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    61.
    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
    63.
    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.

    Serotonin antagonists 3-substituted tetrahydropyridopyrimidinone derivatives for treating 5HT, depression and related disorders
    69.
    发明专利
    Serotonin antagonists 3-substituted tetrahydropyridopyrimidinone derivatives for treating 5HT, depression and related disorders 未知

    公开(公告)号：NZ503486A

    公开(公告)日：2001-04-27

    申请号：NZ50348698

    申请日：1998-10-05

    Applicant: BASF AG

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

    IPC: A61K31/519 ,  A61P1/00 ,  A61P1/14 ,  A61P3/04 ,  A61P5/00 ,  A61P9/12 ,  A61P15/00 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D471/00 ,  C07D471/04 ,  C07D295/04

    Abstract: A 3-substituted tetrahydropyridopyrimidione derivative of the formula shown as a therapeutic composition having a high affinity for 5-HT1B, 5-HT1D and 5-HT1A serotonin receptors. The compounds are suitable for treating pathological states in which the serotonin concentration is reduced such as depression, mood disturbances with central nervous causation (dysthymia), anxiety such as panic attacks, sociophobia, obsessive-compulsive neuroses and post-traumatic stress symptoms, memory disturbances such as dementia, amnesias and age-related loss of memory and psychogenic eating disorders such as anorexia nervosa and bulimia nervosa. Wherein; one of the two radicals X and Y is CH2 and the other is NR1, R1 is hydrogen, C1-6alkyl branched or unbranched, CO-C1-4alkyl, CO2tBu, CO-phenyl and a phenylalkyl-C1-4 radical which in turn may be substituted on the aromatic system by F, Cl, Br, I, C1-4alkyl, C1-4alkoxy, trifluoromethyl, hydroxyl, amino, cyano or nitro, A is branched or unbranched C1-10alkylene or straight-chain or branched C2-10alkylene which comprises at least one group Z which is selected from O, S, NR2, cyclopropyl, CO2, CHOH, a double or triple bond, R2 is hydrogen and C1-4alkyl, B is 4-piperidine, 4-tetrahydro-1,2,3,6 pyridine, 4-piperazine or the corresponding cyclic compounds enlarged by one methylene group, with the linkage to A being via an N atom of B, and Ar is phenyl which is unsubstituted or substituted by C1-6alkyl branched or unbranched, O-C1-6alkyl branched or unbranched, OH, F, Cl, Br, I, trifluoromethyl, NR22, CO2R2, cyano or phenyl, or is tetralin, indan, naphthalene which is unsubstituted or substituted by C1-4alkyl or O-C1-4alkyl, anthracene or 5- or 6-membered aromatic heterocycles having 1 or 2 heteroatoms which are selected, independently of one another, from O and N.

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