talc claim 10 , titanium dioxide and iron oxide.12. A process for the preparation of a pharmaceutical composition according to comprising a. dissolving the binder in a solvent to produce a granulation liquid;b. blending the DPP-IV inhibitor, a diluent, and the disintegrant to produce a pre-mix;c. moistening the pre-mix with the granulation liquid and subsequently granulating the moistened pre-mix;d. optionally sieving the granulated pre-mix through a sieve with a mesh size of at least 1.0 mm;e. drying the granulate at about 40-75° C. until the desired loss on drying value in the range of 1-5% is obtained;f. sieving the dried granulate through a sieve with a mesh size of at least 0.6 mm;g. adding the lubricant to the granulate for final blending.13. The process according to further comprisingh. compressing the final blend into tablet cores;i. preparing a coating suspension;j. coating the tablet cores with the coating suspension to a weight ...

METHOD OF TREATING A VIRAL INFECTION DYSFUNCTION BY DISRUPTING AN ADENOSINE RECEPTOR PATHWAY

Described herein is a method of treating a viral infection such as an influenza infection, in a subject comprising administering an effective amount of a pharmaceutical composition to disrupt a adenosine receptor pathway, such as the Aradenosine receptor pathway, in a subject. The adenosine receptor pathway includes the steps of 1) producing the adenosine precursor adenosine triphosphate (ATP), 2) releasing ATP into the extracel lular space, 3) enzymatic conversion of ATP to adenosine, 4) activation of the adenosine receptor and the adenosine receptor cascade, and 5) clearance of adenosine from the extracellular space by degradation or uptake into a cell. The method includes affecting at least one of these steps so as to decrease the activation of the adenosine receptor pathway. This may be accomplished by decreasing the production, release, or conversion of ATP to adenosine, decreasing the expression of the adenosine receptor, antagonizing adenosine receptor activation, and/or increasing adenosine clearance. 1. A method of treating a subject for a pulmonary , cardiac , and/or renal dysfunction resulting from an influenza infection comprising:administering an effective amount of a pharmaceutical composition to disrupt an adenosine receptor pathway in the subject to treat the pulmonary, cardiac, or renal dysfunction.2. The method of wherein the adenosine receptor pathway is in at least one of the lung tissue claim 1 , the cardiac tissue claim 1 , or the renal tissue of the subject.3. The method of wherein the adenosine receptor pathway is the A-adenosine receptor pathway.4. The method of wherein the disruption of the adenosine receptor pathway includes at least one of the decreasing the synthesis of ATP claim 1 , decreasing the release of ATP from a cell claim 1 , decreasing the conversion of ATP to adenosine claim 1 , decreasing the expression of the adenosine receptor claim 1 , decreasing the activation of the adenosine receptor claim 1 , and increasing the ...

Compositions and methods for treating symptoms of inflammatory related conditions using a combination of an antihistamine and a stimulant

The present invention relates to compositions containing stimulant and anti-histamine compounds, to methods for treating symptoms related to inflammation using the combination compounds, and to a method for preparing the compositions.

INDUCTION OF IMMUNE RESPONSE

Provided are methods and compositions that can be used to treat subjects having a viral infection by provoking an immune response using newly discovered antigens that are non-naturally occurring variations on viral glycoproteins. For example, provided are viral glycoproteins or a fragments thereof, or, DNA constructs encoding for such viral glycoproteins or fragments thereof, wherein the glycoprotein or fragment comprises a glycosylation sequon that includes a non-templated aspartic acid residue. 1. A method for treating a subject having a viral infection comprising: a viral glycoprotein or a fragment thereof,', 'or,', 'a DNA construct encoding for said viral glycoprotein or fragment thereof,, 'administering to said subject a composition comprising'}wherein said glycoprotein or fragment comprises a glycosylation sequon that includes a non-templated aspartic acid residue.2. The method according to wherein said glycoprotein is an envelope protein.3. The method according to wherein said glycoprotein is an HBV small envelope glycoprotein claim 2 , an HBV middle envelope glycoprotein claim 2 , or an HBV large envelope glycoprotein.4. The method according to further comprising administering to said subject a glucosidase inhibitor claim 1 , an antiviral agent claim 1 , or both.5. The method according to wherein said antiviral agent is a nucleoside analog.6. The method according to wherein said antiviral agent is 1-(2-fluoro-5-methyl-beta-L-arabinofuranosyl)-uracil claim 5 , or 2-Amino-9-[(1S claim 5 ,3R claim 5 ,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-6 claim 5 ,9-dihydro-3H-purin-6-one.7. The method according to wherein said glucosidase inhibitor is 6-O-butanoyl castanospermine or a deoxynorjirmycin.8. The method according to wherein said subject is infected with an enveloped virus.9. The method according to wherein said virus is hepatitis B or hepatitis C.10. A viral glycoprotein or a fragment thereof claim 1 ,or,a DNA construct encoding for said viral ...

COMPOSITIONS AND METHODS OF TREATING A PROLIFERATIVE DISEASE WITH A QUINAZOLINONE DERIVATIVE

Provided are methods that relate to a novel therapeutic strategy for the treatment of cancers. In particular, the method comprises administration of Compound A, 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein the compound or a pharmaceutically acceptable salt thereof is the (S)-enantiomer.3. A composition comprising the compound according to or a pharmaceutically acceptable salt thereof claim 1 , and at least one pharmaceutically acceptable excipient.4. The composition according to claim 3 , wherein the composition comprises the (S)-enantiomer of the compound or a pharmaceutically acceptable salt thereof claim 3 ,wherein the (S)-enantiomer of the compound or a pharmaceutically acceptable salt thereof is present in excess of the (R)-enantiomer of the compound or a pharmaceutically acceptable salt thereof.5. The composition according to claim 4 , wherein the composition is substantially free of the (R)-enantiomer of the compound or a pharmaceutically acceptable salt thereof.6. A method of treating a condition in a patient claim 1 , wherein the condition is cancer claim 1 , comprising administering to the patient a composition comprising the compound according to and at least one pharmaceutically acceptable excipient.7. The method according to claim 6 , wherein the composition comprises the (S)-enantiomer of the compound or a pharmaceutically acceptable salt thereof claim 6 ,wherein the (S)-enantiomer of the compound or a pharmaceutically acceptable salt thereof is present in excess of the (R)-enantiomer of the compound or a pharmaceutically acceptable salt thereof.8. The method according to claim 7 , wherein the composition is substantially free of the (R)-enantiomer of the compound or a pharmaceutically acceptable salt thereof.9. The method according to claim 7 , wherein the (S)-enantiomer of the compound or a pharmaceutically acceptable salt thereof predominates over the (R)-enantiomer of the compound or a ...

REMEDY FOR MIGRAINE HEADACHE

A medicated formulation and method of use for treating migraine having a combination of active ingredients including: nicotine, and tryptophan alone and also with phenylalanine and/or, tyrosine, and/or caffeine in an aqueous solution. 1. A medication formulation for treating migraine comprising an aqueous solution containing active ingredients including an effective amount of: nicotine , tryptophan , phenylalanine , tyrosine and caffeine , wherein the nicotine comprises not less than 0.222 mg.2. A medication formulation for treating migraine comprising an aqueous solution containing active ingredients including an effective amount of: nicotine and tryptophan , wherein the nicotine comprises not less than 0.222 mg.3. The medication formulation for treating migraine of claim 2 , further comprising an effective amount of phenylalanine.4. The medication formulation for treating migraine of claim 3 , further comprising an effective amount of tyrosine.5. The medication formulation for treating migraine of claim 4 , further comprising an effective amount of caffeine.6. The medication formulation for treating migraine of claim 1 , wherein the solution contains 0.222 mg nicotine claim 1 , 40 mg tryptophan claim 1 , 20 mg phenylalanine claim 1 , 60 mg tyrosine claim 1 , and 85 mg caffeine in two liquid ounces of water.7. The medicated formulation of wherein the nicotine represents about 0.11% by weight of the active ingredients.8. The medicated formulation of wherein the tryptophan represents between 15 and 30% by weight of the active ingredients.9. The medicated formulation of wherein the phenylalanine represents between 5 and 15% by weight of the active ingredients.10. The medicated formulation of wherein the tyrosine represents between 20 and 30% by weight of the active ingredients.11. The medicated formulation of wherein the caffeine represents between 35 and 50% by weight of the active ingredients.12. The medicated formulation of wherein the active ingredients are by ...

COMPOSITION FOR INHIBITING THE ACTIVITY OF INOSITOL 1,4,5-TRIPHOSPHATE RECEPTOR SUBTYPE III

An agent for inhibiting the activity of inositol-1,4,5-triphospate receptor subtype 3 (IPR3), containing caffeine and/or its analogs, and/or their pharmaceutically acceptable salts, as an active ingredient, is provided. A composition for preventing and/or treating a disease associated with Ca release through IPR3, containing the IPR3 inhibiting agent, is also provided. 1. A method of inhibiting inositol-1 ,4 ,5-triphospate receptor subtype 3 (IPR3) comprising administering at least one compound selected from the group consisting of caffeine , 7-isopropyl theophylline , 7-(β-hydroxyethyl)theophylline , xanthine , theophylline , 1 ,7-dimethyl-3-isobutyl xanthine , and their pharmaceutically acceptable salts , as an active ingredient , in a patient in need thereof.2. A method of treating a disease associated with over-release of Ca release comprising administering at least one compound selected from the group consisting of caffeine , 7-isopropyl theophylline , 7-(β-hydroxyethyl)theophylline , xanthine , theophylline , 1 ,7-dimethyl-3-isobutyl xanthine , and their pharmaceutically acceptable salts as an active ingredient , in a patient in need thereof.3. The method according to claim 2 , wherein said disease associated with over-release of Ca release is one or more selected from the group consisting of brain stroke claim 2 , anxiety claim 2 , overactive bladder syndrome claim 2 , inflammatory bowel disease claim 2 , irritable bowel syndrome claim 2 , interstitial colitis claim 2 , brain external injuries claim 2 , migraine claim 2 , chronic claim 2 , neuropathic or acute pain claim 2 , drug or alcohol addiction claim 2 , neuropathic disorder claim 2 , mental disorder claim 2 , sleep disorder claim 2 , phobic disorder claim 2 , obsessive-compulsive disorder claim 2 , post-traumatic stress disorder (PTSD) claim 2 , depression claim 2 , epilepsy claim 2 , diabetes claim 2 , cancer/tumor claim 2 , male infertility; hypertension claim 2 , pulmonary hypertension claim 2 , ...

Topical antiviral formulations

The disclosure provides antiviral pharmaceutical compositions comprising one or more antiviral compounds and 2-deoxy-D-glucose in the form of lip-balms, creams and ointments. A specific embodiment discloses a lip-balm composition comprising acyclovir and 2-deoxy-D-glucose.

NOVEL PHARMACEUTICAL DOSAGE FORMS COMPRISING VALGANCICLOVIR HYDROCHLORIDE

The present invention provides novel solid pharmaceutical dosage forms for oral administration, after being constituted in water. The solid dosage forms comprise a therapeutically effective amount of valganciclovir hydrochloride and a non-hygroscopic organic acid present in an amount sufficient to stabilize the valganciclovir hydrochloride in a predetermined amount of water. The present invention also provides novel liquid pharmaceutical dosage forms for oral administration after constituting the solid pharmaceutical dosage form with water. A non-hygroscopic bulking agent may optionally be included in the above dosage form. These novel pharmaceutical dosage forms are useful in the treatment or control of viruses such as herpes simplex virus and cytomegalovirus. The present invention also provides a method for treating these diseases employing the solid and liquid pharmaceutical dosage forms and a method for preparing these pharmaceutical dosage forms. 2. The solid dosage form according to claim 1 , wherein valganciclovir hydrochloride is present in an amount from about 10% to about 90% claim 1 , by weight of the total composition.3. The solid dosage form according to claim 1 , wherein the non-hygroscopic organic acid is selected from the group consisting of fumaric acid claim 1 , succinic acid claim 1 , and adipic acid.4. The solid dosage form according to claim 4 , wherein the non-hygroscopic organic acid is fumaric acid.5. The solid dosage form according to claim 1 , wherein the non-hygroscopic organic acid is aspartic acid or glutamic acid.6. The solid dosage form according to claim 1 , further comprising an effective amount of a non-hygroscopic bulking agent.7. The solid dosage form according to claim 7 , wherein the non-hygroscopic bulking agent is selected from the group consisting of mannitol and lactose.8. The solid dosage form according to claim 8 , wherein the non-hygroscopic bulking agent is mannitol.9. The solid dosage form according to claim 7 , wherein ...

