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1.发明申请公开(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
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。
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2.发明申请Template-fixed beta-hairpin peptidomimetics with cxcr4 antagonizing activity 有权具有cxcr4拮抗活性的模板固定β-发夹肽模拟物公开(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
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。
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3.发明授权Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity 有权模板固定β-发夹肽模拟物与CXCR4拮抗活性公开(公告)号：US08895695B2
公开(公告)日：2014-11-25
申请号：US12828998
申请日：2010-07-01
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
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. 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）的模板固定和半乳糖肽模拟物，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盐中定义，具有CXCR4拮抗性质。 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。
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4.发明授权公开(公告)号：US07838496B2
公开(公告)日：2010-11-23
申请号：US10550778
申请日：2003-05-02
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , Barbara Romagnoli , John Anthony Robinson
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , Barbara Romagnoli , John Anthony Robinson
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 and salts thereof. They have CXCR4-antagonizing properties and can be used as medicaments. 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）的模板固定和模板肽模拟物; 其中Z1和Z2是4和6或5和7个α-氨基酸残基及其盐的模板固定链。 它们具有CXCR4拮抗特性，可用作药物。 这些胶体蛋白模拟物可以通过基于混合固相和溶液相合成策略的方法来制造。
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5.发明申请TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 有权具有CXCR4拮抗活性的模板固定的BETA-HAIRPIN PEPTIDOMIMETICS公开(公告)号：US20110245155A1
公开(公告)日：2011-10-06
申请号：US12828998
申请日：2010-07-01
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
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）的模板固定和半乳糖肽模拟物，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拮抗性质并且可以使用 用于预防健康个体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。 这些可以通过基于混合固相和溶液相合成策略的方法制造。
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6.发明授权Template-fixed δ-hairpin peptidomimetics with CXCR4 antagonizing activity 有权具有CXCR4拮抗活性的模板固定的δ-发夹肽模拟物公开(公告)号：US07786078B2
公开(公告)日：2010-08-31
申请号：US10555088
申请日：2004-04-29
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
IPC分类号： A61K38/12
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. 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）的模板固定和半乳糖肽模拟物，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盐中定义，具有CXCR4拮抗性质。 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。
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公开(公告)号：US08865656B2
公开(公告)日：2014-10-21
申请号：US13319052
申请日：2009-05-07
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa1, Xaa2, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa12, Xaa13, Xaa14, Xaa15 and Xaa16 being amino acid residues of certain types which are defined in the description and the claims, 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 immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptides can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 通式为（Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物，Cys4之间的二硫键 和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa1，Xaa2，Xaa3，Xaa5，Xaa6，Xaa7，Xaa8，Xaa12，Xaa13，Xaa14，Xaa15和Xaa16， 具有CXCR4拮抗特性，可用于预防健康个体中的HIV感染，或用于减缓和阻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和/或作为诱导干细胞动员以调节组织修复的试剂。 这些肽可以通过基于混合固相和溶液相合成策略的方法制造。
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公开(公告)号：US08716242B2
公开(公告)日：2014-05-06
申请号：US13513550
申请日：2009-12-04
申请人： Sophie Barthélémy , Christian Bisang , Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Jürg Zumbrunn , Tobias Remus , Guillaume Lemercier
发明人： Sophie Barthélémy , Christian Bisang , Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Jürg Zumbrunn , Tobias Remus , Guillaume Lemercier
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), and pharmaceutically acceptable salts thereof, with Xaa 1-Xaa 16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing properties and prolonged half-lives in vivo 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 immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： （-Xaa1-Xaa2-Xaa3-Xaa4-Xaa8-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物及其药学上可接受的盐 其中Xaa 1-Xaa 16是在说明书和权利要求书中定义的某些类型的氨基酸残基，具有CXCR4拮抗特性和体内延长的半衰期，并且可用于预防健康个体的HIV感染或减缓 并阻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和/或作为诱导干细胞动员以调节组织修复的试剂。 这些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。
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公开(公告)号：US20120283196A1
公开(公告)日：2012-11-08
申请号：US13513550
申请日：2009-12-04
申请人： Sophie Barthélémy , Christian Bisang , Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Jürg Zumbrunn , Tobias Remus , Guillaume Lemercier
发明人： Sophie Barthélémy , Christian Bisang , Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Jürg Zumbrunn , Tobias Remus , Guillaume Lemercier
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), and pharmaceutically acceptable salts thereof, with Xaa 1-Xaa 16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing properties and prolonged half-lives in vivo 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 immunosuppression; or during apheresis collections eases of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.
摘要翻译： （-Xaa1-Xaa2-Xaa3-Xaa4-Xaa8-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物及其药学上可接受的盐 其中Xaa 1-Xaa 16是在说明书和权利要求书中定义的某些类型的氨基酸残基，具有CXCR4拮抗特性和体内延长的半衰期，并且可用于预防健康个体的HIV感染或减缓 并阻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; 或在血浆分离术收集期间减少外周血干细胞和/或作为诱导干细胞调动以调节组织修复的试剂。 这些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来制造。
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公开(公告)号：US09073973B2
公开(公告)日：2015-07-07
申请号：US11913511
申请日：2005-05-02
CPC分类号： C07K7/64 , A61K38/4886
摘要： Dye conjugates of template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 14 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), 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 CXCR4 antagonizing properties, and are useful for cancer therapy; diagnostic imaging; for detection of tumors and other abnormalities; for photoacoustic tumor imaging, detection and therapy; and for sonofluorescence tumor imaging, detection and therapy. The various dyes forming part of these conjugates are useful over the range of 300-1200 nm, the exact range being dependent upon the particular dye. These dye conjugates of β-hairpin peptidomimetic can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 通式（I）的模板固定和平滑肽模拟物的染料缀合物，其中Z是14个α-氨基酸残基的模板固定链，这取决于它们在链中的位置（从N-末端计数 氨基酸）是Gly或Pro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中定义，及其盐具有CXCR4拮抗性质，并且可用于癌症治疗; 诊断成像; 用于检测肿瘤等异常; 用于光声肿瘤成像，检测和治疗; 并用于超声荧光肿瘤成像，检测和治疗。 形成这些共轭物的一部分的各种染料在300-1200nm的范围内是有用的，确切的范围取决于特定的染料。 这些染色偶联物，可以通过基于混合固相和溶液相合成策略的方法制造。
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