1379974-95-4Relevant academic research and scientific papers
EZH2 Inhibitors
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Paragraph 0154; 0156, (2018/11/02)
The present invention relates to compounds that inhibit EZH2 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
SUBSTITUTED DIHYDROISOQUINOLINONE COMPOUNDS
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Paragraph 0507, (2015/12/30)
This invention relates to compounds of general formula (I) in which R1, R2, R3, R4, L, X and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
Phenethyl nicotinamides, a novel class of NaV1.7 channel blockers: Structure and activity relationship
Kers, Inger,MacSari, Istvan,Csjernyik, Gabor,Nyloef, Martin,Skogholm, Karin,Sandberg, Lars,Minidis, Alexander,Bueters, Tjerk,Malmborg, Jonas,Eriksson, Anders B.,Lund, Per-Eric,Venyike, Elisabet,Luo, Lei,Nystroem, Jan-Erik,Besidski, Yevgeni
, p. 6108 - 6115 (2012/10/30)
The NaV1.7 ion channel is an attractive target for development of potential analgesic drugs based on strong genetic links between mutations in the gene coding for the channel protein and inheritable pain conditions. The (S)-N-chroman-3-ylcarboxamide series, exemplified by 1, was used as a starting point for development of new channel blockers, resulting in the phenethyl nicotinamide series. The structure and activity relationship for this series was established and the metabolic issues of early analogues were addressed by appropriate substitutions. Compound 33 displayed acceptable overall in vitro properties and in vivo rat PK profile.
