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    • 13. 发明授权
    • Modulators of acetylcholine receptors
    • 乙酰胆碱受体的调节剂
    • US5594011A
    • 1997-01-14
    • US337640
    • 1994-11-10
    • Ian A. McDonaldJeffrey P. WhittenNicholas D. Cosford
    • Ian A. McDonaldJeffrey P. WhittenNicholas D. Cosford
    • C07D401/04C07D405/14C07F7/08A61K31/44
    • C07D401/04C07D405/14C07F7/0814
    • In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia; disorders of attention and focus; disorders of extrapyramidal motor function; mood and emotional disorders; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function; pheochromocytoma; cardiovascular dysfunction hypertension and cardia arrhythmias; comedication in surgical procedures, and the like.
    • 根据本发明,提供了一类作为乙酰胆碱受体调节剂的吡啶化合物。 本发明的化合物从其结合位点取代乙酰胆碱受体配体。 本发明化合物可以作为乙酰胆碱受体的激动剂,部分激动剂,拮抗剂或变构调节剂,并且可用于各种治疗应用,例如治疗阿尔茨海默病和涉及记忆丧失和/或痴呆的其它病症; 注意力集中的障碍; 锥体束运动功能紊乱; 情绪和情绪障碍; 药物滥用,包括戒断综合征和替代治疗; 神经内分泌障碍和食物摄入失调; 伤害感受障碍和疼痛控制; 自主神经障碍包括胃肠蠕动和功能障碍; 嗜铬细胞瘤 心血管功能障碍高血压和心律失常; 外科手术中的喜剧等。
    • 15. 发明授权
    • Methods of modulating processes mediated by excitatory amino acid receptors
    • 调节由兴奋性氨基酸受体介导的过程的方法
    • US06956049B1
    • 2005-10-18
    • US09387135
    • 1999-08-31
    • Nicholas D. P. CosfordIan A. McDonaldStephen D. HessMark A. Varney
    • Nicholas D. P. CosfordIan A. McDonaldStephen D. HessMark A. Varney
    • A61K31/425C07D277/00A51K31/425
    • C07D277/22A61K31/425
    • In accordance with the present invention, there are provided methods of modulating the activity of excitatory amino acid receptors using a specifically defined class of heterocyclic compounds. In one embodiment, there are provided methods of modulating metabotropic glutamate receptors. The present invention also discloses methods of treating disease using heterocyclic compounds. Diseases contemplated include cerebral ischemia, chronic neurodegeneration, psychiatric disorders, schizophrenia, mood disorders, emotion disorders, disorders of extrapyramidal motor function, obesity, disorders of respiration, motor control and function, attention deficit disorders, concentration disorders, pain disorders, neurodegenerative disorders, epilepsy, convulsive disorders, eating disorders, sleep disorders, sexual disorders, circadian disorders, drug withdrawal, drug addiction, compulsive disorders, anxiety, panic disorders, depressive disorders, skin disorders, retinal ischemia, retinal degeneration, glaucoma, disorders associated with organ transplantation, asthma, ischemia and astrocytomas. The invention further discloses methods of preventing disease conditions related to diseases of the pulmonary system, diseases of the nervous system, diseases of the cardiovascular system, diseases of the gastrointestinal system, diseases of the endocrine system, diseases of the exocrine system, diseases of the skin, cancer and diseases of the ophthalmic system. The invention also discloses pharmaceutically acceptable salt forms of heterocyclic compounds.
    • 根据本发明,提供了使用特定限定类杂环化合物调节兴奋性氨基酸受体活性的方法。 在一个实施方案中,提供了调节代谢型谷氨酸受体的方法。 本发明还公开了使用杂环化合物治疗疾病的方法。 预期的疾病包括脑缺血,慢性神经变性,精神疾病,精神分裂症,情绪障碍,情绪障碍,锥体外系运动功能障碍,肥胖症,呼吸障碍,运动控制和功能,注意力缺陷障碍,集中症,疼痛障碍,神经变性疾病, 癫痫症,惊厥性疾病,进食障碍,睡眠障碍,性障碍,昼夜节律障碍,药物戒断,药物成瘾,强迫症,焦虑症,恐慌症,抑郁症,皮肤病症,视网膜缺血,视网膜变性,青光眼,器官移植相关疾病 ,哮喘,局部缺血和星形细胞瘤。 本发明还公开了预防与肺系统疾病,神经系统疾病,心血管系统疾病,胃肠系统疾病,内分泌系统疾病,外分泌系统疾病, 皮肤,癌症和眼科疾病。 本发明还公开了药学上可接受的杂环化合物的盐形式。
    • 16. 发明授权
    • Modulators of acetylcholine receptors
    • 乙酰胆碱受体的调节剂
    • US5723477A
    • 1998-03-03
    • US484413
    • 1995-06-07
    • Ian A. McDonaldJeffrey P. WhittenNicholas D. Cosford
    • Ian A. McDonaldJeffrey P. WhittenNicholas D. Cosford
    • C07D401/04C07D405/14C07F7/08C07D401/02A61K31/44
    • C07D401/04C07D405/14C07F7/0814
    • The present invention provides a class of pyridine compounds which are modulators of acetylcholine receptors, i.e., compounds which displace acetylcholine receptor ligands from their binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine recepters, and are useful for a variety of therapeutic applications, such as the treatment of Alzheimer's disease and other disorders involving memory loss and/or dementia; disorders of attention and focus; disorders of extrapyramidal motor function; mood and emotional disorders; substance abuse including withdrawal syndromes and substitution therapy; neuroendocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders of nociception and control of pain; autonomic disorders including dysfunction of gastrointestinal motility and function; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.
    • 本发明提供了一类吡啶化合物,其是乙酰胆碱受体的调节剂,即从其结合位点取代乙酰胆碱受体配体的化合物。 本发明化合物可用作乙酰胆碱受体的激动剂,部分激动剂,拮抗剂或变构调节剂,并且可用于各种治疗应用,例如治疗阿尔茨海默病和涉及记忆丧失和/或痴呆的其它病症; 注意力集中的障碍; 锥体束运动功能紊乱; 情绪和情绪障碍; 药物滥用,包括戒断综合征和替代治疗; 神经内分泌障碍和食物摄入异常,包括贪食症和厌食症; 伤害感受障碍和疼痛控制; 自主神经障碍包括胃肠蠕动和功能障碍; 嗜铬细胞瘤 心血管功能障碍,包括高血压和贲门节律不正,外科手术中的喜剧等。