ВЫДЕЛЕННЫЙ ПОЛИПЕПТИД, ОБЛАДАЮЩИЙ АНТИВИРУСНОЙ АКТИВНОСТЬЮ (ВАРИАНТЫ), КОДИРУЮЩИЙ ЕГО ПОЛИНУКЛЕОТИД(ВАРИАНТЫ), ЭКСПРЕССИРУЮЩИЙ ВЕКТОР, РЕКОМБИНАНТНАЯ КЛЕТКА-ХОЗЯИН, СПОСОБ ПОЛУЧЕНИЯ ПОЛИПЕПТИДА, АНТИТЕЛО, СПЕЦИФИЧНОЕ К ПОЛИПЕПТИДУ, И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ПОЛИПЕПТИД

Изобретение относится к области биотехнологии, конкретно к получению цитокинов класса II, и может быть использовано в медицине. Полученные белки zcyto20, zcyto21, zcyto22, zcyto24 и zcyto25 являются наиболее близкородственными с интерфероном-α на уровне аминокислотной последовательности. Рецептор для этого семейства белков служит рецептор цитокинов класса II. Белки могут быть получены рекомбинантным путем с использованием клетки-хозяина, трансформированной экспрессирующим вектором, который содержит соответствующие белкам нуклеиновые кислоты. На основе белков zcyto20, zcyto21, zcyto22, zcyto24 и zcyto25 получают антивирусную фармацевтическую композицию и специфические антитела. Изобретение позволяет получить новый цитокин, который стимулирует клетки гемопоэтической линии дифференцировки и обладает выраженной антивирусной активностью. 19 н. и 5 з.п. ф-лы, 21 табл.

ТЕРАПИЯ ДЛЯ ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ

Предложены фармацевтическая композиция для лечения гиперактивного мочевого пузыря (ГАМП), содержащая терапевтически эффективное количество первого соединения (является антимускариновым или антихоли-нергическим агентом) и терапевтически активное количество второго соединения (вызывает стимуляцию слюнных желез), причем (i) первое соединение является оксибутинином или его приемлемой солью и второе соединение является пилокарпином или его солью; или (ii) первое соединение является толтеродином или его солью и второе соединение является пилокарпином или его солью, и соответствующий способ лечения пациента, включающий введение вышеописанной фармацевтической композиции. Показано, что антимускариновая активность оксибутинина, ответственная за его терапевтическое действие на ГАМП, остается неизменной после введения композиции при полной нейтрализации его неблагоприятного побочного действия - сухости во рту. Это приводит к более переносимому, эффективному и рентабельному лечению. 2 н. и 13 з.п. ф-лы ...

СПОСОБ ЛЕЧЕНИЯ СТРЕССОВОГО НЕДЕРЖАНИЯ МОЧИ СЛАБОЙ И СРЕДНЕЙ СТЕПЕНИ ВЫРАЖЕННОСТИ У ЖЕНЩИН

Изобретение относится к медицине, а именно к урологии и гинекологии. На фоне физиологического наполнения мочевого пузыря выполняют трансуретральное введение в парауретральные ткани проксимальной части уретры гетерогенного геля, при помощи фиброуретроскопа или ригидного уретроцистоскопа, в три точки, как на фигуре 1: по боковым и нижней стенкам уретры на глубину 3 мм, до формирования папул объемообразующего вещества гетерогенного геля общим объемом 1-3 мл, с размером частиц от 150 до 300 микрометров, содержащий 30% коллагенсодержащего экстракта и 70% моносахаридов. Способ позволяет сократить время лечения пациентов, минимизировать возможные риски и избежать осложнений, связанных с оперативным лечением, улучшить качество жизни пациентов, снизить экономические затраты за счет сокращения времени лечения. 1 ил., 2 пр.

ПРОИЗВОДНЫЕ 1,2,4,5-ТЕТРАГИДРОБЕНЗО[D]АЗЕПИНОВ И ЛЕКАРСТВЕННОЕ СРЕДСТВО НА ИХ ОСНОВЕ

Изобретение относится к органической химии и может найти применение в медицине. Описываются производные 1,2,4,5-тетрагидробензо[d]азепинов общей формулы I где Х обозначает -N=, =N-, -N<, >С= или =С<, Y обозначает -N=, =N-, -NH-, -СН= или =СН-, пунктирная линия может обозначать связь, а радикалы R1-R16 такие, как это описано в формуле изобретения, а также их фармацевтически приемлемые соли в их рацемической и оптически активной форме. Также описывается лекарственное средство, которое может найти применение при лечении или предупреждении острых и/или хронических неврологических нарушений. Технический результат - получены новые соединения, обладающие полезными биологическими свойствами. 2 н. и 11 з.п. ф-лы, 1 табл.

ПРИМЕНЕНИЕ 6-ДИМЕТИЛАМИНОМЕТИЛ-1-ФЕНИЛЦИКЛОГЕКСАНОВЫХ СОЕДИНЕНИЙ ДЛЯ ТЕРАПИИ НЕДЕРЖАНИЯ МОЧИ

Настоящее изобретение относится к области медицины и фармакологии и касается применения замещенных производных 6-диметиламинометил-1-фенилциклогексана формулы (I) для получения лекарственного средства, предназначенного для лечения учащенных позывов к мочеиспусканию, соответственно недержания мочи. Описываемое лекарственное средство обладает меньшими побочными эффектами и/или анальгетическими эффектами. 2 н. и 10 з.п. ф-лы, 2 табл.

ВОДНЫЙ ГЕЛЬ, СОДЕРЖАЩИЙ КАППА-КАРРАГЕНАН В КАЧЕСТВЕ ГЕЛЕОБРАЗУЮЩЕГО АГЕНТА И, ПО МЕНЬШЕЙ МЕРЕ, 85% ВОДЫ

Изобретение относится к области ветеринарии. Водный гель для профилактики и лечения заболеваний нижнего мочевого тракта у кошек и собак, включает (а) эффективное количество гелеобразующего агента, который представляет собой каппа-каррагенан, (b) эффективное количество вещества, повышающего аппетит кошек или собак, и (с) по меньшей мере 85 масс.% воды. Изобретение обеспечивает снижение концентрации минеральных компонентов в моче в результате увеличения ее продукции. 5 н. и 13 з.п. ф-лы, 1 табл.

ПРОИЗВОДНЫЕ ОКСИМА ПИПЕРАЗИНА, ОБЛАДАЮЩИЕ АНТАГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ ПО ОТНОШЕНИЮ К РЕЦЕПТОРУ НЕЙРОКИНИНА-1 (НК-1).

Настоящее изобретение относится к производным оксима пиперазина общей формулы I в которой Х - фенил или пиридил, замещенный 1 или 2 заместителями; - Y - 2- или 3-индолил, фенил, 7-аза-индол-3-ил, 3-индазолил, 2-нафтил, 3-бензо[b]тиофенил или 2-бензофуранил, которые могут быть замещены; n=0-3; m=0-2; - R1 - NH2, морфолино, тиоморфолино, 2-, 3- или 4-пиридил или 4-СН3-пиперазинил. Соединения обладают антагонистической активностью по отношению к рецептору нейрокинина и могут быть использованы для лечения состояний тревоги. Описана также фармацевтическая композиция на основе соединений формулы I, способ ее получения и применения. 5 н. и 2 з.п. ф-лы.

ПРЕПАРАТ ДЛИТЕЛЬНОГО ВЫСВОБОЖДЕНИЯ ДЛЯ СНИЖЕНИЯ ЧАСТОТЫ МОЧЕИСПУСКАНИЯ И СПОСОБ ЕГО ПРИМЕНЕНИЯ

Группа изобретений относится к медицине, а именно к урологии, и может быть использована для снижения частоты мочеиспускания. Для этого субъекту вводят фармацевтическую композицию, состоящую из эффективных количеств золпидема, составленного для немедленного высвобождения, и одного или более анальгетических средств, составленных для длительного или отсроченного высвобождения. Также предложена фармацевтическая композиция, состоящая из эффективных количеств золпидема, составленного для немедленного высвобождения, и одного или более анальгетических средств, составленных для длительного или отсроченного высвобождения. Группа изобретений обеспечивает эффективное подавление сокращений гладкой мускулатуры мочевого пузыря. 2 н.п. ф-лы, 9 табл., 8 пр., 1 ил.

ПРОИЗВОДНЫЕ ХИНУКЛИДИНА, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ЛЕЧЕНИЯ И ПРОМЕЖУТОЧНЫЕ ВЕЩЕСТВА

Изобретение относится к новым производным хинуклидина общей формулы (I) где © представляет фенильное кольцо, С4-С9 гетероароматическую группу, содержащую один или несколько гетероатомов, нафталинильную, 5,6,7,8-тетрагидронафталинильную или бифенильную группу; R1, R2 и R3 представляет водород, галоген, фенил и др.; n представляет целое число от 0 до 4; А представляет группу -CH=CR6-, -CR6=CH-, -CR6 R7 и др.; R6 и R7 представляют водород, алкил и др.; m представляет целое число от 0 до 8; р представляет целое число от 1 до 2; заместитель в азониабициклическом кольце может находиться в положении 2, 3 или 4, включая все возможные конфигурации асимметрических атомов углерода; В представляет собой группу формулы i) или ii) где R10 представляет водород, гидроксильную группу или метил; R8 и R9 каждый представляет где R11 представляет водород, галоген, алкил; Q представляет одинарную связь, -СН2- и др.; Х представляет фармацевтически приемлемый анион моно- или поливалентной кислоты. Соединения формулы ...

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.

АКТИВАТОР KCNQ2-5 КАНАЛОВ

Изобретение относится к соединению, представленному общей формулой (I), или его фармацевтически приемлемой соли, которые могут найти применение для профилактики и/или лечения заболевания, связанного с KCNQ2-3 каналом. В формуле (I) X1 представляет собой C-R6; X2 представляет собой C-R7; R11 представляет собой (1) OR1 или (2) NH2; R1 представляет собой (1) атом водорода или (2) C1-4 алкильную группу; каждый R2 и R3 независимо представляет собой (1) атом водорода или (2) C1-4 алкильную группу, которая может быть замещена атомом галогена, где R2 и R3 не могут оба одновременно представлять собой атом водорода; каждый R4, R5, R6 и R7 независимо представляет собой (1) атом водорода, (2) атом галогена или (3) C1-4 алкильную группу, где R4 и R5 не могут оба одновременно представлять собой атом водорода; Y представляет собой (1) -NH- или (2) связь; R8 представляет собой (1) атом водорода или (2) C1-4 алкильную группу; R9 представляет собой (1) цикл A, (2) C1-6 алкильную группу, (3) -C1-4 алкилен-цикл ...

СОСТАВЫ БИОПРЕПАРАТОВ ДЛЯ ВНУТРИПУЗЫРНОЙ ИНСТИЛЛЯЦИИ

Заявленная группа изобретений относится к области медицины и представляет собой фармацевтическую композицию для лечения нейрогенной или идиопатической дисфункции мочевого пузыря, содержащую терапевтически эффективное количество вещества, полученного из клостридий, и по меньшей мере один пермеабилизирующий агент, причем вещество, полученное из клостридий, является ботулиническим токсином, и причем по меньшей мере один пермеабилизирующий агент содержит неионогенное поверхностно-активное вещество и мукоадгезивное вещество, представляющее собой катионный полимер, и причем по меньшей мере один пермеабилизирующий агент присутствует в количестве, эффективном для существенного и обратимого повышения проницаемости стенки мочевого пузыря для вещества, полученного из клостридий и способ лечения пациента с нейрогенной дисфункцией мочевого пузыря, включающий: внутрипузырную инстилляцию на стенку мочевого пузыря пациента заявленной фармацевтической композиции. Заявленная группа изобретений высокоэффективна ...

ФОСФАТНЫЕ ПРОИЗВОДНЫЕ ФТОРОКСИНДОЛОВ И СПОСОБ ЛЕЧЕНИЯ С ИХ ИСПОЛЬЗОВАНИЕМ

Изобретение относится к группе новых соединений формулы (I) где волнообразная связь обозначает рацемат, (R)-энантиомер или (S)-энантиомер; А представляет собой прямую связь или (С=O); В представляет собой прямую связь, кислород или азот; m имеет значение 0 или 1; n имеет значение 1, 2 или 3; R1 и R2 каждый независимо является водородом или C1-6алкилом, и когда R1 представляет собой водород, R2 может также быть P(O)OR5OR6; R3 и R4 каждый независимо является водородом или C1-4 алкилом; R5 и R6 каждый независимо является водородом, или к их нетоксичным фармацевтически приемлемым солям или сольватам. Изобретение также относится к способу лечения заболеваний, чувствительных к раскрытию активируемых кальцием калиевых каналов. Технический результат - получение новых биологически активных соединений и способ лечения заболеваний, чувствительных к раскрытию активируемых кальцием калиевых каналов большой проводимости у млекопитающего. 2 н. и 7 з.п. ф-лы, 1 табл.

ПРОИЗВОДНЫЕ ХИНУКЛИДИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ЛЕЧЕНИЯ РЕСПИРАТОРНЫХ ЗАБОЛЕВАНИЙ

Изобретение относится к новым соединениям, которые представляют собой соединения, выбранные из 3(R)-(2-гидрокси-2, 2-дитиен-2-илацетокси)-1-(3-феноксипропил)-1-азониабицикло[2,2,2]октана, X- и 1-фенэтил-3(R-)-(9[Н]-ксантен-9-карбонилокси)-1-азониабицикло-[2,2,2]октана, X-, где X- представляет собой фармацевтически приемлемый анион моно- или поливалентной кислоты, обладающим ингибирующей активностью в отношении мускариновых М3 рецепторов, к фармацевтической композиции на их основе и к способу лечения респираторного заболевания. 3 н. и 17 з.п. ф-лы, 1 табл.

СОЕДИНЕНИЕ, ОБЛАДАЮЩЕЕ СОКРАЩАЮЩЕЙ ДЕТРУЗОР АКТИВНОСТЬЮ И РЕЛАКСИРУЮЩЕЙ УРЕТРАЛЬНЫЙ СФИНКТЕР АКТИВНОСТЬЮ

Изобретение относится к соединению, представленному формулой (I), гдепредставляет собой α-конфигурацию;представляет собой β-конфигурацию; ипредставляет собой α-конфигурацию, β-конфигурацию или их произвольную смесь, его соль, или его смесь с диастереомером в произвольном соотношении, или его циклодекстриновый клатрат. Изобретение относится к фармацевтической композиции для предупреждения, лечения и/или уменьшения интенсивности дисфункции сокращения мочевого пузыря и/или дисфункции уретральной релаксации, содержащей, в качестве активного ингредиента, соединение, представленное формулой (I). Изобретение также относится к соединению, представленному формулой (I-a), где Rпредставляет собой C-C-алкильную группу, такую как метил, этил, пропил, изопропил, бутил, изобутил или трет-бутил;представляет собой α-конфигурацию;представляет собой β-конфигурацию; ипредставляет собой α-конфигурацию, β-конфигурацию или их произвольную смесь, его соль, или его смесь с диастереомером в произвольном соотношении ...

АЛЬФА-АМИНОАМИДНЫЕ ПРОИЗВОДНЫЕ, ИСПОЛЬЗУЕМЫЕ ДЛЯ ЛЕЧЕНИЯ РАССТРОЙСТВ НИЖНИХ МОЧЕВЫВОДЯЩИХ ПУТЕЙ

Изобретение относится к применению терапевтического средства, представляющего собой α-аминоамидное соединение формулы (I): ! ! в которой R представляет собой фенильное кольцо, необязательно замещенное одним или двумя заместителями, независимо выбранными из галогена, гидрокси, циано, C1-С6-алкила, C1-С6-алкокси или трифторметила; R1 представляет собой водород или C1-С6-алкил; R2 и R3 независимо выбирают из водорода, С1-С4-алкила; R4 и R5 независимо представляют собой водород, C1-С6-алкил; Х представляет собой О или S; Y и Z, взятые вместе с Х и фенильным кольцом, с которым связаны Y и X, образуют 5-7-членный насыщенный гетероцикл, содержащий атомы О или S, или Y и Z представляют собой водород; или его изомеров, смесей и фармацевтически приемлемых солей для получения лекарственного средства для лечения расстройств нижних мочевыводящих путей. Изобретение также относится к фармацевтической композиции. 3 н. и 5 з.п. ф-лы, 3 ил.

НОВЫЕ ПРОИЗВОДНЫЕ 3,3-ДИФЕНИЛПРОПИЛАМИНОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ (ВАРИАНТЫ) И СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Описываются производные 3,3-дифенилпропиламинов общих формул I и VII1, где R и R1 независимо выбраны из водорода, С1-С6алкила, С3-С10циклоалкила, С1-С6алкилкарбонила, С1-С6алкоксикарбонила, замещенного или незамещенного бензола и др., Х представляет собой третичную аминогруппу, Y и Z независимо представляют собой одинарную связь между (СН2)n группой и карбонильной группой, О, S или NH, А представляет собой водород (1Н) или дейтерий (2Н), n является числом от 0 до 12, и их соли с физиологически приемлемыми кислотами, их свободные основания, способы их получения; фармацевтические композиции, содержащие эти соединения, а также применение этих соединений для приготовления антимускаринового лекарства. Технический результат заключается в получении новых пролекарств антимускариновых агентов с хорошими фармакокинетическими свойствами по сравнению с существующими лекарствами, такими как оксибутинин и толтеродин. Полученные соединения и содержащие их фармацевтические композиции применяют для лечения ...

СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ НЕДЕРЖАНИЯ МОЧИ

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

СПОСОБ ЛЕЧЕНИЯ ЗЛОКАЧЕСТВЕННЫХ ОПУХОЛЕЙ МОЧЕВОГО ПУЗЫРЯ

Изобретение относится к медицине, онкологии, и может быть использовано для фотодинамической терапии поверхностного рака мочевого пузыря. Для этого за 2 часа до лазерного воздействия в полость мочевого пузыря вводят химиопрепарат митомицин С в дозе 40 мг на 50 мл 0,9% физиологического раствора. Воздействуют лазером через внутрипузырную жидкую оптическую среду. Способ позволяет повысить эффективность противоопухолевого лечения за счет увеличения десмосомальных промежутков опухолевых тканей, что облегчает транспорт химиопрепарата, присутствие фотосенсибилизатора в опухолевых клетках способствует максимальной концентрации химиопрепарата в опухоли по отношению к нормальной слизистой, а также увеличению продолжительности воздействия химиопрепарата на опухоль, потенцирования воздействия на опухоль фотодинамической терапии.

