利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

88 条记录 (耗时 0.037 秒)

    Substituted pyridine compounds useful as modulators of acetylcholine receptors
    1.
    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。

    Substituted aryl compounds useful as modulators of acetylcholine receptors
    2.
    发明授权
    Substituted aryl compounds useful as modulators of acetylcholine receptors 失效
    可用作乙酰胆碱受体调节剂的取代芳基化合物

    公开(公告)号：US06316490B1

    公开(公告)日：2001-11-13

    申请号：US08860954

    申请日：1997-07-08

    申请人： Jean-Michel Vernier ,  Ian A. McDonald

    发明人： Jean-Michel Vernier ,  Ian A. McDonald

    IPC分类号： C07D20708

    CPC分类号： B64C23/06 ,  Y02T50/162

    摘要： In accordance with the present invention, a novel class of substituted aryl compounds (containing ether, ester, amide, ketone or thioether substitution) 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 displacing one or more acetylcholine receptor ligands, e.g., 3H-nicotine, from mammalian neuronal membrane binding sites. Invention compounds may act as agonists, partial agonists, antagonists or allosteric modulators of acetylcholine receptors. Therapeutic indications for compounds with activity as 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 of nociception and control of pain; autonomic disorders including dysfimction 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： 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芳基化合物（含有醚，酯，酰胺，酮或硫醚取代基）。 在特定方面，本发明的化合物能调节乙酰胆碱受体。 本发明的化合物能够从哺乳动物神经元膜结合位点置换一个或多个乙酰胆碱受体配体，例如3H-烟碱。 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。 具有作为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; 伤害感受障碍和疼痛控制; 自主神经障碍包括消化道运动功能障碍和功能如炎症性肠病，肠易激综合征，腹泻，便秘，胃酸分泌和溃疡; 嗜铬细胞瘤，包括高血压和心律失常的心血管功能障碍，以及在外科应用中的共用药用途。

    Purines as reverse transcriptase inhibitors
    5.
    发明授权
    Purines as reverse transcriptase inhibitors 失效
    嘌呤作为逆转录酶抑制剂

    公开(公告)号：US08372852B2

    公开(公告)日：2013-02-12

    申请号：US13470122

    申请日：2012-05-11

    申请人： Alex Shaginian ,  Samedy Ouk ,  Jean-Michel Vernier ,  Anthony B. Pinkerton

    发明人： Alex Shaginian ,  Samedy Ouk ,  Jean-Michel Vernier ,  Anthony B. Pinkerton

    IPC分类号： C07D473/28 ,  C07D473/34 ,  A61K31/52 ,  A61P31/18 ,  C07D487/04 ,  A61K31/519

    CPC分类号： C07D487/04 ,  C07D473/18

    摘要： Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders. In some embodiments, the enzyme inhibitors are compounds of formula (I) or a pharmaceutically acceptable salt or tautomer thereof:

    摘要翻译： 本文描述的是新的酶抑制剂。 在一些实施方案中，酶抑制剂是逆转录酶抑制剂，特别是HIV逆转录酶抑制剂。 本文还描述了含有它们的组合物和使用它们的方法。 因此，本文所述的化合物和组合物可用于体外和体内抑制HIV逆转录酶，作为治疗或预防HIV，AIDS或相关病症的方法。 在一些实施方案中，酶抑制剂是式（I）的化合物或其药学上可接受的盐或互变异构体：

    Substituted arylamino-1,2,3,4-tetrahydro naphthalenes and-2,3-dihydro-1H-indenes as potassium channel modulators
    8.
    发明授权
    Substituted arylamino-1,2,3,4-tetrahydro naphthalenes and-2,3-dihydro-1H-indenes as potassium channel modulators 有权
    取代的芳基氨基-1,2,3,4-四氢萘和2,3-二氢-1H-茚作为钾通道调节剂

    公开(公告)号：US07960436B2

    公开(公告)日：2011-06-14

    申请号：US11810114

    申请日：2007-06-04

    申请人： Huanming Chen ,  Jean-Michel Vernier

    发明人： Huanming Chen ,  Jean-Michel Vernier

    IPC分类号： A61K31/16 ,  C07C235/16

    CPC分类号： C07C271/30 ,  C07C233/43 ,  C07C2601/08 ,  C07C2602/08 ,  C07C2602/10

    摘要： This invention provides compounds of formula I where Ar1 is a 5- to 10-member mono- or bicyclic aromatic group, optionally substituted; where the —NR3R4 group is situated ortho to the NHC(═X) group; n=1 or 2; X═O or S; Y is O or S; and q=1 or 0. The invention also provides pharmaceutical compositions comprising compounds of formula I and/or salts, esters, and prodrugs thereof. These compounds modulate the activation and inactivation of potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders—such as seizure disorders—which are affected by modulation of potassium ion channels.

    摘要翻译： 本发明提供式I化合物，其中Ar 1是任选取代的5-至10-元单环或双环芳基; 其中-NR 3 R 4基团位于NHC（= X）基团的邻位; n = 1或2; X = O或S; Y为O或S; 并且q = 1或0.本发明还提供包含式I化合物和/或其盐，酯和前药的药物组合物。 这些化合物调节钾通道的活化和失活。 这些化合物可用于治疗和预防受钾离子通道调节影响的疾病和病症（例如发作障碍）。