3-(4-氨基吡啶-3-基)丙烯酸脂 | 773132-83-5

• 物质功能分类: 医药中间体 - 杂环化合物 - 吡啶类化合物
• 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
• 中文名称: 3-(4-氨基吡啶-3-基)丙烯酸脂
• 英文名称: 3-(4-Amino-3-pyridinyl)-2-propenoic acid
• 英文别名: (E)-3-(4-aminopyridin-3-yl)prop-2-enoic acid
• CAS: 773132-83-5
• 化学式: C₈H₈N₂O₂
• 分子量: 164.16
• InChiKey: DVXPOYXSNKWPOE-OWOJBTEDSA-N

物化性质

• 密度：
  1.361

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  76.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILARY TANGLES<br/>[FR] PYRROLO [2,3-C] PYRIDINES EN TANT QU'AGENTS D'IMAGERIE D'ENCHEVÊTREMENTS NEUROFIBRILLAIRES
  申请人：MERCK SHARP & DOHME

  公开号：WO2015188368A1

  公开（公告）日：2015-12-17

  Pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts are disclosed, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha- synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, the compounds are used as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. Futher, the compounds are useful for measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.

  公开了式(I)的吡咯吡啶化合物或其药学上可接受的盐，这些化合物可能适用于成像tau聚集体、β-折叠聚集体、β-淀粉样聚集体或α-突触核蛋白聚集体，因此在结合和成像阿尔茨海默病患者的tau聚集体方面是有用的。更具体地，这些化合物被用作正电子发射断层扫描（PET）成像中的示踪剂，用于研究体内脑部的tau沉积，以便诊断阿尔茨海默病和其他以tau病理为特征的神经退行性疾病。此外，这些化合物对于测量治疗阿尔茨海默病和其他以tau病理为特征的神经退行性疾病的临床疗效是有用的。
• [EN] PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILARY TANGLES<br/>[FR] PYRROLO[2,3-C]PYRIDINES UTILISABLES EN TANT QU'AGENTS D'IMAGERIE POUR LES ENCHEVÊTREMENTS NEUROFIBRILLAIRES
  申请人：MERCK SHARP & DOHME

  公开号：WO2015191506A2

  公开（公告）日：2015-12-17

  The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.

  本发明涉及式(I)的吡咯吡啶化合物或其药学上可接受的盐，可能适用于成像tau聚集体、β-折叠聚集体、β-淀粉样聚集体或α-突触核聚集体，因此有助于在阿尔茨海默病患者中结合和成像tau聚集体。更具体地，本发明涉及使用本发明化合物作为正电子发射断层扫描（PET）成像中的示踪剂，以研究体内脑中的tau沉积物，从而诊断阿尔茨海默病和其他以tau病理学为特征的神经退行性疾病。本发明还涉及一种测量治疗阿尔茨海默病和其他以tau病理学为特征的神经退行性疾病的临床疗效的方法。
• Novel therapeutic compounds
  申请人：Breinlinger Eric C.

  公开号：US20090069288A1

  公开（公告）日：2009-03-12

  Disclosed herein are novel compounds of Formula (I), wherein the variables are defined as herein. The compounds of Formula (I) are useful as kinase inhibitors and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases as well as proliferative disorders such as cancer.

  本文公开了公式（I）的新化合物，其中变量如本文所定义。公式（I）的化合物可用作激酶抑制剂，因此可用于治疗某些疾病和病症，特别是炎症性疾病和疾病以及增生性疾病，如癌症。
• Substituted Azaquinazolines Having an Antiviral Action
  申请人：Wunberg Tobias

  公开号：US20080132515A1

  公开（公告）日：2008-06-05

  This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.

  本发明涉及取代的氮杂喹唑啉，其制备方法，含有它们的制药组合物，以及它们用于治疗和/或预防疾病的用途，特别是用作抗病毒剂，特别是针对巨细胞病毒的用途。
• SUBSTITUTED AZAQUINAZOLINES HAVING AN ANTIVIRAL ACTION
  申请人：WUNBERG Tobias

  公开号：US20100179174A1

  公开（公告）日：2010-07-15

  This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.

  本发明涉及取代的氮杂喹噻啉，其制备过程，含有它们的药物组合物，以及它们用于治疗和/或预防疾病的用途，特别是用作抗病毒剂，特别是对抗巨细胞病毒。