178448-14-1Relevant articles and documents
HETEROCYCLIC COMPOUNDS AS INHIBITORS OF RAS AND METHODS OF USE THEREOF
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Page/Page column 146, (2018/04/21)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R", Q, W, X, Y, Z, n1, n2and '--" are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also disclosed.
In vitro intrinsic clearance-based optimization of N3- phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists
Hartz, Richard A.,Ahuja, Vijay T.,Rafalski, Maria,Schmitz, William D.,Brenner, Allison B.,Denhart, Derek J.,Ditta, Jonathan L.,Deskus, Jeffrey A.,Yue, Eddy W.,Arvanitis, Argyrios G.,Lelas, Snjezana,Li, Yu-Wen,Molski, Thaddeus F.,Wong, Harvey,Grace, James E.,Lentz, Kimberley A.,Li, Jianqing,Lodge, Nicholas J.,Zaczek, Robert,Combs, Andrew P.,Olson, Richard E.,Mattson, Ronald J.,Bronson, Joanne J.,Macor, John E.
experimental part, p. 4161 - 4172 (2010/02/28)
A series of pyrazinone-based heterocycles was identified as potent and orally active corticotropinreleasing factor-1 (CRF1) receptor antagonists. Selected compounds proved efficacious in an anxiety model in rats; however, pharmacokinetic proper
Use of EP4 receptor ligands in the treatment of IL-6 involved diseases
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Page 110, (2010/02/06)
Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.
Structure-activity relationships of alkyl- and alkoxy-substituted 1,4- dihydroquinoxaline-2,3-diones: Potent and systemically active antagonists for the glycine site of the NMDA receptor
Cai, Sui Xiong,Kher, Sunil M.,Zhou, Zhang-Lin,Ilyin, Victor,Espitia, Stephen A.,Tran, Minhtam,Hawkinson, Jon E.,Woodward, Richard M.,Weber, Eckard,Keana, John F. W.
, p. 730 - 738 (2007/10/03)
We report on a series of alkyl- and alkoxy-substituted 1,4- dihydroquinoxaline-2,3-diones (QXs), prepared as a continuation of our structure-activity relationship (SAR) study of QXs as antagonists for the glycine site of the N-methyl-D-aspartate (NMDA) re