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51. 发明专利

AU2007315374A1 Triaza-benzo[e]azulene derivatives for the treatment of tumors 未知
公开(公告)号：AU2007315374A1
公开(公告)日：2008-05-08
申请号：AU2007315374
申请日：2007-09-29
申请人： MERCK PATENT GMBH
发明人： GREINER HARTMUT , HOELZEMANN GUENTER , AMENDT CHRISTIANE
IPC分类号： C07D487/04 , A61K31/55 , A61P35/00

52. 发明专利

AT384723T 未知
公开(公告)号：AT384723T
公开(公告)日：2008-02-15
申请号：AT05789235
申请日：2005-10-04
申请人： MERCK PATENT GMBH
发明人： STAEHLE WOLFGANG , HOELZEMANN GUENTER , RAUTENBERG WILFRIED
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00

53. 发明专利

AU2006334899A1 Triazole derivatives 未知
公开(公告)号：AU2006334899A1
公开(公告)日：2007-07-19
申请号：AU2006334899
申请日：2006-11-24
申请人： MERCK PATENT GMBH
发明人： GRAEDLER ULRICH , GREINER HARTMUT , HOELZEMANN GUENTER , CEZANNE BERTRAM , AMENDT CHRISTIANE
IPC分类号： C07D487/04 , A61K31/38 , A61K31/55 , A61P35/00 , C07D513/04
摘要： 76 named polyaza-benzo[e]azulene compounds (A), are new. 76 Polyaza-benzo[e]azulene compounds (A), their derivatives, solvates, salts, tautomers and stereoisomers, including mixtures, are new: e.g. (R,S)-8-hydroxy-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-1-(3-chlorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; (R,S)- or (+)-(S)-8-chloro-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-methoxy-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; (R,S)-1-(5-chloro-2-fluorophenyl)-8-(methoxy or hydroxy)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-4-methyl-1-(3-(CF 3or ethoxy)phenyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S) -1-(3-bromophenyl)-8-chloro-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 1-(2-chloropyridin-4-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(2,5-dichlorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (-)-(R)-8-chloro-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(5-chloro-2-fluorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-1-[8-chloro-4-methyl-1-(6-methylpyridin-2-yl)-4,5-dihydro-2,3,6,10b-benzo[e]azulen-6-yl]ethanone; (R,S)-4-methyl-1-pyridin-2-yl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; (R,S)-1-(3-hydroxyphenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; (R,S)-1-(3-chlorophenyl)-8-methoxy-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-methoxy-4-methyl-1-pyridin-2-yl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(3-chlorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-4-methyl-1-pyridin-2-yl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 8-chloro-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 1-pyridin-2-yl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; 8-methoxy-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 3-(8-chloro-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-1yl)phenol; 1-(3-hydroxyphenyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; 8-chloro-1-(3-methoxyphenyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 8-chloro-1-(pyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 8-methoxy-1-(3-methoxyphenyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 8-methoxy-1-(pyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 9-bromo-1-(pyridin-3-yl or pyridin-4-yl)-5,6-dihydro-4H-2,3,6,7,10b-pentaaza-benzo[e]azulene; 9-bromo-1-(4-methoxyphenyl or phenyl)-5,6-dihydro-4H-2,3,6,7,10b-pentaaza-benzo[e]azulene; (R,S)-1-(4-methoxyphenyl or phenyl)-4-methyl-4,5-dihydro-6-thia-2,3,10b-triaza-benzo[e]azulene; 1-(2-methoxyphenyl or 4-methoxyphenyl)-4,5-dihydro-6-thia-2,3,10b-triaza-benzo[e]azulene; (R,S)-1-(4-hydroxyphenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-9-methoxy-1-(4-methoxyphenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-4-methyl-1-phenyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-9-ol; (R,S)-8-chloro-4-methyl-1-(o-tolyl or m-tolyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(2-chlorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-4,9-dimethyl-1-phenyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-4-methyl-1-phenyl-9-CF 3-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-4-methyl-1-phenyl-9-CF 3-4,5-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene-6-carbaldehyde; (R,S)-1-(5-bromopyridin-3-yl)-8-methoxy-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-1-(5-bromopyridin-3-yl)-8-chloro-9-methoxy-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-methoxy-4-methyl-1-[6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-9-methoxy-4-methyl-1-[6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-9-methoxy-4-methyl-1-[6-methylpyridin-2-yl]-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 1-phenyl-4,5-dihydro-6-thia-2,3,10b-triaza-benzo[e]azulene; (R,S)-9-chloro-1-(5-chloro-2-fluorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene trifluoroacetate; (R,S)-8-chloro-1-(4-methoxypyridin-2-yl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-4-methyl-1-(2-methylthiazol-5-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-9-bromo-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(3-fluorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(3-CF 3O-phenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(5-chlorothiophen-2-yl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene and (R,S)-8-chloro-1-(5-methyl-2H-pyrazol-3-yl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene. ACTIVITY : Cytostatic; Vasotropic; Anti-HIV; Nootropic; Neuroprotective; Antiarteriosclerotic; Vulnerary. No details of tests are given. MECHANISM OF ACTION : Transforming growth factorbeta (TGFbeta ) receptor kinase inhibitor. (R,S)-8-hydroxy-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene (A1) has IC50 for inhibition of TGFbeta of 1.8x10 -7>M.

