1-Phenyl-2-(3,5,7-triaza-1-azoniatricyclo[3.3.1.13,7]decan-1-yl)ethanone

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-Phenyl-2-(3,5,7-triaza-1-azoniatricyclo[3.3.1.13,7]decan-1-yl)ethanone
• 化学式: C14H19N4O+
• 分子量: 259.33
• InChiKey: FYFDJTHLFJOHDO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  26.8
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• CHEMICAL COMPOUNDS
  申请人：Axten Jeffrey Michael

  公开号：US20110275611A1

  公开（公告）日：2011-11-10

  The invention is directed to 6-(4-pyrimidinyl)-1H-indazole derivatives. Specifically, the invention is directed to compounds according to Formula (I) wherein R 1 -R 4 are defined herein. The compounds of the invention axe inhibitors of PDK1 and can be useful in the treatment of immune and metabolic diseases and disorders characterized by constitutively activated ACG kinases such as cancer and more specifically cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention

  本发明涉及6-(4-嘧啶基)-1H-吲唑衍生物。具体而言，本发明涉及公式（I）中R1-R4所定义的化合物。本发明的化合物是PDK1的抑制剂，可用于治疗免疫和代谢性疾病和障碍，这些疾病和障碍以恒定激活的ACG激酶为特征，例如乳腺、结肠和肺癌等。因此，本发明还涉及包含本发明化合物的制药组合物。本发明还涉及使用本发明化合物或包含本发明化合物的制药组合物抑制PDK1活性和治疗相关障碍的方法。
• BICYCLIC PYRIMIDINONES AND USES THEREOF
  申请人：Jones Eric Dale

  公开号：US20100168063A1

  公开（公告）日：2010-07-01

  The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.

  本发明提供公式I的化合物或其药学上可接受的衍生物、盐或前药。此外，还提供了一种治疗或预防受体内病毒感染的方法，包括向该受体内给予公式I的化合物或其药学上可接受的衍生物、盐或前药的有效剂量。还提供了一种包含公式I的药物组成物或药物。
• Bicyclic pyrimidinones and uses thereof
  申请人：Jones Eric Dale

  公开号：US20120232035A1

  公开（公告）日：2012-09-13

  The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.

  本发明提供了公式I的化合物或其药学上可接受的衍生物、盐或前药。还提供了一种治疗或预防受体内病毒感染的方法，包括向该受体内给予公式I的化合物或其药学上可接受的衍生物、盐或前药的有效量。还提供了一种包含公式I化合物的药物组合物或药物。
• NOVEL DRUG TARGETS TO OVERCOME DE NOVO DRUG-RESISTANCE IN MULTIPLE MYELOMA
  申请人：University of Florida Research Foundation, Inc.

  公开号：US20130281389A1

  公开（公告）日：2013-10-24

  Topoisomerase II alpha (topo IIα) is exported from the cell nucleus in human myeloma cells by a chromosome-maintenance protein-1 (CRM1)-dependent mechanism, resulting in topo II inhibitor resistance. The nuclear export signal (NES) of topo IIα is unique, making it a potential target for small molecule inhibitors. Small molecules NES inhibitors were identified, which inhibited binding of topo IIα to the export receptor CRM1. Inhibition was specific to topo IIα as p53 trafficking was unaffected along with topo IIα protein expression and function (decatenation). These topo IIα-specific nuclear export inhibitors may potentially lead to a new approach in circumventing drug resistance in multiple myeloma. The compounds provide a protocol for treating multiple myeloma or an oncogenic disease. Further, the topoisomerase II nuclear export signal inhibitor may be combined with a topoisomerase II inhibitor.
• US8143268B2
  申请人：——

  公开号：US8143268B2

  公开（公告）日：2012-03-27