4-(2-氟苯氧基)哌啶(HCL) | 3413-29-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 中文名称: 4-(2-氟苯氧基)哌啶(HCL)
• 英文名称: 4-(2-fluorophenoxy)piperidine hydrochloride
• 英文别名: 4-(2-fluoro-phenoxy)-piperidine hydrochloride；4-(2-fluorophenoxy)piperidine;hydrochloride
• CAS: 3413-29-4
• 化学式: C₁₁H₁₄FNO*ClH
• 分子量: 231.698
• InChiKey: LPYCXDRKDWMHGU-UHFFFAOYSA-N

物化性质

• 熔点：
  180-181 °C

计算性质

• 辛醇/水分配系数(LogP)：
  2.38
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  21.3
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  6-chloro-N-methylpyridazine-3-carboxamide 、 4-(2-氟苯氧基)哌啶(HCL) 在 三乙胺 作用下， 以 乙腈 为溶剂， 反应 0.33h， 以61%的产率得到6-[4-(2-fluorophenoxy)piperidin-1-yl]-N-methylpyridazine-3-carboxamide
  参考文献：
  名称：

  Discovery of Potent, Selective, Orally Bioavailable Stearoyl-CoA Desaturase 1 Inhibitors

  摘要：

  Stearoyl-CoA desaturase 1 (SCD1) catalyzes the committed step in the biosynthesis of monounsaturated fatty acids from saturated, long-chain fatty acids. Studies with SCD1 knockout mice have established that these animals are lean and protected from leptin deficiency-induced and diet-induced obesity, with greater whole body insulin sensitivity than wild-type animals. In this work, we have discovered a series of potent, selective, orally bioavailable SCD1 inhibitors based on a known pyridazine carboxamide template. The representative lead inhibitor 28c also demonstrates excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells.

  DOI：

  10.1021/jm070219p
• 作为产物：
  描述：

  2-氟苯酚 在 盐酸 、 偶氮二甲酸二叔丁酯 、 三苯基膦 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 反应 2.5h， 生成 4-(2-氟苯氧基)哌啶(HCL)
  参考文献：
  名称：

  Discovery of Potent, Selective, Orally Bioavailable Stearoyl-CoA Desaturase 1 Inhibitors

  摘要：

  Stearoyl-CoA desaturase 1 (SCD1) catalyzes the committed step in the biosynthesis of monounsaturated fatty acids from saturated, long-chain fatty acids. Studies with SCD1 knockout mice have established that these animals are lean and protected from leptin deficiency-induced and diet-induced obesity, with greater whole body insulin sensitivity than wild-type animals. In this work, we have discovered a series of potent, selective, orally bioavailable SCD1 inhibitors based on a known pyridazine carboxamide template. The representative lead inhibitor 28c also demonstrates excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells.

  DOI：

  10.1021/jm070219p

文献信息

• Pyridinyl Amides for the Treatment of CNS and Metabolic Disorders
  申请人：Collantes Elizabeth Martha

  公开号：US20090197859A1

  公开（公告）日：2009-08-06

  The present invention relates to novel pyridinyl derivatives of Formula wherein Y, Z, L, R 1 through R 11 , n, m, p, q, t are as defined herein, that are 5-HT receptor ligands, particularly the 5-HT6 subtype, and as such are useful for treating diseases wherein modulation of 5-HT activity is desired. The present invention relates to novel pyridinyl derivatives including their pharmaceutically acceptable salts. The invention also relates to processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing and the uses of such compounds in treating diseases of the central nervous system such as schizophrenia.

  本发明涉及一种新颖的吡啶基衍生物，其化学式如下所示：其中Y、Z、L、R1至R11、n、m、p、q、t的定义如本文所述，它们是5-HT受体配体，特别是5-HT6亚型，因此可用于治疗需要调节5-HT活性的疾病。本发明涉及包括其药用盐在内的新型吡啶基衍生物。该发明还涉及用于制备、制备中间体、含有这些化合物的药物组合物以及在治疗中枢神经系统疾病如精神分裂症中使用这些化合物的过程。
• SULFONYL PIPERIDINE DERIVATIVES AND THEIR USE FOR TREATING PROKINETICIN MEDIATED DISEASES
  申请人：TAKEDA PHARMACEUTICAL COMPANY LIMITED

  公开号：US20150111922A1

  公开（公告）日：2015-04-23

  The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) in which m, n, W, X, Y, Z, R 1 , R 2 , R 3 and R 4 are as defined in the specification, for use in the treatment or prevention of a diseases o conition mediated by a prokineticin, such as psychiatric and neurological conditions.

  本发明提供了公式（I）的化合物及其药学上可接受的盐：（I）其中m、n、W、X、Y、Z、R1、R2、R3和R4如规范中所定义，用于治疗或预防由前动力素介导的疾病或情况，例如精神和神经疾病。
• THERAPEUTIC COMPOUNDS
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US20130324576A1

  公开（公告）日：2013-12-05

  The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which m, n, W, X, Y, Z, R, R 1 , R 2 , R 3 and R 4 are as defined in the specification, for use in therapy.

  本发明提供公式（I）的化合物及其药学上可接受的盐，其中m、n、W、X、Y、Z、R、R1、R2、R3和R4在规范中定义，用于治疗。
• SUBSTITUTED N-[2-(4-PHENOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE AND N-[2-(4-BENZYLOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE DERIVATIVES AND THEIR USE AS P2X7 RECEPTOR ANTAGONIST
  申请人：AXXAM S.p.A.

  公开号：EP3290416A1

  公开（公告）日：2018-03-07

  The present invention relates to novel substituted phenoxy- and benzyloxy-piperidine compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.

  本发明涉及具有 P2X7 受体（P2X7）拮抗特性的式 (I) 的新型取代苯氧基和苄氧基哌啶化合物、包含这些化合物的药物组合物、制备这些化合物的化学工艺及其在治疗或预防动物，特别是人类与 P2X7 受体活性相关疾病中的用途。
• Substituted N-[2-(4-phenoxypiperidin-1-yl)-2-(1,3-thiazol-5-yl)ethyl]benzamide and N-[2-(4-benzyloxypiperidin-1-yl)-2-(1,3-thiazol-5-yl)ethyl]benzamide derivatives P2X7 receptor antagonists
  申请人：Axxam S.P.A.

  公开号：US10669267B2

  公开（公告）日：2020-06-02

  The present invention relates to novel substituted phenoxy- and benzyloxy-piperidine compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.

  本发明涉及具有 P2X7 受体（P2X7）拮抗特性的式 (I) 的新型取代苯氧基和苄氧基哌啶化合物、包含这些化合物的药物组合物、制备这些化合物的化学工艺及其在治疗或预防动物，特别是人类与 P2X7 受体活性相关疾病中的用途。