专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20070066573A1 Pyrrole and pyrazole derivatives as potentiators of glutamate receptors 失效
标题翻译：吡咯和吡唑衍生物作为谷氨酸受体的增效剂
公开(公告)号：US20070066573A1
公开(公告)日：2007-03-22
申请号：US10570985
申请日：2004-09-27
申请人： Pamela Albaugh , Esteban Dominguez-Manzanares , Jian Hong , William Hornback , Delu Jiang , Paul Ornstein , Michelle Thompson , Eric Tromiczak , Zhipei Wu , Hamideh Zarrinmayeh , Dennis Zimmerman , Ana Castano Mansanet , Larry Huffman , William Miller
发明人： Pamela Albaugh , Esteban Dominguez-Manzanares , Jian Hong , William Hornback , Delu Jiang , Paul Ornstein , Michelle Thompson , Eric Tromiczak , Zhipei Wu , Hamideh Zarrinmayeh , Dennis Zimmerman , Ana Castano Mansanet , Larry Huffman , William Miller
IPC分类号： A61K31/675 , A61K31/433 , A61K31/4196 , A61K31/42 , A61K31/425 , A61K31/415 , A61K31/416 , A61K31/4025 , A61K31/401 , C07D417/02 , C07D413/02 , C07D405/02 , C07D403/02
CPC分类号： C07D207/34 , C07D207/36 , C07D231/14 , C07D401/10 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/10 , C07D409/10 , C07D409/12 , C07D413/10 , C07D417/10
摘要： The present invention relates to pyrrole and pyrazole compounds of formula (I) and their pharmaceutically acceptable salts, and further relates to their use in treating schizophrenia, cognitive deficits associated with schizophrenia, Alzheimer's disease, dementia of the Alzheimer's type, mild cognitive impairment, or depression. The compounds act as potentiators on glutamate receptors, in particular AMPA and the GluR family.
摘要翻译：本发明涉及式（I）的吡咯和吡唑化合物及其药学上可接受的盐，并且还涉及它们在治疗精神分裂症，与精神分裂症相关的认知缺陷，阿尔茨海默病，阿尔茨海默氏型痴呆，轻度认知障碍或萧条。这些化合物作为谷氨酸受体，特别是AMPA和GluR家族的增效剂。

2. 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。

3. 发明授权

US07060451B2 Methods for screening GABA-modulatory compounds for specified pharmacological activities 失效
标题翻译：筛选用于规定药理活性的GABA调节化合物的方法
公开(公告)号：US07060451B2
公开(公告)日：2006-06-13
申请号：US10045396
申请日：2001-11-09
申请人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
发明人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
IPC分类号： G01N33/567 , C07K1/00 , C07H21/04 , C12N1/20 , C12P21/02
CPC分类号： G01N33/9426 , G01N2333/70571 , G01N2500/00
摘要： Methods are provided that are useful in assaying compounds for cognitive enhancing properties, anxiolytic properties, hypnotic properties, or antidepressant properties. These methods involve determining the in vitro efficacy and EC50 of the compounds at defined series of cloned GABAA subtype receptors composed of specific variants of α, β, and γ subunits in order to develop and an activity profile for each compound. Optionally, the binding affinities of the compounds at GABAA receptors are also determined. As an additional step the in vivo effects of the compounds may be tested in animal models.
摘要翻译：提供了可用于测定化合物的认知增强性质，抗焦虑性质，催眠性质或抗抑郁药性质的方法。这些方法包括确定在由α，β和γ亚基的特异性变体组成的限定的克隆的GABA亚型亚型受体系列中的化合物的体外功效和EC 50 为每个化合物开发和活动资料。任选地，还测定了化合物在GABA A A受体上的结合亲和力。作为附加步骤，可以在动物模型中测试化合物的体内作用。

4. 发明申请

US20050288321A1 Kinase inhibitors 失效
标题翻译：激酶抑制剂
公开(公告)号：US20050288321A1
公开(公告)日：2005-12-29
申请号：US10506029
申请日：2003-03-05
申请人： Pamela Albaugh , Jochen Ammenn , Timothy Burkholder , Joshu Clayton , Scott Conner , Brian Cunningham , Thomas Engler , Kelly Furness , James Henry , Sushant Malhotra , Mark Joseph Tebbe
发明人： Pamela Albaugh , Jochen Ammenn , Timothy Burkholder , Joshu Clayton , Scott Conner , Brian Cunningham , Thomas Engler , Kelly Furness , James Henry , Sushant Malhotra , Mark Joseph Tebbe
IPC分类号： C07D491/052 , A61K31/404 , A61K31/405 , A61K31/4355 , A61K31/437 , A61K31/438 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/4741 , A61K31/4745 , A61K31/496 , A61K31/506 , A61P3/10 , A61P5/50 , A61P25/28 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D451/04 , C07D471/02 , C07D471/04 , C07D491/04 , C07D43/14
CPC分类号： C07D451/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D471/04 , C07D491/04
摘要： The present invention provides kinase inhibitors of Formula (I).
摘要翻译：本发明提供式（I）的激酶抑制剂。

