N-(1,2,3-benzothiadiazol-6-yl)-N'-phenylurea | 685123-50-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: N-(1,2,3-benzothiadiazol-6-yl)-N'-phenylurea
• 英文别名: 1-(1,2,3-benzothiadiazol-6-yl)-3-phenylurea
• CAS: 685123-50-6
• 化学式: C₁₃H₁₀N₄OS
• 分子量: 270.31
• InChiKey: UENZGSOUYQOBAA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  95.2
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• [EN] HRI ACTIVATORS USEFUL FOR THE TREATMENT OF CARDIOMETABOLIC DISEASES<br/>[FR] ACTIVATEURS DE HRI UTILES POUR LE TRAITEMENT DE MALADIES CARDIOMÉTABOLIQUES
  申请人：UNIV BARCELONA

  公开号：WO2018010856A1

  公开（公告）日：2018-01-18

  New compounds of formula (I) are provided,wherein: X is CH or N, preferably CH; n is 1-5, preferably 1-2; m is 0-5, preferably 1-2; and, when m is 2-5, two of the R2 radicals taken together with two adjacent carbons of the benzene ring can form a 5- or 6-membered heterocyclic ring fused with the benzene ring. Compounds (I) are heme-regulated inhibitor (HRI) activators and useful for the prevention or treatment of cardiometabolic diseases such as metabolic syndrome, obesity, insulin resistance, type 2 diabetes mellitus, non-alcoholic fatty liver disease, steatosis, non-alcoholic steatohepatitis, hypertension, dyslipidemia, atherosclerosis, and heart disease.

  提供了化合物（I）的新配方，其中：X为CH或N，优选为CH; n为1-5，优选为1-2; m为0-5，优选为1-2; 当m为2-5时，两个R2基团与苯环上相邻的两个碳原子共同形成一个与苯环融合的5-或6元杂环。化合物（I）是血红素调节酶（HRI）激活剂，可用于预防或治疗代谢综合征、肥胖症、胰岛素抵抗、2型糖尿病、非酒精性脂肪肝病、脂肪肝、非酒精性脂肪性肝炎、高血压、血脂异常、动脉粥样硬化和心脏疾病。
• N,N'-DIARYLUREA COMPOUNDS AND N,N'-DIARYLTHIOUREA COMPOUNDS AS INHIBITORS OF TRANSLATION INITIATION
  申请人：Aktas Bertal Huseyin

  公开号：US20120115915A1

  公开（公告）日：2012-05-10

  Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.

  本文提供了抑制翻译起始的组合物和方法。描述了使用N，N'-二芳基脲和/或N，N'-二芳基硫脲化合物治疗（1）细胞增生性疾病，（2）非增生性退行性疾病，（3）病毒感染和/或（4）与病毒感染相关的疾病的组合物、方法和试剂盒。
• N,N'-Diarylurea Compounds and N,N'-Diarylthiourea Compounds as Inhibitors of Translation Initiation
  申请人：President and Fellows of Harvard College

  公开号：US20160318857A1

  公开（公告）日：2016-11-03

  Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N′-diarylureas and/or N,N′-diarylthiourea compounds are described.
• HRI ACTIVATORS USEFUL FOR THE TREATMENT OF CARDIOMETABOLIC DISEASES
  申请人：UNIVERSITAT DE BARCELONA

  公开号：US20190322632A1

  公开（公告）日：2019-10-24

  Compounds of formula (I) include: X is CH or N, preferably CH; n is 1-5, preferably 1-2; m is 0-5, preferably 1-2; and, when m is 2-5, two of the R 2 radicals taken together with two adjacent carbons of the benzene ring can form a 5- or 6-membered heterocyclic ring fused with the benzene ring. Compounds of formula (I) are heme-regulated inhibitor (HRI) activators and useful for prevention or treatment of cardiometabolic diseases such as metabolic syndrome, obesity, insulin resistance, type 2 diabetes mellitus, non-alcoholic fatty liver disease, steatosis, non-alcoholic steatohepatitis, hypertension, dyslipidemia, atherosclerosis, and heart disease.
• US9421211B2
  申请人：——

  公开号：US9421211B2

  公开（公告）日：2016-08-23