Aminoacyl derivatives
    1.
    发明授权
    Aminoacyl derivatives 失效
    氨基酰基衍生物

    公开(公告)号:US4421744A

    公开(公告)日:1983-12-20

    申请号:US379614

    申请日:1982-05-18

    申请人: James J. Gormley

    发明人: James J. Gormley

    摘要: Peptide and pseudopeptide derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 stand for defined hydrocarbyl or halo-hydrocarbyl substituents, for example alk-2-enyl radicals; .dbd.N--A-- stands for a defined amino acid residue; B, D and E, which may be the same or different, stand for a valency bond or a defined amino acid residue; F stands for a defined amino acid residue; X stands for a carboxy, ester or amide group; and the linkages between the amino acid residues are peptide linkages or at least one of said linkages is a defined pseudo linkage; and pharmaceutically-acceptable salts thereof. Processes for the manufacture of the compounds. Pharmaceutical compositions comprising one of the compounds and a pharmaceutical diluent or carrier. The compounds are antagonists at the opiate receptors, and most of them are selective .delta.-receptor antagonists.

    摘要翻译: 下式的肽和假肽衍生物:其中R 1和R 2代表定义的烃基或卤代烃基取代基,例如烷-2-烯基; = N-A-代表定义的氨基酸残基; B,D和E可以相同或不同,代表价键或限定的氨基酸残基; F代表定义的氨基酸残基; X代表羧基,酯或酰胺基; 氨基酸残基之间的连接是肽键,或至少一个所述键是定义的假键; 及其药学上可接受的盐。 用于制造化合物的方法。 包含化合物之一和药物稀释剂或载体的药物组合物。 这些化合物是阿片受体的拮抗剂,其中大多数是选择性的δ-受体拮抗剂。