专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

22. 发明专利

CA2928009A1 1 -(5-TERT-BUTYL-2-ARYL-PYRAZOL-3-YL)-3-[2-FLUORO-4-[(3-OXO-4H-PYRIDO[2, 3-B]PYRAZIN-8-YL)OXY]PHENYL]UREA DERIVATIVES AS RAF INHIBITORS FOR THE TREATMENT OF CANCER 未知
公开(公告)号：CA2928009A1
公开(公告)日：2015-05-28
申请号：CA2928009
申请日：2014-11-25
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL
发明人： SPRINGER CAROLINE JOY , MARAIS RICHARD , GIROTTI ROMINA , NICULESCU-DUVAZ DAN , NICULESCU-DUVAZ ION , ZAMBON ALFONSO
IPC分类号： C07D471/04 , A61K31/4985 , A61P35/00
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 1-(5-tert-butyl-2-aryl-pyrazol-3-yl)- 3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as "TBAP compounds") that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including: proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of mutant BRAF; disorders ameliorated by the inhibition of BRAF and CRAF; disorders associated with RAS mutations and/or MAPK pathway activation; disorders ameliorated by the inhibition of SRC, p38, FGFRA, VEGFR-2 (KDR), and/or LCK; etc.

23. 发明专利

AU2014253528A1 Pyrido[2,3-b]pyrazine-8-substituted compounds and their use 未知
公开(公告)号：AU2014253528A1
公开(公告)日：2014-11-13
申请号：AU2014253528
申请日：2014-10-23
申请人： CANCER RES INST ROYAL , CANCER REC TECH LTD
发明人： SPRINGER CAROLINE JOY , MARAIS RICHARD , SUIJKERBUIJK BARTHOLOMEUS MARINUS JOSEPHUS MARIE , ZAMBON ALFONSO , NOURRY ARNAUD , MENARD DELPHINE , NICULESCU-DUVAZ DAN , NICULESCU-DUVAZ ION
IPC分类号： C07D471/04
摘要： The present invention pertains generally to the field of therapeutic compounds for treating 5 proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin 8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, 10 to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

24. 发明专利

ES2469367T3 1-(5-Terc-butil-2-fenil-2H-pirazol-3-il)-3-[2-fluoro-4-(1-metil-2-oxo-2,3-dihidro-1H-imidazo[4,5-b]piridin-7-iloxi)-fenil]-urea y compuestos relacionados y su uso en terapia 未知
公开(公告)号：ES2469367T3
公开(公告)日：2014-06-18
申请号：ES11701856
申请日：2011-01-27
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL
发明人： SPRINGER CAROLINE , NICULESCU-DUVAZ ION , MARAIS RICHARD , NICULESCU-DUVAZ DAN , ZAMBON ALFONSO , MENARD DELPHINE
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
摘要： Un compuesto seleccionado entre los compuestos de la siguiente fórmula, y sales, hidratos y solvatos farmacéuticamente aceptables de los mismos:**Fórmula** en la que -J- es independientemente: o**Fórmula** y en la que -R es independientemente: -H, -Me, -F, -Cl, -Br o -I; y en la que -R se sitúa en posiciones meta- o para- en el anillo fenilo.

