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    • 65. 发明授权
    • Ethynyl-alanine aryl/alkylsulfonyl-terminated amino-diol compounds for
treatment of hypertension
    • 用于治疗高血压的乙炔基 - 丙氨酸芳基/烷基磺酰基封端的氨基二醇化合物
    • US5314920A
    • 1994-05-24
    • US916447
    • 1992-07-20
    • Barbara B. ChenGunnar J. HansonJohn S. Baran
    • Barbara B. ChenGunnar J. HansonJohn S. Baran
    • C07C317/44A61K31/16
    • C07C317/44C07C2101/02C07C2101/14
    • Compounds characterized generally as ethynyl alanine aryl/alkylsulfonyl-terminated amino diol derivatives 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 propargyl or a propargyl-containing moeity; wherein R.sup.7 is cyclohexylmethyl; and wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl.
    • 通常表示乙炔基丙氨酸芳基/烷基磺酰基封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下式的化合物,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,氟萘基甲基和氯萘基甲基 ; 其中R2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,氟萘基甲基和氯萘基甲基; 其中R5是炔丙基或含炔丙基的摩尔; 其中R 7为环己基甲基; 并且其中R8选自正丙基,异丁基,环丙基,环丙基甲基,烯丙基和乙烯基。