DIPEPTIDES CONTAINING 2-THIOACYL GROUP AT N-TERMINAL AMINO ACID RESIDUE AS VASOPEPTIDASE INHIBITORS Russian patent published in 2007 - IPC C07K5/06 A61K38/05 A61P9/12 

FIELD: organic chemistry, peptides, biochemistry.

SUBSTANCE: invention relates to compounds of the formula (I): , wherein R means hydrogen atom; R₁ means carbocyclic aryl substituted optionally with halogen atom or (carbocyclic aryl or biaryl)-(lower)-alkyl substituted optionally with trifluoromethyl group or halogen atom; alk means (lower)-alkylene; R₃ means hydrogen atom or acyl substituted optionally with alkoxy-group, morpholinyl, triazolyl or piperazinyl groups; R₄ means hydrogen atom substituted optionally with methoxy-(lower)-alkyl or oxacycloalkyl group; R₅ means hydrogen atom or (lower)-alkyl; R₆ means (lower)-alkyl; R₇ means (lower)-alkyl; or R₆ and R₇ in common with carbon atom to which they are bound mean 3-10-membered cycloalkylidene; X means -O-,-S(O)_n-, -NHCO- wherein n = 0 or 2; -COOR₂ means carboxyl or derivative of carboxyl group as a pharmaceutically acceptable ester wherein R₂ is chosen from (lower)-alkyl, morpholine carbonylmethyl, dimethylaminocarbonylmethyl or diethylaminocarbonylmethyl, or its pharmaceutically acceptable salt. Proposed compounds are used as dual inhibitors of angiotensin-converting enzyme and neutral endopeptidase and as inhibitor of endothelin-converting enzyme also.

EFFECT: valuable medicinal and biochemical properties of dipeptides.

8 cl, 7 ex