54. 发明专利

DE102005061840A1 New polyaza-benzo-azulene compounds are transforming growth factor-beta receptor kinase inhibitors used for treating e.g. cancer, HIV infection and Alzheimer's disease 未知
公开(公告)号：DE102005061840A1
公开(公告)日：2007-06-28
申请号：DE102005061840
申请日：2005-12-23
申请人： MERCK PATENT GMBH
发明人： CEZANNE BERTRAM , AMENDT CHRISTIANE , GREINER HARTMUT , GRAEDLER ULRICH , HOELZEMANN GUENTER
IPC分类号： C07D487/04 , A61K31/551 , A61K31/5517 , A61K31/554 , A61P35/00 , C07D471/14 , C07D513/04
摘要： 76 named polyaza-benzo[e]azulene compounds (A), are new. 76 Polyaza-benzo[e]azulene compounds (A), their derivatives, solvates, salts, tautomers and stereoisomers, including mixtures, are new: e.g. (R,S)-8-hydroxy-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-1-(3-chlorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; (R,S)- or (+)-(S)-8-chloro-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-methoxy-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; (R,S)-1-(5-chloro-2-fluorophenyl)-8-(methoxy or hydroxy)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-4-methyl-1-(3-(CF 3or ethoxy)phenyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S) -1-(3-bromophenyl)-8-chloro-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 1-(2-chloropyridin-4-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(2,5-dichlorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (-)-(R)-8-chloro-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(5-chloro-2-fluorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-1-[8-chloro-4-methyl-1-(6-methylpyridin-2-yl)-4,5-dihydro-2,3,6,10b-benzo[e]azulen-6-yl]ethanone; (R,S)-4-methyl-1-pyridin-2-yl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; (R,S)-1-(3-hydroxyphenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; (R,S)-1-(3-chlorophenyl)-8-methoxy-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-methoxy-4-methyl-1-pyridin-2-yl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(3-chlorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-4-methyl-1-pyridin-2-yl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 8-chloro-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 1-pyridin-2-yl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; 8-methoxy-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 3-(8-chloro-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-1yl)phenol; 1-(3-hydroxyphenyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-8-ol; 8-chloro-1-(3-methoxyphenyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 8-chloro-1-(pyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 8-methoxy-1-(3-methoxyphenyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 8-methoxy-1-(pyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 9-bromo-1-(pyridin-3-yl or pyridin-4-yl)-5,6-dihydro-4H-2,3,6,7,10b-pentaaza-benzo[e]azulene; 9-bromo-1-(4-methoxyphenyl or phenyl)-5,6-dihydro-4H-2,3,6,7,10b-pentaaza-benzo[e]azulene; (R,S)-1-(4-methoxyphenyl or phenyl)-4-methyl-4,5-dihydro-6-thia-2,3,10b-triaza-benzo[e]azulene; 1-(2-methoxyphenyl or 4-methoxyphenyl)-4,5-dihydro-6-thia-2,3,10b-triaza-benzo[e]azulene; (R,S)-1-(4-hydroxyphenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-9-methoxy-1-(4-methoxyphenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-4-methyl-1-phenyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulen-9-ol; (R,S)-8-chloro-4-methyl-1-(o-tolyl or m-tolyl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(2-chlorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-4,9-dimethyl-1-phenyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-4-methyl-1-phenyl-9-CF 3-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-4-methyl-1-phenyl-9-CF 3-4,5-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene-6-carbaldehyde; (R,S)-1-(5-bromopyridin-3-yl)-8-methoxy-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-1-(5-bromopyridin-3-yl)-8-chloro-9-methoxy-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-methoxy-4-methyl-1-[6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-9-methoxy-4-methyl-1-[6-(2,2,2-trifluoroethoxy)pyridin-3-yl]-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-9-methoxy-4-methyl-1-[6-methylpyridin-2-yl]-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; 1-phenyl-4,5-dihydro-6-thia-2,3,10b-triaza-benzo[e]azulene; (R,S)-9-chloro-1-(5-chloro-2-fluorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene trifluoroacetate; (R,S)-8-chloro-1-(4-methoxypyridin-2-yl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-4-methyl-1-(2-methylthiazol-5-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-9-bromo-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(3-fluorophenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(3-CF 3O-phenyl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene; (R,S)-8-chloro-1-(5-chlorothiophen-2-yl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene and (R,S)-8-chloro-1-(5-methyl-2H-pyrazol-3-yl)-4-methyl-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene. ACTIVITY : Cytostatic; Vasotropic; Anti-HIV; Nootropic; Neuroprotective; Antiarteriosclerotic; Vulnerary. No details of tests are given. MECHANISM OF ACTION : Transforming growth factorbeta (TGFbeta ) receptor kinase inhibitor. (R,S)-8-hydroxy-4-methyl-1-(6-methylpyridin-2-yl)-5,6-dihydro-4H-2,3,6,10b-tetraaza-benzo[e]azulene (A1) has IC50 for inhibition of TGFbeta of 1.8x10 -7>M.

