4-(2-(2-fluorophenyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl)pyridine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-(2-(2-fluorophenyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl)pyridine
• 英文别名: 4-[2-(2-fluorophenyl)-4-(4-fluorophenyl)-1H-imidazol-5-yl]pyridine
• 化学式: C₂₀H₁₃F₂N₃
• 分子量: 333.34
• InChiKey: QIFJOFNVIVQRNJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  25
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  41.6
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] 2,4,5-TRI-SUBSTITUTED AZOLE-BASED CASEIN KINASE 1 INHIBITORS AS INDUCERS FOR CARDIOMYOGENESIS<br/>[FR] INHIBITEURS DE LA CASÉINE KINASE 1 À BASE D'AZOLE 2,4,5-TRI-SUBSTITUÉ EN TANT QU'INDUCTEURS DE LA CARDIOMYOGENÈSE
  申请人：AGENCY SCIENCE TECH & RES

  公开号：WO2015119579A1

  公开（公告）日：2015-08-13

  This invention relates to a method for inducing or enhancing the differentiation of pluripotent stem cells into cardiomyocyte via casein kinase 1 inhibition said method comprising culturing the stem cells in the presence of a medium comprising a casein kinase 1 inhibitor of the formula (I) or (II) or a stereoisomer, tautomer, or a salt thereof wherein R1, R2 and R3 independently from another represent hydrogen, optionally substituted alkyl, alkenyl, alkynyl, heterocyclyl, heteroaryl or aryl; X represents NR4, O or S; and R4 represents hydrogen, optionally substituted alkyl, alkenyl, alkynyl, heterocyclyl, heteroaryl or aryl. The method can be used in the late phase of stem cell differentiation and in the compounds of formula (I) or (II) in combination with other small molecules can lead to especially high differentiation of stem cells into cardiomyocytes. The invention further relates to novel compounds which can be used in the method of the invention and kits for stem cell differentiation.

  本发明涉及一种通过酪蛋白激酶1抑制诱导或增强多能干细胞向心肌细胞分化的方法，所述方法包括将干细胞培养在含有式(I)或(II)的酪蛋白激酶1抑制剂的培养基中，或其立体异构体、互变异构体或盐中，其中R1、R2和R3独立地表示氢、可选择地取代的烷基、烯烃基、炔烃基、杂环基、杂芳基或芳基；X表示NR4、O或S；R4表示氢、可选择地取代的烷基、烯烃基、炔烃基、杂环基、杂芳基或芳基。该方法可用于干细胞分化的后期阶段，结合式(I)或(II)的化合物与其他小分子一起可导致干细胞特别高效地分化为心肌细胞。该发明还涉及可用于该方法的新化合物以及用于干细胞分化的试剂盒。
• Producing mesodermal cell types and methods of using the same
  申请人：The Board of Trustees of the Leland Stanford Junior University

  公开号：US10787640B2

  公开（公告）日：2020-09-29

  Methods are provided for the generation of mesodermal cell types and derivatives thereof. Also provided are methods for generating purified populations of mesodermal cell types and derivatives thereof. The instant disclosure also provides methods of screening for cellular responses of the generated mesodermal cell types and derivatives thereof. Also provide are methods for screening for organismal phenotypes induced by introduction of the generated mesodermal cell types and derivatives thereof. Treatment methods making use of the generated mesodermal cell types and derivatives thereof are also provided. The instant disclosure also provides systems, compositions, and kits for practicing the methods of the disclosure.

  提供了生成中胚层细胞类型及其衍生物的方法。还提供了生成纯化的中胚层细胞类型及其衍生物的方法。本发明还提供了筛选所产生的中胚层细胞类型及其衍生物的细胞反应的方法。本发明还提供了通过引入所产生的中胚层细胞类型及其衍生物来筛选生物表型的方法。还提供了利用生成的中胚层细胞类型及其衍生物的治疗方法。本发明还提供了用于实施本发明方法的系统、组合物和试剂盒。
• 2,4,5-tri-substituted azole-based casein kinase 1 inhibitors as inducers for cardiomyogenesis
  申请人：AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH

  公开号：US10865384B2

  公开（公告）日：2020-12-15

  This invention relates to a method for inducing or enhancing the differentiation of pluripotent stem cells into cardiomyocyte via casein kinase 1 inhibition said method comprising culturing the stem cells in the presence of a medium comprising a casein kinase 1 inhibitor of the formula (I) or (II) or a stereoisomer, tautomer, or a salt thereof wherein R1, R2 and R3 independently from another represent hydrogen, optionally substituted alkyl, alkenyl, alkynyl, heterocyclyl, heteroaryl or aryl; X represents NR4, O or S; and R4 represents hydrogen, optionally substituted alkyl, alkenyl, alkynyl, heterocyclyl, heteroaryl or aryl. The method can be used in the late phase of stem cell differentiation and in the compounds of formula (I) or (II) in combination with other small molecules can lead to especially high differentiation of stem cells into cardiomyocytes. The invention further relates to novel compounds which can be used in the method of the invention and kits for stem cell differentiation.

  本发明涉及一种通过抑制酪蛋白激酶1诱导或增强多能干细胞向心肌细胞分化的方法，所述方法包括在含有式(I)或(II)的酪蛋白激酶1抑制剂或其立体异构体、同系物或盐的培养基存在下培养干细胞，其中R1、R2和R3独立地代表氢、任选取代的烷基、烯基、炔基、杂环基、杂芳基或芳基；X 代表 NR4、O 或 S；R4 代表氢、任选取代的烷基、烯基、炔基、杂环基、杂芳基或芳基。该方法可用于干细胞分化的后期阶段，式（I）或（II）化合物与其他小分子结合使用，可使干细胞分化为心肌细胞的程度特别高。本发明进一步涉及可用于本发明方法和干细胞分化试剂盒的新型化合物。
• Compounds for reducing c-Myc in c-Myc overexpressing cancers background
  申请人：The Trustees of Columbia University in the City of New York

  公开号：US10882863B2

  公开（公告）日：2021-01-05

  The invention relates to new compounds that reduce c-Myc expression and useful for cancer treatment, particularly hematological cancers such as aggressive B- and T-cell lymphomas. The new compounds may be combined with adjunct c-Myc inhibor agents such as a PI3K inhibitor, CK-1 inhibitor, Akt-inhibitor, proteasome inhibitor and/or mTor inhibitor. The c-Myc reducing agent may be provided as a lead-in treatment to reduce or initiate reduction of c-Myc prior to administration of the adjunct cancer therapeutic agent. Treatment with a c-Myc reducing agent modulates the disease state of the c-Myc overexpressing cancer making it less malignant and more susceptible to adjunctive cancer therapies.

  本发明涉及可降低 c-Myc 表达并可用于癌症治疗的新化合物，特别是血液肿瘤，如侵袭性 B 细胞和 T 细胞淋巴瘤。新化合物可与辅助性 c-Myc 抑制剂如 PI3K 抑制剂、CK-1 抑制剂、Akt-抑制剂、蛋白酶体抑制剂和/或 mTor 抑制剂结合使用。c-Myc还原剂可作为先导疗法，在使用辅助癌症治疗剂之前减少或开始减少c-Myc。使用c-Myc还原剂治疗可调节c-Myc过表达癌症的疾病状态，使其恶性程度降低，更容易接受辅助癌症疗法。
• 2,4,5-TRI-SUBSTITUTED AZOLE-BASED CASEIN KINASE 1 INHIBITORS AS INDUCERS FOR CARDIOMYOGENESIS
  申请人：Agency for Science, Technology and Research

  公开号：EP3102207B1

  公开（公告）日：2022-05-11