MK-0533 | 668455-28-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: MK-0533
• 英文别名: (2R)-2-(3-{3-[(4-methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoic acid；(2R)-2-{3-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}butanoic acid；(R)-2-(3-(3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl)phenoxy)butanoic acid；(2R)-2-[3-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)indol-1-yl]phenoxy]butanoic acid
• CAS: 668455-28-5
• 化学式: C₂₈H₂₄F₃NO₆
• 分子量: 527.497
• InChiKey: STWITCBWQHTJFJ-XMMPIXPASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7
• 重原子数：
  38
• 可旋转键数：
  9
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  87
• 氢给体数：
  1
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  MK-0533 在 水 作用下， 生成 (2R)-2-{3-[3-(4-methoxybenzoyl)-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl]phenoxy}butanoic acid dihydrate
  参考文献：
  名称：

  WO2006/99077

  摘要：

  公开号：
• 作为产物：
  描述：

  tert-butyl (2R)-2-(3-{3-[(4-methoxyphenyl)carbonyl]-2-methyl-6-(trifluoromethoxy)-1H-indol-1-yl}phenoxy)butanoate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 MK-0533
  参考文献：
  名称：

  [EN] INDOLES HAVING ANTI-DIABETIC ACTIVITY
  [FR] INDOLES A ACTIVITE ANTIDIABETIQUE

  摘要：

  印度戊酸取代的吲哚类化合物或芳基氧烷酸取代的吲哚类化合物是PPAR-γ的激动剂或部分激动剂，对于治疗和控制与2型糖尿病相关的症状性高血糖、以及常伴有2型糖尿病的血脂异常、高血脂、高胆固醇、高甘油三酯和肥胖等方面具有用处。

  公开号：

  WO2004020408A1

文献信息

• [EN] COMPOUNDS AS DGAT-1 INHIBITORS<br/>[FR] COMPOSÉS EN TANT QU'INHIBITEURS DE DGAT-1
  申请人：MERCK SHARP & DOHME

  公开号：WO2013096093A1

  公开（公告）日：2013-06-27

  Described herein are compounds of formula I. The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

  本发明描述了公式I的化合物。公式I的化合物作为DGAT1抑制剂，可用于预防、治疗或作为治疗高脂血症、糖尿病和肥胖的药物。
• [EN] SUBSTITUTED CYCLOPROPYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT<br/>[FR] COMPOSÉS CYCLOPROPYLE SUBSTITUÉS, COMPOSITIONS CONTENANT DE TELS COMPOSÉS ET PROCÉDÉS DE TRAITEMENT
  申请人：MERCK SHARP & DOHME

  公开号：WO2011019538A1

  公开（公告）日：2011-02-17

  Substituted cyclopropyl compounds of the formula I: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.

  取代的环丙基化合物公式I：被披露为用于治疗或预防2型糖尿病和类似病症的有用物质。药物可接受的盐也包括在内。这些化合物作为G蛋白偶联受体GPR-119的激动剂是有用的。
• HETEROCYCLIC DERIVATIVES AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE
  申请人：Isabel Elise

  公开号：US20110301143A1

  公开（公告）日：2011-12-08

  Heterocyclic compounds of structural formula (I), or a pharmaceutically acceptable salt thereof, wherein W is a R 1 — substituted heteroaryl, R 1 is an heteroaryl ring substituted with an ester or carboxylic acid containing radical, X-T is N—CR 5 R 6 , C═CR 5 or CR 13 —CR 5 R 6 , Y is a bond or —C(O)—, a and b represent an integer selected from 1 to 4, and Ar is an optionally substituted phenyl or naphtyl, are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD) The heterocyclic compounds are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, atherosclerosis, obesity, diabetes, neurological disease, Metabolic Syndrome, insulin resistance, cancer, liver steatosis, and non-alcoholic steatohepatitis.

  结构式（I）的杂环化合物，或其药学上可接受的盐，其中W是R1-取代的杂芳基，R1是取代有酯基或羧基的杂芳基环，X-T是N—CR5R6，C═CR5或CR13—CR5R6，Y是键或—C(O)—，a和b代表选自1到4的整数，Ar是可选择取代的苯基或萘基，是硬脂酰辅酶A 9-脱饱和酶（SCD）的抑制剂。这些杂环化合物对于预防和治疗与异常脂质合成和代谢有关的疾病非常有用，包括心血管疾病、动脉粥样硬化、肥胖症、糖尿病、神经系统疾病、代谢综合征、胰岛素抵抗、癌症、肝脂肪变性和非酒精性脂肪肝。
• [EN] IMIDAZOLE DERIVATIVES<br/>[FR] DÉRIVÉS D'IMIDAZOLE
  申请人：INTERVET INT BV

  公开号：WO2012164071A1

  公开（公告）日：2012-12-06

  Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.

  本文描述了式(I)的化合物。式(I)的化合物作为DGAT1抑制剂，可用于预防、治疗或作为高脂血症、糖尿病和肥胖的治疗药物。
• AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
  申请人：Biftu Tesfaye

  公开号：US20100120863A1

  公开（公告）日：2010-05-13

  The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

  本发明涉及结构式I的新型取代氨基四氢吡喃衍生物，它们是二肽基肽酶-IV酶的抑制剂，可用于治疗或预防二肽基肽酶-IV酶参与的疾病，如糖尿病，特别是2型糖尿病。该发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在预防或治疗二肽基肽酶-IV酶参与的疾病中的用途。