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1. 发明申请

WO2011060937A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CCR10 ANTAGONISTIC ACTIVTY 审中-公开
标题翻译：具有CCR10拮抗活性的模板固定化肽
公开(公告)号：WO2011060937A1
公开(公告)日：2011-05-26
申请号：PCT/EP2010/007016
申请日：2010-11-18
申请人： POLYPHOR AG , JUNG, Françoise , GOMBERT, Frank, Otto , OBRECHT, Daniel , BISANG, Christian , BARTHELEMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
发明人： JUNG, Françoise , GOMBERT, Frank, Otto , OBRECHT, Daniel , BISANG, Christian , BARTHELEMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
IPC分类号： C07K7/64 , C07K7/08 , A61K38/04
CPC分类号： A61K38/00 , C07K7/06 , C07K7/08 , C07K7/64
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to antagonize the receptor CCR10. They can be used as medicaments to treat or prevent diseases or conditions in the area of dermatological and cutaneous disorders, inflammation, allergic disorders, respiratory diseases, diseases of the gastro-intestinal tract, ophthalmic diseases, haematology and cancer. 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）的新型模板固定的β-发夹肽模拟物，其中单个元件T或P是沿任一方向连接的α-氨基酸残基，其取决于其在链中的位置如说明书中所定义，权利要求及其盐具有拮抗受体CCR10的性质。它们可用作治疗或预防皮肤病和皮肤病，炎症，过敏性疾病，呼吸系统疾病，胃肠道疾病，眼科疾病，血液学和癌症领域的疾病或病症的药物。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。

2. 发明申请

WO2011060832A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CCR10 ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有CCR10拮抗活性的模板固定肽
公开(公告)号：WO2011060832A1
公开(公告)日：2011-05-26
申请号：PCT/EP2009/065572
申请日：2009-11-20
申请人： POLYPHOR AG , JUNG, Françoise , GOMBERT, Frank Otto , OBRECHT, Daniel , BISANG, Christian , BARTHÉLÉMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
发明人： JUNG, Françoise , GOMBERT, Frank Otto , OBRECHT, Daniel , BISANG, Christian , BARTHÉLÉMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
IPC分类号： C07K7/64 , C07K7/08 , A61K38/04
CPC分类号： A61K38/00 , C07K7/06 , C07K7/08 , C07K7/64
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain are defined in the description and the claims, and salts thereof, have the property to antagonize the receptor CCR10. They can be used as medicaments to treat or prevent diseases or conditions in the area of dermatological and cutaneous disorders, inflammation, allergic disorders, respiratory diseases, diseases of the gastro-intestinal tract, ophthalmic 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.
摘要翻译：通式（I）的新型模板固定的β-发夹肽模拟物，其中单个元件T或P是沿任一方向连接的α-氨基酸残基，根据其在链中的位置在说明书和权利要求书中定义，及其盐具有拮抗受体CCR10的性质。它们可用作治疗或预防皮肤病和皮肤病，炎症，过敏性疾病，呼吸系统疾病，胃肠道疾病，眼科疾病，血液病和癌症等疾病或病症的药物。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。

3. 发明申请

WO2011066869A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
标题翻译： BETA-HAIRPIN PEPTIDMIMETICS
公开(公告)号：WO2011066869A1
公开(公告)日：2011-06-09
申请号：PCT/EP2009/066462
申请日：2009-12-04
申请人： POLYPHOR AG , BARTHÉLÉMY, Sophie , BISANG, Christian , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZUMBRUNN, Jürg , REMUS, Tobias , LEMERCIER, Guillaume
发明人： BARTHÉLÉMY, Sophie , BISANG, Christian , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZUMBRUNN, Jürg , REMUS, Tobias , LEMERCIER, Guillaume
IPC分类号： C07K7/64 , C07K1/04 , A61K38/00
CPC分类号： C07K7/08 , A61K38/00 , C07K7/64
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa 1 -Xaa 2 -Xaa 3 -Xaa 4 -Xaa 5 -Xaa 6 -Xaa 7 -Xaa 8 -Xaa 9 -Xaa 10 -Xaa 11 - Xaa 12 -Xaa 13 -Xaa 14 -Xaa 15 -Xaa 16 -), and pharmaceutically acceptable salts thereof, with Xaa 1 -Xaa 16 being amino acid residues of certain types which are defined in thedescription 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： ß-通式为Cyclo（-Xaa1 -Xaa2 -Xaa3 -Xaa4 -Xaa5 -Xaa6 -Xaa7 -Xaa8 -Xaa9 -Xaa10 -Xaa11 -Xaa12 -Xaa13 -Xaa14 -Xaa15 -Xaa16 - ）的发夹肽模拟物及其药学上可接受的盐，Xaa 1 -Xaa 16是在描述和权利要求书中定义的某些类型的氨基酸残基，具有CXCR4拮抗性质和体内延长的半衰期，并且可用于预防健康个体的HIV感染或减缓和停止感染患者病毒进展; 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制造。

