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    2-SUBSTITUTED 1,2-BENZISOTHIAZOLE DERIVAYIVES AND THEIR USE AS SEROTONIN ANTAGONISTS (5-HT1A, 5-HT1B AND 5-HT1D)
    12.
    发明专利
    2-SUBSTITUTED 1,2-BENZISOTHIAZOLE DERIVAYIVES AND THEIR USE AS SEROTONIN ANTAGONISTS (5-HT1A, 5-HT1B AND 5-HT1D) 未知

    公开(公告)号：BG104332A

    公开(公告)日：2001-02-28

    申请号：BG10433200

    申请日：2000-04-11

    Applicant: BASF AG

    Inventor： LUBISCH WILFRIED ,  DULLWEBER UTA ,  STARCK DOROTHEA ,  STEINER GERD ,  BACH ALFRED ,  EMLING FRANZ ,  GARCIA-LADONA XAVIER ,  TESCHENDORF HANS-JUERGEN ,  WICKE KARSTEN

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

    Abstract: The invention relates to 2-substituted 1,2-benzisothiazole derivatives of formula wherein R1 and R2 represent (C1-C6) alkyl, independently of each other; A represents branched or unbranched (C1-10)-alkylene or straight-chained or branched (C2-10)-alkylene comprising at least one group Z which is selected from O, S, NR7, cyclopropyl, CHOH, a double or triple bond; B represents 4-piperidine, 4-tetrahydro-1, 2, 3, 6 pyridine, 4-piperazine and the corresponding ring compounds enlarged with a methylene group, an N-atom of B providing the link with A; Ar represents phenyl which is optionally substituted by (C1-6) alkyl -branched or unbranched-, O-(C1-6)-alkyl-branched or unbranched-, FH, F, Cl, Br, I, fluoromethyl, NR5R6, CO2R7, cyano or phenyl; tetralin, indan, highly condensed aromatics such as naphthalin optionally substituted by (C1-4) alkyl or O(C1-4) alkyl, anthracene or 5- or 6-membered aromatic heterocyclene with 1 to 2 heteroatoms which are selected independently of each other from O and N and which can still be anellated with further aromatic radicals such as quinoline, isoquinoline, phthalazine, indole and quinazoline which can itself be substituted again with phenyl; and R3 and R4 have the meanings given in the description. The invention also relates to the production of the inventive derivatives and to their use as serotonin antagonists. 7 claims

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