METHOD FOR TREATMENT OF BRAIN CANCERS

A method for preventing and/or treating brain tumor, including administering caffeine and/or its analog, and/or their pharmaceutically acceptable salt, as an active ingredient, to a patient in need thereof, is provided. The method for preventing or treating brain tumor has an activity to inhibit invasion, migration, and proliferation of brain tumor cells, and thereby very effective for the prevention and treatment of brain tumor. 1. A method for treatment of a brain tumor , comprising administering a therapeutically effective amount of at least one selected from the group consisting of caffeine , 7-isopropyl theophylline , 7-(β-hydroxyethyl)theophylline , xanthine , theophylline , 1 ,7-dimethyl-3-isobutyl xanthine , and their pharmaceutically acceptable salts , to a patient in need thereof.2. The method according to claim 1 , wherein the brain tumor is one or more selected from the group consisting of glioma claim 1 , meningioma claim 1 , pituitary adenoma claim 1 , schwannoma claim 1 , craniopharyngioma claim 1 , and congenital brain tumor.3. The method according to claim 2 , wherein the glioma is glioblastoma.4. The method according to claim 1 , wherein the treatment of a brain tumor is by selectively blocking inositol-1 claim 1 ,4 claim 1 ,5-triphospate receptor subtype 3 (IPR3) on lesion cells. This application is a Continuation application of pending U.S. Ser. No. 12/865,127 filed on Nov. 19, 2010, which is the National Stage Application of International Application No. PCT/KR2008/000602 filed on Jan. 31, 2008, which claims priority to Korean Patent Application No. 10-2008-0010155 filed on Jan. 31, 2008, the contents of which are incorporated herein by reference.(a) Field of the InventionA method for preventing and/or treating brain tumor, including administering caffeine and/or its analog, and/or their pharmaceutically acceptable salt, as an active ingredient, to a patient in need thereof, is provided.(b) Description of the Related ArtThe term “brain tumor (or ...

Integrated Neuromodulation System for Mood Enhancement of a Living Human Subject

The present invention is an ingestable blended formulation which will cause a series of distinct biochemical changes in-vivo; initiate desirable psychological consequences in that person; and induce an observable increase in cognitive functions for that living human subject. In particular, the initiated psychological events will generate a positive change in one's personal perceptions, evoke optimism as the subjective state of mind, and elicit a more sociable attitude and favorable mood as the observable behavior of the affected human person. Moreover, in addition to the initiation of a more positive state of mind, another major result and effect of ingesting the blended formulation is an observable amplification of human brain functions and a substantive increase of human concentration, focus and memory. 1. A non-prescription blended formulation suitable for ingestion by a living human subject , and which after ingestion is able to induce a more positive mood for and to initiate an observable enhancement of cognitive functions in a living human subject , said blended formulation comprising:a controlled admixture of five essential active ingredients, each of which is able to pass the blood-brain barrier in-vivo, said controlled admixture being limited to(a) not less than two different naturally existing nootropic dopamine neurotransmitter agonist,(b) not less than one naturally existing nootropic acetylecholine neurotransmitter agonist,(c) not less than one naturally existing nootropic serotonin neurotransmitter agonist,(d) not less than one naturally existing nootropic gamma-aminobutyric acid (GABA) neurotransmitter agonist, and(e) at least one nootropic adenosine antagonists,wherein the ratio of all individual nootropic neurotransmitter agonists to all individual nootropic adenosine antagonists is proportionally not less than 5:1, andwherein the neurotransmitter replenishment balance for the admixture of essential active agents mathematically is zero (“0”) in ...

PHARMACEUTICAL COMPOSITIONS AND METHODS FOR TREATING GASTROINTESTINAL INFECTIONS AND DISORDERS

Methods of treating gastrointestinal disorders, in a patient in need thereof, including disorders of the liver and pancreas, using an amount of an orally dosed TLR-7 compound in an amount sufficient to increase IFN in the gastrointestinal area, including the liver, but not significantly increasing systemic IFN. 1. A method of treating a gastrointestinal disorder in a human patient in need thereof , comprising administering to the patient an orally administered amount of a TLR agonist sufficient to provide modified IFN expression in the gastrointestinal area , but in an amount less than sufficient to significantly alter systemic IFN.3. The method of wherein the gastrointestinal disorder is cancer or a pathogen infection.4. The method of wherein the cancer is hepatocellular cancer claim 3 , colorectal cancer claim 3 , gastrinoma claim 3 , insulinoma claim 3 , glucagonoma claim 3 , pancreatic ductal adenocarcinoma claim 3 , VIPoma claim 3 , somatostatinoma claim 3 , ACTHoma claim 3 , adenocarcinoma of the stomach claim 3 , leiomyosarcoma or adenomatous polyposis.5. The method of wherein the pathogen infection is a parasitic infection.6Clonorchis sinensis, Opisthorchis felineus, Opisthorchis viverrini, Dicrocoelium dendriticum, Elaeophora elaphi, Fasciola, Plasmodium, Amoebiasis, Pseudosuccinea columella, Schistosoma mansoni, Visceral leishmaniasis, Histomonas meleagridis, Histomoniasis, Echinococcus multilocularis, Fasciolosis, Schistosomiasis, Capillaria hepatica,Clonorchiasis, ToxoplasmosisOpisthorchiasis.. The method of wherein the parasitic infection is: Prosthogonimidae claim 5 , Alveolar hydatid disease claim 5 , or7. The method of wherein the pathogen infection is a fungal infection.8. The method of wherein the fungal infection is histoplasmosis claim 7 , coccidiodomycosis claim 7 , North American blastomycosis or cryptococcosis.9. The method of wherein the pathogen infection is a bacterial infection.10. The method of wherein the pathogen infection is a viral ...

COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES

Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein. 2. The method of claim 1 , wherein both of Rand Rare H.3. The method of claim 1 , wherein both of Rand Rare alkyl.4. The method of claim 1 , wherein both of Rand Rare methyl.5. The method of claim 1 , wherein m is 1.6. The method of claim 1 , wherein L is NRSO claim 1 , SONR claim 1 , C(O)NR claim 1 , NRC(O) claim 1 , OC(O)NR claim 1 , NRC(O)O claim 1 , or NRC(O)NR.7. The method of claim 1 , wherein L is C(O)NRor NRC(O).8. The method of claim 1 , wherein Ris thiazolyl.9. The method of claim 1 , wherein Ris phenyl.10. The method of claim 1 , wherein Ris phenyl substituted with 2 R.11. The method of claim 1 , wherein Ris H.12. The method of claim 1 , wherein the compound is administered via intramuscular injection.13. The method of claim 1 , wherein the compound is administered topically.14. The method of claim 1 , wherein the compound is administered by topical ocular administration.15. The method of claim 1 , wherein the compound is administered prior to the exposure to the chemical warfare agent.16. The method of claim 1 , wherein the compound is administered after exposure to the chemical warfare agent.17. The method of claim 1 , wherein the chemical warfare agent is tear gas.18. The method of claim 1 , wherein the chemical warfare agent is chlorine.19. The method of claim 1 , wherein the chemical warfare agent is mustard gas.20. The method of claim 1 , wherein the subject is a human.21. The method of claim 1 , wherein the compound is administered orally. This application claims priority from U.S. Ser. No. 61/127,662, filed May 14, 2008, and U.S. Ser. No. 61/082,809, filed Jul. 22, 2008, both of which are incorporated herein by reference in their entirety.The invention relates to compounds and compositions useful for treating injuries caused by chemical warfare and similar agents.A variety of ion channel proteins exist to mediate ion flux across ...

COMPOSITION FOR ENHANCING PHYSICAL PERFORMANCE

This invention relates to a composition that contains quercetin, vitamin B1, vitamin B2, vitamin B3, vitamin B6, vitamin B12, vitamin C, caffeine, epigallocatechin gallate, epicatechin, epicatechin gallate, and epigallocatechin. 1. (canceled)2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. A method of making a preparation for use in improving overall strength , increasing fatigue recovery , increasing endurance to exercise , or increasing skeletal muscle mass in a mammal in need thereof , said comprising contacting a composition comprising quercetin , vitamin C , and vitamin B3 with a suitable diluent.11. The method of claim 10 , wherein the diluent is selected from the group consisting of water claim 10 , lactose and corn starch.12. The method of claim 10 , wherein the preparation comprises 20-2000 mg quercetin claim 10 , 50-2000 mg vitamin C claim 10 , and 0.1-2000 mg vitamin B3.13. The method of claim 10 , wherein the preparation comprises a green tea extract.14. The method of claim 10 , wherein the preparation comprises at least one of caffeine claim 10 , epigallocatechin gallate claim 10 , epicatechin claim 10 , epicatechin gallate claim 10 , and epigallocatechin.15. The method of claim 14 , wherein the preparation comprises at least one of 10-500 mg of epigallocatechin gallate claim 14 , 10-500 mg of epicatechin claim 14 , 10-500 mg of epicatechin gallate claim 14 , and 10-500 mg of epigallocatechin.16. The method of claim 10 , wherein the preparation comprises at least one of vitamin B1 claim 10 , vitamin B2 claim 10 , vitamin B6 claim 10 , vitamin B12 claim 10 , and vitamin E.17. The method of claim 16 , wherein the preparation comprises at least one of 0.1-50 mg of vitamin B1 claim 16 , 0.1-150 mg of vitamin B2 claim 16 , 0.1-200 mg of vitamin B6 claim 16 , and 5-150 μg of vitamin B 12.18. The method of claim 10 , wherein the preparation comprises at least one of CoQ-10 claim 10 , soy isoflavones ...

METHODS AND COMPOSITIONS FOR THE TREATMENT OF INFECTIONS

The instant invention provides preparations comprising an oxidizing antimicrobial agent such as chlorine dioxide and a heterocyclic compound that improves the antibacterial effect of the oxidizing antimicrobial agent preparation. The invention has particular use as an eye care preparation such as an eye drop. The invention further provides methods for reducing bacterial colonization and treating infection. 1. A preparation comprising an oxidizing antibacterial agent and a heterocyclic compound that improves the antibacterial effect of the oxidizing agent.2. The preparation of claim 1 , wherein the heterocyclic compound is a bicyclic compound.3. The preparation of claim 2 , wherein the heterocyclic compound is a xanthine.4. The preparation of claim 2 , wherein the bicyclic compound is selected from the group consisting of caffeine claim 2 , theophylline claim 2 , dyphylline claim 2 , theobromine claim 2 , xanthine claim 2 , xanthinol claim 2 , methylxanthine claim 2 , and aminophylline.5. The preparation of claim 4 , wherein the bicyclic compound is dyphylline.6. The preparation of wherein said oxidizing antibacterial agent is chlorine dioxide.7. The preparation of claim 6 , wherein the chlorine dioxide is present in a concentration of about 25-125 ppm.8. The preparation of claim 7 , wherein the chlorine dioxide is present in a concentration of about 50-75 ppm.9. The preparation of claim 8 , wherein the chlorine dioxide is present in a concentration of about 60 ppm.10. The preparation of claim 1 , wherein the preparation is in the form of a solution claim 1 , cream claim 1 , paste claim 1 , ointment claim 1 , or gel.11. The preparation of claim 1 , wherein the preparation is incorporated into a sustained-release carrier.12. The preparation of wherein said sustained-release carrier is selected from the group consisting of a sustained-release polymer claim 11 , a liposome and a microcapsule.13. The preparation of claim 1 , wherein the preparation is a solution.14. The ...

SUBCUTANEOUS THERAPEUTIC USE OF DPP-4 INHIBITOR

The present invention relates to methods for treating and/or preventing metabolic diseases comprising the subcutaneous or transdermal administration of a therapeutically effective amount of a certain DPP-4 inhibitor. The invention further relates to a subcutaneous combination of a certain DPP-4 inhibitor and GLP-1 having a short half life, particularly for reducing weight. 1) A pharmaceutical combination , composition or kit comprising linagliptin , and a GLP-1 analogue having a short half life or native GLP-1.2) The combination claim 1 , composition or kit according to claim 1 , which is for subcutaneous administration of the active components.3) The combination claim 1 , composition or kit according to claim 1 , which is for simultaneous administration of the active components.4) The combination according to claim 1 , wherein the GLP-1 analogue or native GLP-1 and the linagliptin are present each in separate dosage forms.5) The combination according to claim 1 , wherein the GLP-1 analogue or native GLP-1 and the linagliptin are present in the same dosage form.6) The combination according to claim 1 , wherein the GLP-1 analogue or native GLP-1 and the linagliptin are comprised in a pharmaceutical composition for subcutaneous injection administration.7) The combination according to claim 1 , wherein the GLP-1 analogue or native GLP-1 and the linagliptin are comprised in a pharmaceutical kit claim 1 , where each of the active components is for subcutaneous injection administration.8) A method of using the combination claim 1 , composition or kit according to for treating obesity or overweight claim 1 , or reducing body weight or body fat claim 1 , or suppressing appetite in a subject claim 1 , said method comprising administering linagliptin subcutaneously and the GLP-1 analogue or native GLP-1 subcutaneously to the subject.9) A method for treating and/or preventing obesity or overweight or for reducing body weight in a subject claim 1 , said method comprising ...

