公开(公告)号：DE19746612A1

公开(公告)日：1999-04-29

申请号：DE19746612

申请日：1997-10-22

Applicant: BASF AG

Inventor： LUBISCH WILFRIED DR ,  DULLWEBER UTA DR ,  STARCK DOROTHEA DR ,  STEINER GERD DR ,  BACH ALFRED DR ,  EMLING FRANZ DR ,  GARCIA-LADONA FRANCISCO JAVIER ,  TESCHENDORF HANS-JUERGEN DR ,  WIECKE KARSTEN DR

IPC: A61K31/428 ,  A61P25/24 ,  A61P43/00 ,  C07D275/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  A61K31/445 ,  A61K31/44 ,  A61K31/425

Abstract: 2-Substituted 1,2-benzisothiazole derivatives (I) and their acid salts are new. 2-Substituted 1,2-benzisothiazole derivatives of formula (I) and their enantiomers, diastereomers, tautomers and acid salts are new. R , R = independently 1-6C alkyl; R , R = independently H, 1-6C alkyl, OH, 1-6C alkoxy, F, Cl, Br, I, CF3, NR R , CO2R , NO2, CN, pyrrolo, or phenyl-(1-4C alkyl), which may itself be ring-substituted by F, Cl, Br, I, 1-4C alkyl, 1-4C alkoxy, CF3, OH, NH2, CN or NO2; R , R = independently H, 1-6C alkyl, benzoyl, CO2-tert.-butyl, (1-4C alkyl)carbonyl or together form a 5- or 6-membered ring, which may contain a second N atom (e.g. piperazinyl); R = H or 1-6C alkyl; A = 1-10C alkylene or 2-10C alkylene containing one or more Z groups; Z = O, S, NR , cyclopropyl, CHOH, or a double or triple bond; B = 4-piperidine, 4-(1,2,3,6-tetrahydropyridine), 4-piperazine or one of these rings N-bound to A via a methylene group; Ar = phenyl (optionally substituted by 1-6C alkyl, 1-6C alkoxy, OH, F, Cl, Br, I, CF3, NR R , CO2R , CN or phenyl), tetralinyl, indanyl, other condensed aromatic moieties e.g. naphthalinyl (optionally substituted by 1-4C alkyl or 1-4C alkoxy), anthracenyl, or a 5- or 6-membered aromatic heterocycle with 1 or 2 O or N heteroatoms, which can be anellated with other aromatic groups.