ПРОИЗВОДНЫЕ БЕНЗОНАФТОАЗУЛЕНА, ПРИМЕНЕНИЕ ИХ В КАЧЕСТВЕ ПРОМЕЖУТОЧНЫХ ПРОДУКТОВ И ДЛЯ ПОЛУЧЕНИЯ ФАРМАЦЕВТИЧЕСКИХ КОМПОЗИЦИЙ, ПРЕДНАЗНАЧЕННЫХ ДЛЯ ИНГИБИРОВАНИЯ ПРОДУЦИРОВАНИЯ ФНО-alpha

Описываются производные бензонафтоазулена формулы (I), где Х представляет собой О или S; Y и Z означают водород; группы или означают структуры R1 представляет собой где R2 и R3 одновременно или независимо друг от друга могут представлять собой Н, С1-С4-алкил или вместе с N означают гетероцикл, выбранный из морфолинила, пиперидинила или пирролидинила; n - целое число от 0 до 3; m - целое число 1; Q1 и Q2 независимо друг от друга представляют собой кислород или группу , где y1 и у2 независимо друг от друга представляют собой водород или С1-С4-алкил. Описываются производные бензонафтоазулена формулы (Ia), отличающиеся от соединения формулы (I) тем, что R1 представляет собой C1-С7-алкил, замещенный гидроксилом, или С1-С7-алкилоксикарбонил. Соединения формулы (I) ингибируют продуцирование ФНО-α, и соединения формулы (Ia) являются промежуточными продуктами для получения соединений формулы (I). Описываются также применение соединений формулы (Ia), где R1 - COz Et, CH2OH для получения соединений ...

ПРОИЗВОДНЫЕ ГЛЮКОПИРАНОЗИЛОКСИПИРАЗОЛА И ИХ ПРИМЕНЕНИЕ В ЛЕКАРСТВЕННЫХ СРЕДСТВАХ

Данное изобретение относится к новым производным глюкопиранозилоксипиразола общей формулы где R - водород, низшие алкил, ацил, алкоксикарбонил, ацилоксиметил или алкоксикарбонилоксиметил; один из Q и Т представляет группу общей формулы (где Р - водород, низшие ацил или алкоксикарбонил); тогда как другой - низший алкил или галоген(низший алкил); R2 - водород, низшие алкил, алкокси, алкилтио, галоген(низший алкил) или галоген; и при условии, что Р не представляет водород, когда R - водород или низший алкил, их фармацевтически приемлемым солям, фармацевтическим композициям для предотвращения реабсорбции глюкозы в почке и проявляющим ингибиторную активность в отношении SGLT2 человека, фармацевтическим комбинациям, которые используются для предотвращения или лечения заболеваний, связанных с гипергликемией. 9 н. и 27 з.п. ф-лы, 6 табл.

4-ЗАМЕЩЕННЫЕ ИМИДАЗОЛ-2-ТИОНЫ И ИМИДАЗОЛ-2-ОНЫ В КАЧЕСТВЕ АГОНИСТОВ АЛЬФА2B- И АЛЬФА2C- АДРЕНЕРГИЧЕСКИХ РЕЦЕПТОРОВ

Изобретение относится к соединениям формулы где переменная Y в кольце является необязательной и представляет собой гетероатом, выбранный из N, О и S, при условии, что атом N является трехвалентным, а атомы О или S - двухвалентными; k - целое число от 0 до 1; n - целое число, равное 0, 1 или 2; р - целое число, равное 0, 1 или 2; Х означает О или S; пунктирные линии представляют собой связь или ее отсутствие при условии, что в кольце имеется только одна двойная связь, а две примыкающие пунктирные линии связью не являются; R1, R2, R3 и R4 независимо представляют собой Н, фенил, где указанная фенильная группа необязательно независимо замещена одним, двумя или тремя заместителями - C1-6-алкилом, SO3Н, N3, галогеном, CN, NO2, NH2, C1-6-алкокси, C1-6-тиоалкокси, C1-6-алкиламиногруппой, C1-6-диалкиламиногруппой, С2-6-алкинилом, С2-C6-алкенилом; 5- или 6-членный гетероарил, содержащий от 1 до 3 гетероатомов, выбранных из О, S и N, где указанные гетероарильные группы необязательно независимо замещены ...

НОВЫЕ НЕСТЕРОИДНЫЕ ПРОТИВОВОСПАЛИТЕЛЬНЫЕ ВЕЩЕСТВА, СОСТАВЫ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Настоящее изобретение относится к новым нестероидным противовоспалительным соединениям, представленным формулой I: где М представляет собой макролидную субъединицу формулы D представляет собой нестероидную субъединицу, полученную из нестероидного противовоспалительного средства, L представляет собой соединительную группу с формулой X1-(CH2)m-Q-(CH2)n-X2, или их фармацевтически допустимым солям или отдельным диастереоизомерам. Кроме того, настоящее изобретение относится к способу получения соединений формулы I (варианты), к фармацевтическому составу на основе соединений формулы I или их фармацевтически допустимых солей, а также к применению соединений формулы I или их фармацевтически допустимых солей для получения медикамента (варианты). Значение заместителей R1-R6, А, В, Е, U, Y, Z, W, S1, М, D, X1, X2, Q, m, n указаны в формуле изобретения. 7 н. и 4 з.п. ф-лы, 1 табл., 7 схем.

ПРОИЗВОДНЫЕ ФУМАРОВОЙ КИСЛОТЫ В КАЧЕСТВЕ ИНГИБИТОРА NF-kappaB

Предложено применение одного или нескольких незамещенных или замещенных диалкиловых эфиров фумаровой кислоты и моноалкиловых эфиров фумаровой в качестве специфического ингибитора транскрипции NF-kappaB-зависимого гена в фармацевтической композиции для лечения опосредованных NF-kappaB заболеваний, выбранных из группы, состоящей из прогрессирующей системной склеродермии, сифилитического остеохондрита (болезнь Вегера), Cutis marmorata, (Livedo Reticularis), болезни Бехчета, панартериита, неспецифического язвенного колита, васкулита, остеоартрита, подагры, артериосклероза, синдрома Рейтера, бронхолегочного грануломатоза, типов энцефалита, эндотоксического шока (септически-токсический шок), сепсиса, пневмонии, энцефаломиелита, нервно-психической анорексии, Т-лимфоматоза Реннерта, мезангиального нефрита, постангиопластического рестеноза, цитомегаловирусной ретинопатии, аденовирусных заболеваний, таких как аденовирусные простудные заболевания, аденовирусная фарингоконъюнктивальная лихорадка и ...

АМИНОБЕНЗОФЕНОНЫ КАК ИНГИБИТОРЫ ИЛ-1 БЭТА И TNF-АЛЬФА

Изобретение относится к соединению общей формулы I (I) где R1 означает независимо один или несколько одинаковых или различных заместителей, выбираемых из группы, состоящей из галогена, (С1-С3)алкила, (С1-С3)алкокси; при условии, что когда R1 означает один заместитель, он находится в ортоположении, и когда R1 означает более чем один заместитель, по меньшей мере один заместитель R1 находится в ортоположении; R2 означает один заместитель в ортоположении, причем указанный заместитель выбирают из группы, состоящей из галогена и (С1-С3)алкокси; R3 означает галоген; R4 означает водород; Х означает кислород; и его соль с фармацевтически приемлемой кислотой или их гидрат или сольват. Предложен способ получения соединения формулы I, включающей сочетание амина формулы II с кислотой формулы III или ее активированным производным, особенно трифторуксусным ангидридом. Предложена фармацевтическая композиция, обладающая ингибирующей активностью в отношении секреции 1β-интерлейкина, фактора α-некроза опухолевых ...

НОВАЯ СОЛЬ И МЕДИЦИНСКОЕ ПРИМЕНЕНИЕ

Изобретение относится к тозилату 4-[2-(5-Амино-1Н-пиразол-4-ил)-4-хлорфенокси]-5-хлор-2-фтор-N-(1,3-тиазол-4-ил)бензолсульфонамида. Данное соединение является кристаллическим веществом и характеризуется порошковой рентгенограммой (PXRD), которая имеет любые три, четыре, пять или шесть характеристических два тета (2θ) пиков, которые выбирают из группы, включающей 9,0, 9,3, 10,0, 10,7, 11,6, 12,5, 12,9, 13,2, 13,8, 14,4, 16,0, 16,6, 17,5, 17,8, 18,1, 21,4 и 23,4° (±0,2° 2θ), при использовании рентгеновского излучения CuKalpha1 (длина волны = 1,5406). Изобретение также относится к применению 4-[2-(5-амино-1Н-пиразол-4-ил)-4-хлорфенокси]-5-хлор-2-фтор-N-(1,3-тиазол-4-ил)бензолсульфонамида тозилата для изготовления медикамента для лечения боли, предпочтительно невропатической, ноцицептивной, или воспалительной боли, или для лечения заболевания, связанного с повышенными уровнями мочевой кислоты в крови. Технический результат - 4-[2-(5-амино-1Н-пиразол-4-ил)-4-хлорфенокси]-5-хлор-2-фтор-N-(1,3 ...

ЗАМЕЩЕННЫЕ БЕТА-КАРБОЛИНЫ

Изобретение относится к производным карболина общей формулы I где R3-H, -OH, -O-(С1-С6)-алкил, R4-N(R17)2, где R17-H, -(С1 -С6)-алкил, -С(O)-фенил, -С(O)-(С1-С10)-алкил, -С(O)-O-(С1-С6)-алкил, -S(O)y-R14, где у=0, 1 или 2, R14 -(С1-С6)-алкил, фенил, замещенный галогеном, или R4-NH2, -NH-C(O)-R15, где R15 - пирролидин, пиразолидин, фуран, пиридин, пиразин, имидазолин, изоксазолидин, 2-изоксазолин, тиофен, возможно замещенный CF3 или -(С1-С6)-алкилом; -(С3-С7)-циклоалкил, -N((R13)2, где R13-H или фенил при условии, что N(R13)2 не означает NH2; фенил, возможно замещенный -(С1-С6)-алкилом, -CF3, или два заместителя у фенила образуют диоксолановое кольцо, R5-H, или R4 и R5 вместе с атомом N образуют гетероцикл. Описан способ их получения. Соединения формулы I являются подходящими для получения лекарственных средств для профилактики и лечения заболеваний, в процесс развития которых вовлечена повышенная активность lkB. 2 н. и 4 з.п.ф-лы, 2 табл.

СПОСОБ ИНГИБИРОВАНИЯ АКТИВНОСТИ ЧЕЛОВЕЧЕСКОГО TNFα (ВАРИАНТЫ), ПРИМЕНЕНИЕ ВЫДЕЛЕННОГО АНТИТЕЛА ЧЕЛОВЕКА ИЛИ ЕГО АНТИГЕНСВЯЗЫВАЮЩЕГО ФРАГМЕНТА В КАЧЕСТВЕ КОМПОНЕНТА ДЛЯ ПРОИЗВОДСТВА ЛЕКАРСТВЕННОГО СРЕДСТВА (ВАРИАНТЫ) И ВЫДЕЛЕННОЕ ЧЕЛОВЕЧЕСКОЕ АНТИТЕЛО ИЛИ ЕГО АНТИГЕНСВЯЗЫВАЮЩИЙ ФРАГМЕНТ

Изобретение относится к области медицины и касается применения выделенных антител человека или его фрагментов в качестве компонента для производства лекарственного средства, которое специфически связывает фактор некроза опухоли α(hTNFα). Эти антитела обладают высокой аффинностью в отношении hTNFa (например Kd=10-8 М или менее), низкой скоростью диссоциации (например Koff=10-3 с-1 или менее) и нейтрализуют активность hTNFα in vitro и in vivo. Антитела, соответствующие изобретению, могут быть антителом полной длины или его антиген-связывающим фрагментом. Антитела или фрагменты антител, соответствующие изобретению, используют для детекции hTNFα и для ингибрования активности hTNFα, например, у человека, страдающего от нарушения, при котором активность hTNFα является вредной. Преимущество изобретения заключается в разработке новых высокоаффинных рекомбинантных антител к hTNFα или их фрагментов с низкой кинетикой диссоциацией. 8 н. и 7 з.п. ф-лы, 17 табл., 11 ил.

ХИНОЛИНОВЫЕ СОЕДИНЕНИЯ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ИХ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ЛЕКАРСТВЕННОГО СРЕДСТВА, ИНГИБИРУЮЩЕГО ТРАНСПОРТЕР УРАТОВ

Изобретение относится к области органической химии, а именно к производному хинолина формулы (А) или к его фармацевтически приемлемой соли, где Z выбран из O или -NH-; Wпредставляет собой N; Wпредставляет собой CR; Wпредставляет собой CR; Rвыбран из водорода и Rвыбран из метила; или Rвыбран из водорода и Rвыбран из этила; или Rвыбран из водорода и Rвыбран из изопропила; или Rи Rоба выбраны из метила; или Rи Rоба выбраны из этила; или Rи Rоба выбраны из н-пропила; Rвыбран из группы, включающей водород, галоген, C-C-алкил, C-циклоалкил, C-арил, гетероарил, выбранный из пиридина, где указанный алкил, арил или гетероарил независимо и необязательно замещены одним-тремя заместителями, которые выбраны из группы, включающей галоген, циано, оксо-, С-алкил, С-галогеналкил, -OR; Rвыбран из группы, включающей галоген, C-C-алкил, C-циклоалкил, C-арил, гетероарил, выбранный из пиридина, где указанный алкил, арил или гетероарил независимо и необязательно замещены одним-тремя заместителями, которые выбраны ...

ИСПОЛЬЗОВАНИЕ ПРОИЗВОДНЫХ (3-ТРИГАЛОМЕТИЛФЕНОКСИ)-(4-ГАЛОФЕНИЛ) УКСУСНОЙ КИСЛОТЫ ДЛЯ ЛЕЧЕНИЯ РЕЗИСТЕНТНОСТИ К ИНСУЛИНУ, ДИАБЕТА II ТИПА, ГИПЕРЛИПИДЕМИИ И ГИПЕРУРИКЕМИИ

Изобретение относится к усовершенствованным способам модулирования диабета II типа у млекопитающего и модулирования резистентности к инсулину, включающим введение указанному млекопитающему, нуждающемуся в этом, (-)стереоизомера соединения формулы I, в которой R выбран из группы, состоящей из гидрокси, низшего аралкокси, ди-низшего алкиламино-низшего алкокси, низшего алканамидо низшего алкокси, бензамидо-низшего алкокси, уреидо-низшего алкокси, N'-низшего алкил-уреидо-низшего алкокси, карбамоил-низшего алкокси, галофеноксизамещенного низшего алкокси, карбамоилзамещенного фенокси, или R представляет собой гидролизуемую сложноэфирную группировку; каждый Х независимо представляет собой галоген; или его фармацевтически приемлемой соли, причем (-)стереоизомер по существу не содержит (+)стереоизомера соединения. Изобретение также относится к фармацевтическим композициям, содержащим (-)стереоизомер соединения формулы I и где композиции обладают существенно сниженным ингибирующим эффектом на цитохром ...

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

Изобретение относится к производным амида формулы I где R3 представляет собой (1-6С)алкил или галоген; m равно 0, 1, 2 или 3; R1 представляет собой гидрокси, галоген, трифторметил, нитро, амино, (1-6С)алкил, (2-6С)алкенил, (2-6С)алкинил, (1-6С)алкокси, (1-6С)алкиламино, ди-[(1-6С)алкил] амино, амино-(2-6С)алкиламино, (1-6С)алкиламино-(2-6С)алкиламино и т.д. или R1 представляет собой арил, арил-(1-6С)алкил, гетероарил, гетероарил-(1-6С)алкил, гетероарилокси, гетероарил-(1-6С)алкокси, гетероциклил, гетероциклил-(1-6С)алкил или гетероциклилокси, р равно 0, 1 или 2; R2 представляет собой гидрокси, галоген, трифторметил, (1-6С)алкил или (1-6С)алкокси; R4 представляет собой амино, (1-6С)алкиламино, ди-[(1-6С)алкил] амино, амино-(1-6С)алкил, (1-6С)алкиламино-(1-6С)алкил и т.д. или R4 представляет собой гетероарил, гетероарил-(1-6С)алкил, гетероарилокси, гетероарил-(1-6С)алкокси, гетероциклил и т.д., q равно 0, 1, 2, 3 или 4 и Q2 представляет собой гетероарил, гетероарилокси или гетероарил-(1-6С ...

АМИНОБЕНЗОФЕНОНЫ

Изобретение относится к новым производным аминобензофенонов общей формулы I, обладающих свойствами ингибитора интерлейкина-1β(IL-1β) и фактора некроза опухоли(ТМР-α). Соединения могут найти применение для получения лекарственного средства для лечения и профилактики заболеваний, связанных с регулирующей системой цитокинов, таких как воспалительные заболевания. Изобретение также относится к фармацевтическим композициям и применению. В общей формуле I ! ! Х является кислородом; R1 является (C1-C3)алкилом, R2 является одним или более, одинаковыми или разными заместителями, выбранными из группы, включающей водород и галоген; R3 является одним или более, одинаковыми или разными заместителями, выбранными из группы, включающей водород и галоген, R4 является водородом, R5 является водородом, R6 является (C1-C10)алкил-гетероциклилом, (C1-C10)алкилом, (C2-C10)олефиновой группой, гетероциклилом, Y1R21, Y2R22 или Y4R24; где (C1-C10)алкил, (C2-C10)олефиновая группа замещены одним или более одинаковыми ...

СВОБОДНАЯ ОТ АГРЕГАТОВ УРАТОКСИДАЗА ДЛЯ ПРИГОТОВЛЕНИЯ НЕИММУНОГЕННЫХ ПОЛИМЕРНЫХ КОНЪЮГАТОВ

Изобретение относится к области медицины и может быть использовано в фармацевтической промышленности. Препарат уриказы грибков, бактерий, беспозвоночных или растений очищают от агрегатов уриказы, превышающих размеры октамера. Результирующий препарат уриказы содержит не более 2% указанных агрегатов от общего количества уриказных субъединиц. При связывании данного препарата с полиэтиленоксидом получают конъюгат активной уриказы. Полученный конъюгат активной уриказы используют в фармацевтической композиции для снижения уровня мочевой кислоты в жидкостях и тканях организма. Применение изобретения позволяет уменьшить иммуногенное действие уриказы, не ухудшая ее уриколитическое действие. 4 н. и 25 з.п. ф-лы, 14 ил.

МЕДИЦИНСКОЕ ПРИМЕНЕНИЕ АНЕМОЗИДА B4 ПРОТИВ ОСТРОГО ПОДАГРИЧЕСКОГО АРТРИТА

Группа изобретений относится к области медицины и фармацевтики и может быть использована для лечения острого подагрического артрита. Предложено применение анемозида B4 для получения лекарственного средства для лечения острого подагрического артрита, а также способ лечения острого подагрического артрита, включающий стадию введения анемозида В4 нуждающемуся пациенту. Изобретение обеспечивает новую альтернативную стратегию лечения острого подагрического артрита. 2 н. и 11 з.п. ф-лы, 2 табл., 2 пр.

