3-methyl-2-oxoimidazolidin-1-carbonyl chloride | 57451-84-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑烷类
• 英文名称: 3-methyl-2-oxoimidazolidin-1-carbonyl chloride
• 英文别名: 3-methyl-2-oxo-imidazolidine-1-carbonyl chloride；1-chlorocarbonyl-2-oxo-3-methyl-imidazolidine；1-Chlorcarbonyl-2-oxo-3-methyl-imidazolidin；1-Chlorcarbonyl-2-oxo-3-methyl-imidazolidn；3-Methyl-2-oxoimidazolidine-1-carbonyl chloride
• CAS: 57451-84-0
• 化学式: C₅H₇ClN₂O₂
• 分子量: 162.576
• InChiKey: OIOGFDPKEOSFCZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  10
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  40.6
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-((2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl)oxy)pyridin-2-amine 、 3-methyl-2-oxoimidazolidin-1-carbonyl chloride 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 4.0h， 以80 mg的产率得到3-methyl-N-(5-((2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yl)oxy)pyridin-2-yl)-2-oxoimidazolidine-1-carboxamide
  参考文献：
  名称：

  IMIDAZOLIDINONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES

  摘要：

  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。

  公开号：

  US20140315917A1
• 作为产物：
  描述：

  1-甲基-2-咪唑啉酮 、 光气 在 吡啶 作用下， 以 二氯甲烷 、 甲苯 为溶剂， 反应 1.0h， 生成 3-methyl-2-oxoimidazolidin-1-carbonyl chloride
  参考文献：
  名称：

  IMIDAZOLIDINONES AND ANALOGS EXHIBITING ANTI-CANCER AND ANTI-PROLIFERATIVE ACTIVITIES

  摘要：

  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。

  公开号：

  US20140315917A1

文献信息

• INDOLIN-2-ONE DERIVATIVES AS PROTEIN KINASE INHIBITORS
  申请人：ANNJI PHARMACEUTICAL CO., LTD.

  公开号：US20130281451A1

  公开（公告）日：2013-10-24

  A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer.

  揭示了一类新型的吲哚啉-2-酮衍生物。这些化合物是蛋白激酶抑制剂，可用于治疗癌症等过度增殖性疾病。
• Inhibitors of protein tyrosine kinase activity
  申请人：Raeppel Stephane

  公开号：US20080004273A1

  公开（公告）日：2008-01-03

  This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

  这项发明涉及抑制蛋白酪氨酸激酶活性的化合物。具体而言，该发明涉及抑制生长因子受体蛋白酪氨酸激酶活性的化合物，导致受体信号传导的抑制，例如抑制VEGF受体信号传导和HGF受体信号传导。更具体地，该发明涉及用于抑制VEGF受体信号传导和HGF受体信号传导的化合物、组合物和方法。该发明还提供了用于治疗细胞增殖性疾病和病况的组合物和方法。
• INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY
  申请人：Saavedra Mario Oscar

  公开号：US20080064718A1

  公开（公告）日：2008-03-13

  This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

  本发明涉及抑制蛋白酪氨酸激酶活性的化合物。特别是，本发明涉及抑制生长因子受体蛋白酪氨酸激酶活性的化合物，从而抑制受体信号传导，例如抑制VEGF受体信号和HGF受体信号的传导。更具体地，本发明涉及用于抑制VEGF受体信号和HGF受体信号的化合物、组合物和方法。本发明还提供了用于治疗细胞增殖性疾病和病状的组合物和方法。
• KINASE INHIBITORS AND USES THEREOF
  申请人：Raeppel Stephane

  公开号：US20080255155A1

  公开（公告）日：2008-10-16

  This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds, compositions and methods for the inhibition of kinase activity. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions.

  本发明涉及抑制蛋白酪氨酸激酶活性的化合物。具体而言，本发明涉及抑制激酶活性的化合物、组合物和方法。本发明还提供用于治疗细胞增殖性疾病和病症的化合物、组合物和方法。
• Indolin-2-one derivatives as protein kinase inhibitors
  申请人：Annji Pharmaceutical Co., Ltd.

