Patent ID: 6509368
Filing Date: 2003-01-21
Classification: A61K,A61P

Abstract:
A method of treating a disease state selected from the group consisting of rheumatoid arthritis, periodontitis, arteriosclerotic plaques, osteoporosis, arthrosis, metastasis and neoangiogenesis of tumors, ulceration of the cornea and reactions of the skin to UV radiation in a mammal, said method comprising administering to said mammal an effective protease inhibiting amount of a catechol derivative corresponding to formula I: whereinR1 represents H, aryl-heterocyclyl, C1-16-alkyl, aryl, CHO, CON(CH3)2, COCH3, CO-tert.-butyl, heterocyclyl or C2-16-alkenyl; R2 represents H, aryl-heterocyclyl, C1-16-alkyl, aryl, CHO, CON(CH3)2, COCH3, CO-tert.-butyl, heterocyclyl or C2-16-alkenyl; R3 represents H, OH, C2-16-alkoxy or C2-6-alkenyl-COO-C1-6-alkyl; R4 represents aryl, â€”CH&boxH;CH-naphthyl, unsubstituted and/or OHâ€”, NH2â€” or halo-substituted C2-16-mono- or di-alkynyl, â€”C(O)-heterocyclyl, or R3 and R4 together with the carbon atoms of the aromatic ring to which they are bound form a 4- to 6-membered saturated or partially unsaturated cyclic hydrocarbon ring; and R5 represents aryl, â€”CH&boxH;CH-aryl, H, unsubstituted and/or OHâ€”, NH2â€” or halo-substituted C2-16-mono- or di-alkynyl, heterocyclyl, â€”C(O)-heterocyclyl, C1-8-alkyl, or R4 and R5 together with the carbon atoms of the aromatic ring to which they are bound form a 4- to 6-membered saturated or partially unsaturated cyclic hydrocarbon ring; or a pharmaceutically acceptable salt thereof.