218631-48-2Relevant academic research and scientific papers
LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
-
Paragraph 0803, (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.
HUMAN PLASMA KALLIKREIN INHIBITORS
-
Page/Page column 144; 145, (2015/11/02)
Disclosed are compounds of formula (I), as described herein, and pharmaceutically acceptable salts thereof. The compounds are inhibitors of plasma kallikrein. Also provided are pharmaceutical compositions comprising at least one compound of the invention, and methods involving use of the compounds and compositions of the invention in the treatment and prevention of diseases and conditions characterized by unwanted plasma kallikrein activity.
Discovery of 1-(2-Aminomethylphenyl)-3-trifluoromethyl-N-[3-fluoro-2′ -(aminosulfonyl)[1,1′-biphenyl)]-4-yl]-1H-pyrazole-5-carboxyamide (DPC602), a Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor
Pruitt, James R.,Pinto, Donald J. P.,Galemmo Jr., Robert A.,Alexander, Richard S.,Rossi, Karen A.,Wells, Brian L.,Drummond, Spencer,Bostrom, Lori L.,Burdick, Debra,Bruckner, Robert,Chen, Haiying,Smallwood, Angela,Wong, Pancras C.,Wright, Matthew R.,Bai, Steven,Luettgen, Joseph M.,Knabb, Robert M.,Lam, Patrick Y. S.,Wexler, Ruth R.
, p. 5298 - 5315 (2007/10/03)
Factor Xa, a serine protease, is at the critical juncture between the intrinsic and extrinsic pathways of the coagulation cascade. Inhibition of factor Xa has the potential to provide effective treatment for both venous and arterial thrombosis. We recentl
INHIBITORS OF FACTOR XA WITH A NEUTRAL P1 SPECIFICITY GROUP
-
, (2008/06/13)
The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: STR1 or pharmaceutically acceptable salt forms thereof, wherein R and E may be groups such as methoxy and halo.
