BICYCLIC AMIDES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
    2.
    发明申请
    BICYCLIC AMIDES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 审中-公开
    用于增强谷氨酰胺能突触反应的双环酰胺

    公开(公告)号:WO2009023126A2

    公开(公告)日:2009-02-19

    申请号:PCT/US2008/009508

    申请日:2008-08-08

    IPC分类号: A61K31/519 A61K31/53

    摘要: 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, hi 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.

    摘要翻译: 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,包括增强负责基本和更高级行为的脑网络中的突触中的受体功能。 这些参与调节呼吸的脑网络以及与记忆障碍有关的认知能力,诸如在各种痴呆症中观察到的,在不同大脑区域之间的神经元活动的不平衡中,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,以及涉及神经营养因子缺乏的障碍,以及呼吸障碍如过量饮酒,阿片制剂,阿片类药物, 巴比妥类药物,麻醉剂或神经毒素,或其中呼吸抑制导致形成诸如中枢性睡眠呼吸暂停,中风性睡眠呼吸暂停,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 ,普拉德 - 威利氏综合征和溺水。在一个特定的方面,本发明涉及可用于治疗此类病症的双环酰胺化合物,以及使用这些化合物进行治疗的方法。

    BENZOXAZINES FOR ENHANCING SYNAPTIC RESPONSE
    3.
    发明申请
    BENZOXAZINES FOR ENHANCING SYNAPTIC RESPONSE 审中-公开
    用于增强反应的苯并噻唑

    公开(公告)号:WO1997036907A1

    公开(公告)日:1997-10-09

    申请号:PCT/US1997005184

    申请日:1997-03-28

    IPC分类号: C07D498/14

    CPC分类号: C07D498/04 C07D498/14

    摘要: Compounds of formula (I) in which R and R are independently selected from the group consisting of H and R O such that at least one of R and R is R O; in which R is a member selected from the group consisting of H, alkyl and halo-substituted alkyl; or R and R together form a single divalent moiety selected from the group consisting of (II), (III), (IV), (V), (VI) and (VII) are disclosed for use in enhancing synaptic responses mediated by AMPA receptors. The compounds are effective in the treatment of subjects suffering from impaired nervous or intellectual functioning due to deficiencies in the number or strength of excitatory synapses or in the number of AMPA receptors. The compounds can also be used for the treatment of non-impaired subjects for enhancing performance in sensory-motor and cognitive tasks which depend on brain networks utilizing AMPA receptors, for improving the performance of subjects with memory deficiencies, for treating schizophrenia, and for improving memory encoding.

    摘要翻译: 其中R 1和R 2独立地选自H和R 4 O的式(I)化合物,使得R 1和R 2中的至少一个是R 1, 4> O; 其中R 4是选自H,烷基和卤素取代的烷基的成员; 或者R 1和R 2一起形成选自(II),(III),(IV),(V),(VI)和(VII)的单一二价基团,用于 增强由AMPA受体介导的突触反应。 由于兴奋性突触的数量或强度的缺乏或AMPA受体的数量的不足,这些化合物对于遭受神经或智力功能受损的受试者是有效的。 这些化合物还可用于治疗非受损受试者,以增强感觉运动和认知任务中的表现,这取决于使用AMPA受体的脑网络,改善记忆缺陷的受试者的表现,治疗精神分裂症和改善 内存编码。

    BICYCLIC AMIDE DERIVATIVES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
    4.
    发明申请
    BICYCLIC AMIDE DERIVATIVES FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 审中-公开
    用于增强谷氨酸反应的双相酰胺衍生物

    公开(公告)号:WO2010087981A2

    公开(公告)日:2010-08-05

    申请号:PCT/US2010/000255

    申请日:2010-01-29

    摘要: 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, 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 bicyclic amide compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

    摘要翻译: 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,以及诸如卒中诱导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,肥胖低通气综合征,婴儿猝死综合征 综合征,Rett综合征,脊髓损伤,创伤性脑损伤,Cheney-Stokes呼吸,Ondine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。

    3-SUBSTITUTED-[1,2,3]-BENZOTRIAZINONE COMPOUND FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
    5.
    发明申请
    3-SUBSTITUTED-[1,2,3]-BENZOTRIAZINONE COMPOUND FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 审中-公开
    3-取代 - [1,2,3] - 苯并噻嗪酮化合物,用于增强谷氨酸反应性

    公开(公告)号:WO2008085506A1

    公开(公告)日:2008-07-17

    申请号:PCT/US2007/026416

    申请日:2007-12-28

    IPC分类号: A01N57/00 A61K31/675

    CPC分类号: C07D498/04

    摘要: This invention relates to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias, and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to a compound useful for treatment of such conditions, and methods of using this compound for such treatment.

    摘要翻译: 本发明涉及预防和治疗脑功能不全,包括在负责高阶行为的脑网络突触中增强受体功能。 这些脑网络涉及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,以及不同脑区域之间神经元活动的不平衡,如帕金森病,精神分裂症和情感障碍等疾病中所提出的。 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,以及使用该化合物进行这种治疗的方法。

    3-SUBSTITUTED-[1,2,3]BENZOTRIAZINONE COMPOUNDS FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
    6.
    发明申请
    3-SUBSTITUTED-[1,2,3]BENZOTRIAZINONE COMPOUNDS FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES 审中-公开
    3-取代的 - [1,2,3]苯并噻嗪酮化合物,用于增强谷氨酸反应性

    公开(公告)号:WO2008085505A1

    公开(公告)日:2008-07-17

    申请号:PCT/US2007/026415

    申请日:2007-12-28

    IPC分类号: A01N43/64 A61K31/53

    摘要: This invention relates to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed in a variety of dementias and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.

    摘要翻译: 本发明涉及预防和治疗脑功能不全,包括在负责高阶行为的脑网络突触中增强受体功能。 这些脑网络涉及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,以及在不同脑区域之间的神经元活动的不平衡,如在帕金森病,精神分裂症和情感障碍等疾病中所提出的。 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。