СПОСОБ ЛЕЧЕНИЯ РАКА МОЧЕВОГО ПУЗЫРЯ

Изобретение относится к медицине, а именно к онкоурологии, и может быть использовано в предоперационном периоде при лечении местнораспространенных и рецидивных форм рака мочевого пузыря. Предложено у больных производить последовательно забор крови по 100 мл в два стерильных флакона с глюгициром. Затем в первый флакон вводить доксорубиции из расчета 50-60 кг/м2 и циклофосфан 600-800 мг/м2, во второй флакон вводить циплатин из расчета 80-100 мг/м2, после экспозиции в термостате при t = 36,5 - 37,7oС в течение 30 мин производить реинфузию аутокрови с цитостатиками в затемненных флаконах, сначала первого флакона с циклофосфаном и доксорубицином, затем для уменьшения нефротоксичности проводить гидротацию 5%-ным раствором глюкозы 1000 мл, затем реинфузия второго флакона с препаратом платины, в заключение вводить раствор гемодеза с 2 мл лазикса. Препараты вводят один раз в неделю, всего на курс лечения 2-3 инфузии. Способ позволяет уменьшить размеры опухоли, улучшить состояние больного, сохранить ...

ЗАМЕЩЕННЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Описываются новые замещенные гетероциклические соединения формулы I, где А означает двухвалентный радикал, выбранный из -О-СО-, -CH2O-CO- и др., как указано в п.1 формулы, R1 означает водород или C1-C4-алкил; m - 2, 3; Ar1 означает фенил, возможно замещенный галогеном, гидроксилом, C1-C4-алкокси, C1-C4-алкилом, трифторметилом, метилендиокси; Т означает -CH2-Z, -CH(C6H5 )2, -C(C6H5)3. Соединения формулы I обладают сродством к рецепторам тахикинина при ингибиторной константе Ki ниже 10-8 М. Описывается способ получения соединений формулы I и промежуточные соединения, используемые в нем. Описывается также фармацевтическая композиция, обладающая антагонистической активностью к рецепторам нейрокининов, содержащая в качестве активного вещества соединение формулы I. 12 с. и 13 з.п.ф-лы, 3 табл.

СПОСОБ ЛЕЧЕНИЯ ГИПЕРАКТИВНОСТИ МОЧЕВОГО ПУЗЫРЯ

Изобретение относится к медицине, а именно к лечению дисфункции мочевого пузыря, обусловленной гиперактивностью детрузора. Способ представляет собой инстилляцию антихолинэргического препарата, содержащего оксибутинина гидрохлорид в физиологически приемлемой дозе, отличающийся тем, что используют антихолинэргический препарат, содержащий дополнительно димексид и водный раствор поливинилового спирта, причем упомянутый препарат вводят в форме раствора стандартным объемом 20 мл однократно через день до исчезновения клинических признаков заболевания. Предложенный способ позволяет повысить эффективность лечения за счет улучшения трансэпителиального проникновения оксибутинина через слизистую мочевого пузыря. 1 табл.

СПОСОБ ЛЕЧЕНИЯ НЕЙРОГЕННОЙ ДИСФУНКЦИИ МОЧЕВОГО ПУЗЫРЯ

Изобретение относится к медицине, в частности к урологии, и может быть использовано для лечения нейрогенной дисфункции мочевого пузыря у детей и взрослых. Для этого предлагают вводить альфа-1-адреноблокатор, например доксазозин. Способ обеспечивает эффективное лечение, в том числе, недержания мочи у детей с миелодисплазией. 3 з.п. ф-лы.

ПРИМЕНЕНИЕ АНТАГОНИСТОВ АКТИВИРУЕМЫХ ПРОТЕАЗОЙ РЕЦЕПТОРОВ 1 (PAR-1) ДЛЯ ПРОФИЛАКТИКИ И/ИЛИ ЛЕЧЕНИЯ ФУНКЦИОНАЛЬНЫХ ПАТОЛОГИЧЕСКИХ СОСТОЯНИЙ В ОБЛАСТИ ТАЗА И ПРОМЕЖНОСТИ

Группа изобретений относится к медицине. Предложено применение антагониста PAR1, выбранного из ворапаксара, атопаксара, 3-(2-хлорфенил)-1-[4-(4-фторбензил)пиперазин-1-ил]пропенона и их фармацевтически приемлемых солей в качестве лекарственного средства для профилактики и/или лечения функционального патологического состояния в области таза и промежности, выбранного из группы синдром раздраженного мочевого пузыря, синдром гиперактивного мочевого пузыря, хронической боли в области таза и промежности и недержания мочи, и фармацевтическая композиция того же назначения на основе указанных соединений. Технический результат состоит в снижении усиленных сократительных реакций воспалённого или гиперактивного мочевого пузыря. 2 н. и 13 з.п. ф-лы, 12 ил.

СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ НЕДЕРЖАНИЯ МОЧИ В СТАРЧЕСКОМ ВОЗРАСТЕ

Изобретение относится к созданию фитотерапевтических средств для лечения недержания мочи в пожилом возрасте. Средство для лечения старческого недержания мочи, представляющее собой водный настой травы смолевки обыкновенной, полученный путем настаивания 3 ч. л. измельченной травы с 700 мл воды в течение 10 часов в теплом месте, при этом температура воды должна быть 80°С. Проведенный курс лечения заявленным средством показывает положительное терапевтическое воздействие заявленного средства на процесс лечения. Средство не обладает побочным действием и проявляет тонизирующее воздействие на мускулатуру мочевого пузыря.

ПРИМЕНЕНИЕ 2-АЛКОКСИФЕНИЛ-ЗАМЕЩЕННЫХ ИМИДАЗОТРИАЗИНОВ

... 1. Применение 2-фенил-замещенных имидазотриазинонов общей формулы (I) в которой R1 означает метил или этил, R2 означает этил или пропил, R3 и R4 являются одинаковыми или различными и означают неразветвленную или разветвленную алкильную цепь, имеющую до 5 атомов углерода, которая, при необходимости, до двух раз одинаково или различно замещена гидрокси или метокси, или R3 и R4 вместе с атомом азота образуют кольцо пиперидинила, морфолинила, тиоморфолинила или остаток формулы где R5 означает водород, формил, ацил или алкоксикарбонил, имеющий соответственно до 3 атомов углерода, или неразветвленный или разветвленный алкил, имеющий до 3 атомов углерода, который, при необходимости, от одного до двух раз, одинаково или различно замещен гидрокси, карбоксилом, неразветвленным или разветвленным алкокси или алкоксикарбонилом, имеющим соответственно до 3 атомов углерода, или группами формул -(D)a -NR6R7или -P(O)(OR8)(OR9), где а означает число 0 или 1, D означает группу формулы -СО, R6 и R7 являются ...

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 5, 6, 6А, 11B-ТЕТРАГИДРО-7-ОКСА-5-АЗАБЕНЗО[С]ФЛУОРЕН-6-КАРБОНОВОЙ КИСЛОТЫ В КАЧЕСТВЕ NMDA-АНТАГОНИСТОВ

... 1. Замещенные производные 5,6,6а,11b-тетрагидро-7-окса-5-азабензо[с]флуорен-6-карбоновой кислоты общей формулы I в представленном виде либо в виде их кислот или их оснований, либо в виде их солей, прежде всего физиологически совместимых солей, либо в виде их сольватов, прежде всего гидратов, прежде всего в виде их физиологически совместимых солей с катионами или основаниями либо с анионами или кислотами, необязательно в виде их рацематов, их чистых стереоизомеров, прежде всего энантиомеров или диастереомеров либо в виде смесей стереоизомеров, прежде всего энантиомеров или диастереомеров, в любом их соотношении в смеси, где R1, R2, R3 и R4 независимо друг от друга обозначают Н, F, Cl, Br, I, CN, NO2 или С1-С18алкил, С2-С18 алкенил либо С2-С18алкинил, каждый из которых является разветвленным либо неразветвленным, одно- или многозамещенным либо незамещенным, С3-С8циклоалкил, который является насыщенным либо ненасыщенным, одно- или многозамещенным либо незамещенным, соответственно соответствующий ...

ОСНОВНЫЕ НЕПЕПТИДНЫЕ АНТАГОНИСТЫ БРАДИКИНИНА И ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

... 1. Соединения общей формулы (I): в которой R1 означает атом водорода или C1-C4алкильную группу; R2 и R3, которые могут быть одинаковыми или различными, представляют C1-C4алкильную группу, или R2 и R3 вместе с атомом углерода, к которому они присоединены, образуют циклическую алифатическую группу, содержащую 3-7 атомов углерода, или гетероциклическую алифатическую группу, содержащую 3-7 атомов, один или два из которых выбраны из группы N, O, S, и другие являются атомами C; R4 и R5, которые могут быть одинаковыми или различными, означают атом водорода или C1-C4алкильную группу; X выбран из группы, включающей галоген, OR1, SR1, CN, C1-C4алкил; B содержит, по меньшей мере, одну аминогруппу с основными характеристиками или тетраалкиламмонийную группу и может быть выбран из группы, включающей: -NR6(CH2)nNHCOY, NR6(CH2)nN(R6 )-Y, NR6(CH2)nN(Y)2, NR6Y, N(Y)2, N(Y)(CH2)pY1 и из остатков: ; R6 означает атом водорода, C1-C6алкил; n=1-12 и Y выбран из водорода, (CH2)pY1, (CH2)pNR6Y1, (CH2)pN(Y1)2, ...

ПРОИЗВОДНЫЕ-АМИНОАМИДОВ, ПРИМЕНИМЫЕ В КАЧЕСТВЕ ПРОТИВОВОСПАЛИТЕЛЬНЫХ АГЕНТОВ

... 1. Способ лечения воспаления из одного или более воспалительных расстройств у нуждающегося в этом пациента, являющегося человеком,, включающий введение пациенту количества по меньшей мере одного противовоспалительного агента, эффективного для уменьшения или предотвращения воспаления, который представляет собой альфа-аминоамидное соединение формулы (I) где A представляет собой -(CH2)n-X-группу, где n является целым числом от 0 до 5, X является CH2, -O-, -S- или -NH-; s равно 1 или 2; R представляет собой фурильное, тиенильное или пиридильное кольцо или фенильное кольцо, необязательно замещенное одним или двумя заместителями, независимо выбираемыми из галогена, гидрокси, циано, C1-C6 алкила, C1-C6 алкокси или трифторметила; R1 представляет собой водород или C1-C6 алкил, или C3-C7 циклоалкил; R2 и R3 независимо выбирают из водорода; C1-C4 алкила, необязательно замещенного гидрокси или фенилом; фенила, необязательно замещенного одним или двумя заместителями, независимо выбираемыми из C1-C6 ...

ЗАМЕЩЕННЫЕ 2-ТИО-3,5-ДИЦИАНО-4-ФЕНИЛ-6-АМИНОПИРИДИНЫ И ЛЕКАРСТВЕННОЕ СРЕДСТВО НА ИХ ОСНОВЕ

Изобретение относится к замещенным 2-тио-3,5-дициано-4-фенил-6-аминопиридинам, представленным структурой формулы (I) в которой n означает 2, 3 или 4, R1 означает водород или алкил с 1-4 атомами углерода и R2 означает пиридил или тиазолил, который может быть замещен алкилом с 1-4 атомами углерода, галогеном, амино, диметиламино, ацетиламино, гуанидино, пиридиламино, тиенилом, пиридилом, морфолинилом, а также тиазолилом, при необходимости замещенным алкилом с 1-4 атомами углерода, или фенилом, при необходимости содержащим до трех заместителей в виде галогена, алкила с 1-4 атомами углерода или алкокси с 1-4 атомами углерода, и к их солям, гидратам, гидратам солей и сольватам, а также к замещенным 2-тио-3,5-дициано-4-фенил-6-аминопиридина формулы (I), обладающим свойствами агониста рецептора А1 аденозина. Также данное изобретение описывает лекарственное средство, обладающее свойствами агониста рецептора А1 аденозина. Технический результат - получены новые соединения, обладающие полезными биологическими ...

СПОСОБ ЛЕЧЕНИЯ АТОНИИ МОЧЕВОГО ПУЗЫРЯ ПОСЛЕ РАДИКАЛЬНЫХ ОПЕРАТИВНЫХ ВМЕШАТЕЛЬСТВ ПРИ РАКЕ МАТКИ

Изобретение относится к медицине, в частности к консервативной гинекологии. Сущность изобретения: после выведения остаточной мочи в мочевой пузырь вводят 90-100 г подогретого до 40-42°С рыбьего жира. Способ позволяет восстановить самостоятельное мочеиспускание при атонии мочевого пузыря после радикальных оперативных вмешательств при раке матки.

ИСПОЛЬЗОВАНИЕ СОЕДИНЕНИЙ РЯДА 3-АРОЛОКСИПРОПИЛАМИНОВ В ЛЕЧЕНИИ НЕДЕРЖАНИЯ

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

ЛЕКАРСТВЕННЫЙ СБОР ДЛЯ ЛЕЧЕНИЯ И ПРОФИЛАКТИКИ АДЕНОМЫ ПРОСТАТЫ И ЦИСТИТА

Изобретение относится к медицине, а именно к фитотерапевтическим средствам лечения и профилактики аденомы простаты и цистита, применяемым самостоятельно, а также в комплексе с другими средствами лечения заболеваний этого характера. Изобретение решает задачу создания лекарственного сбора для лечения больных аденомой простаты и цистита, не имеющего нежелательных побочных влияний, простого в изготовлении, содержащего доступные и недорогие компоненты, при очень хорошем терапевтическом эффекте. Сбор имеет следующий состав, мас.ч.: корень солодки 1; cемя каштана конского 2; лист орешника 3; трава смолевки татарской или поникающей 2; плод шиповника 3.

Антагонисты рецептора брадикинина

... 1. Соединение формулы IA где R5А обозначает -XA-R6A или –N(R7A)R8A, где XA обозначает пиперидинилен или пиперазинилен, R6A обозначает Н, С1-С4алкил, С3-С4алкенил, С3-С4алкинил, С1-С4(алкоксиалкил), С1-С4 (карбоксиалкил), С5-С7гетероциклическую группу или фенилС1-С4алкил; R7A обозначает аминоС1-С4алкил или моно- или ди(С1-С5алкил)амино-С2-С5алкил и R8A обозначает Н, Сl-С4алкил или имеет значения, указанные для R7A; X1 обозначает двухвалентную группу формулы IA’ где n = 0 или 1; X3 обозначает СН или N; (а) X4 обозначает прямую связь, R3A и R4A вместе обозначают этилен и m = 2; или (б) X4 обозначает прямую связь, R3A обозначает Н, С1-С4алкил, С3-С6циклоалкил, С3-С6алкенил, С3-С6 алкинил, С7-С10аралкил или С6-C9 гетероаралкил, R4A обозначает Н и m = 1 или 2 или 3; или (в) X4 обозначает -CH(R12 )-, R3A обозначает Н и R4A и R12 вместе обозначают пропилен и m = 1, или этилен и m = 2; X2 обозначает двухвалентную группу формулы IA’’ где X3 обозначает СН или N; R11 обозначает С1-С4алкил, С3-С6циклоалкил ...

НОВАЯ ФОРМА (R)-N-[5МЕТИЛ-8-(4-МЕТИЛПИПЕРАЗИН-1-ИЛ)-1,2,3,4-ТЕТРАГИДРО-2-НАФТИЛ]-4-МОР ФОЛИНОБЕНЗАМИДА

... 1. Форма А моногидробромида (R)-N-[5-метил-8-(4-метилпиперазин-1-ил)-1,2,3,4-тетрагидро-2-нафтил]-4-морфолинобензамида. 2. Форма А моногидробромида (R)-N-[5-метил-8-(4-метилпиперазин-1-ил)-1,2,3, 4-тетрагидро-2-нафтил]-4-морфолинобензамида по п.1, которая представляет собой по существу кристаллографически чистую Форму А моногидробромида (R)-N-[5-метил-8-(4-метилпиперазин-1-ил)-1,2,3, 4-тетрагидро-2-нафтил]-4-морфолинобензамида. 3. Форма А моногидробромида (R)-N-[5-метил-8-(4-метилпиперазин-1-ил)-1,2,3, 4-тетрагидро-2-нафтил]-4-морфолинобензамида по п.2, содержащая не более 10% любой другой кристаллической формы моногидробромида (R)-N-[5-метил-8-(4-метилпиперазин-1-ил)-1,2,3, 4-тетрагидро-2-нафтил]-4-морфолинобензамида. 4. Форма А моногидробромида (R)-N-[5-метил-8-(4-метилпиперазин-1-ил)-1,2,3,4-тетрагидро-2-нафтил]-4-морфолинобензамида по п.1, дающая картину дифракции рентгеновских лучей на порошке, демонстрирующую по существу следующие d-значения и относительные интенсивности.

3-ЦИАНОХИНОЛИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ EGF-R И HER2 КИНАЗ

... 1. Соединение формулы (I) где Z является -NH-, -O-, -S- или -NR-; R является алкилом, содержащим от 1 до 6 атомов углерода, или карбоалкилом, содержащим от 2 до 7 атомов углерода; Х является циклоалкилом, содержащим от 3 до 7 атомов углерода, который может быть необязательно замещен одним или более алкилом, содержащим от 1 до 6 атомов углерода; или Х является пиридинилом, пиримидинилом или арилом, которые могут быть необязательно моно-, ди- или три-замещены заместителем, выбранным из группы, включающей галоген, алкил, содержащий от 1 до 6 атомов углерода, алкенил, содержащий от 2 до 6 атомов углерода, алкинил, содержащий от 2 до 6 атомов углерода, азидо, гидроксиалкил, содержащий от 1 до 6 атомов углерода, галогенметил, алкоксиметил, содержащий от 2 до 7 атомов углерода, алканоилоксиметил, содержащий от 2 до 7 атомов углерода, алкокси, содержащий от 1 до 6 атомов углерода, алкилтио, содержащий от 1 до 6 атомов углерода (алкилС1-С6)S-, гидрокси, трифторметил, циано, нитро, карбокси, карбоалкокси ...

КОМПОЗИЦИЯ ДЛЯ ТЕРАПИИ РАКА САПОНИНАМИ ИЛИ САПОГЕНИНАМИ

... 1. Состав, содержащий усиливающее активность количество двух или более сапонинов, двух или более сапогенинов или одного или более сапонина в комбинации с одним или более сапогенином и имеющий противораковую активность. 2. Состав по п.1, в котором сапонины и сапогенины выбираются из группы, содержащей Rh2, агликон протапанаксатриол и агликон протопанаксадиол. 3. Состав по п.2, содержащий между приблизительно 1 и 90% каждого из Rh2, агликона протопанаксатриола и агликона протопанаксадиола. 4. Состав по п.3, содержащий между приблизительно 1 и 50% Rh2, между приблизительно 5 и 40% агликона протопанаксатриола и между приблизительно 5 и 75% агликона протопанаксадиола. 5. Состав по п.3, содержащий между приблизительно 5 и 40% Rh2, между приблизительно 4 и 50% агликона протопанаксатриола и между приблизительно 10 и 70% агликона протопанаксадиола. 6. Состав по п.1, в котором один или несколько из упомянутых сапонинов и сапогенинов экстрагируются из растительного материала. 7. Состав по п.6, в котором ...

