3-Dimethylamino-4-ethyl-propiophenon

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 3-Dimethylamino-4-ethyl-propiophenon
• 英文别名: 1-Dimethylamino-2-(4-ethyl-benzoyl)-ethan；3-(Dimethylamino)-1-(4-ethylphenyl)-1-propanone；3-(dimethylamino)-1-(4-ethylphenyl)propan-1-one
• 化学式: C₁₃H₁₉NO
• mdl: MFCD03820031
• 分子量: 205.3
• InChiKey: MKFIKNCPWMNGBS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• Therapeutic Agent for Type 2 Diabetes
  申请人：NATIONAL UNIVERSITY CORPORATION KUMAMOTO UNIVERSITY

  公开号：US20160060235A1

  公开（公告）日：2016-03-03

  An object of the present invention is to provide a novel therapeutic agent for a patient with type 2 diabetes, a cause of which is the abnormal synthesis of insulin attributed to the abnormal modification of tRNA Lys (UUU) in pancreatic β cells having Cdkal1 gene mutation. The present inventors have used (1) a screening system using E. coli in which correct translation into luciferase requires frameshift resulting from mistranslation during protein translation, (2) a screening system using the pancreatic islet of Langerhans isolated from a pancreatic β cell-specific Cdkal1-deficient mouse, and (3) a screening system using a pancreatic β cell-specific Cdkal1-deficient mouse, and found that a compound represented by any of the following formulas (I) to (III) can serve as a therapeutic agent for a patient with type 2 diabetes with Cdkal1 gene mutation resulting in the reduced ability to secrete insulin.

  本发明的一个目的是为2型糖尿病患者提供一种新型治疗剂，其原因是由于胰岛素的异常合成归因于胰岛β细胞中tRNALys(UUU)的异常修饰，其具有Cdkal1基因突变。本发明者已经使用了（1）使用大肠杆菌的筛选系统，其中正确的翻译成荧光酶需要在蛋白质翻译过程中由于错误翻译而导致的移码，（2）使用从胰岛β细胞特异性Cdkal1缺陷小鼠中分离的Langerhans胰岛的筛选系统，以及（3）使用胰岛β细胞特异性Cdkal1缺陷小鼠的筛选系统，并发现以下任一式（I）至（III）所代表的化合物可以作为一种治疗剂，用于具有Cdkal1基因突变且导致胰岛素分泌能力降低的2型糖尿病患者。
• Propiophenone derivatives and their preparation and pharmaceutical use
  申请人：MARUHO Co., Ltd.

  公开号：EP0423524A2

  公开（公告）日：1991-04-24

  The present invention relates to compounds represented by the general formula I in which X₁, X₂represent hydrogen, C₁₋₄-alky phenyl, halogen, C₁₋₄-alkoxy or dialkylamino with C₁₋₄-alkyl groups, or X₁ and X₂ together represent phenylene or indane-2,3-diyl, Z₁, Z₂represent hydrogen or hydroxy, or together represent oxygen or -O(CH₂)₂O-, Y₁, Y₂represent hydrogen, C₁₋₃-alkyl or phenyl, Arepresents a group derived from a cyclic amine, and nrepresents 0, 1 or 2, in the form of the free base or in the form of addition salts, preferably pharmaceutically acceptable salts, to methods for their preparation, and to their pharmaceutical use as central muscle relaxants and anticonvulsives.

  本发明涉及通式 I 所代表的化合物 其中 X₁、X₂代表氢、C₁₋₄-烷基苯基、卤素、C₁₋₄-烷氧基或带有C₁₋₄-烷基的二烷基氨基，或者X₁和X₂一起代表亚苯基或茚-2,3-二基、 Z₁、Z₂代表氢或羟基，或共同代表氧或-O(CH₂)₂O-、 Y₁、Y₂代表氢、C₁₋₃-烷基或苯基、 代表由环胺衍生的基团、 和 n 代表 0、1 或 2、 这些化合物以游离碱或加成盐（最好是药学上可接受的盐）的形式存在，其制备方 法以及作为中枢性肌肉松弛剂和抗惊厥药的药用用途也是如此。
• MITOCHONDRIAL ALDEHYDE DEHYDROGENASE-2 MODULATORS AND METHODS OF USE THEREOF
  申请人：The Board of Trustees of the Leland Stanford Junior University

  公开号：EP2126574B1

  公开（公告）日：2015-12-23
• Mitochondrial Aldehyde Dehydrogenase-2 Modulators and Methods of Use Thereof
  申请人：MOCHLY-ROSEN DARIA

  公开号：US20110105602A2

  公开（公告）日：2011-05-05

  The present invention provides compounds that function as modulators of mitochondrial aldehyde dehydrogenase-2 (ALDH2) activity; and pharmaceutical compositions comprising the compounds. The present invention provides therapeutic methods involving administering a subject compound, or a subject pharmaceutical composition. The present invention further provides assays for identifying agonists of ALDH2.
• US9102651B2
  申请人：——

  公开号：US9102651B2

  公开（公告）日：2015-08-11