GYKI52466,盐酸盐 | 192065-56-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯二氮卓类
• 中文名称: GYKI52466,盐酸盐
• 中文别名: 4-(8-甲基-9H-[1,3]二氧杂环戊并[4,5-h][2,3]苯并二氮杂卓-5-基)苯胺盐酸盐(1:1)；AMPA受体选择性阻断剂前体
• 英文名称: GYKI 52466 hydrochloride
• 英文别名: 4-(8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl)aniline;hydrochloride
• CAS: 192065-56-8
• 化学式: C17H16ClN3O2
• 分子量: 329.8
• InChiKey: RUBSCPARMVJNKX-UHFFFAOYSA-N

物化性质

• 溶解度：
  DMSO：可溶0.39mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  3.19
• 重原子数：
  23
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.18
• 拓扑面积：
  69.2
• 氢给体数：
  2
• 氢受体数：
  5

安全信息

• 海关编码：
  2934999090

文献信息

• [EN] LACTONE INTERMEDIATES OF NICOTINAMIDE RIBOSIDE AND NICOTINATE RIBOSIDE<br/>[FR] INTERMÉDIAIRES DE LACTONE DE NICOTINAMIDE RIBOSIDE ET DE NICOTINATE RIBOSIDE
  申请人：UNIV BELFAST

  公开号：WO2018033639A1

  公开（公告）日：2018-02-22

  The present invention is directed to lactones of the following structural formula for use as precursors of NAD, and their use as nutritional supplements.

  本发明涉及以下结构式的内酯，用作NAD的前体，并且它们的用途作为营养补充剂。
• [EN] PREPARATION AND USE OF CRYSTALLINE BETA-D-NICOTINAMIDE RIBOSIDE<br/>[FR] PRÉPARATION ET UTILISATION DE BÊTA-D-NICOTINAMIDE RIBOSIDE CRISTALLIN
  申请人：GLAXOSMITHKLINE IP NO 2 LTD

  公开号：WO2015186068A1

  公开（公告）日：2015-12-10

  Provided herein are crystalline beta-D-nicotinamide riboside chloride compositions and methods of preparation and use thereof. Also provided are related pharmaceutical compositions and methods of use thereof. The crystalline beta-D-nicotinamide riboside chloride compositions may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, or for increasing insulin sensitivity in a subject.

  本文提供晶体质的β-D-烟酰胺核苷酸氯化物组合物的制备和使用方法。还提供相关的药物组合物及其使用方法。晶体质的β-D-烟酰胺核苷酸氯化物组合物可用于治疗需要提高NAD水平的疾病或疾病，包括线粒体疾病或疾病，胰岛素抵抗，代谢综合征，糖尿病，肥胖症或用于增加受试者胰岛素敏感性。
• [EN] SUBSTITUTED 2,3-BENZODIAZEPIN-4-ONES AND THE USE THEREOF<br/>[FR] 2,3-BENZODIAZEPINE-4-ONES A SUBSTITUTION ET LEUR UTILISATION
  申请人：COCENSYS, INC.

  公开号：WO1997034878A1

  公开（公告）日：1997-09-25

  (EN) The invention relates to substituted 2,3-benzodiazepin-4-ones which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, CMV retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition enhancers. The invention also is directed to the process for the preparation of the substituted 2,3-benzodiazepin-4-ones.(FR) L'invention concerne des 2,3-benzodiazépine-4-ones à substitution, lesquelles sont des antagonistes ou des modulateurs positifs de récepteurs AMPA, ainsi que leur emploi dans le traitement, la prévention ou l'amélioration de pertes neuronales associées à l'ictus, l'ischémie globale et focale, les traumas du système nerveux central, l'hypoglycémie et la chirurgie, ainsi que dans le traitement ou l'amélioration d'états associés à des maladies neurodégénératives, y compris la maladie d'Alzheimer, la sclérose latérale amyotrophique, la maladie de Huntington, la maladie de Parkinson et le syndrome de Down, dans le traitement, la prévention ou l'amélioration d'états associés aux conséquences négatives de la surstimulation des acides aminés excitateurs, dans le traitement ou l'amélioration d'états associés à l'angoisse, la psychose, les convulsions, la douleur chronique, le glaucome, la rétinite à CMV, l'incontinence urinaire, les spasmes musculaires et pour pratiquer une anesthésie. Les composés de l'invention sont également utiles dans le traitement ou l'amélioration d'états associés aux conséquences négatives d'une déficience en acides aminés excitateurs telle que la schizophrénie, la maladie d'Alzheimer et la malnutrition ainsi que le développement anormal des nerfs, et en tant qu'activateur de la cognition. L'invention concerne également le procédé de préparation des 2,3-benzodiazepine-4-ones à substitution.

