安罗替尼盐酸盐 | 1360460-82-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 安罗替尼盐酸盐
• 中文别名: 盐酸安罗替尼
• 英文名称: Anlotinib dihydrochloride
• 英文别名: 1-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxyquinolin-7-yl]oxymethyl]cyclopropan-1-amine;dihydrochloride
• CAS: 1360460-82-7
• 化学式: C23H24Cl2FN3O3
• 分子量: 480.4
• InChiKey: UUAKQNIPIXQZFN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.68
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  82.4
• 氢给体数：
  4
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  1-(((4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl)oxy)methyl)cyclopropylbenzyl carbamate 生成 安罗替尼盐酸盐
  参考文献：
  名称：

  Spiro Substituted Compounds As Angiogenesis Inhibitors

  摘要：

  本发明涉及一种公式I的螺环（四碳）取代化合物，其制备方法，含有其作为活性成分的制药组合物，治疗与血管生成相关的疾病状态的方法，例如与蛋白酪氨酸激酶相关的癌症，以及它们作为药物用于在温血动物（如人类）中产生抑制酪氨酸激酶减少作用的用途。

  公开号：

  US20080227811A1

文献信息

• Spiro substituted compounds as angiogenesis inhibitors
  申请人：——

  公开号：US08148532B2

  公开（公告）日：2012-04-03

  The present invention relates to compound of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.

  本发明涉及式I化合物，其制备方法，含其作为活性成分的制药组合物，用于治疗与血管生成有关的疾病状态的方法，例如与蛋白酪氨酸激酶相关的癌症，以及它们作为药物用于在温血动物，例如人类中产生酪氨酸激酶抑制作用的制剂。
• Spiro Substituted Compounds As Angiogenesis Inhibitors
  申请人：Chen Guoqing Paul

  公开号：US20080227811A1

  公开（公告）日：2008-09-18

  The present invention relates to spiro (tetracarbon) substituted compound of Formula I, processes for their preparation, pharmaceutical compositions containing them as active ingredient, methods for the treatment of disease states associated with angiogenesis, such as cancers associated with protein tyrosine kinases, to their use as medicaments for use in the production of inhibition of tyrosine kinases reducing effects in warm-blooded animals such as humans.

  本发明涉及一种公式I的螺环（四碳）取代化合物，其制备方法，含有其作为活性成分的制药组合物，治疗与血管生成相关的疾病状态的方法，例如与蛋白酪氨酸激酶相关的癌症，以及它们作为药物用于在温血动物（如人类）中产生抑制酪氨酸激酶减少作用的用途。
• METHOD FOR TREATING TUMOUR, PHARMACEUTICAL COMPOSITION AND MEDICINE BOX KIT
  申请人：Chia Tai Tianqing Pharmaceutical Group Co.,Ltd

  公开号：EP3153169A1

  公开（公告）日：2017-04-12

  The present invention provides 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopro-pylamine used for combating a tumor. Specially, the present invention refers to method for treating tumor, pharmaceutical composition and medicinal kit related to the described compound. Administrating the compound with a suitable dosage regimen can not only make the patient's plasma concentration maintain the level of 100 ng/ml or lower, but also achieve effects of treatments and obtain benefits for various tumours.

  本发明提供了用于防治肿瘤的 1-[[[4-(4-氟-2-甲基-1H-吲哚-5-基)氧基-6-甲氧基喹啉-7-基]氧基]甲基]环丙基胺。具体而言，本发明是指与所述化合物相关的治疗肿瘤的方法、药物组合物和药包。以合适的剂量方案服用该化合物，不仅能使患者血浆浓度维持在 100 ng/ml 或更低水平，还能达到治疗效果，对各种肿瘤均有益处。
• METHODS AND USES OF QUINOLINE DERIVATIVES IN THE TREATMENT OF SOFT TISSUE SARCOMAS AND PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF SAME
  申请人：Chia Tai Tianqing Pharmaceutical Group Co.,Ltd

  公开号：EP3153170A1

  公开（公告）日：2017-04-12

  The present invention addresses methods and uses of quinoline derivatives in the treatment of tumours and pharmaceutical compositions for treatment of same. Specifically, the present invention involves a method and applications for the use of the quinoline derivative 1-[[[4-(4-fluoro-2-methyl-1H-indol-5-yl)oxy-6-methoxyquinolin-7-yl]oxy]methyl]cyclopropylamine in the treatment of soft tissue sarcomas and pharmaceutical compositions for treatment of same.

  本发明涉及喹啉衍生物治疗肿瘤的方法和用途以及治疗肿瘤的药物组合物。具体而言，本发明涉及一种喹啉衍生物 1-[[[4-(4-氟-2-甲基-1H-吲哚-5-基)氧基-6-甲氧基喹啉-7-基]氧基]甲基]环丙胺治疗软组织肉瘤的方法和应用以及治疗软组织肉瘤的药物组合物。
• QUINOLINE DERIVATIVE AGAINST NON-SMALL CELL LUNG CANCER
  申请人：Chai Tai Tianqing Pharmaceutical Group Co., Ltd.

  公开号：EP3231797A1

  公开（公告）日：2017-10-18

  Provided in the present application is a quinoline derivative against non-small cell lung cancer. 1 - [[[4-(4-fluoro-2-methyl-1H-indole-5-yl)oxy-6-methoxyquinoline-7-yl]oxy]methyl]cyclopropylamine or a pharmaceutically acceptable salt thereof as provided in the present application can be used for treating non-small cell lung cancer, and with respect to placebos, can significantly increase the progression-free survival of a patient with non-small cell lung cancer. The 1- [[[4-(4-fluoro-2-methyl-1H-indole-5-yl)oxy-6-methoxyquinoline-7-yl]oxy]methyl]cyclopropylamine or a pharmaceutically acceptable salt thereof as provided in the present application can be used for treating lung adenocarcinoma, and with respect to placebos, can significantly increase the progression-free survival of a patient with lung adenocarcinoma.

  本申请提供了一种防治非小细胞肺癌的喹啉衍生物。本申请提供的1-[[[4-(4-氟-2-甲基-1H-吲哚-5-基)氧基-6-甲氧基喹啉-7-基]氧基]甲基]环丙胺或其药学上可接受的盐可用于治疗非小细胞肺癌，与安慰剂相比，可显著提高非小细胞肺癌患者的无进展生存期。本申请提供的1-[[[4-(4-氟-2-甲基-1H-吲哚-5-基)氧基-6-甲氧基喹啉-7-基]氧基]甲基]环丙胺或其药学上可接受的盐可用于治疗肺腺癌，相对于安慰剂，可显著提高肺腺癌患者的无进展生存期。