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11. 发明授权

US07371752B2 Aryl fused substituted 4-oxy-pyridines 失效
标题翻译：芳基稠合取代的4-氧 - 吡啶
公开(公告)号：US07371752B2
公开(公告)日：2008-05-13
申请号：US11003195
申请日：2004-12-03
申请人： Guolin Cai , Pamela Albaugh , Jun Yuan
发明人： Guolin Cai , Pamela Albaugh , Jun Yuan
IPC分类号： A61K31/495 , A61K31/44 , C07D487/00 , C07D471/02
CPC分类号： C07D215/233 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D495/04
摘要： Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了下式的化合物：其中X，Q，W和如本文所定义。这些化合物是用于GABA A A受体的激动剂，拮抗剂或反向激动剂或GABAAβ受体的激动剂，拮抗剂或反向激动剂的前药，因此可用于诊断和治疗焦虑，抑郁症，唐氏综合征，睡眠和癫痫发作障碍，用苯二氮卓类药物服用过量，并增加记忆力。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A A受体定位的探针。

12. 发明申请

US20050154008A1 Aryl fused substituted 4-oxy-pyridines 失效
标题翻译：芳基稠合取代的4-氧 - 吡啶
公开(公告)号：US20050154008A1
公开(公告)日：2005-07-14
申请号：US11003195
申请日：2004-12-03
申请人： Guolin Cai , Pamela Albaugh , Jun Yuan
发明人： Guolin Cai , Pamela Albaugh , Jun Yuan
IPC分类号： A61P25/22 , A61P25/24 , A61P25/28 , C07D215/22 , C07D215/233 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D495/04 , C07D471/02 , A61K31/47 , A61K31/4745
CPC分类号： C07D215/233 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D495/04
摘要： Disclosed are compounds of the formula: wherein X, Q, W and are as defined herein. These compounds are agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了下式的化合物：其中X，Q，W和如本文所定义。这些化合物是用于GABA A A受体的激动剂，拮抗剂或反向激动剂或GABA A A受体的激动剂，拮抗剂或反向激动剂的前体药物，因此可用于诊断和治疗焦虑，抑郁症，唐氏综合征，睡眠和癫痫发作障碍，用苯二氮卓类药物服用过量，并增加记忆力。还提供药物组合物，包括包装的药物组合物。本发明的化合物也可用作组织样品中GABA A A受体定位的探针。

13. 发明申请

US20080146546A1 Bicyclic and Tricyclic Heteroaromatic Compounds 审中-公开
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US20080146546A1
公开(公告)日：2008-06-19
申请号：US12025490
申请日：2008-02-04
申请人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
IPC分类号： A61K31/55 , C07D221/06 , A61K31/4353 , C07D295/00 , A61K31/5377 , A61P25/00 , A61K31/541 , A61K31/496 , C07D223/02
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。还公开了可用于制备这些化合物的中间体。

14. 发明申请

US20060217384A1 Bicyclic and tricyclic heteroaromatic compounds 失效
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US20060217384A1
公开(公告)日：2006-09-28
申请号：US11442812
申请日：2006-05-30
申请人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
IPC分类号： C07D487/04 , A61K31/503 , A61K31/4745
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。还公开了可用于制备这些化合物的中间体。

15. 发明授权

US07053093B2 Bicyclic and tricyclic hetroaromatic compounds 失效
标题翻译：双环和三环杂芳族化合物
公开(公告)号：US07053093B2
公开(公告)日：2006-05-30
申请号：US10352519
申请日：2003-01-28
申请人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
IPC分类号： C07D471/04 , A61K31/437 , A61K25/24 , A61P25/22
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中W，Q，X，X 1，Y和Z如本文所定义。这些化合物以高选择性和/或高亲和力结合GABA A A受体的苯并二氮杂位点，因此可用于治疗中枢神经系统（CNS）疾病和用作GABA < 组织样品中的受体。还公开了可用于制备这些化合物的中间体。

16. 发明授权

US06703393B2 (Oxo-pyrazolo[1,5a]pyrimidin-2-yl) alkyl-carboxamides 失效
标题翻译：（氧代 - 吡唑并[1,5a]嘧啶-2-基）烷基 - 甲酰胺
公开(公告)号：US06703393B2
公开(公告)日：2004-03-09
申请号：US10107790
申请日：2002-03-27
申请人： Guiying Li , John Peterson , Pamela Albaugh
发明人： Guiying Li , John Peterson , Pamela Albaugh
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof where the variables R1, R2, A, R4, R5, R6, R6′, n, and W are defined herein. These compounds bind to the benzodiazepine site of GABAA receptors are provided and, therefore can be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中变量R1，R2，A，R4，R5，R6，R6'，n和W如本文所定义。这些化合物结合到GABA A受体的苯并二氮杂位点，因此可用于调节配体在体内或体外与GABA A受体的结合，并且特别可用于治疗各种中枢神经系统（CNS）人类，驯养的伴侣动物和家畜。

