2-呋喃丙酸,b-氨基-5-(3-氯苯基)- | 83570-44-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 2-呋喃丙酸,b-氨基-5-(3-氯苯基)-
• 中文别名: 6-乙基喹喔啉
• 英文名称: 6-ethyl-quinoxaline
• 英文别名: 6-Ethylquinoxaline
• CAS: 83570-44-9
• 化学式: C₁₀H₁₀N₂
• 分子量: 158.203
• InChiKey: NHOOTVPICXUNMW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  12
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  (3-Ethyl-phenyl)-[2-(phenyl-hydrazono)-eth-(E)-ylidene]-amine 600.0 ℃ 、1.33 Pa 条件下， 反应 0.5h， 以11%的产率得到5-乙基喹喔啉
  参考文献：
  名称：

  McNab, Hamish, Journal of the Chemical Society. Perkin transactions I, 1982, # 8, p. 1941 - 1946

  摘要：

  DOI：

文献信息

• COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE 4 POLYPEPTIDES
  申请人：Arvinas, Inc.

  公开号：US20190151295A1

  公开（公告）日：2019-05-23

  The present disclosure relates to bifunctional compounds, which find utility as modulators of Interleukin-1 Receptor-Associated Kinase 4 (IRAK-4); the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hppel-Lindau, cereblon, ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

  本公开涉及双功能化合物，其作为白细胞介素-1受体相关激酶4（IRAK-4；目标蛋白）的调节剂具有实用性。具体而言，本公开涉及包含一端结合E3泛素连接酶的Von Hppel-Lindau、cereblon配体的双功能化合物，另一端结合目标蛋白的部分，使得目标蛋白靠近泛素连接酶以实现目标蛋白的降解（和抑制）。本公开展示了与目标蛋白的降解/抑制相关的广泛药理活性。本公开的化合物和组合物用于治疗或预防由目标蛋白聚集或积累导致的疾病或紊乱。
• DIPHENYL DERIVATIVES AND USES THEREOF
  申请人：NOVARTIS AG

  公开号：US20190077773A1

  公开（公告）日：2019-03-14

  The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

  本公开提供了一种公式(I)的化合物： 或其药用可接受的盐，以及其用于激活生长因子途径、促进伤口愈合、促进组织修复以及治疗听力损失、骨骼肌损失、器官退化、组织损伤、神经退化和肌肉萎缩的治疗用途。本公开还提供了药物组合物和组合物。本公开还涉及将此类化合物用于研究或其他非治疗目的。
• PROTEIN KINASE INHIBITORS
  申请人：Song Yonghong

  公开号：US20090054425A1

  公开（公告）日：2009-02-26

  Compounds, particularly compounds having spleen tyrosine kinase (Syk) inhibition activity, having the following structure: or a pharmaceutically acceptable salt thereof, wherein R 1 is structure (a), (b), (c) or (d): and R a , R b , R c , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed, as well as uses of the same to treat a condition or disorder mediated by a Syk and/or JAK kinase.

  化合物，特别是具有脾酪氨酸激酶（Syk）抑制活性的化合物，具有以下结构： 或其药学上可接受的盐， 其中R 1 为结构（a）、（b）、（c）或（d）： 而R a ，R b ，R c ，R 2 ，R 3 ，R 4 ，R 5 ，R 6 和R 7 如本文所定义。涉及其制备和使用的方法，以及含有其的药物组合物，也被揭示，以及使用其来治疗由Syk和/或JAK激酶介导的疾病或疾病。
• MODULATORS OF INTERLEUKIN-1 RECEPTOR-ASSOCIATED KINASE
  申请人：Durand-Reville Thomas

  公开号：US20110021513A1

  公开（公告）日：2011-01-27

  The present invention relates to modulators of IRAK kinase and provides compositions comprising such modulators, as well as methods therewith for treating conditions or diseases mediated by or associated with IRAK kinase.

  本发明涉及IRAK激酶的调节剂，并提供包含这些调节剂的组合物，以及利用这些调节剂治疗由IRAK激酶介导或相关的疾病或病症的方法。
• ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS
  申请人：Pinto Donald J.P.

  公开号：US20100016316A1

  公开（公告）日：2010-01-21

  The present invention provides compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L 1 , R 3 , R 4 , R 8a , R 11 and M are as defined herein. The compounds of Formula (I) or (II) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

  本发明提供了化合物的结构式（I）或（II）： 或其立体异构体、互变异构体、药学上可接受的盐或溶剂形式，其中变量A、L1、R3、R4、R8a、R11和M如本文所定义。结构式（I）或（II）的化合物是凝血级联和/或接触激活系统的丝氨酸蛋白酶酶的选择性抑制剂；例如凝血酶、Xa因子、XIa因子、IXa因子、VIIa因子和/或血浆激肽。具体而言，涉及选择性XIa因子抑制剂或fXIa和血浆激肽的双重抑制剂的化合物。本发明还涉及包含这些化合物的药物组合物以及使用它们治疗血栓栓塞和/或炎症性疾病的方法。