Amino acid derivatives, a process for producing them and...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/435 (2006.01) C07D 495/04 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1243032

- 29 - Abstract Amino Acid Derivatives, Process for their Preparation and Pharmaceutical Preparations Containing them The specification described new amino acids derivatives of formula (X) Image (I) wherein R1 represents a hydrogen atom, an alkyl group with 1 to 6 carbon atoms or a phenylalkyl group with 7 to 12 carbon atoms; R2 represents a hydrogen atom; an alkyl group with 1 to 4 carbon atoms or a phenylalkyl group with 7 to 12 carbon atoms, R3 represents a hydrogen atom or an alkyl group with 1 to 6 carbon atoms; n and m each represent 0, 1 or 2, the sum of n and m being 1 or 2; X, Y and Z each represent a group or atom selected from oxygen or sulphur atoms or NR4, CR5, CHR5, Image , groups, provided that only one of the radicals X, Y and Z can represent oxygen or sulphur atoms or Image groups and only one or two of the radicals X, Y and Z can represent an NR4 group; R4 represents a hydrogen atom or an alkyl group with 1 to 4 carbon atoms; and - 30 - R5 represents a hydrogen atom or, together with a vicinal radical R5, a phenyl ring, or in the case when both m and n = 1, the dihydro form with its double bond in conjunction to the C- terminal carboxyl group, and their salts. a process for producing them, pharmaceutical compositions containing one or more compounds of general formula I as active substance, and their use in pharmaceuticals. The new amino acid derivatives have a long- lasting hypotensive effect which is based on an inhibition of the angiotensin I-converting enzyme.

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