2-(2-氟-4-碘苯基氨基)-1,5-二甲基-6-氧代-N-(2-(乙烯基氧基)乙氧基)-1,6-二氢吡啶-3-甲酰胺 | 934639-06-2

• 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: 2-(2-氟-4-碘苯基氨基)-1,5-二甲基-6-氧代-N-(2-(乙烯基氧基)乙氧基)-1,6-二氢吡啶-3-甲酰胺
• 英文名称: 2-(2-fluoro-4-iodophenylamino)-1,5-dimethyl-6-oxo-N-(2-(vinyloxy)ethoxy)-1,6-dihydropyridine-3-carboxamide
• 英文别名: N-(2-ethenoxyethoxy)-2-(2-fluoro-4-iodoanilino)-1,5-dimethyl-6-oxopyridine-3-carboxamide
• CAS: 934639-06-2
• 化学式: C₁₈H₁₉FIN₃O₄
• 分子量: 487.269
• InChiKey: JZBQFLNWUKMAKK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  79.9
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-(2-氟-4-碘苯基氨基)-1,5-二甲基-6-氧代-N-(2-(乙烯基氧基)乙氧基)-1,6-二氢吡啶-3-甲酰胺 在 resultant solution 、 PTFE 、 CR13 作用下， 以 甲醇 为溶剂， 生成 AZD 8330; 2-(2-氟-4-碘苯氨基)-N-(2-羟基乙氧基)-1,5-二甲基-6-氧代-1,6-二氢吡啶-3-甲酰胺
  参考文献：
  名称：

  Crystalline forms of 2-(2-flouro-4-iodophenylamino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxamide

  摘要：

  本发明揭示了2-(2-氟-4-碘苯氨基)-N-(2-羟乙氧基)-1,5-二甲基-6-氧代-1,6-二氢吡啶-3-羧酰胺的晶体形式，用于治疗哺乳动物中的高增殖性疾病，如癌症和炎症以及炎症状况。还揭示了使用这种化合物治疗哺乳动物的高增殖性疾病的方法和包含这种化合物的制药组合物。

  公开号：

  US08299076B2
• 作为产物：
  描述：

  methyl 2-chloro-1-methyl-6-oxo-1,6-dihydropyridine-3-carboxylate 在 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride N-溴代丁二酰亚胺(NBS) 、 lithium hexamethyldisilazane 作用下， 以 四氢呋喃 、 1,4-二氧六环 、 正己烷 、 N,N-二甲基甲酰胺 、 甲苯 为溶剂， 反应 6.09h， 生成 2-(2-氟-4-碘苯基氨基)-1,5-二甲基-6-氧代-N-(2-(乙烯基氧基)乙氧基)-1,6-二氢吡啶-3-甲酰胺
  参考文献：
  名称：

  WO2008/125820

  摘要：

  公开号：

文献信息

• COMBINATION 059
  申请人：SMITH Paul David

  公开号：US20090099174A1

  公开（公告）日：2009-04-16

  This invention relates to a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to; a combination product, as defined herein, comprising a MEK inhibitor and a mTOR-selective inhibitor; a combination product, as defined herein, comprising a kit of parts comprising a MEK inhibitor and a mTOR-selective inhibitor; use of the combination product, as defined herein, in the treatment of cancer; a method of treating cancer comprising administering the combination product, as defined herein, to a patient. The combination product, as defined herein, and methods of the invention are also useful in the treatment of other diseases associated with the activity of MEK, and/or mTOR.

  本发明涉及一种组合产品，其定义为包括MEK抑制剂和mTOR选择性抑制剂，并且涉及在患者中产生抗癌效果的方法，因此在治疗患者的癌症方面非常有用。更具体地，本发明涉及：一种组合产品，其定义为包括MEK抑制剂和mTOR选择性抑制剂；一种组合产品，其定义为包括MEK抑制剂和mTOR选择性抑制剂的组件套件；使用此组合产品在癌症治疗中的方法；一种治疗癌症的方法，包括向患者投与此组合产品。此组合产品和本发明的方法也适用于治疗与MEK和/或mTOR活性相关的其他疾病。
• COMBINATION COMPRISING A MEK INHIBITOR AND AN AURORA KINASE INHIBITOR 188
  申请人：Mundt Kirsten Elisabeth