25. 发明专利

ES2520940T3 Compuestos de pirido[2,3-b]pirazina 8-sustituida y su uso 未知
公开(公告)号：ES2520940T3
公开(公告)日：2014-11-12
申请号：ES08862089
申请日：2008-12-19
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL
发明人： SPRINGER CAROLINE JOY , NICULESCU-DUVAZ DAN , NICULESCU-DUVAZ ION , MARAIS RICHARD , SUIJKERBUIJK BARTHOLOMEUS MARINUS JOSEPHUS MARIE , ZAMBON ALFONSO , NOURRY ARNAUD , MENARD DELPHINE
IPC分类号： C07D471/04
摘要： Un compuesto seleccionado de compuestos de la siguiente fórmula, y sales, hidratos y solvatos farmacéuticamente aceptables de los mismos:**Fórmula** en la que: -RQ1 es independientemente-H, -R1, -R1X, -Cl, -OH, -OR1, -OR1X, -SH, -SR1, -NH2, -NHR1, -NR1 2 o -NRRARRB; en donde: cada -R1 es independientemente alquilo C1-6 alifático saturado, y está sin sustituir o sustituido, por ejemplo, con uno o más grupos seleccionados entre -OH, -OR11, NH2, -NHR11 y -NR11 2, en el que cada -R11 es independientemente alquilo C1-3 alifático saturado; cada -R1X es independientemente alquilo C1-4 alifático saturado sustituido con uno o más grupos seleccionados entre -F, -Cl, -Br e -I; y -NRRARRB es independientemente azetidino, pirrolidino, piperidino, piperazino, morfolino, azepino o diazepino, y está opcionalmente sustituido con uno o más grupos seleccionados entre alquilo C1-4 alifático saturado; -RQ2 es independientemente -H, -R2, -R2X, -Cl, -OH, -OR2, -OR2X, -SH, -SR2, -NH2, -NHR2, -NR22 o -NRRCRRD; en donde: cada -R2 es independientemente alquilo C1-6 alifático saturado, y está sin sustituir o sustituido con uno o más grupos seleccionados entre -OH, OR22, -NH2, -NHR22 y -NR22 2, en donde cada -R22 es independientemente alquilo C1-3 alifático saturado; cada -R2X es independientemente alquilo C1-4 alifático saturado sustituido con uno o más grupos seleccionados entre -F, -Cl, -Br e -I; y -NRRCRRD es independientemente azetidino, pirrolidino, piperidino, piperazino, morfolino, azepino o diazepino, y está opcionalmente sustituido con uno o más grupos seleccionados entre alquilo C1-4 alifático saturado; -X- es independientemente -O-, -S-, -S(>=O)- o -S(>=O)2-; -M- se selecciona independientemente entre:**Fórmula**

26. 发明专利

NZ586418A PYRIDO[2,3-B]PYRAZINE-8-SUBSTITUTED COMPOUNDS AND THEIR USE 未知
公开(公告)号：NZ586418A
公开(公告)日：2012-09-28
申请号：NZ58641808
申请日：2008-12-19
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL
发明人： SPRINGER CAROLINE JOY , NICULESCU-DUVAZ DAN , NICULESCU-DUVAZ ION , MARAIS RICHARD , SUIJKERBUIJK BARTHOLOMEUS MARINUS JOSEPHUS MARIE , ZAMBON ALFONSO , NOURRY ARNAUD , MENARD DELPHINE
IPC分类号： C07D471/04 , A61K31/4375 , A61K31/4985
摘要： Disclosed are 8-aryloxy-pyrido[2,3-b]pyrazine, 8-aryloxy-pyrido[3,2-b]pyrazin-3-one and 8-aryloxy-2-oxo-1,2-dihydropyrido[2,3-b]pyrazine derivatives as represented by the general formula, wherein RQ1 is independently H, R1, R1X, Cl, OH, OR1, OR1x, SH, SR1, NH2, NHR1, NR12 or NRRARRB; RQ2 is independently H, R2, R2X, Cl, OH, OR2, OR2x, SH, -SR2, NH2, NHR2, NR22 or NRRCRRD; X is independently O, S, S(=O), or SO2; M is an optionally substituted phenyl or naphthalene group as defined herein; L is a nitrogen containing linker (as defined herein); and J is an optionally substituted phenyl or C5-6heteroaryl moiety; and wherein the remaining substituents are as defined herein. Representative compounds include 1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(4-(2-oxo-1,2-dihydro-pyrido[2,3-b]pyrazin-8-yloxy)phenyl)urea, 1-(3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl)-3-(4-(3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yloxy)phenyl)urea, 1-(2-fluoro-4-(3-methyl-2-oxo-1,2-dihydropyrido[3,2-b]pyrazin-8-yloxy)phenyl)-3-(2-fluoro-5-(trifluoromethyl} phenyl)urea, N-(3-(3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yloxy)phenyl)-3-(trifluoromethoxy)benzamide and 3-tert-butyl-N-(3-(3-oxo-3,4-dihydropyrido[2,3-b]pyrazin-8-yloxy)phenyl)benzamide. Further disclosed is a pharmaceutical composition which comprises a compound as defined above, and a pharmaceutically acceptable carrier or diluent, for the treatment of a disease or disorder that is ameliorated by the inhibition of RAF function, and particularly for the treatment of proliferative disorders including cancer, melanoma and for the treatment of colorectal cancer.

