Bradykinin antagonist pseudopeptide derivatives of substituted
4-keto-1,3,8-triazaspiro[4.5]decan-3-alkanoic acids
    61.
    发明授权
    Bradykinin antagonist pseudopeptide derivatives of substituted 4-keto-1,3,8-triazaspiro[4.5]decan-3-alkanoic acids 失效
    取代的4-酮基-1,3,8-三氮杂螺[4.5]癸烷-3-链烷酸的缓激肽拮抗剂假肽衍生物

    公开(公告)号:US5610142A

    公开(公告)日:1997-03-11

    申请号:US416524

    申请日:1995-04-03

    CPC classification number: C07K7/18 A61K38/00

    Abstract: Novel compounds with as few as three natural amino acids that incorporate a substituted 4-keto-1,3,8-triazaspiro[4.5]decan-3-alkanoyl bridge in place of selected fragments of peptidic bradykinin receptor antagonists are pseudopeptides with potent bradykinin receptor antagonist actions. These pseudopeptides and their pharmaceutical compositions are of benefit in treating conditions and diseases of mammals, including humans, in which an excess of bradykinin or a related kinin is produced endogenously or is received exogenously, for example via insect bite.

    Abstract translation: 具有少至三个天然氨基酸的新型化合物,其掺入取代的4-酮基-1,3,8-三氮杂螺[4.5]癸烷-3-烷酰基桥代替肽缓激肽受体拮抗剂的选定片段是具有有效的缓激肽受体的假肽 拮抗作用。 这些假肽及其药物组合物在治疗哺乳动物(包括人)的条件和疾病方面是有益的,其中过量的缓激肽或相关的激肽是内源产生的或外源性地接受,例如通过昆虫咬。

    Bradykinin antagonist pseudopeptide derivatives of olefinic
aminoalkanoic acids
    62.
    发明授权
    Bradykinin antagonist pseudopeptide derivatives of olefinic aminoalkanoic acids 失效
    烯酰氨基链烷酸的缓激肽拮抗剂假肽衍生物

    公开(公告)号:US5541286A

    公开(公告)日:1996-07-30

    申请号:US281907

    申请日:1994-07-28

    Applicant: Donald J. Kyle

    Inventor: Donald J. Kyle

    CPC classification number: C07K7/18 A61K38/00

    Abstract: Pseudopeptide compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acids at at positions 2 through 5 are replaced by olefinic aminoalkenoyl groups to reduce the peptide nature of the compounds.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.

    Abstract translation: 基于修饰的缓激肽序列的假肽化合物是有效的缓激肽受体拮抗剂。 位置2至5处的氨基酸被烯属的氨基烯酰基代替,以降低化合物的肽性质。 所产生的类似物可用于治疗其中产生或注射过量的缓激肽或相关激肽的哺乳动物和人的病症和疾病,例如通过昆虫叮咬。

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