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    111.
    发明专利
    未知

    公开(公告)号：NO996045D0

    公开(公告)日：1999-12-08

    申请号：NO996045

    申请日：1999-12-08

    Applicant: BASF AG

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

    IPC: A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P25/24 ,  A61P43/00 ,  C07D495/14 ,  C07D

    Abstract: PCT No. PCT/EP98/03231 Sec. 371 Date Dec. 8, 1999 Sec. 102(e) Date Dec. 8, 1999 PCT Filed May 29, 1998 PCT Pub. No. WO98/56793 PCT Pub. Date Dec. 17, 19983-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I where R1 is a hydrogen atom, a C1-C4-alkyl group, an acetyl group, a phenylalkyl C1-C4 radical, the aromatic system being unsubstituted or substituted by halogen, C1-C4-alkyl, trifluoromethyl, hydroxyl, C1-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, 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 can 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 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.

    3-SUBSTITUTED PYRIDO [3',4':4,5] THIENO [2,3-D] PYRIMIDINE DERIVATIVES, AND PRODUCTION AND USE OF THE SAME
    115.
    发明专利
    3-SUBSTITUTED PYRIDO [3',4':4,5] THIENO [2,3-D] PYRIMIDINE DERIVATIVES, AND PRODUCTION AND USE OF THE SAME 未知

    公开(公告)号：CA2293440A1

    公开(公告)日：1998-12-17

    申请号：CA2293440

    申请日：1998-05-29

    Applicant: BASF AG

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

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

    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 R1 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, R2 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 5HT1A. 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.

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