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公开(公告)号：US09556234B2
公开(公告)日：2017-01-31
申请号：US14555796
申请日：2014-11-28
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 B-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-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 where cancer is mediated or resulting from CXCR4 receptor activity.
摘要翻译： 模板固定的B发夹肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro），Cys4 和Gys11及其药学上可接受的盐，其中X为Ala或Tyr，具有CXCR4拮抗性质，可用于癌症介导或由CXCR4受体活性产生的地方。
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公开(公告)号：US10787486B2
公开(公告)日：2020-09-29
申请号：US16190459
申请日：2018-11-14
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 where cancer is mediated or resulting from CXCR4 receptor activity.
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公开(公告)号：US08921325B2
公开(公告)日：2014-12-30
申请号：US13764099
申请日：2013-02-11
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 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。
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公开(公告)号：US10730912B2
公开(公告)日：2020-08-04
申请号：US15392586
申请日：2016-12-28
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：US10144765B2
公开(公告)日：2018-12-04
申请号：US15851270
申请日：2017-12-21
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-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gysl1, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.
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公开(公告)号：US09538752B2
公开(公告)日：2017-01-10
申请号：US14175160
申请日：2014-02-07
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：US11421001B2
公开(公告)日：2022-08-23
申请号：US17013111
申请日：2020-09-04
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 where cancer is mediated or resulting from CXCR4 receptor activity.
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公开(公告)号：US20180127467A1
公开(公告)日：2018-05-10
申请号：US15851270
申请日：2017-12-21
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-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gysl1, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity
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公开(公告)号：US09879047B2
公开(公告)日：2018-01-30
申请号：US15379820
申请日：2016-12-15
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-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-D-Pro-Pro), disulfide bond between Cys4 and Gysl1, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for where cancer is mediated or resulting from CXCR4 receptor activity.
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公开(公告)号：US09596852B2
公开(公告)日：2017-03-21
申请号：US14175193
申请日：2014-02-07
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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