N-[5-[6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-yl]oxypyridin-2-yl]-2,5-dioxo-1-phenyl-7,8-dihydro-6H-quinoline-3-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: N-[5-[6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinolin-4-yl]oxypyridin-2-yl]-2,5-dioxo-1-phenyl-7,8-dihydro-6H-quinoline-3-carboxamide
• 化学式: C₃₈H₃₇N₅O₆
• 分子量: 659.7
• InChiKey: HJHCUWIEHYPGCH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  49
• 可旋转键数：
  11
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  123
• 氢给体数：
  1
• 氢受体数：
  9

文献信息

• QUINOLINE DERIVATIVE
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：US20160168121A1

  公开（公告）日：2016-06-16

  A compound represented by general formula (I) has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases.

  通式（I）所代表的化合物通过引入一种独特的双环结构，在其中饱和碳环与吡啶酮环融合，具有强烈的Axl抑制活性，并可作为Axl相关疾病的治疗剂，例如急性髓性白血病、黑色素瘤、乳腺癌、胰腺癌和胶质瘤、肾脏疾病、免疫系统疾病和循环系统疾病的治疗剂。
• THERAPEUTIC AGENT FOR SOLID CANCERS, WHICH CONTAINS AXL INHIBITOR AS ACTIVE INGREDIENT
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP3695839A1

  公开（公告）日：2020-08-19

  The present invention addresses the problem of finding an effective method for treating solid cancers and providing a pharmaceutical product therefor. The present invention provides a therapeutic agent for solid cancers, which contains N-5-[(6, 7-dimethoxy-4-quinolinyl)oxy]-2-pyridinyl}-2, 5- dioxo-1-phenyl-1, 2, 5, 6, 7, 8-hexahydro-3-quinolinecarboxamide, a pharmaceutically acceptable salt thereof, or a hydrate of the compound or the salt as an active ingredient, and which is characterized by being administered in combination with osimertinib or a pharmaceutically acceptable salt thereof. The combination of the present invention exerts a strong antitumor effect, and is therefore useful for treatment of solid cancers.

  本发明要解决的问题是找到一种治疗实体癌的有效方法，并为此提供一种药物产品。本发明提供了一种治疗实体癌的药物，其含有N-5-[(6，7-二甲氧基-4-喹啉基)氧基]-2-吡啶基}-2，5-二氧代-1-苯基-1，2，5，6，7，8-六氢-3-喹啉甲酰胺、其药学上可接受的盐或该化合物或该盐的水合物作为活性成分，其特征在于与奥希替尼或其药学上可接受的盐联合给药。本发明的组合物具有很强的抗肿瘤作用，因此可用于治疗实体瘤。
• PHARMACEUTICAL FOR CANCER TREATMENT INCLUDING AX1 INHIBITOR AS AN EFFECTIVE COMPONENT
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP3673907A1

  公开（公告）日：2020-07-01

  The present invention addresses the problem of identifying an effective method for curing cancer and providing a pharmaceutical product for cancer treatment. Provided is a pharmaceutical for cancer treatment, characterized by being administered as the combination of an Axl inhibitor and an anti-cancer agent (e.g., cytotoxic anti-cancer agent, molecularly targeted drug, and anti-CTLA-4 antibody), the Axl inhibitor including a compound represented by general formula (I) (in the formula, all symbols are as defined in the description), a salt thereof, a solvate thereof, an N-oxide substance thereof, or a prodrug of any of them. This combination exhibits a strong anti-tumor effect and is therefore useful for treatment of hematological cancer and/or solid cancer.

  本发明要解决的问题是确定一种有效的癌症治疗方法，并提供一种癌症治疗药物产品。本发明提供了一种用于癌症治疗的药品，其特征在于以Axl抑制剂和抗癌剂（如细胞毒性抗癌剂、分子靶向药物和抗CTLA-4抗体）的组合给药，Axl抑制剂包括通式（I）所代表的化合物（式中，所有符号如描述中所定义）、其盐、其溶液、其N-氧化物或它们中任何一种的原药。这种组合物具有很强的抗肿瘤作用，因此可用于治疗血液肿瘤和/或实体肿瘤。
• Quinoline derivative
  申请人：ONO PHARMACEUTICAL CO., LTD.

  公开号：US10208022B2

  公开（公告）日：2019-02-19

  A compound represented by general formula (I) has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases

  通式(I)代表的化合物通过引入饱和碳环与吡啶酮环融合的独特双环结构，具有很强的 Axl 抑制活性，可作为 Axl 相关疾病的治疗剂，例如急性髓性白血病、黑色素瘤、乳腺癌、胰腺癌和胶质瘤等癌症、肾脏疾病、免疫系统疾病和循环系统疾病的治疗剂。
• DRUG FOR CANCER THERAPY CHARACTERIZED BY ADMINISTERING COMBINATION BETWEEN AXL INHIBITOR AND IMMUNE CHECKPOINT INHIBITOR
  申请人：ONO Pharmaceutical Co., Ltd.

  公开号：EP3421039B1

  公开（公告）日：2021-10-06