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1. 发明申请

WO2011092469A8 1-(5-TERT-BUTYL-2-PHENYL-2H-PYRAZOL-3-YL)-3-[2-FLUORO-4-(1-METHYL-2-OXO-2,3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-7-YLOXY)-PHENYL]-UREA AND RELATED COMPOUNDS AND THEIR USE IN THERAPY 审中-公开
标题翻译： 1-（5-叔丁基-2-苯基-2H-吡唑-3-基）-3- [2-氟-4-（1-甲基-2-氧代-2,3-二氢-1H-咪唑并[ 4,5-B]吡啶-7-YLOXY） - 苯基] - 及其相关化合物及其在治疗中的用途
公开(公告)号：WO2011092469A8
公开(公告)日：2012-08-16
申请号：PCT/GB2011000106
申请日：2011-01-27
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL , SPRINGER CAROLINE , NICULESCU-DUVAZ ION , MARAIS RICHARD , NICULESCU-DUVAZ DAN , ZAMBON ALFONSO , MENARD DELPHINE
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
CPC分类号： A61K31/437 , A61K31/4353 , C07D401/02 , C07D471/04
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (I) (for convenience, collectively referred to herein as "IP compounds"), which, inter alia, are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS ("mutant RAS cancer"). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及下列通式（I）的某些化合物（为了方便起见，统称为“IP化合物”），其特别可用于治疗癌症，例如以突变RAS（“突变RAS癌症”）为特征的癌症。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在治疗癌症中的用途，例如突变RAS癌症。

2. 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.

3. 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.

4. 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.

5. 发明专利

NZ601085A 1-(5-tert-butyl-2-phenyl-2h-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy 未知
公开(公告)号：NZ601085A
公开(公告)日：2015-04-24
申请号：NZ60108511
申请日：2011-01-27
申请人： CANCER REC TECH LTD , CANCER RES INST ROYAL
发明人： ZAMBON ALFONSO , NICULESCU-DUVAZ DAN , MENARD DELPHINE , MARAIS RICHARD , SPRINGER CAROLINE , NICULESCU-DUVAZ ION
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
摘要： Disclosed herein is 1-(3-tert-butyl-1-phenyl-1H-pyrazol-5-yl)-3-(2-fluoro-4-(1-N-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-7-yloxy)phenyl)urea and related RA substituted compounds, and the use thereof in the treatment of cancer, such as mutant RAS cancer, more specifically pancreatic cancer; thyroid (e.g., follicular; undifferentiated papillary) cancer; colorectal cancer; seminoma; myelodysplastic syndrome (MDS); lung cancer (e.g., lung adenocarcinoma); liver cancer; leukemia (e.g., acute myelogenous leukemia (AML)); melanoma; bladder cancer; kidney cancer; breast cancer, ovarian cancer, bile duct cancer, or glioma.

7. 发明专利

CA2915425A1 VACCINIA VIRUS FOR GENE-DIRECTED ENZYME PRODRUG THERAPY 未知
公开(公告)号：CA2915425A1
公开(公告)日：2014-12-24
申请号：CA2915425
申请日：2014-06-18
申请人： CANCER RES INST ROYAL
发明人： MARAIS RICHARD , SPRINGER CAROLINE , TOMMASINI SERENA
IPC分类号： A61K35/76 , A61K31/135 , A61K38/48 , A61P35/00
摘要： Methods of making vaccinia viruses for gene-directed prodrug therapy are disclosed and their use in the treatment of disease is provided. In particular, the anti-tumour effects of vaccinia viruses that are modified to express a prodrug-activating enzyme are disclosed.

8. 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**

9. 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.

10. 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.

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