СОДЕРЖАЩЕЕ КОНДЕНСИРОВАННУЮ КОЛЬЦЕВУЮ СТРУКТУРУ ПРОИЗВОДНОЕ И ЕГО ПРИМЕНЕНИЕ В МЕДИЦИНЕ

Настоящее изобретение относится к соединениям, представленным формулой (I), где Хи Xнезависимо представляют собой СН или N; кольцо U представляет собой бензольное кольцо, пиразольное кольцо, 1,2,4-оксадиазольное кольцо, 1,2,4-тиадиазольное кольцо, изотиазольное кольцо, оксазольное кольцо, пиридиновое кольцо, тиазольное кольцо или тиофеновое кольцо; m представляет собой целое число, имеющее значение от 0 до 1; n представляет собой целое число, имеющее значение от 0 до 3; Rпредставляет собой гидроксигруппу или Cалкил; Rпредставляет собой любой из (1)-(3): (1) атом галогена; (2) гидроксигруппу; (3) Cалкил, или Cалкокси, каждый из которых может независимо содержать любую группу, выбранную из группы заместителей α; группа заместителей α включает атом фтора и гидроксигруппу, или его фармацевтически приемлемая соль. Также изобретение относится к фармацевтической композиции, обладающей ингибирующей активностью в отношении ксантиноксидазы, включающей в качестве активного ингредиента соединение формулы ...

КОНДЕНСИРОВАННЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ПРОИЗВОДНЫЕ, СОДЕРЖАЩИЕ ИХ МЕДИЦИНСКИЕ КОМПОЗИЦИИ И ИХ МЕДИЦИНСКОЕ ПРИМЕНЕНИЕ

Настоящее изобретение относится к производному формулы (I) и его применению в качестве ингибитора натрийзависимого переносчика глюкозы (SGLT) человека для лечения заболеваний, связанных с гипергликемией: ! ! где А1 - О или S; А2 - СН или N; R1 или R4 - группа формулы (S): ! ! где R5, R6 - водород, гидроксил, галоген, алкил, алкокси-, алкилтио; Q - алкилен, алкенилен, алкилен-O-, алкилен-S-, -O-алкилен-, -S-алкилен-, алкилен-O-алкилен-, -алкилен-S-алкилен-; А - фенил; R2, R3 - водород; G - группа формул: ! ! или ! ! Е1 - водород, фтор, гидроксил; Е2 - водород, фтор, метил, гидроксиметил. Технический результат - получение новых ингибиторов SGLT человека. 5 н. и 10 з.п. ф-лы, 7 табл.

ПРОИЗВОДНЫЕ ПИРАЗОЛО [1,5-А] ПИРИДИНА, ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ И СПОСОБ ИХ ПОЛУЧЕНИЯ

Использование: в химико-фармацевтической промышленности. Сущность изобретения: производные пиразоло /1,5-a/ пиридина общей формулы I: где R1 - фенил, R2 - низший (алканоил) низший алкил, А - низший алкенилен или их фармацевтически приемлемые соли и способ их получения. Реагент I: соединения формулы II. Реагент II: производные пиперидина формулы III. Способ включает факультативные стадии удаления карбоксизащитных групп и/или получения соединений формулы I, где R2 означает амидированный карбокси (низший) алкил. Соединения являются антагонистами аденозина. Структура соединений формул I-III: 2 с. и 4 з.п. ф-лы.

СПОСОБ ПОЛУЧЕНИЯ ИНГИБИТОРОВ 5-ЛИПОКСИГЕНАЗЫ, ИМЕЮЩИХ РАЗЛИЧАЮЩИЕСЯ ГЕТЕРОЦИКЛИЧЕСКИЕ СИСТЕМЫ

Описан способ получения соединения формулы (1.3.0), где является группой, выбранной из формул (1.3.2), (1.3.3), (1.3.4) или (1.3.5), включающий образование реакционной смеси, состоящей из карбоксамида формулы (2.0.0) и соответствующего бициклического N-гетероцикла в апротонном растворителе в присутствии сильного основания в твердой форме, выбранного из группы, включающей гидроксид натрия и гидроксид калия, и (необязательно) в присутствии каталитического количества карбоната цезия, Cs2СО3 или катализатора межфазного переноса с последующим нагреванием указанной реакционной смеси в атмосфере азота, в результате чего образуется целевое соединение. Также раскрыты способ получения одного из конкретных соединений и способ получения мезилатной соли соединения. Изобретение представляет собой улучшенный способ получения известных и новых ингибиторов 5-липоксигеназы, полезных при лечении воспалительных заболеваний и аллергии. 4 с. и 4 з.п. ф-лы, 3 табл.

СРЕДСТВО ДЛЯ ЛЕЧЕНИЯ ГИПЕРУРИКЕМИИ

Орально применяемый терапевтический препарат для лечения гиперурикемии, содержит в качестве активного вещества соль оксипуринола - щелочную, щелочноземельную, N-метил-D-глюкаминовую. Соли оксипуринола менее токсичны, оказывают терапевтический эффект при более низких концетрациях, чем аллопуринол.

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 ...

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 ...

ЗАМЕЩЕННЫЕ БЕТА-КАРБОЛИНЫ

... 1. Соединение формулы I и/или стереоизомерная форма соединений формулы I, и/или физиологически приемлемая соль соединений формулы I, где B6, В7, В8 и В9 независимо выбраны из группы, состоящей из атома углерода и атома азота, где B6, В7, B8 и В9 вместе не представляют собой более двух атомов азота одновременно; где в случае а) заместители R1, R2 и R3, независимо один от другого, представляют собой 1.1 атом водорода, 1.2 галоген, 1.3 -CN, 1.4 -СООН, 1.5 -NO2, 1.6 -NH2, 1.7 -O-(C1-С10)-алкил, где алкил является незамещенным или моно-пента-замещенным, независимо один от другого 1.7.1 фенилом, который является незамещенным или моно-пента-замещенным галогеном или -О-(C1-C4)-алкилом, 1.7.2 галогеном, 1.7.3 -NH2, 1.7.4 -ОН, 1.7.5 -COOR16, где R16 представляет собой атом водорода или -(C1-С10)-алкил, 1.7.6 -NO2, 1.7.7 -S(O)y-R14, где y равно нулю, 1 или 2, R14 представляет собой -(C1 -С10)-алкил, фенил, который является незамещенным или моно-пента-замещенным, как определено для заместителей в 1.7.1 ...

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 ...

СПОСОБ ЛЕЧЕНИЯ РЕВМАТОИДНОГО АРТРИТА ПОСРЕДСТВОМ ЛЕКАРСТВЕННОГО ПРЕПАРАТА НА ОСНОВЕ ВЫДЕЛЕННОГО ЧЕЛОВЕЧЕСКОГО АНТИТЕЛА ИЛИ ЕГО АНТИГЕНСВЯЗЫВАЮЩЕГО ФРАГМЕНТА

... 1. Применение выделенного антитела человека или его антигенсвязывающего фрагмента, которое диссоциирует из человеческого TNFα с константой диссоциации K, составляющей по большей мере 1·10М, и константой скорости K, составляющей по большей мере 1·10с, где указанные константы определены посредством поверхностного плазменного резонанса, и нейтрализует цитотоксичность человеческого TNFα в стандартном анализе с использованием L929 in vitro с IC, составляющей по большей мере 1·10М, в качестве ингредиента при изготовлении лекарственного средства для лечения ревматоидного артрита посредством введения указанного средства в комбинации с метотрексатом.2. Применение по п.1, в котором выделенное антитело человека или его антигенсвязывающий фрагмент диссоциирует из человеческого TNFα с константой скорости K, составляющей по большей мере 5·10с.3. Применение по п.1, в котором выделенное антитело человека или его антигенсвязывающий фрагмент диссоциирует из человеческого TNFα с константой скорости K, составляющей ...

СПОСОБ СНИЖЕНИЯ УРОВНЯ МОЧЕВОЙ КИСЛОТЫ В ОРГАНИЗМЕ ЧЕЛОВЕКА

Способ снижения уровня мочевой кислоты в организме человека, включающий использование лекарственного растения, отличающийся тем, что в качестве основного действующего начала используют натуральную цельную микроводоросль спирулину платенсис с микроэлементом селен курсом по две таблетки два раза в день в течение 21-28 дней по показаниям, причем препарат принимают под контролем микроскопии сыворотки крови в динамике и при условии исчезновения кристаллов мочевой кислоты в форме зерен, лучей определяют нормализацию уровня мочевой кислоты.

ХИНОЛИНОВЫЕ СОЕДИНЕНИЯ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ИХ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ЛЕКАРСТВЕННОГО СРЕДСТВА, ИНГИБИРУЮЩЕГО ТРАНСПОРТЕР УРАТОВ

4-ЗАМЕЩЕННЫЕ ИМИДАЗОЛ-2-ТИОНЫ И ИМИДАЗОЛ-2-ОНЫ В КАЧЕСТВЕ АГОНИСТОВ АЛЬФА - 2В И АЛЬФА-2С АДРЕНЭРГИЧЕСКИХ РЕЦЕПТОРОВ

... 1. Соединения формулы где переменная Y в кольце является необязательной и представляет собой гетероатом, выбранный из N, О и S, при условии что атом N является трехвалентным, а атомы О или S - двухвалентными; k - целое число от 0 до 1; n - целое число, равное 0, 1 или 2; р - целое число, равное 0, 1 или 2; Х означает О или S; пунктирные лини представляют собой связь или ее отсутствие, при условии, что в кольце имеется только одна двойная связь, а две примыкающие пунктирные линии связью не являются; R1, R2, R3 и R4 независимо представляют собой Н, фенил, где указанная фенильная группа необязательно независимо замещена одним, двумя или тремя заместителями - C1-6-алкилом, SO3Н, N3, галогеном, CN, NO2, NH2, C1-6-алкокси, C1-6-тиоалкокси, C1-6-алкиламиногруппой, C1-6-диалкиламиногруппой, С2-6-алкинилом, С2-6-алкенилом; 5- или 6-членный гетероарил, содержащий от 1 до 3 гетероатомов, выбранных из О, S и N, где указанные гетероарильные группы необязательно независимо замещены одним, двумя или тремя ...

АМИДЫ ФУМАРОВОЙ КИСЛОТЫ

... 1. Применение амидов фумаровой кислоты общей формулы (I) R1 означает OR3 или связанный через амидную связь D- или L-аминокислотный остаток -NH-CHR4-COOH, где R3 означает атом водорода, линейную или разветвленную, незамещенную или замещенную (С1-С24 )-алкильную группу, фенильную группу или (С6-С10)-аралкильную группу и R4 означает боковую цепь природной или синтетической аминокислоты, и R2 означает связанный через амидную связь D- или L-аминокислотный остаток -NH-CHR5-COOH или связанный через амидную связь пептидный остаток из 2-100 аминокислот, где R5 означает боковую цепь природной или синтетической аминокислоты, для приготовления лекарственного средства (1) для лечения аутоиммунного заболевания, выбранного из группы, состоящей из полиартрита, рассеянного склероза, реакций “трансплантат против хозяина”, ювенильного диабета, тиреодита Хасимото, болезни Грейвса (или базедовой болезни), системной красной волчанки (SLE), синдрома Шегрена, пернициозной анемии и хронического активного (волчаночного ...

ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ НА ОСНОВЕ N-6 ЗАМЕЩЕННОГОАДЕНИНА, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ИХ ПРИМЕНЕНИЕ ДЛЯ ПРИГОТОВЛЕНИЯ ЛЕКАРСТВЕННЫХ ПРЕПАРАТОВ, КОСМЕТИЧЕСКИХ ПРЕПАРАТОВ И РЕГУЛЯТОРОВ РОСТА, ФАРМАЦЕВТИЧЕСКИЕ ПРЕПАРАТЫ, КОСМЕТИЧЕСКИЕ ПРЕПАРАТЫ И РЕГУЛЯТОРЫ РОСТА, СОДЕРЖАЩИЕ ЭТИ СОЕДИНЕНИЯ

... 1. Гетероциклические соединения, основанные на N6 -замещенном аденине с общей формулой I и его фармацевтически приемлемые соли, где R2 является водородом, галогеном, гидрокси-, алкокси-, амино-, гидразо-, меркапто-, метилмеркапто-, карбоксил-, циано-, нитро-, амидо-, сульфо-, сульфамидо-, ациламино-, ацилокси-, алкиламино-, диалкиламино-, алкилмеркапто-, циклоалкил- и карбамоил-группой, R6 является алкилом, замещенным алкилом, циклоалкилом, замещенным циклоалкилом, циклоалкилалкилом, арилалкилом, гетероалкилом, циклогетероалкилалкилом или R6’-X, где Х является -О-, -S-, -NH-, -N(C1-6 алкил)-; R6’ является водородом, алкилом, замещенным алкилом, ацилом, циклоалкилом, замещенным циклоалкилом, арилом, замещенным арилом, гетероциклом, гетероарилом, замещенным гетероарилом, арилалкилом, циклогетероалкилом, замещенным циклогетероалкилом, гетероарилалкилом, гетероалкилом, циклоалкилалкилом, циклогетеролкилом, амидо и сульфо; где родовые группы замещения имеют значения, идентичные определениям ...

Способ получения колхамина

Способ получения производных бензо/в/ тиофенона-2 или их солей

Способ получения средства для лечения пяточной шпоры и способ лечения пяточной шпоры

Использование: изобретение относится к медицине и касается способа получения средства для лечения пяточной шпоры. Целью изобретения является снятие болевого синдрома. Сущность изобретения заключается в смешивании чистотела в виде сухой травы в соотношении 0,7-0,8 или в виде листостебельной части 3,5 с водой до 100 мл, нагревания смеси до 90-95°С и последующего охлаждения до 70-75°С. Принятие ножных ванн ежедневно при температуре 40-70°С по 30-40 мин с последующим сухим компрессором в течение 6-8 ч. Положительный эффект заключается в снятии болевого синдрома в течение 10 процедур . 2 с.п.ф-лы, ...

Ein Arzneimittel zur Behandlung von Gicht und dessen Herstellungsverfahren

Die vorliegende Erfindung offenbart ein Arzneimittel zur Behandlung von Gicht und dessen Herstellungsverfahren. Das Medikament zur Behandlung von Gicht umfasst nach Gewichtsteilen Lotus Plumule 5-15, Spina Date Seed 10-15, Houttuynia cordata 13-20, Angelica sinensis 12-28 und Herba Pyrolae 5-12. Das Arzneimittel zur Behandlung von Gicht gemäß der vorliegenden Erfindung weist im Vergleich zu den Arzneimitteln des Standes der Technik andere Bestandteile auf und kann die Mängel der Arzneimittel im Stand der Technik überwinden.

VERFAHREN ZUR HERSTELLUNG NEUER PHENYLPIPERIDINDERIVATE

Heteroarylphenylpyrazolverbindungen zur Verwendung als analgetisches/entzündungshemmendes Mittel

4,6-DIPHENYLPYRIDINDERIVATE ALS ENTZÜNDUNGSHEMMENDE MITTEL

AROYLPYRIDINONE

SUBSTITUIERTE IMIDAZOLE MIT CYTOKIN-INHIBIERENDER WIRKUNG

Substituierte Pyrazole als P38-kinaseinhibitoren

CHEMICAL COMPOUNDS

BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES

Highly effective diuretic antihypertensives, i.e., benzofuran or benzothiophene derivatives having a substituted propenoyl group at the 5-position, which are classified into loop diuretics with less adverse effects and can be administered orally at a daily dosage of 0.5-200 mg or parenterally of 0.01-50 mg.

6-Vinyl-furo-(3,4-c)-pyridine derivatives

This invention relates to new 1,3-dihydro-6-vinyl-7-hydroxy-furo-(3,5-c)-pyridine derivatives of the general formula: wherein each of A1 and A2 independently represents various hydrocarbon substituents, to a process for the preparation of these compounds from the corresponding 7-chloromethyl derivative and to pharmaceutical composition containing them. The compounds are useful as diuretics.

Novel use

Chemical compounds

Therapeutic agents

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

2,3-Diaryl-pyrazolo (1,5-b) pyridazines derivatives their preparation and their use as cycooxygenase 2(cox-2) inhibitors

2-Aminopyridines containing fused ring substituents

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

Azaindoles.

Nicotinamide biaryl derivatives useful as inhibitors of PDE4 isozymes.

Il-8 receptor antagonists

Sulfonylbenzene compounds as anti-inflammatory/analgesic agents

Farnesyl protein transferase inhibitors for treating arthropathies

Orally administered controlled drug delivery system providing temporal and spatial control

New salt of thiazolidinedione and its polymorphs as antidiabetic agents and methods for obtaining them.

Substituted pyridinones as modulators of P38 MAP kinase.

Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compound and methods of treatment using the compounds are also disclosed.

Azaindoles.

The invention is directed to compositions containing physiologically active compounds of general formula (I) wherein R1 is aryl or heteroaryl: R2 represent hydrogen, acyl, cyano, halo, lower alkenyl or lower alkyl optionally substituted by a substituent selected from cyano, heteroaryl, heterocycloalkyl, -Z1R8,-C(=O)-NY3Y4,-CO2R8,-NY3Y4,-N(R6)-C(=O)-R7, -N(R6)-C(=O)-NY3Y4,-N(R6)-C(=O)-OR7,-N(R6)-SO2-R7,-N(R6)-SO2-NY3Y4 and one or more halogen atoms; R3 represents hydrogen, aryl, cyno, halo, heteroaryl, lower alkyl,-C(=O)-OR5 or -C(=O)-NY3Y; and X1 represents N.CH. C-halo, C-CN,C-R7,C-NY3Y4,C-OH, C-Z2R7, C-C(=O)-OR5, C-C(=O)-NY3Y4, C-N(R8)-C(=0)-R7,C-SO2-NY3Y4,C-N(R8)-SO2-R7,C-alkenyl or C-NO2; and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (I). Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.

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

Farnesyl protein transferase inhibitors for treating arthropathies.

The present invention is concerned with the finding that farnesyl protein transferase inhibitors are useful for preparing a pharmaceutical composition for treating arthropathies such as rheumatoid arthritis, osteoarthritis, juvenile arthritis, and gout.

Orally administered controlled drug delivery system providing temporal and spatial control.

