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    • 1. 发明申请
    • SUBSTITUTED SPIROKETAL DERIVATIVES AND USE THEREOF AS THERAPEUTIC DRUG FOR DIABETES
    • 取代的螺旋体衍生物及其作为治疗药物用于糖尿病的药物
    • US20110275703A1
    • 2011-11-10
    • US12375363
    • 2007-07-27
    • Tsutomu SatoKiyofumi HondaTakahiro KawaiKoo Hyeon Ahn
    • Tsutomu SatoKiyofumi HondaTakahiro KawaiKoo Hyeon Ahn
    • A61K31/352A61P3/04A61K31/381A61P3/10C07D493/10C07D409/14
    • C07H19/01
    • The present invention provides a compound represented by Formula (II): wherein R1 is a chlorine atom, a fluorine atom, a methyl group or an ethynyl group; Ar is a group represented by the following Formula (a), Formula (b), Formula (c) or Formula (d): wherein R2 is a C1-6 alkyl group which may be substituted with one or more halogen atoms, a C1-6 alkoxy group which may be substituted with one or more halogen atoms, a C1-3 alkylthio group, a halogen atom, a C1-3 alkylcarbonyl group or a C2-5 alkynyl group which may be substituted with —OR4; R3 is a hydrogen atom or a C1-3 alkyl group; R4 is a hydrogen atom or a C1-3 alkyl group; provided that Ar is a group represented by Formula (a) when R1 is a fluorine atom, methyl group or an ethynyl group, and that R2 is methoxy group, an ethoxy group, an isopropyl group, a propyl group, a trifluoromethyl group, a trifluoromethoxy group, 2-fluoroethyl group or 1-propynyl group when R1 is a methyl group or a pharmaceutically acceptable salt or a solvate thereof and a pharmaceutical agent, a pharmaceutical composition and so on comprising the compound.
    • 本发明提供由式(II)表示的化合物:其中R1是氯原子,氟原子,甲基或乙炔基; Ar是由下式(a),式(b),式(c)或式(d)表示的基团:其中R 2是可以被一个或多个卤素原子取代的C 1-6烷基,C 1 可以被一个或多个卤素原子取代的C 1-6烷氧基,可以被-OR 4取代的C 1-3烷硫基,卤素原子,C 1-3烷基羰基或C 2-5炔基; R3是氢原子或C1-3烷基; R4是氢原子或C1-3烷基; 条件是当R1为氟原子,甲基或乙炔基时,Ar为式(a)所示的基团,R2为甲氧基,乙氧基,异丙基,丙基,三氟甲基, 三氟甲氧基,2-氟乙基或1-丙炔基,R 1为甲基或其药学上可接受的盐或溶剂化物,药物组合物,药物组合物等。