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1. 发明申请

WO2012075253A2 PHARMACEUTICAL COMPOSITIONS 审中-公开
标题翻译：药物组合物
公开(公告)号：WO2012075253A2
公开(公告)日：2012-06-07
申请号：PCT/US2011062837
申请日：2011-12-01
申请人： NOVARTIS AG , CAO YU , HACKL WOLFGANG , LI PING , LI SHOUFENG , MIRZA TAHSEEN , ZEHENDER HARTMUT , ZHU JIAHAO
发明人： CAO YU , HACKL WOLFGANG , LI PING , LI SHOUFENG , MIRZA TAHSEEN , ZEHENDER HARTMUT , ZHU JIAHAO
IPC分类号： A61K9/16 , A61P35/00
CPC分类号： C07D471/04 , A61K9/1617 , A61K9/1623 , A61K9/1635 , A61K9/1641 , A61K9/1694 , A61K31/00
摘要： The present invention relates to a pharmaceutical composition for the oral administration of a therapeutic compound of formula (I), which comprises granules that comprise at least therapeutic compound of formula (I) (see below), particularly 2-Methyl-2-[4-(3-methyl-2-oxo-8- quinolin-3-yl-2,3-dihydro-imidazo[4,5-c]quinolin-1-yl)-phenyl]-propionitrile or 8-(6-methoxy-pyridin-3-yl)-3-methyl-1-(4-piperazin-1-yl-3-trifluoromethyl-phenyl)-1,3-dihydro-imidazo[4,5-c]quinolin-2-one, or a tautomer thereof, or a pharmaceutically acceptable salt, or a hydrate or solvate thereof; at least one non-ionic surfactant that is Vitamin E-TPGS in an amount ranging from about 15 to about 80% by weight of the composition; and at least one a dissolution enhancing agent selected from polyethylene glycol, polyethylene oxide, and any combination of the foregoing. The present invention also relates to processes for making such pharmaceutical compositions; a kit comprising such pharmaceutical composition and the instructions provide that the pharmaceutical composition may be taken immediately to about thirty minutes after the consumption of food; and related uses and methods of treatment.
摘要翻译：本发明涉及用于口服施用式（I）的治疗性化合物的药物组合物，其包含至少包含式（I）的治疗性化合物（参见下文），尤其是2-甲基-2- [4 - （3-甲基-2-氧代-8-喹啉-3-基-2,3-二氢 - 咪唑并[4,5-c]喹啉-1-基） - 苯基] - 丙腈或8-（6-甲氧基 - 吡啶-3-基）-3-甲基-1-（4-哌嗪-1-基-3-三氟甲基 - 苯基）-1,3-二氢 - 咪唑并[4,5-c]喹啉-2-酮，或其互变异构体，或其药学上可接受的盐或水合物或溶剂化物; 至少一种非离子表面活性剂，其量为组合物重量的约15至约80％的量的维生素E-TPGS; 和至少一种选自聚乙二醇，聚环氧乙烷和前述的任意组合的溶解增强剂。本发明还涉及制造这种药物组合物的方法; 包含此类药物组合物和说明书的试剂盒提供了可以立即在食物消耗后约三十分钟服用药物组合物; 以及相关的用途和治疗方法。

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