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1. 发明授权

US5696260A Certain cycloalkyl imidazopyrimidines, a new class of gaba brain receptor ligands 失效
标题翻译：某些环烷基咪唑并嘧啶，一类新的gaba脑受体配体
公开(公告)号：US5696260A
公开(公告)日：1997-12-09
申请号：US492806
申请日：1995-06-20
申请人： Kenneth Shaw , Alan Hutchison
发明人： Kenneth Shaw , Alan Hutchison
IPC分类号： A61K31/505 , A61P25/20 , C07D487/04
CPC分类号： C07D487/04
摘要： Disclosed are compounds of the formula: ##STR1## or pharmaceutically acceptable non-toxic salts thereof wherein: R.sub.9 and Y are substituents as defined herein; and R.sub.a and R.sub.b independently represent halogen, hydroxy, amino, mono or dialkylamino where each alkyl is straight or branched chain alkyl having 1-6 carbon atoms, straight or branched chain lower alkyl having 1-6 chain atoms, or straight or branched chain lower alkoxy having 1-6 carbon atoms, where R.sub.a and R.sub.b each appear at most only once on the phenyl ring which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.
摘要翻译：公开了下式的化合物：其中：R 9和Y是如本文所定义的取代基; 并且R a和R b独立地表示卤素，羟基，氨基，单或二烷基氨基，其中每个烷基是具有1-6个碳原子的直链或支链烷基，具有1-6个链原子的直链或支链低级烷基，或直链或支链低级具有1-6个碳原子的烷氧基，其中R a和R b在苯环上最多仅出现一次，该化合物是GABAa脑受体或其前药的高选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，用苯二氮卓类药物服用过量，提高警惕性。

2. 发明授权

US5597920A Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes 失效
标题翻译： Gabaa受体亚型和使用咪唑并喹啉和吡咯并嘧啶结合gabaa受体亚型筛选药物化合物的方法
公开(公告)号：US5597920A
公开(公告)日：1997-01-28
申请号：US876050
申请日：1992-04-30
申请人： Kenneth Shaw , Alan Hutchison , Andrew Thurkauf , John Tallman
发明人： Kenneth Shaw , Alan Hutchison , Andrew Thurkauf , John Tallman
IPC分类号： G01N33/53 , A61K31/495 , A61K31/505 , A61P25/08 , A61P25/20 , A61P25/28 , C07B59/00 , C07D487/04 , G01N33/534 , G01N33/566 , G01N33/94 , C07D487/06 , C07D487/02
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, where formulas I and II are ##STR1## and the pharmaceutically acceptable salts thereof where: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent hydrogen, halogen, alkyl or alkoxy substituents;R5 is hydrogen or lower alkyl;X and Y represent hydrogen, halogen, alkyl or alkoxy substituents; andZ 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.
摘要翻译：本发明提供了利用式I和II化合物筛选药物化合物的方法，其中式I和II是其中R 1，R 2，R 3和R 4表示氢，卤素，烷基或烷氧基取代基; R5是氢或低级烷基; X和Y表示氢，卤素，烷基或烷氧基取代基; Z是氢或氟。本发明还提供用氚或碘的同位素放射性标记的式I和II的氚或碘同位素放射性标记的化合物。本发明还提供了与式I或II化合物特异性结合的新型GABAa受体亚型。本发明还提供了与式I或II化合物原位结合的GABAa受体亚型。本文提供的化合物选择性结合GABAa结合位点的新亚型。配体在这种独特的受体群体上的选择性相互作用导致药理学特异性，这可能导致优异的抗焦虑药，认知增强剂，抗惊厥药和镇静催眠药。

