Plasma kallikrein inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsNatalija Cernaka, Anthony K. Ogawa, Alan C. Cheng, Jianming Bao, Phillip Patrick Sharp, Jovan Alexander Lopez, Dong Xiao, Haiqun Tang
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 one or more disease states that could benefit from inhibition of plasma kallikrein, including hereditary angioedema, uveitis, posterior uveitis, wet age-related macular degeneration, diabetic macular edema, diabetic retinopathy and retinal vein occlusion. The compounds are selective inhibitors of plasma kallikrein.
Claims18
A compound of the Formula I:
- wherein X is —CH2—, —NH(C═O)CH2— or —(C═O)NHCH2—;
- is phenyl or heteroaryl, which can be monocyclic or bicyclic, wherein said phenyl is optionally substituted with halo and said heteroaryl is optionally substituted with halo, hydroxy, C1-6 alkyl or oxo;
- R1 is selected from the group consisting of hydrogen, halo, hydroxy and C1-6 alkyl;
- R2 is selected from the group consisting of hydrogen, halo, hydroxy and C1-6 alkyl;
- R3 is selected from the group consisting of hydrogen, heterocyclyl, which can be monocyclic or bicyclic, heteroaryl and NR4R5, wherein said heteroaryl is optionally substituted with one or two substituents independently selected from the group consisting of oxo and C1-6 alkyl and said heterocyclyl is optionally substituted with one to three substituents independently selected from the group consisting of halo, hydroxy, cyano and Rx;
- R4 is selected from the group consisting of hydrogen, cyclopropyl and C1-6 alkyl;
- R5 is selected from the group consisting of hydrogen and C1-6 alkyl, which is optionally substituted with one to three substituents selected from the group consisting of halo, hydroxy and cyano;
- Rx is hydrogen or C1-6 alkyl, which is optionally substituted with one to three substituents selected from the group consisting of halo, hydroxy and methoxy;
- n is an integer from zero to two;
- or a pharmaceutically acceptable salt thereof.
(canceled)
(canceled)
Dependencies are inferred from the claim text.