申请人:Moritani Yasunori
公开号:US20090048256A1
公开(公告)日:2009-02-19
The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]:
wherein
R
1
and R
2
are the same or different and an optionally substituted aryl group etc.,
R
3
is an alkyl group etc.,
E is one of the following groups of the formula (i) to (iv):
Q
1
is a single bond, an alkylene group or a group of the formula: —N(R
7
)—,
R
7
is a hydrogen atom or an alkyl group,
Q
2
is a single bond, an oxygen atom or an alkylene group,
R
4
is a cycloalkyl group, a group of the formula: —N(R
5
)(R
6
) etc.,
one of R
5
and R
6
is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R
8
)(R
9
) etc.,
D is an oxygen atom etc.,
R
A1
is an amino group etc.,
R
A2
is an optionally substituted aliphatic heterocyclic group,
R is an alkyl group optionally substituted by one to three halogen atom(s) etc.,
one of R
8
and R
9
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效CB1拮抗活性的吡唑化合物,具有以下式[I]:其中R1和R2相同或不同,且可以是取代的芳基等,R3是烷基等,E是以下式(i)至(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,其中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,可选取代为1至3个卤原子等,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。