公开(公告)号：FI965039A0

公开(公告)日：1996-12-16

申请号：FI965039

申请日：1996-12-16

Applicant: BASF AG

Inventor： BUEHM 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 ,  C07K

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.

公开(公告)号：CA2210989A1

公开(公告)日：1996-08-15

申请号：CA2210989

申请日：1996-02-06

Applicant: BASF AG

Inventor： HORNBERGER WILFRIED ,  PFEIFFER THOMAS ,  SEITZ WERNER ,  ZIERKE THOMAS ,  MACK HELMUT ,  H FFKEN HANS WOLFGANG ,  B HM HANS-JOACHIM ,  KOSER STEFAN

IPC: A61K38/55 ,  A61K38/00 ,  A61P7/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/072 ,  C07K5/087 ,  A61K38/05

Abstract: The invention concerns thrombin inhibitors of formula (I), wherein R1, A, B, and D have the meanings given in the description, and intermediate products for the preparation thereof. The compounds of formula (I) are suitable for combating diseases.

公开(公告)号：CA2207874A1

公开(公告)日：1996-06-13

申请号：CA2207874

申请日：1995-11-25

Applicant: BASF AG

Inventor： SEITZ WERNER ,  PFEIFFER THOMAS ,  MACK HELMUT ,  KOSER STEFAN ,  HORNBERGER WILFRIED ,  ZIERKE THOMAS ,  HOEFFKEN HANS WOLFGANG ,  BOEHM HANS-JOACHIM

IPC: A61K38/00 ,  A61K38/05 ,  A61K38/55 ,  A61P7/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/072 ,  C07K5/087

Abstract: The invention pertains to compounds of formula (I), wherein R1, A and B are as indicated in the description, and to their preparation. The new compounds can be used for combatting diseases.

公开(公告)号：ZA200200459B

公开(公告)日：2004-05-26

申请号：ZA200200459

申请日：2002-01-18

Applicant: BASF AG

Inventor： KNOPP MONIKA ,  KOSER STEFAN ,  SCHAEFER BERND

IPC: C07D277/20 ,  C07D277/56 ,  C07D

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.

公开(公告)号：BR0012710A

公开(公告)日：2002-04-09

申请号：BR0012710

申请日：2000-07-11

Applicant: BASF AG

Inventor： KNOPP MONIKA ,  KOSER STEFAN ,  SCHOFER 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.

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.

公开(公告)号：ID24639A

公开(公告)日：2000-07-27

申请号：ID20000266

申请日：1998-08-14

Applicant: BASF AG

Inventor： BLANK STEFAN ,  SARCK DOROTHEA ,  TREIBER HANS-JORG ,  KOSER STEFAN ,  SCHAFER BERND ,  HOGER 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 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.

公开(公告)号：BR9811177A

公开(公告)日：2000-07-25

申请号：BR9811177

申请日：1998-08-14

Applicant: BASF AG

Inventor： BLANK STEFAN ,  STACK DOROTHEA ,  TREIBER HANS-JOERG ,  KOSER STEFAN ,  SCHOFER 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 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.

公开(公告)号：DE59507755D1

公开(公告)日：2000-03-09

申请号：DE59507755

申请日：1995-11-25

Applicant: BASF AG

Inventor： BOEHM HANS JOACHIM ,  KOSER STEFAN ,  MACK HELMUT ,  PFEIFFER THOMAS ,  SEITZ WERNER ,  HOEFFKEN HANS WOLFGANG ,  HORNBERGER WILFRIED ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61K38/05 ,  A61K38/55 ,  A61P7/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/065 ,  C07K5/072 ,  C07K5/087

公开(公告)号：ZA9807239B

公开(公告)日：2000-02-14

申请号：ZA9807239

申请日：1998-08-13

Applicant: BASF AG

Inventor： BLANK STEFAN ,  STARCK DOROTHEA ,  TREIBER HANS-JOERG ,  KOSER STEFAN ,  SCHAEFER 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 ,  C07D ,  A61K

CPC classification number: C07D239/56