  公开号：US20100004247A1

  公开（公告）日：2010-01-07

  The present invention relates to a therapeutic combination comprising a MEK inhibitor and an Aurora kinase inhibitor, and to methods for the production of an anti-cancer effect in a patient, which is accordingly useful in the treatment of cancer in a patient. More specifically the present invention relates to: a therapeutic combination comprising a MEK inhibitor and an Aurora kinase inhibitor; a combination product comprising a MEK inhibitor and an Aurora kinase inhibitor, a kit of parts comprising a MEK inhibitor and an Aurora kinase inhibitor; use of a therapeutic combination, combination product or kit of parts in the treatment of cancer; a method of treating cancer comprising administering the therapeutic combination, combination product or kit of parts to a patient. The therapeutic combination and methods of the invention are also useful in the treatment of conditions in which the inhibition of MEK and/or Aurora kinase is beneficial.

  本发明涉及一种治疗组合物，包括MEK抑制剂和Aurora激酶抑制剂，以及在患者中产生抗癌效果的方法，因此在患者的癌症治疗中有用。更具体地，本发明涉及：一种治疗组合物，包括MEK抑制剂和Aurora激酶抑制剂；一种组合产品，包括MEK抑制剂和Aurora激酶抑制剂；一种零件套件，包括MEK抑制剂和Aurora激酶抑制剂；使用治疗组合物、组合产品或零件套件治疗癌症的方法；将治疗组合物、组合产品或零件套件输注给患者治疗癌症的方法。本发明的治疗组合物和方法也适用于治疗MEK和/或Aurora激酶抑制有益的情况。
• Heterocyclic Inhibitors of Mek and Methods of Use Thereof
  申请人：Marlow Allison L.

  公开号：US20080280957A1

  公开（公告）日：2008-11-13

  Disclosed are MEK inhibitors useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.

  本发明揭示了MEK抑制剂，其在哺乳动物的高增殖性疾病，如癌症和炎症，以及炎症状况的治疗中有用。还揭示了使用这些化合物治疗哺乳动物高增殖性疾病的方法和含有这些化合物的制药组成物。
• COMBINATION OF AN MEK INHIBITOR AND THE SRC KINASE INHIBITOR AZD0530 FOR USE IN THE TREATMENT OF CANCER
  申请人：Carragher Neil Oliver

  公开号：US20090291961A1

  公开（公告）日：2009-11-26

  The invention relates to a combination for use in the treatment of cancer comprising a MEK inhibitor and the Src kinase inhibitor AZD0530.

  该发明涉及一种用于癌症治疗的组合物，包括MEK抑制剂和Src激酶抑制剂AZD0530。
• COMBINATION THERAPY COMPRISING AZD2171 AND AZD6244 OR MEK-INHIBITOR II
  申请人：Wedge Stephen Robert

  公开号：US20100130519A1

  公开（公告）日：2010-05-27

  The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises the administration of AZD2171 in combination with AZD6244 or MEK Inhibitor II; to a pharmaceutical composition comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II; to a combination product comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II for use in a method of treatment of a human or animal body by therapy; to a kit comprising AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II; to the use of AZD2171 and AZD6244 or AZD2171 and MEK Inhibitor II in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.

  本发明涉及一种用于在温血动物（如人类）中产生抗血管生成和/或降低血管通透性的方法，该温血动物可以选择性地接受电离辐射治疗，特别是用于治疗癌症的方法，特别是涉及实体肿瘤的癌症，该方法包括将AZD2171与AZD6244或MEK Inhibitor II联合给药；一种包含AZD2171和AZD6244或AZD2171和MEK Inhibitor II的药物组合物；一种包含AZD2171和AZD6244或AZD2171和MEK Inhibitor II的联合产品，用于治疗人或动物体的方法；一种包含AZD2171和AZD6244或AZD2171和MEK Inhibitor II的工具包；使用AZD2171和AZD6244或AZD2171和MEK Inhibitor II制造药物，用于在温血动物（如人类）中产生抗血管生成和/或降低血管通透性的方法，该温血动物可以选择性地接受电离辐射治疗。