公开(公告)号：US20070078079A1

公开(公告)日：2007-04-05

申请号：US10555088

申请日：2004-04-29

申请人： Jurg Zumbrunn ,  Steven Demarco ,  Sergio Lociuro ,  Jan Vrijbloed ,  Frank Gombert ,  Reshmi Mukherjee ,  Kerstin Moehle ,  Daniel Obrecht ,  John Robinson ,  Heiko Henze ,  Barbara Romagnoli ,  Christian Ludin

发明人： Jurg Zumbrunn ,  Steven Demarco ,  Sergio Lociuro ,  Jan Vrijbloed ,  Frank Gombert ,  Reshmi Mukherjee ,  Kerstin Moehle ,  Daniel Obrecht ,  John Robinson ,  Heiko Henze ,  Barbara Romagnoli ,  Christian Ludin

IPC分类号： A61K38/12 ,  C07K5/12

CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K1/047 ,  C07K7/08

摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 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 during apheresis collections of peripheral blood stem cells. 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： 通式（I）的模板固定的β-发夹肽模拟物，其中Z是12,14或18个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端开始计数 氨基酸）是Gly，NMeGly，Pro或Pip，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书中定义，及其盐具有CXCR4拮抗特性，可用于 预防健康人中的艾滋病毒感染或减缓和停止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 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; 或在外周血干细胞的分离采集期间。 这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。

公开(公告)号：US20060234923A1

公开(公告)日：2006-10-19

申请号：US10550778

申请日：2003-05-02

申请人： Jurg Zumbrunn ,  Steven Demarco ,  Sergio Lociuro ,  Daniel Obrecht ,  Barbara Romagnoli ,  John Robinson

发明人： Jurg Zumbrunn ,  Steven Demarco ,  Sergio Lociuro ,  Daniel Obrecht ,  Barbara Romagnoli ,  John Robinson

IPC分类号： A61K38/12 ,  C07K7/64

CPC分类号： C07K7/06 ,  C07K7/08 ,  C07K14/001

摘要： Template-fixed β-hairpin peptidomimetics of the General Formula (I); wherein Z1 and Z2 are template-fixed chains of 4 and 6 or 5 and 7 α-amino acid residues which, depending on their positions in the chain are Gly, or Pro, 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 prevent or to reduce HIV infections or to inhibit the growth of cancer cells or to inhibit inflammation. They can be used as medicaments to treat or prevent HIV infections and/or cancer or inflammatory disorders. These β-sheet peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

摘要翻译： 通式（I）的模板固定的β-发夹肽模拟物; 其中Z 1和Z 2是4和6或5和7个α-氨基酸残基的模板固定链，根据其在链中的位置是Gly， 或Pro，或某些类型，其作为上述公式中的其余符号在说明书和权利要求书及其盐中定义，具有预防或减少HIV感染或抑制癌细胞生长或 以抑制炎症。 它们可用作治疗或预防艾滋病毒感染和/或癌症或炎性疾病的药物。 这些β-折叠肽模拟物可以通过基于混合固相和溶液相合成策略的方法制造。