4-Phenoxy-1-propan-2-ylpiperidine | 1569020-56-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: 4-Phenoxy-1-propan-2-ylpiperidine
• CAS: 1569020-56-9
• 化学式: C₁₄H₂₁NO
• 分子量: 219.327
• InChiKey: AKWUANLCZYFFGZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  16
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.57
• 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：

  4-Phenoxy-1-propan-2-ylpiperidine 在 aluminum (III) chloride 作用下， 以 1,2-二氯乙烷 、 异丙醇 为溶剂， 生成 3-Methyl-5-[4-(1-propan-2-ylpiperidin-4-yl)oxyphenyl]-3,4-diazabicyclo[4.1.0]hept-4-en-2-one
  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 、 丙酮 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 4-Phenoxy-1-propan-2-ylpiperidine
  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

• [EN] TRIAZACYCLODODECANSULFONAMIDE ("TCD")-BASED PROTEIN SECRETION INHIBITORS<br/>[FR] INHIBITEURS DE SÉCRÉTION DE PROTÉINE À BASE DE TRIAZACYCLODODÉCANSULFONAMIDE ("TCD")
  申请人：KEZAR LIFE SCIENCES

  公开号：WO2019178510A1

  公开（公告）日：2019-09-19

  Provided herein are triazacyclododecansulfonamide ("TCD")-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.

  本文提供了基于三氮杂环十二烷磺酰胺（"TCD"）的蛋白质分泌抑制剂，例如Sec61的抑制剂，其制备方法，相关的药物组合物，以及使用它们的方法。例如，本文提供了符合Formula（I）的化合物及其药用盐和包括它们的组合物。本文披露的化合物可以用于治疗炎症和/或癌症等疾病。
• Gonadotropin Releasing Hormone Receptor Antagonist, Preparation Method Thereof And Pharmaceutical Composition Comprising The Same
  申请人：Kim Seon Mi

  公开号：US20130137661A1

  公开（公告）日：2013-05-30

  Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.

  披露了作为促性腺激素释放激素（“GnRH”）受体拮抗剂有用的化合物。
• IL-17 Ligands And Uses Thereof
  申请人：DICE Molecules SV LLC.

  公开号：US20200247785A1

  公开（公告）日：2020-08-06

  Provided herein are novel ligands and pharmaceutical compositions thereof which modulate IL-17A. Also provided are methods for preparing the IL-17A modulators. Such compounds may be useful in the treatment and/or prevention of, for example, inflammation, cancer or autoimmune disease.

  本文提供了新型配体及其药物组合物，可调节IL-17A。还提供了制备IL-17A调节剂的方法。这些化合物可能在治疗和/或预防炎症、癌症或自身免疫疾病等方面有用。
• NOVEL VANILLOID RECEPTOR LIGANDS AND USE THEREOF FOR THE PRODUCTION OF PHARMACEUTICAL PREPARATIONS
  申请人：Lee Jeewoo

  公开号：US20070105861A1

  公开（公告）日：2007-05-10

  The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.

  本发明涉及新型辣椒素受体配体，以及用于其生产的方法，含有这些化合物的药物制剂以及利用这些化合物生产药物制剂的用途。
• 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。