Purine compounds as prodrugs of a2b adenosine receptor antagonists, their process and medicinal applications

The present disclosure relates to purine compounds of formula (I) or formula (II) or its tautomers, polymorphs, stereoisomers, solvates or a pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by thereof as A2B adenosine receptor antagonists. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by the mediation of adenosine A2B receptor. Such conditions include, but are not limited to, asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders including inflammatory bowel disease, sickle cell disease, and/or autoimmune diseases, and to their use in treating mammals for various disease states, such as gastrointestinal disorders, immunological disorders, hypersensitivity disorders, neurological disorders, and cardiovascular diseases due to both cellular hyperproliferation and apoptosis, and the like. The present disclosure also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.

Methods and compositons for cell-proliferation-related disorders

Methods of treating and evaluating subjects having neoactive mutants of IDH (e.g., IDH1 or IDH2).

Substituted quinazolines, the preparation thereof and the use thereof in pharmaceutical compositions

The present invention relates to substituted quinazolines of formula (I): 2. The compound of formula (I) according to claim 1 , in whichR1 and R2 are the same or different and are independently selected from 3-(R)-amino-piperidin-1-yl, (2-amino-2-methyl-propyl)-methylamino and (2-(S)-amino-propyl)-methylamino;or a tautomer, enantiomer, diastereomer, mixture or salt thereof.3. The compound of formula (I) according to claim 1 , in which X and Y are the same claim 1 , or a tautomer claim 1 , enantiomer claim 1 , diastereomer claim 1 , mixture or salt thereof.6. Physiologically acceptable salt of the compound according to with an inorganic or organic acid or base.7. Pharmaceutical composition containing a compound of formula (I) according to claim 1 , or a physiologically acceptable salt thereof with an inorganic or organic acid or base claim 1 , optionally together with one or more pharmaceutically acceptable excipients.8. Use of a compound according to for preparing a pharmaceutical composition which is suitable for treating type II diabetes mellitus or obesity.9. Process for preparing a pharmaceutical composition according to claim 7 , characterised in that the compound of formula (I) or a physiologically acceptable salt thereof with an inorganic or organic acid or base is incorporated in one or more pharmaceutically acceptable excipients.10. A method of treating or preventing type II diabetes mellitus or obesity claim 1 , the method comprising administering the compound according to claim 1 , and optionally one or more other active substances claim 1 , to a patient.11. The method according to claim 10 , wherein the one or more other active substances is selected from metformin claim 10 , metformin; sulphonylureas claim 10 , nateglinide claim 10 , repaglinide claim 10 , thiazolidinediones (e.g. pioglitazone) claim 10 , PPAR-gamma agonists claim 10 , alpha-glucosidase blockers claim 10 , insulin or insulin analogues claim 10 , and GLP-1 and GLP-1 analogues.12. ...

METHODS OF INCREASING EFFICIENCY OF VECTOR PENETRATION OF TARGET TISSUE

Methods for increasing the efficiency of target tissue penetration of an adeno-associated virus (AAV) vector in a patient are provided. In some aspects, the methods involve inhibiting the interaction of the serum protein galectin 3 binding protein (G3BP) with AAV vector. Further provided are methods for reducing tissue distribution of a virus or for neutralizing a virus harbored by an organ destined for transplant, or newly transplanted, by administering a composition comprising G3BP. 135.-. (canceled)36. A method of AAV-mediated gene delivery in a subject or method for increasing the efficiency of target tissue penetration of an adeno-associated virus (AAV) vector comprising the administration of a G3BP depleting or neutralizing compound in a patient in need thereof.37. The method of claim 36 , wherein the AAV vector is an AAV6 claim 36 , AAV1 claim 36 , AAV5 claim 36 , or AAV8 vector.38. The method of claim 36 , wherein said compound is a G3BP antibody.39. The method of claim 38 , wherein the antibody is a monoclonal antibody.40. The method of claim 38 , wherein the antibody is a depleting antibody.41. The method of claim 36 , wherein said compound is a G3BP inhibitor selected from the group consisting of: galectins claim 36 , sugars claim 36 , agonistic viral protein claim 36 , murine C reactive protein claim 36 , empty AAV capsids claim 36 , fragments of G3BP capable of interacting with native G3BP claim 36 , and small molecules.42. The method of claim 36 , wherein said compound is administered prior to or substantially simultaneously with exposure of the subject to said virus.43. An AAV vector structurally modified so that the interaction of said AAV vector with G3BP is decreased in comparison to the non modified AAV vector claim 36 , wherein the structural modification involves replacing the capsid of said vector with an AAV capsid claim 36 , comprising a mutation in a VP protein of said capsid resulting in a decrease in the interaction between the vector and ...

Pharmaceutical Combination

A combination comprising as components (a) the compound 3-(3-Dimethylamino-1-ethyl-2-methyl-propyl)-phenol, and (b) one or more non-steroidal anti-inflammatory drugs (NSAIDs); a pharmaceutical salt comprising said components; a compound derived from said components; a pharmaceutical formulation and a dosage form comprising said combination, salt, or compound; as well as a method of treating pain, e.g. chronic or acute pain, in a mammal characterized in that components (a) and (b) are administered simultaneously or sequentially to a mammal, wherein component (a) may be administered before or after component (b) and wherein components (a) or (b) are administered to the mammal either via the same or a different pathway of administration. 24.-. (canceled)5. The composition of claim 1 , wherein said compound corresponding to formula (I′) is present in the form of a solvate.6. The composition of claim 1 , wherein said compound corresponding to formula (I′) is present in the form of an acid addition salt.79.-. (canceled)10. The composition of claim 1 , wherein said compound corresponding to formula (I′) is in the form of an acid addition salt of hydrochloride.1114.-. (canceled)15. The composition of claim 1 , wherein said non-steroidal anti-inflammatory drug (NSAID) is Ibuprofen.16. The composition of claim 1 , wherein components (a) and (b) are present as a salt formed from these two components.17. The composition of claim 1 , wherein components (a) and (b) are present in a weight ratio such that the composition will exert a synergistic effect upon administration to a patient.1839.-. (canceled)40. A composition comprising a combination of (i) and (ii) claim 1 , wherein{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) is a composition as defined in , and'}{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(ii) is a salt comprising a salt formed from both components (a) and (b) as defined in .'}41. The composition of claim 40 , wherein said composition is in the form ...

OLEAGINOUS PHARMACEUTICAL AND COSMETIC FOAM

The invention relates to stable oleaginous cosmetic or therapeutic foam compositions containing certain active agents, having unique therapeutic properties and methods of treatment using such compositions. The foamable composition includes at least one solvent selected from a hydrophobic solvent, a silicone oil, an emollient, a co-solvent, and mixtures thereof, wherein the solvent is present at a concentration of about 70% to about 96.5% by weight of the total composition, at least a non-ionic surface-active agent at a concentration of about 0.1% to less than about 10% by weight of the total composition; at least one gelling agent at a concentration of about 0.1% to about 5% by weight of the total composition; a therapeutically effective amount of at least one active agent; and at least one liquefied or compressed gas propellant, at a concentration of about 3% to about 25% by weight of the total composition. 2. The composition of claim 1 , further comprising a therapeutically effective amount of at least one active agent.3. The composition of claim 1 , wherein the composition has less than about 5% by weight of the carrier of lower alcohols having up to 5 carbon atoms in their carbon chain skeleton.4. The composition of claim 1 , wherein the composition further comprises at least one liquefied or compressed gas propellant claim 1 , at a concentration of about 3% to about 25% by weight of the carrier.5. The composition of claim 1 , wherein the composition is contained within a pressurized container.6. The composition of claim 1 , wherein the co-solvent is selected from the group consisting of a polyol claim 1 , a sulfoxide claim 1 , and mixtures thereof.7. The composition of claim 1 , wherein the co-solvent is selected from the group consisting of glycerol claim 1 , propylene glycol claim 1 , hexylene glycol claim 1 , diethylene glycol claim 1 , propylene glycol n-alkanols claim 1 , terpenes claim 1 , di-terpenes claim 1 , tri-terpenes claim 1 , terpen-ols claim 1 , ...

TREATMENT OF GENOTYPED DIABETIC PATIENTS WITH DPP-IV INHIBITORS SUCH AS LINAGLIPTIN

The present invention relates to methods for preventing or treating of metabolic disorders and related conditions, such as in certain patient groups. 113-. (canceled)14. Method for preventing , slowing the progression of , delaying or treating a metabolic disorder selected from the group consisting of type 1 diabetes mellitus , type 2 diabetes mellitus , impaired glucose tolerance , impaired fasting blood glucose , hyperglycemia , postprandial hyperglycemia , overweight , obesity and metabolic syndrome , orfor improving glycemic control and/or for reducing of fasting plasma glucose, of postprandial plasma glucose and/or of glycosylated hemoglobin HbA1c in a patient in need thereof, or for preventing, slowing, delaying or reversing progression from impaired glucose tolerance, impaired fasting blood glucose, insulin resistance and/or from metabolic syndrome to type 2 diabetes mellitus, orfor preventing, slowing the progression of, delaying or treating of a condition or disorder selected from the group consisting of complications of diabetes mellitus such as cataracts and micro- and macrovascular diseases, such as nephropathy, retinopathy, neuropathy, tissue ischaemia, diabetic foot, arteriosclerosis, myocardial infarction, acute coronary syndrome, unstable angina pectoris, stable angina pectoris, stroke, peripheral arterial occlusive disease, cardiomyopathy, heart failure, heart rhythm disorders and vascular restenosis, or for reducing body weight or preventing an increase in body weight or facilitating a reduction in body weight, orfor preventing, slowing, delaying or treating the degeneration of pancreatic beta cells and/or the decline of the functionality of pancreatic beta cells and/or for improving and/or restoring the functionality of pancreatic beta cells and/or restoring the functionality of pancreatic insulin secretion, orfor preventing, slowing, delaying or treating diseases or conditions attributed to an abnormal accumulation of liver fat, orfor maintaining ...

NOVEL METHOD TO IMPROVE THE SAFETY AND EFFICACY OF CAFFEINE

The present invention relates to methods and compositions for reducing side effects associated with caffeine consumption. The methods comprise administering a Receptor Switcher, such as N-acetyl cysteine, in combination with caffeine. 1. A method of reducing , minimizing , or eliminating side effects associated with caffeine consumption comprising:(a) administering caffeine to a subject; and(b) administering at least one Receptor Switcher to the subject.2. The method of claim 1 , wherein the side effects associated with caffeine consumption are selected from the group consisting of increased stress and anxiety claim 1 , agitation claim 1 , restlessness claim 1 , insomnia claim 1 , irritability and anger claim 1 , cravings claim 1 , stomach pain (tenderness claim 1 , bloating) claim 1 , constipation claim 1 , unusual weakness claim 1 , seizure (convulsions) claim 1 , twitching or uncontrolled muscle movements claim 1 , fever claim 1 , fast or slow heart rate claim 1 , loss of appetite claim 1 , anxiety claim 1 , restlessness claim 1 , depression claim 1 , aggravation of premenstrual syndrome (PMS) claim 1 , fibrocystic breast disease claim 1 , psychiatric side effects (confusion and psychotic symptoms) claim 1 , increased blood pressure claim 1 , decrease in insulin sensitivity claim 1 , hypoglycemia claim 1 , and hyperglycemia.3. The method of claim 1 , wherein more than one receptor switcher is administered to the subject.4. The method of claim 1 , wherein the daily consumption of caffeine is selected from the group consisting of less than or equal to about 1500 mg claim 1 , less than or equal to about 1400 mg claim 1 , less than or equal to about 1300 mg claim 1 , less than or equal to about 1200 mg claim 1 , less than or equal to about 1100 mg claim 1 , less than or equal to about 1000 mg claim 1 , less than or equal to about 900 mg claim 1 , less than or equal to about 800 mg claim 1 , less than or equal to about 700 mg claim 1 , with 600 mg claim 1 , less than ...

