N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-3-氟苯基]-4-乙氧基-1-(4-氟-2-甲基苯基)-1H-吡唑-3-甲酰胺 | 1361030-48-9

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-[4-[(6,7-二甲氧基-4-喹啉基)氧基]-3-氟苯基]-4-乙氧基-1-(4-氟-2-甲基苯基)-1H-吡唑-3-甲酰胺
• 中文别名: 化合物LDC1267；LDC1267游离态
• 英文名称: LDC1267
• 英文别名: N-[4-(6,7-dimethoxyquinolin-4-yl)oxy-3-fluorophenyl]-4-ethoxy-1-(4-fluoro-2-methylphenyl)pyrazole-3-carboxamide
• CAS: 1361030-48-9
• 化学式: C₃₀H₂₆F₂N₄O₅
• 分子量: 560.557
• InChiKey: ISPBCAXOSOLFME-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.7
• 重原子数：
  41
• 可旋转键数：
  9
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  96.7
• 氢给体数：
  1
• 氢受体数：
  9

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335

文献信息

• [EN] THERAPUETIC USES OF SELECTED PYRIMIDINE COMPOUNDS WITH ANTI-MER TYROSINE KINASE ACTIVITY<br/>[FR] UTILISATIONS THÉRAPEUTIQUES DE COMPOSÉS SÉLECTIONNÉS DE PYRIMIDINE AYANT UNE ACTIVITÉ TYROSINE KINASE ANTIMÈRE
  申请人：UNIV NORTH CAROLINA

  公开号：WO2015157127A1

  公开（公告）日：2015-10-15

  Uses of pyrimidines with anti-Mer tyrosine kinase activity as anti-infective agents, immunostimulatory and immunomodulatory agents, anti-cancer agents (including against MerTK -/- tumors and ITD and TKD mutant forms of Acute Myeloid Leukemia (AML)), and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms.

  将嘧啶类化合物用作抗Mer酪氨酸激酶活性的抗感染剂、免疫刺激剂和免疫调节剂、抗癌剂（包括对MerTK -/-肿瘤和急性髓样白血病（AML）的ITD和TKD突变形式），以及作为辅助剂与化疗、放疗或其他肿瘤标准治疗联合使用。
• Pharmaceutically active compounds as Axl inhibitors
  申请人：Lead Discovery Center GmbH

  公开号：EP2423208A1

  公开（公告）日：2012-02-29

  The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

  本发明涉及一般式(I)的1-氮杂环-2-羧酰胺及/或其药学上可接受的盐，这些衍生物作为药理活性剂的用途，特别用于治疗和/或预防Axl受体酪氨酸激酶亚家族引起的疾病，包括癌症和原发性肿瘤转移，以及含有至少一种上述1-氮杂环-2-羧酰胺衍生物和/或其药学上可接受的盐的药物组合物。
• PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS
  申请人：Schultz-Fademrecht Carsten

  公开号：US20140018365A1

  公开（公告）日：2014-01-16

  The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

  本发明涉及1-氮杂环-2-羧酰胺和/或其药学上可接受的盐，这些衍生物被用作药物活性剂，特别用于治疗和/或预防Axl受体酪氨酸激酶亚家族引起的疾病，包括癌症和原发性肿瘤转移，以及含有至少一种所述的1-氮杂环-2-羧酰胺衍生物和/或其药学上可接受的盐的制药组合物。
• THERAPEUTIC USES OF SELECTED PYRAZOLOPYRIMIDINE COMPOUNDS WITH ANTI-MER TYROSINE KINASE ACTIVITY
  申请人：The University of North Carolina at Chapel Hill

  公开号：US20150290212A1

  公开（公告）日：2015-10-15

  Pyrazolopyrimidine compounds, methods of use, and processes for making compounds with anti-Mer tyrosine kinase activity comprising Formula I, II, III, IV, or a pharmaceutically acceptable composition, salt, isotopic analog, or prodrug thereof, are provided. The pyrazolopyrimidine compounds described herein have Mer tyrosine kinase (MerTK) inhibitory activity and are useful as anti-infective agents, immunostimulatory and immunomodulatory agents, anti-cancer agents (including against MerTK −/− tumors and ITD and TKD mutant forms of Acute Myeloid Leukemia (AML)), and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms.

  本文提供了具有抗Mer酪氨酸激酶活性的化合物公式I、II、III、IV或其药学上可接受的组合物、盐、同位素类似物或前药的使用方法和制备过程。这些在此处描述的吡唑并嘧啶化合物具有Mer酪氨酸激酶(MerTK)抑制活性，并且可用作抗感染剂、免疫刺激和免疫调节剂、抗癌剂(包括对MerTK -/-肿瘤和急性髓细胞白血病的ITD和TKD突变体)以及作为伴随化疗、放疗或其他肿瘤标准治疗的辅助剂。
• THERAPEUTIC USES OF SELECTED PYRROLOPYRIMIDINE COMPOUNDS WITH ANTI-MER TYROSINE KINASE ACTIVITY
  申请人：The University of North Carolina at Chapel Hill

  公开号：US20150290197A1

  公开（公告）日：2015-10-15

  Uses of pyrrolopyrimidines with anti-Mer tyrosine kinase activity as anti-infective agents, immunostimulatory and immunomodulatory agents, anti-cancer agents (including against MerTK−/− tumors and ITD and TKD mutant forms of Acute Myeloid Leukemia (AML)), and as adjunctive agents in combination with chemotherapeutic, radiation or other standard of care for neoplasms.

  使用具有抗Mer酪氨酸激酶活性的吡咯吡嘧啶作为抗感染剂、免疫刺激剂和免疫调节剂，抗癌剂（包括对MerTK-/-肿瘤和急性髓细胞白血病（AML）的ITD和TKD突变体），以及作为辅助剂与化疗、放疗或其他标准治疗方法结合治疗肿瘤。