tert-butyl 4-hydroxy-4-(1-methyl-1H-imidazol-2-yl)piperidine-1-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: tert-butyl 4-hydroxy-4-(1-methyl-1H-imidazol-2-yl)piperidine-1-carboxylate
• 英文别名: tert-butyl 4-hydroxy-4-(1-methylimidazol-2-yl)piperidine-1-carboxylate
• 化学式: C₁₄H₂₃N₃O₃
• 分子量: 281.355
• InChiKey: XPCSGLOCNMXROR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  67.6
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  tert-butyl 4-hydroxy-4-(1-methyl-1H-imidazol-2-yl)piperidine-1-carboxylate 在 盐酸 、 sodium hydride 作用下， 以 1,4-二氧六环 、 N,N-二甲基甲酰胺 、 mineral oil 为溶剂， 反应 11.0h， 生成 4-methoxy-4-(1-methyl-1H-imidazol-2-yl)piperidine
  参考文献：
  名称：

  [EN] BICYCLIC AZA COMPOUNDS AS MUSCARINIC M1 RECEPTOR AND/OR M4 RECEPTOR AGONISTS
  [FR] COMPOSÉS AZA BICYCLIQUES EN TANT QU'AGONISTES DU RÉCEPTEUR MUSCARINIQUE M1.

  摘要：

  公开号：

  WO2015118342A8
• 作为产物：
  描述：

  N-叔丁氧羰基-4-哌啶酮 在 正丁基锂 作用下， 以 四氢呋喃 为溶剂， 反应 12.0h， 以84%的产率得到tert-butyl 4-hydroxy-4-(1-methyl-1H-imidazol-2-yl)piperidine-1-carboxylate
  参考文献：
  名称：

  Acetamides and benzamides that are useful in treating sexual dysfunction

  摘要：

  本发明涉及使用式（I）的化合物治疗性功能障碍，以及含有式（I）化合物的组合物用于治疗性功能障碍。

  公开号：

  US20030229094A1

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] PIPERIDIN-1 -YL AND AZEPIN-1 -YL CARBOXYLATES AS MUSCARINIC M4 RECEPTOR AGONISTS<br/>[FR] CARBOXYLATES DE PIPÉRIDIN-1-YLE ET D'AZÉPIN-1-YLE À TITRE D'AGONISTES DU RÉCEPTEUR MUSCARINIQUE M4
  申请人：TAKEDA PHARMACEUTICAL

  公开号：WO2014122474A1

  公开（公告）日：2014-08-14

  The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R2 and R3 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimer's disease and various cognitive disorders as well as in the treatment or alleviation of pain.

  本发明提供了式（I）的肌氨酸M4受体激动剂及其药用盐，其中m、n、p、q、R、R2和R3如规范中所定义，其制备方法，含有它们的药物组合物以及它们在治疗精神分裂症、阿尔茨海默病和各种认知障碍以及治疗或缓解疼痛中的用途。
• [EN] E-FLUORO-4-(PYRIDIN-2-YL)-PIPERIDINE-1-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) FOR THE TREATMENT OF PAIN<br/>[FR] DERIVES DE 4-FLUORO-4-(PYRIDIN-2-YL)-PIPERIDINE-1-CARBOXAMIDE ET COMPOSES ASSOCIES MODULANT LA FONCTION DU RECEPTEUR VANILLOIDE (VR1) POUR LE TRAITEMENT DE LA DOULEUR
  申请人：MERCK SHARP & DOHME

  公开号：WO2005051390A1

  公开（公告）日：2005-06-09

  Compounds of formula (I): wherein: A1 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; A2 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from 0, N and S, at most one heteroatom being O or S; L is a bond or C1-6alkylene; R1 and R2 independently chosen from hydrogen and C1-6alkyl or Rl and R2 may, together, form a methylene or ethylene bridge; W is halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; X is O, S or NR3 or X, together with the atom to which it is attached, and Y, form an unsaturated five-membered ring together with A2; Y is a bond, C1-4alkylene, NH or NH(CH2)1-3; or a pharmaceutically acceptable salt thereof; other substituents are defined in claim 1; which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).

