ARYLPIPERAZINES, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION Russian patent published in 2004 - IPC

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to arylpiperazines of the general formula (I): wherein B is phenyl, pyridyl or pyrimidyl; each R₃ is hydrogen, halogen atom, NO₂, COOR wherein R is hydrogen atom, C_1-6-alkyl, CN, CF₃, C_1-6-alkyl, -S-C_1-6-alkyl, -SO-Cl-C_1-6-alkyl, SO₂-Cl-C_1-6-alkyl, C_1-6-alkoxy-group and up to C₁₀-aryloxy-group; n = 1, 2 or 3; p is direct bond; A is piperazinyl; X₁ and X₂ mean nitrogen atom; Y means -SO₂-; Z means N(OH)- CHO; Q means -CH₂-; R₁ means hydrogen atom, C_1-6-alkyl, C_5-7-cycloalkyl up to C₁₀-aryl, up to C₁₀- heteroaryl, up to C_1-2-aralkyl, up to C₁₂-heteroarylalkyl; R₄ means hydrogen atom, C_1-6-alkyl and others; R₂ means hydrogen atom, C_1-6-alkyl, or in common with R₁ it forms carbocyclic or heterocyclic spiro 5-, 6- or 7- membered ring comprising at least one heteroatom taken among N, O or S; group Q can be linked with either R₁ or with R₂ to form 5-, 6- or 7-membered alkyl or heteroalkyl ring comprising one or some atoms of O, S or N. Piperazines of the formula (I) are used as inhibitors of metalloproteinases, especially as inhibitors of MMP- 13. EFFECT: improved preparing methods, valuable biochemical properties of compounds. 8 cl, 22 ex