申请人:WYETH
公开号:US20030045511A1
公开(公告)日:2003-03-06
This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure:
1
wherein R
1
and R
2
may be single substituents or fused; R
3
is H, OH, NH
2
, C
1
to C
6
alkyl, COR
C
, or optionally substituted C
1
to C
6
alkyl, C
3
to C
6
alkenyl, or alkynyl; R
C
is H, or optionally substituted C
1
to C
3
alkyl, aryl, C
1
to C
3
alkoxy, or C
1
to C
3
aminoalkyl; R
4
is H, halogen, CN, NO
2
, or optionally substituted C
1
to C
6
alkyl, alkynyl, C
1
to C
6
alkoxy, amino, or C
1
to C
6
aminoalkyl; and R
5
is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.
本发明涉及使用取代的吲哚啉衍生物化合物进行环状联合疗法和方案,这些化合物是孕激素受体拮抗剂,具有以下一般结构:1其中,R1和R2可以是单一取代基或融合基;R3为H、OH、NH2、C1到C6烷基、CORC或可选取代的C1到C6烷基、C3到C6烯基或炔基;RC为H或可选取代的C1到C3烷基、芳基、C1到C3烷氧基或C1到C3氨基烷基;R4为H、卤素、CN、NO2或可选取代的C1到C6烷基、炔基、C1到C6烷氧基、氨基或C1到C6氨基烷基;R5为苯环、五元或六元杂环环;或其药学上可接受的盐。治疗方法包括避孕、继发性闭经、功能性出血、子宫平滑肌瘤、子宫内膜异位症、多囊卵巢综合症、癌症、腺癌、副作用最小化或食欲刺激。