ПРОИЗВОДНЫЕ ОКСИМА ПИПЕРАЗИНА, ОБЛАДАЮЩИЕ АНТАГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ ПО ОТНОШЕНИЮ К РЕЦЕПТОРУ НК-1

... 1. Соединение общей формулы (1) где Х представляет фенил или пиридил, замещенный 1 или 2 заместителями из группы CH3, CF3, OCH3, галоген, циано и 5-CF3-тетразол-1-ил, Y представляет 2- или 3-индолил, фенил, 7-аза-индол-3-ил или 3-индазолил, 2-нафтил, 3-бензо[b]тиофенил или 2-бензофуранил, которые могут быть замещены одним или более галогенами или алкилами(1-3С), n имеет значение 0-3, m имеет значение 0-2, R1 представляет NH2, NH-алкил(1-3С), диалкил(1-3С)N, морфолино или морфолино, замещенный одной или двумя метильными и/или метоксиметильными группами, тиоморфолино, 1,1-диоксотиоморфолино, 2-, 3- или 4-пиридил или 4-CH3-пиперазинил, R2 является водородом, алкилом(1-4С) или фенилом или R2 вместе с (СН2)m, где m равно 1, и промежуточными атомами углерода, азота и кислорода образует изоксазолильную или 4,5-дигидроизоксазолильную группу, R3 и R4 независимо представляют водород или метил или R3и R4 вместе являются кислородом, и их физиологически приемлемые соли. 2. Соединение по п.1, имеющее ...

Способ лечения воспалительных заболеваний нижних мочевых путей

СПОСОБ Л1:Ч1-ИИЯ ВОСП.,1И ТЕЛЬНЫХ ЗАБО;ПЛЗЛПМП ППЖ1 И. МОЧКВЫХ ПУТПП, включающим шк;::.: .ляции .мочевогч) иузьитя и.ш хретры раствором димексида, от.тчиншщпси . По, с иеЛ1)Ю yiie/iiiMCiiiin 11ср11()да ремиссии .taooлеваиия , ииетил.чяаии проводят рас: nopiiM димексида с добав/нмпкл li него aiiiaioak . средства.

Phenylacetate und Derivate, allein oder in Kombination mit anderen Verbindungen, zur Behandlung von neoplastischen und anderen Erkrankungen

WASSERFREIE SALZE

BUPROPION METABOLITE UND VERFAHREN ZUR DEREN SYNTHESE UND VERWENDUNG

Acridinederivat als therapeutisches Mittel

Neue Carbaminsäureester mit anticholinerger Wirksamkeit

Die vorliegende Erfindung betrifft neue Carbaminsäureester der allgemeinen Formel 1 DOLLAR F1 worin X·-· und die Gruppen A, R·1·, R·2·, R·3· und R·4· die in den Ansprüchen und in der Beschreibung genannten Bedeutungen haben können, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel, insbesondere als Arzneimittel mit anticholinerger Wirksamkeit.

FUROPYRIDIN- UND FUROPYRIMIDINDERIVATE ZUR BEHANDLUNG VON HYPERPROLIFERATIVEN ERKRANKUNGEN

Modafinil-enthaltende pharmazeutische Zusammensetzung

Substituierte 2-Oxy-3,5-dicyano-4-aryl-6-aminopyridine und ihre Verwendung

The use of compounds of formula (I) as medicaments, novel compounds of formula (I) and a method for production thereof are disclosed. Compounds of formula (I) are effective as adenosine receptor ligands.

BEHANDLUNG DES HARNBLASENKREBSES DURCH MYCOBACTERIUM PHLEI ZELLWAND

METHODE ZUR BEHANDLUNG VON ERKRANKUNGEN DER UNTEREN HARNWEGE

TOPISCHE ZUSAMMENSETZUNG UND METHODE ZUR BEHANDLUNG VON HARNINKONTINENZ

VERWENDUNG EINER POLLENEXTRAKT-HÄLTIGEN VERBINDUNG ZUR BEHANDLUNG VON DYSPHORIE

(S,S)-Reboxetin zur Behandlung von Fibromyalgie und anderen somatoformen Störungen

N-Benzensulfonyl-L-Prolin Derivate und deren Verwendung als Bradykinin Antagonisten

Pyrazolo[4,3-d]pyrimidin-Derivate und diese enthaltende pharmazeutische Zubereitungen

KAPPA REZEPTOR OPIOID PEPTIDE

KONDENSIERTE 1,2,4-THIADIAZINDERIVATE, IHRE HERSTELLUNG UND VERWENDUNG

Neuropeptid Y Antagonisten

Medicinal composition for regulating release and process for producing the same

A particle size-controlling substance containing a drug, polyethylene oxide having a molecular weight of 2,000,000 or more and particle size-controlling agent (a substance having appropriate plasticizing properties and binding force) for the polyethylene oxide wherein at least the particle size-controlling agent as specified above is uniformly dispersed in the polyethylene oxide; a medicinal composition for regulating release which contains the particle size-controlling substance; and a process for producing the medicinal composition for regulating release which contains the particle size-controlling substance. By using polyethylene oxide powder/grains in which the specific particle size-controlling agent for polyethylene oxide is uniformly dispersed and which have powder characteristics appropriate for tabletting, a medicinal composition for regulating release showing favorable content uniformity can be provided.

Therapeutic agents

Pharmaceutical formulations for the treatment of an overactive bladder

Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads. The compositions comprising tolterodine find use in the treatment of an overactive bladder, the pilocarpine being used to counter the dry mouth side effect of tolterodine.

Organic compounds

Compositions and methods for preventing or treating incontinence, overactive bladder, or menstrual cramping

Methods and compositions for preventing or treating incontinence, overactive bladder, or menstrual cramping in a subject are described. A method can include providing a composition. The composition can include a modification agent. The modification agent can include a strain of Lactobacillus or a ferment or a metabolite thereof. The modification agent can provide neuromodulation activity by up-regulating at least one of maoA enzymes, maoB enzymes, and grin-1 genes. The method can also include administering the composition to the subject to prevent or treat incontinence, overactive bladder, or menstrual cramping. In some aspects, the modification agent can decrease a level of extracellular ATP in a target environment.

Biaryl ether derivatives useful as monomine reuptake inhibitors

AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS

Stabilized pharmaceutical compositions comprising fesoterodine

1-Trifluoromethyl-4-hydroxy-7- piperidinylaminomethy lchroman derivatives

Therapeutic formulation for administering tolterodine with controlled release

Method of treating of demyelinating diseases or conditions.

Azetidines

Substituted benzolactam compounds

AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS

Method of treating of demyelinating disease or conditions.

Pyrazolopyrimidinones for sexual dysfunction

Pyrazolopyrimidinone cgmp PDE5 inhibitors for the treatment of sexual disfunction

Pyrazolo[4,3-D] pyrimidine derivatives.

Compounds of formula (I) wherein R1. R2, R4 and R13 are as defined or a pharmaceudcally or veterinarfly acceptable salt or polymorph thereof, or a phannaceutically or veterinarfly acceptable solvate or pro-drug thereof: are potent and selective inhibitors of type 5 cyclic guanosine 3*. 5'-monophosphate pbospbodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

Therapeutic formulation for administering tolterodine with controlled release.

A method and formulation for treating unstable or overactive urinary bladder, wherein tolterodine or a tolterodine-related compound, or a pharmaceutically acceptable salt thereof, is administered to a patient in a pharmaceutically effective amount thereof through a controlled release formulation that administers tolterodine or said tolterodine-related compound, or salt thereof, at a controlled rate for at least 24 hours.

1-Trifluoromethyl-4-hydroxy-7- piperidinylaminomethy lchroman derivatives

Pyrazolopyridine cGMP PDE5 inhibitors for the treament of sexual dysfunction.

Compounds of the formulae (IA) and (IB): wherein R1 is Ci to C3 alkyl optionally substituted with phenyl, Het or a N-linked heterocyclic group selected from piperidinyl and morpholinyl; wherein said phenyl group is optionally substituted by one or more substitutents selected from Ci to C4 alkoxy; halo; CN; CF3; OCF3 or Ci to C4 alkyl wherein said Ci to C< alkyl group is optionally substituted by C, to C* haloalkyl or haloalkoxy either of which is substituted by one or more halo atoms; R2 is Ci to C6 alkyl and R1 is OR3 or NR5R5, or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity are potent and selective inhibitors of type 5 cyclic guanosine 3',5'-monophosphate phosphodiesterase (cGMP PDE5) and have utility in the treatment of, inter alia, male erectile dysfunction (MED) and female sexual dysfunction (FSD).

Pyrazolopyrimidinones for sexual dysfunction.

Compounds.of.formulae (lA).and.(IB): R30 or pharmaceutically or veterinariiy acceptable salts thereof, or pharmaceutically or veterinariiy acceptable solvates of either entity, wherein R' is C, to C3 alkyl substituted with C3 to. C6 cycloalkyl, CONR5R5 or a N-linked heterocyclic group; (CK2)nHet or (CH2)Ar; R2 is C, to C6 alkyl; R3 is C, to Cs aikyl optionally substituted with C, to C4 alkoxy; R4 is SO2NR7Ra; R5 and R6 are each independently selected from H and C, to C4 alkyl optionally substituted with C, to C4 alkoxy. or, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic'group; R7 and R8, together with the nitrogen atom to which they are attached,.form a 4-R10-piperazinyi group; R10 is H or C, to C4 alkyl optionally substituted with OH, C, to C4 alkoxy or CONH2; Het is an optionally, substituted C-linked 5- or 6-membered heterocyclic group; Ar is optionally substituted phenyl; and n is 0 or 1; are potent and selective cGMP PDE5 inhibitors ...

1-Trifluoromethyl-4-hydroxy-7-piperidinylaminomethylchroman derivatives.

This invention relates to novel 1-trifluoromethyl-4-hydroxy-7-piperidinyl-aminomethylchroman derivatives of formula (I) wherein R1 is C1-6 alkyl; R2 is hydrogen, C1-C6 alkyl, halo C1-C6 alkyl or phenyl; R3 is hydrogen or halo; and R4 and R5 are independently hydrogen, C1-C6 alkyl or halo C1-C6 alkyl, their pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and the use of such compounds to treat CNS, gastrointestinal and other disorders.

New controlled release bead, a method of producing the same and multiple unit formulation comprising it.

A controlled release bead comprises: (i) a core unit of substantially water-soluble or water-swellable inert material; (ii) a first layer on the core unit of a substantially water-insoluble polymer; (iii) a second layer covering the first layer and containing an active ingredient; and (iv) a third layer of polymer on the second layer effective for controlled release of the active ingredient, wherein the first layer is adapted to control water penetration into the core. A method of producing the controlled release bead is also disclosed.

AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS

AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS

Azetidines.

The invention provides compounds of the general formula:- and acceptable salts thereof which display pharmacological activity as antagonists of tachykinins including neurokinen A (NKA) neurokinin B (NKB) and Substance P for the prevention of inflammatory diseases over a wide spectrum.

Method of treating of demyelinating diseases or conditions.

N-(Pyridinyl)-1H-indol-1 -amines of formula I provide a unique combination of blocking properties for both the potassium and sodium channels. These compounds are useful for the treatment of Demyelinating Diseases and Conditions such as Multiple Sclerosis, Spinal Cord Injury, Traumatic Brain Injury and Stroke. The compounds are also useful for Stroke Rehabilitation, the treatment of Bladder Irritation and Dysfunction, and the treatment of Neuropathic Pain and Chemokine-Induced Pain.

Carbamates derived from arylalkylamines

Pyrazolopyrimidinones for sexual dysfunction

New controlled release bead a method of producing the same and multiple unit formulation comprising it

Novel 1,4-dihydropyridine compounds as bradykinin antagonists.

The present invention relates to compounds of the formula wherein each a is independently halo;y is -(ch2)m-,-c(o)-or-s(o)-;r1 and r2 are independently c1-4 alkyl is substituted azacycloalkyl etc.; r4 is phenyl substituted at the 2 position with a substituent selected from substituted c 1-7 alkyl, substituted c1-7 alkoxy, amine, etc; r5 is hydrogen or c1-4 alkyl; m is 0, 1 or 2; and n is 0,1,2,3,4,or 5. The present invention also relates to phamaceutical compositions containing such compounds and to the use of such compounds in the treatment and prevention of inflammation, asthma, allergic rhinitis, pain and other disorders.

Carbamates derived from arylalkylamines.

The invention relates to carbamates having general structure (I), wherein: Rl, R2 and R3 are H, OH, SH, CN, F, CI, Br, I, (C1-C4-alkylthio, (C1-C4)-alkoxyl, (C1-C4)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C1 -C4)-alkyl and (CrC4)-alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quaternary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3 muscarinic receptor, and selectively, the M2 receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.

Azetidines

Therapeutic formulation for administering tolterodine with controlled release

NOVEL PIPERAZINE

A compound of formula (1)or the pharmaceutically acceptable salt thereof; wherein a,b,c,d,e,j,R1,R2,R3, and R4, are as defined above useful to treat inflammation and other immune disorders.

Substituted benzolactam compounds.

This invention relates to compounds of general formula (i); or pharmaceutically acceptable salt threof, w, t, y, x, q, r1, r2, and r3 are adefined herein. This invention also relates to compounds of formula (i), depicted above, wherein y is -nh-; t is(2s,3s)-2-phenylpiperridin-3-yl where the phenyl group of said (2s, 3s)-2-phenylpiperridine-3-yl may optionally be substituted with fluro; q is oxygen and is double bonded to the carbon atom to which it is attached, x is methoxy or ethoxy, r1 is hydrogen, methyl or halo-c1-c2 alkyl, w is methylene, ethylene or vinylene; r2 and r3 are independently hydrogen or methyl, or one fo r2 or r3 may be hydroxy, when w is ethylene, r2 and r3 are both methyl, when w is methylene, and r2 and r3 are both hydrogen, when vinylene. The invention is further directed to methods of treating vasrious cns and other disorders using said compounds and pharmaceutical compositions.

Fused bicyclic or tricyclic amino acids.

The compounds of the instant invention are bicyclic or tricyclic amino acids useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders,neurodegerative disorders, depression, anxiety, panic, pain,arthritis, neuropathological disoders, sleep disorders,visceral pain disoders, and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one more of the compounds are also included.

Pyrazolopyrimidinone cgmp PDE5 inhibitors for the treatment of sexual disfunction

Biaryl ether derivatives useful as monoamine reuptake inhibitors.

The present invention relates to compounds of formula (I) and to their pharmaceutically acceptable salts. Compounds of formula (I) exhibit activity as serotonin, norepinephrine, and dopanine reuptake inhibitors and can be used in the treatment of central nervous system and other disorders.

Benzoamide piperidine compounds as substance p antagonists

The present invention relates to certain benzoamide piperidine containing compounds of formula 1and related compounds that exhibit activity as NK-1 receptor antagonists, (eg., substance P receptor antagonists), to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system disorders, inflamatory disorders, cardiovascular disorders, ophthalmic disorders, gastrointestinal disorders, disorders caused by helicobacter pylori, disorders of the immune system, urinary incontinence, pain, migraine, emesis, angiogenesis and other disorders.

AZETIDINYLOXYPHENYLPYRROLIDINE COMPOUNDS

Antibodies to CD40.

Composition and Methods for the Diagnosis and Treatment of Tumor

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

Use of jasmonate to treat bladder dysfunction

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

Fused compounds that inhibit vanilloid receptor subtype 1 (vr1) receptor

The present invention discloses novel compounds of general formula (I) or a pharmaceutically acceptable salt or prodrug thereof (in which X 1 -X 5 , R 5 -R 8b , Z 1 -Z 2 and Ar 1 are defined herein), a method for inhibiting the VR1 receptor in mammals using these compounds, a method for controlling pain in mammals, and pharmaceutical compositions including those compounds and a process for making those compounds.

Composition comprising fesoterodine and fiber

The invention relates to a pharmaceutical composition containing (a) fesoterodine and/or fesoterodine metabolites and (b) fibers, wherein the weight ratio of components (a):(b) is in the range from 1:50 to 1:2; and oral dosage forms containing the pharmaceutical composition. The invention further relates to dry methods of preparing those dosage forms.

Combinations of trospium and salivary stimulants for the treatment of overactive bladder

Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of immediate release trospium, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.

Combinations of darifenacin and salivary stimulants for the treatment of overactive bladder

Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release darifenacin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.

Combinations of oxybutynin and salivary stimulants for the treatment of overactive bladder

Disclosed herein are pharmaceutical compositions comprising a therapeutically effective amount of extended release oxybutynin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of treating a patient suffering from overactive bladder, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release oxybutynin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods of alleviating a side effect of treatment for overactive bladder in a patient suffering therefrom, the method comprising identifying a patient in need thereof, and administering to the patient a therapeutically effective amount of extended release oxybutynin, or a pharmaceutically acceptable salt thereof, and a therapeutically effective amount of pilocarpine, or a pharmaceutically acceptable salt thereof.

Cyclohexylamines

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

Botulinum toxin compositions and methods

Disclosed herein are methods of using extracellular matrix digesting enzymes and neurotoxins, such as a Clostridial neurotoxins, to treat various medical conditions, such as overactive bladder, benign prostatic hyperplasia, hyperhidrosis, for example.

Short synthesis of tolterodine, intermediates and metabolites

A process is described for the preparation of intermediates which can be used for preparation of agents for urinary incontinence therapy, specifically to 2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenol and its prodrugs.

Quinoxaline compound

The present inventors have investigated a compound which has a PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibitory action, thereby completing the present invention.

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

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

Process for the preparation of 1 - (2-methyl-4- (2,3,4,5-tetrahydro-1-benzazepin-1-ylcarbonyl) benzylcarbamoyl) - l - proline - n, n-dimethylamide

The present invention relates to a new process for the preparation of a crystalline polymorph of a vasopressin V 2 agonist.

