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    • 66. 发明授权
    • Caspase inhibitors and uses thereof
    • 胱天蛋白酶抑制剂及其用途
    • US07612091B2
    • 2009-11-03
    • US10743563
    • 2003-12-22
    • Jean-Damien CharrierMichael MortimoreJohn R. Studley
    • Jean-Damien CharrierMichael MortimoreJohn R. Studley
    • C07D215/22A61K31/47
    • C07D401/12C07D217/24C07D405/12C07D417/12
    • The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 is: C1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF3, Cl, F, OMe, OEt, OCF3, CN, or NMe2; C1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with —O— or —NR5—; R2 is C1-6 straight chained or branched alkyl; R3 is hydrogen, halo, OCF3, CN, or CF3; R4 is hydrogen, halo, OCF3, CN, or CF3; and each R5 is independently H, C1-6 straight chained or branched alkyl, aryl, —O—C1-6 straight chained or branched alkyl, or —O-aryl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated disease, particularly in the central nervous system.
    • 本发明提供式I化合物:其中:X为-OR1或-N(R5)2,Y为卤素,三氟苯氧基或四氟苯氧基; R 1是:C 1-6直链或支链烷基,烯基或炔基,其中烷基,烯基或炔基任选被任选取代的芳基CF 3,Cl,F,OMe,OEt,OCF 3,CN或NMe 2取代; C 1-6环烷基,其中环烷基中的1-2个碳原子任选被-O-或-NR 5 - 取代; R2是C1-6直链或支链烷基; R3是氢,卤素,OCF3,CN或CF3; R4是氢,卤素,OCF3,CN或CF3; 每个R 5独立地为H,C 1-6直链或支链烷基,芳基,-O-C 1-6直链或支链烷基或-O-芳基。 本发明还提供了使用这种组合物治疗半胱天冬酶介导的疾病,特别是中枢神经系统的药物组合物和方法。