5-(氨基甲基)呋喃-2-甲腈 | 776277-28-2

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 5-(氨基甲基)呋喃-2-甲腈
• 英文名称: 5-(Aminomethyl)furan-2-carbonitrile
• CAS: 776277-28-2
• 化学式: C₆H₆N₂O
• 分子量: 122.126
• InChiKey: AIBYYQLJOMFINU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  63
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 海关编码：
  2932190090

反应信息

• 作为反应物：
  描述：

  5-(氨基甲基)呋喃-2-甲腈 、 4-methyl-2-(4-(benzyloxy)-2-oxopyridin-1(2H)-yl)thiazole-5-carboxylic acid 以the title compound was obtained as a colorless solid in 72% yield的产率得到2-(4-(benzyloxy)-2-oxopyridin-1(2H)-yl)-N-((5-cyanofuran-2-yl)methyl)-4-methylthiazole-5-carboxamide
  参考文献：
  名称：

  ORGANIC COMPOUNDS

  摘要：

  本发明提供了能够调节硬脂酰辅酶A脱饱和酶活性的杂环衍生物。本发明还涵盖使用这些衍生物调节硬脂酰辅酶A脱饱和酶活性的方法，以及包含这些衍生物的制药组合物。

  公开号：

  US20090156615A1

文献信息

• ORGANIC COMPOUNDS
  申请人：Dales Natalie

  公开号：US20090156615A1

  公开（公告）日：2009-06-18

  The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

  本发明提供了调节硬脂酰辅酶A去饱和酶活性的杂环衍生物。还涵盖了利用这些衍生物调节硬脂酰辅酶A去饱和酶活性的方法以及包含这些衍生物的药物组合物。
• [EN] THROMBIN INHIBITORS<br/>[FR] INHIBITEURS DE THROMBINE
  申请人：LG CHEMICAL LTD

  公开号：WO2000039124A1

  公开（公告）日：2000-07-06

  The present invention relates to thrombin inhibitors of formula (I), wherein A, B, C, D, E, F and n have the meaning given in the description, that are useful as anticoagulants. In particular, this invention relates to peptide derivatives having high antithrombotic activity and high oral bioavailability.

  本发明涉及式(I)的凝血酶抑制剂，其中A、B、C、D、E、F和n具有描述中给定的含义，可用作抗凝剂。特别是，本发明涉及具有高抗血栓活性和高口服生物利用度的肽衍生物。
• Low-molecular serine proteases inhibitors comprising polyhydroxy-alkyl and polyhydroxy-cycloalkyl radicals
  申请人：——

  公开号：US20040048815A1

  公开（公告）日：2004-03-11

  The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or quanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates.Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.

  本发明涉及新型的氨基脲和胍类化合物，其生产和使用以及作为胰蛋白酶类丝氨酸蛋白酶竞争性抑制剂的用途，特别是作为凝血酶和补体蛋白酶CIs和C1r的抑制剂。本发明还涉及含有所述化合物作为活性成分的制药组合物，以及将该化合物用作凝血酶抑制剂、抗凝剂、补体抑制剂和抗炎剂的用途。新型组合物的特点是将具有氨基脲或胍类功能的丝氨酸蛋白酶抑制剂与具有两个或更多羟基功能的烷基基团连接起来，所述烷基基团源自糖衍生物。因此，几种糖结构组分或从糖中衍生的组分可以相互连接。这种将糖衍生物连接起来的原理使得可以获得口服活性化合物。
• LOW-MOLECULAR SERINE PROTEASES INHIBITORS COMPRISING POLYHYDROXY-ALKYL AND POLYHYDROXY-CYCLOALKYL RADICALS
  申请人：Herr Dieter

  公开号：US20110071285A1

  公开（公告）日：2011-03-24

  The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases CIs and C1r. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or guanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.

  本发明涉及新型的酰胺和脲类化合物，其生产和使用以及作为胰蛋白酶型丝氨酸蛋白酶竞争性抑制剂的用途，特别是作为凝血酶和补体蛋白酶CIs和C1r的抑制剂。本发明还涉及含有该化合物作为活性成分的制药组合物，以及将该化合物用作凝血酶抑制剂、抗凝剂、补体抑制剂和抗炎药的用途。这些新型化合物的特点是将具有酰胺或脲基功能的丝氨酸蛋白酶抑制剂与具有两个或更多羟基功能的烷基基团连接起来，其中该烷基基团来源于糖衍生物。因此，几种糖结构组分或从糖中衍生的组分可以相互连接。该连接糖衍生物的原理使得可以获得口服活性化合物。
• Synthesis of AC1903 analogs as potent transient receptor potential canonical channel 4/5 inhibitors and biological evaluation
  作者：Lili Chen、Zhuang Zhang、Hongtao Tian、Shan Jiang、Yunyun Ji、Mengru Liu、Jianhua Shen、Zhengyu Cao、Kai Wang

  DOI：10.1016/j.bmc.2022.116853

  日期：2022.8

  Transient receptor potential canonical (TRPC) channels are a class of non-selective cation channels expressed in a variety of tissues and organ systems where they functionally regulate physiological and pathological processes. TRPC5 has been shown to be a promising target for focal segmental glomerulosclerosis treatment. In this study, we report the synthesis and biological evaluation of a novel series

  瞬时受体电位经典 (TRPC) 通道是一类在各种组织和器官系统中表达的非选择性阳离子通道，它们在功能上调节生理和病理过程。TRPC5 已被证明是局灶节段性肾小球硬化治疗的有希望的靶点。在这项研究中，我们报告了一系列基于苯并咪唑的新型 TRPC5 抑制剂的合成和生物学评价。一种化合物8b在抑制 TRPC5 通道活性方面的效力是母体化合物 AC1903 的 100 倍。有趣的是，AC1903 和8b都以相似的效力抑制了 TRPC4 通道活性。化合物8b还显着减弱硫酸鱼精蛋白诱导的足细胞细胞骨架重组、白细胞介素 (IL)-17 诱导的细胞增殖和人角质形成细胞 HaCaT 细胞中促炎介质的表达。