| 867161-54-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• CAS: 867161-54-4
• 化学式: C₂₉H₂₈N₆O
• 分子量: 476.581
• InChiKey: FQUOGEWRQYVMRQ-ZRZAMGCNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.77
• 重原子数：
  36.0
• 可旋转键数：
  4.0
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.28
• 拓扑面积：
  81.57
• 氢给体数：
  1.0
• 氢受体数：
  7.0

反应信息

• 作为产物：
  描述：

  在 氨 作用下， 以 异丙醇 为溶剂， 反应 24.0h， 生成
  参考文献：
  名称：

  Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors

  摘要：

  A series of novel, potent quinolinyl-derived imidazo[1,5-a]pyrazine IGF-IR (IGF-1R) inhibitors most notably, cis-3-(3-azetidin-1-ylmethylcyclobutyl)-1-(2-plienylquinotin-7-yl)imidazo[1,5-a]pyrazin-8-ylamine (AQIP)-is described. Synthetic details, structure-activity relationships, and in vitro biological activity are reported for the series. Key in vitro and in vivo biological results for AQIP are reported, including: inhibition of ligand-stimulated autophosphorylation of IGF-IR and downstream pathways in 3T3/huIGFIR cells; inhibition of proliferation and induction of DNA fragmentation in human tumor cell lines; a pharmacokinetic profile suitable for once-per-day oral dosing; antitumor activity in a 3T3/huIGFIR xenograft model; and effects on insulin and glucose levels. (C) 2007 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2007.10.061

文献信息

• 6,6-Bicyclic Ring Substituted Heterobicyclic Protein Kinase Inhibitors
  申请人：Arnold Lee D.

  公开号：US20090118499A1

  公开（公告）日：2009-05-07

  Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

  该公式化合物及其药学上可接受的盐，其中X1、X2、X3、X4、X5、X6、X7、R1和Q1的定义如下，可抑制IGF-1R酶，用于治疗和/或预防高增殖性疾病，如癌症、炎症、牛皮癣、过敏/哮喘、免疫系统疾病和疾病和中枢神经系统疾病和病症。
• 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
  申请人：OSI Pharmaceuticals, Inc.

  公开号：EP2168968A1

  公开（公告）日：2010-03-31

  Compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

  式 (I) 的化合物 及其药学上可接受的盐，其中 X1、X2、X3、X4、X5、X6、X7、R1 和 Q1 在此定义，抑制 IGF-1R 酶，可用于治疗和/或预防过度增殖性疾病，如癌症、炎症、牛皮癣、过敏/哮喘、免疫系统疾病和病症、中枢神经系统疾病和病症。
• 6,6-BICYCLIC RING SUBSTITUTED HETEROBICYCLIC PROTEIN KINASE INHIBITORS
  申请人：OSI Pharmaceuticals, Inc.

  公开号：EP1740591B1

  公开（公告）日：2009-06-17
• Combined treatment with 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitor and anti-cancer agents
  申请人：Arnold D. Lee

  公开号：US20080014200A1

  公开（公告）日：2008-01-17

  The present invention provides a method for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of an anti-cancer agent and an IGF1R inhibitor compound of Formula I combination, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The IGF1R inhibitor is represented by Formula I: wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein.
• Combination cancer therapy
  申请人：Arnold Lee D.

  公开号：US20080267957A1

  公开（公告）日：2008-10-30

  Methods and compositions for treating tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially (a) a therapeutically effective amount of an anti-cancer agent and (b) an IGF1R inhibitor compound of Formula I, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. Suitable IGF1R inhibitor may be represented by Formula I: wherein X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , X 7 , R 1 , and Q 1 are defined herein.