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111. 发明专利

AU2006334899B2 Triazole derivatives 未知
公开(公告)号：AU2006334899B2
公开(公告)日：2012-06-07
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： Novel triazole derivatives, inhibitors of TGF-beta receptor I kinase, of application, amongst other things, to the treatment of tumours.

112. 发明专利

CA2803665A1 2,4- DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER 未知
公开(公告)号：CA2803665A1
公开(公告)日：2012-01-05
申请号：CA2803665
申请日：2011-05-31
申请人： MERCK PATENT GMBH
发明人： DORSCH DIETER , JONCZYK ALFRED , HOELZEMANN GUENTER , AMENDT CHRISTIANE , ZENKE FRANK
IPC分类号： C07D471/04 , A61K31/4375 , A61P35/00 , C07D519/00
摘要： The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.

113. 发明专利

CA2790613A1 HETARYLAMINONAPHTHYRIDINES 未知
公开(公告)号：CA2790613A1
公开(公告)日：2011-08-25
申请号：CA2790613
申请日：2011-01-10
申请人： MERCK PATENT GMBH
发明人： JONCZYK ALFRED , DORSCH DIETER , ZENKE FRANK , AMENDT CHRISTIANE
IPC分类号： C07D453/02
摘要： Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.

114. 发明专利

AR077133A1 ALCOXI-TIENOPIRIMIDINAS, COMPOSICIONES FARMACEUTICAS Y USO DE LOS MISMOS PARA EL TRATAMIENTO DE ENFERMEDADES INDUCIDAS POR QUINASAS 未知
公开(公告)号：AR077133A1
公开(公告)日：2011-08-03
申请号：ARP100102153
申请日：2010-06-18
申请人： MERCK PATENT GMBH
发明人： HOELZEMANN GUENTER , ZENKE FRANK , DORSCH DIETER , GREINER HARTMUT , AMENDT CHRISTIANE
IPC分类号： C07D495/04 , A61K31/519 , A61P35/00
摘要： Los nuevos derivados de alcoxi-tienopirimidina de la formula (1) donde R1 denota un carboarilo mono- o bicíclico C6-10 o un heteroarilo mono- o bicíclico C2-9 y 1 a 4 átomos de N, O y/o S, cada uno de los cuales puede estar monosustituido con Hal, CN y/o A; R2 denota H, A, Cyc, -Alk-Cyc, Q o Het; Q denota alquilo no ramificado o ramificado C1-10, en el que al menos un átomo de H está reemplazado por al menos un sustituyente seleccionado del grupo de Hal, CN, NH2, NHA, NAA, -CO-NH2, -CO-NHA, -CO-NAA, OH, OA, -OAlk-OH, -OAlk-OA, -OAlk-NAA, -CHOH-Alk-OH, Het, -Oalk-Het, Ar, -OAlk-Ar, y/o en donde uno o dos grupos adyacentes CH2 están reemplazados, de modo independiente entre sí, por un grupo -CH=CH- y/o -C:::C-; A denota alquilo no ramificado o ramificado C1-10, en el que 1-7 átomos de H pueden estar reemplazados por Hal; Cyc denota cicloalquilo C3-7, en el que 1-4 átomos de H pueden estar reemplazados, de modo independiente entre sí, por A, Hal, OH, -Alk-OH y/u OA; Alk denota alquileno, alquenilo o alquinilo C1-6, en el que 1-4 átomos de H pueden estar reemplazados, de modo independiente entre sí, por Hal y/o CN; Het denota un heterociclo mono- o bicíclico saturado, insaturado o aromático C2-9 y 1 a 4 átomos de N, O y/o S, que puede estar mono-, di- o trisustituido con al menos un sustituyente seleccionado del grupo de Hal, A, OH, OA, -Alk-OH, -Alk-OA, -Alk-Het1, -Alk-NAA, SO2A, =O (oxígeno del carbonilo); Ar denota un carbociclo mono- o bicíclico saturado, insaturado o aromático C6-10, que puede estar mono-, di- o trisustituido con al menos un sustituyente seleccionado del grupo de Hal, A, OH, CA, -Alk-OH, -Alk-OA, -Alk-Het1, -Alk-NAA, -OAlk-Het1, SO2NH2, SO2NHA, SO2NAA; Het1 denota un heterociclo monocíclico saturado, insaturado o aromático C2-6 y 1 a 4 átomos de N, O y/o S; y Hal denota F, CI, Br o I; y/o sus sales fisiologicamente aceptables. Son inhibidores de la quinasa del receptor TGF-beta1 y se pueden emplear, entre otras cosas, para el tratamiento de tumores.

