申请人:TANIMOTO Koichi
公开号:US20120202992A1
公开(公告)日:2012-08-09
Pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of formula [I]:
wherein R
1
and R
2
are the same or different and each is an optionally substituted aryl group, etc.,
R
0
is hydrogen, an alkyl group, etc.,
E is —C(═O)— or —SO
2
—,
R is a group of formula [i], [ii] or [iii], etc:
Ring A is a C
3-8
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.,
R
3
is an alkyl group optionally substituted by an alkylthio group,
R
4
is hydrogen atom, an alkyl group, etc.,
one of R
A
and R
B
is an alkyl group, etc., and the other is hydrogen, an alkyl group, etc., or a pharmaceutically acceptable salt thereof.
一种具有CB1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物,其化学式为[I]:其中R1和R2相同或不同,且每个都是可选取代的芳基基团等,R0为氢、烷基基团等,E为—C(═O)—或—SO2—,R为式[i]、[ii]或[iii]等的基团:环A为C3-8环烷基团,可选地融合到苯环或苯环上,Q为单键或亚甲基基团,环B为4-至7-成员的脂肪族杂环基团,所述环基团通过其环碳原子与相邻的氮原子结合,X为硫原子等,R3为可选取代的烷基基团,R4为氢原子、烷基基团等,RA和RB中的一个为烷基基团等,另一个为氢、烷基基团等,或其药学上可接受的盐。