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    2-SUBSTITUTED 1,2-BENZISOTHIAZOLE DERIVAYIVES AND THEIR USE AS SEROTONIN ANTAGONISTS (5-HT1A, 5-HT1B AND 5-HT1D)
    53.
    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

    3-substituted 3,4 dihydro-thieno[2,3-d]pyrimidine for treating depression
    54.
    发明专利
    3-substituted 3,4 dihydro-thieno[2,3-d]pyrimidine for treating depression 未知

    公开(公告)号：NZ502238A

    公开(公告)日：2001-02-23

    申请号：NZ50223898

    申请日：1998-05-29

    Applicant: BASF AG

    Inventor： STEINER GERD ,  DULLWEBER UTA ,  STARCK DOROTHEA ,  BACH ALFRED ,  WICKE KARSTEN ,  TESCHENDORF HANS-JURGEN ,  GARCIA-LADONA FRANCISCO-JAVIER ,  EMLING FRANZ

    IPC: A61K31/495 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/04

    Abstract: PCT No. PCT/EP98/03230 Sec. 371 Date Dec. 6, 1999 Sec. 102(e) Date Dec. 6, 1999 PCT Filed May 29, 1998 PCT Pub. No. WO98/56792 PCT Pub. Date Dec. 17, 19983-Substituted 3,4-dihydrothieno[2,3-d]pyrimidine derivatives of the formula I where R1 and R2 are a hydrogen atom or a C1-C4-alkyl group, R3 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4-alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which may be unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, hydroxyl, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitro groups, and may contain 1 nitrogen atom, or to a 5- or 6-membered ring, which may contain 1-2 oxygen atoms, A is NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, carbon atom or CH, it being possible for the linkage between Y and Z also to be a double bond, and n is 2, 3 or 4, and the physiologically tolerated salts thereof.

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