ethyl 5-morpholino-2-(pyridin-3-yl)thiazole-4-carboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: ethyl 5-morpholino-2-(pyridin-3-yl)thiazole-4-carboxylate
• 英文别名: Ethyl 5-morpholino-2-(pyridin-3-yl)thiazole-4-carboxylate；ethyl 5-morpholin-4-yl-2-pyridin-3-yl-1,3-thiazole-4-carboxylate
• 化学式: C₁₅H₁₇N₃O₃S
• 分子量: 319.384
• InChiKey: AJGUEJCYQSHWND-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  22
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  92.8
• 氢给体数：
  0
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  5-溴噻唑-4-甲酸乙酯 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 N-溴代丁二酰亚胺(NBS) 、 caesium carbonate 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 反应 5.0h， 生成 ethyl 5-morpholino-2-(pyridin-3-yl)thiazole-4-carboxylate
  参考文献：
  名称：

  [EN] AZEPIN-2-ONE DERIVATIVES AS RSV INHIBITORS
  [FR] DÉRIVÉS D'AZÉPIN-2-ONE EN TANT QU'INHIBITEURS DU VRS

  摘要：

  本发明公开了化合物的结构式(I)，或其药学上可接受的盐、酯或前药：这些化合物抑制呼吸道合胞病毒(RSV)。本发明还涉及包含上述化合物的药物组合物，用于治疗患有RSV感染的受试者。该发明还涉及通过给予包含本发明化合物的药物组合物来治疗受试者的RSV感染的方法。

  公开号：

  WO2019094920A1

文献信息

• [EN] ARYLDIAZEPINE DERIVATIVES AS RSV INHIBITORS<br/>[FR] DÉRIVÉS D'ARYLDIAZÉPINE UTILISÉS EN TANT QU'INHIBITEURS DU VRS
  申请人：ENANTA PHARM INC

  公开号：WO2018226801A1

  公开（公告）日：2018-12-13

  The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof, which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

  本发明公开了式（I）的化合物，以及其药学上可接受的盐、酯或前药，其抑制呼吸道合胞病毒（RSV）。本发明还涉及包含上述化合物的药物组合物，用于治疗患有RSV感染的受试者。该发明还涉及通过给予包含本发明化合物的药物组合物来治疗受试者的RSV感染的方法。
• Azepin-2-one derivatives as RSV inhibitors
  申请人：Enanta Pharmaceuticals, Inc.

  公开号：US10647711B2

  公开（公告）日：2020-05-12

  The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

  本发明公开了式（I）化合物或其药学上可接受的盐、酯或原药： 其可抑制呼吸道合胞病毒（RSV）。本发明进一步涉及包含上述化合物的药物组合物，用于给受 RSV 感染的患者用药。本发明还涉及通过施用包含本发明化合物的药物组合物治疗受试者 RSV 感染的方法。
• Aryldiazepine derivatives as RSV inhibitors
  申请人：Enanta Pharmaceuticals, Inc.

  公开号：US10752598B2

  公开（公告）日：2020-08-25

  The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

  本发明公开了式（I）化合物及其药学上可接受的盐、酯或原药： 它们可抑制呼吸道合胞病毒（RSV）。本发明进一步涉及包含上述化合物的药物组合物，用于给受 RSV 感染的患者用药。本发明还涉及通过施用包含本发明化合物的药物组合物治疗受试者 RSV 感染的方法。
• ARYLDIAZEPINE DERIVATIVES AS RSV INHIBITORS
  申请人：Enanta Pharmaceuticals, Inc.

  公开号：US20180354912A1

  公开（公告）日：2018-12-13

  The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
• AZEPIN-2-ONE DERIVATIVES AS RSV INHIBITORS
  申请人：Enanta Pharmaceuticals, Inc.

  公开号：US20190152968A1

  公开（公告）日：2019-05-23

  The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from RSV infection. The invention also relates to methods of treating an RSV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.