348133-45-9Relevant academic research and scientific papers
2, 4-DI-(NITROGEN CONTAINING GROUP) SUBSTITUTED PYRIMIDINE COMPOUND AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0218, (2018/07/29)
Provided are a 2, 4-di-(nitrogen containing group) substituted pyrimidine compound represented by a general formula (I), a pharmaceutically acceptable salt and a stereoisomer thereof, a preparation method thereof, and a use thereof in preparation of anti-tumor drugs. The compound having a structural feature shown in the general formula (I) can selectively suppress activity of mutant epidermal growth factor receptors (EGFR), including single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. The compound has a weak suppression effect on wild-type EFGR and a very high selectivity, and thus it has a potential to be used in preparation of drugs for treating EGFR mutant tumors, especially non-small cell lung cancer (NSCLC) comprising a T790M EGFR mutation.
PARG INHIBITORY COMPOUNDS
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Paragraph 00291; 00292; 00295; 00296, (2016/07/05)
The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity: wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
Bamborough, Paul,Barnett, Heather A.,Becher, Isabelle,Bird, Mark J.,Chung, Chun-Wa,Craggs, Peter D.,Demont, Emmanuel H.,Diallo, Hawa,Fallon, David J.,Gordon, Laurie J.,Grandi, Paola,Hobbs, Clare I.,Hooper-Greenhill, Edward,Jones, Emma J.,Law, Robert P.,Le Gall, Armelle,Lugo, David,Michon, Anne-Marie,Mitchell, Darren J.,Prinjha, Rab K.,Sheppard, Robert J.,Watson, Allan J. B.,Watson, Robert J.
, p. 552 - 557 (2016/07/06)
The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engag
1,3-dimethyl benzimidazolones are potent, selective inhibitors of the brpf1 bromodomain
Demont, Emmanuel H.,Bamborough, Paul,Chung, Chun-Wa,Craggs, Peter D.,Fallon, David,Gordon, Laurie J.,Grandi, Paola,Hobbs, Clare I.,Hussain, Jameed,Jones, Emma J.,Le Gall, Armelle,Michon, Anne-Marie,Mitchell, Darren J.,Prinjha, Rab K.,Roberts, Andy D.,Sheppard, Robert J.,Watson, Robert J.
, p. 1190 - 1195 (2015/04/27)
The BRPF (bromodomain and PHD finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. Here, we report the discovery, binding mode, and structure-activity relationship (SAR) of the firs
TRICYCLIC COMPOUNDS AS TEC KINASE INHIBITORS
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, (2013/11/05)
The present invention is directed to tricyclic compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermed
Substituted piperazine derivatives, the preparation thereofand their use as medicaments
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, (2008/06/13)
The present invention relates to substituted piperazine derivatives of general formula , (I wherein Ra, Rb, Rc, Rf, Rg, X, m and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.
