ТИОЭФИРЗАМЕЩЕННЫЕ ИМИДАЗОХИНОЛИНЫ

Описываются имидазохинолиновые производные формулы (I) где Х представляет собой алкил, -CHR3-; Z представляет собой -S-, -SO- или -SO2- группу; R1 выбран из группы, включающей алкил и незамещенный фенил; R2 выбран из группы, включающей атом водорода; алкил; алкил-Y-алкил; каждый R3 представляет собой атом водорода; Y представляет собой -О-; n равен 0. Описывается также тетраимидазохинолиновое производное, фармацевтические композиции на их основе, способ стимулирования биосинтеза цитокина в организме животного. Предлагаемые в изобретении соединения и композиции могут вызывать биосинтез различных цитокинов и в связи с этим использоваться для лечения различных болезней, включая вирусные и опухолевые заболевания. 9 н. и 11 з.п. ф-лы, 1 табл.

МОНОКЛОНАЛЬНОЕ АНТИТЕЛО ПРОТИВ ИНТЕРЛЕЙКИНА-31

Изобретение относится к биотехнологии. Предложено выделенное антитело, которое специфически связывается по меньшей мере с одним из собачьего интерлейкина-31 (IL-31) или кошачьего IL-31. Такие антитела могут быть представлены в форме диагностических и/или ветеринарных композиций, полезных для лечения сопровождающегося зудом и/или аллергического состояния у собак или кошек. Изобретение расширяет арсенал средств лечения животных. 9 н. и 18 з.п. ф-лы, 23 ил., 5 табл., 12 пр.

ПРОИЗВОДНЫЕ ХИНАЗОЛИНА

Изобретение относится к новым соединениям, представленным нижеследующей формулой (I), или их фармакологически приемлемым солям, обладающим противозудным действием. Соединения настоящего изобретения могут быть использованы как противозудное средство при атопическом заболевании, таком как атопический дерматит, в случае, когда стероидное лекарственное средство является неэффективным. В формуле (I) ! ! R представляет собой С1-6алкокси, необязательно замещенный метокси, или амино монозамещенный С1-6алкилом, где группа R-C(=O)- присоединена в мета- или пара-положении. 5 н. и 16 з.п. ф-лы, 15 ил., 4 табл.

ПРИМЕНЕНИЕ КОНЦЕНТРАТА КОБЫЛЬЕГО МОЛОКА, ВЫСУШЕННОГО НА БИОЛОГИЧЕСКИ ИНЕРТНОЙ, ВЫСОКОДИСПЕРСНОЙ МАТРИЦЕ

Изобретение относится к области медицины. Изобретение характеризуется тем, что концентрат кобыльего молока, высушенного при температуре от 10 до 50°С при давлении от 1 до 50 мбар, на биологически инертной, высокодисперсной матрице, которой является высокодисперсный диоксид кремния, применяют для получения препарата для орального приема при лечении заболеваний нейродермита и псориаза. Препарат дополнительно содержит незаменимые аминокислоты, гидрокарбонат, калий, карбонат, цитрат, кальций, магний, витамин С, витамин Е, ниацин, цинк, железо, бета-каротин, пантотеновую кислоту, марганец, витамин В6, В2, В1, В12, медь, натрий, биотин, фолиевую кислоту, молибден, селен, ксантан, фруктозу, лимонную кислоту, или, по меньшей мере, из двух таких веществ. Изобретение обеспечивает применение концентрата кобыльего молока орально для лечения нейродермита и псориаза, стоек при хранении и содержит высококачественные компоненты в концентрированной форме, что обеспечивает его эффективность. 5 з.п. ф-лы, ...

ПИРАЗОЛЬНЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ СОЕДИНЕНИЙ-АНТАГОНИСТОВ H4

Изобретение относится к соединению формулы (1) или его фармацевтически приемлемой соли, которые обладают активностью антагониста рецептора Н4 и могут найти применение для лечения связанных с такой активностью заболеваний. В формуле (1) X представляет собой СН или N; n равно 2; R1 выбран из Н или С1-3 алкила; R2 представляет собой Н или метил и А представляет собой необязательно замещенное пиразольное кольцо, которое связано с кольцом, содержащим X, углерод-углеродной связью, где (i) А представляет собой необязательно замещенное пиразольное кольцо, выбранное из указанных ниже, где R3 выбран из Н; C1-6 неароматической углеводородной группы, выбранной из алкила, необязательно замещенного 1-6 атомами фтора, или циклоалкила, необязательно замещенного 1-6 атомами фтора; (CH2)mR6, где m равно от 1 до 3 и R6 выбран из CN, ОН, С1-С3 алкокси и необязательно замещенного 4-6-членного насыщенного гетероциклического кольца, содержащего 1 гетероатом, выбранный из О и N, где необязательный заместитель ...

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.

Применение антагониста рецептора NK-1 серлопитанта при зуде

Группа изобретений относится к медицине и касается лечения зуда у пациента, который нуждается в таком лечении. Указанное лечение включает стадию, на которой вводят пациенту терапевтически эффективное количество 3-[(3aR,4R,5S,7aS)-5-[(1R)-1-[3,5-бис(трифторметил)фенил]этокси]-4-(4-фторфенил)-1,3,3а,4,5,6,7,7а-октагидроизоиндол-2-ил]циклопент-2-ен-1-она (серлопитанта) или его фармацевтически приемлемой соли, сольвата или полиморфа. Также предложен способ введения серлопитанта пациенту. Группа изобретение обеспечивает лечение зуда разного генеза у пациента, при этом разработанная схема введения препарата обеспечивает продолжительный противозудный эффект. 2 н. и 32 з.п. ф-лы, 4 ил., 7 табл., 6 пр.

МОДУЛЯТОРЫ СВЯЗАННЫХ С MAS РЕЦЕПТОРОВ G-БЕЛКА X4 И СВЯЗАННЫЕ С НИМИ ПРОДУКТЫ И СПОСОБЫ

Изобретение относится к соединению, имеющему одну из следующих структур, или его фармацевтически приемлемой соли: Соединение № Структура 1-55 1-78 5-1 4-10 1-65 4-11 1-58 1-56 9-1 1-82 1-85 1-29 1-101 2-3 1-103 1-112 4-7 11-1 Изобретение также относится к фармацевтической композиции и способу лечения MRGPR X4-зависимых состояний на основе указанного соединения. Технический результат: получено новое соединение и фармацевтическая композиция на его основе, которые могут найти применение в медицине для лечения MRGPR X4-опосредованных заболеваний. 4 н. и 35 з.п. ф-лы, 7 ил., 70 табл., 70 пр.

ПРОИЗВОДНОЕ ХИНАЗОЛИНА И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ

Настоящее изобретение относится к производному хиназолина, представленному общей формулой [1], или его фармацевтически приемлемой соли ! , где R1-R6 имеют значения, представленные в п.1 формулы, за исключением соединения, в котором R5 представляет собой водород, и R6 представляет собой -NH2. Изобретение также относится к фармацевтической композиции, обладающей активностью противозудного средства, содержащей в качестве активного ингредиента указанное выше производное хиназолина или его фармацевтически приемлемую соль. Технический результат - получение нового производного хиназолина с меньшим раздражающим действием на кожу и превосходным действием существенного подавления поведения расчесывания, а также противозудного средства, содержащего такое производное хиназолина в качестве активного ингредиента. 2 н. и 7 з.п. ф-лы, 250 пр., 7 табл.

СПОСОБ ИДЕНТИФИКАЦИИ ПРОТИВОЗУДНОГО ЭФФЕКТА АНТИДЕПРЕССАНТА

Изобретение относится к клинической фармакологии и касается способа идентификации антидепрессанта, обладающего противозудным эффектом, с использованием компьютерной программы для расчета моделей химических структур, при котором осуществляют визуальный анализ всех устойчивых конформеров молекулы антидепрессанта и при обнаружении хотя бы одного устойчивого конформера, содержащего структуру из двух взаимоцентрированных ароматических колец, плоскости которых способны ориентироваться под углом 120° по отношению друг к другу, идентифицируют антидепрессант, обладающий противозудным эффектом, а также прогнозируют применение антидепрессанта, идентифицированного вышеописанным способом, для лечения зуда. Технический результат: идентификация противозудного эффекта антидепрессантов. 2 н.п. ф-лы, 1 табл.

БЕНЗИМИДАЗОЛЬНЫЕ ПРОИЗВОДНЫЕ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Настоящее изобретение относится к новым производным бензимидазола общей формулы (I) или к его фармакологически приемлемым солям, где R' представляет собой С6-арильную группу, которая может быть замещенной 1-3 группами, независимо выбранными из группы заместителей (а), или гетероциклическую группу, которая представляет пиридил, дигидробензофуранил, 1,3-бензодиоксолил, тетрагидропиранил, тетрагидрофуранил, которая может быть замещенной 1-3 группами, независимо выбранными из группы заместителей (а), R2 представляет собой C1-С6 алкильную группу, R3 представляет собой С6-арильную группу, которая может быть замещенной 1-2 группами, независимо выбранными из группы заместителей (a), Q представляет собой группу, представленную формулой =СН-, или атом азота и группа заместителей (а) представляет собой группу, состоящую из атома галогена, C1-С6 алкильной группы, C1-С6 галогенированной алкильной группы, карбоксильной группы, C1-C7 алкилкарбонильной группы, C2-C7 алкоксикарбонильной группы, C1-С6 алкоксигруппы ...

СОЛЬ ПРИСОЕДИНЕНИЯ КИСЛОТЫ СОЕДИНЕНИЯ, ИНГИБИРУЮЩЕГО Trk

Изобретение относится к новым соединениям - пара-толуолсульфонату и ди(пара-толуолсульфонату 1-{2-[4-(2-амино-5-хлор-3-пиридинил)фенокси]-5-пиримидинил}-3-[2-(метилсульфонил)-5-(трифторметил)фенил]мочевины и их кристаллическим формам. Соединения обладают Trk ингибирующей активностью, устойчиво ингибируют повышенную проницаемость сосудов NGF, не характеризуются взаимодействием с лекарственными средствами и обладают превосходной растворимостью и всасываемостью по сравнению со свободными основаниями. Соединения могут быть использованы при лечении различных заболеваний связанных с Trk, таких как боль, зуд, расстройство нижних мочевыводящих путей, астма, аллергический ринит, воспалительное заболевание кишечника, болезнь Шагаса, злокачественная опухоль и т.д. Пара-толуолсульфонат 1-{2-[4-(2-амино-5-хлор-3-пиридинил)фенокси]-5-пиримидинил}-3-[2-(метилсульфонил)-5-(трифторметил)фенил]мочевины может представлять собой кристалл, который характеризуется порошковой рентгеновской дифрактограммой, содержащей ...

ПРОИЗВОДНЫЕ МОЧЕВИНЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Изобретение относится к новым производным мочевины общей формулы (I) и их фармацевтически приемлемым солям, где А представляет собой -СН- или атом азота, R1 представляет собой С3-10 алкил, С3-10циклоалкил, С3-10циклоалкил-С1-10алкил, 6-членный азотсодержащий гетероциклил, 6-членный азотсодержащий гетероциклил-С1-10 алкил, фенил, фенил-С1-10алкил, 5-10-членный гетероарил или 5-10-членный гетероарил-С1-10алкил и др.; R2 представляет собой водород, С1-6алкил, С0-2 алкил-С3-10циклоалкил, С0-2алкил-фенил, С3-10циклоалкил-С0-2алкил или фенил-С0-2алкил; R5 представляет собой C1-6алкил, С3 -10циклоалкил, 6-членный азотсодержащий гетероциклил и др.; L1 представляет собой -S-, -S(О)-, -S(O)2, -С(O)-, -N(Rc)-, -CH2- и др.; L2 представляет собой ковалентную связь, -О-, -С(O)-, -ОС(O)-, -N(Rc)- и др.; W представляет собой О или S; Z представляет собой -C(O)ORd; Rc, Rd и Re представляют собой водород или алкил; Rb представляет собой -ORe, -NO2, галоген, -CN, -CF3, C1-6алкил; р представляет собой целое ...

АЛЬФА-ЗАМЕЩЕННЫЕ ОМЕГА-3 ЛИПИДЫ, КОТОРЫЕ ЯВЛЯЮТСЯ АКТИВАТОРАМИ ИЛИ МОДУЛЯТОРАМИ РЕЦЕПТОРА, АКТИВИРУЕМОГО ПРОЛИФЕРАТОРАМИ ПЕРОКСИСОМ (PPAR)

Изобретение относится к новым омега-3 липидным соединениям общей формулы (I) или к их любой фармацевтически приемлемой соли, где в формуле (I): Rи Rявляются одинаковыми или разными и могут быть выбраны из группы заместителей, состоящей из атома водорода, гидроксигруппы, С-Салкильной группы, атома галогена, C-Салкоксигруппы, С-Салкилтиогруппы, С-Салкоксикарбонильной группы, карбоксигруппы, аминогруппы и С-Салкиламиногруппы; Х представляет собой карбоновую кислоту или ее карбоксилат, выбранный из этилкарбоксилата, метилкарбоксилата, н-пропилкарбоксилата, изопропилкарбоксилата, н-бутилкарбоксилата, втор-бутилкарбоксилата или н-гексилкарбоксилата, карбоновую кислоту в форме триглицерида, диглицерида, 1-моноглицерида или 2-моноглицерида, или карбоксамид, выбранный из первичного карбоксамида, N-метилкарбоксамида, N,N-диметилкарбоксамида, N-этилкарбоксамида или N,N-диэтилкарбоксамида; и Y является С-Салкеном с двумя или более двойными связями, имеющими Е- и/или Z-конфигурацию. Также описаны фармацевтические ...

КОМПОЗИЦИЯ ДЛЯ КОЖИ

Изобретение относится к композиции для кожи, включающей липофильные и гидрофильные компоненты, для нанесения на кожу, отличающейся тем, что существует в виде двухфазной системы и посредством этого способна создавать в коже полупроницаемую мембрану, причем указанный липофильный компонент включает жирную кислоту, содержащую 14-20 атомов углерода или смесь любых указанных жирных кислот и диметилполисилоксан, и указанный гидрофильный компонент включает триэтаноламин, монопропиленгликоль, поливинилпирролидон, и один или более компонентов, выбранных из глицерина, сорбита, полиэтиленгликоля или их смеси, а также к способу получения описанной выше композиции для кожи, который отличается тем, что в отдельном контейнере растворяют в воде липофильные компоненты, подлежащие объединению с гидрофильными компонентами, которые смешивают и которыми проводят реакцию в другом сосуде, и к способу облегчения или предупреждения зуда или любого другого раздражения кожи. Технический результат: композиция для кожи ...

ПРОИЗВОДНЫЕ АМИДА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

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... 1. Производное триазаспиро[5.5]ундекана формулы (I) где R1 имеет формулу (1) или (2) где G представляет связь, С1-4 алкилен, С2-4 алкенилен, или -СО-; кольцо А представляет собой (1) С5-10-членное моно- или бикарбоциклическое кольцо или (2) 5-10-членный моно- или бициклический гетероцикл, содержащий 1-2 атома азота и/или 1-2 атома кислорода; R6 представляет (1) С1-4алкил, (2) галоген, (3) нитрил, (4) трифторметил, (5) -OR8, (6) -SR9, (7) -NR10R11, (8) -COOR12, (9) -CONR13R14, (10) -SO2NR15R16, (11) NR17SO2R18, (12) -S(O)R19, (13) -SO2R20, (14) -N(SO2R21)2, (15) С1-4алкил, замещенный заместителем, выбранным из (а) -OR8, (b) -NR10R11, и (с) Сус 1, или (16) -NR27COR28, где R8-R17 каждый независимо представляет (1) водород, (2) С1-4алкил, (3) Сус 1, (4) -OR22, и (5) C1-4алкил, замещенный заместителем, выбранным из (a) -OR22, (b) -NR23R24, (с) -COOR25 и (d) Сус 1, или R10 и R11, R13 и R14 или R15 и R16, каждый независимо, вместе с атомом азота, к которому они присоединены, образуют 5-6-членный ...

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 ...

