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    • 4. 发明授权
    • Bicyclic amide derivatives for enhancing glutamatergic synaptic responses
    • 用于增强谷氨酸能突触反应的双环酰胺衍生物
    • US08507482B2
    • 2013-08-13
    • US13348171
    • 2012-01-11
    • Rudolf MuellerLeslie J. Street
    • Rudolf MuellerLeslie J. Street
    • A61K31/5375C07D265/28
    • C07D498/08A61K31/5375A61K45/06A61K2300/00
    • 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 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, 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 conditions such as stroke-induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, among others. In a particular aspect, the invention relates to bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.
    • 本发明涉及用于预防和治疗脑功能不全的化合物,药物组合物和方法,包括在负责基本和高级行为的脑网络中的突触中增强受体功能。 参与如记忆障碍相关的认知能力的这些脑网络,例如在各种痴呆症中观察到的,在不同脑区域之间的神经元活动不平衡中,正如帕金森病,精神分裂症,睡眠呼吸暂停症, 注意缺陷多动障碍和情感或情绪障碍,以及涉及神经营养因子缺乏的疾病,以及诸如卒中诱发的中枢性睡眠呼吸暂停,阻塞性睡眠呼吸暂停,先天性通气不足综合征等疾病。 在一个特定方面,本发明涉及可用于治疗这些病症的双环酰胺化合物,以及使用这些化合物进行这种治疗的方法。
    • 10. 发明授权
    • Di-substituted amides for enhancing glutamatergic synaptic responses
    • 用于增强谷氨酸能突触反应的二取代酰胺
    • US08404682B2
    • 2013-03-26
    • US13226146
    • 2011-09-06
    • Leslie StreetRudolf MuellerSteven Lee
    • Leslie StreetRudolf MuellerSteven Lee
    • A61K31/5377A61K31/4245A61K31/4439A61K31/454A61K31/433A61K31/498
    • A61K31/4245A61K45/06C07D271/12C07D285/14C07D405/12C07D413/12C07D417/12
    • 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.
    • 本发明涉及用于预防和治疗脑功能不全的化合物,药物组合物和方法,包括在负责基本和高级行为的脑网络中的突触中增强受体功能。 涉及呼吸调节的这些脑网络,以及与记忆障碍有关的认知能力,例如在各种痴呆中观察到的,在不同脑区域之间的神经元活动不平衡中,如在帕金森病, 精神分裂症,呼吸抑制,睡眠呼吸暂停,注意缺陷多动障碍和情感或情绪障碍,以及涉及神经营养因子缺乏的疾病,以及呼吸障碍,例如过量的酒精,阿片剂,阿片样物质, 巴比妥酸盐,麻醉剂或神经毒素,或呼吸抑制结果形成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,先天性通气不足综合征,肥胖低通气综合征,婴儿猝死综合征 ,Rett综合征,脊髓损伤,创伤性脑损伤,Cheney-Stokes呼吸,Ondines诅咒 ,Prader-Willi综合征和溺水。 在一个特定方面,本发明涉及可用于治疗这些病症的化合物,以及使用这些化合物进行这种治疗的方法。