Patent ID: 6346622
Filing Date: 2002-02-12
Classification: A61P,C07D

Abstract:
A 2-substituted 1,2-benzoisothiazole derivative of the formula I whereR1 and R2 are, independently of one another, (C1-6) alkyl, R3, R4 are, independently of one another, hydrogen, (C1-6) alkyl branched or unbranched, OH, Oâ€”(C1-6)-alkyl branched or unbranched, F, Cl, Br, I, trifluoromethyl, NR5R6, CO2R7, nitro, cyano, pyrrole, a phenylalkyl C1-C4 radical which in turn can be substituted on the aromatic system by F, Cl, Br, I, C1-C4 alkyl, C1-C4 alkoxy, trifluoromethyl, hydroxyl, amino, cyano or nitro, R5 and R6 are, independently of one another, hydrogen, (C1-6) alkyl branched or unbranched, COPh, CO2tBu, COâ€”(C1-4)-alkyl or together are a 5- or 6-membered ring which may contain a second nitrogen, R7 is hydrogen or (C1-6) alkyl branched or unbranched, A is branched or unbranched (C1-10)-alkylene or straight-chain or branched (C2-10)-alkylene which contains one or more groups Z selected from O, S, NR7, cyclopropyl, CHOH, a double or a triple bond, B is 4-piperidine, 4-tetrahydro-1,2,3,6-pyridine, 4-piperazine and homopiperazine, the linkage to A taking place by one nitrogen atom of B, and Ar is phenyl which is unsubstituted or substituted by (C1-6) alkyl branched or unbranched, Oâ€”(C1-6)-alkyl branched or unbranched, OH, F, Cl, Br, I, trifluoromethyl, NR5R6, CO2R7, cyano or phenyl or is tetralin, indan, a fused aromatic system selected from the group consisting of naphthyl which is unsubstituted or substituted by (C1-4) alkyl or O(C1-4) alkyl, anthracene and 5- or 6-membered aromatic heterocycles having 1 or 2 nitrogen atoms which may be substituted by methyl and/or trifluoromethyl and which may also be fused to other aromatic radicals, its possible enantiomers and diastereomers, tautomeric forms and its salts with physiologically tolerated acids.