1219130-57-0Relevant articles and documents
SYK INHIBITORS
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Paragraph 3283; 3289-3291, (2016/10/07)
The present disclosure a Syk compound inhibitors, including state cancer and inflammation and various disease States thereof in the treatment of relates to the use of. In one aspect a particular embodiment, . given by formula I which is marked as a chemical structure of compound. In formula said, X 1, X 2, X 3, R 2, R 3, R 4, R 5, and Y has described herein is. The present disclosure of a formula I compounds or a pharmaceutically acceptable salt of pharmaceutical compositions including, mediated by Syk and to treat conditions a employing these compounds and compositions further provides a method. (by machine translation)
Discovery of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors
Lv, Yongcong,Li, Mengyuan,Cao, Sufen,Tong, Linjiang,Peng, Ting,Wei, Lixin,Xie, Hua,Ding, Jian,Duan, Wenhu
supporting information, p. 1375 - 1380 (2015/07/15)
Vascular endothelial growth factor receptor-2 (VEGFR-2) plays an important role in tumor angiogenesis, and inhibition of the VEGFR-2 signaling pathway has emerged as an attractive strategy for the treatment of cancer. Herein, we describe the design, synthesis, and biological evaluation of anilinopyrimidine-based naphthamide derivatives as potent VEGFR-2 inhibitors. Among the new derivatives, compound 3k exhibited high VEGFR-2 inhibitory potency in both enzymatic and VEGF-induced HUVEC cellular proliferation assays (IC50 = 0.5 and 9.8 nM, respectively). Kinase selectivity profiling revealed that 3k was a highly selective VEGFR-2 inhibitor. Moreover, 3k effectively inhibited angiogenesis in HUVEC tube formation assay.
HETEROCYCLIC BIARYL DERIVATIVE AND PDE INHIBITOR COMPRISING SAME AS ACTIVE INGREDIENT
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Page/Page column 31-32, (2011/08/04)
Novel heterocyclic biaryl derivatives were disclosed which are useful as pharmaceutical agents and which exhibit a phosphodiesterase-inhibitory action. The heterocyclic biaryl derivatives are represented by the following general formula (1): wherein the H
4, 5-DIHYDRO-LH-PYRAZOLE COMPOUNDS AND THEIR PHARMACEUTICAL USES
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Page/Page column 61, (2010/11/03)
Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.