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    • 1. 发明授权
    • Benzothiazepine derivatives and their methods of preparation
    • 苯并硫氮杂衍生物及其制备方法
    • US4539150A
    • 1985-09-03
    • US625656
    • 1984-06-28
    • Tsutomu KatakamiNobuyuki FukazawaHajime IizukaTakashi NishinaIsao Shirakawa
    • Tsutomu KatakamiNobuyuki FukazawaHajime IizukaTakashi NishinaIsao Shirakawa
    • C07D281/10C07D281/02
    • C07D281/10
    • This invention relates to benzothiazepine derivatives of the general formula ##STR1## where K is hydrogen or a --CH.sub.2 COOR.sub.2 group where R.sub.2 is hydrogen or a lower alkyl group, Z is hydrogen or phenyl except when both K and Z are hydrogen, and Y is hydrogen, a --CHR.sub.3 --COOR.sub.1 group, an alkanoyl group or a --COO(CH.sub.2).sub.n R.sub.4 group where R.sub.1 is hydrogen or a lower alkyl group, R.sub.3 is hydrogen, an alkyl group, an alkylphenyl group or an aryl-lower alkyl group, R.sub.4 is an aryl group and n is a whole number of 1 to 10, and to their methods of preparation.The benzothiazepine derivatives of this invention, including their salts, have a powerful inhibitory effect on the angiotensin converting enzyme and exert a marked depressor effect in such models of hypertension as spontaneously occurring hypertensive rats and the like, so that they are useful as drugs for the treatment of hypertension and other cardiovascular diseases. In addition, these compounds are also useful as intermediates for the synthesis of coronary dilators, psychotropic drugs and the like.
    • 本发明涉及通式为(I)的苯并硫氮杂衍生物,其中K是氢或-CH 2 COOR 2基团,其中R 2是氢或低级烷基,Z是氢或苯基,除了当K和Z都是氢时, Y是氢,-CHR 3 -COOR 1基团,烷酰基或-COO(CH 2)n R 4基团,其中R 1是氢或低级烷基,R 3是氢,烷基,烷基苯基或芳基 - 低级烷基 基团,R 4为芳基,n为1〜10的整数,及其制备方法。 包括其盐在内的本发明的苯并硫氮杂衍生物对血管紧张素转化酶具有强大的抑制作用,并且在自发发生的高血压大鼠等高血压模型中发挥明显的抑制作用,因此它们可用作药物 治疗高血压等心血管疾病。 此外,这些化合物也可用作合成冠状动脉扩张剂,精神药物等的中间体。