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    • 1. 发明授权
    • Pyrazolones derivatives
    • 吡唑啉酮衍生物
    • US5968967A
    • 1999-10-19
    • US51085
    • 1998-04-13
    • Keizo TanikawaTakashi MatsumotoMasumi NakamuraYasunori AsadaNorimasa Shudo
    • Keizo TanikawaTakashi MatsumotoMasumi NakamuraYasunori AsadaNorimasa Shudo
    • A61K31/415A61K31/44A61K31/4427A61K31/445A61K31/47A61K31/495A61P7/02A61P9/08A61P9/10C07D231/12C07D231/14C07D231/20C07D231/22C07D401/04C07D401/06C07D401/14C07D403/04C07D403/06
    • C07D231/12C07D231/14C07D231/20C07D231/22C07D401/04C07D401/06C07D401/14C07D403/04
    • A pyrazolone derivative represented by general formula (I) or a salt thereof: ##STR1## [wherein one of X.sup.1 and X.sup.2 is ##STR2## (wherein A is a cyano group, a cyano C.sub.1-4 alkyl group, an amino group, an amino C.sub.1-4 alkyl group, an amidino group or a guanidino group, R.sup.1 and R.sup.2 are independently hydrogen atoms, halogen atoms, C.sub.1-6 alkyl groups or the like) or the like],the other of X.sup.1 and X.sup.2 is a C.sub.1-6 alkyl group, a C.sub.3-6 alkenyl group, an aryl C.sub.1-4 alkyl group or an aryl group,one of Y.sup.1 and Y.sup.2 is ##STR3## (wherein Q is an oxygen atom or a sulfur atom, Z.sup.1 is an oxygen atom, a --NR.sup.7 -- group or a --CHR.sup.7 -- group, Z.sup.2 is a cyclic C.sub.3-7 alkylene group, a C.sub.1-3 alkylene group, a --CH.sub.2 CO-- group or --CH.sub.2 CH.sub.2 CO-- group, Z.sup.3 is an oxygen atom, a sulfur atom, a sulfinyl group, a sulfonyl group or the like, Z.sup.4 is a C.sub.1-3 alkylene group, and Z.sup.5 is a carboxyl group or the like, andthe other of Y.sup.1 and Y.sup.2 is a D-E- group [wherein E is a bond, a C.sub.1-4 alkylene group or a phenylene group, and D is a hydrogen atom, a C.sub.1-6 alkyl group or the like which has an inhibitory action on platelet aggregation and is useful as a preventive or therapeutic agent for various thrombotic diseases.
    • PCT No.PCT / JP96 / 02944 Sec。 371日期:1998年4月13日 102(e)1998年4月13日PCT PCT 1996年10月11日PCT公布。 第WO97 / 13757号公报 日本1997年4月17日由通式(I)表示的吡唑啉酮衍生物或其盐:其中X1和X2之一为(其中A为氰基,氰基C1-4烷基,氨基,氨基 C 1-4烷基,脒基或胍基,R 1和R 2独立地为氢原子,卤素原子,C 1-6烷基等),X 1和X 2中的另一个为C 1-6 烷基,C 3-6烯基,芳基C 1-4烷基或芳基,Y1和Y2之一为(其中Q为氧原子或硫原子,Z1为氧原子,-NR7- 基团或-CHR7-基团,Z2为环状C3-7亚烷基,C1-3亚烷基,-CH2CO-基或-CH2CH2CO-基,Z3为氧原子,硫原子,亚磺酰基, 磺酰基等,Z4为C1-3亚烷基,Z5为羧基等,Y1和Y2中的另一个为DE-基[其中E为键,C1-4亚烷基 基团或亚苯基,D为氢原子,C1-6烷基 对血小板聚集具有抑制作用,可用作各种血栓性疾病的预防或治疗剂。