A pharmaceutical composition in the form of tablets or capsules provides a combination of temporal and spatial control of drug delivery to a patient for effective therapeutic results. The pharmaceutical composition comprises a drug, a gas generating component, a swelling agent, a viscolyzing agent, and optionally a gel forming polymer. The swelling agent belongs to a class of compounds known as superdisintegrants (e.g., cross-linked polyvinylpyrrolidone or sodium carboxymethylcellulose). The viscolyzing agent initially and the gel forming polymer thereafter form a hydrated gel matrix which entraps the gas, causing the tablet or capsule to float so that it is retained in the stomach or upper part of the small intestine (spatial control). At the same time, the hydrated gel matrix creates a tortuous diffusion path for the drug, resulting in sustained release of the drug (temporla control). A preferred once daily ciprofloxacin formulation comprises 69.9% ciprofloxacin base, 0.34% sodium alginate ...

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).

New salt of thiazolidinedione and its polymorphs as antidiabetic agents and methods for obtaining them.

This invention relates to a new salt of thiazolidinedione and its polymorphs which has high hypoglycemiant activity and which are therefore potentially useful in the treatment and/or prophylaxis of diabetes and/or other alterations or complications inherent to diabetes, such as hyperglycemia or hyperlipidemia. This invention also relates to a methodfor making thereof.

Certain 1, 4, 5-Tri-substituted imidazole compounds useful as cytokine.

This invention relates to certain 5-(optionally substituted aryl or heteroaryl)-4-(optionally substituted heteroaryl)-1-(optionally substituted heterocyclyl or heterocyclylalkyl)or -1- optionally substituted alkyl or alkenyl - imidazoles and derivatives thereof. Synthetic processes for the preparation of said tri-substituted imidazoles is described. The aforementioned imidazoles are useful for treating cytokine mediated diseases. The compounds of the invention are incorporated into pharmaceutical compositions for use in treating cytokine related diseases.

New salt of thiazolidinedione and its polymorphs as antidiabetic agents and methods for obtaining them.

Therapeutic combinations for cardiovascular and inflammatory indications.

The preseni invention provides therapeutic combinations and methods for treating or preventing a hypercholes-Icrolemia-relatcd or an inflammation-related condition in a subject in need of such treatment or prevention. One therapeutic com-bination comprises an ASBT inhibitor combined with COX-2 inhibitor. A further therapeutic combination comprises an ASBT inhibitor, a COX-2 inhibitor and an HMG Co-A rcductasc inhibitor. Another therapeutic combination comprises a chromene COX-2 inhibitor and an HMG Co-A reductase inhibitor.

2,3-Diaryl-Pyrazolo[1,5-B] pyridazines derivatives, their preparation and their use as cyclooxygenase 2(COX-2) inhibitors.

The invention provides the compounds of formula (i)and pharmaceutically acceptable derivatives thereof in which: r0 is halogen, c1-6alkyl, c1-6alkoxy, c1-6alkoxy substituted by one or more fluorine atoms, or o(ch2)nr4r5; r1 and r2 are independently selected from h, c1-6alkyl, c1-6alkyl, substituted by one or more fluorine atoms, c1-6alkoxy, c1-6hydroxyalkyl, sc1-6alkyl, c(o)h, c(o)c1-6alkyl, c1-6alkylsulphonyl, c1-6alkoxy substituted by one or more fluorine atoms, o(ch2)nc02c1-6alkyl, o(ch2)nsc1-6alkyl, (ch2)nnr4r5, (ch2)nsc1-6alkyl or c(o)nr4r5; with the proviso that when r0 is at the 4-position and is halogen, at least one of r1 and r2 is c1-6alkylsulphonyl, c1-6alkoxy substituted by one or more fluorine atoms, o(ch2)nco2c1-6alkyl, o(ch2)nsc1-6alkyl, (ch2)nnr4r5 or (ch2)nsc1-6alkyl, c(o)nr4r5; r3 is c1-6alkyl or nh2; r4 and r5 are independently selected from h, or c1-6alkyl or, together with the nitrogen atom to which they are attached, form a 4-8 membered saturated ring; and n is 1-4 ...

Orally administered controlled drug delivery system providing temporal and spatial control

Sulfonylbenzene compounds as anti-inflammatory/analgesic agents.

This invention provides a compound of the formula or its pharmaceutically acceptable salt thereof, wherein a is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (i)are attached to ring atoms of ring a, which are adjacent to each other; r1 is optionally substituted aryl or heteroaryl, with the proviso that when a is pyrazole, r1 is heteroaryl; r2 is c1-4 alkyl, halo-substituted c1-4 alkyl, c1-4 alkylamino, c1-4 dialkylamino or amino; r3, r4 and r5 are independently hydrogen, halo, c1-4 alkyl, halo substituted c1-4 alkyl or the like; ot two of r3, r4 and r5 are taken together with atoms to which they are attached and form a 4-7 membered ring; r6 and r7 are independently hydrogen, halo, c1-4 alkyl, halo-substituted c1-4 alkyl, c1-4 alkoxy, c1-4 alkylthio, c1-4 alkylamino or n,n-di c1-4 alkylamino; and m and n are independently 1, 2, 3 ...

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents.

This invention provides a compound of the formula (i); or the pharmaceutically acceptable salts thereof, wherein y1, y2, y3, and y4 are independently selected from n, ch, etc., r1 is h, c1-8 alkyl, etc., q1 is 5-12 membered monocyclic or bicyclic aromatic ring optonally containing up to 4 heteroatoms selected from o,n and s,etc., a is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from o,n and s,etc.;B is c1-6 alkylene optionally substituted with an oxo group, etc.; w is nh, o, etc.; r2 is h,c1-4 alkyl, etc.; z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from o,n and s, etc.; l is halo, c1-4 alkyl,,etc.; m is0, 1 or 2; r3 and r4 are independently selected from o,n and s, etc.; l is halo, c1-4 alkyl ; r5 is h, c1-4 alkyl, etc.; q2 is a 5-12 membered monocyclic or bicyclic aromatic ring ortricyclic ring optionally containing up to 3 heteroatoms selected from o, n and s, etc. These compounds ...

Substituted Pyrazoles as P38 Kinase inhibitors

A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by formula (ia), wherein r1, r2, r3 and r4 are as described in the specification.

Substituted pyrazoles as P38 kinase inhibitors

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.

Azaindoles

Novel compounds

Heterocyclo-alkylsulfonyl pyrazole derivatives as ant-inflammatory/analgesic agents.

The present invention relates to compounds of formula (i)wherein r2, r3, r6 and a are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflamation and other inlamation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and alzheimers's disease, in mammals (preferably humans, dogs, cats and livestock) ...

2,3-Diaryl-pyrazolo (1,5-b) pyridazines derivatives their preparation and their use as cycooxygenase 2(cox-2) inhibitors

Substituted pyrazoles as p38 Kinase inhibitors.

A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by formula (i)wherein r1, r2, r3 and r4 are as described in the specification ...

2-aminopyridines containing fused ring substituents.

The present invention relates 2-aminopyridine derivatives oformula (i)or pharmaceutically acceptable salts threof, wherin a and b form a rring fused to the phenyl ring, said ring being satured or unsatured and containeing from 5to 7 ring member atoms, where said ring member atoms may optionally comprise from 1to2 heteroatoms selected independently from the group consisting of n, o, or s, provided that no two adjacent ring members are heteroatoms; x is oxygen or a single bond; y is (c1-c6)alkyl; r1 is hydrogen, (c1-c6)alkyl or a (c1-c6 alkyl)group substituted with-nr2r3 wherin r2 and r3 are either selected independently from the group consting of h, alkyl,aryl,aralkyl or tetrahydronaphthalene, wherin said aryl group or said aryl moiety of said aralkl group is phenyl or naphthyl, said alkyl group, or said alkyl moiety of said aralkyl group contains from one to six carbon atoms and is straight-chained or branched, and said tetrahydronaphthalene or said aryl moiety of said aralkyl group is ...

Farnesyl protein transferase inhibitors for treating arthropathies

Pteridinones as kinase inhibitors.

Disclosed are compounds of formulae (ia), (ib), (ic), (id)wherein w is nh, s , so, or so2; r2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heteocycle; q is hydrogen or lower alkyl; r4 and r6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and r8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or r8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks)and growth factor-mediated kinases. The present invention also provides a method of treating ...

Substituted pyridinones as modulators of P38 MAP kinase

Intraorally disintergrating valdecoxib compositions prepared by spray drying process

Orally disintergrating valdecoxib fast-melt tablets and processes for preparing such dosage forms are provided. The compositions are useful in treatment or prophylaxis of cycloosygenase-2 mediated conditions and disorders.

Benzamide and heteroarylamide as P2X7 receptor antagonists

The present invention relates to novel to P2X7 inhibitors of' formula (I) and to processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them, and their use in therapy. The active compounds of the present invention are potent inhihitors of P2X7 and as such are useful in the treatmentof inflammation, osteoarthrits, rheumatoid arthritis, cancer, reperfusion ischemia in stroke or heart attack, autoimmune diseases and other disorders.

Spiro-pyrimidine-2,4,6-Trione Metalloproteinase inhibitors

The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said "A" is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutical compositions and methods of treating inflamation, cancer and other disorders.

EP4 receptor inhibitors to treat rheumatoid arthritis.

The invention features a method of treating rheumatoid arthritis in a mammal comprising administering an agent that inhibits prostaglandin ep4 receptor (EP4) activity. Also featured is a method of identifying agents that selectively inhibit EP4 activity in vivo.

Azaindoles.

Il-8 receptor antagonists

Farnesyl protein transferase inhibitors for treating arthropathies

New salt of thiazolidinedione and its polymorphs as antidiabetic agents and methods for obtaining them.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

Azaindoles

Piperazinyl-, piperidinyl- and morpholinyl-derivatives as novel inhibitors of histone deacetylase.

Inhibitors of histone deacetylase.

Pteridinones as kinase inhibitors.

Carbonylamino-derivatives as novel inhibitors of histone deacetylase.

2-Aminopyridines containing fused ring substituents.

Ep-4 receptor inhibitors to treat rheumatoid arthritis.

Substituted pyridinones as modulators of P38 map kinase.

Collagen extraction from aquatic animals

The present invention relates to the use of fish skin as novel industrial source of collagen. Advantageously, said skin is obtained after the filleting or cutting of the fresh fish and frozen immediately after filleting/cutting, thus guaranteeing a very good quality of the base material, both from the bacteriological standpoint and from the standpoint of the native property of the protein.

Ameliorant for renal insufficiency

The present invention relates to an agent for improving renal dysfunction comprising as an active ingredient a compound represented by the following formula (1): wherein each R 1 , R 2 , and R 3 represents a hydrogen atom or a methyl group, and X represents a linear or branched alkylene or alkenylene group having 10 to 28 carbon atoms.

PEG-Urate Oxidase Conjugates and Use Thereof

A naturally occurring or recombinant urate oxidase (uricase) covalently coupled to poly(ethylene glycol) or poly(ethylene oxide) (both referred to as PEG), wherein an average of 2 to 10 strands of PEG are conjugated to each uricase subunit and the PEG has an average molecular weight between about 5 kDa and 100 kDa. The resulting PEG-uricase conjugates are substantially non-immunogenic and retain at least 75% of the uricolytic activity of the unmodified enzyme.

Reagents, Methods and Systems to Suppress Pro-Inflammatory Cytokines

The present invention relates to reagents, methods and systems to treat inflammation and pain in a subject using small interfering RNA (siRNA) molecules targeted to either TNFα, IL1 IL6 and other pro-inflammatory cytokines.

Corticosteroids for the Treatment of Joint Pain

Corticosteroid microparticle formulations are provided for use for treating pain, including pain caused by inflammatory diseases such as osteoarthritis or rheumatoid arthritis, and for slowing, arresting or reversing structural damage to tissues caused by an inflammatory disease, for example damage to articular and/or peri-articular tissues caused by osteoarthritis or rheumatoid arthritis. Corticosteroid microparticle formulations are administered locally as a sustained release dosage form (with or without an immediate release component) that results in efficacy accompanied by clinically insignificant or no measurable effect on endogenous cortisol production.

PEG-Urate Oxidase Conjugates and Use Thereof

A naturally occurring or recombinant urate oxidase (uricase) covalently coupled to poly(ethylene glycol) or poly(ethylene oxide) (both referred to as PEG), wherein an average of 2 to 10 strands of PEG are conjugated to each uricase subunit and the PEG has an average molecular weight between about 5 kDa and 100 kDa. The resulting PEG-uricase conjugates are substantially non-immunogenic and retain at least 75% of the uricolytic activity of the unmodified enzyme.

Anti-inflammatory drug

Provided is a new anti-inflammatory drug that produces an anti-inflammatory effect by modulating macrophage function. Specifically, a new anti-inflammatory drug that produces an anti-inflammatory effect through induction of M2 macrophages using activin species is provided.

Crystalline forms of febuxostat

New forms of Febuxostat have been prepared and characterized. These forms are useful, for example, in the chronic management of hyperuricemia in patients with gout.

Dexamethasone Formulations in a Biodegradable Material

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

Variant Forms of Urate Oxidase and Use Thereof

Genetically modified proteins with uricolytic activity are described. Proteins comprising truncated urate oxidases and methods for producing them, including PEGylated proteins comprising truncated urate oxidase are described.

Tetrazole compounds for reducing uric acid

Uric acid in mammalian subjects is reduced and excretion of uric acid is increased by administering a compound of Formula I. The uric acid-lowering effects of the compounds of this invention are used to treat or prevent a variety of conditions including gout, hyperuricemia, elevated levels of uric acid that do not meet the levels customarily justifying a diagnosis of hyperuricemia, renal dysfunction, kidney stones, cardiovascular disease, risk for developing cardiovascular disease, tumor-lysis syndrome, cognitive impairment, early-onset essential hypertension, and Plasmodium falciparum -induced inflammation.

Process for preparing biphenyl imidazole compounds

The invention provides processes for preparing intermediates useful for preparing compounds of the formula: or a salt thereof, where R 1-3 are as defined in the specification.

N-Acylated Hyaluronic Acid for Hyperuricemia and Gouty Arthritis

The invention provides a pharmaceutical composition of hyaluronic acid comprising repeating units of a disaccharide comprising glucuronic acid and N-acetylglucosamine, wherein a portion of the N-acetyl groups of the N-acetylglucosamine have been independently replaced with a group of the formula —N—C(O)—(C-C)-alkyl for treating hyperuicemia and gouty arthritis. Studies show that this composition is promising as an anti-gout therapeutic agent, which combines both anti-inflammatory actions as well as anti uracemic effects. 2. The pharmaceutical composition according to claim 1 , wherein the hyaluronic acid derivative is cross-linked.3. The pharmaceutical composition according to claim 1 , wherein R is —C(O)—(C)-alkyl.4. The pharmaceutical composition according to claim 1 , wherein the portion of N-acetyl groups which are replaced is at least about 10%.5. The pharmaceutical composition according to claim 1 , wherein the portion of N-acetyl groups which are replaced is between about 20% to about 80%.6. The pharmaceutical composition according to claim 1 , wherein the molecular weight is at least about 30 kDa.7. The pharmaceutical composition according to claim 1 , wherein the molecular weight is between about 20 kDa to about 250 kDa.8. A method for preventing or treating of a condition or disease selected from the group consisting of hyperuricemia claim 1 , gouty arthritis claim 1 , tophaceous gout claim 1 , gout claim 1 , gouty inflammation claim 1 , nephropathy claim 1 , liver disease claim 1 , liver damage claim 1 , or nonalcoholic fatty liver disease claim 1 , uric acid induced pain claim 1 , oxidative stress diseases claim 1 , acute gout claim 1 , uric acid nephropathy claim 1 , uric acid renal stones claim 1 , cardiovascular disease claim 1 , kidney diseases claim 1 , Duchenne Muscular Dystrophy claim 1 , Lesch-Nyhan syndrome claim 1 , psoriasis claim 1 , tumor lysis syndrome claim 1 , and urinary calculi claim 1 ,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, ...

LACTOBACILLUS PLANTARUM STRAIN TCI227 AND USES OF THE LACTOBACILLUS PLANTARUM STRAIN TCI227 FOR REGULATING EXPRESSION OF IL-1BETA GENE, TNF-ALPHA GENE, MMP1a GENE AND TIMP1 GENE, AND TREATING GOUT

The present disclosure provides a strain and a method for regulating expression of IL-1β gene, TNF-α gene, MMP1α gene and TIMP1 gene, and treating gout using the strain. 1Lactobacillus plantarum. A method for regulating expression of interleukin-1β (IL-1β) gene , tumor necrosis factor-α (TNF-α) gene , matrix metallopeptidase 1α(MMP1α) gene , and TIMP metallopeptidase inhibitor 1 (TIMP1) gene , comprising administering to a subject in need thereof a composition comprising an effective amount of a strain.2. The method according to claim 1 , wherein the expression of IL-1β gene claim 1 , TNF-α gene claim 1 , and MMP1α gene is down-regulated claim 1 , and the expression of TIMP1 gene is up-regulated.3Lactobacillus plantarum. The method according to claim 1 , wherein the effective amount of the strain is at least 5×10cells/mL.4Lactobacillus plantarum. The method according to claim 1 , wherein the strain comprises an inactivated bacterium.5. The method according to claim 1 , wherein the composition is a medicament or a food product.6Lactobacillus plantarum. The method according to claim 1 , wherein the strain is deposited in Deutsche Sammlung von Mikroorganismen and Zellkulturen under an accession number DSM 33287.7Lactobacillus plantarum. A method for treating gout claim 1 , comprising administering to a subject in need thereof a composition comprising an effective amount of a strain.8Lactobacillus plantarum. The method according to claim 7 , wherein the effective amount of the strain is at least 1×10cells/day.9Lactobacillus plantarum. The method according to claim 7 , wherein the strain comprises an inactivated bacterium.10. The method according to claim 7 , wherein the composition is a medicament or a food product.11Lactobacillus plantarum. The method according to claim 7 , wherein the strain is deposited in Deutsche Sammlung von Mikroorganismen und Zellkulturen under an accession number DSM 33287.12Lactobacillus plantarum. A strain for relieving gout claim 7 , which ...

Method for producing orotic acid derivative

Provided is a method for producing an orotic acid derivative, the method comprising a condensation step of performing, under a basic condition, a condensation reaction between an orotic acid halide represented by General Formula (I) and a compound represented by General Formula (II) to generate an orotic acid derivative represented by General Formula (III); and a neutralization crystallization step of precipitating crystals of orotic acid by neutralization crystallization to separate a liquid containing the orotic acid derivative from the crystals of orotic acid, after the condensation step. In General Formula (I), (II), or (III), X is a halogen atom, and A is a group represented by General Formula (A-1) or (A-2). In General Formula (A-1) or (A-2), R 1 is a hydrogen atom or an organic group, and R 2 and R 3 are each independently an organic group. In a case where R 1 is an organic group, R 1 and R 2 may be bonded to each other to form a ring.

Genetically modified mesenchymal stem cells expressing alpha-1 antitrypsin (aat)

Genetically modified mesenchymal stem cells can be used as a medicament in the treatment of medical conditions associated with inflammation and/or an unwanted immune response in subjects without an alpha1-antitrypsin (AAT) deficiency. The stem cells include an exogenous nucleic acid, which includes (i) an Alpha-1 antitrypsin (AAT) encoding region operably linked to (ii) a promoter or promoter/enhancer combination.

