4-氨基-5,8-二氟喹啉 | 874818-15-2

• 物质功能分类: 医药中间体 - 杂环化合物 - 喹啉类化合物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 4-氨基-5,8-二氟喹啉
• 英文名称: 4-Amino-5,8-difluoroquinoline
• 英文别名: 5,8-difluoroquinolin-4-amine
• CAS: 874818-15-2
• 化学式: C₉H₆F₂N₂
• 分子量: 180.15
• InChiKey: ABLPERMEPTWCLZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS
  申请人：Turner Sean Colm

  公开号：US20120172376A1

  公开（公告）日：2012-07-05

  The present invention relates to novel heterocyclic compounds of formula I wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3β, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3β activity using the compounds.

  本发明涉及式I的新颖杂环化合物，其中变量如权利要求或说明书中所定义，这些化合物可用于抑制糖原合酶激酶3（GSK-3），包含这些化合物的组合物，以及使用这些化合物制备用于治疗对调节、优选抑制GSK-3β活性化合物敏感的医疗病症的药物的用途，以及使用这些化合物治疗对调节GSK-3β活性化合物敏感的医疗病症的方法。
• 1-(QUINOLIN-4-YL)-3-(6-(TRIFLUOROMETHYL)-PYRIDIN-2-YL)UREA AND 1-(QUINOLIN-4-YL)-3-(6-(TRIFLUOROMETHYL)-PYRAZINE-2-YL)UREA DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 (GSK-3) INHIBITORS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES
  申请人：AbbVie Deutschland GmbH & Co. KG

  公开号：EP3351543A1

  公开（公告）日：2018-07-25

  The present invention relates to 1-(quinolin-4-yl)-3-(6-(trifluoromethyl)-pyridin-2-y)urea and 1-(quinolin-4-yl)-3-(6-(trifluoromethyl)-pyrazine-2-yl) urea derivates of formula (I-2): as glycogen synthase kinase 3 (GSK-3) for treating e.g. schizophrenia, Alzheimer's disease, behavioural and psychiatric symptoms of dementia, Parkinson's disease, tauopathies, vascular dementia, acute stroke and other traumatic injuries, cerebrovascular accidents, brain and spinal cord trauma, peripheral neuropathies, bipolar disorders, retinopathies, glaucoma, pain, rheumatoid arthritis and osteoarthritis. A preferred example is e.g. 1-(quinolin-4-yl)-3-(6-(trifluoromethyl)-pyridin-2-yl)urea.

  本发明涉及式 (I-2) 的 1-(喹啉-4-基)-3-(6-(三氟甲基)-吡啶-2-基)脲和 1-(喹啉-4-基)-3-(6-(三氟甲基)-吡嗪-2-基)脲衍生物： 作为糖原合酶激酶 3（GSK-3）用于治疗精神分裂症、阿尔茨海默病、痴呆的行为和精神症状、帕金森病、陶氏病、血管性痴呆、急性中风和其他外伤、脑血管意外、脑和脊髓创伤、周围神经病、双相情感障碍、视网膜病变、青光眼、疼痛、类风湿性关节炎和骨关节炎等。一个优选的例子是 1-(喹啉-4-基)-3-(6-(三氟甲基)-吡啶-2-基)脲。
• US9090592B2
  申请人：——

  公开号：US9090592B2

  公开（公告）日：2015-07-28
• US9540370B2
  申请人：——

  公开号：US9540370B2

  公开（公告）日：2017-01-10
• [EN] HETEROCYCLIC COMPOUNDS AND THEIR USE AS GLYCOGEN SYNTHASE KINASE-3 INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE LA GLYCOGÈNE SYNTHASE KINASE-3
  申请人：ABBOTT GMBH & CO KG

  公开号：WO2012089828A2

  公开（公告）日：2012-07-05

  The present invention relates to novel heterocyclic compounds of formula (I), wherein the variables are as defined in the claims or the description, which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), compositions containing the compounds, their use for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a compound that modulates, preferably inhibits, the activity of glycogen synthase kinase 3β, and methods of treatment of medical disorders susceptible to treatment with a compound that modulates glycogen synthase kinase 3β activity using the compounds.