7-(diethylamino)-3-{2-[(2-methoxyphenyl)amino]-1,3-thiazol-4-yl}-2H-chromen-2-one

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 香豆素及其衍生物
• 英文名称: 7-(diethylamino)-3-{2-[(2-methoxyphenyl)amino]-1,3-thiazol-4-yl}-2H-chromen-2-one
• 英文别名: 7-(diethylamino)-3-[2-(2-methoxyanilino)-1,3-thiazol-4-yl]chromen-2-one
• 化学式: C₂₃H₂₃N₃O₃S
• 分子量: 421.5
• InChiKey: IKTOYTYOVKDFMN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.3
• 重原子数：
  30
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  91.9
• 氢给体数：
  1
• 氢受体数：
  7

文献信息

• COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING HYPERPROLIFERATIVE DISEASES
  申请人：DISCOVERYBIOMED, INC.

  公开号：US20160038475A1

  公开（公告）日：2016-02-11

  Coumarin derivative compounds and methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The methods include administering to a subject a compound as described herein. Also provided are methods for inhibiting the interaction between two or more heat shock protein chaperones in a cell.

  本发明提供了香豆素衍生物化合物及其治疗过度增殖性疾病（如癌症、多囊肾病和不同组织的纤维化（例如特发性肺纤维化））的方法。该方法包括向受试者施用本文所述的化合物。此外，本发明还提供了一种抑制细胞内两个或更多热休克蛋白分子伴侣相互作用的方法。
• COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING CYSTIC FIBROSIS, CHRONIC OBSTRUCTIVE PULMONARY DISEASE, AND MISFOLDED PROTEIN DISORDERS
  申请人：DISCOVERYBIOMED, INC.

  公开号：US20160024065A1

  公开（公告）日：2016-01-28

  Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis and chronic obstructive pulmonary diseases). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.

  提供了一种能够有效拯救卤离子外流、delF508-CFTR蛋白质加工和细胞顶部功能氯离子传输的小说CFTR校正化合物。还提供了治疗蛋白质折叠失调（例如，囊性纤维化和慢性阻塞性肺疾病）的方法。该方法包括给予CFTR校正化合物或其药学上可接受的盐或前药。还提供了在细胞中拯救卤离子外流、纠正细胞中delF508-CFTR蛋白质处理缺陷和纠正功能性delF508-CFTR氯通道的方法。
• Coumarin derivatives and methods of use in treating hyperproliferative diseases
  申请人：DISCOVERYBIOMED, INC.

  公开号：US10369145B2

  公开（公告）日：2019-08-06

  Coumarin derivative compounds and methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The methods include administering to a subject a compound as described herein. Also provided are methods for inhibiting the interaction between two or more heat shock protein chaperones in a cell.

  提供了香豆素衍生物化合物和治疗过度增殖性疾病的方法，如癌症、多囊肾和不同组织的纤维化（如特发性肺纤维化）。这些方法包括向受试者施用本文所述的化合物。还提供了抑制细胞中两种或多种热休克蛋白伴侣之间相互作用的方法。
• US9815825B2
  申请人：——

  公开号：US9815825B2

  公开（公告）日：2017-11-14
• [EN] COUMARIN DERIVATIVES AND METHODS OF USE IN TREATING CYSTIC FIBROSIS, CHRONIC OBSTRUCTIVE PULMONARY DISEASE, AND MISFOLDED PROTEIN DISORDERS<br/>[FR] DÉRIVÉS DE COUMARINE ET LEURS MÉTHODES D'UTILISATION DANS LE TRAITEMENT DE LA FIBROSE KYSTIQUE, DE LA BRONCHOPNEUMOPATHIE CHRONIQUE OBSTRUCTIVE ET DES TROUBLES LIÉS À DES PROTÉINES MAL REPLIÉES
  申请人：DISCOVERYBIOMED INC

  公开号：WO2014152213A2

  公开（公告）日：2014-09-25

  Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis and chronic obstructive pulmonary diseases). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.