Bifunctional Compounds and Use for Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders or uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided.

Pharmaceutical formulation

Disclosed are aqueous pharmaceutical compositions which provide sustained released delivery of corticosteroid compounds. The pharmaceutical composition comprises a soluble corticosteroid and at least one viscosity enhancing agent. Also provided are methods for using the pharmaceutical compositions in an epidural injection, intra-articular injection, or an intra-lesional injection.

Methods for desensitization of uricase

Disclosed are methods for treating gouty arthropathy in a subject that is allergic to a uricase. In some aspect, disclosed herein are methods for desensitizing a subject allergic to a uricase.

Method involving 1-benzotriazolyl carbonate esters of poly(ethylene glycol)

The invention provides for preparing a polymer-active agent conjugate, the method comprising the steps of reacting an amino acid derivative with a biologically active agent under conditions to form a polymer-active agent conjugate.

Compounds and Their Use for Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders of uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided. 2. The compound according to claim 1 , wherein the 5-member heterocyclic ring of Formula (II) is a substituted or unsubstituted triazole.3. The compound according to ; wherein claim 1 , in Formula (II) claim 1 , —XRis —SCHor —OCH.46.-. (canceled)7. The compound according to claim 1 , wherein claim 1 , in Formula (I):a) X and W are each independently O or S;{'sub': '2', 'b) Y is OH or NH;'}{'sub': 3', '2, 'c) T is —C(NH)NH—, —NHC(O)—, —C(SCH)N—, —C(NOH)NH—, —C(N—NH)NH—, or —CONH;'}{'sup': '2', 'sub': '3', 'd) each Ron the barbiturate ring is independently H or CH;'}e) A is phenyl, branched cycloalkyl, or unbranched cycloalkyl; and{'sub': '3', 'f) Z, if present, is phenyl or CF.'}810.-. (canceled)1110. The compound according to claim ; wherein claim 1 , in Formula (III) claim 1 , f is —S(O)—.1213.-. (canceled)14. The compound according to claim 1 , wherein claim 1 , in Formula (IV) claim 1 , f is —NH— claim 1 , —C(O)— or —C(—O(CH)O—)—.15. The compound according to claim 14 , wherein X on the fused ring structure is O.1617.-. (canceled)18. The compound according to wherein claim 1 , in Formula (V) claim 1 , each Ris H.1920.-. (canceled)21. The compound according to claim 1 , wherein claim 1 , in Formula (VI) claim 1 , U is —O— or —NH— claim 1 , and the 5-member heterocyclic ring is triazole.2223.-. (canceled)24. The compound according to wherein claim 1 , in Formula (VII) claim 1 , the unfused 5-member heterocyclic ring is triazole.2526.-. (canceled)27. The compound ...

Compounds And Their Use For Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders of uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided. 2. The compound according to claim 1 , wherein the 5-member heterocyclic ring is substituted or unsubstituted triazole claim 1 , or substituted or unsubstituted pyrazole.3. The compound according to claim 1 , wherein Z is —OH or —CFon the 5-member heterocyclic ring and/or —CF3 on the phenyl ring.4. The compound according to claim 1 , wherein both Z are absent claim 1 , wherein Z is absent from the phenyl group and present on the 5-member heterocyclic ring claim 1 , or wherein Z is present on the phenyl group and absent from the 5-member heterocyclic ring.5. The compound according to claim 4 , wherein Z is absent from the phenyl group claim 4 , and Z on the heterocyclic 5-membered ring is CF.6. The compound according to claim 4 , wherein Z on the phenyl group is CF claim 4 , and Z is absent from the heterocyclic 5-membered ring.7. The compound according to claim 1 , which is selected from the group consisting of compounds having a structure represented by Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , Formula (I) claim 1 , and Formula (I) claim 1 , and tautomers thereof.8. (canceled)9. A pharmaceutical composition comprising a compound according to ; a tautomer thereof claim 1 , or a combination thereof claim 1 , and a pharmaceutically acceptable carrier.10. The pharmaceutical ...

THIAZOLE-5-CARBOXYLIC ACID DERIVATIVE AND PREPARATION METHOD AND USE THEREOF

The present disclosure relates to a thiazole-5-carboxylic acid derivative represented by Formula (I), a stereoisomer and/or pharmaceutically acceptable salt thereof. The compound of Formula (I), the stereoisomer and/or pharmaceutically acceptable salt thereof of the present disclosure can be used to prepare a medicament for preventing or treating hyperuricemia and/or gout, and can be prepared into dosage forms for various administration routes. The compounds provided in the present disclosure have good tolerance, safety and excellent uric acid-lowering activity. 2. The thiazole-5-carboxylic acid derivative according to claim 1 , wherein each of one or more hydrogen atoms of the above R claim 1 , R claim 1 , Rand Rgroups is independently substituted by halogen claim 1 , hydroxyl claim 1 , alkoxyl claim 1 , alkylcarbonyloxy claim 1 , aldehyde claim 1 , carboxyl claim 1 , alkylcarbonyl claim 1 , alkyloxycarbonyl claim 1 , alkylaminoalkyloxycarbonyl claim 1 , amino claim 1 , alkylamino claim 1 , alkyl claim 1 , hydroxyalkyl claim 1 , carboxyalkyl claim 1 , aminoalkyl or alkylaminoalkyl.3. The thiazole-5-carboxylic acid derivative according to claim 2 , wherein each of the R claim 2 , R claim 2 , Rand Ris independently selected from a hydrogen atom claim 2 , halogen claim 2 , hydroxyl claim 2 , oxo claim 2 , aldehyde claim 2 , carboxyl claim 2 , amino claim 2 , alkyl claim 2 , halogenated alkyl claim 2 , aminoalkyl claim 2 , aminoalkylamino claim 2 , alkoxyl claim 2 , alkyloxyalkyl claim 2 , alkyloxyalkyloxy claim 2 , alkylcarbonyl claim 2 , alkylcarbonyloxy claim 2 , alkyloxycarbonyl claim 2 , alkylamino claim 2 , alkylaminoalkyl claim 2 , hydroxylalkylamino claim 2 , hydroxylalkylamino alkyl claim 2 , alkylaminoalkyloxycarbonyl claim 2 , hydroxylalkyl claim 2 , hydroxylalkyloxy claim 2 , carboxylalkyl or aminoalkyl.4. The thiazole-5-carboxylic acid derivative according to claim 3 , wherein the alkyl is C-Calkyl.5. The thiazole-5-carboxylic acid derivative according to ...

DIMETHYL FUMARATE (DMF) FOR PREVENTION OR TREATMENT OF GOUT, ACNE, DIABETES, VITILIGO AND/OR PYODERMA GANGRENOSUM

A compound specified by formula (I), in particular dimethylfumarate (trans-1,2-ethylenedicarboxylic acid dimethyl ester) is provided for use in prevention or therapy of gout, acne, pyoderma gangrenosum, Vitiligo, cardiovascular disease, metabolic syndrome, diabetes and/or complications of diabetes. Also provided are a dosage form comprising said compound and a method of treatment comprising administration of said compound to a patient in need thereof. 2. The compound specified by formula (I) , wherein each R1 is methyl (CH) , for use in prevention or therapy of gout , acne , type 2 diabetes , Vitiligo and/or pyoderma gangrenosum.3. A dosage form comprising the compound according to for use in prevention or therapy of gout claim 1 , acne claim 1 , type 2 diabetes claim 1 , Vitiligo and/or pyoderma gangreno sum.4. A method of treatment or prevention of gout claim 1 , acne claim 1 , type 2 diabetes claim 1 , Vitiligo and/or pyoderma gangrenosum claim 1 , comprising administration of the compound according to to a patient in need thereof.5. A dosage form comprising the compound according to for use in prevention or therapy of gout claim 2 , acne claim 2 , type 2 diabetes claim 2 , Vitiligo and/or pyoderma gangrenosum.6. A method of treatment or prevention of gout claim 2 , acne claim 2 , type 2 diabetes claim 2 , Vitiligo and/or pyoderma gangrenosum claim 2 , comprising administration of the compound according to to a patient in need thereof. Dimethyl fumarate (DMF, CAS number 624-49-7) is approved as a drug for the treatment of psoriasis and multiple sclerosis (MS).DMF is known to be an NRF2 (Nuclear factor erythroid 2 related factor 2) activator: it activates the basic leucine zipper transcription factor NRF2. The expression of NRF2 target genes has thus been generally assumed to underlie the therapeutic effect of DMF.Other known NRF2 activators include Sulforaphane (SFN), tertiary butylhydrochinone (tBHQ), CDDO-imidazolide and 15-deoxy-Δ-12,14-prostaglandin J(15d-PGD ...

Scalable Production of Standardized Extracellular Vesicles, Extracellular Vesicle Preparations and Uses Thereof

Preparations comprising an enriched population of extracellular vesicles (nEVs) having a negatively charged surface, and that are CD81+ and CD9−, are provided. Improved processes and methods for producing an enriched population of nEVs from non-murine cells, especially human origin cells and/or tissues, are disclosed. Therapeutic methods for using the preparations, including for reducing brain inflammation and treatment of various pathologies associated with brain inflammation, such as by intravenous or intranasal administration, are also described. Methods and preparations for reducing brain inflammation associated with traumatic brain injury (TBI) are also disclosed. A method for treating a patient having suffered a mild traumatic injury (mTMI), or concussion, such as a sports-related head injury, is also disclosed. The nEVs are also demonstrated to reduce the expression level of IL-Iβ in brain tissue of an animal having had traumatic brain injury. Methods for improving cognitive function and performance in animals after a traumatic brain injury is also demonstrated using the preparations of nEVs disclosed herein.

MEDICAMENT FOR USE IN TREATING GOUT

A medicament for use in treating gout, the medicament being a glycoprotein, a mixture of polysaccharide and protein, a polypeptide or a protein. 1. A medicament for use in treating gout , characterized in that the medicament is a glycoprotein , or a mixture of polysaccharide and protein , or a polypeptide , or a protein.2. The medicament according to claim 1 , wherein the medicament is a marine algal glycoprotein.3. The medicament according to claim 2 , wherein the said glycoproteins comprises claim 2 , by weight content claim 2 , 1-99% sugar and 1-99% protein; the said marine algal glycoprotein comprises claim 2 , by weight content claim 2 , 1-99% sugar and 1-99% protein; the said mixture of polysaccharide and protein comprises claim 2 , by weight content claim 2 , 1-99% sugar and 1-99% protein.4. The medicament according to claim 2 , wherein a molecular weight of the glycoprotein is 0.2 to 3000 kDa; a molecular weight of the marine algal glycoprotein is 0.2 to 3000 kDa; as for the mixture of polysaccharide and protein claim 2 , a molecular weight of the polysaccharide is 0.2-3000 kDa claim 2 , and a molecular weight of the protein is 0.2-3000 kDa.5. The medicament according to claim 1 , wherein it comprises claim 1 , by weight content claim 1 , 1-99 portions of glycoprotein and 1-25 portions of glucuronic acid.6. The medicament according to claim 1 , wherein it comprises claim 1 , by weight content claim 1 , 1-99 portions of glycoprotein and 1-25 portions of glucuronic acid claim 1 , 2-9 portions of indigo naturalis.7. The medicament according to claim 2 , wherein the algae comprises one or more kinds of blue-green algae claim 2 , green algae claim 2 , red algae claim 2 , gold algae claim 2 , and brown algae.8achyranthes. The medicament according to claim 1 , wherein it comprises claim 1 , by weight content claim 1 , 1-99 portions of glycoprotein claim 1 , 8-14 portions of indigo naturalis claim 1 , and 7-13 portions of twotooth root.9achyranthes. The medicament ...

Sodium salt of uric acid transporter inhibitor and crystalline form thereof

Provided are a sodium salt of a uric acid transporter inhibitor and a crystalline form thereof, In particular, provided are a uric acid transporter (URAT1) inhibitor 1-((6-bromo-quinoline-4-yl)thio)cyclobutyl sodium formate (the compound of formula (I)), a crystal form I, and preparation method thereof. The obtained crystal form I of the compound of formula (I) has a good crystal form stability and chemical stability, and the crystallization solvent used has a low toxicity and low residue, and can be better used in clinical treatment.

A type of aryl benzofuran amidated derivative and medical use thereof

The present invention relates to a type of aryl benzofuran amidated derivatives, the medical use thereof, and the preparation method; said derivatives have antioxidation activity, and xanthine oxidase inhibitory activity, and can be used for antioxidation and for preparing compositions, drugs and health products and treating gout and hyperuricemia. 3. The aryl benzofuran amidated derivative of claim 1 , wherein applications of aryl benzofuran amidated derivative comprise preparing antioxidants claim 1 , clearing free radicals claim 1 , preparing xanthine oxidase inhibitors claim 1 , and compositions claim 1 , drugs and health care products for treating gout or hyperuricemia.4. The aryl benzofuran amidated derivative of claim 1 , wherein a synthesis method of aryl benzofuran amidated derivative is as follows:(1) mixing salvianolic acid C with a first inorganic base to obtain a first mixture, ultrasonically dissolving the first mixture in a first organic solvent to obtain a second mixture, and heating the second mixture and continuously detecting a reaction of the second mixture; after the reaction is completed, carrying out a first separation and purification method by silica gel column chromatography to obtain an intermediate Tournefolic acid A;{'sub': '2', '(2) adding SOClto a second organic solvent under ice bath cooling, and reacting for 30 min to obtain a first solvent, then adding amino compounds selecting from alanine, phenylalanine, cysteine, tyrosine, methionine, tryptophan, and D/L-DOPA to the first solvent to obtain a second solvent, stirring the second solvent at room temperature, concentrating and evaporating the second solvent by a second separation and purification method before washing and drying the second solvent to obtain series of carboxyl-protected amino derivatives;'}(3) mixing the intermediate Tournefolic acid A with the series of carboxyl-protected amino derivatives at a mole ratio of 1:1.1-2 under an action of a condensing agent to be a third ...

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING A SYMPTOM ASSOCIATED WITH GOUT OR HYPERURICEMIA

The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway. 2. The compound of claim 1 , wherein X is —OH and Ris H.3. The compound of claim 2 , wherein each of R claim 2 , R claim 2 , R claim 2 , and Ris deuterium.4. The compound of claim 2 , wherein each of R claim 2 , R claim 2 , and Ris deuterium and Ris —F.5. The compound of claim 2 , wherein Rand Rare deuterium and Rand Rare H.6. The compound of claim 2 , wherein Rand Rare H and Rand Rare deuterium.7. The compound of claim 1 , wherein X is —F and Ris H.8. The compound of claim 7 , wherein each of R claim 7 , R claim 7 , and Ris H claim 7 , and Ris deuterium.9. The compound of claim 7 , wherein each of R claim 7 , R claim 7 , and Ris H claim 7 , and Ris deuterium.10. The compound of claim 7 , wherein Rand Rare deuterium and Rand Rare H.11. The compound of claim 7 , wherein Rand Rare H and Rand Rare deuterium.12. The compound of claim 7 , wherein Rand Rare H and Rand Rare deuterium.13. The compound of claim 7 , wherein each of R claim 7 , R claim 7 , R claim 7 , and Ris deuterium.14. The compound of claim 1 , wherein X is —Cl and Ris H.15. The compound of claim 14 , wherein each of R claim 14 , R claim 14 , R claim 14 , and Ris deuterium.16. The compound of claim 1 , wherein X is —F and Ris —F.17. The compound of claim 16 , wherein each of R claim 16 , R claim 16 , R claim 16 , and Ris deuterium.19. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient.20. A method of treating hyperuricemia or gout in a mammal claim 1 , comprising administering to the mammal a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof. This application is a continuation of International Application No. PCT/US2017/041763, filed on ...

Methods of administering inhibitory anti-factor xii/xiia monoclonal antibodies

The invention relates to inhibitory anti-factor XII/FXIIa antibodies and methods of their use.

METHOD FOR REGULATING EXPRESSION OF IL-1b GENE, MMP1a GENE AND TIMP1 GENE OF CHONDROCYTES USING LACTOBACILLUS PLANTARUM STRAIN TCI227

The present disclosure provides a method for regulating expression of IL-1β gene, MMP1a gene and TIMP1 gene of chondrocytes using a strain TCI227. 1Lactobacillus plantarum. A method for regulating expression of interleukin-1β (IL-1β) gene , matrix metallopeptidase 1a (MMP1a) gene , and TIMP metallopeptidase inhibitor 1 (TIMP1) gene of chondrocytes , comprising administering to a subject in need thereof a composition comprising an effective amount of a strain.2. The method according to claim 1 , wherein the expression of IL-1β gene and MMP1a gene is down-regulated claim 1 , and the expression of TIMP1 gene is up-regulated.3Lactobacillus plantarum. The method according to claim 1 , wherein the effective amount of the strain is at least 5×10cells/mL.4Lactobacillus plantarum. The method according to claim 1 , wherein the strain comprises an inactivated bacterium.5. The method according to claim 1 , wherein the composition is a medicament or a food product.6the Lactobacillus plantarum. The method according to claim 1 , wherein strain is deposited in Deutsche Sammlung von Mikroorganismen and Zellkulturen under an accession number DSM 33287. This application is a division of U.S. patent application No. 16/693,758, filed on Nov. 25, 2019, which claims priority to Taiwan patent application No. 108123471, filed on Jul. 3, 2019, the entirety of which are incorporated herein by reference.The contents of the electronic sequence listing (P200725USI-D1_ST25.txt; Size: 1.7 KB; and Date of Creation: Dec. 3, 2021) is herein incorporated by reference in its entirety.The present invention relates to a method of a strain TC1227 for regulating expression of IL-1β gene, MMP1a gene and TIMP1 gene of chondrocytes.Gout, also known as hyperuricemia, is mainly a purine metabolic disorder. When the human body cannot metabolize purine from the human body, the purine in the body would further oxidize to form uric acid. The uric acid would deposit in the joints in the form of sodium salts, causing ...

Method of making longan seed extract

A method of making longan seed extract is provided with choosing an extraction solvent; heating the extraction solvent to a first predetermined temperature; adding pulverized longan seed to the extraction solvent to prepare a solution; maintaining the solution at a second temperature for a predetermined period of time to obtain an extracted substance; filtering the extracted substance; and drying and cooling the filtered extracted substance to produce an extract.

Method for evaluating urate transport-related disease factor and inflammation-related disease factor

A method and evaluation kit are provided, in which a high-capacity urate transporter is identified to assist in the early treatment and prevention of urate transport-related disease and inflammation-related disease. The method can include a step for detecting variations in genes that encode ABCG2 protein. When a subject has an SNP of V12M, R113X, Q126X, Q141K, F2085, G268R, E334X, S441N, L447V, S486N, F506SfsX4, R575X, and/or C608X, it can be concluded that the subject has a factor that is capable of inducing urate transport failure, or a state or disease attributable to that failure. When a subject has an SNP of V12M, it can be concluded that, unlike the other SNPs, there is a possibility that the subject does not possess such a factor because, although this variation itself does not lead to a change in urate transport capability, said variation is related to linkage disequilibrium with other SNPs.

