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公开(公告)号：EP1249233B1
公开(公告)日：2008-08-20
申请号：EP00976387.1
申请日：2000-11-21
申请人： SHIONOGI & CO., LTD.
发明人： KAWANISHI, Yasuyuki Shionogi & Co., Ltd. , TAKENAKA, Hideyuki Shionogi & Co., Ltd. , HANASAKI, Kohji Shionogi & Co., Ltd. , OKADA, Tetsuo Shionogi & Co., Ltd.
IPC分类号： A61K31/18 , C07C311/06 , C07C311/20 , C07C311/46 , C07C323/40 , C07D207/12 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D213/75 , C07D215/36 , C07D217/04 , C07D219/10 , C07D231/16 , C07D231/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D285/06 , C07D295/12 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72 , A61P3/00
CPC分类号： C07D249/08 , A61K31/00 , A61K31/18 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/4453 , A61K31/451 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61K31/63 , A61K31/635 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/44 , C07C2603/18 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72
摘要： NPYY5 receptor antagonists which contain compounds represented bygeneral formula (I), prodrugs thereof, pharmaceutically acceptable salts thereof or solvates of the same wherein R1 represents lower alkyl, cycloalkyl, etc.; R2 represents hydrogen, lower alkyl, etc.; n is 1 or 2; X represents lower alkylene, lower alkenylene, arylene, cycloalkylene, etc.; Y represents CONR?7, CSNR7, NR7CO, NR7¿CS, etc. (wherein R7 represents hydrogen or lower alkyl); and Z represents lower alkyl, an optionally substituted hydrocarbon cycle, an optionally substituted heterocycle, etc.
摘要翻译： 神经肽Y5受体拮抗剂包含新的或已知的氨基亚磺酰基或氨基磺酰基衍生物（I）。 神经肽Y5受体拮抗剂包括式（I）的氨基亚磺酰基或氨基磺酰基衍生物，其前药，盐或溶剂合物。 R 1取代的低级烷基，环烷基或芳基，或R 1 + R 2低级亚烷基; n：1或2; X：（CR 3R 4）pA（CR 5R 6）q，HetU，NR 2 X或任选取代的低级亚烷基，低级亚烯基，CO-低级亚烷基或CO-低级亚烯基; A：任选取代的亚环烷基，亚环烯基，二亚环烷基，亚芳基或二价杂环; p，q：0或1; Het：哌啶二基，哌嗪二基，吡啶二基，吡嗪二基，吡咯烷二基或吡咯烷基，全部通过N连接到NR 2上; U：键，低级亚烷基或低级亚烯基; Y：OCONR 7，CONR 7，CSNR 7，NR 7CO或NR 7CS; R 2 -R 7H或低级烷基; Z：任选取代的低级烷基，低级烯基，氨基，低级烷氧基，碳环基或杂环基。 化合物（I），其盐，前药和溶剂合物也包括独立权利要求，其中：（i）X = 2-6C亚烷基或3-6C亚烯基; 且R 1 =任选取代的3-10C烷基或5或6C环烷基; 条件是当Y = NR 7时，Z不为低级烷基苯基氨基，低级羟烷基苯基氨基或酰基苯基氨基; （ii）A =亚杂芳基或任选取代的亚环烷基，亚环烯基，双环亚烷基或哌啶子基; 且R 1 =任选取代的3-10C烷基或5或6C环烷基; 和（iii）A =对亚苯基; R 1 = 3-10C烷基或5或6C环烷基，Z =对 - 低级烷基亚苯基; 条件是当R 1 =异丙基时，Z不是对正丁基亚苯基。 活动：厌食 降糖; 低血压; 降血脂; 抗动脉硬化; cardiant。 神经肽Y5拮抗剂。 在测定中，式（Ia）化合物显示出10.1nM的神经肽Y5结合的IC 50值和1.9nM的中国仓鼠卵巢细胞中的cAMP。 [图片]。
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公开(公告)号：EP1249233A1
公开(公告)日：2002-10-16
申请号：EP00976387.1
申请日：2000-11-21
申请人： SHIONOGI & CO., LTD.
