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155 条记录 (耗时 0.018 秒)

    5-substituted amino-4-hydroxy-pentenoic acid derivatives and their use
    28.
    发明授权
    5-substituted amino-4-hydroxy-pentenoic acid derivatives and their use 失效

    公开(公告)号：US4927565A

    公开(公告)日：1990-05-22

    申请号：US133642

    申请日：1987-12-16

    申请人： Seiichi Tanaka ,  Yutaka Koike ,  Masato Nakano ,  Shugo Atsuumi ,  Hajime Morishima ,  Kenji Matsuyama

    发明人： Seiichi Tanaka ,  Yutaka Koike ,  Masato Nakano ,  Shugo Atsuumi ,  Hajime Morishima ,  Kenji Matsuyama

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K5/062 ,  C07K5/065

    CPC分类号： C07K5/06026 ,  C07K5/0207 ,  C07K5/06078 ,  A61K38/00 ,  Y10S530/86

    摘要： A 5-substituted amino-4-hydroxy-pentenoic acid or its salt represented by the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 which may be the same or different is a hydrogen atom, a lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, an aryloxycarbonyl group, an aralkyloxycarbonyl group or a lower alkanoyl group which may be substituted by from one to three substituents selected from the group consisting of an amino group, a hydroxyl group, a carboxyl group, an aryloxy group, an aralkyloxycarbonylamino group, a lower alkoxycarbonylamino group and a ##STR2## group (wherein each of X.sup.1 and X.sup.2 which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, or X.sup.1 and X.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom) and which may further contain a double bond in its carbon chain, each of R.sup.3, R.sup.4 and R.sup.6 which may be the same or different is a hydrogen atom, a lower alkyl group, a cycloalkyl group, a cycloalkylalkyl group, an aryl group, an aralkyl group or a residue of an acidic neutral or basic amino acid, R.sup.5 is a hydrogen atom or a lower alkyl group, R.sup.7 is a hydrogen atom, a lower alkyl, cycloalkyl, cycloalkylalkyl or aralkyl group which may be substituted by one or two hydroxyl groups or a residue of an acidic, neutral or basic amino acid, R.sup.8 is a hydroxymethyl group or a --CO--R.sup.9 group (wherein R.sup.9 is a hydroxyl group, a --OY group (wherein Y is a lower alkyl group, an aryl group, an aralkyl group, a lower alkoxyalkyl group, a lower alkanoyloxyalkyl group, a lower alkoxycarbonyloxyalkyl group, or a 1-phthalidyl group) or ##STR3## group (wherein each of Y.sup.1 and Y.sup.2 which may be the same or different is a hydrogen atom, a lower alkyl group, an aryl group, an aralkyl group or a cycloalkyl group, or Y.sup.1 and Y.sup.2 form together with the adjacent nitrogen atom a 5- or 6-membered heterocyclic group which may further contain a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), and each of n and m which may be the same or different is 0 or 1.

    Novel renin inhibiting polypeptide analogs containing S-aryl-D- or L- or DL-cysteinyl, 3-(arylthio)lactic acid or 3-(arylthio)alkyl moieties
    29.
    发明授权
    Novel renin inhibiting polypeptide analogs containing S-aryl-D- or L- or DL-cysteinyl, 3-(arylthio)lactic acid or 3-(arylthio)alkyl moieties 失效
    含有S-芳基-D-或L-或DL-半胱氨酰，3-（芳硫基）乳酸或3-（芳硫基）烷基部分的新型肾素抑制多肽类似物

    公开(公告)号：US4894437A

    公开(公告)日：1990-01-16

    申请号：US85674

    申请日：1987-06-29

    申请人： Ruth E. TenBrink

    发明人： Ruth E. TenBrink

    IPC分类号： C07D233/54 ,  C07K5/02

    CPC分类号： C07D233/64 ,  C07K5/0227 ,  Y10S530/80 ,  Y10S530/86

    摘要： The present invention provides novel renin-inhibiting peptides of the formula X-A.sub.6 -B.sub.5 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 -G.sub.12 -H.sub.13 -I.sub.14 -Z, wherein X and Z are terminal groups, C.sub.8 contains S-aryl-D- or L- or DL-cysteinyl, 3-(arylthio)lactic acid, and 3-(arylthio)alkyl moieties, and the remaining variables are amino acid residues. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.

    摘要翻译： PCT No.PCT / US86 / 02227 Sec。 371日期1987年6月29日第 102（e）日期1987年6月29日PCT提交1986年10月21日PCT公布。 出版物WO87 / 02986 日期：1987年5月21日本发明提供了式X-A6-B5-C8-D9-E10-F11-G12-H13-I14-Z的新型肾素抑制肽，其中X和Z是末端基， S-芳基-D-或L-或DL-半胱氨酰，3-（芳硫基）乳酸和3-（芳硫基）烷基部分，其余变量是氨基酸残基。 这种抑制剂可用于诊断和控制肾素依赖性高血压。