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1. 发明申请

WO0100188A2 TETRAHYDROQUINOLINYL-6-METHYLDIHYDROTHIADIAZINONE DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：四氢-6- METHYLDIHYDROTHIADIAZINON衍生物及其
公开(公告)号：WO0100188A2
公开(公告)日：2001-01-04
申请号：PCT/EP0005571
申请日：2000-06-16
申请人： BAYER AG , STOLTEFUSS JUERGEN , BRAEUNLICH GABRIELE , LOEGERS MICHAEL , SCHMECK CARSTEN , NIELSCH ULRICH , BECHEM MARTIN , GERDES CHRISTIAN , SPERZEL MICHAEL , LUSTIG KLEMENS , STUERMER WERNER
发明人： STOLTEFUSS JUERGEN , BRAEUNLICH GABRIELE , LOEGERS MICHAEL , SCHMECK CARSTEN , NIELSCH ULRICH , BECHEM MARTIN , GERDES CHRISTIAN , SPERZEL MICHAEL , LUSTIG KLEMENS , STUERMER WERNER
IPC分类号： A61K31/549 , A61P7/00 , A61P7/06 , A61P13/12 , A61P31/18 , C07D417/04 , C07D417/14 , A61K31/00
CPC分类号： C07D417/04 , A61K31/549 , C07D417/14
摘要： The invention relates to the area of erythropoiesis, in particular to the use of tetrahydroquinolinyl-6-methyldihydrothiadiazinones of general formula (I) for preventing and/or treating anaemia. The invention also relates to novel tetrahydroquinolinyl-6-methyldihydrothiadiazinone derivatives and to the production thereof.
摘要翻译：本发明涉及红细胞生成的领域。特别地，使用6-四氢喹啉基，methyldihydrothiadiazinonen将描述用于贫血的预防和/或治疗的通式（I）。此外，新的四氢喹啉基-6- methyldihydrothiadiazinon衍生物和它们的制备描述。

2. 发明申请

WO0164652A9 SUBSTITUTED 5-METHYLDIHYDROPYRIDAZINONES AND THEIR USE IN THE PROPHYLAXIS AND/OR TREATMENT OF ANEMIAS 审中-公开
标题翻译：取代的5 METHYLDIHYDROPYRIDAZINONE和它们在预防和/或治疗的贫血
公开(公告)号：WO0164652A9
公开(公告)日：2002-07-04
申请号：PCT/EP0101873
申请日：2001-02-20
申请人： BAYER AG , BRAEUNLICH GABRIELE , LOEGERS MICHAEL , STOLTEFUSS JUERGEN , SCHMECK CARSTEN , NIELSCH ULRICH , STUERMER WERNER , GERDES CHRISTOPH , LUSTIG KLEMENS , SPERZEL MICHAEL
发明人： BRAEUNLICH GABRIELE , LOEGERS MICHAEL , STOLTEFUSS JUERGEN , SCHMECK CARSTEN , NIELSCH ULRICH , STUERMER WERNER , GERDES CHRISTOPH , LUSTIG KLEMENS , SPERZEL MICHAEL
IPC分类号： A61P7/06 , C07D237/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/50
CPC分类号： C07D401/12 , C07D237/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to the field of erythropoiesis and, in particular, relates to 5-methyldihydropyridazinones of general formula (I) and to the use thereof as medicaments, preferably for the prophylaxis of and/or for combating anemias.
摘要翻译：本发明涉及红细胞生成的领域。特别地，5-Methyldihydropyridazinone通式（I）和它们作为药物的用途，优选用于所描述的预防和/或防治贫血。

3. 发明专利

BG63691B1 CYCLOALKANOPYRIDINES 未知
公开(公告)号：BG63691B1
公开(公告)日：2002-09-30
申请号：BG10174797
申请日：1997-07-04
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 , GIERA HENRY , SCHUHMACHER JOACHIM , PAULSEN HOLGER , NAAB PAUL , CONRAD MICHAEL , STOLTEFUSS JUERGEN
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
摘要： The cycloalkanopyridines are produced when suitable cycloalkanopyridines react with suitable metallorganic compounds or with Wittich or Grignard reagents or when compounds of the type of cycloalkanopyridinalcohols react with suitable bromine compounds, optionally the functional groups are alternating, respectively. The cycloalkanopyridines are suitable as active components for medicamentous forms, in particular for such used in the treatment of hyperlipoproteinemia and atherosclerosis. 10 claims

