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公开(公告)号:TR200000406T2
公开(公告)日:2000-05-22
申请号:TR200000406
申请日:1998-08-14
Applicant: BASF AG
Inventor: BLANK STEFAN , STARCK DOROTHEA , TREIBER HANS-JORG , KOSER STEFAN , SCHAFER BERND , THYES MARCO , HOEGER THOMAS
IPC: A61K20060101 , C07D239/56 , A61K31/395 , A61K31/497 , A61K31/505 , A61K31/506 , A61P1/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P43/00 , C07D20060101 , C07D239/42 , C07D239/46 , C07D295/125 , C07D403/00 , C07D403/12 , C07D403/14
Abstract: The fumaric acid salt (A) of 2-{3-[4-(2-tert. butyl-6-trifluoromethyl- pyrimidin-4-yl)piperazin-1- yl]propylmercapto}pyrimidin-4-ol (I) is new. The fumarate salt (A) of the pyrimidin-4-ol derivative of formula (I) is new. The tautomers, solvates and hydrates of (A) are also new. ACTIVITY : Neuroleptic; antidepressant; antiemetic; antihistamine. MECHANISM OF ACTION : Dopamine D 3 receptor ligand. (A) has a selectivity Ki D 2/Ki D 3 of 120.
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公开(公告)号:CZ9900620A3
公开(公告)日:2000-05-17
申请号:CZ62099
申请日:1997-08-21
Applicant: BASF AG
Inventor: SCHAFER BERND , ZIERKE THOMAS
IPC: C07B43/00 , C07D213/78 , C07D271/06 , C07D401/12 , C07D413/12
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公开(公告)号:CZ428899A3
公开(公告)日:2000-03-15
申请号:CZ428899
申请日:1998-06-02
Applicant: BASF AG
Inventor: SCHAFER BERND
IPC: C07D207/20 , C07D417/12
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公开(公告)号:AU8335298A
公开(公告)日:1998-12-21
申请号:AU8335298
申请日:1998-06-02
Applicant: BASF AG
Inventor: SCHAFER BERND
IPC: C07D405/12 , C07D207/20 , C07D207/22 , C07D413/12 , C07D417/12
Abstract: PCT No. PCT/EP98/03284 Sec. 371 Date Dec. 1, 1999 Sec. 102(e) Date Dec. 1, 1999 PCT Filed Jun. 2, 1998 PCT Pub. No. WO98/55456 PCT Pub. Date Dec. 10, 1998The invention relates to a process for preparing chiral 3,4-dehydroproline compounds of formula (I), in which R, R' and R'' have the meanings given in the description. The invention is characterized by a pyrrolecarboxylic acid derivative compound of formula (II) reacted first with an alkali or alkaline earth metal in ammonia and then with an aqueous salt solution or a compound of formula (III) in which X is a leaving group to form the final chiral product compound.
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公开(公告)号:NO961544L
公开(公告)日:1996-04-18
申请号:NO961544
申请日:1996-04-18
Applicant: BASF AG
Inventor: SCHAFER BERND , MAYER HORST
IPC: C07D251/46 , B01J27/122 , B01J27/138 , B01J31/04 , B01J31/22 , C07D251/16 , C07D
Abstract: PCT No. PCT/EP94/03331 Sec. 371 Date Mar. 29, 1996 Sec. 102(e) Date Mar. 29, 1996 PCT Filed Oct. 10, 1994 PCT Pub. No. WO95/11237 PCT Pub. Date Apr. 27, 1995A process for preparing asymmetrically substituted triazines of the formula I I where R1 is hydrogen, methyl or ethyl, R2 and R3 independently of one another are an unsubstituted or substituted hydrocarbon radical, by reaction of a cyanoguanidine of the formula II II with a carboxylic acid derivative in the presence of an alcohol of the formula III R2-OHIII,which comprises reacting a carboxylic acid ester of the formula IV R3-COOR4IV,where R3 has the abovementioned meaning and R4 is an unsubstituted or substituted hydrocarbon radical, in the presence of a base or of a carboxamide selected from the group consisting of N,N-dialkylformamide, N,N-dialkylacetamide and N-methylpyrrolidone and in the presence of a salt or of a salt-like compound of the elements magnesium, calcium, aluminum, zinc, copper, iron, cobalt, nickel or chromium, is described.
