1202645-17-7Relevant articles and documents
A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors
Schulte, Christie A.,Deaton, David N.,Diaz, Elsie,Do, Young,Gampe, Robert T.,Guss, Jeffrey H.,Hancock, Ashley P.,Hobbs, Heather,Hodgson, Simon T.,Holt, Jason,Jeune, Michael R.,Kahler, Kirsten M.,Kramer, H. Fritz,Le, Joelle,Mortenson, Paul N.,Musetti, Caterina,Nolte, Robert T.,Orband-Miller, Lisa A.,Peckham, Gregory E.,Petrov, Kim G.,Pietrak, Beth L.,Poole, Chuck,Price, Daniel J.,Saxty, Gordon,Shillings, Anthony,Smalley, Terrence L.,Somers, Don O.,Stewart, Eugene L.,Stuart, J. Darren,Thomson, Stephen A.
, (2021)
Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally active imidazopyridine inhibitor of H-PGDS, 20b. Herein, describes the identification of 2 classes of inhibitors, their syntheses, and their challenges.
METHODS FOR DELAYING, PREVENTING, AND TREATING ACQUIRED RESISTANCE TO RAS INHIBITORS
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Paragraph 00504, (2022/01/04)
The present disclosure relates to compositions and methods for the treatment of diseases or disorders (e.g., cancer) with bi-steric inhibitors of mTOR in combination with RAS inhibitors. Specifically, in some embodiments this disclosure includes compositions and methods for inducing apoptosis of tumor cells and/or for delaying, preventing, or treating acquired resistance to RAS inhibitors using bi-steric mTOR inhibitors.
Discovery of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold
Deng, Yongqi,Doty, Amy,Ferguson, Heidi,Fradera, Xavier,Han, Yongxin,Jonathan Bennett, David,Knemeyer, Ian,Lesburg, Charles A.,Li, Derun,Liu, Kun,Martinot, Theo,Otte, Karin,Richard Miller, J.,Sciammetta, Nunzio,Sloman, David,Vincent, Stella,Yu, Wensheng
, (2021/08/27)
A series of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold were identified with good cellular and human whole blood activity against IDO1. These inhibitors contain multiple chiral centers and all diastereomers were separated. The absolute stereochemistry of each isomers were not determined. Compounds 15 and 27 stood out as leads due to their good cellular as well as human whole blood IDO1 inhibition activity, low unbound clearance, and reasonable mean residence time in rat cassette PK studies.