1361941-21-0Relevant academic research and scientific papers
Scaffold Morphing Identifies 3-Pyridyl Azetidine Ureas as Inhibitors of Nicotinamide Phosphoribosyltransferase (NAMPT)
Palacios, Daniel S.,Meredith, Erik L.,Kawanami, Toshio,Adams, Christopher M.,Chen, Xin,Darsigny, Veronique,Palermo, Mark,Baird, Daniel,George, Elizabeth L.,Guy, Chantale,Hewett, Jeffrey,Tierney, Laryssa,Thigale, Sachin,Wang, Louis,Weihofen, Wilhelm A.
, p. 1524 - 1529 (2019/11/03)
Small molecules that inhibit the metabolic enzyme NAMPT have emerged as potential therapeutics in oncology. As part of our effort in this area, we took a scaffold morphing approach and identified 3-pyridyl azetidine ureas as a potent NAMPT inhibiting motif. We explored the SAR of this series, including 5 and 6 amino pyridines, using a convergent synthetic strategy. This lead optimization campaign yielded multiple compounds with excellent in vitro potency and good ADME properties that culminated in compound 27.
PYRAZOLOPYRIDINES AND PYRAZOLOPYRIDINES AND THEIR USE AS TYK2 INHIBITORS
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Page/Page column 187, (2012/06/01)
The invention provides compounds of Formula (I), stereoisomers or pharmaceutically acceptable salts thereof, wherein A, X, R1, R2, R4 and R5 are defined herein, a pharmaceutical composition that includes a compound of Formula (I) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of using the compound or composition in therapy, as TYK2 Kinase inhibitors.
PYRIDINONES/PYRAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF
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, (2012/03/26)
Pyridone and pyrazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
