Substituted dipeptide amides #2

C - Chemistry – Metallurgy – 07 – K

Patent

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530/5.06

C07K 5/06 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1279950

ABSTRACT OF THE DISCLOSURE This invention encompasses compounds of the formula Image and the pharmaceutically acceptable acid addition salts thereof wherein R1 is lower alkoxy or -O-(CH2)n-phenyl where the phenyl may be optionally substituted with halogen, -NO2,-CN, -NH2 or lower alkyl whereln n is 1 to 4; R2 and R3 represent lower alkyl, halogen, lower alkoxy or one of R2 or R3 is hydrogen and the other is lower alkyl, lower alkoxy, or halogen; R4, R5, R7, R8, and R9 represent hydrogen or lower alkyl, R6 represents hydrogen, lower alkyl, lower alkenyl, or -(CH2)m-cycloalkyl wherein m is 1 to 4 and the cycloalkyl has 3 to 8 carbon atoms; R10 ia -(CH2)p-phenyl wherein p is 1 to 4; and 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. This invention also encompasses compounds where R1 is hydroxy, provided at least one of R4, R5, R6 or R9 is lower alkyl. The compounds of this invention are useful analgesic agents.

515814

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