4-(2-hydroxyethyl)thiomorpholin-3-one | 88620-20-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻嗪类
• 英文名称: 4-(2-hydroxyethyl)thiomorpholin-3-one
• CAS: 88620-20-6
• 化学式: C₆H₁₁NO₂S
• 分子量: 161.225
• InChiKey: ZXAWOADUYSLPKF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  65.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4-(2-hydroxyethyl)thiomorpholin-3-one 在 hydrazine hydrate 、 三乙胺 、 三苯基膦 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 70.0h， 生成 2-((2-oxo-2-((2-(3-oxothiomorpholino)ethyl)amino)ethyl)thio)acetic acid
  参考文献：
  名称：

  WO2019183577A5

  摘要：

  公开号：

  WO2019183577A5
• 作为产物：
  描述：

  4-(2-((tert-butyldimethylsilyl)oxy)ethyl)thiomorpholin-3-one 在 盐酸 作用下， 以 甲醇 、 二氯甲烷 为溶剂， 反应 3.0h， 以87%的产率得到4-(2-hydroxyethyl)thiomorpholin-3-one
  参考文献：
  名称：

  WO2019183577A5

  摘要：

  公开号：

  WO2019183577A5

文献信息

• Humectant compositions containing thiamorpholinone or a derivative
  申请人：L'Oreal

  公开号：US04539320A1

  公开（公告）日：1985-09-03

  A composition for topical application to the skin comprises, in an appropriate cosmetic vehicle, as an active agent, a compound of the formula ##STR1## wherein, R.sub.1 and R.sub.2 represent hydrogen or lower alkyl; R.sub.3 represents hydrogen, alkyl containing 1-4 carbon atoms, mono- or polyhydroxyalkyl having 2-16 carbon atoms, carbamylalkyl, carboxyalkyl or alkoxycarbonylalkyl; R.sub.4 represents hydrogen or --COOR.sub.5 represents hydrogen, alkyl having 1-18 carbon atoms optionally interrupted by one or more hetero atoms, or mono- or polyhydroxyalkyl having 2-18 carbon atoms; and n is 0 or 1. This composition improves the elasticity and suppleness of the skin.

  一种用于皮肤局部应用的组合物，包括适当的化妆品载体和作为活性剂的公式化合物##STR1##其中，R.sub.1和R.sub.2代表氢或低碳基；R.sub.3代表氢，含1-4个碳原子的烷基，2-16个碳原子的单糖或多糖基烷基，氨基甲酸烷基，羧基烷基或烷氧羰基烷基；R.sub.4代表氢或--COOR.sub.5代表氢，含1-18个碳原子的烷基，可选地由一个或多个杂原子中断，或含2-18个碳原子的单糖或多糖基烷基；n为0或1。该组合物可改善皮肤的弹性和柔软度。
• Modulators of G-protein coupled receptors
  申请人：Carmot Therapeutics, Inc.

  公开号：US11535660B1

  公开（公告）日：2022-12-27

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize or partially agonize or antagonize) glucagon?like peptide?1 receptor (“GLP?1R”) and/or the gastric inhibitory polypeptide receptor (“GIPR”). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP?1R and/or GIPR activities is beneficial for the treatment or prevention of the underlying pathology and/or symptoms and/or progression of the disease, disorder, or condition. In some embodiments, the modulation results in an enhancement of (e.g., an increase in) existing levels (e.g., normal or below normal levels) of GLP?1R and/or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple)-arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.

  本公开的化学实体（如化合物或该化合物的药学上可接受的盐和/或水合物和/或原药）可调节（如激动或部分激动或拮抗）胰高血糖素样肽1受体（"GLP?1R"）和/或胃抑制多肽受体（"GIPR"）。这些化学实体是有用的，例如，用于治疗患有疾病、失调或病症的受试者（例如人类），在这种情况下，调节（例如，激动、部分激动或拮抗）GLP?1R 和/或 GIPR 的活性有利于治疗或预防潜在的病理和/或症状和/或疾病、失调或病症的进展。在一些实施方案中，调节的结果是增强（如增加）现有水平（如正常或低于正常水平）的GLP?1R和/或GIPR活性（如信号传导）。在某些实施方案中，本文所述的化学实体可进一步调节（如减弱、解除耦合）--相对于原生配体的信号转导。本公开还包括组合物以及使用和制造所述化学实体的其他方法。
• LANG, G.;MAIGNAN, J.;LEVEQUE, J. -L.;RASSENEUR, L.
  作者：LANG, G.、MAIGNAN, J.、LEVEQUE, J. -L.、RASSENEUR, L.

  DOI：——

  日期：——
• MODULATORS OF G-PROTEIN COUPLED RECEPTORS
  申请人：Carmot Therapeutics, Inc.

  公开号：EP3768294A1

  公开（公告）日：2021-01-27
• [EN] MODULATORS OF G-PROTEIN COUPLED RECEPTORS<br/>[FR] MODULATEURS DE RÉCEPTEURS COUPLÉS À LA PROTÉINE
  申请人：CARMOT THERAPEUTICS INC

  公开号：WO2019183577A1

  公开（公告）日：2019-09-26

  This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize or partially agonize or antagonize) glucagon?like peptide?1 receptor ("GLP?1R") and/or the gastric inhibitory polypeptide receptor ("GIPR"). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP?1R and/or GIPR activities is benficial for the treatment or prevention of the underlying pathology and/or symptoms and/or progression of the disease, disorder, or condition. In some embodiments, the modulation results in an enhancment of (e.g., an increase in) existing levels (e.g., normal or below normal levels) of GLP?1R and/or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple) -arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.