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公开(公告)号:ES2178676T3
公开(公告)日:2003-01-01
申请号:ES95926898
申请日:1995-07-14
Applicant: BASF AG
Inventor: HELLENDAHL BEATE , LANSKY ANNEGRET , MUNSCHAUER RAINER , BIALOJAN SIEGFRIED , UNGER LILIANE , TESCHENDORF HANS-JURGEN
IPC: C07D239/26 , A61K31/505 , A61K31/506 , A61P25/16 , A61P25/24 , A61P25/26 , C07D239/38 , C07D239/46 , C07D239/56 , C07D239/60 , C07D401/00 , C07D401/12
Abstract: The present invention relates to the use of pyrimidine compounds of the following formula:wherein R1, R2, R3, A, B and Ar have the meanings indicated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D3 ligands.
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公开(公告)号:ES2178455T3
公开(公告)日:2002-12-16
申请号:ES99938298
申请日:1999-07-20
Applicant: BASF AG
Inventor: STEINER GERD , HOGER THOMAS , UNGER LILIANE , TESCHENDORF HANS-JURGEN , JUCHELKA FRIEDER
IPC: A61K31/425 , A61K31/428 , A61P25/00 , C07D417/06
Abstract: Compounds of the formula I:in which R1, R2, R3 and R4 have the meanings stated in the description, are described.The novel compounds are suitable for controlling diseases.
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公开(公告)号:AU749539B2
公开(公告)日:2002-06-27
申请号:AU9068398
申请日:1998-07-23
Applicant: BASF AG
Inventor: STEINER GERD , DULLWEBER UTA , STARCK DOROTHEA , BACH ALFRED , WICKE KARSTEN , TESCHENDORF HANS-JURGEN , GARCIA-LADONA FRANCISCO JAVIER , EMLING FRANZ
IPC: A61K31/435 , A61P25/24 , C07D495/14
Abstract: 3-Substituted 3,4,5,7-tetrahydropyrrolo[3',4':4,5]thieno-[2,3-d]pyrimidine derivatives of the formula Iin which the substituents have the meanings stated in the description, their preparation and their use as drugs.
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公开(公告)号:SK7112001A3
公开(公告)日:2001-12-03
申请号:SK7112001
申请日:1999-11-12
Applicant: BASF AG
Inventor: STEINER GERD , MUNSCHAUER RAINER , GROSS GERHARD , TRAUT MARTIN , UNGER LILIANE , TESCHENDORF HANS-JURGEN
IPC: C07D403/06 , A61K31/403 , A61K31/4045 , A61K31/407 , A61K31/4184 , A61K31/424 , A61K31/427 , A61K31/4709 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/517 , A61K31/519 , A61K31/542 , A61P25/00 , A61P25/28 , A61P25/30 , A61P25/36 , C07D209/52 , C07D407/12 , C07D409/12 , C07D417/06 , C07D471/04 , C07D498/04 , C07D513/04 , A61K31/416 , A61K31/428 , A61K31/538
Abstract: The invention relates to the use of N-substituted 3-azabicycloalkane derivatives of formula (I), wherein B, R , R and n have the meanings given in the description, for combating diseases of addiction and other diseases of the central nervous system.
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公开(公告)号:TR200100476T2
公开(公告)日:2001-07-23
申请号:TR200100476
申请日:1999-07-20
Applicant: BASF AG
Inventor: STEINER GERD , HOEGER THOMAS , UNGER LILIANE , TESCHENDORF HANS-JURGEN , JUCHELKA FRIEDER
IPC: A61K31/4184 , A61P25/20 , A61P25/24 , A61P25/30 , C07D403/06
Abstract: The invention relates to compounds of formula (1), wherein R , R and R have the meaning cited in the description. The novel substances are suitable for use in disease control.
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公开(公告)号:TR200100475T2
公开(公告)日:2001-06-21
申请号:TR200100475
申请日:1999-07-20
Applicant: BASF AG
Inventor: STEINER GERD , HOGER THOMAS , UNGER LILIANE , TESCHENDORF HANS-JURGEN , JUCHELKA FRIEDER
IPC: A61K31/425 , A61K31/428 , A61P25/00 , C07D417/06
Abstract: Compounds of the formula I:in which R1, R2, R3 and R4 have the meanings stated in the description, are described.The novel compounds are suitable for controlling diseases.
