4-(thiophen-2-ylmethyl)pyridine | 130406-96-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 4-(thiophen-2-ylmethyl)pyridine
• CAS: 130406-96-1
• 化学式: C₁₀H₉NS
• 分子量: 175.254
• InChiKey: VPIPCTYBGGKPAO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.5
• 重原子数：
  12
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  41.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-(thiophen-2-ylmethyl)pyridine 生成 1-methyl-4-(thiophen-2-ylmethyl)-3,6-dihydro-2H-pyridine;hydrochloride
  参考文献：
  名称：

  EFANGE, S. M. N.;MICHELSON, R. H.;REMMEL, R. P.;BOUDREAU, R. J.;DUTTA, A.+, J. MED. CHEM., 33,(1990) N2, C. 3133-3138

  摘要：

  DOI：
• 作为产物：
  描述：

  pyridin-4-yl(thiophen-2-yl)methanol 在 锌 resultant residue 、 水 、 disodium;carbonate 、 乙醚 、 Brine 、 Sodium sulfate-III 作用下， 以 溶剂黄146 为溶剂， 反应 16.0h， 以to get the desired compound as an oily liquid (3.2 g, 87%)的产率得到4-(thiophen-2-ylmethyl)pyridine
  参考文献：
  名称：

  Tetrahydropyridine derivatives as FabI inhibitors

  摘要：

  本发明涉及公式（1）的四氢吡啶衍生物，可作为抗菌剂在治疗和预防疾病或紊乱中具有治疗作用，特别是作为FabI抑制剂。其中X、Y、Z和“n”在规范中给出的含义相同，并且具有在抑制Enoyl-ACP还原酶酶（FabI）活性方面具有优势的疾病或紊乱的治疗用途。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抑制剂化合物和其药学上可接受的载体、稀释剂或辅料的制药配方。

  公开号：

  US09062075B2

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。
• [EN] TETRAHYDROPYRIDINE DERIVATIVES AS FabI INHIBITORS<br/>[FR] DÉRIVÉS DE TÉTRAHYDROPYRIDINE SERVANT D'INHIBITEURS DE FABI
  申请人：AURIGENE DISCOVERY TECH LTD

  公开号：WO2014195844A1

  公开（公告）日：2014-12-11

  The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and "n" have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers 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 in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明涉及式（1）的四氢吡啶衍生物，可作为抗菌剂，更具体地作为FabI抑制剂的治疗用途。其中X、Y、Z和“n”的含义与说明书中给出的含义相同，并且其药学上可接受的盐和立体异构体在治疗和预防疾病或紊乱方面具有用处，特别是在抑制烯酰-ACP还原酶酶（FabI）活性具有优势的疾病或紊乱的治疗中的应用。本发明还提供了合成和给药FabI抑制化合物的方法。本发明还提供了包含至少一种FabI抑制化合物以及药学上可接受的载体、稀释剂或赋形剂的药物制剂。
• p38 MAP kinase inhibitors
  申请人：——

  公开号：US20010044538A1

  公开（公告）日：2001-11-22

  The present invention relates to compounds of Formula (I) 1 that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

  本发明涉及公式（I）1的化合物，它们是p-38 MAP激酶抑制剂，包含它们的制药组合物，使用它们的方法，以及制备这些化合物的方法。
• p38 map kinase inhibitors
  申请人：——

  公开号：US20020013354A1

  公开（公告）日：2002-01-31

  The present invention relates to compounds of Formula (I) 1 that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

  本发明涉及一种式（I）的化合物，该化合物是p-38 MAP激酶抑制剂，包含它们的制药组合物，使用它们的方法以及制备这些化合物的方法。
• Tetrahydropyridine derivatives as FabI inhibitors
  申请人：Aurigene Discovery Technologies Limited

  公开号：US09062075B2

  公开（公告）日：2015-06-23

  The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers 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 in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

  本发明涉及公式（1）的四氢吡啶衍生物，可作为抗菌剂在治疗和预防疾病或紊乱中具有治疗作用，特别是作为FabI抑制剂。其中X、Y、Z和“n”在规范中给出的含义相同，并且具有在抑制Enoyl-ACP还原酶酶（FabI）活性方面具有优势的疾病或紊乱的治疗用途。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抑制剂化合物和其药学上可接受的载体、稀释剂或辅料的制药配方。