4-(2-(1H-1,2,4-triazol-1-yl)pyridin-4-yloxy)-2-fluorobenzenamine | 1070162-78-5

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 4-(2-(1H-1,2,4-triazol-1-yl)pyridin-4-yloxy)-2-fluorobenzenamine
• 英文别名: 2-fluoro-4-[2-(1,2,4-triazol-1-yl)pyridin-4-yl]oxyaniline
• CAS: 1070162-78-5
• 化学式: C₁₃H₁₀FN₅O
• 分子量: 271.254
• InChiKey: WFQCXPMYMLBRQP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 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：
  78.8
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2,2,2-trichloroethyl (3-(tert-butyl)isoxazol-5-yl)carbamate 、 4-(2-(1H-1,2,4-triazol-1-yl)pyridin-4-yloxy)-2-fluorobenzenamine 在 1-甲基吡咯烷 作用下， 以 1,4-二氧六环 为溶剂， 生成 1-(4-(2-(1H-1,2,4-triazol-1-yl)pyridin-4-yloxy)-2-fluorophenyl)-3-(3-tert-butylisoxazol-5-yl)urea
  参考文献：
  名称：

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

  摘要：

  本发明的化合物在哺乳动物癌症的治疗中发挥作用，特别是人类癌症，包括但不限于恶性黑色素瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、宫颈癌、原发肿瘤部位的转移、骨髓增殖性疾病、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、以增殖过度导致失明的眼部疾病，包括各种视网膜病变、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、异常融合蛋白及其多态形式，或由c-Kit激酶引起的疾病、其致癌形式、异常融合蛋白及其多态形式。

  公开号：

  US20080261961A1
• 作为产物：
  描述：

  4-((2-chloropyridin-4-yl)oxy)-2-fluoroaniline 、 sodium triazole 在 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 N-甲基吡咯烷酮 为溶剂， 生成 4-(2-(1H-1,2,4-triazol-1-yl)pyridin-4-yloxy)-2-fluorobenzenamine
  参考文献：
  名称：

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

  摘要：

  本发明的化合物在哺乳动物癌症的治疗中发挥作用，特别是人类癌症，包括但不限于恶性黑色素瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、宫颈癌、原发肿瘤部位的转移、骨髓增殖性疾病、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、以增殖过度导致失明的眼部疾病，包括各种视网膜病变、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、异常融合蛋白及其多态形式，或由c-Kit激酶引起的疾病、其致癌形式、异常融合蛋白及其多态形式。

  公开号：

  US20080261961A1

文献信息

• 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。
• KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES
  申请人：Deciphera Pharmaceuticals, LLC.

  公开号：EP2146717A1

  公开（公告）日：2010-01-27
• [EN] KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFERATIVE DISEASES AND OTHER PROLIFERATIVE DISEASES<br/>[FR] INHIBITEURS DE KINASE UTILES POUR LE TRAITEMENT DES MALADIES MYLÉOPROLIFÉRATIVES ET D'AUTRES MALADIES PROLIFÉRATIVES
  申请人：DECIPHERA PHARMACEUTICALS LLC

  公开号：WO2008140895A1

  公开（公告）日：2008-11-20

  [EN] Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, 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, 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, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.
  [FR] La présente invention concerne des composés utiles dans le traitement des cancers des mammifères et en particulier des cancers humains y compris, mais sans limitation, des tumeurs malignes, des mélanomes, des glioblastomes, du cancer des ovaires, du cancer du pancréas, du cancer de la prostate, des cancers des poumons, des cancers du sein, des cancers des reins, des cancers du col de l'utérus, des métastases des sites tumoraux principaux, des maladies myéloprolifératives, des leucémies, des carcinomes papillaires de la thyroïde, du cancer bronchique à petites cellules, du mésothéliome, du syndrome hyperéosinophile, des tumeurs stromales digestives, des cancers du colon, des maladies oculaires caractérisées par une hyperprolifération aboutissant à une perte de la vue, y compris une variété de rétinopathies, de l'arthrite rhumatoïde, de l'asthme, de la maladie pulmonaire chronique obstructive, de la mastocytose, de la leucémie des mastocytes, d'une maladie causée par la kinase c-Abl, des formes oncogéniques de cette maladie, des protéines de fusion aberrantes de celles-ci et leurs polymorphes ou d'une maladie causée par la kinase c-Kit, leurs formes oncogéniques, leurs protéines aberrantes et leurs polymorphes.
• KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES
  申请人：Flynn Daniel L.

  公开号：US20080261961A1

  公开（公告）日：2008-10-23

  Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, 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, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyctosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.

  本发明的化合物在哺乳动物癌症的治疗中发挥作用，特别是人类癌症，包括但不限于恶性黑色素瘤、胶质母细胞瘤、卵巢癌、胰腺癌、前列腺癌、肺癌、乳腺癌、肾癌、宫颈癌、原发肿瘤部位的转移、骨髓增殖性疾病、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、以增殖过度导致失明的眼部疾病，包括各种视网膜病变、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、异常融合蛋白及其多态形式，或由c-Kit激酶引起的疾病、其致癌形式、异常融合蛋白及其多态形式。