Hypersulfated disaccharides to treat elastase related disorders

Hypersulfated disaccharides of formula I and other hypersulfated disaccharides disclosed herein are used to treat diseases or conditions associated with human neutrophil elastase imbalances. The disaccharides and/or intermediates useful to prepare such compounds are prepared from heparin. The diseases and conditions which are treated with a compound of formula I include chronic obstructive pulmonary disorder (COPD) and cystic fibrosis (CF). The formulations are delivered to the lungs in an aerosol formulation or dry powder means or via nebulization. Oral forms are also suitable.

Antiviral compound and cox-2 inhibitor combination therapy for functional somatic syndromes, including combination of famciclovir and celecoxib

The present invention relates to methods of treating fibromyalgia, by administering a therapeutically-effective combination of an antiviral component and a COX-2 inhibitor component. The invention is further related to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound famciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is also related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of famciclovir and celecoxib.

Inhaled Combination Therapy

There is provided the use of a methylxanthine derivative such as theophylline and a steroid in a synergistic combination for the treatment of chronic obstructive pulmonary disease, wherein the combination is administered by the inhaled route for pulmonary delivery. 1. A method for the treatment of chronic obstructive pulmonary disease (COPD) , comprising administering by the inhaled route for pulmonary delivery to a human subject in need thereof a composition comprising theophylline at a dose between 0.033 and 25 mg/day and a corticosteroid selected from the group consisting of mometasone furoate and beclomethasone dipropionate.2. The method of claim 1 , wherein the theophylline is administered in an amount of 0.05 to 12.5 mg two times per day.3. The method of claim 1 , wherein the theophylline is administered in an amount of 0.033 to 8 mg three times per day.4. The method of claim 1 , wherein the composition comprises one or more pharmaceutically acceptable additives claim 1 , diluents and/or carriers.5. The method of claim 1 , wherein the theophylline is administered at a dose that achieves plasma levels between 1 pg/L and 1 mg/L.6. The method of claim 1 , wherein the inhaled corticosteroid is mometasone furoate.7. The method of claim 6 , wherein the mometasone furoate is administered at doses between 50 μg and 1000 μg per day.8. The method of claim 7 , wherein the mometasone furoate is administerd at daily doses between 110 μg and 880 μg.9. The method of claim 1 , wherein the inhaled corticosteroid is beclomethasone dipropionate.10. The method of claim 9 , wherein the beclomethasone dipropionate is administered at daily doses between 20 μg and 2000 μg.11. The method of claim 10 , wherein the beclomethasone dipropionate is administered at daily doses between 40 μg and to 800 μg.12. The method of claim 1 , wherein the corticosteroid and theophylline are co-administered. The present invention provides the inhaled use of methylxanthine derivatives such as ...

VALACICLOVIR AND MELOXICAM COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound valaciclovir and a therapeutically-effective amount of the COX-2 inhibitor meloxicam. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of valaciclovir and meloxicam. 1. A combination comprising a therapeutically-effective amount of valaciclovir and a therapeutically-effective amount of meloxicam , wherein the amount of valaciclovir is present in a unit dosage form from about 750 mg to about 1500 mg , and wherein the amount of meloxicam is present in a unit dosage form from about 15 mg to about 30 mg.2. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form from about 750 mg to about 1050 mg.3. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form from about 1050 mg to about 1500 mg.4. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form selected from the group consisting of about 750 mg claim 1 , about 1050 mg claim 1 , about 1250 mg and about 1500 mg.5. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form of about 750 mg or about 1250 mg.6. The combination of claim 1 , wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.7. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form of about 750 mg or about 1250 mg claim 1 , and wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.8. A method to treat a subject susceptible to or afflicted with one or more functional somatic syndrome conditions comprising: fibromyalgia claim 1 , chronic fatigue syndrome claim 1 , irritable bowel syndrome claim 1 , chronic pain claim 1 , chronic headache ...

ACICLOVIR AND MELOXICAM COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound aciclovir and a therapeutically-effective amount of the COX-2 inhibitor meloxicam. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of aciclovir and meloxicam. 1. A combination comprising a therapeutically-effective amount of aciclovir and a therapeutically-effective amount of meloxicam , wherein the amount of aciclovir is present in a unit dosage form from about 400 mg to about 1600 mg , and wherein the amount of meloxicam is present in a unit dosage form from about 15 mg to about 30 mg.2. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form from about 400 mg to about 800 mg.3. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form from about 800 mg to about 1600 mg.4. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form selected from the group consisting of about 400 mg claim 1 , about 800 mg claim 1 , about 1200 mg and about 1600 mg.5. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form of about 400 mg or about 800 mg.6. The combination of claim 1 , wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.7. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form of about 400 mg or about 1200 mg claim 1 , and wherein the amount of meloxicam is present in a unit dosage form of about 15 mg or about 30 mg.8. A method to treat a subject susceptible to or afflicted with one or more functional somatic syndrome conditions comprising: fibromyalgia claim 1 , chronic fatigue syndrome claim 1 , irritable bowel syndrome claim 1 , chronic pain claim 1 , chronic headache claim 1 , chronic neck pain claim ...

ACICLOVIR AND CELECOXIB COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound aciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of aciclovir and celecoxib. 1. A combination comprising a therapeutically-effective amount of aciclovir and a therapeutically-effective amount of celecoxib , wherein the amount of aciclovir is present in a unit dosage form from about 400 mg to about 1600 mg , and wherein the amount of celecoxib is present in a unit dosage form from about 100 mg to about 800 mg.2. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form from about 400 mg to about 800 mg.3. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form from about 800 mg to about 1600 mg.4. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form selected from the group consisting of about 400 mg claim 1 , about 800 mg claim 1 , about 1200 mg and about 1600 mg.5. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form of about 400 mg or about 800 mg.6. The combination of claim 1 , wherein the amount of celecoxib is present in a unit dosage form from about 100 mg to about 400 mg.7. The combination of claim 1 , wherein the amount of celecoxib is present in a unit dosage form from about 400 mg to about 800 mg.8. The combination of claim 1 , wherein the amount of celecoxib is present in a unit dosage form selected from the group consisting of about 100 mg claim 1 , about 200 mg claim 1 , about 400 mg and about 800 mg.9. The combination of claim 1 , wherein the amount of celecoxib is present in a unit dosage form of about 200 mg or about 400 mg.10. The combination of claim 1 , wherein the amount of ...

ACICLOVIR AND DICLOFENAC COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound aciclovir and a therapeutically-effective amount of the COX-2 inhibitor diclofenac. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of aciclovir and diclofenac. 1. A combination comprising a therapeutically-effective amount of aciclovir and a therapeutically-effective amount of diclofenac , wherein the amount of aciclovir is present in a unit dosage form from about 400 mg to about 1600 mg , and wherein the amount of diclofenac is present in a unit dosage form from about 100 mg to about 150 mg.2. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form from about 400 mg to about 800 mg.3. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form from about 800 mg to about 1600 mg.4. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form selected from the group consisting of about 400 mg claim 1 , about 800 mg claim 1 , about 1200 mg and about 1600 mg.5. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form of about 400 mg or about 800 mg.6. The combination of claim 1 , wherein the amount of diclofenac is present in a unit dosage form of about 100 mg or about 150 mg.7. The combination of claim 1 , wherein the amount of aciclovir is present in a unit dosage form of about 400 mg or about 1200 mg claim 1 , and wherein the amount of diclofenac is present in a unit dosage form of about 100 mg or about 150 mg.8. A method to treat a subject susceptible to or afflicted with one or more functional somatic syndrome conditions comprising: fibromyalgia claim 1 , chronic fatigue syndrome claim 1 , irritable bowel syndrome claim 1 , chronic pain claim 1 , chronic headache claim 1 , chronic ...

VALACICLOVIR AND CELECOXIB COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound valaciclovir and a therapeutically-effective amount of the COX-2 inhibitor celecoxib. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of valaciclovir and celecoxib. 1. A combination comprising a therapeutically-effective amount of valaciclovir and a therapeutically-effective amount of celecoxib , wherein the amount of famciclovir is present in a unit dosage form from about 750 mg to about 1500 mg , and wherein the amount of celecoxib is present in a unit dosage form from about 100 mg to about 800 mg.2. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form from about 750 mg to about 1050 mg.3. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form from about 1050 mg to about 1500 mg.4. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form selected from the group consisting of about 750 mg claim 1 , about 1050 mg claim 1 , about 1250 mg and about 1500 mg.5. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form of about 750 mg or about 1250 mg.6. The combination of claim 1 , wherein the amount of celecoxib is present in a unit dosage form from about 100 mg to about 400 mg.7. The combination of claim 1 , wherein the amount of celecoxib is present in a unit dosage form from about 400 mg to about 800 mg.8. The combination of claim 1 , wherein the amount of celecoxib is present in a unit dosage form selected from the group consisting of about 100 mg claim 1 , about 200 mg claim 1 , about 400 mg and about 800 mg.9. The combination of claim 1 , wherein the amount of celecoxib is present in a unit dosage form of about 200 mg or about 400 mg.10. The combination of claim ...

VALACICLOVIR AND DICLOFENAC COMBINATION THERAPY FOR FUNCTIONAL SOMATIC SYNDROMES

The present invention relates to pharmaceutical compositions comprising a combination of a therapeutically-effective amount of the antiviral compound valaciclovir and a therapeutically-effective amount of the COX-2 inhibitor diclofenac. The invention is further related to methods of treating functional somatic syndromes by administering a therapeutically-effective combination of valaciclovir and diclofenac. 1. A combination comprising a therapeutically-effective amount of valaciclovir and a therapeutically-effective amount of diclofenac , wherein the amount of valaciclovir is present in a unit dosage form from about 750 mg to about 1500 mg , and wherein the amount of diclofenac is present in a unit dosage form from about 100 mg to about 150 mg.2. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form from about 750 mg to about 1050 mg.3. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form from about 1050 mg to about 1500 mg.4. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form selected from the group consisting of about 750 mg claim 1 , about 1050 mg claim 1 , about 1250 mg and about 1500 mg.5. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form of about 750 mg or about 1250 mg.6. The combination of claim 1 , wherein the amount of diclofenac is present in a unit dosage form of about 100 mg or about 150 mg.7. The combination of claim 1 , wherein the amount of valaciclovir is present in a unit dosage form of about 750 mg or about 1250 mg claim 1 , and wherein the amount of diclofenac is present in a unit dosage form of about 100 mg or about 150 mg.8. A method to treat a subject susceptible to or afflicted with one or more functional somatic syndrome conditions comprising: fibromyalgia claim 1 , chronic fatigue syndrome claim 1 , irritable bowel syndrome claim 1 , chronic pain claim 1 , chronic ...

LIP COSMETIC FORMULATIONS

Cosmetic formulations suitable for application to the lips are described herein. The lip cosmetic formulations can contain at least caffeine, extract of and extract of green tea. The lip cosmetic formulations can also contain a bioavailable chromium source and/or L-carnitine. Optionally, the lip cosmetic formulations can also contain a sunscreen. 1. A lip cosmetic formulation comprising:caffeine;{'i': 'Hoodia gordonii', 'extract of ; and'}extract of green tea.2Hoodia gordonii. The lip cosmetic formulation of claim 1 , wherein a concentration of the caffeine claim 1 , the extract of and the extract of green tea each range between about 0.5% and about 3.0% by weight of the lip cosmetic formulation.3. The lip cosmetic formulation of claim 2 , further comprising:a bioavailable chromium source.4. The lip cosmetic formulation of claim 3 , wherein the bioavailable chromium source comprises chromium picolinate.5. The lip cosmetic formulation of claim 4 , wherein a concentration of the chromium picolinate ranges between about 0.05% and about 3.0% by weight of the lip cosmetic formulation.6. The lip cosmetic formulation of claim 3 , further comprising:a sunscreen.7. The lip cosmetic formulation of claim 6 , wherein the sunscreen provides a sun protection factor of at least about 30.8. The lip cosmetic formulation of claim 3 , further comprising:L-carnitine.9. The lip cosmetic formulation of claim 8 , wherein a concentration of the L-carnitine ranges between about 0.5% and about 3.0% by weight of the lip cosmetic formulation.10. The lip cosmetic formulation of claim 8 , further comprising:a sunscreen.11. The lip cosmetic formulation of claim 10 , wherein the sunscreen provides a sun protection factor of at least about 30.12. The lip cosmetic formulation of claim 2 , further comprising:a sunscreen.13. The lip cosmetic formulation of claim 12 , wherein the sunscreen provides a sun protection factor of at least about 30.14. The lip cosmetic formulation of claim 1 , further ...

