| 摘要 |
Novel diamino acid derivative dual inhibitors of neutral endopeptidase and angiotensin converting enzyme of the formula (* CHEMICAL STRUCTURE *) wherein: Z is amino, lower alkylamino, di-(lower alkyl)amino R9C(O)NH- or an optionally substituted guanidino group; R1 is hydrogen or R7R8N-; R2 is hydrogen, lower alkyl, cyclolower alkyl, aryllower alkyl or heteroaryllower alkyl; and R3 is hydrogen, lower alkyl or cyclolower alkyl; or R2 and R3, together with the carbon to which they are attached, comprise a 3-7 membered carboxyclic ring; R4 is hydrogen, lower alkyl, aryl lower alkyl or heteroaryllower alkyl; R5 and R6 are independently hydroxy, lower alkoxy, amino, aryllower alkoxy, lower alkylamino and di-(lower alkyl)amino; R7 is R9C(O)- or R10SO2-; and R8 is hydrogen, lower alkyl, aryllower alkyl or aryl; or R7 and R8, together with the nitrogen to which they are attached, comprise a 5-7 membered ring; R9 is lower alkyl, aryllower alkyl, aryl, heteroaryllower alkyl, heteroaryl, lower alkoxy, aryllower alkoxy, amino, alkylamino or dialkylamino; R10 is lower alkyl, aryl lower alkyl, aryl, heteroaryl lower alkyl, amino, lower alkylamino, di-(lower alkyl)amino or heteroaryl; n is 1, 2, 3, 4 or 5; and m is 1, 2, 3, 4 or 5; or a pharmaceutically acceptable addition salt thereof, useful in the treatment of cardiovascular disorders, are disclosed.
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