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1.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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2.发明授权New meso-azacyclic aromatic acid amides and esters as novel serotonergic agents 失效新的内消旋 - 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：US5516782A
公开(公告)日：1996-05-14
申请号：US443605
申请日：1995-05-18
IPC分类号： C07D471/08 , C07D487/04 , C07D487/08 , C07D471/06 , A61K31/445
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New meso-azacyclic aromatic acid amides and esters as novel serotonergic agents 失效新的内消旋 - 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：US5318977A
公开(公告)日：1994-06-07
申请号：US973090
申请日：1992-11-06
IPC分类号： A61K31/435 , A61P25/24 , A61P25/26 , C07D471/08 , C07D487/04 , C07D487/08 , A61K31/395 , C07D471/18 , C07D487/18
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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4.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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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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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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公开(公告)号：US5591749A
公开(公告)日：1997-01-07
申请号：US424934
申请日：1995-04-19
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 disturbances (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（特别是伴有焦虑的抑郁症），认知障碍，药物滥用依赖和戒断，胃肠蠕动障碍（包括食管反流，消化不良，胃潴留，肠易激综合征 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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公开(公告)号：US5521193A
公开(公告)日：1996-05-28
申请号：US445057
申请日：1995-05-19
申请人： Daniel L. Flynn , Alan E. Moormann , Daniel P. Becker , Michael S. Dappen , Roger Nosal , Robert L. Shone , Clara I. Villamil
发明人： Daniel L. Flynn , Alan E. Moormann , Daniel P. Becker , Michael S. Dappen , Roger Nosal , Robert L. Shone , Clara I. Villamil
IPC分类号： C07D403/12 , C07D471/18 , C07D487/04 , C07D487/08 , A61K31/395 , C07D221/02
CPC分类号： C07D403/12 , C07D487/04 , C07D487/08
摘要： This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated, conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof.
摘要翻译： 本发明涉及可用于治疗HT4和/或HT3介导的下式的化合物或其药学上可接受的盐的化合物。
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公开(公告)号：US5260303A
公开(公告)日：1993-11-09
申请号：US666113
申请日：1991-03-07
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 , C07D453/06
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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10.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：US5219850A
公开(公告)日：1993-06-15
申请号：US896281
申请日：1992-06-10
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受体的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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