5-[2-(2,6-dimethyl-4'-trifluoromethyl-biphenyl-4-yloxy)-1,1-dimethyl-ethyl]-thiophene-2-carboxylic acid methyl ester | 906101-84-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 5-[2-(2,6-dimethyl-4'-trifluoromethyl-biphenyl-4-yloxy)-1,1-dimethyl-ethyl]-thiophene-2-carboxylic acid methyl ester
• 英文别名: methyl 5-[1-[3,5-dimethyl-4-[4-(trifluoromethyl)phenyl]phenoxy]-2-methylpropan-2-yl]thiophene-2-carboxylate
• CAS: 906101-84-6
• 化学式: C₂₅H₂₅F₃O₃S
• 分子量: 462.533
• InChiKey: SAZYLTAIRLAVSU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.9
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  63.8
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2,6-二甲基-4-(三氟甲基)-[1,1-联苯]-4-醇 、 5-(2-hydroxy-1,1-dimethyl-ethyl)-thiophene-2-carboxylic acid methyl ester 在 三苯基膦 、 1,1'-azodicarbonyl-dipiperidine 作用下， 以 甲苯 为溶剂， 以42%的产率得到5-[2-(2,6-dimethyl-4'-trifluoromethyl-biphenyl-4-yloxy)-1,1-dimethyl-ethyl]-thiophene-2-carboxylic acid methyl ester
  参考文献：
  名称：

  SUBSTITUTED THIOPHENE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES

  摘要：

  公开号：

  EP1856090B1

文献信息

• Glucagon receptor antagonists, preparation and therapeutic uses
  申请人：Eli Lilly and Company

  公开号：US08084489B2

  公开（公告）日：2011-12-27

  The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

  本发明揭示了一种新的化合物式(I)或其药学上可接受的盐，该化合物具有胰高血糖素受体拮抗剂或反向激动剂活性，以及使用这些化合物的方法和制备这些化合物的中间体和方法。在另一实施例中，本发明揭示了包括化合物式(I)的N种药物组合物，以及使用它们治疗糖尿病和其他胰高血糖素相关代谢障碍等方法。
• Glucagon Receptor Antagonists, Preparation and Therapeutic Uses
  申请人：Chappell Mark Donald

  公开号：US20100137417A1

  公开（公告）日：2010-06-03

  The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

  本发明揭示了公式（I）的新化合物或其药学上可接受的盐，具有胰高血糖素受体拮抗剂或反向激动剂活性，以及使用这些化合物的方法，以及制备这些化合物的中间体和方法。在另一种实施方式中，本发明揭示了包含公式（I）的N个化合物的药物组合物，以及使用它们治疗糖尿病和其他胰高血糖素相关代谢紊乱等方法。
• US8084489B2
  申请人：——

  公开号：US8084489B2

  公开（公告）日：2011-12-27
• [EN] GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES<br/>[FR] ANTAGONISTES DU RECEPTEUR DU GLUCAGON, LEUR PREPARATION ET LEURS UTILISATIONS THERAPEUTIQUES
  申请人：LILLY CO ELI

  公开号：WO2006086488A2

  公开（公告）日：2006-08-17

  [EN] The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.
  [FR] La présente invention concerne des nouveaux composés de formule (I) ou des sels associés acceptables pharmaceutiquement qui possèdent un antagoniste du récepteur du glucagon ou une activité agoniste inverse, ainsi que des méthodes d'utilisation de ces composés et intermédiaires et des méthodes de préparation de tels composés. Dans un autre mode de réalisation, cette invention a pour objet des compositions pharmaceutiques renfermant des composés de formule (I), ainsi que des méthodes les employant dans le traitement de troubles diabétiques et d'autres troubles métaboliques liés au glucagon, et similaire.
• SUBSTITUTED THIOPHENE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES
  申请人：ELI LILLY AND COMPANY

  公开号：EP1856090B1

  公开（公告）日：2009-10-14