  公开号：US08946282B2

  公开（公告）日：2015-02-03

  A novel class of indoline-2-one derivatives are disclosed. These compounds are protein kinase inhibitors which are useful for treating hyperproliferative diseases such as cancer. In one aspect, the invention relates to a compound a compound of Formula A: or a pharmaceutically acceptable salt thereof, wherein: Ra is hydrogen, (C6-C18)aryl, halo(C6-C18)aryl, or (C1-C6)alkoxy(C6-C18)aryl; Rb is hydrogen, (C3-C18)heteroaryl, (C1-C6)alkoxy(C3-C18)heteroaryl; (C1-C6)alkyl(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxy(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)carboxyalkyl(C3-C18)heteroaryl; (C1-C6)alkyl(C1-C6)alkylamino(C1-C6)alkylcarbamoyl)(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C18)aryl(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxycarbonyl)(C3-C18)heteroaryl, (C1-C6)alkyl(C1-C6)alkoxy(C1-C6)oxyalkyl(C3-C18)heteroaryl, (C1-C6)alkyl(C3-C6)heterocyclylcarbonyl(C3-C18)heteroaryl, (C1-C6)alkyl(C3-C6)heterocyclyl(C1-C6)oxyalkyl(C3-C18)heteroaryl, or (C1-C6)alkyl((C3-C6)heterocyclyl(C1-C6)alkylcarbamoyl)(C3-C18)heteroaryl; Rc is hydrogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido; Rd is hydrogen, halogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido; Re is-hydrogen, benzoylureido, halobenzoylureido, halo(C1-C6)alkoxybenzoylureido, (C1-C6)alkoxybenzoylureido, (C1-C6)alkylaminobenzoylureido, (C1-C6)alkylbenzoylureido, nitrobenzoylureido, (C1-C6)haloalkylbenzoylureido, (C1-C6)haloalkylhalobenzoylureido, halo(C6-C18)arylcarbomylacetamido, (C1-C6)alkoxy(C6-C18)arylcarbomylacetamido, (C1-C6)alkoxy(C6-C18)arylcarbamoyl(C3-C6)cycloalkylamido, halo(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, (C3-C6)cycloalkyl(C3-C18)heteroarylcarbonylamino, (C1-C6)alkylamino(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, halo(C1-C6)alkoxy(C6-C18)aryl(C3-C18) heteroarylcarbonylamino, (C1-C6)alkoxy(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, (C1-C6)alkyl(C3-C18)heteroarylcarbonylamino, aryl(C3-C18)heteroarylcarbonylamino, (C1-C6)haloalkylhalo(C6-C18)aryl(C3-C6)heterocyclylcarbonylamino, (C1-C6)haloalkyl(C6-C18)aryl(C3-C18)heteroarylcarbonylamino, halo(C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)oxyalkyl(C3-C6)heterocyclylamido, (C1-C6)alkoxy(C1-C6)alkyl(C3-C18)heteroarylamido, (C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)alkyl(C1-C18)aryl(C3-C18)heteroarylamido, (C1-C6)haloalkyl(C6-C18)aryl(C3-C18)heteroarylamido, (C1-C6)alkyl(C3-C18)heteroarylamido, or (C1-C6)alkoxy(C6-C18)aryl(C3-C18)heteroarylamido; and Rf is hydrogen, (C1-C6)alkoxybenzoylureido, or halo(C6-C18)aryl(C3-C18)heteroarylamido.

