申请人:——
公开号:US20020049204A1
公开(公告)日:2002-04-25
This invention provides compounds of Formula (I):
1
wherein R
1
and R
2
may be single substituents or fused to form spirocyclic or hetero-spirocyclic rings; R
3
is H, OH, NH
2
, C
1
to C
6
alkyl, substituted C
1
to C
6
alkyl, C
3
to C
6
alkenyl, substituted C
1
to C
6
alkenyl, alkynyl, or substituted alkynyl, COR
C
; R
C
is H, C
1
to C
3
alkyl, substituted C
1
to C
3
alkyl, aryl, substituted aryl, C
1
to C
3
alkoxy, substituted C
1
to C
3
alkoxy, C
1
to C
3
aminoalkyl, or substituted C
1
to C
3
aminoalkyl;
R
4
is H, halogen, CN, NO
2
, C
1
to C
6
alkyl, substituted C
1
to C
6
alkyl, alkynyl, or substituted alkynyl, C
1
to C
6
alkoxy, substituted C
1
to C
6
alkoxy, amino, C
1
to C
6
aminoalkyl, or substituted C
1
to C
6
aminoalkyl; and R
5
is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO
2
or NR
6
and containing one or two independent substituents from the group including H, halogen, CN, NO
2
, amino, and C
1
to C
3
alky, C
1
to C
3
alkoxy, C
1
to C
3
aminoalkyl, COR
F
, or NR
G
COR
F
; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.
这项发明提供了Formula (I)的化合物:
其中R1和R2可以是单个取代基或融合形成螺环或杂环螺环;R3为H、OH、NH2、C1到C6烷基、取代的C1到C6烷基、C3到C6烯基、取代的C1到C6烯基、炔基或取代的炔基、CORC;RC为H、C1到C3烷基、取代的C1到C3烷基、芳基、取代的芳基、C1到C3烷氧基、取代的C1到C3烷氧基、C1到C3氨基烷基或取代的C1到C3氨基烷基;
R4为H、卤素、CN、NO2、C1到C6烷基、取代的C1到C6烷基、炔基或取代的炔基、C1到C6烷氧基、取代的C1到C6烷氧基、氨基、C1到C6氨基烷基或取代的C1到C6氨基烷基;R5从包括O、S、SO、SO2或NR6的1、2或3个杂原子的五元或六元环的三取代苯环中选择,并含有来自包括H、卤素、CN、NO2、氨基和C1到C3烷基、C1到C3烷氧基、C1到C3氨基烷基、CORF或NRGCORF的一个或两个独立取代基;或其药学上可接受的盐,以及将这些化合物用作孕激素受体拮抗剂的药物组合物和方法。