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57 条记录 (耗时 0.051 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。

    Imidazopyridines and related derivatives as selective modulators of bradykinin B2 receptors
    2.
    发明授权
    Imidazopyridines and related derivatives as selective modulators of bradykinin B2 receptors 失效
    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。

    Substituted imidazoles as selective modulators of Bradykinin B2 receptors
    4.
    发明授权
    Substituted imidazoles as selective modulators of Bradykinin B2 receptors 失效
    取代的咪唑作为缓激肽B2受体的选择性调节剂

    公开(公告)号：US06509366B2

    公开(公告)日：2003-01-21

    申请号：US09764805

    申请日：2001-01-17

    申请人： Stanislaw Rachwal ,  Alan Hutchison ,  Kenneth Shaw ,  George D. Maynard ,  Xiao-shu He ,  Robert DeSimone ,  Kevin Hodgetts

    发明人： Stanislaw Rachwal ,  Alan Hutchison ,  Kenneth Shaw ,  George D. Maynard ,  Xiao-shu He ,  Robert DeSimone ,  Kevin Hodgetts

    IPC分类号： A61K314174

    CPC分类号： C07D233/64 ,  C07D233/68 ,  C07D401/06

    摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein Y, R1, R2, R3, R4, R5, R6, R7 R7′ are variables defined herein, which compounds are modulators of Bradykinin B2 receptors. These compounds are therefore 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盐，其中Y，R 1，R 2，R 3，R 4，R 5，R 6，R 7 R 7'是本文定义的变量，该化合物是缓激肽B2受体的调节剂。 因此，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液 - 脑肿瘤屏障。

    2-aminoquinolinecarboxamides: neurokinin receptor ligands
    5.
    发明授权
    2-aminoquinolinecarboxamides: neurokinin receptor ligands 失效
    2-氨基喹啉甲酰胺：神经激肽受体配体

    公开(公告)号：US06894044B2

    公开(公告)日：2005-05-17

    申请号：US10115409

    申请日：2002-04-03

    申请人： Jun Yuan ,  George D. Maynard ,  Alan Hutchison

    发明人： Jun Yuan ,  George D. Maynard ,  Alan Hutchison

    IPC分类号： A61K31/47 ,  A61P25/00 ,  A61P25/28 ,  C07D215/50 ,  C07D401/04 ,  C07D453/06 ,  C07D491/10 ,  A61K31/4709

    CPC分类号： A61K31/47 ,  C07D215/50 ,  C07D401/04 ,  C07D453/06 ,  C07D491/10 ,  Y10S206/828

    摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.

    摘要翻译： 公开了下式的化合物或其药学上可接受的盐或药学上可接受的溶剂化物，其中R 1，R 2，R 3，X， 本文定义Q 1和Q 2 2，这些化合物是神经激肽受体特别是NK-3受体的配体，并且可用于治疗广泛范围的 疾病或病症，包括但不限于抑郁症，焦虑症，精神病，肥胖症，疼痛，帕金森病，阿尔茨海默病，神经变性疾病，运动​​障碍，呼吸系统疾病，炎性疾病，神经病，免疫疾病，偏头痛，胆汁功能异常和皮炎。

    1-aryl-4-substituted isoquinolines
    6.
    发明授权
    1-aryl-4-substituted isoquinolines 失效
    1-芳基-4-取代的异喹啉

    公开(公告)号：US07915288B2

    公开(公告)日：2011-03-29

    申请号：US11587906

    申请日：2005-05-06

    申请人： Kyungae Lee ,  Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Scott Mitchell

    发明人： Kyungae Lee ,  Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Scott Mitchell

    IPC分类号： C07D217/02 ,  A61K31/47

    CPC分类号： C07D405/12 ,  A61K31/47 ,  C07D217/14 ,  C07D217/16 ,  C07D217/22 ,  C07D401/04 ,  C07D401/06 ,  C07D401/14 ,  C07D413/14

    摘要： 1-aryl-4-substituted isoquinoline or 1-aryl-3,4-disubstituted isoquinoline analogues of Formula I and Formula II, as follows: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I and II bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 1-aryl-4-substituted isoquinolines or 1-aryl-3,4-disubstituted isoquinolines, which are useful as probes for the localization of C5a receptors.

    摘要翻译： 式I和式II的1-芳基-4-取代的异喹啉或1-芳基-3,4-二取代的异喹啉类似物如下：其中R1，R2，R3，R8，R9，A和Ar如本文所定义。 这些化合物是C5a受体的配体。 优选的式I和II化合物以高亲和力结合C5a受体，并在C5a受体上呈现中性拮抗剂或反向激动剂活性。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物在治疗各种炎性，心血管和免疫系统疾病中的用途。 此外，本发明提供标记的1-芳基-4-取代的异喹啉或1-芳基-3,4-二取代的异喹啉，其可用作C5a受体定位的探针。

    4-substituted quinoline derivatives
    9.
    发明授权
    4-substituted quinoline derivatives 失效
    4-取代喹啉衍生物

    公开(公告)号：US06413982B1

    公开(公告)日：2002-07-02

    申请号：US09536922

    申请日：2000-03-28

    申请人： Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Stanislaw Rachwal

    发明人： Jun Yuan ,  George D. Maynard ,  Alan Hutchison ,  Stanislaw Rachwal

    IPC分类号： A61L3147

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/04 ,  C07D487/04 ,  G01N33/9426 ,  G01N2333/70571

    摘要： Disclosed are compounds of the Formula where R1, R2, R3, R4, X, Y1, and Y2 are defined herein. These compounds bind with high affinity to NK-3 receptors and/or GABAA receptors. Also provided are pharmaceutical compositions comprising these compounds, and methods of treating patients suffering from various central nervous system and peripheral diseases or disorders with these pharmaceutical compositions. This invention also relates to the use of such compounds in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. The compounds of this invention are also useful as probes for the localization of NK-3 receptors and GABAA receptors.

    摘要翻译： 公开了本文定义的化学式R 1，R 2，R 3，R 4，X，Y 1和Y 2的化合物。 这些化合物以高亲和力结合NK-3受体和/或GABA A受体。 还提供了包含这些化合物的药物组合物，以及用这些药物组合物治疗患有各种中枢神经系统和外周疾病或病症的患者的方法。 本发明还涉及这样的化合物与一种或多种其它CNS剂组合用于增强其它CNS剂的作用的用途。 本发明的化合物也可用作NK-3受体和GABA A受体定位的探针。