  本发明揭示了一类新型的吲哚啉-2-酮衍生物。这些化合物是蛋白激酶抑制剂，可用于治疗癌症等增殖性疾病。在一个方面，本发明涉及化合物A的化合物或其药学上可接受的盐，其中：Ra是氢、(C6-C18)芳基、卤代(C6-C18)芳基或(C1-C6)烷氧基(C6-C18)芳基；Rb是氢、(C3-C18)杂环芳基、(C1-C6)烷氧基(C3-C18)杂环芳基、(C1-C6)烷基(C3-C18)杂环芳基、(C1-C6)烷基(C1-C6)烷氧基(C3-C18)杂环芳基、(C1-C6)烷基(C1-C6)羧基烷基(C3-C18)杂环芳基、(C1-C6)烷基(C1-C6)烷基氨基(C1-C6)烷基氨基甲酰基)(C3-C18)杂环芳基、(C1-C6)烷基(C1-C18)芳基(C3-C18)杂环芳基、(C1-C6)烷基(C1-C6)烷氧羰基)(C3-C18)杂环芳基、(C1-C6)烷基(C1-C6)烷氧基(C1-C6)氧基烷基(C3-C18)杂环芳基、(C1-C6)烷基(C3-C6)杂环烷基羰基(C3-C18)杂环芳基、(C1-C6)烷基(C3-C6)杂环芳基(C1-C6)氧基烷基(C3-C18)杂环芳基或(C1-C6)烷基((C3-C6)杂环芳基(C1-C6)烷基氨基甲酰基)(C3-C18)杂环芳基；Rc是氢、(C1-C6)烷氧基苯甲酰脲基或卤代(C6-C18)芳基(C3-C18)杂环芳基酰胺基；Rd是氢、卤素、(C1-C6)烷氧基苯甲酰脲基或卤代(C6-C18)芳基(C3-C18)杂环芳基酰胺基；Re是氢、苯甲酰脲基、卤代苯甲酰脲基、卤代(C1-C6)烷氧基苯甲酰脲基、(C1-C6)烷氧基苯甲酰脲基、(C1-C6)烷基氨基苯甲酰脲基、(C1-C6)烷基苯甲酰脲基、硝基苯甲酰脲基、(C1-C6)卤代烷基苯甲酰脲基、(C1-C6)卤代烷基卤代苯甲酰脲基、卤代(C6-C18)芳基羧酰乙酰胺基、(C1-C6)烷氧(C6-C18)芳基羧酰乙酰胺基、(C1-C6)烷氧(C6-C18)芳基氨基甲酰基(C3-C6)环烷基酰胺基、卤代(C6-C18)芳基(C3-C18)杂环芳基酰胺基、(C3-C6)环烷基(C3-C18)杂环芳基酰胺基、(C1-C6)烷基氨基(C6-C18)芳基(C3-C18)杂环芳基酰胺基、卤代(C1-C6)烷氧(C6-C18)芳基(C3-C18)杂环芳基酰胺基、(C1-C6)烷氧(C6-C18)芳基(C3-C18)杂环芳基酰胺基、(C1-C6)烷基(C3-C18)杂环芳基酰胺基、芳基(C3-C18)杂环芳基酰胺基、(C1-C6)卤代烷基卤代(C6-C18)芳基(C3-C6)杂环烷基酰胺基、(C1-C6)卤代烷基(C6-C18)芳基(C3-C18)杂环芳基酰胺基、卤代(C6-C18)芳基(C3-C18)杂环芳基酰胺基、(C1-C6)氧基烷基(C3-C6)杂环酰胺基、(C1-C6)烷氧(C1-C6)烷基(C3-C18)杂环芳基酰胺基、(C6-C18)芳基(C3-C18)杂环芳基酰胺基、(C1-C6)烷基(C1-C18)芳基(C3-C18)杂环芳基酰胺基、(C1-C6)卤代烷基(C6-C18)芳基(C3-C18)杂环芳基酰胺基、(C1-C6)烷基(C3-C18)杂环芳基酰胺基或(C1-C6)烷氧(C6-C18)芳基(C3-C18)杂环芳基酰胺基；Rf是氢、(C1-C6)烷氧基苯甲酰脲基或卤代(C6-C18)芳基(C3-C18)杂环芳基酰胺基。