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7.
公开(公告)号:NZ334350A
公开(公告)日:2000-07-28
申请号:NZ33435097
申请日:1997-08-22
Applicant: BASF AG
Inventor: STEINER GERD , LUBISCH WILFRIED , BACH ALFRED , EMLING FRANZ , WICKE KARSTEN , TESCHENDORF HANS-JURGEN , BEHL BERTHOLD , CHEETHAM SHARON , KERRRIGAN FRANK
IPC: A61K31/435 , A61K31/519 , A61P25/24 , A61P43/00 , C07D211/00 , C07D239/00 , C07D333/00 , C07D495/14 , A61K31/495
Abstract: In the compounds of formula I: R1 is a hydrogen atom, a C1-C4 alkyl group, an acetyl or benzoyl group, a phenylalkyl C1-C4 radical (the aromatic optionally being substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano or nitro groups), a naphthylalkyl C1-C3 group, a phenylalkanone C2-C3 radical or a phenylcarbamoylalkyl C2 radicalgroup (wherein the phenyl group can be substituted by halogen). R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group, each of which can optionally be mono-di- or tri-substituted by halogen atoms, C1-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups, and each of these may be fused to a benzene nucleus optionally mono- or di-substituted by halogen atoms, C1-C4 alkyl, hydroxyl, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups, and optionally containing 1 nitrogen atom, or a 5- or 6-member ring which can contain between 1 and 2 oxygen atoms or be substituted by a phenyl-C1-C2 alkyl or alkoxy group, wherein the phenyl group can be substituted by halogen, a methyl, trifluoromethyl or methoxy group; A is NH or an oxygen atom; B is hydrogen or methyl; C is hydrogen, methyl or hydroxyl; X is a nitrogen atom; Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH; Z is a nitrogen atom, a carbon atom or CH, wherein the bond between Y and Z can also be a double bond; and n is the number 2, 3 or 4. These compounds are suitable as medicaments for treating diseases in which the serotonin concentration is reduced and in which the activity of the presynaptic receptors 5-HT1B, 5-HT1A, 5HT1D is to be blocked within a therapeutic context without greatly influencing other receptors.
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公开(公告)号:SK174399A3
公开(公告)日:2000-05-16
申请号:SK174399
申请日:1998-05-29
Applicant: BASF AG
Inventor: STEINER GERD , DULLWEBER UTA , STARCK DOROTHEA , BACH ALFRED , WICKE KARSTEN , TESCHENDORF HANS-JURGEN , GARCIA-LADONA FRANCISCO JAVIER , EMLING FRANZ
IPC: A61K31/505 , A61K31/519 , A61P25/00 , A61P25/24 , A61P43/00 , C07D495/14
Abstract: PCT No. PCT/EP98/03231 Sec. 371 Date Dec. 8, 1999 Sec. 102(e) Date Dec. 8, 1999 PCT Filed May 29, 1998 PCT Pub. No. WO98/56793 PCT Pub. Date Dec. 17, 19983-Substituted 3,4,5,6,7,8-hexahydropyrido [3',4':4,5]-thieno[2,3-d]pyrimidine derivatives of the formula I where R1 is a hydrogen atom, a C1-C4-alkyl group, an acetyl group, a phenylalkyl C1-C4 radical, the aromatic system being unsubstituted or substituted by halogen, C1-C4-alkyl, trifluoromethyl, hydroxyl, C1-C4-alkoxy, amino, cyano or nitro groups, or is a phenylalkanone radical, it being possible for the phenyl group to be substituted by halogen, R2 is a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluoromethoxy, hydroxyl, C1-C4-alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and which may be fused to a benzene nucleus which can be unsubstituted or mono- or disubstituted by halogen atoms, C1-C4-alkyl, hydroxyl, trifluoromethyl, C1-C4-alkoxy, amino, cyano or nitro groups and may contain 1 nitrogen atom, or to a 5- or 6-membered ring which may contain 1-2 oxygen atoms, A is NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2-CH, Z is a nitrogen atom, carbon atom or CH, it also being possible for the linkage between Y and Z to be a double bond, and n is 2, 3 or 4, and the physiologically tolerated salts thereof.
