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Azachromonyl/azachromonylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy amp;bgr;-amino acid derivatives

机译:氮杂色氮基/氮杂色氮烷基-N-末端环烷氧基-C-末端氨基羟基&-氨基酸衍生物

摘要

Non-peptidyl compounds characterized generally as azachromonyl/azachromonylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy &bgr;-amino acid derivatives are useful as renin inhibitors for treatment of hypertension. Compounds of particular interest are of the formula ##STR1## wherein R.sub.1 is selected from ##STR2## wherein each of Y and Z is independently selected from hydrido, chloro, fluoro, methoxy and dimethylamino; wherein n is a number selected from zero through four, inclusive; wherein each of R.sub.2 and R.sub.4 is independently selected from hydrido and methyl; wherein R.sub.3 is methyl or ethyl; wherein R.sub.5 is cyclohexylmethyl; wherein R.sub.6 and R.sub. 7 are taken together to form a partially saturated or fully saturated heterocyclic ring containing five to eight ring members with one or two ring members being oxygen atoms and the remaining ring members being carbon atoms, and which heterocyclic ring may be optionally substituted with lower alkyl; or a pharmaceutically-acceptable salt thereof.
机译:通常表征为氮杂苯甲酰基/氮杂苯甲酰基烷基-N-末端环烷氧基-C-末端氨基羟基和氨基酸衍生物的非肽基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具有式## STR1 ##,其中R.1选自## STR2 ##,其中Y和Z各自独立地选自氢,氯,氟,甲氧基和二甲基氨基;其中n是选自0至4之间的数字。其中R 2和R 4各自独立地选自氢和甲基;其中R 3是甲基或乙基;其中R 5是环己基甲基;其中R.sub.6和R.sub。将7与7结合形成部分饱和或完全饱和的杂环,该杂环包含5至8个环成员,其中一个或两个环成员为氧原子,其余的环成员为碳原子,并且该杂环可任选地被低级烷基取代;或其药学上可接受的盐。

著录项

  • 公开/公告号US5290787A

    专利类型

  • 公开/公告日1994-03-01

    原文格式PDF

  • 申请/专利权人 G. D. SEARLE & CO.;

    申请/专利号US19920914718

  • 发明设计人 GUNNAR J. HANSON;

    申请日1992-07-16

  • 分类号A61K31/35;C07D471/04;

  • 国家 US

  • 入库时间 2022-08-22 04:32:11

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