发明人： KAWANISHI, Yasuyuki Shionogi & Co., Ltd. , TAKENAKA, Hideyuki Shionogi & Co., Ltd. , HANASAKI, Kohji Shionogi & Co., Ltd. , OKADA, Tetsuo Shionogi & Co., Ltd.
IPC分类号： A61K31/18
CPC分类号： C07D249/08 , A61K31/00 , A61K31/18 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/4453 , A61K31/451 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61K31/63 , A61K31/635 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/44 , C07C2603/18 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72
摘要： The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I):
wherein
R 1 is lower alkyl, cycloalkyl or the like,
R 2 is hydrogen, lower alkyl or the like,
n is 1 or 2,
X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like,
Y is CONR 7 , CSNR 7 , NR 7 CO, NR 7 CS or the like,
Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R 7 is hydrogen or lower alkyl,
prodrug, pharmaceutically acceptable salt or solvate thereof-
公开(公告)号：EP1249233B9
公开(公告)日：2009-08-05
申请号：EP00976387.1
申请日：2000-11-21
申请人： SHIONOGI & CO., LTD.
发明人： KAWANISHI, Yasuyuki Shionogi & Co., Ltd. , TAKENAKA, Hideyuki Shionogi & Co., Ltd. , HANASAKI, Kohji Shionogi & Co., Ltd. , OKADA, Tetsuo Shionogi & Co., Ltd.
IPC分类号： A61K31/18 , C07C311/06 , C07C311/20 , C07C311/46 , C07C323/40 , C07D207/12 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D213/75 , C07D215/36 , C07D217/04 , C07D219/10 , C07D231/16 , C07D231/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D285/06 , C07D295/12 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72 , A61P3/00
CPC分类号： C07D249/08 , A61K31/00 , A61K31/18 , A61K31/341 , A61K31/351 , A61K31/357 , A61K31/37 , A61K31/381 , A61K31/4015 , A61K31/402 , A61K31/4035 , A61K31/41 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/433 , A61K31/44 , A61K31/4409 , A61K31/4453 , A61K31/451 , A61K31/495 , A61K31/4965 , A61K31/505 , A61K31/5375 , A61K31/63 , A61K31/635 , C07C311/06 , C07C311/07 , C07C311/08 , C07C311/14 , C07C311/20 , C07C311/21 , C07C311/46 , C07C323/40 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/44 , C07C2603/18 , C07D207/09 , C07D207/12 , C07D207/16 , C07D209/08 , C07D209/48 , C07D209/88 , C07D211/58 , C07D211/62 , C07D213/75 , C07D213/82 , C07D215/36 , C07D215/38 , C07D217/04 , C07D219/10 , C07D231/12 , C07D231/16 , C07D231/56 , C07D233/56 , C07D233/68 , C07D239/42 , C07D277/56 , C07D277/70 , C07D285/06 , C07D295/135 , C07D307/68 , C07D307/91 , C07D311/16 , C07D317/66 , C07D333/38 , C07D333/72
摘要： NPYY5 receptor antagonists which contain compounds represented bygeneral formula (I), prodrugs thereof, pharmaceutically acceptable salts thereof or solvates of the same wherein R1 represents lower alkyl, cycloalkyl, etc.; R2 represents hydrogen, lower alkyl, etc.; n is 1 or 2; X represents lower alkylene, lower alkenylene, arylene, cycloalkylene, etc.; Y represents CONR?7, CSNR7, NR7CO, NR7¿CS, etc. (wherein R7 represents hydrogen or lower alkyl); and Z represents lower alkyl, an optionally substituted hydrocarbon cycle, an optionally substituted heterocycle, etc.
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