- SYNTHESIS OF INHIBITORS OF EZH2
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Provided herein are synthetic methods for the preparation of EZH2 inhibitors.
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- CRYSTALLINE FORMS OF (R)-N-((4-METHOXY-6-METHYL-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)-2-METHYL-1-(1-(1-(2,2,2-TRIFLUOROETHYL)PIPERIDIN-4-YL)ETHYL)-1H-INDOLE-3-CARBOXAMIDE
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The present disclosure relates to a crystalline Forms A, B, and C of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide, each of which are useful as modulators the activity of histone methyl modifying enzymes. The present disclosure also provides pharmaceutically acceptable compositions comprising the crystalline forms and methods of using said compositions in the treatment of various disorders. Formula (I)
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Paragraph 0078
(2017/03/21)
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- Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitabl
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Polycomb repressive complex 2 (PRC2) has been shown to play a major role in transcriptional silencing in part by installing methylation marks on lysine 27 of histone 3. Dysregulation of PRC2 function correlates with certain malignancies and poor prognosis
- Vaswani, Rishi G.,Gehling, Victor S.,Dakin, Les A.,Cook, Andrew S.,Nasveschuk, Christopher G.,Duplessis, Martin,Iyer, Priyadarshini,Balasubramanian, Srividya,Zhao, Feng,Good, Andrew C.,Campbell, Robert,Lee, Christina,Cantone, Nico,Cummings, Richard T.,Normant, Emmanuel,Bellon, Steven F.,Albrecht, Brian K.,Harmange, Jean-Christophe,Trojer, Patrick,Audia, James E.,Zhang, Ying,Justin, Neil,Chen, Shuyang,Wilson, Jon R.,Gamblin, Steven J.
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p. 9928 - 9941
(2016/11/19)
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- MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Agents having the structural Formula (II) for modulating histone methyl modifying enzymes, compositions and uses thereof for instance as anti-cancer agents are provided herein.
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Paragraph 0090; 0091
(2014/08/20)
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- MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
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Paragraph 00316; 00317
(2013/08/28)
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