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    1.
    发明专利
    未知

    公开(公告)号：DE19724979A1

    公开(公告)日：1998-12-17

    申请号：DE19724979

    申请日：1997-06-13

    Applicant: BASF AG

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

    IPC: A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14 ,  A61K31/55

    Abstract: The invention relates to 3-substituted 3,4,5,6,7,8-hexahydro-pyrido [3',4':4,5] thieno [2,3-d] pyrimidine derivatives of formula (I) wherein R is a hydrogen atom, a C1-C4 alkyl group, an acetyl group, a phenyl alkyl C1-C4 radical, the aromatic being optionally substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano or nitro groups, or a phenylalkanon radical in which the phenyl group can be substituted by halogen, R means a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and said group can be optionally anellated with a benzene nucleus which can be optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and may contain one nitrogen atom, or with a 5 or 6-membered ring which may contain 1-2 oxygen atoms, A represents NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2CH, Z represents a nitrogen atom, carbon atom or CH and the bond between Y and Z can also be a double bond, and n represents the number 2, 3 or 4. The invention also relates to the physiologically compatible salts of the inventive 3-substituted pyrido [3',4':4,5] thieno [2,3-d] pyrimidine derivatives. The inventive compounds show a high level of affinity for the serotonin receptors 5-HT1B, 5-HT1D and 5-HT1A. The affinity for said receptors is approximately equal, at least on the same scale. Some of the inventive compounds also have a good capacity for inhibiting serotonin reuptake, a property used in most antidepressants.

    2.
    发明专利
    未知

    公开(公告)号：DE19724980A1

    公开(公告)日：1998-12-17

    申请号：DE19724980

    申请日：1997-06-13

    Applicant: BASF AG

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

    IPC: A61K31/495 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/04 ,  A61K31/505 ,  A61K31/55

    Abstract: The invention relates to 3-substituted 3,4 dihydro-thieno[2, 3-d] pyrimidine derivatives of formula (I) wherein R and R mean a hydrogen atom or a C1-C4 alkyl group, R represents a phenyl, pyridyl, pyrimidinyl or pyrazinyl group optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups, said group being optionally anellated with a benzene nucleus which is optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and may contain optionally 1 nitrogen atom, or with a 5 or 6-membered ring which may contain 1-2 oxygen atoms, A represents NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z represents a nitrogen atom, carbon atom or CH and the bond between Y and Z can also be a double bond, and n is the number 2, 3 or 4. The invention also relates to the physiologically compatible salts of the inventive 3-substituted 3,4 dihydro-thieno[2,3-d] pyrimidine derivatives.

    New 2-substituted 1,2-benzisothiazole derivatives
    4.
    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.

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