3-(4-methyl-1-(piperidin-4-yl)-1H-pyrazol-3-yl)-1H-pyrazolo[3,4-b]pyridine | 1206708-82-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡唑并吡啶类
• 英文名称: 3-(4-methyl-1-(piperidin-4-yl)-1H-pyrazol-3-yl)-1H-pyrazolo[3,4-b]pyridine
• 英文别名: 3-(4-methyl-1-piperidin-4-ylpyrazol-3-yl)-2H-pyrazolo[3,4-b]pyridine
• CAS: 1206708-82-8
• 化学式: C₁₅H₁₈N₆
• 分子量: 282.348
• InChiKey: SVAYZJNCMKCBQY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  71.4
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  Tert-butyl 4-[3-(1-tert-butylpyrazolo[3,4-b]pyridin-3-yl)-4-methylpyrazol-1-yl]piperidine-1-carboxylate 在 三乙基硅烷 、 三氟乙酸 作用下， 以35%的产率得到3-(4-methyl-1-(piperidin-4-yl)-1H-pyrazol-3-yl)-1H-pyrazolo[3,4-b]pyridine
  参考文献：
  名称：

  [EN] TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS
  [FR] INHIBITEURS DE PYRAZOLOPYRIDINE KINASE TRICYLIQUE

  摘要：

  本发明涉及公式（I）的化合物，其作为蛋白激酶抑制剂具有用途。该发明还提供包含上述化合物的药学上可接受的组合物，并提供使用这些组合物治疗各种疾病、症状或紊乱的方法。该发明还提供制备本发明化合物的方法。

  公开号：

  WO2010011768A1

文献信息

• TRI-CYCLIC PYRAZOLOPYRIDINE KINASE INHIBITORS
  申请人：Brenchley Guy

  公开号：US20120184534A1

  公开（公告）日：2012-07-19

  The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.

  本发明涉及用作蛋白激酶抑制剂的化合物。本发明还提供了包括所述化合物的药学上可接受的组合物以及使用这些组合物治疗各种疾病、状况或障碍的方法。本发明还提供了制备所述化合物的方法。
• Stem cell modulation II
  申请人：University of Canberra

  公开号：US10736892B2

  公开（公告）日：2020-08-11

  Disclosed are methods and compositions for modulating cancer stem cells. More particularly, the present invention discloses the use of protein kinase C theta inhibitors (PKC-θ) for inhibiting the growth of PKC-θ-overexpressing cells including cancer stem cells, for enhancing the biological effects of chemotherapeutic drugs or irradiation on cancer cells, for treating cancer, including metastatic cancer and/or for preventing cancer recurrence.

  本发明公开了调节癌症干细胞的方法和组合物。更具体地说，本发明公开了蛋白激酶C theta抑制剂（PKC-θ）的用途，用于抑制包括癌症干细胞在内的PKC-θ过表达细胞的生长，增强化疗药物或照射对癌细胞的生物效应，治疗癌症，包括转移性癌症和/或预防癌症复发。
• Stem Cell Modulation II
  申请人：UNIVERSITY OF CANBERRA

  公开号：US20160354367A1

  公开（公告）日：2016-12-08

  Disclosed are methods and compositions for modulating cancer stem cells. More particularly, the present invention discloses the use of protein kinase C theta inhibitors (PKC-θ) for inhibiting the growth of PKC-θ-overexpressing cells including cancer stem cells, for enhancing the biological effects of chemotherapeutic drugs or irradiation on cancer cells, for treating cancer, including metastatic cancer and/or for preventing cancer recurrence.
• Compositions for Modulating Cancer Stem Cells and Uses Therefor
  申请人：University of Canberra

  公开号：US20170266140A1

  公开（公告）日：2017-09-21

  Disclosed are compositions and methods for modulating cancer stem cells. More particularly, the present invention discloses the use of lysine demethylase (LSD) inhibitors and protein kinase C theta inhibitors (PKC-θ) for inhibiting the growth of LSD- and/or PKC-θ-overexpressing cells including cancer stem cells, for enhancing the biological effects of chemotherapeutic drugs or irradiation on cancer cells, for treating cancer, including non-metastatic and metastatic cancer and/or for preventing cancer recurrence.
• IMMUNOGENIC COMPOSITIONS AND USES THEREFOR
  申请人：Epiaxis Therapeutics Pty Ltd

  公开号：US20200282010A1

  公开（公告）日：2020-09-10

  The present invention discloses the use of protein kinase C (PKC-θ) inhibitors for enhancing the immune effector function of functionally repressed T-cells that have undergone epithelial to mesenchymal transition (EMT). In specific embodiments, PKC-θ inhibitors are disclosed for use in enhancing susceptibility of exhausted T-cells to reinvigoration by PD-1 binding antagonists. The compositions of the present invention find utility in treating a range of disorders including T-cell dysfunctional disorders such as pathogenic infections and hyperproliferative disorders.