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公开(公告)号：JPH10212248A
公开(公告)日：1998-08-11
申请号：JP35366697
申请日：1997-12-22
Applicant: BASF AG
Inventor： ISOLA ARTHUR MARK , HOLMAN NICHOLAS JOHN , TOMETZKI GERALD BERNARD , WATTS JOHN PAUL , KOSER STEFAN , KLINTZ RALF , MUENSTER PETER
IPC: C07B63/02 , C07C41/44 , C07C43/225 , C07C45/72 , C07C45/85 , C07C49/255 , C07C201/16 , C07C205/56 , C07D209/08 , C07D209/10 , C07D209/48 , C07D235/18 , C07D319/06 , C07D487/04
Abstract: PROBLEM TO BE SOLVED: To obtain the subject compound of which oxide content is decreased by adding a metal salt to form a complex thereof with trisubstituted phosphine and separating the complex formed from the mixture. SOLUTION: A reducing agent such as a trisubstituted phosphine represented by the formula (R is H, a 1-6C alkyl; R and R are each H, a 1-6C alkyl; R and R are each H, a 1-6C alkyl; R -R are each H, a 1-6C haloalkyl) is oxidized to form the oxide. A metal salt of an alkali metal is added to the oxide in a range from 0.25-5 molar equivalent based on the oxide to effect the Mitsunobu reaction. In the reaction, the reaction mixture is kept at the temperature ranging from 0 to 120 deg.C for 16 hours at maximum, then cooled down in the temperature range from -10 deg.C - the ambient temperature to form complex. The remaining complex is separated by filtration or centrifugation to decrease the oxide.
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公开(公告)号：HRP950338B1
公开(公告)日：2005-10-31
申请号：HRP950338
申请日：1995-06-14
Applicant: BASF AG
Inventor： BOEHM HANS-JOACHIM , KOSER STEFAN , MACK HELMUT , PFEIFFER THOMAS , SEITZ WERNER , HOEFFKEN HANS WOLFGANG , HORNBERGER WILFRIED
IPC: A61K31/40 , A61K38/00 , A61K38/05 , A61K38/55 , A61K47/48 , A61P7/02 , C07C279/00 , C07D205/04 , C07D207/06 , C07D207/16 , C07D207/48 , C07D211/60 , C07K5/06 , C07K5/065 , C07K5/072 , C07K5/078
Abstract: Compounds of the formula and the salts thereof with physiologically tolerated acids and the stereoisomers thereof, in which the substituents have the meanings stated in the description, are described. Also disclosed are intermediates for their preparation. The compounds are suitable for controlling diseases.
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公开(公告)号：AT237631T
公开(公告)日：2003-05-15
申请号：AT95923231
申请日：1995-06-06
Applicant: BASF AG
Inventor： BOEHM HANS-JOACHIM , KOSER STEFAN , MACK HELMUT , PFEIFFER THOMAS , SEITZ WERNER , HOEFFKEN HANS WOLFGANG , HORNBERGER WILFRIED
IPC: A61K31/40 , A61K38/00 , A61K38/05 , A61K38/55 , A61K47/48 , A61P7/02 , C07C279/00 , C07D205/04 , C07D207/06 , C07D207/16 , C07D207/48 , C07D211/60 , C07K5/06 , C07K5/065 , C07K5/072 , C07K5/078
Abstract: Compounds of the formula and the salts thereof with physiologically tolerated acids and the stereoisomers thereof, in which the substituents have the meanings stated in the description, are described. Also disclosed are intermediates for their preparation. The compounds are suitable for controlling diseases.
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公开(公告)号：TR200200181T2
公开(公告)日：2002-08-21
申请号：TR200200181
申请日：2000-07-11
Applicant: BASF AG
Inventor： KNOPP MONIKA , KOSER STEFAN , SCHAFER BERND
IPC: C07D277/20 , C07D277/56
Abstract: The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ibin whichn=1 or 2 andfor n=1, X is chloride, bromide, triflate and hydrogen sulfate andfor n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula IIis stirred with a cysteine ester of the formula III,in which R is branched or linear C1-10-alkyl orwhere n=0, 1 or 2 and R is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.
