DERIVATIVES OF BICYCLIC IMINOACIDS AS MATRIX METALLOPROTEINASE INHIBITORS Russian patent published in 2008 - IPC C07D217/24 C07D217/26 A61K31/47 A61P19/10 

FIELD: chemistry.

SUBSTANCE: invention concerns compounds of the formula (I): and/or all stereoisomer forms of compound of the formula (I) and/or mix of these forms at any ratio, and/or physiologically acceptable salt of compound of the formula (I), where A is -(C₀-C₄)-alkylene; B is -(C₀-C₄)-alkylene or residue -B1-B2-B3-, where B1 is -(CH₂)_n-, where m is integer 0; B3 is -(CH₂)_m-, where m is integer 0; so that amount of n and m is 0; and B2 is -O-; cycle 1 or cycle 2 are equal or differ and denote independently 1) covalent link, 2)-(C₆-C₁₄)-aryl which is an aromatic hydrocarbon residue with 6-14 carbon atoms in a cycle, where the said aryl is unsubstituted or independently monosubstituted by G, or 3) 4-15-member heterocycle which is a cyclic system with 4-15 carbon atoms located in one, two or three interconnected cyclic systems, and containing one heteroatom selected out of nitrogen or oxygen, where the said heterocycle is unsubstituted or independently monosubstituted by G; G is 1) hydrogen atom, 2) halogen atom, 3)-O-R12, where R12 is a) hydrogen atom, b)-(C₁-C₆)-alkyl, where alkyl is unsubstituted or trisubstituted by halogen atom, c)-C(O)-O-R13, where R13 is c)1)-(C₁-C₆)-alkyl, where alkyl is unsubstituted, 4)-NO₂, 5)-CN, 6)-N(R15)-R12, where R15 is 6)1)hydrogen atom, X stands for -OH or -NH-OH; n1 is integer 2; n2 is integer 3; together with that, that the sum of n1 and n2 is 5; R1, R2, R3, R4 and R5 are equal or different and independently from each other stand for 1) hydrogen atom, 2)-C(O)-R8, where R8 is 2)1) hydrogen atom, 2)2)-(C₁-C₆)-alkyl, where alkyl is unsubstituted. The invention also concerns method of obtaining compounds of the formula (I) and medical preparation for matrix metalloproteinase inhibition.

EFFECT: new derivatives of saturated bicyclic iminoacids with useful biological properties.

4 cl, 1 tbl, 29 ex