2-morpholinoisonicotinoyl chloride | 295349-76-7

• 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-morpholinoisonicotinoyl chloride
• 英文别名: 2-Morpholinopyridine-4-carbonyl chloride；2-morpholin-4-ylpyridine-4-carbonyl chloride
• CAS: 295349-76-7
• 化学式: C₁₀H₁₁ClN₂O₂
• 分子量: 226.663
• InChiKey: OQFAXSPFUPJZMP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  42.4
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-morpholinoisonicotinoyl chloride 在 palladium on activated charcoal 氢气 、 三乙胺 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 生成 N-(3-amino-4-methylphenyl)-2-morpholinopyridine-4-carboxamide
  参考文献：
  名称：

  A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis

  摘要：

  A novel p38 MAP kinase inhibitor structural class was discovered through selectivity screening. The rational analogue design, synthesis and structure-activity relationship of this series of bisamide inhibitors is reported. The inhibition in vitro of human p38alpha enzyme activity and lipopolysaccharide-induced tumour necrosis factor-alpha release is described for the series. The activity in vivo and pharmacokinetic properties are exemplified for the more potent analogues. (C) 2004 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2004.08.006
• 作为产物：
  描述：

  2-(4-吗啉基)异烟酸 在 草酰氯 、 N,N-二甲基甲酰胺 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 2-morpholinoisonicotinoyl chloride
  参考文献：
  名称：

  DIAZANAPHTHALEN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF

  摘要：

  本公开涉及使用二氮萘化合物或其类似物治疗通过激活Wnt途径信号传导特征的疾病的方法。更具体地，本公开涉及在治疗由Wnt途径信号传导激活所特征化的疾病（例如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺部疾病、炎症、自身免疫疾病和骨关节炎）中使用二氮萘化合物或其类似物，以及调节由Wnt途径信号传导介导的细胞事件，以及与DYRK1A过表达相关的神经病症/紊乱/疾病。

  公开号：

  US20190127370A1

文献信息

• DIAZANAPHTHALEN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF
  申请人：Samumed, LLC

  公开号：US20190127370A1

  公开（公告）日：2019-05-02

  Diazanaphthalene compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a diazanaphthalene compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

  本公开涉及使用二氮萘化合物或其类似物治疗通过激活Wnt途径信号传导特征的疾病的方法。更具体地，本公开涉及在治疗由Wnt途径信号传导激活所特征化的疾病（例如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺部疾病、炎症、自身免疫疾病和骨关节炎）中使用二氮萘化合物或其类似物，以及调节由Wnt途径信号传导介导的细胞事件，以及与DYRK1A过表达相关的神经病症/紊乱/疾病。
• Amide derivatives
  申请人：ASTRAZENECA AB

  公开号：US20030186966A1

  公开（公告）日：2003-10-02

  This invention concerns amide derivatives of Formula (I) wherein X is CH or N; Y is CH or N; m is 0-3; R 1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-3; R 2 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and (1-6C)alkoxycarbonyl; R 3 is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; q is 0-4; and Q is a group such as aryl, aryloxy, aryl-(1-6C)alkoxy, arylamino, N-(1-6C)alkyl-arylamino and aryl-(1-6C)alkylamino; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.

  本发明涉及式（I）的酰胺衍生物，其中X为CH或N; Y为CH或N; m为0-3; R1为羟基、卤素、三氟甲基、氰基、巯基、硝基、氨基、羧基和氨基甲酰基等基团; n为0-3; R2为羟基、卤素、三氟甲基、氰基、巯基、硝基、氨基、羧基和(1-6C)烷氧基甲酰基等基团; R3为氢、卤素、(1-6C)烷基或(1-6C)烷氧基; q为0-4; Q为芳基、芳氧基、芳基-(1-6C)烷氧基、芳基氨基、N-(1-6C)烷基芳基氨基和芳基-(1-6C)烷基氨基等基团; 或其药学上可接受的盐或体内可降解的酯; 以及制备它们的方法、含有它们的制药组合物以及它们在通过细胞因子介导的疾病或医疗状况的治疗中的应用。
• 2-AMINOQUINAZOLINE DERIVATIVES
  申请人：Kishikawa Kuniyuki

  公开号：US20090137583A1

  公开（公告）日：2009-05-28

  The present invention provides 2-aminoquinazoline derivatives represented by formula (I): wherein R 1 and R 2 may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, and the like; X represents a bond or CR 7a R 7b wherein R 7a and R 7b may be the same or different and each represents a hydrogen atom, and the like; when X is a bond, R 3 represents substituted or unsubstituted aryl or a substituted or unsubstituted aromatic heterocyclic group; when X is CR 7a R 7b wherein R 7a and R 7b have the same meanings as defined above, respectively, R 3 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted aryl, and the like; R 4 represents a hydrogen atom, hydroxy, substituted or unsubstituted lower alkoxy, and the like; and R 5 represents a hydrogen atom, substituted or unsubstituted aryl, and the like, or a pharmaceutically acceptable salt thereof.

  本发明提供了由式(I)表示的2-氨基喹唑啉衍生物：其中R1和R2可以相同或不同，每个代表氢原子，取代或未取代的低烷基等；X表示键或CR7aR7b，其中R7a和R7b可以相同或不同，每个代表氢原子等；当X为键时，R3表示取代或未取代的芳基或取代或未取代的芳香杂环基；当X为CR7aR7b时，其中R7a和R7b的含义分别如上所定义，R3表示取代或未取代的低烷氧基，取代或未取代的芳基等；R4表示氢原子，羟基，取代或未取代的低烷氧基等；而R5表示氢原子，取代或未取代的芳基等，或其药学上可接受的盐。
• Diazanaphthalen-3-yl carboxamides and preparation and use thereof
  申请人：Samumed, LLC

  公开号：US10703748B2

  公开（公告）日：2020-07-07

  Diazanaphthalene compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a diazanaphthalene compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.

  本发明公开了用于治疗各种疾病和病理的重氮萘化合物。更具体地说，本公开涉及重氮萘化合物或其类似物在治疗以 Wnt 通路信号激活为特征的疾病（如癌症、异常细胞增殖、血管生成、阿尔茨海默病、肺病、炎症、自身免疫性疾病和骨关节炎）、调节由 Wnt 通路信号介导的细胞事件以及与 DYRK1A 过度表达相关的神经系统状况/紊乱/疾病中的用途。
• WO2006/118256
  申请人：——

  公开号：——

  公开（公告）日：——