| abstract |
REFERS TO AROMATIC SULFONE-HYDROXAMATES OF FORMULA I WHERE A1 IS H, ALKYLCARBONYL, ALCOXYCARBONYL, CARBOCYCLYLCARBONYL, CARBOCYCLYLALKYLCARBONYL, HETEROCYCLYLCARBONYL, BETWEEN OTHERS; A2 AND A3 TOGETHER TO WHICH THEY ARE BOTH UNITED FORM A REPLACED HETEROCYCLYL CONTAINING BETWEEN 5 AND 8 MEMBERS; E1 IS O, SO2, S, N (R1), CONR1, AMONG OTHERS; E2 IS RENTAL, CYCLOALKYL, ALKYL CYCLOALKYL, CYCLOALKYLALKYL, ALKYCYCLOALKYLALKYL, AMONG OTHERS; E2 FORMS A LINK OF AT LEAST 2 ATOMS OF C BETWEEN E1 AND E3; E3 IS CO, C (NR3), N (R4), AMONG OTHERS; E4 IS SELECTED FROM THE GROUP FORMED BY A LINK, ALKYL, ALKYL; E5 IS H, OH, ALKYL, ALKENYL, ALKINYL, ALCOXI, AMONG OTHERS; R1 AND R2 ARE H, ALKYL; R3 IS H, OH; R4 IS H, ALKYL, CARBOCYCLYL, CARBOCYCLYLALKYL, HETEROCYCLYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE 4 [[4- (3-AMINOPROPOXI) -PHENYL] SULFONIL] TETRAHYDRO-2H-PYRAN-4-CARBOXYL 1,1-DIMETHYLETHYL ESTER MONOCLORHYDRATE, 4 - [[4 - [[5- (METHOXY-METHYLAMINE) -5-OXOPENTIL] OXY] PHENYL] SULFONIL] -N- (TETRAHIDRO-2H-PIRAN-2-IL) OXY] -2H-PYRAN-4-CARBOXAMIDA, AMONG OTHERS. THE AROMATIC SULFONE HYDROXAMATE COMPOUNDS INHIBIT THE ACTIVITY OF MMP MATRIX METALOPROTEINASES AND THE ACTIVITY OF AGRECANASE AND ARE USEFUL FOR THE TREATMENT OF FIBROTIC, CARDIOVASCULAR DISEASES, OSTEOARTHRITIS, METALASSTORE |