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32 条记录 (耗时 0.038 秒)

    Aryl and hetroaryl fused aminoalkyl-imidazole derivatives: selective modulators of bradykinin B2 receptors
    1.
    发明授权
    Aryl and hetroaryl fused aminoalkyl-imidazole derivatives: selective modulators of bradykinin B2 receptors 失效
    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。

    Aryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
    4.
    发明授权
    Aryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors 失效
    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：US06627624B1

    公开(公告)日：2003-09-30

    申请号：US09541797

    申请日：2000-03-31

    申请人： Robert W. DeSimone ,  Alan Hutchison ,  Kenneth Shaw ,  Daniel L. Rosewater

    发明人： Robert W. DeSimone ,  Alan Hutchison ,  Kenneth Shaw ,  Daniel L. Rosewater

    IPC分类号： C07D47104

    CPC分类号： C07D401/06 ,  C07D235/14 ,  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。

    Heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors
    5.
    发明授权
    Heteroaryl fused aminoalkyl-imidazole derivatives: selective modulators of GABAa receptors 失效
    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：US06380210B1

    公开(公告)日：2002-04-30

    申请号：US09540454

    申请日：2000-03-31

    申请人： Robert W. DeSimone ,  Alan Hutchison ,  Kenneth Shaw ,  Daniel L. Rosewater

    发明人： Robert W. DeSimone ,  Alan Hutchison ,  Kenneth Shaw ,  Daniel L. Rosewater

    IPC分类号： A61K3150

    CPC分类号： C07D401/06 ,  C07D235/14 ,  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。

    Cycloalkyl and aryl fused aminoalkyl-imidazole derivatives: modulators and GLP-1 receptors
    8.
    发明授权
    Cycloalkyl and aryl fused aminoalkyl-imidazole derivatives: modulators and GLP-1 receptors 失效
    环烷基和芳基稠合的氨基烷基 - 咪唑衍生物：调节剂和GLP-1受体

    公开(公告)号：US06271241B1

    公开(公告)日：2001-08-07

    申请号：US09539835

    申请日：2000-03-31

    申请人： Robert W. DeSimone ,  Alan Hutchison

    发明人： Robert W. DeSimone ,  Alan Hutchison

    IPC分类号： A61K31435

    CPC分类号： C07D471/04 ,  C07D235/14 ,  G01N2333/72

    摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein X, R1, R2, R3, R4, R5, R6, R7, A, B, C, and D are variables defined herein. Such compounds useful in treatment of obesity and diabetes. The invention also provides labeled probes for the localization of cellular receptors that are involved in the modulation of blood glucose levels.

    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X，R 1，R 2，R 3，R 4，R 5，R 6，R 7，A，B，C和D是本文定义的变量。 这些化合物可用于治疗肥胖症和糖尿病。 本发明还提供了用于调节血糖水平的细胞受体定位的标记探针。

    Capsaicin receptor ligands
    10.
    发明授权
    Capsaicin receptor ligands 失效
    辣椒素受体配体

    公开(公告)号：US06723730B2

    公开(公告)日：2004-04-20

    申请号：US09910442

    申请日：2001-07-20

    申请人： Rajagopal Bakthavatchalam ,  Alan Hutchinson ,  Robert W. DeSimone ,  Kevin J. Hodgetts ,  James E. Krause ,  Geoffrey G. White

    发明人： Rajagopal Bakthavatchalam ,  Alan Hutchinson ,  Robert W. DeSimone ,  Kevin J. Hodgetts ,  James E. Krause ,  Geoffrey G. White

    IPC分类号： C07D295192

    CPC分类号： C07D213/74 ,  C07D213/75 ,  C07D217/22 ,  C07D241/20 ,  C07D405/12 ,  C07D417/12

    摘要： Disclosed are diaryl piperazines and related compounds of the following Formula: wherein the variables are as defined in the specification. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

    摘要翻译： 公开了下式的二芳基哌嗪和相关化合物：其中变量如说明书中所定义。 这些化合物是辣椒素受体的选择性调节剂，包括人类辣椒素受体，因此可用于治疗慢性和急性疼痛病症，瘙痒和尿失禁。 还提供了治疗这种疾病以及包装的药物组合物的方法。 本发明的化合物也可用作辣椒素受体定位的探针，也可用作辣椒素受体结合和辣椒素受体介导的阳离子电导测定中的标准。 给出了在受体定位研究中使用化合物的方法。