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    • 10. 发明申请
    • Substituted Pyrrole Derivative
    • 取代的吡咯衍生物
    • US20080176906A1
    • 2008-07-24
    • US11793113
    • 2005-12-13
    • Nobuyuki MatsunagaTakenori Hitaka
    • Nobuyuki MatsunagaTakenori Hitaka
    • A61K31/4439C07D401/06C07D413/12A61P35/00A61K31/40C07D207/32
    • C07D207/327C07D207/34C07D401/06C07D413/14
    • The present invention provides a novel pyrrole derivative having excellent androgen receptor antagonism, which is represented by the formula: wherein R1 represents a hydrogen atom, a cyano group or a group represented by the formula COORA (wherein RA represents an optional substituted C1-6 alkyl group), R2 and R4 are the same or different, and each represents a hydrogen atom, a C1-6 alkyl group, a C3-6 cycloalkyl group, a trifluoromethyl group, an amino-C1-6 alkyl group, a mono- or di-substituted amino-C1-6 alkyl group, an optionally halogenated C1-6 alkyl group substituted with an optionally substituted hydroxyl group, a C2-6 alkenyl group substituted with an optionally substituted hydroxyl group, a C1-6 alkyl group substituted with an optionally substituted and optionally oxidized thiol group, an optionally substituted with and optionally oxidized thiol group, a cyano group, an acyl group, an optionally substituted oxazolyl group or a 1,3-dioxolan-2-yl group, R3 represents a group represented by the formula: (wherein X represents a halogen atom, Y represents a carbon atom or a nitrogen atom, Alk represents an optionally substituted C1-4 alkylene group, and RB represents a hydrogen atom or an acyl group), and R5 represents a phenyl group which has a cyano group at a 4-position or a 3-position thereof, and may be further substituted, or a salt thereof. The present invention also provides an androgen receptor antagonist containing the pyrrole derivative, or a salt thereof.
    • 本发明提供具有优异雄激素受体拮抗作用的新型吡咯衍生物,其由下式表示:其中R 1表示氢原子,氰基或由式COOR < A (其中R A表示任选的取代的C 1-6烷基),R 2和R 4 各自相同或不同,各自表示氢原子,C 1-6烷基,C 3-6环烷基,三氟甲基 氨基-C 1-6烷基,一取代或二取代的氨基-C 1-6烷基,任意卤代的C 1〜 被任选取代的羟基取代的6个C 1 -C 6烷基,被任意取代的羟基取代的C 2-6-6烯基,C 1-6烷基 被任选取代的和任选被氧化的硫醇基团取代的基团,任选地被任选地被氧化物取代 硫醇基,氰基,酰基,任选取代的恶唑基或1,3-二氧戊环-2-基,R 3表示由下式表示的基团:(其中X 表示卤原子,Y表示碳原子或氮原子,Alk表示任选取代的C 1-4 - 亚烷基,R B表示氢原子或 酰基),R 5表示在4位或3位具有氰基的苯基,可以进一步被取代,或其盐。 本发明还提供含有吡咯衍生物或其盐的雄激素受体拮抗剂。