3. 发明授权

US5426186A Certain cycloalkyl imidazopyrimidines, a new class of GABA brain receptor ligands 失效
标题翻译：某些环烷基咪唑并嘧啶，一类新的GABA脑受体配体
公开(公告)号：US5426186A
公开(公告)日：1995-06-20
申请号：US30122
申请日：1993-03-03
申请人： Kenneth Shaw , Alan Hutchison
发明人： Kenneth Shaw , Alan Hutchison
IPC分类号： A61K31/505 , A61P25/20 , C07D487/04
CPC分类号： C07D487/04
摘要： This invention encompasses compounds of the formula: ##STR1## and pharmaceutically acceptable non-toxic salts thereof wherein: n is 0, 1, or 2, X is ##STR2## and R.sub.1, R.sub.2, R.sub.3, W and Y are variables These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs thereof and are useful in the diagnosis and treatment of anxiety, sleep, and seizure disorders, overdose with benzodiazepine type drugs, and enhancement of alertness.
摘要翻译： PCT No.PCT / US91 / 06174 Sec。 371日期1993年3月3日 102（e）日期1993年3月3日PCT 1991年9月4日PCT。本发明包括下式的化合物：其中n为0,1或2，X为 R1，R2，R3，W和Y是变量这些化合物是用于GABAa脑受体或其前药的高选择性激动剂，拮抗剂或反向激动剂，并且可用于诊断和治疗焦虑，睡眠和癫痫发作，过量服用苯二氮卓类药物，提高警惕性。

4. 发明申请

US20050014939A1 Fused pyrrolecarboxamides: GABA brain receptor ligands 审中-公开
标题翻译：融合的吡咯甲酰胺：GABA脑受体配体
公开(公告)号：US20050014939A1
公开(公告)日：2005-01-20
申请号：US10909022
申请日：2004-07-30
申请人： Pamela Albaugh , Kenneth Shaw , Alan Hutchison
发明人： Pamela Albaugh , Kenneth Shaw , Alan Hutchison
IPC分类号： A61K51/04 , C07D209/42 , C07D209/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D417/14 , C07D471/04 , C07D417/02 , C07D413/02 , C07
CPC分类号： C07D471/04 , A61K51/0419 , A61K51/0446 , A61K51/0453 , A61K51/0455 , A61K51/0459 , A61K51/0463 , C04B35/632 , C07D209/42 , C07D209/52 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , C07D417/14 , G01N2333/70571
摘要： Substituted pyrrolecarboxamide compounds are disclosed. 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 and are therefore useful in the diagnosis and treatment of anxiety, depression, Alzheimer's dementia, 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：公开了取代的吡咯甲酰胺化合物。这些化合物是用于GABA A受体的高选择性激动剂，拮抗剂或反向激动剂或GABA 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，阿尔茨海默氏痴呆，睡眠和发作障碍，过量与苯二氮卓类药物和增强记忆。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受体定位的探针。

5. 发明授权

US06420365B1 Imidazopyridines and related derivatives as selective modulators of bradykinin B2 receptors 失效
标题翻译：咪唑并吡啶类和相关衍生物作为缓激肽B2受体的选择性调节剂
公开(公告)号：US06420365B1
公开(公告)日：2002-07-16
申请号：US09765159
申请日：2001-01-17
申请人： John M. Peterson , Alan Hutchison , Kenneth Shaw , Kevin Hodgetts , George D. Maynard , Richard Lew
发明人： John M. Peterson , Alan Hutchison , Kenneth Shaw , Kevin Hodgetts , George D. Maynard , Richard Lew
IPC分类号： A61K31435
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein A, B, C, D, Y, R1, R3, R4, R5, and R6 are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatory disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility, glaucoma, pain, asthma, and rhinitis and for the increase of permeability of the blood-brain barrier or the blood-brain-tumor barrier.
摘要翻译：公开了下式的化合物或其药学上可接受的无毒性盐，其中A，B，C，D，Y，R 1，R 3，R 4，R 5和R 6是本文定义的变量，该化合物是缓激肽B2受体的调节剂。这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛，经皮腔内冠状动脉血管成形术，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症，青光眼，疼痛，哮喘和鼻炎的再狭窄，以及增加血脑屏障或血脑屏障的渗透性，肿瘤屏障。

