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公开(公告)号:CA2186788A1
公开(公告)日:1995-10-05
申请号:CA2186788
申请日:1995-03-20
Applicant: BASF AG
Inventor: ULTSCH ANDREAS , STERRER SYLVIA , BACH ALFRED , LEMAIRE HANS-GEORG , HOEGER THOMAS
IPC: G01N33/566 , C07K14/705 , C12N5/10 , C12N15/09 , C12N15/12 , C12P21/02 , C12R1/91
Abstract: The invention concerns a method for the preparation of eucaryotic cell lines for the permanently ectopic expression of glutamate receptors, the cell lines being prepared by the transformation of cells containing nucleic acids coding for glutamate receptors. The method is characterized in that, during the establishment of the cell lines, at least one of the following conditions is satisfied for the culture: a) the transformed cells are cultured in a culture medium containing a glutamate precursor; b) the transformed cells are cultured in the presence of a glutamate-receptor antagonist: c) the transformed cells ant cultured in a first phase under conditions in which glutamate-receptor expression is repressed and in a second phase under conditions in which the repression is discontinued. The invention also concerns the cell lines thus obtained and their use.
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公开(公告)号:AT234616T
公开(公告)日:2003-04-15
申请号:AT95926897
申请日:1995-07-14
Applicant: BASF AG
Inventor: HELLENDAHL BEATE , LANSKY ANNEGRET , RENDENBACH-MUELLER BEATRICE , BACH ALFRED , UNGER LILIANE , TESCHENDORF HANS-JUERGEN , WICKE KARSTEN
IPC: C07D277/22 , A61K31/425 , A61K31/426 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4439 , A61K31/445 , A61K31/454 , A61K31/496 , A61K31/54 , C07D277/20 , C07D277/32 , C07D277/36 , C07D277/42 , C07D285/12 , C07D285/125 , C07D285/135 , C07D417/12
Abstract: PCT No. PCT/EP95/02783 Sec. 371 Date Jan. 14, 1997 Sec. 102(e) Date Jan. 14, 1997 PCT Filed Jul. 14, 1995 PCT Pub. No. WO96/02249 PCT Pub. Date Feb. 1, 1996The present invention relates to the use of thiazole and thiadiazole compounds of the following formula: where R1, A, B and Ar have the meanings stated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders of the central nervous system.
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公开(公告)号:ES2172222T3
公开(公告)日:2002-09-16
申请号:ES98951491
申请日:1998-10-05
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , DULLWEBER UTA , STARCK DOROTHEA , STEINER GERD , BACH ALFRED , EMLING FRANZ
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
Abstract: 3-substituted tetrahydropyridopyrimidinone derivatives of the formula (I) wherein the radicals have the meanings given in the Description, to a method for producing said derivatives and, to their use for producing active ingredients for drugs.
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公开(公告)号:CZ290678B6
公开(公告)日:2002-09-11
申请号:CZ2000462
申请日:1998-07-23
Applicant: BASF AG
Inventor: STEINER GERD , DULLWEBER UTA , STARCK DOROTHEA , BACH ALFRED , WICKE KARSTEN , TESCHENDORF HANS-JUERGEN , GARCIA-LADONA XAVIER , EMLING FRANZ
IPC: A61K31/435 , A61P25/24 , C07D495/14 , A61K31/4365
Abstract: In the present invention there are disclosed 3,4,5,7-tetrahydropyrrolo[3?, 4?:4,5]thieno[2,3-d]pyrimidine derivatives substituted in position 3 of the general formula I in which the substituents have specific meaning, and their use as a medicament for treating depressions and related disorders with effect as the selective antagonists 5-HTi1A and 5-HTi1B.
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135.
公开(公告)号:AU748666B2
公开(公告)日:2002-06-06
申请号:AU9748498
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
Abstract: 3-substituted tetrahydropyridopyrimidinone derivatives of the formula (I) wherein the radicals have the meanings given in the Description, to a method for producing said derivatives and, to their use for producing active ingredients for drugs.
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136.
公开(公告)号:NZ503604A
公开(公告)日:2002-03-01
申请号:NZ50360498
申请日:1998-10-05
Applicant: BASF AG
Inventor: BACH ALFRED , EMLING FRANZ , GARCIA-LADONA XAVIER , TESCHENDORF HANS-JURGEN , WICKE KARSTEN , LUBISCH WILFRED , DULLWEBER UTA , STARCK DOROTHEA , STEINER GERD
IPC: A61K31/428 , A61P25/24 , A61P43/00 , C07D275/06 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , A61K31/425
Abstract: 2-Substituted 1,2-benzisothiazole derivatives of formula (I) and their enantiomers, diastereomers, tautomers and acid salts are disclosed. R1 and R2 are independently C1-6 alkyl; R3 and R4 are independently H, C1-6 alkyl, OH, C1-6 alkoxy, F, Cl, Br, I, CF3, NR5R6, CO2R7, NO2, CN, pyrrolo, or phenyl-(C1-4 alkyl), which may itself be ring-substituted by F, Cl, Br, I, C1-4 alkyl, C1-4 alkoxy, CF3, OH, NH2, CN or NO2; R5 and R6 are independently H, C1-6 alkyl, benzoyl, CO2-tert.-butyl, (C1-4 alkyl)carbonyl or together form a 5- or 6-membered ring, which may contain a second N atom (e.g. piperazinyl); R7 is H or C1-6 alkyl; A is C1-10 alkylene or C2-10 alkylene containing one or more Z groups; Z is O, S, NR7, cyclopropyl, CHOH, or a double or triple bond; B is 4-piperidine, 4-(1,2,3,6-tetrahydropyridine), 4-piperazine or one of these rings N-bound to A via a methylene group; Ar is phenyl (optionally substituted by C1-6 alkyl, C1-6 alkoxy, OH, F, Cl, Br, I, CF3, NR5R6, CO2R7, CN or phenyl), tetralinyl, indanyl, other condensed aromatic moieties e.g. naphthalinyl (optionally substituted by C1-4 alkyl or C1-4 alkoxy), anthracenyl, or a 5- or 6-membered aromatic heterocycle with 1 or 2 O or N heteroatoms, which can be fused with other aromatic groups.
