(S)-2-amino-N-(2-morpholin-4-yl-ethyl)-2-phenyl-acetamide

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: (S)-2-amino-N-(2-morpholin-4-yl-ethyl)-2-phenyl-acetamide
• 英文别名: (2S)-2-amino-N-(2-morpholin-4-ylethyl)-2-phenylacetamide
• 化学式: C₁₄H₂₁N₃O₂
• 分子量: 263.34
• InChiKey: BPWQWFIOURQEFB-ZDUSSCGKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  19
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  67.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  苯乙酸 、 (S)-2-amino-N-(2-morpholin-4-yl-ethyl)-2-phenyl-acetamide 在 N,N-二异丙基乙胺 、 3-(二乙氧基邻酰氧基)-1,2,3-苯并三嗪-4-酮 作用下， 以 二氯甲烷 为溶剂， 反应 16.08h， 以63%的产率得到(S)-N-(2-morpholin-4-yl-ethyl)-2-phenyl-2-phenylacetylamino-acetamide
  参考文献：
  名称：

  Design and synthesis of potential dual NK1/NK3 receptor antagonists

  摘要：

  The tachykinin NK1 and NK3 receptors are a novel drug target for schizophrenia in order to treat not only the positive and cognitive symptoms, but also the associated co-morbid depression and sleep disturbances associated with the disease. A novel class of peptidomimetic derivatives based on a versatile phenylglycine central core was synthesized and tested in vitro as dual NK1/NK3 receptor antagonists. From this series emerged compounds with good NK1 receptor affinity, although only modest dual NK1/NK3 receptor affinity was observed with one of these analogs. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2013.12.033
• 作为产物：
  描述：

  Cbz-L-苯甘氨酸 在 10 wt% Pd(OH)2 on carbon 、 氢气 、 N,N-二异丙基乙胺 、 3-(二乙氧基邻酰氧基)-1,2,3-苯并三嗪-4-酮 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 36.08h， 生成 (S)-2-amino-N-(2-morpholin-4-yl-ethyl)-2-phenyl-acetamide
  参考文献：
  名称：

  Design and synthesis of potential dual NK1/NK3 receptor antagonists

  摘要：

  The tachykinin NK1 and NK3 receptors are a novel drug target for schizophrenia in order to treat not only the positive and cognitive symptoms, but also the associated co-morbid depression and sleep disturbances associated with the disease. A novel class of peptidomimetic derivatives based on a versatile phenylglycine central core was synthesized and tested in vitro as dual NK1/NK3 receptor antagonists. From this series emerged compounds with good NK1 receptor affinity, although only modest dual NK1/NK3 receptor affinity was observed with one of these analogs. (C) 2013 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2013.12.033

文献信息

• [EN] METHODS AND COMPOUNDS FOR TREATING ALCOHOL USE DISORDERS AND ASSOCIATED DISEASES<br/>[FR] PROCÉDÉS ET COMPOSÉS POUR LE TRAITEMENT DE TROUBLES D'UTILISATION D'ALCOOL ET DE MALADIES ASSOCIÉES
  申请人：PHARMATROPHIX INC

  公开号：WO2018039641A1

  公开（公告）日：2018-03-01

  Methods and compounds for treating alcohol use disorder and associated diseases. Included is the administering to a subject in need there of an effective amount of a compound having a modulating effect on p75NTR.

  治疗酒精使用障碍和相关疾病的方法和化合物。包括向需要的受试者施用对p75NTR具有调节作用的化合物的有效量。
• NEUROTROPHIN MIMETICS AND USES THEREOF
  申请人：Longo Frank M.

  公开号：US20110230479A1

  公开（公告）日：2011-09-22

  The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.

  本申请涉及一种新型神经营养因子类似物化合物。该申请还公开了通过给哺乳动物施用有效量的这种化合物来治疗与p75表达相关的疾病，例如p75表达细胞的降解或功能障碍。
• DEUTERATED COMPOUNDS USEFUL FOR TREATING NEURODEGENERATIVE DISEASES
  申请人：PharmatrophiX, Inc.

  公开号：US20160229823A1

  公开（公告）日：2016-08-11

  The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.

  本申请涉及新型神经营养因子类似物的氘代化合物。该申请还揭示了通过给哺乳动物以有效量的这种氘代化合物来治疗涉及表达p75的细胞降解或功能障碍的疾病。
• METHODS AND COMPOUNDS FOR TREATING ALCOHOL USE DISORDERS AND ASSOCIATED DISEASES
  申请人：PHARMATROPHIX, INC.

  公开号：US20190231787A1

  公开（公告）日：2019-08-01

  Methods and compounds for treating alcohol use disorder and associated diseases. Included is the administering to a subject in need there of an effective amount of a compound having a modulating effect on p75NTR.
• US9464066B2
  申请人：——

  公开号：US9464066B2

  公开（公告）日：2016-10-11