  本发明涉及取代的2,3-苯二氮平-4-酮，其为AMPA受体的拮抗剂或正向调节剂，并用于治疗、预防或改善与中风、全局和局部缺血、中枢神经系统创伤、低血糖和手术相关的神经元丢失，以及治疗或改善包括阿尔茨海默病、肌萎缩性侧索硬化症、亨廷顿病、帕金森病和唐氏综合征在内的神经退行性疾病，治疗、预防或改善兴奋性氨基酸过度刺激的不良后果，治疗或改善焦虑、精神病、惊厥、慢性疼痛、青光眼、CMV视网膜炎、尿失禁、肌肉痉挛和诱导麻醉，以及治疗或改善兴奋性氨基酸缺乏的不良后果，如精神分裂症、阿尔茨海默病和营养不良和神经发育不良，并作为认知增强剂。本发明还涉及制备取代的2,3-苯二氮平-4-酮的过程。
• Substituted quinazolines and analogs and the use thereof
  申请人：Euro-Celtique S.A.

  公开号：US20030033089A1

  公开（公告）日：2003-02-13

  The invention relates to novel quinazolines and heterocycles which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating, preventing or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, myoclonus, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition and learning enhancers.

  本发明涉及新型的喹唑啉和杂环化合物，它们是AMPA受体的拮抗剂或正向调节剂，并用于治疗、预防或改善与中风、全局和局部缺血、中枢神经系统创伤、低血糖和手术相关的神经元丧失，以及治疗或改善包括阿尔茨海默病、肌萎缩性侧索硬化、亨廷顿病、帕金森病和唐氏综合症在内的神经退行性疾病，治疗、预防或改善兴奋性氨基酸过度刺激的不良后果，治疗、预防或改善焦虑、精神病、惊厥、慢性疼痛、青光眼、视网膜炎、尿失禁、肌肉痉挛和诱导麻醉，以及治疗或改善兴奋性氨基酸缺乏的不良后果，如精神分裂症、肌阵挛、阿尔茨海默病和营养不良和神经发育不良，并作为认知和学习增强剂。
• Pharmaceutical combinations for the treatment of stroke and traumatic brain injury
  申请人：——

  公开号：US20020045656A1

  公开（公告）日：2002-04-18

  This invention relates to methods of treating traumatic brain injury (TBI) or hypoxic or ischemic stroke, comprising administering to a patient in need of such treatment an NR2B subtype selective N-methyl-D-aspartate (NMDA) receptor antagonist in combination with either: (a) a neutrophil inhibitory factor (NIF); (b) a sodium channel antagonist; (c) a nitric oxide synthase (NOS) inhibitor; (d) a glycine site antagonist; (e) a potassium channel opener; (f) an AMPA/kainate receptor antagonist; (g) a calcium channel antagonist; (h) a GABA-A receptor modulator (e.g., a GABA-A receptor agonist); or (i) an antiinflammatory agent.

  本发明涉及治疗创伤性脑损伤（TBI）或缺氧性或缺血性中风的方法，包括向需要此类治疗的患者注射NR2B亚型选择性N-甲基-D-天门冬氨酸（NMDA）受体拮抗剂，与以下任一组合：（a）中性粒细胞抑制因子（NIF）；（b）钠通道拮抗剂；（c）一氧化氮合酶（NOS）抑制剂；（d）甘氨酸位点拮抗剂；（e）钾通道开放剂；（f）AMPA / kainate受体拮抗剂；（g）钙通道拮抗剂；（h）GABA-A受体调节剂（例如，GABA-A受体激动剂）；或（i）抗炎药物。