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公开(公告)号：US20050032793A1
公开(公告)日：2005-02-10
申请号：US10728946
申请日：2003-12-08
申请人： Norman Abood , Daniel Flynn , Daniel Becker , Brian Bax , Hui Li , Roger Nosal , Lori Schretzman , Clara Villamil
发明人： Norman Abood , Daniel Flynn , Daniel Becker , Brian Bax , Hui Li , Roger Nosal , Lori Schretzman , Clara Villamil
IPC分类号： C07D265/22 , A61K31/535 , A61P31/12 , A61P43/00 , C07D265/12 , C07D265/24 , C07D413/04 , C07D413/12 , C07D417/12
CPC分类号： C07D265/24 , C07D413/04 , C07D413/12 , C07D417/12
摘要： A class of compounds for the treatment of viral infections. Compounds of particular interest are defined by Formula I wherein R-R4 are as defined herein, or a pharmaceutically-acceptable salt thereof.
摘要翻译： 一类用于治疗病毒感染的化合物。 特别感兴趣的化合物由式I定义，其中R-R 4如本文所定义，或其药学上可接受的盐。
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2.发明授权Pharmaceutically useful meso-azacyclic amides of imidazopyridine carboxylic acids and analogs thereof 失效咪唑并吡啶羧酸及其类似物的药学有用的内消旋 - 氮杂环酰胺
公开(公告)号：US5137893A
公开(公告)日：1992-08-11
申请号：US666278
申请日：1991-03-07
IPC分类号： C07D519/00
CPC分类号： C07D519/00
摘要： The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is benefical. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbances (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
摘要翻译： 含有本文所述的内消旋 - 侧链侧链的咪唑并吡啶可用作5-羟色胺5-HT 3受体的拮抗剂。 因此，它们可用于治疗其中5-HT 3受体拮抗作用有益的人和动物。 治疗指示但不限于治疗焦虑症，精神病，抑郁症（特别是伴有焦虑的抑郁症），认知障碍，药物滥用依赖和/或戒断，胃肠蠕动障碍（包括食管反流，消化不良，肠易激综合征 ），由化疗药引起的呕吐和内脏痛。 此外，本发明的化合物可以用作生物活性化合物的鼻吸收增强剂。
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3.发明授权5-substituted(4,5-c)imidazopyridine compounds which have useful platelet activating factor antagonistic activity 失效具有有用的血小板活化因子拮抗活性的5-取代（4,5-c）咪唑并吡啶化合物
公开(公告)号：US4914108A
公开(公告)日：1990-04-03
申请号：US167671
申请日：1988-03-14
申请人： Ish K. Khanna , Roger Nosal , Richard M. Weier
发明人： Ish K. Khanna , Roger Nosal , Richard M. Weier
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： This invention relates to novel 5-substituted [4,5-c]imidazopyridine derivatives useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention also relates to pharmaceutical compositions of such substituted imidazopyradines.
摘要翻译： 本发明涉及可用于治疗由血小板活化因子介导的疾病或病症的新的5-取代的[4,5-c]咪唑并吡啶衍生物。 本发明还涉及这种取代的咪唑并嗪的药物组合物。
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4.发明授权Process for the preparation of amidino phenyl pyrrolidine beta-alanine urea analogs 失效制备脒基苯基吡咯烷β-丙氨酸脲类似物的方法
公开(公告)号：US5610296A
公开(公告)日：1997-03-11
申请号：US349333
申请日：1994-12-05
IPC分类号： A61K31/40 , A61K31/4015 , A61P7/02 , C07C323/60 , C07D207/26 , C07D207/273 , C07D207/12
CPC分类号： C07D207/273
摘要： The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
摘要翻译： 本发明涉及通过在碱存在下在合适的非质子溶剂中通过用三甲基锍卤化物或三甲基氧化锍卤化物处理甲硫氨酸类似物，从式IMA图谱的甲硫氨酸类似物制备式“的内酰胺的方法 。 本发明进一步涉及使用这种甲硫氨酸和内酰胺化合物作为中间体制备脒基苯基吡咯烷基β-丙氨酸脲类似物，β-丙氨酸脲类似物可用作抗血栓形成剂。
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公开(公告)号：USRE35218E
公开(公告)日：1996-04-23
申请号：US292894
申请日：1994-08-18
IPC分类号： A61K31/435 , A61K31/439 , A61K31/55 , A61P1/00 , A61P1/08 , A61P1/12 , A61P1/14 , A61P25/04 , A61P25/06 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , C07C20060101 , C07D20060101 , C07D209/52 , C07D471/18 , C07D487/08 , C07D487/18 , C07D491/056 , A61K31/395 , C07D451/00 , C07D451/02 , C07D451/14
CPC分类号： C07D487/08
摘要： An azatetracycle compound useful as 5HT.sub.3 antagonists of the general formula ##STR1## wherein D is a tetracycle of the structure ##STR2## wherein Ar is an aromatic moiety and B is either NH or O.
摘要翻译： 可用作通式为“IMAGE”的5HT3拮抗剂的azatetracycle化合物，其中D是结构式（IMAGE）或者IMAGE的四环，其中Ar是芳族部分，B是NH或O.
