9-[(3S)-1-acryloyl-3-piperidinyl]-6-amino-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one | 1351635-67-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 9-[(3S)-1-acryloyl-3-piperidinyl]-6-amino-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one
• 英文别名: (S)-9-(1-acryloylpiperidin-3-yl)-6-amino-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one；GS-4059；ONO-4059；6-amino-7-(4-phenoxyphenyl)-9-[(3S)-1-prop-2-enoylpiperidin-3-yl]purin-8-one
• CAS: 1351635-67-0
• 化学式: C₂₅H₂₄N₆O₃
• 分子量: 456.504
• InChiKey: KSUDUUBCXJUFRL-SFHVURJKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  34
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  105
• 氢给体数：
  1
• 氢受体数：
  6

安全信息

• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302

文献信息

• PURINONE DERIVATIVE
  申请人：Yamamoto Shingo

  公开号：US20130079327A1

  公开（公告）日：2013-03-28

  Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.

  由一般公式（I）表示的化合物（公式中的所有符号符合说明中的定义）是除了具有Btk选择性抑制活性外，还表现出优异的代谢稳定性，可以避免肝毒性或类似情况，从而可以为B细胞或肥大细胞参与的疾病提供安全的治疗药物。
• PURINONE DERIVATIVE AS BTK KINASE INHIBITOR
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：EP3112368A1

  公开（公告）日：2017-01-04

  Compounds represented by general formula (I) as drawn below (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.

  下图中通式（I）所代表的化合物（式中所有符号均符合说明中的定义），除了具有 Btk 选择性抑制活性外，还具有极佳的代谢稳定性，可避免肝毒性等，因此可为 B 细胞或肥大细胞参与的疾病提供安全的治疗剂。
• Purinone derivative
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：US10233185B2

  公开（公告）日：2019-03-19

  Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.

  通式（I）所代表的化合物（式中的所有符号均符合说明中的定义）除了具有 Btk 选择性抑制活性外，还具有极佳的代谢稳定性，可避免肝毒性或类似毒性，因此可为 B 细胞或肥大细胞参与的疾病提供安全的治疗剂。
• Cancer treatment combinations
  申请人：The Regents of the University of California

  公开号：US10688181B2

  公开（公告）日：2020-06-23

  There are provided, inter alia, compositions and methods for treatment of cancer. The methods include administering to a subject in need a therapeutically effective amount of a Bruton's tyrosine kinase (BTK) antagonist and a ROR-1 antagonist. Further provided are pharmaceutical compositions including a BTK antagonist, ROR-1 antagonist and a pharmaceutically acceptable excipient. In embodiments, the BTK antagonist is ibrutinib and the ROR-1 antagonist is cirmtuzumab.

  除其他外，还提供了治疗癌症的组合物和方法。这些方法包括向有需要的受试者施用治疗有效量的布鲁顿酪氨酸激酶（BTK）拮抗剂和ROR-1拮抗剂。进一步提供的药物组合物包括 BTK 拮抗剂、ROR-1 拮抗剂和药学上可接受的赋形剂。在实施方案中，BTK拮抗剂是伊布替尼，ROR-1拮抗剂是cirmtuzumab。
• Combination of anti-CD20 antibody, P13 kinase-delta selective inhibitor, and BTK inhibitor to treat b-cell proliferative disorders
  申请人：TG Therapeutics, Inc.

  公开号：US10966977B2

  公开（公告）日：2021-04-06

  Methods for inhibiting proliferation of a B-cell population are provided comprising administering a combination of agents, comprising: (i) at least one P13K-delta selective inhibitor; (ii) at least one anti-CD20 antibody; and (iii) at least one Bruton's tyrosine kinase (BTK) inhibitor. Methods for treating B-cell proliferative disorders, such as B-cell hematological malignancies, as well as kits for carrying out the claimed methods, are also provided.

  本发明提供了抑制 B 细胞群增殖的方法，包括施用药物组合，其中包括：(i) 至少一种 P13K-delta 选择性抑制剂；(ii) 至少一种抗 CD20 抗体；以及 (iii) 至少一种布鲁顿酪氨酸激酶 (BTK) 抑制剂。还提供了治疗B细胞增殖性疾病（如B细胞血液恶性肿瘤）的方法，以及用于实施所述方法的试剂盒。