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公开(公告)号:BG103122A
公开(公告)日:1999-09-30
申请号:BG10312299
申请日:1999-01-27
Applicant: BASF AG
Inventor: STEINER GERD , LUBISCH WILFRIED , BACH ALFRED , EMLING FRANZ , WICKE KARSTEN , TESCHENDORF HANS-JURGEN , BEHL BERTHOLD , KERRIGAN FRANK , CHEETHAM SHARON
IPC: A61K31/435 , A61K31/519 , A61P25/24 , A61P43/00 , C07D211/00 , C07D239/00 , C07D333/00 , C07D495/14
Abstract: The 3-substituted 3,4,5,6,7.8-hexahydro-pyrido[4', 3':4,5]-thieno [2,3-d] pyrimidine derivatives can be used asmedicamentous forms for diseases where there is redud serotoninconcentration and where, within the therapy, the activity of thepresnaptic receptors 5-HT1B-, 5-HT1A-, 5-HT1D-, should be blockedwithout seriously affecting any other receptors. Depression is anexample for such morbid state. The compounds have formulain which R1 is hydrogen, C1-C4-alkyl group, acetyl, benzoyl,phenylalkyl-C1-C4-residue where the aromatic residue is optionallysubstituted with halogen, C1-C4-alkyl, trifluoromethyl, hydroxy-,C1-C4-alkoxy-, amino-, cyano- or nitrogroups or isnaphtalene-C1-C4-alkyl residue, phenylalkanon-C2-C4-residue orphenylcarbamoylalkyl-C2-residue where the phenyl group can besubstituted by halogen; R2 optionally is mono-, di- ortrisubstituted with halogen atoms, C1-C4-alkyl, trifluoromethyl,trifluormethoxy, hydroxy, C1-C4-alkoxy, amino-, monomethylamino-,diethylamino-, cyano- or nitrogroup, phenyl, pyridyl, pyrimidinylor pyrasinyl reside which can optionally be ringed by one benzenering which optionally can be mono- or disubstituted with halogenatom, C1-C4-alkyl, hydroxy, trifluormethyl, C1-C4-alkoxy, amino-,cyano- or nitrogroup, and optionally can contain one nitrogen atomor be ringed by 5- or 6-member ring which can contain one to twooxygen atoms, or can be substituted by phenyl-C1-C2-alkyl, oralkoxygroup, respectively, where the phenyl residue can besubstituted with halogen, methyl, trifluormethyl or methoxygroup.A is NH or oxygen, B is hydrogen or methyl, C is hydrogen, methylor hydroxy, X is nitrogen atom, Y is the group CH2, CH2- CH2,CH2-CH2-CH2 or CH2-CH, Z is nitrogen atom, carbon or CH where thebond between Y and Z can be double, n has the value of 2, 3 or 4.The invention also relates to physiologically acceptable salts ofthe above compounds.6 claims
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公开(公告)号:CZ75999A3
公开(公告)日:1999-06-16
申请号:CZ75999
申请日:1997-08-22
Applicant: BASF AG
Inventor: STEINER GERD , LUBISCH WILFRIED , BACH ALFRED , EMLING FRANZ , WICKE KARSTEN , TESCHENDORF HANS-JURGEN , BEHL BERTHOLD , CHEETHAM SHARON , KERRRIGAN FRANK
IPC: A61K31/435 , A61K31/519 , A61P25/24 , A61P43/00 , C07D211/00 , C07D239/00 , C07D333/00 , C07D495/14
Abstract: A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidine compound of formula IwhereinR1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl,R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring,A is NH or oxygen,B is hydrogen or methyl,C is hydrogen, methyl or hydroxyl,X is nitrogen,Y is CH2, CH2-C2, CH2-C2-CH2 or CH2-CH,Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, andn is 2, 3 or 4,or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.
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