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    143.
    发明专利
    未知

    公开(公告)号：TR199900503T2

    公开(公告)日：1999-07-21

    申请号：TR9900503

    申请日：1997-08-22

    Applicant: BASF AG

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

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14 ,  A61K31/445

    Abstract: A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine compound of formula IwhereinR1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl,R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring,A is NH or oxygen,B is hydrogen or methyl,C is hydrogen, methyl or hydroxyl,X is nitrogen,Y is CH2, CH2-C2, CH2-C2-CH2 or CH2-CH,Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, andn is 2, 3 or 4,or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.

    3-SUBSTITUTED PYRIDO [3',4':4,5] THIENO [2,3-D] PYRIMIDINE DERIVATIVES, AND PRODUCTION AND USE OF THE SAME
    148.
    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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