1-Ethyl-4-phenoxypiperidine | 1569020-51-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 1-Ethyl-4-phenoxypiperidine
• CAS: 1569020-51-4
• 化学式: C₁₃H₁₉NO
• 分子量: 205.3
• InChiKey: LEVVTDQPVLZUSK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  15
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.54
• 拓扑面积：
  12.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3-氧杂二环[3.1.0]己烷-2,4-二酮 、 1-Ethyl-4-phenoxypiperidine 在 aluminum (III) chloride 作用下， 以 1,2-二氯乙烷 为溶剂， 生成
  参考文献：
  名称：

  Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): Histamine H3 receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity

  摘要：

  A series of fused cyclopropyl-4,5-dihydropyridazin-3-one (3,4-diaza-bicyclo[4.1.0] hept-4-en-2-one) phenoxypiperidine analogs was designed and synthesized, leading to the identification of (1R, 6S)-5[ 4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0] hept-4-en-2-one (R, S-4a) as a secondgeneration pyridazin-3-one H3R antagonist. Compound R, S-4a was a potent H3R functional antagonist in vivo in the rat dipsogenia model, demonstrated potent wake activity in the rat EEG/EMG model, and enhanced short-term memory in the rat social recognition memory model at doses as low as 0.03-0.3 mg/kg po. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.01.061
• 作为产物：
  描述：

  4-Phenoxypiperidine-1-carboxylic acid 、 丙醛 在 sodium cyanoborohydride 作用下， 以 甲醇 、 溶剂黄146 、 N,N-二甲基甲酰胺 为溶剂， 生成 1-Ethyl-4-phenoxypiperidine
  参考文献：
  名称：

  Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): Histamine H3 receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity

  摘要：

  A series of fused cyclopropyl-4,5-dihydropyridazin-3-one (3,4-diaza-bicyclo[4.1.0] hept-4-en-2-one) phenoxypiperidine analogs was designed and synthesized, leading to the identification of (1R, 6S)-5[ 4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0] hept-4-en-2-one (R, S-4a) as a secondgeneration pyridazin-3-one H3R antagonist. Compound R, S-4a was a potent H3R functional antagonist in vivo in the rat dipsogenia model, demonstrated potent wake activity in the rat EEG/EMG model, and enhanced short-term memory in the rat social recognition memory model at doses as low as 0.03-0.3 mg/kg po. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.01.061

文献信息

• ARYLPIPERIDINYL AND ARYLPYRROLIDINYL MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS
  申请人：Niu Deqiang

  公开号：US20080279821A1

  公开（公告）日：2008-11-13

  The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

  本发明涉及具有以下结构的化合物I，或其药用可接受的盐、酯或前药：这些化合物抑制丝氨酸蛋白酶活性，特别是乙型肝炎病毒（HCV）NS3-NS4A蛋白酶的活性。因此，本发明的化合物干扰乙型肝炎病毒的生命周期，并且还可用作抗病毒剂。本发明还涉及含有上述化合物的制药组合物，用于治疗患有HCV感染的受试者。该发明还涉及通过给受试者施用含有本发明化合物的制药组合物来治疗受试者的HCV感染的方法。
• N-Substituted-Heterocycloalkyloxybenzamide Compounds and Methods of Use
  申请人：Singh Rajinder

  公开号：US20110306767A1

  公开（公告）日：2011-12-15

  The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R 1 , R 2 , R 3 , R 4 , T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

  本发明提供了N-取代-杂环烷氧基苯甲酰胺化合物，以及其制备的药物组合物和使用方法。本发明的一个实施例是一种具有以下结构的化合物，在该结构中，R1、R2、R3、R4、T、n、w和x如本文所述。在本发明的某些实施例中，本发明的化合物可以激活AMPK通路，并可用于治疗代谢相关的疾病和病状。
• Substituted pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
  申请人：Array BioPharma, Inc.

  公开号：US10172845B2

  公开（公告）日：2019-01-08

  Provided herein are compounds of the Formula I: or pharmaceutically acceptable salt or solvate thereof, wherein A, B, X1, X2, X3, X4, Ring D, E, Ra, Rb, n and m have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including RET-associated diseases and disorders.

  本文提供的是式 I 的化合物： 或其药学上可接受的盐或溶液，其中 A、B、X1、X2、X3、X4、环 D、E、Ra、Rb、n 和 m 具有说明书中给出的含义，它们是 RET 激酶的抑制剂，可用于治疗和预防可用 RET 激酶抑制剂治疗的疾病，包括 RET 相关疾病和失调。
• Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors
  申请人：Array BioPharma, Inc.

  公开号：US10174027B2

  公开（公告）日：2019-01-08

  Provided herein are compounds of the General Formula I: and stereoisomers and pharmaceutically acceptable salts or solvates thereof, in which A, B, D, E, X1, X2, X3 and X4 have the meanings given in the specification, which are inhibitors of RET kinase and are useful in the treatment and prevention of diseases which can be treated with a RET kinase inhibitor, including diseases or disorders mediated by a RET kinase.

  本文提供的是通式 I 的化合物： 及其立体异构体和药学上可接受的盐或溶液，其中 A、B、D、E、X1、X2、X3 和 X4 具有说明书中给出的含义，它们是 RET 激酶的抑制剂，可用于治疗和预防可以用 RET 激酶抑制剂治疗的疾病，包括由 RET 激酶介导的疾病或紊乱。
• ARYLPIPERIDINYL AND ARYLPYRROLIDINYL TRIPEPTIDE HEPATITIS C SERINE PROTEASE INHIBITORS
  申请人：Niu Deqiang

  公开号：US20080317712A1

  公开（公告）日：2008-12-25

  The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.