167705-70-6Relevant academic research and scientific papers
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.
Design and synthesis of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2- yl)-1H-quinolin-2-ones as VEGFR-2 kinase inhibitors
Han, Sun-Young,Choi, Jie Won,Yang, Jeon,Chae, Chong Hack,Lee, Jongkook,Jung, Heejung,Lee, Kwangho,Ha, Jae Du,Kim, Hyoung Rae,Cho, Sung Yun
scheme or table, p. 2837 - 2842 (2012/05/20)
A series of 3-(4,5,6,7-tetrahydro-3H-imidazo[4,5-c]pyridin-2-yl)-1H- quinolin-2-ones have been identified as a new class of VEGFR-2 kinase inhibitors. A variety of (4,5,6,7-tetrahydro-imidazo[5,4-c]pyridin-2-yl)-acetic acid ethyl esters were synthesized, and their VEGFR-2 inhibitory activity was evaluated. Described herein are the preparation of the series and the effects of the compounds on VEGFR-2 kinase activity.
Synthetic applications of 2-aryl-4-piperidones. X. Synthesis of 3-aminopiperidines, potential substance P antagonists
Diez,Diez, Anna,Voldoire,Voldoire, Aline,Lopez,Lopez, Isabel,Rubiralta,Rubiralta, Mario,Segarra,Segarra, Victor,Pages,Pages, Lluis,Palacios,Palacios, Jose M.
, p. 5143 - 5156 (2007/10/02)
A general method is described for the synthesis of 3-aminopiperidines from 4-piperidones based on a KOEt treatment of the tosylate of the corresponding oximes (Neber rearrangement). The procedure is applied to the synthesis of N-benzyl-3-amino-4,4-diethoxypiperidine (13), (R)-N-(2-hydroxy-1-phenyl)ethyl analogues 18, and 2-phenyl derivatives 27-28. The methoxybenzylation of the primary amino group of these aminopiperidines leads to a series of potential substance P antagonists.
