(-) 3-[4-[2-(3,4-dihydro-2H-benzo[b][1,4]thiazin-4-yl)ethoxy]phenyl]-2-ethoxypropanoic acid

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 苯丙酸
• 英文名称: (-) 3-[4-[2-(3,4-dihydro-2H-benzo[b][1,4]thiazin-4-yl)ethoxy]phenyl]-2-ethoxypropanoic acid
• 英文别名: (-)-3-[4-[2-(2,3-dihydro-1,4-benzothiazin-4-yl)ethoxy]phenyl]-2-ethoxypropanoic acid；3-[4-[2-(2,3-Dihydro-1,4-benzothiazin-4-yl)ethoxy]phenyl]-2-ethoxypropanoic acid
• 化学式: C₂₁H₂₅NO₄S
• 分子量: 387.5
• InChiKey: GKBWKSJWXJMEEQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  27
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  84.3
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (-) 3-[4-[2-(3,4-dihydro-2H-benzo[b][1,4]thiazin-4-yl)ethoxy]phenyl]-2-ethoxypropanoic acid 在 草酰氯 、 氨 作用下， 以 二氯甲烷 、 水 为溶剂， 反应 2.5h， 以54%的产率得到(+/-) 3-[4-[2-(2,3-Dihydro-1,4-benzothiazin-4-yl)ethoxy]phenyl]-2-ethoxypropanamide
  参考文献：
  名称：

  Substituted bicyclic heterocycles, process for their preparation and their use as antiobesity and hypocholesterolemic agents

  摘要：

  本发明涉及新型抗肥胖和降低胆固醇的化合物、它们的衍生物、类似物、互变异构体、立体异构体、多晶形态、药学上可接受的盐、药学上可接受的溶剂和药学上可接受的含有它们的组合物。更具体地，本发明涉及一般式(I)的新型β-芳基-α-氧代取代烷基羧酸、它们的衍生物、类似物、互变异构体、立体异构体、多晶形态、药学上可接受的盐、药学上可接受的溶剂和药学上可接受的含有它们的组合物。

  公开号：

  US07348426B1
• 作为产物：
  描述：

  (+/-) Methyl-3-[4-[2-(2,3-dihydro-1,4-benzothiazin-4-yl)ethoxy]phenyl]-2-ethoxypropanoate 以63%的产率得到(-) 3-[4-[2-(3,4-dihydro-2H-benzo[b][1,4]thiazin-4-yl)ethoxy]phenyl]-2-ethoxypropanoic acid
  参考文献：
  名称：

  Bicyclic compounds and their use in medicine, process for their preparation and pharmaceutical compositions containing them

  摘要：

  式(I)的化合物、其互变异构体、立体异构体、多晶型、药学上可接受的盐或药学上可接受的溶剂，可用于预防或治疗由胰岛素抵抗或糖耐量受损引起的糖尿病或由胰岛素抵抗或糖耐量受损引起的糖尿病并发症。这些化合物还可用于降低血液中的胆固醇、体重、血糖、甘油三酯和游离脂肪酸水平。

  公开号：

  US06265401B1

文献信息

• [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF BICYCLIC ANTIDIABETIC AGENTS<br/>[FR] PROCEDE AMELIORE POUR LA PREPARATION D'AGENTS ANTIDIABETIQUES BICYCLIQUES
  申请人：REDDYS LAB LTD DR

  公开号：WO2003099800A1

  公开（公告）日：2003-12-04

  The present invention relates to an improved process for the preparation of antidiabetic compounds having the formula (1). where R represents (C1-C6)alkyl group, X represents sulphur or oxygen atom

  本发明涉及一种改进的制备抗糖尿病化合物的方法，其化学式为(1)，其中R代表(C1-C6)烷基基团，X代表硫或氧原子。
• Pharmaceutically acceptable salts of bicyclic compounds
  申请人：DR. REDDY'S LABORATORIES LTD.

  公开号：US20020142993A1

  公开（公告）日：2002-10-03

  The present invention relates to pharmaceutically acceptable salts of compound of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. 1

  本发明涉及一般式（I）化合物的药学上可接受的盐、其衍生物、类似物、互变异构体、立体异构体、多晶形态、药学上可接受的溶剂化合物，以及包含它们的药学上可接受的组合物。
• [EN] SALTS OF BENZOTHIAZINE AND BENZOXAZINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM<br/>[FR] SELS DE DERIVES DE BENZOTHIAZINE ET DE BENZOXAZINE ET COMPOSITIONS PHARMACEUTIQUES A BASE DE CES SELS
  申请人：REDDY RESEARCH FOUNDATION

  公开号：WO2002030914A1

  公开（公告）日：2002-04-18

  The present invention relates to pharmaceutically acceptable salts of compound of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. wherein R1 represents hydrogen, halogen atom such as fluorine, chlorine, bromine or iodine; hydroxy, nitro, cyano or lower alkyl group; R2 represents hydrogen, lower alkyl or oxo group; X represents a heteroatom selected from oxygen or sulfur; R3 represents hydrogen or lower alkyl group; n is an integer ranging from 1-4; M represents a counter ion or a moiety which forms a pharmaceutically acceptable salt; p is an integer ranging from 1 to 2.

  本发明涉及一般式(I)的化合物的药学上可接受的盐、它们的衍生物、类似物、互变异构体、立体异构体、多晶形、药学上可接受的溶剂化物以及含有它们的药学上可接受的组合物。其中，R1代表氢、卤原子，例如氟、氯、溴或碘；羟基、硝基、氰基或较低的烷基基团；R2代表氢、较低的烷基或氧代基团；X代表从氧或硫中选择的杂原子；R3代表氢或较低的烷基基团；n为1-4之间的整数；M代表一个计数离子或形成药学上可接受的盐的基团；p为1至2之间的整数。
• Novel bicyclic compounds and their use in medicine; process for their preparation and pharmaceutical compositions containing them
  申请人：DR. REDDY'S RESEARCH FOUNDATION AND REDDY-CHEMINOR, INC.

  公开号：US20010051619A1

  公开（公告）日：2001-12-13

  Compounds of formula (I) 1 its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates can be used to prevent or treat diabetes caused by insulin resistance or impaired glucose tolerance or complications of diabetes caused by insulin resistance or impaired glucose tolerance. The compounds can also be used to reduce cholesterol, body weight, blood glucose, triglycerides and free fatty acids in the blood.

  式（I）的化合物及其互变异构体、立体异构体、多晶形态、药学上可接受的盐或药学上可接受的溶剂，可用于预防或治疗由胰岛素抵抗或糖耐量受损引起的糖尿病或由胰岛素抵抗或糖耐量受损引起的糖尿病并发症。这些化合物还可用于降低血液中的胆固醇、体重、血糖、甘油三酯和游离脂肪酸。
• Bicyclic compounds and their use in medicine; process for their preparation and pharmaceutical compositions containing them
  申请人：Dr. Reddy's Laboratories Ltd.

  公开号：US06809095B2

  公开（公告）日：2004-10-26

  A method for preventing or treating complications of diabetes by administering a compound of formula (I) its tautomeric forms, its stereoisomers, its polymorphs, its pharmaceutically acceptable salts or its pharmaceutically acceptable solvates.

  通过给予公式（I）的化合物、其互变异构体、立体异构体、多晶型、药学上可接受的盐或药学上可接受的溶剂，来预防或治疗糖尿病并发症的方法。