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    3-SUBSTITUTED PYRIDO [3',4': 4,5] THIENO [2,3-D] PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND USE
    46.
    发明专利
    3-SUBSTITUTED PYRIDO [3',4': 4,5] THIENO [2,3-D] PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND USE 未知

    公开(公告)号：MY132993A

    公开(公告)日：2007-10-31

    申请号：MYPI9802644

    申请日：1998-06-13

    Applicant: BASF AG

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

    IPC: A61K31/495 ,  A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14

    Abstract: 3-SUBSTITUTED 3,4,S,6,7,8-HEXAHYDROPYRIDO [3',4':4,5]-THIENO[2,3-D]PYRIRNIDINE DERIVATIVES OF THE FORMULA I WHERE RL IS A HYDROGEN ATOM, A CL-C4-ALKYL GROUP, AN ACETYL GROUP, A PHENYLALKYL CL-C4 RADICAL, THE AROMATIC SYSTEM BEING UNSUBSTITUTED OR SUBSTITUTED BY HALOGEN, CL-C4-ALKYL, TRIFLUOROMETHYL, HYDROXYL, CL-C4-ALKOXY, AMINO, CYANO OR NITRO GROUPS, OR IS A PHENYLALKANONE RADICAL, IT BEING POSSIBLE FOR THE PHENYL GROUP TO BE SUBSTITUTED BY HALOGEN, R2 IS A PHENYL, PYRIDYL, PYRIMIDINYL OR PYRAZINYL GROUP WHICH IS UNSUBSTITUTED OR'MONO- OR DISUBSTITUTED BY HALOGEN ATOMS, CL-C4-ALKYL, TRIFLUOROMETHYL, TRIFLUOROMETHOXY, HYDROXYL, CL-C4- ALKOXY, AMINO, MONOMETHYLAMINO, DIMETHYLAMINO, CYANO OR NITRO GROUPS AND WHICH MAY BE FUSED TO A BENZENE NUCLEUS WHICH CAN BE UNSUBSTITUTED OR MONO- OR DISUBSTITUTED BY HALOGEN ATOMS, CL-C4 ALKYL, HYDROXYL, TRIFLUOROMETHYL, CL-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 ALSO BEING POSSIBLE FOR THE LINKAGE BETWEEN Y AND Z TO BE A DOUBLE BOND, AND N IS 2, 3 OR 4, AND THE PHYSIOLOGICALLY TOLERATED SALTS THEREOF.

    New 2-substituted 1,2-benzisothiazole derivatives
    48.
    发明专利
    New 2-substituted 1,2-benzisothiazole derivatives 未知

    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.

    49.
    发明专利
    未知

    公开(公告)号：DE19636769A1

    公开(公告)日：1998-03-12

    申请号：DE19636769

    申请日：1996-09-10

    Applicant: BASF AG

    Inventor： STEINER GERD DR ,  LUBISCH WILFRIED DR ,  BACH ALFRED DR ,  EMLING FRANZ DR ,  WICKE KARSTEN DR ,  TESCHENDORF HANS-JUERGEN DR ME ,  BEHL BERTHOLD DR ,  KERRIGAN FRANK DR ,  CHEETHAM SHARON DR

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14 ,  A61K31/44 ,  A61K31/38 ,  A61K31/505

    Abstract: The invention concerns 3-substituted 3,4,5,6,7,8-hexahydro-pyrido[4,3':4,5]thieno-[2,3-d]pyrimidine derivatives of formula (I) in which: R designates a hydrogen atom, a C1-C4 alkyl group, an acetyl or benzoyl group, a phenylalkyl C1-C4 group - the aromatic optionally being substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano or nitro groups - a naphthylalkyl C1-C3 group, a phenylalkanone C2-C3 group or a phenylcarbamoylalkyl C2 group, wherein the phenyl group can be substituted by halogen; R designates a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which can optionally be mono-, di- or tri-substituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and can optionally be anellated with a benzene nucleus, which can optionally be mono- or di-substituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and can optionally contain 1 nitrogen atom, or with a 5- or 6-member ring which can contain between 1 and 2 oxygen atoms, or can be substituted by a phenyl-C1-C2 alkyl or alkoxy group, wherein the phenyl group can be substituted by halogen, a methyl, trifluoromethyl or methoxy group; A designates NH or an oxygen atom; B designates hydrogen or methyl; C designates hydrogen, methyl or hydroxy; X designates a nitrogen atom; Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH; Z designates a nitrogen atom, a carbon atom or CH, wherein the bond between Y and Z can also be a double bond; and n is the number 2, 3 or 4, and their physiologically compatible salts. These compounds are suitable as medicaments for treating diseases in which the serotonin concentration is reduced and in which the activity of the presynaptic receptors 5-HT1B, 5-HT1A, 5HT1D is to be blocked within a therapeutic context without greatly influencing other receptors. Such diseases include, for example, depression.

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