Inhibitors of tissue transglutaminase 2 (tg2) and uses thereof
AssigneesNorthwestern University, THE UNITED STATES GOVERMENT as represented by the DEPARTMENT OF VETERAN'S AFFAIRS
InventorsGary E. Schiltz, Daniela E. Matei, Purav Vagadia
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Abstract
Disclosed are compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject in need thereof. The disclosed compounds inhibit the activity of tissue transglutaminase 2 (TG2). As such, the disclosed compounds and pharmaceutical compositions may be utilized in methods for treating a subject having or at risk for developing a disease or disorder that is associated with TG2 activity which may be cell proliferative diseases and disorders such as cancer.
Claims22
A compound of a formula:
- or a salt or solvate thereof,
- wherein:
- Z is pyrimidinyl or 5,7-diazaindolinyl and Z optionally is substituted at one or more ring positions with alkyl, alkoxy, amino, alkylamino, dialkylamino, heteroaryl, or halo;
- V is NR1 or O, wherein R1 is hydrogen or alkyl;
- m is selected from 0-6;
- Y is an aryl group, a diaryl group, or a heteroaryl group, and Y optionally is substituted at one or more ring positions with haloalkyl;
- n is selected from 0-6;
- W is NR2 or CH, wherein R2 is hydrogen or alkyl;
- R3 and R3′ are hydrogen or R3 and R3′ together form oxo;
- p is selected from 0-6;
- and
- X is an aryl group or a heteroaryl group, and X optionally is substituted at one or more ring positions with one or more of alkyl, alkoxy, halo;
- amino;
- alkylamino, or aryl;
- and
- optionally with the proviso that if m is 0, n is 0, and p is 1, then X is not N-imidazyl or indol-3-yl;
- and
- optionally with the proviso that if m is 0, n is 0, and p is 1, then Z is not 4-dimethylamino-pyrimidin-2-yl or 4-pyrrolidin-1-yl-pyrimidin-2-yl.
Dependencies are inferred from the claim text.