5-trimethylsilanylethynyl-pyridin-3-ylamine | 1207351-07-2

• 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
• 英文名称: 5-trimethylsilanylethynyl-pyridin-3-ylamine
• 英文别名: 5-(2-(Trimethylsilyl)ethynyl)pyridin-3-amine；5-(2-trimethylsilylethynyl)pyridin-3-amine
• CAS: 1207351-07-2
• 化学式: C₁₀H₁₄N₂Si
• 分子量: 190.32
• InChiKey: ZDVLCBQSRSQFHK-UHFFFAOYSA-N

物化性质

• 沸点：
  301.5±42.0 °C(Predicted)
• 密度：
  1.01±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.89
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  38.9
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-trimethylsilanylethynyl-pyridin-3-ylamine 在 甲醇 、 potassium carbonate 作用下， 反应 0.5h， 以96%的产率得到5-乙炔吡啶-3-胺
  参考文献：
  名称：

  5-Alkynyl-pyridines

  摘要：

  这项发明涉及一般式(I)的5-炔基吡啶 它们作为PI3Kα活性抑制剂的用途，含有它们的药物组合物，以及它们作为治疗和/或预防由细胞过度或异常增殖引起的疾病及相关症状（如癌症）的药物的用途。 R1到R6和n的含义如权利要求和说明书中所述。

  公开号：

  EP2546249A1
• 作为产物：
  描述：

  5-溴-3-氨基吡啶 、 三甲基乙炔基硅 在 双三苯基磷二氯化钯 、 碘化亚铜 氮气 、 乙酸乙酯 作用下， 以 TEA 为溶剂， 反应 32.08h， 以to afford 5-(2-(trimethylsilyl)ethynyl)pyridin-3-amine (0.279 g, 27% yield) as a white solid的产率得到5-trimethylsilanylethynyl-pyridin-3-ylamine
  参考文献：
  名称：

  Methods and Compositions for the Treatment of Myeloproliferative Diseases and other Proliferative Diseases

  摘要：

  提供了一种调节野生型激酶物种、其致癌形式、异常融合蛋白以及任何上述多态性的激酶活性的方法，该方法采用Ia公式的化合物。

  公开号：

  US20110189167A1

文献信息

• [EN] NEW 5-ALKYNYL-PYRIDINES<br/>[FR] NOUVELLES 5-ALKYNYL-PYRIDINES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2012101186A1

  公开（公告）日：2012-08-02

  This invention relates to 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of P13Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.

  这项发明涉及一般式(I)的5-炔基吡啶，它们作为P13Kalpha活性抑制剂的用途，含有它们的药物组合物，以及它们作为治疗和/或预防由过度或异常细胞增殖和相关疾病条件（如癌症）所特征的疾病的药物的用途。R1到R6和n的含义如索赔和说明书中所述。
• NEW 5-ALKYNYL-PYRIDINES
  申请人：WUNBERG Tobias

  公开号：US20130023533A1

  公开（公告）日：2013-01-24

  5-alkynyl-pyridine of general formula (I) which are inhibitors of the activity of PI3K alpha, and their use in the treatment of diseases characterized by excessive or abnormal cell proliferation, such as cancer.

  通用式（I）的5-炔基吡啶是PI3Kα活性抑制剂，可用于治疗由细胞过度或异常增殖引起的疾病，如癌症。
• KINASE INHIBITORS USEFUL FOR THE TREATMENT OF MYLEOPROLIFIC DISEASES AND OTHER PROLIFERATIVE DISEASES
  申请人：Flynn Daniel L.

  公开号：US20080261965A1

  公开（公告）日：2008-10-23

  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, mastocyclosis, 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，特别是人类癌症的治疗中具有实用性，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、高嗜酸性综合征、胃肠道间质瘤、结肠癌、眼部疾病，其特征为过度增殖导致失明，包括各种视网膜病变、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、由c-Abl激酶引起的疾病、其致癌形式、异常融合蛋白和多态形式，或者由c-Kit激酶引起的疾病，其致癌形式、异常融合蛋白和多态形式。
• 5-ALKYNYL-PYRIMIDINES
  申请人：Wunberg Tobias

  公开号：US20110281838A1

  公开（公告）日：2011-11-17

  The present invention encompasses compounds of general Formula (1) wherein R 1 to R 4 are defined as in claim 1 , which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.

  本发明涵盖了通式（1）中定义为权利要求1中所述的R1至R4的化合物，这些化合物适用于治疗由过度或异常细胞增殖所特征的疾病，并且可以用于制备具有上述特性的药物。
• 5-ALKYNYL-PYRIDINES
  申请人：Wunberg Tobias

  公开号：US20110098275A1

  公开（公告）日：2011-04-28

  The present invention encompasses compounds of general formula (1) wherein R 1 to R 4 , m and n are defined as in the specification, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.

  本发明涵盖了通式（1）中定义的化合物，其中R1至R4，m和n如规范中所定义，适用于治疗由过度或异常细胞增殖特征的疾病，并且可以用于制备具有上述特性的药物。