4-(6-Morpholin-4-yl-8-oxa-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl)aniline

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 呋喃吡啶类
• 英文名称: 4-(6-Morpholin-4-yl-8-oxa-3,5,10-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl)aniline
• 化学式: C₁₉H₁₇N₅O₂
• 分子量: 347.4
• InChiKey: BSHBESKYBXZYTB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  26
• 可旋转键数：
  2
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  90.3
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• TRIAZINE, PYRIMIDINE AND PYRIDINE ANALOGS AND THEIR USE AS THERAPEUTIC AGENTS AND DIAGNOSTIC PROBES
  申请人：Cmiljanovic Vladimir

  公开号：US20110275762A1

  公开（公告）日：2011-11-10

  The invention relates to novel therapeutic agents and diagnostic probes. The invention also relates to phosphoinositide 3-kinase (PI3K) and mammalian target of rapamycin (mTOR) inhibitor triazine-, pyrimidine- and pyridine-based compoundŝ Formula (I), their stereoisomers, geometric isomers, tautomers, solvates, metabolites, N-oxide derivatives, pharmaceutically acceptable salts, and prodrugs thereof compositions of the new compounds; either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the new compounds, either alone or in combination with at least one additional therapeutic agent, for treating disorders mediated by lipid kinases. •Methods of using compounds of Formula (I) for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. (Formula I)

  本发明涉及新型治疗剂和诊断探针。本发明还涉及磷脂酰肌醇3-激酶（PI3K）和哺乳动物雷帕霉素靶蛋白酶（mTOR）抑制剂三嗪基、嘧啶基和吡啶基化合物̂公式（I），它们的立体异构体、几何异构体、互变异构体、溶剂化物、代谢物、N-氧化衍生物、药学上可接受的盐以及前药的组合物；新化合物的组合物，可以单独使用或与至少一种额外的治疗剂结合，与药学上可接受的载体；以及使用新化合物的方法，可以单独使用或与至少一种额外的治疗剂结合，用于治疗由脂质激酶介导的疾病。公开了使用公式（I）化合物的方法，用于哺乳动物细胞中的体外、原位和体内诊断、预防或治疗这种疾病或相关病理条件。(公式I)
• CONDENSED HETEROARYL DERIVATIVES
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1277738A1

  公开（公告）日：2003-01-22

  The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

  本发明提供了一种可用作磷脂酰肌醇 3 激酶（PI3K）抑制剂和抗肿瘤剂的药物组合物，并提供了一种新型双环或三环融合杂芳基衍生物或其盐，该衍生物具有优异的 PI3K 抑制活性和癌细胞生长抑制活性。
• Compositions to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
  申请人：Race Oncology Ltd.

  公开号：US10548876B2

  公开（公告）日：2020-02-04

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to bisantrene or derivatives, analogs, or prodrugs thereof.

  本发明描述了通过提高单一疗法的疗效或减少副作用来改善以前因治疗效果不理想而受到限制的治疗剂的疗效的方法和组合物。这些方法和组合物尤其适用于双蒽或其衍生物、类似物或原药。
• Combinatorial methods to improve the therapeutic benefit of bisantrene and analogs and derivatives thereof
  申请人：Race Oncology Ltd.

  公开号：US11147800B2

  公开（公告）日：2021-10-19

  The present invention describes methods and compositions for improving the therapeutic efficacy of therapeutic agents previously limited by suboptimal therapeutic performance by either improving efficacy as monotherapy or reducing side effects. Such methods and compositions are particularly applicable to bisantrene or derivatives, analogs, or prodrugs thereof.

  本发明描述了通过提高单一疗法的疗效或减少副作用来改善以前因治疗效果不理想而受到限制的治疗剂的疗效的方法和组合物。这些方法和组合物尤其适用于双蒽或其衍生物、类似物或原药。
• Fused heteroaryl derivatives
  申请人：——

  公开号：US20020151544A1

  公开（公告）日：2002-10-17

  The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.

  本发明提供了一种可用作磷脂酰肌醇 3 激酶（PI3K）抑制剂和抗肿瘤剂的药物组合物，并提供了一种新型双环或三环融合杂芳基衍生物或其盐，该衍生物具有优异的 PI3K 抑制活性和癌细胞生长抑制活性。