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31. 发明专利

PL334899A1 NOVEL 2-AMINO-SUBSTITUTED PYRIDINES 未知
公开(公告)号：PL334899A1
公开(公告)日：2000-03-27
申请号：PL33489998
申请日：1998-01-23
申请人： BAYER AG
发明人： SCHMECK CARSTEN , BRANDES ARNDT , LOEGERS MICHAEL , SCHMIDT GUNTER , BREMM KLAUS-DIETER , BISCHOFF HILMAR , SCHMIDT DELF , SCHUHMACHER JOACHIM
IPC分类号： A61K31/4409 , A61K31/451 , A61P3/06 , A61P9/10 , C07D213/74 , C07D401/04 , A61K31/44
摘要： The invention relates to novel 2-amino-substituted pyridines which are produced by first converting corresponding pyridine aldehydes into the corresponding hydroxides by means of metal-organic compounds such as Grignard compounds, and then reducing said hydroxides to a deshydroxy compound. The novel 2-amino-substituted pyridines are suitable for use as active ingredients in medicaments, particularly those used in the treatment of arteriosclerosis

32. 发明专利

TR199901857T2 未知
公开(公告)号：TR199901857T2
公开(公告)日：1999-10-21
申请号：TR9901857
申请日：1998-01-23
申请人： BAYER AG
发明人： SCHMECK CARSTEN , BRANDES ARNDT , LOEGERS MICHAEL , SCHMIDT GUNTER , BREMM KLAUS-DIETER , BISCHOFF HILMAR , SCHMIDT DELF , SCHUHMACHER JOACHIM
IPC分类号： A61K31/4409 , A61K31/451 , A61P3/06 , A61P9/10 , C07D213/74 , C07D401/04 , A61K31/44
摘要： The invention relates to novel 2-amino-substituted pyridines which are produced by first converting corresponding pyridine aldehydes into the corresponding hydroxides by means of metal-organic compounds such as Grignard compounds, and then reducing said hydroxides to a deshydroxy compound. The novel 2-amino-substituted pyridines are suitable for use as active ingredients in medicaments, particularly those used in the treatment of arteriosclerosis

33. 发明专利

HU9701158A1 BICYCLIC CONDENSED PYRIDINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, PROCESS FOR PRODUCING THEM AND THEIR USE 未知
公开(公告)号：HU9701158A1
公开(公告)日：1999-09-28
申请号：HU9701158
申请日：1997-07-07
申请人： BAYER AG
发明人： ANGERBAUER ROLF , BISCHOFF HILMAR , BRANDES ARNDT , BREMM KLAUS-DIETER , LOEGERS MICHAEL , SCHMECK CARSTEN , SCHMIDT DELF , SCHMIDT GUENTER , SCHUHMACHER JOACHIM
IPC分类号： C07D221/04 , A61K31/435 , A61K31/44 , A61P3/06 , A61P9/00 , A61P9/10 , C07D221/16
摘要： Bicyclic condensed pyridine compounds of formula (I) and their salts and N-oxides are new. A = 6-10C aryl optionally substituted by 1-3 halo, OH, CF3, OCF3 or 1-7C alkyl, acyl, hydroxyalkyl or alkoxy groups, or by one NR3R4 group; R3, R4 = independently H, phenyl or 1-6C alkyl; D = R5-T- or (R6)(R7)(R8)C-; R5, R6 = independently 3-8C cycloalkyl, 6-10C aryl or a 5-7 membered aromatic optionally benzocondensed heterocycle containing 1-3 S, N and/or O heteroatoms, optionally substituted by 1-3 independent halo, OH, CF3, OCF3, COOH, 1-6C alkyl, alkoxy, acyl or alkoxycarbonyl groups, or is substituted by phenyl, phenoxy or thiophenyl groups, themselves optionally substituted by halo, CF3 or OCF3, or the ring systems may be substituted by an NR9R10 group; R9, R10 = as for R3, R4; T = 1-10C alkylene or alkenylene, optionally substituted by 1 or 2 OH groups; R7 = H or halo; R8 = H, halo, azido, CF3, OCF3, OH, 1-5C alkoxy or NR11R12; R11, R12 = as for R3, R4; or R7+R8 = a carbonyl group; E = 3-8C cycloalkyl or 1-8C alkyl which is optionally substituted by 3-8C cycloalkyl or OH; R1+R2 = 1-8C alkylene group which is annelated to a phenyl ring and is substituted by CO, a group of formula (i) or OR13; a = 1-3; R13 = H, 1-6C alkyl, acyl or alkoxycarbonyl or a group of formula Si(R14)(R15)(R16); R14, R15, R16 = independently 1-6C alkyl or phenyl; Both ring systems may be substituted by 1-3 independent halo, COOH or 1-6C alkyl, alkoxy or alkoxycarbonyl groups.

