MACROCYCLES WITH HETROCYCLIC P2' GROUPS AS FACTOR XIA INHIBITORS

• Main Authors: Tianan FANG, Leon M. SMITH, II, Donald J. P. PINTO, Michael J. ORWAT, William R. EWING, Ruth R. WEXLER, Wu YANG, Yeheng ZHU, James R. CORTE, Indawati DE LUCCA, Andrew K. DILGER, Yufeng WANG, Kumar Balashanmuga PABBISETTY
• Format: Patent
• Language: English; Spanish
• Published: 03.10.2016
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The present invention provides compounds of Formula (I): 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. La presente invención proporciona compuestos de la Fórmula (I): (ver Fórmula) o estereoisómeros, tautómeros o sales de aquellos aceptables desde el punto de vista farmacéutico, en donde todas las variables son como se definen en la presente. Estos compuestos son inhibidores selectivos del factor XIa o inhibidores duales de FXIa y calicreína plasmática. La presente invención también se refiere a composiciones farmacéuticas que comprenden estos compuestos y a métodos para tratar trastornos tromboembólicos y/o inflamatorios mediante su uso.