Histone demethylase inhibitors
AssigneeQuanticel Pharmaceuticals, Inc.
InventorsZhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
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Abstract
Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.
Claims25
A compound of Formula (II), or a pharmaceutically acceptable salt thereof,
- wherein,
- R1 is hydrogen, halogen, —OH, —OR5, —N(R5)2, alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, carbocyclylalkyl, heterocyclylalkyl, aralkyl, or heteroarylalkyl;
- R2 is hydrogen, halogen, —OH, —OR5, —N(R5)2, alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, carbocyclylalkyl, heterocyclylalkyl, aralkyl, or heteroarylalkyl;
- R4 is hydrogen or alkyl;
- and
- each R5 is independently hydrogen, alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, carbocyclylalkyl, heterocyclylalkyl, aralkyl, or heteroarylalkyl.
A compound of Formula (IV) or a pharmaceutically acceptable salt thereof,
- wherein,
- R1 is hydrogen, halogen, —OH, —OR5, —N(R5)2, alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, carbocyclylalkyl, heterocyclylalkyl, aralkyl, or heteroarylalkyl;
- R2 is hydrogen, halogen, —OH, —OR5, —N(R5)2, alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, carbocyclylalkyl, heterocyclylalkyl, aralkyl, or heteroarylalkyl;
- R3 is —O—X—Y;
- R4 is hydrogen or alkyl;
- each R5 is independently hydrogen, alkyl, carbocyclyl, heterocyclyl, aryl, heteroaryl, carbocyclylalkyl, heterocyclylalkyl, aralkyl, or heteroarylalkyl;
- X is C1-C8 alkylene or
- where n is 0 to 4;
- and
- Y is hydrogen, carbocyclyl, aryl, or heteroaryl.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound Formula (II) or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound Formula (IV) or a pharmaceutically acceptable salt thereof.
A method for inhibiting a histone-demethylase enzyme comprising contacting a histone demethylase enzyme with a compound of Formula (II).
A method for inhibiting a histone-demethylase enzyme comprising contacting a histone demethylase enzyme with a compound of Formula (IV).
A method for treating cancer in subject comprising administering to the subject in need thereof a composition comprising a compound of Formula (II) or pharmaceutically acceptable salt thereof.
A method for treating cancer in subject comprising administering to the subject in need thereof a composition comprising a compound of Formula (IV) or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.