53475-53-9Relevant academic research and scientific papers
1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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Paragraph 0210-0211, (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.
Zinc (II)-mediated selective O-benzylation of 2-Oxo-1,2-dihydropyridines systems
Zhou, Qifan,Du, Fangyu,Liang, Xinjie,Liu, Wenqiang,Fang, Ting,Chen, Guoliang
, (2018/08/21)
The selective O-benzylation of 2-oxo-1,2-dihydropyridines plays a critical role in organic synthesis of natural products and biological active molecules. Herein we report a novel ternary system of ZnO, ZnCl2 and N,N-diisopropylethylamine (DIEA), that is highly effective for selective O-benzylation of 2-oxo-1,2-dihydropyridines using abundant substituted benzyl halides and related substituted 2-oxo-1,2-dihydropyridines compounds. This process allows access to a variety of O-benzyl products under mild reaction conditions, which are important synthetic intermediates in the protection of functional groups, and represents a new method toward the development for the O-benzylation of 2-oxo-1,2-dihydropyridines.
INHIBITORS OF EZH2
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Page/Page column 50; 51, (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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Page/Page column 57-58, (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.
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.
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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Page/Page column 51-52, (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.
SUBSTITUTED DIHYDROISOQUINOLINONE COMPOUNDS
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Paragraph 0474, (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 FUSED LACTAMS AS EZH2 MODULATORS
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Page/Page column 65, (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.
ARYL AND HETEROARYL FUSED LACTAMS
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Paragraph 0791; 0792; 0806; 0808, (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
