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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Thiohydantoin inhibitors of collagen-induced and ADP-induced platelet aggregation 失效胶原诱导的血友病素抑制剂和ADP诱导的血小板聚集
公开(公告)号：US5137904A
公开(公告)日：1992-08-11
申请号：US359003
申请日：1989-05-30
申请人： John S. Baran , Tom Lindberg , Robert H. Mazur , Alan E. Moorman , Doug Steinman
发明人： John S. Baran , Tom Lindberg , Robert H. Mazur , Alan E. Moorman , Doug Steinman
IPC分类号： C07D233/86
CPC分类号： C07D233/86
摘要： A series of ethers and thioethers of 5-methanol thiohydantoins, unsubstituted at the number one position heterocyclic nitrogen atom of the thiohydantoin ring, useful in reversing the effects of collagen and ADP-induced platelet aggregation.
摘要翻译： 一系列5-甲基硫代乙内酰脲的醚和硫醚，其在硫代乙内酰脲环的杂环氮原子的第一位未被取代，可用于逆转胶原和ADP诱导的血小板聚集的作用。
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