2,2-Difluoro-1-[4-methyl-2-(6-trifluoromethyl-pyridin-3-yl)-thiazol-5-yl]-butan-1-ol | 933781-79-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2,2-Difluoro-1-[4-methyl-2-(6-trifluoromethyl-pyridin-3-yl)-thiazol-5-yl]-butan-1-ol
• 英文别名: 2,2-difluoro-1-[4-methyl-2-[6-(trifluoromethyl)pyridin-3-yl]-1,3-thiazol-5-yl]butan-1-ol
• CAS: 933781-79-4
• 化学式: C₁₄H₁₃F₅N₂OS
• 分子量: 352.328
• InChiKey: KDSSXZCLUQDBHY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  23
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.43
• 拓扑面积：
  74.2
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  2,2-Difluoro-1-[4-methyl-2-(6-trifluoromethyl-pyridin-3-yl)-thiazol-5-yl]-but-3-en-1-ol 在 钯 氢气 作用下， 以 乙酸乙酯 为溶剂， 反应 3.0h， 以to obtain 490 mg 2,2-Difluoro-1-[4-methyl-2-(6-trifluoromethyl-pyridin-3-yl)-thiazol-5-yl]-butan-1-ol as a white solid的产率得到2,2-Difluoro-1-[4-methyl-2-(6-trifluoromethyl-pyridin-3-yl)-thiazol-5-yl]-butan-1-ol
  参考文献：
  名称：

  Phenyl-1,2,4-Oxadiazolone Derivatives, Processes For Their Preparation and Methods For Their Use as Pharmaceuticals

  摘要：

  本发明的创新化合物由苯基和吡啶基-1,2,4-噁唑酮衍生物及其生理上可接受的盐和功能衍生物组成，已被证明具有过氧化物酶体增殖激活受体（PPARdelta）激动剂活性。本发明的化合物由以下公式组成：其中取代基R1-R5和R7-R10在此定义。这些化合物在哺乳动物的脂质和碳水化合物代谢的调节和调节中具有治疗效果，因此适用于治疗2型糖尿病，动脉粥样硬化，心血管疾病等疾病。

  公开号：

  US20080261979A1

文献信息

• Phenyl-1,2,4-Oxadiazolone Derivatives, Processes For Their Preparation and Methods For Their Use as Pharmaceuticals
  申请人：Keil Stefanie

  公开号：US20080261979A1

  公开（公告）日：2008-10-23

  The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.

  本发明的创新化合物由苯基和吡啶基-1,2,4-噁二唑酮衍生物以及它们的生理上可接受的盐和功能衍生物组成，已被证明具有过氧化物酶体增殖激活受体（PPARδ）激动剂活性。本发明的化合物由以下公式组成：其中取代基R1-R5和R7-R10在此定义。这些化合物在哺乳动物的脂质和碳水化合物代谢的调节和调控方面具有治疗效果，因此适用于治疗糖尿病、动脉粥样硬化、心血管疾病等疾病。
• PHENYL- AND PYRIDINYL- 1, 2 , 4 - OXADIAZOLONE DERIVATIVES, PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
  申请人：Sanofi-Aventis

  公开号：EP1931337A2

  公开（公告）日：2008-06-18
• US7709481B2
  申请人：——

  公开号：US7709481B2

  公开（公告）日：2010-05-04
• [EN] PHENYL-1,2,4-OXADIAZOLONE DERIVATIVES , PROCESSES FOR THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS<br/>[FR] DERIVES DE PHENYL-1,2,4-OXADIAZOLONE : PROCEDES DE PREPARATION ET UTILISATION COMME PRODUITS PHARMACEUTIQUES
  申请人：SANOFI AVENTIS DEUTSCHLAND

  公开号：WO2007039177A2

  公开（公告）日：2007-04-12

  (EN) The invention relates to phenyl-1,2,4-oxadiazolone derivatives in all its stereoisomeric forms and mixtures in any ratio, and its physiologically acceptable salts and tautomeric forms showing PPARdelta agonist activity. What is described are compounds of the formula (I), wherein the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.(FR) L'invention concerne des dérivés de phényl-1,2,4-oxadiazolone sous toutes leurs formes stéréoisomères et leurs mélanges dans des proportions quelconques, ainsi que les sels physiologiquement acceptables et les formes tautomères de deux-ci qui exercent une activité agoniste sur les récepteurs PPARΔ. L'invention décrit ainsi des composés représentés par la formule (I), dans laquelle les radicaux sont tels que définis dans la description, ainsi que les sels physiologiquement acceptables de ceux-ci et les procédés utilisés pour les obtenir. Ces composés sont utilisés pour traiter et/ou prévenir les troubles du métabolisme des acides gras, les troubles de l'utilisation du glucose, les troubles impliquant l'insulinorésistance et la démyélinisation, ainsi que d'autres troubles neurodégénératifs du système nerveux central et périphérique.
• Phenyl-1,2,4-oxadiazolone derivatives, processes for their preparation and methods for their use as pharmaceuticals
  申请人：Sanofi-Aventis

  公开号：US07709481B2

  公开（公告）日：2010-05-04

  The inventive compounds of the present invention are comprised of phenyl and pyridinyl-1,2,4-oxadiazolone derivatives and their physiologically acceptable salts and functional derivatives that are shown to provide peroxisome proliferator activator receptor (PPARdelta) agonist activity. The compounds of the present invention are comprised of the formula: wherein the substituents R1-R5 and R7-R10 are defined herein. The compounds are therapeutically effective in the regulation and modulation of lipid and carbohydrate metabolism in mammals and are thus suitable for the treatment of diseases such as type-2 diabetes, atherosclerosis, cardiovascular disorders and the like.

  本发明的创新化合物包括苯基和吡啶基-1,2,4-噁二唑酮衍生物及其生理上可接受的盐和功能衍生物，这些化合物被证明具有过氧化物酶体增殖激活受体（PPARδ）激动剂活性。本发明的化合物由以下公式组成：其中取代基R1-R5和R7-R10在此定义。这些化合物在哺乳动物的脂质和碳水化合物代谢的调节和调节中具有治疗效果，因此适用于治疗2型糖尿病、动脉粥样硬化、心血管疾病等疾病。