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71. 发明专利

AR065786A1 DERIVADOS DE PIRIMIDINAS CONDENSADAS CON HETEROCICLOS,PROCEDIMIENTO DE PREPARACION,MEDICAMENTOS QUE LAS CONTIENEN Y USOS COMO INHIBIDORES DE PROTEINAS MOTORAS MITOTICAS,EN EL TRATAMIENTO DEL CANCER. 未知
公开(公告)号：AR065786A1
公开(公告)日：2009-07-01
申请号：ARP080101127
申请日：2008-03-19
申请人： MERCK PATENT GMBH
发明人： SCHIEMANN KAI , FINSINGER DIRK , AMENDT CHRISTIANE , ZENKE FRANK
IPC分类号： C07D491/147 , C07D491/153 , C07D495/14 , C07D487/14 , A61K31/4738 , A61K31/4741 , A61K31/4743 , A61K31/4745 , A61P35/00
摘要： Los compuestos caracterizados por la formula (1) en donde E es un resto del grupo de formulas (2); X es O, NR o S; R1, R2 son, de modo independiente entre sí, H, A, Hal, SA, (CH2)pCN, SCN, (CF2)pCF3, SF5, OA, O(CF2)pCF3, S(CF2)pCF3, NR2, NRCOR, NRSO2R, NR(CH2)pNR2, ONR(CH2)pNR2, SO2NR(CH2)pNR2, CONR2, SO2NR2, COOR; R3 es H, A; A es alquilo lineal o ramificado C1-10, cicloalquilo C3-7; R4 es arilo o heteroarilo sustituido o mono- o polisustituido con arilo o heteroarilo, que puede estar sustituido con Hal, NO2, CN, A, OR, OCOR, NR2, CF3, OCF3, OCH(CF3)2, Hal, NO2, CN, OR, A, -(CY2)n-OR, -OCOR, -(CY2)n-CO2R, -(CY2)n-CN o -(CY2)n-NR2; Y es H, A, Hal, OR; R es H, A, (CH2)pO(CH2)pR3, (CH2)pNA(CH2)pR3; W es CH2, C=O, C=S o un enlace simple; Q1 es NR, O, S o un enlace simple; Z es -SO2-, -SO-, CO, CS, un resto del grupo de formulas (3) o un enlace simple; Q2 es NR, S, O o un enlace simple; R5 es H, (CY2)pNR2, (CY2)pOR, (CY2)pSR, un resto de formula (4), -(CY2)pQ1COQ1R, (CY2)pCOOR y, siempre que Q2 sea un enlace simple, también Hal; Hal es F, Br o Cl; n es 1, 2, 3 o 4, m es 0, 1 o 2, p es 0, 1, 2, 3, 4, 5, 6, 7 u 8; y s es 0, 1 o 2; así como sus derivados, solvatos, tautomeros, sales y estereoisomeros, incluyendo sus mezclas en todas las proporciones, y medicamentos que los contienen para utilizar en el tratamiento de tumores.

