THIOLSULFONAMIDE INHIBITORS OF METALLOPROTEASE Russian patent published in 2003 - IPC

FIELD: organic chemistry, biochemistry, medicine. SUBSTANCE: in- vention relates to thiolsulfonamides of formulas: (Ia) , (IIa) or (IIIa) , (IVa) , (IVb) where R¹ represents radical of length above the saturated chain among four carbon atoms but shorter than saturated chain among eighteen carbon atoms. At rotation on axis passing through position 1 linked with SO₂ and position 4,6- membered ring or through position 1 linked with SO₂-group and linked with substituent position of 3- or 5- membered ring it determines three-dimensional volume being its maximal size by width is about from one phenyl ring to about three phenyl rings in direction transverse to the rotation axis. R² means dihydro-group, C₁-C₆-alkyl, phenyl-C₁-C₄-alkyl, heteroaryl-C₁-C₄-alkyl, C₂-C₄-alkyl substituted with amino-group; C₂-C₄-alkyl, substituted monosubstituted amino-group or disubstituted amino-group where substituents at nitrogen atom of monosubstituted or disubstituted amino-group are taken among C₁-C₆-alkyl, aryl-C₁-C_6/ -alkyl, C₅-C₈-cycloalkyl and C₁-C₆-alkylcarbonyl, or where two substituents and nitrogen atom to which they are linked form in common pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyrazinyl, pyrimidinyl and others; R² can mean hydrido-group only then when R¹ means 4-(phenylazo)-phenyl; R⁴ means hydroxycarbonyl, aminocarbonyl, C₁-C₆-alkyl; R⁹ means C₁-C₆-alkyl, phenyl and others. Proposed compounds are inhibitors of metalloproteases activity that allows to use their in treatment of states associated with pathological activity of matrix metalloprotease. EFFECT: valuable medicinal properties of compounds. 30 cl, 99 tbl