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    Template-fixed peptidomimetics
    4.
    发明授权
    Template-fixed peptidomimetics 有权
    模板固定肽模拟物

    公开(公告)号：US08921325B2

    公开(公告)日：2014-12-30

    申请号：US13764099

    申请日：2013-02-11

    申请人： Universitaet Zuerich ,  Polyphor Ltd.

    发明人： Daniel Obrecht ,  Frank Gombert ,  Steven J. Demarco ,  Christian Ludin ,  Jan Wim Vrijbloed ,  Kerstin Moehle ,  John-Anthony Robinson ,  Reshmi Mukherjee ,  Heiko Henze ,  Barbara Romagnoli

    IPC分类号： A61K38/12 ,  C07K7/56

    CPC分类号： C07K7/56 ,  A61K38/00 ,  A61K38/12 ,  C07K7/64

    摘要： The template-fixed β-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where Cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or, in particular, for stem cell mobilization of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.

    摘要翻译： 模板固定和固定肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro），Cys4和 Gys11及其药学上可接受的盐，X为Ala或Tyr，具有CXCR4拮抗性质，可用于预防健康个体的HIV感染或减缓和阻止感染患者的病毒进展; 或其中癌症介导或由CXCR4受体活性产生; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或特别是用于干细胞移动外周血干细胞和/或间充质干细胞（MSC）和/或其它干细胞，其保留取决于CXCR4-受体。 这些和包装肽模拟物可以通过使用基于混合固相和溶液相合成策略的方法，使用肽化学方面熟练的技术熟知的方法来制造。

    TEMPLATE-FIXED PEPTIDOMIMETICS
    8.
    发明申请
    TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
    模板固定蛋白质

    公开(公告)号：US20140107031A1

    公开(公告)日：2014-04-17

    申请号：US14134566

    申请日：2013-12-19

    申请人： POLYPHOR LTD.

    发明人： Daniel Obrecht ,  Frank Gombert ,  Steven J. Demarco ,  Christian Ludin ,  Alexander Lederer ,  Christian Bisang ,  Odile Sellier-Kessler ,  Francoise Jung ,  Reshmi Mukherjee ,  Heiko Henze ,  Barbara Romagnoli

    IPC分类号： C07K7/64 ,  C07K5/02

    CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K5/02 ,  C07K5/101 ,  C07K5/1013 ,  C07K5/1016 ,  C07K5/1021 ,  C07K5/1024 ,  C07K7/06 ,  C07K7/08

    摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 4 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory diseases, haematological diseases and cancer.These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    摘要翻译： 模板固定和通用的肽模拟物，其中Z是4个α-氨基酸残基的模板固定链，取决于其在链中的位置（从N-末端氨基酸开始计数）为Gly， 或某些类型，其作为上述式中的其余符号在说明书和权利要求书及其权利要求中所定义，具有激动或拮抗GPCR受体如CXCR3，尿素调节素和CCR10的性质。 它们可以用作治疗或预防心血管疾病，皮肤病，内分泌系统和激素失调，代谢疾病，炎性疾病，神经疾病，呼吸系统疾病，血液病和癌症等疾病的药物。 这些可以通过基于混合固相和溶液相合成策略的方法制造。