申请人:Mitsubishi Tanabe Pharma Corporation
公开号:US07872006B2
公开(公告)日:2011-01-18
The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]:
wherein
R1 and R2 are the same or different and an optionally substituted aryl group etc.,
R3 is an alkyl group etc.,
E is one of the following groups of the formula (i) to (iv):
Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—,
R7 is a hydrogen atom or an alkyl group,
Q2 is a single bond, an oxygen atom or an alkylene group,
R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc.,
one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc.,
D is an oxygen atom etc.,
RA1 is an amino group etc.,
RA2 is an optionally substituted aliphatic heterocyclic group,
R is an alkyl group optionally substituted by one to three halogen atom(s) etc.,
one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.
本发明涉及一种具有强CB1拮抗活性的吡唑化合物,其具有以下式[I]:其中R1和R2相同或不同,可选地取代芳基等;R3是烷基等;E是以下式(i)到(iv)中的一种基团:Q1是单键,烷基或式:—N(R7)—的基团,R7是氢原子或烷基;Q2是单键,氧原子或烷基;R4是环烷基,式:—N(R5)(R6)等的基团,R5和R6中的一个是氢原子或烷基,另一个是烷基,式:—N(R8)(R9)等的基团;D是氧原子等;RA1是氨基等;RA2是可选取代的脂肪族杂环基团;R是烷基,可选地被一个到三个卤原子等取代;R8和R9中的一个是氢原子或烷基,另一个是烷基等;或其药学上可接受的盐。