721959-71-3Relevant academic research and scientific papers
1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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, (2020/08/30)
The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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, (2017/01/23)
This invention relates to novel compounds 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.
INHIBITORS OF EZH2
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, (2017/03/14)
The present invention relates to compounds that inhibit activity of the histone lysine methyltransferase, Enhancer of Zeste Homolog 2 (EZH2), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, such as hematologic and solid tumors.
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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, (2016/05/19)
This invention relates to novel compounds according to Formula (I) which are inhibitors of Enhancer of Zeste Homo log 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors
Kung, Pei-Pei,Rui, Eugene,Bergqvist, Simon,Bingham, Patrick,Braganza, John,Collins, Michael,Cui, Mei,Diehl, Wade,Dinh, Dac,Fan, Connie,Fantin, Valeria R.,Gukasyan, Hovhannes J.,Hu, Wenyue,Huang, Buwen,Kephart, Susan,Krivacic, Cody,Kumpf, Robert A.,Li, Gary,Maegley, Karen A.,McAlpine, Indrawan,Nguyen, Lisa,Ninkovic, Sacha,Ornelas, Martha,Ryskin, Michael,Scales, Stephanie,Sutton, Scott,Tatlock, John,Verhelle, Dominique,Wang, Fen,Wells, Peter,Wythes, Martin,Yamazaki, Shinji,Yip, Brian,Yu, Xiu,Zehnder, Luke,Zhang, Wei-Guo,Rollins, Robert A.,Edwards, Martin
, p. 8306 - 8325 (2016/10/03)
A new enhancer of zeste homolog 2 (EZH2) inhibitor series comprising a substituted phenyl ring joined to a dimethylpyridone moiety via an amide linkage has been designed. A preferential amide torsion that improved the binding properties of the compounds was identified for this series via computational analysis. Cyclization of the amide linker resulted in a six-membered lactam analogue, compound 18. This transformation significantly improved the ligand efficiency/potency of the cyclized compound relative to its acyclic analogue. Additional optimization of the lactam-containing EZH2 inhibitors focused on lipophilic efficiency (LipE) improvement, which provided compound 31. Compound 31 displayed improved LipE and on-target potency in both biochemical and cellular readouts relative to compound 18. Inhibitor 31 also displayed robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes.
ARYL FUSED LACTAMS AS EZH2 MODULATORS
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, (2016/04/19)
This invention relates to compounds of Formula (I) in which R1, R2, R3, R4, X and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
SUBSTITUTED DIHYDROISOQUINOLINONE COMPOUNDS
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, (2015/12/30)
This invention relates to compounds of general formula (I) in which R1, R2, R3, R4, L, X and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
ARYL AND HETEROARYL FUSED LACTAMS
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, (2014/07/08)
This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
NITROGENOUS HETEROCYCLIC DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, MEDICINAL USE THEREOF AND INTERMEDIATE THEREFOR
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Page 24, (2010/02/06)
The present invention is to provide a nitrogen-containing heterocyclic derivative represented by the general formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof, which exerts an excellent inhibitory activity in human SGLT2 and