ИНГИБИРОВАНИЕ STAT-1

Применение двунитевых ДНК-олигонуклеотидов, однонитевых антисмысловых олигонуклеотидов, антисмысловых векторов экспрессии или двунитевых олигонуклеотидов РНК-интерференции, пригодных для ингибирования активности STAT-1, для изготовления лекарства для предотвращения или терапии сердечно-сосудистых осложнений, таких, например, как рестеноз после чрезкожной ангиопластики или стеноз венозного шунта, реакции трансплантат против хозяина, ишемических/реперфузионных повреждений при хирургических операциях и трансплантации органов, соответственно, иммунологических реакций гиперчувствительности, в частности аллергического ринита, лекарственных и пищевых аллергий, в частности крапивницы и глютеновой болезни (спру), контактной экземы и комплексных иммунных заболеваний, в частности альвеолита, артрита, гломерулонефрита и аллергического васкулита, воспалительных хондро- и остеопатий, в частности артроза, подагры, остита и остеомиелита, полиневрита, как острого, так и подострого соответственно, инфекционного ...

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4-АМИНОЦИКЛОГЕКСАНОЛА

... 1. Замещенные производные 4-аминоциклогексанола общей формулы I в которой R1 и R2 независимо друг от друга обозначают Н или С1-8алкил либо С3-8циклоалкил, каждый из которых является насыщенным либо ненасыщенным, разветвленным либо неразветвленным, одно- либо многозамещенным или незамещенным, арил либо гетероарил, каждый из которых является одно- либо многозамещенным или незамещенным, или присоединенный через C1-3алкилен арил, С3-8циклоалкил либо гетероарил, каждый из которых является одно- либо многозамещенным или незамещенным, при этом R1 и R2 оба не могут одновременно обозначать Н, или остатки R1 и R2 совместно образуют кольцо и обозначают СН2СН2ОСН2СН2, CH2CH2NR5CH2CH2 или (CH2)3-6, где R5 обозначает Н или С1-8алкил либо С3-8циклоалкил, каждый из которых является насыщенным либо ненасыщенным, разветвленным либо неразветвленным, одно- либо многозамещенным или незамещенным, арил либо гетероарил, каждый из которых является одно- либо многозамещенным или незамещенным, или присоединенный ...

СОЛИ ЗАМЕЩЕННЫХ ПРОИЗВОДНЫХ 1,2,3,4-ТЕТРАГИДРОХИНОЛИН-2- КАРБОНОВОЙ КИСЛОТЫ

... 1. Замещенные производные 1,2,3,4-тетрагидрохинолин-2-карбоновой кислоты общей формулы I в виде их физиологически совместимых солей с катионами, соответственно основаниями, 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, при этом R1 и R2 совместно являются в каждом случае одно- или многозамещенными либо незамещенными и образуют группу -(СН2)n-, где n обозначает число от 3 до 10, -СН=СН-СН2-, -СН2-СН=СН-, -СН=СН-СН2-СН2-, -СН2-СН2-СН=СН-, -СН2-СН=СН-СН2-, -СН2-СН=СН-СН2-СН2-, -СН2-СН2-СН=СН-СН2-, -СН2-СН2-СН=СН-СН2 -СН2-, -O-СН2-СН2-, -СН2-СН2-O-, -O-СН2-СН2-СН2-, -СН2-СН2-СН2-O-, -СН2-O-СН2-, -СН2-СН2-O-СН2-, -CH2-O-CH2-CH2-, где X обозначает О или S; R3 обозначает Н или С1-С18алкил, С2-С18алкенил либо С2-С18алкинил, каждый из которых является разветвленным или неразветвленным, одно- или многозамещенным либо незамещенным ...

ПРОИЗВОДНЫЕ ПИПЕРИДИНА ПОЛЕЗНЫЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРОВ ХЕМОКИНОВ

... 1. Соединение формулы (I) где Т представляет собой С(O) или S(O)2; W представляет собой С(O) или S(O)2; Х представляет собой СН2, О или NH; Y представляет собой CR5 или N; R1 представляет собой возможно замещенный арил или возможно замещенный гетероциклил; R2 представляет собой водород или C1-6алкил; R3 представляет собой водород или возможно замещенный C1-6алкил; R4 представляет собой алкил, возможно замещенный арил, возможно замещенный аралкил или возможно замещенный гетероциклил; R5 представляет собой водород или C1-6алкил; где вышеупомянутые арильные и гетероциклильные группировки возможно замещены галогеном, циано, нитро, гидрокси, оксо, S(O)pR25, OC(O)NR6R7, NR8R9, NR10 C(O)R11, NR12C(O)NR13R14, S(O)2NR15R16, NR17S(O)2R18, C(O)NR19R20, C(O)R21, CO2R22, NR23CO2R24, C1-6алкилом, CF3, группировкой C1-6алкокси(C1-6)алкил, C1-6алкокси, OCF3, C1-6алкокси(C1-6)алкокси, C2-6алкилтио, C2-6алкенилом, C2-6алкинилом, C3-10циклоалкилом (который сам возможно замещен C1-4алкилом или оксо), метилендиокси ...

ЗАМЕЩЕННЫЕ АЗЕПИНО[4,3-b]ИНДОЛЫ, ФАРМАЦЕВТИЧЕСКАЯКОМПОЗИЦИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

Изобретение относится к новым гидрированным азепино[4,3-b]индолам общей формулы 1, их рацематам, оптическим изомерам, геометрическим изомерам, их фармацевтически приемлемым солям и/или гидратам, которые обладают нейропротекторными, когнитивно-стимулирующими и антигистаминными свойствами и могут найти применение при лечении различных неврологических расстройств, аллергических и аутоиммунных заболеваний, например, для улучшения памяти. В общей формуле 1 пунктирная линия с сопровождающей ее сплошной линией представляет собой одинарную или двойную связь; R1 и R2 независимо друг от друга представляют собой заместители аминогруппы, выбранные из водорода; возможно замещенного C1-C8-алкила, возможно замещенного арилом, 5-6-членным азагетероциклилом; C1-C8-алкоксикарбонила; возможно замещенного фенила; возможно замещенных карбониламино или тиокарбониламино; замещенного ацила; C1-C8-алкилсульфонила; возможно замещенного арилсульфонила; при этом заместители в указанных R1 и R2 независимо выбираются ...

ПРОИЗВОДНЫЕ НИКОТИНАМИДА, ПОЛЕЗНЫЕ В КАЧЕСТВЕ Р38-ИНГИБИТОРОВ

... 1. Соединение формулы (I) где R1 выбран из водорода, С1-6алкила, возможно замещенного группами в количестве до трех включительно, выбранными из С1-6алкокси, галогена и гидрокси, С2-6алкенила, С3-7 циклоалкила, возможно замещенного одной или более чем одной С1-6алкильной группой, фенила, возможно замещенного группами в количестве до трех включительно, выбранными из R5 и R6, и гетероарила, возможно замещенного группами в количестве до трех включительно, выбранными из R5 и R6; R2 выбран из водорода, С1-6алкила и -(CH2)q-C3-7циклоалкил, возможно замещенного одной или более чем одной С1-6алкильной группой, или (СН2)mR1 и R2 совместно с атомом азота, к которому они присоединены, образуют (четырех-шести)членное гетероциклическое кольцо, возможно замещенное С1-6алкильными группами в количестве до трех включительно; R3 представляет собой хлоро или метил; R4 представляет собой группу -NH-CO-R7 или -CO-NH-(CH2)q -R8; R5 выбран из С1-6алкила, С1-6алкокси, -{СН2)q-С3-7циклоалкил, возможно замещенного ...

СРЕДСТВО ДЛЯ УХОДА ЗА КОЖЕЙ, ВОЛОСАМИ, НОГТЯМИ, ПОЛОСТЬЮ РТА ЧЕЛОВЕКА, УЛУЧШАЮЩЕЕ ИХ СОСТОЯНИЕ И ВНЕШНИЙ ВИД

... 1. Средство для ухода за кожей, волосами, ногтями, полостью рта человека, улучшающее их состояние и внешний вид, выбранное из группы: парфюмерное средство, косметическое средство, гигиеническое средство, характеризующееся тем, что содержит легкую очищенную воду в виде компонента или основы, при этом содержание1 H216O в легкой очищенной воде составляет не менее 997,13 г/кг от общего количества Н2О, а суммарное содержание1Н217О,1H218O,1HD16O,1HD17O,1HD18O, D216O, D217O, D218O в легкой очищенной воде составляет не более 2,87 г/кг от общего количества Н2O, и приемлемые парфюмерные компоненты и/или основу, и/или косметические компоненты и/или основу, и/или гигиенические компоненты и/или основу, и/или активные субстанции. 2.Средство, по п.1, отличающееся тем, что содержание1Н216О в легкой очищенной воде составляет не менее 997,36 г/кг от общего количества Н2О, при этом суммарное количество1H217O,1H218O,1HD16О,1HD17O,1HD18O, D216O, D217O, D218O в легкой очищенной воде составляет не более 2,64 ...

ПРИМЕНЕНИЕ ТВЕРДОЙ ПЕРОРАЛЬНОЙ ДОЗИРОВОЧНОЙ КОМПОЗИЦИИ ПРОЛОНГИРОВАННОГО ДЕЙСТВИЯ ДЛЯ ПРИГОТОВЛЕНИЯ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Предложено применение твердой пероральной дозировочной композиции пролонгированного действия, включающей (а) ядро, содержащее эффективное количество псевдоэфедрина или его соли, (b) первую оболочку, покрывающую ядро и включающую набухающий в воде пленкообразующий нейтральный или катионогенный сополимерный сложный эфир, модификатор пленки и смазывающее вещество, и с) вторую оболочку, покрывающую первую оболочку и включающую эффективное количество деслоратадина, причем количество псевдоэфедрина или его соли достаточно для обеспечения максимума средних геометрических значений концентрации псевдоэфедрина в плазме, от 345 до 365 нг/мл, за время от 7,60 до 8,40 ч, а количество деслоратадина достаточно для обеспечения максимума его средних геометрических значений концентрации в плазме, от 2,10 до 2,45 нг/мл, за период от 4,0 до 4,5 ч после приема разовой дозы указанной композиции, для приготовления лекарственного средства для лечения аллергических и/или воспалительных состояний верхних и нижних ...

СРЕДСТВО НАРУЖНОГО ПРИМЕНЕНИЯ ДЛЯ КОЖИ

... 1. Средство наружного применения для кожи, содержащее в качестве активных компонентов одно или более соединений, выбранных из группы, состоящей из 5-аминолевулиновой кислоты, ее соли и их производного, и соединение железа. ! 2. Средство наружного применения для кожи по п.1, которое дополнительно содержит мочевину в качестве активного компонента. ! 3. Средство наружного применения для кожи по п.1 или 2, в котором соединение железа представляет собой одно или более соединений, выбранных из группы, состоящей из цитрата железа (II), цитрата натрия-железа, цитрата аммония-железа, ацетата железа, оксалата железа, сукцината железа (II), сукцината и цитрата натрия-железа, пирофосфата железа (II), пирофосфата железа (III), гемового железа, декстрана железа, лактата железа, глюконата железа (II), диэтилентриаминпентаацетата натрия-железа, диэтилентриаминпентаацетата аммония-железа, этилендиаминтетраацетата натрия-железа, этилендиаминпентаацетата аммония-железа, триэтилентетраамина железа, дикарбоксиметилглутамата ...

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 ...

РАСТВОРИТЕЛЬ-ИНГРЕДИЕНТ ДЛЯ ПАРФЮМЕРНО-КОСМЕТИЧЕСКИХ СРЕДСТВ, СПОСОБ ЕГО ПОЛУЧЕНИЯ И СПОСОБ ЕГО ХРАНЕНИЯ

Изобретение относится к косметике. Растворитель-ингредиент для парфюмерно-косметических средств представляет собой настой в воде минерала шунгита группы III А. Для получения растворителя шунгит берут дробленым с размером фракции 1,5-20 мм, в соотношении с водой 1:1 по объему, выдерживают их совместно при комнатной температуре в течение 2-3 суток при периодическом перемешивании, после чего сливают настой и сокращают его в объеме путем выпаривания при атмосферном давлении в 2 раза, после чего вновь подвергают контакту с твердым веществом, в качестве которого используют тот же минерал шунгит с размером фракции 40-80 мм в соотношении с настоем 1:1 по объему, выдерживают их совместно при комнатной температуре в течение 4-5 суток без перемешивания и сливают готовый настой. При транспортировке или длительном хранении растворителя в качестве консерванта используют минерал шунгит с размером фракции 15-25 мм, помещенный в тару в количестве 5-10% от объема растворителя.

ПРОИЗВОДНЫЕ ТРИАЗАСПИРО[5.5]УНДЕКАНА И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ЭТИ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ АКТИВНОГО ИНГРИДИЕНТА

... 1. Производное триазаспиро[5.5]ундекана формулы (I) [где R1 представляет (1) водород, (2) C1-18-алкил, (3) С2-18-алкенил, (4) С2-18-алкинил, (5) - COR6, (6) - CONR7R8, (7) - COOR9, (8) - SO2R10, (9) - COCOOR11, (10) - CONR12COR13, (11) Сус 1 или (12) C1-18-алкил, C2-18 -алкенил или С2-18-алкинил, замещенные 1-5 заместителями, необязательно выбранными из (а) галогена, (b) - CONR7R8, (с) - COOR9, (d) - OR14, (e) - SR15, (f) - NR16R17, (g) - NR18COR19, (h) - SO2NR20R21 (i) - OCOR22, (j) - NR23SO2R24 (k) - NR25COOR26, (1) - NR27CONR28R29, (m) Cyc 1, (n) кето или (о) - N(SO2R24)2, (где каждый из R6-R9, R11-R21, R23, R25 и R27-R29 независимо представляет (1) водород, (2) C1-8-алкил, (3) С2-8-алкенил, (4) C2-8-алкинил, (5) Сус 1 или (6) C1-8-алкил, С2-8-алкенил или С2-8-алкинил, замещенные 1-5 заместителями, необязательно выбранными из (а) Сус 1, (b) галогена, (с) - OR30, (d) - SR31, (е) - NR32R33, (f) - COOR34, (g) - CONR35R36, (h) - NR37COR38, (i) - NR39SO2R40 или (j) - N(SO2R40)2, или R7 и ...

Замещенные производные аминометилфенилциклогексана

... 1. Замещенные производные аминометилфенилциклогексана общей формулы I, соответственно Iа, в том числе в виде диастереомеров или энантиомеров, а также их свободного основания или одной из солей, образованных с соответствующей физиологически приемлемой кислотой, прежде всего в виде гидрохлорида, в которых R1 и R1' обозначают один независимо от другого Н, C1-С10алкил, С2-С10алкинил или С2-С10алкенил, каждый из которых является разветвленным или неразветвленным, одно- или многозамещенным либо незамещенным, F, C1, Br, I, NR6R6', NO2, CN, OR6, SR6, OC(O)R6, C(O)OR6, C(O)R6 или C(O)NR6R6', где R6 и R6' обозначают Н, C1 -С10алкил, С2-С10алкенил или С2-С10алкинил, каждый из которых является разветвленным или неразветвленным, одно- или многозамещенным либо незамещенным, С3-С7циклоалкил, который является насыщенным либо ненасыщенным, одно- или многозамещенным либо незамещенным, или соответствующий гетероцикл, в котором С-атом в кольце заменен на N, S либо О, алкиларил, который является насыщенным ...

КОМПОЗИЦИИ ДЛЯ КОСМЕТИЧЕСКИХ ПРЕПАРАТОВ, СРЕДСТВ ЛИЧНОЙ ГИГИЕНЫ, КОМПОНЕНТОВ ОЧИЩАЮЩЕГО ДЕЙСТВИЯ, ПИЩЕВЫХ ДОБАВОК, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ

... 1. Косметическая композиция, содержащая биоактивное стекло и практически безводную косметическую рецептуру. 2. Композиция по п.1, в которой используют биоактивное стекло полученное плавлением. 3. Композиция по п.1, в которой используют золь-гель производное биоактивное стекло. 4. Композиция по п.1, в которой биоактивное стекло представляет собой водный экстракт. 5. Композиция по п.1, в которой практически безводную косметическую рецептуру выбирают из группы состоящей из губной помады, бальзама для губ, теней для век, крема-основы для ухода за кожей вокруг глаз, тонального крема и пудры для лица. 6. Композиция по п.1, используемая в рецептуре Примера 4В. 7. Композиция по п.1, используемая в рецептуре Примера 4С. 8. Композиция по п.1, используемая в рецептуре Примера 5. 9. Композиция по п.1, используемая в рецептуре Примера 6. 10. Композиция по п.1, используемая в рецептуре Примера 7. 11. Композиция по п.1, используемая в рецептуре Примера 8. 12. Композиция по п.1, используемая в рецептуре ...

