219552-64-4Relevant academic research and scientific papers
LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
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Paragraph 0733; 0741, (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.
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors
Varnes, Jeffrey G.,Wacker, Dean A.,Jacobson, Irina C.,Quan, Mimi L.,Ellis, Christopher D.,Rossi, Karen A.,He, Ming Y.,Luettgen, Joseph M.,Knabb, Robert M.,Bai, Steven,He, Kan,Lam, Patrick Y.S.,Wexler, Ruth R.
, p. 6481 - 6488 (2008/03/18)
A new series of pyrazole-based factor Xa inhibitors have been identified as part of our ongoing efforts to optimize previously reported clinical candidate razaxaban. Concern over the possible formation of primary aniline metabolites via amide hydrolysis led to the replacement of the primary amide linker between the pyrazole and phenyl moieties with secondary amides. This was accomplished by replacing the aniline with a variety of heterobicycles, of which indolines were the most potent. The indoline series demonstrated subnanomolar factor Xa binding Kis, modest to high selectivity versus other serine proteases, and good in vitro clotting activity. A small number of indoline fXa inhibitors were profiled in a dog pharmacokinetic model, one of which demonstrated pharmacokinetic parameters similar to that of clinical candidate razaxaban.
Substituted benzazoles and methods of their use as inhibitors of Raf kinase
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Page 241, (2008/06/13)
New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
Antithrombotic agents
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, (2008/06/13)
This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
Synthesis and reactions of N-protected 3-nitroindoles
Pelkey,Gribble
, p. 1117 - 1122 (2007/10/03)
Treatment of N-protected indoles 3 with acetyl nitrate generated in situ at low temperatures affords the corresponding 3-nitroindoles 2 in good to excellent yields. Deprotection of 1-acetyl-3-nitroindole (2h) with DBU gives 3-nitroindole (1). Reaction of
