CXCR4 receptor compounds
    1.
    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

    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。

    CXCR5 RECEPTOR COMPOUNDS
    2.
    发明申请
    CXCR5 RECEPTOR COMPOUNDS 审中-公开
    CXCR5受体化合物

    公开(公告)号:US20110300167A1

    公开(公告)日:2011-12-08

    申请号:US13127666

    申请日:2009-11-04

    CPC分类号: C07K14/7158 A61K38/00

    摘要: The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor CXCR5. The CXCR5 receptor compounds are derived from the intracellular loops and domains of the CXCR5 receptor. The invention also relates to the use of these CXCR5 receptor compounds and pharmaceutical compositions comprising the CXCR5 receptor compounds in the treatment of diseases and conditions associated with CXCR5 receptor modulation such as autoimmune diseases including lupus, HIV and rheumatoid arthritis, Primary Sjogren's Syndrome, chronic lymphocytic leukemia, Burkitt Lymphoma, colon and breast cancer tumor metastasis, Multiple Sclerosis and compromised immune function.

    摘要翻译: 本发明一般涉及G蛋白偶联受体CXCR5的变构调节剂(例如,负变构和正变构调节剂,变构兴奋剂和前变体调节剂)的化合物。 CXCR5受体化合物衍生自CXCR5受体的细胞内环和结构域。 本发明还涉及这些CXCR5受体化合物和包含CXCR5受体化合物的药物组合物在治疗与CXCR5受体调节相关的疾病和病症的应用,例如包括狼疮,HIV和类风湿性关节炎的自身免疫性疾病,原发性干燥综合征,慢性淋巴细胞 白血病,伯基特淋巴瘤,结肠癌和乳腺癌肿瘤转移,多发性硬化和免疫功能受损。

    CXCR4 Receptor Compounds
    3.
    发明申请
    CXCR4 Receptor Compounds 有权
    CXCR4受体化合物

    公开(公告)号:US20130210709A1

    公开(公告)日:2013-08-15

    申请号:US13127443

    申请日:2009-11-04

    IPC分类号: C07K7/08 C07K14/715 C07K7/06

    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 CX-CR4 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 trans-plantation, 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CX-CR4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转移,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

    IPC分类号: C07K14/705

    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。