Inhibitors of cell proliferation, angiogenesis, fertility, and muscle contraction
申请人:——
公开号:US20030064989A1
公开(公告)日:2003-04-03
The invention concerns inhibitors of cell proliferation, angiogenesis, fertility, and muscle contraction, characterized by formula I
1
wherein,
X, Y and Z independently represent C or N;
------ is an optional double bond;
n is
0
or 1;
R
1
, R
2
, and R
4
independently represent hydrogen, a chemical bond, C
1-10
alkyl; C
2-10
alkenyl; C
2-10
alkinyl; aryl; aryl-C
1-10
alkyl; C
3-10
heterocyclyl; C
5-10
heteroaryl; halo, CF
3
; NO
2
; NHC(O)R*, OR, said alkyl, alkenyl, alkinyl, aryl, arylalkyl, heterocyclyl, or heteroaryl being optionally substituted;
R
3
, R
5
, and R
6
independently represent hydrogen, C
1-10
alkyl; C
2-10
alkenyl; C
2-10
alkinyl; aryl; aryl-C
1-10
alkyl; C
3-10
heterocyclyl; C
5-10
heteroaryl; halo, CF
3
; NO
2
; NHC(O)R*, OR, said alkyl, alkenyl, alkinyl, aryl, heterocyclyl, or heteroaryl being optionally substituted; or
R
5
and R
6
together form a 5- or 6-member aryl, heterocyclyl or heteroaryl group;
R is hydrogen or C
1-6
alkyl;
R* is hydrogen, or C
1-6
alkyl, or OH,
wherein the optional substituents are preferably selected from the group of one to three OH, C
1-6
alkyl, halo, NO
2
, C
1-6
alkoxy, and CF3,
or a pharmaceutically acceptable salt thereof.
该发明涉及细胞增殖、血管生成、生育和肌肉收缩的抑制剂,其特征在于以下公式I1:
其中,X、Y和Z独立表示C或N;------是一个可选的双键;n为0或1;R1、R2和R4独立表示氢、化学键、C1-10烷基;C2-10烯基;C2-10炔基;芳基;芳基-C1-10烷基;C3-10杂环烷基;C5-10杂芳基;卤素、三氟甲基;NO2;NHC(O)R*、OR,所述的烷基、烯基、炔基、芳基、芳基烷基、杂环烷基或杂芳基可以是可选的取代基;R3、R5和R6独立表示氢、C1-10烷基;C2-10烯基;C2-10炔基;芳基;芳基-C1-10烷基;C3-10杂环烷基;C5-10杂芳基;卤素、三氟甲基;NO2;NHC(O)R*、OR,所述的烷基、烯基、炔基、芳基、芳基烷基、杂环烷基或杂芳基可以是可选的取代基;或者R5和R6一起形成一个5-或6-成员的芳基、杂环烷基或杂芳基;R为氢或C1-6烷基;R*为氢、或C1-6烷基、或OH,其中可选的取代基优选从一个到三个OH、C1-6烷基、卤素、NO2、C1-6烷氧基和三氟甲基中选择,或其药学上可接受的盐。