首页> 外国专利> Propargyl-terminated cycloalkylalkyl-P2-site substituted aryl/alkylsulfonyl-terminated alanine amino-diol compounds for treatment of hypertension

Propargyl-terminated cycloalkylalkyl-P2-site substituted aryl/alkylsulfonyl-terminated alanine amino-diol compounds for treatment of hypertension

机译:用于治疗高血压的炔丙基末端的环烷基烷基-P2-位取代的芳基/烷基磺酰基末端的丙氨酸氨基-二醇化合物

摘要

Compounds characterized generally as being propargyl- terminated aryl/alkylsulfonyl-terminated amino diol derivatives having a cycloalkylalkyl group at the P2 substitution site are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein R.sup.1 is selected from isopropyl, isobutyl, sec-butyl, tert-butyl, phenyl, fluorophenyl, chlorophenyl, benzyl, fluorobenzyl, chlorobenzyl, naphthyl, fluoronaphthyl, chloronaphthyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; and wherein R. sup.8 is propargyl or a propargyl-containing moiety.
机译:通常特征为在P2取代位点具有环烷基烷基的炔丙基-末端的芳基/烷基磺酰基-末端的氨基二醇衍生物的化合物可用作治疗高血压的肾素抑制剂。特别感兴趣的化合物是式## STR1的化合物,其中R 1选自异丙基,异丁基,仲丁基,叔丁基,苯基,氟苯基,氯苯基,苄基,氟苄基,氯苄基,萘基,氟萘基,氯萘基,氟萘甲基和氯萘甲基;其中R 2选自氢,甲基,乙基和苯基;其中R 3选自氢,环己基甲基,苄基,氟苄基,氯苄基,氟萘甲基和氯萘甲基;其中R 5选自含3至约12个碳原子的环烷基烷基;其中R 7是环己基甲基;并且其中R.sup.8是炔丙基或含炔丙基的部分。

著录项

  • 公开/公告号US5268391A

    专利类型

  • 公开/公告日1993-12-07

    原文格式PDF

  • 申请/专利权人 C. D. SEARLE & CO.;

    申请/专利号US19920916557

  • 申请日1992-07-20

  • 分类号A61K31/16;C07C323/25;

  • 国家 US

  • 入库时间 2022-08-22 04:32:34

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