34. 发明专利

HRP970330A2 CYCLOALKANO PYRIDINES 未知
公开(公告)号：HRP970330A2
公开(公告)日：1998-04-30
申请号：HRP970330
申请日：1997-06-17
申请人： BAYER AG
发明人： SCHMIDT GUNTER , BRANDES ARNDT , ANGERBAUER ROLF , LOEGERS MICHAEL , MUELLER-GLIEMANN MATTHIAS , SCHMECK CARSTEN , BREMM KLAUS-DIETER , BISCHOFF HILMER , SCHMIDT DELF , SCHUHMACHER JOACHIM , GIERA HENRY , PAULSEN HOLGER , NAAB PAUL , CONRAD MICHAEL , STOLTEFUSS JUERGEN
IPC分类号： A61K31/435 , A61K31/47 , A61K31/4709 , C07D215/20 , A61K31/473 , A61P3/06 , A61P9/00 , A61P9/10 , C07C225/18 , C07D215/22 , C07D215/36 , C07D215/40 , C07D215/54 , C07D221/04 , C07D221/16 , C07D221/20 , C07D405/06 , C07D491/056 , C07D491/08 , C07D491/10 , C07D491/107 , C07F7/18
摘要： Cycloalkano-pyridine compounds of formula (I) and their salts and N-oxides are new. A = 6-10C aryl (optionally up to penta-substituted by halo, NO2, OH, CF3, OCF3, 1-7C alkyl, 1-7C acyl, 1-7C hydroxyalkyl, 1-7C alkoxy or NR3R4); R3, R4 = H, phenyl or 1-6C alkyl; D = 6-10C aryl (optionally substituted by phenyl, halo, NO2, CF3 or OCF3), LR5, C(R6)(R7)R8 or XVTR9; R9 = 3-6C cycloalkyl, 6-10C aryl or 5-7 membered, optionally benzo-condensed, optionally unsaturated mono- bi or tri-cyclic heterocycle with 1-4 S, N and/or O (all optionally up to penta-substituted by halo, NO2, OH, CF3, CN, COOH, OCF3, 1-6C alkyl, 1-6C acyl, 1-6C alkylthio, 1-6C alkoxy or alkoxycarbonyl, 6-10C aryl (optionally substituted by aryl or CF3) or 5-7 membered, optionally benzo-condensed, heteroaryl with 1-3 N, O and/or S heteroatoms), and/or OR10, SR11, SO2R12 or NR13, R14; R10-R12 = 6-10C aryl (optionally mono- to di-substituted, by phenyl, halo or 1-6C alkyl); R5, R6 = as for R9 or a group of formula (a) or (b); R7 = H or halo; R8 = H, halo, N3, CF3, OH, OCF3, 1-6C alkoxy, 1-6C alkyl or NR15R16; or R7+R8 = O or NR17; R17 = H, 1-6C alkyl, 1-6C acyl or 1-6C alkoxy; L = 1-8C alkylene or 2-8C alkenylene (both optionally mono- or di- substituted by OH); T, X = bond or 1-8C alkylene, provided they are not both a bond; V = O, S or NR18; R13-R16, R18 = as R3, R4; E = 3-8C cycloalkyl, 1-8C alkyl (optionally substituted by 3-8C cycloalkyl or OH) or phenyl (optionally substituted by halo or CF3); R1+R2 = 1-7C alkylene substituted by carbonyl and/or Z, and optionally also geminal, optionally substituted by up to 6 Z' and/or up to 5 Z", and/or 1,2-(CH2)c, SO2C6H5, (CO)dNR23R24 