公开(公告)号：SK1182000A3

公开(公告)日：2000-09-12

申请号：SK1182000

申请日：1998-08-14

Applicant: BASF AG

Inventor： BLANK STEFAN ,  STARCK DOROTHEA ,  TREIBER HANS-JOERG ,  KOSER STEFAN ,  SCHAFER BERND ,  THYES MARCO ,  HOGER 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.

公开(公告)号：HRP950271B1

公开(公告)日：2000-08-31

申请号：HRP950271

申请日：1995-05-04

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  HARALD BERNARD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  JANITSCHKE LOTHAR ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MULLER STEFAN ,  POTZOLLI BERND DE ,  RITTER KURT ,  THYES MARCO ,  ZIERKE THOMAS

IPC: A61K38/08 ,  A61K38/00 ,  A61P35/00 ,  C07K1/08 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C07K14/52

Abstract: PCT No. PCT/EP95/01577 Sec. 371 Date Nov. 4, 1996 Sec. 102(e) Date Nov. 4, 1996 PCT Filed Apr. 26, 1995 PCT Pub. No. WO95/30691 PCT Pub. Date Nov. 16, 1995The compound Me2Val-Val-MeVal-Pro-Pro-NHBzlxHCl is described. It is prepared from Z-Val-Val-MeVal-Pro-OR1 where Z and R1 have the meanings stated in the description. The compound shows antineoplastic activity.

公开(公告)号：ZA987239B

公开(公告)日：2000-02-14

申请号：ZA987239

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: A61K20060101 ,  A61K31/395 ,  A61K31/497 ,  C07D239/56 ,  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

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：CA2301297A1

公开(公告)日：1999-02-25

申请号：CA2301297

申请日：1998-08-14

Applicant: BASF AG

Inventor： SCHAFER BERND ,  STARCK DOROTHEA ,  BLANK STEFAN ,  THYES MARCO ,  TREIBER HANS-JORG ,  KOSER STEFAN ,  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 invention relates to the fumaric acid salt from 2-{3-4-(2-T-butyl-6-trifluoromethylpyridin-4-yl) piperazin-1-yl! propylmercapto} pyrimidin-4-ol and to pharmaceutical agents containing said salt. The salt can be used for treating diseases which respond to dopamine-D3 ligands. It is very stable at a low pH and is therefore especially suitable for oral administration.

公开(公告)号：HUT75709A

公开(公告)日：1997-05-28

申请号：HU9603068

申请日：1995-04-26

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  DE POTZOLLI BERND ,  HAUPT ANDREAS ,  JANITSCHKE LOTHAR ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MUELLER STEFAN ,  RITTER KURT ,  THYES MARCO ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61P35/00 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06

Abstract: Compounds of the formulawhere R1, R2, R3 and R4 have the meaning stated in the description, and a process for preparing them are described. The compounds are suitable as starting material for synthesizing substances which are active against tumors.

公开(公告)号：NO964688A

公开(公告)日：1997-01-02

申请号：NO964688

申请日：1996-11-05

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  JANITSCHKE LOTHAR ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MULLER STEFAN ,  POTZOLLI BERND DE ,  RITTER KURT ,  THYES MARCO ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61K38/08 ,  A61P35/00 ,  C07K1/08 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06 ,  C07K14/52

CPC classification number: C07K7/06 ,  A61K38/00 ,  C07K5/101 ,  Y02P20/55

公开(公告)号：CA2189691A1

公开(公告)日：1995-11-16

申请号：CA2189691

申请日：1995-04-26

Applicant: BASF AG

Inventor： AMBERG WILHELM ,  BERNARD HARALD ,  BUSCHMANN ERNST ,  HAUPT ANDREAS ,  JANITSCHKE LOTHAR ,  JANSSEN BERND ,  KARL ULRICH ,  KLING ANDREAS ,  MUELLER STEFAN ,  DE POTZOLLI BERND ,  RITTER KURT ,  THYES MARCO ,  ZIERKE THOMAS

IPC: A61K38/00 ,  A61P35/00 ,  C07K5/10 ,  C07K5/103 ,  C07K7/06

Abstract: Compounds of formula (I) are disclosed, wherein R1, R2, R3, and R4 have the meanings indicated in the description, as well as a process for the production of these compounds. The compounds are suitable for use as starting material for the synthesis of substances which have anti-tumour properties.

公开(公告)号：CA2167406A1

公开(公告)日：1995-01-26

申请号：CA2167406

申请日：1994-06-28

Applicant: BASF AG

Inventor： VIERGUTZ WOLFGANG ,  THYES MARCO

IPC: C07D471/08

Abstract: Described is an improved method of preparing N,N'-dibenzylbispidine by reacting N-benzylpiperidone with benzylamine and subsequent reduction.

公开(公告)号：DE3644462A1

公开(公告)日：1988-07-07

申请号：DE3644462

申请日：1986-12-24

Applicant: BASF AG

Inventor： THYES MARCO ,  STEINER GERD

IPC: B01J27/125 ,  C07B31/00 ,  C07B41/06 ,  C07B61/00 ,  C07C45/00 ,  C07C45/46 ,  C07C45/65 ,  C07C49/675 ,  C07C49/697 ,  C07C49/755 ,  C07C67/00

Abstract: 5H-Dibenzo[a,d]cyclohepten-5-ones (I) (I) (A and B being radicals for completing aromatic ring systems) are prepared by converting (Z)-2-(2-arylethenyl)arylcarboxylic acids (II) (II) or E/Z-isomer mixtures thereof with a halogenating agent for carboxylic acids at from (-30 DEG ) to +120 DEG C. to the corresponding carbonyl halides (III) (III) where X is halogen, and cyclizing said carbonyl halides at from 0 DEG to 100 DEG C. in the presence of a Lewis acid.

公开(公告)号：CA1229597A

公开(公告)日：1987-11-24

申请号：CA445508

申请日：1984-01-18

Applicant: BASF AG

Inventor： ROSSY PHILLIP A ,  THYES MARCO ,  FRANKE ALBRECHT ,  KOENIG HORST ,  LEHMANN HANS D ,  GRIES JOSEF ,  FRIEDRICH LUDWIG ,  LENKE DIETER

IPC: A61K31/50 ,  A61K31/502 ,  A61K31/535 ,  A61K31/55 ,  A61P1/04 ,  A61P7/02 ,  A61P9/12 ,  C07D237/04 ,  C07D237/14 ,  C07D237/26 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14 ,  C07D521/00 ,  C07D237/00

Abstract: This invention relates to the preparation of novel 6-(acylaminoaryl)-3(2H)-pyridazinones of the formula (I) where the substituents on the phenylene radical are meta or para to one another, A and B are each hydrogen or together form a bond, R1 and R2 are each hydrogen or C1-C3-alkyl, or, where A and B are hydrogen, together form a C1-C4-alkylene radical, R3 is straight-chain C1-C4 alkylene which can be substituted by 1 or 2 C1-C5-alkyl groups, and R4 is a) pyrrol-1-yl, imidazol-1-yl, pyrazol-1-yl of 1,2,4triazol-1-yl, or b) a group of the formula II (II) c) a group of the formula III (III) d) a group of the formula IV -NR10R11 (IV) e) a group of the formula V (V) f) a group of the formula VI (VI) These compounds inhibit thrombocyte aggregation and gastric secretion and have hypotensive and positively inotropic properties.