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公开(公告)号:NO961544A
公开(公告)日:1996-04-18
申请号:NO961544
申请日:1996-04-18
Applicant: BASF AG
Inventor: SCHAFER BERND , MAYER HORST
IPC: C07D251/46 , B01J27/122 , B01J27/138 , B01J31/04 , B01J31/22 , C07D251/16 , C07D
CPC classification number: C07D251/16
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公开(公告)号:CA2174332A1
公开(公告)日:1995-04-27
申请号:CA2174332
申请日:1994-10-10
Applicant: BASF AG
Inventor: MAYER HORST , SCHAFER BERND
IPC: C07D251/16
Abstract: Described is a method of preparing unsymmetrically substituted triazines of formula (I), in which R1 is hydrogen, methyl or ethyl, R2 and R3, independently of each other, are an optionally substituted hydrocarbon group, by reacting a cyanoguanidine of formula (II) with a carboxylic acid derivative in the presence of an alcohol of formula (III), the method being characterized in that the reaction is carried out with a carboxylic acid ester of formula (IV), in which R3 is as defined above and R4 is an optionally substituted hydrocarbon group, in the presence of a base or a carboxylic acid amide selected from the group comprising N,N-dialkylformamide, N,N-dialkylacetamide and N-methylpyrrolidone and in the presence of a salt or a salt-like compound of one of the elements magnesium, calcium, aluminium, zinc, copper, iron, cobalt, nickel and chromium.
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公开(公告)号:CA2418749A1
公开(公告)日:2003-02-10
申请号:CA2418749
申请日:2001-08-09
Applicant: BASF AG
Inventor: GENESTE HERVE , SCHAFER BERND
IPC: C07C37/00 , C07C37/50 , C07C39/24 , C07C45/00 , C07C45/60 , C07C47/565 , C07C49/825 , C07C51/15 , C07C65/05 , C07D309/12 , C07F5/02 , C07F7/08
Abstract: The invention relates to a method for producing 2- and 2,5-substituted derivatives of 4-(trifluoromethyl)-phenol and 4-(2-trifluoromethyl)-phenyl)- 2- tetrahydropyranyl) ether and to novel derivatives. Said method is characterised in that a compound of formula (2) 4-(trifluoromethylphenyl)-2- (tetrahydropyranyl) ether is reacted with an electrophile E-X or a combinati on of electrophiles E-X and E-Y in the presence of a base, X and Y having the meanings given in the description.
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39.
公开(公告)号:NZ502675A
公开(公告)日:2001-06-29
申请号:NZ50267598
申请日:1998-08-14
Applicant: BASF AG
Inventor: HOGER THOMAS , BLANK STEFAN , STARCK DOROTHEA , TREIBER HANS-JORG , KOSER STEFAN , SCHAFER BERND , THYES MARCO
IPC: A61K20060101 , A61K31/395 , C07D239/56 , A61K31/497 , A61K31/505 , A61K31/506 , A61P1/08 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/24 , A61P43/00 , C07D20060101 , C07D239/42 , C07D239/46 , C07D295/125 , C07D403/00 , C07D403/12 , C07D403/14
Abstract: The specification describes the fumaric acid salt (A) of 2-(3-(4-(2-tert.butyl-6-trifluoromethyl- pyrimidin-4-yl)piperazin-1yl)propylmercapto)pyrimidin-4-ol (I). The fumaric salt of this known compound (WO96/02519) is reported to have very good affinity and high selectivity for the D3 receptor and is therefore useful for treating disorders which respond to dopamine D3 ligands such as schizophrenia, depressions, neuroses and psychoses.
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公开(公告)号:CA2373068A1
公开(公告)日:2000-11-16
申请号:CA2373068
申请日:2000-05-03
Applicant: BASF AG
Inventor: KREI GEORG ARNOLD , ASCHERL HERMANN , SCHAFER BERND , HARMS GUIDO
IPC: C12N9/99 , A61K38/00 , A61P7/02 , A61P9/00 , A61P25/00 , A61P35/00 , C07K5/065 , C07K5/06 , C07K1/14 , A61K31/40 , A61K31/44
Abstract: The invention relates to a method for producing thrombin inhibitors which ha ve a constant weight and which are of formula (I), whereby n represents 0, 1, 2 and tautomers thereof, whereby an aqueous solution of the active substance i s spray dried.
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