Amide derivatives

Details Amide derivatives Amide derivatives

C - Chemistry, Metallurgy

07

K

530/5.06

C07K 5/06 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1246550

A B S T R A C T Amide Derivatives Amide derivatives of the formula:- Image wherein either R1 is aryl or heterocyclic and A1 is a direct link, or R1 is aryl or heterocyclic, or hydrogen or amino and A1 is alkylene; X is -CH2- or -CO- or has the formula Image wherein R11 and R12, which may be the same or different, each is alkyl, or R11 and R12 are joined to form alkylene; A2 is alkylene; R2 is hydrogen, aryl or alkyl which is unsubstituted or which bears an aryl substituent; R3 is hydrogen or alkyl which is unsubstituted or which bears a halogeno, hydroxy, amino, guanidino, carboxy, carbamoyl, mercapto, alkoxy, alkylamino, dialkylamino, cyclic amino, alkylthio, alkanoylamino, alkoxycarbonyl, arylalkoxycarbonyl, aryl or heterocyclyl substituent; R4 is alkyl which is unsubstituted or which bears an aryl substituent, or R4 is phenyl or alkylphenyl; n is 0 or 1; and either R5, R6, R15 and R16 are all hydrogen, or R5 and R6 are both hydrogen and R15 and R16 together form tetramethylene; or R5 and R6 together form a second bond between the two carbon atoms to which they are attached and R15 and R16 together form buta-1,3- dien-1,4-diyl;or a salt thereof; processes for their manuacture and pharmaceutical compositions containing them. The compounds are inhibitors of angiotensin converting enzyme.

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