Substituted dipeptide amides.

摘要

The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: <CHEM> and the pharmaceutically acceptable acid addition salts thereof wherein R<1> is hydrogen, lower alkyl, hydroxy, lower alkoxy, -O(CH2)nphenyl with the phenyl optionally substituted by halogen, -NO2, -CN, -NH2 or lower alkyl wherein n is 1 to 4; R<2> and R<3> represent lower alkyl, halogen, or lower alkoxy, or either one of R<2> or R<3> is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R<4>, R<5>, R<6>, and R<9> may be the same or different and represent hydrogen, lower alkyl, cycloalkyl having 3 to 8 carbons, unsaturated lower alkyl, or -(CH2)mcycloalkyl with the cycloalkyl having 3 to 8 carbons and m is 1 to 4; R10 is hydrogen or -(CH2)pphenyl or with the phenyl optionally substituted with -NH2, -OH, halogen, -NO2, or lower alkyl or -(CH2)p thienyl wherein p is 1 to 4; one of R<7> or R<8> is -(CH2)f-S(O)z-(CH2)q-CH3 where f is 1 to 3 and q is 0 to 3, z is 0, 1 or 2 and the other is hydrogen or lower alkyl, or R<7> and R<8> together with carbon w is <CHEM> where x and y are independently 1 to 3 and z is 0, or 2. V represents an asymmetric carbon that may be recemic or have the D or L configuration; W represents an asymmetric carbon when R<7> and R<8> are not the same that may be recemic or have the D or L configuration. The compounds of this invention are useful as analgesic and/or antihypertensive agents.