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11. 发明申请

WO2006117011A1 DYE CONJUGATES OF TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定肽的DYE结合
公开(公告)号：WO2006117011A1
公开(公告)日：2006-11-09
申请号：PCT/EP2005/004751
申请日：2005-05-02
申请人： POLYPHOR Ltd. , UNIVERSITÄT ZÜRICH , DE MARCO, Steven, J. , GOMBERT, Frank , OBRECHT, Daniel , LUDIN, Christian , ROMAGNOLI, Barbara
发明人： DE MARCO, Steven, J. , GOMBERT, Frank , OBRECHT, Daniel , LUDIN, Christian , ROMAGNOLI, Barbara
IPC分类号： C07K7/64 , A61K38/04 , G01N33/68
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 abnormalties; 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）的模板固定的β-发夹肽模拟物的染料缀合物，其中Z是14个氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基开始计数酸）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及其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。 β-发夹肽模拟物的这些染料缀合物可以通过基于混合固相和溶液相合成策略的方法制备。

12. 发明申请

WO2006087001A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH PROTEASE INHIBITORY ACTIVITY 审中-公开
标题翻译：具有蛋白酶抑制活性的模板固定的BETA-HAIRPIN PEPTIDOMIMETICS
公开(公告)号：WO2006087001A1
公开(公告)日：2006-08-24
申请号：PCT/EP2005/001622
申请日：2005-02-17
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , DEMARCO, Steven, J. , MOEHLE, Kerstin , HENZE, Heiko , SELLIER, Odile , JUNG, Françoise , GOMBERT, Frank , OBRECHT, Daniel , LUDIN, Christian
发明人： DEMARCO, Steven, J. , MOEHLE, Kerstin , HENZE, Heiko , SELLIER, Odile , JUNG, Françoise , GOMBERT, Frank , OBRECHT, Daniel , LUDIN, Christian
IPC分类号： C07K7/06 , C07K7/08 , C07K7/64 , A61K38/04
CPC分类号： C07K7/06 , A61K38/00 , C07K1/061 , C07K7/08 , C07K7/64
摘要： Templates-fixed β-hairpin peptidomimetics of the general formulae (I), wherein Z is a chain of 11 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 Pro(4NHCOPhe), 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 inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. 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：模板固定的通式（I）的β-发夹肽模拟物，其中Z是11个α-氨基酸残基的链，其取决于其在链中的位置（从N-末端氨基酸开始计数）为Gly，或Pro或Pro（4NHCOPhe），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，并且具有抑制蛋白酶特别是丝氨酸蛋白酶的性质，特别是丝氨酸蛋白酶组织蛋白酶G或弹性蛋白酶或类胰蛋白酶。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造。

13. 发明申请

WO2004033489A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY 审中-公开
标题翻译：具有抗微生物活性的模板固定肽
公开(公告)号：WO2004033489A1
公开(公告)日：2004-04-22
申请号：PCT/EP2002/011048
申请日：2002-10-02
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , VRIJBLOED, Jan, Wim , OBRECHT, Daniel , LOCURIO, Sergio , GOMBERT, Frank , LUDIN, Christian , ROBINSON, John, Anthony , LEDERER, Alexander , SHANKARAMMA, Shivaprasad
发明人： VRIJBLOED, Jan, Wim , OBRECHT, Daniel , LOCURIO, Sergio , GOMBERT, Frank , LUDIN, Christian , ROBINSON, John, Anthony , LEDERER, Alexander , SHANKARAMMA, Shivaprasad
IPC分类号： C07K7/64
CPC分类号： C07K7/64 , A61K38/00
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, at least one of these residues being of the type of N-substituted glycines, which types, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit the growth of or to kill microorganisms. 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）的模板固定的β-发夹肽模拟物，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，这些残基中的至少一种是N-取代的甘氨酸类型，其类型作为上述式中的其余符号在说明书和权利要求书中定义，以及其盐具有抑制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。

14. 发明授权

US10787486B2 Template-fixed peptidomimetics 有权
公开(公告)号：US10787486B2
公开(公告)日：2020-09-29
申请号：US16190459
申请日：2018-11-14
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 , C07K7/64 , C07K7/56 , A61K38/00
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.

15. 发明申请

US20170107259A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY 审中-公开
公开(公告)号：US20170107259A1
公开(公告)日：2017-04-20
申请号：US15392586
申请日：2016-12-28
申请人： POLYPHOR LTD. , UNIVERSITAET ZUERICH
发明人： Steven J. DEMARCO , Wim VRIJBLOED , Ricardo DIAS , John Anthony ROBINSON , Nityakalyani SRINIVAS , Frank GOMBERT , Daniel OBRECHT
IPC分类号： C07K7/64
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.

16. 发明授权

US08921325B2 Template-fixed peptidomimetics 有权
标题翻译：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。

17. 发明授权

US10000535B2 Template-fixed peptidomimetics 有权
公开(公告)号：US10000535B2
公开(公告)日：2018-06-19
申请号：US14134566
申请日：2013-12-19
申请人： POLYPHOR LTD.
发明人： Daniel Obrecht , Frank Gombert , Steve J. DeMarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
IPC分类号： A61K38/00 , A61P7/00 , A61P9/00 , A61K38/12 , A61P35/00 , C07K14/72 , C07K14/705 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K7/64 , C07K5/103 , C07K5/107 , C07K5/113 , C07K5/117 , C07K7/06 , C07K7/08 , 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.

18. 发明申请

US20170096453A1 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
公开(公告)号：US20170096453A1
公开(公告)日：2017-04-06
申请号：US15379820
申请日：2016-12-15
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： 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-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

19. 发明授权

US09556234B2 Template-fixed peptidomimetics 有权
标题翻译：模板固定肽模拟物
公开(公告)号：US09556234B2
公开(公告)日：2017-01-31
申请号：US14555796
申请日：2014-11-28
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： C07K7/56 , C07K7/64 , A61K38/12
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , C07K7/64
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。

20. 发明授权

US10562933B2 Template-fixed beta-hairpin peptidomimetics with protease inhibitory activity 有权
公开(公告)号：US10562933B2
公开(公告)日：2020-02-18
申请号：US16130520
申请日：2018-09-13
申请人： POLYPHOR LTD. , UNIVERSITAT ZURICH
发明人： Steven J. Demarco , Kerstin Moehle , Heiko Henze , Odile Sellier , Francoise Jung , Frank Gombert , Daniel Obrecht , Christian Ludin
IPC分类号： A61K38/12 , C07K7/06 , C07K7/08 , C07K7/64 , C07K1/06 , A61K38/00
摘要： Template-fixed β-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 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 Pro(4NHCOPhe), 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 inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. 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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