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公开(公告)号：US08685922B2
公开(公告)日：2014-04-01
申请号：US12161065
申请日：2007-01-15
申请人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and Solution phase synthetic strategy.
摘要翻译： 通式（I）的模板固定和半乳糖肽模拟物，其中Z是12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-末端氨基酸开始计数） 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，以及其盐具有选择性抑制微生物生长或杀死诸如假单胞菌 铜绿假单胞菌 它们可以用作食品，化妆品，药物或其他含营养材料的消毒剂，或用作治疗或预防感染的药物。 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。
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公开(公告)号：US20140187471A1
公开(公告)日：2014-07-03
申请号：US14175160
申请日：2014-02-07
申请人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections.These β-hairpin peptidomimetics can be manufactured by processes which are 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12个α-氨基酸残基的模板固定链，取决于它们在链中的位置（从N-末端氨基酸开始计数）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及其盐中定义，具有选择性抑制绿脓假单胞菌等微生物生长或杀死微生物的性质。 它们可以用作食品，化妆品，药物或其他含营养材料的消毒剂，或用作治疗或预防感染的药物。 这些和平滑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：US09521846B2
公开(公告)日：2016-12-20
申请号：US14074251
申请日：2013-11-07
申请人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
摘要翻译： 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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公开(公告)号：US20140187472A1
公开(公告)日：2014-07-03
申请号：US14175193
申请日：2014-02-07
申请人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections.These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
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公开(公告)号：US20140087994A1
公开(公告)日：2014-03-27
申请号：US14074251
申请日：2013-11-07
申请人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
IPC分类号： C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections.These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
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公开(公告)号：US20100240592A1
公开(公告)日：2010-09-23
申请号：US12161065
申请日：2007-01-15
申请人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyana Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyana Srinivas , Frank Gombert , Daniel Obrecht
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and Solution phase synthetic strategy.
摘要翻译： 通式（I）的模板固定和半乳糖肽模拟物，其中Z是12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-末端氨基酸开始计数） 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，以及其盐具有选择性抑制微生物生长或杀死诸如假单胞菌 铜绿假单胞菌 它们可以用作食品，化妆品，药物或其他含营养材料的消毒剂，或用作治疗或预防感染的药物。 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。
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7.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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8.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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9.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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公开(公告)号：US08399611B2
公开(公告)日：2013-03-19
申请号：US12528926
申请日：2007-02-28
申请人： Daniel Obrecht , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
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
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 Cys11, 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 for treating inflammation, 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.
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 Cys11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; 或用于治疗炎症，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。
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