依鲁替尼代谢物 | 1654820-87-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: 依鲁替尼代谢物
• 英文名称: Pci-45227
• 英文别名: 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidin-1-yl]-2,3-dihydroxypropan-1-one
• CAS: 1654820-87-7
• 化学式: C₂₅H₂₆N₆O₄
• 分子量: 474.5
• InChiKey: NWKPMPRXJGMTKQ-DIAVIDTQSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  35
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  140
• 氢给体数：
  3
• 氢受体数：
  8

文献信息

• 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。
• COMBINATIONS OF BRUTON'S TYROSINE KINASE INHIBITORS AND CYP3A4 INHIBITORS
  申请人：PHARMACYCLICS LLC

  公开号：US20160022683A1

  公开（公告）日：2016-01-28

  Combinations of Bruton's tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, with CYP3A4 inhibitors are provided. Also provided are methods of treating cancers, and autoimmune disorders by administering combinations of Bruton's tyrosine kinase (Btk) inhibitors, e.g., 1-4((R)-3-(4-amino-3-(4-phenoxyphenyl)-1 H-pyrazolo[3, 4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, and CYP3A4 inhibitors.
• IBRUTINIB COMBINATION THERAPY
  申请人：PHARMACYCLICS LLC

  公开号：US20160287592A1

  公开（公告）日：2016-10-06

  Combinations of Bruton's tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, with a second anticancer agent are provided. Also provided are methods of treating cancers, and autoimmune disorders by administering combinations of Bruton's tyrosine kinase (Btk) inhibitors, e.g., 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, and second anticancer agents.
• 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：US20190175592A1

  公开（公告）日：2019-06-13

  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.