专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2009130487A1 ARYL-QUINOLYL COMPOUNDS AND THEIR USE 审中-公开
标题翻译： ARYL-QUINOLYL化合物及其用途
公开(公告)号：WO2009130487A1
公开(公告)日：2009-10-29
申请号：PCT/GB2009/001077
申请日：2009-04-27
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE) , NICULESCU-DUVAZ, Ion , ZAMBON, Alfonso , NICULESCU-DUVAZ, Dan , WHITTAKER Steven , MARAIS, Richard , SPRINGER, Caroline Joy
发明人： NICULESCU-DUVAZ, Ion , ZAMBON, Alfonso , NICULESCU-DUVAZ, Dan , WHITTAKER Steven , MARAIS, Richard , SPRINGER, Caroline Joy
IPC分类号： C07D471/04 , A61K31/4985 , A61P35/00
CPC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 aryl-quinolyl 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.
摘要翻译：本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些芳基 - 喹啉基化合物，其特别地抑制RAF（例如，B-RAF）活性。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体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制细胞增殖，以及通过抑制RAF，RTK等改善的增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。

2. 发明申请

WO2015075483A1 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 审中-公开
标题翻译： 1-（5-叔丁基-2-亚氨基 - 吡咯-3-基）-3- [2-氟-4 - [（3-氧代-4H-吡啶并[2,3-b]吡嗪-8-基））OXY]苯胺]尿素衍生物作为RAF抑制剂治疗癌症
公开(公告)号：WO2015075483A1
公开(公告)日：2015-05-28
申请号：PCT/GB2014/053490
申请日：2014-11-25
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
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
CPC分类号： C07D471/04
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.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地说，本发明涉及某些1-（5-叔丁基-2-芳基 - 吡唑-3-基）-3- [2-氟-4 - [（3-氧代-4H-吡啶并[2,3 -b]吡嗪-8-基）氧基]苯基]脲化合物（在本文中称为“TBAP化合物”），特别是抑制RAF（例如BRAF，CRAF等）。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体外和体内都用于抑制RAF（例如BRAF，CRAF等）的用途; 并治疗疾病，包括：增殖性疾病; 癌症（包括例如恶性黑素瘤，结肠直肠癌，胰腺癌）; 炎; 免疫学障碍; 病毒感染; 纤维化疾病; 与突变形式的RAF（例如BRAF，CRAF等）相关的疾病; 通过抑制RAF（例如BRAF，CRAF等）改善的疾病; 通过突变BRAF的抑制改善的疾病; 通过抑制BRAF和CRAF而改善的疾病; 与RAS突变和/或MAPK通路活化相关的疾病; 通过抑制SRC，p38，FGFRA，VEGFR-2（KDR）和/或LCK而改善的疾病; 等等

3. 发明申请

WO2015075482A1 PROCESS FOR THE PREPARATION OF 8-(4-AMINOPHENOXY)-4H-PYRIDO[2,3-B]PYRAZIN-3-ONE DERIVATIVES 审中-公开
标题翻译：制备8-（4-氨基苯氧基）-4H-吡啶并[2,3-b]吡嗪-3-酮衍生物的方法
公开(公告)号：WO2015075482A1
公开(公告)日：2015-05-28
申请号：PCT/GB2014/053489
申请日：2014-11-25
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
发明人： ZAMBON, Alfonso , NICULESCU-DUVAZ, Dan , CHUBB, Richard , SPRINGER, Caroline Joy
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)- 4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl- phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
摘要翻译：本发明一般涉及有机化学合成领域，特别涉及合成8-（4-氨基苯氧基）-4H-吡啶并[2,3-b]吡嗪-3-酮和相关化合物的某些方法（由4-（4-氨基苯氧基）吡啶-2,3-二胺和相关化合物（在本文中表示为（1）），通过与乙醛酸（本文表示为（2））反应）表示为（3））。化合物（3）可用于合成已知的抗癌剂，例如1-（5-叔丁基-2-（4-甲基 - 苯基） - 吡唑-3-基）-3- [2- 氟-4 - [（3-氧代-4H-吡啶并[2,3-b]吡嗪-8-基）氧基]苯基]脲。

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