Anti-Cellulite Composition and Method of Treating Cellulite

A cellulite-reducing topical composition comprising a lecithin organogel, an ethylene oxide-propylene oxide-ethylene oxide triblock copolymer, caffeine, a retinoid, and optionally at least one vitamin, vitamin derivative or vitamin precursor. 1. A cellulite-reducing topical composition comprising:(a) about 5% to about 13% by weight of a lecithin organogel,(b) 1% to 3% by weight of a ethylene oxide-propylene oxide-ethylene oxide triblock copolymer,(c) 1% to 5% caffeine, and(d) a dermatologically acceptable carrier base.2. The cellulite reducing topical composition of further comprising about 0.1% to about 3.0% claim 1 , by weight claim 1 , of a retinoid.3. The cellulite reducing topical composition of wherein the retinoid is retinol.4. The cellulite reducing topical composition of further comprising about 0.1% to about 6.0% claim 1 , by weight claim 1 , of at least one vitamin claim 1 , vitamin derivative or vitamin precursor.5. The cellulite reducing topical composition of wherein the at least one vitamin derivative is tocopherol acetate claim 4 , ascorbyl palmitate claim 4 , or a mixture thereof.6. The cellulite reducing topical composition of wherein the organogel is comprised of soy lecithin and isopropyl palmitate.7Centella asiatica, Coleus forskolii, Ginkgo biloba. The cellulite reducing topical composition of wherein the organogel further comprises at least one anti-cellulite active ingredient selected from the group of: anti-inflammatory agents; extracts of ; ursolic acid; short-chain peptides having from 2 to 12 amino acids; MMP-inhibitors; theophylline and derivatives thereof; carnitine and derivatives thereof.8. The cellulite reducing topical composition of wherein the ethylene oxide-propylene oxide-ethylene oxide triblock copolymer comprises about 70% claim 1 , by weight claim 1 , ethylene oxide.9. A method of reducing cellulite in human skin claim 1 , and the visual manifestations thereof claim 1 , comprising the step of applying to the skin an amount of ...

MUCOADHESIVE BUCCAL TABLETS FOR THE TREATMENT OF OROFACIAL HERPES

The present invention relates to the treatment and/or prevention of muco-cutaneous herpes simplex virus diseases using prolonged release mucoadhesive buccal tablets comprising an acyclic guanosine antiviral agent. These tablets are particularly-suitable for the treatment and/or prevention of orofacial herpes. 116-. (canceled)18. The method of claim 17 , wherein a single dose of said acyclic guanosine antiviral agent is administered.19. The method of claim 17 , wherein the patient is suffering from (a) prodromal symptoms or (b) erythemal or papular symptoms.20. The method of claim 19 , wherein the patient is suffering from prodromal symptoms and the mucoadhesive buccal tablet is administered within two hours claim 19 , within 90 minutes claim 19 , or within one hour of appearance of prodromal symptoms.21. The method of claim 17 , wherein the patient is suffering from pre-vesicular symptoms of orofacial herpes claim 17 , and wherein mucoadhesive buccal tablet is administered to the site of said non-pre-vesicular symptoms.22. The method of claim 17 , wherein the acyclic guanosine antiviral agent is acyclovir.23. The method of claim 22 , wherein said mucoadhesive buccal tablet comprises acyclovir in an amount of 50 mg.24. The method of claim 22 , wherein the mucoadhesive buccal tablet comprises acyclovir in an amount of 100 mg.25. The method of claim 22 , wherein the mucoadhesive buccal tablet provides sustained release of acyclovir for a period of at least 24 hours in at least 70% of patients following administration.26. The method of claim 17 , wherein the mucoadhesive buccal tablet adheres to said oral mucosa for a period of at least 6 hours claim 17 , at least 8 hours claim 17 , at least 10 hours or at least 12 hours following administration.27. The method of claim 17 , wherein the mucoadhesive buccal tablet provides a Cof at least 300 claim 17 ,000 ng/ml or at least 350 claim 17 ,000 ng/ml.28. The method of claim 17 , wherein the mucoadhesive buccal tablet provides ...

Herbal Supplement Prepared From Pelargonium Citronellum

An extraction method for extracts of with improved methylhexaneamine content is provided. The method involves separating the oil phase from the aqueous phase; concentrating the aqueous phase; purifying the oil phase; and recombining the resulting material. Additionally, extracts of prepared by the extraction method are provided. The extracts are useful in compositions, for example as dietary supplements, and for appetite suppression. 1Pelargonium. An extract of isolated from natural sources , said extract comprising at least 1% methylhexaneamine.2. The extract of wherein the extract is produced by:{'i': 'geranium', 'a. providing one or more whole crushed plants;'}b. adding water and alcohol to the crushed plant to obtain a mixture;c. reflowing the mixture;d. extracting the mixture to separate an essential oil phase from an aqueous phase;e. stewing and separating the essential oil phase to obtain a purified essential oil;f. concentrating the aqueous phase;g. drying the concentrated aqueous phase to obtain a powder; andh. combining the purified essential oil with the powder to obtain the extract.3Pelargonium. A method of processing to provide an extract containing at least 1% methylhexaneamine comprising:{'i': 'geranium', 'a. providing one or more whole crushed plants;'}b. adding water and alcohol to the crushed plant to obtain a mixture;c. reflowing the mixture;d. extracting the mixture to separate an essential oil phase from an aqueous phase;e. stewing and separating the essential oil phase to obtain a purified essential oil;f. concentrating the aqueous phase;g. drying the concentrated aqueous phase to obtain a powder; andh. combining the purified essential oil with the powder to obtain the extract.4. The method of wherein drying the concentrated aqueous phase to obtain a powder is accomplished by spray drying.5. The method of wherein concentrating the aqueous phase is preformed at low temperature.6. The method of wherein extracting the mixture to separate an ...

Papillomavirus pseudoviruses for detection and therapy of tumors

Disclosed herein are methods of detecting tumors, monitoring cancer therapy, and selectively inhibiting the proliferation and/or killing of cancer cells utilizing a papilloma pseudovirus or a papilloma virus-like particle (VLP)

PHARMACEUTICAL COMPOSITION AND USES THEREOF

The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and/or a SGLT-2 inhibitor drug, and metformin XR, processes for the preparation thereof, and their use to treat certain diseases. 1. A pharmaceutical composition comprising:a) an extended release core comprising metformin (particularly metformin hydrochloride) and one or more excipients;b) an optional seal and/or barrier coating; and a DPP-4 inhibitor, preferably linagliptin, and', 'a SGLT-2 inhibitor, preferably 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene,', 'and one or more excipients., 'c) an immediate release coating comprising at least one active pharmaceutical ingredient selected from'}2. The pharmaceutical composition according to claim 1 , wherein the inner extended release core a) is a formulation comprising metformin hydrochloride claim 1 , a swellable and/or extended release polymer claim 1 , and one or more further excipients.3. The pharmaceutical composition according to claim 1 , wherein the immediate release coating c) is a film coat formulation comprising:the at least one active pharmaceutical ingredient, preferably a stabilizer for stabilizing linagliptin (preferably L-arginine), andone or more film-coating agents selected from hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol (PVA), ethyl cellulose, hydroxypropyl cellulose, polydextrose, methacrylic and/or acrylic polymer, or a mixture thereof,optionally one or more plasticizers selected from polyethylene glycol, propylene glycol, diethyl phthalate, tributyl sebacate and/or triacetin, or a mixture thereof,optionally a glidant selected from talc, magnesium stearate and fumed silica, andoptionally one or more pigments and/or colorants.4. The pharmaceutical composition according to claim 1 , wherein the immediate release coating c) is a film coat formulation comprising linagliptin claim 1 , L-arginine as stabilizer claim 1 , a film- ...

PHARMACEUTICAL COMPOSITION

The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine Areceptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HTantagonist or the like), and the like. 150-. (canceled)52. The method according to claim 51 , wherein the antidepressant drug is a tricyclic antidepressant claim 51 , a tetracyclic antidepressant claim 51 , a selective serotonin reuptake inhibitor claim 51 , a selective noradrenalin reuptake inhibitor claim 51 , a dopamine reuptake inhibitor claim 51 , a serotonin-noradrenalin reuptake inhibitor claim 51 , a monoamine oxidase inhibitor or a serotonin 2 (5-HT) antagonist.53. The method according to claim 51 , wherein the antidepressant drug is a tricyclic antidepressant.54. The method according to claim 53 , wherein the tricyclic antidepressant is imipramine hydrochloride claim 53 , clomipramine hydrochloride claim 53 , amitriptyline hydrochloride claim 53 , nortriptyline hydrochloride claim 53 , amoxapine claim 53 , trimipramine maleate claim 53 , lofepramine claim 53 , lofepramine hydrochloride claim 53 , dosulepin hydrochloride claim 53 , protriptyline claim 53 , doxepin or desipramine hydrochloride.55. The method according to claim 51 , wherein the antidepressant drug is a tetracyclic antidepressant.56. The method according to claim 55 , wherein the tetracyclic antidepressant is maprotiline hydrochloride claim 55 , mianserin hydrochloride or setiptiline maleate.57. The method according to claim 51 , wherein the antidepressant drug is a ...

Methods for Treating Diseases and HSV Using Antibodies to Aminophospholipids

Disclosed are surprising discoveries concerning the role of anionic phospholipids and aminophospholipids in tumor vasculature and in viral entry and spread, and compositions and methods for utilizing these findings in the treatment of cancer and viral infections. Also disclosed are advantageous antibody, immunoconjugate and duramycin-based compositions and combinations that bind and inhibit anionic phospholipids and aminophospholipids, for use in the safe and effective treatment of cancer, viral infections and related diseases. 1. A method of quantifying viral load in a biological sample , comprising contacting said biological sample with a first antibody , or an antigen-binding fragment thereof , in an amount effective to bind viruses in said biological sample and quantifying the bound viruses; wherein said first antibody binds to phosphatidylserine on the luminal surface of tumor vascular endothelial cells when administered to an animal with a solid tumor and wherein said first antibody exhibits significant binding to an ELISA plate coated with phosphatidylserine in an ELISA conducted in the presence of serum , but no detectable binding to an ELISA plate coated with phosphatidylcholine in an ELISA conducted in the presence of serum , wherein said ELISA conducted in the presence of serum comprises the steps of:(a) coating a first ELISA plate with phosphatidylserine to prepare a PS-coated ELISA plate and coating a second ELISA plate with phosphatidylcholine to prepare a PC-coated ELISA plate;(b) blocking said PS-coated ELISA plate and said PC-coated ELISA plate with a blocking buffer comprising 10% serum;(c) adding said first antibody diluted in said blocking buffer to said PS-coated ELISA plate and said PC-coated ELISA plate under conditions effective to allow binding of said first antibody to said PS-coated ELISA plate and said PC-coated ELISA plate in the presence of serum; and(d) detecting the binding of said first antibody to said PS-coated ELISA plate and said ...

COMPOSITIONS FOR TREATING CANCER-RELATED FATIGUE AND METHODS OF SCREENING THEREOF

An animal model has been developed based the understanding that a central mechanism in patients with CTRF is that chemotherapy and/or radiation initiates canonical pathways leading to the development of disrupted sleep architecture, resulting in disruption of REM sleep and fatigue and cognitive dysfunction. Drugs that restore the activity patterns and levels towards normal and/or decrease the pro-inflammatory cytokines associated with the disrupted sleep, should be effective in alleviating one or more symptoms of CTRF. Pentoxifylline was demonstrated to improve activity levels in animals treated with etoposide. 1. A method of alleviating cancer treatment-related fatigue comprising administering an effective amount of a drug which restores the activity/sleep patterns and levels towards normal and/or decreases the pro-inflammatory cytokines associated with disrupted sleep.2. The method of wherein the drug increases IL-6 levels.3. The method of wherein the pro-inflammatory cytokines are TNF-alpha claim 1 , IL-1 claim 1 , or an activator of IL-1ra and IL-10.4. The method of wherein the cancer treatment is chemotherapy claim 1 , radiation or a combination thereof.5. The method of claim 1 , wherein the drug is selected from the group consisting of Aminophylline claim 1 , Paraxanthine claim 1 , Pentoxifylline claim 1 , Rolipram claim 1 , Ibuditant claim 1 , Piclamilast claim 1 , Luteolin claim 1 , Drotaverine claim 1 , Sildenafil claim 1 , Tadalafil claim 1 , Vardenafil claim 1 , Dipyridamole claim 1 , Cilomilast claim 1 , Roflumilast claim 1 , Allopurinol claim 1 , Oxypurinol claim 1 , Tisopurine claim 1 , Febuxostat claim 1 , Inositol claim 1 , Deslanoside claim 1 , Digitoxin claim 1 , Digoxin claim 1 , Clomipramine claim 1 , Imipramine claim 1 , Valproate claim 1 , Verapamil claim 1 , Desipramine claim 1 , Fluvastin claim 1 , Lovostatin claim 1 , pravastatin claim 1 , Azalide claim 1 ,Azithromycin, Boromycin, brefeldin A, clarithromycin, dirithromycin, erythromycin, ...

