SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATIOSUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECN AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS EPTORS
    53.
    发明申请
    SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATIOSUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECN AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS EPTORS 审中-公开
    取代的吡啶衍生物,其制备用吡啶衍生物,其制备及其作为乙酰胆碱受体调节剂的作用及其作为乙酰胆碱受体调节剂的用途

    公开(公告)号:WO9631475A3

    公开(公告)日:1997-02-06

    申请号:PCT/US9605078

    申请日:1996-04-04

    CPC classification number: C07D401/06 C07D213/38 C07F7/0814

    Abstract: In accordance with the present invention, there are provided compounds having the structure (I), wherein: A, B, N?α, Rα, Z, R2, R4, R5 and R6¿ are defined as in the description. 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 (including AIDS dementia); disorders of attention and focus (such as attention deficit disorders); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; 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 such as inflammatory bowel disease, irritable bowel syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.

    Abstract translation: 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氏病和涉及记忆丧失和/或痴呆的其它病症(包括AIDS痴呆) ; 注意力集中障碍(如注意力缺陷障碍); 锥体外系运动功能紊乱,如帕金森病,亨廷顿疾病,吉列斯·杜列特综合征和迟发性运动障碍; 情绪和情绪障碍如抑郁,恐慌,焦虑和精神病; 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功能障碍和功能障碍,如炎性肠病,肠易激综合征,腹泻,便秘,胃酸分泌和溃疡; 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。

    SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS
    54.
    发明申请
    SUBSTITUTED PYRIDINE DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MODULATORS OF ACETYLCHOLINE RECEPTORS 审中-公开
    取代的吡啶衍生物,其制备及其作为乙酰胆碱受体的调节剂

    公开(公告)号:WO1996031475A2

    公开(公告)日:1996-10-10

    申请号:PCT/US1996005078

    申请日:1996-04-04

    CPC classification number: C07D401/06 C07D213/38 C07F7/0814

    Abstract: In accordance with the present invention, there are provided compounds having the structure (I), wherein: A, B, N , R , Z, R , R , R and R are defined as in the description. 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 (including AIDS dementia); disorders of attention and focus (such as attention deficit disorders); disorders of extrapyramidal motor function such as Parkinson's disease, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, panic, anxiety and psychosis; 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 such as inflammatory bowel disease, irritable bowels syndrome, diarrhea, constipation, gastric acid secretion and ulcers; pheochromocytoma; cardiovascular dysfunction including hypertension and cardia arrhythmias, comedication in surgical procedures, and the like.

    Abstract translation: 根据本发明,提供具有结构(I)的化合物,其中:A,B,N,R,Z,R 2,R 4,R 5, 和R 6如在说明书中所定义。 本发明的化合物从其结合位点取代乙酰胆碱受体配体。 本发明化合物可以充当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氏病和涉及记忆丧失和/或痴呆的其它病症(包括AIDS痴呆) ; 注意力障碍(如注意力缺陷障碍); 锥体外系运动功能紊乱,如帕金森病,亨廷顿疾病,吉列斯·杜列特综合征和迟发性运动障碍; 心情和情绪障碍如抑郁,恐慌,焦虑和精神病; 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,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功能障碍和功能障碍,如炎性肠病,肠易激综合征,腹泻,便秘,胃酸分泌和溃疡; 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。

    NAPHTHYRIDINE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS
    60.
    发明申请
    NAPHTHYRIDINE DERIVATIVES AS POTASSIUM CHANNEL MODULATORS 审中-公开
    萘啶衍生物作为钾通道调节剂

    公开(公告)号:WO2009018466A1

    公开(公告)日:2009-02-05

    申请号:PCT/US2008/071803

    申请日:2008-07-31

    CPC classification number: C07D471/04

    Abstract: This invention provided compounds of formula (I), where W and Z are, independently, CH or N, and where other substituents are defined herein. Such compounds are potassium channel modulators. The invention also provides a composition comprising a pharmaceutically acceptable carrier or excipient and at least one of the following: a pharmaceutically effective amount of a compound of formula (I); a pharmaceutically acceptable salt of a compound of formula (I); a pharmaceutically acceptable ester of a compound of formula (I). The invention also provides a method of preventing or treating a disease or disorder which is affected by activities of potassium channels, comprising administering to a patient in need thereof a therapeutically effective amount of a compound of formula (I) or a salt or ester or solvate thereof.

    Abstract translation: 本发明提供式(I)化合物,其中W和Z独立地是CH或N,并且其中其它取代基在本文中定义。 这些化合物是钾通道调节剂。 本发明还提供包含药学上可接受的载体或赋形剂和以下至少一种的组合物:药学上有效量的式(I)化合物; 式(I)化合物的药学上可接受的盐; 式(I)化合物的药学上可接受的酯。 本发明还提供了一种预防或治疗受钾通道活性影响的疾病或病症的方法,包括向有需要的患者施用治疗有效量的式(I)化合物或其盐或酯或溶剂合物 它们。

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