AN AGENT FOR TREATING NOCTURNAL POLLAKIURIA

[Problem] To provide a novel therapeutic agent for nocturnal pollakiuria. 14-. (canceled)5. A method for treating nocturnal pollakiuria , comprising administering to a subject in need thereof (6S)—N-[4-({(2S ,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4 ,6 ,7 ,8-tetrahydropyrrolo[1 ,2-a]pyrimidine-6-carboxamide in an effective amount to treat nocturnal pollakiuria.6. The method according to claim 5 , wherein the effective amount of the (6S)—N-[4-({(2S claim 5 ,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4 claim 5 ,6 claim 5 ,7 claim 5 ,8-tetrahydropyrrolo[1 claim 5 ,2-a]pyrimidine-6-carboxamide is administered to a subject belonging to a group of patients whose average value of the frequency of urination at night is 1.0 or more and 1.8 or less.7. The method according to claim 5 , wherein the effective amount of the (6S)—N-[4-({(2S claim 5 ,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4 claim 5 ,6 claim 5 ,7 claim 5 ,8-tetrahydropyrrolo[1 claim 5 ,2-a]pyrimidine-6-carboxamide is administered orally once daily at a daily dosage of 50 mg or more and 100 mg or less.8. The method according to claim 6 , wherein the effective amount of the (6S)—N-[4-({(2S claim 6 ,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4 claim 6 ,6 claim 6 ,7 claim 6 ,8-tetrahydropyrrolo[1 claim 6 ,2-a]pyrimidine-6-carboxamide is administered orally once daily at a daily dosage of 50 mg or more and 100 mg or less. The present invention relates to an agent for treating nocturnal pollakiuria.Nocturnal pollakiuria is a complaint that one has to wake up one or more times for urinating at night, and is one of the symptoms (urinary urgency, pollakiuria, nocturnal pollakiuria, and urge urinary incontinence) resulting from overactive bladder (OAB). Nocturnal pollakiuria causes nocturnal awakening and is closely associated with sleep disorders, thereby reducing QOL remarkably (Non Patent Literature 1). ...

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

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

Human-enzyme mediated depletion of cystine for treating patients with cystinuria

Methods and compositions related to the engineering of a protein with L-cyst(e)ine degrading enzyme activity are described. For example, in certain aspects there may be disclosed a modified cystathionine-γ-lyase comprising one or more amino acid substitutions and capable of degrading L-cyst(e)ine. Furthermore, certain aspects of the invention provide compositions and methods for the treatment of cancer with L-cyst(e)ine using the disclosed proteins or nucleic acids.

Methods comprising desmopressin

The present disclosure is directed to reducing nocturnal voids by administering a dose of desmopressin over a minimum treatment period compared to before administration, and maintaining or improving the reduction of nocturnal voids over the minimum treatment period.

HYALURONAN COMPOSITIONS, AND USES THEREOF IN TREATMENT OF INTERSTITIAL CYSTITIS

A hydrogel composition for treatment of interstitial cystitis is described and comprises crosslinked hyaluronan particles dispersed throughout a crosslinked hyaluronan hydrogel matrix, wherein the hyaluronan is high molecular weight hyaluronan. The composition is formulated for direct bladder instillation in a human. The hyaluronan particles are nano-sized hyaluronan particles, or agglomerates of nano-sized hyaluronan particles, or a mixture thereof. 1. (canceled)2. A method of treating interstitial cystitis in a mammal , comprising administering a hydrogel composition to the mammal by direct bladder instillation , in which the hydrogel composition comprises crosslinked high molecular weight hyaluronan particles dispersed and suspended throughout a hydrogel matrix , in which the hydrogel composition is formulated for direct bladder instillation in a mammal.3. The method of claim 2 , wherein the hydrogel composition provides a barrier effect to facilitate the restoration/regeneration of the urothelium layer of the bladder.4. The method of claim 2 , wherein the hydrogel composition suppresses inflammatory cytokine production.5. The method of claim 2 , wherein the hydrogel composition decreases the permeability of the bladder wall.6. The method of claim 2 , in which the hydrogel matrix is hyaluronan.7. The method of claim 2 , wherein the hydrogel matrix is crosslinked high molecular weight hyaluronan.8. The method of claim 2 , wherein the high molecular weight hyaluronan particles are nano-sized particles claim 2 , or agglomerates of nano-sized HA particles claim 2 , or a combination thereof.9. The method of claim 2 , wherein a weight ratio of high molecular weight hyaluronan particles to hydrogel matrix is about 1:10 to 10:1 or about 1: to 2:1.10. The method of claim 2 , wherein the high molecular weight hyaluronan is chemically crosslinked with a crosslinking moiety and in which the crosslinking moiety is an optionally functionalised ethylene glycol.11. The method of ...

USE OF STEM CELL EXOSOMES FOR TREATING OVERACTIVE BLADDER

The disclosure relates to use of stem cell exosomes in preparing a medicament for treating overactive bladder. It has been confirmed that stem cell exosomes are effective in the treatment of overactive bladder and can be used in preparing a medicament for treating overactive bladder. 1. A method for treating overactive bladder in a subject , comprising administrating stem cell exosomes to the subject in need thereof.2. The method according to claim 1 , wherein the stem cell exosomes are at least one selected from embryonic stem cell exosomes claim 1 , mesenchymal stem cell exosomes claim 1 , and induced pluripotent stem cell exosomes.3. A medicament for treating overactive bladder claim 1 , comprising an active ingredient and a pharmaceutically acceptable auxiliary claim 1 , the active ingredients comprising stem cell exosomes.4. The medicament according to claim 3 , wherein the stem cell exosomes are at least one selected from embryonic stem cell exosomes claim 3 , mesenchymal stem cell exosomes claim 3 , and induced pluripotent stem cell exosomes.5. The medicament according to claim 3 , wherein the stem cell exosomes are humanized stem cell exosomes or murine stem cell exosomes.6. The medicament according to claim 3 , wherein the medicament is in a dosage form of tablets claim 3 , capsules claim 3 , granules claim 3 , pills claim 3 , injections claim 3 , or sustained-release preparations.7. The medicament according to claim 6 , wherein the medicament is tablets claim 6 , and the pharmaceutically acceptable auxiliary is at least one selected from the group consisting of a diluent claim 6 , a binder claim 6 , a wetting agent claim 6 , a disintegrant claim 6 , and a lubricant.8. The medicament according to claim 7 , wherein the diluent is at least one selected from the group consisting of starch claim 7 , dextrin claim 7 , sucrose claim 7 , glucose claim 7 , lactose claim 7 , mannitol claim 7 , sorbitol claim 7 , xylitol claim 7 , microcrystalline cellulose claim 7 , ...

Collagenase Clostridium Histolyticum Injection Therapies

Collagenase (EN3835) is a proteinase that can hydrolyze the triple-helical region of collagen under physiological conditions. EN3835 targets the collagenase structural matrix at the site of injection and does not require systemic exposure. Embodiments include methods of lysing subdermal and submucosal collagen to treat various conditions such as bladder dysfunction, esophageal stenosis, benign prostatic hyperplasia, tracheal stenosis, subglottic stenosis and scleroderma. 1Clostridium histolyticum. A method of treating a patient with bladder dysfunction comprising injection of an effective amount of collagenase from at or near the bladder an/or the detrusor muscle of the bladder.2. The method of claim 1 , wherein the bladder dysfunction causes one or more of urinary incontinence and urinary retention.3. The method of claim 1 , wherein the injection comprises multiple injections at a plurality of sites at or near the bladder and/or the detrusor muscle of the bladder.4. The method of claim 3 , wherein each of the multiple injections is comprised of a volume of about 0.2 ml or less.5. The method of claim 1 , wherein a total of 0.01 mg to 0.5 mg of collagenase in solution is injected.6. The method of claim 1 , wherein a total of 0.02 mg to 0.05 mg of collagenase in solution is injected.7. The method of claim 1 , including an additional step of endoscopic dilation.8. The method of claim 1 , wherein the collagenase is comprised of equal amounts of Clostridial class I collagenase (AUX-I) and Clostridial class II collagenase (AUX-II).9. The method of claim 1 , wherein the collagenase is injected using a syringe with a rack and pinion component.10. A method of treating bladder dysfunction in a patient comprising steps of:a) identifying a patient with signs and/or symptoms of bladder dysfunction,{'i': 'Clostridium histolyticum', '#text': 'b) injecting an effective amount of collagenase from at a first plurality of sites at or near the bladder and/or the detrusor muscle of the ...

Therapeutic and diagnostic methods for cancer

The present invention provides therapeutic and diagnostic methods and compositions for cancer, for example, bladder cancer. The invention provides methods of treating bladder cancer, methods of determining whether a patient suffering from bladder cancer is likely to respond to treatment comprising a PD-L1 axis binding antagonist, methods of predicting responsiveness of a patient suffering from bladder cancer to treatment comprising a PD-L1 axis binding antagonist, and methods of selecting a therapy for a patient suffering from bladder cancer, based on expression levels of a biomarker of the invention (e.g., PD-L1 expression levels in tumor-infiltrating immune cells in a tumor sample obtained from the patient) and/or based on the determination of a tumor sample subtype.

METHODS FOR TREATING BLADDER AND URETHRA DYSFUNCTION AND DISEASE

Methods of treating bladder or urethra dysfunction or disease in a subject and methods of increasing bladder smooth muscle contractility or increasing bladder wall volume in a subject are disclosed. In some examples, a purine nucleoside phosphorylase (PNPase) inhibitor or purine nucleoside substrate is administered, such as 8-aminoguanine or forodesine. 1. A method of treating bladder or urethra dysfunction or disease in a subject , comprising:selecting a subject with bladder or urethra dysfunction or disease; andadministering to the subject a therapeutically effective amount of a purine nucleoside phosphorylase (PNPase) inhibitor or a PNPase purine nucleoside substrate, thereby treating the bladder or urethra dysfunction or disease.2. The method of claim 1 , wherein the PNPase inhibitor is a guanine comprising a substituent at the 8-position claim 1 , a guanosine comprising a substituent at the 8-position claim 1 , an inosine comprising a substituent at the 8-position claim 1 , a hypoxanthine comprising a substituent at the 8-position claim 1 , a PNPase transition state analog claim 1 , or a pharmaceutically acceptable salt thereof.3. The method of claim 2 , wherein the substituent is amine claim 2 , hydroxyl claim 2 , nitro claim 2 , nitroso claim 2 , alkoxy claim 2 , carbonyl claim 2 , halogen claim 2 , carboxyl claim 2 , ester claim 2 , carbonate claim 2 , amide claim 2 , or haloaliphatic.4. The method of claim 2 , wherein the substituent is amine.5. The method of claim 2 , wherein the guanine comprising a substituent at the 8-position is 8-aminoguanine.6. The method of claim 2 , wherein the PNPase transition state analog is:7-[(2S,3S,4R,5R)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-3H,4H,5H-pyrrolo[3,2-d]pyrimidin-4-one;7-(((3R,4R)-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-yl)methyl)-3H-pyrrolo[3,2-d]pyrimidin-4(5H)-one;7-(((2R,3S)-1,3,4-trihydroxybutan-2-ylamino)methyl)-3H-pyrrolo[3,2-d]pyrimidin-4(5H)-one;7-((1,3-dihydroxypropan-2-ylamino)methyl)-3H- ...

Prophylactic agent and/or therapeutic agent for stress urinary incontinence

An object to be solved by the present invention is to provide a superior prophylactic agent and/or therapeutic agent for stress urinary incontinence. The present invention provides a prophylactic agent and/or a therapeutic agent for stress urinary incontinence comprising an effective amount of 4-piperidyl diphenylpropoxyacetate or a salt thereof, and a pharmaceutical carrier.

Process and intermediates for the production of 17(20)-ene b-seco steroids

The invention pertains to a process for producing a compound of formula (11) wherein R7 and R8 are each independently selected from H, halogen, alkyl, aryl, or alkylaryl, R42 is H or a protective group, R43 is H or R3, wherein R3 is a protective group, by contacting a compound of formula (10) with an olefmation reagent, wherein compound of formula (10) comprises a counter acid X1 when R42═H and R43═H.

Combination of tasquinimod or a pharmaceutically acceptable salt thereof and a pd-1 and/or pd-l1 inhibitor, for use as a medicament

The present invention concerns a combination comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and a PD-1 and/or PD-L1 inhibitor, for use as a medicament. It also concerns a pharmaceutical composition comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and PD-1 and/or PD-L1 inhibitor.

Composition for preventing, treating and improving of voiding dysfunction comprising extract from Piper longum L.

The present invention relates to a pharmaceutical composition for preventing or treating voiding dysfunction and a health functional food for preventing or improving of voiding dysfunction, comprising extract of Piper Longum L. as an active ingredient. The extract of Piper Longum L. according to the present invention is not only harmless, but also has outstanding effects of preventing, treating and improving voiding dysfunction by being involved in various mechanisms related to voiding dysfunction simultaneously so that it may increase a micturition interval, decrease a micturition pressure, increase a bladder capacity, inhibit detrusor contraction and induce relaxation of detrusor.

METHODS OF TREATING OVERACTIVE BLADDER USING TROSPIUM

The present application provides methods of treating overactive bladder and methods of training or retraining bladder, prolonging symptom relief, improving the quality of life and/or neuronal remodeling in an individual having overactive bladder, by administering an effective amount of trospium locally to the bladder of the individual for at least about 24 hours. 1. A method of training the bladder of an individual having overactive bladder comprising administering an effective amount of trospium locally to the bladder of the individual for at least about 24 hours.2. A method of prolonging symptom relief for an individual having overactive bladder comprising administering an effective amount of trospium locally to the bladder for at least about 24 hours , wherein the individual experiences relief of a symptom for at least about 24 hours after trospium administration is completed.3. A method of improving the quality of life of an individual having overactive bladder comprising administering an effective amount of trospium locally to the bladder for at least about 24 hours , wherein the quality of life of the individual is improved upon treatment with trospium.4. The method of claim 2 , wherein the individual having overactive bladder experiences at least about 50% of baseline symptom relief for at least about 7 days after trospium administration is completed.5. The method of wherein trospium is continuously administered locally to the bladder for at least about 42 days.6. The method of wherein the method further comprises administering an effective amount of trospium locally to the bladder every 3 months or on an as needed (prn) basis.7. A method of treating overactive bladder comprising continuously administering an effective amount of trospium locally to the bladder of the individual for at least about 42 days.8. The method of claim 7 , wherein trospium is continuously administered for about 84 days.9. The method of claim 6 , wherein trospium is continuously ...

COMPOSITION FOR BKCA CHANNEL ACTIVATION

The present invention relates to novel compounds capable of activating BKCa channels. The use of a composition of the present invention can effectively activate the BKCa channels, and can be used for prevention or treatment of various diseases caused by the deactivation of BKCa channels or the degradation of BKCa channel activity. 2. The method of claim 1 , wherein when Ris C-Calkyl or alkenyl claim 1 , Ris methoxy.3. The method of claim 1 , wherein Ris hydrogen claim 1 , 3-methyl-2-buten-1-yl claim 1 , or 2-isopropenyl-5-methyl-4-hexen-1-yl.4. The method of claim 3 , wherein when Ris hydrogen claim 3 , Ris hydroxy.5. The method of claim 3 , wherein when Ris 3-methyl-2-butene-1-yl claim 3 , Ris hydroxy.6. The method of claim 3 , wherein when Ris 2-isopropenyl-5-methyl-4-hexen-1-yl claim 3 , Ris methoxy.7. The method of claim 1 , wherein Ris hydroxy claim 1 , and claim 1 , each of Rand Ris independently hydrogen or hydroxy.8. The method of claim 7 , wherein at least one of Rand Ris hydrogen.9. The method of claim 1 , wherein the flavanone derivative represented by the chemical formula 1 is a compound selected from a group consisting of kurarinone claim 1 , naringenin and leachianone G.10. The method of claim 1 , wherein the composition shifts a conductance-voltage (G-V) correlation of the BKchannel toward a negative voltage. This application is a Continuation Application of U.S. patent application Ser. No. 16/082,257 filed Sep. 4, 2018, which is a national stage filing under 35 U.S.C § 371 of PCT application number PCT/KR2017/002291 filed on Mar. 2, 2017 which is based upon and claims the benefit of priority to Korean Patent Application No. 10-2016-0025327 filed on Mar. 2, 2016 in the Korean Intellectual Property Office. The disclosures of the above-listed applications are hereby incorporated by reference herein in their entirety.The present disclosure relates to novel compounds to activate a BKchannel.Ca-activated K+ channel (BKchannel) with great electrical ...

HYALURONAN COMPOSITIONS, AND USES THEREOF IN TREATMENT OF INTERSTITIAL CYSTITIS

A hydrogel composition for treatment of interstitial cystitis is described and comprises crosslinked hyaluronan particles dispersed throughout a crosslinked hyaluronan hydrogel matrix, wherein the hyaluronan is high molecular weight hyaluronan. The composition is formulated for direct bladder instillation in a human. The hyaluronan particles are nano-sized hyaluronan particles, or agglomerates of nano-sized hyaluronan particles, or a mixture thereof. 1. A hydrogel composition for use in a method of treating interstitial cystitis in a mammal , in which the composition comprises crosslinked high molecular weight hyaluronan particles dispersed and suspended throughout a hydrogel matrix , and in which the hydrogel composition is formulated for direct bladder instillation in a human.2. A hydrogel composition of claim 1 , in which the hydrogel composition is administered to the human by direct bladder instillation.3. A hydrogel composition of claim 1 , where the hydrogel composition provides a barrier effect to facilitate the restoration/regeneration of the urothelium layer of the bladder.4. A hydrogel composition of claim 1 , where the hydrogel composition suppresses inflammatory cytokine production.5. A hydrogel composition of claim 1 , in which where the hydrogel composition decreases the permeability of the bladder wall.6. A hydrogel composition of claim 1 , in which the hydrogel matrix is hyaluronan.7. A hydrogel composition of claim 4 , in which the hydrogel matrix is crosslinked high molecular weight hyaluronan.8. A hydrogel composition according to claim 1 , in which the HA particles are nano-sized particles claim 1 , or agglomerates of nano-sized HA particles claim 1 , or a combination thereof.9. A hydrogel composition according to claim 1 , in which a weight ratio of HA particles to hydrogel matrix is about 1:10 to 10:1.10. A hydrogel composition according to claim 1 , in which a weight ratio of HA particles to hydrogel matrix is about 1:2 to 2:1.11. A hydrogel ...

USE OF VIBEGRON TO TREAT OVERACTIVE BLADDER

The present disclosure is directed to a method of treating overactive bladder comprising orally administering to a subject in need thereof an amount of from about 60 mg to about 90 mg (e.g., about 75 mg) of vibegron per day. The present disclosure is also directed to a pharmaceutical unit dosage composition comprising from about 60 mg to about 90 mg (e.g., about 75 mg) of vibegron for oral administration. 1. A method of treating overactive bladder , the method comprising orally administering to a subject in need thereof an amount of from about 60 mg to about 90 mg of vibegron per day.2. The method of claim 1 , wherein the amount of vibegron is about 65 mg to about 85 mg.3. The method of claim 1 , wherein the amount of vibegron is about 70 mg to about 80 mg.4. The method of claim 1 , wherein the amount of vibegron is about 75 mg.5. The method of any one of to claim 1 , wherein the subject has a symptom selected from the group consisting of urgency urinary incontinence claim 1 , urinary urgency claim 1 , urinary frequency claim 1 , or a combination thereof.6. The method of claim 5 , wherein the subject has the symptoms urgency urinary incontinence claim 5 , urinary urgency claim 5 , and urinary frequency.7. The method of any one of to claim 5 , wherein the subject is a human.8. The method of claim 7 , wherein the human is a female.9. The method of claim 7 , wherein the human is a male.10. The method of any one of to claim 7 , wherein the human is over the age of 65 years.11. The method of any one of to claim 7 , wherein the subject suffers from severe renal impairment.12. The method of any one of to claim 7 , wherein the subject suffers from moderate renal impairment.13. The method of any one of to claim 7 , wherein the subject is concomitantly receiving a CYP3A/P-glycoprotein inhibitor.14. The method of any one of to claim 7 , wherein vibegron is administered once per day.15. The method of claim 14 , wherein vibegron is administered with a meal.16. The method of ...