72. 发明专利

ES2311120T3 DERIVADOS DE GLICINAMIDA COMO INHIBIDORES DE QUINASA-RAF. 未知
公开(公告)号：ES2311120T3
公开(公告)日：2009-02-01
申请号：ES03790841
申请日：2003-07-31
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER , WIESNER MATTHIAS , SCHADT OLIVER , AMENDT CHRISTIANE , ZENKE FRANK , SIRRENBERG CHRISTIAN
IPC分类号： A61K31/4409 , C07D213/64 , A61K31/4406 , A61K31/4427 , A61K31/4439 , A61P3/00 , A61P7/02 , A61P9/10 , A61P13/08 , A61P13/12 , A61P15/00 , A61P17/02 , A61P17/06 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/00 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/06 , A61P43/00 , C07D213/65 , C07D213/68 , C07D213/807 , C07D413/12
摘要： Derivados de glicinamida de fórmula II (Ver fórmula) donde Ar 1 se selecciona entre fenilo y oxazolilo, Ar 2 es piridinilo, R 8 , R 9 y R 10 se seleccionan independientemente del grupo que consiste en H, A, cicloalquilo de 3 a 7 átomos de carbono, Hal, CH2Hal, CH(Hal)2, C(Hal)3, NO2, (CH2)nCN, (CH2)nNR 11 R 12 , (CH2)nOR 11 , (CH2)nO(CH2)k NR 11 R 12 , (CH2)nCOOR 12 , (CH2)nCONR 11 R 12 , (CH2)nNR 11 COR 13 , (CH2)nNR 11 CONR 11 R 12 , (CH2)nNR 11 SO2A, (CH2)nSO2NR 11 R 12 , (CH2)nS(O)uR 13 , (CH2)nOC(O)R 13 , (CH2)nCOR 13 , (CH2)nSR 11 , CH=N-OA, CH2CH=N-OA, (CH2)nNHOA, (CH2)nCH=N-R 11 , (CH2)nOC(O)NR 11 R 12 , (CH2)nNR 11 COOR 12 , (CH2)nN(R 11 )CH2CH2 OR 13 , (CH2)nN(R 11 )CH2CH2OCF3, (CH2)nN(R 11 )C(R 13 )HCOOR 12 , C(R 13 )HCOR 12 , (CH2)nN(R 11 )CH2CH2N (R 12 )CH2COOR 12 , (CH2)nN(R 11 )CH2CH2NR 11 R 12 , CH=CHCOOR 11 , CH=CHCH2NR 11 R 12 , CH=CHCH2NR 11 R 12 , CH=CHCH2OR 13 , (CH2)nN(COOR 11 )COOR 12 , (CH2)nN(CONH2)COOR 11 , (CH2)nN(CONH2)CONH2, (CH2)nN(CH2COOR 11 )COOR 12 , (CH2)nN(CH2CONH2)COOR 11 , (CH2)nN(CH2CONH2)CONH2, (CH2)nCHR 13 COR 11 , (CH2)nCHR 13 COOR 11 , (CH2)nCHR 13 CH2OR 14 , (CH2)nOCN y (CH2)nNCO, donde R 11 , R 12 se seleccionan independientemente del grupo que consiste en H, A, (CH2)mAr 3 y (CH2)mHet, o en NR 11 R 12 , R 11 y R 12 forman, junto con el átomo de N al que están enlazados, un heterociclo de 5, 6 o 7 miembros que contiene opcionalmente 1 o 2 heteroátomos adicionales, que pueden ser N, O y S, R 13 , R 14 se seleccionan independientemente del grupo que consiste en H, A, (CH2)mAr 4 y (CH2)mHet, A se selecciona del grupo que consiste en alquilo, alquenilo, cicloalquilo, alquilencicloalquilo, alcoxi y alcoxialquilo, Ar 3 , Ar 4 son residuos hidrocarbonados aromáticos de 5 a 12 átomos de carbono, preferiblemente de 1 a 10, independientes el uno del otro, y opcionalmente pueden estar sustituidos con uno o varios sustituyentes, seleccio-nados del grupo que consiste en A, Hal, NO2, CN, OR 15 , NR 15 R 16 , COOR 15 , CONR 15 R 16 , NR 15 COR 16 , NR 15 CONR 15 R 16 , NR 16 SO2A, COR 15 , SO2R 15 R 16 , S(O)uA y OOCR 15 , Het es un residuo heterocíclico saturado, insaturado o aromático que opcionalmente puede estar sustituido por uno o varios sustituyentes, seleccionados del grupo que consiste en A, Hal, NO2, CN, OR 15 , NR 15 R 16 , COOR 15 , CONR 15 R 16 , NR 15 COR 16 , NR 15 CONR 15 R 16 , NR 16 SO2A, COR 15 , SO2R 15 R 16 , S(O)uA y OOCR 15 , R 15 , R 16 se seleccionan independientemente del grupo que consiste en H, A, (CH2)mAr 5 , donde Ar 6 es un hidrocarburo aromático de 5 o 6 miembros que opcionalmente puede sustituirse con uno o varios sustituyentes seleccionados del grupo que consiste en metilo, etilo, propilo, 2-propilo, ter-butilo, Hal, CN, OH, NH2 y CF3, n, m son...

73. 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

74. 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.

75. 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.

