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    • 1. 发明授权
    • Pyridazinone derivatives
    • 哒嗪酮衍生物
    • US5750523A
    • 1998-05-12
    • US676227
    • 1996-07-23
    • Keizo TanikawaTakashi MatsumotoHiroo MatsumotoNobutomo TsuruzoeHitoshi Nakabeppu
    • Keizo TanikawaTakashi MatsumotoHiroo MatsumotoNobutomo TsuruzoeHitoshi Nakabeppu
    • C07D237/22C07D401/12A61K31/50
    • C07D401/12C07D237/22
    • Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## �wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!. These compounds have strong antiplatelet effects, are excellently safe, and can be used as active ingredients of prophylactic and therapeutic drugs for various thrombotic diseases.
    • PCT No.PCT / JP95 / 00069 Sec。 371日期:1996年7月23日 102(e)日期1996年7月23日PCT提交1995年1月24日PCT公布。 WO95 / 19969 PCT公开 日期:1997年7月27日由式(I)表示的哒嗪酮衍生物和含有它们的抗血小板剂:其中R是氢原子或C1-C4烷基,X是氢原子,氯原子 或溴原子,Ar是吡啶基或被OR 1取代的苯基(其中R1是氢原子或C1-C4烷基)和A {其中A是氢原子,卤原子,C1-C4 烷基或OR 2(其中R 2是氢原子或C 1 -C 4烷基)}是其中一个碳原子被一个OR 1基团取代的C 1 -C 8亚烷基(其中R 1与上述定义相同) ,Z 1和Z 2独立地为氢原子,卤素原子,C 1 -C 4烷基或OR 1基(其中R 1与上述定义相同)]。 这些化合物具有很强的抗血小板作用,非常安全,可用作各种血栓性疾病的预防和治疗药物的活性成分。
    • 2. 发明授权
    • Pyridazinone derivatives
    • 哒嗪酮衍生物
    • US5856327A
    • 1999-01-05
    • US936600
    • 1997-09-24
    • Keizo TanikawaTakashi MatsumotoHiroo MatsumotoNobutomo TsuruzoeHitoshi Nakabeppu
    • Keizo TanikawaTakashi MatsumotoHiroo MatsumotoNobutomo TsuruzoeHitoshi Nakabeppu
    • C07D237/22C07D401/12A61K31/50
    • C07D401/12C07D237/22
    • Pyridazinone derivatives represented by the formula (I) and antiplatelet agents containing them: ##STR1## �wherein R is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, X is a hydrogen atom, a chlorine atom or a bromine atom, Ar is a pyridyl group or a phenyl group substituted with OR.sup.1 (wherein R.sup.1 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and A {wherein A is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or OR.sup.2 (wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group)}, Y is C.sub.1 -C.sub.8 alkylene wherein one carbon atom on the straight chain is substituted with one OR.sup.1 group (wherein R.sup.1 is the same as defined above), and Z.sup.1 and Z.sup.2 are independently a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.4 alkyl group or a OR.sup.1 group (wherein R.sup.1 is the same as defined above)!. These compounds have strong antiplatelet effects, are excellently safe, and can be used as active ingredients of prophylactic and therapeutic drugs for various thrombotic diseases.
    • 由式(I)表示的哒嗪酮衍生物和含有它们的抗血小板剂:其中R是氢原子或C1-C4烷基,X是氢原子,氯原子或溴原子, Ar是吡啶基或被OR 1取代的苯基(其中R1是氢原子或C1-C4烷基)和A {其中A是氢原子,卤素原子,C1-C4烷基或OR2( 其中R 2是氢原子或C 1 -C 4烷基),Y是直链上的一个碳原子被一个OR 1基团取代的C 1 -C 8亚烷基(其中R 1与上述相同),Z 1和 Z2独立地为氢原子,卤素原子,C1-C4烷基或OR1基团(其中R1与上述定义相同)]。 这些化合物具有很强的抗血小板作用,非常安全,可用作各种血栓性疾病的预防和治疗药物的活性成分。
    • 6. 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。