发明公开
EP1173208A2 CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC UREA AND AMIDE DERIVATIVES
审中-公开
避孕组合物,其环状脲和酰胺CONTAIN
- 专利标题: CONTRACEPTIVE COMPOSITIONS CONTAINING CYCLIC UREA AND AMIDE DERIVATIVES
- 专利标题(中): 避孕组合物,其环状脲和酰胺CONTAIN
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申请号: EP00928519.8申请日: 2000-05-01
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公开(公告)号: EP1173208A2公开(公告)日: 2002-01-23
- 发明人: GRUBB, Gary, S. , ZHI, Lin , JONES, Todd, K. , TEGLEY, Christopher, M. , PUWEN, Zhang , FENSOME, Andrew , VIET, Andrew, Q. , SANTILLI, Arthur, A. , TEREFENKO, Eugene, A. , WROBEL, Jay, E. , EDWARDS, James, P.
- 申请人: AMERICAN HOME PRODUCTS CORPORATION , LIGAND PHARMACEUTICALS INCORPORATED
- 申请人地址: Five Giralda Farms Madison, New Jersey 07940-0874 US
- 专利权人: AMERICAN HOME PRODUCTS CORPORATION,LIGAND PHARMACEUTICALS INCORPORATED
- 当前专利权人: AMERICAN HOME PRODUCTS CORPORATION,LIGAND PHARMACEUTICALS INCORPORATED
- 当前专利权人地址: Five Giralda Farms Madison, New Jersey 07940-0874 US
- 代理机构: Hale, Stephen Geoffrey
- 优先权: US198238P 19990504; US552037 20000419
- 国际公布: WO0066103 20001109
- 主分类号: A61K45/06
- IPC分类号: A61K45/06 ; A61K31/57 ; A61K31/565 ; A61P15/18 ; A61K31/495 ; A61K31/12
摘要:
This invention concerns cyclic combination therapies using indoline derivatives which are progesterone receptor antagonists of general structure (I) wherein: A, B and D are N or CH, though not all can be CH; R?1 and R2¿ are H, COR?A, NRBCORA¿, or optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, or aryl groups; or R?1 and R2¿ form a spirocyclic ring; RA is H or optionally substituted alkyl, aryl, alkoxy, or aminoalkyl; RB is H, alkyl alkyl; R3 is H, OH, NH¿2?, alkyl, alkenyl, or COR?C; RC¿ is H, alkyl, aryl, alkoxy, or aminoalkyl; R4 is benzene or a 5 or 6 memebered heteroaromatic ring; RF is H, alkyl, aryl, alkoxy, or aminoalkyl; RG is H or alkyl; R5 is H or alkyl; W is O or a chemical bond; or a pharmaceutically acceptable salt thereof. These methods may be used for contraception or treatment and/or prevention of secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis; polycystic ovary syndrome, carcinomas and adenocarcinomas of the endometrium, ovary, breast, colon, prostate, or minimization of side effects or cyclic menstrual bleeding. Additional uses of the invention include stimulation of food intake.
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