2-(2-Chlorophenyl)-5,7-dihydroxy-8-(3-hydroxy-1-methylpiperidin-4-yl)chromen-4-one;hydron;chloride

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 英文名称: 2-(2-Chlorophenyl)-5,7-dihydroxy-8-(3-hydroxy-1-methylpiperidin-4-yl)chromen-4-one;hydron;chloride
• 英文别名: 2-(2-chlorophenyl)-5,7-dihydroxy-8-(3-hydroxy-1-methylpiperidin-4-yl)chromen-4-one;hydron;chloride
• 化学式: C21H21Cl2NO5
• 分子量: 438.3
• InChiKey: LGMSNQNWOCSPIK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.73
• 重原子数：
  29
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  90.2
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• Inhibitors of Cyclin Dependent Kinases and Their Use
  申请人：Lal Bansi

  公开号：US20110136873A1

  公开（公告）日：2011-06-09

  The present invention relates to novel compounds for the inhibition of cyclin-dependent kinases, and more particularly, to chromenone derivatives of formula (Ia), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and A have the meanings indicated in the claims. The invention also relates to processes for the preparation of the compounds of formula (Ia), to methods of inhibiting cyclin-dependent kinases and of inhibiting cell proliferation, to the use of the compounds of formula (Ia) in the treatment and prophylaxis of diseases, which can be treated or prevented by the inhibition of cyclin-dependent kinases such as cancer, to the use of the compounds of formula (Ia) in the preparation of medicaments to be applied in such diseases. The invention further relates to compositions containing a compound of formula (Ia) either alone or in combination with another active agent, in admixture or otherwise in association with an inert carrier, in particular pharmaceutical compositions containing a compound of formula (Ia) either alone or in combination with another active agent, together with pharmaceutically acceptable carrier substances and auxiliary substances.

  本发明涉及新型化合物，用于抑制细胞周期蛋白依赖性激酶，更具体地说，涉及公式(Ia)的香豆酮衍生物，其中R1、R2、R3、R4、R5、R6、R7和A具有所述权利要求中指示的含义。本发明还涉及制备公式(Ia)化合物的方法，抑制细胞周期蛋白依赖性激酶和抑制细胞增殖的方法，以及使用公式(Ia)化合物治疗和预防通过抑制细胞周期蛋白依赖性激酶治疗或预防的疾病，如癌症，使用公式(Ia)化合物制备应用于此类疾病的药物。本发明还涉及含有公式(Ia)化合物的组合物，单独或与另一活性剂混合，与惰性载体混合或以其他方式与惰性载体相关联，特别是含有公式(Ia)化合物的制药组合物，单独或与另一活性剂混合，以及与药物可接受的载体物质和辅助物质一起使用。
• Pharmaceutical combination for the treatment of cancer
  申请人：Piramal Enterprises Limited

  公开号：US10555931B2

  公开（公告）日：2020-02-11

  The present invention relates to a pharmaceutical combination comprising a CDK inhibitor and at least one antioxidant enzyme inhibitor for use in the treatment of cancer. The present invention also relates to a method for the treatment of cancer comprising administering to a subject in need thereof, a therapeutically effective amount of a CDK inhibitor and a therapeutically effective amount of at least one antioxidant enzyme inhibitor. The pharmaceutical combination of the present invention exhibits synergistic effect when used in the treatment of cancer.

  本发明涉及一种包含 CDK 抑制剂和至少一种抗氧化酶抑制剂的药物组合，用于治疗癌症。本发明还涉及一种治疗癌症的方法，该方法包括向有需要的受试者施用治疗有效量的 CDK 抑制剂和治疗有效量的至少一种抗氧化酶抑制剂。本发明的药物组合用于治疗癌症时具有协同作用。
• COMBINATION OF GLIVEC(STI571) WITH A CYCLIN-DEPENDENT KINASE INHIBITOR, ESPECIALLY FLAVOPIRIDOL IN THE TREATMENT OF CANCER
  申请人：Virginia Commonwealth University

  公开号：EP1496908A1

  公开（公告）日：2005-01-19
• PHARMACEUTICAL COMBINATION COMPRISING A CDK INHIBITOR AND A THIOREDOXIN REDUCTASE INHIBITOR FOR THE TREATMENT OF CANCER
  申请人：Piramal Enterprises Limited

  公开号：EP3148532B1

  公开（公告）日：2021-03-03
• Combination of glivec (sti571) with a cyclin-dependent kinase inhibitor, especially flavopiridol, in the treatment of cancer
  申请人：Dent Paul

  公开号：US20050176725A1

  公开（公告）日：2005-08-11

  The present invention pertains to a combination for simultaneous, separate or sequential use which comprises (a) a cyclin-dependent kinase inhibitor and (b) 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl)pyrimidin-2-ylamino)phenyl]-benzamide and to its use for the treatment of cancer, especially of Bcr/Abl + leukemia resistant to compound of formula I.