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US 2015/0087600 A1Published application
Therapeutically active compounds and their methods of use
AssigneeAgios Pharmaceuticals, Inc.
InventorsJaneta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Zhenwei Cai, Shunqi Yan, Ding Zhou
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Abstract
Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.
Claims20
A compound of formula I or a pharmaceutically acceptable salt or hydrate thereof, wherein:
- R1 is optionally substituted C4-C6 carbocyclyl;
- each R2 and R3 is independently selected from optionally substituted aryl or optionally substituted heteroaryl;
- R4 is saturated heterocyclyl, —CH(R5)N(R5)-heteroaryl, —CH(R5)N(R5)-aryl, —CH(R5)N(R5)-heterocyclyl, —CH(R5)N(R5)-carbocyclyl, heteroaralkyl, —CH2-heterocyclyl, 1H-indol-2-yl, indolin-2-yl, 1,2,3,4-tetrahydroquinolin-2-yl, imidazo[1,2-a]pyridine-5-yl, 5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-5-yl, —(CR5R6)1-4N(R5)C(O)O(C1-C6 alkyl), or —(CR5R6)1-4N(R5)SO2(C1-C6 alkyl), wherein each saturated heterocyclyl, heteroaryl, aryl, heterocyclyl, or carbocyclyl is independently optionally substituted;
- each R5 is independently selected from hydrogen and methyl;
- and
- each R6 is independently selected from hydrogen, methyl, CH2OH, CH(CH3)OH, CH2NH2, or CH(CH3)NH2;
- and provided that:
- (i) R4 is other than thien-2-ylmethyl, 1H-benizimidazol-1-ylmethyl, 1H-indol-3-ylmethyl, or 1H-benzotriazol-1-ylmethyl;
- and (ii) the compound is not N-[2-[[2-(cyclohexylamino)-1-(3-hydroxyphenyl)-2-oxoethyl]phenylamino]-2-oxoethyl]-carbamic acid 1,1-dimethylethyl ester or N-[2-[(2-benzoylphenyl)[2-(cyclohexylamino)-1-(3-hydroxyphenyl)-2-oxoethyl]amino]-2-oxoethyl]-carbamic acid 1,1-dimethylethyl ester.
6 more elements
The compound is selected from any one of compounds from Table 1.
Dependencies are inferred from the claim text.