Amides of cyclomethylen-1,2-bicarboxylic acids having...

Details Amides of cyclomethylen-1,2-bicarboxylic acids having... Amides of cyclomethylen-1,2-bicarboxylic acids having...

C - Chemistry, Metallurgy

07

C

260/452, 260/515

C07C 239/08 (2006.01) C07C 259/06 (2006.01)

Patent

CA 1314903

ABSTRACT The amides of cyclomethylen-1,2-bicarboxylic acids having the formula: Image (I) A represents Image Image R1 represents -H, -CH3 , -CH2-CH3, -CH(CH3)2, Image Image , Image R2 represents -H, CH3. -CH2-CH3, CH(CH3)2, -CH2-CH2-CH3, -CH2-CH(CH3)2 -CH2-CH2-CH2-CH3, -CH2-C6H5, -C6-H5; R3 represents -H, -CH3, -C2H5, Image , Image R5 represents -H, -CH3, -C2H5, -CH2-C6H5, Image Y = -H, -CH3, -CH(CH3)2 Z = -H, -CH3, -C(CH3)3, Image Image , Image R4 = R5, Image m is 0 or 1 and n is an integer varying between 0 and 3, are endowed with ACE-inhibiting activity and are thus therapeutically useful as anti-hypertension agents. For their preparation cyclomethylene-1,2-dicarboxylic acid or a derivative thereof is condensed either with an amino derivative containing a protected hydroxamic group, or with an aminoester, and then in the former case the protecting group is removed, or in the latter case is reacted with either hydroxylamine or N-alkylhydroxylamine.

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