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    Substituted pyridines useful as modulators of acethylcholine receptors
    6.
    发明授权
    Substituted pyridines useful as modulators of acethylcholine receptors 失效
    取代的吡啶可用作乙酰胆碱受体的调节剂

    公开(公告)号：US5852041A

    公开(公告)日：1998-12-22

    申请号：US486324

    申请日：1995-06-07

    申请人： Nicholas D. Cosford ,  Jean-Michel Vernier

    发明人： Nicholas D. Cosford ,  Jean-Michel Vernier

    IPC分类号： C07D213/48 ,  C07D213/82 ,  A61K31/44 ,  C07D213/02

    CPC分类号： C07D213/82 ,  C07D213/48

    摘要： In accordance with the present invention, there 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 (including AIDS dementia); disorders of attention and focus (such as attention deficit disorder); 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.

    摘要翻译： 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。

    Modulators of acetylcholine receptors
    7.
    发明授权
    Modulators of acetylcholine receptors 失效
    乙酰胆碱受体的调节剂

    公开(公告)号：US5723477A

    公开(公告)日：1998-03-03

    申请号：US484413

    申请日：1995-06-07

    申请人： Ian A. McDonald ,  Jeffrey P. Whitten ,  Nicholas D. Cosford

    发明人： Ian A. McDonald ,  Jeffrey P. Whitten ,  Nicholas D. Cosford

    IPC分类号： C07D401/04 ,  C07D405/14 ,  C07F7/08 ,  C07D401/02 ,  A61K31/44

    CPC分类号： C07D401/04 ,  C07D405/14 ,  C07F7/0814

    摘要： 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.

    摘要翻译： 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。

    Substituted pyridines useful as modulators of acetylcholine receptors
    8.
    发明授权
    Substituted pyridines useful as modulators of acetylcholine receptors 失效
    取代的吡啶可用作乙酰胆碱受体的调节剂

    公开(公告)号：US5585388A

    公开(公告)日：1996-12-17

    申请号：US419597

    申请日：1995-04-07

    申请人： Nicholas D. Cosford ,  Jean-Michel Vernier

    发明人： Nicholas D. Cosford ,  Jean-Michel Vernier

    IPC分类号： A61K31/44 ,  A61K31/55 ,  A61P25/04 ,  A61P25/28 ,  A61P43/00 ,  C07D213/38 ,  C07D213/48 ,  C07D213/61 ,  C07D213/82 ,  C07D401/06 ,  C07F7/08 ,  C07D401/04 ,  A61K31/465

    CPC分类号： C07D401/06 ,  C07D213/38 ,  C07F7/0814

    摘要： 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 (including AIDS dementia); disorders of attention and focus (such as attention deficit disorder); 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.

    摘要翻译： 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。

    Antistatic polyamide fiber
    9.
    发明授权
    Antistatic polyamide fiber 失效
    防静电聚酰胺纤维

    公开(公告)号：US3859380A

    公开(公告)日：1975-01-07

    申请号：US44304874

    申请日：1974-02-15

    申请人： ALLIED CHEM

    发明人： CRESCENTINI LAMBERTO ,  WELLS RODNEY LEE

    IPC分类号： C08K5/134 ,  C08L77/00

    CPC分类号： C08K5/1345 ,  C08L77/00 ,  D01F1/09 ,  Y10S524/905 ,  C08L2666/20

    摘要： IN WHICH X HAS A VALUE OF FROM 1 TO 6 AND Y HAS A VALUE OF FROM 6 TO 30; AND

    IN WHICH A is

    WHEREIN X'' HAS A VALUE FROM 1 TO 6 AND Y'' HAS A VALUE OF 1 TO 6.

    WHERE R10 is a divalent radical having 1 to 20 carbon atoms derived from aliphatic, aromatic, cycloaliphatic, aromaticaliphatic, or heterocyclic hydrocarbons. However, with incorporation of this antistatic additive in the polyamide, serious problems have been encountered in melt-spinning due to the frequent occurrence of ''''nubs'''' or enlarged places in the extruded polyamide filament. It has now been found that the occurrence of said nubs in the antistatic polyamide fiber can be greatly reduced by dispersing in the polymer an additional small proportion of a hindered phenol represented by the formulas:

    WHERE R6, R7, R8 and R9 are independently selected from R1, R2, R3, R4 or another monovalent hydrocarbon radical having 1 to 20 carbon atoms as defined for R1, R2, R3 and R4, provided that at least one of R1, R2, R3, R4, R5, R6, R7, R8 or R9 is R''; where n is 3 to 6, r and u are 2, 3, or 4; m, q are 0 to 100; m + q must be >5; w is 2, 3, or 4; p is 2 or 3; f, g, are 0 or 2 to 6; s and t are 0 or a whole number and s + t must be less than 100; a and b are whole numbers; D. the reaction product of A, B and/or C with at least one compound selected from I. DIEPOXIDES, AND II. COMPOUNDS WHICH YIELD THE FOLLOWING DIVALENT RADICALS

    R1, R2, R3 and R4 are independently selected from R'' and monovalent hydrocarbon radicals having 1 to 20 carbon atoms derived from aliphatic, aromatic, cycloaliphatic, aromaticaliphatic, heterocyclic hydrocarbons or -(CrH2rO)m(CpH2pO)q-H; R5 is ethylene radical, R or a divalent radical selected from:

    AND -(CrH2rO)s-(CuH2uO)t-CwH2w-; where R'', R'''', R'''''' and R'''''''' are

    WHERE R is at least one of the alkylene difunctional radicals having 3 to 15 carbon atoms and a radical selected from

    It has been suggested that an antistatic fiber of polyamide can be prepared by uniformly dispersing in the polymer a small proportion of at least one compound having a molecular weight above 1500 selected from the group consisting of compounds represented by the formulas: