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1. 发明申请

WO2005047503A1 TEMPLATE FIXED ΒΕΤΑ-HAIRPIN LOOP MIMETICS AND THEIR USE IN PHAGE DISPLAY 审中-公开
标题翻译：模板固定的BetaEpsilonTauAlpha-HAIRPIN环状物质及其在PHAGE显示中的使用
公开(公告)号：WO2005047503A1
公开(公告)日：2005-05-26
申请号：PCT/EP2003/012783
申请日：2003-11-15
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , VRIJBLOED, Jan, Wim , OBRECHT, Daniel , LOCURIO, Sergio , GOMBERT, Frank, Otto , LUDIN, Christian , JUNG, Françoise
发明人： VRIJBLOED, Jan, Wim , OBRECHT, Daniel , LOCURIO, Sergio , GOMBERT, Frank, Otto , LUDIN, Christian , JUNG, Françoise
IPC分类号： C12N15/10
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02
摘要： Template-fixed β-hairpin mimetics of the general formula R 1 -Cys-Z-Cys-R 2 (I) wherein the two Cys residues are bridged by a disulfide bond thereby forming a cyclic peptide; R l and R 2 are preferably Glu-Thr and Thr-Lys; or Lys-Thr and Thr-Glu; or Thr-Glu and Lys-Thr; or Thr-Lys and Glu-Thr; or Leu-Glu and Lys-Val; or Val-Lys and Glu-Leu; or Glu-Leu and Val-Lys; or Lys-Leu and Val-Glu; or Asn-Gly and Lys-Val; or Val-Gly and Lys-Asn; or Gly-Asn and Val-Lys; or Gly-Val and Asn-Lys; or Gly-Gly and Gly-Gly; or Glu-Leu-Lys and Glu-Val-Lys; or Lys-Val-Glu and Lys-Leu-Glu; or Leu-Glu-Lys and Glu-Lys-Val; or Val-Lys-Glu and Lys-Glu-Leu; or Glu-Lys-Leu and Val-Glu-Lys; or Lys-Glu-Val and Leu-Lys-Glu; or Lys-Glu-Leu and Val-Lys-Glu; or Glu-Lys-Val and Leu-Glu-Lys; or Lys-Val-Gly and Gly-Leu-Glu; or Glu-Leu-Gly and Gly-Val-Lys; or Val-Lys-Gly and Gly-Glu-Leu; or Leu-Glu-Gly and Gly-Lys-Val; or Val-Gly-Lys and Glu-Gly-Leu; or Leu-Gly-Glu and Lys-Gly-Val; or Gly-Gly-Gly and Gly-Gly-Gly; and Z is a chain of n amino acid residues with n being an integer form 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L- α-amino acid are provided. Libraries comprising a plurality of these templates can be used for the construction of phage display derived template-fixed β-hairpin mimetics generating phage display libraries with very high binding constants to targets, thus combining the advantage of screening of large phage display derived template-fixed β-hairpin libraries which in turn considerably facilitates structure-activity studies, and hence the discovery of new molecules with potent activities and with novel selectivities towards different types of targets.
摘要翻译：通式R 1 -Cys-Z-Cys-R 2（I）的模板固定的β-发夹模拟物，其中两个Cys残基被二硫键桥接，从而形成环肽; R 1和R 2优选为Glu-Thr和Thr-Lys; 或Lys-Thr和Thr-Glu; 或Thr-Glu和Lys-Thr; 或Thr-Lys和Glu-Thr; 或Leu-Glu和Lys-Val; 或Val-Lys和Glu-Leu; 或Glu-Leu和Val-Lys; 或Lys-Leu和Val-Glu; 或Asn-Gly和Lys-Val; 或Val-Gly和Lys-Asn; 或Gly-Asn和Val-Lys; 或Gly-Val和Asn-Lys; 或Gly-Gly和Gly-Gly; 或Glu-Leu-Lys和Glu-Val-Lys; 或Lys-Val-Glu和Lys-Leu-Glu; 或Leu-Glu-Lys和Glu-Lys-Val; 或Val-Lys-Glu和Lys-Glu-Leu; 或Glu-Lys-Leu和Val-Glu-Lys; 或Lys-Glu-Val和Leu-Lys-Glu; 或Lys-Glu-Leu和Val-Lys-Glu; 或Glu-Lys-Val和Leu-Glu-Lys; 或Lys-Val-Gly和Gly-Leu-Glu; 或Glu-Leu-Gly和Gly-Val-Lys; 或Val-Lys-Gly和Gly-Glu-Leu; 或Leu-Glu-Gly和Gly-Lys-Val; 或Val-Gly-Lys和Glu-Gly-Leu; 或Leu-Gly-Glu和Lys-Gly-Val; 或Gly-Gly-Gly和Gly-Gly-Gly; 并且Z是n个氨基酸残基的链，其中n是4至20的整数，并且这些n个氨基酸残基中的每一个独立地衍生自任何天然存在的L-α-氨基酸。包含多个这些模板的文库可用于构建噬菌体展示衍生的模板固定的β-发夹模拟物，其产生具有非常高的结合常数的靶标的噬菌体展示文库，因此结合筛选大噬菌体展示衍生模板固定的优点 β-发夹文库反过来极大地促进结构活性研究，从而发现具有有效活性和对不同类型靶标具有新选择性的新分子。

2. 发明申请

WO2008104090A1 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定蛋白质
公开(公告)号：WO2008104090A1
公开(公告)日：2008-09-04
申请号：PCT/CH2007/000101
申请日：2007-02-28
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , DEMARCO, Steven, J. , MUKHERJEE, Reshmi , MOEHLE, Kerstin , ROBINSON, John, Anthony , HENZE, Heiko , ROMAGNOLI, Barbara , OBRECHT, Daniel , GOMBERT, Frank , LUDIN, Christian , VRIJBLOED, Jan, Wim
发明人： DEMARCO, Steven, J. , MUKHERJEE, Reshmi , MOEHLE, Kerstin , ROBINSON, John, Anthony , HENZE, Heiko , ROMAGNOLI, Barbara , OBRECHT, Daniel , GOMBERT, Frank , LUDIN, Christian , VRIJBLOED, Jan, Wim
IPC分类号： C07K7/56 , A61K38/12
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , C07K7/64
摘要： The template-fixed ß-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala- D Pro- 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 preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where Cancer is mediated or resulting fromCXCR4 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 mobilisation 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：模板固定的β-发夹肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-Pro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys- D Pro Pro），Cys4和Gys11之间的二硫键及其药学上可接受的盐，X为Ala或Tyr，具有CXCR4拮抗特性，可用于预防健康个体的HIV感染或减缓和停止感染患者病毒进展; 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动员外周血干细胞和/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β-发夹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，使用肽化学中熟练的人所熟知的方法制备。