DOSING OF VIBEGRON FOR TREATMENT OF OVERACTIVE BLADDER

The present disclosure is directed to a method of treating overactive bladder comprising orally administering to a subject in need thereof an amount of from about 50 mg to about 100 mg (e.g., about 75 mg) of vibegron per day. The present disclosure also provides a method of treating overactive bladder comprising orally administering to a subject in need thereof a first dosage of vibegron per day for a first period and a second dosage of vibegron per day thereafter. 1. A method of treating overactive bladder , the method comprising orally administering to a subject in need thereof a first dosage of vibegron per day for a first period and a second dosage of vibegron per day thereafter , wherein the second dosage is greater than the first dosage.2. The method of claim 1 , wherein the first dosage is from about 50 mg to about 75 mg per day.3. The method of claim 2 , wherein the first dosage is about 50 mg per day.4. The method of claim 2 , wherein the first dosage is about 75 mg per day.5. The method of any one of to claim 2 , wherein the second dosage is from about 75 mg to about 100 mg per day.6. The method of claim 5 , wherein the second dosage is about 75 mg per day.7. The method of claim 5 , wherein the second dosage is about 100 mg per day.8. The method of claim 1 , wherein the first dosage is about 50 mg per day and the second dosage is about 75 mg per day.9. The method of claim 1 , wherein the first dosage is about 50 mg per day and the second dosage is about 100 mg per day.10. The method of claim 1 , wherein the first dosage is about 75 mg per day and the second dosage is about 100 mg per day.11. The method of any one of to claim 1 , wherein the first period is from about one week to about 12 weeks.12. The method of claim 11 , wherein the first period is from about two weeks to about eight weeks.13. The method of any one of to claim 11 , wherein the subject has a symptom selected from the group consisting of urgency urinary incontinence claim 11 , urinary ...

Viral vectors for treating neurogenic detrusor overactivity

The present invention provides a method and a pharmaceutical composition for the treatment of the NDO comprising the viral expression vector carrying a transcription cassette that harbors transgene(s) inhibiting/silencing neurotransmission or synaptic transmission of afferent neurons.

METHOD

The invention provides a method of diagnosing overactive bladder disorder (OAB), the method comprising: measuring the concentrations of one or more of adenosine triphosphate (ATP), acetylcholine (ACh), nitric oxide (NO) and interleukin 5 (IL-5) in a sample obtained from a subject; normalising the concentrations to the concentration of creatinine (Cr) in the sample; range standardising the normalised concentrations and subject's age to the following values: Age to 120 years old; ATP/Cr to 0.000001; ACh/Cr to 0.1; NO to 20000; IL-5/Cr to 100; wherein the likelihood of having OAB (p)=1/1+e, where X=one or more of the following: (a) (−2.688±1.050)+5.472±2.098×subject's age+1.356±0.559×Gender (Female=1, Male=0)+(−7.998±40.273)×[IL-5/Cr]; (b) (−2.141±0.966)+4.506±1.902×subject's age+1.034±0.519×Gender (Female=1, Male=0)+(−5294.063±9075.456)×[ACh/Cr]; (c) (−2.825±1.072)+5.964±2.167×subject's age+1.312±0.562×Gender (Female=1, Male=0)+17.790±58.762×[IL-5/Cr]+(−9180.821±12700.057)×[ACh/Cr]; (d) (−2.993±1.197)+5.580±2.309×subject's age+1.724±0.719×Gender (Female=1, Male=0)+63.571±73.444×[IL-5/Cr]+(−0908.523±13606.752)×[ACh/Cr]+(−566.991±636.589)×[ATP/Cr]; (e) (−3.090±1.200)+5.393±2.256×subject's age+1.797±0.717×Gender (Female=1, Male=0)+34.767±56.331×[IL-5/Cr]+(−562.743±629.316)×[ATP/Cr]; or (f) (−2.650±1.067)+5.516±2.120×subject's age+1.389±0.583×Gender (Female=1, Male=0)+(−4.060±45.238)×[IL-5/Cr]+(−1.456±6.833)×[NO/Cr]; and wherein a pOAB above a threshold indicates that the subject has a high likelihood of having or developing OAB and a pOAB below a threshold indicates that the subject does not have OAB. 1. A method of diagnosing overactive bladder disorder (OAB) , the method comprising:measuring the concentrations of one or more of adenosine triphosphate (ATP), acetylcholine (ACh), nitric oxide (NO) and interleukin 5 (IL-5) in a sample obtained from a subject;normalising the concentrations to the concentration of creatinine (Cr) in the sample;range standardising the ...

COMPOSITION FOR BKCA CHANNEL ACTIVATION

The present invention relates to novel compounds capable of activating BKCa channels. The use of a composition of the present invention can effectively activate the BKCa channels, and can be used for prevention or treatment of various diseases caused by the deactivation of BKCa channels or the degradation of BKCa channel activity. 2. The composition of claim 1 , wherein when Ris C-Calkyl or alkenyl claim 1 , Ris methoxy.3. The composition of claim 1 , wherein Ris hydrogen claim 1 , 3-methyl-2-buten-1-yl claim 1 , or 2-isopropenyl-5-methyl-4-hexen-1-yl.4. The composition of claim 3 , wherein when Ris hydrogen claim 3 , Ris hydroxy.5. The composition of claim 3 , wherein when Ris 3-methyl-2-butene-1-yl claim 3 , Ris hydroxy.6. The composition of claim 3 , wherein when Ris 2-isopropenyl-5-methyl-4-hexen -1-yl claim 3 , Ris methoxy.7. The composition of claim 1 , wherein Ris hydroxy claim 1 , and claim 1 , each of Rand Ris independently hydrogen or hydroxy.8. The composition of claim 7 , wherein at least one of Rand Ris hydrogen.9. The composition of claim 1 , wherein the flavanone derivative represented by the chemical formula 1 is a compound selected from a group consisting of kurarinone claim 1 , naringenin and leachianone G.10. The composition of claim 1 , wherein the composition shifts a conductance-voltage (G-V) correlation of the BKchannel toward a negative voltage.11. A composition for preventing or treating BKchannel activity degradation-related condition claim 1 , disease or disorder claim 1 , wherein the composition includes the composition for BKchannel activation of .12. The composition of claim 11 , wherein the BKchannel activity degradation-related condition claim 11 , disease or disorder is cardiovascular disease claim 11 , obstructive or inflammatory airways disease claim 11 , lower urinary tract disorder claim 11 , impotence claim 11 , anxiety and anxiety-related condition claim 11 , epilepsy or pain. This present application is a national stage filing ...

Photodynamic therapy, formulation usable for this purpose, and method for the production and use thereof

A treatment of cancer, such as, for example, bladder cancer, uses a formulation that contains sodium hypericinate that is bonded to polyvinylpyrrolidone or complexed with polyvinylpyrrolidone.

Modified Pyrazine Derivatives and Uses Thereof

In some embodiments, the invention provides modified pyrazine derivatives containing a central pyrazine ring with two secondary amine groups attached directly to the central pyrazine ring and two amino carbonyl groups attached directly to the central pyrazine ring. The secondary amine groups are terminated by alkyl groups containing from 1 to 6 carbons. The amino carbonyl groups can be terminated by a wide range of substituents including, but not limited to, alkyl and alkylene groups, polyether groups, including poly(ethylene glycol) groups, secondary and tertiary amine groups, polyhydroxylated alkyl groups, amino carbonyl groups, amino thioketone groups, and combinations thereof. In some embodiments, the invention provides modified pyrazine derivatives useful as optical agents in a wide variety of biomedical imaging procedures, including diagnostic and imaging procedures. In an embodiment, for example, modified pyrazine derivatives are provided which are useful in monitoring organ and system functioning, for example in monitoring renal system functioning.

METHOD FOR BIOMIMETIC CULTURE OF UROTHELIAL CELLS AND USES THEREOF

The invention discloses a methodology for the biomimetic culture of urothelial cells from mammalian bladders, including murine, porcine, bovine and human sources to isolate and expand urothelial cells for use in various applications, such as intravesical urothelial cell therapy to treat cystitis and bladder cancer. 1. A method for culturing urothelial cells from a mammalian source , comprising: obtaining a sample of bladder tissue from a mammalian source; (a) dissociating urothelium from mucosa layer of the sample of bladder tissue; (b) isolating dissociated urothelial cells from the sample of bladder tissue; (c) planting the dissociated urothelial cells on a biomimetic culture system; and (d) culturing the dissociated urothelial cells in a biomimetic environment and in a culture medium , wherein the dissociated urothelial cells comprises urothelial stem cells , urothelial progenitor cells or precursor cells thereof.2. The method of claim 1 , wherein the mammalian source is selected from human claim 1 , porcine claim 1 , bovine claim 1 , or equine sources.3. The method of claim 1 , wherein the biomimetic culture system comprises a basement membrane-like support for an adherent cell culture support.4. The method of claim 1 , wherein the culture medium is selected from the group consisting of FBS claim 1 , cell matrix claim 1 , growth factors claim 1 , and signaling pathway modulators.5. The method of claim 1 , wherein the culture medium comprises bFGF claim 1 , and/or antibiotic-antimycotic.6. The method of claim 1 , wherein the culture medium comprises serum claim 1 , ROCK inhibitor claim 1 , BMP inhibitor claim 1 , and/or WNT activator.7. The method of claim 1 , wherein the culture medium comprises extracellular matrix molecules and polysaccharides.8. The method of claim 1 , which further comprises contacting the dissociated urothelial cells with an effective amount of growth factors claim 1 , extracellular matrix molecules polysaccharides and signaling pathway ...

1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES

The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients. 3. A compound according to claim 1 , wherein{'sup': '1', 'Rrepresents methyl or ethyl.'}4. A compound according to claim 1 , wherein{'sup': '3', 'sub': 1', '4, 'Rrepresents C-C-alkyl.'}5. A compound according to claim 1 , wherein{'sup': '3', 'Rrepresents methyl.'}6. A compound according to claim 1 , whereinA represents optionally substituted pyrimidinyl, pyridazinyl, pyridinyl, or pyrazinyl.7. A compound according to claim 6 , wherein A represents optionally substituted pyrimidinyl or pyridazinyl.8. A compound according to claim 7 , wherein{'sub': 3', '3, 'A represents CF-pyrimidinyl or 2-CF-pyrimidin-5-yl.'}9. A compound according to claim 1 , wherein Rrepresents cyclopropylmethyl claim 1 , tetra hydrofuran-2-ylmethyl claim 1 , tetrahydrofuran-3-ylmethyl claim 1 , tetrahydro-2H-pyran-4-ylmethyl claim 1 , which are optionally substituted.10. A compound according to claim 9 , wherein Rrepresents unsubstituted cyclopropylmethyl.11. A compound according to claim 1 , wherein{'sup': '2', 'sub': 2', 'q', '2', 'q', 'c', '2', 'q', '2', 'q, 'Rrepresents —(CH)-(4- to 6-membered heterocycloalkyl), optionally substituted with one or more substituents which are the same or different, at any ring carbon atom; and wherein independently any ring nitrogen atom, if present in said —(CH)-(4- to 6-membered heterocycloalkyl) is substituted with R; and wherein —(CH)-(4- to 6-membered heterocycloalkyl) is preferably —(CH)-morpholinyl; and'}q represents the integer 1.12. A compound according to claim 11 , wherein Rrepresents —(CH)-morpholinyl substituted ...

METHOD FOR IMPROVING BLADDER FUNCTION

The invention pertains to the use of uridine and/or an equivalent thereof and n3-PUFA in the manufacture of a product for restoring or improving bladder function in a subject, in particular in a patient suffering from spinal cord injury. 113-. (canceled)14. A method for restoring or improving bladder function in a subject , comprising administering to the subject a composition comprising:(i) uridine and/or an equivalent thereof and(ii) n-3 PUFA.15. The method according to claim 14 , wherein the subject is suffering from claim 14 , is recovering from and/or has suffered from a neurological disorder.16. The method according to claim 15 , wherein the neurological disorder is from spinal cord injury.17. The method according to claim 14 , wherein the n-3 PUFA is selected from EPA and/or DHA.18. The method according to claim 17 , wherein 500-5000 mg DHA is administered per day.19. The method according to claim 14 , wherein the composition further comprises choline.20. The method according to claim 14 , wherein the composition further comprises B vitamin(s).21. The method according to claim 14 , wherein the composition further comprises phospholipids claim 14 , choline claim 14 , B vitamin(s) and antioxidants.22. The method according to claim 21 , wherein the composition comprises choline claim 21 , vitamin B6 and folic acid.23. The method according to claim 14 , wherein the uridine and/or equivalent thereof is uridine monophosphate.24. The method according to claim 14 , wherein the composition comprises per 125 mL or per daily dosage:(i) 400-800 mg UMP;(ii) n-3 PUFAs comprising (a) 100-500 mg EPA and (b) 900-1500 mg DHA;(iii) 50-600 mg phospholipids;(iv) 200-600 mg choline; (a) 1-5 μg vitamin B12,', '(b) 0.5-3 mg vitamin B6 and', '(c) 200-600 μg folic acid; and, '(v) vitamins B comprising (a) 20-60 mg vitamin E (alpha-TE),', '(b) 60-100 mg vitamin C, and', '(c) 40-80 μg selenium., '(vi) antioxidants comprising'}25. The method according to claim 14 , wherein the ...

BLADDER INSTILLATION COMPOSITION CONTAINING CHONDROITIN SULFATE (20 MG/ML), HYALURONIC ACID (16 MG/ML) AND A PHOSPHATE BUFFER (PH 6.1 TO 7.9) WITH INCREASED STORAGE STABILITY FOR TREATING CYSTITIS

The invention relates to a composition, in particular a pharmaceutical composition, which is suitable in particular for the prophylactic and/or therapeutic treatment preferably of inflammatory diseases of the urogenital tract, in particular inflammatory diseases of the bladder, preferably cystitis, to the uses thereof, to a storage or application device relating to same, to a packaging unit, and finally to a kit which is designed in particular as an instillation system. 115-. (canceled)17. The composition as claimed in claim 16 ,wherein the inflammatory diseases of the urogenital tract are selected among inflammatory diseases of the bladder and cystitis.18. The composition as claimed in claim 16 ,{'sub': 'n', 'wherein the chondroitin sulfate and the physiologically compatible chondroitin sulfate salt each have a number-average molecular weight Mwithin the range of from 2 kDa to 200 kDa; and'}{'sub': 'w', 'wherein the chondroitin sulfate and the physiologically compatible chondroitin sulfate salt each have a weight-average molecular weight Mwithin the range of from 10 kDa to 200 kDa.'}19. The composition as claimed in claim 16 ,wherein the hyaluronic acid and the physiologically compatible hyaluronic acid salt each have a number-average molecular weight Mn within the range of from 10 kDa to 300 kDa; andwherein the hyaluronic acid and the physiologically compatible hyaluronic acid salt each have a weight-average molecular weight Mw within the range of from 10 kDa to 500 kDa.20. The composition as claimed in claim 16 ,wherein the composition comprises the dihydrogen phosphate/monohydrogen phosphate buffer system in a total concentration of dihydrogen phosphate/monohydrogen phosphate buffer system of (1.75±1.65) mg/ml.21. The composition as claimed in claim 16 ,wherein the composition comprises the dihydrogen phosphate/monohydrogen phosphate buffer system in a weight ratio of dihydrogen phosphate to monohydrogen phosphate within the range of from 2:1 to 1:100.22. The ...

PHARMACEUTICAL COMPOSITION FOR ORAL ADMINISTRATION

Disclosed is a pharmaceutical composition for oral administration, comprising 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid, which is a compound having pH-dependent solubility, or a pharmaceutically acceptable salt thereof, and a cellulose derivative. In the pharmaceutical composition for oral administration, the solubility and absorbability of the drug are improved. 1. A pharmaceutical composition for oral administration , comprising 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1 ,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid , or a pharmaceutically acceptable salt thereof , and a cellulose derivative.2. The pharmaceutical composition for oral administration according to claim 1 , wherein the cellulose derivative is hydroxypropyl cellulose and/or hypromellose.3. The pharmaceutical composition for oral administration according to claim 1 , wherein the cellulose derivative is hydroxypropyl cellulose and/or hypromellose.4. The pharmaceutical composition for oral administration according to claim 1 , wherein 1-{5-[(5-{[(2R)-2-ethylpyrrolidin-1-yl]methyl}-4-[4-methoxy-3-(trifluoromethyl)phenyl]-1 claim 1 ,3-thiazol-2-yl)carbamoyl]pyrazin-2-yl}pyperidine-4-carboxylic acid claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a cellulose derivative form a solid dispersion.5. The pharmaceutical composition for oral administration according to claim 1 , further comprising an effervescent substance.6. The pharmaceutical composition for oral administration according to claim 5 , wherein the effervescent substance is sodium hydrogen carbonate.7. The pharmaceutical composition for oral administration according to claim 1 , further comprising a disintegrating component.8. The pharmaceutical composition for oral administration according to claim 7 , wherein the disintegrating component is one ...

Treatment of Lower Urinary Tract Epithelium With Glucagon Like Peptide 2

The present invention provides a method for treating and/or ameliorating a disorder of the lower urinary tract, comprising administering a composition comprising a glucagon like peptide 2 (GLP-2) receptor agonist to a patient in need thereof in an amount sufficient to treat and/or ameliorate the disorder of the lower urinary tract. 1. A method for treating a subject afflicted by a disorder of the subject's lower urinary tract epithelium , wherein the disorder is characterized by damage to epithelial cells in the subject's lower urinary tract epithelium , the method comprising administering a therapeutically effective amount of at least one of GLP-2 , a GLP-2 derivative , and a GLP-2 analog to the subject , wherein the therapeutically effective amount of the at least one of GLP-2 , a GLP-2 derivative , and a GLP-2 analog is sufficient to promote proliferation of the epithelial cells in the subject's lower urinary tract epithelium , thereby treating the subject.2. The method of claim 1 , wherein the disorder of the lower urinary tract epithelium comprises at least one of hemorrhagic cystitis claim 1 , interstitial cystitis/bladder pain syndrome claim 1 , and overactive bladder.3. The method of claim 2 , wherein the interstitial cystitis/bladder pain syndrome comprises Hunner's lesions.4. A method for promoting regeneration of urothelium in a subject claim 2 , wherein the urothelium is characterized by damage to epithelial cells in the subject's uroepithelium claim 2 , the method comprising administering a therapeutically effective amount of at least one of GLP-2 claim 2 , a GLP-2 derivative claim 2 , and a GLP-2 analog to the subject claim 2 , wherein the therapeutically effective amount of the at least one of GLP-2 claim 2 , a GLP-2 derivative claim 2 , and a GLP-2 analog is sufficient to promote proliferation of the epithelial cells in the subject's uroepithelium claim 2 , thereby promoting regeneration of urothelium in a subject.5. The method of claim 4 , wherein ...

