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    Linear free-sulfhydryl-containing oligopeptide derivatives as antihypertensive agents
    1.
    发明授权
    Linear free-sulfhydryl-containing oligopeptide derivatives as antihypertensive agents 失效
    含有线性游离巯基的寡肽衍生物作为抗高血压药

    公开(公告)号：US5106834A

    公开(公告)日：1992-04-21

    申请号：US290667

    申请日：1988-12-27

    申请人： Philippe R. Bovy ,  Robert E. Manning ,  Joan M. O'Neal

    发明人： Philippe R. Bovy ,  Robert E. Manning ,  Joan M. O'Neal

    IPC分类号： A61K38/00 ,  C07K14/58

    CPC分类号： C07K14/582 ,  A61K38/00

    摘要： Synthesis and use of novel oligopeptides are described, many of which peptides contain one or several unnatural amino acids. These short linear peptide derivatives are characterized by the presence of a free sulfhydryl function. These compounds have a high affinity for the Atrial Natriuretic Peptide (ANP) receptor coupled to particulate guanylate cyclase. Such peptides are full agonists at the ANP receptor as demonstrated by the ability of the peptides to stimulate the production of cGMP and to relax smooth muscles in vitro. In accord with these observations, the compounds of the invention lower blood pressure in mammals. Preferred peptides are the following:Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; D-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; L-Pen-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH.sub.2 ; and Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-IleNH.sub.2.

    摘要翻译： 描述了新型寡肽的合成和应用，其中许多肽含有一个或多个非天然氨基酸。 这些短的线性肽衍生物的特征在于存在游离的巯基官能团。 这些化合物对与鸟苷酸环化酶颗粒偶联的心房利钠肽（ANP）受体具有高亲和力。 这些肽是ANP受体的完全激动剂，如通过肽在体外刺激cGMP的产生和放松平滑肌的能力所证明的。 根据这些观察结果，本发明化合物降低了哺乳动物的血压。 优选的肽如下：Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; D-Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; L-Pen-Cha-Gly-Gly-Arg-Ile-Asp-Arg-Ile-GlyNH 2; 和Cys-Cha-Gly-Gly-Arg-Ile-Asp-Arg-IleNH 2。

    Cycloheptimidazolone compounds as angiotensin II antagonists for control of hypertension
    3.
    发明授权
    Cycloheptimidazolone compounds as angiotensin II antagonists for control of hypertension 失效
    环庚咪唑酮化合物作为血管紧张素II拮抗剂用于控制高血压

    公开(公告)号：US5281615A

    公开(公告)日：1994-01-25

    申请号：US840471

    申请日：1992-02-24

    申请人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

    发明人： Philippe R. Bovy ,  Joan M. O'Neal ,  Timothy S. Chamberlain ,  Joe T. Collins

    IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/675 ,  A61P9/00 ,  A61P9/04 ,  A61P9/12 ,  A61P43/00 ,  C07D235/02 ,  C07D403/10 ,  C07F9/6558 ,  C07D257/04

    CPC分类号： C07D235/02 ,  C07D403/10

    摘要： A class of cycloheptimidazolone compounds is described as angiotensin II antagonists for use in control of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, alkyl, halo, alkanoyl, carboxyl, alkoxycarbonyl, phenyl, haloalkyl, alkoxyalkyl, formyl, cyano, alkoxy, phenoxy, phenylthio, alkylthio; wherein R.sup.3 is alkyl, alkenyl, alkynyl, hydroxyalkyl and alkoxyalkyl; wherein each of R.sup.5 through R.sup.13 is independently selected from hydrido, alkyl, haloalkyl, halo, nitro, cyano, hydroxy, alkoxy, alkylthio, aryl, aryloxy, arythio, and acidic groups such as carboxylic acid, with the proviso that at least one of R.sup.9 through R.sup.13 substituents is an acidic group; or a pharmaceutically-acceptable ester, amide or salt thereof.

    摘要翻译： 一类环庚咪唑酮化合物被描述为用于控制高血压的血管紧张素II拮抗剂。 特别感兴趣的化合物是式（*化学结构*）的化合物，其中R 1和R 2各自独立地选自氢，烷基，卤素，烷酰基，羧基，烷氧基羰基，苯基，卤代烷基，烷氧基烷基，甲酰基，氰基，烷氧基，苯氧基 ，苯硫基，烷硫基; 其中R3是烷基，烯基，炔基，羟基烷基和烷氧基烷基; 其中R 5至R 13中的每一个独立地选自氢，烷基，卤代烷基，卤素，硝基，氰基，羟基，烷氧基，烷硫基，芳基，芳氧基，仲氨基和酸性基团如羧酸，条件是至少一个 R9至R13取代基是酸性基团; 或其药学上可接受的酯，酰胺或其盐。