4-(2-(1H-吡唑-4-基)吡啶-4-氧基)-2-氟苯胺 | 1020173-13-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: 4-(2-(1H-吡唑-4-基)吡啶-4-氧基)-2-氟苯胺
• 英文名称: 4-(2-(1H-pyrazol-4-yl)pyridin-4-yloxy)-2-fluorobenzenamine
• 英文别名: 2-fluoro-4-[2-(1H-pyrazol-4-yl)pyridin-4-yl]oxyaniline
• CAS: 1020173-13-0
• 化学式: C₁₄H₁₁FN₄O
• 分子量: 270.266
• InChiKey: HQUOIRHAAZBOKP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  20
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  76.8
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  4-吡唑硼酸频哪醇酯 、 4-((2-chloropyridin-4-yl)oxy)-2-fluoroaniline 在 四(三苯基膦)钯 caesium carbonate 作用下， 以 水 、 N,N-二甲基甲酰胺 为溶剂， 以83%的产率得到4-(2-(1H-吡唑-4-基)吡啶-4-氧基)-2-氟苯胺
  参考文献：
  名称：

  KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES

  摘要：

  本发明涉及一种在治疗高增殖性疾病和哺乳动物癌症，尤其是人类癌症方面有用的新化合物。该发明还涉及调节激酶活性的方法、药物组合物以及治疗个体的方法，包括或使用这些化合物。优选的化合物是在公式Ia-Iww中列出的活性小分子。

  公开号：

  US20080090856A1

文献信息

• KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES
  申请人：Flynn L. Daniel

  公开号：US20080090856A1

  公开（公告）日：2008-04-17

  The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.

  本发明涉及一种在治疗高增殖性疾病和哺乳动物癌症，尤其是人类癌症方面有用的新化合物。该发明还涉及调节激酶活性的方法、药物组合物以及治疗个体的方法，包括或使用这些化合物。优选的化合物是在公式Ia-Iww中列出的活性小分子。
• KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES
  申请人：Flynn Daniel L.

  公开号：US20080269267A1

  公开（公告）日：2008-10-30

  Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Met kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by a Raf kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

  本发明的化合物可用于治疗哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑色素瘤、实体肿瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、肝癌、宫颈癌、原发肿瘤部位的转移、骨髓增生性疾病、慢性髓细胞白血病、白血病、乳头状甲状腺癌、非小细胞肺癌、间皮瘤、高嗜酸性综合征、胃肠道间质瘤、结肠癌、眼部疾病，其特征是过度增殖导致失明，包括各种视网膜病变、糖尿病性视网膜病变、类风湿性关节炎、哮喘、慢性阻塞性肺疾病、肥大细胞增多症、肥大细胞白血病、由c-Abl激酶引起的疾病、其致癌形式、异常融合蛋白和多态体，由c-Kit激酶引起的疾病、其致癌形式、异常融合蛋白和多态体，由c-Met激酶引起的疾病、其致癌形式、异常融合蛋白和多态体，或由Raf激酶引起的疾病、其致癌形式、异常融合蛋白和多态体。
• Kinase Inhibitors Useful for the Treatment of Myleoproliferative Diseases and other Proliferative Diseases
  申请人：Flynn Daniel L.

  公开号：US20110136760A1

  公开（公告）日：2011-06-09

  The present invention is concerned with novel compounds useful in the treatment of hyperproliferative diseases and mammalian cancers, especially human cancers. The invention also pertains to methods of modulating kinase activities, pharmaceutical compositions, and methods of treating individuals, incorporating or using the compounds. The preferred compounds are active small molecules set forth in formulae Ia-Iww.

  本发明涉及一种新型化合物，可用于治疗过度增殖性疾病和哺乳动物癌症，特别是人类癌症。本发明还涉及调节激酶活性的方法、制药组合物以及治疗个体的方法，包括或使用该化合物。优选的化合物是在公式Ia-Iww中列出的活性小分子。
• METHODS AND COMPOSITIONS FOR THE TREATMENT OF MYELOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES
  申请人：Flynn Daniel L.

  公开号：US20120225057A1

  公开（公告）日：2012-09-06

  Compounds of the present invention, alone and in combination with other active agents, find utility in the treatment of hyperproliferative diseases, mammalian cancers and especially human cancers including but not limited to for example malignant melanomas, myeloproliferative diseases, chronic myelogenous leukemia, acute lymphocytic leukemia, a disease caused by c-ABL kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

  本发明的化合物，单独或与其他活性剂联合使用，可用于治疗过度增生性疾病、哺乳动物癌症，特别是人类癌症，包括但不限于恶性黑色素瘤、骨髓增生性疾病、慢性粒细胞白血病、急性淋巴细胞白血病、由c-ABL激酶引起的疾病、其致癌形式、异常融合蛋白和多态性蛋白。
• Kinase inhibitors useful for the treatment of myleoproliferative diseases and other proliferative diseases
  申请人：Deciphera Pharmaceuticals, LLC.

  公开号：EP2481736A1

  公开（公告）日：2012-08-01

  Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, a disease caused by c-Met kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by a Raf kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

  本发明的化合物可用于治疗哺乳动物癌症，尤其是人类癌症，包括但不限于恶性黑色素瘤、实体瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、肝癌、宫颈癌、原发肿瘤部位转移、骨髓增生性疾病、慢性骨髓性白血病、白血病、甲状腺乳头状癌、非小细胞肺癌、间皮瘤、高髓细胞性白血病、间皮瘤、骨髓增生性疾病、慢性骨髓性白血病、白血病、甲状腺乳头状癌、非小细胞肺癌、间皮瘤、嗜酸性粒细胞过多综合征、胃肠道间质瘤、结肠癌、以过度增殖导致失明为特征的眼部疾病，包括各种视网膜病变、糖尿病视网膜病变、类风湿性关节炎、哮喘、慢性阻塞性肺病、肥大细胞增多症、肥大细胞白血病、c-Abl 激酶引起的疾病、其致癌形式、其异常融合蛋白及其多态性、c-Kit 激酶引起的疾病、其致癌形式、c-Met激酶引起的疾病、其致癌形式、其异常融合蛋白及其多态性，或 Raf激酶引起的疾病、其致癌形式、其异常融合蛋白及其多态性。