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2. 发明申请

US20080194656A1 Benzotriazole Derivatives as Cannabinoid Receptor Antagonists 审中-公开
标题翻译：苯并三唑衍生物作为大麻素受体拮抗剂
公开(公告)号：US20080194656A1
公开(公告)日：2008-08-14
申请号：US11912375
申请日：2006-04-24
申请人： Monique Jenny Marie Berwaer , Joannes Theodorus Maria Linders , Peter John King , Geert Maria Robert Van Hecke
发明人： Monique Jenny Marie Berwaer , Joannes Theodorus Maria Linders , Peter John King , Geert Maria Robert Van Hecke
IPC分类号： A61K31/4196 , C07D249/18 , A61K31/427 , A61P25/00 , A61P3/04 , C07D417/10
CPC分类号： A61K31/4192 , C07D249/18 , C07D403/06 , C07D417/06
摘要： The present invention relates to a group of benzotriazole derivatives, infra that are potent cannabinoid-CB1 modulators (known as antagonists or inverse agonists), useful in the treatment obesity, psychiatric and neurological disorders, as well as other diseases involving cannabinoid-CB1 neurotransmission (Current Opinion in Drug Discovery & Development 2004 7(4):498-506) the pharmaceutically acceptable acid addition salts and stereoisomeric forms thereof, wherein R1 is hydrogen, halo, trifluoromethyl, C1-4alkyl, C1-4alkyloxy- or C1-4alkyloxycarbonyl; R2 is hydrogen, phenyl, C3-7cycloalkyl or C1-6alkyl optionally substituted with Ar1; R3 is hydrogen, hydroxyl or C1-6alkyl; Ar1 is phenyl or phenyl substituted with up to three halo substituents; and Het represents a monocyclic 5 or 6 membered partially saturated or aromatic heterocycle selected from furanyl, thienyl, pyrrolyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, thiadiazolyl, pyrimidinyl, pyridinyl, pyrazinyl, triazinyl, pyridazinyl, 2H-pyranyl or 4H-pyranyl wherein said heterocycle is optionally substituted with C1-6alkyl;
摘要翻译：本发明涉及以下一组苯并三唑衍生物，以下是可用于治疗肥胖，精神和神经障碍的有效的大麻素-CB 1 N调节剂（称为拮抗剂或反向激动剂），以及涉及大麻素CB 1神经传递（Current Opinion in Drug Discovery＆Development 2004,7（4）：498-506）的其它疾病，其药学上可接受的酸加成盐和立体异构形式，其中R 1 氢，卤素，三氟甲基，C 1-4烷基，C 1-4烷基氧基或C 1-4烷基氧基羰基 ; R 2是氢，苯基，C 3-7环烷基或任选被Ar 1或O 2取代的C 1-6烷基 >; R 3是氢，羟基或C 1-6烷基; Ar 1是苯基或被至多3个卤素取代基取代的苯基; 并且Het表示选自呋喃基，噻吩基，吡咯基，恶唑基，噻唑基，咪唑基，吡唑基，异唑基，异噻唑基，恶二唑基，三唑基，噻二唑基，嘧啶基，吡啶基，吡嗪基，三嗪基，哒嗪基，吡嗪基等的单环5或6元部分饱和或芳族杂环。其中所述杂环任选被C 1-6烷基取代;

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