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：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：NO991010L

公开(公告)日：1999-03-02

申请号：NO991010

申请日：1999-03-02

Applicant: BASF AG

Inventor： SCHOFER BERND ,  ZIERKE THOMAS

IPC: C07D213/81 ,  C07B43/00 ,  C07C257/10 ,  C07D213/73 ,  C07D213/78 ,  C07D271/06 ,  C07D401/12 ,  C07D413/12 ,  C07K1/06 ,  C07K5/062

Abstract: A process for preparing amidines and their salts with inorganic or organic acids comprises reacting the corresponding nitrile with ammonia, C1-C6-alkylamine or hydrazine in the presence of a mercaptocarboxylic acid and in the presence or absence of an in-organic or organic ammonium salt.

公开(公告)号：NO991010A

公开(公告)日：1999-03-02

申请号：NO991010

申请日：1999-03-02

Applicant: BASF AG

Inventor： SCHOFER BERND ,  ZIERKE THOMAS

IPC: C07D213/81 ,  C07B43/00 ,  C07C257/10 ,  C07D213/73 ,  C07D213/78 ,  C07D401/12 ,  C07K1/06 ,  C07K5/062

CPC classification number: C07D213/78 ,  C07C257/10 ,  C07D401/12

公开(公告)号：NO995939L

公开(公告)日：1999-12-03

申请号：NO995939

申请日：1999-12-03

Applicant: BASF AG

Inventor： SCHOFER 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.

公开(公告)号：NO995939D0

公开(公告)日：1999-12-03

申请号：NO995939

申请日：1999-12-03

Applicant: BASF AG

Inventor： SCHOFER BERND

IPC: C07D405/12 ,  C07D207/20 ,  C07D207/22 ,  C07D413/12 ,  C07D417/12 ,  C07D

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.

公开(公告)号：BR0010440A

公开(公告)日：2002-02-19

申请号：BR0010440

申请日：2000-05-03

Applicant: BASF AG

Inventor： SCHOFER BERND ,  HARMS GUIDO ,  ASCHERL HERMANN ,  KREI GEORG ARNOLD

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 process for preparing constant-weight thrombin inhibitors of the formula Iwhere n is 0, 1, 2, and tautomers thereof,wherein an aqueous solution of the active substance is spray dried.

公开(公告)号：BR0009330A

公开(公告)日：2002-01-08

申请号：BR0009330

申请日：2000-03-17

Applicant: BASF AG

Inventor： SCHOFER BERND ,  HELMCHEN GUENTER ,  KAZMAIER ULI ,  SCHLEICH SIMONE ,  STAHR HELMUT ,  WOLFART VOLKER

IPC: C07D211/78 ,  C07D207/16 ,  C07D207/20 ,  C07D211/70 ,  C07D207/22

Abstract: A process for preparing compounds of the formula Iin whichR is hydrogen, C1-C6-alkoxy, -NHC1-C6-alkyl, -N(C1-C6-alkyl)2, OH, NH2R1 is hydrogen, C1-C6-alkyl, Me3Si, C1-C6-alkyl-SR2 is Boc, C1-C6-acyl, mesyl, benzenesulfonyl, tosyl, trifluoroacetyl, A1-A3-peptiden is 1, 2R4 is H, C1-C6-alkyl,is described.

公开(公告)号：NO20000665D0

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 ,  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 ,  C07D

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：NO20000665A

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: 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

CPC classification number: C07D239/56