141106-23-2Relevant articles and documents
BENZOAZEPINE ANALOGS AS INHIBITING AGENTS FOR BRUTON'S TYROSINE KINASE
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, (2018/11/10)
Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, and methods for their production and compounds of formula (I) for use in treating a disease responsive to the inhibition of Bruton's tyrosine.
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6- dihydrobenzo[f]imidazo[1,2- d ][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2- methylpropanamide (GDC-0032): A β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity
Ndubaku, Chudi O.,Heffron, Timothy P.,Staben, Steven T.,Baumgardner, Matthew,Blaquiere, Nicole,Bradley, Erin,Bull, Richard,Do, Steven,Dotson, Jennafer,Dudley, Danette,Edgar, Kyle A.,Friedman, Lori S.,Goldsmith, Richard,Heald, Robert A.,Kolesnikov, Aleksandr,Lee, Leslie,Lewis, Cristina,Nannini, Michelle,Nonomiya, Jim,Pang, Jodie,Price, Steve,Prior, Wei Wei,Salphati, Laurent,Sideris, Steve,Wallin, Jeffery J.,Wang, Lan,Wei, Binqing,Sampath, Deepak,Olivero, Alan G.
, p. 4597 - 4610 (2013/07/19)
Dysfunctional signaling through the phosphoinositide 3-kinase (PI3K)/AKT/mTOR pathway leads to uncontrolled tumor proliferation. In the course of the discovery of novel benzoxepin PI3K inhibitors, we observed a strong dependency of in vivo antitumor activity on the free-drug exposure. By lowering the intrinsic clearance, we derived a set of imidazobenzoxazepin compounds that showed improved unbound drug exposure and effectively suppressed growth of tumors in a mouse xenograft model at low drug dose levels. One of these compounds, GDC-0032 (11l), was progressed to clinical trials and is currently under phase I evaluation as a potential treatment for human malignancies.
TRICYCLIC HETEROCYCLIC COMPOUNDS
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Page/Page column 214, (2011/06/16)
Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.