N-acetyl-3-(methylthio)propylamine | 54824-91-8

• 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: N-acetyl-3-(methylthio)propylamine
• 英文别名: 3-methylthiopropylamide；N-[3-(Methylsulfanyl)propyl]acetamide；N-(3-methylsulfanylpropyl)acetamide
• CAS: 54824-91-8
• 化学式: C₆H₁₃NOS
• 分子量: 147.241
• InChiKey: ASPAYHQEPZPDPA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  9
• 可旋转键数：
  4
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  54.4
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  1-(2-甲基-1,3-噻嗪烷-3-基)乙酮 、 甲醇 、 sodium t-butanolate 生成 N-acetyl-3-(methylthio)propylamine
  参考文献：
  名称：

  KIM, JHONG K.;SOUMA, YOSHIE;BEUTOW, NORMAN;IBBESON, CHRIS;CASERIO, MARJOR+, J. ORG. CHEM., 54,(1989) N, C. 1714-1720

  摘要：

  DOI：

文献信息

• DENDRITIC POLYETHYLENE GLYCOL DERIVATIVE, AND PREPARATION METHOD AND APPLICATION THEREOF
  申请人：JENKEM TECHNOLOGY CO., LTD. (TIANJIN)

  公开号：US20200131107A1

  公开（公告）日：2020-04-30

  The disclosure discloses a dendritic polyethylene glycol derivative and a preparation method and an application thereof. The dendritic polyethylene glycol derivative has a structure of formula (I), has multiple end functional groups, has a stronger water solubility in comparison with linear-chain polyethylene glycol, and can solve a problem of insufficient water solubility due to the increase of load when modifying an insoluble drug by the polyethylene glycol. The preparation method of the dendritic polyethylene glycol derivative provided by the disclosure has mild reaction conditions, is green and environmentally friendly, is low in cost, and is easy to implement industrialization.

  该披露揭示了一种树枝状聚乙二醇衍生物及其制备方法和应用。该树枝状聚乙二醇衍生物具有式（I）的结构，具有多个末端官能团，在与线性链聚乙二醇相比具有更强的水溶性，并且可以解决由于通过聚乙二醇对不溶性药物进行修饰时载荷增加而导致水溶性不足的问题。该披露提供的树枝状聚乙二醇衍生物的制备方法具有温和的反应条件，绿色环保，成本低，易于实现工业化。
• CETP activity inhibitors
  申请人：Japan Tobacco Inc.

  公开号：US20040229957A1

  公开（公告）日：2004-11-18

  The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): 1 wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X 1 , X 2 , X 3 , and X 4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO 2 —, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof. The compounds represented by the formula (I) can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity and, therefore, is expected to be useful as a new type of a preventive or therapeutic agent for atherosclerosis or hyperlipidemia.

  本发明提供了一种CETP活性抑制剂，其包括以下式（I）所表示的化合物作为活性成分：其中R表示直链或支链烷基；直链或支链烯基；低卤代烷基；取代或未取代的环烷基；取代或未取代的环烯基；取代或未取代的环烷基烷基；取代或未取代的芳基或取代或未取代的杂环基，X1，X2，X3和X4可以相同也可以不同，每个表示氢原子，卤原子，低烷基，低卤代烷基；低烷氧基；氰基；硝基；酰基；或芳基，Y表示—CO—或—SO2—，Z表示氢原子或硫醇保护基，或其前药化合物，药学上可接受的盐，或其水合物或溶剂化物。公式（I）所表示的化合物可以通过选择性抑制CETP活性来增加HDL并同时降低LDL，因此，预计它将作为一种新型的预防或治疗动脉硬化或高脂血症的药物而有用。
• CETP ACTIVITY INHIBITORS
  申请人：Shinkai Hisashi

  公开号：US20130053417A1

  公开（公告）日：2013-02-28

  The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.

  本发明提供了一种CETP活性抑制剂的化合物。该化合物可以通过选择性抑制CETP活性来增加HDL并同时降低LDL，本发明还提供了使用该化合物预防或治疗动脉粥样硬化或高脂血症的方法。
• CETP activity inhibitor
  申请人：Japan Tobacco, Inc., a Japan Corporation

  公开号：US20030092708A1

  公开（公告）日：2003-05-15

  The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): 1 wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X 1 , X 2 , X 3 , and X 4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO 2 —, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof. The compounds represented by the formula (I) can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity and, therefore, is expected to be useful as a new type of a preventive or therapeutic agent for atherosclerosis or hyperlipidemia.

  本发明提供了一种CETP活性抑制剂，其作为活性成分包含由式（I）表示的化合物：1其中R表示直链或支链烷基；直链或支链烯基；低卤代烷基；取代或未取代的环烷基；取代或未取代的环烯基；取代或未取代的环烷基烷基；取代或未取代的芳基或取代或未取代的杂环基，X1、X2、X3和X4可以相同也可以不同，每个表示氢原子、卤原子、低烷基、低卤代烷基、低烷氧基、氰基、硝基、酰基或芳基，Y表示—CO—或—SO2—，Z表示氢原子或巯基保护基，或其前药化合物、药学上可接受的盐、水合物或溶剂化物。由式（I）表示的化合物可以通过选择性抑制CETP活性来增加HDL并同时降低LDL，因此预计可用作新型的动脉粥样硬化或高脂血症的预防或治疗剂。
• Novel Tetracyclic Tetrahydrofuran Derivatives Containing Cyclic Amine Side Chain
  申请人：Cid-Nunez Jose Maria

  公开号：US20080262076A1

  公开（公告）日：2008-10-23

  This invention concerns novel substituted tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain with binding affinities towards dopamine receptors, in particular dopamine D 2 receptors, towards serotonin receptors, in particular 5-HT 2A and 5-HT 2C receptors, and pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein all substituents are defined as in Claim 1.

  本发明涉及一种新型取代四环四氢呋喃衍生物，其含有一个环状胺侧链，具有结合多巴胺受体的亲和力，特别是多巴胺D2受体，对5-HT2A和5-HT2C受体的亲和力，以及包含根据本发明的化合物的制药组合物，其用作药物，特别是用于预防和/或治疗一系列精神和神经疾病，特别是某些精神病、心血管和胃动力紊乱，并提供其生产过程。根据本发明的化合物可以用一般式（I）表示，并包括其药学上可接受的酸或碱盐、N-氧化物形式或季铵盐，其中所有取代基在权利要求书1中定义。