or O; and/or a spiro-bonded group Zb of formula (g)-(k); Z = OR19, or a group of formula (c)-(f); a, b = 1-3; R19 = H, 3-7C cycloalkyl, up to 8C silylalkyl, 1-8C alkyl (optionally substituted by OH, 1-6C alkoxy or Ar), (where alkyl is optionally substituted by OR22) ÄsicÜ, 1-20C acyl or benzoyl (optionally substituted by halo, CF3, NO2 or OCF3) or 1-8C fluoroacyl (with 1-9F); R20, R21 = H, phenyl or 1-6C alkyl; or R20+R21 = 3-6C cycloalkyl; Z" = phenyl, benzoyl, thiophenyl or sulphonylbenzyl (all optionally substituted by halo, CF3, OCF3 or NO2); Z' = halo, NO2, N3, OH, CF3, CN, NC, COOH, 3-7C cycloalkyl, 3-7C cycloalkyloxy, 1-6C alkyl (optionally mono- or di-substituted by OH, benzyloxy, CF3, benzoyl, alkoxy, oxyacyl or carboxy each with 1-4C, and/or phenyl (itself optionally substituted by halo, CF3 or OCF3)), 1-6C alkylthio, 1-6C alkoxy or alkoxycarbonyl; R22 = 1-4C acyl or benzyl; Ar = phenyl (optionally substituted by halo, NO2, CF3, OCF3 or phenyl- or tetrazolyl-substituted phenyl); c = 1-4; d = 0 or 1; R23, R24 = H, 3-6C cycloalkyl, 1-6C alkyl, benzyl or phenyl (optionally mono- or di-substituted by halo, CF3, CN, phenyl or NO2); W= O or S; Y+Y' = 2-6C alkylene; e = 1-7; f = 1 or 2; R25-R31 = H, CF3, phenyl, halo, 1-6C alkyl or 1-6C alkoxy; or R25+R26 or R27+R28 = 1-6C alkylene or W-(CH2)h-W; h = 2-8; R32+R33 = 3-7-membered heterocycle containing O, S, SO, SO2 or NR34; R34 = H, phenyl, benzyl or 1-4C alkyl. Also claimed are the following intermediates: 3-amino-3-cyclopentyl-1-(4-trifluoromethylphenyl)propenone; 2-cyclopentyl-4-(4-fluorophenyl)-7,7-dimethyl-3-(trifluoromethylbenzoy l)-4,6,7,8-tetrahydro-1H-quinolin-5-one; 2-cyclopentyl-4-(4-fluorophenyl)-7,7-dimethyl-3-(4-trifluoromethylbenz oyl)-7,8-dihydro-6H-quinolin-5-one; Ä2-cyclopentyl-4-(4-fluorophenyl)-5-hydroxy-7,7-dimethyl-5,6,7,8-tetra hydroquinolin-3-ylÜ- (4-trifluoromethylphenyl)-methanone; Ä5-(tert. butyldimethylsilanyloxy)-2-cyclopentyl-4-(4-fluorophenyl)-7,7-dimethyl -5,6,7,8-tetrahydroquinolin-3-ylÜ-(4-trifluoromethylphenyl)-me thanone; Ä5-(tert. butyldimethylsilanyloxy)-2-cyclopentyl-4-(4-fluorophenyl)-7,7-dimethyl -5,6,7,8-tetrahydroquinolin-3-ylÜ-(4-trifluoromethylphenyl)-me thanol; and 5-(tert. butyldimethylsilanyloxy)-2-cyclopentyl-4-(4-fluorophenyl)-3-Äfluoro-(4 -trifluoromethylphenyl)-methylÜ-7,7-dimethyl-5,6,7,8-tetrahydr oquinoline.

