942318-15-2Relevant academic research and scientific papers
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group
Corte, James R.,Fang, Tianan,Pinto, Donald J.P.,Orwat, Michael J.,Rendina, Alan R.,Luettgen, Joseph M.,Rossi, Karen A.,Wei, Anzhi,Ramamurthy, Vidhyashankar,Myers, Joseph E.,Sheriff, Steven,Narayanan, Rangaraj,Harper, Timothy W.,Zheng, Joanna J.,Li, Yi-Xin,Seiffert, Dietmar A.,Wexler, Ruth R.,Quan, Mimi L.
, p. 2257 - 2272 (2016/04/26)
Pyridine-based Factor XIa (FXIa) inhibitor (S)-2 was optimized by modifying the P2 prime, P1, and scaffold regions. This work resulted in the discovery of the methyl N-phenyl carbamate P2 prime group which maintained FXIa activity, reduced the number of H
ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
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Page/Page column 229-230, (2008/06/13)
The present invention provides compounds of Formula (I): Formula (I) or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
