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    G protein coupled receptor agonists and antagonists and methods of use
    1.
    发明授权
    G protein coupled receptor agonists and antagonists and methods of use 有权
    G蛋白偶联受体激动剂和拮抗剂及其使用方法

    公开(公告)号：US08440627B2

    公开(公告)日：2013-05-14

    申请号：US11667042

    申请日：2005-11-04

    申请人： Athan Kuliopulos ,  Lidija Covic ,  Nicole Kaneider

    发明人： Athan Kuliopulos ,  Lidija Covic ,  Nicole Kaneider

    IPC分类号： C12P21/04 ,  C07K14/705 ,  A61K38/04

    CPC分类号： C07K14/705 ,  C07K14/7155 ,  C07K14/7158 ,  C07K14/723

    摘要： The invention relates generally to G protein coupled receptors (GPCRs) and in particular to GPCR agonists and antagonists, use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with GPCRs, such as in treating conditions in which chemokine receptors play a role, e.g., sepsis, arthritis, inflammation and autoimmune diseases.

    摘要翻译： 本发明一般涉及G蛋白偶联受体（GPCR），特别是涉及GPCR激动剂和拮抗剂，这些化合物及其药物组合物的用途，例如用于治疗，调节和/或预防与GPCR有关的生理状态，例如 在治疗趋化因子受体起作用的病症中，例如败血症，关节炎，炎症和自身免疫性疾病。

    G Protein Coupled Receptor Agonists and Antagonists and Methods of Use
    2.
    发明申请
    G Protein Coupled Receptor Agonists and Antagonists and Methods of Use 有权
    G蛋白偶联受体激动剂和拮抗剂及其使用方法

    公开(公告)号：US20080214451A1

    公开(公告)日：2008-09-04

    申请号：US11667042

    申请日：2005-11-04

    申请人： Athan Kuliopulos ,  Lidija Covic ,  Nicole Kaneider

    发明人： Athan Kuliopulos ,  Lidija Covic ,  Nicole Kaneider

    IPC分类号： A61K38/00 ,  C07K14/00 ,  A61P43/00

    CPC分类号： C07K14/705 ,  C07K14/7155 ,  C07K14/7158 ,  C07K14/723

    摘要： The invention relates generally to G protein coupled receptors (GPCRs) and in particular to GPCR agonists and antagonists, use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with GPCRs, such as in treating conditions in which chemokine receptors play a role, e.g., sepsis, arthritis, inflammation and autoimmune diseases.

    摘要翻译： 本发明一般涉及G蛋白偶联受体（GPCR），特别是涉及GPCR激动剂和拮抗剂，这些化合物及其药物组合物的用途，例如用于治疗，调节和/或预防与GPCR有关的生理状态，例如 在治疗趋化因子受体起作用的病症中，例如败血症，关节炎，炎症和自身免疫性疾病。

    CXCR4 receptor compounds
    9.
    发明授权
    CXCR4 receptor compounds 有权
    CXCR4受体化合物

    公开(公告)号：US09096646B2

    公开(公告)日：2015-08-04

    申请号：US13127443

    申请日：2009-11-04

    申请人： Thomas J. McMurry ,  Athan Kuliopulos ,  Lidija Covic ,  Boris Tchernychev

    发明人： Thomas J. McMurry ,  Athan Kuliopulos ,  Lidija Covic ,  Boris Tchernychev

    IPC分类号： C07K7/08 ,  C07K14/715 ,  C07K7/06 ,  A61K38/00

    CPC分类号： C07K7/08 ,  A61K38/00 ,  C07K7/06 ,  C07K14/7158

    摘要： The invention relates generally to compounds which are allosteric modulators (e.g., positive and negative allosteric modulators, and allosteric agonists) of the G protein coupled receptor for stromal derived factor 1 (SDF-I), also known as the CXCR4 receptor. The CXCR4 receptor compounds are derived from the intracellular loops and domains of the CXCR4 receptor. The invention also relates to the use of these CXCR4 receptor compounds and pharmaceutical compositions comprising the CXCR4 receptor compounds in the treatment of diseases and conditions associated with CXCR4 modulation such as bone marrow transplantation, chemosensitization, cancer, metastatic disease, inflammatory diseases, HIV infection and stem cell-based regenerative medicine.

    摘要翻译： 本发明一般涉及用于间质衍生因子1（SDF-1）（也称为CXCR4受体）的G蛋白偶联受体的变构调节剂（例如，正和负变构调节剂和变构兴奋剂）的化合物。 CXCR4受体化合物衍生自CXCR4受体的细胞内环和结构域。 本发明还涉及这些CXCR4受体化合物和包含CXCR4受体化合物的药物组合物在治疗与CXCR4调节相关的疾病和病症如骨髓移植，化学敏化，癌症，转移性疾病，炎性疾病，HIV感染和 干细胞再生医学。

    PEPDUCIN DESIGN AND USE
    10.
    发明申请
    PEPDUCIN DESIGN AND USE 审中-公开
    PEPDUCIN设计和使用

    公开(公告)号：US20140087993A1

    公开(公告)日：2014-03-27

    申请号：US14009479

    申请日：2012-04-09

    申请人： Athan Kuliopulos ,  Lidija Covic

    发明人： Athan Kuliopulos ,  Lidija Covic

    IPC分类号： C07K14/705

    CPC分类号： C07K14/705 ,  A61K38/00 ,  C07K2319/00

    摘要： Disclosed here is the rational design and use of potent and specific GPCR antagonist pepducins based on GPCR regions such as the third intracellular loop and adjacent regions.

    摘要翻译： 这里披露了基于GPCR区域（如第三细胞内环和相邻区域）的有效和特异性GPCR拮抗剂pepducin的合理设计和使用。