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    COMPOSITIONS CONTAINING BENZIMIDAZOLONES AND PROGESTOGENS
    1.
    发明公开
    COMPOSITIONS CONTAINING BENZIMIDAZOLONES AND PROGESTOGENS 审中-公开
    苯并咪唑酮组合物和孕激素CONTAIN

    公开(公告)号：EP1173213A1

    公开(公告)日：2002-01-23

    申请号：EP00932006.0

    申请日：2000-05-01

    申请人： American Home Products Corporation ,  LIGAND PHARMACEUTICALS INCORPORATED

    发明人： GRUBB, Gary, S. ,  ZHI, Lin ,  JONES, Todd, K. ,  MARSCHKE, Keith, B. ,  TEGLEY, Christopher, M. ,  ZHANG, Puwen ,  BENDER, Reinhold,H.,W. ,  EDWARDS, JAMES, P. ,  WROBEL, Jay, E. ,  BENDER, Reinhold, H., W.

    IPC分类号： A61K45/06 ,  A61K31/57 ,  A61P15/18

    CPC分类号： A61K45/06 ,  A61K31/415 ,  A61K31/535 ,  A61K31/54 ,  A61K31/56 ,  A61K31/57 ,  A61K31/565 ,  A61K31/495 ,  A61K31/425 ,  A61K31/42 ,  A61K2300/00

    摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having general structure (1) wherein: A is O, S, or NR4; B is a bond between A and C=Q, or the moiety CR?5R6; R4, R5, R6¿ are independently selected from H or optionally substituted C¿1? to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, or heterocyclic groups, or cyclic alkyl constructed by fusing R?4 and R5¿ to form a 5 to 7 membered ring; R1 is selected from H, OH, NH¿2?, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, substituted alkynyl, -COH, or optionally substituted -CO(C1 to C3 alkyl), -CO(aryl), -CO(C1 to C3 alkoxy), or -CO(C1 to C3 aminoalkyl) groups; R?2¿ is selected from H, halogen, CN, NO¿2?, or optionally substituted C1 to C6 alkyl, C1 to C6 alkoxy, or C1 to C6 aminoalkyl groups; R?3¿ is selected from a trisubstituted benzene ring; or a 5- or 6-membered heteroaromatic ring containing 1 or 2 substituents; or a pharmaceutically acceptable salt thereof, in combination with a progestational agent, an estrogen, or both or for the 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. These combinations may also be used in methods of contraception, to stimulate food intake or for minimization of side effects or cyclic menstrual bleeding.