6. 发明授权

US06358949B1 Aryl and hetroaryl fused aminoalkyl-imidazole derivatives: selective modulators of bradykinin B2 receptors 失效
标题翻译：芳基和杂芳基稠合氨基烷基 - 咪唑衍生物：缓激肽B2受体的选择性调节剂
公开(公告)号：US06358949B1
公开(公告)日：2002-03-19
申请号：US09540580
申请日：2000-03-31
申请人： Robert W. DeSimone , Alan Hutchison , Kenneth Shaw , George D. Maynard , John M. Peterson , Richard Lew , Harry L. Brielmann
发明人： Robert W. DeSimone , Alan Hutchison , Kenneth Shaw , George D. Maynard , John M. Peterson , Richard Lew , Harry L. Brielmann
IPC分类号： A61K315377
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: A, B, C and D are N or CH; X is a bond or (un)substituted CH2; R1 is lower alkenyl or (un)substituted lower alkyl; R3 is lower alkyl; and R2, R4, R5, and R6 are variables defined herein; which compounds are useful in the diagnosis and treatment of renal diseases, heart failure, hypertension, Meniere's disease, vaginal inflammation and pain, peripheral circulatory disorders, climacteric disturbance, retinochoroidal circulatroy disorders, myocardial ischemia, myocardial infarction, postmyocardial infarction syndrome, angina pectoris, restenosis after percutaneous transluminal coronary angioplasty, hepatitis, liver cirrhosis, pancreatitis, ileus, diabetes, diabetic complications, male infertility or glaucoma, or for the increase of permeability of blood-brain barrier, pain, asthma, and rhinitis.
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：A，B，C和D是N或CH; X是一个或（un）取代的CH 2; R 1是低级烯基或（取代）低级烷基; R3是低级烷基; 和R2，R4，R5和R6是本文定义的变量;这些化合物可用于诊断和治疗肾脏疾病，心力衰竭，高血压，梅尼埃病，阴道炎症和疼痛，外周循环障碍，更年期障碍，视网膜循环障碍，心肌缺血，心肌梗死，心肌梗死后综合征，心绞痛，经皮腔内冠状动脉成形术后再狭窄，肝炎，肝硬化，胰腺炎，肠梗阻，糖尿病，糖尿病并发症，男性不育症或青光眼，或增加血脑屏障通透性，疼痛，哮喘和鼻炎。

7. 发明授权

US06211365B1 Fused pyrrolecarboxamides; a new class of GABA brain receptor ligands 失效
标题翻译：熔融吡咯烷酰胺; 一类新的GABA脑受体配体
公开(公告)号：US06211365B1
公开(公告)日：2001-04-03
申请号：US09387313
申请日：1999-08-31
申请人： Pamela Albaugh , Gang Liu , Kenneth Shaw , Alan Hutchison
发明人： Pamela Albaugh , Gang Liu , Kenneth Shaw , Alan Hutchison
IPC分类号： C07D41312
CPC分类号： C07D401/12 , C07D209/42 , C07D209/52 , C07D405/12 , C07D413/12
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R3-R6 are as defined herein, 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：公开了下式的化合物或其药学上可接受的无毒盐，其中：G，X，T，n和R3-R6如本文所定义，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。

8. 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。

9. 发明授权

US07348326B2 Heteroaryl fused aminoalkyl imidazole derivatives: selective modulators of GABAa receptors 失效
标题翻译：杂芳基稠合氨基烷基咪唑衍生物：GABAa受体的选择性调节剂
公开(公告)号：US07348326B2
公开(公告)日：2008-03-25
申请号：US11295173
申请日：2005-12-06
申请人： Robert DeSimone , Alan Hutchison , Kenneth Shaw , Daniel Rosewater
发明人： Robert DeSimone , Alan Hutchison , Kenneth Shaw , Daniel Rosewater
IPC分类号： A01N43/58 , A01N43/60 , C07D237/00 , C07D237/02 , C07D513/02
CPC分类号： C07D235/14 , C07D401/06 , C07D405/06 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R1, R2, R3, R4, R5, and R6, are variables defined herein, 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, and are therefore useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, depression, overdose with benzodiazepine drugs, and enhancement of memory and 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A，B，C，D，X，R 1，R 2， R 3，R 4，R 5和R 6是本文定义的变量，这些化合物是高度选择性的激动剂，GABAa脑受体的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，因此可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和癫痫发作障碍，抑郁症，苯并二氮卓过量药物，提高记忆力和警觉性。

10. 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。

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