55. 发明专利

AR052302A1 DERIVADOS DE SULFONAMIDAS, PROCESOS DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN 未知
公开(公告)号：AR052302A1
公开(公告)日：2007-03-14
申请号：ARP050101483
申请日：2005-04-15
申请人： MERCK PATENT GMBH
发明人： HOELZEMANN GUENTER , CRASSIER HELENE , JONCZYK ALFRED , STAEHLE WOLFGANG , RAUTENBERG WILFRIED
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00 , C07D221/00 , C07D239/00
摘要： Los compuestos de la formula (1), en donde: X es una formula (2) o Het1-(CH2)n-; R1, R2, R3, R4, R5 son cada uno, de modo independiente entre sí, H, A, OH, OA, alquenilo C2-6, alquinilo C2-6, NO2, NH2, NHA, NA2, Hal, CN, COOH, COOA, -O-Het, -O- alquilen- Het, -O-alquilen-NR8R9 o CONR8R9; dos radicales adyacentes seleccionados de R1, R2, R3, R4, R5 también son juntos -O-CH2-CH2-, -O- CH2-O- u -O-CH2-CH2-O-; R6, R7 son cada uno, de modo independiente entre sí, H, A, Hal, OH, OA o CN; R8, R9 son cada uno, de modo independiente ente sí, H o A; Het1 es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con Hal, A, OA, OH, alquenilo C2-6, alquinilo C2-6, NO2, NH2, NHA, NA2, COOH, COOA, CN, -O-Het, -O-alquilen-Het, -O-alquilen-NR8R9, CONR8R9 y/o el oxígeno del carbonilo (=O); Het es un heterociclo mono o bicíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con Hal, A, OA, COOA, CN y/o el oxígeno del carbonilo (=O); A es alquilo C1-10, en donde también 1-7 átomos de H pueden estar reemplazados por F y/o cloro; Hal es F, Cl, Br o I; n es 0, 1, 2 o 3; así como sus derivados, solvatos, sales, tautomeros, y estereoisomeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones, son inhibidores de las tirosina quinasas, en especial de la TIE-2, y de las Raf-quinasas, y pueden utilizarse, por ejemplo, para el tratamiento de tumores.

56. 发明专利

CA2618524A1 PYRAZOLE DERIVATIVES HAVING TYROSINKINASE ACTIVITY 未知
公开(公告)号：CA2618524A1
公开(公告)日：2007-02-15
申请号：CA2618524
申请日：2006-07-24
申请人： MERCK PATENT GMBH
发明人： RAUTENBERG WILFRIED , CRASSIER HELENE , HOELZEMANN GUENTER
IPC分类号： C07D487/04 , A61K31/415 , A61K31/505 , A61P35/00 , C07D403/12 , C07D471/04 , C07D473/00 , C07D491/14