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公开(公告)号：US5484946A
公开(公告)日：1996-01-16
申请号：US463657
申请日：1995-06-05
IPC分类号： A61K31/40 , A61K31/4015 , A61P7/02 , C07C323/60 , C07D207/26 , C07D207/273
CPC分类号： C07D207/273
摘要： The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
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公开(公告)号：US5434161A
公开(公告)日：1995-07-18
申请号：US973126
申请日：1992-11-06
IPC分类号： A61K31/40 , A61K31/435 , A61K31/445 , A61K31/4468 , A61K31/46 , A61P43/00 , C07C219/12 , C07C233/62 , C07D211/46 , C07D211/58 , C07D451/04 , C07D451/06 , C07D451/14 , C07D453/02 , C07D471/04 , C07D471/06 , C07D471/22 , C07D487/04 , C07D487/08 , C07D519/00 , A61K31/44
CPC分类号： C07D471/04
摘要： The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
摘要翻译： 本发明的咪唑并吡啶化合物是5-羟色胺能5-HT 3拮抗剂。 因此，它们可用于治疗其中5-HT 3受体拮抗作用有益的人和动物。 治疗指示但不限于治疗焦虑，精神病，抑郁症（特别是伴有焦虑症的抑郁症），认知障碍，药物滥用依赖和戒断，胃肠蠕动窒息（包括食管反流，消化不良，胃潴留，肠易激惹） 综合征），化疗引起的呕吐和内脏痛。 此外，本发明的化合物可以用作生物活性化合物的鼻吸收增强剂。
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8.发明授权Meso-azacyclic amides of imidazopyridine carboxylic acids and analogs thereof as pharmaceuticals 失效咪唑并吡啶羧酸的间 - 环氮杂酰胺及其类似物作为药物
公开(公告)号：US5234921A
公开(公告)日：1993-08-10
申请号：US896244
申请日：1992-06-10
申请人： Daniel L. Flynn , Alan E. Moormann , Roger Nosal
发明人： Daniel L. Flynn , Alan E. Moormann , Roger Nosal
IPC分类号： C07D519/00
CPC分类号： C07D519/00
摘要： The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
摘要翻译： 含有本文所述的内消旋 - 侧链侧链的咪唑并吡啶可用作5-羟色胺5-HT 3受体的拮抗剂。 因此，它们可用于治疗其中5-HT 3受体拮抗作用有益的人和动物。 治疗指示但不限于治疗焦虑症，精神病，抑郁症（特别是伴有焦虑症的抑郁症），认知障碍，药物滥用依赖和/或戒断，胃肠蠕动性窒息（包括食管反流，消化不良，肠易激综合征 ），由化疗药引起的呕吐和内脏痛。 此外，本发明的化合物可以用作生物活性化合物的鼻吸收增强剂。
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9.发明授权Meso-azacyclic aromatic acid amides and esters as novel serotonergic agents 失效中等氮杂环芳香酰胺和酯作为新的5-羟色胺能药剂
公开(公告)号：US5612366A
公开(公告)日：1997-03-18
申请号：US234336
申请日：1994-04-28
IPC分类号： A61K31/435 , A61P25/24 , A61P25/26 , C07D471/08 , C07D487/04 , C07D487/08 , A01K31/40
CPC分类号： C07D471/08 , C07D487/04 , C07D487/08
摘要： The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
摘要翻译： 本发明的内消旋 - 氮杂环芳香酰胺和酯可用于治疗中枢神经系统和胃肠动力障碍，例如胃食管反流，非溃疡性消化不良，胃排空迟缓，肠梗阻，肠易激综合征等 。 此外，本发明的化合物可用作5-羟色胺5-HT 3受体的拮抗剂。 因此，它们可用于治疗其中5-HT 3受体拮抗作用有益的人和动物。 治疗指示但不限于治疗焦虑，精神病，抑郁症（特别是伴有焦虑的抑郁症），认知障碍，药物滥用依赖和/或戒断，肠易激综合征，由化学治疗剂引起的呕吐和内脏痛 。 此外，本发明的化合物可以用作生物活性化合物的鼻吸收增强剂。
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公开(公告)号：US5604239A
公开(公告)日：1997-02-18
申请号：US424732
申请日：1995-04-18
IPC分类号： A61K31/40 , A61K31/435 , A61K31/445 , A61K31/4468 , A61K31/46 , A61P43/00 , C07C219/12 , C07C233/62 , C07D211/46 , C07D211/58 , C07D451/04 , C07D451/06 , C07D451/14 , C07D453/02 , C07D471/04 , C07D471/06 , C07D471/22 , C07D487/04 , C07D487/08 , C07D519/00 , A61K31/44
CPC分类号： C07D471/04
摘要： The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
摘要翻译： 本发明的咪唑并吡啶化合物是5-羟色胺能5-HT 3拮抗剂。 因此，它们可用于治疗其中5-HT 3受体拮抗作用有益的人和动物。 治疗指示但不限于治疗焦虑，精神病，抑郁症（特别是伴有焦虑症的抑郁症），认知障碍，药物滥用依赖和戒断，胃肠蠕动窒息（包括食管反流，消化不良，胃潴留，肠易激惹） 综合征），化疗引起的呕吐和内脏痛。 此外，本发明的化合物可以用作生物活性化合物的鼻吸收增强剂。
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