- EZH2 covalent irreversible inhibitor as well as preparation method and application thereof
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The invention discloses an EZH2 covalent irreversible inhibitor as well as a preparation method and application thereof. The EZH2 covalent irreversible inhibitor comprises a compound with a structure as shown in a formula (I) or a formula (II) or a salt t
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Paragraph 0082; 0085-0086
(2021/08/14)
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- Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin's Lymphoma
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A novel series of benzofuran derived EZH2 inhibitors were discovered through a scaffold hopping approach based on the clinical compound of EPZ-6438. Further rational structure-activity relationship exploration and optimization led to the discovery of more potent EZH2 inhibitors with oral bioavailability in mice and rats. A lead compound EBI-2511 (compound 34) demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations.
- Lu, Biao,Shen, Xiaodong,Zhang, Lei,Liu, Dong,Zhang, Caihua,Cao, Jingsong,Shen, Ru,Zhang, Jiayin,Wang, Dan,Wan, Hong,Xu, Zhibin,Ho, Ming-Hsun,Zhang, Minsheng,Zhang, Lianshan,He, Feng,Tao, Weikang
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- BENZOFURAN DERIVATIVE, PREPARATION METHOD THEREOF AND USE THEREOF IN MEDICINE
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The present invention relates to a benzofuran derivative, a preparation method thereof and a use thereof in medicine. In particular, the present invention relates to the benzofuran derivative as shown by general formula (I), the preparation method thereof, a pharmaceutical composition containing the derivative, and uses thereof as an EZH2 inhibitor and in the prevention and/or treatment of diseases such as tumours and cancers, etc., and in particular uses thereof in the prevention and/or treatment of non-Hodgkin's lymphoma, diffuse large B-cell lymphoma, follicular lymphoma and synovial sarcoma, wherein the definitions of the substituents in the general formula (I) are the same as those defined in the description.
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- Isoindolinone kinase inhibitors
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Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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Page/Page column 29
(2010/02/10)
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- ISOINDOLIN-1-ONE COMPOUNDS AS KINASE INHIBITORS
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Compounds having the formula, (I) are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds and compositions containing the compounds.
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