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alkylamino - ethynyl - alanine - aminodiolverbindungen with imidazolyl / benzimidazolyl - endgruppe for treatment of hypertension

机译:烷基氨基-乙炔基-丙氨酸-氨基二醇杂多酚联用咪唑基/苯并咪唑基-恩妥普酯治疗高血压

摘要

Compounds characterized generally as imidazolyl/benzimidazolyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I wherein A is selected from CO and SO2; wherein X is selected from oxygen atom and methylene; wherein B is selected from imidazolyl and benzimidazolyl groups; wherein R1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R2 is phenylmethyl; wherein each of R3 and R5 is hydrido; wherein R4 is selected from wherein V is selected from hydrido and methyl; wherein R6 is cyclohexylmethyl; wherein R7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.
机译:通常以咪唑基/苯并咪唑基末端的烷基氨基乙炔基丙氨酸氨基二醇衍生物为特征的化合物可用作肾素抑制剂治疗高血压。特别感兴趣的化合物是式I的那些,其中A选自CO和SO 2;其中X选自氧原子和亚甲基;其中B选自咪唑基和苯并咪唑基。其中R1选自氢,甲基,乙基,异丙基和正丙基;其中R2是苯甲基;其中R3和R5各自为氢;其中R4选自其中V选自氢和甲基;其中R6为环己基甲基;其中R7选自异丁基,环丙基和环丙基甲基;其中q是选自0至3之间的数字,包括0和3。其中n是选自0至3之间的数字,包括0和3。或其药学上可接受的盐。

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