2-chloro-4-((6-nitropyridin-3-yl)oxy)pyridine | 1225278-66-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-chloro-4-((6-nitropyridin-3-yl)oxy)pyridine
• 英文别名: 2-Chloro-4-(6-nitropyridin-3-yloxy)pyridine；5-(2-chloropyridin-4-yl)oxy-2-nitropyridine
• CAS: 1225278-66-9
• 化学式: C₁₀H₆ClN₃O₃
• 分子量: 251.629
• InChiKey: SHGODQROPZFTNJ-UHFFFAOYSA-N

物化性质

• 沸点：
  421.8±45.0 °C(Predicted)
• 密度：
  1.477±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  80.8
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-chloro-4-((6-nitropyridin-3-yl)oxy)pyridine 在 氢气 作用下， 以 甲醇 为溶剂， 反应 3.0h， 生成 5-((2-chloropyridin-4-yl)oxy)pyridin-2-amine
  参考文献：
  名称：

  发现 vimseltinib (DCC-3014)，一种高选择性 CSF1R 开关控制激酶抑制剂，用于治疗腱鞘巨细胞瘤 (TGCT) 的临床开发

  摘要：

  基于激酶开关控制抑制的知识，并结合基于结构的药物设计和标准药物化学原理，我们确定了一系列新型的基于二氢嘧啶酮的 CSF1R 激酶抑制剂，相对于大量激酶和非-激酶蛋白靶标。从先导化合物3开始，SAR 优化活动导致发现 vimseltinib（DCC-3014；化合物20），目前正在进行临床评估，用于治疗腱鞘巨细胞瘤 (TGCT)，这是一种与严重发病率相关的局部侵袭性良性肿瘤。2021 爱思唯尔 版权所有。

  DOI：

  10.1016/j.bmcl.2022.128928
• 作为产物：
  描述：

  2-氯-4-吡啶酮 、 5-氟-2-硝基吡啶 在 potassium carbonate 作用下， 以 二甲基亚砜 为溶剂， 反应 48.0h， 以10.8 g的产率得到2-chloro-4-((6-nitropyridin-3-yl)oxy)pyridine
  参考文献：
  名称：

  [EN] Amide compounds and uses thereof
  [FR] COMPOSÉS AMIDES ET LEURS UTILISATIONS

  摘要：

  本文提供了化合物的新型酰胺化合物的公式(I)，包括相同的药物组合物，制备相同的方法以及它们的用途，其中每个符号的定义如描述中所述。

  公开号：

  WO2021197276A1

文献信息

• IMIDAZOLIDINONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES
  申请人：Deciphera Pharmaceuticals, LLC

  公开号：US20140315917A1

  公开（公告）日：2014-10-23

  Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.

  描述了一种化合物，其化学式为I，通过抑制c-FMS（CSF-1R）、c-KIT和/或PDGFR激酶，在治疗癌症、自身免疫疾病和代谢性骨疾病方面具有用途。这些化合物还在治疗其他由c-FMS、c-KIT或PDGFR激酶介导的哺乳动物疾病中发挥作用。
• [EN] 1,2,4-TRIAZOL-5-ONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES<br/>[FR] 1,2,4-TRIAZOL-5-ONES ET ANALOGUES MONTRANT DES ACTIVITÉS ANTICANCÉREUSES ET ANTIPROLIFÉRATIVES
  申请人：DECIPHERA PHARMACEUTICALS LLC

  公开号：WO2014145023A1

  公开（公告）日：2014-09-18

  Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-lR), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.

  描述了一种具有公式I的化合物，通过抑制c-FMS（CSF-lR）、c-KIT和/或PDGFR激酶，在治疗癌症、自身免疫疾病和代谢性骨疾病方面发挥作用。这些化合物还在治疗其他由c-FMS、c-KIT或PDGFR激酶介导的哺乳动物疾病中发挥作用。
• [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。
• N-(AZAARYL)CYCLOLACTAM-1-CARBOXAMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF
  申请人：Abbisko Therapeutics Co., Ltd.

  公开号：US20200071302A1

  公开（公告）日：2020-03-05

  An N-(azaaryl)cyclolactam-1-carboxamide derivative having a structure of formula (I), a preparation method therefor, and a use thereof are disclosed in the application. Each substituent are defined in the specification and claims. The series of compounds of the application can be widely applied in the preparation of drugs for treating cancer, tumor, autoimmune disease, metabolic disease or metastatic disease, particularly for treating ovarian cancer, pancreatic cancer, prostate cancer, breast cancer, cervical cancer, glioblastoma, multiple myeloma, metabolic disease, neurodegenerative disease, primary tumor site metastasis or osseous metastasis cancer, and are expected to be developed into a new generation of CSF-1R inhibitor drugs.

  本申请公开了具有结构式（I）的N-(azaaryl)cyclolactam-1-羧酰胺衍生物，其制备方法及用途。每个取代基在规范和权利要求中有定义。本申请中的化合物系列可广泛应用于制备用于治疗癌症、肿瘤、自身免疫疾病、代谢性疾病或转移性疾病的药物，特别适用于治疗卵巢癌、胰腺癌、前列腺癌、乳腺癌、宫颈癌、胶质母细胞瘤、多发性骨髓瘤、代谢性疾病、神经退行性疾病、原发肿瘤部位转移或骨转移癌症，并有望开发成为新一代CSF-1R抑制剂药物。
• 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。