СПОСОБ ЛЕЧЕНИЯ АЛЛЕРГОДЕРМАТОЗОВ, СОПРОВОЖДАЮЩИХСЯ КСЕРОЗОМ

Способ лечения больных атопическим дерматитом, заключающийся в применении традиционной антигистаминной и десенсибилизирующей терапии, отличающийся эффективным использованием в комплексе с ней эмульсионной мази с экстрактом торфопелоида на пораженные участки кожи 2 раза в сутки на протяжении 7-10 дней.

ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ ПРОПАН-1, 3-ДИАМИНА И ИХ ПРИМЕНЕНИЕ В ФАРМАЦЕВТИКЕ

... 1. Соединение общей структурной формулы (I) или одна из его фармацевтически приемлемых солей , где R1 обозначает С1-12алкил, С3-8циклоалкил, -(С1-6алкил)-С3-8циклоалкил или арил, R2 обозначает С1-12алкил, С3-8циклоалкил, -(С1-6алкил)-С3-8циклоалкил, арил, -(С1-6алкил)арил, гетероциклил или -(С1-6алкил)гетероциклил, при этом R1 и R2 одновременно не обозначают арил или арил и гетероциклил, или R1 и R2 вместе образуют -(СН2)m-кольцо, где m равно 2, 3, 4, 5 или 6, при этом -(CH2)m-кольцо является незамещенным либо одно- или многозамещенным C1-6алкилом, арилом, О-С1-6алкилом и/или O-(С1-6 алкил)арилом или сконденсировано с бензольным ядром; R3 обозначает Н, С1-12алкил, С3-8циклоалкил, -(С1-6алкил)-С3-8циклоалкил, арил, -(С1-6алкил)арил, гетероциклил, -(С1-6алкил)гетероциклил или С(=O)-R7; R4 обозначает Н, С1-12алкил, С3-8циклоалкил, -(С1-6алкил)-С3-8циклоалкил, арил, -(С1-6алкил)арил, гетероциклил или -(С1-6алкил)гетероциклил, или R3 и R4 вместе образуют группу -(СН2)n-, где n равно 3, 4, 5, ...

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 ...

ПРОИЗВОДНЫЕ 2,6-ХИНОЛИНИЛА И 2,6-НАФТИЛА, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ VLA-4

... 1. Соединение, имеющее формулу I, или его фармацевтически приемлемая соль, где Х - представляет собой N или СН; R1 - представляет собой циклоалкил, арил, гетероцикл, аралкил, гетероциклический-алкил, или окси-производное, или группу имеющую формулу: R2 - представляет собой NR4R5, OR4 или –C(=O)NR5R6; R3 - представляет собой тетразол, -CN, CH2OH или -СО-R7; R4 - представляет собой Н, -G1-R8 или группу, имеющую формулу: R5 - представляет собой Н, C1-4-алкил, или NR4R5-группу, являющуюся гетероциклом, или –N=CR9R10; R6 - представляет собой арил, гетероцикл, циклоалкил или аралкил; R7 - представляет собой гидрокси, амино, гидроксиламино, или окси-производное или аминопроизводное; R8 - представляет собой арил, гетероцикл, циклоалкил, аралкил или -NH-арил; R9 - представляет собой арил; и R10 - представляет собой эфир; при условии, что когда Х - представляет собой СН, тогда R1 представляет собой циклоалкил, арил, гетероцикл, аралкил, гетероциклический арил или группу, имеющую формулу: при условии ...

VERBINDUNGEN ALS PDE IV UND TNF INHIBITOREN

VERWENDUNG VON ANTAGONISTEN DES PLÄTTCHEN-AKTIVIERENDEN FAKTORS BEI PRURITUS

OLIGOSACCHARIDEALDONSÄURE UND IHRE TOPISCHE VERABREICHUNG

PHARMAZEUTISCHE ZUBEREITUNG AUF DER BASIS VON RHAMNOLIPID GEGEN DERMATOLOGISCHE ERKRANKUNGEN

NEUE ARYLGLYCINAMIDDERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE VERBINDUNGEN ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN

1,3-DIAZA-DIBENZOAZULENE ALS INHIBITOREN DER PRODUFÜR DEREN HERSTELLUNG

Therapeutische und kosmetische Verwendung von viskosen Zusammensetzungen enthaltend Kohlendioxid

Zusammensetzung zur Haarbehandlung, die ein Pyrimidin-N-oxid-Derivat enthält, ihre Verwendung für die Stimulation des Wachstums der Keratinfasern und/oder für die Verlangsamung ihres Ausfalls

ZUSAMMENSETZUNGEN ZUR BEHANDLUNG VON HAUTERKRANKUNGEN

Arylalkanoylpyridazine

The invention relates to aryl alkanoylpyridazine derivatives of the formula (I) and their physiologically compatible salts and solvates, where R<1>, R<2>, Q and B have the meanings given in claim 1. Said compounds have a phosphodiesterase-IV inhibiting action and can be used in the treatment of allergic disorders, asthma, chronic bronchitis, atopic dermatitis, psoriasis and other skin diseases, inflammatory diseases, auto-immune diseases such as rheumatoid arthritis, multiple sclerosis, Crohn's disease, diabetes mellitus or ulcerative colitis, osteoporosis, transplant rejection reactions, cachexia, tumour growth or tumour metastases, sepsis, memory disturbances, atherosclerosis and AIDS.

VERWENDUNG VON EINEM PRODUKT AUS PFLANZLICHEM ÖL ZUR ERHÖHUNG DER HAUTLIPIDEN PRODUKTION

SULFONAMIDETHER - SUBSTITUIERTE IMIDAZOCHINOLINE

ESTROGEN-17-SULPHAMATE ZUR HEMMUNG VON STEROID SULFATASE

4,6-DIPHENYLPYRIDINDERIVATE ALS ENTZÜNDUNGSHEMMENDE MITTEL

NATÜRLICHER LIGAND VON GPCR CHEMR23 UND DESSEN VERWENDUNG

AROYLPYRIDINONE

IL-8 REZEPTOR ANTAGONISTEN

AMINO-THIOLESTER-VERBINDUNGEN, DIESE ENTHALTENDE PHARMAZEUTISCHE UND KOSMETISCHE ZUSAMMENSETZUNGEN UND IHRE ANWENDUNGEN

Zusammensetzungen enthaltend einen Extrakt aus Echinacea und Linolsäurederivate

Zusammensetzung enthaltend a) einen Extrakt aus Echinacea und b) Linolsäure und/oder Linolsäurederivate.

Mittel gegen Juckreiz

[3'-DESOXY-3-OXO-MeBmt]1-[Val]2-CICLOSPORIN ENTHALTENDE ARZNEIMITTELEMULSION

Organic compounds

Formulation

Bombesin receptor antagonists

Bombesin receptor antagonists are provided which are compounds of formula (I) or pharmaceutically acceptable salts thereof: description. Methods for the preparation of compounds of formula (I) are described also, as are pharmaceutical compositions containing the compounds of the invention. The compounds of the invention have an affinity for the BB1 receptor and some of them also have affinity for the BB2 receptor. Accordingly they may be useful for the diagnosis, prevention, or treatment of male and female sexual dysfunction. They can also be used in the diagnosis, prevention or treatment of anxiety and panic disorders, social phobia, depression, psychoses, sleeping disorders, memory impairment, pulmonary hypertension, lung repair and lung development disorders, cancer including prostate cancer and pancreatic cancer, hepatic porphyria, gastrointestinal secretory disturbances, gastrointestinal disorders including colitis ...

Chemical compounds

Compounds useful in therapy

Purine derivatives

2-Adrenergic receptor agonists

Substituted benzenesulfonamide derivatives as prodrugs of cox-2 inhibitors

Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors

Preventative treatment and remission of allergic diseases

Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes.

Il-8 receptor antagonists

Compositions containing an a tifungal and a phospholipid

Pyrrolo[2,3-d] pyrimidine compounds

Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors

Novel method of treatment

3-azabicyclo (3.1.0) hexane derivatives as opioid receptor antagonists.

The subject invention provides a compound of the formula (I), wherein X, Q, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined. Compounds of formula (I) have activity as opioid receptor antagonists. The subject invention furthermore provides for pharmaceutical compositions and therapeutic methods comprising compounds of formula (I).

Purine derivatives

Pyrrolo [2,3-d] pyrimidine compounds.

A compound of the formula wherein R1, R2 and R3 are inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase' 3 and as such are useful therapy as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.

Purine derivatives.

The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine a2a receptor agonists.

IL-8 Receptor Antagonists.

This invention relates to novel compounds of formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Celecoxib compositions.

Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising particulate celecoxib in an amount of about 10 mg to 1000 mg in intimate mixture with one or more pharmaceutically acceptable excipients. The compositions are useful in treatment or prophylaxis of cyclooxygenase-2 mediated conditions and disorders.

'3-Azabicyclo{3.1.0] hexane derivatives as opiate receptors ligands.

Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.

Substituted benzenesulfonamide derivatives as products of COX-2 inhibitors.

Prodrugs of COX-2 inhibitors are described as beina useful in treating inflammation and inflammation-related disorders.

Pyrrolo {2,3-d} pyrimidine compounds.

A compound of the formula wherein r1, r2, and r3 are as defined above, which are inhibitors of the enzyme protein tyrosine kinases such as janus kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, type i diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, crohn's disease, alzheimer's disease, leukemia and other autoimmune diseases.

Compositions containing an antifungal and a phospholipid.

The invention relates to compositions such as body and hair cleansing products, in particular shampoos, comprising one or more antifungals inhibiting fungal ergosterol biosynthesis as a first active ingredient, a synthetic, amphotheric phospholipid acting both as a second active ingredient and as a surface active ingredient, and art-known body or hair cleansing product ingredients as a carrier.

Pyrrolo[2,3-d] pyrimidine compounds

3-Azabicyclo (3.1.0) hexane derivatives as opiate receptors ligands

Pyrimidinyl carboxamides useful as inhibitors of PDE4 isozymes.

Compounds of formula (1.0.0) are discribed, as well as the usefulness of a pharmaceutical composition for treating inflammatory, respiratory and allergic diseases and conditions, especially asthma; chronic obstructive pulmonary disease (COPD) including chronic bronchitis, emphysema, and brochiectasis; chronic rhinitis, and chronic sinusitis.

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.

Caspase inhibitors and uses thereof.

This invention provides caspase inhibitors having the formula: (i)wherein ring a is an optionally substituted piperidine, tetrahydorquinoline or tettrahydroisoquinolone ring; r1 is hydrogen, chn2, r, or -ch2y; r is an optionally substituted group selected from an aliphatic group, an aryl group, an aralkyl group, a heterocyclic group, or an heterocyclylalkyl group; y is an electronegative leaving group; r2 is co2h, ch2co2h, or esters, amides or isosteres thereof; an optionally substituted aryl group; and r3 is hydrogen, an optionally substituted c1-6alkyl, f2, cn, aryl or r3 is attched to ar to form an unsaturated or partially saturated five or six membered fused ring having 0-2 heteroatoms. The compounds ae useful for treating caspase-mediated disease in mammals.

Soothing cosmetic or pharmaceutical composition comprising a peptide which activates hmg-coa reductase

The present invention relates to a soothing cosmetic or pharmaceutical composition comprising at least one peptide that activates human HMG-CoA reductase of general formula (I): R 1 -(AA) n -X 1 -Gly-Lys-X 2 -(AA) p -R 2 and sequence SEQ ID No. 1 to SEQ ID No. 10, in a physiologically suitable medium. The present invention further relates to the utilization of this novel peptide as a soothing active principle in a cosmetic composition. The invention further applies to a cosmetic treatment method intended to combat skin irritations.

Corrosion current-generating metal particulates and use thereof

Metal particulates capable of generating low levels of corrosion current beneficial for pharmaceutical, cosmetic and other medical uses are provided.

Novel Target for Regulating Multiple Sclerosis

Methods are provided for decreasing demyelinating inflammatory disease in a subject by inhibiting the activity of chemokine-like receptor 1 (CMKLR1). Methods are also provided for screening for agents that find use in treating demyelinating inflammatory disease in a subject.

Enhanced Binding of Pro-Inflammatory Cytokines by Polysaccharide-Antibody Conjugates

We provide monoclonal antibodies against interleukin-1β and tumor necrosis factor-α that remain biologically active in vitro when conjugated to high molecular weight polysaccharides. We report enhanced binding of these cytokines when their monoclonal antibodies are conjugated to alginate compared to non-conjugated monoclonal antibodies. In cell assays, polysaccharide-antibody constructs of the invention inhibited cytokine signaling to comparable levels as that of unmodified antibodies. Conjugation of cytokine-neutralizing antibodies to high molecular weight polymers enhances the affinities cytokine-binding moieties used as anti-inflammatory therapeutics.

Biocompatible materials containing stable complexes of tsg-6 and hyaluronan and method of using same

The present invention provides a biocompatible material in the form of a solid, a water insoluble cross-linked gel or a liposome, which contains a stable comples of TNF-stimulated gene 6 protein (TSG-6) and hyaluronan.

Pure isomers of tritoqualine

The invention provides an isolated stereoisomer of tritoqualine having the structure of FIG. 2 and FIG. 3.

Methods for inhibiting cutaneous inflammation and hyperpigmentation

This invention provides a method of preventing or treating in a subject contact dermatitis which comprises administering to the subject an amount of a compound capable of inhibiting the stem cell factor signaling pathway effective to prevent or treating contact dermatitis so as to thereby prevent or treat contact dermatitis in the subject. This invention also provides a method of preventing or treating in a subject hyperpigmentation, asthma, cutaneous inflammation, anaphylaxis and bronchospasm, mastocytosis, tumors which express activated kit, and conception.

Use of total coumarins of cnidium fruit in preparing medicaments for treating psoriasis

A pharmaceutic composition for treating psoriasis. Ii has an active component and a carrier. The active component has a major active ingredient osthol and a group of minor active ingredients: xanthotoxol, xanthotoxin, isopimpinellin, bergapten, and imperatorine. The major active ingredient osthol accounts for at least 90% by weight of the active component, which accounts for 5-35% by weight of the overall pharmaceutic composition.

N alkylcarbonyl amino lactone compounds and their use

The present invention generally relates to refreshing, soothing, and cooling compounds that affect sensory processes. More particularly, the present invention pertains to certain N-alkylcarbonyl-amino lactone compounds as described herein; compositions and articles comprising such compounds; and methods of treatment, for example, methods of alleviating the discomforts of irritation, itch, and pain in the skin and in the linings of the oral cavity and upper respiratory tract, for example, in methods of treatment of cough.

Topical Compositions with Cannabis Extracts

Various topical compositions including heat-treating mature, dried, powdered Cannabis sativa flower and bud leaves in carriers are disclosed. Various methods for the treatment of pain and methicillin-resistant Staphylococcus aureus (MRSA) infections are disclosed. Methods of making the topical composition, and patches, strips, bandages, and coverings containing the topical composition are also disclosed.

Medicinal Cream Made Using Hydrocortisone Acetate and A Process To Make The Same

The present invention relates to a composition for treating skin inflammation, along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, and a corticosteroid. It discloses a composition for treating skin inflammation, along with skin rejuvenation containing a) a biopolymer in the form of chitosan, b) an active pharmaceutical ingredient (API) composition in the form of hydrocortisone acetate, used in treating skin inflammation c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants and d) water. The active ingredients, namely chitosan, and a corticosteroid in the form of hydrocortisone acetate, are incorporated in cream base for use in treating skin inflammation due to allergy & itching & wounds on human skin involving contacting human skin with the above identified composition.

