Back to results
US 10,472,344 B2Granted
Factor XIa inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsAnthony K. Ogawa, Linda Brockunier, James Tata, Dann L. Parker, Jr., Ming Wang
Life of this patent
Estimating the term…
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.
Claims10
A compound of the formula:
- wherein R1 is aryl or heteroaryl, wherein said aryl and heteroaryl 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, C1-3 alkyl-NR4R5, NHC(O)R4, NHC(O)OR4, C3-6 cycloalkyl and heteroaryl (which is optionally substituted with halo, cyano, C(O)NR4R5 or R4);
- R2 is hydrogen or CH(R2a)(R2b);
- R2a is C1-6 alkyl, aryl, heteroaryl, C3-6 cycloalkyl or heterocyclyl, wherein said alkyl group is optionally substituted with one to three substituents independently selected from the group consisting of halo, cyano and OR4, and wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups are optionally substituted with one to three substituents independently selected from the group consisting of halo, nitro, cyano, oxo, R4 and OR4;
- R2b is hydrogen or C1-6 alkyl, which is optionally substituted with one to three substituents independently selected from the group consisting of halo, hydroxy and cyano;
- R3 is aryl, heteroaryl, C3-10 cycloalkyl or heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl 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, C(O)NR4R5, NR4R5, NHC(O)R4, NHC(O)OR4, NHC(O)C1-4alkyl-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;
- R6 is hydrogen, cyano, halo, R4 or OR4;
- R7 is hydrogen, cyano, halo, R4 or OR4;
- or a pharmaceutically acceptable salt thereof.
7 more elements
Dependencies are inferred from the claim text.