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    Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds
    1.
    发明授权
    Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds 失效
    吡咯并吡啶，吡咯并嘧啶和相关的杂环化合物

    公开(公告)号：US08633193B2

    公开(公告)日：2014-01-21

    申请号：US13014066

    申请日：2011-01-26

    Applicant: Jun Yuan ,  Peter Hrnciar ,  Qin Guo ,  George D. Maynard

    Inventor： Jun Yuan ,  Peter Hrnciar ,  Qin Guo ,  George D. Maynard

    IPC: A61K31/519 ,  C07D487/04 ,  A61P37/00 ,  A61P37/06 ,  A61P11/06 ,  A61P17/06

    CPC classification number: C07D471/04

    Abstract: Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds analogues of the formula: wherein R, R2, R5, E, Z1, Z3, Z4, and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds of the invention 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 pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds, which are useful as probes for the localization of C5a receptors.

    Abstract translation: 吡咯并 - 吡啶，吡咯并 - 嘧啶和相关的杂环化合物，其分子式如下：其中R，R 2，R 5，E，Z 1，Z 3，Z 4和Ar如本文所定义。 这些化合物是C5a受体的配体。 本发明优选的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物以高亲和力结合C5a受体，并在C5a受体上表现出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，本发明提供了标记的吡咯并 - 吡啶，吡咯并 - 嘧啶和相关杂环化合物，其可用作C5a受体定位的探针。

    Imidazopyridines and related derivatives as selective modulators of bradykinin B2 receptors
    3.
    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

    Applicant: John M. Peterson ,  Alan Hutchison ,  Kenneth Shaw ,  Kevin Hodgetts ,  George D. Maynard ,  Richard Lew

    Inventor： John M. Peterson ,  Alan Hutchison ,  Kenneth Shaw ,  Kevin Hodgetts ,  George D. Maynard ,  Richard Lew

    IPC: A61K31435

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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。

    Aryl and hetroaryl fused aminoalkyl-imidazole derivatives: selective modulators of bradykinin B2 receptors
    4.
    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

    Applicant: Robert W. DeSimone ,  Alan Hutchison ,  Kenneth Shaw ,  George D. Maynard ,  John M. Peterson ,  Richard Lew ,  Harry L. Brielmann

    Inventor： Robert W. DeSimone ,  Alan Hutchison ,  Kenneth Shaw ,  George D. Maynard ,  John M. Peterson ,  Richard Lew ,  Harry L. Brielmann

    IPC: A61K315377

    CPC classification number: C07D471/04

    Abstract: 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.

    Abstract translation: 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。

    Aminoalkyl substituted 9H-pyridino[2,3-b] indole and 9H-pyrimidino[4,5-b] indole derivatives
    5.
    发明授权
    Aminoalkyl substituted 9H-pyridino[2,3-b] indole and 9H-pyrimidino[4,5-b] indole derivatives 失效
    氨基烷基取代的9H-吡啶并[2,3-b]吲哚和9H-嘧啶并[4,5-b]吲哚衍生物

    公开(公告)号：US6147085A

    公开(公告)日：2000-11-14

    申请号：US283409

    申请日：1999-04-01

    Applicant: Raymond F. Horvath ,  James W. Darrow ,  George D. Maynard

    Inventor： Raymond F. Horvath ,  James W. Darrow ,  George D. Maynard

    IPC: A61P9/12 ,  A61P25/22 ,  C07D471/04 ,  C07D487/04 ,  A61K31/437

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: Disclosed are compounds of the formula: ##STR1## wherein Ar, R.sup.1, W and X are substituents as defined herein, which compounds are (1) antagonists at CRF.sub.1 receptors and are, therefore, useful in the diagnosis and treatment of stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety; and (2) are neuropeptide Y.sub.1 receptor antagonists, and are therefore useful in the treatment of a variety of clinical conditions which are characterized by the presence of an excess of neuropeptide Y.

    Abstract translation: 公开了下式的化合物：其中Ar，R 1，W和X是如本文所定义的取代基，该化合物是（1）CRF1受体的拮抗剂，因此可用于诊断和治疗应激相关疾病如创伤后 压力障碍（PTSD）以及抑郁，头痛和焦虑; 和（2）是神经肽Y1受体拮抗剂，因此可用于治疗以过量神经肽Y的存在为特征的各种临床病症。

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