27. 发明专利

CA2709257A1 PYRIDO[2,3-B]PYRAZINE-8-SUBSTITUTED COMPOUNDS AND THEIR USE 未知
公开(公告)号：CA2709257A1
公开(公告)日：2009-06-25
申请号：CA2709257
申请日：2008-12-19
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL
发明人： SPRINGER CAROLINE JOY , NICULESCU-DUVAZ DAN , NICULESCU-DUVAZ ION , MARAIS RICHARD , SUIJKERBUIJK BARTHOLOMEUS MARINUS JOSEPHUS MARIE , ZAMBON ALFONSO , NOURRY ARNAUD , MENARD DELPHINE
IPC分类号： C07D471/04
摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.

28. 发明专利

AT555112T 未知
公开(公告)号：AT555112T
公开(公告)日：2012-05-15
申请号：AT07732571
申请日：2007-04-26
申请人： CANCER REC TECH LTD , INST OF CANCER RES THE ROYAL CANCER HOSPITAL , ASTEX THERAPEUTICS LTD
发明人： NICULESCU-DUVAZ DAN , SPRINGER CAROLINE , MARAIS RICHARD , DIJKSTRA HARMEN , MENARD DELPHINE , NICULESCU-DUVAZ ION , DAVIES LAWRENCE , NOURRY ARNAUD
IPC分类号： C07D471/04 , A61K31/437 , A61K31/44 , A61K31/5377 , A61P35/00

29. 发明专利

ES2385103T3 Compuestos de imidazo[4,5-b]piridin-2-ona y análogos de los mismos como compuestos terapéuticos contra el cáncer 未知
公开(公告)号：ES2385103T3
公开(公告)日：2012-07-18
申请号：ES07732571
申请日：2007-04-26
申请人： CANCER REC TECH LTD , INST OF CANCER RES THE ROYAL CANCER HOSPITAL , ASTEX THERAPEUTICS LTD
发明人： NICULESCU-DUVAZ DAN , SPRINGER CAROLINE , MARAIS RICHARD , DIJKSTRA HARMEN , MENARD DELPHINE , NICULESCU-DUVAZ ION , DAVIES LAWRENCE , NOURRY ARNAUD
IPC分类号： C07D471/04 , A61K31/437 , A61K31/44 , A61K31/5377 , A61P35/00
摘要： Un compuesto seleccionado de compuestos de la siguiente fórmula, y sales farmacéuticamente aceptables y solvatos de los mismos: en la que: J es independientemente -NRN1-; RN1 es independientemente -H o -Me; RN2 es independientemente -H o -Me; Y es independientemente -CH >= ; Q es independientemente -O-; cada uno de RP1, RP2, RP5 y RP4 es independientemente -H, -Me, -CF3, -F o -Cl; el grupo A-L- es independientemente A-NH-C( >= O)-NH-, A-C( >= O)-NH- o A-N H-C( >= O)-; A es independientemente fenilo o pirazolilo, y está independientemente sin sustituir o sustituido con uno o más grupos seleccionados de: -(C >= O)NH2, -(C >= O)NMe2, -(C >= O)NEt2, -(C >= O)N(iPr)2, -(C >= O)N(CH2CH2OH)2, -(C >= O)-morfolino, -(C >= O)NHPh, -(C >= O)NHCH2Ph, -F, -Cl, -Br, -I, -CN, -OH, -OMe, -OEt, -O(iPr), -O(tBu), -OPh, -OCH2Ph, -OCF3, -OCH2CF3, -OCF2CF2H, -OCH2CH2OH, -OCH2CH2OMe -OCH2CH2OEt, -OCH2CH2NH2, -20 OCH2CH2NMe2, -OCH2CH2N(iPr)2, -OCH2CH2-morfolino, -OCH2CH2-piperazino, -OCH2CH2-pirrolidino, -OPh-Me, -OPh-OH, -OPh-OMe, -OPh-F, -OPh-Cl, -OPh-Br, -OPh-I, -NH2, -NHMe, -NHEt, -NH(iPr), -NMe2, -NEt2, -N(iPr)2, -N(CH2CH2OH)2, -NHPh, -NHCH2Ph, piperidino, piperazino, morfolino, -NH(C >= O)Me, -NH(C >= O)Et, -NH(C >= O)nPr, -NH(C >= O)Ph, -NHC( >= O)CH2Ph, -NMe(C >= O)Me, -NMe(C >= O)Et, -NMe(C >= O)Ph, -NMeC( >= O)CH2Ph, -SO2Me, -SO2CF3, -SO2Et, -SO2Ph, -SO2PhMe, -SO2CH2Ph, -SO2NH2, O2NHMe, -SO2NHEt, -SO2NMe2 -SO2NEt2 -SO2-25 morfolino, -SO2NHPh, -SO2NHCH2Ph, -CH2Ph, -CH2Ph-Me, -CH2Ph-OH, -CH2Ph-F, -CH2Ph-Cl, -Ph, -Ph-Me, -Ph-OH, -Ph-OMe, -Ph-NH2, -Ph-F, -Ph-Cl, -Ph-Br, -Ph-I, piridilo, pirazinilo, pirimidinilo, piridazinilo, furanilo, tiofenilo, pirrolilo, imidazolilo, pirazolilo, oxazolilo, tiazolilo, tiadiazolilo, pirrolidinilo, imidazolidinilo, pirazolidinilo, piperidinilo, piperazinilo, azepinilo, tetrahidrofuranilo, tetrahidropiranilo, morfolinilo, azetidinilo, -Me, -Et, -nPr, -iPr, -nBu, -iBu, -sBu, -tBu, -nPe, -iPe, ter-Pe, neo-Pe, -cPr, -cHex, -CH >= CH2, -CH2-CH >= CH2, -CF3, -CHF2, -CH2F, -CCl3, -CBr3, -30 CH2CH2F, -CH2CHF2, H2CF3, -CH2OH, -CH2OMe, -CH2OEt, -CH2NH2, -CH2NMe2, -CH2CH2OH, -CH2CH2OMe -CH2CH2OEt, -CH2CH2CH2NH2, -CH2CH2NMe2, -CH2CH2-morfolino, -CH2CH2-piperazino, -CH2CH2-pirrolidino, y >= O; o: A es un grupo pirazolilo seleccionado de grupos de las siguientes fórmulas: en las que: RPY es independientemente alquilo C1-7 saturado; y RN3 es independientemente fenilo, y está independientemente sin sustituir o sustituido con uno o más sustituyentes seleccionados de -F, -Cl, -Br, -I, -OMe, -OCF3, -Me y -CF3.

