(E)-3-(2-(2,7-diazaspiro[3.5]nonan-2-yl)ethyl)-6-(3-oxo-3-(4-(thiophen-2-ylmethyl)-5,6-dihydropyridin-1(2H)-yl)prop-1-en-1-yl)-3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-one2,2,2-trifluoroacetate | 1441353-75-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 氮杂螺癸烷衍生物
• 英文名称: (E)-3-(2-(2,7-diazaspiro[3.5]nonan-2-yl)ethyl)-6-(3-oxo-3-(4-(thiophen-2-ylmethyl)-5,6-dihydropyridin-1(2H)-yl)prop-1-en-1-yl)-3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-one2,2,2-trifluoroacetate
• 英文别名: 3-[2-(2,7-diazaspiro[3.5]nonan-2-yl)ethyl]-6-[(E)-3-oxo-3-[4-(thiophen-2-ylmethyl)-3,6-dihydro-2H-pyridin-1-yl]prop-1-enyl]-1,4-dihydropyrido[2,3-d]pyrimidin-2-one;2,2,2-trifluoroacetic acid
• CAS: 1441353-75-8
• 化学式: C₂HF₃O₂*C₂₉H₃₆N₆O₂S
• 分子量: 646.734
• InChiKey: GNSYWJLGKLGIGN-BJILWQEISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.22
• 重原子数：
  45
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  146
• 氢给体数：
  3
• 氢受体数：
  11

文献信息

• [EN] SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS<br/>[FR] DÉRIVÉS DE PYRIDINE SUBSTITUÉS EN TANT QU'INHIBITEURS DE FABI
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2013080222A1

  公开（公告）日：2013-06-06

  The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula(I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了式(I)的取代吡啶衍生物，其可能作为抗细菌剂，特别是FabI抑制剂，具有治疗用途。式(I)中，R1至R5和L具有说明书中给出的含义，以及用于治疗和预防疾病或失调的药用可接受盐，特别是在有优势使用抗细菌剂，尤其是FabI抑制剂的疾病或失调中的用途。本发明还提供了合成和管理FabI抑制剂化合物的方法。本发明还提供了包含至少一种FabI抑制剂化合物和用于其的药用可接受载体、稀释剂或助剂的药物制剂。
• SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS
  申请人：Aurigene Discovery Technologies Limited

  公开号：US20140336153A1

  公开（公告）日：2014-11-13

  The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particularly FabI inhibitors. Formula (I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明提供了式（I）的取代吡啶衍生物，其可作为抗菌剂，更特别地是FabI抑制剂，具有治疗上的用途。式（I）中，R1至R5和L具有规范中所给出的含义，以及其药学上可接受的盐，在特定的疾病或疾病预防治疗中有用，特别是在有优势的抗菌剂，更特别地是FabI抑制剂的疾病或疾病预防治疗中的使用。本发明还提供了合成和给予FabI抑制剂化合物的方法。本发明还提供了包含至少一种FabI抑制剂化合物的药物配方，以及与其药学上可接受的载体、稀释剂或赋形剂一起使用的药物配方。
• US9062002B2
  申请人：——

  公开号：US9062002B2

  公开（公告）日：2015-06-23