13150-40-8Relevant academic research and scientific papers
Discovery of 3-(4-sulfamoylnaphthyl)pyrazolo[1,5-a]pyrimidines as potent and selective ALK2 inhibitors
Jiang, Jian-kang,Huang, Xiuli,Shamim, Khalida,Patel, Paresma R.,Lee, Arthur,Wang, Amy Q.,Nguyen, Kimloan,Tawa, Gregory,Cuny, Gregory D.,Yu, Paul B.,Zheng, Wei,Xu, Xin,Sanderson, Philip,Huang, Wenwei
supporting information, p. 3356 - 3362 (2018/09/21)
The pyrazolo[1,5-a]pyrimidine LDN-193189 is a potent inhibitor of activin receptor-like kinase 2 (ALK2) but is nonselective for highly homologous ALK3 and shows only modest kinome selectivity. Herein, we describe the discovery of a novel series of potent and selective ALK2 inhibitors by replacing the quinolinyl with a 4-(sulfamoyl)naphthyl, yielding ALK2 inhibitors that exhibit not only excellent discrimination versus ALK3 but also high kinome selectivity. In addition, the optimized compound 23 demonstrates good ADME and in vivo pharmacokinetic properties.
BMP INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 96, (2014/10/15)
The present invention provides small molecule inhibitors of BMP signaling. These compounds may be used to modulate cell growth, differentiation, proliferation, and apoptosis, and thus may be useful for treating diseases or conditions associated with BMP signaling, including inflammation, cardiovascular disease, hematological disease, cancer, and bone disorders, as well as for modulating cellular differentiation and/or proliferation. These compounds may also be used to reduce circulating levels of ApoB-100 or LDL and treat or prevent acquired or congenital hypercholesterolemia or hyperlipoproteinemia; diseases, disorders, or syndromes associated with defects in lipid absorption or metabolism; or diseases, disorders, or syndromes caused by hyperlipidemia.
Bismuth (III) salts as catalysts in the opening of epoxides by amines
Oussaid, Adyl,Garrigues, Bernard,Oussaid, Boualem,Benyaquad, Fatima
, p. 2315 - 2320 (2007/10/03)
BiCl3 and Bi (OTf)3 catalyze the opening of epoxides (1-7) by amines (8-12). High regioselectivities are observed. BiCl3 et Bi (OTf)3 catalysent la reaction d'ouverture des epoxydes (1-7) par les amines (8-12). La reaction est fortement regioselective.