Cosmetic and/or pharmaceutical composition comprising an extract of carob as active agent for activating aquaporin expression

The invention relates to a cosmetic and/or pharmaceutical composition comprising, in a physiologically suitable medium, a carob peptide extract ( Ceratonia siliqua L.) as an active agent for promoting aquaporin expression. The present invention also relates to the use of a carob peptide extract ( Ceratonia siliqua L.), as an active agent for promoting aquaporin expression, in a cosmetic composition for improving the moisturization and the barrier function of the epidermis and for stimulating skin regeneration. The invention also relates to the use of this novel active agent for preparing a pharmaceutical, in particular dermatological, composition for regulating and/or stimulating aquaporin activity. The invention also relates to a cosmetic treatment method for preventing or combating dryness of the skin and mucous membranes and the manifestations of skin aging.

Topical formulation comprising a corticosteroid as active ingredient

Formulation in the form of aqueous suspension of drug particles of a corticosteroid for topical administration are effective for the prophylaxis and/or treatment of a dermatological disease such as atopic dermatitis, acne and psoriasis.

Crystalline forms of the mono-sodium salt of d-isoglutamyl-d-tryptophan

The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 1 (polymorphic form F) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

Pain Relieving Composition

A pain relieving composition that includes an anesthetic in the range of 0.5%-7.0% by weight (“w/w”), an anti-inflammatory agent in the range of 1.0%-11.0% w/w, a moisturizing agent in the range of 0.5%-12.0% w/w, a humectant in the range of 0.5%-13.0% w/w, a penetration enhancing agent in the range of 0.5%-7.0%, and a carrier solvent in the range of 40.0%-97.0% w/w to be used before and/or after procedures which cause damage to human skin.

Pharmaceutical compositions comprising 4-bromo-n-(imidazolidin-2-ylidene)-1h-benzimidazol-5-amine for treating skin diseases

The present invention relates to a method for treating skin diseases in a patient in need thereof which comprises of administering a pharmaceutical composition comprising a therapeutically effective amount of 4-bromo-N-(imidazolidin-2-ylidene)-1H-benzimidazol-5-amine or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients.

Liquid/liquid extraction

The invention relates to a method for the extraction of all unsaponifiable fraction contained in a vegetable oil, an oil originating from a micro-organism or a vegetable butter or in a co-product from the vegetable oil refining industry, such as deodorisation discharge. The method includes at least: A) a step comprising the transformation of the aforementioned oils, butter or co-product from the vegetable oil refining industry or oils originating from micro-organisms into a hydro-alcoholic solution by means of, in particular, a step selected from saponification and esterification steps; B) a step comprising the extraction of the hydro-alcoholic solution in which the fatty fraction is separated from the unsaponitiable fraction by means of liquid/liquid extraction; and C) an optional step comprising the purification of the unsaponiable fraction, selected from the group containing crystallisation and liquid/liquid extraction steps. According to the invention, at least one step from the liquid/liquid extraction steps in step B, the crystallisation steps in step C and the liquid/liquid extraction steps in step C is performed using a first solvent system containing a concentration of solvent selected from among: fluorinated aromatic solvents, particularly trifluorotoluene (BTF) and hexalluorobenzene (BHF); tert-butyl ethers, particularly 2-ethoxy-2-methylpropane, also known as ethyl-tert-butyl-ether (ETU); solvents comprising at least one silicon atom, particularly hexamethyldisiloxane (HMDS) and tertramethylsilane (TMS); methyl-tetrahydrofuran (MeTHF); and mixtures thereof, representing at least 50 vol.-% in relation to the total volume of the solvent system. The invention also relates to the fractions obtained using this method and to compositions containing said fractions.

Crystalline forms of the mono-sodium salt of d-isoglutamyl-d-tryptophan

The present invention relates to crystalline forms of the mono-sodium salt of D-isoglutamyl-D-tryptophan, pharmaceutical compositions comprising them, their use in the treatment of various diseases and conditions, and processes for their preparation. In particular, the present invention relates the crystal modification 2 (polymorphic form I) of the mono-sodium salt of D-isoglutamyl-D-tryptophan.

MONOMERIC FORMS OF HUMAN AMINOACYL-t-RNA SYNTHETASES HAVING NON-CANONICAL BIOLOGICAL ACTIVITIES

Isolated monomelic aminoacyl-tRNA synthetase polypeptides and polynucleotides having non-canonical biological activities are provided, as well as compositions and methods related thereto.

Perfluoro(n-butylcyclohexane) compositions and uses thereof

A perfluoro(n-butylcyclohexane) composition is disclosed with numerous uses including topical and cosmetic applications, e.g., for application to the periocular skin or for the topical treatment of pruritus.

Soluble interleukin-20 receptor

A soluble receptor to IL-20 having two polypeptide subunits, IL-20RA (formerly called ZcytoR7) and IL-20RB (formerly called DIRS1). The two subunits are preferably linked together. In one embodiment one subunit is fused to the constant region of the light chain of an immunoglobulin, and the other subunit is fused to the constant region of the heavy chain of the immunoglobulin. The light chain and the heavy chain are connected via a disulfide bond.

Methods of antagonizing signal transduction in dorsal root ganglion cells

Use of antagonists to IL-31 are used to treat inflammation and pain by inhibiting, preventing, reducing, minimizing, limiting or minimizing stimulation in neuronal tissues. Such antagonists include antibodies and fragments, derivative, or variants thereof. Symptoms such as pain, tingle, sensitization, tickle associated with neuropathies are ameliorated.

Pharmaceutical Composition for Topical Application

A pharmaceutical or cosmetic carrier or composition for topical application characterized by rheological properties which render the carrier or composition semi-solid at rest and a liquid upon application of shear forces thereto. The composition or carrier are prepared by mixing 1-25 percent of a solidifying agent and 75-99 percent of a hydrophobic solvent, by weight, wherein at least one of them has therapeutic or cosmetic benefits, in the presence or absence of a biologically active substance.

Antibodies that bind par-2

The present invention provides compositions and methods relating to or derived from anti-PAR-2 antibodies. In particular embodiments, the invention provides antibodies that bind human PAR-2, PAR-2-binding fragments and derivatives of such antibodies, and PAR-2-binding polypeptides comprising such fragments. Other embodiments provide nucleic acids encoding such antibodies, antibody fragments and derivatives and polypeptides, cells comprising such polynucleotides, methods of making such antibodies, antibody fragments and derivatives and polypeptides, and methods of using such antibodies, antibody fragments and derivatives and polypeptides, including methods of treating or diagnosing subjects having PAR-2-related disorders or conditions.

Methods of antagonizing signal transduction in dorsal root ganglion cells

Use of antagonists to IL-31Ra and OSMRb are used to treat inflammation and pain by inhibiting, preventing, reducing, minimizing, limiting or minimizing stimulation in neuronal tissues. Such antagonists include soluble receptors, antibodies and fragments, derivative, or variants thereof. Symptoms such as pain, tingle, sensitization, tickle associated with neuropathies are ameliorated.

Immunoregulatory peptides and methods of use

Peptides for the treatment of inflammation, and therapeutic uses and methods of using the same are disclosed. Peptides including a transducing sequence are effective for inhibiting cytokine activity and TNF-α secretion through interaction with toll-like receptors. Experiments are described illustrating the efficacy of the compounds in treating otitis media

Agent for fungal dermatitis

The invention provides a method for the treatment of fungal dermatitis. The treatment method involves administering an effective amount of luliconazole or a pharmaceutically acceptable salt thereof to a target in need of a treatment of fungal dermatitis.

Stable Corticosteroid Nanoparticulate Formulations and Methods for the Making and Use thereof

Disclosed are stable corticosteroid nanoparticulate formulations, methods of making and therapeutic uses thereof.

Pain relief compositions, manufacture and uses

The present invention relates to TRPV1 selective agonist topical compositions including capsaicinoid and analgesic agent compositions and methods of manufacture and methods of providing pain relief as well as treating a variety of disorders with such compositions.

Aprepitant l-proline composition and cocrystal

A 1:1:1 aprepitant L-proline H 2 0 composition and a 1:1:1 aprepitant L-proline H 2 0 cocrystal are disclosed as well as pharmaceutical compositions containing a 1:1:1 aprepitant L-proline H 2 0 composition or cocrystal and a pharmaceutically acceptable carrier. The 1:1:1 aprepitant L-proline H 2 0 composition or cocrystal may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pairs, cancer, a skin disease, itch, a respiratory disease, or an addiction.

Variable region sequences of il-31 monoclonal antibodies and methods of use

Novel compositions derived from antigen-binding sites of immunoglobulins having affinity for IL-31 are provided. The compositions exhibit immunological binding properties of antibody molecules capable of binding specifically to a human IL-31. CDR regions derived from same or different immunoglobulin moieties are provided. Also provided are single chain polypeptides wherein V H and V L domains are attached. The sFv molecules can include ancillary polypeptide moieties which can be bioactive, or which provide a site of attachment for other useful moieties. The compositions are useful in specific binding assays, affinity purification schemes, drug or toxin targeting, imaging, and genetic or immunological therapeutics for inflammatory diseases. The invention thus provides novel polypeptides, the DNAs encoding those polypeptides, expression cassettes comprising those DNAs, and methods of inducing the production of the polypeptides. The invention further provides the amino acid sequences of the variable regions of the monoclonal antibodies and use of these monoclonal antibody or antibody fragment in conjunction with an human IgG4 Fc molecule.

Nanoparticles based on poly (lactic glycolic) acid for cosmetic applications

On one hand, the present invention relates to cosmetic compositions comprising poly(lactic glycolic)acid (PLGA) nanoparticles for applications to the skin. On the other hand, it also concerns polymeric nanoparticles having on its surface a plurality of cosmetically active agents, each of said agents being associated to said nanoparticle via oleylcysteineamide, delivery systems for topical application based on said particles and cosmetic formulations comprising said particles.

Clonidine compounds in a biodegradable matrix

Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of clonidine in a matrix at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate matrix formulations are provided within biodegradable polymers, this pain relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.

Formulations containing extracts of echinacea angustifolia and zingiber officinale which are useful in reducing inflammation and peripheral pain

Disclosed is a combination of lipophilic extracts of Zingiber officinale and Echinacea angustifolia for the treatment of itching, peripheral pain, superficial and deep inflammatory and painful states, pain associated with muscle spasms, herpes pain, and radiodermatitis caused by oncological radiotherapy, with or without fungal or bacterial infections.

Substituted heterocylic compounds

The present invention relates to substituted heterocyclic compounds of Formula I or XI: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.

Compositions Comprising Zoledronic Acid or Related Compounds for Relieving Inflammatory Pain and Related Conditions

Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions. Although an oral dosage form with enhanced bioavailability with respect to the bisphosphonate compound can be used, the treatment can also be effective using an oral dosage form that includes a bisphosphonate compound, such as zoledronic acid, wherein the bioavailability of the bisphosphonate is unenhanced, or is substantially unenhanced.

E-selectin antagonists

Compounds, compositions and methods are provided for inhibiting in vitro and in vivo processes mediated by E-selectin binding. More specifically, particular glycomimetic compounds are described, wherein the compounds are E-selectin antagonists.

Topical Patch For Pain Relief Using Cooling Agent

Topical patch preparations that contain an odorless physiological cooling agent, and methods for using the same are provided. The subject topical patch preparations are made up of an adhesive gel composition that is present on a support, where the adhesive gel composition includes the odorless physiological cooling agent, a water-soluble polymer gel, water and a water holding agent. In using the subject topical patch preparations, the topical patch preparations are applied to a skin surface of a subject and maintained at the site of application for a period of time sufficient for an effective amount of the an odorless physiological cooling agent to be administered to the subject. The subject invention finds use in a variety of applications.

Sulfonamide compounds having trpm8 antagonistic activity

Sulfonamide compounds having TRPM8 antagonistic activity are provided. A sulfonamide compound of formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof: (I) wherein Ring A is bicyclic aromatic heterocycle comprised of (a) pyridine is condensed with benzene; or (b) pyridine is condensed with monocyclic aromatic heterocycle, and Ring A binds to a sulfonylamino moiety on a carbon atom adjacent to a nitrogen atom of the pyridine ring constituting Ring A, Ring B is (a) monocyclic or bicyclic aromatic hydrocarbon; (b) monocyclic or bicyclic alicyclic hydrocarbon; (c) monocyclic or bicyclic aromatic heterocycle; or (d) monocyclic or bicyclic non-aromatic heterocycle, Ring C is (a) benzene; or (b) monocyclic aromatic heterocycle, and other symbols are the same as defined in the specification.

Dried product and a process for manufacturing the product

A dried product of an extract from inflammatory rabbit skin inoculated with vaccinia virus having an inhibitory activity for the production of a kallikrein-like substance is produced by admixing the extract with a saccharide, sugar alcohol or ascorbic acid before reaching dryness, and then drying the admixture to a solid form such as granules. The dried product may be employed to produce a solid preparation for oral administration, such as tablets, having an inhibitory activity for the production of a kallikrein-like substance.

Pharmaceutical composition for treatment and prevention of th3 march-related diseases

The present invention provides a medicinal agent and a method for each of various testing or the like, which enable the treatment and prevention, particularly preventive treatment, of Th3 march-related diseases. The present invention also provides a pharmaceutical composition for treating and/or preventing Th3 march-related diseases, which comprises zinc, calcium and phosphorus and additionally comprises pumpkin seeds and corn silk, and which preferably can activate the DNA repairing ability of a zinc finger, particularly the ability of repairing defect or mutation of DNA for a filaggrin gene, of a zinc finger.

Composition for treating aids and associated conditions

An Aids and associated conditions related to Aids treating compositions is disclosed. The compositions comprise: a medicament selected from an extract of at least one of the following plant families: Apocynaceae ( Pleioscarpa Bicarpellata ); Annonaceae ( Cleistopholis Patens ); Dichapetalaceae ( Dichapetehan Madagasca Riense ); Annoceae ( Uvaristrum Pierreanum ); Cynocynaceae ( Strophantus Gratus ); Asclepiadaceae ( Gongronema Latifolium ); Combretaceae ( Combretum Racemosum ); Apocynaceae ( Alostonia Boonei ); Amaranthaceae ( Alternanthera Pungens ); Aroceae ( Anchomanes Differmis ); Cyperaceae ( Seleria Voivinil ); Anacardiaceae ( Lannea Acida ); Bignodaceae ( Kigelia Africana ); Bombacaceae ( Ceiba Pentanota ); Anarcardiaceae ( Antrocaryon Micraster ); Bombacaceae ( Bombax Bounopozense ): Anarcardiaceae ( Spondias Mombin ); Caricaceae ( Carica Papaya ); a glyceryl ester of any of the foregoing extracts; a saponin of any of the foregoing extracts; an alkaloid of any of the foregoing extracts; a protein of any of the foregoing extracts; a fat of any of the foregoing extracts; a sugar of any of the foregoing extracts; and any mixture of any of the foregoing.

Hyaluronic acid composition

An injectable hyaluronic acid composition including a hyaluronic acid; a local anesthetic selected from the group of amide and ester type local anesthetics or a combination thereof; and an ascorbic acid derivative in an amount which prevents or reduces the effect on the viscosity and/or elastic modulus G′ of the composition caused by the local anesthetic upon sterilization by heat. Further, the medical and non-medical, such as cosmetic, use of such a composition, and a method of manufacturing such a composition.

Composition for the Treatment of Skin Conditions

A topical composition for the treatment of skin conditions. The composition comprises an antifungal agent, an anti-inflammatory agent and an antimicrobial agent together with a pharmaceutically acceptable excipient. The anti-inflammatory is present at a concentration of less than 0.01% wt of the composition and the antimicrobial agent has the general formula (I): (Formula (I)).

Novel, protective, anti-inflammatory receptor and its use in preservation of mitochondrial function, wound healing and repair

Provided herein is a novel mitochondrial Angiotensin II type 1 and type 2 AT 1 R and AT 2 R receptor which plays a role in protection of mitochondria against oxidative damage. Evidence from animal studies indicates a role for this receptor in preservation of mitochondria and up-regulation of survival genes, anti-inflammatory action, and improvement of wound healing in the skin and soft tissues. Pharmaceutical compositions for treatment directed to preserving mitochondrial function, anti-inflammation, wound healing and decreasing the signs of aging, as well as medicaments and their use are also provided.

