Substituted benzene compounds
AssigneeEpizyme, Inc.
InventorsKevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki, Syuji Shirotori, Wataru Itano, Wanjun Zheng
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AssigneeEpizyme, Inc.
InventorsKevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki, Syuji Shirotori, Wataru Itano, Wanjun Zheng
Estimating the term…
The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
A compound of Formula III:
A compound of Formula II:
A compound of Formula VI or VII:
Dependencies are inferred from the claim text.
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1,4-Oxazines, e.g. morpholine: not condensed and containing further heterocyclic rings, e.g. timolol
Non condensed pyridines; Hydrogenated derivatives thereof: having oxo groups directly attached to the heterocyclic ring
Containing further heterocyclic ring systems: containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
Having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines: 1,4-Oxazines, e.g. morpholine
About 7 years of term left · ends 15 Oct 2033 (estimated)
The contents of the text file named “EPIZ-029N01US-ST25.txt”, which was created on Apr. 14, 2015 and is 5 KB in size, are hereby incorporated by reference in their entireties.
This invention was developed subject to a Joint Research Agreement between Epizyme, Inc. and Eisai Co., Ltd.
There is an ongoing need for new agents as inhibitors of EZH2 activity, which can be used for treating EZH2-mediated disorder (e.g., cancer).
The present invention provides novel substituted benzene compounds, synthetic methods for making the compounds, pharmaceutical compositions containing them and various uses of the compounds.
In one aspect, the invention relates to a compound according to Formula I:
or a pharmaceutically acceptable salt thereof; wherein R701 is H, F, OR707, NHR707, —(C≡C)—(CH2)n7—R708, phenyl, 5- or 6-membered heteroaryl, C3-8 cycloalkyl, or 4-7 membered heterocycloalkyl containing 1-3 heteroatoms, wherein the phenyl, 5- or 6-membered heteroaryl, C3-8 cycloalkyl or 4-7 membered heterocycloalkyl each independently is optionally substituted with one or more groups selected from halo, C1-3 alkyl, OH, O—C1-6 alkyl, NE-C1-6 alkyl, and, C1-3 alkyl substituted with C3-8 cycloalkyl or 4-7 membered heterocycloalkyl containing 1-3 heteroatoms, wherein each of the O—C1-6 alkyl and NH—C1-6 alkyl is optionally substituted with hydroxyl, O—C1-3 alkyl or NH—C1-3 alkyl, each of the O—C1-3 alkyl and NH—C1-2 alkyl being optionally further substituted with O—C1-3 alkyl or NH—C1-3 alkyl; each of R702 and R703, independently is H, halo, C1-4 alkyl, C1-6 alkoxyl or C6-C10 aryloxy, each optionally substituted with one or more halo; each of R704 and R705, independently is C1-4 alkyl; R706 is cyclohexyl substituted by N(C1-4 alkyl)2 wherein one or both of the C1-4 alkyl is substituted with C1-6 alkoxy; or R706 is tetrahydropyranyl; R707 is C1-4 alkyl optionally substituted with one or more groups selected from hydroxyl, C1-4 alkoxy, amino, mono- or di-C1-4 alkylamino, C3-8 cycloalkyl, and 4-7 membered heterocycloalkyl containing 1-3 heteroatoms, wherein the C3-8 cycloalkyl or 4-7 membered heterocycloalkyl each independently is further optionally substituted with C1-3 alkyl; R708 is C1-4 alkyl optionally substituted with one or more groups selected from OH, halo, and C1-4 alkoxy, 4-7 membered heterocycloalkyl containing 1-3 heteroatoms, or O—C1-6 alkyl, wherein the 4-7 membered heterocycloalkyl can be optionally further substituted with OH or C1-6 alkyl; and n7 is 0, 1 or 2.