1329166-65-5Relevant articles and documents
Macrocyclic factor XIa inhibitors
Wang, Cailan,Corte, James R.,Rossi, Karen A.,Bozarth, Jeffrey M.,Wu, Yiming,Sheriff, Steven,Myers, Joseph E.,Luettgen, Joseph M.,Seiffert, Dietmar A.,Wexler, Ruth R.,Quan, Mimi L.
, p. 4056 - 4060 (2017)
A series of macrocyclic factor XIa (FXIa) inhibitors was designed based on an analysis of the crystal structures of the acyclic phenylimidazole compounds. Further optimization using structure-based design led to inhibitors with pM affinity for FXIa, excellent selectivity against a panel of relevant serine proteases, and good potency in the activated partial thromboplastin time (aPTT) clotting assay.
CYCLIC P1 LINKERS AS FACTOR XIA INHIBITORS
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Paragraph 00305, (2013/03/26)
The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
MACROCYCLES AS FACTOR XIA INHIBITORS
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Page/Page column 139, (2011/09/15)
The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.