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    APJ RECEPTOR COMPOUNDS
    1.
    发明申请
    APJ RECEPTOR COMPOUNDS 审中-公开
    APJ受体化合物

    公开(公告)号：US20120028888A1

    公开(公告)日：2012-02-02

    申请号：US13127428

    申请日：2009-11-04

    申请人： Jay Janz ,  Athan Kuliopulos ,  Thomas J. McMurry

    发明人： Jay Janz ,  Athan Kuliopulos ,  Thomas J. McMurry

    IPC分类号： A61K38/16 ,  C07K7/06 ,  C07K7/08 ,  C07K14/00 ,  C07K5/10 ,  A61K38/03 ,  A61K38/04 ,  A61K38/08 ,  A61K38/10 ,  A61P9/12 ,  A61P9/10 ,  A61P35/00 ,  A61P35/04 ,  A61P3/10 ,  A61P3/04 ,  A61P37/00 ,  A61P31/18 ,  C07K5/08

    CPC分类号： C07K14/7158 ,  A61K38/00 ,  A61K47/542 ,  A61K47/554

    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 apelin, also known as the APJ receptor. The APJ receptor compounds are derived from the intracellular loops and domains of the the APJ receptor. The invention also relates to the use of these APJ receptor compounds and pharmaceutical compositions comprising the APJ receptor compounds in the treatment of diseases and conditions associated with APJ receptor modulation, such as heart diseases (e.g., hypertension and tension and heart failure, such as congestive heart failure), cancer, diabetes, stem cell trafficking, fluid homeostasis, cell proliferation, immune function, obesity, metastatic disease, and HIV infection.

    摘要翻译： 本发明一般涉及G蛋白偶联受体apelin（也称为APJ受体）的变构调节剂（例如，负变构和正变构调节剂，变构激动剂和前变体调节剂）的化合物。 APJ受体化合物衍生自APJ受体的细胞内环和结构域。 本发明还涉及这些APJ受体化合物和包含APJ受体化合物的药物组合物在治疗与APJ受体调节有关的疾病和病症如心脏病（例如高血压和张力和心力衰竭，例如充血性 心力衰竭），癌症，糖尿病，干细胞运输，流体体内平衡，细胞增殖，免疫功能，肥胖，转移性疾病和HIV感染。

    Production, purification, cleavage and use of fusion peptides
    4.
    发明授权
    Production, purification, cleavage and use of fusion peptides 失效
    融合肽的生产，纯化，切割和使用

    公开(公告)号：US5648244A

    公开(公告)日：1997-07-15

    申请号：US127692

    申请日：1993-09-27

    申请人： Athan Kuliopulos ,  Christopher T. Walsh

    发明人： Athan Kuliopulos ,  Christopher T. Walsh

    IPC分类号： C07K14/39 ,  C12N9/64 ,  C12N9/90 ,  C12N15/62 ,  C12N15/09 ,  C12N15/63 ,  C12N15/70

    CPC分类号： C12N9/644 ,  C07K14/39 ,  C12N15/62 ,  C12N9/90 ,  C12Y304/21022 ,  C07K2319/00 ,  C07K2319/23 ,  C07K2319/75

    摘要： A method for producing a fusion peptide. A vector is provided with nucleic acid encoding a carrier peptide and at the 3' end of the nucleic acid, a unidirectional restriction endonuclease cleavage site recognized by a restriction endonuclease with the ability to create a non-palindromic 3-base overhang. The vector is cleaved with the restriction endonuclease to produce a cleaved vector. One or more nucleic acids encoding a desired peptide and having at least a 3-base overhang at each end configured and arranged for ligation with the cleaved vector is then ligated to the cleavage site.

    摘要翻译： 一种融合肽的制备方法。 向载体提供编码载体肽的核酸，并且在核酸的3'末端，由限制性内切核酸酶识别的单向限制性内切核酸酶切割位点具有产生非回文性3-碱基突出端的能力。 用限制性内切核酸酶切割载体以产生切割的载体。 编码所需肽并且在每个末端具有至少3个碱基突出端的一个或多个核酸被配置并排列用于与切割的载体连接，然后连接到切割位点。

    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。