6-ethynyl-N-(3-(1-methyl-1H-pyrazol-4-yl)-5-(morpholinomethyl)phenyl)quinazolin-2-amine | 1036745-90-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 6-ethynyl-N-(3-(1-methyl-1H-pyrazol-4-yl)-5-(morpholinomethyl)phenyl)quinazolin-2-amine
• 英文别名: 6-ethynyl-N-[3-(1-methylpyrazol-4-yl)-5-(morpholin-4-ylmethyl)phenyl]quinazolin-2-amine
• CAS: 1036745-90-0
• 化学式: C₂₅H₂₄N₆O
• 分子量: 424.505
• InChiKey: IVNHGEWUUQCUFI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  32
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  68.1
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  6-ethynyl-N-(3-(1-methyl-1H-pyrazol-4-yl)-5-(morpholinomethyl)phenyl)quinazolin-2-amine 在 间氯过氧苯甲酸 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 4-(3-(6-ethynylquinazolin-2-ylamino)-5-(1-methyl-1H-pyrazol-4-yl)benzyl)morpholine 4-oxide
  参考文献：
  名称：

  [EN] 2 -ARYLAMINOQUINAZOLINES FOR TREATING PROLIFERATIVE DISEASES
  [FR] 2 -ARYLAMINOQUINAZOLINES DESTINÉES AU TRAITEMENT DES MALADIES PROLIFÉRATIVES

  摘要：

  这项发明提供了一种抑制PDKI的新型化合物。还提供了包括这些化合物的药物组合物，以及使用这些化合物或组合物治疗增殖性疾病，如癌症的方法。

  公开号：

  WO2009153313A1

文献信息

• Novel compounds for treating proliferative diseases
  申请人：Jain Rama

  公开号：US20100121052A1

  公开（公告）日：2010-05-13

  The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.

  本发明提供了一些新的化合物，这些化合物是PDK1的抑制剂。同时提供了包括这些化合物的药物组合物，以及使用这些化合物或组合物治疗增生性疾病（如癌症）的方法。
• Methods for use of TSLP and agonists and antagonists thereof
  申请人：Leonard J. Warren

  公开号：US20050249712A1

  公开（公告）日：2005-11-10

  Methods are disclosed herein for specifically inducing proliferation of CD4 + T cells. The methods are of use in treating immunodeficiencies, such as an immunodeficiency produced by infection with an immunodeficiency virus, such as infection with a human immunodeficiency virus (HIV). The methods include contacting isolated mammalian CD4+ T cells with an effective amount of a thymic stromal derived lymphopoietin (TSLP) polypeptide or a therapeutically effective amount of nucleic acid encoding the TSLP polypeptide, thereby inducing proliferation of the T cells. Methods are also disclosed for treating an IgE mediated disorder, such as asthma. The methods include administering to a subject a therapeutically effective amount of a TSLP antagonist. Transgenic mice are also disclosed herein. The somatic and germ cells of these mice include a disrupted thymic stromal lymphopoietin receptor (TSLP) gene, the disruption being sufficient to inhibit the interaction of TSLP with its receptor, and a disrupted γ c gene, the disruption being sufficient to reduce signaling through the γ c . The mice exhibit diminished thymic cellularity. Methods of using these mice for drug screening are also disclosed.

  本文公开了特异性诱导 CD4 + T 细胞增殖的方法。这些方法可用于治疗免疫缺陷，如感染免疫缺陷病毒（如感染人类免疫缺陷病毒（HIV））后产生的免疫缺陷。这些方法包括使分离的哺乳动物 CD4+ T 细胞与有效量的胸腺基质衍生淋巴细胞生成素（TSLP）多肽或治疗有效量的编码 TSLP 多肽的核酸接触，从而诱导 T 细胞增殖。还公开了治疗 IgE 介导的疾病（如哮喘）的方法。这些方法包括向受试者施用治疗有效量的 TSLP 拮抗剂。本文还公开了转基因小鼠。这些小鼠的体细胞和生殖细胞包括被破坏的胸腺基质淋巴细胞生成素受体（TSLP）基因，这种破坏足以抑制 TSLP 与其受体的相互作用，以及被破坏的 γ c 基因，这种干扰足以减少通过γ c .这种小鼠的胸腺细胞功能减弱。还公开了利用这些小鼠进行药物筛选的方法。
• 2 -ARYLAMINOQUINAZOLINES FOR TREATING PROLIFERATIVE DISEASES
  申请人：Novartis AG

  公开号：EP2307385A1

  公开（公告）日：2011-04-13
• METHODS FOR USE OF TSLP AND AGONISTS AND ANTAGONISTS THEREOF
  申请人：Leonard J. Warren

  公开号：US20070237787A1

  公开（公告）日：2007-10-11

  Methods are disclosed herein for specifically inducing proliferation of CD4 + T cells. The methods are of use in treating immunodeficiencies, such as an immunodeficiency produced by infection with an immunodeficiency virus, such as infection with a human immunodeficiency virus (HIV). The methods include contacting isolated mammalian CD4+ T cells with an effective amount of a thymic stromal derived lymphopoietin (TSLP) polypeptide or a therapeutically effective amount of nucleic acid encoding the TSLP polypeptide, thereby inducing proliferation of the T cells. Methods are also disclosed for treating an IgE mediated disorder, such as asthma. The methods include administering to a subject a therapeutically effective amount of a TSLP antagonist. Transgenic mice are also disclosed herein. The somatic and germ cells of these mice include a disrupted thymic stromal lymphopoietin receptor (TSLP) gene, the disruption being sufficient to inhibit the interaction of TSLP with its receptor, and a disrupted γ c gene, the disruption being sufficient to reduce signaling through the γ c . The mice exhibit diminished thymic cellularity. Methods of using these mice for drug screening are also disclosed.
• US7731953B2
  申请人：——

  公开号：US7731953B2

  公开（公告）日：2010-06-08