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1. 发明申请

US20020143044A1 Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives; new classes of dopamine receptor subtype specific ligands 失效
标题翻译：某些4-氨基甲基-2-取代的咪唑衍生物和2-氨基甲基-4-取代的咪唑衍生物; 新类型的多巴胺受体亚型特异性配体
公开(公告)号：US20020143044A1
公开(公告)日：2002-10-03
申请号：US10100691
申请日：2002-03-18
申请人： Neurogen Corporation
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： A61K031/4178 , A61K031/417 , C07D403/02 , C07D233/64 , C07D233/22
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds of the formula: 1 wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may together form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以一起形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

2. 发明申请

US20030018025A1 Certain 4-aminomethyl-2-substituted imidazole derivatives and 2-aminomethyl-4-substituted imidazole derivatives: new classes of dopamine receptor subtype specific ligands 审中-公开
标题翻译：某些4-氨基甲基-2-取代的咪唑衍生物和2-氨基甲基-4-取代的咪唑衍生物：新类型的多巴胺受体亚型特异性配体
公开(公告)号：US20030018025A1
公开(公告)日：2003-01-23
申请号：US10156262
申请日：2002-05-28
申请人： Neurogen Corporation, Corporation of the State of Delaware
发明人： Andrew Thurkauf , Raymond F. Horvath , Jun Yuan , John M. Peterson
IPC分类号： C07D43/02 , A61K031/55 , A61K031/454
CPC分类号： C07D233/64 , C07D233/90 , C07D235/18 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/04 , C07D409/14 , C07D487/08
摘要： Disclosed are compounds of the formula: 1 wherein R1 represents optionally substituted aryl, heteroaryl, arylalkyl, or cycloalkyl groups; X, Z, and Y are optionally substituted nitrogen or carbon atoms; R3 and R4 are organic or inorganic substitutents which may togther form ring structutes; m is zero, one or two; and R5 and R6 are are organic or inorganic substituents; and the pharmaceutically acceptable addition salts thereof, which compounds are highly selective partial agonists or antagonists at brain dopamine receptor subtypes or prodrugs thereof and are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中R 1表示任选取代的芳基，杂芳基，芳烷基或环烷基; X，Z和Y任选被取代的氮或碳原子; R3和R4是可以形成环结构的有机或无机取代基; m为零，一或二; R5和R6是有机或无机取代基; 和其药学上可接受的加成盐，该化合物是脑多巴胺受体亚型或其前药的高选择性部分激动剂或拮抗剂，并且可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

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。

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