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

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

Alkalization of urinary bladder wall prior to treatment with intravesical heparin and alkalinized lidocaine to enhance relief of bladder pain symptoms

The present invention is directed to an improved method of treating diseases and conditions associated with bladder pain, particularly interstitial cystitis. In general, a method according to the present invention comprises: (1) instilling into the bladder of a subject with a disease or condition associated with bladder pain a quantity and concentration of a physiologically compatible buffer to raise the pH of the bladder epithelium sufficiently to reduce acidosis associated with the disease or condition; (2) allowing the physiologically compatible buffer of (a) to remain in the bladder for a period sufficiently long to enable the buffer to raise the pH; (3) removing the physiologically compatible buffer of (1) from the bladder; and (4) instilling into the bladder a quantity of a composition comprising: (i) a heparinoid; (ii) a local anesthetic; and (iii) a buffer, wherein the composition has a pH of from about 7.0 to about 7.4 to treat the disease or condition associated with bladder pain. The present invention also is directed to kits for practicing the method.

Cyclohexylamines

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

METHODS COMPRISING DESMOPRESSIN

The present disclosure is directed to reducing nocturnal voids by administering a dose of desmopressin over a minimum treatment period compared to before administration, and maintaining or improving the reduction of nocturnal voids over the minimum treatment period. 127-. (canceled)28. A method of further reducing nocturnal voids in a female patient in need thereof comprising:measuring the patient's serum sodium level;administering to the patient, with a serum sodium level of at least 130 mmol/L, prior to bedtime an orodispersible dose of desmopressin chosen from 25 μg, 50 μg, and 100 μg over a first treatment period of about 28 days, wherein the dose is taken from 0.8 to 3 hours prior to the patient's bedtime and once daily and the dose is measured as the free base;measuring the patient's serum sodium level after the first treatment period; and continuing to administer the orodisperible dose of desmopressin prior to bedtime over a second contiguous treatment period of at least 28 days to about 1 year if the female patient has a serum sodium level of at least 130 mmol/L,wherein the nocturnal voids over the second treatment period are further reduced in view of the reduction in the nocturnal voids over the first treatment period and wherein the reduction in the nocturnal voids over the first treatment period is determined based on the patient's nocturnal voids before administration of the orodispersible dose of desmopressin for the first treatment period.29. The method according to claim 28 , wherein the dose of desmopressin is supplied in the form of the acetate salt of desmopressin.30. The method according to claim 28 , wherein the orodispersible dose of desmopressin is a dosage form comprising desmopressin acetate claim 28 , gelatin claim 28 , mannitol claim 28 , and citric acid.31. The method according to claim 28 , wherein the patient in need thereof has nocturia or nocturnal polyuria.32. The method according to claim 28 , wherein the reduction in nocturnal ...

Combination of tasquinimod or a pharmaceutically acceptable salt thereof and a pd-1 and/or pd-l1 inhibitor, for use as a medicament

The present invention concerns a combination comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and a PD-1 and/or PD-L1 inhibitor, for use as a medicament. It also concerns a pharmaceutical composition comprising tasquinimod, or a pharmaceutically acceptable salt thereof, and PD-1 and/or PD-L1 inhibitor.

CRYSTAL POLYMORPHISM OF KCNQ2-5 CHANNEL ACTIVATOR

Crystal polymorphism may exist in a crystalline compound. In the case where crystal polymorphism exists, depending on the crystal form, solubility, dissolution rate, stability against heat, light, humidity, etc. or the like is different. Accordingly, in the production of a pharmaceutical product, it is a very important task to select a crystal form of a drug substance most suitable for a disease indication and a dosage form. The present invention relates to novel crystal forms (A crystal, W crystal, and a hydrate crystal (H crystal)) of a compound I having a strong opening action with respect to KCNQ2-5 channels. 1. A crystal of 1-[(5-chloro-2-pyridinyl)methyl]-3-{2 ,6-dichloro-4-[(2S)-1 ,1 ,1-trifluoro-2-hydroxy-2-propanyl]phenyl}urea , having at least peaks of about 15.3 , 16.9 , 17.4 , 19.3 , and 19.6 °2θ in a powder X-ray diffraction spectrum.2. The crystal of 1-[(5-chloro-2-pyridinyl)methyl]-3-{2 claim 1 ,6-dichloro-4-[(2S)-1 claim 1 ,1 claim 1 ,1-trifluoro-2-hydroxy-2-propanyl]phenyl}urea according to claim 1 , having no peaks of about 7.0 and 9.2 °2θ in a powder X-ray diffraction spectrum.3. The crystal of 1-[(5-chloro-2-pyridinyl)methyl]-3-{2 claim 1 ,6-dichloro-4-[(2S)-1 claim 1 ,1 claim 1 ,1-trifluoro-2-hydroxy-2-propanyl]phenyl}urea according to claim 1 , further having peaks of about 11.3 claim 1 , 11.6 claim 1 , 11.9 claim 1 , 12.8 claim 1 , 13.9 claim 1 , 16.4 claim 1 , 18.1 claim 1 , 20.5 claim 1 , 21.1 claim 1 , 22.2 claim 1 , 22.8 claim 1 , 23.5 claim 1 , 23.8 claim 1 , 24.3 claim 1 , and 24.7 °2θ in a powder X-ray diffraction spectrum.4. The crystal of 1-[(5-chloro-2-pyridinyl)methyl]-3-{2 claim 1 ,6-dichloro-4-[(2S)-1 claim 1 ,1 claim 1 ,1-trifluoro-2-hydroxy-2-propanyl]phenyl}urea according to claim 1 , characterized by a powder X-ray diffraction spectrum chart shown in .5. A crystal of 1-[(5-chloro-2-pyridinyl)methyl]-3-{2 claim 1 ,6-dichloro-4-[(2S)-1 claim 1 ,1 claim 1 ,1-trifluoro-2-hydroxy-2-propanyl]phenyl}urea claim 1 , having an ...

METHODS FOR TREATMENT OF INTERSTITIAL CYSTITIS

The present application relates to methods and uses of CB2 target agent local anaesthetics such as beta-caryophyllene for treatment of interstitial cystitis in a subject, optionally together with the administration or use of an additional agent for treating interstitial cystitis such as dimethyl sulfoxide (DMSO) or methylsulfonylmethane (MSM). 1. A method of treating interstitial cystitis in a subject , the method comprising administering a CB2 target agent local anaesthetic to the subject.2. The method of claim 1 , wherein the CB2 target agent local anaesthetic is a CB2 orthosteric agonist agent local anaesthetic.3. The method of claim 2 , wherein the CB2 orthosteric agonist agent local anaesthetic is beta-caryophyllene.4. The method of claim 3 , further comprising administering an additional agent for treating interstitial cystitis in the subject.5. The method of claim 4 , wherein the additional agent is dimethyl sulfoxide.6. The method of claim 5 , wherein the dimethyl sulfoxide is administered intravesically as an aqueous solution comprising from about 5% to about 50% dimethyl sulfoxide.7. The method of claim 6 , wherein the aqueous solution comprises about 5% dimethyl sulfoxide.8. The method of claim 4 , wherein the additional agent is methylsulfonylmethane.9. The method of claim 8 , wherein the methylsulfonylmethane is administered intravesically as an aqueous solution comprising about 5% methylsulfonylmethane.10. The method of claim 8 , wherein the methylsulfonylmethane is administered orally.11. The method of claim 3 , wherein the CB2 target agent local anaesthetic is administered orally.12. The method of claim 11 , wherein the oral administration is in the form of a capsule comprising the CB2 target agent local anaesthetic.13. The method of claim 12 , wherein the CB2 target agent local anaesthetic is administered in combination with methylsulfonylmethane and the capsule further comprises the methylsulfonylmethane.14. The method of claim 3 , wherein the CB2 ...

Methods of treating bladder cancer

The present invention provides methods and compositions for treating bladder cancer, including metastatic bladder cancer and non-muscle-invasive bladder cancer, by administering a composition comprising nanoparticles that comprise mTOR inhibitor and optionally an albumin.

METHODS FOR TREATMENT OF INTERSTITIAL CYSTITIS

The present application relates to methods and uses of CB2 target agent local anaesthetics such as beta-caryophyllene for treatment of interstitial cystitis in a subject, optionally together with the administration or use of an additional agent for treating interstitial cystitis such as dimethyl sulfoxide (DMSO) or methylsulfonylmethane (MSM). 1. A method of treating interstitial cystitis in a subject , the method comprising administering a CB2 target agent local anaesthetic to the subject.2. The method of claim 1 , wherein the CB2 target agent local anaesthetic is a CB2 orthosteric agonist agent local anaesthetic.3. The method of claim 2 , wherein the CB2 orthosteric agonist agent local anaesthetic is beta-caryophyllene.4. The method of claim 3 , further comprising administering an additional agent for treating interstitial cystitis in the subject.5. The method of claim 4 , wherein the additional agent is dimethyl sulfoxide.6. The method of claim 5 , wherein the dimethyl sulfoxide is administered intravesically as an aqueous solution comprising from about 5% to about 50% dimethyl sulfoxide.7. The method of claim 6 , wherein the aqueous solution comprises about 5% dimethyl sulfoxide.8. The method of claim 4 , wherein the additional agent is methylsulfonylmethane.9. The method of claim 8 , wherein the methylsulfonylmethane is administered intravesically as an aqueous solution comprising about 5% methylsulfonylmethane.10. The method of claim 8 , wherein the methylsulfonylmethane is administered orally.11. The method of claim 3 , wherein the CB2 target agent local anaesthetic is administered orally.12. The method of claim 11 , wherein the oral administration is in the form of a capsule comprising the CB2 target agent local anaesthetic.13. The method of claim 12 , wherein the CB2 target agent local anaesthetic is administered in combination with methylsulfonylmethane and the capsule further comprises the methylsulfonylmethane.14. The method of claim 3 , wherein the CB2 ...

Compositions and methods for urinary bladder regeneration

The present invention provides compositions and methods for the regeneration of tissue. In particular, the present invention provides mesenchymal stem cells (MSCs) and endothelial progenitor cells (EPCs) for bladder regeneration.

PHARMACEUTICAL COMPOSITION OF INSULIN GLARGINE AND AMINO ACIDS

There is provided a pharmaceutical composition comprising: (a) insulin glargine, (b) at least two amino acids, and optionally (c) one or more pharmaceutically acceptable excipients. In particular, there is provided a pharmaceutical composition comprising: (a) insulin glargine, (b) arginine and isoleucine in a weight ratio of about 1:2, and optionally (c) one or more pharmaceutically acceptable excipients. 1. A pharmaceutical composition comprising: (a) insulin glargine , (b) arginine and isoleucine in a weight ratio of 1:2 , and optionally (c) one or more pharmaceutically acceptable excipients.2. A pharmaceutical composition comprising: (a) insulin glargine , (b) arginine and isoleucine in a weight ratio of about 1:2 , and optionally (c) one or more pharmaceutically acceptable excipients , wherein the pharmaceutical composition is compatible when mixed with another insulin having isoelectric point between 4.0 and 5.7.3. A stable biphasic pharmaceutical composition comprising: (a) insulin glargine in a suspension form , (b) another insulin having isoelectric point between 4.0 and 5.7 , (c) arginine and isoleucine in a weight ratio of 1:2 , and optionally , (d) one or more pharmaceutically acceptable excipients , wherein the pharmaceutical composition has a pH between 6.0 to 8.0.4. The pharmaceutical composition of or , wherein the composition has pH in between 2 to 8.5. The pharmaceutical composition of or , wherein the another having isoelectric point between 4.0 and 5.7 is selected from the group comprising insulin human , insulin isophane (NPH) , insulin lispro , insulin lispro protamine , insulin glulisine , insulin aspart , insulin aspart protamine , Gly(A21) human insulin , Gly(A21) Lys(B28) human insulin , Gly(A21) Lys(B28) Pro(B29) human insulin , Gly(A21) Asp(B28) , insulin degludec and insulin detemir.67.-. (canceled)8. The pharmaceutical composition of or , wherein the pharmaceutical composition is in the form of solution.9. The pharmaceutical composition ...

Sulfamides as trpm8 modulators

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein Y, R 1 , R 2 , R 3 , R 4 , R A , and R B are defined herein.

ANTI-MGLUR5 ANTIBODIES AND USES THEREOF

This invention generally pertains to antibodies and antigen-binding antibody Fragments, preferably humanized, chimeric, and human antibodies and antigen-binding antibody fragments. compositions containing such antibodies and antigen-binding antibody fragments or cells, e.g., immune cells such as T, Treg, or NK cells which express same, wherein such antibodies and antigen-binding antibody Fragments specifically bind to mGluR5. The invention also relates to therapeutic and diagnostic uses for the antibodies, antigen-binding antibody fragments, and compositions thereof. 1. An isolated antibody , or antigen-binding antibody fragment , that binds to human mGluR5 and antagonizes , inhibits , neutralizes or blocks at least one biological effect associated with human mGluR5 , wherein the isolated antibody or antigen-binding antibody fragment is selected from the group consisting of a monoclonal antibody; a monospecific antibody; a polyspecific antibody; a human antibody; a humanized antibody; a chimeric antibody; a tetrameric antibody; a tetravalent antibody; a bispecific antibody; a multispecific antibody; a single chain antibody; a domain-specific antibody; a single domain antibody; a domain-deleted antibody; an scFc fusion protein; a synthetic antibody; a recombinant antibody; a hybrid antibody; a mutated antibody; CDR-grafted antibodies; an antigen-binding antibody fragment; an Fab; an F(ab′)2; an Fab′ fragment; an Fv fragment; a single-chain Fv (scFv) fragment; an Fd fragment; a dAb fragment; a diabody; a nanobody; a bivalent nanobody; a shark variable IgNAR domain; a VH antibody; a camelid antibody; a chimeric antigen receptor (CAR) , a Bispecific T cell Engager (BiTE) , and a minibody.23-. (canceled)4. The isolated antibody or antigen-binding antibody fragment according to claim 1 , wherein the antibody or antigen-binding antibody fragment is not N-glycosylated.5. The isolated antibody or antigen-binding antibody fragment according to claim 1 , which allosterically ...

Methods of Manipulating Phagocytosis Mediated by CD47

Methods are provided to manipulate phagocytosis of cancer cells, including e.g. leukemias, solid tumors including carcinomas, etc.

PROSTATE FUNCTION SUPPORT FORMULA

The invention provides unit dosage forms and methods that are effective to improve prostate function. Such unit dosage forms and methods are useful to decrease bladder discomfort and improve urinary flow in men. 1. A unit dosage form suitable for oral administration in a human comprising:300 mg±30 mg of Saw Palmetto;450 mg±45 mg of Beta-Sitosterol;150 mg±15 mg of Pygeum Africanum;75 mg±7.5 mg of Green Tea extract;15 mg±1.5 mg of Lycopene; and30 mg±3 mg of Stinging Nettle.2. The unit dosage form of that further comprises Vitamin E.3. The unit dosage form of that further comprises Vitamin B-6.4. The unit dosage form of that further comprises zinc as zinc gluconate.5. The unit dosage form of that further comprises selenium as amino acid chelate.6. The unit dosage form of that further comprises copper as copper gluconate.7. The unit dosage form of that further comprises 2-(3 claim 1 ,4-dihydroxyphenyl)-3 claim 1 ,5 claim 1 ,7-trihydroxy-4H-chromen-4-one.8. The unit dosage form of that further comprises one or more amino acids selected from L-alanine claim 1 , L-glutamic acid and glycine.9. The unit dosage form of that further comprises one or more excipients selected from hydroxypropyl methylcellulose claim 1 , rice concentrate claim 1 , and silica.10. The unit dosage form of that further comprises one or more excipients selected from gelatin claim 1 , magnesium stearate claim 1 , stearic acid claim 1 , and microcrystalline cellulose.11. The unit dosage form of that is formulated as a capsule or a tablet.12. A method to improve prostate function in a man in need thereof comprising administering a unit dosage form of to the man.13. The method of wherein bladder discomfort is decreased.14. The method of wherein urinary flow is improved.15. The method of wherein the unit dosage form is administered in the form of three capsules or tablets per day.16. The unit dosage form suitable for oral administration in a human of comprising:300 mg±15 mg of Saw Palmetto;450 mg±22.5 mg ...

PROPHYLACTIC OR THERAPEUTIC AGENT FOR HYPERACTIVE BLADDER

various side effects are reported for existing overactive bladder therapeutic drugs, and prophylactic or therapeutic agents for overactive bladder without side effects have been eagerly desired. The present invention provides a prophylactic or therapeutic agent for overactive bladder that comprises 5-aminolevulinic acids (ALAs) as the active ingredient. 1. A pharmaceutical composition for use in prevention or treatment of overactive bladder comprising the compound shown by the following Formula (I):{'br': None, '[Chemical Formula 1]'}{'br': None, 'sup': 1', '2, 'sub': 2', '2', '2, 'R—NHCHCOCHCHCOOR\u2003\u2003(I)'}{'sup': 1', '2, '(wherein Rrepresents a hydrogen atom or an acyl group, and Rrepresents a hydrogen atom, a linear or branched alkyl group, a cycloalkyl group, an aryl group, or an aralkyl group)'}or a salt thereof.2. The pharmaceutical composition according to claim 1 , characterized in that said overactive bladder is overactive bladder showing a symptom of frequent urination.3. The pharmaceutical composition according to claim 1 , characterized in that:{'sup': '1', 'Ris selected from the group consisting of a hydrogen atom, an alkanoyl group having 1-8 carbons, and an aroyl group having 7-14 carbons, and'}{'sup': '2', 'Ris selected from the group consisting of a hydrogen atom, a linear or branched alkyl group having 1-8 carbons, a cycloalkyl group having 3-8 carbons, an aryl group having 6-14 carbons, and an aralkyl group having 7-15 carbons.'}4. The pharmaceutical composition according to claim 3 , characterized in that Rand Rare hydrogen atoms.5. The pharmaceutical composition according to any one of to claim 3 , characterized in that it further contains one or more types of metal-containing compounds.6. The pharmaceutical composition according to claim 5 , characterized in that the metal-containing compound is a compound containing iron claim 5 , magnesium claim 5 , zinc claim 5 , nickel claim 5 , vanadium claim 5 , copper claim 5 , chromium claim 5 , ...

