1-(7-甲氧基喹啉-4-基)-3-[6-(三氟甲基)吡啶-2-基]脲 | 1384424-80-9

• 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: 1-(7-甲氧基喹啉-4-基)-3-[6-(三氟甲基)吡啶-2-基]脲
• 英文名称: 1-(7-methoxyquinolin-4-yl)-3-(6-(trifluoromethyl)pyridin-2-yl)urea
• 英文别名: A 1070722；1-(7-Methoxyquinolin-4-yl)-3-[6-(trifluoromethyl)pyridin-2-yl]urea
• CAS: 1384424-80-9
• 化学式: C₁₇H₁₃F₃N₄O₂
• 分子量: 362.311
• InChiKey: VQPBIJGXSXEOCU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  76.1
• 氢给体数：
  2
• 氢受体数：
  7

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。
• METHOD FOR GENERATING FUNCTIONAL SKELETAL MUSCLE FIBERS INNERVATED BY MOTONEURONS
  申请人：Association Française contre les Myopathies (AFM)

  公开号：EP3913047A1

  公开（公告）日：2021-11-24

  The present invention relates to a method for the generation of functional skeletal muscle fibers innervated by motoneurons, from pluripotent stem cells.

  本发明涉及一种利用多能干细胞生成由运动神经元支配的功能性骨骼肌纤维的方法。
• Differentiation of hepatocyte-like cells from stem cells
  申请人：Agency for Science, Technology and Research

  公开号：US10323228B2

  公开（公告）日：2019-06-18

  Disclosed are methods of differentiating stem cells in order to obtain hepatocyte-like cells, the method comprising the steps of a) subjecting definitive endoderm to at least one epigenetic modulator to obtain hepatoblasts and b) subjecting the hepatoblasts to at least one stem cell differentiation pathway inhibitor to obtain hepatocyte-like cells; wherein steps a) and b) do not comprise the use of a growth factor. In one preferred embodiment, the epigenetic modulator may be sodium butyrate and/or DMSO and the stem cell differentiation pathway inhibitor may be SB431542 and/or DMSO. Also disclosed are hepatocyte-like cells obtained from the method and uses of these cells such as drug screening.

  本发明公开了分化干细胞以获得肝细胞样细胞的方法，该方法包括以下步骤：a)将确定的内胚层置于至少一种表观遗传调节剂中以获得肝母细胞；b)将肝母细胞置于至少一种干细胞分化途径抑制剂中以获得肝细胞样细胞；其中步骤a)和b)不包括使用生长因子。在一个优选的实施方案中，表观遗传调节剂可以是丁酸钠和/或二甲基亚砜，干细胞分化途径抑制剂可以是SB431542和/或二甲基亚砜。还公开了从该方法中获得的肝细胞样细胞以及这些细胞的用途，如药物筛选。
• Derivation of hepatic stem cells and mature liver cell types and uses thereof
  申请人：AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

  公开号：US10683484B2

  公开（公告）日：2020-06-16

  This application describes liver stem cells (LSC), and differentiated hepatocytes, cholangiocytes, and 3D cellular structures derived therefrom. Methods for producing LSC and mature, differentiated hepatocytes and cholangiocytes in culture are provided. Also provided are cell culture systems and cell culture media for producing a homogenous population of liver stem cells that remain in an undifferentiated state over multiple passages in culture. The LSC and methods are useful for producing homogenous populations of hepatocytes and cholangiocytes for downstream applications. The LSC can be transplanted into subjects to treat liver diseases.

  本申请介绍了肝干细胞（LSC）、分化的肝细胞、胆管细胞以及由此衍生的三维细胞结构。本申请提供了在培养过程中产生 LSC 以及成熟、分化的肝细胞和胆管细胞的方法。此外，还提供了细胞培养系统和细胞培养基，用于产生在培养过程中多次传代保持未分化状态的同源肝干细胞群。这种肝干细胞和方法可用于生产下游应用所需的同源肝细胞和胆管细胞。肝干细胞可移植到受试者体内治疗肝脏疾病。