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    Methods of modulating processes mediated by excitatory amino acid receptors
    1.
    发明授权
    Methods of modulating processes mediated by excitatory amino acid receptors 失效
    调节由兴奋性氨基酸受体介导的过程的方法

    公开(公告)号：US06956049B1

    公开(公告)日：2005-10-18

    申请号：US09387135

    申请日：1999-08-31

    申请人： Nicholas D. P. Cosford ,  Ian A. McDonald ,  Stephen D. Hess ,  Mark A. Varney

    发明人： Nicholas D. P. Cosford ,  Ian A. McDonald ,  Stephen D. Hess ,  Mark A. Varney

    IPC分类号： A61K31/425 ,  C07D277/00 ,  A51K31/425

    CPC分类号： C07D277/22 ,  A61K31/425

    摘要： 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.

    摘要翻译： 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。

    Substituted pyridine compounds useful as modulators of acetylcholine receptors
    2.
    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
    3.
    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。

    Peptide, peptide analog and amino acid analog protease inhibitors
    4.
    发明授权
    Peptide, peptide analog and amino acid analog protease inhibitors 失效
    肽，肽类似物和氨基酸类似蛋白酶抑制剂

    公开(公告)号：US6017887A

    公开(公告)日：2000-01-25

    申请号：US443931

    申请日：1995-05-18

    申请人： Benito Munoz ,  Ian A. McDonald ,  Elisabeth Albrecht

    发明人： Benito Munoz ,  Ian A. McDonald ,  Elisabeth Albrecht

    IPC分类号： A61K38/00 ,  C07C237/22 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/083 ,  A61K38/05

    CPC分类号： C07K5/0808 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06165 ,  C07K5/06191 ,  A61K38/00

    摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.B is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is an alcohol, particularly a secondary alcohol.

    摘要翻译： 提供了化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。 其中R 1优选为2-甲基丙烯，2-丁烯，正亮氨酸等;式（I），（II）和（III） R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; RB优选为异丁基; RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; X是醇，特别是仲醇。

    Modulators of acetylcholine receptors
    5.
    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：US5703100A

    公开(公告)日：1997-12-30

    申请号：US485398

    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： A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61P1/00 ,  A61P9/00 ,  A61P21/00 ,  A61P25/00 ,  A61P25/02 ,  A61P29/00 ,  C07D401/04 ,  C07D405/14 ,  C07F7/08

    CPC分类号： C07D401/04 ,  C07D405/14 ,  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。

    Methods of treating neurodegenerative disorders using protease inhibitors
    8.
    发明授权
    Methods of treating neurodegenerative disorders using protease inhibitors 失效
    使用蛋白酶抑制剂治疗神经变性疾病的方法

    公开(公告)号：US5872101A

    公开(公告)日：1999-02-16

    申请号：US444361

    申请日：1995-05-18

    申请人： Benito Munoz ,  Ian A. McDonald ,  Elisabeth Albrecht

    发明人： Benito Munoz ,  Ian A. McDonald ,  Elisabeth Albrecht

    IPC分类号： A61K38/00 ,  C07C237/22 ,  C07K5/02 ,  C07K5/06 ,  C07K5/065 ,  C07K5/078 ,  C07K5/083 ,  A61K38/05

    CPC分类号： C07K5/0808 ,  C07C237/22 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/06043 ,  C07K5/06078 ,  C07K5/06165 ,  C07K5/06191 ,  A61K38/00

    摘要： Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.8 is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is an alcohol, particularly a secondary alcohol.

    摘要翻译： 提供了化合物和化合物用于治疗以沉淀淀粉样蛋白为特征的疾病的方法。 其中R 1优选为2-甲基丙烯，2-丁烯，正亮氨酸;式（I），（II）和（III）的化合物为： R2，R4和R8各自独立地是甲基或乙基; R3优选为异丁基或苯基; R5优选为异丁基; R6是H或甲基; R7-（Q）n优选为苄氧羰基或乙酰基; Q优选为-C（O） - ; R8优选为异​​丁基; RA = - （T）m-（D）m -R 1，其中T优选为氧或碳，D优选为单不饱和C 3-4烯基; X是醇，特别是仲醇。

    Modulators of acetylcholine receptors
    9.
    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：US5594011A

    公开(公告)日：1997-01-14

    申请号：US337640

    申请日：1994-11-10

    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 ,  A61K31/44

    CPC分类号： C07D401/04 ,  C07D405/14 ,  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; 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.

    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。