Substituted dipeptide amides 4

Details Substituted dipeptide amides 4 Substituted dipeptide amides 4

C - Chemistry, Metallurgy

07

K

530/5.06

C07K 5/06 (2006.01) C07D 333/20 (2006.01) C07D 333/38 (2006.01) C07D 333/48 (2006.01) C07D 335/02 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1262013

ABSTRACT The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: Image and the pharmaceutically acceptable acid addition salts thereof wherein Rl is hydrogen, lower alkyl, hydroxy, lower alkoxy, -O(CH2)nphenyl with the phenyl optionally substituted by halogen, -N02, -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, and R9 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)phenyl or with the phenyl optionally substituted with -NH2, -OH, halogen, -N02, or lower alkyl or -(CH2)p thienyl wherein p is 1 to 4; one of R7 or R8 is -(CH2)f-S(O)z-(CH2)q-CH3 where f is 1 to 3 and q is O to 3, z is O, 1 or 2 and the other is hydrogen or lower alkyl, or R7 and R8 together with carbon w is Image where x and y are independently 1 to 3 and z is O, or 2. V represents an asymmetric carbon that may be recemic or have the D or L configuration; W represents an asymmetric carbon when R7 and R8 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 antihypertansive agents.

515887

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