1-[2-amino-4-(trifluoromethyl)phenyl]indoline | 73551-84-5

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1-[2-amino-4-(trifluoromethyl)phenyl]indoline
• 英文别名: 1-(2-amino-4-trifluoromethylphenyl)indoline；1-(2-Amino-4-trifluormethylphenyl)-indolin；2-(2,3-Dihydro-1H-indol-1-YL)-5-(trifluoromethyl)-phenylamine；2-(2,3-dihydroindol-1-yl)-5-(trifluoromethyl)aniline
• CAS: 73551-84-5
• 化学式: C₁₅H₁₃F₃N₂
• 分子量: 278.277
• InChiKey: OZMPKNJOSOOJBN-UHFFFAOYSA-N

物化性质

• 沸点：
  391.8±42.0 °C(Predicted)
• 密度：
  1.327±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.8
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  29.3
• 氢给体数：
  1
• 氢受体数：
  5

安全信息

• 危险等级：
  IRRITANT

反应信息

• 作为反应物：
  描述：

  1-[2-amino-4-(trifluoromethyl)phenyl]indoline 、 氯化异氰盐酸盐 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 2.5h， 以90.1%的产率得到N-[2-(1-indolinyl)-5-(trifluoromethyl)phenyl]isonicotinamide
  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
• 作为产物：
  描述：

  1-(2-nitro-4-trifluoromethyl-phenyl)-2,3-dihydro-indole 在 盐酸 、 tin(ll) chloride 、 水 、 碳酸氢钠 作用下， 以 甲醇 为溶剂， 反应 8.0h， 以93.9%的产率得到1-[2-amino-4-(trifluoromethyl)phenyl]indoline
  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

• Benzo[b]pyrrolo[3,2,1-jk][1,4]benzodiazepines having dopamine receptor
  申请人：Hoechst-Roussel Pharmaceuticals Inc.

  公开号：US04663453A1

  公开（公告）日：1987-05-05

  The invention relates to benzopyrrolobenzodiazepines and quinobenzodiazepines of the formula ##STR1## where X and Y may be the same or different and each is hydrogen, halogen, CF.sub.3, lower alkyl, lower alkoxy, lower alkylthio and lower alkylsulfonyl, p and q are independently 1 or 2; R.sub.1 is hydrogen when R.sub.2 is bonded to R.sub.3 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; R.sub.3 is hydrogen when R.sub.1 is bonded to R.sub.2 to form a --(CH.sub.2).sub.m --CH.sub.2 -- group or a --CH.dbd.CH-- group; m is 1 or 2; R.sub.4 is NR.sub.5 R.sub.6 wherein R.sub.5 is hydrogen or lower alkyl and R.sub.6 is hydrogen, lower alkyl or a group of the formula (CH.sub.2).sub.n NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are lower alkyl, and n is 2 or 3, ##STR2## wherein R.sub.9 is lower alkyl, ##STR3## wherein R.sub.10 is CH.sub.2 CH.sub.2 OH, lower alkyl, phenyl, phenyl substituted by halogen, CF.sub.3, lower alkyl, lower alkoxy or lower alkylthio, benzyl, benzyl in which the phenyl group is substituted by halogen, CF.sub.3, lower alkyl, lower alkoxy or lower alkylthio or CO.sub.2 R.sub.11 wherein R.sub.11 is lower alkyl, or a pharmaceutically acceptable acid salt thereof.

  该发明涉及苯并吡咯苯二氮杂环和喹诺苯二氮杂环，其化学式为##STR1##其中X和Y可以相同也可以不同，每个都是氢、卤素、CF.sub.3、低烷基、低烷氧基、低烷硫基和低烷基磺酰基，p和q独立地为1或2；R.sub.1为氢，当R.sub.2与R.sub.3连接形成--(CH.sub.2).sub.m --CH.sub.2 --基团或--CH.dbd.CH--基团时；R.sub.3为氢，当R.sub.1与R.sub.2连接形成--(CH.sub.2).sub.m --CH.sub.2 --基团或--CH.dbd.CH--基团时；m为1或2；R.sub.4为NR.sub.5 R.sub.6，其中R.sub.5为氢或低烷基，R.sub.6为氢、低烷基或(CH.sub.2).sub.n NR.sub.7 R.sub.8基团，其中R.sub.7和R.sub.8为低烷基，n为2或3，##STR2##其中R.sub.9为低烷基，##STR3##其中R.sub.10为CH.sub.2 CH.sub.2 OH、低烷基、苯基、被卤素、CF.sub.3、低烷基、低烷氧基或低烷硫基取代的苯基、苄基、苄基中苯基被卤素、CF.sub.3、低烷基、低烷氧基或低烷硫基取代或CO.sub.2 R.sub.11，其中R.sub.11为低烷基，或其药学上可接受的酸盐。
• Indolo-,1,2-dihydroindolo-, and 1,2,6,7-tetrahydroindolo [1,7-ab][1,5]
  申请人：American Hoechst Corporation

  公开号：US04186199A1

  公开（公告）日：1980-01-29

  What is disclosed are ##STR1## wherein X is hydrogen, halogen or trifluoromethyl; Y is hydrogen, halogen or trifluoromethyl; R is hydrogen, loweralkyl, cycloalkyl, phenyl, halophenyl, furyl, pyridinyl, 4-methylpiperazin-1-ylethyl or phenylloweralkyl; R.sup.1 is hydrogen; n and m are independently 0 or 1, but n is not 0 when m is 1, and the bonds between ring positions 1 and 2 and between positions 6 and 7 are respectively saturated when n and m are 1 and are unsaturated when n and m are 0; pharmaceutically acceptable acid addition salts thereof; methods of preparing said compounds; pharmaceutical compositions including said compounds; methods of treatment using the compounds; and intermediates therefor. These compounds are useful as analgesic and anti-inflammatory agents, as well as intermediates for the preparation of other pharmaceutically active compounds.

  所披露的是##STR1##其中X为氢、卤素或三氟甲基；Y为氢、卤素或三氟甲基；R为氢、低碳基、环烷基、苯基、卤代苯基、呋喃基、吡啶基、4-甲基哌嗪-1-乙基或苯基低碳基；R.sup.1为氢；n和m独立地为0或1，但当m为1时，n不为0，当n和m为1时，1和2号环位置之间的键和6和7号位置之间的键分别饱和，当n和m为0时，它们是不饱和的；药学上可接受的酸盐；制备这些化合物的方法；包括这些化合物的制药组合物；使用这些化合物的治疗方法；以及其中间体。这些化合物可用作镇痛和抗炎剂，以及其他药学活性化合物的制备中间体。
• 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。
• 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。