CRYSTAL AND SALT OF 4-(NAPHTHALEN-1-YL)-4H-1,2,4-TRIAZOLE COMPOUND AND PREPARATION METHOD THEREFOR

Disclosed are a crystal of a 4-(naphthalene-1-yl)-4H-1,2,4-triazole compound (1) and a preparation method therefor, also comprised are applications of the crystal in preparing a medicament for treating an abnormal uric acid level-related disease. 2. The crystal form A claim 1 , crystal form D or amorphous form I of compound 1 as defined in claim 1 , wherein the crystal form A of compound 1 has an X-ray powder diffraction pattern comprising characteristic diffraction peaks at angle 2θ of 7.16±0.2° claim 1 , 12.50±0.2° claim 1 , 14.61±0.2° claim 1 , 17.98±0.2° claim 1 , 19.62±0.2° claim 1 , 22.30±0.2° claim 1 , 24.63±0.2° claim 1 , and 26.37±0.2°;and/or, the crystal form D of compound 1 has an X-ray powder diffraction pattern thereof comprising characteristic diffraction peaks at angle 2θ of 9.19±0.2°, 10.87±0.2°, 11.63±0.2°, 13.72±0.2°, 14.41±0.2°, 16.90±0.2°, 19.95±0.2°, and 22.22±0.2°.3. The crystal form A claim 2 , crystal form D or amorphous form I of compound 1 as defined in claim 2 , wherein the crystal form A of compound 1 has an X-ray powder diffraction pattern comprising characteristic diffraction peaks at angle 2θ of 7.16±0.2° claim 2 , 9.56±0.2° claim 2 , 11.30±0.2° claim 2 , 12.50±0.2° claim 2 , 14.61±0.2° claim 2 , 17.98±0.2° claim 2 , 18.72±0.2° claim 2 , 19.62±0.2° claim 2 , 22.30±0.2° claim 2 , 24.63±0.2° claim 2 , and 26.37±0.2°;and/or, the crystal form D of compound 1 has an X-ray powder diffraction pattern comprising characteristic diffraction peaks at angle 2θ of 9.19±0.2°, 10.87±0.2°, 11.63±0.2°, 13.72±0.2°, 14.41±0.2°, 16.90±0.2°, 19.95±0.2°, 22.22±0.2°, and 26.11±0.2°.4. The crystal form A claim 3 , crystal form D or amorphous form I of compound 1 as defined in claim 3 , wherein the crystal form A of compound 1 has an X-ray powder diffraction pattern as shown in ;{'figref': {'@idref': 'DRAWINGS', 'FIG. 19'}, 'and/or, the crystal form D of compound 1 has an X-ray powder diffraction pattern as shown in .'}5. The crystal form A claim 1 , crystal ...

Methods and Compositions for the Treatment of Pain and/or Inflammation

Pharmaceutical and veterinary compositions for oral administration comprising a therapeutically effective amount of at least one coxib together with a therapeutically effective amount of pentosan polysulfate or a pharmaceutically acceptable salt thereof are described. The compositions have application for the prophylaxis or treatment of pain and/or inflammation. There is also described a pharmaceutical or veterinary composition comprising a therapeutically effective amount of at least one coxib. The compositions in at least some forms may be lactose free and/or provided in a non-gelatin capsule. Further, there are provided methods for administration of a therapeutically effective amount of at least one coxib in combination with pentosan polysulfate or a pharmaceutically acceptable salt thereof for the prophylaxis or treatment of pain and/or inflammation.

COMPOSITION FOR PREVENTING, AMELIORATING, OR TREATING HYPERURICEMIA OR METABOLIC DISORDERS RELATED WITH HYPERURICEMIA COMPRISING EXTRACT OF ALPINIA OXYPHYLLA AS EFFECTIVE INGREDIENT

The present invention relates to a composition for preventing, ameliorating, or treating hyperuricemia or metabolic disorders related with hyperuricemia comprising an extract of as an effective ingredient. Because the extract of of the present invention can reduce the uric acid amount in blood of an animal model and is derived from natural products, and the raw materials can be easily obtained, it can be widely used in industries that are related to hyperuricemia or metabolic disorders related with hyperuricemia. It can be effectively used for prevention, amelioration, or treatment of gout or gouty arthritis, in particular. 18-. (canceled)9Alpinia oxyphylla. A method for preventing or treating hyperuricemia or metabolic disorder related with hyperuricemia , the method comprising administering to a subject in need thereof a composition comprising an extract of as an effective ingredient.10. The method of claim 9 , wherein the subject suffers from hyperuricemia.11. The method of claim 9 , wherein the subject suffers from the metabolic disorder related with hyperuricemia12. The method of claim 9 , wherein the subject suffers from the metabolic disorder related with hyperuricemia selected from the group consisting of acute gout claim 9 , chronic gout claim 9 , gouty flare claim 9 , gouty arthritis claim 9 , gouty kidney stone claim 9 , gouty nephropathy claim 9 , and a combination thereof.13Alpinia oxyphylla. The method of claim 9 , wherein the extract of is extracted by using C-Clower alcohol claim 9 , water claim 9 , or a mixture thereof as a solvent.14. The method of claim 9 , wherein the composition is included in a functional health food.15. The method of claim 9 , wherein the composition is a pharmaceutical composition.16. The method of claim 15 , wherein the pharmaceutical composition further comprises a uric acid salt-lowering agent.17. The method of claim 16 , wherein the uric acid salt-lowering agent is at least one selected from the group consisting of ...

Inhibitory anti-factor xii/xiia monoclonal antibodies and their uses

The invention relates to inhibitory anti-factor XII/FXIIa antibodies and methods of their use.

Composition for preventing or treating uric acid-related disease

Disclosed in the present invention is use of lysozyme in the preparation of a drug for preventing or treating a uric acid-related disease, a drug for reducing uric acid, and a drug for promoting uric acid excretion. Also disclosed in the present invention are a pharmaceutical composition for preventing or treating a uric acid-related disease, a pharmaceutical composition for reducing uric acid, and a pharmaceutical composition for promoting uric acid excretion, and a method for preventing or treating a uric acid-related disease, reducing uric acid and promoting uric acid excretion.

Compounds and Their Use for Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders associated with excess uric acid, and for maintaining normal uric acid levels in blood or serum, or the whole body, are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided. 2. The compound according to claim 1 , wherein three of a claim 1 , b claim 1 , c claim 1 , d claim 1 , and e are nitrogen.3. The compound according to claim 1 , wherein Ris —CH.4. The compound according to claim 3 , wherein —XRis —SCHor —OCH.5. The compound according to claim 4 , wherein A is substituted phenyl.6. The compound according to claim 5 , wherein A is —CFsubstituted phenyl7. The compound according to claim 6 , which has a structure represented by Formula (II).8. The compound according to claim 1 , which is selected from the group consisting of compounds having a structure represented by Formula (II) Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula ( ...

INDOLIZINE DERIVATIVES, COMPOSITION AND METHODS OF USE

Provided are certain URAT1 inhibitors, pharmaceutical compositions thereof, and methods of use therefor. 4. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein L is selected from O and S.5. A compound of or a pharmaceutically acceptable salt thereof claim 4 , wherein L is S.6. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Rand Rare independently selected from Calkyl claim 1 , and optionally substituted with 1 claim 1 , 2 or 3 Rgroups claim 1 , or Rand Rtogether with the carbon atom to which they are attached form a ring of 3 to 7 members containing 0 claim 1 , 1 claim 1 , or 2 heteroatoms independently selected from oxygen claim 1 , sulfur and nitrogen claim 1 , and optionally substituted with 1 claim 1 , 2 or 3 Rgroups.7. A compound of or a pharmaceutically acceptable salt thereof claim 6 , wherein Rand Rtogether with the carbon atom to which they are attached form cyclopropyl claim 6 , cyclobutyl claim 6 , cyclopentyl or cyclohexyl claim 6 , and optionally substituted with 1 claim 6 , 2 or 3 Rgroups.8. A compound of or a pharmaceutically acceptable salt thereof claim 7 , wherein Rand Rtogether with the carbon atom to which they are attached form cyclobutyl claim 7 , and optionally substituted with 1 claim 7 , 2 or 3 halogen claim 7 , Calkyl claim 7 , OH claim 7 , or Calkoxy.9. A compound of or a pharmaceutically acceptable salt thereof claim 8 , wherein Rand Rtogether with the carbon atom to which they are attached form cyclobutyl claim 8 , and optionally substituted with 1 claim 8 , 2 or 3 F claim 8 , methyl claim 8 , OH claim 8 , or OCH.10. A compound of or a pharmaceutically acceptable salt thereof claim 6 , wherein Rand Rare methyl claim 6 , and optionally substituted with 1 claim 6 , 2 or 3 Rgroups.11. A compound of or a pharmaceutically acceptable salt thereof claim 10 , wherein Rand Rare methyl claim 10 , and optionally substituted with 1 claim 10 , 2 or 3 OH claim 10 , OCHand F.12. A compound of or ...

Methods for Reducing Uric Acid Levels Using Barbiturate Derivatives

Methods for reducing uric acid levels in blood or serum of a subject employing metabolites of merbarone as active agents. Methods for treating or preventing disorders of uric acid metabolism are also provided. The metabolites can be formulated as pharmaceutical compositions comprising the metabolites and a pharmaceutically acceptable carrier for use in these methods.

Carboxylic acid urat1 inhibitor containing diarylmethane structure, preparation method and use thereof

The present invention relates to the pharmaceutical field for the treatment of hyperuricemia and gout. In particular, the present invention relates to a carboxylic acid urate transporter 1 (URAT1) inhibitor of a general formula (I) containing a diarylmethane structure and a preparation method thereof, and a pharmaceutical composition containing the same and a use thereof in the preparation of medicaments for treating hyperuricemia and gout, wherein R 1 is selected from H, C 1 -C 10 alkyl, C 3 -C 10 cycloalkyl, F, Cl, Br, I, CN, NO 2 , SR 4 or OR 4 ; R 2 is selected from H, F, Cl, Br or I; R 3 is selected from H or C 1 -C 4 alkyl; X is selected from S or CH 2 ; wherein R 4 is selected from C 1 -C 10 alkyl.

Preparation Method of Agrocybe Aegerita Extract and its use in Preparing Medicine for Lowering Uric Acid

The present invention relates to a preparation method of Agrocybe aegerita extract and its use in the preparation of lowering uric acid drugs, including: (1) Crush the dried fruit bodies of Agrocybe aegerita; (2) Separate the filter residue and the filtrate within 120 hours of extraction with 100-3000% ethanol by volume weight percentage at 0-100° C., and repeat it for 1-10 times; (3) Combine the filtrates obtained in step (2), concentrate to 25-35 mL and freeze-dry to obtain the alcohol extract; (4) Use 100-3000% water by volume percentage as a solvent to extract the alcohol-extracted filter residues of step (2) at 0-100° C. within 120 hours, separate the filter residue and the filtrate, repeat it for 1-10 times; (5) The filtrates obtained in step (4) are combined and concentrated to 25-35 mL, and lyophilized to obtain the water extract. The Agrocybe aegerita extract has a significant lowering uric acid effect with small side effects, can be used to prepare medicines for relieving gout symptoms, and provides a new direction for improving the current phenomenon of high side effects of gout drugs.

Novel crystalline polymorphs of pyridine derivative and method for producing the same

Disclosed are crystals of 2-(5-chloropyridin-3-yl)-1-(2,5-dichlorobenzyl)-4-methyl-1H-imidazole-5-carboxylic acid useful as therapeutic or prophylactic agents for gout, hyperuricemia, and the like, and a method for producing the crystals.

Thiophene, Manufacturing Method Thereof, And Pharmaceutical Application Of Same

The present invention discloses a thiophene used as a uric acid transporter (URAT1) inhibitor and application of the thiophene in preparing a pharmaceutical product for treating a disease related to abnormal uric acid levels, specifically in preparing a pharmaceutical product for treating hyperuricemia and gouty arthritis. The invention specifically relates to a compound as represented by formula (I) or a pharmaceutically acceptable salt thereof. 2. The compound claim 1 , the pharmaceutically acceptable salt and the tautomer thereof according to claim 1 , wherein claim 1 , R is selected from F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , OH claim 1 , CN claim 1 , NH claim 1 , COOH claim 1 , C(═O)NH claim 1 , or selected from Calkyl claim 1 , N claim 1 ,N′-di(Calkyl)amino claim 1 , Calkyl-NH— claim 1 , Calkyl-O— claim 1 , Calkyl-S(═O)— claim 1 , Calkyl-S(═O)— claim 1 , each of which is optionally substituted by 1 claim 1 , 2 or 3 of R′.5. (canceled)6. The compound claim 4 , the pharmaceutically acceptable salt and the tautomer thereof according to claim 4 , wherein claim 4 , Ris selected from H claim 4 , Me claim 4 , Et.9. (canceled)10. (canceled)11. The compound claim 1 , the pharmaceutically acceptable salt and the tautomer thereof according to any claim 1 , wherein claim 1 , Ris selected from H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , OH claim 1 , CN claim 1 , NH claim 1 , Me claim 1 , Et;{'sub': '6', 'or, Ris selected from H, F, Cl, Br, I, OH, CN, NH, Me, Et;'}{'sub': 7', '2', '1-3', '1-3', '1-3', '1-3', '3-6, 'or, Ris selected from H, F, Cl, Br, I, OH, CN, NH, COOH, or selected from the group consisting of Calkyl, C(═O)OCalkyl, C(═O)N(Calkyl)Calkyl, Ccycloalkyl, phenyl, pyrazolyl, imidazolyl, thiazolyl, oxazolyl, isoxazolyl, isothiazolyl, pyridyl and pyrimidyl, each of which is optionally substituted by 1, 2 or 3 of R.'}12. (canceled)16. (canceled)18. (canceled)22. (canceled)25. A pharmaceutical composition claim 1 , comprising the compound ...

Phenyl urea derivatives as n-formyl peptide receptor modulators

The present invention relates to phenyl urea derivatives useful for the treatment of inflammatory diseases, pharmaceutical compositions containing them and their use as tools or as pharmaceuticals as modulators of the N-formyl peptide receptor (FPR), including FPR1 and FPR2, or as selective agonists of the FPR1 receptor.

Messenger RNA Therapy for Treatment of Articular Disease

The present invention provides, among other things, a method of intra-articular delivery of messenger RNA (mRNA), comprising administering into a joint of a subject in need of delivery a composition comprising an mRNA encoding a protein, such that the administering of the composition results in expression of the protein encoded by the mRNA in the joint.

PDE4 Inhibitor

Provided is a compound represented by formula (1a) or a pharmacologically acceptable salt thereof. However, R 1 to R 6 in the formula each independently represent an alkyl group or the like.

NITROGEN-CONTAINING HETEROARYL COMPOUND AND PHARMACEUTICAL USE THEREOF

The invention provides a compound having a GLUT9 inhibitory activity. The compound is of Formula [I] 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein -L-COOH is —COOH.3. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0 or 1.4. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 0 or 1.5. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris (1) hydrogen or (2) halogen.6. The compound according to or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': '4', 'Ris'}{'sub': '1-8', '(1) Calkyl optionally substituted with 1 to 3 substituents independently selected from the following Group A,'}{'sub': '1-6', '(2) halo Calkyl, or'}{'sup': 41', '42', '41', '42, 'sub': '1-6', '(3) —CON(R)(R) wherein Rand Rare each independently hydrogen or Calkyl, and'}Group A consists of(a) hydroxy,{'sub': 1-3', '1-3, '(b) Calkoxy optionally substituted with one hydroxy or one Calkoxy,'}{'sub': '1-3', '(c) halo Calkoxy,'}{'sub': '3-6', '(d) Ccycloalkyl optionally substituted with one hydroxy, and'}(e) phenyl.18. A pharmaceutical composition comprising the compound according to any one of and - or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.19. (canceled)20. (canceled)21. A method for the inhibition of GLUT9 in a mammal in need of such inhibition claim 1 , which comprises administering a pharmaceutically effective amount of the compound according to any one of and - or a pharmaceutically acceptable salt thereof to the mammal.22. A method for the treatment or prophylaxis of a disease selected from the group consisting of hyperuricemia and gout in a mammal in need of such treatment or prophylaxis claim 1 , which comprises administering a pharmaceutically effective amount of the compound according to any one of and - or a pharmaceutically acceptable salt ...

COMPOSITION FOR PROMOTING URIC ACID EXCRETION, COMPOSITION FOR INHIBITING URAT1 AND COMPOSITION FOR LOWERING BLOOD URIC ACID LEVEL

The present invention aims to provide a composition for promoting uric acid excretion. Specifically, the present invention aims to provide a composition for promoting uric acid excretion, wherein the composition promotes uric acid excretion by URAT1 inhibition, a composition for inhibiting URAT1, a composition for lowering blood uric acid level, a method of promoting uric acid excretion, a method of inhibiting URAT1, and a method of lowering blood uric acid level. The present invention relates to a composition for promoting uric acid excretion and the like, containing at least one flavanone compound selected from the group consisting of a flavanone free of methoxy groups or having one methoxy group and a flavanone glycoside free of methoxy groups or having one methoxy group as an active ingredient. 1. A composition for promoting uric acid excretion , comprising:at least one flavanone compound selected from the group consisting of a flavanone free of methoxy groups or having one methoxy group and a flavanone glycoside free of methoxy groups or having one methoxy group, as an effective ingredient.2. The composition for promoting uric acid excretion according to claim 1 ,wherein the flavanone compound is at least one compound selected from the group consisting of isoxanthohumol, naringenin, hesperidin, and eriodictyol.3. The composition for promoting uric acid excretion according to claim 1 ,wherein the flavanone compound is isoxanthohumol.4. The composition for promoting uric acid excretion according to claim 1 ,wherein the composition promotes uric acid excretion by URAT1 inhibition.5. A composition for inhibiting URAT1 claim 1 , comprising:at least one flavanone compound selected from the group consisting of a flavanone free of methoxy groups or having one methoxy group and a flavanone glycoside free of methoxy groups or having one methoxy group.6. The composition for inhibiting URAT1 according to claim 5 ,wherein the flavanone compound is at least one compound ...