57. 发明专利

AT350379T 未知
公开(公告)号：AT350379T
公开(公告)日：2007-01-15
申请号：AT03782241
申请日：2003-11-27
申请人： MERCK PATENT GMBH
发明人： HEINRICH TIMO , BOETTCHER HENNING , SCHIEMANN KAI , HOELZEMANN GUENTER , VAN AMSTERDAM CHRISTOPH , BARTOSZYK GERD , GREINER HARTMUT , SEYFRIED CHRISTOPH , BRUNET MICHEL , ZEILLER JEAN , BERTHELON JEAN
IPC分类号： A61K31/404 , A61P25/00 , C07D405/12
摘要： Benzodioxepines of the formula (I) and physiologically tolerated salts and solvates thereof, in which R 1 , R 2 , R 3 , R 4 , A, B, a and b have the meanings indicated in claim 1, are ligands of the 5HT1A receptors and/or the 5HT4 receptors with simultaneously strong serotonin reuptake inhibition. They can be employed for the treatment and prophylaxis of various diseases.

58. 发明专利

DE50304892D1 未知
公开(公告)号：DE50304892D1
公开(公告)日：2006-10-12
申请号：DE50304892
申请日：2003-10-30
申请人： MERCK PATENT GMBH
发明人： HOELZEMANN GUENTER , SCHIEMANN KAI , HEINRICH TIMO , BOETTCHER HENNING , LEIBROCK JOACHIM , VAN AMSTERDAM CHRISTOPH , BARTOSZYK GERD , SEYFRIED CHRISTOPH
IPC分类号： A61K31/4439 , A61K31/4709 , C07D401/12
摘要： Novel indole derivatives of the formula (I), in which X, Y, R 1 , R 1' , m and n have the meanings indicated in Patent Claim 1, have a strong affinity to the 5-HT 1A and in some cases to the 5-HT 1D receptors. The compounds inhibit serotonin reuptake, exhibit serotonin-agonistic and -antagonistic properties and are suitable as antidepressants, anxiolytics and for the treatment of neurodegenerative diseases

59. 发明专利

AU2006231002A1 Pyrazole derivatives 未知
公开(公告)号：AU2006231002A1
公开(公告)日：2006-10-12
申请号：AU2006231002
申请日：2006-03-08
申请人： MERCK PATENT GMBH
发明人： CRASSIER HELENE , RAUTENBERG WILFRIED , HOELZEMANN GUENTER
IPC分类号： C07D401/12 , A61K31/4412 , A61P35/00
摘要： Pyrazole derivatives (I) and their solvates, salts, tautomers and/or stereoisomers are new. Pyrazole derivatives of formula (I) and their solvates, salts, tautomers and/or stereoisomers are new. R 1>phenyl (optionally substituted with 1-3 of A and/or hal); R 2>A, R 1> or Het; A : 1-6C alkyl, where 1-5 of H atoms are replaced by F and/or Cl; Het : aromatic heterocycle with 1-4 of N-, O- and/or S atoms that are replaced by 1-2 of hal and/or A; and hal : F, Cl, Br or I. Independent claims are included for: (1) the preparation of (I); (2) a medicament comprising (I) and optionally carrier and/or additives; and (3) use of (I) for the manufacture of a medicament to treat disease associated with the inhibition, regulation or modulation by signal transduction kinase. [Image] ACTIVITY : Cytostatic; Antiinflammatory; Antiangiogenic; Antidiabetic; Ophthalmological; Antiarthritic; Antirheumatic; Antipsoriatic; Dermatological; Antiallergic; Immunosuppressive; Osteopathic; Antibacterial; Gynecological; Vulnerary. MECHANISM OF ACTION : Tyrosine kinase inhibitor; Tyrosine protein kinase (TIE-2) inhibitor; Raf-Kinase inhibitor.

60. 发明专利

AU2005304087A1 4-amino-5-oxo-8-phenyl-5H-pyrido-[2,3-D]-pyrimidine derivatives as tyrosine kinase and RAF kinase inhibitors for the treatment of tumours 未知
公开(公告)号：AU2005304087A1
公开(公告)日：2006-05-18
申请号：AU2005304087
申请日：2005-10-20
申请人： MERCK PATENT GMBH
发明人： ADAN JAUME , ROSELL-VIVES ELISABET , CRASSIER HELENE , HOELZEMANN GUENTER , RAUTENBERG WILFRIED , CASES CLAUDIA , TARRASON GEMA , ACKERMANN KARL-AUGUST , JONCZYK ALFRED
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00 , A61P35/02 , C07C275/28
摘要： Compounds of the formula (I), in which R6, R7, R8, R9, Het1, X and X′ have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.

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