N-[4-[3-[4-Isopropyl-2-[4-(trifluoromethyl)phenyl]thiazol-5-yl]propionyl]phenyl]-N-methylglycine | 954372-21-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: N-[4-[3-[4-Isopropyl-2-[4-(trifluoromethyl)phenyl]thiazol-5-yl]propionyl]phenyl]-N-methylglycine
• 英文别名: 2-[N-methyl-4-[3-[4-propan-2-yl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]propanoyl]anilino]acetic acid
• CAS: 954372-21-5
• 化学式: C₂₅H₂₅F₃N₂O₃S
• 分子量: 490.546
• InChiKey: AFGQYDIASXFBSL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  34
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  98.7
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为产物：
  描述：

  N-[4-[3-[4-isopropyl-2-[4-(trifluoromethyl)phenyl]thiazol-5-yl]propionyl]phenyl]-N-methylglycine ethyl ester 在 sodium hydroxide 、 乙醇 、 水 、 盐酸 作用下， 以 四氢呋喃 、 乙醇 为溶剂， 反应 0.83h， 以78%的产率得到N-[4-[3-[4-Isopropyl-2-[4-(trifluoromethyl)phenyl]thiazol-5-yl]propionyl]phenyl]-N-methylglycine
  参考文献：
  名称：

  ACTIVATING AGENT FOR PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR

  摘要：

  公开号：

  EP2014652B1

文献信息

• ACTIVATING AGENT FOR PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR DELTA
  申请人：Sakuma Shogo

  公开号：US20090298896A1

  公开（公告）日：2009-12-03

  A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPARδ. wherein G a is O, CH 2 or the like; A a is thiazole, oxazole, or thiophene, which can have a substituent such as C 1-8 alkyl, C 1-8 alkoxy, halogen, C 1-8 alkyl substituted with halogen or the like; B a is a C 1-8 alkylene or C 2-8 alkenylene chain; and each of R 1a and R 2a independently is hydrogen, C 1-8 alkyl, C 1-8 alkoxy, halogen, C 1-8 alkyl substituted with halogen or the like.

  以下通式（II）所代表的化合物或其盐被用作PPARδ的激活剂。其中G是O，CH2或类似物；A是噻唑、噁唑或噻吩，可以具有C1-8烷基、C1-8烷氧基、卤素、C1-8卤代烷基或类似物的取代基；B是C1-8烷基或C2-8烯基烷链；R1a和R2a各自独立地是氢、C1-8烷基、C1-8烷氧基、卤素、C1-8卤代烷基或类似物。
• Use of PPAR Delta Ligands for the Treatment or Prevention of Inflammation or Energy Metabolism/Production Related Diseases
  申请人：Barbaras Ronald

  公开号：US20110092517A1

  公开（公告）日：2011-04-21

  Provided herein are methods for treatment, prevention, or amelioration of one or more symptoms of a disease or condition related to disorders of insulin and/or glucose metabolism, inflammatory conditions, mitochondrial disease, muscle disorders, or pulmonary disorders, involving administering a PPARδ agonist or a pharmaceutical composition comprising a PPARδ agonist. In one embodiment, the disease or condition is selected from myopathy, inflammatory vascular diseases, Parkinson's and Alzheimer's diseases, systemic inflammatory disorders, renal ischemia, inflammatory rheumatic disorders, and inflammatory diseases of the lung. In another embodiment, methods for increasing oxidative muscle fibers, reducing mitochondria disease, decreasing insulin resistance, decreasing plasma glucose, or decreasing weight, involving administering a PPARδ agonist or a pharmaceutical composition comprising a PPARδ agonist, are provided.

  本文提供了治疗、预防或改善与胰岛素和/或葡萄糖代谢紊乱、炎症性疾病、线粒体病、肌肉疾病或肺部疾病相关的一种或多种症状的方法，其中涉及给予一种PPARδ激动剂或含有PPARδ激动剂的制剂。在一种实施例中，所述疾病或症状被选自肌无力、炎症性血管疾病、帕金森和阿尔茨海默病、全身性炎症性疾病、肾脏缺血、炎症性风湿病和肺部炎症性疾病。在另一种实施例中，提供了通过给予PPARδ激动剂或含有PPARδ激动剂的制剂来增加氧化肌纤维、减少线粒体疾病、降低胰岛素抵抗、降低血浆葡萄糖或减轻体重的方法。
• Activating agent for peroxisome proliferator activated receptor δ
  申请人：Sakuma Shogo

  公开号：US08404726B2

  公开（公告）日：2013-03-26

  A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPARδ. wherein Ga is O, CH2 or the like; Aa is thiazole, oxazole, or thiophene, which can have a substituent such as C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like; Ba is a C1-8 alkylene or C2-8 alkenylene chain; and each of R1a and R2a independently is hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like.

  以下通式（II）所表示的化合物或其盐被用作PPARδ的激活剂，其中：Ga为O、CH2或类似物；Aa为噻唑、噁唑或噻吩，其可以具有C1-8烷基、C1-8烷氧基、卤素、C1-8卤代烷基或类似物的取代基；Ba为C1-8烷基或C2-8烯基烷链；每个R1a和R2a独立地为氢、C1-8烷基、C1-8烷氧基、卤素、C1-8卤代烷基或类似物。
• WOUND-HEALING AGENT
  申请人：Nippon Chemiphar Co., Ltd.

  公开号：EP3456327A1

  公开（公告）日：2019-03-20

  A wound-healing agent is provided by using a benzisoxazole compound represented by the following general formula (I), a tautomer, a stereoisomer, or a pharmaceutically acceptable salt of the compound, a solvate of any of the foregoing, or the like, which exerts a PPARδ agonist effect.

  通过使用由下式通式（I）代表的苯并异噁唑化合物、该化合物的同系物、立体异构体或药学上可接受的盐、上述任一化合物的溶液或类似物，提供了一种伤口愈合剂，该伤口愈合剂具有 PPARδ 激动剂的效果。
• USE OF PPAR DELTA LIGANDS FOR THE TREATMENT OR PREVENTION OF INFLAMMATION OR ENERGY METABOLISM/PRODUCTION RELATED DISEASES
  申请人：Cerenis Therapeutics S.A.

  公开号：EP2464349A2

  公开（公告）日：2012-06-20