N-[2-(1-piperidinyl)-5-(trifluoromethyl)phenyl]isonicotinthioamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: N-[2-(1-piperidinyl)-5-(trifluoromethyl)phenyl]isonicotinthioamide
• 英文别名: N-[2-piperidin-1-yl-5-(trifluoromethyl)phenyl]pyridine-4-carbothioamide
• 化学式: C₁₈H₁₈F₃N₃S
• 分子量: 365.422
• InChiKey: FOBKWLXNEMSEHR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  60.2
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  N-(2-(哌啶-1-基)-5-(三氟甲基)苯基)异烟酰胺 在 劳森试剂 、 sodium hydroxide 作用下， 以 甲苯 、 水 为溶剂， 反应 12.0h， 以33.7%的产率得到N-[2-(1-piperidinyl)-5-(trifluoromethyl)phenyl]isonicotinthioamide
  参考文献：
  名称：

  METHOD OF REGULATING PHOSPHORYLATION OF SR PROTEIN AND ANTIVIRAL AGENTS COMPRISING SR PROTEIN ACTIVITY REGULATOR AS THE ACTIVE INGREDIENT

  摘要：

  公开号：

  EP1712242B1

文献信息

• Method for controlling sr protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control sr protein activity
  申请人：Hagiwara Masatoshi

  公开号：US20070135367A1

  公开（公告）日：2007-06-14

  The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.

  本发明提供了：（1）通过减少或抑制SR蛋白活性作用的抗病毒剂，更具体地，（i）通过增强SR蛋白的去磷酸化作用的抗病毒剂，和（ii）通过抑制磷酸化SR蛋白的蛋白质的抗病毒剂；（2）通过抑制SR蛋白表达的抗病毒剂，和（3）通过激活拮抗SR蛋白的蛋白质的抗病毒剂。本发明还提供了抑制磷酸化SR蛋白的SRPKs的化合物。这些化合物抑制SR蛋白的活性并具有抗病毒活性。各种新病毒，包括SARS，已经出现，因此本发明提供了适用于新病毒的持久的广谱抗病毒剂。
• METHODS FOR CONTROLLING SR PROTEIN PHOSPHORYLATION, AND ANTIVIRAL AGENTS WHOSE ACTIVE INGREDIENTS COMPRISE AGENTS THAT CONTROL SR PROTEIN ACTIVITY
  申请人：Hagiwara Masatoshi

  公开号：US20100016359A1

  公开（公告）日：2010-01-21

  The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.

  本发明提供：（1）抗病毒剂，通过减少或抑制SR蛋白的活性发挥作用，更具体地，（i）通过增强SR蛋白的去磷酸化作用发挥作用的抗病毒剂，以及（ii）通过抑制磷酸化SR蛋白的蛋白质发挥作用的抗病毒剂；（2）通过抑制SR蛋白的表达发挥作用的抗病毒剂，以及（3）通过激活对抗SR蛋白的蛋白质发挥作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPKs的化合物。这些化合物抑制SR蛋白的活性，并具有抗病毒活性。各种新的病毒，包括SARS，已经出现，因此本发明提供适用于新病毒的持久广谱抗病毒剂。
• ANILINE DERIVATIVE HAVING ANTI-RNA VIRAL ACTIVITY
  申请人：Onogi Hiroshi

  公开号：US20110059950A1

  公开（公告）日：2011-03-10

  Viruses, and particularly RNA viruses, have high mutation rates. Hence, antiviral agents that have been developed to date targeting protease or reverse transcriptase of viruses have quickly lost their effectiveness and resistant viruses have emerged. Also, in recent years, viral diseases caused by various new viruses such as SARS, avian influenza, and the hepatitis C have become social menaces. Therefore, the development of a novel antiviral agent that can cope with a virus resistant to an existing drug or a new virus and has a wide range of applications has been demanded. The present invention provides a novel anti-RNA viral agent and a method for use thereof. The present invention further provides an anti-RNA viral agent that is also effective against a new virus or a drug-resistant virus, and a method for use thereof.

  病毒，特别是RNA病毒，具有较高的突变率。因此，迄今为止开发的针对病毒蛋白酶或反转录酶的抗病毒药物很快失去了效力，出现了耐药病毒。此外，近年来，由各种新病毒引起的病毒性疾病，如SARS，禽流感和丙型肝炎，已成为社会问题。因此，需要开发一种新型抗病毒药物，可以应对对现有药物产生耐药性的病毒或新的病毒，并具有广泛的应用范围。本发明提供了一种新型抗RNA病毒药物及其使用方法。本发明还提供了一种对新病毒或耐药病毒也有效的抗RNA病毒药物及其使用方法。
• Method for controlling SR protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control SR protein activity
  申请人：——

  公开号：US07569536B2

  公开（公告）日：2009-08-04

  The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.

  本发明提供以下内容：（1）抗病毒剂，通过减少或抑制SR蛋白的活性来发挥作用，更具体地，（i）通过增强SR蛋白的去磷酸化作用来发挥作用的抗病毒剂，以及（ii）通过抑制SR蛋白磷酸化的蛋白质来发挥作用的抗病毒剂；（2）通过抑制SR蛋白的表达来发挥作用的抗病毒剂，以及（3）通过激活对抗SR蛋白的蛋白质来发挥作用的抗病毒剂。本发明还提供抑制磷酸化SR蛋白的SRPKs的化合物。这些化合物抑制SR蛋白的活性，并具有抗病毒活性。各种新的病毒，包括SARS，已经出现，因此本发明提供了适用于新病毒的持久的广谱抗病毒剂。
• Methods for controlling SR protein phosphorylation, and antiviral agents whose active ingredients comprise agents that control SR protein activity
  申请人：Masatoshi Hagiwara

  公开号：US08338362B2

  公开（公告）日：2012-12-25

  The present invention provides: (1) antiviral agents that act by reducing or inhibiting the activity of SR proteins, more specifically, (i) antiviral agents that act by enhancing dephosphorylation of SR proteins, and (ii) antiviral agents that act by inhibiting proteins that phosphorylate SR proteins; (2) antiviral agents that act by inhibiting the expression of SR proteins, and (3) antiviral agents that act by activating proteins that antagonize SR proteins. The present invention also provides compounds that inhibit SRPKs, which phosphorylate SR proteins. Such compounds inhibit the activity of SR proteins and have antiviral activities. Various new viruses including SARS have emerged, and thus the present invention provides long-lasting broad-spectrum antiviral agents applicable to new viruses.

  本发明提供了以下内容：（1）抗病毒剂，通过降低或抑制SR蛋白活性来发挥作用，更具体地说，（i）通过增强SR蛋白去磷酸化的抗病毒剂，和（ii）通过抑制SR蛋白磷酸化的蛋白质的抗病毒剂；（2）通过抑制SR蛋白表达的抗病毒剂，和（3）通过激活对抗SR蛋白的蛋白质的抗病毒剂。本发明还提供了抑制SR蛋白激酶（SRPKs）的化合物，这些化合物抑制SR蛋白的活性，并具有抗病毒活性。各种新的病毒，包括SARS，已经出现，因此本发明提供了适用于新病毒的长效广谱抗病毒剂。