1-(2-{4-[5-(dimethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]phenoxy}-5-pyrimidinyl)-3-[2'-methyl-4-(trifluoromethyl)-2-biphenylyl]urea

• 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: 1-(2-{4-[5-(dimethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]phenoxy}-5-pyrimidinyl)-3-[2'-methyl-4-(trifluoromethyl)-2-biphenylyl]urea
• 英文别名: N'-[2-[4-[5-(dimethylamino)pyrazolo[1,5-a]pyrimidin-3-yl]phenoxy]pyrimidin-5-yl]-N-[2-(2-methylphenyl)-5-(trifluoromethyl)phenyl]carbamimidic acid
• 化学式: C₃₃H₂₇F₃N₈O₂
• 分子量: 624.625
• InChiKey: UYWQHKWNLPQAMN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6
• 重原子数：
  46
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  110
• 氢给体数：
  2
• 氢受体数：
  10

文献信息

• Trk-INHIBITING COMPOUND
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：US20160000783A1

  公开（公告）日：2016-01-07

  The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

  本发明提供了一种药物，其中包含具有Trk抑制活性的化合物作为预防和/或治疗Trk相关疾病的活性成分，例如疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或查加斯病。通式（I）所表示的化合物，其中所有符号都表示规范中描述的相同含义，其盐，N-氧化物，溶剂化物或前药是作为具有Trk抑制活性的药物成分在预防和/或治疗疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或查加斯病等疾病中有用的。
• TRK-INHIBITING COMPOUND
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP3459935A1

  公开（公告）日：2019-03-27

  The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

  本发明提供了一种含有具有 Trk 抑制活性的化合物的药物，作为预防和/或治疗 Trk 相关疾病（如疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或南美锥虫病）的活性成分。通式 (I) 所代表的化合物： 其中所有符号代表的含义与说明书中描述的相同、 其盐、其 N-氧化物、其溶解物或其原药可用作具有 Trk 抑制活性的药物成分，用于预防和/或治疗疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或南美锥虫病等疾病。
• METHOD FOR TREATING CANCER BY COMBINATION OF Trk INHIBITOR AND KINASE INHIBITOR
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP3679932A1

  公开（公告）日：2020-07-15

  An object of the present invention is to provide a combination therapy in which an antitumor effect is enhanced as compared to when a Trk inhibitor or any of various kinase inhibitors is administered alone. A Trk inhibitor, particularly, a compound represented by General Formula (I): wherein all symbols have the same meanings as symbols described in this specification, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof is useful as an active ingredient of a cancer therapeutic agent used in combination with one or more drugs selected from the group consisting of an MEK inhibitor, a CDK4/6 inhibitor, an EGFR inhibitor and a JAK1/2 inhibitor.

  本发明的目的是提供一种联合疗法，与单独使用Trk抑制剂或各种激酶抑制剂中的任何一种相比，该疗法的抗肿瘤效果更强。Trk抑制剂，特别是通式(I)所代表的化合物： 其中所有符号与本说明书中描述的符号具有相同的含义，其盐、其 N-氧化物、其溶液或其原药可作为癌症治疗剂的活性成分，与选自 MEK 抑制剂、CDK4/6 抑制剂、表皮生长因子受体抑制剂和 JAK1/2 抑制剂组成的组中的一种或多种药物联合使用。
• UREA DERIVATIVES AS TRK-INHIBITING COMPOUNDS
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP3800183A1

  公开（公告）日：2021-04-07

  The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

  本发明提供了一种含有具有 Trk 抑制活性的化合物的药物，作为预防和/或治疗 Trk 相关疾病（如疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或南美锥虫病）的活性成分。通式 (I) 所代表的化合物： 其中所有符号代表的含义与说明书中描述的相同、 其盐、其 N-氧化物、其溶解物或其原药可用作具有 Trk 抑制活性的药物成分，用于预防和/或治疗疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或南美锥虫病等疾病。
• Trk-inhibiting compound
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：US10300060B2

  公开（公告）日：2019-05-28

  The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.

  本发明提供了一种含有具有Trk-抑制活性的化合物的药物，作为预防和/或治疗Trk相关疾病（如疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或南美锥虫病）的活性成分。通式(I)（其中所有符号代表与说明书所述相同的含义）代表的化合物、其盐、其 N-氧化物、其溶解物或其原药可作为具有 Trk 抑制活性的药物成分，用于预防和/或治疗疼痛、瘙痒、下尿路功能障碍、哮喘、过敏性鼻炎、炎症性肠病或南美锥虫病等疾病。