115. 发明专利

ZA201007979B THIENOPYRIMIDINES 未知
公开(公告)号：ZA201007979B
公开(公告)日：2011-07-27
申请号：ZA201007979
申请日：2010-11-08
申请人： MERCK PATENT GMBH
发明人： HOELZEMANN GUENTER , GREINER HARTMUT , AMENDT CHRISTIANE , ZENKE FRANK
摘要： Novel thienopyrimidines of the formula (I), in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TGF-beta receptor kinase, and can be employed, inter alia, for the treatment of tumours.

116. 发明专利

ES2357625T3 TETRAHIDROQUINOLINAS A EMPLEAR COMO MODULADORES DE LA PROTEINA MOTORA MITOTICA EG5. 未知
公开(公告)号：ES2357625T3
公开(公告)日：2011-04-28
申请号：ES06754091
申请日：2006-06-02
申请人： MERCK PATENT GMBH
发明人： FINSINGER DIRK , AMENDT CHRISTIANE , ZENKE FRANK , SCHIEMANN KAI , BRUGE DAVID , BUCHSTALLER HANS-PETER , EMDE ULRICH
IPC分类号： C07D215/42 , A61K31/47 , A61P35/00 , C07D215/12 , C07D215/54 , C07D221/06 , C07D405/04 , C07D409/04 , C07D471/08
摘要： Compuestos de la fórmula I **Fórmula** donde significan: W CH o N, R1, R2, R3 independientemente unos de otros, H, A, arilo, heteroarilo, Hal, - (CY2)n-SA, -(CY2)n-SCF3, ( CY2)n-SCN, -(CY2)n-CF3, -(CY2)n- OCF3, cicloalquilo, -SCH3, -SCN, -CF3, -OCF3, -OA, -(CY2)n- OH, ( CY2)n-CO2R, -(CY2)n-CN, -(CY2)n-Hal, (CH2)nR, -(CY2)n-NR2, (CY2)n-OR, (CY2)n-OCOA, -SCF3, (CY2)nCONR2, -(CY2)n-NHCOA, -(CY2)n-NHSO2A, SF5, Si(CH3)3, CO-(CY2)n- CH3, -(CY2)n-N-pirrolidona, (CH2)nNRCOOR, NRCOOR, NCO, CH2(CH2)nCOOR, NHCOOR, CH2(CH2)nOH, NR(CH2)nOH, CH2NH2, (CH2)nNR2, CH(OH)R2, CH2NHCOR, (CH2)narilo, CH2(CH2)nheteroarilo, (CH2)nR1, NH(CH2)nCOOR, CH2 (CH2)nX(CH2)narilo, CH2(CH2)nX(CH2)nheteroarilo, NH(CH2)nCONR2, XCONR(CH2)nNR2, N[(CH2)nXCOOR]CO(CH2)n-arilo, N[(CH2)nXR]CO(CH2)narilo, N[(CH2)nXR]CO(CH2)nXarilo, N[(CH2)nXR]SO2 (CH2)n-arilo, N[(CH2)nNRCOOR]CO(CH2)narilo, N[(CH2)nNR2]CO(CH2)n-arilo, N[(CH2)nNR2]CO(CH2)nNR15 arilo, N[(CH2)nNR2]SO2(CH2)n-arilo, N[(CH2)nXR]CO(CH2)n-heteroarilo, N[(CH2)nXR]CO(CH2)nX-heteroarilo, N[(CH2)nXR]SO2(CH2)n-heteroarilo, N[(CH2)nNRCOOR]CO(CH2)n-heteroarilo, N[(CH2)nNR2]CO (CH2)nheteroarilo, N[(CH2)nNR2]CO(CH2)nNR-heteroarilo, pudiendo estar los grupos CY2 no adyacentes sustituidos también por X, R1 y R3, juntos también, -N-C(CF3)=N-, -N-CR=N-, -N-N=N-, Y H, A, Hal, OR1, N(R1)2, E-R1 A alquilo o cicloalquilo, donde uno o varios átomos de H pueden estar sustituidos por Hal y/o uno o varios grupos CH2 no adyacentes pueden estar sustituidos por X, Hal F, Cl, Br o I R H o A, en radicales germinales R juntos también