2-Methyl-4-(piperidin-4-yloxy)pyridine | 1400692-05-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-Methyl-4-(piperidin-4-yloxy)pyridine
• 英文别名: 2-methyl-4-piperidin-4-yloxypyridine
• CAS: 1400692-05-8
• 化学式: C₁₁H₁₆N₂O
• 分子量: 192.261
• InChiKey: VYDBQUILPMNJAH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.3
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.55
• 拓扑面积：
  34.2
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-Methyl-4-(piperidin-4-yloxy)pyridine 以 二氯甲烷 、 异丙醇 为溶剂， 反应 17.0h， 生成 2-Methyl-5-[4-(2-methylpyridin-4-yl)oxypiperidin-1-yl]-1,2,4-triazol-3-amine
  参考文献：
  名称：

  [EN] NOVEL SUBSTITUTED TRIAZOLYL PIPERAZINE AND TRIAZOLYL PIPERIDINE DERIVATIVES AS GAMMA SECRETASE MODULATORS
  [FR] NOUVEAUX DÉRIVÉS DE TRIAZOLYLPIPÉRAZINE ET TRIAZOLYLPIPÉRIDINE SUBSTITUÉS À TITRE DE MODULATEURS DE GAMMA SÉCRÉTASES

  摘要：

  本发明涉及一种新型的Formula(I)中的取代三唑基哌嗪和三唑基哌啶衍生物，其中R1、R2、R3、R4a、R4b、R5、X、Y1、Y2、L1和L2的含义如权利要求中所定义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新型化合物的方法，包括将该化合物作为活性成分的药物组合物以及将该化合物用作药物的用途。

  公开号：

  WO2012126984A1
• 作为产物：
  描述：

  4-氯-2-甲基吡啶 在 盐酸 、 sodium t-butanolate 作用下， 以 二甲基亚砜 、 异丙醇 为溶剂， 反应 49.5h， 生成 2-Methyl-4-(piperidin-4-yloxy)pyridine
  参考文献：
  名称：

  [EN] NOVEL SUBSTITUTED TRIAZOLYL PIPERAZINE AND TRIAZOLYL PIPERIDINE DERIVATIVES AS GAMMA SECRETASE MODULATORS
  [FR] NOUVEAUX DÉRIVÉS DE TRIAZOLYLPIPÉRAZINE ET TRIAZOLYLPIPÉRIDINE SUBSTITUÉS À TITRE DE MODULATEURS DE GAMMA SÉCRÉTASES

  摘要：

  本发明涉及一种新型的Formula(I)中的取代三唑基哌嗪和三唑基哌啶衍生物，其中R1、R2、R3、R4a、R4b、R5、X、Y1、Y2、L1和L2的含义如权利要求中所定义。根据本发明的化合物可用作γ-分泌酶调节剂。本发明还涉及制备这种新型化合物的方法，包括将该化合物作为活性成分的药物组合物以及将该化合物用作药物的用途。

  公开号：

  WO2012126984A1

文献信息

• [EN] OGA INHIBITOR COMPOUNDS<br/>[FR] COMPOSÉS INHIBITEURS D'OGA
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2019243530A1

  公开（公告）日：2019-12-26

  The present invention relates to O-GIcNAc hydrolase (OGA) inhibitors having the structure shown in formula (I). The invention is also directed to pharmaceutical compositions comprising such compounds to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C90RF72 mutations. wherein RB is an aromatic heterobicyclic radical selected from the group consisting of (b-1) to (b-6).

  本发明涉及具有式(I)所示结构的O-GIcNAc水解酶（OGA）抑制剂。该发明还涉及包含这种化合物的药物组合物、制备这种化合物和组合物的方法，以及利用这种化合物和组合物预防和治疗抑制OGA有益的疾病，如tau病变，特别是阿尔茨海默病或进行性上核性麻痹；以及伴有tau病理的神经退行性疾病，特别是由C90RF72突变引起的肌萎缩侧索硬化或额颞叶痴呆症。其中RB是从（b-1）到（b-6）组成的芳香杂双环基团。
• NOVEL SUBSTITUTED TRIAZOLYL PIPERAZINE AND TRIAZOLYL PIPERIDINE DERIVATIVES AS GAMMA SECRETASE MODULATORS
  申请人：Biscoff Francois Paul

  公开号：US20140011816A1

  公开（公告）日：2014-01-09

  The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) wherein R 1 , R 2 , R 3 , R 4a , R 4b , R 5 , X, Y 1 , Y 2 , L 1 , and L 2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
• 1,2,4-Triazolo [4,3-A] Pyridine Derivatives And Their Use For The Treatment Of Prevention Of Neurological And Psychiatric Disorders
  申请人：JANSSEN PHARMACEUTICALS, INC.

  公开号：US20170333426A1

  公开（公告）日：2017-11-23

  The present invention relates to methods of treating various central nervous system disorders using novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.
• OGA INHIBITOR COMPOUNDS
  申请人：Janssen Pharmaceutica NV

  公开号：US20210122763A1

  公开（公告）日：2021-04-29

  The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.
• US8987276B2
  申请人：——

  公开号：US8987276B2

  公开（公告）日：2015-03-24