  化合物的结构式（I）：其中：A1是苯基，含有一个、两个或三个氮原子的六元芳香杂环，或者含有最多四个来自O、N和S的杂原子的五元芳香杂环，其中最多有一个杂原子是O或S；A2是苯基，含有一个、两个或三个氮原子的六元芳香杂环，或者含有最多四个来自0、N和S的杂原子的五元芳香杂环，其中最多有一个杂原子是O或S；L是键或C1-6烷基；R1和R2独立选择自氢和C1-6烷基，或者R1和R2可以一起形成亚甲基或乙烯桥；W是卤素，C1-6烷基，卤代C1-6烷基，C1-6烷氧基或卤代C1-6烷氧基；X是O、S或NR3或X与其连接的原子和Y一起形成与A2一起的不饱和五元环；Y是键，C1-4烷基，NH或NH(CH2)1-3；或其药学上可接受的盐；其他取代基在权利要求1中定义；这些化合物可用作治疗化合物，特别是在疼痛治疗和通过调节vanilloid-1受体（VR1）功能改善的其他病症的治疗中。
• E-fluoro-4-(pyridin-2-yl)-piperidine-1-carboxamide derivatives and related compounds which modulate the function of the vanilloid-1 receptor (vr1) for the treatment of pain
  申请人：Bayliss Tracy

  公开号：US20070135423A1

  公开（公告）日：2007-06-14

  Compounds of formula (I): wherein: A 1 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; A 2 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; L is a bond or C 1-6 alkylene; R 1 and R 2 independently chosen from hydrogen and C 1-6 alkyl or R 1 and R 2 may, together, form a methylene or ethylene bridge; W is halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; X is O, S or NR 3 or X, together with the atom to which it is attached, and Y, form an unsaturated five-membered ring together with A 2 ; Y is a bond, C 1-4 alkylene, NH or NH(CH 2 ) 1-3 ; or a pharmaceutically acceptable salt thereof; other substituents are defined in claim 1 ; which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).

  式(I)的化合物：其中：A1是苯基，含有一个、两个或三个氮原子的六元芳杂环，或含有最多四个来自O、N和S的杂原子的五元芳杂环，至多一个杂原子为O或S；A2是苯基，含有一个、两个或三个氮原子的六元芳杂环，或含有最多四个来自O、N和S的杂原子的五元芳杂环，至多一个杂原子为O或S；L是键或C1-6烷基；R1和R2独立选择自氢和C1-6烷基，或R1和R2可共同形成亚甲基或乙烯基桥；W是卤素、C1-6烷基、卤代C1-6烷基、C1-6烷氧基或卤代C1-6烷氧基；X是O、S或NR3或X与其所连接的原子和Y共同形成一个不饱和的五元环，并与A2一起；Y是键、C1-4烷基、NH或NH(CH2)1-3；或其药学上可接受的盐；其他取代基在权利要求书中有定义；它们在治疗疼痛和其他通过调节vanilloid-1受体（VR1）功能改善的疾病中特别有用。
• CYCLIC PEPTIDE COMPOUNDS
  申请人：Yamanaka Toshio

  公开号：US20100120672A1

  公开（公告）日：2010-05-13

  The present invention relates to a new cyclic peptide compound or a salt thereof, which has anti-hepatitis C virus activities based on inhibitory activity against the RNA replication of hepatitis C virus replicon, a process for preparation thereof, a pharmaceutical composition comprising the same, and a method for prophylactic and/or therapeutic treatment of hepatitis C in a human being or an animal.

  本发明涉及一种新的环肽化合物或其盐，其基于对丙型肝炎病毒复制体RNA复制的抑制活性具有抗丙型肝炎病毒活性，以及其制备方法，包含该化合物的制药组合物，以及用于预防和/或治疗人类或动物丙型肝炎的方法。