H o A, en radicales germinales R juntos también -(CH2)5, - (CH2)4- o -(CH2)n-X-(CH2)n, o -(CH2)n-Z-(CH2)n, R4 H R5 -(CY2)n-E-(CY2)n-XR1, (CH2)2OH, (CH2)3OH, (CH2)2NRR1, (CH2)3NRR1, (CH2)2CH(OH)CH2OH, (CH2)2CH(OH)CH2NRR1, (CH2)2CH(OH)CH2NR(CH2)2NRR1, (CH2)2CH(OH)CH2NR5(CH2)2NR, (CH2)2CH(OH)CH2-E-R1, Q o (CH2)2CH(OH)CH2NR(CH2)2OR, E NR1SO2-, -SO2NR1-. -CONR1-, -NR1CO-, -COO-, -OOC-, NR1CONR1-, -OCONR1-, -NR1COO, -CSNR1-, 30 NR1CS-, -NR1CSNR1-, -SCONR1-, -NR1COS-, -OCSNR1-, NR1CSO-, SCSNR1-, -NR1CSS o un enlace simple X O, S o NR1, Q (CH2)pHal, CHO, CORa, (CH2)pRa, (CH2)pOCORa, (CH2)pXR1, (CH2)pNCOR1, (CH2)pN(R1)2, (CH2)pOR1, (CH2)pOCON(R1)2, (CH2)pOCOOR1, (CH2)pNHCON(R1)2, (CH2)pNHCOOR1, (CH2)pCN, (CH2)pCOOR1, (CH2)p-E- (CH2)pR1, (CH2)p-E-(CH2)pRa, pudiendo estar los grupos CH2- no adyacentes sustituidos también por X. OR, NHR, NR2, NR(CH2)n-arilo, NR(CH2)nOR, COOR, radical N-pirrolidona, OCOR, NR(CH2)nNR2, N[(CH2)nNR2]CO(CH2)n-arilo, N[(CH2)nNHCOOR]CO-arilo, R1, N[CH2(CH2)nOR]2, NR(CH2)nNCOOR, X (CH2)nX(CH2)nXR, NR(CH2)nX(CH2)nOH, NR(CH2)nO(CH2)nOH, (CH2)nCOOR, O(CO)NR(CH2)nOR, O (CO)(CH2)nNR2, NR(CH2)nNR2, N[(CH2)nNR2]CO(CH2)n-arilo, N[(CH2)nXR]CO(CH2)n-arilo, N[(CH2)nXR] CO(CH2)n-heteroarilo, N[(CH2)nNR2]CO(CH2)n-heteroarilo, N[(CH2)nNR2]CO(CH2)nR1, N(R)(CH2)nN(R) COOR, XCOO(CH2)nNR2, OSO2A, OSO2CF3, OSO2Ar, OCONR2, OCH2(CH2)nNR2 Z CH2, X, CHCONH2, CH(CH2)nNR1COOR1, CHNR1COOR1, CHCON(R1)2, NCO, CH(CH2)nCOOR1, NCOOR1, CH(CH2)nOH, N(CH2)nOH, CHNH2, CH(CH2)nN(R1)2, CH(CH2)nN(R1)2, C(OH)R1, CHNCOR1, NCOR1, N(CH2)n-arilo, N(CH2)nheteroarilo, CHR1, NR1, CH(CH2)n-arilo, CH(CH2)n-heteroarilo, CH(CH2)nR1, N(CH2)nCOOR1, CH(CH2)nX(CH2)nR1, CH(CH2)nX(CH2)nRa, N(CH2)nCON(R1)2, XCONR1(CH2)nN(R1)2, CO(CH2)nR1, CO(CH2)nR1, CO(CH2)nXR1, SO2(CH2)nR1, O(CH2)nN(R1)2, X(CH2)nN(R1)2, NCO(CH2)nN(R1)2, CHRa, NRa, R6 arilo o heteroarilo no sustituido o mono- o poli-sustituido, que puede estar sustituido por Hal, NO2, CN, A, OR, OCOR, COR, NR2, CF3, OCF3, OCH(CF3)2, Hal, NO2, CN, OR, A, -(CY2)n-OR, -OCOR, -(CY2)n-CO2R, ( CY2)n-CN, - NCOR, -COR o -(CY2)n-NR2, R7 (C=O)-R, (C=O)NR2, (C=O)-OR, H o A, donde R5 y R7 pueden significar juntos también -(CH2)n-, m 0, 1 o 2 n 0, 1, 2, 3, 4, 5, 6 o 7 y p 0, 1, 2, 3, 4, o 5, preferentemente 2 o 3 S 0, 1, 2, 3, 4, 5, 6 o 7, preferentemente 0, así como sus solvatos, tautómeros, sales y estereoisómeros, incluyendo sus mezclas en todas las proporciones.

