2-fluoro-4-[2-(1-methyl-1H-pyrazol-4-yl)-pyrimidin-4-yloxy]-phenylamine | 943314-82-7

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-fluoro-4-[2-(1-methyl-1H-pyrazol-4-yl)-pyrimidin-4-yloxy]-phenylamine
• 英文别名: 2-Fluoro-4-[2-(1-methylpyrazol-4-yl)pyrimidin-4-yl]oxyaniline
• CAS: 943314-82-7
• 化学式: C₁₄H₁₂FN₅O
• 分子量: 285.281
• InChiKey: ALNMFZOYVKIHRL-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  21
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  78.8
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• NOVEL SUBSTITUTED PYRIMIDINYLOXY UREAS USEFUL AS INHIBITORS OF PROTEIN KINASES
  申请人：Lang Hengyuan

  公开号：US20070155764A1

  公开（公告）日：2007-07-05

  The present invention relates to compounds and methods useful as inhibitors of protein kinases, including B-Raf and several receptor tyrosine and cytoplasmic tyrosine kinases. The present invention is directed to new substituted pyrimidinyloxy urea compounds of Formulas II, III and IV and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulating of protein kinase activity in a human or animal subject are also provided for the treatment diseases such as cancers.

  本发明涉及化合物和方法，用作蛋白激酶的抑制剂，包括B-Raf以及几种受体酪氨酸激酶和细胞质酪氨酸激酶。本发明涉及新的取代嘧啶氧基脲化合物II、III和IV的配方及其作为药物治疗疾病的应用。还提供了在人类或动物主体中调节蛋白激酶活性的方法，用于治疗癌症等疾病。
• [EN] CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES<br/>[FR] AMIDES DE CYCLOPROPANE ET ANALOGUES PRÉSENTANT DES ACTIVITÉS ANTICANCÉREUSES ET ANTIPROLIFÉRATIVES
  申请人：DECIPHERA PHARMACEUTICALS LLC

  公开号：WO2010051373A1

  公开（公告）日：2010-05-06

  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, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.

  本发明的化合物在治疗哺乳动物癌症，尤其是人类癌症方面具有实用性，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、由高增殖导致失明的眼部疾病，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，以及由PDGFR-α激酶、PDGFR-β激酶、c-KIT激酶、cFMS激酶、c-MET激酶和致癌形式、异常融合蛋白和任何上述激酶的多态体引起的疾病。
• KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES
  申请人：Flynn Daniel L.

  公开号：US20080269254A1

  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, 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具有实用价值，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、骨髓增生性疾病、白血病、乳头状甲状腺癌、非小细胞肺癌、间皮瘤、高嗜酸性综合症、胃肠道间质瘤、结肠癌、眼病，其特征为导致失明的过度增殖，包括各种视网膜病变、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、由c-Abl激酶引起的疾病、其癌变形式、异常融合蛋白和多态形式，或由c-Kit激酶引起的疾病，其癌变形式、异常融合蛋白和多态形式。
• CYCLOPROPANE AMIDES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
  申请人：Flynn Daniel L.

  公开号：US20100120806A1

  公开（公告）日：2010-05-13

  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, and diseases caused by PDGFR-α kinase, PDGFR-β kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.

  本发明的化合物在哺乳动物癌症治疗中具有实用性，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、慢性髓性白血病、白血病、乳头状甲状腺癌、非小细胞肺癌、间皮瘤、高嗜酸性综合症、胃肠道间质瘤、结肠癌、眼部疾病，其特征为细胞过度增殖导致失明，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、慢性阻塞性肺疾病、肥大细胞增多症、肥大细胞白血病以及由PDGFR-α激酶、PDGFR-β激酶、c-KIT激酶、cFMS激酶、c-MET激酶和任何上述激酶的癌变形式、异常融合蛋白和多态性引起的疾病。
• US8278331B2
  申请人：——

  公开号：US8278331B2

  公开（公告）日：2012-10-02