公开(公告)号：US20120202992A1

公开(公告)日：2012-08-09

申请号：US13418811

申请日：2012-03-13

申请人： Koichi TANIMOTO ,  Mariko OI ,  Yasunori TSUBOI ,  Yasunori MORITANI

发明人： Koichi TANIMOTO ,  Mariko OI ,  Yasunori TSUBOI ,  Yasunori MORITANI

IPC分类号： C07D487/04

CPC分类号： C07D487/04

摘要： Pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of formula [I]: wherein R1 and R2 are the same or different and each is an optionally substituted aryl group, etc., R0 is hydrogen, an alkyl group, etc., E is —C(═O)— or —SO2—, R is a group of formula [i], [ii] or [iii], etc: Ring A is a C3-8 cycloalkyl group optionally fused to a benzene ring or a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom, etc., R3 is an alkyl group optionally substituted by an alkylthio group, R4 is hydrogen atom, an alkyl group, etc., one of RA and RB is an alkyl group, etc., and the other is hydrogen, an alkyl group, etc., or a pharmaceutically acceptable salt thereof.

摘要翻译： 具有式[I]的CB 1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R1和R2相同或不同，并且各自为任选取代的芳基等，R 0是氢， 烷基等，E是-C（= O） - 或-SO 2 - ，R是式[ⅰ]，[ⅱ]或[ⅲ]等基团：环A是任选的C 3-8环烷基 稠合到苯环或苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基，所述环状基团通过其环碳原子与相邻氮原子结合， X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等，RA和RB之一是烷基等，另一个是氢 ，烷基等，或其药学上可接受的盐。