公开(公告)号：WO2005115977A1

公开(公告)日：2005-12-08

申请号：PCT/JP2005/010197

申请日：2005-05-27

Applicant: TANABE SEIYAKU CO., LTD. ,  MORITANI, Yasunori ,  FURUKUBO, Shigeru ,  TSUBOI, Yasunori ,  OKAGAKI, Chieko ,  OKU, Akira ,  HIRANO, Naomitsu

Inventor： MORITANI, Yasunori ,  FURUKUBO, Shigeru ,  TSUBOI, Yasunori ,  OKAGAKI, Chieko ,  OKU, Akira ,  HIRANO, Naomitsu

IPC: C07D207/14

CPC classification number: C07D207/14 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D491/04

Abstract: The present invention relates to a novel pyrrolidine compound, which has a potent antagonistic activity against central cannabinoid (CB1) receptor, having the formula [I]: wherein each of R 1 and R 2 is (A) optionally substituted aryl (or heteroaryl) group, or (B) both of the groups combine to form a group of the formula: one of R 3 and R 4 is hydrogen and another is hydrogen, hydroxyl, hydroxyalkyl, etc., or both of R 3 and R 4 combine to form oxo group, R 5 is hydrogen or alkyl, Y is single bond, oxygen atom or a group of the formula: -N(R 7 )-, R 6 is optionally substituted hydrocarbon group or optionally substituted cyclic group, R 7 is alkyl or alkyloxycarbonylalkyl, provided that R 6 is not 4-amino-5-chloro- 2-methoxyphenyl group when Y is single bond and one of the R 3 and R 4 is hydrogen and another is hydroxymethyl, or a pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及一种对中枢大麻素（CB1）受体具有有效拮抗活性的新型吡咯烷化合物，其具有式[I]：其中R 1和R 2各自为（A）任选取代的芳基 （或杂芳基）基团，或（B）两个基团结合形成下式的基团：R 3和R 4之一是氢，另一个是氢，羟基，羟基烷基等，或两者 R 3和R 4结合形成氧代基，R 5是氢或烷基，Y是单键，氧原子或下式的基团-N（R 7） - ，R 任选取代的烃基或任意取代的环状基团，R 7是烷基或烷氧基羰基烷基，条件是当Y是单键时，R 6不是4-氨基-5-氯-2-甲氧基苯基，一个 的R 3和R 4是氢，另一个是羟甲基或其药学上可接受的盐。