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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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公开(公告)号:NZ290388A
公开(公告)日:2001-04-27
申请号:NZ29038895
申请日:1995-07-14
Applicant: BASF AG
Inventor: HELLENDAHL BEATE , LANSKY ANNEGRET , RENDENBACH-MULLER BEATRICE , BACH ALFRED , UNGER LILIANE , TESCHENDORF HANS-JURGEN , WICKE CARSTEN
IPC: A61K31/33 , A61K31/415 , A61K31/44 , C07D233/84 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4425 , A61K31/445 , A61K31/495 , A61K31/496 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D213/56 , C07D213/64 , C07D213/65 , C07D213/70 , C07D213/73 , C07D213/79 , C07D213/81 , C07D233/90 , C07D307/79 , C07D333/24 , C07D333/28 , C07D333/38 , C07D471/18
Abstract: Use of a compound of the formula Het-A-B-Ar and the salts thereof with physiologically tolerated acids, in the manufacture of a medicament for treating disorders that respond to dopamine D3 receptor antagonists, wherein: A is a straight or branched alkylene group which contains at least one group which is selected from among O, S, NR4, CONR4, NR4 CO, COO, and OCO; B is a radical of formulae (I); Ar is a phenyl, pyridyl, pyrimidyl or triazinyl, where Ar may have one to four substituents selected from the group consisting of OR4, alkyl, alkenyl, alkynyl, halogen, CN, CO2R4, NO2, SO2R4, SO3R4, NR4R5, SO2NR4R5, SR4, CF3, CHF2, a 5- or a 6-membered carbocyclic, aromatic or non-aromatic ring and a 5- or a 6-membered heterocyclic, aromatic or non-aromatic ring having 1 to 3 hetero atoms which are selected from O, S and N, where the carbocyclic or the heterocyclic ring is unsubstituted or substituted by alkyl, halogen, O-alkyl, OH, NO2 or CF3, and where Ar may also be fused to a 5- or 6-membered carbocyclic, aromatic ring or to a 5- or 6-membered heterocyclic, aromatic or non-aromatic ring having 1 to 3 heteroatoms which are selected from O, S and N, where the carbocyclic or the heterocyclic ring is unsubstituted or substituted by -alkyl, halogen, O-alkyl, OH, NO2 or CF3; Het is a group of formulae (II); R1, R2 and R3 are, independently of one another, H, halogen, OR5, NR4R5, SR4, CF3, CN or alkyl which is unsubstituted or substituted by OH, O-alkyl or halogen; R4 is H or alkyl unsubstituted or substituted by OH, O-alkyl or halogen; R5 is the meaning indicated for R4 or is COR4 or CO2R4.
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公开(公告)号:PL340726A1
公开(公告)日:2001-02-26
申请号:PL34072698
申请日:1998-07-23
Applicant: BASF AG
Inventor: STEINER GERD , DULLWEBER UTA , STARCK DOROTHEA , BACH ALFRED , WICKE KARSTEN , TESCHENDORF HANS-JUERGEN , GARCIA-LADONA FRANCISCO-JAVIER , EMLING FRANZ
IPC: A61K31/435 , A61P25/24 , C07D495/14 , A61K31/519
Abstract: 3-Substituted 3,4,5,7-tetrahydropyrrolo[3',4':4,5]thieno-[2,3-d]pyrimidine derivatives of the formula Iin which the substituents have the meanings stated in the description, their preparation and their use as drugs.
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公开(公告)号:TR200001080T2
公开(公告)日:2001-01-22
申请号:TR200001080
申请日:1998-10-05
Applicant: BASF AG
Inventor: LUBISCH WILFRIED , DULLWEBER UTA , STARCK DORETHEA , STEINER GERD , BACH ALFRED , EMLING FRANZ , GARCIA-LADONA XAVIER , TESCHENDORF HANS-JURGEN , WICKE KARSTEN
IPC: A61K31/428 , A61P25/24 , A61P43/00 , C07D275/06 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
Abstract: where the substituents have the meanings indicated in the description, their preparation and use as serotonin antagonists.
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