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62. 发明专利

ZA976020B Heterocyclic-fused pyridines. 未知
公开(公告)号：ZA976020B
公开(公告)日：1998-02-02
申请号：ZA976020
申请日：1997-07-07
申请人： BAYER AG
发明人： SCHMECK CARSTEN , MULLER-GLIEMANN MATTHIAS , SCHMIDT GUNTER , BRANDES ARNDT , ANGERBAUER ROLF , LOGERS MICHAEL , BREMM KLAUS-DIETER , BISCHOFF HILMAR , SCHMIDT DELF , SCHUHMACHER JOACHIM
IPC分类号： C07D491/044 , A61K31/435 , A61K31/44 , A61K31/4418 , A61K31/445 , A61K31/451 , A61K31/55 , A61P3/06 , A61P9/10 , C07C229/14 , C07D211/86 , C07D211/90 , C07D213/80 , C07D401/04 , C07D471/04 , C07D491/04 , C07D491/20 , C07D493/14 , C07D495/04 , C07F7/18 , C07D
摘要： Condensed pyridine derivatives of formula (I), and their salts and N-oxides, are new. A = 6-10C aryl (optionally mono- to penta-substituted by halo, OH, CF3, OCF3, NO2, 1-7C alkyl, acyl, hydroxyalkyl or alkoxy, or NR3R4; D = XR5or C(R6)(R7)R8; R5, R6 = 3-8C cycloalkyl, 6-10C aryl, or 5-7 membered heteroaromatic (optionally benzocondensed containing up to 3 heteroatoms from N, O, S), (optionally mono- to penta- substituted by CF3, NO2, OCF3, halo, OH, COOH, 1-6C alkyl, acyl, alkoxy or alkoxycarbonyl, or Ar, OAr or SAr), where the rings are optionally substituted by NR9R10; Ar = phenyl optionally substituted by halo, CF3 or OCF3; X = 1-8C alkylene or alkenylene optionally mono- - di-substituted by OH; R7 = H or halo; R8 = H, halo, N3, CF3, OCF3, OH, 1-5C alkoxy or NR11R12; or R7+R8 = O; R3, R4, R9-R12 = H, phenyl or 1-6C alkyl; E = 3-8C cycloalkyl, or 1-8C alkyl (optionally substituted by 3-8C cycloalkyl or OH); R1+R2 = heterocyclic ring (formed from 1-6C alkylene, interrupted by O, S, SO2 or NR13, and optionally benzocondensed and containing a double bond) which is substituted by CO, OR14 or a group of formula (a), and optionally mono- to penta- substituted by 1-6C alkoxy or alkoxycarbonyl, CF3, halo, OH, carbonyl, Ar1, and/or optionally mono- to hexa- substituted by 3-8C cycloalkyl or cycloalkoxy, 1-6C alkyl (optionally substituted by OH, CF3, phenyl or 1-5C alkoxy) and/or optionally substituted by a spiro-residue of formula (b), (c) or (d); a = 1-3; Ar1 = phenyl (optionally substituted by halo, CF3, NO2, OH, or 1-6C alkoxy or alkoxycarbonyl); R13 = H, 1-6C alkyl, 1-6C acyl, or benzyl or phenyl (both optionally mono- or di-substituted by halo, OH, NO2, CF3, 1-6C alkyl or 1-6C acyl); R14 = H, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C acyl, ≤ 6C alkoxycarbonyl or SiR15R16R17; R15-R17 = phenyl or 1-6C alkyl; W = O or S; Y = 2-6C alkylene; c = 1-7; d = 1-2; R18-R24 = H, CF3, phenyl, halo, 1-6C alkyl or alkoxy; or R18+R19 or R20+R21 = 1-6C alkylene or W(CH2)fW; and f = 2-8.

63. 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.

64. 发明专利

TR199700583A2 未知
公开(公告)号：TR199700583A2
公开(公告)日：1998-01-21
申请号：TR9700583
申请日：1997-07-04
申请人： BAYER AG
发明人： BRANDES ARNDT , LOGERS MICHAEL , SCHMIDT GUNTER , ANGERBAUER ROLF , SCHMECK CARSTEN , BREMM KLAUS-DIETER , BISCHOFF HILMAR , SCHMIDT DELF , SCHUHMACHER JOACHIM
IPC分类号： C07D221/04 , A61K31/435 , A61K31/44 , A61P3/06 , A61P9/00 , A61P9/10 , C07D221/16 , C07D , A61K
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.

65. 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.

68. 发明专利

CA2209640A1 CYCLOALKANO-PYRIDINES 未知
公开(公告)号：CA2209640A1
公开(公告)日：1998-01-08
申请号：CA2209640
申请日：1997-07-04
申请人： BAYER AG
发明人： BISCHOFF HILMAR , SCHMECK CARSTEN , ANGERBAUER ROLF , STOLTEFUSS JUERGEN , CONRAD MICHAEL , SCHUHMACHER JOACHIM , SCHMIDT GUNTER , BRANDES ARNDT , MUELLER-GLIEMANN MATTHIAS , GIERA HENRY , BREMM KLAUS-DIETER , PAULSEN HOLGER , NAAB PAUL , L GERS MICHAEL , SCHMIDT DELF
IPC分类号： C07D215/20 , A61K31/435 , A61K31/47 , 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 , C07D401/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D473/00 , C07F7/10 , C07D405/14 , A61K31/495 , A61K31/535 , A61K31/695
摘要： The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hyperlipopro-teinaemia and arteriosclerosis.

69. 发明专利

SK36197A3 2-ARYLSUBSTITUTED PYRIDINES, PROCESS FOR PRODUCTION THEREOF, THEIR USE AND DRUGS CONTAINING THE SAME 未知
公开(公告)号：SK36197A3
公开(公告)日：1997-11-05
申请号：SK36197
申请日：1997-03-19
申请人： BAYER AG
发明人： SCHMIDT GUNTER , ANGERBAUER ROLF , BRANDES ARNDT , LOGERS MICHAEL , MULLER-GLIEMANN MATTHIAS , BISCHOFF HILMAR , SCHMIDT DELF , WOHLFEIL STEFAN
IPC分类号： A61K31/435 , A61K31/44 , A61K31/4418 , C07D221/18 , A61K31/4427 , A61K31/455 , A61P3/06 , A61P9/10 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/50 , C07D213/53 , C07D401/06 , C07D417/06 , C07D213/16 , C07C47/32
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.

70. 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.

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