3. 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。

4. 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。

5. 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。

6. 发明公开

EP1689863A1 TEMPLATE FIXED BETA-HAIRPIN LOOP MIMETICS AND THEIR USE IN PHAGE DISPLAY 有权
标题翻译：模具固定BETA-HAIRPINLOOPMIMETIKA及其使用噬菌体展示
公开(公告)号：EP1689863A1
公开(公告)日：2006-08-16
申请号：EP03779935.0
申请日：2003-11-15
申请人： Polyphor Ltd. , Universität Zürich
发明人： VRIJBLOED, Jan, Wim , OBRECHT, Daniel , LOCURIO, Sergio , GOMBERT, Frank, Otto , LUDIN, Christian , JUNG, Françoise
IPC分类号： C12N15/10 , C07K7/04
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02
摘要： Template-fixed β-hairpin mimetics of the general formula R1-Cys-Z-Cys-R2 (I) wherein the two Cys residues are bridged by a disulfide bond thereby forming a cyclic peptide; Rl and R2 are preferably Glu-Thr and Thr-Lys; or Lys-Thr and Thr-Glu; or Thr-Glu and Lys-Thr; or Thr-Lys and Glu-Thr; or Leu-Glu and Lys-Val; or Val-Lys and Glu-Leu; or Glu-Leu and Val-Lys; or Lys-Leu and Val-Glu; or Asn-Gly and Lys-Val; or Val-Gly and Lys-Asn; or Gly-Asn and Val-Lys; or Gly-Val and Asn-Lys; or Gly-Gly and Gly-Gly; or Glu-Leu-Lys and Glu-Val-Lys; or Lys-Val-Glu and Lys-Leu-Glu; or Leu-Glu-Lys and Glu-Lys-Val; or Val-Lys-Glu and Lys-Glu-Leu; or Glu-Lys-Leu and Val-Glu-Lys; or Lys-Glu-Val and Leu-Lys-Glu; or Lys-Glu-Leu and Val-Lys-Glu; or Glu-Lys-Val and Leu-Glu-Lys; or Lys-Val-Gly and Gly-Leu-Glu; or Glu-Leu-Gly and Gly-Val-Lys; or Val-Lys-Gly and Gly-Glu-Leu; or Leu-Glu-Gly and Gly-Lys-Val; or Val-Gly-Lys and Glu-Gly-Leu; or Leu-Gly-Glu and Lys-Gly-Val; or Gly-Gly-Gly and Gly-Gly-Gly; and Z is a chain of n amino acid residues with n being an integer form 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L- α-amino acid are provided. Libraries comprising a plurality of these templates can be used for the construction of phage display derived template-fixed β-hairpin mimetics generating phage display libraries with very high binding constants to targets, thus combining the advantage of screening of large phage display derived template-fixed β-hairpin libraries which in turn considerably facilitates structure-activity studies, and hence the discovery of new molecules with potent activities and with novel selectivities towards different types of targets.

7. 发明授权

EP1879911B1 DYE CONJUGATES OF TEMPLATE-FIXED PEPTIDOMIMETICS 失效
标题翻译：面具固定肽染料结合物
公开(公告)号：EP1879911B1
公开(公告)日：2011-08-17
申请号：EP05739422.3
申请日：2005-05-02
申请人： Polyphor Ltd. , Universität Zürich
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.

8. 发明公开

EP1879911A1 DYE CONJUGATES OF TEMPLATE-FIXED PEPTIDOMIMETICS 失效
标题翻译：面具固定肽染料结合物
公开(公告)号：EP1879911A1
公开(公告)日：2008-01-23
申请号：EP05739422.3
申请日：2005-05-02
申请人： Polyphor Ltd. , Universität Zürich
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.

9. 发明公开

EP1856140A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH PROTEASE INHIBITORY ACTIVITY 有权转让
标题翻译：蛋白酶抑制效果MATRIX固定BETA发夹肽
公开(公告)号：EP1856140A1
公开(公告)日：2007-11-21
申请号：EP05707463.5
申请日：2005-02-17
申请人： Polyphor Ltd. , Universität Zürich
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.

10. 发明授权

EP1689863B1 TEMPLATE FIXED BETA-HAIRPIN LOOP MIMETICS AND THEIR USE IN PHAGE DISPLAY 有权
标题翻译：模具固定BETA-HAIRPINLOOPMIMETIKA及其使用噬菌体展示
公开(公告)号：EP1689863B1
公开(公告)日：2014-05-28
申请号：EP03779935.0
申请日：2003-11-15
申请人： Polyphor Ltd. , Universität Zürich
发明人： VRIJBLOED, Jan, Wim , OBRECHT, Daniel , LOCURIO, Sergio , GOMBERT, Frank, Otto , LUDIN, Christian , JUNG, Françoise
IPC分类号： C12N15/10 , C07K7/04
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02

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