17. 发明授权

US06414147B1 2-amino-9-alkylpurines: GABA brain receptor ligands 失效
标题翻译： 2-氨基-9-烷基嘌呤：GABA脑受体配体
公开(公告)号：US06414147B1
公开(公告)日：2002-07-02
申请号：US09470940
申请日：1999-12-22
申请人： Kevin S. Currie , Pamela Albaugh , Paul Chen
发明人： Kevin S. Currie , Pamela Albaugh , Paul Chen
IPC分类号： C07D47318
CPC分类号： C07D473/00 , C07D473/18 , C07D473/24
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: W is oxygen or sulfur; X is (un)substituted lower alkyl; or X is (un)substituted aryl or heteroaryl; Y is hydrogen or lower alkyl; Z is lower alkenyl, lower alkynyl, or (un)substituted lower alkyl; T is (un)substituted aryl or heteroaryl. The 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. Thus these compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, Down's Syndrome, overdose with benzodiazepine drugs, and for the enhancement of memory.
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：W是氧或硫; X是（un）取代的低级烷基; 或者X是（未）取代的芳基或杂芳基; Y是氢或低级烷基; Z是低级烯基，低级炔基或（未）取代的低级烷基; T是（未）取代的芳基或杂芳基。该化合物是高度选择性的激动剂，拮抗剂或GABAa脑受体的反向激动剂，或GABAa脑受体的激动剂，拮抗剂或反向激动剂的前药。因此，这些化合物可用于诊断和治疗焦虑症，睡眠和癫痫发作障碍，唐氏综合症，苯并二氮卓类药物过量以及增强记忆功能。

18. 发明授权

US07008947B2 (Oxo-pyrazolo[1,5a]pyrimidin-2-yl)alkyl-carboxamides 失效
标题翻译：（氧代 - 吡唑并[1,5a]嘧啶-2-基）烷基 - 甲酰胺
公开(公告)号：US07008947B2
公开(公告)日：2006-03-07
申请号：US10796509
申请日：2004-03-09
申请人： Guiying Li , John Peterson , Pamela Albaugh
发明人： Guiying Li , John Peterson , Pamela Albaugh
IPC分类号： C07D487/04 , C07D471/04 , A61P25/22 , A61P25/24 , A61P25/28
CPC分类号： C07D487/04
摘要： Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof where the variables R1, R2, A, R4, R5, R6, R6′, n, and W are defined herein. These compounds bind to the benzodiazepine site of GABAA receptors are provided and, therefore can be used to modulate ligand binding to GABAA receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中R 1，R 2，A，R 4，R 3， R 5，R 6，R 6，N和W如本文所定义。提供了这些化合物与GABA A 2 S受体的苯并二氮杂位点结合，因此可用于体内或体外调节配体与GABA A受体的结合，特别是可用于治疗人类各种中枢神经系统（CNS）疾病，驯养伴侣动物和家畜。

19. 发明授权

US06720339B2 Certain fused pyrrolecarboxamides; a new class of GABA brain receptor ligands 失效
标题翻译：某些融合的吡咯甲酰胺; 一类新的GABA脑受体配体
公开(公告)号：US06720339B2
公开(公告)日：2004-04-13
申请号：US10090935
申请日：2002-03-05
申请人： Pamela Albaugh , Gang Liu , Alan Hutchison
发明人： Pamela Albaugh , Gang Liu , Alan Hutchison
IPC分类号： A61K31403
CPC分类号： C07D401/12 , C07D209/42 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. These 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 and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
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：W表示取代或未取代的芳基或杂芳基; T是氢，卤素，羟基，氨基或烷基; X是氢，羟基或低级烷基; m是0 ，1或2; n为0,1或2; 并且R 3和R 4表示取代或未取代的有机残基。这些化合物是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，睡眠和癫痫发作障碍，用苯二氮卓类药物过量并用于增强记忆力。

20. 发明授权

US5925770A Certain fused pyrrolecarboxanilides; a new class of gaba brain receptor ligands 失效
标题翻译：某些融合的吡咯甲酰苯胺; 一类新的gaba脑受体配体
公开(公告)号：US5925770A
公开(公告)日：1999-07-20
申请号：US73030
申请日：1998-05-05
申请人： Pamela Albaugh , Alan Hutchison
发明人： Pamela Albaugh , Alan Hutchison
IPC分类号： A61K31/404 , C07C233/58 , C07D209/08 , C07D209/42 , C07D209/52 , C07D307/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04
CPC分类号： C07D209/08 , A61K31/404 , C07D209/42 , C07D209/52 , C07D307/84 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/04 , C07D417/12 , C07D471/04
摘要： The present invention encompasses structures of the formula: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## wherein: W represents substituted or unsubstituted phenyl;X is hydrogen,T is hydrogen, and n is 3,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 and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.
摘要翻译：本发明包括下式的结构：或其药学上可接受的无毒盐，其中：其中：W表示取代或未取代的苯基; X是氢，T是氢，n是3，这些化合物是用于GABAa脑受体的高选择性激动剂，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，睡眠和癫痫发作，用苯二氮卓类药物过量并用于记忆增强。

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