FIELD: medicine; pharmaceuticals.
SUBSTANCE: invention relates to compounds applicable in medicine of general formula (I), their optical isomers and salts of attachment to a pharmaceutically acceptable acid:
,
where Ak1 is C1-C6-alkyl chain, X is -(CH2)m-, -CH(R)-, -N(R)-, -CH2-N(R)-, –N(R)-CH2- or -CH2-N(R)-CH2-, m is 0 or integer from 1 to 4, R is a hydrogen atom or a group selected from C1-C6-alkyl, -Ak2-Ar1, -Ak2-Ar1-Ar2 and –Ak2-Ar1-O-Ar2, -Ak2-cyclohexyl or -Ak2-OH; Ak2 is a linear or branched C1-C6-alkyl chain; Ar1 and Ar2, which can be identical or different, each represents an aryl or heteroaryl group; R1 and R2 each represent a hydrogen atom when X is -(CH2)m-, -CH(R)-, -N(R)-, -CH2-N(R)- or –N(R)-CH2-, or together form a bond when X is -CH2-N(R)-CH2-; R3 denotes NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl; Cy is a group selected from cyclohexyl, aryl and heteroaryl, Ak3 is C1-C3 alkyl chain, R4 and R5 each represent a hydrogen atom, where aryl is phenyl, naphthyl or biphenyl, optionally substituted with one or more groups, identical or different, selected from halogen, hydroxy, linear or branched (C1-C6)-alkyl, optionally substituted with one or more halogen atoms, methylsulfonyl, methylthio, carboxy, linear or branched (C1-C6)-alkoxy, optionally substituted with one or more halogen atoms, linear or branched (C1-C6)-aminoalkyl, amino group of aminoalkyl group is optionally substituted with one or two groups of linear or branched (C1-C6)-alkyl, and heteroaryl means 5–11-membered monocyclic aromatic group or a bicyclic aromatic or partially aromatic group and containing one, two or three heteroatoms selected from oxygen, nitrogen or sulfur, provided that heteroaryl can optionally be substituted with one or more groups identical or different, selected from halogen, hydroxy, amino, oxo, linear or branched (C1-C6)-alkyl, optionally substituted with one or more halogen atoms, linear or branched (C1-C6)-alkoxy.
EFFECT: novel compounds and pharmaceutical compositions based thereon, effective for TAFIa inhibition for treating and preventing cerebral circulation disorders, myocardial infarction, angina pectoris, arteritis of lower extremities, thromboses, particularly venous thromboses, pulmonary embolism, aortic aneurysm or dementia.
20 cl, 1 tbl, 268 ex
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