5-fluoro-N-(6-methylpyridin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine | 1235312-62-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 5-fluoro-N-(6-methylpyridin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine
• 英文别名: 5-fluoro-N-(6-methylpyridin-2-yl)-4-(1H-pyrazol-4-yl)-1,3-thiazol-2-amine
• CAS: 1235312-62-5
• 化学式: C₁₂H₁₀FN₅S
• 分子量: 275.309
• InChiKey: RWSWSYCPVVLWJB-UHFFFAOYSA-N

物化性质

• 沸点：
  515.2±60.0 °C(predicted)
• 密度：
  1.458±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  94.7
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  5-fluoro-N-(6-methylpyridin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine 、 溶剂黄146 在 potassium cyanide 作用下， 以 水 为溶剂， 反应 2.5h， 以3%的产率得到4-(5-fluoro-2-(6-methylpyridin-2-ylamino)thiazol-4-yl)-1H-pyrazole-1-carboxamide
  参考文献：
  名称：

  [EN] NOVEL THIAZOLES DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
  [FR] NOUVEAUX DÉRIVÉS DE THIAZOLE ET LEUR EMPLOI EN TANT QUE MODULATEURS ALLOSTÉRIQUES POSITIFS DES RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE

  摘要：

  本发明涉及式（I）的新化合物，其中M、P、A和（B）n如式（I）中所定义；该发明化合物是代谢型谷氨酸受体-亚型4（"mGluR4"）的调节剂，对于治疗或预防中枢神经系统疾病以及其他受mGluR4受体调节的疾病具有用处。该发明还涉及制药组合物以及利用这类化合物制造药物的用途，以及利用这类化合物预防和治疗涉及mGluR4的疾病的用途。

  公开号：

  WO2010079239A1
• 作为产物：
  描述：

  N-(4-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-fluorothiazol-2-yl)-6-methylpyridin-2-amine 在 二氯甲烷 、 乙酸乙酯 、 magnesium sulfate 、 crude product 、 乙醚 作用下， 以 三氟乙酸 为溶剂， 反应 0.13h， 以to yield 5-fluoro-N-(6-methylpyridin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine (0.12 mmol, 33 mg, 50%) as a beige solid的产率得到5-fluoro-N-(6-methylpyridin-2-yl)-4-(1H-pyrazol-4-yl)thiazol-2-amine
  参考文献：
  名称：

  Thiazoles derivatives and their use as positive allosteric modulators of metabotropic glutamate receptors

  摘要：

  本发明涉及公式（I）的新化合物，其中M、P、A和（B）n如公式（I）中所定义；发明化合物是代谢型谷氨酸受体亚型4（“mGluR4”）的调节剂，可用于治疗或预防中枢神经系统疾病以及其他受mGluR4受体调节的疾病。本发明还涉及制药组合物以及使用这种化合物制造药物的用途，以及使用这种化合物预防和治疗涉及mGluR4的疾病的用途。

  公开号：

  US09073907B2

文献信息

• NOVEL THIAZOLES DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
  申请人：Bolea Christelle

  公开号：US20110257179A1

  公开（公告）日：2011-10-20

  The present invention relates to novel compounds of Formula (I), wherein M, P, A and (B) n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.

  本发明涉及公式（I）的新化合物，其中M，P，A和（B）n如公式（I）中所定义；发明化合物是代谢型谷氨酸受体-亚型4（“mGluR4”）的调节剂，对于治疗或预防中枢神经系统疾病以及其他由mGluR4受体调节的疾病有用。本发明还涉及制药组合物以及使用这种化合物制造药物的用途，以及使用这种化合物预防和治疗涉及mGluR4的疾病的用途。
• NOVEL 2-AMINO-4-PYRAZOLYL-THIAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
  申请人：Boléa Christelle

  公开号：US20130210809A1

  公开（公告）日：2013-08-15

  The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.

  本发明涉及式（1）的新化合物，其中M，A和B如式（I）中所定义; 发明化合物是代谢型谷氨酸受体亚型4（“mGluR4”）的调节剂，可用于治疗或预防中枢神经系统疾病以及其他受mGluR4受体调节的疾病。本发明还涉及制药组合物和使用这些化合物制造药物的用途，以及使用这些化合物预防和治疗mGluR4参与的疾病的用途。
• US9073907B2
  申请人：——

  公开号：US9073907B2

  公开（公告）日：2015-07-07
• [EN] NOVEL 2-AMINO-4-PYRAZOLYL-THIAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS<br/>[FR] NOUVEAUX DÉRIVÉS DE 2-AMINO-4-PYRAZOLYL-THIAZOLE ET LEUR UTILISATION EN TANT QUE MODULATEURS ALLOSTÉRIQUES DES RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE
  申请人：ADDEX PHARMACEUTICALS SA

  公开号：WO2012009009A2

  公开（公告）日：2012-01-19

  The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors - subtype 4 ("mGluR4") which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
• [EN] NOVEL THIAZOLES DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS<br/>[FR] NOUVEAUX DÉRIVÉS DE THIAZOLE ET LEUR EMPLOI EN TANT QUE MODULATEURS ALLOSTÉRIQUES POSITIFS DES RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE
  申请人：ADDEX PHARMACEUTICALS SA

  公开号：WO2010079239A1

  公开（公告）日：2010-07-15

  The present invention relates to novel compounds of Formula (I), wherein M, P, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors - subtype 4 ("mGluR4") which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.

  本发明涉及式（I）的新化合物，其中M、P、A和（B）n如式（I）中所定义；该发明化合物是代谢型谷氨酸受体-亚型4（"mGluR4"）的调节剂，对于治疗或预防中枢神经系统疾病以及其他受mGluR4受体调节的疾病具有用处。该发明还涉及制药组合物以及利用这类化合物制造药物的用途，以及利用这类化合物预防和治疗涉及mGluR4的疾病的用途。