175153-03-4Relevant articles and documents
Ring size changes in the development of class I HDAC inhibitors
Cho, Er-Chieh,Liu, Chi-Yuan,Tang, Di-Wei,Lee, Hsueh-Yun
, p. 1387 - 1401 (2021/07/06)
Five pathways involving different ring structures led to generation of fourteen thienylbenzamides (7–20) which display the structure-activity relationships of class I HDAC inhibitors. All the synthesised compounds inhibit HDAC1 and HDAC2 selectively over other isoforms and many inhibit DLD1 and HCT116 cells more effectively than a parent compound. Compounds 8 and 16 inhibit HCT116 cells by activation of the apoptosis pathway.
LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
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, (2017/04/28)
The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties
Corte, James R.,Fang, Tianan,Pinto, Donald J.P.,Han, Wei,Hu, Zilun,Jiang, Xiang-Jun,Li, Yun-Long,Gauuan, Jolicia F.,Hadden, Mark,Orton, Darren,Rendina, Alan R.,Luettgen, Joseph M.,Wong, Pancras C.,He, Kan,Morin, Paul E.,Chang, Chong-Hwan,Cheney, Daniel L.,Knabb, Robert M.,Wexler, Ruth R.,Lam, Patrick Y.S.
, p. 2845 - 2849 (2008/12/21)
Introduction of the phenyl piperidinone and phenyl pyridinone P4 moieties in the anthranilamide scaffold led to potent, selective, and orally bioavailable inhibitors of factor Xa. Anthranilamide 28 displayed comparable efficacy to apixaban in the rabbit a