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US 2019/0055212 A1Published application
Histone demethylase inhibitors
OwnerStephen Gwaltneyinventor
Life of this patent
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Abstract
This disclosure relates to compounds that inhibit histone demethylase activity. In particular, the disclosure relates to compounds that inhibit histone lysine demethylase KDM5B, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions disclosed herein.
Claims27
A compound of formula (I):
- or a pharmaceutical salt thereof:
- wherein:
- R1 is —COOR6, —C(O)N(H)CN, —C(O)N(H)OH, or tetrazolyl;
- R2 is C0-C6 alkyl-R7;
- R3 and R4 are each independently selected from hydrogen, halogen, alkyl, alkoxy, —(CH2)nOH, —(CH2)nC(O)NHR6, —(CH2)nC(O)NHR5, —(CH2)n C(O)NHR7, —(CH2)n C(O)NR6R7, —(CH2), N(R6)C(O)R5, (CH2)nN(R6)C(O)R7, or —(CH2)nNHC(O)R5, —(CH2)n NHC(O)R7, carbocyclyl, heterocyclyl, aryl, heteroaryl, alkylcarbocyclyl, alkylheterocyclyl, alkylaryl, alkylheteroaryl, wherein each of the carbocyclyl, heterocyclyl, aryl, heteroaryl, alkylcarbocyclyl, alkylheterocyclyl, alkylaryl, alkylheteroaryl is optionally substituted with one or more R;
- or R3 and R4 and the carbon atoms to which they are attached form a 5-7 membered unsaturated, partial unsaturated or saturated ring system optionally containing 1-3 heteroatoms selected from N, O or S, and further optionally substituted with one or more R5;
- R5 is alkyl, alkenyl, alkynyl, halogen, haloalkyl, alkoxy, cyano, amino, —COOR6, C(O)NHR6, C(O)N(R6)2, N(R6)C(O)R3, NHC(O)R3 aryloxy, or optionally substituted heterocyclyl;
- R6 is hydrogen or alkyl;
- R7 is hydrogen, carbocyclyl, heterocyclyl, aryl, or heteroaryl, wherein each of the carbocyclyl, heterocyclyl, aryl, or heteroaryl may be optionally substituted with one or more R5;
- or
- R6 and R7 and the nitrogen atom to which they are attached form a 4-7 membered unsaturated, partial unsaturated or saturated ring system optionally containing 1-3 heteroatoms selected from N, O or S, and further optionally substituted with one or more R;
- and
- m and n are each independently zero or an integer between 1 and 3.
10 more elements
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Dependencies are inferred from the claim text.