CX1739 | 1086377-48-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶二唑类
• 英文名称: CX1739
• 英文别名: N-methyl-N-(tetrahydro-2H-pyran-4-yl)-2,1,3-benzoxadiazole-5-carboxamide；Upb5G360MA；N-methyl-N-(oxan-4-yl)-2,1,3-benzoxadiazole-5-carboxamide
• CAS: 1086377-48-1
• 化学式: C₁₃H₁₅N₃O₃
• 分子量: 261.28
• InChiKey: IRYRMRDDVXULFG-UHFFFAOYSA-N

物化性质

• 沸点：
  442.1±55.0 °C(Predicted)
• 密度：
  1.31±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  68.5
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  6-carboxybenzo[c][1,2,5]oxadiazole 1-oxide 在 palladium 10% on activated carbon 氯化亚砜 、 氢气 、 sodium hydroxide 、 亚磷酸三乙酯 作用下， 以 甲醇 、 乙醇 、 甲苯 为溶剂， 反应 10.0h， 生成 CX1739
  参考文献：
  名称：

  WO2008/143963

  摘要：

  公开号：

文献信息

• DI-SUBSTITUTED AMIDES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
  申请人：Street Leslie

  公开号：US20120035173A1

  公开（公告）日：2012-02-09

  This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, among numerous others. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

  本发明涉及化合物、药物组合物及其在预防和治疗脑供血不足方面的应用方法，包括增强与基本和高级行为有关的脑网络中突触中受体功能。这些脑网络涉及呼吸调节和与记忆障碍相关的认知能力，例如在各种痴呆症中观察到的情况，以及在不同脑区域之间的神经活动失衡中所建议的帕金森病、精神分裂症、呼吸抑制、睡眠呼吸暂停、注意力缺陷多动障碍和情感或心境障碍等多种疾病。在一个特定的方面，本发明涉及用于治疗此类疾病的化合物，以及使用这些化合物进行此类治疗的方法。
• Di-substituted amides for enhancing glutamatergic synaptic responses
  申请人：Cortex Pharmaceuticals, Inc.

  公开号：US08013003B2

  公开（公告）日：2011-09-06

  This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

  本发明涉及化合物、药物组合物及其使用方法，用于预防和治疗脑血供不足，包括增强大脑网络中负责基本和高级行为的突触受体功能。这些大脑网络涉及呼吸调节和与记忆障碍相关的认知能力，例如多种痴呆症，神经元活动在不同脑区之间的失衡，如帕金森病、精神分裂症、呼吸抑制、睡眠呼吸暂停、注意力缺陷多动障碍和情感或情绪障碍，以及神经营养因子缺乏相关的疾病，以及呼吸方面的疾病，如酒精、鸦片、阿片、巴比妥酸盐、麻醉剂或神经毒素过量，或呼吸抑制由中枢性睡眠呼吸暂停、中风引起的中枢性睡眠呼吸暂停、阻塞性睡眠呼吸暂停、先天性低通气综合症、肥胖低通气综合症、婴儿猝死综合症、雷特综合症、脊髓损伤、创伤性脑损伤、切尼-斯托克斯呼吸、昏迷和溺水等医疗状况引起。在特定方面，本发明涉及用于治疗这些疾病的化合物以及使用这些化合物进行治疗的方法。
• Di-Substituted Amides for Enhancing Glutamatergic Synaptic Responses
  申请人：Cortex Pharmaceuticals, Inc.

  公开号：US20130137733A1

  公开（公告）日：2013-05-30

  This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi's syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

  本发明涉及化合物、制药组合物和用于预防和治疗脑供血不足的方法，包括增强大脑网络中负责基本和高级行为的突触中受体的功能。这些大脑网络涉及呼吸调节和与记忆障碍相关的认知能力，例如在多种痴呆症中观察到的情况，以及在不同脑区域之间的神经活动失衡中所建议的疾病，如帕金森病、精神分裂症、呼吸抑制、睡眠呼吸暂停、注意力缺陷多动症和情感或情绪障碍，以及神经营养因子缺乏所涉及的疾病，以及呼吸方面的疾病，例如酒精、鸦片、阿片类、巴比妥类、麻醉剂或神经毒素过量，或呼吸抑制由中枢性睡眠呼吸暂停、中风引起的中枢性睡眠呼吸暂停、阻塞性睡眠呼吸暂停、先天性低通气综合征、肥胖性低通气综合征、婴儿猝死综合征、雷特综合征、脊髓损伤、颅脑创伤、切尼-斯托克斯呼吸、昏迷和溺水等医疗状况引起。在特定方面，本发明涉及用于治疗这些疾病的化合物，以及使用这些化合物进行治疗的方法。
• WO2008143963A1
  申请人：——

  公开号：——

  公开（公告）日：——
• Compositions And Methods For Treating Attention Deficit Disorders
  申请人：LIPPA Arnold Stan

  公开号：US20190112300A1

  公开（公告）日：2019-04-18

  The present invention relates to ampakines, including low impact ampakines, and pharmaceutical compositions and methods employing ampakines for treating central nervous system (CNS) disorders, including attention deficit disorders. Novel compositions and methods are provided employing anti-ADHD ampakines to treat attention deficit hyperactivity disorder (ADHD) and related cognitive, behavioral and psychiatric conditions.