pyrazin-2-yl-(4,5,6,8-tetrahydro-3-thia-1,7,8-triaza-cyclopenta[e]azulen-2-yl)-amine | 1314140-03-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: pyrazin-2-yl-(4,5,6,8-tetrahydro-3-thia-1,7,8-triaza-cyclopenta[e]azulen-2-yl)-amine
• 英文别名: N-pyrazin-2-yl-5-thia-3,11,12-triazatricyclo[8.3.0.02,6]trideca-1(10),2(6),3,12-tetraen-4-amine
• CAS: 1314140-03-8
• 化学式: C₁₃H₁₂N₆S
• 分子量: 284.344
• InChiKey: UAZAFDBTOFCZMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  108
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  1,3-环庚二酮 在 potassium carbonate 、 4-甲氧基氯苄 、 肼 作用下， 以 四氢呋喃 、 甲醇 、 乙腈 为溶剂， 反应 5.08h， 生成 pyrazin-2-yl-(4,5,6,8-tetrahydro-3-thia-1,7,8-triaza-cyclopenta[e]azulen-2-yl)-amine
  参考文献：
  名称：

  三环噻唑并吡唑衍生物作为代谢型谷氨酸受体4正变构调节剂。

  摘要：

  越来越多的证据支持通过正构激动剂或正变构调节剂（PAM）激活代谢型谷氨酸受体4（mGlu4受体），可以对帕金森氏病，焦虑症和疼痛等疾病提供有效的干预措施。 。出于多种原因，mGlu4 PAM可能比mGlu4激动剂具有多个优势。作为我们为帕金森氏病等中枢神经系统（CNS）疾病寻找治疗药物的努力的一部分，我们一直专注于代谢型谷氨酸受体。在此，我们报告了一系列以三环噻唑并吡唑类为mGlu4 PAM的研究。

  DOI：

  10.1021/jm200290z

文献信息

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

  公开号：US20130252944A1

  公开（公告）日：2013-09-26

  The present invention relates to novel compounds of Formula (I), wherein M, A and Y are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR 4 ”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR 4 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 mGluR 4 is involved.

  本发明涉及式(I)的新型化合物，其中M、A和Y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。
• [EN] NOVEL FUSED PYRAZOLE DERIVATIVES AND THEIR USE AS ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS<br/>[FR] NOUVEAUX DÉRIVÉS DE PYRAZOLE FONDUS ET LEUR UTILISATION EN TANT QUE MODULATEURS ALLOSTÉRIQUES DES RÉCEPTEURS MÉTABOTROPIQUES DU GLUTAMATE
  申请人：ADDEX PHARMACEUTICALS SA

  公开号：WO2012009000A2

  公开（公告）日：2012-01-19

  The present invention relates to novel compounds of Formula (I), wherein M, A and Y 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.
• Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators
  作者：Sang-Phyo Hong、Kevin G. Liu、Gil Ma、Michael Sabio、Michelle A. Uberti、Maria D. Bacolod、John Peterson、Zack Z. Zou、Albert J. Robichaud、Darío Doller

  DOI：10.1021/jm200290z

  日期：2011.7.28

  There is an increasing amount of evidence to support that activation of the metabotropic glutamate receptor 4 (mGlu4 receptor), either with an orthosteric agonist or a positive allosteric modulator (PAM), provides impactful interventions in diseases such as Parkinson’s disease, anxiety, and pain. mGlu4 PAMs may have several advantages over mGlu4 agonists for a number of reasons. As part of our efforts

  越来越多的证据支持通过正构激动剂或正变构调节剂（PAM）激活代谢型谷氨酸受体4（mGlu4受体），可以对帕金森氏病，焦虑症和疼痛等疾病提供有效的干预措施。 。出于多种原因，mGlu4 PAM可能比mGlu4激动剂具有多个优势。作为我们为帕金森氏病等中枢神经系统（CNS）疾病寻找治疗药物的努力的一部分，我们一直专注于代谢型谷氨酸受体。在此，我们报告了一系列以三环噻唑并吡唑类为mGlu4 PAM的研究。