Small molecule inhibitors of trpa1

The present invention relates to the use of compounds which are capable of attenuating skin irritation when they are applied to the skin. Skin irritation can be caused, inter alia, by ingredients of cosmetic or pharmaceutical compositions and/or environmental irritants. In particular, the present invention relates to compounds having the property of antagonizing the activation of the transient receptor potential (TRP) ankyrin 1 (TRPA1) ion channel and the use of said compounds as soothing agents. Such compounds can be used in many fields, particularly in personal-care products, cosmetics, textile and packaging products, pharmaceutical compositions, medical devices, and foodstuffs. The present invention further relates to products and/or pharmaceutical compositions containing said compounds. The present invention also relates to the use of the compounds described herein for the modulation of the taste of a food product.

Tight junctions modulators

The present invention relates to a new therapy targeted at the restoration or improvement of tight junction function. Aberrant TJ function, is characteristic of many chronic skin diseases. The inventors demonstrated that plant polyphenols or flavonoids and Cis-urocanic acid modulates tight junction structure and function in mammalian keratinocytes and provided tight junction modulators, pharmaceutical compositions and methods for preventing or treating impaired tight junction function in stratified mammalian epithelia.

Hyaluronic acid composition

An injectable hyaluronic acid composition including a hyaluronic acid; a local anesthetic selected from the group of amide and ester type local anesthetics or a combination thereof; and an ascorbic acid derivative in an amount which prevents or reduces the effect on the viscosity and/or elastic modulus G′ of the composition caused by the local anesthetic upon sterilization by heat. Further, the medical and non-medical, such as cosmetic, use of such a composition, and to a method of manufacturing such a composition.

USE OF BULLEYACONITINE A

The present disclosure belongs to the field of pharmaceuticals. Disclosed is a use of bulleyaconitine A in treating pruritus or a secondary lesion thereof, especially pruritus induced by histamine and/or chloroquine. 1. A method of treating and/or preventing skin pruritus and/or a secondary lesion thereof , comprising administering bulleyaconitine A to a subject in need thereof.2. The method according to claim 1 , wherein a dosage of bulleyaconitine A is 0.125 mg/kg mouse body weight/d−0.5 mg/kg mouse body weight/d.3. The method according to claim 1 , wherein a dosage of the bulleyaconitine A is 0.01375 mg/kg human body weight/d−0.055 mg/kg human body weight/d.4. The method according to claim 1 , wherein the skin pruritus is neuropathic itch.5. The method according to claim 4 , wherein the skin pruritus is an itch caused by histamine and/or chloroquine.6. The method according to claim 1 , wherein bulleyaconitine A is present in a medicament which comprises a pharmaceutically acceptable carrier claim 1 , and bulleyaconitine A is present in the medicament in an amount of 0.2%-88% by mass.7. The method according to claim 6 , wherein the medicament is in a dosage form of oral preparation claim 6 , injection preparation or external preparation.8. The method according to claim 7 , wherein the oral preparation includes hard capsules claim 7 , dripping pills claim 7 , granules claim 7 , tablets claim 7 , mixtures claim 7 , soft capsules claim 7 , concentrated pills claim 7 , oral solutions or powders.9. The method according to claim 7 , wherein the injection preparation is injection solution or lyophilized powder for injection.10. The method according to claim 7 , wherein the external preparation is tincture claim 7 , ointment claim 7 , cream claim 7 , paste claim 7 , aerosol claim 7 , spray claim 7 , powder claim 7 , otic preparation claim 7 , lotion claim 7 , rinse claim 7 , liniment claim 7 , paint claim 7 , film preparation claim 7 , gelatin or patch. This application ...

Lactobacillus Crispatus KBL693 Strain and Use Thereof

A strain of Lactobacillus crispatus KBL693 and the use thereof are disclosed. The strain of Lactobacillus crispatus KBL693 (Accession No. KCTC 13519BP) attenuates allergic reactions of cells, significantly improves symptoms of atopic dermatitis, and exhibits anti-inflammatory and anti-fungal effects. Thus, the single strain alone can achieve all the purposes of alleviating atopic dermatitis and other allergic diseases and improving inflammatory diseases and autoimmune diseases, thereby finding advantageous applications as a probiotic substance. In addition, the strain, based on the anti-fungal activity thereof, can be advantageously utilized in a skin external preparation against various skin diseases caused by fungi, and in a cosmetic composition and a functional patch for alleviating sensitive skin.

FORMULATION FOR USE IN THE TREATMENT OF UREMIC PRURITUS

There is provided a topical formulation comprising a nucleophile, such as amino acids and most polypetides and/or a derivative thereof, for use in the treatment or prevention of itchy dry skin caused by urea, such as in uremic pruritus, of a subject. The amino acid may be histidine and the derivative may be a histidine degradation product, a peptide of histidine, a peptide of histidine and one or more additional amino acids, and a pharmaceutically-acceptable salt of histidine. 115.-. (canceled)16. A topical formulation comprising:(a) a polyaphron composition; and(b) at least 0.2 w/w % of a nucleophilic compound.17. The topical formulation according to claim 16 , wherein the nucleophilic compound is a nucleophilic amino acid claim 16 , a peptide and/or a derivative thereof.18. The topical formulation according to claim 16 , wherein the nucleophilic compound comprises a nucleophilic amino acid claim 16 , and the nucleophilic amino acid comprises histidine or a derivative of histadine.19. The topical formulation according to claim 16 , wherein the formulation comprises:(a) 0.5 w/w % to 5 w/w % of the nucleophilic compound.20. The topical formulation according to claim 16 , wherein the formulation comprises:(a) 2 w/w % to 5 w/w % of the nucleophilic compound.21. The topical formulation according to claim 16 , wherein the formulation comprises:(a) 2 w/w % to 15 w/w % of the nucleophilic compound.22. The topical formulation according to claim 17 , wherein the derivative is selected from one or more of a histidine degradation product claim 17 , a peptide of histidine claim 17 , a peptide of histidine and one or more additional amino acids claim 17 , and a pharmaceutically acceptable salt of histidine.23. The topical formulation according to claim 18 , wherein the histidine comprises L-histidine.24. The topical formulation according to claim 18 , wherein the histidine and/or the derivative of histidine is the only active ingredient in the pharmaceutical composition.25. The ...

OINTMENT

An ointment is provided. The ointment stably comprises an oxazole compound that has specific inhibitory activity against PDE4 and that is represented by the following formula (11). The ointment can be efficiently absorbed into the skin. 2. The ointment according to claim 1 , comprising the oxazole compound dissolved in a base component.3. The ointment according to claim 2 , wherein the base component comprises a solvent for dissolving the oxazole compound in the solvent claim 2 , and an ointment base for dispersing or dissolving the solvent in the ointment base.4. The ointment according to claim 3 , wherein the ointment base comprises a hydrocarbon.5. The ointment according to claim 3 , wherein the solvent comprises a polar compound that is a liquid at room temperature.6. The ointment according to claim 3 , wherein the ointment base is an ointment base for dispersing the solvent in the ointment base claim 3 , and the solvent in the form of droplets claim 3 , in which the oxazole compound is dissolved claim 3 , is dispersed in the ointment base.7. The ointment according to claim 3 , wherein the ointment base comprises at least beeswax.8. The ointment according to claim 7 , wherein the beeswax is not chemically bleached.9. The ointment according to claim 1 , for use in the treatment and/or prevention of eczema and dermatitis. The present invention relates to an ointment comprising an oxazole compound.PTL 1 and 2 report an oxazole compound having specific inhibitory activity against phosphodiesterase 4 (PDE4) and a method for producing the oxazole compound. PDE4 is predominant in inflammatory cells. Inhibition of PDE4 increases intracellular cAMP levels, and increased cAMP levels down-regulate inflammatory response through expression regulation of TNF-α, IL-23, or other inflammatory cytokines. Increases in cAMP levels also increase anti-inflammatory cytokines, such as IL-10. Thus, the oxazole compound is thought to be suitable for use as an anti-inflammatory agent. For ...

Synergistic Compositions and Devices for Gynecological Procedures

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

Rosacea Treatment Method

Topical application of a 2% (w/w) Delphinidin cream, twice per day, treats rosacea and maintains normal healthy skin in patients with rosacea. 1. A method for treating a condition selected from the group consisting of rosacea and lupus , the method comprising applying topically , twice per day , to a patient that has been diagnosed as having a condition selected from the group consisting of rosacea and lupus , a topical cream comprising from 0.08% (w/w) to 0.2% (w/w) of Delphinidin.2. The method of claim 1 , wherein the Delphinidin comprises at least one glucoside moiety.3. The method of claim 2 , wherein the Delphinidin comprises at least one compound selected from the group consisting of: delphinidin-3-O-sambubioside 5-O-glucoside claim 2 , delphinidin 3 claim 2 ,5-O-diglucoside claim 2 , delphinidin-3-O-sambubioside and delphinidin-3-O-glucoside.4. The method of claim 3 , wherein the Delphinidin comprises delphinidin-3-O-sambubioside 5-O-glucoside claim 3 , delphinidin 3 claim 3 ,5-O-diglucoside claim 3 , delphinidin-3-O-sambubioside and delphinidin-3-O-glucoside.5. The method of claim 1 , where the condition comprises rosacea.6. The method of claim 2 , where the condition comprises rosacea.7. The method of claim 3 , where the condition comprises rosacea.8. The method of claim 4 , where the condition comprises rosacea.9. The method of claim 1 , where the condition comprises lupus.10. The method of claim 2 , where the condition comprises lupus.11. The method of claim 3 , where the condition comprises lupus.12. The method of claim 4 , where the condition comprises lupus. This application is a divisional of co-pending Ser. No. 16/358,798, filed Mar. 20, 2019, the contents of which are here incorporated by reference.None.None.None.None.Rosacea is a chronic skin disease. It affect the face: the cheeks, nose, eyes, chin and forehead. It is characterized by recurrent episodes of flushing, erythema (redness), papules (pimples), pustules and telangiectasia (permanent ...

ESTER AND CARBONATE PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS

The invention provides compounds of formula (I): 126-. (canceled)30. The pharmaceutical composition of claim 27 , further comprising one or more additional therapeutic agents.31. The pharmaceutical composition of claim 27 , wherein the pharmaceutical composition is selected from the group consisting of a lotion claim 27 , cream claim 27 , gel claim 27 , stick claim 27 , spray claim 27 , ointment claim 27 , paste claim 27 , foam claim 27 , and mousse.32. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is a lotion.33. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is a cream.34. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is a gel.35. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is a stick.36. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is a spray.37. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is an ointment.38. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is a paste.39. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is a foam.40. The pharmaceutical composition of claim 31 , wherein the pharmaceutical composition is a mousse.41. The pharmaceutical composition of claim 27 , wherein the compound claim 27 , or a pharmaceutically acceptable salt thereof claim 27 , is present at between 0.1 and 10% by weight.42. The pharmaceutical composition of claim 27 , wherein the compound claim 27 , or a pharmaceutically acceptable salt thereof claim 27 , is present at between 0.25 and 5% by weight.43. The pharmaceutical composition of claim 27 , wherein the compound claim 27 , or a pharmaceutically acceptable salt thereof claim 27 , is present at between 0.05 and 0.5% by weight. This application claims the benefit of U.S. Provisional Application No. 62/837,829, filed on Apr. 24, ...

Anti-human interleukin 5(il-5) monoclonal antibody and use thereof

Disclosed in the present invention are an antibody targeting IL-5, a preparation method therefor and use thereof. In particular, disclosed in the present invention is a novel murine-derived or chimeric monoclonal antibody targeting IL-5. Also disclosed in the present invention is a method for preparing said monoclonal antibody. The monoclonal antibody of the present invention is capable of binding IL-5 antigen with high specificity, has high affinity and can well alleviate a series of asthma symptoms caused by IL-5, thereby achieving the effect of treating asthma.

Treatment of uremic pruritus

The present invention relates to methods for treating uremic pruritus with anti-pruritic compositions, wherein the method provides a therapeutic effect in a patient.

COMPOSITION FOR PREVENTING OR IMPROVING INFLAMMATION INCLUDING EXTRACT OF SEED OF NEW SOYBEAN CULTIVAR SCEL-1

Provided are a composition for preventing or improving inflammation, the composition including an extract of a seed of soybean (L.) Merrill cultivar SCEL-1, and a method of preventing occurrence of inflammation in a subject or improving inflammation in a subject, the method including injecting the composition to a subject. 1Glycine max. A composition for preventing or improving inflammation , the composition comprising , as an active ingredient , an extract obtained by performing an extraction process on a seed of soybean (L.) Merrill cultivar SCEL-1 by using water , C-Calcohol , or a mixture thereof , wherein the seed contains cyanidin-3-O-glucoside , procyanidin B2 , and epicatechin , wherein an amount of the procyanidin B2 is greater than that of the cyanidin-3-O-glucoside , and a representative sample of the seed is deposited with the Korean Agricultural Culture Collection (KACC) , which is an International Depository Authority (IDA) under the Budapest Treaty on the International Recognition of the Deposit of Microorganisms for the Purpose of Patent Procedure under the accession number KACC 88002BP on Nov. 8 , 2018.2. The composition of claim 1 , wherein a total amount of cyanidine-3-O-glucoside claim 1 , procyanidine B2 claim 1 , and epicatechin in the extract is in a range of 2.1% to 3.4% based on a total weight of the extract.3. The composition of claim 2 , wherein the cyanidin-3-O-glucoside claim 2 , the procyanidin B2 claim 2 , and the epicatechin are contained at a ratio of 1:2.0 to 2.1:0.43 to 0.48 based on a total weight of the extract.4. The composition of claim 1 , wherein an amount of the extract is in a range of 0.005% to 99.9% based on a total weight of the composition.5. The composition of claim 1 , wherein the inflammation includes skin inflammation claim 1 , atopic dermatitis claim 1 , or chronic obstructive pulmonary disease (COPD).6. The composition of claim 1 , wherein the composition is food claim 1 , a cosmetic composition claim 1 , or a ...

NOVEL ARID5A PEPTIDE INHIBITORS

AT-rich interactive domain-containing protein 5a (Arid5a) inhibitors can include mid-sized peptides (peptides having less than 15 amino acids) that inhibit the activity of Arid5a. The peptides include the sequence of SEQ ID NO: 1. In an embodiment, the Arid5a peptide inhibitors can include a peptide having a sequence selected from the group consisting of SEQ ID NO: 2, SEQ ID NO:3, and SEQ ID NO:4. The Arid5a peptide inhibitors can be useful for experimental investigation and treating a disease or disorder, such as, inflammation, diseases associated with inflammation, cancer, and autoimmune disease. 1. A peptide , consisting of the amino acid sequence of SEQ ID NO: 1.2. A pharmaceutical composition claim 1 , comprising: the peptide of and a pharmaceutically acceptable carrier.3. A peptide claim 1 , comprising at least one sequence selected from the group consisting of SEQ ID NO: 2 claim 1 , and SEQ ID NO: 4.4. A pharmaceutical composition claim 3 , comprising: the peptide of and a pharmaceutically acceptable carrier.5. A method of treating a disease claim 1 , comprising administering a therapeutically effective amount of the peptide of to a patient in need thereof claim 1 , the disease comprising at least one of inflammation claim 1 , cancer claim 1 , and autoimmune disease.6. The method as recited in claim 5 , wherein the autoimmune disease is multiple sclerosis.7. (canceled)8. A method of treating a disease claim 3 , comprising administering a therapeutically effective amount of the synthetic peptide of to a patient in need thereof claim 3 , the disease comprising at least one of inflammation claim 3 , cancer claim 3 , and/or autoimmune disease.9. The method as recited in claim 8 , wherein the disease is multiple sclerosis.10. A method of screening for a peptide inhibitor for Arid5a claim 8 , comprising:selecting an Arid5a peptide inhibitor based upon in silico predicted binding of candidate Arid5a peptide inhibitors to SEQ ID NO: 5.11. A method of screening for a ...

