5-(2,6-difluorophenyl)-N-(4-(piperidin-4-ylmethoxy)pyrimidin-5-yl)thiophene-2-carboxamide | 1422470-10-7

• 分子结构分类: 有机化合物 - 有机杂环化合物
• 英文名称: 5-(2,6-difluorophenyl)-N-(4-(piperidin-4-ylmethoxy)pyrimidin-5-yl)thiophene-2-carboxamide
• 英文别名: 5-(2,6-difluorophenyl)-N-[4-(piperidin-4-ylmethoxy)pyrimidin-5-yl]thiophene-2-carboxamide
• CAS: 1422470-10-7
• 化学式: C₂₁H₂₀F₂N₄O₂S
• 分子量: 430.478
• InChiKey: PUAPKAREQIUKAD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  30
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  104
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• PIM KINASE INHIBITORS AND PREPARATION METHODS AND USE IN MEDICINAL MANUFACTURE THEREOF
  申请人：GE Yu

  公开号：US20140162999A1

  公开（公告）日：2014-06-12

  PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds as represented by Formula I. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.

  本发明涉及一种具有以下式子表示的结构的PIM激酶抑制剂化合物，以及该化合物的异构体、对映体、二对映异构体、互变异构体和药学上可接受的盐。该化合物能够显著抑制PIm激酶活性，并可用于制备用于治疗PIM激酶介导疾病（如癌症、自身免疫疾病、过敏反应或器官移植排斥等）的药物。此外，还提供了制备上述式子所示化合物的方法。
• PIM KINASE INHIBITOR AND PREPARATION METHOD AND USE IN MEDICINAL MANUFACTURE THEREOF
  申请人：Jikai Biosciences Inc.

  公开号：EP2743271A1

  公开（公告）日：2014-06-18

  The present invention provided a PIM kinase inhibitor - a compound with a general structural formula represented by Formula I. Also provided are isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts represented by Formula 1. E, J1, J2, Q, X, Y, Z and m in Formula I are defined in Claim 1. A PIM biochemical assay shows that the compounds (1-63) of the present invention can significant inhibit PIM-1 kinase activity. At 3 micromolar concentration, the compounds of the present invention can inhibit PIM-2 and PIM-3 activities by as much as 100%. Therefore, the PIM kinase inhibitors of the present invention can be used to prepare drugs to treat PIM kinase mediated diseases such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection, thus have great clinical value. Also provided are preparation methods for the compounds represented by Formula 1.

  本发明提供了一种PIM激酶抑制剂--通式结构式由式I代表的化合物。还提供了由式 1 表示的异构体、非对映异构体、对映体、同系物和药学上可接受的盐。式 I 中的 E、J1、J2、Q、X、Y、Z 和 m 在权利要求 1 中定义。PIM生化试验表明，本发明的化合物（1-63）能显著抑制PIM-1激酶的活性。在 3 微摩尔浓度下，本发明化合物对 PIM-2 和 PIM-3 活性的抑制率高达 100%。因此，本发明的 PIM 激酶抑制剂可用于制备治疗 PIM 激酶介导的疾病（如癌症、自身免疫性疾病、过敏反应或器官移植排异反应等）的药物，具有极大的临床价值。本发明还提供了式 1 所代表化合物的制备方法。
• [EN] PIM KINASE INHIBITOR AND PREPARATION METHOD AND USE IN MEDICINAL MANUFACTURE THEREOF<br/>[FR] INHIBITEUR DE PIM KINASE ET PROCÉDÉ DE PRÉPARATION ET UTILISATION DANS LA FABRICATION MÉDICINALE DE CELUI-CI
  申请人：JIKAI BIOSCIENCES INC

  公开号：WO2013020370A1

  公开（公告）日：2013-02-14

  本发明提供了一种式（I）所示的PIM激酶抑制剂，其中E，J，Q，X，Y，Z，m如权利要求1所定义。本发明的PIM激酶抑制剂用于制备治疗或预防癌症、自身免疫性疾病、过敏性反应疾病、动脉粥样硬化或抗器官移植排斥反应的药物。
• PIM KINASE INHIBITORS AND PREPARATION METHOD AND USE IN MEDICINAL MANUFACTURE THEREOF
  申请人：Jikai Biosciences Inc.

  公开号：EP2743271B1

  公开（公告）日：2017-05-31
• US9090594B2
  申请人：——

  公开号：US9090594B2

  公开（公告）日：2015-07-28