N-(3-methyl-1,2,4-thiadiazol-5-yl)-6-[(4-methyl-4H-1,2,4-triazol-3-yl)thio]-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]thio}pyridine-2-carboxamide | 1018966-11-4

• 分子结构分类: 有机化合物 - 有机硫化合物 - 硫醚类
• 英文名称: N-(3-methyl-1,2,4-thiadiazol-5-yl)-6-[(4-methyl-4H-1,2,4-triazol-3-yl)thio]-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]thio}pyridine-2-carboxamide
• 英文别名: N-(3-methyl-1,2,4-thiadiazol-5-yl)-6-[(4-methyl-1,2,4-triazol-3-yl)sulfanyl]-3-[4-(2-pyrrolidin-1-ylethoxy)phenyl]sulfanylpyridine-2-carboxamide
• CAS: 1018966-11-4
• 化学式: C₂₄H₂₆N₈O₂S₃
• 分子量: 554.721
• InChiKey: UIXKDBYNNVAUDG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.4
• 重原子数：
  37
• 可旋转键数：
  10
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  190
• 氢给体数：
  1
• 氢受体数：
  11

反应信息

• 作为产物：
  描述：

  四氢吡咯 生成 N-(3-methyl-1,2,4-thiadiazol-5-yl)-6-[(4-methyl-4H-1,2,4-triazol-3-yl)thio]-3-{[4-(2-pyrrolidin-1-ylethoxy)phenyl]thio}pyridine-2-carboxamide
  参考文献：
  名称：

  2-PYRIDINECARBOXAMIDE DERIVATIVE HAVING GK-ACTIVATING EFFECT

  摘要：

  公开了一种化合物(I)及其药用可接受的盐。这些化合物具有激活葡萄糖激酶的作用，因此可用于治疗糖尿病和肥胖。R1和R2分别独立表示较低的烷基基团；X1表示一个公式(II-1)的基团：其中：R11和R12分别独立表示氢原子或较低的烷基基团，或者与它们结合的氮原子一起，R11和R12可以形成一个4-至7-成员的含氮脂肪环（构成4-至7-成员的含氮脂肪环的一个碳原子可以被氧原子替代），或者与(CH2)m中的一个碳原子一起，R11和R12可以形成一个4-至7-成员的含氮脂肪环；m表示一个从1到3的整数。

  公开号：

  US20080090799A1

文献信息

• [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。
• 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。
• [EN] SUBSTITUTED AMINOTETRAHYDROTHIOPYRANS AND DERIVATIVES THEREOF AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES<br/>[FR] AMINOTÉTRAHYDROTHIOPYRANES SUBSTITUÉS ET DÉRIVÉS DE CEUX-CI UTILISÉS EN TANT QU'INHIBITEURS DE LA DIPEPTIDYLPEPTIDASE-IV DANS LE CADRE DU TRAITEMENT DU DIABÈTE
  申请人：MERCK SHARP & DOHME

  公开号：WO2011103256A1

  公开（公告）日：2011-08-25

  The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof 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.

  本发明涉及一种新型的取代氨基四氢硫代吡喃及其衍生物，其化学结构式为(I)，这些化合物是二肽基肽酶-IV酶的抑制剂，对于治疗或预防二肽基肽酶-IV酶参与的疾病非常有用，例如糖尿病，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] BICYCLO [2.2.2] OCTAN-1-YLCARBOXYLIC ACID COMPOUNDS AS DGAT-1 INHIBITORS<br/>[FR] COMPOSÉS D'ACIDE BICYCLO[2.2.2]OCTAN-1-YLCARBOXYLIQUE COMME INHIBITEURS DE LA DGAT-1
  申请人：INTERVET INT BV

  公开号：WO2013068328A1

  公开（公告）日：2013-05-16

  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.

  本文描述的是式(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。
• [EN] IMIDAZOLE DERIVATIVES<br/>[FR] DÉRIVÉS D'IMIDAZOLE
  申请人：MERCK SHARP & DOHME

  公开号：WO2013074387A1

  公开（公告）日：2013-05-23

  Disclosed herein are novel imidazole derivative compounds i.e., benzimidazole and aza-benzimidazole derivatives that act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperiipidemia, diabetes mellitus and obesity. Further disclosed are methods of treating various DGAT1 -related diseases, and the use of such imidazole compounds as described herein in the manufacture of a medicament for such treatment.

  本文披露了一种新型咪唑衍生物化合物，即苯并咪唑和氮杂苯并咪唑衍生物，其作为DGAT1抑制剂，并可用于预防、治疗或作为高脂血症、糖尿病和肥胖的治疗药物。进一步披露了治疗各种与DGAT1相关疾病的方法，以及将本文所述的咪唑化合物用于制造用于该治疗的药物的用途。