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US 2018/0000795 A1Published application
FACTOR XIa INHIBITORS
AssigneeMerck Sharp & Dohme Corp.
InventorsEric Mertz, Weiguo Liu, Scott D. Edmondson, Amjad Ali, Ying-Duo Gao, Santhosh F. Neelamkavil, Sung-Sau So, Remond Moningka, Wanying Sun, Alan Hruza, Linda L. Brockunier
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Abstract
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
Claims17
A compound of the formula:
- wherein X is —(C═O)NH or —NH(C═O)—;
- R1 is aryl, heteroaryl or C3-6 cycloalkyl, wherein said aryl, heteroaryl and cycloalkyl groups are optionally substituted with one to three substituents independently selected from the group consisting of halo, nitro, cyano, oxo, R4, OR4, (C═O)R4, (C═O)OR4, NR4R5, NH(C═O)R4, NH(C═O)OR4, C3-6 cycloalkyl and heteroaryl which is optionally substituted with R4;
- R2 is hydrogen, hydroxy, halo or C1-6 alkyl, wherein said alkyl is optionally substituted with one or two substituents independently selected from the group consisting of halo, OR4 or C3-6 cycloalkyl;
- R3 is aryl, heteroaryl or C3-10 cycloalkyl wherein said aryl, heteroaryl and cycloalkyl groups are optionally substituted with one to three substituents independently selected from the group consisting of halo, nitro, cyano, oxo, R4, OR4, (C═O)R4, (C═O)OR4, NR4R5, NH(C═O)R4, NH(C═O)OR4 and heteroaryl;
- R4 is hydrogen or C1-6 alkyl, which is optionally substituted with one to three groups independently selected from the group consisting of halo and hydroxy;
- R5 is hydrogen or C1-6 alkyl, which is optionally substituted with one to three groups independently selected from the group consisting of halo and hydroxy;
- Rx is hydrogen, hydroxy or halo;
- Rz is hydrogen, hydroxy, methoxy or halo;
- or a pharmaceutically acceptable salt thereof.
6 more elements
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(canceled)
Dependencies are inferred from the claim text.