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1.发明授权NOVEL GABAa RECEPTOR SUBTYPES AND METHODS FOR SCREENING DRUG COMPOUNDS USING IMIDAZOQUINOXALINES AND PYRROLOPYRIMIDINES TO BIND TO GABAa RECEPTOR SUBTYPES 失效新GABAA受体亚型和方法筛选药物的连接使用GABAA受体亚型结合及imidazoquinoxalines的吡咯
公开(公告)号：EP0639275B1
公开(公告)日：1997-09-17
申请号：EP93910819.7
申请日：1993-04-30
申请人： NEUROGEN CORPORATION
IPC分类号： G01N33/566 , G01N33/94 , G01N33/60 , C07D471/14 , C07D487/04
CPC分类号： G01N33/9426 , C07B59/002 , G01N33/566 , G01N33/948 , G01N2500/20
摘要： The present invention provides methods for screening drug compounds utilizing compounds of formulas (I and II), and the pharmaceutically acceptable salts thereof where: R1, R2, R3, and R4 represent hydrogen, halogen, alkyl or alkoxy substituents; R5 is hydrogen or lower alkyl; X and Y represent hydrogen, halogen, alkyl or alkoxy substituents; and Z is hydrogen or fluorine. The invention also provides tritium or iodine isotope radiolabeled compounds of the formulas (I and II) radiolabeled with tritium or isotopes of iodine. The invention further provides novel GABAa receptor subtypes which specifically bind to compounds of formulas (I or II). The invention also provides GABAa receptor subtypes which are bound in situ to a compound of formula (I or II). The compounds provided herein bind selectively to a novel subtype of the GABAa binding site. Selective interaction of ligands at this unique receptor population results in pharmacological specificity which may lead to superior anxiolytics, cognition enhancers, anticonvulsants and sedative hypnotics.
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2.发明公开NOVEL GABAa RECEPTOR SUBTYPES AND METHODS FOR SCREENING DRUG COMPOUNDS USING IMIDAZOQUINOXALINES AND PYRROLOPYRIMIDINES TO BIND TO GABAa RECEPTOR SUBTYPES 失效新GABAA受体亚型和方法筛选药物的连接，使用AN GABAA受体亚型结合及imidazoquinoxalines的吡咯的。
公开(公告)号：EP0639275A1
公开(公告)日：1995-02-22
申请号：EP93910819.0
申请日：1993-04-30
申请人： NEUROGEN CORPORATION
CPC分类号： G01N33/9426 , C07B59/002 , G01N33/566 , G01N33/948 , G01N2500/20
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3.发明授权METHODS FOR SCREENING GABA-MODULATORY COMPOUNDS FOR SPECIFIED PHARMACOLOGICAL ACTIVITIES 有权GABA调节化合物对某些药理作用筛选方法
公开(公告)号：EP1177445B1
公开(公告)日：2007-07-11
申请号：EP00928860.6
申请日：2000-05-05
申请人： NEUROGEN CORPORATION
发明人： TALLMAN, John , GALLAGER, Dorothy , SHAW, Kenneth , WHITE, Geoffrey , CRANDALL, Marci , CASSELLA, James , RAJACHANDRAN, Lavanya , ALBAUGH, Pamela
IPC分类号： G01N33/566 , G01N33/94
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 alpha , beta , and gamma 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.
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4.发明公开METHODS FOR SCREENING GABA-MODULATORY COMPOUNDS FOR SPECIFIED PHARMACOLOGICAL ACTIVITIES 有权GABA调节化合物对某些药理作用筛选方法
公开(公告)号：EP1177445A1
公开(公告)日：2002-02-06
申请号：EP00928860.6
申请日：2000-05-05
申请人： NEUROGEN CORPORATION
发明人： TALLMAN, John , GALLAGER, Dorothy , SHAW, Kenneth , WHITE, Geoffrey , CRANDALL, Marci , CASSELLA, James , RAJACHANDRAN, Lavanya , ALBAUGH, Pamela
IPC分类号： G01N33/566 , G01N33/94
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 η 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.
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