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING A SYMPTOM ASSOCIATED WITH GOUT OR HYPERURICEMIA

The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway. 2. The compound of claim 1 , wherein X is —OH.3. The compound of claim 2 , wherein —Ris —H.4. (canceled)5. The compound of claim 1 , wherein X is —F.6. The compound of claim 5 , wherein —Ris —H.79.-. (canceled)10. A pharmaceutical composition comprising:a pharmaceutically acceptable carrier and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a compound of , or a pharmaceutically acceptable salt thereof.'}1120.-. (canceled)21. A method of treating hyperuricemia or gout in a mammal claim 1 , comprising administering to the mammal a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof.2228.-. (canceled)29. The method of claim 21 , wherein the composition further comprises a xanthine oxidase inhibitor.30. The method of claim 29 , wherein the xanthine oxidase inhibitor is allopurinol oxypurinol claim 29 , febuxostat claim 29 , topiroxostat claim 29 , or inositol.3143.-. (canceled) This application is a continuation of application Ser. No. 16/268,367, filed Feb. 5, 2019, which is a continuation of application Ser. No. 16/151,641, filed Oct. 4, 2018, now U.S. Pat. No. 10,239,854, issued Mar. 26, 2019, which is a continuation of International Application No. PCT/US2017/041763, filed on Jul. 12, 2017, entitled “COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING A SYMPTOM ASSOCIATED WITH GOUT OR HYPERURICEMIA”, which claims the benefit of priority to U.S. provisional patent application No. 62/363,473, filed on Jul. 18, 2016. This and all other extrinsic materials discussed herein are incorporated by reference in their entirety. Where a definition or use of a term in an incorporated reference is inconsistent or contrary to the definition of that term provided herein, the definition of that term provided ...

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING A SYMPTOM ASSOCIATED WITH GOUT OR HYPERURICEMIA

The inventive subject matter provides compounds, compositions and methods for lowering serum acid (sUA) for the treatment of gout, and having reduced liver toxicity, associated with CYP2C9 metabolic pathway. 2. The method of claim 1 , wherein X is —OH and Ris H.3. The method of claim 2 , wherein each of R claim 2 , R claim 2 , R claim 2 , and Ris deuterium.4. The method of claim 2 , wherein each of R claim 2 , R claim 2 , and Ris deuterium and Ris —F.5. The method of claim 2 , wherein Rand Rare deuterium and Rand Rare H.6. The method of claim 2 , wherein Rand Rare H and Rand Rare deuterium.7. The method of claim 1 , wherein X is —F and Ris H.8. The method of claim 7 , wherein each of R claim 7 , R claim 7 , and Ris H claim 7 , and Ris deuterium.9. The method of claim 7 , wherein each of R claim 7 , R claim 7 , and Ris H claim 7 , and Ris deuterium.10. The method of claim 7 , wherein Rand Rare deuterium and Rand Rare H.11. The method of claim 7 , wherein Rand Rare H and Rand Rare deuterium.12. The method of claim 7 , wherein Rand Rare H and Rand Rare deuterium.13. The method of claim 7 , wherein each of R claim 7 , R claim 7 , R claim 7 , and Ris deuterium.14. The method of claim 1 , wherein X is —Cl and Ris H.15. The method of claim 14 , wherein each of R claim 14 , R claim 14 , R claim 14 , and Ris deuterium.16. The method of claim 1 , wherein X is —F and Ris —F.17. The method of claim 16 , wherein each of R claim 16 , R claim 16 , R claim 16 , and Ris deuterium. This application is a continuation of application Ser. No. 16/151,641, filed Oct. 4, 2018, which is a continuation of International Application No. PCT/US2017/041763, filed on Jul. 12, 2017, entitled “COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING A SYMPTOM ASSOCIATED WITH GOUT OR HYPERURICEMIA”, which claims the benefit of priority to U.S. provisional patent application No. 62/363,473, filed on Jul. 18, 2016. This and all other extrinsic materials discussed herein are incorporated by ...

Fused heterocyclic derivative and pharmaceutical use thereof

Compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. Fused heterocyclic derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, or prodrugs thereof, or pharmaceutically acceptable salts thereof. In the formula (I), ring U represents C 6-10 aryl or the like; R 1 independently represents a hydrogen atom, a hydroxy group, C 1-6 alkyl or the like; m represents an integral number from 1 to 2; ring Q represents 5-membered heteroaryl; n represents an integral number from 1 to 3; R 2 independently represents a hydrogen atom, a halogen atom, C 1-6 alkyl or the like.

Compounds and Their Use for Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders associated with excess uric acid, and for maintaining normal uric acid levels in blood or serum, or the whole body, are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided. 2. The compound according to claim 1 , wherein three of a claim 1 , b claim 1 , c claim 1 , d claim 1 , and e are nitrogen.3. The compound according to claim 1 , wherein Ris —CH.4. The compound according to claim 3 , wherein —XRis —SCHor —OCH.5. The compound according to claim 4 , wherein A is substituted phenyl.6. The compound according to claim 5 , wherein A is —CFsubstituted phenyl7. The compound according to claim 6 , which has a structure represented by Formula (II).8. The compound according to claim 1 , which is selected from the group consisting of compounds having a structure represented by Formula (II) Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula (II) claim 1 , Formula ( ...

Compounds and Their Use for Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders associated with excess uric acid, and for maintaining normal uric acid levels in blood or serum, or the whole body, are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided. 2. The compound according to claim 1 , wherein A is thiazole or isothiazole.3. The compound according to claim 1 , wherein three of a claim 1 , b claim 1 , c claim 1 , d claim 1 , and e are nitrogen.5. A pharmaceutical composition comprising the compound claim 1 , tautomer claim 1 , or combination thereof of claim 1 , and a pharmaceutically acceptable carrier.613. The pharmaceutical composition according to claim claim 1 , which comprises a compound having a structure represented by Formula (II) or a tautomer thereof.7. A method for reducing uric acid levels in blood claim 1 , serum or a whole body of a subject claim 1 , or for preventing elevation of uric acid levels in blood claim 1 , serum or a whole body of a subject claim 1 , or for treating or preventing a disorder associated with excess uric acid claim 1 , comprising administering to a subject in need thereof the compound claim 1 , the tautomer claim 1 , or combination thereof of in an amount effective to reduce blood or serum uric acid levels.8. The method according to claim 7 , wherein the disorder associated with excess uric acid is selected from gout claim 7 , hyperuricemia claim 7 , tumor lysis syndrome claim 7 , kidney disease claim 7 , arthritis claim 7 , kidney stones claim 7 , kidney failure claim 7 , urolithiasis claim 7 , plumbism claim 7 , hyperparathyroidism claim 7 , psoriasis claim 7 , inborn genetic errors of metabolism such as Lesch-Nyhan syndrome claim 7 , ...

Method of treating, or at least inhibiting the onset of, urate transport failure

Methods of treating, or at least inhibiting the onset of, urate transport failure are provided. The methods can include a step for detecting variations in genes that encode ABCG2 protein. When a subject has an SNP of V12M, R113X, Q126X, Q141K, F208S, G268R, E334X, S441N, L447V, S486N, F506SfsX4, R575X, and/or C608X, it can be concluded that the subject has a factor that is capable of inducing urate transport failure, or a state or disease attributable to that failure. When a subject has an SNP of V12M, it can be concluded that, unlike the other SNPs, there is a possibility that the subject does not possess such a factor because, although this variation itself does not lead to a change in urate transport capability, said variation is related to linkage disequilibrium with other SNPs.

Inhibition of the renin-angiotensin system for the treatment of renal, vascular and cartilage pathology

A method of treating a disease or condition in which up-regulating GAGs is therapeutically beneficial is disclosed. The method comprises locally administering to a subject a therapeutically effective amount of an agent capable of down-regulating activity or expression of a component of the renin-angiotensin system.

Total Flavonoids Extract of Gynura Formosana Kitam., Preparation Method Therefor and Use Thereof for Treating Hyperuricemia

Disclosed is a total flavonoids extract of ., containing 80%-85% of rutin by weight percent content. The results of pharmacological experiments show that the extract can lower the activity of xanthine oxidase in the liver of a hyperuricemia model mouse and reduce the synthesis of uric acid to a certain degree and has a certain uric acid-lowering effect, and can be used as a potential drug for treating hyperuricemia or gout. The method for preparing the total flavonoids extract of . comprises: after an extraction step, selecting a complex enzyme composed of enzymes with a specific composition and a specific ratio for enzymolosis, and further carrying out the step of extracting and concentrating with macroporous resin and isolating and purifying with macroporous resin, so that the HPLC purity of rutin in the resulting total flavonoids extract of . reaches 80%-85%. 1Gynura formosana KitamGynura formosana Kitam. A method for treating hyperuricemia or gout , comprising the step of administrating a total flavonoid extract from . to a subject in need , wherein the total flavonoid extract from . , comprises , in weight percent , 80-85% of rutin.2Gynura formosana Kitam. The method of claim 1 , wherein the total flavonoid extract from . is prepared by the steps of:{'i': 'Gynura formosana Kitam', '(1) Extraction: extracting . with an extraction solvent to obtain an extraction solution, and adjusting the extraction solution to a pH of 4-8 to obtain a reaction solution;'}(2) Enzymolysis: adding a complex enzyme into the reaction solution to carry out enzymolysis through a forced circular reaction at a temperature of 30° C. to 50° C. for 1 to 4 hours, then carrying out suction filtration, and collecting a filtrate;(3) Extraction and Concentration: extracting the filtrate by using a macroporous resin A to obtain an extracted solution, and concentrating the extracted solution to obtain a concentrated solution;(4) Separation and Purification: centrifuging the concentrated solution, ...

Novel Imidazopyridine Thioglycolic Acid Derivatives as Potent Inhibitors of Human Urate Transporter 1

It relates to the imidazopyridine thioglycolic acid derivatives, the preparation, and use thereof. The invention contained imidazopyridine thioglycolic acid derivatives with the formula I or II or III. Also described here are preparation of imidazopyridine thioglycolic acid derivatives, pharmaceutical compositions comprising these compounds as therapy and prevention for gout. 6. A process for treating an arthritis comprising a step of administrating to a subject in need a therapeutically effective amount of the compound of or its pharmaceutically acceptable salt; said arthritis is a gout.7. A pharmaceutical composition comprising a therapeutically effective amount of the compound of claim 1 , one or more pharmaceutical acceptable carrier or excipient. This invention concerns imidazopyridine thioglycolic acid derivatives for treating hyperuricemia and gout. Also described herein are the preparation of these derivatives as potent inhibitors of human urate transporter 1, belonging to the field of organic synthesis and medicine technology.Uric acid, the final product of purine catabolism, is physiologically excreted in the urine. the source of uric acid includes endogenous and exogenous, of which endogenous uric acid accounts for approximately 80%, while the remainder is derived from dietary purines. Thus, overproduction of uric acid or insufficient renal elimination can cause hyperuricemia, which is generally defined as a serum level of uric acid of >6.0 mg/dL. Hyperuricemia can be asymptomatic, but when the blood uric acid concentration exceeds 6.8 mg/dL without treatment, monosodium urate crystallizes and is deposited in joints or surrounding tissues. This is the cause of gout, a severe disease that affects millions of people, especially adult men, worldwide. Both hyperuricemia and gout are associated with a range of chronic diseases, including hypertension, diabetes mellitus, metabolic syndrome, and renal and cardiovascular diseases.Currently, there are several drug ...

Gene Editing to Improve Joint Function

The present invention provides compositions and methods for treating joint disorders that are characterized by an inflammatory component. In some aspects, the compositions and methods are to prevent the progression of osteoarthritis and other arthritides and to treat osteoarthritis and other arthritides in a mammalian joint. 165-. (canceled)66. A pharmaceutical composition for the treatment or prevention of a joint disease or condition , comprising:a therapeutically effective amount of one or more nucleic acids encoding a Clustered Regularly Interspaced Short Palindromic Repeats (CRISPR) gene-editing system, the system comprising:(i) a CRISPR Associated Protein 9 (Cas9) protein; and the at least one guide RNA comprises a crRNA sequence that is complementary to a target sequence in exon 4 of the IL-1α gene, and', 'the target sequence is adjacent to a protospacer adjacent motif (PAM) sequence for the Cas9 protein., '(ii) at least one guide RNA targeting an IL-1α gene, wherein67. The pharmaceutical composition of claim 66 , wherein the composition comprises one or more viral vectors collectively comprising the one or more nucleic acids.68. The pharmaceutical composition of claim 67 , wherein the one of more viral vectors comprise a recombinant virus selected from a retrovirus claim 67 , an adenovirus claim 67 , an adeno-associated virus claim 67 , a lentivirus claim 67 , and a herpes simplex virus-169. The pharmaceutical composition of claim 67 , wherein the one of more viral vectors comprise a recombinant adeno-associated virus (AAV).70. The pharmaceutical composition of claim 69 , wherein the recombinant AAV is of serotype 5 (AAV5).71. The pharmaceutical composition of claim 69 , wherein the recombinant AAV is of serotype 6 (AAV6).72. The pharmaceutical composition of claim 67 , wherein the one of more viral vectors comprise:a first viral vector comprising a first nucleic acid, in the one or more nucleic acids, encoding the Cas9 protein; anda second viral vector ...

TOLERIZATION REDUCES INTOLERANCE TO PEGLOTICASE AND PROLONGS THE URATE LOWERING EFFECT (TRIPLE)

The disclosure provides methods of treating gout in patients comprising administering a PEGylated uricase. Also provided are methods of treating gout in patients comprising co-administering a PEGylated uricase and azathioprine immunosuppressive therapy. Also provided are methods of reducing intolerance or enhancing immuno-tolerance to a PEGylated uricase and prolonging the urate lowering effect comprising co-administration of the PEGylated uricase and azathioprine immunosuppressive therapy. 1. A method of treating gout in a patient weighing <120 kg and having a serum uric acid level of ≥6 mg/dL , comprising:administering a PEGylated uricase to said patient at a tolerizing dosage regimen, wherein the tolerizing dosage regimen comprises 8 mg intravenously on a weekly basis for 3 weeks for a total of 3 doses; andafter the tolerizing dosage regimen, administering the PEGylated uricase at a dosage of 8 mg intravenously every 2 weeks for a total of 11 doses.2. A method of treating gout in a patient weighing ≥120 kg and having a serum uric acid level of ≥6 mg/dL , comprising:administering a PEGylated uricase to said patient at a tolerizing dosage regimen comprising 8 mg, 12 mg, or 16 mg intravenously at the first week of treatment for a total of one dose, followed by 8 mg intravenously on a weekly basis for 2 weeks after the first week of treatment, for a total of 2 doses; andafter the tolerizing dosage regimen, administering the PEGylated uricase at a dosage of 8 mg intravenously every 2 weeks for a total of 11 doses.3. A method of treating gout in a patient weighing <120 kg and having a serum uric acid level of ≥6 mg/dL , comprising:co-administering a PEGylated uricase and azathioprine (AZA) immunosuppressive therapy to said patient using a dosage regimen comprising 8 mg PEGylated uricase intravenously every 2 weeks for a total of 13 doses; anda dose of 1.25 mg/kg azathioprine orally daily for one week, for a total of 7 doses, followed by 2.5 mg/kg orally daily, wherein ...

REDUCING IMMUNOGENICITY TO PEGLOTICASE

The disclosure provides methods of treating gout in patients comprising administering a PEGylated uricase. Also provided are methods of treating gout in patients comprising co-administering a PEGylated uricase and MMF. Also provided are methods of reducing intolerance to a PEGylated uricase and prolonging the urate lowering effect comprising co-administration of the PEGylated uricase and MMF. 1. A method of treating gout in a patient having a serum uric acid level of ≥6 mg/dL comprising:administering mycophenolate mofetil (MMF) to said patient at a dose of 500 mg twice per day orally for a period of 2 weeks prior to the first administration of a PEGylated uricase;co-administering a PEGylated uricase and MMF to said patient using a dosage regimen comprising a dose of 8 mg of the PEGylated uricase intravenously every 2 weeks for a total of 12 doses; and a dose of 1000 mg MMF twice per day orally, wherein the co-administered MMF is administered concurrently with each administration of the PEGylated uricase;administering 8 mg of the PEGylated uricase at a dosage of 8 mg intravenously every 2 weeks for a total of 12 doses.2. A method of reducing or preventing loss of response to a PEGylated uricase and prolonging the urate lowering effect comprising co-administration of the PEGylated uricase at a dosage of 8 mg intravenously every 2 weeks and mycophenolate mofetil (MMF) at a dosage of 1000 mg twice per day orally to a patient having a serum uric acid level of ≥6 mg/dL prior to PEGylated uricase treatment initiation;wherein the co-administration of the PEGylated uricase and MMF result in the serum uric acid level being normalized relative to a patient not receiving co-administration of the PEGylated uricase and MMF immunosuppressive therapy.3. The method of or , further comprising a prophylactic regimen of colchicine for a period of at least 2 weeks prior to the first administration of the PEGylated uricase.4. The method of any of to , wherein the SUA levels of the ...

REDUCING IMMUNOGENICITY TO PEGLOTICASE

The disclosure provides methods of treating gout in patients comprising administering a PEGylated uricase. Also provided are methods of treating gout in patients comprising co-administering a PEGylated uricase and methotrexate (MTX). Also provided are methods of reducing immunogenicity of a PEGylated uricase and prolonging the urate lowering effect comprising co-administration of the PEGylated uricase and MTX. 1. A method of treating gout in a patient having a serum uric acid (SUA) level of ≥6 mg/dL comprising:administering methotrexate (MTX) to said patient at a dose of about 5 mg to about 50 mg per week for a period of 4 weeks prior to a first administration of a PEGylated uricase; andco-administering the PEGylated uricase and MTX to said patient using a dosage regimen comprising a dose of about 0.5 mg to about 24 mg of the PEGylated uricase intravenously every 2 weeks for a total of 26 doses, and a dose of about 5 to about 50 mg of MTX per week, wherein the co-administered MTX is administered concurrently with each administration of the PEGylated uricase.2. A method of reducing immunogenicity to PEGylated uricase and prolonging the urate lowering effect comprising co-administering a PEGylated uricase at a dosage of about 0.5 mg to about 24 mg intravenously every 2 weeks and methotrexate (MTX) at a dosage of 15 mg per week to a patient having a serum uric acid (SUA) level of ≥6 mg/dL prior to PEGylated uricase treatment initiation , wherein the administration of the PEGylated uricase and MTX result in the SUA level being reduced relative to a patient not receiving co-administration of the PEGylated uricase and MTX immunosuppressive therapy.3. The method of or , wherein the PEGylated uricase is administered at a dose of 8 mg and MTX is administered at a dose of 15 mg.4. The method of any of to , further comprising administering folic acid to said patient at a dosage of 1 mg per day.5. The method of any of to , further comprising an altered dosage of MTX , wherein ...

Anti-Prokineticin Receptor (PROKR) Antibodies and Uses Thereof

The present invention provides antibodies that bind to prokineticin receptors (PROKRs) and methods of using same. According to certain embodiments of the invention, the antibodies are fully human antibodies that bind to human PROKR1 and/or PROKR2. The present invention includes antibodies that bind cell surface-expressed PROKR1 and/or PROKR2. In certain embodiments, the antibodies of the present invention are capable of blocking prokineticin (PK)-mediated activation of one or more PROKR. The antibodies of the invention are useful for the treatment of various diseases and disorders mediated by prokineticin signaling.

