ARYLPIPERAZINES, METHODS FOR THEIR PREPARING, PHARMACEUTICAL COMPOSITION
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, C1-6-alkyl, CN, CF3, C1-6-alkyl, -S-C1-6-alkyl, -SO-Cl-C1-...
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Zusammenfassung: | 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, C1-6-alkyl, CN, CF3, C1-6-alkyl, -S-C1-6-alkyl, -SO-Cl-C1-6-alkyl, SO2-Cl-C1-6-alkyl, C1-6-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, C1-6-alkyl, C5-7-cycloalkyl up to C10-aryl, up to C10- heteroaryl, up to C1-2-aralkyl, up to C12-heteroarylalkyl; R4 means hydrogen atom, C1-6-alkyl and others; R2 means hydrogen atom, C1-6-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 |
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