5-(6-aminopurin-9-yl)-N-ethyl-3,4-dihydroxy-2-oxolanecarboxamide | 78647-50-4

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物 - 嘌呤核苷
• 英文名称: 5-(6-aminopurin-9-yl)-N-ethyl-3,4-dihydroxy-2-oxolanecarboxamide
• 英文别名: 5-(6-aminopurin-9-yl)-N-ethyl-3,4-dihydroxyoxolane-2-carboxamide
• CAS: 78647-50-4
• 化学式: C₁₂H₁₆N₆O₄
• 分子量: 308.29
• InChiKey: JADDQZYHOWSFJD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  22
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  148
• 氢给体数：
  4
• 氢受体数：
  8

文献信息

• Methods of treating cancer
  申请人：Corvus Pharmaceuticals, Inc.

  公开号：US10912776B2

  公开（公告）日：2021-02-09

  Provided herein are, inter alia, methods of treating cancer by administering to a subject a therapeutically effective amount of an adenosine-A2A(A2A) receptor antagonist or a combination of an adenosine-A2A(A2A) receptor antagonist and a programmed cell death protein 1(PD-1) signaling pathway inhibitor. Further provided are pharmaceutical compositions including an A2A receptor antagonist, a PD-1 signaling pathway inhibitor and a pharmaceutically acceptable excipient. Further provided are methods of detecting cellular effects, for example expression of pCREB, before, after or during adenosine receptor antagonist treatment.

  本文特别提供了通过向受试者施用治疗有效量的腺苷-A2A(A2A)受体拮抗剂或腺苷-A2A(A2A)受体拮抗剂与程序性细胞死亡蛋白1(PD-1)信号通路抑制剂的组合来治疗癌症的方法。还提供了包括 A2A 受体拮抗剂、PD-1 信号通路抑制剂和药学上可接受的赋形剂的药物组合物。还提供了在腺苷受体拮抗剂治疗之前、之后或期间检测细胞效应（例如 pCREB 的表达）的方法。
• Methods and compositions for producing pancreatic beta cells
  申请人：The Regents of the University of California

  公开号：US11332716B2

  公开（公告）日：2022-05-17

  Compositions and methods of producing mammalian cell populations that include a high proportion of pancreatic beta cells are described herein. Such cell populations are useful for treatment of diabetes. Also provided are materials and methods for the direct differentiation of stem cells, such as embryonic stem cells, into functional pancreatic beta cells. The disclosure provides the benefit of direct differentiation, which results in the production of functional pancreatic beta cells efficiently and at low cost.

  本文描述了生产包括高比例胰腺β细胞的哺乳动物细胞群的组合物和方法。这种细胞群可用于治疗糖尿病。还提供了将胚胎干细胞等干细胞直接分化为功能性胰腺β细胞的材料和方法。本公开内容提供了直接分化的好处，可高效低成本地生产功能性胰腺β细胞。
• Methods and Compositions for Producing Pancreatic Beta Cells
  申请人：The Regents of the University of California

  公开号：US20180216076A1

  公开（公告）日：2018-08-02

  Compositions and methods of producing mammalian cell populations that include a high proportion of pancreatic beta cells are described herein. Such cell populations are useful for treatment of diabetes. Also provided are materials and methods for the direct differentiation of stem cells, such as embryonic stem cells, into functional pancreatic beta cells. The disclosure provides the benefit of direct differentiation, which results in the production of functional pancreatic beta cells efficiently and at low cost.
• Method for Increasing Plant Stress Tolerance and Seed Dormancy
  申请人：The Australian National University

  公开号：US20180355369A1

  公开（公告）日：2018-12-13

  The present invention provides a method for increasing the levels of 3′-phosphoadenosine-5′-phosphate (PAP) or a derivative or analogue thereof in cells of said plant compared to an untreated or wild-type plant grown under the same stress conditions. The methods may comprise administration to the plant and/or the soil it is growing in of: PAP or a derivative or analogue thereof, a substance that enhances or promotes synthesis or accumulation of PAP or said derivative or analogue thereof; or a substance that inhibits or compromises an activity metabolising or removing PAP or said derivative or analogue thereof. Alternatively, the methods may comprise genetic modification of cells of said plant which modifications allow for increased accumulation of PAP or a derivative or analogue thereof in cells of said plant (or in seeds thereof) at least under stress conditions compared to a wild-type plant. The methods find particular application in increasing the tolerance of plants to abiotic stress conditions, which may be selected from increased salinity, increased sodium levels, drought, light stress and pH stress. The present invention also provides a method for extending the dormancy of a seed, as compared to an untreated seed, said method comprising accumulating in cells within said seed an increased level of PAP or a derivative or analogue thereof compared to an untreated or wild-type seed.
• METHODS OF TREATING CANCER
  申请人：Corvus Pharmaceuticals, Inc.

  公开号：US20190076433A1

  公开（公告）日：2019-03-14

  Provided herein are, inter alia, methods of treating cancer by administering to a subject a therapeutically effective amount of an adenosine-A2A(A2A) receptor antagonist or a combination of an adenosine-A2A(A2A) receptor antagonist and a programmed cell death protein 1(PD-1) signaling pathway inhibitor. Further provided are pharmaceutical compositions including an A2Areceptor antagonist, a PD-1 signaling pathway inhibitor and a pharmaceutically acceptable excipient. Further provided are methods of detecting cellular effects, for example expression of pCREB, before, after or during adenosine receptor antagonist treatment.