3-(2-methylbutan-2-yl)-1H-pyridin-2-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 3-(2-methylbutan-2-yl)-1H-pyridin-2-one
• 化学式: C₁₀H₁₅NO
• 分子量: 165.23
• InChiKey: WQIKLIURHYQRES-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  29.1
• 氢给体数：
  1
• 氢受体数：
  1

文献信息

• HISTONE METHYLTRANSFERASE EZH2 INHIBITOR, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
  申请人：ANCUREALL PHARMACEUTICAL (SHANGHAI) CO., LTD.

  公开号：US20190345139A1

  公开（公告）日：2019-11-14

  The invention relates to a histone methyltransferase EZH2 inhibitor, a preparation method and pharmaceutical use thereof. In particular, the invention relates to a compound represented by the general formula (I), a preparation method thereof, a pharmaceutical composition containing the same, and a use thereof as a histone methyltransferase EZH2 inhibitor for treating diseases associated with the histone methyltransferase EZH2, especially cancer. The definition of each substituents in the general formula (I) is same as the definition in the specification.

  这项发明涉及一种组蛋白甲基转移酶EZH2抑制剂，其制备方法和药用。具体而言，该发明涉及一种由通式（I）表示的化合物，其制备方法，含有该化合物的药物组合物，以及将其用作组蛋白甲基转移酶EZH2抑制剂治疗与组蛋白甲基转移酶EZH2相关的疾病，特别是癌症。通式（I）中每个取代基的定义与规范中的定义相同。
• Substituted 6,5-fused bicyclic heteroaryl compounds
  申请人：Epizyme, Inc.

  公开号：US10273223B2

  公开（公告）日：2019-04-30

  The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.

  本发明涉及取代的6,5-融合双环杂芳基化合物。本发明还涉及含有这些化合物的药物组合物，以及通过向有需要的受试者施用这些化合物和药物组合物来治疗癌症的方法。
• Tricyclic heterocycles as BET protein inhibitors
  申请人：Incyte Corporation

  公开号：US10464947B2

  公开（公告）日：2019-11-05

  The present invention relates to tricyclic heterocycles of Formula (I): which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

  本发明涉及式 (I) 的三环杂环： 它们是 BET 蛋白如 BRD2、BRD3、BRD4 和 BRD-t 的抑制剂，可用于治疗癌症等疾病。
• Method for treating cancer
  申请人：Epizyme, Inc.

  公开号：US10946024B2

  公开（公告）日：2021-03-16

  The present invention provides a method for treating or alleviating a symptom of a disorder, e.g., immune evasion, cancer-cell induced immune dysfunction, reduced immune response, lowered inflammation, decreased expression of a major histocompatibility complex (MHC), or cancer, characterized by aberrant, misregulated, or increased Enhancer of Zeste Homolog 2 (EZH2) activity in a cell or subject in need thereof by contacting the cell or administering to the subject a therapeutically effective amount of an EZH2 inhibitor.

  本发明提供了一种治疗或缓解紊乱症状的方法，例如免疫逃避、癌细胞诱导的免疫功能障碍、免疫反应减弱、炎症反应减弱、主要组织相容性复合体（MHC）表达减弱或癌症，这些紊乱症状的特征是需要治疗的细胞或受试者的泽斯特同源酶2（EZH2）活性异常、失调或增强，其方法是通过与细胞接触或向受试者施用治疗有效量的EZH2抑制剂。
• Combination therapy for treating cancer
  申请人：Epizyme, Inc.

  公开号：US11026949B2

  公开（公告）日：2021-06-08

  The present disclosure relates to compositions comprising inhibitors of human histone methyltransferase EZH2 and one or more other therapeutic agents (such as tyrosine kinase inhibitors or VEGF/VEGFR inhibitors), particularly anticancer agents such as sunitinib, and methods of combination therapy for administering to subjects in need thereof for the treatment of cancer.

  本公开涉及包含人组蛋白甲基转移酶EZH2抑制剂和一种或多种其他治疗剂（如酪氨酸激酶抑制剂或血管内皮生长因子/血管内皮生长因子受体抑制剂），特别是抗癌剂（如舒尼替尼）的组合物，以及向需要其治疗癌症的受试者施用的联合治疗方法。