RO-5126766 | 1415559-58-8

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 香豆素及其衍生物
• 英文名称: RO-5126766
• 英文别名: 2-[3-[[3-Fluoro-2-(sulfamoylamino)pyridin-4-yl]methyl]-4-methyl-2-oxochromen-7-yl]oxypyrimidine
• CAS: 1415559-58-8
• 化学式: C₂₀H₁₆FN₅O₅S
• 分子量: 457.442
• InChiKey: BVMZBFGSSMFRKD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  155
• 氢给体数：
  2
• 氢受体数：
  11

文献信息

• Novel Coumarin Derivative Having Antitumor Activity
  申请人：Iikura Hitoshi

  公开号：US20110092700A1

  公开（公告）日：2011-04-21

  The present invention provides a compound represented by general formula (1) below or a pharmaceutically acceptable salt thereof: wherein: X is selected from heteroaryl etc., Y 1 and Y 2 are selected from —N═ etc., Y 3 and Y 4 are selected from —CH═ etc., A is selected from sulfamide etc., R 1 is selected from hydrogen etc., and R 2 is selected from C 1-6 alkyl etc. The compound or salt has sufficiently high antitumor activity, and is useful in the treatment of cell proliferative disorders, particularly cancers. The present invention also provides a pharmaceutical composition containing the compound or salt as an active ingredient.

  本发明提供一种由下式（1）或其药学上可接受的盐所表示的化合物：其中，X选自杂环芳基等；Y1和Y2选自—N═等；Y3和Y4选自—CH═等；A选自磺酰胺等；R1选自氢等；R2选自C1-6烷基等。该化合物或盐具有足够高的抗肿瘤活性，并可用于治疗细胞增殖性疾病，特别是癌症。本发明还提供一种含有该化合物或盐作为活性成分的制药组合物。
• p27 Protein Inducer
  申请人：Sakai Toshiyuki

  公开号：US20110009398A1

  公开（公告）日：2011-01-13

  The present invention provides a p27 protein inducing agent comprising a compound represented by general formula (11) below or pharmaceutically acceptable salt thereof as an active ingredient: wherein G 1 , G 2 , G 3 and G 8 are each independently selected from —N═ etc., Ring G 6 is selected from divalent aryl etc., A is selected from amino etc., G 4 is selected from oxygen etc., G 5 is selected from oxygen etc., G 7 is selected from —CH 2 — etc., and R 2 is selected from C 1-6 alkyl etc.

  本发明提供了一种p27蛋白诱导剂，其包含以下通式（11）所表示的化合物或其药学上可接受的盐作为活性成分：其中G1，G2，G3和G8各自独立地选择自—N═等，环G6选择自双价芳基等，A选择自氨基等，G4选择自氧等，G5选择自氧等，G7选择自—CH2—等，R2选择自C1-6烷基等。
• Anti-infective strategy against influenza virus and S. aureus coinfections
  申请人：Atriva Therapeutics GmbH

  公开号：US10456440B2

  公开（公告）日：2019-10-29

  The present invention relates to MEK inhibitor, p38 inhibitor and/or NFκB inhibitor for use in a method for the prophylaxis and/or treatment of a co-infection comprising a bacterial infection and an influenza virus infection or a bacterial infection alone. Also provided are compositions comprising such inhibitors for use in the prophylaxis and/or treatment of a co-infection comprising a bacterial infection and an influenza virus infection or a bacterial infection alone. In addition an in vitro test system, wherein the test system comprises cultured cells infected with an influenza virus and a bacterium or with a bacterium alone is provided.

  本发明涉及MEK抑制剂、p38抑制剂和/或NFκB抑制剂，用于预防和/或治疗由细菌感染和流感病毒感染或单纯细菌感染组成的合并感染的方法。还提供了包含此类抑制剂的组合物，用于预防和/或治疗由细菌感染和流感病毒感染或单纯细菌感染组成的合并感染。此外，还提供了一种体外测试系统，其中测试系统包括感染流感病毒和细菌或仅感染细菌的培养细胞。
• Novel-anti-infective strategy against influenza virus and S. aureus coinfections
  申请人：ATRIVA THERAPEUTICS GMBH

  公开号：US11135263B2

  公开（公告）日：2021-10-05

  The present invention relates to MEK inhibitor, p38 inhibitor and/or NFκB inhibitor for use in a method for the prophylaxis and/or treatment of a co-infection comprising a bacterial infection and an influenza virus infection or a bacterial infection alone. Also provided are compositions comprising such inhibitors for use in the prophylaxis and/or treatment of a co-infection comprising a bacterial infection and an influenza virus infection or a bacterial infection alone. In addition an in vitro test system, wherein the test system comprises cultured cells infected with an influenza virus and a bacterium or with a bacterium alone is provided.

  本发明涉及MEK抑制剂、p38抑制剂和/或NFκB抑制剂，用于预防和/或治疗由细菌感染和流感病毒感染或单纯细菌感染组成的合并感染的方法。还提供了包含此类抑制剂的组合物，用于预防和/或治疗由细菌感染和流感病毒感染或单纯细菌感染组成的合并感染。此外，还提供了一种体外测试系统，其中测试系统包括感染流感病毒和细菌或仅感染细菌的培养细胞。
• p27 PROTEIN INDUCER
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP2172198B1

  公开（公告）日：2014-04-16