35. 发明专利

MX9705083A CICLOALCANO-PIRIDINAS, PROCEDIMIENTO PARA SU OBTENCION Y MEDICAMENTOS QUE LAS CONTIENEN. 未知
公开(公告)号：MX9705083A
公开(公告)日：1998-01-31
申请号：MX9705083
申请日：1997-07-07
申请人： BAYER AG
发明人： SCHMIDT GUNTER , BRANDES ARNDT , ANGERBAUER ROLF , LOEGERS MICHAEL , GLIEMANN MATTHIAS MUELLER , SCHMECK CARSTEN , BREMM KLAUS DIETER , BISCHOFF HILMAR , SCHMIDT DELF
IPC分类号： C07C225/18 , C07D215/22 , C07D215/36 , C07D215/40 , C07D221/04 , C07D221/16 , C07D221/20 , C07D405/06 , C07D491/08 , C07D491/10 , C07F7/18 , C07D235/00
摘要： Las cicloalcano-piridinas se obtienen haciendo reaccionar los correspondientes cicloalcano-piridin-aldehidos con los compuestos metalorgánicos o reactivos de Wittig o de Grignard adecuados o haciendo reaccionar compuestos del tipo ciclo-alcano-piridinalcoholes con unos compuestos de bromo adecuados y variando, dado el caso, los grupos funcionales de modo correspondiente. Las cicloalcano-piridinas son adecuadas como sustancias activas en medicamentos, en especial en medicamentos para el tratamiento de la hiperlipoproteinemia y la arterioesclerosis.