COMPOSITION FOR RELIEVING ITCH OR IRRITATION OF SKIN, COMPRISING THYMOL TRIMETHOXYCINNAMATE

The present disclosure discloses a composition for relieving skin itch or irritation, which contains thymol trimethoxycinnamate or a stereoisomer, salt, hydrate or solvate thereof as an active ingredient, and a method for relieving skin itch or skin irritation by administering the composition to a subject in need of reliving of skin itch or irritation. The composition according to an aspect of the present disclosure has a superior effect of relieving skin itch or skin irritation by inhibiting the voltage-gated sodium channel Nav1.7 without side effects. 1. A method for relieving skin itch or skin irritation , comprising administering an effective amount of a composition comprising thymol trimethoxycinnamate or a stereoisomer , salt , hydrate or solvate thereof to a subject in need of relieving skin itch or skin irritation.3. The method according to claim 1 , wherein an administration dosage of the thymol trimethoxycinnamate or a stereoisomer claim 1 , salt claim 1 , hydrate or solvate thereof is 0.37-37 mg/kg/day.4. The method according to claim 1 , wherein a content of the thymol trimethoxycinnamate or a stereoisomer claim 1 , salt claim 1 , hydrate or solvate thereof is 0.001-20 wt % based on the total weight of the composition.5. The method according to claim 1 , wherein the relieving skin itch or skin irritation is by inhibiting the voltage-gated sodium channel Nav1.7.6. The method according to claim 1 , wherein the skin itch or skin irritation is induced by a chemical substance.7. The method according to claim 1 , wherein the composition is a composition for external application to skin.8. The method according to claim 1 , wherein the composition is a food composition.9. The method according to claim 1 , wherein the composition is a cosmetic composition.10. The method according to claim 1 , wherein the composition is a pharmaceutical composition. This application claims the priority of Korean Patent Application No. 10-2020-0096647 filed on Aug. 3, 2020, the ...

Laureth-4 containing topical formulations

The present invention is a method and composition comprising laureth-4 in topical formulations, wherein the laureth-4 increases the penetration of active ingredients across the skin. In a particularly preferred embodiment, the active ingredient is SHR0302.

COMPOSITIONS AND METHODS FOR REDUCING INFLAMMATION

The present invention is directed to a method of producing compositions derived from culturing cells under hypoxic conditions on a biocompatible surface in vitro. The culturing method produces both an extracellular matrix composition and a conditioned culture medium composition, which may be used separately or in combination to obtain physiologically acceptable compositions useful in a variety of medical and therapeutic applications. 1. A method for reducing inflammation in a subject comprising administering to the subject a conditioned culture medium (CCM) composition or an extracellular matrix (ECM) composition , wherein the CCM and ECM compositions are produced by the method comprising culturing fibroblast cells on microcarrier beads or a three-dimensional surface under hypoxic conditions of 1-5% oxygen , thereby producing multipotent stem cells which produce a CCM and an ECM fraction , thereby reducing inflammation.2. The method of claim 1 , wherein the inflammation is associated with bone degeneration claim 1 , spinal disk degeneration claim 1 , osteoarthritis claim 1 , pruritis claim 1 , skin inflammation claim 1 , psoriasis claim 1 , multiple sclerosis claim 1 , rheumatoid arthritis claim 1 , osteoarthritis claim 1 , systemic lupus erythematosus claim 1 , Hashimoto's thyroidis claim 1 , myasthenia gravis claim 1 , diabetes type I or II claim 1 , asthma claim 1 , inflammatory lung injury claim 1 , inflammatory liver injury claim 1 , inflammatory glomerular injury claim 1 , atopic dermatitis claim 1 , allergic contact dermatitis claim 1 , irritant contact dermatitis claim 1 , seborrhoeic dermatitis claim 1 , Sjoegren's syndrome claim 1 , keratoconjunctivitis claim 1 , uveitis claim 1 , inflammatory bowel disease claim 1 , Crohn's disease claim 1 , ulcerative colitis claim 1 , an inflammatory disease of the joints claim 1 , skin claim 1 , or muscle claim 1 , acute or chronic idiopathic inflammatory arthritis claim 1 , myositis claim 1 , a demyelinating disease ...

ANTIBODY TO FIBROSIS-RELATED MOLECULE AND MEDICAL APPLICATION THEREOF

The present invention provides an antibody to a fibrosis-related molecule and medical application thereof. The antibody of the present invention is an antibody that binds to CHL1 protein and an antibody that neutralizes the binding of the CHL1 protein to a fibroblast. 1. A method for analyzing the presence or absence of inflammation in a tissue in a subject , comprising determining the presence of secreted CHL1 protein in the tissue , a body fluid , or excrement obtained from the subject.2. The method according to claim 1 , wherein the presence or absence of the CHL1 protein is detected using an antibody that binds to secreted CHL1 protein claim 1 , or an antigen-binding fragment thereof.3. The method according to claim 1 , wherein the presence or absence of the CHL1 protein is detected using an antibody or an antigen-binding fragment thereof that binds to secreted CHL1 protein claim 1 , wherein the antibody or the fragment has a heavy chain variable region having heavy chain CDR1 having the amino acid sequence set forth in SEQ ID NO: 1 claim 1 , heavy chain CDR2 having the amino acid sequence set forth in SEQ ID NO: 2 and heavy chain CDR3 having the amino acid sequence set forth in SEQ ID NO: 3 claim 1 , and a light chain variable region having light chain CDR1 having the amino acid sequence set forth in SEQ ID NO: 5 claim 1 , light chain CDR2 having the amino acid sequence set forth in SEQ ID NO: 6 and light chain CDR3 having the amino acid sequence set forth in SEQ ID NO: 7.4. The method according to claim 1 , wherein the excrement is a feces and the tissue is intestine.5. A method of detecting inflammation in an intestine in a subject claim 1 , comprising detecting CHL1 protein in a feces obtained from the subject claim 1 , and determining that inflammation is detected in the intestine in a subject claim 1 , based on the presence of CHL1 protein.6. A method of claim 2 , further comprising administering to the subject an antibody that binds to secreted CHL1 ...

Endomucin As An Anti-Inflammatory Agent

The invention provides compositions and methods for utilizing endomucin as an anti-inflammatory Agent

METHOD FOR REDUCING ITCHING IN ATOPIC DERMATITIS

This invention relates to a method for treating atopic dermatitis, comprising administering an effective amount of N-acyltryptamine represented by Formula (I): 2. The method according to claim 1 , comprising reducing itching in atopic dermatitis.3. The method according to claim 1 , wherein R is a saturated aliphatic hydrocarbon group having 6 to 17 carbon atoms in Formula (I).4. The method according to claim 2 , wherein R is a saturated aliphatic hydrocarbon group having 6 to 17 carbon atoms in Formula (I).5. The method according to claim 1 , comprising administering externally the N-acyltryptamine represented by Formula (I) claim 1 , or a pharmaceutically acceptable salt claim 1 , hydrate or solvate thereof.6. The method according to claim 2 , comprising administering externally the N-acyltryptamine represented by Formula (I) claim 2 , or a pharmaceutically acceptable salt claim 2 , hydrate or solvate thereof.7. The method according to claim 3 , comprising administering externally the N-acyltryptamine represented by Formula (I) claim 3 , or a pharmaceutically acceptable salt claim 3 , hydrate or solvate thereof.8. The method according to claim 4 , comprising administering externally the N-acyltryptamine represented by Formula (I) claim 4 , or a pharmaceutically acceptable salt claim 4 , hydrate or solvate thereof. The present invention relates to an atopic dermatitis therapeutic agent which has a therapeutic effect equivalent to adrenocorticosteroid hormone and little side effect and exhibits an effect especially on itching.The number of patients with allergic diseases (allergic rhinitis, hay fever, bronchial asthma, atopic dermatitis and the like) has increased with change to the Westernized life style in recent years, and this is a great problem. Especially, atopic dermatitis is a disease frequently occurring in infants, with a prevalence of 10% or more among infants, and tends to be complicated with other atopic diseases with growth, and thus a disease about ...

Treatment of the pruritic symptoms of liver disease

The present disclosure relates to methods for treating patients with pruritus associated with liver disease with anti-pruritic compositions; methods for treating patients with pruritus associated with obstructive cholestasis secondary to bile duct obstruction due to non-hepatic tissue disease; and the anti-pruritic compositions used in such methods.

Salt of a pyrimido[6,1-a]isoquinolin-4-one compound

The present invention relates to a pharmaceutically acceptable acid addition salt of: (i) 9,10-dimethoxy-2-(2,4,6-tri-methylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one (RPL554); and (ii) ethane-1,2-disulfonic acid, ethanesulfonic acid, methanesulfonic acid, benzenesulfonic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, phosphoric acid or sulfuric acid.

SKIN PREPARATION COMPOSITION FOR EXTERNAL USE CONTAINING COMPLEX HYALURONIC ACID

Disclosed is a skin preparation composition for external use containing complex hyaluronic acid as an active ingredient, and specifically relates to a skin preparation composition for external use that contains hyaluronic acid, sodium hyaluronate, and hydrolyzed hyaluronic acid as active ingredients, and are excellent in an active oxygen scavenging effect, a wrinkle improvement effect, a moisturizing effect, a skin irritation relief effect, an acne prevention effect, an atopy improvement effect, and an anti-inflammatory effect, an hair damage prevention effect, and a hair loss prevention and hair growth effect. 1. A skin preparation composition for external use containing complex hyaluronic acid ,wherein complex hyaluronic acid obtained by mixing hyaluronic acid, sodium hyaluronate, and hydrolyzed hyaluronic acid is contained by 0.001 to 3 weight % with respect to the total composition.2. The skin preparation composition for external use containing complex hyaluronic acid according to claim 1 ,wherein the skin preparation composition for external use has an anti-aging effect.3. The skin preparation composition for external use containing complex hyaluronic acid according to claim 1 ,wherein the skin preparation composition for external use has an irritation relief function.4. The skin preparation composition for external use containing complex hyaluronic acid according to claim 1 ,wherein the skin preparation composition for external use has an atopic skin improvement function. The present invention relates to a skin preparation composition for external use containing complex hyaluronic acid as an active ingredient, and specifically relates to a skin preparation composition for external use that contains hyaluronic acid, sodium hyaluronate, and hydrolyzed hyaluronic acid as active ingredients, and are excellent in an active oxygen scavenging effect, a wrinkle improvement effect, a moisturizing effect, a skin irritation relief effect, an acne prevention effect, an ...

TREATMENT OF PRURITUS IN HORSES

The present invention relates to compositions, immunogenic or vaccine compositions and pharmaceutical compositions for the prevention or treatment of a condition or disorder selected from a pruritic condition or an allergic condition, of equine mammals, preferably of horses. Furthermore, the invention provides methods for preventing or treating pruritus, preferably pruritus associated with a pruritic condition or an allergic condition such as allergic dermatitis, of equine mammals, preferably of horses. 2. The composition for use of claim 1 , wherein said condition or disorder is not the prevention or treatment of insect bite hypersensitivity (IBH) of an equine mammal claim 1 , preferably of a horse.4. The composition for use of any one of the preceding claims claim 1 , wherein said eIL-31 antigen comprises claim 1 , or preferably is claim 1 , a protein with the amino sequence selected from SEQ ID NO:1 claim 1 , SEQ ID NO:2 claim 1 , SEQ ID NO:3 claim 1 , SEQ ID NO:4 claim 1 , SEQ ID NO:5.5. The composition for use of any one of the or claim 1 , wherein said eIL-5 antigen comprises claim 1 , or preferably is claim 1 , a protein with the amino sequence selected from SEQ ID NO:6 claim 1 , SEQ ID NO:7 claim 1 , SEQ ID NO:8 claim 1 , SEQ ID NO:9 and SEQ ID NO:10.6. The composition for use of any one of the preceding claims claim 1 , wherein said core particle is a virus-like particle (VLP) claim 1 , preferably a recombinant VLP claim 1 , and wherein preferably said second core particle is a virus-like particle (VLP) claim 1 , preferably a recombinant VLP.7. The composition for use of claim 6 , wherein said VLP is derived from a plant virus or is a VLP of an RNA bacteriophage claim 6 , and wherein preferably said VLP is a VLP of RNA bacteriophage Qβ claim 6 , wherein said VLP of RNA bacteriophage Qβ comprises claim 6 , consists essentially of claim 6 , or alternatively consists of claim 6 , recombinant coat proteins comprising or preferably consisting of SEQ ID NO:24.8. ...

CXCR2 ANTIBODIES AND USES THEREOF

The invention relates to CXCR2, to antibodies and related fragments thereof for binding to CXCR2, to production of said antibodies and fragments and to use of said antibodies and fragments for detection and therapy of various conditions. 1. A C-X-C motif chemokine receptor 2 (CXCR2) antibody comprising a light chain variable region and a heavy chain variable region , wherein said light chain variable region comprises:a CDR L1 as set forth in SEQ ID NO:1, a CDR L2 as set forth in SEQ ID NO:2 and a CDR L3 as set forth in SEQ ID NO:3; andwherein said heavy chain variable region comprises:a CDR H1 as set forth in SEQ ID NO:4, a CDR H2 as set forth in SEQ ID NO:5, and a CDR H3 as set forth in SEQ ID NO:6.2. A C-X-C motif chemokine receptor 2 (CXCR2) antibody comprising a light chain variable region and a heavy chain variable region , where in said light chain variable region comprises:a CDR L1 as set forth in SEQ ID NO:11, a CDR L2 as set forth in SEQ ID NO:12 and a CDR L3 as set forth in SEQ ID NO:13; andwherein said heavy chain variable region comprises:a CDR H1 as set forth in SEQ ID NO:14, a CDR H2 as set forth in SEQ ID NO:15, and a CDR H3 as set forth in SEQ ID NO:16.3. A C-X-C motif chemokine receptor 2 (CXCR2) antibody comprising a light chain variable region and a heavy chain variable region , wherein said light chain variable region comprises:a CDR L1 as set forth in SEQ ID NO:21, a CDR L2 as set forth in SEQ ID NO:22 and a CDR L3 as set forth in SEQ ID NO:23; andwherein said heavy chain variable region comprises:a CDR H1 as set forth in SEQ ID NO:24, a CDR H2 as set forth in SEQ ID NO:25, and a CDR H3 as set forth in SEQ ID NO:26.4. A C-X-C motif chemokine receptor 2 (CXCR2) antibody comprising a light chain variable region and a heavy chain variable region , wherein said light chain variable region comprises:a CDR L1 as set forth in SEQ ID NO:1, a CDR L2 as set forth in SEQ ID NO:2 and a CDR L3 as set forth in SEQ ID NO:3; andwherein said heavy chain variable ...

ANTIBODY TO FIBROSIS-RELATED MOLECULE AND MEDICAL APPLICATION THEREOF

The present invention provides an antibody to a fibrosis-related molecule and medical application thereof. The antibody of the present invention is an antibody that binds to CHL1 protein and an antibody that neutralizes the binding of the CHL1 protein to a fibroblast. 1. An antibody that binds to CHL1 protein , or an antigen-binding fragment thereof , wherein the antibody or the antigen-binding fragment thereof neutralizes the binding of the CHL1 protein to a non-immune and non-epithelial non-hemocyte cell of the lamina propria and a submucosal layer.2. An antibody that binds to CHL1 protein , or an antigen-binding fragment thereof , wherein the antibody is(1) an antibody having a heavy chain variable region having heavy chain CDR1 having the amino acid sequence set forth in SEQ ID NO: 1, heavy chain CDR2 having the amino acid sequence set forth in SEQ ID NO: 2 and heavy chain CDR3 having the amino acid sequence set forth in SEQ ID NO: 3, and a light chain variable region having light chain CDR1 having the amino acid sequence set forth in SEQ ID NO: 5, light chain CDR2 having the amino acid sequence set forth in SEQ ID NO: 6 and light chain CDR3 having the amino acid sequence set forth in SEQ ID NO: 7, or(2) an antibody that competes with the antibody (1) for binding to the CHL1 protein.3. The antibody or the antigen-binding fragment thereof according to claim 2 , wherein the antibody is (3) an antibody having a heavy chain variable region having the amino acid sequence set forth in SEQ ID NO: 4 and a light chain variable region having the amino acid sequence set forth in SEQ ID NO: 8 claim 2 , or (4) an antibody that competes with the antibody (3) for binding to the CHL1 protein.4. A pharmaceutical composition comprising an antibody or an antigen-binding fragment thereof according to and a pharmaceutically acceptable carrier.5. A method comprising administering to a subject in need thereof an antibody or an antigen-binding fragment thereof according to claim 1 , ...