METHOD OF TREATING PAIN OR INTERSTITIAL CYSTITIS USING INDOLE COMPOUND

Provided is a therapeutic or prophylactic agent for pain or interstitial cystitis comprising N-[2-(6,6-dimethyl-4,5,6,7-tetrahydro-H-indazol-3-yl)-1H-indol-6-yl]-N-methyl-(2S)-2-(morpholin-4-yl)propanamide or a pharmaceutically acceptable salt thereof. 2. The method of claim 1 , wherein the pain is neuropathic pain claim 1 , nociceptive pain claim 1 , or mixed pain.3. The method of claim 1 , wherein the pain is inflammatory pain claim 1 , musculoskeletal pain claim 1 , or cancer pain.4. The method of claim 1 , wherein the pain is pain of osteoarthritis claim 1 , low back pain claim 1 , pain of interstitial cystitis claim 1 , or pain of diabetic peripheral neuropathy.5. The method of claim 1 , wherein the pain is pain of rheumatoid arthritis.6. The method of claim 1 , wherein the pain is not pain of rheumatoid arthritis.7. The method of claim 1 , wherein the pain is painful bladder syndrome claim 1 , bladder pain syndrome claim 1 , or chronic pelvic pain syndrome.8. The method of claim 1 , wherein the pain is associated with inflammation claim 1 , pancreatitis claim 1 , kidney stones claim 1 , a headache claim 1 , dysmenorrhea claim 1 , musculoskeletal pain claim 1 , a sprain claim 1 , visceral pain claim 1 , an ovarian cyst claim 1 , prostatitis claim 1 , cystitis claim 1 , inflammatory bowel disease claim 1 , post-surgical pain claim 1 , a migraine claim 1 , trigeminal neuralgia claim 1 , burns claim 1 , wounds claim 1 , trauma claim 1 , post-herpetic neuralgia claim 1 , a musculoskeletal disease claim 1 , ankylosing spondylitis claim 1 , a periarticular pathology claim 1 , cancer claim 1 , bone metastases claim 1 , HIV claim 1 , myocardial infarction claim 1 , fracture claim 1 , gout claim 1 , joints claim 1 , sciatica claim 1 , a sickle cell crisis claim 1 , endometriosis claim 1 , fibromyalgia claim 1 , incisional pain claim 1 , erythromelalgia claim 1 , malignant melanoma claim 1 , Sjogren's syndrome claim 1 , asthma claim 1 , chronic abacterial prostatitis ...

SOLUTION COMPRISING THE CHLORIDE HYDROCHLORIDE SALT OF 4-(5-(2-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-N,2-DIMETHYLPROPANAMIDO)-4-(o-TOLYL)PYRIDIN-2-YL)-1-METHYL-1-((PHOSPHONOOXY)METHYL)PIPERAZIN-1-IUM (FOSNETUPITANT) AND PALONOSETRON HYDROCHLORIDE IN COMBINATION WITH DEXAMETHASONE AS A NEUROKININ RECEPTOR MODULATOR

Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the neurokinin (NK) receptor. The compounds have the general formula (I): 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare each independently selected from the group consisting of hydrogen claim 1 , hydroxy claim 1 , amino claim 1 , alkyl claim 1 , alkenyl claim 1 , cycloalkyl claim 1 , halogen claim 1 , cyano claim 1 , —ORand CF.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein X is —NRC(O).4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Y is a heterocycloalkyl or heterocycloalkylalkyl.11. A method of treating emesis claim 1 , bladder dysfunction claim 1 , depression or anxiety claim 1 , in a patient in need thereof claim 1 , comprising administering to said patient a therapeutically effective amount of a compound of formula (I) according to .12. The method of claim 11 , wherein said emesis comprises chemotherapy induced nausea and vomiting (CINV) claim 11 , radiation therapy induced nausea and vomiting (RINV) claim 11 , or post-operative nausea and vomiting (PONV).13. The method of claim 11 , wherein said emesis is induced by moderately or highly emetogenic chemotherapy.14. The method of claim 11 , wherein said emesis is acute and delayed emesis induced by moderately or highly emetogenic chemotherapy.15. (canceled)16. (canceled)17. The method of claim 11 , wherein said compound or a pharmaceutically acceptable salt thereof claim 11 , is intravenously administered at a dosage of from about 10 mg to about 200 mg based on the netupitant portion of the molecule.18. The method of claim 11 , wherein said emesis is acute and delayed emesis induced by moderately or highly emetogenic chemotherapy claim 11 , further comprising ...

METHODS OF USE FOR OENOTHEIN A AND B FROM EPILOBIUM SPECIES

The invention provides medicaments comprising an oenothein, including oral formulations to treat inflammation or to treat hormone balance in perimenopausal, menopausal and postmenopausal women. The oenothein for use in such formulations, such as oenothein A and oenothein B, maybe purified from natural sources, such as , and used in combination with a cannabinoid, such as cannabidiol (CBD), cannabigerol (CBG) or tetrahydrocannabinol (THC). 1. A method of treating one or more symptoms of overactive bladder in a subject comprising administering to the subject a therapeutically effective amount of a composition comprising oenothein A and B , and a cannabinoid ,wherein the one or more symptoms of overactive bladder are selected from the group consisting of frequency or urgency, nocturia, increase in urinary micturition frequency, urinary incontinence, hormone balance for perimenopausal, menopausal, postmenopausal women and inflammation, andwherein the cannabinoid is cannabidiol (CBD), tetrahydrocannabinol (THC), cannabigerol (CBG), or a combination thereof.2. The method of claim 1 , wherein a therapeutically effective amount comprises a daily administration of about 350 mg to about 400 mg of oenothein A and B claim 1 , and about 0.05 mg to about 50 mg of CBD claim 1 , about 1 mg to about 15 mg of THC claim 1 , or about 0.05 mg to about 500 mg of CBG.3. The method of claim 1 , wherein a therapeutically effective amount to treat chronic symptoms comprises about 1000 mg of oenothein A and B claim 1 , and about 1 claim 1 ,000 mg to about 2 claim 1 ,000 mg of CBD claim 1 , about 30 mg to about 100 mg of THC claim 1 , or about 500 mg to about 1000 mg of CBG.4. The method of claim 1 , wherein the composition is formulated as a concentrated oil extracts infused sublingual spray claim 1 , a tincture claim 1 , an edible claim 1 , a gel capsule claim 1 , a pH-resistant capsule claim 1 , a topical salve claim 1 , drops claim 1 , or an aerosol.5. The method of claim 1 , wherein the ...

Recombinant Mycobacterium as an Immunotherapeutic Agent for the Treatment of Cancer

The invention relates to a recombinant Mycobacterium cell for use as an immunotherapeutic agent in the treatment of cancer, particularly in the treatment of solid tumors. More particularly, the invention relates to the immunotherapy of bladder carcinoma.

Multi-unit drug delivery devices and methods

Abstract of the Disclosure Implantable drug delivery devices include a housing defining a reservoir, a first unit within the reservoir, and a second unit within the reservoir. The first unit contains a drug and the second unit contains a functional agent that facilitates release of the drug. Intravesical drug delivery devices include a housing portion containing a drug formulation and a housing portion containing an excipient, and are configured to release the drug according to a first release profile and the excipient according to a second release profile. Methods include inserting any of these devices into a patient and releasing drug from the device.

Il-8 inihibitors for use in the treatment of some urological disorders

The present invention relates to IL-8 inhibitor compounds, preferably dual CXCR1/CXCR2 receptor inhibitors, useful in the treatment and/or prevention of interstitial cystitis/painful bladder syndrome (IC/PBS) and/or over active bladder (OAB), also including IC/PBS and/or OAB induced by anticancer therapy. Methods of treatment and/or prevention, combinations and kits comprising said IL-8 inhibitors are also covered therein.

Recombinant Mycobacterium as an Immunotherapeutic Agent for the Treatment of Cancer

The invention relates to a recombinant Mycobacterium cell for use as an immunotherapeutic agent in the treatment of cancer, particularly in the treatment of solid tumors. More particularly, the invention relates to the immunotherapy of bladder carcinoma. 1Mycobacterium bovis. A recombinant cell which comprises a recombinant nucleic acid molecule encoding a fusion polypeptide comprising:(a) a domain capable of eliciting an immune response, and(b) a Listeria phagolysosomal escape domain for use as immunotherapeutic agent in the treatment of bladder carcinoma.2. The cell of which is a urease-deficient cell.3M. bovis. The cell of which is a recombinant BCG cell from strain Danish subtype Prague.4M. bovisM. tuberculosis.. The cell of claim 1 , wherein the domain capable of eliciting an immune response is selected from immunogenic peptides or polypeptides from or5. The cell of claim 1 , wherein the recombinant nucleic acid molecule does not comprise any functional selection marker.6. The cell of claim 1 , wherein the fusion polypeptide comprises(a) a domain capable of eliciting an immune response comprising the amino acid sequence from aa.41 to aa.51 in SEQ ID No.2, and{'i': 'Listeria', '(b) a phagolysosomal escape domain encoded by a nucleic acid molecule selected from'}(i) a nucleotide sequence comprising nucleotides 211-1722 as shown in SEQ ID No.1,(ii) a nucleotide sequence which encodes the same amino acid sequence as the sequence from (i), and(iii) a nucleotide sequence hybridising under stringent conditions with the sequence from (i) or (ii).7. The cell of claim 1 , wherein the bladder carcinoma is non-invasive bladder carcinoma claim 1 , particularly carcinoma in situ (T) claim 1 , non-invasive papillary carcinoma (T) claim 1 , or a tumor invading subepithelial connective tissue (T).8. The cell of claim 1 , wherein the treatment comprises local administration of the immunotherapeutic agent to the tumor site claim 1 , particularly after surgery.9. The cell of claim ...

PIPERAZINE DERIVATIVE

[Problem] To provide a compound useful as an MCreceptor agonist. 2: The compound or salt thereof according to claim 1 , wherein{'sup': '1', 'sub': 1-6', '3-8, 'Rrepresents Calkyl which may be substituted, Ccycloalkyl, or an oxygen-containing saturated hetero ring,'}{'sup': '3', 'sub': 1-6', '3-8, 'Rrepresents Calkyl, Ccycloalkyl which may be substituted, or phenyl which may be substituted,'}{'sup': 4a', '9', '9, 'sub': 1-4', '2, 'Rrepresents H, Calkyl, —C(O)R, or —S(O)R,'}{'sup': '4b', 'sub': '1-6', 'Rrepresents H or Calkyl,'}{'sup': 4a', '4b', '4a', '4b, 'sub': 1-6', '1-6, 'in a case where Rrepresents H, Ralso represents H, and in a case where Rrepresents Calkyl, Ralso represents Calkyl, and'}{'sup': '9', 'sub': 1-6', '3-8, 'Rrepresents Calkyl or Ccycloalkyl.'}5: The compound or salt thereof according to claim 4 , wherein{'sup': '3', 'sub': 1-6', '3-8, 'Rrepresents Calkyl, Ccycloalkyl, or phenyl which may be substituted with one cyano group,'}{'sup': 4a', '9, 'Rrepresents —C(O)R,'}{'sup': '4b', 'Rrepresents H, and'}{'sup': '8', 'X represents CR.'}6: The compound or salt thereof according to claim 5 , wherein{'sup': '1', 'sub': '1-6', 'Rrepresents Calkyl,'}{'sup': '3', 'sub': '3-8', 'when n represents 0, Rrepresents Ccycloalkyl, and'}{'sup': '3', 'sub': '1-6', 'when n represents 1, Rrepresents Calkyl.'}7: The compound or salt thereof according to claim 6 , wherein{'sup': '1', 'Rrepresents tert-butyl,'}{'sup': 2a', '2b, 'Rand Rare the same as or different from each other and each represent H or methyl,'}{'sup': 2a', '2b, 'Rand Rdo not simultaneously represent H,'}{'sup': '3', 'when n represents 0, Rrepresents cyclohexyl,'}{'sup': '3', 'when n represents 1, Rrepresents isopropyl or tert-butyl,'}{'sup': '8', 'X represents CR,'}{'sup': '6', 'Rrepresents F or Cl,'}{'sup': '8', 'Rrepresents H or F, and'}{'sup': '9', 'Rrepresents methyl.'}8: The compound or salt thereof according to claim 1 , wherein the compound is selected from the group consisting of:N-{(1S)-2-[(3S)-4 ...

NEUROMODULATION DEVICE

The present invention provides improved devices, systems and methods to provide for control of bladder function. Aspects of the present disclosure relate to an apparatus, system and/or a method for modulating the neural activity of afferent fibres of the pelvic nerve to bladder function. In one aspect, the disclosure relates to the use of pharmaceutical compositions in patients undergoing neuromodulation therapy. 1. An apparatus for modulating the neural activity of afferent fibres of at least one pelvic nerve of a patient , the apparatus comprising:a first actuator configured to apply a first signal to said at least one pelvic nerve of the patient; anda controller coupled to the first actuator, the controller controlling the signal to be applied by the actuator, such that the signal modulates the neural activity of the afferent fibres of the nerve to produce a physiological response in the patient.2. An apparatus according to claim 1 , wherein the apparatus comprises a second actuator coupled to the controller and configured to apply a second signal to a pudendal nerve of the patient claim 1 , wherein the controller controls the signal to be applied by the second actuator such that the signal modulates the neural activity of the pudendal nerve to produce a physiological response in the patient.3. An apparatus according to claim 1 , wherein each signal is independently selected from an electrical signal claim 1 , an optical signal claim 1 , an ultrasonic signal and a thermal signal.4. An apparatus according to claim 1 , wherein the first signal is an electrical signal claim 1 , and the first actuator configured to apply said electrical signal is an electrode.5. An apparatus according to claim 1 , wherein the first signal comprises an alternating current (AC) waveform.6. An apparatus according to claim or claim 5 , wherein the first signal comprises a sub-kilohertz frequency AC waveform.7. An apparatus according to claim 2 , wherein the second signal comprises a sub- ...

Method for xeno-free generation of a population of hmpc

The present invention concerns a method of generating a population of skeletal muscle derived human muscle precursor cells. For this purpose, a specialized FBS-free cell growth medium is used. The invention further concerns a composition comprising such a population of hMPCs for use as a medicament, especially in the treatment of skeletal muscle dysfunction.

OXYBUTYNIN-CONTAINING TRANSDERMAL ABSORPTION PREPARATION

An oxybutynin-containing transdermal absorption preparation includes a support layer that is formed of a base fabric and has water repellency in at least a part thereof, and an adhesive layer laminated on one side of the support layer, in which the adhesive layer includes an adhesive composition containing oxybutynin or a pharmaceutically acceptable salt thereof, cholesterols, and a rubber adhesive base. The oxybutynin may be oxybutynin hydrochloride. A portion having the water repellency may be formed by a fluorine-containing compound. The base fabric may be a knitted fabric. 1. An oxybutynin-containing transdermal absorption preparation , which is a patch comprising:a support layer that is formed of a base fabric and has water repellency in at least a part thereof; andan adhesive layer laminated on one side of the support layer,wherein the adhesive layer includes an adhesive composition containing oxybutynin or a pharmaceutically acceptable salt thereof, cholesterols, and a rubber adhesive base.2. The oxybutynin-containing transdermal absorption preparation according to claim 1 ,wherein the oxybutynin is oxybutynin hydrochloride.3. The oxybutynin-containing transdermal absorption preparation according to claim 1 ,wherein a portion having the water repellency is formed by a fluorine-containing compound.4. The oxybutynin-containing transdermal absorption preparation according to claim 1 ,wherein the base fabric is a knitted fabric.5. The oxybutynin-containing transdermal absorption preparation according to claim 1 ,wherein the rubber adhesive base contains a styrene-isoprene-styrene block copolymer.6. The oxybutynin-containing transdermal absorption preparation according to claim 2 ,wherein a content percentage of the oxybutynin is 4% to 50% relative to the adhesive composition, andcholesterol is used for the cholesterols, and a content percentage thereof is 0.05 to 10% relative to the adhesive composition. The present invention relates to a transdermal absorption ...

METHODS FOR TREATING, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF

The present invention relates to methods, pharmaceutical compositions and uses thereof for treating and alleviating Alport syndrome, various aspects and symptoms associated with Alport syndrome in a patient in need thereof comprising administering empagliflozin to the patient. 1. A method comprising:administering empagliflozin to a patient in order to at least one of:(i) treat Alport syndrome in the patient;(ii) improve renal function or delay or slow an impairment of the renal function in the patient diagnosed with Alport syndrome;(iii) delay progression of chronic kidney disease in the patient diagnosed with Alport syndrome;(iv) treat or alleviate glomerular hypertension in the patient diagnosed with Alport syndrome;(v) treat, including slowing or reversing the progression of, albuminuria and/or proteinuria in the patient diagnosed with Alport syndrome;(vi) improve a glomerular filtration rate or delay or slow a decline of the glomerular filtration rate in the patient diagnosed with Alport syndrome.26.-. (canceled)7. The method according to claim 1 , wherein the patient has an eGFR equal to or greater than 20 mL/min/1.73m.8. The method according to claim 1 , wherein the adult patient has an eGFR lower than 75 mL/min/1.73 mor lower than 90 mL/min/1.73m.9. The method according to claim 1 , wherein the patient has an elevated protein-to-creatinine ratio (PCR) greater or equal than 300 mg/g creatinine claim 1 , an elevated level of proteinuria of equal or greater than 200 mg protein per day (24 h urine protein) or an elevated albumin-to-creatinine ratio (ACR) greater or equal than 200 mg/g creatinine or greater or equal than 300 mg/g creatinine.10. The method according to claim 1 , wherein empagliflozin is administered at a dose in a range from 1 mg to 25 mg per day to the patient.11. The method according to wherein empagliflozin is administered at a dose of 10 mg per day to the patient.12. The method according to claim 1 , wherein empagliflozin is administered in ...

