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1. 发明申请

US20030092912A1 Heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa Receptors 审中-公开
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：US20030092912A1
公开(公告)日：2003-05-15
申请号：US10115361
申请日：2002-04-03
申请人： Neurogen Corporation, a corporation of the state of Delaware
发明人： Robert W. DeSimone , Alan Hutchison , Kenneth Shaw , Daniel L. Rosewater
IPC分类号： C07D471/02 , C07D473/00
CPC分类号： C07D401/06 , C07D235/14 , C07D405/06 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of the formula: 1 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性盐，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， GABAa脑受体的GABAa脑受体的选择性激动剂，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，因此可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和发作障碍，抑郁症，过量与苯二氮类药物，并增强记忆力和警觉性。

2. 发明申请

US20030153754A1 Fused pyrrolecarboxamides; a new class of GABA brain receptor ligands 审中-公开
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：US20030153754A1
公开(公告)日：2003-08-14
申请号：US10303096
申请日：2002-11-22
申请人： Neurogen Corporation, A Corporation of the State of Delaware
发明人： Pamela Albaugh , Gang Liu , Kenneth Shaw , Alan Hutchison
IPC分类号： C07D413/02 , C07D403/02 , C07D45/02 , C07D209/36
CPC分类号： C07D401/12 , C07D209/42 , C07D209/52 , C07D405/12 , C07D413/12
摘要： Disclosed are the compounds of the formula: 1 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脑的高选择性激动剂，拮抗剂或反向激动剂 GABAa脑受体的激动剂，拮抗剂或反向激动剂的受体或前体药物。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。

3. 发明申请

US20020151550A1 Aryl and heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of bradykinin B2 receptors 审中-公开
标题翻译：芳基和杂芳基稠合的氨基烷基 - 咪唑衍生物：缓激肽B2受体的选择性调节剂
公开(公告)号：US20020151550A1
公开(公告)日：2002-10-17
申请号：US10100697
申请日：2002-03-18
申请人： Neurogen Corporation
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： C07D471/02 , C07D491/02 , A61K031/52
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: 1 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是键或（取代的）取代的CH 2; R1是低级烯基或（未）取代的低级烷基; R3是低级烷基; R2，R4，R5和R6是本文定义的变量; 哪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，男性不育症或青光眼，或增加血脑屏障，疼痛，哮喘和鼻炎的通透性后再狭窄。

4. 发明申请

US20020019410A1 Imidazoloisoquinolines 失效
标题翻译：咪唑并异喹啉
公开(公告)号：US20020019410A1
公开(公告)日：2002-02-14
申请号：US09867304
申请日：2001-05-29
申请人： Neurogen Corporation
发明人： Guolin Cai , Kenneth Shaw
IPC分类号： A61K031/4745 , C07D471/04
CPC分类号： C07D471/04 , C07D217/24 , C07D237/32 , C07D487/04
摘要： Disclosed are compounds of the formula: 1 and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein n, R1, R2, R3, W, Q, and X are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，前药和溶剂化物，其中n，R 1，R 2，R 3，W，Q和X在本文中定义，该化合物以高选择性和对苯并二氮杂位点的高亲和力的GABA A受体，因此可用于治疗某些中枢神经系统（CNS）疾病和作为组织样品中GABA A受体定位的探针。

5. 发明申请

US20020119911A1 Methods for screening GABA-modulatory compounds for specified pharmacological activities 审中-公开
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：US20020119911A1
公开(公告)日：2002-08-29
申请号：US10045375
申请日：2001-11-09
申请人： Neurogen Corporation
发明人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
IPC分类号： A61K031/00 , G01N033/53
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 null,null,and null 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。这些方法涉及确定化合物在由α，β和γ亚基的特异性变体组成的克隆的GABAA亚型受体的体外功效和EC 50，以便开发每种化合物的活性谱。任选地，还测定了化合物在GABA 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