36. 发明专利

NO973145L 未知
公开(公告)号：NO973145L
公开(公告)日：1998-01-09
申请号：NO973145
申请日：1997-07-07
申请人： BAYER AG
发明人： SCHMIDT GUNTER , BRANDES ARNDT , ANGERBAUER ROLF , LOEGERS MICHAEL , MUELLER-GLIEMANN MATTHIAS , SCHMECK CARSTEN , BREMM KLAUS DIETER , BISCHOFF HILMAR , SCHMIDT DELF , SCHUHMACHER JOACHIM , GIERA HENRY , PAULSEN HOLGER , NAAB PAUL , CONRAD MICHAEL , STOLTEFUSS JUERGEN
IPC分类号： A61K31/435 , A61K31/47 , C07D215/20 , A61K31/4709 , A61K31/473 , A61P3/06 , A61P9/00 , A61P9/10 , C07C225/18 , C07D215/22 , C07D215/36 , C07D215/40 , C07D215/54 , C07D221/04 , C07D221/16 , C07D221/20 , C07D405/06 , C07D491/056 , C07D491/08 , C07D491/10 , C07D491/107 , C07F7/18
摘要： Cycloalkano-pyridine compounds of formula (I) and their salts and N-oxides are new. A = 6-10C aryl (optionally up to penta-substituted by halo, NO2, OH, CF3, OCF3, 1-7C alkyl, 1-7C acyl, 1-7C hydroxyalkyl, 1-7C alkoxy or NR3R4); R3, R4 = H, phenyl or 1-6C alkyl; D = 6-10C aryl (optionally substituted by phenyl, halo, NO2, CF3 or OCF3), LR5, C(R6)(R7)R8 or XVTR9; R9 = 3-6C cycloalkyl, 6-10C aryl or 5-7 membered, optionally benzo-condensed, optionally unsaturated mono- bi or tri-cyclic heterocycle with 1-4 S, N and/or O (all optionally up to penta-substituted by halo, NO2, OH, CF3, CN, COOH, OCF3, 1-6C alkyl, 1-6C acyl, 1-6C alkylthio, 1-6C alkoxy or alkoxycarbonyl, 6-10C aryl (optionally substituted by aryl or CF3) or 5-7 membered, optionally benzo-condensed, heteroaryl with 1-3 N, O and/or S heteroatoms), and/or OR10, SR11, SO2R12 or NR13, R14; R10-R12 = 6-10C aryl (optionally mono- to di-substituted, by phenyl, halo or 1-6C alkyl); R5, R6 = as for R9 or a group of formula (a) or (b); R7 = H or halo; R8 = H, halo, N3, CF3, OH, OCF3, 1-6C alkoxy, 1-6C alkyl or NR15R16; or R7+R8 = O or NR17; R17 = H, 1-6C alkyl, 1-6C acyl or 1-6C alkoxy; L = 1-8C alkylene or 2-8C alkenylene (both optionally mono- or di- substituted by OH); T, X = bond or 1-8C alkylene, provided they are not both a bond; V = O, S or NR18; R13-R16, R18 = as R3, R4; E = 3-8C cycloalkyl, 1-8C alkyl (optionally substituted by 3-8C cycloalkyl or OH) or phenyl (optionally substituted by halo or CF3); R1+R2 = 1-7C alkylene substituted by carbonyl and/or Z, and optionally also geminal, optionally substituted by up to 6 Z' and/or up to 5 Z", and/or 1,2-(CH2)c, SO2C6H5, (CO)dNR23R24 or O; and/or a spiro-bonded group Zb of formula (g)-(k); Z = OR19, or a group of formula (c)-(f); a, b = 1-3; R19 = H, 3-7C cycloalkyl, up to 8C silylalkyl, 1-8C alkyl (optionally substituted by OH, 1-6C alkoxy or Ar), (where alkyl is optionally substituted by OR22) ÄsicÜ, 1-20C acyl or benzoyl (optionally substituted by halo, CF3, NO2 or OCF3) or 1-8C fluoroacyl (with 1-9F); R20, R21 = H, phenyl or 1-6C alkyl; or R20+R21 = 3-6C cycloalkyl; Z" = phenyl, benzoyl, thiophenyl or sulphonylbenzyl (all optionally substituted by halo, CF3, OCF3 or NO2); Z' = halo, NO2, N3, OH, CF3, CN, NC, COOH, 3-7C cycloalkyl, 3-7C cycloalkyloxy, 1-6C alkyl (optionally mono- or di-substituted by OH, benzyloxy, CF3, benzoyl, alkoxy, oxyacyl or carboxy each with 1-4C, and/or phenyl (itself optionally substituted by halo, CF3 or OCF3)), 1-6C alkylthio, 1-6C alkoxy or alkoxycarbonyl; R22 = 1-4C acyl or benzyl; Ar = phenyl (optionally substituted by halo, NO2, CF3, OCF3 or phenyl- or tetrazolyl-substituted phenyl); c = 1-4; d = 0 or 1; R23, R24 = H, 3-6C cycloalkyl, 1-6C alkyl, benzyl or phenyl (optionally mono- or di-substituted by halo, CF3, CN, phenyl or NO2); W= O or S; Y+Y' = 2-6C alkylene; e = 1-7; f = 1 or 2; R25-R31 = H, CF3, phenyl, halo, 1-6C alkyl or 1-6C alkoxy; or R25+R26 or R27+R28 = 1-6C alkylene or W-(CH2)h-W; h = 2-8; R32+R33 = 3-7-membered heterocycle containing O, S, SO, SO2 or NR34; R34 = H, phenyl, benzyl or 1-4C alkyl. Also claimed are the following intermediates: 3-amino-3-cyclopentyl-1-(4-trifluoromethylphenyl)propenone; 2-cyclopentyl-4-(4-fluorophenyl)-7,7-dimethyl-3-(trifluoromethylbenzoy l)-4,6,7,8-tetrahydro-1H-quinolin-5-one; 2-cyclopentyl-4-(4-fluorophenyl)-7,7-dimethyl-3-(4-trifluoromethylbenz oyl)-7,8-dihydro-6H-quinolin-5-one; Ä2-cyclopentyl-4-(4-fluorophenyl)-5-hydroxy-7,7-dimethyl-5,6,7,8-tetra hydroquinolin-3-ylÜ- (4-trifluoromethylphenyl)-methanone; Ä5-(tert. butyldimethylsilanyloxy)-2-cyclopentyl-4-(4-fluorophenyl)-7,7-dimethyl -5,6,7,8-tetrahydroquinolin-3-ylÜ-(4-trifluoromethylphenyl)-me thanone; Ä5-(tert. butyldimethylsilanyloxy)-2-cyclopentyl-4-(4-fluorophenyl)-7,7-dimethyl -5,6,7,8-tetrahydroquinolin-3-ylÜ-(4-trifluoromethylphenyl)-me thanol; and 5-(tert. butyldimethylsilanyloxy)-2-cyclopentyl-4-(4-fluorophenyl)-3-Äfluoro-(4 -trifluoromethylphenyl)-methylÜ-7,7-dimethyl-5,6,7,8-tetrahydr oquinoline.

