会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 9. 发明授权
    • Purine derivatives and their use as anti-coagulants
    • 嘌呤衍生物及其作为抗凝剂的用途
    • US5753635A
    • 1998-05-19
    • US689979
    • 1996-08-16
    • Brad O. BuckmanRaju MohanMichael M. Morrissey
    • Brad O. BuckmanRaju MohanMichael M. Morrissey
    • C07D487/04A61K31/52A61P7/02A61P43/00C07D473/00C07D473/02C07D473/04C07D473/16C07D473/18C07D473/30C07D473/22
    • C07D473/00C07D473/04
    • This invention is directed to purine derivatives of the following formulae: ##STR1## wherein Z.sup.1 is --O--, --N(R.sup.10)-- or --CH.sub.2 O--; Z.sup.2 is --O--, --N(R.sup.10)-- or --OCH.sub.2 --; R.sup.1 and R.sup.4 are each independently hydrogen, halo, alkyl, --OR.sup.10, --C(O)OR.sup.10, --C(O)N(R.sup.10)R.sup.11, --N(R.sup.10)R.sup.11, --N(R.sup.10)C(O)R.sup.10, or --N(H)S(O).sub.2 R.sup.13 ; R.sup.2 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.10, --C(NH)N(H)C(O)OR.sup.13, --C(NH)N(H)C(O)R.sup.10, --C(NH)N(H)S(O).sub.2 R.sup.13, or --C(NH)N(H)C(O)N(H)R.sup.10 ; R.sup.3 is halo, alkyl, haloalkyl, haloalkoxy, ureido, cyano, guanidino, --OR.sup.10, --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.10, --C(O)N(R.sup.10)R.sup.11, --R.sup.12 --C(O)N(R.sup.10)R.sup.11, --CH(OH)C(O)N(R.sup.10)R.sup.11, --N(R.sup.10)R.sup.11, --R.sup.12 --N(R.sup.10)R.sup.11, --C(O)OR.sup.10, --R.sup.12 --C(O)OR.sup.10, --N(R.sup.10)C(O)R.sup.10, (1,2)-tetrahydropyrimidinyl (optionally substituted by alkyl), (1,2)-imidazolyl (optionally substituted by alkyl), or (1,2)-imidazolinyl (optionally substituted by alkyl); R.sup.5 is hydrogen, halo, alkyl, cycloalkyl, haloakyl, aryl, aralkyl, alkylthio, hydroxy, mercapto, alkoxy, or --N(R.sup.10)R.sup.11 ; and R.sup.6 is defined herein. These compounds are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
    • 本发明涉及以下分子式的嘌呤衍生物:其中Z 1为-O - , - N(R 10) - 或(III)的化合物 -CH 2 O- Z2是-O - , - N(R10) - 或-OCH2-; R 1和R 4各自独立地为氢,卤素,烷基,-OR 10,-C(O)OR 10,-C(O)N(R 10)R 11,-N(R 10)R 11,-N(R 10) ,或-N(H)S(O)2 R 13; R 2是-C(NH)NH 2,-C(NH)N(H)OR 10,-C(NH)N(H)C(O)OR 13,-C(NH)N(H)C(O) -C(NH)N(H)S(O)2 R 13或-C(NH)N(H)C(O)N(H) R 3是卤素,烷基,卤代烷基,卤代烷氧基,脲基,氰基,胍基,-OR 10,-C(NH)NH 2,-C(NH)N(H)OR 10,-C(O)N(R 10)R 11,-R 12 -C(O)N(R10)R11,-CH(OH)C(O)N(R10)R11,-N(R10)R11,-R12-N(R10)R11,-C(O)OR10, R 12 -C(O)OR 10,-N(R 10)C(O)R 10,(1,2) - 四氢嘧啶基(任选被烷基取代),(1,2) - 咪唑基(任选被烷基取代) ,2) - 咪唑啉基(任选被烷基取代); R5是氢,卤素,烷基,环烷基,卤代烷基,芳基,芳烷基,烷硫基,羟基,巯基,烷氧基或-N(R10)R11; 并且R6在本文中定义。 这些化合物可用作抗凝剂。 本发明还涉及含有本发明化合物的药物组合物,以及使用该化合物治疗以血栓形成活性为特征的疾病状态的方法。