| 摘要 |
The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: <IMAGE> and the pharmaceutically acceptable acid addition salts thereof wherein R1 is hydrogen, lower alkyl, hydroxy, -OCO2 lower alkyl, lower alkoxy, -O(CH2)n-phenyl with the phenyl optionally substituted by halogen, -NO2, -CN, -NH2 or lower alkyl wherein n is 1 to 4; R2 and R3 represent lower alkyl, halogen, or lower alkoxy, or either one of R2 or R3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R4, R5, R6, R7, R8, and R9 may be the same or different and represent hydrogen or lower alkyl; R10 is selected from the group consisting of -(ALK)X where ALK represents alkylene, thioalkylene, oxyalkylene, having 1 to 5 carbon atoms; alkenylene and alkynylene having 2 to 4 carbon atoms; and X represents pyridyl, pyrimidinyl, 9H-fluoren-9-yl, diphenylmethyl, thienyl, carboxy, lower alkoxy carbonyl, substituted phenyl wherein the phenyl substituent is amino, hydroxy, halogen, nitro, methylenedioxy, lower alkyl, carboxy, lower alkoxycarbonyl, lower alkoxy, carboxamide, diloweralkylamino or X represents phenyl when ALK is not alkylene; or R10 is <IMAGE> where p and q are independently 1 to 4; or R9 and R10 together with N is <IMAGE> where r and t are independently 1 to 4; v represents an asymmetric carbon that may be racemic or have the D or L configuration; w represents an asymmetric carbon when R7 and R8 are not the same that may be racemic or have the D or L configuration. These compounds are useful as analgesic and/or antihypertensive compounds.
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