6. 发明申请

US20030181455A1 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：US20030181455A1
公开(公告)日：2003-09-25
申请号：US10352519
申请日：2003-01-28
申请人： Neurogen Corporation, A Corporation of the State of Delaware
发明人： Jun Yuan , Pamela Albaugh , Kenneth Shaw , Alan Hutchison
IPC分类号： A61K031/503 , A61K031/4745 , C07D487/14
CPC分类号： C07D217/26 , C07D237/30 , C07D471/04 , C07D487/04 , C07D519/00 , G01N2333/70571
摘要： Disclosed are compounds of the formula: 1 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）疾病和作为组织样品中GABA A受体定位的探针。还公开了可用于制备这些化合物的中间体。

7. 发明申请

US20010011133A1 Oxo-pyridoimidazole-carboxamides: GABA brain receptor ligands 失效
标题翻译：氧 - 吡啶并咪唑 - 甲酰胺：GABA脑受体配体
公开(公告)号：US20010011133A1
公开(公告)日：2001-08-02
申请号：US09761601
申请日：2001-01-16
申请人： Neurogen Corporation.
发明人： Bogumila Rachwal , Pamela Albaugh , Kenneth Shaw
IPC分类号： C07D471/00 , C07D491/00 , C07D498/00 , C07D513/00 , C07D515/00
CPC分类号： C07D471/04
摘要： Disclosed are compounds of the formula: 1 or the pharmaceutically acceptable non-toxic salts thereof where R1-R4 and A are 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, depression, sleep, cognitive and seizure disorders, 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R1-R4和A在本文中定义，该化合物是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，唐氏综合症，抑郁症，睡眠，认知和癫痫发作，用苯二氮卓类药物服用过量，提高警觉性。

8. 发明申请

US20040023993A1 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：US20040023993A1
公开(公告)日：2004-02-05
申请号：US10609941
申请日：2003-06-30
申请人： Neurogen Corporation A Corporation of the State of Delaware
发明人： Robert W. DeSimone , Alan Hutchison , Kenneth Shaw , Daniel L. Rosewater
IPC分类号： C07D471/02 , A61K031/52 , C07D473/00
CPC分类号： C07D401/06 , C07D235/14 , C07D405/06 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of the formula: 1 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性盐，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， GABAa脑受体的GABAa脑受体的选择性激动剂，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，因此可用于诊断和治疗焦虑症，唐氏综合征，睡眠，认知和发作障碍，抑郁症，过量与苯二氮类药物，并增强记忆力和警觉性。

9. 发明申请

US20020115611A1 Methods for screening GABA-modulatory compounds for specified pharmacological activities 审中-公开
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：US20020115611A1
公开(公告)日：2002-08-22
申请号：US10045230
申请日：2001-11-09
申请人： Neurogen Corporation
发明人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
IPC分类号： A61K038/17 , G01N033/53 , G01N033/567
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 null,null, and null 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。这些方法涉及确定化合物在由α，β和γ亚基的特异性变体组成的克隆的GABAA亚型受体的体外功效和EC 50，以便开发每种化合物的活性谱。任选地，还测定了化合物在GABA 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

10. 发明申请

US20020103108A1 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：US20020103108A1
公开(公告)日：2002-08-01
申请号：US10045396
申请日：2001-11-09
申请人： Neurogen Corporation
发明人： John Tallman , Dorothy Gallager , Kenneth Shaw , Geoffrey White , Marci Crandall , James Cassella , Lavanya Rajachandran , Pamela Albaugh
IPC分类号： A61K031/00 , G01N033/53 , G06F019/00 , G01N033/48 , G01N033/50
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 null, null, and null 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。这些方法涉及确定化合物在由α，β和γ亚基的特异性变体组成的克隆的GABAA亚型受体的体外功效和EC 50，以便开发每种化合物的活性谱。任选地，还测定了化合物在GABA 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

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