Control of Blood Vessel Physiology To Treat Skin Disorders

In a method for treating an affected skin region of a patient having a skin disorder, a vasodilation composition is applied to an affected skin region of a patient, the affected skin region exhibiting a skin disorder characterized by at least one abnormal blood vessel, and the affected skin region is then treated so as to non-invasively disrupt tissue architecture, e.g., by inducing ischemia, of the at least one abnormal blood vessel. A vasoconstriction composition can then be applied to the skin region to cause vasoconstriction of the at least one blood vessel in order to promote healing. 1. A method for treating an affected skin region of a patient having a skin disorder , the method comprising:a) applying a vasodilation composition to an affected skin region of a patient, said affected skin region exhibiting a skin disorder characterized by at least one abnormal blood vessel, wherein said blood vessel comprises a tissue architecture, and where said application is for a time sufficient to induce vasodilation of said at least one abnormal blood vessel in said affected skin region; andb) non-invasively disrupting the tissue architecture of said at least one abnormal blood vessel.2. The method of claim 1 , wherein said skin disorder is rosacea.3. The method of claim 1 , wherein said skin disorder is telangiectasia.4. The method of claim 1 , wherein said skin disorder comprises at least one vascular lesion.5. The method of claim 1 , wherein said skin disorder is selected from the group consisting of spider veins claim 1 , varicose veins claim 1 , actinically damaged skin claim 1 , venous hypertension claim 1 , Poikiloderma vasculare atrophicans claim 1 , vascular malformations claim 1 , and hemangioma.6. The method of claim 1 , wherein said vasodilation composition comprises arginine.7. The method of claim 6 , wherein said vasodilation composition further comprises tolazoline.8. The method of claim 1 , wherein said vasodilation composition comprises methyl nicotinate. ...

COFFEE EXTRACTS AS INGREDIENTS OF FOODS, DRUGS, COSMETICS, DIETARY SUPPLEMENTS, AND BIOLOGICS

Embodiments are related to compositions of matter comprising a food, drug, cosmetic, dietary supplement, or biologic product, said product comprised of a phytochemical fraction recovered from a crude caffeine, said phytochemical fraction having a ratio of polyphenols to caffeine of about 20, 10-30 or 40, or greater than 10. In related embodiments, said phytochemical fraction is a retentate of a filtration process of a water suspension of crude caffeine, and wherein said crude caffeine is a product of a green coffee bean decaffeination process. In other related embodiments, said compositions of matter are useful for facilitating neuroprotection, inhibiting COX-2 or stimulating glucose uptake. 1. A composition of matter comprising a food product , said food product comprised of a phytochemical fraction recovered from a crude caffeine , said phytochemical fraction having a ratio of polyphenols to caffeine of about 20 , 10-30 or 40 , or greater than 10.2. The composition of matter of claim 1 , wherein said phytochemical fraction is a retentate of a filtration process of a water suspension of crude caffeine claim 1 , and wherein said crude caffeine is a product of a green coffee bean decaffeination process.3. A process for producing a food product comprising either supplementing a food with claim 1 , or supplementing a component of a food with claim 1 , a phytochemical fraction recovered from a crude caffeine claim 1 , said phytochemical fraction being that as described in claim 1 , whereby said food product is produced.4. A composition of matter comprising a drug product claim 1 , said drug product comprised of a phytochemical fraction recovered from a crude caffeine claim 1 , said phytochemical fraction having a ratio of polyphenols to caffeine of about 20 claim 1 , 10-30 or 40 claim 1 , or greater than 10.5. The composition of matter of claim 4 , wherein said phytochemical fraction is a retentate of a filtration process of a water suspension of crude caffeine claim 4 ...

Methods, Compounds and Compositions Relating to Activating a Latent Virus

The present invention relates to, inter alia, an anti-microtubule agent for use in a method of treating a subject having a latent virus, the method comprising: administering the anti-microtubule agent and an anti-viral agent to the subject. 134-. (canceled)35. A method of treating a subject having a latent virus comprising administering an anti-microtubule agent and an anti-viral agent to the subject.37. The method of treating a subject having a latent virus according to claim 36 , wherein X is S claim 36 , —Y is ═O claim 36 , and R claim 36 , R claim 36 , Rand Rare all H.39. The method of treating a subject having a latent virus according to claim 38 , wherein R claim 38 , R claim 38 , Rare each H and Rand Rare each independently selected from hydrogen claim 38 , hydroxy and optionally substituted alkoxy claim 38 , with at least one of Rand Rbeing hydroxy or optionally substituted alkoxy.40. The method of treating a subject having a latent virus according to claim 38 , wherein X is S claim 38 , —Y is ═O claim 38 , R claim 38 , R claim 38 , Rand Rare all H claim 38 , R claim 38 , R claim 38 , R claim 38 , Rare each H and Ris methoxy.41. The method of treating a subject having a latent virus according to claim 35 , wherein the anti-microtubule agent is selected from genistein claim 35 , vincristine claim 35 , vinblastine claim 35 , vindesine claim 35 , vinorelbin claim 35 , taxotere claim 35 , maytansin claim 35 , rhizoxin claim 35 , taxane compounds claim 35 , and combinations thereof.42. The method of treating a subject having a latent virus according to claim 35 , wherein the anti-viral agent is an agent for treating a herpes virus.43. The method of treating a subject having a latent virus according to claim 35 , wherein the anti-viral agent is selected from cidofovir claim 35 , acyclovir claim 35 , valaciclovir claim 35 , ganciclovir claim 35 , valganciclovir claim 35 , penciclovir claim 35 , famciclovir claim 35 , vidarabine claim 35 , cytarabine claim 35 , ...

Phospholipid drug analogs

Provided in some embodiments are compositions comprising a compound having a structure according to Formula A or Formula B: or a pharmaceutically acceptable salt, tautomer or hydrate thereof, where X 2 is a bond or linker, X 3 is bond or —PO 4 —, and X 1 , R 1 , R 2 , R 3 , and n are described herein. Also provided in some embodiments are methods for making and using such compounds and compositions.

COMBINATION COMPRISING AN ATP ANALOG AND AN ADENOSINE RECEPTOR ANTAGONIST OR A NUCLEOBASE/NUCLEOSIDE ANALOG FOR THE TREATMENT OF CANCER

A method for treating an ATP analog-induced side effect in a subject comprises administering an effective amount of an adenosine receptor antagonist to the subject. A method for treating cancer in a subject comprises administering a nucleobase and/or nucleoside prior to administering an ATP analog. 1233-. (canceled)234. A method for treating and/or preventing an ATP analog-induced side effect in a subject , the method comprising administering an effective amount of an adenosine receptor antagonist to the subject.235. The method of claim 234 , wherein the ATP analog is selected from a tyrosine kinase inhibitor claim 234 , an mTOR inhibitor claim 234 , a Bcl-2 inhibitor claim 234 , and a PARP inhibitor.236. The method of claim 235 , wherein the PARP inhibitor comprises at least one of olaparib claim 235 , ABT 888 claim 235 , and BSI-221.237. The method of claim 235 , wherein the tyrosine kinase inhibitor comprises at least one of axtinib claim 235 , bosutinib claim 235 , brivanib claim 235 , cediranib claim 235 , dasatinib claim 235 , erlotinib claim 235 , gefitinib claim 235 , imatinib claim 235 , lapatinib claim 235 , lestaurtinib claim 235 , nilotinib claim 235 , pazopanib claim 235 , semaxanib claim 235 , sorafenib claim 235 , sunitinib claim 235 , vandetanib claim 235 , and vatalanib.238. The method of claim 235 , wherein the Bcl-2 inhibitor comprises ABT 263.239. The method of claim 238 , wherein the adenosine receptor antagonist is specific for the adenosine Areceptor.240. The method of claim 234 , wherein the adenosine receptor antagonist comprises at least one methylxanthine.241. The method of claim 240 , wherein the at least one methylxanthine comprises at least one of caffeine claim 240 , theophylline claim 240 , and aminophylline.242. The method of claim 234 , wherein the ATP analog and the adenosine receptor antagonist are administered simultaneously.243. The method of claim 234 , wherein the ATP analog is administered before the adenosine receptor ...

TREATMENT OF MOTOR NEURON DISEASE

Provided herein are methods and compositions for the treatment of motor neuron diseases including, for example, amyotrophic lateral sclerosis. Suitable therapeutic agents include, for example, agents that up-regulate the expression IGF-II or guanine deaminase in a cell. 1. A method for treating a motor neuron disease in a human patient comprising administering to said patient a therapeutically effective amount of an agent that up-regulates IGF-II gene expression.2. The method of claim 1 , wherein the therapeutic agent up-regulates IGF-II by at least 2-fold in said patient.3. The method of or claim 1 , wherein the agent is selected from the group consisting of eletriptan hydrobromide claim 1 , modafinil claim 1 , dicloxacillin sodium claim 1 , thiamphenicol claim 1 , ceftibuten claim 1 , tacrine HCl claim 1 , fluoxetine claim 1 , citalopram claim 1 , fluvoxamine maleate claim 1 , amoxapine claim 1 , atomoxetine HCl claim 1 , olmesartan medoxomil claim 1 , guanabenz acetate claim 1 , hydralazine HCl claim 1 , methyldopate HCl claim 1 , diltiazem HCl claim 1 , glyburide claim 1 , flurbiprofen claim 1 , carprofen claim 1 , meloxicam sodium claim 1 , diclofenac sodium claim 1 , levodopa claim 1 , olanzapine claim 1 , chlorpromazine claim 1 , valacyclovir HCl claim 1 , levocarnitine claim 1 , ropinirole claim 1 , vardenafil HCl claim 1 , guaifenesin claim 1 , omeprazole claim 1 , cetirizine HCl claim 1 , azelastine hydrochloride claim 1 , ramelteon claim 1 , nicotine ditartrate claim 1 , zolpidem claim 1 , aspartame claim 1 , thiamine claim 1 , riboflavin claim 1 , niacinamide claim 1 , sildenafil HCl claim 1 , tadalafil HCl and dexamethasone acetate.4. The method of claim 3 , wherein the agent is vardenafil HCl.5. The method of claim 4 , wherein the therapeutically effective amount is from 1 mg to 50 mg per day.6. The method of claim 3 , wherein the agent is guanabenz acetate.7. The method of claim 6 , wherein the therapeutically effective amount is from 1 mg to 10 mg ...

COMBINATION THERAPY

The present invention relates to methods for treating and/or preventing metabolic diseases comprising the combined administration of a GLP-1 receptor agonist and a DPP-4 inhibitor. 1) A combination comprisinga GLP-1 receptor agonist and linagliptin,for separate, sequential or simultaneous therapeutic use of the active components.2) The combination according to claim 1 , wherein the GLP-1 receptor agonist is selected from exenatide claim 1 , exenatide LAR claim 1 , liraglutide claim 1 , taspoglutide claim 1 , semaglutide claim 1 , albiglutide claim 1 , lixisenatide and dulaglutide.3) The combination according to claim 1 , wherein the GLP-1 receptor agonist and linagliptin are present each in separate dosage forms.4) The combination according to for sequential use of the active components.5) The combination according to for sequential use of the GLP-1 receptor agonist followed by linagliptin.6) A method of using the combination according to for reducing and maintaining body weight and/or body fat in an overweight or obesity patient with or without diabetes.7) A method of using the combination according to for treatment of type 2 diabetes claim 1 , obesity or both claim 1 , said treatment comprisingadministering an effective amount of the GLP-1 receptor agonist to the patient for inducing body weight loss and/or body fat loss, andadministering an effective amount of linagliptin to the patient for maintaining the reduced body weight and/or body fat.8) A method of using the combination according to for treatment of type 2 diabetes claim 1 , obesity or both claim 1 , said treatment comprising the stepsi) administering an effective amount of the GLP-1 receptor agonist to the patient for inducing body weight loss and/or body fat loss, andii) administering an effective amount of linagliptin to the patient for maintaining the reduced body weight and/or body fat,wherein linagliptin treatment ii) is subsequent to the GLP-1 receptor agonist treatment i).9) A method of using the ...

