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US 9,956,210 B2Granted
Enhancer of zeste homolog 2 inhibitors
AssigneeGlaxoSmithKline LLC
InventorsJoelle Lorraine Burgess, Steven David Knight
Life of this patent
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Abstract
This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Claims1
A method of treating non-Hodgkin's lymphoma comprising administering to a patient with non-Hodgkin's lymphoma a therapeutically effective amount of a compound of formula (I):
- wherein:
- R1 is methyl;
- R2 is methyl;
- R3 is hydrogen;
- R4 is methyl;
- R5 is —NRaRb;
- R6 is phenyl, wherein said phenyl is optionally substituted by —(C1-C6)alkyl(Rc);
- Rc is —NRaRb;
- and
- Ra and Rb are each independently hydrogen, (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, (C3-C10)cycloalkyl, (C5-C8)cycloalkenyl, heterocycloalkyl, or aryl, wherein said (C1-C8)alkyl, (C2-C8)alkenyl, (C2-C8)alkynyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, or aryl group is optionally substituted by 1, 2 or 3 groups independently selected from the group consisting of halo, hydroxyl, (C1-C4)alkoxy, amino, (C1-C4)alkylamino, —N((C1-C4)alkyl)2, —CO2H, —CO2(C1-C4)alkyl, —CONH2, —CONH(C1-C4)alkyl, —CON((C1-C4)alkyl)2, —SO2(C1-C4)alkyl, —SO2NH2, —SO2NH(C1-C4)alkyl, and —SO2N((C1-C4)alkyl)2;
- and wherein said heterocycloalkyl is selected from the group consisting of pyrrolidinyl, tetrahydrofuranyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, and tetrahydropyranyl;
- or Ra and Rb taken together with the nitrogen to which they are attached represent a 5 or 6 membered saturated ring, optionally containing an additional heteroatom selected from oxygen, nitrogen, and sulfur, wherein said ring is optionally substituted by 1, 2 or 3 groups independently selected from the group consisting of (C1-C4)alkyl, (C1-C4)haloalkyl, amino, (C1-C4)alkylamino, ((C1-C4)alkyl)((C1-C4)alkyl)amino, hydroxyl, oxo, (C1-C4)alkoxy, and (C1-C4)alkoxy(C1-C4)alkyl;
- or a pharmaceutically acceptable salt thereof.
10 more elements
Dependencies are inferred from the claim text.