5-({6-chloro-5-[4-(1-hydroxy-1-methylethyl)phenyl]-1H-benzimidazol-2-yl}oxy)-2-methylbenzoic acid | 1219738-67-6

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 5-({6-chloro-5-[4-(1-hydroxy-1-methylethyl)phenyl]-1H-benzimidazol-2-yl}oxy)-2-methylbenzoic acid
• 英文别名: 5-[[6-chloro-5-[4-(2-hydroxypropan-2-yl)phenyl]-1H-benzimidazol-2-yl]oxy]-2-methylbenzoic acid
• CAS: 1219738-67-6
• 化学式: C₂₄H₂₁ClN₂O₄
• 分子量: 436.895
• InChiKey: PJADJONHBDISTN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.2
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  95.4
• 氢给体数：
  3
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  5-{[5-(4-acetylphenyl)-6-chloro-1H-benzimidazol-2-yl]oxy}-2-methylbenzoic acid 、 甲基溴化镁 在 cerium(III) chloride 、 盐酸 作用下， 以 四氢呋喃 、 水 为溶剂， 生成 5-({6-chloro-5-[4-(1-hydroxy-1-methylethyl)phenyl]-1H-benzimidazol-2-yl}oxy)-2-methylbenzoic acid
  参考文献：
  名称：

  NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL AS ANTI-DIABETIC AGENTS

  摘要：

  结构式（I）的新化合物是AMP-蛋白激酶的激活剂，并且在治疗、预防和抑制由AMPK激活的蛋白激酶介导的疾病方面非常有用。本发明的化合物在治疗2型糖尿病、高血糖、代谢综合征、肥胖、高胆固醇血症和高血压方面非常有用。

  公开号：

  US20100081643A1

文献信息

• [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。
• [EN] DIARYLMETHYLAMIDE DERIVATIVE HAVING MELANIN-CONCENTRATING HORMONE RECEPTOR ANTAGONISM<br/>[FR] DÉRIVÉ DE DIARYLMÉTHYLAMIDE PRÉSENTANT UNE ACTIVITÉ D'ANTAGONISTE DES RÉCEPTEURS DE L'HORMONE DE MÉLANO-CONCENTRATION
  申请人：MERCK SHARP & DOHME

  公开号：WO2011037771A1

  公开（公告）日：2011-03-31

  The present invention is directed to diarylmethylamide derivatives represented of structural formula I which are melanin-concentrating hormone receptor antagonists, and are useful as an agent for the prevention, treatment, or remedy of various circulatory diseases, neurological diseases, metabolic diseases, reproductive system diseases, respiratory diseases, digestive diseases, and the like. 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 melanin-concentrating hormone is involved. I

  本发明涉及结构式I所代表的二芳基甲酰胺衍生物，其为黑色素浓集激素受体拮抗剂，并且可用作预防、治疗或缓解各种循环系统疾病、神经系统疾病、代谢性疾病、生殖系统疾病、呼吸系统疾病、消化系统疾病等的药物。该发明还涉及包含这些化合物的药物组合物以及在黑色素浓集激素参与的这些疾病的预防或治疗中使用这些化合物和组合物。
• 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] SUBSTITUTED AMINOPIPERIDINES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES<br/>[FR] AMINOPIPÉRIDINES SUBSTITUÉES UTILISÉES EN TANT QU'INHIBITEURS DE LA DIPEPTIDYL PEPTIDASE-IV DANS LE CADRE DU TRAITEMENT DU DIABÈTE
  申请人：MERCK SHARP & DOHME

  公开号：WO2011037793A1

  公开（公告）日：2011-03-31

  The present invention is directed to novel substituted aminopiperidines 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-ΪV 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的新型取代氨基哌啶，它们是二肽基肽酶-IV酶的抑制剂，并且在治疗或预防二肽基肽酶-IV酶参与的疾病中有用，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在预防或治疗二肽基肽酶-IV酶参与的这类疾病中使用这些化合物和组合物。
• [EN] SPIRO ISOXAZOLINE COMPOUNDS AS SSTR5 ANTAGONISTS<br/>[FR] COMPOSÉS SPIROISOXAZOLINES EN TANT QU'ANTAGONISTES SSTR5
  申请人：MERCK SHARP & DOHME

  公开号：WO2011146324A1

  公开（公告）日：2011-11-24

  Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.

  结构式（I）的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，对于对抗SSTR5有响应的疾病的治疗、控制或预防是有用的，如2型糖尿病、胰岛素抵抗、脂质紊乱、肥胖、动脉粥样硬化、代谢综合征、抑郁症和焦虑症。