Substituted quinazolines and analogs and the use thereof
    4.
    发明授权
    Substituted quinazolines and analogs and the use thereof 失效
    取代的喹唑啉和类似物及其用途

    公开(公告)号:US06765006B2

    公开(公告)日:2004-07-20

    申请号:US10219755

    申请日:2002-08-16

    IPC分类号: C07D23726

    摘要: 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.

    摘要翻译: 本发明涉及作为AMPA受体的拮抗剂或阳性调节剂的新型喹唑啉和杂环,以及其用于治疗,预防或改善与中风,全身和局灶性缺血,CNS创伤,低血糖和手术相关的神经元损失以及治疗 或改善神经变性疾病,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征,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症如精神分裂症,肌阵挛,阿尔茨海默病和营养不良及神经发育不良后果,以及认知和学习增强剂 。

    Substituted quinazolines and analogs and use thereof
    5.
    发明授权
    Substituted quinazolines and analogs and use thereof 有权
    取代的喹唑啉和类似物及其用途

    公开(公告)号:US06465472B1

    公开(公告)日:2002-10-15

    申请号:US09654839

    申请日:2000-09-01

    IPC分类号: C07D23726

    摘要: 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.

    摘要翻译: 本发明涉及作为AMPA受体的拮抗剂或阳性调节剂的新型喹唑啉和杂环,以及其用于治疗,预防或改善与中风,全身和局灶性缺血,CNS创伤,低血糖和手术相关的神经元损失以及治疗 或改善神经变性疾病,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征,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症如精神分裂症,肌阵挛的不良后果。 阿尔茨海默病和营养不良和神经发育不良,以及认知和学习增强剂。

    Isoquinolinamine and phthalazinamine derivatives: corticotropin-releasing factor receptor CRF1 specific ligands
    7.
    发明授权
    Isoquinolinamine and phthalazinamine derivatives: corticotropin-releasing factor receptor CRF1 specific ligands 失效
    异喹啉胺和酞嗪胺衍生物:促肾上腺皮质激素释放因子受体CRF1特异性配体

    公开(公告)号:US06353103B1

    公开(公告)日:2002-03-05

    申请号:US09648200

    申请日:2000-08-25

    IPC分类号: C07D23726

    摘要: Disclosed are compounds that are highly selective partial agonists or antagonists at human CRF1 receptors that are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety. The compounds have the formula or the pharmaceutically acceptable salts thereof wherein Ar, R1, R2, R3, R4 and W are various organic and inorganic substituents.

    摘要翻译: 公开了在人CRF1受体上是高选择性部分激动剂或拮抗剂的化合物,其可用于治疗应激相关疾病如创伤后应激障碍(PTSD)以及抑郁症,头痛和焦虑症的诊断和治疗。 所述化合物具有其药学上可接受的盐,其中Ar,R 1,R 2,R 3,R 4和W是各种有机和无机取代基。