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公开(公告)号：SK1062002A3
公开(公告)日：2002-07-02
申请号：SK1062002
申请日：2000-07-11
Applicant: BASF AG
Inventor： KNOPP MONIKA , KOSER STEFAN , SCHAFER BERND
IPC: C07D277/20 , C07D277/56
Abstract: The invention relates to processes for preparing 2-aminomethyl-4-cyanothiazole and its salts of the formulae Ia and Ibin whichn=1 or 2 andfor n=1, X is chloride, bromide, triflate and hydrogen sulfate andfor n=2, X is sulfate, which comprises the process step where the aminonitrile of the formula IIis stirred with a cysteine ester of the formula III,in which R is branched or linear C1-10-alkyl orwhere n=0, 1 or 2 and R is branched or linear C1-C10C10-alkyl or C1-C4-alkoxy or C1-C4-dialkylamino in an inert solvent in the presence of a base at from 0° C. to 80° C. until the reaction has essentially proceeded to completion, and to the compounds of the formulae Ia and Ib.
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Patent Agency Ranking
公开(公告)号：HU0003710A2
公开(公告)日：2001-10-28
申请号：HU0003710
申请日：1998-08-14
Applicant: BASF AG
Inventor： BLANK STEFAN , HOEGER THOMAS , KOSER STEFAN , SCHAEFER BERND , STARCK DOROTHEA , THYES MARCO , TREIBER HANS-JOERG
IPC: C07D239/56 , A61K20060101 , 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：DE10005792A1
公开(公告)日：2001-08-16
申请号：DE10005792
申请日：2000-02-10
Applicant: BASF AG
Inventor： KOSER STEFAN , MUNDINGER KLAUS , KASEL WOLFGANG , KINGMA AREND JOUKE , DOCKNER TONI
Abstract: Preparation of bisphenol alkoxylates comprises reacting bisphenol(s) with an alkylene oxide in the presence of a phosphine catalyst free from alkali metal hydroxide. An independent claim is also included for the use of specified triaryl-phosphine catalysts in the preparation of bisphenol alkoxylates.
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公开(公告)号：BG104122A
公开(公告)日：2000-11-30
申请号：BG10412200
申请日：2000-02-03
Applicant: BASF AG
Inventor： BLANK STEFAN , STARCK DOROTHEA , TREIBER HANS-JOERG , KOSER STEFAN , SCHAFER BERND , THYES MARCO , HOEGER THOMAS
IPC: C07D239/56 , A61K20060101 , 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 invention relates to a salt of the fumaric acid with 2-{3-[4-(2-tret.-butyl-6-trifluoromethylpyrimidin-4-yl)piperazin-1 -yl]propylmercapto}pyrimidin-4-ol and to a pharmaceutical form containing it. The salt can be used for the treatment of diseases dependant on dopamine-D3-ligands. It is very stable at low pH adn is, therefore, particularly suitable for peroral administration. 3 claims
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公开(公告)号：CZ2000450A3
公开(公告)日：2000-10-11
申请号：CZ2000450
申请日：1998-08-14
Applicant: BASF AG
Inventor： BLANK STEFAN , STARCK DOROTHEA , TREIBER HANS-JOERG , KOSER STEFAN , SCHAFER BERND , THYES MARCO , HOEGER THOMAS
IPC: A61K31/505 , C07D239/56
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公开(公告)号：NO20000665L
公开(公告)日：2000-02-10
申请号：NO20000665
申请日：2000-02-10
Applicant: BASF AG
Inventor： BLANK STEFAN , STARCK DOROTHEA , TREIBER HANS-JOERG , KOSER STEFAN , SCHOFER BERND , THYES MARCO , HOEGER THOMAS
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 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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