Histone demethylase inhibitors
AssigneeCelgene Quanticel Research, Inc.
InventorsZhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennan Wallace
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Abstract
The present embodiments provide for substituted triazolylpyridine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for modulating the activity of histone demethylase enzymes. Additionally, the subject compounds and compositions are useful for the treatment of cancer or other neoplastic diseases, or maladies associated with abnormal histone demethylase activity. Accordingly, the substituted triazolylpyridine derivative compounds described herein are useful in methods and medicaments for treating cancer.
Claims4
A method of inhibiting a histone demethylase enzyme selected from a group comprising FBXL10, JARID1B, JMJD2C and JMJD3 comprising contacting a histone demethylase enzyme with an effective amount of a compound of Formula II
- wherein a compound of Formula II is optionally a pharmaceutically acceptable salt thereof, and wherein
- R2 is halogen or —CF3;
- R3 is hydrogen, halogen, —OH, —OR6, —N(R6)2, or alkyl, carbocyclyl, aryl optionally substituted with halogen, carbocyclylalkyl, or aralkyl optionally substituted with halogen or alkyl;
- R4 is hydrogen, halogen, —OH, —OR6, —N(R6)2, or alkyl, carbocyclyl, aryl, carbocyclylalkyl, or aralkyl;
- wherein
- each R6 is independently hydrogen, or optionally substituted alkyl, carbocyclyl, aryl, carbocyclylalkyl, or aralkyl;
- and
- R5 is hydrogen, methyl, ethyl, isopropyl, t-butyl, —CHF2, —CH2F, —CF3, —CH2OH, —CHCH3OH, or —C(CH3)2OH.
Dependencies are inferred from the claim text.