117. 发明专利

AT487721T 未知
公开(公告)号：AT487721T
公开(公告)日：2010-11-15
申请号：AT07818574
申请日：2007-09-29
申请人： MERCK PATENT GMBH
发明人： HOELZEMANN GUENTER , GREINER HARTMUT , AMENDT CHRISTIANE
IPC分类号： C07D487/04 , A61K31/55 , A61P35/00

118. 发明专利

ZA200907305B Substituted tetrahydroquinolines 未知
公开(公告)号：ZA200907305B
公开(公告)日：2010-06-30
申请号：ZA200907305
申请日：2009-10-19
申请人： MERCK PATENT GMBH
发明人： SCHIEMANN KAI , FINSINGER DIRK , AMENDT CHRISTIANE , ZENKE FRANK
IPC分类号： A61K20100101 , A61P20100101 , C07D20100101
摘要： Compounds of the formula (I), in which R1, R2, R3, R4, R5, X, Y, W, Q1, Q2, Z, s and m have the meanings indicated in Claim 1, can be employed, inter alia, for the treatment of tumors.

119. 发明专利

ZA200806358B Triazole Derivatives 未知
公开(公告)号：ZA200806358B
公开(公告)日：2009-12-30
申请号：ZA200806358
申请日：2008-07-22
申请人： MERCK PATENT GMBH
发明人： CEZANNE BERTRAM , AMENDT CHRISTIANE , GREINER HARTMUT , GRAEDLER ULRICH , HOELZEMANN GUENTER
IPC分类号： A61K20100101 , A61P20100101 , C07D20100101
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.

120. 发明专利

AU2009235729A1 Thienopyrimidines 未知
公开(公告)号：AU2009235729A1
公开(公告)日：2009-10-15
申请号：AU2009235729
申请日：2009-03-23
申请人： MERCK PATENT GMBH
发明人： HOELZEMANN GUENTER , GREINER HARTMUT , ZENKE FRANK , AMENDT CHRISTIANE
IPC分类号： C07D495/04 , A61K31/519 , A61P31/00
摘要： Novel thienopyrimidines of the formula (I), in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TGF-beta receptor kinase, and can be employed, inter alia, for the treatment of tumours.

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