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31. 发明授权

US6156898A Substituted 1,4-dihydro-4-oxonicotinic carboxamides; GABA brain receptor ligands 失效
标题翻译：取代的1,4-二氢-4-氧代烟酰甲酰胺; GABA脑受体配体
公开(公告)号：US6156898A
公开(公告)日：2000-12-05
申请号：US258836
申请日：1999-02-26
申请人： Robert W. DeSimone , Charles Manly
发明人： Robert W. DeSimone , Charles Manly
IPC分类号： C07D213/82 , C07D215/56 , C07D417/12 , C07D211/90
CPC分类号： C07D213/82 , C07D215/56 , C07D417/12
摘要： Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: R.sub.1 is lower alkyl;R.sub.2 is hydrogen or lower alkyl; orR.sub.1 and R.sub.2 together represent a 2, 3, or 4 carbon alkylene moiety that together with the pyridone ring to which they are attached form a 5, 6, or 7 membered carbocyclic ring; andW is (un)substituted lower alkyl, aryl, arylalkyl, or heteroaryl; orW is NR.sub.3 COR.sub.4, COR.sub.4, CONR.sub.3 R.sub.4 or CO.sub.2 R.sub.4 where R.sub.3 and R.sub.4 are the same or different and represent hydrogen or lower alkyl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒盐，其中：R 1是低级烷基; R2是氢或低级烷基; 或者R 1和R 2一起代表2,3或4个碳亚烷基部分，与它们所连接的吡啶酮环一起形成5,6或7元碳环; 并且W是（未）取代的低级烷基，芳基，芳基烷基或杂芳基; 或W是NR 3 COR 4，COR 4，CONR 3 R 4或CO 2 R 4，其中R 3和R 4相同或不同并且表示氢或低级烷基，该化合物是GABAa脑受体或激动剂，拮抗剂或反向激动剂前药的高选择性激动剂，拮抗剂或反向激动剂用于GABAa脑受体。这些化合物可用于诊断和治疗焦虑，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

32. 发明授权

US6143760A Substituted 4-oxo-napthyridine-3-carboxamides: GABA brain receptor ligands 失效
标题翻译：取代的4-氧代 - 萘啶-3-甲酰胺：GABA脑受体配体
公开(公告)号：US6143760A
公开(公告)日：2000-11-07
申请号：US139456
申请日：1998-08-25
申请人： Pamela A. Albaugh , Robert W. DeSimone , Gang Liu
发明人： Pamela A. Albaugh , Robert W. DeSimone , Gang Liu
IPC分类号： C07D471/04 , A61K31/44 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention encompasses structures of the Formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: x is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; andY is (un)substituted alkyl, aryl, or heteroaryl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.
摘要翻译：本发明包括式或其药学上可接受的无毒盐的结构，其中：x是氢，卤素，（未）取代的烷基，（未）取代的烷氧基或氨基; 并且Y是（未）取代的烷基，芳基或杂芳基，该化合物是GABAa脑受体的高度选择性激动剂，拮抗剂或反向激动剂或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。这些化合物可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作，以及用苯二氮卓类药物过量并提高警觉性。

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