发明名称 |
Pyrido[2,3-B]pyrazin-8-substituted compounds and their use |
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. |
申请公布号 |
US9155737(B2) |
申请公布日期 |
2015.10.13 |
申请号 |
US201414543379 |
申请日期 |
2014.11.17 |
申请人 |
INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE);CANCER RESEARCH TECHNOLOGY LIMITED |
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 |
分类号 |
A61K31/4985 |
主分类号 |
A61K31/4985 |
代理机构 |
Clark & Elbing LLP |
代理人 |
Clark & Elbing LLP |
主权项 |
1. A method of treatment of asthma or chronic obstructive pulmonary disease, comprising administering to a subject in need of treatment a therapeutically-effective amount of a compound of the following formulae, or a pharmaceutically acceptable salt thereof: wherein: —RPH1 is independently —F or —SMe; and —RPY1 is independently phenyl or pyridyl, and is optionally substituted with one or more substituents selected from —F, —Cl, —Br, —I, —R5, —OH, —OR5, —CF3, —OCF3, wherein each —R5 is independently saturated aliphatic C1-4alkyl. |
地址 |
London GB |