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    Hydrophobic pseudo-peptides
    1.
    发明授权
    Hydrophobic pseudo-peptides 失效
    疏水假肽

    公开(公告)号：US5047399A

    公开(公告)日：1991-09-10

    申请号：US218402

    申请日：1988-07-13

    申请人： Laura S. Lehman ,  Michael F. Czarniecki

    发明人： Laura S. Lehman ,  Michael F. Czarniecki

    IPC分类号： C07K5/02 ,  C07K5/083

    CPC分类号： C07K5/0804 ,  C07K5/0207

    摘要： Novel hydrophobic psuedo-peptides of formula I ##STR1## wherein R.sub.1 is lower alkyl or -CH.sub.2 CONR.sub.6 R.sub.7 ; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently lower alkyl, cycloalkyl lower alkyl, aryl lower alkyl, heteroaryl lower alkyl, aryl lower alkoxy, substituted aryl lower alkyl, wherein the aryl portion is substituted with 1-3 substituents independently selected from lowr alkyl, hydroxyl, lower alkoxy and halogeno, substituted heteroaryl lower alkyl wherein the substituents on the heteroaryl portion are as defined for aryl lower alkyl, substituted cycloalkyl lower alkyl, wherein the substituents on the cycloalkyl portion are as defined for aryl lower alkyl, and substituted aryl lower alkoxy wherein the substituents are as defined for aryl lower alkyl;R.sub.6 and R.sub.7 are independently hydrogen or lower alkyl;X.sub.1, X.sub.2, X.sub.3, X.sub.4 and X.sub.5 are independently ##STR2## cis or trans --CR.sub.8 .dbd.CR.sub.9 --, --CHR.sub.8 CHR.sub.9 --, --CH.sub.2 NR.sub.8 --, ##STR3## provided that when R.sup.4 is methyl, X.sub.4 is not --CONH--; R.sub.8 and R.sub.9 are independently hydrogen or lower alkyl;the pharmaceutically acceptable salts thereof,a nd pharmaceutical compositions thereof, useful in the treatment of hypertension are disclosed.

    摘要翻译： 式I的新型疏水性伪肽其中R 1是低级烷基或-CH 2 CONR 6 R 7; R2，R3，R4和R5独立地为低级烷基，环烷基低级烷基，芳基低级烷基，杂芳基低级烷基，芳基低级烷氧基，取代芳基低级烷基，其中芳基部分被1-3个独立地选自低级烷基， 羟基，低级烷氧基和卤素取代的杂芳基低级烷基，其中杂芳基部分上的取代基如芳基低级烷基取代的环烷基低级烷基所定义，其中环烷基部分上的取代基如芳基低级烷基所定义，取代的芳基低级 烷氧基，其中取代基如芳基低级烷基所定义; R6和R7独立地是氢或低级烷基; X1，X2，X3，X4和X5独立地为顺式或反式-CR8 = CR9-，-CHR8CHR9-，-CH2NR8-，，条件是当R4为甲基时，X4不为-CONH-; R8和R9独立地是氢或低级烷基; 公开了其可用于治疗高血压的药学上可接受的盐及其药物组合物。