30. 发明专利

MX2014010509A COMPUESTOS DE 3-ARIL-5-SUBSTITUIDO-ISOQUINOLIN-1-ONA Y SU USO TERAPEUTICO. 未知
公开(公告)号：MX2014010509A
公开(公告)日：2014-10-14
申请号：MX2014010509
申请日：2013-03-07
申请人： CANCER RES INST ROYAL
发明人： ASHWORTH ALAN , LORD CHRISTOPHER JAMES , ELLIOTT RICHARD JAMES ROWLAND , NICULESCU-DUVAZ DAN , PORTER RODERICK , BOFFEY RAYMOND JOHN , BAYFORD MELANIE JAYNE , FIRTH-CLARK STUART , JARVIS ASHLEY NICHOLAS , PERRIOR TREVOR ROBERT , KEY REBEKAH ELISABETH
IPC分类号： A61P35/00 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/506 , C07D217/14 , C07D217/16 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D487/04 , C07D487/08 , C07D487/10
摘要： La presente invención se refiere generalmente al campo de compuestos terapéuticos. Más específicamente la presente invención concierne a ciertos compuestos de 3-aril-5-sustituido-2H -isoquinolin-1-ona que, inter alia, inhiben PARP (por ejemplo, PARP1, TNKS1, TNKS2, etc.) y7o señalización Wnt. La presente invención también concierne una composición farmacpeutica que comprende tales compuestos, y el uso de tales compuestos y composiciones, ambos in vitro y in vivo, para inhibir PARP (por ejemplo, PARP1, TNKS1, TNKS2, etc.); para inhibir la señalización Wnt; para tartar los trastornos que son aliviados por la inhibición de PARP (por ejemplo, PARP1, TNKS1, TNKS2, etc.); para tartar trastornos que son aliviados por la inhibición de la señalización Wnt; para tratar las condiciones proliferativas tal como cáncer, etc. (ver Fórmula).

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式