4-Quinazolinyloxy-diaryl ureas as novel BRAFV600E inhibitors
摘要:
Aryl phenyl ureas with a 4-quinazolinoxy substituent at the meta-position of the phenyl ring are potent inhibitors of mutant and wild type BRAF kinase. Compound 7 (1-(5-tert-butylisoxazol-3-yl)-3-(3-(6,7-dimethoxyquinazolin-4-yloxy) phenyl) urea hydrochloride) exhibits good pharmacokinetic properties in rat and mouse and is efficacious in a mouse tumor xenograft model following oral dosing. (C) 2011 Elsevier Ltd. All rights reserved.
MACROCYCLIC COMPOUNDS AND THEIR USE AS KINASE INHIBITORS
申请人:Combs Andrew Paul
公开号:US20090286778A1
公开(公告)日:2009-11-19
The present invention relates to macrocyclic compounds of Formula I:
or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
Sequential C–H activation enabled expedient delivery of polyfunctional arenes
作者:Wensen Ouyang、Xiaoqing Cai、Xiaojian Chen、Jie Wang、Jianhang Rao、Yang Gao、Yanping Huo、Qian Chen、Xianwei Li
DOI:10.1039/d1cc03243g
日期:——
Modularconstruction of polyfunctional arenes from abundant feedstocks stands as an unremitting pursue in synthetic chemistry, accelerating the discovery of drugs and materials. Herein, using the multiple C–H activation strategy with versatile imidate esters, the expedient delivery of molecular libraries of densely functionalized sulfur-containing arenes was achieved, which enabled the concise construction
[EN] AZAINDOLE DERIVATIVES AS MULTI KINASE INHIBITORS<br/>[FR] DÉRIVÉS AZA-INDOLIQUES UTILISÉS COMME INHIBITEURS DE MULTIPLES KINASES
申请人:ORIBASE PHARMA
公开号:WO2014102377A1
公开(公告)日:2014-07-03
The present invention relates to compounds of the following formula (I) and/or the pharmaceutically acceptable addition salts, solvates, enantiomers, diastereoisomers thereof, as well as mixtures thereof. The subject matter of the present invention thus also includes the preparation of compounds of formula (I), their uses, in particular in the inhibition of protein kinases which are implicated for example in numerous diseases such as cancers or immune system disorders.
Natural gallic acid catalyzed aerobic oxidative coupling with the assistance of MnCO<sub>3</sub> for synthesis of disulfanes in water
作者:Lijuan Song、Wenhao Li、Wenxue Duan、Jichao An、Shanyu Tang、Longjia Li、Guanyu Yang
DOI:10.1039/c9gc00091g
日期:——
value in synthetic chemistry and bioscience. To pursue a sustainable approach for such a synthesis, an aerobic oxidative coupling method for the efficient preparation of organic disulfanes, using a low-toxic natural gallic acid as an organocatalyst, inexpensive MnCO3 as a cocatalyst, O2 as the terminal oxidant and water as the solvent, has been successfully developed. Such metal–organic cooperative catalytic
DERIVATIVES OF 1-PHENYL-2-PYRIDINYL ALKYL ALCOHOLS AS PHOSPHODIESTERASE INHIBITORS
申请人:Chiesi Farmaceutici S.p.A.
公开号:US20130079313A1
公开(公告)日:2013-03-28
The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.