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    • 16. 发明申请
    • CYCLOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS
    • CYCOCARBAMATE衍生物作为孕激素受体调节剂
    • WO00066571A1
    • 2000-11-09
    • PCT/US2000/011822
    • 2000-05-01
    • C07D265/12A61K31/536A61K31/537A61P15/00A61P15/18A61P35/00A61P43/00C07D265/18C07D413/04C07D413/10C07D417/04C07F9/6533
    • C07D265/18C07D413/04C07D413/10C07D417/04
    • This invention provides compounds of Formula (I) wherein R and R may be single substituents or fused to form spirocyclic or heterospirocyclic rings; R is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, COR ; R is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy , substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R 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, SO2 or NR and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, COR , or NR COR ; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.
    • 本发明提供式(I)化合物,其中R 1和R 2可以是单取代基或稠合形成螺环或杂环环; R 3是H,OH,NH 2,C 1至C 6烷基,取代的C 1 -C 6烷基,C 3至C 6烯基,取代的C 1至C 6烯基,炔基或取代的炔基。 R C是H,C 1至C 3烷基,取代的C 1至C 3烷基,芳基,取代的芳基,C 1至C 3的烷氧基,取代的C 1至C 3的烷氧基,C 1至C 3的氨基烷基或取代的C 1至C 3氨基烷基; R 4是H,卤素,CN,NO 2,C 1至C 6烷基,取代的C 1 -C 6烷基,炔基或取代的炔基,C 1至C 6烷氧基,取代的C 1至C 6烷氧基,取代的C 1至C 6烷氧基, 至C6氨基烷基或取代的C1至C6氨基烷基; R 5选自具有1,2或3个杂原子的五元或六元环的三取代苯环,所述杂原子包括O,S,SO,SO 2或NR 6,并含有一个或两个独立的取代基 包括H,卤素,CN,NO 2,氨基和C 1至C 3烷基,C 1至C 3烷氧基,C 1至C 3氨基烷基,COR F或NR G COR F; 或其药学上可接受的盐,以及使用该化合物作为孕酮受体的拮抗剂的药物组合物和方法。