5. 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。

6. 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。

7. 发明授权

US6013650A Certain aryl fused imidazopyrimidines; a new class of GABA brain receptor ligands 失效
标题翻译：某些芳基稠合的咪唑并嘧啶; 一类新的GABA脑受体配体
公开(公告)号：US6013650A
公开(公告)日：2000-01-11
申请号：US167241
申请日：1998-10-06
申请人： Andrew Thurkauf , Al Hutchison , Pamela Albaugh
发明人： Andrew Thurkauf , Al Hutchison , Pamela Albaugh
IPC分类号： A61K31/00 , A61K31/505 , A61K31/535
CPC分类号： A61K31/00
摘要： Disclosed is a method for treating a subject non-human animal or domestic pet exhibiting symptoms of anxiety with a compound of the formula: ##STR1## wherein X is oxygen or sulfur;W is (un)substituted phenyl, thienyl or pyridyl; and ##STR2## represents (un)substituted aryl or heteroaryl as defined in the specification.
摘要翻译：公开了一种用下式化合物治疗患有焦虑症状的受试者非人动物或家养宠物的方法：其中X是氧或硫; W是（取代的）取代的苯基，噻吩基或吡啶基; 并且表示（un）取代的芳基或杂芳基，如说明书中所定义。

8. 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。

9. 发明授权

US5723462A 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是一类新的GABA脑受体配体
公开(公告)号：US5723462A
公开(公告)日：1998-03-03
申请号：US639166
申请日：1996-04-26
申请人： Pamela Albaugh , Gang Liu , Alan Hutchison
发明人： Pamela Albaugh , Gang Liu , Alan Hutchison
IPC分类号： C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D239/70 , A61K31/425 , C07D209/18 , C07D275/02
CPC分类号： C07D401/12 , C07D403/12 , C07D409/12 , C07D417/12 , C07D471/04
摘要： Disclosed are compounds of formula I: ##STR1## wherein R.sub.8 and R.sub.9 independently represent hydrogen or organic substituents; W represents optionally substituted thiazolyl or quinoxalinyl; X is hydrogen, hydroxy or lower alkyl; and T is hydrogen, halogen, hydroxy, nitro, amino or 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 receptor. 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：公开了式I的化合物：其中R8和R9独立地表示氢或有机取代基; W表示任选取代的噻唑基或喹喔啉基; X是氢，羟基或低级烷基; T是氢，卤素，羟基，硝基，氨基或烷基，这些化合物是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。

10. 发明授权

US5306819A Certain aryl a cycloalkyl fused imidazopyrazinols; and new class of GABA brain receptor ligands 失效
标题翻译：某些芳基环烷基稠合咪唑并吡唑啉; 和新一类的GABA脑受体配体
公开(公告)号：US5306819A
公开(公告)日：1994-04-26
申请号：US936589
申请日：1992-08-27
申请人： Pamela Albaugh , Alan Hutchison , Charles Blum
发明人： Pamela Albaugh , Alan Hutchison , Charles Blum
IPC分类号： C07D471/14 , C07D487/04 , C07D487/10 , C07D487/14 , C07D487/20
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention encompasses structures of the formula: ##STR1## and the pharmaceutically acceptable non-toxic salts thereof wherein: ##STR2## where W represents an aromatic group substituted with various organic and inorganic substituents;X, Y are hydrogen, halogen, hydroxy or amino with the proviso that at least X or Y is hydroxy;A, B C, and D, represent nitrogen or a carbon atom substituted with various organic and inorganic substituents;E represents oxygen, sulfur or substituted nitrogen;R.sub.3, R.sub.4, R.sub.12, and R.sub.13 are variables representing various organic and inorganic substituents; andn is 0, 1, or 2.
摘要翻译：本发明包括下式的结构：其中W表示被各种有机和无机取代基取代的芳族基团，其中：其中W表示被各种有机和无机取代基取代的芳族基团; X，Y是氢，卤素，羟基或氨基，条件是至少X或Y是羟基; A，B C和D表示氮或被各种有机和无机取代基取代的碳原子; E表示氧，硫或取代的氮; R3，R4，R12和R13是表示各种有机和无机取代基的变量; n为0,1或2。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式