FLUORENONE COMPOUND FOR THE TREATMENT OF GOUT

The present invention provides a method for treating or preventing gout in a subject afflicted therewith comprising administering a compound presented or an ester or salt thereof, so as to thereby treat or prevent the gout in the subject. 2. The method of claim 1 , wherein the compound treats gout in the subject.3. The method of claim 2 , wherein the treating comprises increasing uric acid levels in the urine of the subject.4. The method of claim 2 , wherein the treating comprises reducing uric acid levels in the blood of the subject.5. The method of claim 2 , wherein the treating comprises increasing uric acid clearance in the subject; or the treating comprises decreasing uric acid reabsorption in the kidneys of the subject; or the treating comprises increasing renal clearance of uric acid in the subject.67-. (canceled)8. The method of claim 2 , wherein the treating comprises reducing one or more symptoms associated with gout in the subject.9. The method of claim 8 , wherein the one or more symptoms associated with gout are joint pain claim 8 , joint inflammation claim 8 , joint redness claim 8 , decreased range of motion at the joint.10. The method of claim 1 , wherein the compound prevents gout in the subject.11. The method of claim 10 , wherein the preventing comprises increasing uric acid levels in the urine of the subject; or the preventing comprises reducing uric acid levels in the blood of the subject; or the preventing comprises increasing uric acid clearance in the subject; or the preventing comprises decreasing uric acid reabsorption in the kidneys of the subject; or the preventing comprises increasing renal clearance of uric acid in the subject.1215-. (canceled)16. The method of claim 10 , wherein the preventing comprises reducing one or more symptoms associated with gout in the subject.17. The method of claim 16 , wherein the one or more symptoms associated with gout are joint pain claim 16 , joint inflammation claim 16 , joint redness claim 16 , ...

COMPOSITION FOR DECREASING SERUM URIC ACID LEVEL

Provided is a composition for reducing serum uric acid level, which contains glycine and tryptophan. The serum uric acid level in a subject can be decreased when the subject intakes the composition. 15-. (canceled)6. A composition for reducing serum uric acid level , comprising glycine and tryptophan.7. The composition according to claim 6 , having a weight ratio of tryptophan to glycine in the range of 0.01 and 0.15.8. The composition according to claim 6 , wherein glycine intake is in the range of 1 g and 10 g per dose.9. The composition according to claim 7 , wherein glycine intake is in the range of 1 g and 10 g per dose.10. A food and drink product for reducing serum uric acid level claim 6 , comprising the composition according to .11. A serum uric acid level reducer claim 6 , comprising the composition according to .12. A method for reducing serum uric acid level claim 6 , comprising administrating a composition containing glycine and tryptophan.13. The method according to claim 12 , wherein the composition has a weight ratio of tryptophan to glycine in the range of 0.01 and 0.15.14. The method according to claim 12 , wherein glycine intake is in the range of 1 g and 10 g per dose.15. The method according to claim 12 , treating a disease whose pathological condition is improved by reducing serum uric acid level.16. The method according to claim 15 , wherein the disease is at least one selected from the group consisting of gout claim 15 , hyperuricemia claim 15 , gouty tophus claim 15 , renal failure claim 15 , gout kidneys claim 15 , prostatic hypertrophy claim 15 , edema claim 15 , and urinary calculi including renal stones claim 15 , ureteral stones claim 15 , and bladder stones.17. A method for treating a disease whose pathological condition is improved by reducing serum uric acid level claim 15 , comprising administrating a composition containing glycine and tryptophan.18. The method according to claim 17 , wherein the composition has a weight ratio of ...

Therapeutic or prophylactic agent for tumor lysis syndrome

The purpose of the present invention is to provide a novel therapeutic or prophylactic agent for tumor lysis syndrome. The present invention is a therapeutic or prophylactic agent for tumor lysis syndrome, which comprises a 2-phenylthiazole compound represented by formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

URAT1 INHIBITOR FOR PROMOTING URIC ACID EXCRETION

The present invention belongs to the field of medicinal chemistry. Specifically disclosed is a class of URAT1 inhibitors for promoting uric acid excretion, which are compounds as represented by the structure of formula (I) or pharmaceutically acceptable salts thereof. Experiments show that the compounds provided by the present invention have a very good inhibitory effect on the transport of uric acid by hURAT1 in HEK293 transfected cells, and that such compounds have a good application prospect in the treatment of hyperuricemia or gout. 2. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein ring A is a cyclohexene ring or a non-aromatic six-membered ring containing at least one O or/and N atom.3. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein ring A is cyclohexene ring claim 1 , 3 claim 1 ,4-dihydro-2H-pyran ring claim 1 , tetrahydropyran ring claim 1 , 2 claim 1 ,3 claim 1 ,4 claim 1 ,5-tetrahydropyridine ring claim 1 , 5 claim 1 ,6-dihydro-2H-1 claim 1 ,3-oxazine ring or 1 claim 1 ,2 claim 1 ,5 claim 1 ,6-tetrahydropyrimidine ring.4. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris selected from one or more of the group consisting of hydrogen claim 1 , deuterium claim 1 , fluorine claim 1 , chlorine claim 1 , bromine claim 1 , hydroxy claim 1 , cyano claim 1 , Calkyl claim 1 , Chaloalkyl and Calkoxy; m is 0 claim 1 , 1 or 2.5. The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris selected from one or more of the group consisting of hydrogen claim 1 , deuterium claim 1 , halogen claim 1 , cyano claim 1 , vinyl claim 1 , ethynyl claim 1 , Calkyl claim 1 , substituted Calkyl claim 1 , Calkoxy claim 1 , substituted Calkoxy claim 1 , Calkylthio claim 1 , substituted Calkylthio; the substituent is selected from the group consisting of deuterium claim 1 , halogen claim 1 , Calkyl claim 1 , Ccycloalkyl and Calkoxy; n ...

Compounds and Their Use for Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders associated with excess uric acid, and for maintaining normal uric acid levels in blood or serum, or the whole body, are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided. 2. The compound according to claim 1 , wherein three of a claim 1 , b claim 1 , c claim 1 , d claim 1 , and e are nitrogen.3. The compound according to claim 1 , wherein Ris —CH.4. The compound according to claim 3 , wherein —XRis —SCHor —OCH.5. The compound according to claim 4 , wherein A is substituted phenyl.6. The compound according to claim 5 , wherein A is —CFsubstituted phenyl.10. The compound according to claim 9 , wherein A is thiazole or isothiazole.11. The compound according to claim 10 , wherein three of a claim 10 , b claim 10 , c claim 10 , d claim 10 , and e are nitrogen.13. A pharmaceutical composition comprising a compound having a structure represented by Formula (I) or Formula (II); a tautomer of Formula (I) of Formula (II) claim 10 , or a combination thereof claim 10 , and a pharmaceutically acceptable carrier.14. The pharmaceutical composition according to claim 13 , which comprises a compound having a structure represented by Formula (II) or a tautomer thereof.15. A method for reducing uric acid levels in blood claim 13 , serum or a whole body of a subject claim 13 , or for preventing elevation of uric acid levels in blood claim 13 , serum or a whole body of a subject claim 13 , or for treating or preventing a disorder associated with excess uric acid claim 13 , comprising administering to a subject in need thereof a compound having a structure represented by Formulae (I) or Formula (II); a tautomer of Formula (I) or ...

COMPOUND FOR TREATING OR PREVENTING HYPERURICEMIA OR GOUT

The invention discloses a class of compounds for treating or preventing hyperuricemia or gout, which is a compound shown in general formula (I) or a pharmaceutically acceptable salt. These compounds and their pharmaceutically acceptable salts in the invention are useful for the promotion of uric acid excretion to treat or prevent hyperuricemia or gout. 2. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': 1', '2, 'sub': 1-3', '1-3', '1-3', '1-3', '1-3', '3-4', '1-3, 'Rand Rare independently selected from the group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, cyano, hydroxyl, Calkyl, substituted Calkyl, Calkoxy, or substituted Calkoxy; Wherein the substituents are independently selected from the group consisting of deuterium, halogen, Calkyl, Ccycloalkyl or Calkoxy.'}3. The compound of or a pharmaceutically acceptable salt thereof claim 2 , wherein:{'sup': 1', '2, 'sub': 1-3', '1-3', '1-3, 'Rand Rare independently selected from the group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, CN, Calkyl, Chalogenated alkyl or Calkoxy.'}4. The compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': '3', 'sub': 1-3', '3-4', '1-2', '3-4, 'Ris selected from the substituted or unsubstituted group consisting of Calkyl and Ccycloalkyl; Wherein the substituents are independently selected from the group consisting of deuterium, halogen, Calkyl or Ccycloalkyl.'}5. The compound of claim 1 , wherein:{'sup': 4', '5, 'sub': 1-2', '1-2', '1-2', '1-2', '1-2', '1-2', '1-2', '3-4', '1-3, 'Rand Rare independently selected from the group consisting of hydrogen, deuterium, halogen, cyano, ethylene, acetylene, Calkyl, substituted Calkyl, Calkoxy, substituted Calkoxy, Calkylthio, or substituted Calkylthio; Wherein the substituents are independently selected from the group consisting of deuterium, halogen, Calkyl, Ccycloalkyl or Calkoxy.'}6. The compound of claim 1 , wherein:{'sup': 4', '5, 'sub': 1- ...

Benzimidazole derivatives, preparation method therefor, and applications thereof

The present invention belongs to the pharmaceutical field, and relates to a preparation method for a series of benzimidazole derivatives, their pharmaceutical salts and pharmaceutically acceptable prodrugs, a pharmaceutical composition containing the derivatives, and the uses of the derivatives and pharmaceutical composition in the preparation of antigout drugs and in the treatment of related diseases.

Ligands that bind tgf-beta receptor ii

The disclosure provides an anti-TGFbetaRII immunoglobulin single variable domain. Suitably, an anti-TGFbetaRII immunoglobulin single variable domain in accordance with the disclosure is one having an amino acid sequence as set forth in any one of SEQ ID NO:1-28 having up to 5 amino acid substitutions, deletions or additions. The disclosure further provides a polypeptide and pharmaceutical composition for treating a disease associated with TGFbeta signalling and suitably a disease selected from the group of: tissue fibrosis, such as pulmonary fibrosis, including idiopathic pulmonary fibrosis; liver fibrosis, including cirrhosis and chronic hepatitis; rheumatoid arthritis; ocular disorders; fibrosis of the skin, including keloid of skin; Dupuytren's Contracture; kidney fibrosis such as nephritis and nephrosclerosis; wound healing; scarring reduction; and a vascular condition, such as restenosis.

Compounds And Their Use For Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders of uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided. 2. The compound according to claim 1 , wherein a claim 1 , b claim 1 , c claim 1 , d claim 1 , and e for a 5-member heterocyclic ring.3. The compound according to claim 2 , wherein the 5-member heterocyclic ring is substituted or unsubstituted triazole claim 2 , or substituted or unsubstituted pyrazole.4. The compound according to claim 3 , wherein Z is —OH or —CFon the 5-member heterocyclic ring and/or —CFon the phenyl ring.5. The compound according to claim 1 , wherein both Z are absent claim 1 , wherein Z is absent from the phenyl group and present on the 5-member heterocyclic ring claim 1 , or wherein Z is present on the phenyl group and absent from the 5-member heterocyclic ring.6. The compound according to claim 5 , wherein Z is absent from the phenyl group claim 5 , and Z on the heterocyclic 5-membered ring is CF.7. The compound according to claim 5 , wherein Z on the phenyl group is CF claim 5 , and Z is absent from the heterocyclic 5-membered ring.8. A pharmaceutical composition comprising a compound according to ; a tautomer thereof claim 1 , or a combination thereof claim 1 , and a pharmaceutically acceptable carrier.9. The pharmaceutical composition according to claim 8 , which is formulated for controlled or extended release of the compound or combination thereof.10. A method for reducing uric acid levels in blood or serum of a subject comprising administering to a subject in need thereof a compound according to ; a tautomer thereof claim 1 , or a ...

SCALABLE PRODUCTION OF STANDARDIZED EXTRACELLULAR VESICLES, EXTRACELLULAR VESICLE PREPARATIONS AND USES THEREOF

Preparations comprising an enriched population of extracellular vesicles (nEVs) having a negatively charged surface, and that are CD81+ and CD9−, are provided. Improved processes and methods for producing an enriched population of nEVs from non-murine cells, especially human origin cells and/or tissues, are disclosed. Therapeutic methods for using the preparations, including for reducing brain inflammation and treatment of various pathologies associated with brain inflammation, such as by intravenous or intranasal administration, are also described. Methods and preparations for reducing brain inflammation associated with traumatic brain injury (TBI) are also disclosed. A method for treating a patient having suffered a mild traumatic injury (mTMI), or concussion, such as a sports-related head injury, is also disclosed. The nEVs are also demonstrated to reduce the expression level of IL-Iβ in brain tissue of an animal having had traumatic brain injury. Methods for improving cognitive function and performance in animals after a traumatic brain injury is also demonstrated using the preparations of nEVs disclosed herein. 1. A pharmaceutical preparation comprising an enriched population of selected extracellular vesicles having a negatively charged surface , said selected negative extracellular vesicles (n-EVs) lacking a CD9 surface epitope (CD9).2. The pharmaceutical preparation of wherein the selected extracellular vesicles having a mean size of about 80 nm to about 250 nm.3. The pharmaceutical preparation of suitable for intravenous administration or intranasal administration.4. The pharmaceutical preparation of wherein the selected extracellular vesicles comprise at least about 50% by volume of the pharmaceutical preparation.5. The pharmaceutical preparation of wherein the selected extracellular vesicles lack any combination of two or more of the surface epitopes selected from the group consisting essentially of: CD29 claim 1 , CD44 claim 1 , CD49c claim 1 , CD49f ...

Compounds and Their Use for Reducing Uric Acid Levels

Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders of uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided. 2. The compound according to claim 1 , wherein the 5-member heterocyclic ring is a substituted or unsubstituted triazole.3. The compound according to claim 1 , wherein-XRis —SCHor —OCH.4. The compound according to wherein claim 1 , in Formula (I):a) X and W are each independently O or S;{'sub': '2', 'b) Y is OH or NH;'}{'sub': 3', '2, 'c) T is —C(NH)NH—, —NHC(O)—, —C(SCH)N—, —C(NOH)NH—, —C(N—NH)NH—, or —CONH;'}{'sup': '2', 'sub': '3', 'd) each Ron the barbiturate ring is independently H or CH;'}e) A is phenyl, branched cycloalkyl, or unbranched cycloalkyl; and{'sub': '3', 'f) Z, if present, is phenyl or CF.'}5. The compound according to claim 1 , wherein claim 1 , in Formula (III) claim 1 , f is —S(O)—.6. The compound according to wherein claim 1 , in Formula (IV) claim 1 , f is —NH— claim 1 , —C(O)— or —C(—O(CH)O—)—.7. The compound according to claim 6 , wherein X on the fused ring structure is O.8. The compound according to wherein claim 1 , in Formula (V) claim 1 , each Ris H.9. The compound according to wherein claim 1 , in Formula (VI) claim 1 , U is —O— or —NH— claim 1 , and the 5-member heterocyclic ring is triazole.10. The compound according to wherein claim 1 , in Formula (VII) claim 1 , the unfused 5-member heterocyclic ring is triazole.11. A pharmaceutical composition comprising a compound having a structure represented by any of Formulae (I) claim 1 , and (III)-(VIII); a tautomer of any of Formulae (I) claim 1 , and (III)-(VIII) claim 1 , or a combination ...

Human plasma-like medium

In some aspects, described herein are cell culture media that are useful for in vitro culture of mammalian cells. The culture media contain a variety of small organic compounds that are found in normal adult human blood. Also described are methods of using the culture media for a variety of purposes. Also described are methods of treating cancer.

REDUCING IMMUNOGENICITY TO PEGLOTICASE

The disclosure provides methods of treating gout in patients comprising administering a PEGylated uricase. Also provided are methods of treating gout in patients comprising co-administering a PEGylated uricase and MMF. Also provided are methods of reducing intolerance to a PEGylated uricase and prolonging the urate lowering effect comprising co-administration of the PEGylated uricase and MMF. 1. A method of treating gout in a patient having a serum uric acid level of ≥6 mg/dL comprising:administering mycophenolate mofetil (MMF) to said patient at a dose of 500 mg twice per day orally for a period of 2 weeks prior to the first administration of a PEGylated uricase;co-administering a PEGylated uricase and MMF to said patient using a dosage regimen comprising a dose of 8 mg of the PEGylated uricase intravenously every 2 weeks for a total of 12 doses; and a dose of 1000 mg MMF twice per day orally, wherein the co-administered MMF is administered concurrently with each administration of the PEGylated uricase;administering 8 mg of the PEGylated uricase at a dosage of 8 mg intravenously every 2 weeks for a total of 12 doses.2. A method of reducing or preventing loss of response to a PEGylated uricase and prolonging the urate lowering effect comprising co-administration of the PEGylated uricase at a dosage of 8 mg intravenously every 2 weeks and mycophenolate mofetil (MMF) at a dosage of 1000 mg twice per day orally to a patient having a serum uric acid level of ≥6 mg/dL prior to PEGylated uricase treatment initiation;wherein the co-administration of the PEGylated uricase and MMF result in the serum uric acid level being normalized relative to a patient not receiving co-administration of the PEGylated uricase and MMF immunosuppressive therapy.3. The method of or , further comprising a prophylactic regimen of colchicine for a period of at least 2 weeks prior to the first administration of the PEGylated uricase.4. The method of any of to , wherein the SUA levels of the ...

