Macrocycles as factor xia inhibitors

602266 Disclosed are 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. Also disclosed are pharm...

Full description

Saved in:
Bibliographic Details
Main Authors PINTO DONALD J. P, FANG TIANAN, WANG YUFENG, SMALLHEER JOANNE M, JEON YOON, ROSSI KAREN A, CORTE JAMES R, HU ZILUN, QUAN MIMI L, YANG WU, DECICCO CARL P
Format Patent
LanguageEnglish
Published 30.05.2014
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
Online AccessGet full text

Cover

More Information
Summary:602266 Disclosed are 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. Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using them. Examples of compound of formula (I) are: (9S,14S)-14-[(E)-3-(5-Chloro-2-tetrazol-1-yl-phenyl)-acryloylamino]-5-(2-methoxyethoxycarbonylamino)-8,16-diaza-tricyclo[13.3.1.02,7]nonadeca-1(19),2,4,6,15,17-hexaene-9-carboxylic acid ethyl ester, bis-trifluoroacetic acid salt; (9R,14S)-14-[(E)-3-(5-Chloro-2-tetrazol-1-yl-phenyl)-acryloylamino]-5-methoxycarbonylamino-8,17-diaza-tricyclo[13.3.1.02,7]nonadeca-1(19),2(7),3,5,15,17-hexaene-9-carboxylic acid ethyl ester 2-TFA salt and 9R,14S)-14-[(E)-3-(5-Chloro-2-tetrazol-1-yl-phenyl)-acryloylamino]-5-methoxycarbonylamino-8,16-diaza-tricyclo[13.3.1.02,7]nonadeca-1(19),2(7),3,5,15,17-hexaene-9-carboxylic acid ethyl ester.
Bibliography:Application Number: NZ20110602266