Sulfated Glycosaminoglycan Biomaterials as Proteoglycan Mimics

Polymer conjugates are provided that are capable of mimicking functions of natural proteoglycans found in the extracellular matrix of connective tissues. The polymer conjugates of the invention have utility in treating a subject suffering soft tissue degenerative conditions. Also provided are simple and scalable chemical processes for the preparation of the polymer conjugates of the invention. 1. A method of preparing a water-soluble sulfated GAG conjugate , comprising the steps of:i) contacting a sulfated GAG in aqueous solution at a concentration of 2 wt %-20 wt % with an effective amount of linking agent, such as a bifunctional linker, wherein the molar ratio of GAG hydroxyl groups to linking agent is less than that required for gel formation, under conditions sufficient to react the linking agent with the sulfated GAG to form a solution comprising a soluble polymer characterized by pendant linking groups;ii) adding additional sulfated GAG to the solution of step (i) in an amount sufficient to react with a portion of the pendant linking groups to form a soluble polymer conjugate with a bottlebrush architecture characterized by remaining pendant linking groups; andiii) adding a modifier characterized by a reactive moiety under conditions sufficient to react the remaining pendant linking groups with the reactive modifier to form a water-soluble sulfated GAG bottlebrush conjugate bearing the modifier.2. The method of claim 1 , wherein the product of step i) has a substantially linear structure.3. The method of claim 1 , wherein the sulfated GAG conjugate product of step-iii has a molecular weight of 100 claim 1 ,000 Da to 5 claim 1 ,000 claim 1 ,000 Da.4. The method of claim 1 , wherein the sulfated GAG of step-i has a molecular weight of about 1 claim 1 ,000 Da claim 1 , 5 claim 1 ,000 Da claim 1 , 10 claim 1 ,000 Da claim 1 , 15 claim 1 ,000 Da claim 1 , 20 claim 1 ,000 Da claim 1 , 30 claim 1 ,000 Da claim 1 , 40 claim 1 ,000 Da claim 1 , 50 claim 1 ,000 Da claim ...

Methods of use for oenothein a and b from epilobium species

The invention provides medicaments comprising an oenothein, including oral formulations to treat inflammation or to treat hormone balance in perimenopausal, menopausal and postmenopausal women. The oenothein for use in such formulations such as oenothein A or oenothein B maybe purified from natural sources, such as Epilobium.

Methods and compositions for treatment of interferon-resistant tumors

The present invention provides a method for the treatment of “interferon resistant” tumors (i.e., tumors resistant to treatment with exogenously-administered interferon polypeptide) through the use of a non-replicating agent which induces human cells to express interferon species. In particular it is noted that inducing interferon expression in the patient's body possesses properties not associated with exogenously-produced intravenously-administered interferon proteins. The present invention further provides compositions useful in the treatment of cancer resistant to treatment with exogenous interferon polypeptide, by using a non-replicating agent which induces human cells to express interferon species, e.g., an antigenic, replication-deficient virus optionally carrying an interferon transgene.

Sulfated Glycosaminoglycan Biomaterials as Proteoglycan Mimics

Polymer conjugates are provided that are capable of mimicking functions of natural proteoglycans found in the extracellular matrix of connective tissues. The polymer conjugates of the invention have utility in treating a subject suffering soft tissue conditions. Also provided are simple and scalable chemical processes for the preparation of the polymer conjugates of the invention. 1. A polymer conjugate comprising a plurality of sulfated glycosaminoglycan (GAG) polymer chains , wherein each sulfated GAG polymer chain is linked to one or more sulfated GAG polymer chains via a linker derived from a linking agent , and wherein the polymer conjugate is soluble in aqueous solution and has a molecular weight that is 3× to 100× that of an individual , nonlinked sulfated GAG.2. The polymer conjugate of claim 1 , comprising a plurality of sulfated GAG polymer chains and at least one additional polymer linked via a linker.3. The polymer conjugate of claim 2 , wherein the additional polymer is hyaluronic acid or carboxymethylcellulose.45-. (canceled)6. The polymer conjugate of claim 1 , wherein the linker agent has a molecular weight less than 1000 Da.79-. (canceled)10. The polymer conjugate of claim 1 , wherein the linker agent has a molecular weight less than 150 Da.11. The polymer conjugate of claim 1 , wherein the linker agent is selected from the group consisting of divinylsulfone (DVS) claim 1 , diepoxides claim 1 , epichlorohydrin (Epi) claim 1 , and butanedioldiglycidyl ether (BDDE).12. The polymer conjugate of claim 11 , wherein the linker agent is divinylsulfone (DVS).13. The polymer conjugate of claim 1 , wherein the sulfated GAG is selected from the group consisting of chondroitin sulfate claim 1 , heparan sulfate claim 1 , dermatan sulfate claim 1 , keratan sulfate claim 1 , and combinations thereof.14. The polymer conjugate of claim 1 , wherein the linker is randomly linked along a GAG polymer chain.15. The polymer conjugate of claim 1 , wherein the polymer ...

THERAPEUTIC OR PROPHYLACTIC AGENT FOR NOCTURNAL POLYURIA

There is provided a pharmaceutical composition which includes, as an active ingredient, a combination drug formulation of potassium citrate and sodium citrate hydrate or a sodium bicarbonate formulation. The prevention or treatment of nocturnal polyuria is achieved by administering the pharmaceutical composition. 122-. (canceled)23. A method for treating or preventing nocturnal polyuria , comprising administering an effective amount of an agent comprisingi) citric acid or a pharmaceutically acceptable salt thereof, or hydrates thereof, or mixtures thereof; orii) sodium bicarbonate,to a subject in need of treatment or prevention for nocturnal polyuria.24. A method for treating or preventing nocturnal enuresis , comprising administering an effective amount of an agent containingi)citric acid or a pharmaceutically acceptable salt thereof, or hydrates thereof, or mixtures thereof; orii) sodium bicarbonate,to a subject in need of treatment or prevention for nocturnal enuresis.25. The method according to claim 23 , wherein the agent is a medicine.26. The method according to claim 24 , wherein the agent is a medicine.27. The method according to claim 23 , wherein the agent is administered in combination with a V2 receptor agonist.28. The method according to claim 24 , wherein the agent is administered in combination with a V2 receptor agonist.29. The method according to claim 23 , which is designed so that citric acid or a pharmaceutically acceptable salt thereof claim 23 , or hydrates thereof are administered in an amount that improves acidic urine in gout or hyperuricemia.30. The method according to claim 24 , which is designed so that citric acid or a pharmaceutically acceptable salt thereof claim 24 , or hydrates thereof are administered in an amount that improves acidic urine in gout or hyperuricemia.31. The method according to claim 23 , wherein the agent is administered to a patient with chronic kidney disease.32. The method according to claim 24 , wherein the agent ...

Composition and Methods for Treatment of Bladder Dysfunction

A nutritional supplement and method of treating or preventing urogenital system disorders including urinary incontinence, overactive bladder, enuresis, benign prostatic hyperplasia, nocturia, cystitis, and urinary calculi, without unwanted side effects. The supplement comprises vitamin D3, nitric oxide precursor, pumpkin seed extract and prebiotic fiber in a particular composition.

Combinations of acetylcholinesterase inhibitors and muscarinic agonists and methods of use thereof

A method of treating one or more symptoms associated with underactive bladder in a patient suffering therefrom by administering to the patient a therapeutically effective amount of an acetylcholinesterase inhibitor (AChEI) and an amount of a muscarinic receptor agonist effective to reduce the volume of post void residual in the patient obtained by treatment with the AChEI alone.

FOAM-FORMING COMPOSITIONS FOR DELIVERING AN ACTIVE TO A BODY CAVITY

Provided is a foam-forming formulation and method of administrating a medically active or cosmetic or reliving compound to the skin, to a would or to a body cavity. The foam-forming formulation contains monoglyceride crystals, a hydrophilic blowing agent in an amount to blow the foam-forming composition and form a foam, water, and a medical, cosmetic or reliving compound. The foam-forming composition is suitable application to skin, wounds and body cavities when blown to form the foam and the foam melts at a body temperature to release the content. Also provided is a foam-forming composition vehicle for delivering an active agent. 1. A foam-forming pharmaceutical composition for delivering active agents to the surface of the body or to body cavities comprising:water;solid lipid crystals suspended in the water, the solid lipid crystals having a melting point in their crystalline state of less than 37° C. and more than 25° C.; anda nonlipophillic propellant for blowing the composition and forming a foam, wherein the solid lipid crystals being present in an amount to support a foam when the composition is blown by the propellant, and the composition is adapted for application to the body cavity when blown so that when the foam is heated by the body cavity the foam degrades at the melting point and releases contents of the foam to tissues in the body cavity.2. The foam-forming composition according to claim 1 , wherein the lipid crystals are selected from the group consisting of phospholipids claim 1 , mono or di acylglycerides claim 1 , lipid esters of lactic acid claim 1 , and n-acetylethanolamides.3. The foam-forming composition according to claim 1 , wherein the lipids being present in an amount of at least 0.5% and at the most 28% by weight based on the weight of composition.4. The foam-forming composition according to claim 1 , comprising an effective amount of a medically active claim 1 , cosmetic or relieving agent.5. The foam-forming composition according to ...

Compositions comprising il-2 fusion proteins and methods for treating neoplasia

The invention provides methods of treating neoplasia, for example bladder cancer, by administering an IL-2 fusion protein and one or more therapeutic agents, where the IL-2 fusion protein does not necessarily have to target the neoplasia.

Conjugates for treating diseases caused by psma expressing cells

The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

Chondroitin sulfate derivative and agent for treating bladder diseases

Provided is a compound in which a group derived from chondroitin sulfate and a group derived from a steroid are covalently bonded together via a spacer represented by general formula (I). In the formula, m represents an integer of 0 or 1. Here, if m=0, R 1 represents a group selected from the group consisting of electron-donating groups and steric hindrance groups. If m=1, R 1 represents a group selected from the group consisting of a hydrogen atom, electron-donating groups and steric hindrance groups. —HN—(CH 2 ) m —CHR 1 —CO—  (I)

Drug treatment of overactive bladder

Provided are methods of treating an overactive bladder in a patient which include: administering a Myosin II ATPase inhibitor compound; or administering an X group and Y group substituted (3a-hydroxy-1-phenyl-1,2,3,3a-tetrahydro-4H-pyrrolo[2,3b] quinolin-4-one) compound of Formula 1 or administering an X group and Y group substituted (3a-hydroxy-1-phenyl-1,2,3,3a-tetrahydro-4H-pyrrolo[2,3b] quinolin-4-one) compound of Formula II; or administering pharmaceutically-acceptable salts, racemic mixtures, enantiomers, or prodrugs of said compounds, useful in their active form as inhibitors of Myosin II ATPase related to over-active bladder. Optionally the compounds are administered intervesicularly into the bladder. Also provided are pharmaceutical compositions comprising said compounds useful in their active form, as methods of treating a patient suffering from an over-active bladder related to inhibition of Myosin II ATPase. These pharmaceutical compositions also may contain one or more other compounds useful in their active form, as methods of treating a patient suffering from an over-active bladder.

TREATMENT OF SIDE EFFECTS OF BOTULINUM THERAPIES

The disclosure is directed to the use of a pharmaceutical product to accelerate recovery of adverse side-effects resulting from neurotoxin therapy for bladder dysfunction. 1. A method of mitigating the side-effects of botulinum toxin therapy in a patient in need thereof , wherein the patient has received botulin toxin for treating overactive bladder or urinary urgency , the method comprising locally administering one or more of anticholinesterases to a bladder muscle denervated by a botulinum toxin.2. The method of claim 1 , wherein the botulinum toxin is botulinum toxin type A.3. The method of claim 1 , wherein the one or more anticholinesterases is selected from the group consisting of neostigmine claim 1 , edrophonium claim 1 , pyridostigmine claim 1 , physostigmine claim 1 , rivastigmine claim 1 , donepezil claim 1 , galantamine claim 1 , and combinations thereof.3. The method of claim 1 , wherein the one or more anticholinesterases is selected from the group consisting of neostigmine claim 1 , edrophonium claim 1 , pyridostigmine claim 1 , physostigmine claim 1 , rivastigmine and combinations thereof.4. The method claim 1 , wherein the anticholinesterase is pyridostigmine.5. The method claim 1 , wherein the anticholinesterase is rivastigmine.7. The method of claim 1 , wherein the one or more anticholinesterases is a reversible anticholinesterase having one or more of groups selected from carbamate claim 1 , tertiary ammonium claim 1 , and quaternary ammonium claim 1 ,8. The method of any of - claim 1 , wherein the locally administering is by intradetrusor injection into the bladder muscle.9. The method of any of - claim 1 , wherein the locally administering is by intravesical instillation into the bladder or the bladder muscle.10. The method of claim 9 , wherein the intravesical instillation extends the dwell time of the one or more anticholinesterases within the bladder.11. The method of claim 10 , wherein the dwell time is extended by means of a medical ...

Diagnosis and treatment of motility disorders of the gut and bladder, and of fibromyalgia

Described herein are methods and systems for the detection of anti-vinculin antibodies, for determining a presence or likely presence of a gastrointestinal motility disorder, bladder motility disorder, or fibromyalgia. Further provided are methods of selecting and/or administering a therapy based on the presence or absence of anti-vinculin anti bodies.

Administration of monobactam for the treatment of urinary tract infection

Methods for the treatment of a bacterial infection such as a urinary tract infection are described. In particular, methods for treatment of a bacterial infection, such as a urinary tract infection comprising administration of LYS228 are disclosed.

Neoadjuvant therapy for bladder cancer

This invention relates to a neoadjuvant therapy for bladder cancer in bladder cancer patients who are scheduled for a cystectomy and methods of carrying out such a neoadjuvant therapy. In particular the invention relates to a composition comprising hexyl 5-ALA ester (HAL) or a pharmaceutically acceptable salt thereof for use in a neoadjuvant therapy for bladder cancer in a bladder cancer patient who is scheduled for a cystectomy, the therapy comprises instilling said composition into the bladder of said patient and exposing the inside of said bladder to light.

Multi-unit drug delivery devices and methods

Implantable drug delivery devices include a housing defining a reservoir, a first unit within the reservoir, and a second unit within the reservoir. The first unit contains a drug and the second unit contains a functional agent that facilitates release of the drug. Intravesical drug delivery devices include a housing portion containing a drug formulation and a housing portion containing an excipient, and are configured to release the drug according to a first release profile and the excipient according to a second release profile. Methods include inserting any of these devices into a patient and releasing drug from the device.

Cd73 blockade

This disclosure relates to antibodies that bind an epitope present on CD73 expressed at the surface of cells, including tumor cells, and that inhibit the enzymatic (ecto-5′ nucleotidase) activity of the CD73 enzyme. Such agents can be used for the treatment of diseases such as cancers.

Organic compounds

AGENT FOR TREATING NOCTURNAL POLLAKIURIA

[Problem] To provide a novel therapeutic agent for nocturnal pollakiuria. 13-. (canceled)4. A method for treating nocturnal pollakiuria , comprising administering to a subject in need thereof (6S)—N-[4-({(2S ,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4 ,6 ,7 ,8-tetrahydropyrrolo[1 ,2-a]pyrimidine-6-carboxamide in an effective amount to treat nocturnal pollakiuria.5. The method according to claim 4 , wherein the (6S)—N-[4-({(2S claim 4 ,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4 claim 4 ,6 claim 4 ,7 claim 4 ,8-tetrahydropyrrolo[1 claim 4 ,2-a]pyrimidine-6-carboxamide is administered to a subject belonging to a group of patients whose average value of frequency of urination at night is 1.0 or more and 1.8 or less.6. The method according to claim 4 , wherein the (6S)—N-[4-({(2S claim 4 ,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4 claim 4 ,6 claim 4 ,7 claim 4 ,8-tetrahydropyrrolo[1 claim 4 ,2-a]pyrimidine-6-carboxamide is administered orally once daily at a daily dosage of 50 mg or more and 100 mg or less.7. The method according to claim 6 , wherein the (6S)—N-[4-({(2S claim 6 ,5R)-5-[(R)-hydroxy(phenyl)methyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4 claim 6 ,6 claim 6 ,7 claim 6 ,8-tetrahydropyrrolo[1 claim 6 ,2-a]pyrimidine-6-carboxamide is administered to a subject belonging to a group of patients whose average value of frequency of urination at night is 1.0 or more and 1.8 or less. The present invention relates to an agent for treating nocturnal pollakiuria.Nocturnal pollakiuria is a complaint that one has to wake up one or more times for urinating at night, and is one of the symptoms (urinary urgency, pollakiuria, nocturnal pollakiuria, and urge urinary incontinence) resulting from overactive bladder (OAB). Nocturnal pollakiuria causes nocturnal awakening and is closely associated with sleep disorders, thereby reducing QOL remarkably (Non Patent Literature 1).Desmopressin, which is ...

Stabilized pharmaceutical compositions comprising fesoterodine

The present application relates to a pharmaceutical composition comprising fesoterodine or a pharmaceutically acceptable salt or solvate thereof and a stabilizer selected from the group consisting of xylitol, sorbitol, polydextrose, isomalt and dextrose.

抗前列腺特异性膜抗原(psma)的人单克隆抗体

本发明公开了与PSMA结合的分离的人单克隆抗体，并且涉及相关的抗体为基础的组合物和分子。通过V－D－J重组和同种型转换在能产生人单克隆抗体的多种同种型的非人转基因动物例如转基因小鼠中能产生所述人抗体。还公开了含有所述人抗体的药物组合物，非人转基因动物，和产生人抗体的杂交瘤，以及使用所述人抗体的治疗和诊断方法。

Human monoclonal antibodies to prostate specific membrane antigen (PSMA)

Conjugates for treating diseases caused by PSMA expressing cells

The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

Conjugates for treating diseases caused by PSMA expressing cells

The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

Conjugates for treating diseases caused by PSMA expressing cells

The invention described herein pertains to the diagnosis, imaging, and/or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and/or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

Modified human IGF-1R antibodies.

Combination therapy methods for treatment of proliferative diseases

métodos de terapia combinada para tratamento de doenças proliferativas. a presente invenção refere-se a métodos de terapia combinada para tratamento de uma doença proliferativa (tal como câncer) compreendendo uma primeira terapia compreendendo administração a um indivíduo de uma quantidade eficaz de uma taxano em uma composição em nanopartícula e uma segunda terapia a qual pode incluir administração de uma quantidade eficaz de pelo menos um outro agente que modifica a epigenética em uma célula. Combination therapy methods for treatment of proliferative diseases. The present invention relates to combination therapy methods for treating a proliferative disease (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition and a second therapy which may be used. include administering an effective amount of at least one other epigenetic modifying agent to a cell.

CONJUGATES FOR DELIVERY OF MEDICINES AND METHODS OF TREATMENT OF DISEASES CAUSED BY CELLS EXPRESSING PSMA

Настоящее изобретение, описанное в настоящем документе, относится к диагностике, визуализации и/или лечению популяций патогенных клеток. В частности, настоящее изобретение, описанное в настоящем документе, относится к диагностике, визуализации и/или лечению заболеваний, вызванных клетками, экспрессирующими PSMA, такими как клетки рака предстательной железы, с применением соединений, способных нацеливаться на клетки, экспрессирующие PSMA. The present invention described herein relates to the diagnosis, visualization, and / or treatment of populations of pathogenic cells. In particular, the present invention described herein relates to the diagnosis, imaging and / or treatment of diseases caused by cells expressing PSMA, such as prostate cancer cells, using compounds capable of targeting cells expressing PSMA.

NEW OSSIALCHILPIPERAZINE