39. 发明专利

NO971269L 未知
公开(公告)号：NO971269L
公开(公告)日：1997-09-22
申请号：NO971269
申请日：1997-03-19
申请人： BAYER AG
发明人： SCHMIDT GUNTER , ANGERBAUER ROLF , BRANDES ARNDT , LOEGERS MICHAEL , MUELLER-GLIEMANN MATTHIAS , BISCHOFF HILMAR , SCHMIDT DELF , WOHLFEIL STEFAN
IPC分类号： A61K31/435 , A61K31/44 , C07D221/18 , A61K31/4418 , A61K31/4427 , A61K31/455 , A61P3/06 , A61P9/10 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/53 , C07D401/06 , C07D417/06
摘要： 2,6-Diaryl-3-alkyl-4-(alkyl or alkenyl)-5-(alkyl or cycloalkyl)-pyridine derivatives of formula (I) and their salts are new. A, E = 6-10C aryl (optionally mono- to penta- substituted by halo, OH, CF3, OCF3, NO2, -NR R , 1-7C alkyl, 1-7C acyl, 1-7C hydroxyalkyl or 1-7C alkoxy); D = 1-8C hydroxyalkyl; L = 1-8C alkyl (optionally substituted by 3-8C cycloalkyl or OH) or 3-8C cycloalkyl; T = XR or COR ; R , R = 3-8C cycloalkyl, or 6-10C aryl or 5-7 membered optionally benzo-fused heteroaryl containing 1-3 S, N and/or O atoms (both optionally mono-, di- or trisubstituted by CF3, OCF3, halo, OH, COOH, NO2, 1-6C alkyl, 1-6C acyl, 1-6C alkoxy or ≤ 6C alkoxycarbonyl, Ar, OAr or SAr) and the cyclic groups are optionally substituted by NR R ; Ar = phenyl (optionally substituted by halo, CF3 or OCF3); X = alkyl or alkenyl with up to 10C (both optionally mono- or di- substituted by OH or halo) or CHR6; R = H, halo, SH, N3, CF3, OH, OCF3, 1-5C alkoxy or -NR R ; R , R , R -R = H, Ph or 1-6C alkyl.

40. 发明专利

NO971269A 未知
公开(公告)号：NO971269A
公开(公告)日：1997-09-22
申请号：NO971269
申请日：1997-03-19
申请人： BAYER AG
发明人： SCHMIDT GUNTER , ANGERBAUER ROLF , BRANDES ARNDT , LOEGERS MICHAEL , MUELLER-GLIEMANN MATTHIAS , BISCHOFF HILMAR , SCHMIDT DELF , WOHLFEIL STEFAN
IPC分类号： C07D221/18 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/4427 , A61K31/455 , A61P3/06 , A61P9/10 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/53 , C07D401/06 , C07D417/06
CPC分类号： C07D213/30 , C07D213/38 , C07D213/50 , C07D401/06 , C07D417/06

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