2-(3,6-dihydro-2H-pyran-4-yl)-4-nitropyridine | 848580-47-2

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 2-(3,6-dihydro-2H-pyran-4-yl)-4-nitropyridine
• 英文别名: 2-(3,6-dihydro-2H-pyran-4-yl)-4-nitro-pyridine
• CAS: 848580-47-2
• 化学式: C₁₀H₁₀N₂O₃
• 分子量: 206.201
• InChiKey: ROIGSZAZUDIHSV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  67.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(3,6-dihydro-2H-pyran-4-yl)-4-nitropyridine 在 钯 氢气 、 甲醇 、 dichloromethane MeOH Et3N 作用下， 以 四氢呋喃 、 溶剂黄146 为溶剂， 反应 16.0h， 以Flash chromatography (methanol/dichloromethane/triethylamine 100/5/1) afforded 4.75 g (100%) 2-(tetrahydro-pyran-4-yl)-pyridin-4-ylamine as a light yellow oil的产率得到2-tetrahydropyran-4-ylpyridin-4-amine
  参考文献：
  名称：

  Thiazolopyridine

  摘要：

  本发明涉及式I的化合物，其中R1和R2如下所述。这些化合物对A2A受体具有高亲和力，并对A1和A3受体具有良好的选择性。这些化合物在治疗阿尔茨海默病、抑郁症、帕金森病和注意力缺陷多动障碍等方面是有用的。

  公开号：

  US20050065151A1
• 作为产物：
  描述：

  2-溴-4-硝基吡啶 、 3,6-二氢-2H-吡喃-4-硼酸频哪醇酯 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 potassium carbonate 作用下， 以 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 以54.87%的产率得到2-(3,6-dihydro-2H-pyran-4-yl)-4-nitropyridine
  参考文献：
  名称：

  [EN] THIOPHENE COMPOUNDS WITH CYCLIC AMIDES, AND USES THEREOF
  [FR] COMPOSÉS THIOPHÈNE AYANT DES AMIDES CYCLIQUES, ET LEURS UTILISATIONS

  摘要：

  本文提供了包含四环核心的化合物，例如Formula (I)和Formula (II)的化合物，以及这些化合物的药用盐、溶剂合物、互变异构体、同位素或同分异构体。本文还提供了使用这些化合物或其药用盐、溶剂合物、互变异构体、同位素或同分异构体来抑制类固醇调节元件结合蛋白（SREBP）途径的组分的方法，例如SREBP或SREBP裂解激活蛋白（SCAP）。此外，还提供了治疗患有肝病、非酒精性脂肪肝、胰岛素抵抗或癌症等疾病的方法。

  公开号：

  WO2021097123A1

文献信息

• Thiazolopyridine
  申请人：Norcross David Roger

  公开号：US20050065151A1

  公开（公告）日：2005-03-24

  The present invention relates to compounds of formula I wherein R 1 and R 2 are described hereinbelow. These compounds have high affinity to A 2A receptors and good selectivity to A 1 and A 3 receptors. These compounds are useful, inter alia, in the treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.

  本发明涉及式I的化合物，其中R1和R2如下所述。这些化合物对A2A受体具有高亲和力，并对A1和A3受体具有良好的选择性。这些化合物在治疗阿尔茨海默病、抑郁症、帕金森病和注意力缺陷多动障碍等方面具有用途。
• THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP1670805A1

  公开（公告）日：2006-06-21
• US7273865B2
  申请人：——

  公开号：US7273865B2

  公开（公告）日：2007-09-25
• [EN] THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS<br/>[FR] DERIVES DE THIAZOLOPYRIDINE EN TANT QUE LIGANDS DU RECEPTEUR D'ADENOSINE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2005028484A1

  公开（公告）日：2005-03-31

  The present invention relates to compounds of the general formula (I) wherein R1 is morpholin-4-yl, phenyl or tetrahydropyran-4-yl; R2 is -(CH2)n-aryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkoxy, lower alkyl, -(CH2)n NR’R', -0 (CH2)n-O -lower alkyl, or -(CH2)n-heterocyclyl, or is heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, -(CH2)n NR'R', -(CH2)n-heterocyclyl, which is optionally substituted by hydroxy or lower alkoxy, or is -(CH2)n-heterocyclyl, optionally substituted by one or more substituents selected from the group consisting of -(CH2)n,-OH, -(CH2)n-O-lower alkyl or lower alkyl, or is -(CH2)n-cycloalkyl, or is - (CH2)n,-O -lower alkyl, or is NR'R’’, or is benzo[1,3]dioxole, 2-methyl-l-oxo-2,8-diaza-spiro[4,5] decane, 2-oxa-5-aza­bicyclo [2.2.1]heptane or I-oxa-8-aza-spiro[4.5]decane; R',R' are independently from each other lower alkyl, - (CH2)n ,-O -lower alkyl or cycloalkyl, optionally substituted by hydroxy; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or against asthma, allergic responses, hypoxia, ischaernia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for disorders such as coronary artery disease and heart failure. The most preferred indications in accordance with the present invention are those which include disorders of the central nervous system, for example the treatment or prevention of Alzheimer's disease, certain depressive disorders, drug addiction, neuroprotection and Parkinson's disease as well as ADHD.
• [EN] THIOPHENE COMPOUNDS WITH CYCLIC AMIDES, AND USES THEREOF<br/>[FR] COMPOSÉS THIOPHÈNE AYANT DES AMIDES CYCLIQUES, ET LEURS UTILISATIONS
  申请人：CAPULUS THERAPEUTICS LLC

  公开号：WO2021097123A1

  公开（公告）日：2021-05-20

  Provided herein are compounds comprising a four-ring core, such as compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts, solvates, tautomers, isotopes, or isomers thereof. Also provided herein are methods of inhibiting a component of the sterol regulatory element binding protein (SREBP) pathway, such as an SREBP or SREBP cleavage activating protein (SCAP), using these compounds, or pharmaceutically acceptable salts, solvates, tautomers, isotopes, or isomers thereof. Further provided are methods of treating a disorder in a subject in need thereof, such as liver disease, non-alcoholic steatohepatitis, insulin resistance, or cancer.

  本文提供了包含四环核心的化合物，例如Formula (I)和Formula (II)的化合物，以及这些化合物的药用盐、溶剂合物、互变异构体、同位素或同分异构体。本文还提供了使用这些化合物或其药用盐、溶剂合物、互变异构体、同位素或同分异构体来抑制类固醇调节元件结合蛋白（SREBP）途径的组分的方法，例如SREBP或SREBP裂解激活蛋白（SCAP）。此外，还提供了治疗患有肝病、非酒精性脂肪肝、胰岛素抵抗或癌症等疾病的方法。