Compounds and Dosage Regimen for Use in the Prevention or Treatment of Chronic Inflammatory and/or Autoimmune Diseases

The present invention refers to a 2-({3-fluoro-3′-methoxy-[1,1′-biphenyl]-4-yl}carbamoyl)cyclopent-1-ene-1-carboxylic acid) according to formula (I) 2. A compound that is 2-({3-fluoro-3′-methoxy-[1 claim 1 ,1′-biphenyl]-4-yl}carbamoyl)cyclopent-1-ene-1-carboxylic acid) or salts thereof or solvates of the said compound or the salts thereof for use as a medicament in a patient in need thereof according to claim 1 , wherein said subsequent dose is 28-200 μmol of the active moiety of the compound daily.3. A compound that is 2-({3-fluoro-3′-methoxy-[1 claim 1 ,1′-biphenyl]-4-yl}carbamoyl)cyclopent-1-ene-1-carboxylic acid) or salts thereof or solvates of the said compound or the salts thereof for use as a medicament in a patient in need thereof according to claim 1 , wherein said patient suffers from a chronic inflammatory and/or autoimmune disease.4carinii. A compound that is 2-({3-fluoro-3′-methoxy-[1 claim 1 ,1′-biphenyl]-4-yl}carbamoyl)cyclopent-1-ene-1-carboxylic acid) or salts thereof or solvates of the said compound or the salts thereof for use as a medicament in a patient in need thereof according to claim 1 , wherein said patient suffers from a chronic inflammatory and/or autoimmune disease selected from the group consisting of rheumatism claim 1 , acute immunological disorders claim 1 , autoimmune diseases claim 1 , diseases caused by malignant cell proliferation claim 1 , inflammatory diseases claim 1 , diseases that are caused by protozoal infestations in humans and animals claim 1 , diseases that are caused by viral infections and neumocystis claim 1 , fibrosis claim 1 , uveitis claim 1 , rhinitis claim 1 , asthma or athropathy.5. A compound that is 2-({3-fluoro-3′-methoxy-[1 claim 1 ,1′-biphenyl]-4-yl}carbamoyl)cyclopent-1-ene-1-carboxylic acid) or salts thereof or solvates of the said compound or the salts thereof for use as a medicament in a patient in need thereof according to claim 1 , wherein said patient suffers from a chronic inflammatory and/or ...

Crystal form of urat1 inhibitor, and preparation method therefor

Disclosed are a crystal form of a URAT1 inhibitor, and a preparation method therefor.

CORDYCEPS MILITARIS MEDIUM POLYSACCHARIDE, METHOD FOR SEPARATING AND PURIFYING SAME, AND USE THEREOF

A medium polysaccharide, a method for separating and purifying same, and the use thereof, wherein the polysaccharide comprises the following monosaccharides in mole percentages: 0.11% ribose, 0.11% rhamnose, 0.45% arabinose, 0.13% xylose, 14.50% mannose, 83.96% glucose, and 0.73% galactose. The extraction method does not affect the biological activity of the medium polysaccharide P1; the obtained purified polysaccharide P1 has high purity and stable properties, and has significant effects on resistance to oxidation, lowering uric acid and bacteriostasis, which are beneficial to human metabolism; due to the low cost, the purified polysaccharide P1 can be further used in the development of health products, drugs and cosmetics. 1Cordyceps militaris. A medium polysaccharide , characterized by comprising the following monosaccharides in mole percentages: 0.11% ribose , 0.11% rhamnose , 0.45% arabinose , 0.13% xylose , 14.50% mannose , 83.96% glucose , and 0.73% galactose.2Cordyceps militaris. The medium polysaccharide according to claim 1 , characterized by having an average molecular weight of 2.18 k Da.3Cordyceps militaris. The medium polysaccharide according to claim 1 , characterized by comprising sulfate groups claim 1 , pyranose rings and alpha-glucosidic bonds.4Cordyceps militaris. A method for separation and purification of the medium polysaccharide according to claim 1 , comprising the following steps:{'i': Cordyceps militaris', 'Cordyceps militaris', 'Cordyceps militaris, '(1) extraction of the medium polysaccharide: drying the rice medium leftovers, pulverizing and sieving same to obtain a dry powder of the leftovers; weighing the dry powder and adding 15-16 times distilled water by mass into same, performing an ultrasonic treatment for at least 30 min, performing a reflux extraction at 70° C. for 1.5 h-2.0 h, pooling the extract solutions after several extractions, and filtering the pooled extract and concentrating same to obtain a polysaccharide concentrate; ...

Heterocyclic compounds, processes for producing them and pharmaceutical compositions comprising them

Novel heterocyclic compounds capable of lowenng the und acid levels in plasma and unne having the formula (I) wherein R 2 and R 2 are independently hydrogen, lower alkyl, phenyl or substituted phenyl, or R' and R 2 may form a four to eight-membered carbon ring together with the carbon atom to which they are attached: R 3 is hydrogen or lower alkyl: R 4 is one or two radicals selected from a group consisting of hydrogen, halogen, nitro. lower alkyl. phenyl. substituted phenyl, -OR 5 and -SO 2 NR 6 R 6 ; R 5 is hydrogen. lower alkyl phenyl-substituted lower alkyl. carboxymethyl or ester thereof, hydroxethyl or ether thereof, or allyl; R 6 and R 6 are independently hydrogen or lower alkyl: R 7 is hydrogen or a pharmaceutically active ester-forming group: A is a straight or branched hydrocarbon radical having one to five carbon atoms: B is halogen. oxygen, or dithiolane; Y is oxygen. sulfur, nitrogen or substituted nitrogen; Z is oxygen, nitrogen or substituted nitrogen: dotted line represents the presence or absence of a single bond, processes for their production and pharmaceutical compositions comprising them.

Dendritic polymers with enhanced amplification and interior functionality

Dendritic polymers of the macromolecular structure of Figure 1 are disclosed. The dendritic polymers have enhanced amplification and interior functionality. The dendritic polymers are made by use of fact, reactive ring-opening chemistry (or other fast reactions) combined with the use of branch cell reagents in a controlled manner to rapidly and precisely build dendritic structures with cleaner chemistry and often with single products. Additional benefits include lower excesses of regents, lower levels of dilution, higher capacity, more easily scaled to commercial dimensions, new ranges of materials, and lower cost. The compositions prepared have novel internal functionality, including increased thermal stability and no reverse Michael's reaction, and reach encapsulation surface densities at lower generations.

Imidazopyridinones as p38 map kinase inhibitors

The present invention relates to imidazopyridinones processes for their preparation and their use in medicaments, especially for the treatment of COPD.

The sodium salt of the (-)-enantiomer of omeprazole

Ligand (ACT-4-L) to a receptor on the surface of activated CD4+ T-cells

The invention provides ligands and fragments thereof to a receptor on the surface of activated CD4 + T-cells. An exemplary ligand is designated ACT-4-L-h-1. Preferred fragments include purified extracellular domains of ligands. The invention also provides humanized and human antibodies to the ligand. The invention further provides methods of using the ligand and the antibodies in treatment of diseases and conditions of the immune system. The invention also provides methods of monitoring activated CD4 + T-cells using the ligands or fragments thereof.

Ligand (ACT-4-L) to a receptor on the surface of activated CD4+ T-cells

The invention provides ligands and fragments thereof to a receptor on the surface of activated CD4 + T-cells. An exemplary ligand is designated ACT-4-L-h-1. Preferred fragments include purified extracellular domains of ligands. The invention also provides humanized and human antibodies to the ligand. The invention further provides methods of using the ligand and the antibodies in treatment of diseases and conditions of the immune system. The invention also provides methods of monitoring activated CD4 + T-cells using the ligands or fragments thereof.

Phosphoramidate and phosphorothioamidate oligomeric compounds

Compounds are provided having the structure: ##STR1## wherein the L groups are spanner or linker units, the Y and T group are functional groups for interacting with target molecules of interest, the X groups are oxygen or sulfur and the E groups are H, conjugate groups or intermediate groups used during the synthesis of the compounds are prepared using H phosphonate type chemistry wherein the functional groups are added during an oxidization step.

Solid preparation containing single crystal form

There are provided a solid preparation containing a single crystal of 2-(3-cyano-4-isobutyloxyphenyl)-4-methyl-5-thiazolecarboxyl ic acid, an excipient and a disintegrating agent, and a method for producing the same.

3-UREIDO-PIRIDOFURANOS y -PIRIDOTIOFENOS, PROCEDURE FOR ITS PREPARATION, COMPOSITION THAT UNDERSTANDS THEM AND USE OF SUCH COMPOUNDS FOR THE PREPARATION OF MEDICINES.

Se refiere a 3-urea-piridofuranos y -piridotiofenos, según fórmula (I), donde E, G, L, M, Q, R1, R2, R3, R4 y T están definidos en la memoriadescriptiva. Los 3-urea-piridofuranos y -piridotiofenos se pueden usar como ingredientes activos enm edicamentos, en particular en medicamentos para eltratamiento de trastornos inflamatorios agudos y crónicos. Asimismo se refiere al procedimiento para preparar dichos compuestos, a composiciones que loscontienen y el uso de dichos compuestos parala preparación de medicamentos. It refers to 3-urea-pyridofurans and -pyridothiophenes, according to formula (I), where E, G, L, M, Q, R1, R2, R3, R4 and T are defined in the specification. The 3-urea-pyridofurans and -pyridothiophenes can be used as active ingredients in medicines, in particular in medicines for the treatment of acute and chronic inflammatory disorders. It also refers to the process for preparing said compounds, to compositions containing them and the use of said compounds for the preparation of drugs.

REDUCING IMMUNOGENICITY TO PEGLOTICASE

The disclosure provides methods of treating gout in patients comprising administering a PEGylated uricase. Also provided are methods of treating gout in patients comprising co-administering a PEGylated uricase and methotrexate (MTX). Also provided are methods of reducing immunogenicity of a PEGylated uricase and prolonging the urate lowering effect comprising co-administration of the PEGylated uricase and MTX. 1. A method of treating gout in a patient having a serum uric acid (SUA) level of ≥6 mg/dL comprising:administering methotrexate (MTX) to said patient at a dose of about 5 mg to about 50 mg per week for a period of 4 weeks prior to a first administration of a PEGylated uricase; andco-administering the PEGylated uricase and MTX to said patient using a dosage regimen comprising a dose of about 0.5 mg to about 24 mg of the PEGylated uricase intravenously every 2 weeks for a total of 26 doses, and a dose of about 5 to about 50 mg of MTX per week, wherein the co-administered MTX is administered concurrently with each administration of the PEGylated uricase.2. (canceled)3. The method of claim 1 , wherein the PEGylated uricase is administered at a dose of 8 mg and MTX is administered at a dose of 15 mg.4. The method of claim 1 , further comprising administering folic acid to said patient at a dosage of 1 mg per day.5. The method of claim 1 , further comprising an altered dosage of MTX claim 1 , wherein the altered dosage comprises:administering folic acid to said patient at a dosage of about 2 mg per day; oradministering MTX to said patient at a dosage of about 7.5 mg twice per day; oradministering MTX to said patient at a dosage of about 10 mg, wherein the altered dosage of MTX is based on laboratory findings.6. The method of claim 5 , wherein the altered dosage of MTX comprises a temporary stop for laboratory parameters selected from the group consisting of WBC levels of less than about 3.0×10/L claim 5 , platelet levels of less than about 50×10/L claim 5 , ...

New seven-transmembrane receptor V28

Acides indenyl-acetiques et procede pour les

Foerlaekemedel foer allopurinol.

결절성 통풍 치료에서의 요산염 저하 요법 동안의 통풍결절 반응을 평가하는 방법

본 발명에서는 효과적인 요산염 저하 요법을 이용하는 통풍결절 부하량 감소를 평가하기 위한 시스템 및 방법을 개발하였다. 통풍결절 반응을 평가하기 위한 컴퓨터 보조 방법의 첫번째 적용은 표준화된 디지털 사진촬영술, 컴퓨터 보조 측정 및 독립적 판독자 및 맹검 주요 판독자 범례에 의한 통풍결절의 분석을 포함하였다. 통풍결절 크기의 감소를 정량하기 위한 디지털 사진의 컴퓨터 보조 분석을 위한 방법의 능력은 결절성 통풍의 치료에서 요산염 저하 요법 모니터링 도구로서의 이의 유용성을 입증한다.

取代苯甲酸

本发明涉及式I化合物及R为氢时与碱所形成 的药用盐。 式中R为氢，低级烷基，-(CH 2 ) 2 N(R 3 ) 2 或 -CH 2 OOCR 3 ，其中R 3 为低级烷基；R 1 为 CH 3 (CH 2 ) n -，其中n为9—17，或R 4 (CH 2 ) p -，其中p 为2—18和R 4 为1-或2-萘氧基，2，3-或3，4-二羟 基苯基，2，3-或3，4-二苄氧基苯基，苯基，苯氧基，或取 代苯基或苯氧基，式I化合物为潜在的磷脂酶 A 2 (PLA 2 )抑制剂，因此可用于治疗牛皮癣，肠炎，哮喘， 变态反应，关节炎，皮炎，痛风，肺病，心肌局部缺血，以 及创伤引起的发炎，如脊髓损伤等疾病。

DESAZAGUANINAS SUBSTITUTED IN 9 AND NOT SUBSTITUTED IN 8.

LA ESPECIFICACION DESCRIBE LOS COMPUESTOS DE FORMULA (I), EN LA QUE (A)-CH2 THE SPECIFICATION DESCRIBES THE COMPOUNDS OF FORMULA (I), IN WHICH (A) -CH2

Способы для оценки реакции тофуса в течение снижающего уровень уратов лечения при лечении узелковой подагры

1. Способ оценки и/или количественной оценки реакции тофуса у пациента в течение снижающего уровень уратов лечения, включающий в себя этапы, на которых:a) получают фотографию каждого исходного тофуса до снижающего уровень уратов лечения и каждого тофуса после указанного лечения;b) измеряют наибольший размер и перпендикулярный размер указанного тофуса до и после указанного лечения;с) вычисляют площадь указанного тофуса до и после указанного лечения посредством перемножения указанного наибольшего размера и указанного перпендикулярного размера;d) сравнивают площадь тофуса до и после указанного снижающего уровень уратов лечения; иe) указывают, что изменение площади тофуса относительно указанного исходного значения коррелирует с терапевтической эффективностью.2. Способ по п.1, в котором снижающее уровень уратов лечение, предоставляемое нуждающемуся в нем пациенту, представляет собой лечение пегилированной уриказой.3. Способ по п.2, в котором пегилированную уриказу вводят в дозировке 8 мг каждые 2 недели.4. Способ по п.2, в котором пегилированную уриказу вводят в дозировке 8 мг каждые 4 недели.5. Способ по п.2, в котором снимают фотографии тофуса после 25 недель лечения пегилированной уриказой.6. Способ по п.2, в котором снимают фотографии тофуса после 19 недель лечения пегилированной уриказой.7. Способ по п.2, в котором снимают фотографии тофуса после 13 недель лечения пегилированной уриказой.8. Способ по п.1, в котором указанный пациент страдает от подагры.9. Способ по п.8, в котором указанная подагра является невосприимчивой к традиционному лечению.10. Способ по п.9, в котором указанная подагра является хронической или узелково РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2012 102 392 A (51) МПК A61B 5/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2012102392/15, 25.06.2010 (71) Заявитель(и): САВИЕНТ ФАРМАСЬЮТИКАЛЗ, ИНК. (US), КОРЕЛЭБ ПАРТНЕРС, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет: (43) Дата ...

피리딘메틸 술피닐-1H-벤즈이미다졸 화합물의 광학적으로 순수한 염(Optically Pure Salts of Pyridinylmethyl sulfinyl-1H-Benzimidazole compounds)

광학적으로 순수한 새로운 화합물인(+)-5-메톡시-2-[[(4-메톡시-3,5-디메틸-2-피리디닐)메틸]술피닐]-1H-벤즈이미다졸 또는 (-)-5-메톡시-2-[[(4-메톡시-3,5-디메틸-2-피리디닐)메틸]술피닐]-1H-벤즈이미다졸의 Na + , Mg 2+ , Li + , K + , Ca 2+ 및 N + (R) 4 (여기서, R는 탄소 원자 수가 1 내지 4개인 알킬기임)염과 그 제조방법 및 그 화합물을 유효 성분으로 함유하고 있는 약제와, 이 약제에 있어서의 그 화합물의 용도 및 그 화합물을 제조함으로써 얻어지는 중간체.

OPTICALLY PURE Na+, Mg2+, Li+, K+ OR Ca2+ SALTS OF (-)-5-METHOXY-2-[[(4- -METHOXY-3,5-DIMETHYL-2-PYRIDINYL)METHYL]SULFINYL]-1H-BENZ-IMIDAZOLE, METHOD OF THEIR SYNTHESIS, PHARMACEUTICAL COMPOSITION BASED ON SAID AND INTERMEDIATE COMPOUND

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to optically pure Na + , Mg 2+ , Li + , K + or Ca 2+ salts of (-)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole that show activity inhibiting an acid gastric secretion. EFFECT: improved method of synthesis, inhibition of gastric secretion. 17 cl, 1 dwg, 2 tbl, 13 ex Эс ПЧ Го ВУ” 2 137 766” С1 ОМ С 070 401/12, Аб К 31/44/(С 07 О 401/12, 213:63, 239:93), С 07 М 7:00 РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 95105587/04, 21.05.1994 (71) Заявитель: Астра Актиеболаг (5Е) (24) Дата начала действия патента: 21.05.1994 (72) Изобретатель: Пер Леннарт Линдберг (3Е), (30) Приоритет: 28.05.1993 ЗЕ 9301830-7 Сверкер Вон Унге (ЗЕ) (46) Дата публикации: 20.09.1999 (73) Патентообладатель: Астра Актиеболаг (3Е) (56) Ссылки: ОЕ 4035455 АЛ, 1992. ЕР 005129 АЛ, 1979. ЕР 0124495 А2, 1984. Машковский М.Д. Лекарственные средства. -М.: Медицина, 1987, ч.2, с.30-34. (85) Дата перевода заявки РСТ на национальную фазу: 27.01.95 (86) Заявка РСТ: ЗЕ 94100509 (27.05.94) (87) Публикация РСТ: М/О 94/27988 (08.12.94) (98) Адрес для переписки: 103735, Москва, ул.Ильинка 5/2, Союзпатент, Лебедевой Н.Г. (54) ОПТИЧЕСКИ ЧИСТЫЕ МА*, МС?*, 11*, К* ИЛИ СА?* СОЛИ (-)-5-МЕТОКСИ-2[[(4-МЕТОКСИ-3,5-ДИМЕТИЛ-2-ПИРИДИНИЛ)МЕТИЛ] СУЛЬФИНИЛ]-1Н-БЕНЗИМИДАЗОЛА, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМКОМПОЗИЦИЯ НА ИХ ОСНОВЕ И ПРОМЕЖУТОЧНОЕ СОЕДИНЕНИЕ (57) Реферат: быстрые метаболизаторы Оптически чистые Ма*, Ма?*, *, К* или Са?* соли 50 т —+ (+)-омепразол (-)-5-метокси-2-[[(4-метокси-3 ,5-диметил-2-пи 1250 -\ —=_ (-)-омепразол ридинил) метил] сульфинил] -1Н-бензимидазола обладают ингибирующей 1000 1 —*^ (+) -омепразоя желудочную кислотную секрецию 750 активностью. 4 с. и 13 з.п. ф-лы, 2 ил., 2 табл. 500 - Концентрация (нмоль/л) 250 + 0 1 2 3 4 5 6 Время (часы) Фиг. 1 2137766 С1 КО Эс ПЧ Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ ...

Crystalline form of URAT1 inhibitor and method for preparing the same

본 발명은 URAT1억제제의 결정형 및 그 제조방법을 개시하였다. The present invention discloses a crystalline form of an URAT1 inhibitor and a method for producing the same.