Polymer matrix compositions comprising a high concentration of bio-fermented sodium hyaluronate and uses thereof

The present invention relates to stable polymer matrix compositions comprising high concentrations (from about 1.5% w/w to about 3.5% w/w) sodium hyaluronate obtained from a Streptococcus zooepidemicus source and a non-ionic polymer. The polymer matrix composition further comprises polyethylene glycol and methylparaben, and utilizes ingredients that are of pharmaceutical or compendial grade. The polymer matrix compositions may optionally comprise an active ingredient. The present polymer matrix compositions may be used in the treatment of wounds, burns, certain dermatological conditions, vaginal dryness, and in topical, transdermal delivery and sustained release of active ingredients.

Topically administered strontium-containing complexes for treating pain, pruritis and inflammation

Therapeutically-active compositions that combine strontium with at least one additional molecules that increase the overall therapeutic potency of the combination beyond the potency of any of the separate constituents. Specifically, the combinations perform two important functions; (1) they increase the ability of topically-applied strontium to inhibit both acute sensory irritation (e.g., pruritus and pain), redness, swelling and inflammation (collectively defined for purposes of this description, “irritation”) and the chronic irritation that is characteristic of and contributes to the development and maintenance of painful or pruritic neuropathic conditions; and (2) they decrease the strontium activated pathways that are known to enhance the development and maintenance of pain, pruritis and neuropathic conditions.

Stable topical compositions of fenoldopam

The present disclosure is directed to a topical composition, e.g., a physically and chemically stable topical composition of Fenoldopam comprising about 0.1% to about 5% by weight of Fenoldopam or a pharmaceutically acceptable salt thereof, at least one polyacrylamide-type gelling agent, at least one cellulose-type gelling agent, and at least one solvent, wherein the Fenoldopam is substantially solubilized in the composition, and wherein the composition is stable for at least twelve months at 25° C. and 60% relative humidity.

PHARMACEUTICAL COMPOSITIONS COMPRISING CANNABIDIOL AND BETA-CARYOPHYLLENE AND METHODS FOR THEIR USE

The disclosure describes compositions comprising beta-caryophyllene (BCP) and cannabidiol (CBD). The disclosure also describes compositions which further introduce low levels of THC. The disclosure further describes methods of making and using said compositions, including for the treatment of chronic pain, neurological disorders including epilepsy, addiction and inflammatory skin conditions. The disclosure further describes the use of fluorinated-CBD derivatives for treating inflammatory skin conditions. 1. A pharmaceutical composition for reducing inflammation , comprising Cannabidiol (CBD) and (E)-Beta Caryophyllene ((E)-BCP) , wherein the molar ratio of CBD to (E)-BCP is from about 1:1 to about 1:33.3.2. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition consists essentially of CBD and (E)-BCP.3. The pharmaceutical composition of claim 1 , wherein the molar ratio of CBD to (E)-BCP is from about 1:1 to about 1:30.4. The pharmaceutical composition of claim 1 , wherein the molar ratio of CBD to (E)-BCP is from about 1:1 to about 1:2.5. The pharmaceutical composition of claim 1 , wherein a single dose comprises a combined CBD and (E)-BCP content of 300-500 milligrams.6. The pharmaceutical composition of claim 1 , wherein the composition is an oral dose; a parenteral injection; a transdermal patch claim 1 , cream claim 1 , or ointment; or an oral mucosal absorption formulation.7. The pharmaceutical composition of claim 1 , wherein the composition is an oral dose.8. The pharmaceutical composition of claim 1 , wherein the composition is a parenteral injection.9. The pharmaceutical composition of claim 1 , wherein the composition is a transdermal patch claim 1 , cream claim 1 , or ointment.10. The pharmaceutical composition of claim 1 , wherein the composition is formulated for oral mucosal absorption.11. The pharmaceutical composition of claim 1 , wherein the composition is a sublingual dose.12. The pharmaceutical composition of claim 1 , ...

9,11-SECOSTEROIDS AND THE USE OF 9,11-SECOSTEROIDS IN PREPARING PHARMACEUTICAL COMPOSITIONS FOR INHIBITING INFLAMMATION

A method for inhibiting inflammatory in a subject is provided, comprising: administering a pharmaceutical composition comprising an effective amount of 9,11-secosteroids. 3. The method of claim 1 , wherein the 9 claim 1 ,11-secosteroids inhibits inflammation via inhibiting the superoxide anion generation by human neutrophils.4. The method of claim 1 , wherein the 9 claim 1 ,11-secosteroids inhibits inflammation via inhibiting the elastase release by human neutrophils.5. The method of claim 1 , wherein the effective amount of 9 claim 1 ,11-secosteroids is 1˜10 μM.6. The method of claim 1 , wherein the effective amount of 9 claim 1 ,11-secosteroids is 1.63˜8.07 μM. This application claims the benefit of TW patent Application No. 109126808, filed Aug. 7, 2020, which application is incorporated herein by reference.The present invention is related to a method for inhibiting inflammation by compounds extracted from coral. Particularly, the present invention is related to a method for inhibiting inflammation by 9,11-secosteroids.Inflammation is one aspect of the regular host reaction to injury or infection caused by toxic chemicals, dead cells, pathogens, irritants, or allergens. Neutrophils play an important role in a variety of infectious and inflammatory diseases so as to become an attractive target for therapeutic interventions.A lot of herbs and plant-derived compounds have been found to alleviate inflammation; however, very few sources have been identified in marine environments. Soft corals are reported to produce a variety of secondary metabolites with diverse pharmacological activities. Most of the metabolites from soft corals are sesquiterpenes, diterpenes, and steroids.The soft coral belongs to the order Alcyonacea, which has been shown to produce a remarkable diversity of steroids in large quantities. The 9,11-secosteroids found in marine invertebrates such as sponges, corals, ascidians, and mollusks can be structurally characterized by the C-9/11 oxidative ...

Nitric Oxide Releasing Pharmaceutical Compositions

The present invention generally relates to nitric oxide releasing pharmaceutical compositions and methods of using the same.

Water-in-oil emulsion

The present invention relates to a water-in-oil emulsion and its use as a skin care product, in particular as a cosmetic and as a (dermatologic) medicament for aged skin. The emulsion contains a disperse/internal aqueous phase comprising an α-hydroxy-C 2 -C 6 -carboxylic acid, a continuous/external oil phase and an emulsifier system, comprising polyglyceryl-3-polyricinoleate, sorbitan oleate and sucrose polystearate, wherein the emulsion has a pH of 1 to 5.

Bioactive compositions from ginseng plant (panax spp.) and methods for their production and use

The present invention relates to bioactive compositions (including, for example, bioactive serum fractions and bioactive extracts) derived from ginseng ( Panax spp.) fresh whole plant, a particular part of the plant (e.g., rhizome, roots, leaves, stems, flowers, fruit) or any combination of these plant parts. The bioactive serum fractions and bioactive extracts are free of or substantially free of pulegone and/or free of or substantially free of proteins. The present invention also provides products comprising the bioactive serum fractions and/or bioactive extracts. The present invention further provides methods of making and using the bioactive serum fractions and/or bioactive extracts. Further, the bioactive serum fractions and bioactive extracts have anti-inflammatory and/or anti-irritant and/or anti-aging activities.

Compositions and methods for treatment of inflammatory autoimmune diseases

Provided are compositions and methods for treatment of inflammatory autoimmune diseases. The composition comprises fexofenadine or terfenadine, and may further comprise another TNF-α activity inhibitor. The method comprises administering to a subject in need of treatment a therapeutically effective amount of fexofenadine, and optionally another TNF-α activity inhibitor.

TREATMENT OF INFLAMMATION

A method of treating an inflammatory disease or disorder is disclosed. The method comprises administering to the subject a therapeutically effective amount of a peptide comprising an amino acid sequence selected from the group consisting of SEQ ID NOs: 11-15. The inflammatory disease is not cancer, osteoporosis, rheumatic arthritis, osteoarthritis or angiogenesis-related eye disease. 1. A method of treating an inflammatory disease or disorder in a subject in need thereof , the method comprising administering to the subject a therapeutically effective amount of a peptide comprising an amino acid sequence selected from the group consisting of SEQ ID NOs: 11-15 , wherein said inflammatory disease is not cancer , osteoporosis , rheumatic arthritis , osteoarthritis or angiogenesis-related eye disease , thereby treating the inflammatory disease of disorder.2. The method of claim 1 , wherein said disease or disorder is atherosclerosis or a graft rejection disease.3. The method of claim 2 , wherein the graft rejection disease is selected from the group consisting of chronic graft rejection claim 2 , subacute graft rejection claim 2 , hyperacute graft rejection claim 2 , acute graft rejection and graft versus host disease.4. The method of claim 2 , wherein the graft rejection disease is graft versus host disease.5. The method of claim 1 , wherein the inflammatory disease or disorder is not associated with a behavioral condition.6. The method of claim 1 , wherein said inflammatory disease or disorder is associated with a type I interferon activity.7. The method of claim 1 , wherein the peptide is cyclic.8. The method of claim 1 , wherein the peptide is capable of binding to αVβ3 integrin.9. The method of claim 7 , wherein the N terminus of the peptide is bound to the C terminus of the peptide.10. The method of claim 9 , wherein the N terminal amino acid and the C terminal amino acids are cysteines.11. The method of claim 1 , wherein the peptide is no more than 20 amino acids ...

Process for the preparation of fluticasone propionate form i

The invention relates to a novel crystallisation process for preparing fluticasone propionate as crystalline form 1 polymorph with controlled particle size and suitable for micronisation. Said process comprises the step of dissolving fluticasone propionate in acetone or in a mixture of acetone and water and then adding this solution to water or to a mixture of water 10 and acetone, thereby causing fluticasone propionate to crystallise out of the solution as crystalline form.

BIASED POTENT OPIOID-LIKE AGONISTS AS IMPROVED MEDICATIONS TO TREAT CHRONIC AND ACUTE PAIN AND METHODS OF USING THE SAME

The present invention is directed to a compound having Formula (I) and its enantiomer: wherein the definitions of n, R, X, Y and Y, and Z are provided in the disclosure. The invention is also directed to pharmaceutical compositions of the disclosed compounds, as well as their use as opioid-like agonists in the treatment of pain. 4. The compound of and its enantiomer claim 1 , wherein X is OH and V is —C(O)ORor OR claim 1 , wherein each Ris H or a substituted or unsubstituted C-Calkyl.5. The compound of and its enantiomer claim 1 , wherein Z is —(CRR)W claim 1 , wherein Rand Rare each H claim 1 , W is a substituted or unsubstituted C-Caryl claim 1 , and m is an integer of 1 to 5.6. The compound of and its enantiomer claim 1 , wherein Z is —CHCHW claim 1 , wherein W is unsubstituted C-Caryl claim 1 , C-Caryl substituted with —F claim 1 , —Cl claim 1 , —Br claim 1 , —OH claim 1 , —NHor —NO claim 1 , unsubstituted C-Cheteroaryl claim 1 , or C-Cheteroaryl substituted with —F claim 1 , —Cl claim 1 , —Br claim 1 , —OH claim 1 , —NHor —NO.9. The compound of and its enantiomer claim 1 , wherein Rand Rare each independently H.10. The compound of and its enantiomer claim 1 , wherein m2 is 2 or 3.11. The compound of and its enantiomer claim 1 , wherein R is H or halogen.15. A pharmaceutical composition claim 1 , comprising a therapeutically effective amount of the compound of or its enantiomer together with a pharmaceutically acceptable carrier.16. The pharmaceutical composition of claim 15 , wherein the pharmaceutically acceptable carrier is selected from the group consisting of binders claim 15 , buffering agents claim 15 , coloring agents claim 15 , diluents claim 15 , disintegrants claim 15 , emulsifiers claim 15 , flavorants claim 15 , glidants claim 15 , lubricants claim 15 , preservatives claim 15 , stabilizers claim 15 , surfactants claim 15 , tableting agents claim 15 , and wetting agents claim 15 , and combinations thereof.17. The pharmaceutical composition of claim ...

Peptide analogues with an excellent moisturizing effect and use thereof

The present invention relates to a peptide analogue or a pharmaceutically acceptable salt thereof with excellent moisturizing effect, and use thereof for moisturization. More specifically, the present invention relates to a novel peptide analogue or a pharmaceutically acceptable salt thereof, a method for preparation thereof, a moisturizing cosmetic composition comprising the same as an active ingredient, and a pharmaceutical composition for prevention and treatment of xeroderma.

A COMPOSITION FOR PREVENTING OR TREATING PRURITUS

The present disclosure relates to a composition for preventing, improving or treating pruritus by using a naturally derived ingredient. The composition of the present disclosure may be used to improve or treat pruritus caused by various causes safely and effectively without the risk of side effects. 2. The composition according to claim 1 , wherein the pruritus is selected from a group consisting of paroxysmal pruritus claim 1 , winter itch claim 1 , pruritus ani claim 1 , pruritus vulvae claim 1 , pruritus scroti claim 1 , aquagenic pruritus claim 1 , scalp pruritus claim 1 , nasal pruritus claim 1 , neck itch claim 1 , oral pruritus and ocular pruritus.3. The composition according to claim 1 , wherein the pruritus is pruritus accompanied by an internal disease selected from a group consisting of cholestatic pruritus claim 1 , chronic renal failure claim 1 , malignant tumor claim 1 , iron-deficiency anemia claim 1 , polycythemia vera claim 1 , hyperparathyroidism claim 1 , hypoparathyroidism claim 1 , diabetes and acquired immune deficiency syndrome.4. The composition according to claim 1 , wherein the pruritus is pruritus accompanied by a psychocutaneous disorder selected from a group consisting of lichen simplex chronicus claim 1 , prurigo claim 1 , trichotillomania claim 1 , neurotic excoriation claim 1 , cutaneous behavior disorder and delusional parasitosis.5. The composition according to claim 1 , wherein the composition is in a form selected from a group consisting of a formulation for external application to the skin claim 1 , an aerosol claim 1 , a spray claim 1 , an eye drop claim 1 , an oral medication and an injection.8. The composition according to claim 7 , wherein the cosmetic composition is in the form of a tonic claim 7 , a shampoo claim 7 , a rinse claim 7 , a hair conditioner claim 7 , a hair spray claim 7 , a powder claim 7 , a gel claim 7 , a cream claim 7 , an essence claim 7 , a lotion claim 7 , a sol-gel claim 7 , an emulsion claim 7 , an ...

PHYSIOLOGICALLY ACTIVE PREPARATION COMPRISING N-ACETYL-GLUCOSAMINE FOR THE TREATMENT OF BACK PAIN

A physiologically active composition for use in a method for the prophylaxis and/or treatment of back pain comprises N-acetyl-glucosamine or a suitable derivative of N-acetyl-glucosamine. 110-. (canceled)11. A physiologically active composition comprising N-acetyl-glucosamine or a derivative of N-acetyl-glucosamine for use in a method for the prophylaxis and/or treatment of back pain.12. The composition according to claim 11 , further comprising silica.13. The composition according to claim 12 , wherein the silica is provided in the form of a constituent of a bamboo extract.14. The composition according to claim 11 , further comprising collagen.15. The composition according to claim 14 , wherein the collagen is provided in the form of a constituent of a collagen hydrolysate.16. The composition according to claim 11 , further comprising hyaluronic acid.17. The composition according to claim 16 , wherein the hyaluronic acid is provided in the form of a constituent of a collagen hydrolysate.18. The composition according to claim 11 , further comprising at least one of lysine and vitamin C.19. A physiologically active composition which comprises at least two components claim 11 , of which a first component is silica and a second component is N-acetyl-glucosamine or a derivative of N-acetyl-glucosamine.20. The composition according to claim 19 , wherein silica is provided in the form of a constituent of a bamboo extract.21. The composition according to claim 19 , further comprising at least one of collagen claim 19 , hyaluronic acid claim 19 , lysine and vitamin C.22. The composition according to in the form of an oral dosage form.23. The composition according to in the form of an oral dosage form.24. A nutritional supplement comprising the composition as in .25. A nutritional supplement comprising the composition as in .26. A method for the prophylaxis and/or treatment of back pain claim 19 , comprising:administering a physiologically active composition comprising N- ...