Indolin-2-one derivatives as protein kinase inhibitors

A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.

Use of (R)-Penciclovir Triphosphate for the Manufacture of a Medicament for the Treatment of Viral Diseases

A method of treatment of: i) HIV-1 infections in mammals, including humans; or ii) HBV infections in mammals, including humans; which method comprises the administration to the human in need of such treatment, an effective amount of the (R)-enantiomer of the triphosphate of a compound of formula (A) or a pharmaceutically acceptable salt thereof; and compounds for use in the method. 2. A method claim 1 , composition or use according to wherein the (R)-PCV-TP is in the form of a bioprecursor which is a derivative of (R)-PCV-MP which liberates intracellularly (R)-PCV-MP which is in turn converted to (R)-PCV-TP. This invention relates to treatment of human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infection.When used herein, ‘treatment’ includes prophylaxis as appropriate.EP-A-141927 (Beecham Group p.l.c.) discloses penciclovir (PCV), the compound of formula (A):and salts, phosphate esters and acyl derivatives thereof, as antiviral agents. The sodium salt hydrate of penciclovir is disclosed in EP-A-216459 (Beecham Group p.l.c.). Penciclovir and its antiviral activity is also disclosed in Abstract P.VII-5 p. 193 of ‘Abstracts of 14th Int. Congress of Microbiology’, Manchester, England 7-13 September 1986 (Boyd et. al.).Orally active bioprecursors of the compound of formula (A) are of formulaand salts and derivatives thereof as defined under formula (A); wherein X is Calkoxy, NHor hydrogen. The compounds of formula (B) wherein X is Calkoxy or NHare disclosed in EP-A-141927 and the compounds of formula (B) wherein X is hydrogen, disclosed in EP-A-182024 (Beecham Group p.l.c.) are preferred prodrugs. A particularly preferred example of a compound of formula (B) is that wherein X is hydrogen and wherein the two OH groups are both in the form of the acetyl derivative, described in Example 2 of EP-A-182024, hereinafter referred to as famciclovir.EP-A-388049 (Beecham Group p.l.c.), discloses the use of penciclovir/famciclovir in the treatment of hepatitis B virus ...

Acyclovir Formulations

The present invention relates to an acyclovir formulation having improved bioavailability resulting in better efficacy and/or requiring less frequent administration. 4. A pharmaceutical composition of claim 1 , wherein the delivery agent is selected from the group consisting of Delivery agents is SNAC or SNAD or a pharmaceutically acceptable salt thereof.5. The pharmaceutical composition of wherein the delivery agent is N-(8-[2-hydroxybenzoyl]-amino)caprylic acid or a pharmaceutically acceptable salt thereof.6. The pharmaceutical composition of wherein the delivery agent is wherein the delivery agent is N-(10-[2-hydroxybenzoyl]-amino)decanoic acid or a pharmaceutically acceptable salt thereof.7. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition provides bioavailability (i.e. claim 1 , AUC) substantially equivalent to the acyclovir formulation marketed as Zovirax® under U.S. FDA NDA No. 18828 claim 1 , 19909 claim 1 , or 20089 when:(1) 200, 400, or 800 mg of the acyclovir formulation is administered every 4 hours 5 times daily,(2) 400 mg of the acyclovir formulation is administered 2 times daily,(3) 200 mg of the acyclovir formulation is administered 3 times daily,(4) 200 mg of the acyclovir formulation is administered 4 times daily, or(5) 200 mg of the acyclovir formulation is administered 5 times daily.8. A dosage unit form comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(A) the pharmaceutical compositions of ; and'} (b) a diluent,', '(c) a disintegrant,', '(d) a lubricant,', '(e) a plasticizer,', '(f) a colorant,', '(g) a dosing vehicle, or', '(h) any combination thereof., '(B) (a) an excipient,'}9. The dosage unit form of claim 8 , wherein the dosage unit form is in the form of a tablet claim 8 , a capsule claim 8 , a particle claim 8 , a powder claim 8 , a sachet claim 8 , or a liquid.10. The dosage unit form of claim 8 , wherein the dosing vehicle is a liquid selected from the group consisting of water claim 8 , ...

CYCLOPROPANECARBOXYLATE ESTERS OF PURINE ANALOGUES

Cyclopropanecarboxylate esters of purine analogues, method of making and using the same for treating herpes virus infections and tumors are disclosed. 2. The compound of claim 1 , wherein{'sub': x', 'y, 'Rand Rare each independently hydrogen or methyl; and'}{'sub': 'y', 'Ris hydrogen, methyl, trifluoromethyl, phenyl, 4-bromophenyl, 2-furyl, or 2-pyridyl.'}3. The compound of claim 2 , wherein{'sub': x', 'z, 'Rand Rare each independently hydrogen; and'}{'sub': 'y', 'Ris hydrogen, methyl, trifluoromethyl, phenyl, 4-bromophenyl, 2-furyl, or 2-pyridyl.'}4. The compound of claim 2 , wherein{'sub': 'x', 'Ris methyl; and'}{'sub': y', 'z, 'Rand Rare each independently hydrogen.'}5. The compound of claim 2 , wherein{'sub': 'x', 'Ris hydrogen; and'}{'sub': y', 'z, 'Rand Rare each independently methyl.'}6. The compound of claim 2 , wherein the compound is selected from the group consisting of1-amino-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-yl methoxy)-3-hydroxypropyl ester,1-amino-2-(4-bromo-phenyl)-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-3-hydroxypropyl ester,1-amino-2-phenyl-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-3-hydro propyl ester,1-amino-2-methyl-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-3-hydroxypropyl ester,1-amino-2-trifluoromethyl-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-3-hydroxypropyl ester,1-amino-2-furan-2-yl-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-ylmethoxy)-3-hydroxypropyl ester, and1-amino-2-pyridin-2-yl-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1,6-dihydro-purin-9-yl-methoxy)-3-hydroxypropyl ester.7. The compound of claim 2 , wherein the compound is 1-methylamino-cyclopropanecarboxylic acid 2-(2-amino-6-oxo-1 claim 2 ,6-dihydro-purin-9-ylmethoxy)-3-hydroxypropyl ester.8. The compound of claim 2 , wherein the compound is 1-amino-2 claim 2 ,2-dimethyl- ...

Synthetic lethality in cancer

There is described herein compounds, compositions and methods for inducing synthetic lethality in a cancer cell(s).

Combination Therapy for Cancer

An agent comprises a vector having a functional gene, a prodrug which can be converted into a cytotoxic agent by an expression product of the gene, and another cytotoxic agent, as a combined preparation for simultaneous, sequential or separate use in the therapy of cancer or of a disease characterised by an impaired mismatch repair (MMR) pathway, wherein the dosage regimen comprises beginning another cytotoxic agent therapy no later than 7 days after the prodrug therapy has finished. 1. A method of treating glioblastoma multiforme , said method comprising the steps of:a. Diagnosing in a human patient glioblastoma multiforme;b. Identifying in said patient at least one glioblastoma multiforme tumor;c. Resectioning said glioblastoma multiforme tumor to remove at least part of said glioblastoma multiforme tumor and expose tumor bed tissue;d. Administering to said tumor bed tissue an AdHSV-tk adenoviral vector having a gene coding for thymidine kinase, whereby said AdHSV-tk adenoviral vector transfects said tumor bed tissue and said tumor bed tissue expresses said gene coding for thymidine kinase;e. Within about 5 to about 19 days after administering said adenoviral vector to said human patient, further administering to said human patient ganciclovir;f. Administering to said human patient temozolomide per os or by intravenous infusion.2. The method of claim 1 , wherein said glioblastoma multiforme is recurrent glioblastoma multiforme.3. The method of claim 1 , wherein said temozolamide is administered in a plurality of 28-day cycles claim 1 , each cycle comprising administration of a dose of about 150 mg/mper day each day for days 1-5 of said 28-day cycle claim 1 , followed by a dose of about 0 mg/mper day for days 6-28 of said 28-day cycle.4. The method of claim 3 , wherein said plurality of 28-day cycles is preceded by period of about 42 days wherein temozolamide is administered at a dosage of about 75 mg/mper day.5. The method of claim 1 , wherein said AdHSV-tk ...

USE OF A DPP-4 INHIBITOR IN PODOCYTES RELATED DISORDERS AND/OR NEPHROTIC SYNDROME

The present invention relates to methods for treating and/or preventing podocytes related disorders and/or nephrotic syndrome comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for treating and/or preventing a metabolic disease in a patient with or at risk of podocytes related disorders and/or nephrotic syndrome. 2. The method according to claim 1 , wherein the DPP-4 inhibitor is linagliptin claim 1 , optionally in combination with one or more other active agents claim 1 , and the method is for treating claim 1 , preventing and/or reducing the risk of podocyte related disorders claim 1 , disturbance of podocyte function claim 1 , podocyte loss or injury claim 1 , and/or podocytopathy.3. The method according to claim 1 , wherein the DPP-4 inhibitor is linagliptin claim 1 , optionally in combination with one or more other active agents claim 1 , and the method is for treating claim 1 , preventing or reducing the risk of nephrotic syndrome.4. The method according to claim 3 , wherein the nephrotic syndrome includes claim 3 , is caused by or is associated with minimal change disease (MCD) claim 3 , membranous nephropathy (MN) and/or focal segmental glomerulosclerosis (FSGS).5. The method according to claim 4 , wherein the nephrotic syndrome is primary or secondary.6. The method according to claim 4 , wherein the nephrotic syndrome is resistant or refractory to conventional therapy.7. The method according to claim 1 , wherein the DPP-4 inhibitor is linagliptin claim 1 , optionally in combination with one or more other active agents claim 1 , and the method is for treating claim 1 , preventing and/or reducing the risk of minimal change disease (MCD) claim 1 , membranous nephropathy (MN) and/or focal segmental glomerulosclerosis (FSGS).8. The method according to claim 1 , wherein the DPP-4 inhibitor is linagliptin claim 1 , optionally in combination with one or more other active agents claim ...

Fused heterocyclic compounds

The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.

USE OF A DPP-4 INHIBITOR IN SIRS AND/OR SEPSIS

The present invention relates to methods for treating and/or preventing SIRS and/or sepsis comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for treating and/or preventing a metabolic disease in a patient with or at risk of SIRS and/or sepsis. 2. The method according to claim 1 , wherein the DPP-4 inhibitor is linagliptin claim 1 , optionally in combination with one or more other active agents claim 1 , and the method is for increasing survival rate and/or reducing mortality claim 1 , morbidity or hospitalisation of a patient with or at risk of SIRS and/or sepsis (SIRS/sepsis).3. The method according to wherein the DPP-4 inhibitor is claim 1 , optionally in combination with one or more other active agents claim 1 , and the method is for treating claim 1 , preventing or reducing the likelihood or risk of complications associated with SIRS and/or sepsis claim 1 , such as e.g. severe SIRS/sepsis claim 1 , SIRS/septic shock and/or multi-organ failure.4. The method according to claim 1 , wherein the DPP-4 inhibitor is linagliptin claim 1 , optionally in combination with one or more other active agents claim 1 , and the method is for reducing the risk or likelihood of multi-organ failure in a patient with or at risk of SIRS and/or sepsis (SIRS/sepsis).5. The method according to claim 1 , wherein the DPP-4 inhibitor is linagliptin claim 1 , optionally in combination with one or more other active agents claim 1 , and the method is for reducing the risk or likelihood of septic shock in a patient with or at risk of SIRS and/or sepsis (SIRS/sepsis).6. The method according to claim 1 , wherein the DPP-4 inhibitor is linagliptin claim 1 , optionally in combination with one or more other active agents claim 1 , and the method is for reducing the risk or likelihood of severe sepsis in a patient with or at risk of SIRS and/or sepsis (SIRS/sepsis).7. The method according to claim 1 , wherein the DPP- ...