76. 发明专利

CA2611889A1 SUBSTITUTED TETRAHYDROQUINOLINES 未知
公开(公告)号：CA2611889A1
公开(公告)日：2007-05-18
申请号：CA2611889
申请日：2006-05-17
申请人： MERCK PATENT GMBH
发明人： ZENKE FRANK , SCHIEMANN KAI , HEISS NINA , AMENDT CHRISTIANE , EMDE ULRICH , FINSINGER DIRK
IPC分类号： C07D491/04 , A61K31/4355 , A61K31/436 , A61K31/4375 , A61K31/4706 , A61K31/4709 , A61P35/00 , C07D215/42 , C07D401/04 , C07D471/04
摘要： Compounds of the formula (I), in which W, R, R1, R2, R3, R4, R4', R5, R5', R 6, R6', s and R7 have the meanings indicated in claim 1 can be employed inter alia for the treatment of tumours.

77. 发明专利

MXPA06014293A TETRAHIDROQUINOLINAS. 未知
公开(公告)号：MXPA06014293A
公开(公告)日：2007-02-19
申请号：MXPA06014293
申请日：2005-06-03
申请人： MERCK PATENT GMBH
发明人： FINSINGER DIRK , AMENDT CHRISTIANE , BUCHSTALLER HANS-PETER , ZENKE FRANK , SCHIEMANN KAI , EMDE ULRICH , BRUGE DAVID , STAEHLE WOLFGANG
IPC分类号： A61K31/4355 , C07D221/00 , A61K31/436 , C07D317/00 , C07D319/00 , C07D491/04
摘要： Los compuestos de la formula I (ver formula I) en la que W, R, R1, R2, R3, R4, R5, R6 y R7 tienen los significados indicados en la reivindicacion 1, pueden ser utilizados, por ejemplo, para el tratamiento de tumores.

78. 发明专利

CA2611892A1 TETRAHYDROQUINOLINE DERIVATIVES 未知
公开(公告)号：CA2611892A1
公开(公告)日：2006-12-21
申请号：CA2611892
申请日：2006-05-31
申请人： MERCK PATENT GMBH
发明人： AMENDT CHRISTIANE , ZENKE FRANK , BUCHSTALLER HANS-PETER , STAEHLE WOLFGANG , BRUGE DAVID , SCHIEMANN KAI , FINSINGER DIRK
IPC分类号： C07D221/16 , A61K31/473 , A61K31/4741 , A61K31/496 , A61P35/00 , C07D401/08 , C07D491/04
摘要： Compounds of formula I in which s, k, I, W, R1, R2, R3 and U have the meanin gs given in claim 1 can be used, inter alia, for the treatment of tumors.

79. 发明专利

AU2006257414A1 Tetrahydroquinolines used in the form of modulators of mitotic motor-proteins Eg5 未知
公开(公告)号：AU2006257414A1
公开(公告)日：2006-12-21
申请号：AU2006257414
申请日：2006-06-02
申请人： MERCK PATENT GMBH
发明人： FINSINGER DIRK , BUCHSTALLER HANS-PETER , AMENDT CHRISTIANE , BRUGE DAVID , ZENKE FRANK , SCHIEMANN KAI , EMDE ULRICH
IPC分类号： C07D215/42 , A61K31/47 , A61P35/00 , C07D215/12 , C07D215/54 , C07D221/06 , C07D405/04 , C07D409/04 , C07D471/08

80. 发明专利

CA2609391A1 QUINAZOLINONES 未知
公开(公告)号：CA2609391A1
公开(公告)日：2006-11-30
申请号：CA2609391
申请日：2006-05-17
申请人： MERCK PATENT GMBH
发明人： BUCHSTALLER HANS-PETER , AMENDT CHRISTIANE , ZENKE FRANK , SCHIEMANN KAI , EMDE ULRICH , FINSINGER DIRK
IPC分类号： C07D239/90 , A61K31/517 , A61P35/00 , C07D239/91
摘要： Disclosed are compounds of formula (I), wherein R, R1, R2, R3, R4, R5, R6, R7, R8, Z1, Z2, Z3, k, and Y1 have the meanings indicated in claim 1. Said compounds can be used for the treatment of tumors, among other things.

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