Tivozanib hydrochloride | 682745-43-3

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: Tivozanib hydrochloride
• 英文别名: N-[2-chloro-4-(6,7-dimethoxyquinolin-4-yloxy)phenyl]-N’-(5-methylisoxazol-3-yl)urea hydrochloride；Tivozanib hydrochloride anhydrous；1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea;hydrochloride
• CAS: 682745-43-3
• 化学式: C₂₂H₁₉ClN₄O₅*ClH
• 分子量: 491.331
• InChiKey: NVOQFPILSQNESS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.06
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  108
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  N-[2-氯-4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基]-N’-(5-甲基-3-异恶唑基)脲 在 盐酸 作用下， 以 丙醇 、 DMF (N,N-dimethyl-formamide) 、 水 为溶剂， 反应 1.0h， 以83.8%的产率得到Tivozanib hydrochloride
  参考文献：
  名称：

  N-{2-CHLORO-4-[(6,7-DIMETHOXY-4-QUINOLYL)OXY]PHENYL}-N'-(5-METHYL-3-ISOXAZOLYL)UREA SALT IN CRYSTALLINE FORM

  摘要：

  公开号：

  EP1559715B1

文献信息

• N-{2-chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}-n'-(5-methyl-3-isoxazolyl)urea salt in crystalline form
  申请人：Matsunaga Naoki

  公开号：US20060052415A1

  公开（公告）日：2006-03-09

  The present invention provides a crystal of a pharmaceutically acceptable salt of N-2-chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}-N′-(5-methyl-3-isoxazolyl) urea. This crystal of salt is usable for the therapy of a disease selected from the group consisting of tumors, diabetic retinopathy, chronic rheumatism, psoriasis, atherosclerosis, Kaposi's sarcoma, and exudation type age-related maculopathy, and has characteristics suitable for applications of oral pharmaceutical preparations.

  本发明提供了一种药用可接受盐的晶体，其化学名称为N-2-氯-4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基}-N'-(5-甲基-3-异噁唑基)脲。该盐晶体可用于治疗肿瘤、糖尿病视网膜病变、慢性风湿病、银屑病、动脉硬化、卡波西肉瘤和渗出型老年性黄斑变性等疾病，并具有适用于口服药物制剂的特性。
• N-{2-chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}-n′-(5-methyl-3-isoxazolyl)urea salt in crystalline form
  申请人：Kirin Beer Kabushiki Kaisha

  公开号：US07166722B2

  公开（公告）日：2007-01-23

  The present invention provides a crystal of a pharmaceutically acceptable salt of N-2-chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}-N′-(5-methyl-3-isoxazolyl) urea. This crystal of salt is usable for the therapy of a disease selected from the group consisting of tumors, diabetic retinopathy, chronic rheumatism, psoriasis, atherosclerosis, Kaposi's sarcoma, and exudation type age-related maculopathy, and has characteristics suitable for applications of oral pharmaceutical preparations.

  本发明提供了一种药用可接受盐的晶体，该盐为N-2-氯-4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基}-N'-(5-甲基-3-异噁唑基)脲的盐晶体。该盐晶体可用于治疗肿瘤、糖尿病视网膜病变、慢性风湿病、银屑病、动脉粥样硬化、卡波西肉瘤和渗出性老年性黄斑变性等疾病，并具有适用于口服药物制剂的特性。
• N-[2-CHLORO-4-(6,7-DIMETHOXY-4-QUINOLYL)OXY]PHENYL]-N'-(5-METHYL-3-ISOXAZOLYL)UREA SALT IN CRYSTALLINE FORM
  申请人：KIRIN BEER KABUSHIKI KAISHA

  公开号：EP1559715A1

  公开（公告）日：2005-08-03

  The present invention provides a crystal of a pharmaceutically acceptable salt of N-2-chloro-4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl}-N'-(5-m ethyl-3-isoxazolyl) urea. This crystal of salt is usable for the therapy of a disease selected from the group consisting of tumors, diabetic retinopathy, chronic rheumatism, psoriasis, atherosclerosis, Kaposi's sarcoma, and exudation type age-related maculopathy, and has characteristics suitable for applications of oral pharmaceutical preparations.

  本发明提供了一种N-2-氯-4-[(6,7-二甲氧基-4-喹啉基)氧基]苯基}-N'-(5-甲基乙基-3-异恶唑基)脲的药学上可接受的盐的晶体。这种晶体盐可用于治疗选自肿瘤、糖尿病视网膜病变、慢性风湿病、银屑病、动脉粥样硬化、卡波西肉瘤和渗出型老年性黄斑病变等疾病，并具有适合口服药物制剂应用的特性。
• MEDICINAL COMPOSITION
  申请人：Kyowa Hakko Kirin Co., Ltd.

  公开号：EP3513809A1

  公开（公告）日：2019-07-24

  The present invention relates to a therapeutic agent for an ophthalmic disease comprising a vascular endothelial growth factor (VEGF) receptor inhibitor or an epidermal growth factor (EGF) receptor inhibitor in a nanoparticle form, having a property to be retained in a posterior eye tissue when systemically administered.

  本发明涉及一种用于眼科疾病的治疗剂，该治疗剂包含一种纳米颗粒形式的血管内皮生长因子（VEGF）受体抑制剂或表皮生长因子（EGF）受体抑制剂，在全身给药时具有保留在眼球后组织中的特性。
• Pharmaceutical composition
  申请人：Kyowa Kirin Co., Ltd.

  公开号：US10894043B2

  公开（公告）日：2021-01-19

  The present invention relates to a therapeutic agent for an ophthalmic disease comprising a vascular endothelial growth factor (VEGF) receptor inhibitor or an epidermal growth factor (EGF) receptor inhibitor in a nanoparticle form, having a property to be retained in a posterior eye tissue when systemically administered.

  本发明涉及一种用于眼科疾病的治疗剂，该治疗剂包含一种纳米颗粒形式的血管内皮生长因子（VEGF）受体抑制剂或表皮生长因子（EGF）受体抑制剂，在全身给药时具有保留在眼球后组织中的特性。