DHPCC9 | 1192248-37-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: DHPCC9
• 英文别名: 1,10-dihydropyrrolo[2,3-a]carbazole-3-carbaldehyde
• CAS: 1192248-37-5
• 化学式: C₁₅H₁₀N₂O
• 分子量: 234.257
• InChiKey: VWNCOFUKBTYAON-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  18
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  48.6
• 氢给体数：
  2
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  DHPCC9 在 甲醇 、 sodium tetrahydroborate 作用下， 反应 1.0h， 以67%的产率得到(1,10-dihydropyrrolo[2,3-a]carbazol-3-yl)methanol
  参考文献：
  名称：

  Novel Pyrrolo [2,3-A] Carbazoles and Use Thereof as PIM Kinase Inhibitors

  摘要：

  这项发明涉及吡咯并[2,3-a]咔唑衍生物，以及制备该衍生物的方法，以及将其用作PIM激酶抑制剂的用途。该发明特别适用于制药领域。

  公开号：

  US20110263669A1
• 作为产物：
  描述：

  1-benzenesulfonyl-1,10-dihydropyrrolo[2,3-a]carbazole 在 草酰氯 、 水 、 sodium hydroxide 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 27.16h， 生成 DHPCC9
  参考文献：
  名称：

  Novel Pyrrolo [2,3-A] Carbazoles and Use Thereof as PIM Kinase Inhibitors

  摘要：

  这项发明涉及吡咯并[2,3-a]咔唑衍生物，以及制备该衍生物的方法，以及将其用作PIM激酶抑制剂的用途。该发明特别适用于制药领域。

  公开号：

  US20110263669A1

文献信息

• Formylated N-heterocyclic derivatives as FGFR4 inhibitors
  申请人：Buschmann Nicole

  公开号：US10189813B2

  公开（公告）日：2019-01-29

  The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.

  本发明提供了一种式（I）化合物或其药学上可接受的盐； 一种制造所述化合物的方法及其治疗用途。本发明进一步提供了一种药理活性剂组合和包含所述化合物的药物组合物。
• Synthesis, Kinase Inhibitory Potencies, and in Vitro Antiproliferative Evaluation of New Pim Kinase Inhibitors
  作者：Rufine Akué-Gédu、Emilie Rossignol、Stéphane Azzaro、Stefan Knapp、Panagis Filippakopoulos、Alex N. Bullock、Jenny Bain、Philip Cohen、Michelle Prudhomme、Fabrice Anizon、Pascale Moreau

  DOI：10.1021/jm901018f

  日期：2009.10.22

  Members of the Pim kinase family have been identified as promising targets for the development of antitumor agents. After a screening of pyrrolo[2,3-a]- and [3,2-a]carbazole derivatives toward 66 protein kinases, we identified pyrrolo[2,3-a]carbazole as a new scaffold to design potent Pim kinase inhibitors. In particular, compound 9 was identified as a low nM selective Pim inhibitor. Additionally, several pyrrolo[2,3-a]carbazole derivatives showed selectivity for Pim-1 and Pim-3 over Pim-2. In vitro antiproliferative activities of 9 and 28, the most potent Pim inhibitors identified, were evaluated toward three human solid cancer cell lines (PA1, PC3, and DU145) and one human fibroblast primary culture, revealing IC50 values in the micromolar range. Finally, the crystal structure of Pim-1 complexed with lead compound 9 was determined. The structure revealed a non-ATP mimetic binding mode with no hydrogen bonds formed with the kinase hinge region and explained the selectivity of pyrrolo[2,3-a]carbazole derivatives for Pim kinases.
• NOUVEAUX PYRROLO[2,3-a]CARBAZOLES ET LEUR UTILISATION COMME INHIBITEURS DES KINASES PIM
  申请人：Centre National de la Recherche Scientifique

  公开号：EP2326649B1

  公开（公告）日：2012-03-28
• FORMYLATED N-HETEROCYCLIC DERIVATIVES AS FGFR4 INHIBITORS
  申请人：NOVARTIS AG

  公开号：EP3274344B1

  公开（公告）日：2019-04-24
• Formylated N-heterocyclic derivatives as FGFR4 inhibitors.
  申请人：Novartis AG

  公开号：US20190105309A1

  公开（公告）日：2019-04-11

  The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; a method for manufacturing said compound, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition comprising said compound.