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    Substituted pyridine compounds useful as modulators of acetylcholine receptors
    71.
    发明授权
    Substituted pyridine compounds useful as modulators of acetylcholine receptors 失效
    可用作乙酰胆碱受体调节剂的取代吡啶化合物

    公开(公告)号：US06632823B1

    公开(公告)日：2003-10-14

    申请号：US08996308

    申请日：1997-12-22

    申请人： Jean-Michel Vernier ,  Nicholas D. P. Cosford ,  Ian A. McDonald

    发明人： Jean-Michel Vernier ,  Nicholas D. P. Cosford ,  Ian A. McDonald

    IPC分类号： C07D21300

    CPC分类号： C07D213/70 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/46 ,  C07D213/32 ,  C07D213/52 ,  C07D401/12 ,  C07D451/02 ,  C07D451/04 ,  C07D471/08

    摘要： In accordance with the present invention, a novel class of substituted pyridine compounds (optionally containing ether, ester, amide, ketone or thioether substitutions) that promote the release of ligands involved in neurotransmission have been discovered. In a particular aspect compounds of the present invention are capable of modulating acetylcholine receptors. The compounds of the present invention are capable of modulating acetylcholine receptors. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors. Therapeutic indications for compounds with activity at acetylcholine receptors include diseases of the central nervous system such as Alzheimer's disease and other diseases involving memory loss and/or dementia (including AIDS dementia); cognitive dysfunction (including disorders of attention, focus and concentration), disorders of extrapyramidal motor function such as Parkinson's disease, progressive supramuscular palsy, Huntington's disease, Gilles de la Tourette syndrome and tardive dyskinesia; mood and emotional disorders such as depression, anxiety and psychosis; substance abuse including withdrawal symptoms and substitution therapy; neurocrine disorders and dysregulation of food intake, including bulimia and anorexia; disorders or 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 cardiac arrhythmias, as well as co-medication uses in surgical applications.

    摘要翻译： 已经发现，根据本发明，已经发现了促进参与神经传递的配体释放的新一类取代的吡啶化合物（任选地含有醚，酯，酰胺，酮或硫醚取代）。 在具体方面，本发明的化合物能够调节乙酰胆碱受体。 本发明的化合物能够调节乙酰胆碱受体。 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。 具有乙酰胆碱受体活性的化合物的治疗适应症包括中枢神经系统的疾病如阿尔茨海默氏病和涉及记忆丧失和/或痴呆（包括AIDS痴呆）的其它疾病; 认知功能障碍（包括注意力集中和集中注意力障碍），帕特森氏病，锥体运动功能障碍，进行性肌肉麻痹，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，焦虑和精神病; 药物滥用，包括戒断症状和替代治疗; 神经分泌障碍和食物摄入异常，包括贪食症和厌食症; 疾病或疼痛的伤害和控制; 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，包括高血压和心律失常，以及在外科应用中的共同用药用途。

    Derivatives of 4-(N-azacycloalkyl) anilides as potassium channel modulators
    76.
    发明授权
    Derivatives of 4-(N-azacycloalkyl) anilides as potassium channel modulators 有权
    4-（N-氮杂环烷基）苯胺的衍生物作为钾通道调节剂

    公开(公告)号：US08367684B2

    公开(公告)日：2013-02-05

    申请号：US12138251

    申请日：2008-06-12

    申请人： Jean-Michel Vernier ,  Samedy Ouk ,  Martha A. De La Rosa

    发明人： Jean-Michel Vernier ,  Samedy Ouk ,  Martha A. De La Rosa

    IPC分类号： A01N43/54 ,  A61K31/505

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04

    摘要： This invention provides potassium channel modulators which are compounds of formula I where at least one of W and Z is N; where the moiety is one of Groups A or B below A where Ar is a 1,2-fused, six membered ring aromatic group, bearing substituents R1 and R2 as defined below, and containing zero or one ring nitrogen atom; and where other substituents are defined herein. The invention also provides a composition comprising a pharmaceutically acceptable carrier and at least one of the following: i) a pharmaceutically effective amount of a compound of formula I and ii) a pharmaceutically acceptable salt, ester, or prodrug thereof. 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, ester, or prodrug thereof.

    摘要翻译： 本发明提供钾通道调节剂，其为W和Z中至少一个为N的式I化合物; 其中该部分是A之下的A或B族之一，其中Ar是1,2-稠合的六元环芳族基团，带有如下定义的取代基R 1和R 2，并且含有一个或多个环氮原子; 并且其中其它取代基在本文中定义。 本发明还提供包含药学上可接受的载体和至少一种以下的组合物：i）药学有效量的式I化合物和ii）其药学上可接受的盐，酯或前药。 本发明还提供了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，酯或前药 。