Substituted tyrosyl alanine dipeptide amides

C - Chemistry – Metallurgy – 07 – K

Patent

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530/7.12, 167/10

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

Patent

CA 1258950

ABSTRACT The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: Image and the pharmaceutically acceptable acid addition salts thereof wherein R1 represents straight or branched lower alkyl having 1 to 4 carbons; R2 represents hydrogen, hydroxy, -OCO2R1 substituent or lower alkyl having 1 to 4 carbons; R3 represents a hydrogen or lower alkyl having 1 to 6 carbons; R4 and R5 may be the same or different and represent hydrogen or lower alkyl having 1 to 6 carbons; n is 1 to 6; X represents a hydrogen, hydroxy or OCO2R1 substituent; A represents a cyclohexyl, phenyl or phenyl substituted with one or more lower alkyls containing 1 to 6 carbons, one or more amino, hydroxy, halogen, nitro or lower alkoxy substituent having 1 to 6 carbons; V represents the asymmetric carbon that may be racemic or have the D or L configuration; W represents the asymmetric carbon when R4 and R5 are not the same that may optionally be racemic or have the D or L configuration. These compounds are useful as analgesic and/or antihypertensive agents.

474423

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