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US 10,894,777 B2Granted
TG2 inhibitor piperazine compounds and uses thereof
AssigneesUniversity of Ottawa, University of Maryland, Baltimore, University of Rochester
InventorsJeffrey W. Keillor, Abdullah Akbar, Richard L. Eckert, Matthew Fisher, Gail V. W. Johnson
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Abstract
There are provided Tissue Transglutaminase (TG2) inhibitor compounds, and compositions and methods of use thereof for the prevention or treatment of a cancer. Compounds of Formula I, and pharmaceutically acceptable salts thereof, are provided:
Claims12
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein:
- R1 is —C(O)—Ra;
- R2 is H or C1-6 alkyl, wherein C1-6 alkyl is optionally substituted with one or more substituents independently selected from the group consisting of C(O)NH2, C(O)OH, C(O)OC1-6 alkyl, NH2, NHC1-6 alkyl, N(C1-6 alkyl)2, OH, and OC(O)NH2;
- R3 is —C(O)—Re or —S(O)2—Rb;
- Ra is —CH2CH2-phenyl, —OCH2-phenyl, —OCH2-naphthalen-2-yl, —OCH2-pyridin-3-yl, —OCH2-quinolin-3-yl, phenyl, naphthalen-2-yl, or pyridin-3-yl;
- Rb is phenyl, naphthalen-1-yl, 5-(dimethylamino)naphthalen-1-yl, naphthalen-2-yl, 7-hydroxy-2H-chromen-2-on-3-yl, or 7-methoxy-2H-chromen-2-on-3-yl;
- and
- n is 1, 2, 3, or 4.
6 more elements
Dependencies are inferred from the claim text.