796062-33-4Relevant articles and documents
FUSED BICYCLIC RAF INHIBITORS AND METHODS FOR USE THEREOF
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Paragraph 0586; 0589; 0590, (2022/02/09)
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method o
Design and synthesis of a Pan-Janus kinase inhibitor clinical candidate (PF-06263276) suitable for inhaled and topical delivery for the treatment of inflammatory diseases of the lungs and skin
Jones, Peter,Storer, R. Ian,Sabnis, Yogesh A.,Wakenhut, Florian M.,Whitlock, Gavin A.,England, Katherine S.,Mukaiyama, Takasuke,Dehnhardt, Christoph M.,Coe, Jotham W.,Kortum, Steve W.,Chrencik, Jill E.,Brown, David G.,Jones, Rhys M.,Murphy, John R.,Yeoh, Thean,Morgan, Paul,Kilty, Iain
, p. 767 - 786 (2017/02/05)
By use of a structure-based computational method for identification of structurally novel Janus kinase (JAK) inhibitors predicted to bind beyond the ATP binding site, a potent series of indazoles was identified as selective pan-JAK inhibitors with a type 1.5 binding mode. Optimization of the series for potency and increased duration of action commensurate with inhaled or topical delivery resulted in potent pan-JAK inhibitor 2 (PF-06263276), which was advanced into clinical studies.