7-Nitro-2,3-Dioxo-2,3-Dihydroquinoxaline-6-Carbonitrile

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 7-Nitro-2,3-Dioxo-2,3-Dihydroquinoxaline-6-Carbonitrile
• 化学式: C9H2N4O4
• 分子量: 230.14
• InChiKey: IAWXTSMHXFRLQR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  97.4
• 氢给体数：
  0
• 氢受体数：
  5

文献信息

• [EN] TRIPARTITE MODULATORS OF ENDOSOMAL G PROTEIN-COUPLED RECEPTORS<br/>[FR] MODULATEURS TRIPARTITES DE RÉCEPTEURS COUPLÉS AUX PROTÉINES G DES ENDOSOMES
  申请人：TAKEDA PHARMACEUTICALS CO

  公开号：WO2017112792A1

  公开（公告）日：2017-06-29

  The present invention relates to tripartite compounds comprising a modulator moiety for endosomal G protein-coupled receptors like neurokinin-1 receptor, a linker and a lipid anchor suitable for anchoring the tripartite compound into a plasma membrane. The present invention also relates to a prodrug and a pharmaceutical composition comprising the tripartite compound and the use of the tripartite compound for the treatment of a disease or disorder mediated by endosomal G protein-coupled receptors signalling like NK1R signalling.

  本发明涉及三部分化合物，包括用于内体高尔基蛋白偶联受体（如神经激肽-1受体）的调节子基团，一个连接物和一个适合将三部分化合物锚定到细胞膜的脂质锚。本发明还涉及一种前药和含有三部分化合物的药物组合物，以及利用三部分化合物治疗由内体高尔基蛋白偶联受体信号传导介导的疾病或紊乱的用途。
• PHARMACEUTICALLY ACTIVE COMPOUNDS AS DAG-LIPASE INHIBITORS
  申请人：Universiteit Leiden

  公开号：EP3095787A1

  公开（公告）日：2016-11-23

  The present invention relates to novel compounds which are highly selective inhibitors of diacylglycerol lipase α and β. These compounds are suitable for the treatment or prevention of disorders associated with, accompanied by or caused by increased 2-arachidonoylglycerol levels. Diacylglycerol lipase-α (alternative name: Sn1-specific diacylglycerol hydrolase a; DAGL-α) and -β are enzymes responsible for the biosynthesis of the endocannabinoid 2-arachidonoylglycerol. Selective and reversible inhibitors are required to study the function of DAGLs in neuronal cells in an acute and temporal fashion. The inventive ompounds are in particular suitable for the treatment of neurodegenerative diseases, inflammatory diseases, drug abuse and impaired energy balance, such as obesity.

  这项发明涉及一种新型化合物，它们是高选择性的二酰甘油脂酶α和β的抑制剂。这些化合物适用于治疗或预防与增加2-花生四烯酰基甘油水平相关、伴随或由此引起的疾病。二酰甘油脂酶-α（另一名称：Sn1特异性二酰甘油水解酶a；DAGL-α）和-β是负责内源大麻素2-花生四烯酰基甘油的生物合成的酶。需要选择性和可逆的抑制剂来研究神经细胞中DAGLs的功能，以一种急性和暂时的方式。这些创新的化合物特别适用于治疗神经退行性疾病、炎症性疾病、药物滥用和受损的能量平衡，如肥胖症。
• PAK INHIBITORS FOR THE TREATMENT OF CELL PROLIFERATIVE DISORDERS
  申请人：AFRAXIS, INC.

  公开号：US20130116263A1

  公开（公告）日：2013-05-09

  Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of cell proliferative disorders and/or CNS disorders.

  本文提供了PAK抑制剂以及利用PAK抑制剂治疗细胞增殖性疾病和/或中枢神经系统疾病的方法。
• [EN] 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS<br/>[FR] COMPOSÉS 6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE ET LEUR UTILISATION COMME MODULATEURS ALLOSTÉRIQUES NÉGATIFS DES RÉCEPTEURS MGLUR2
  申请人：JANSSEN PHARMACEUTICA NV

  公开号：WO2014195311A1

  公开（公告）日：2014-12-11

  The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula (I) as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved, especially CNS disorders.

  本发明涉及一种新型的Formula (I)的6,7-二氢吡唑并[1,5-a]吡嗪-4(5H)-酮衍生物，作为代谢型谷氨酸受体亚型2 ("mGluR2")的负变构调节剂（NAMs）。该发明还涉及包含这些化合物的药物组合物，用于制备这些化合物和组合物的方法，以及用于预防或治疗涉及代谢型受体亚型2的疾病的化合物和组合物的用途，特别是中枢神经系统疾病。
• PHARMACEUTICAL COMPOSITION FOR MODULATING THE RESPONSE OF A GABA-A RECEPTOR
  申请人：Universität Wien

  公开号：EP3498273A1

  公开（公告）日：2019-06-19

  The present invention relates to a pharmaceutical composition for use as a medicament and to the use of the pharmaceutical composition for modulating the response of a GABAA receptor and the treatment of conditions like insomnia, anxiety, cardiac disease and/or epilepsy. Furthermore, the present invention refers to new active agents suitable for said pharmaceutical compositions.

  本发明涉及一种用作药物的药物组合物，以及用于调节GABAA受体响应和治疗失眠、焦虑、心脏疾病和/或癫痫等病症的药物组合物的用途。此外，本发明涉及适用于上述药物组合物的新活性药剂。