1404115-38-3Relevant articles and documents
HIF-2α INHIBITORS FOR TREATING IRON OVERLOAD DISORDERS
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Paragraph 0739, (2016/05/02)
The present disclosure relates to HIF-2α inhibitors and methods of making and using them for treating iron overload disorders. Certain compounds were potent in HIF-2α scintillation proximity assay, luciferase assay, and VEGF ELISA assay, and reduced liver iron accumulation and serum iron parameters in both prophylactic and treatment mouse models.
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.