872459-77-3Relevant articles and documents
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
SIX-MEMBERED HETEROCYCLES USEFUL AS SERINE PROTEASE INHIBITORS
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Page/Page column 80, (2010/02/15)
The present invention provides compounds of Formula (I) or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, X1, X2, X3, X4, and X5 are as defined herein. The compounds of Formula (I) are useful as 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.