2-Chloro-5-fluoro-6-morpholinonicotinonitrile

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 2-Chloro-5-fluoro-6-morpholinonicotinonitrile
• 英文别名: 2-chloro-5-fluoro-6-morpholin-4-ylpyridine-3-carbonitrile
• 化学式: C₁₀H₉ClFN₃O
• 分子量: 241.65
• InChiKey: IZHYDDAJCJERBE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  16
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  49.2
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  3-氰基-2,6-二氯-5-氟吡啶 、 吗啉 、 三乙胺 在 二氯甲烷 、 水 、 Brine 作用下， 以 乙腈 为溶剂， 反应 1.0h， 以to yield 1.06 g of the title compound的产率得到2-Chloro-5-fluoro-6-morpholinonicotinonitrile
  参考文献：
  名称：

  N-PROP-2-YNYL CARBOXAMIDE DERIVATIVES AND THEIR USE AS TRPA1 ANTAGONISTS

  摘要：

  公式I的化合物中，其中A、B、X、Z和R1-R6如权利要求中所定义的那样，表现出TRPA1活性，因此可用作TRPA1调节剂。

  公开号：

  US20150376130A1

文献信息

• [EN] INHIBITORS OF TRYPTOPHAN DIOXYGENASES (IDO1 AND TDO) AND THEIR USE IN THERAPY<br/>[FR] INHIBITEURS DE TRYPTOPHANE DIOXYGÉNASES (IDO1 ET TDO) ET LEUR UTILISATION EN THÉRAPIE
  申请人：AUCKLAND UNISERVICES LTD

  公开号：WO2016024233A1

  公开（公告）日：2016-02-18

  Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR1, N or N-oxide; X is CR2, N or N-oxide; Y is CR3, N or N-oxide; Z is CR4, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and R9 and R10 are as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer.

  描述了包含具有IDO1和/or TDO抑制活性的3-氨基异恶唑啉化合物I的药物组合物，其中W是CR1，N或N-氧化物；X是CR2，N或N-氧化物；Y是CR3，N或N-氧化物；Z是CR4，N或N-氧化物；W、X、Y和Z中的至少一个是N或N-氧化物；R9和R10如所定义。还描述了使用这些化合物治疗各种疾病，如癌症的方法。
• Inhibitors of tryptophan dioxygenases (IDO1 and TDO) and their use in therapy
  申请人：AUCKLAND UNISERVICES LIMITED

  公开号：US10888567B2

  公开（公告）日：2021-01-12

  Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR1, N or N-oxide; X is CR2, N or N-oxide; Y is CR3, N or N-oxide; Z is CR4, N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and R9 and R10 are as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer.

  描述了包含具有 IDO1 和/或 TDO 抑制活性的式 I 的 3-氨基异噁唑吡啶化合物的药物组合物，其中 W 是 CR1、N 或 N-氧化物；X 是 CR2、N 或 N-氧化物；Y 是 CR3、N 或 N-氧化物；Z 是 CR4、N 或 N-氧化物；W、X、Y 和 Z 中至少有一个是 N 或 N-氧化物；R9 和 R10 如所定义。 还描述了使用此类化合物治疗各种疾病（如癌症）的方法。
• INHIBITORS OF TRYPTOPHAN DIOXYGENASES (IDO1 AND TDO) AND THEIR USE IN THERAPY
  申请人：Auckland Uniservices Limited

  公开号：EP3180002A1

  公开（公告）日：2017-06-21
• INHIBITORS OF TRYPTOPHAN DIOXYGENASES (IDO1 and TDO) AND THEIR USE IN THERAPY
  申请人：Palmer Brian Desmond

  公开号：US20170224701A1

  公开（公告）日：2017-08-10

  Pharmaceutical compositions comprising 3-aminoisoxazolopyridine compounds of the Formula I having IDO1 and/or TDO inhibitory activity are described, where W is CR 1 , N or N-oxide; X is CR 2 , N or N-oxide; Y is CR 3 , N or N-oxide; Z is CR 4 , N or N-oxide; and at least one of W, X, Y, and Z is N or N-oxide; and R 9 and R 10 are as defined. Also described are methods of using such compounds in the treatment of various conditions, such as cancer.
• US9533952B2
  申请人：——

  公开号：US9533952B2

  公开（公告）日：2017-01-03