2-(4-{2-tert-butyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl}phenyl)ethyl N-[(4-methylbenzene)sulfonyl]carbamate | 415906-01-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-(4-{2-tert-butyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl}phenyl)ethyl N-[(4-methylbenzene)sulfonyl]carbamate
• 英文别名: 2-[4-(2-tert-butyl-4,6-dimethylimidazo[4,5-c]pyridin-1-yl)phenyl]ethyl N-(4-methylphenyl)sulfonylcarbamate
• CAS: 415906-01-3
• 化学式: C₂₈H₃₂N₄O₄S
• 分子量: 520.652
• InChiKey: MHDGNBXHAQYYLD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  37
• 可旋转键数：
  8
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  112
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• EP4 INHIBITORS AND USE THEREOF
  申请人：Arrys Therapeutics, Inc.

  公开号：US20190314390A1

  公开（公告）日：2019-10-17

  The present invention provides use of an agent that inhibits EP4 activity and an immuno-oncology agent, or a composition thereof, for treatment of a cancer.

  本发明提供了一种使用抑制EP4活性的药剂和免疫肿瘤药剂或其组合物用于治疗癌症的方法。
• SELECTIVE EP4 RECEPTOR AGONISTIC SUBSTANCE FOR TREATMENT OF CANCER
  申请人：RaQualia Pharma Inc

  公开号：EP2422779A1

  公开（公告）日：2012-02-29

  This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.

  本发明提供了一种用于治疗癌症的药物，该药物可减少癌症的发生。本发明涉及一种对前列腺素 E2 受体（EP4 受体）具有抑制活性且由以下通式（I）、（II）、（III）或（IV）表示的化合物或其药学上可接受的盐、或包含该化合物或该盐的药物组合物用于制造治疗癌症的药物的用途。本发明涉及一种治疗癌症的方法，包括向人或动物施用本发明化合物或其药学上可接受的盐，或包含本发明化合物或盐的药物组合物。该化合物或其药学上可接受的盐，或该药物组合物可与一种或多种第二活性剂结合使用。
• SELECTIVE EP4 RECEPTOR ANTAGONISTIC SUBSTANCE FOR TREATMENT OF CANCER
  申请人：RaQualia Pharma Inc

  公开号：EP2965756A1

  公开（公告）日：2016-01-13

  This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV), or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.

  本发明提供了一种用于治疗癌症的药物，该药物可减少癌症的发生。本发明涉及一种对前列腺素 E2 受体（EP4 受体）具有抑制活性且由以下通式（I）、（II）、（III）或（IV）表示的化合物或其药学上可接受的盐、或包含该化合物或该盐的药物组合物用于制造治疗癌症的药物的用途。本发明涉及一种治疗癌症的方法，包括向人或动物施用本发明化合物或其药学上可接受的盐，或包含本发明化合物或盐的药物组合物。该化合物或其药学上可接受的盐或药物组合物可与一种或多种第二活性剂结合使用。
• Use of EP4 receptor antagonists in the treatment of cartilage disease
  申请人：AskAt Inc.

  公开号：US10391086B2

  公开（公告）日：2019-08-27

  The invention is a method of treating osteoarthritis or normalizing a condition of osteoarthritis comprising administering to an animal or a human in need thereof a therapeutically effective amount of 3-[2-(4-2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl}phenyl)ethyl]-1-[(4-methylbenzene)sulfonyl]urea or a pharmaceutically acceptable salt thereof.

  本发明是一种治疗骨关节炎或使骨关节炎病情正常化的方法，包括向需要的动物或人类施用治疗有效量的 3-[2-(4-2-乙基-4,6-二甲基-1H-咪唑并[4,5-c]吡啶-1-基}苯基)乙基]-1-[(4-甲基苯)磺酰基]脲或其药学上可接受的盐。
• Selective EP4 receptor antagonistic substance for treatment of cancer
  申请人：AskAt Inc.

  公开号：US10611761B2

  公开（公告）日：2020-04-07

  This invention provides a medicament for the treatment of cancer, which cause a reduction of cancer. This invention relates to use of a compound which has inhibitory activities against prostaglandin E2 receptor (EP4 receptor) and is represented by the following general formula (I), (II), (III), or (IV) or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt for the manufacture of a medicament for the treatment of cancer. The invention relates to a method for treatment of cancer comprising administering the compound or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising the compound or the salt to humans or animals. The compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition may be used in combination with one or more second active agents.

  本发明提供了一种用于治疗癌症的药物，该药物可减少癌症的发生。本发明涉及一种对前列腺素 E2 受体（EP4 受体）具有抑制活性且由以下通式（I）、（II）、（III）或（IV）表示的化合物或其药学上可接受的盐，或包含该化合物或盐的药物组合物的用途，用于制造治疗癌症的药物。本发明涉及一种治疗癌症的方法，包括向人或动物施用本发明化合物或其药学上可接受的盐，或包含本发明化合物或盐的药物组合物。该化合物或其药学上可接受的盐，或该药物组合物可与一种或多种第二活性剂结合使用。