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1. 发明授权

US5703100A Modulators of acetylcholine receptors 失效
标题翻译：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。

2. 发明授权

US5594011A Modulators of acetylcholine receptors 失效
标题翻译：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。

3. 发明授权

US5723477A Modulators of acetylcholine receptors 失效
标题翻译：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。

4. 发明授权

US5710324A Inhibitors of nitric oxide biosynthesis 失效
标题翻译：一氧化氮生物合成抑制剂
公开(公告)号：US5710324A
公开(公告)日：1998-01-20
申请号：US317458
申请日：1994-10-04
申请人： Jeffrey P. Whitten , Ian A. McDonald , Laurie E. Lambert , Niall S. Doherty
发明人： Jeffrey P. Whitten , Ian A. McDonald , Laurie E. Lambert , Niall S. Doherty
IPC分类号： A61K38/00 , C07K5/068 , A61K31/195 , C07C61/04
CPC分类号： C07K5/06086 , A61K38/00
摘要： The present invention is directed to a new class of compound which are useful as inhibitors of the biosynthesis of nitric oxide.
摘要翻译：本发明涉及可用作一氧化氮生物合成抑制剂的新类化合物。

5. 发明授权

US5877202A Indole derivatives useful to treat estrogen-related neoplasms and disorders 失效
标题翻译：用于治疗雌激素相关性肿瘤和疾病的吲哚衍生物
公开(公告)号：US5877202A
公开(公告)日：1999-03-02
申请号：US594505
申请日：1996-01-31
申请人： Alan J. Bitonti , Ian A. McDonald , Francesco G. Salituro , Jeffrey P. Whitten , Esa T. Jarvi , Paul S. Wright
发明人： Alan J. Bitonti , Ian A. McDonald , Francesco G. Salituro , Jeffrey P. Whitten , Esa T. Jarvi , Paul S. Wright
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/405 , A61P35/00 , A61P35/02 , C07D209/18 , C07D209/22 , C07D209/24 , C07D209/26 , C07D209/28 , C07D209/42 , C07D209/14
CPC分类号： C07D209/42 , C07D209/18 , C07D209/22 , C07D209/24 , C07D209/26 , C07D209/28
摘要： The present invention relates to novel indole derivatives useful in down-regulating estrogen receptor expression. Also included are methods for the treatment of neoplasms or of controlling the growth of a neoplasm in a patient afflicted with a neoplastic disease, especially estrogen-dependent neoplasms such as those associated with breast, ovarian and cervical tissue. Another embodiment of the present invention is a method of prophylactically treating a patient at risk of developing a neoplastic disease state. Also provided is a method for treating autoimmune diseases. Also included are pharmaceutical compositions of the novel indole derivatives.
摘要翻译：本发明涉及可用于下调雌激素受体表达的新型吲哚衍生物。还包括用于治疗肿瘤的方法或控制患有肿瘤性疾病，特别是与乳腺，卵巢和子宫颈组织相关的雌激素依赖性肿瘤的患者的肿瘤生长的方法。本发明的另一个实施方案是预防性治疗患有发展为肿瘤疾病状态的风险的患者的方法。还提供了治疗自身免疫性疾病的方法。还包括新型吲哚衍生物的药物组合物。

6. 发明授权

US5567710A Polycyclic fused ring modulators of acetylcholine receptors 失效
标题翻译：乙酰胆碱受体的多环稠环调节剂
公开(公告)号：US5567710A
公开(公告)日：1996-10-22
申请号：US322757
申请日：1994-10-13
申请人： Jeffrey P. Whitten , Ian A. McDonald , Jean-Michel Vernier
发明人： Jeffrey P. Whitten , Ian A. McDonald , Jean-Michel Vernier
IPC分类号： C07D471/04 , C07D491/14 , C07D491/147 , A61K31/44
CPC分类号： C07D491/14 , C07D471/04
摘要： In accordance with the present invention, there is provided a class of polycyclic fused ring 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.
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多环稠环化合物。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。

7. 发明授权

US5318992A Inhibitors of nitric oxide biosynthesis 失效
标题翻译：一氧化氮生物合成抑制剂
公开(公告)号：US5318992A
公开(公告)日：1994-06-07
申请号：US91082
申请日：1993-07-13
申请人： Jeffrey P. Whitten , Ian A. McDonald , Laurie E. Lambert , Niall S. Doherty
发明人： Jeffrey P. Whitten , Ian A. McDonald , Laurie E. Lambert , Niall S. Doherty
IPC分类号： A61K38/00 , C07C243/36 , C07C271/24 , C07C279/14 , C07C281/02 , C07C281/06 , C07C281/16 , C07K5/068 , A61K31/195 , A61K31/22
CPC分类号： C07K5/06086 , C07C243/36 , C07C271/24 , C07C279/14 , C07C281/02 , C07C281/06 , C07C281/16 , A61K38/00 , C07C2101/02 , Y10S514/921
摘要： The present invention is a method of treating hypotension and shock using select ornithine or N.sup.G -arginine derivatives.
摘要翻译：本发明是使用选择性鸟氨酸或NG-精氨酸衍生物治疗低血压和休克的方法。

8. 发明授权

US06316490B1 Substituted aryl compounds useful as modulators of acetylcholine receptors 失效
标题翻译：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。

9. 发明授权

US6017887A Peptide, peptide analog and amino acid analog protease inhibitors 失效
标题翻译：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。

10. 发明授权

US4346110A Method for treating depression 失效
标题翻译：治疗抑郁症的方法
公开(公告)号：US4346110A
公开(公告)日：1982-08-24
申请号：US268554
申请日：1981-06-01
申请人： Michael G. Palfreyman , Ian A. McDonald
发明人： Michael G. Palfreyman , Ian A. McDonald
IPC分类号： A61K31/195 , C07D309/12 , A61K31/24
CPC分类号： C07D309/12 , A61K31/195
摘要： 2-Amino-3-(3'-hydroxyphenyl)-3-butenoic acid or 2-amino-3-(3',4'-dihydroxyphenyl)-3-butenoic acid can be used to treat depression either alone or in combination with an extracerebrally acting AADC inhibitor.
摘要翻译： 2-氨基-3-（3'-羟基苯基）-3-丁烯酸或2-氨基-3-（3'，4'-二羟基苯基）-3-丁烯酸可以单独使用或与一种肌内作用的AADC抑制剂。

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