MUCOSAL BIOADHESIVE SLOW RELEASE CARRIER FOR DELIVERING ACTIVE PRINCIPLES

A mucosal bioadhesive slow release carrier comprising an active principle and devoid of starch, lactose, which can release the active principal for a duration of longer than 20 hours. This bioadhesive carrier contains a diluent, an alkali metal alkylsulfate, a binding agent, at least one bioadhesive polymer and at least one sustained release polymer, as well as a method for its preparation. 36. A prolonged release mucoadhesive tablet comprising:15% by weight microcrystalline cellulose;4.5% by weight sodium lauryl sulfate;0.4% by weight polyvinylpyrrolidone;20% of a mucoadhesive agent selected from milk protein concentrate, pea protein, carbopol 974, and chitosan;15% hypromellose;1% magnesium stearate;0.4% colloidal silica; and50 mg of acyclovir;wherein the acyclovir is in primary granules which also comprise the microcrystalline cellulose, the sodium lauryl sulfate, and the polyvinylpyrrolidone; andwherein the tablet is formed by compressing a mixture of the primary granules, the milk concentrate protein, the hypromellose, the magnesium stearate, and the colloidal silica.37. The tablet of claim 36 , wherein the mucoadhesive agent is milk protein concentrate. The present invention relates to a bioadhesive slow release carrier for the extended and controlled release of an active principle that can be used on mucosal surfaces. A process for manufacturing the bioadhesive system, a method for delivering an active ingredient to a mammal, as well as methods of treating, curing or preventing various medical conditions are also disclosed.Mucous membranes are linings of ectodermic origin, covered in epithelium, and are involved in absorption and secretion. They line various body cavities that are exposed to the external environment as well as internal organs, such as the nostrils, the lips, the ears, the genital area, the digestive tract and the anus. Parts of the body featuring mucous membranes include most of the respiratory tract and the entire gastrointestinal tract, as ...

PROLONGED RELEASE BIOADHESIVE THERAPEUTIC SYSTEMS

The present invention concerns a prolonged release bioadhesive mucosal therapeutic system containing at least one active principle, with an active principle dissolution test of more than 70% over 8 hours and to a method for its preparation. Said bioadhesive therapeutic system comprises quantities of natural proteins representing at least 50% by weight of active principle and at least 20% by weight of said tablet, between 10% and 20% of a hydrophilic polymer, and compression excipients, and comprising between 4% and 10% of an alkali metal alkylsulphate to reinforce the local availability of active principle and between 0.1% and 1% of a monohydrate sugar. 1. A prolonged release bioadhesive therapeutic system containing at least one active principle , having an active principle dissolution percentage of more than 70% over 8 hours , comprising quantities of natural proteins representing at least 50% by weight of active principle and at least 20% by weight of said bioadhesive therapeutic system , between 10% and 20% of a hydrophilic polymer , compression excipients , and comprising between 3.5% and 10% of an alkali metal alkylsulphate.2. The bioadhesive therapeutic system according to claim 1 , wherein said bioadhesive therapeutic system is a mucoadhesive tablet.3. The bioadhesive therapeutic system according to claim 2 , wherein the alkali metal alkylsulphate is sodium laurylsulphate or diethylsulphosuccinate.4. The bioadhesive therapeutic system according to claim 3 , in the form of a tablet in which the alkylsulphate is sodium laurylsulphate in a concentration of 3.5% to 10% claim 3 , of the total weight of the compounds in the tablet.5. The bioadhesive therapeutic system according to claim 1 , wherein the compression excipients contain corn starch.6. The bioadhesive therapeutic system according to claim 1 , in which one of the active principle is an antifungal from the broad spectrum azole family.7. The bioadhesive therapeutic system according to claim 6 , in the ...

Use of TRPA1 Antagonists to Prevent or Treat Infections Caused by Biological-Warfare Agents

Provided are methods for preventing and treating injuries caused by exposure to biological warfare agents. The methods include administering to a subject in need thereof an effective amount of a TRPA1 antagonist or a pharmaceutically acceptable salt thereof. In an embodiment the TRPA1 antagonist is selected from the group consisting of compounds of formula I 1. A method of preventing or treating an injury resulting from exposure to a biological-warfare agent , comprising administering to a subject in need thereof an effective amount of a TRPA1 antagonist or a pharmaceutically acceptable salt thereof.4. The method of claim 2 , wherein the TRPA1 antagonist is administered orally.5. The method of claim 2 , wherein the TRPA1 antagonist is administered via intramuscular injection.6. The method of claim 2 , wherein the TRPA1 antagonist is administered topically.7. The method of claim 2 , wherein the TRPA1 antagonist is administered by topical ocular administration.8. The method of claim 2 , wherein the TRPA1 antagonist is administered prior to the exposure to the biological-warfare agent.9. The method of claim 2 , wherein the TRPA1 antagonist is administered after exposure to the biological-warfare agent.10Bacillus anthracisBurkholderia malleiBurkholderia pseudomalleiClostridium botulinumFrancisella tularensisVibrio choleraeYersinia pestis. The method of claim 2 , wherein the biological-warfare agent is (anthrax) claim 2 , (glanders) claim 2 , (melioidosis) claim 2 , toxin (botulism) claim 2 , Ebola virus claim 2 , (tularemia) claim 2 , Marburg virus claim 2 , (cholera) claim 2 , alphaviruses claim 2 , Venezuelan equine encephalitis virus claim 2 , eastern equine encephalitis virus claim 2 , western equine encephalitis virus claim 2 , filoviruses claim 2 , arenaviruses claim 2 , Lassa virus claim 2 , Machupo virus or (plague).11Bacillus anthracis. The method of claim 2 , wherein the biological-warfare agent is (anthrax).12Yersinia pestis. The method of claim 2 , wherein ...

Combination therapy for the treatment of diabetes and related conditions

Combinations of DPP-4 inhibitors with GPR119 agonists, as well as to the use of these combinations for treating and/or preventing metabolic diseases, particularly diabetes (especially type 2 diabetes mellitus) and conditions related thereto. 3. The pharmaceutical composition according to claim 1 , wherein the DPP-4 inhibitor is 1-[(4-methylquinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-(3-(R)-aminopiperidin-1-yl)xanthine.4. The pharmaceutical composition according to claim 1 , wherein the GPR119 agonist is4-[6-(6-methanesulfonyl-2-methylpyridin-3-ylamino)-5-methylpyrimidin-4-yloxy]piperidine-1-carboxylic acid isopropyl ester or a pharmaceutically acceptable salt thereof.5. The pharmaceutical composition according to claim 1 , wherein the GPR119 agonist is 4-[5-methoxy-6-(2-methyl-6-[1 claim 1 ,2 claim 1 ,4]triazol-1-ylpyridin-3-ylamino)pyrimidin-4-yloxy]piperidine-1-carboxylic acid isopropyl ester or a pharmaceutically acceptable salt thereof.6. The pharmaceutical composition according to claim 1 , wherein the GPR119 agonist is 4-[5-methyl-6-(2-methylpyridin-3-yloxy)pyrimidin-4-yloxy]piperidine-1-carboxylic acid isopropyl ester or a pharmaceutically acceptable salt thereof.7. The pharmaceutical composition according to claim 1 , wherein the GPR119 agonist is {6-[1-(3-isopropyl-[1 claim 1 ,2 claim 1 ,4]oxadiazol-5-yl)piperidin-4-yloxy]-5-methoxypyrimidin-4-yl}-(6-methanesulfonyl-2-methylpyridin-3-yl)amine or a pharmaceutically acceptable salt thereof.8. The pharmaceutical composition according to claim 1 , wherein the GPR119 agonist is 4-[6-(6-methanesulfonyl-2-methylpyridin-3-ylamino)-5-methylpyrimidin-4-yloxy]piperidine-1-carboxylic acid isopropyl ester or a pharmaceutically acceptable salt thereof.9. The pharmaceutical composition according to claim 1 , wherein the GPR119 agonist is 4-[6-(6-methanesulfonyl-4-methylpyridin-3-ylamino)-5-methoxypyrimidin-4-yloxy]piperidine-1-carboxylic acid isopropyl ester or a pharmaceutically acceptable salt thereof.10. The ...

Combination Therapy for Cancer

An agent comprises a vector having a functional gene, a prodrug which can be converted into a cytotoxic agent by an expression product of the gene, and another cytotoxic agent, as a combined preparation for simultaneous, sequential or separate use in the therapy of cancer or of a disease characterised by an impaired mismatch repair (MMR) pathway, wherein the dosage regimen comprises beginning the another cytotoxic agent therapy no later than 7 days after the prodrug therapy has finished.

USE OF KERATINOCYTES AS A BIOLOGICALLY ACTIVE SUBSTANCE IN THE TREATMENT OF WOUNDS, SUCH AS DIABETIC WOUNDS, OPTIONALLY IN COMBINATION WITH A DPP-4 INHIBITOR

The invention relates to new keratinocytes which may be cultured in vitro and the use thereof for preparing a product which can be used to treat acute and chronic wounds, in combination with a DPP-4 inhibitor. 1. A method for treating wounds , the method comprising administering keratinocytes in combination with a DPP-4 inhibitor to a patient in need thereof , wherein the keratinocytes are not immortalised and may be doubled at least 150 times by in vitro cell culture methods.2. The method according to claim 1 , wherein the keratinocytes are isolated from the epidermal parts of a foreskin.3. The method according to claim 1 , characterised in that the keratinocytes are cells from the culture KC-BI-1 (DSM ACC 2514) claim 1 , or keratinocytes derived therefrom.4. The method according to claim 1 , wherein said keratinocytesa. cannot be replicated in the absence of foetal calf serum and/orb. in the absence of feeder cells and/orc. in the absence of Epidermal Growth Factor (EGF).5. The method according to claim 1 , wherein the said keratinocytes have little or no telomerase activity in comparison to immortalised keratinocytes.6. The method according to claim 1 , characterised in that the said keratinocytes can be replicated at least 200 times by in vitro cell culture methods.7. The method according to claim 1 , characterised in that the said keratinocytes can be replicated at least 250 times by in vitro cell culture methods.8. The method according to claim 1 , characterised in that the said keratinocytes can be replicated at least 300 times by in vitro cell culture methods.9. A pharmaceutical combination comprising a DPP-4 inhibitor and a carrier comprising keratinocytes claim 1 , whereina. the carrier is partially colonised with keratinocytes; orb. the carrier is completely colonised with keratinocytes; andwherein the keratinocytes are not immortalised and may be doubled at least 150 times by in vitro cell culture methods.10. The pharmaceutical combination according to ...

USE OF A DPP-4 INHIBITOR IN AUTOIMMUNE DIABETES, PARTICULARLY LADA

The present invention relates to methods for treating and/or preventing autoimmune diabetes, particularly LADA, as well as diseases related or associated therewith, comprising the administration of an effective amount of a certain DPP-4 inhibitor, as well as to the use of a certain DPP-4 inhibitor for modifying disease trajectory of autoimmune diabetes (particularly LADA). 2. The method according to claim 1 , wherein human patient has or is at risk of a cardiovascular and/or renal disease selected from the group consisting of myocardial infarction claim 1 , stroke claim 1 , peripheral arterial occlusive disease claim 1 , diabetic nephropathy claim 1 , micro- or macroalbuminuria claim 1 , acute or chronic renal impairment claim 1 , hyperuricemia and hypertension.3. The according to claim 1 , wherein the human patient has nephropathy claim 1 , impaired renal function claim 1 , chronic kidney disease claim 1 , and micro- or macroalbuminuria.4. The method of claim 1 , wherein the human patient has mild claim 1 , moderate or severe renal impairment claim 1 , or end stage renal disease.5. The method of claim 1 , wherein the human patient patient has microalbuminuria or diabetic nephropathy.6. The method of claim 1 , wherein the one or more other active agents is selected from the group consisting of metformin claim 1 , thiazolidinediones claim 1 , insulin and insulin analogues.7. A method for modifying the disease trajectory of latent autoimmune diabetes of adults (LADA) in a human patient claim 1 , the method comprising administering to said human patient linagliptin claim 1 , optionally in combination with one more other active agents selected from the group consisting of metformin claim 1 , thiazolidinediones claim 1 , insulin and insulin analogues claim 1 , wherein said human patient has one or more autoantibodies selected from the group consisting of GAD-65 claim 1 , anti-GAD claim 1 , ICA claim 1 , IA-2A claim 1 , ZnT8 (anti-ZnT8) and IAA.8. The method according to ...