4. 发明专利

BG63661B2 3-AMINO-1-PROPENON DERIVATIVE 未知
公开(公告)号：BG63661B2
公开(公告)日：2002-08-30
申请号：BG10588301
申请日：1997-07-04
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： 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 , C07C49/203 , C07C49/217
摘要： The 3-amino-3-cyclopentyl-1-(4-trifluoromethylphenyl) propenon with structural formula is a new compound finding application as an intermediate form for the synthesis of cycloalkanepyridines with general formula wherein the meanings of the substituents are given in the description. These compounds are used as active ingredients for medicamentous forms for the prevention and treatment of hyperlipoproteinaemia and atherosclerosis. 2 claims

5. 发明专利

NO309270B1 未知
公开(公告)号：NO309270B1
公开(公告)日：2001-01-08
申请号：NO973143
申请日：1997-07-07
申请人： BAYER AG
发明人： SCHMECK CARSTEN , MUELLER-GLIEMANN MATTHIAS , SCHMIDT GUNTER , BRANDES ARNDT , ANGERBAUER ROLF , LOEGERS 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 , A61K31/395
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.

6. 发明专利

HU9701169A2 CYCLOALKANO-PYRIDINE DERIVATIVES, INTERMEDIATES, PREPARATION AND USE THEREOF, PHARMACEUTICAL COMPOSITIONS CONTAINING THESE COMPOUNDS 未知
公开(公告)号：HU9701169A2
公开(公告)日：1999-06-28
申请号：HU9701169
申请日：1997-07-08
申请人： BAYER AG
发明人： ANGERBAUER ROLF , BISCHOFF HILMAR , BRANDES ARNDT , BREMM KLAUS-DIETER , CONRAD MICHAEL , GIERA HENRY , LOEGERS MICHAEL , MUELLER-GLIEMANN MATTHIAS , NAAB PAUL , PAULSEN HOLGER , SCHMECK CARSTEN , SCHMIDT DELF , SCHMIDT GUENTER , SCHUHMACHER JOACHIM , 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.

7. 发明专利

BR9701348A 未知
公开(公告)号：BR9701348A
公开(公告)日：1998-11-10
申请号：BR9701348
申请日：1997-03-19
申请人： BAYER AG
发明人： ANGERBAUER ROLF , BRANDES ARNDT , LOEGERS MICHAEL , MUELLER-GLIEMANN MATTHIAS , BISCHOFF HILMAR , SCHMIDT DELF , WOHLFEIL STEFAN , SCHMIDT GUNTER
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 , C07D213/24 , C07D213/78
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.

8. 发明专利

BR9703884A 未知
公开(公告)号：BR9703884A
公开(公告)日：1998-09-01
申请号：BR9703884
申请日：1997-07-08
申请人： BAYER AG
发明人： MUELLER-GLIEMANN MATTHIAS , SCHMECK CARSTEN , BREMM KLAUS-DIETER , BISCHOFF HILMAR , SCHMIDT DELF , SCHUHMACHER JOACHIM , GIERA HENRY , PAULSEN HOLGER , BRANDES ARNDT , SCHMIDT GUNTER , ANGERBAUER ROLF , LOEGERS MICHAEL
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 , A01N43/42
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.

9. 发明专利

HRP970333A2 HETEROCYCLIC CONDENSED PYRIDINES 未知
公开(公告)号：HRP970333A2
公开(公告)日：1998-04-30
申请号：HRP970333
申请日：1997-06-17
申请人： BAYER AG
发明人： SCHMECK CARSTEN , MUELLER-GLIEMANN MATTHIAS , SCHMIDRT GUNTER , BRANDES ARNDT , ANGERBAUER ROLF , LOEGERS 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
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.

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