ANTI-INFLAMMATORY COMPOSITION COMPRISING ACYLHYDRAZONE DERIVATIVE

The present invention relates to a composition for preventing, alleviating or treating inflammatory diseases, comprising, as an active ingredient, an acylhydrazone derivative compound, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. an acylhydrazone derivative compound, a stereoisomer thereof or a pharmaceutically acceptable salt thereof, of the present invention, effectively inhibits inflammatory cytokines and inflammatory signaling pathways, thereby effectively alleviating symptoms of inflammatory diseases such as dermatitis. Therefore, the composition according to the present invention may be effectively used for the prevention, alleviation or treatment of inflammatory diseases. 118-. (canceled)20. The method of claim 19 , wherein Ris methyl claim 19 , and Ris methyl or ethyl.22. The method of claim 19 , wherein the inflammatory disease is selected from the group consist of dermatitis claim 19 , allergies claim 19 , psoriasis claim 19 , eczema claim 19 , pruritis claim 19 , itching of the skin claim 19 , hives claim 19 , idiopathic chronic urticaria claim 19 , scleroderma claim 19 , nasal polyps claim 19 , rhinitis claim 19 , chronic sinusitis claim 19 , nasal congestion claim 19 , nasal itching claim 19 , asthma claim 19 , chronic obstructive pulmonary disease claim 19 , rheumatoid arthritis claim 19 , conjunctivitis claim 19 , keratoconjunctivitis claim 19 , ophthalmitis claim 19 , dry eye claim 19 , heart failure claim 19 , arrhythmia claim 19 , atherosclerosis claim 19 , multiple sclerosis claim 19 , inflammatory bowel disease claim 19 , inflammatory pain claim 19 , neuropathic pain claim 19 , osteoarthritis pain claim 19 , and thyroid autoimmune disease.23. The method of claim 22 , wherein the inflammatory disease is dermatitis.24. The method of claim 23 , wherein the dermatitis is atopic dermatitis claim 23 , contact dermatitis or allergic dermatitis.25. The method of claim 19 , wherein the compound suppresses an expression of ...

Treatments of ocular allergy with alcaftadine

Compositions, kits and methods for the treatment or prevention of ocular allergies and inflammation and the symptoms thereof comprising alcaftadine or a pharmaceutically acceptable salt thereof.

Compositions and methods for treatment of diseases

A method for treating or preventing laminitis is provided comprising administering to an ungulate a therapeutically or prophylactically effective amount of a camelid protease inhibitor. Typically the ungulate is a horse and the camelid protease inhibitor is an inhibitor of equine metalloproteinases and equine serine proteases. The inhibitor may be isolated from blood from healthy camelid or may be generated by inoculating camelid with purified equine metalloproteinase enzymes and serine proteases or with snake venom metalloproteinases, such as those obtained from Bothrops jararaca . The inhibitor may a homodimer antibody or an antigen binding fragment of same. Also provided are compositions comprising such camelid protease inhibitors.

Methods Of Treating Pruritus

The present disclosure related to methods of treating pruritus in a subject by topically administering detomidine, or a pharmaceutically acceptable salt thereof, to the subject. 1. A method of treating pruritus as a symptom of a neurological condition in a subject in need thereof comprising topically administering to the subject a pharmaceutical composition comprising 0.01-5 wt % of detomidine.2. The method of claim 1 , wherein the pruritus is acute.3. The method of claim 1 , wherein the pruritus is chronic.4. The method of claim 1 , wherein the neurological condition is notalgia paresthetica claim 1 , brachioradial pruritus claim 1 , postherpetic neuralgia claim 1 , stroke claim 1 , small fiber neuropathy claim 1 , trigeminal trophic syndrome claim 1 , Creutzfeldt-Jakob disease claim 1 , chemotherapy-induced neuropathy claim 1 , HIV-related neuropathy or multiple sclerosis.5. The method of claim 1 , wherein the detomidine is detomidine hydrochloride.6. The method of claim 5 , wherein the detomidine hydrochloride is anhydrous detomidine hydrochloride.7. The method of claim 5 , wherein the detomidine hydrochloride is detomidine hydrochloride monohydrate.8. The method claim 1 , wherein the pharmaceutical composition is in the form of a gel claim 1 , a cream claim 1 , an ointment claim 1 , an emulsion claim 1 , an emu-gel claim 1 , a foam claim 1 , a suspension or a spray-patch.9. The method of claim 8 , wherein the pharmaceutical composition is in the form of a gel.10. The method of claim 1 , wherein the pharmaceutical composition comprises 0.033 wt % claim 1 , 0.1 wt % claim 1 , 0.33 wt % or 1 wt % detomidine.11. The method of claim 1 , wherein the pharmaceutical composition comprises detomidine as the sole active agent.12. The method of claim 1 , further comprising administering to the subject at least one additional active agent.13. The method of claim 12 , wherein the additional active agent is selected from the group consisting of corticosteroids claim 12 , ...

Veterinary compositions and methods of use therefor

Veterinary compositions comprising hyaluronic acid with a molecular weight of at least 800,000 Daltons and cannabidiol, veterinary compositions comprising hyaluronic acid with a molecular weight of at least 800,000 Daltons and cannabidiol Complex, and methods for treating ailments and/or symptoms of said ailments in non-human subjects in need thereof by administering an effective amount of such compositions.

SHIKIMATE ANALOGUES AND METHODS OF USE

The present disclosure, in at least certain embodiments, is directed to shikimate (shikimic acid) analogues and compositions thereof, kits which contain the shikimate analogues or compositions thereof, and methods of use of the compounds and compositions for treating epithelial surfaces before or following exposure to irritants, allergens, and toxic agents (for example, urushiol). 2. The composition of claim 1 , comprising a plurality of shikimate analogues.3. The composition of claim 1 , wherein the at least one secondary compound is selected from the group consisting of propylene glycol claim 1 , sodium metasilicate claim 1 , chlorhexidine claim 1 , diethanolamine claim 1 , borates claim 1 , zinc pyrithione claim 1 , ammonia claim 1 , trimethyl ammonia claim 1 , 3-(N-morpholino)propane sulfonic acid (MOPS) claim 1 , 1 claim 1 ,4-diazabicyclo[2.2.2]octane (DABCO) claim 1 , triethanolamine claim 1 , morpholine claim 1 , barium hydroxide claim 1 , 9-Azajulolidine claim 1 , sodium iodide claim 1 , potassium iodide claim 1 , Lugol's Iodine claim 1 , iodine tincture claim 1 , povidone-iodine claim 1 , benzalkonium chloride claim 1 , cetrimonium bromide claim 1 , Brilliant Green claim 1 , triarylmethane dyes claim 1 , Malachite green claim 1 , octenidine dihydrochloride claim 1 , phenoxyethanol claim 1 , USP Tincture of Iodine claim 1 , USP Strong Iodine Tincture claim 1 , 1 claim 1 ,3-dibromo-5 claim 1 ,5-dimethylhydantoin (DBDMH) claim 1 , methyl cellulose claim 1 , and methyl ethyl cellulose.4. The composition of claim 1 , wherein the at least one secondary compound is selected from the group consisting of glycols claim 1 , polyols claim 1 , alditols claim 1 , and saccharides.5. The composition of claim 1 , wherein the at least one secondary compound is a polysaccharide.6. The composition of claim 1 , wherein the at least one secondary compound is selected from the group consisting of pharmaceutically-acceptable excipients claim 1 , diluents claim 1 , carriers claim 1 ...

COMPOSITIONS INCLUDING BENZENESULFONAMIDE-CONTAINING NON-STEROIDAL ANTI-INFLAMMATORY DRUGS, SILK FIBROIN, AND A GELLING AGENT AND USES THEREOF

Provided herein are compositions that include a benzenesulfonamide-containing NSAID, silk fibroin, and a gelling agent. Also provided are kits that include any of these compositions, and methods of making any of these compositions. Also provided are methods of treating an inflammatory and/or pain condition in a subject and methods of reducing inflammation, pain, or fever in a subject in need thereof, that include administering a therapeutically effective amount of any of these compositions. 1163.-. (canceled)164. A composition comprising a benzenesulfonamide-containing non-steroidal anti-inflammatory drug (NSAID) , silk fibroin , and a gelling agent.165. The composition of claim 164 , wherein the gelling agent is selected from the group consisting of glycerol (glycerin) claim 164 , polyethylene glycol (PEG) claim 164 , sorbitol claim 164 , triethylamine claim 164 , 2-pyrrolidone claim 164 , alpha-cyclodextrin claim 164 , benzyl alcohol claim 164 , beta-cyclodextrin claim 164 , dimethyl sulfoxide claim 164 , dimethylacetamide (DMA) claim 164 , dimethylformamide claim 164 , ethanol claim 164 , gamma-cyclodextrin claim 164 , glycerol formal claim 164 , hydroxypropyl beta-cyclodextrin claim 164 , kolliphor 124 claim 164 , kolliphor 181 claim 164 , kolliphor 188 claim 164 , kolliphor 407 claim 164 , kolliphor EL (cremaphor EL) claim 164 , cremaphor RH 40 claim 164 , cremophor RH 60 claim 164 , d-alpha-tocopherol claim 164 , PEG 1000 succinate claim 164 , polysorbate 20 claim 164 , polysorbate 80 claim 164 , solutol HS 15 claim 164 , sorbitan monooleate claim 164 , poloxamer-407 claim 164 , poloxamer-188 claim 164 , Labrafil M-1944CS claim 164 , Lrabfil M-2125CS claim 164 , Labrasol claim 164 , Gellucire 44/14 claim 164 , Softigen 767 claim 164 , mono- and di-fatty acid esters of PEG 300 claim 164 , PEG 400 claim 164 , or PEG 1750 claim 164 , kolliphor RH60 claim 164 , N-methyl-2-pyrrolidone claim 164 , castor oil claim 164 , corn oil claim 164 , cottonseed oil claim 164 ...

THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF

The invention provides a method of treating a disease or condition in a mammal by administering a compound having the general formula I: 5. The method of claim 1 , wherein ring “B” is selected from the group consisting of cyclobutyl claim 1 , cyclopentyl claim 1 , and cyclohexyl.14. The method of claim 1 , wherein wherein n is 2 claim 1 , 3 claim 1 , 4 claim 1 , or 5.15. The method of claim 1 , wherein ring “A” is a 6-15 membered carbocycle claim 1 , a 6-10 membered aryl claim 1 , or a 4-6 membered heterocycle.18. The method of claim 1 , wherein Xis absent; Xis —O—; m is 1; and -(L)- is an optionally substituted Calkylene.19. The method of claim 1 , wherein wherein:ring “A” is a 6-15 membered carbocycle, a 6-10 membered aryl, or a 4-6 membered heterocycle;{'sup': '1', 'Xis absent;'}{'sup': '2', 'Xis —O—;'}m is 1; and{'sub': '1-4', '-(L)- is an optionally substituted Calkylene.'} This application is a divisional of U.S. application Ser. No. 16/685,335, filed 15 Nov. 2019, which is a continuation of U.S. application Ser. No. 15/896,970, filed 14 Feb. 2018, now abandoned, which is a continuation of International Application No. PCT/US2016/048477, filed 24 Aug. 2016, which claims the benefit of U.S. Provisional Application No. 62/210,891, filed 27 Aug. 2015. The entire content of the applications referenced above are hereby incorporated by reference.The present invention relates to organic compounds useful for therapy in a mammal, and in particular to inhibitors of sodium channel (e.g., NaV1.7) that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the modulation of sodium channels.Voltage-gated sodium channels are transmembrane proteins that initiate action potentials in nerve, muscle and other electrically excitable cells, and are a necessary component of normal sensation, emotions, thoughts and movements (Catterall, W. A., Nature (2001), Vol. 409, pp. 988-990). These channels ...

Process for preventing or slowing the appearance of unattractive signs, generated by pollutants present in the atmosphere, on the skin, the scalp, the hair or the mucous membranes

Process with the aim of preventing or slowing the appearance of unattractive signs, generated by the pollutants present in the atmosphere, on the skin, the scalp, the hair or the mucous membranes, or indeed of eliminating them, including a step of application of a cosmetic formulation for topical use, including at least one cosmetically acceptable excipient and an effective amount of at least one glycolic extract (GE) of a unialgal biomass of small multicellular macroalgae originating from the Florideophyceae class. The extract, for the use thereof in a therapeutic method for treating signs of irritation of the skin, the scalp or the mucous membranes, manifesting as redness, sensations of stinging and/or itching, signs of deterioration of the hair, manifesting as an increase in the porosity thereof, the dulling thereof, and/or the weakening thereof with regard to mechanical stresses.

NOVEL SPORICHTHYACEAE MICROORGANISM AND USE THEREOF

Provided is a microorganism of the genus belonging to the family Sporichthyaceae, or a culture thereof, or a composition for preventing, improving, or treating skin conditions or inflammatory diseases including the same. 1EpidermidibacteriumEpidermidibacterium. A novel microorganism of the genus (gen.) belonging to the family Sporichthyaceae and having the following mycological characteristics:(1) rod-shaped;(2) non-motile;(3) Gram-positive; and(4) non-spore-forming.2. The microorganism of claim 1 , wherein the microorganism further has any one of the following mycological characteristics:(1) oxidase- or catalase-negative;(2) MK-9(H4) is detectable therefrom;(3) a polar lipid is one or more selected from the group consisting of phosphatidylethanolamine (PE), phosphatidylinositol (PI), phosphatidylglycerol (PG), phosphatidylcholine (PC), and three unidentified lipids (UL); and(4) a DNA G+C content is 68.9 mol %.3EpidermidibacteriumEpidermidibacterium keratiniEpidermidibacterium keratini. The microorganism of claim 1 , wherein the microorganism of the genus is (sp.).4Epidermidibacterium keratini. The microorganism of claim 3 , wherein the has one or more of the following mycological characteristics:(1) 0.5 μm to 0.3 μm in length, and 0.3 μm to 0.1 μm in diameter;(2) colonies are round, convex, and pale yellow;(3) growth is observed on Reasoner's 2A (R2A) agar, but not on nutrient agar (NA), yeast extract malt extract agar (ISP 2), and trypticase soy agar (TSA);(4) growth is observed on R2A agar at 15° C. to 35° C. (optimum temperature: 25° C.), but not at 10° C. or 40° C.;(5) growth is observed at pH 5.0 to 6.5 and at a NaCl concentration of up to 10% (optimum pH 6.0, 0% NaCl);(6) nitrate is reduced to nitrite;(7) casein and starch are degraded, but DNA and carboxymethylcellulose are not degraded; and(8) characteristics described in Tables 1 to 3 are observed.5Epidermidibacterium keratini. The microorganism of claim 3 , wherein the comprises a 16S rRNA gene having a ...

Embelia concinna extract comprising flavonoids in cosmetic and pharmaceutical compositions

The present invention deals with an Embelia extract—preferably an extract from Embelia concinna titrated in flavonoids—, its process for preparation and its use in a cosmetical or pharmaceutical composition for the treatment of skin sensitivity, for the treatment of allergic reactions of the skin, for soothing and for the treatment of itching skin and for the regulation of inflammatory drifts in the skin

USE OF A PAR-1 ANTAGONIST FOR THE TREATMENT OF A CHRONIC INFLAMMATORY INTESTINAL DISEASE

Disclosed is the use of a PAR-1 antagonist, in particular selected from vorapaxar, atopaxar and 3-2-(chloro-phenyl)-1-[4-(4-fluoro-benzyl)-piperazine-1-yl]propenone, for the prevention and/or treatment of a chronic inflammatory disease of the intestine and of the colon in a mammal, in particular Crohn's disease.

Compounds and compositions as c-kit kinase inhibitors

The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of c-kit or c-kit and PDGFR (PDGFRα, PDGFRβ) kinases.

Analogs of Dextromethorphan with Balanced Receptor Activities

Substituted analogs of dextromethorphan (DM) are disclosed, which are shown to have substantial binding affinity at both NMDA and sigma-1 receptors, and which are degraded by human liver enzymes more slowly than dextromethorphan. The analogs are useful as alternatives to dextromethorphan, and can provide the same benefits without requiring co-administration of a cytochrome P-450 enzyme inhibitor.