4. 发明申请

WO2010127704A1 BETA-HAIRPIN PEPTIDOMIMETICS HAVING CXCR4 ANTAGONIZING ACTIVITY 审中-公开
标题翻译：具有CXCR4拮抗活性的BETA-HAIRPIN PEPTIDOMIMETICS
公开(公告)号：WO2010127704A1
公开(公告)日：2010-11-11
申请号：PCT/EP2009/055563
申请日：2009-05-07
申请人： POLYPHOR AG , OBRECHT, Daniel , GOMBERT, Frank, Otto , LEDERER, Alexander , ROMAGNOLI, Barbara , BISANG, Christian
发明人： OBRECHT, Daniel , GOMBERT, Frank, Otto , LEDERER, Alexander , ROMAGNOLI, Barbara , BISANG, Christian
IPC分类号： C07K7/08 , C07K7/02 , A61K38/10 , A61P29/00 , A61P31/18 , A61P35/00
CPC分类号： C07K7/08 , C07K1/061 , C07K7/02
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa 1 -Xaa 2 -Xaa 3 -Cys 4 -Xaa 5 -Xaa 6 -Xaa 7 -Xaa 8 -Arg 9 -Tyr 10 -Cys 11 - Xaa 12 -Xaa 13 -Xaa 14 -Xaa 15 -Xaa 16 -), disulfide bond between Cys 4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa 1 , Xaa 2 , Xaa 3 , Xaa 5 , Xaa 6 , Xaa 7 , Xaa 8 , Xaa 12 , Xaa 13 , Xaa 14 , Xaa 15 and Xaa 16 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： ß-通式为（Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的发夹肽模拟物，Cys4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拮抗性，可用于预防健康个体的艾滋病毒感染，或用于缓解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和/或作为诱导干细胞动员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。

5. 发明申请

WO2011095220A1 TEMPLATE - FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 审中-公开
标题翻译：模板 - 具有CXCR7调节活性的固定肽
公开(公告)号：WO2011095220A1
公开(公告)日：2011-08-11
申请号：PCT/EP2010/051440
申请日：2010-02-05
申请人： POLYPHOR AG , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , BISANG, Christian , LUDIN, Christian
发明人： GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , BISANG, Christian , LUDIN, Christian
IPC分类号： A61K38/12 , C07K7/64 , C07K14/72
CPC分类号： C07K7/64 , A61K38/00
摘要： Specific template-fixed β- hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C=O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.
摘要翻译：通式（I）的具体的模板固定的β-发夹肽模拟物，其中单个元件T或P是从连接的羰基（C = O）连接到下一元素的氮（N）连接的α-氨基酸残基顺时针方向，并且其中所述元件取决于它们在链中的位置在描述中定义，并且权利要求具有作用于受体CXCR7的性质。因此，这些β-发夹肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经疾病，心血管疾病，呼吸系统疾病，胃肠道疾病或疾病泌尿系疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。

6. 发明申请

WO2010015287A2 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定的多形性
公开(公告)号：WO2010015287A2
公开(公告)日：2010-02-11
申请号：PCT/EP2008/060494
申请日：2008-08-08
申请人： POLYPHOR AG , UNIVERSITÄT ZÜRICH , ROBINSON, John Anthony , MÖHLE, Kerstin , SEITZ, Markus , MAILLARD, Ludovic T. , MOUNME, Roba , GOMBERT, Frank Otto , SELLIER-KESSLER, Odile , HENZE, Heiko , OBRECHT, Daniel , BISANG, Christian , LEDERER, Alexander
发明人： ROBINSON, John Anthony , MÖHLE, Kerstin , SEITZ, Markus , MAILLARD, Ludovic T. , MOUNME, Roba , GOMBERT, Frank Otto , SELLIER-KESSLER, Odile , HENZE, Heiko , OBRECHT, Daniel , BISANG, Christian , LEDERER, Alexander
CPC分类号： C07K1/02 , C07K7/56 , C07K7/64
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 8 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are GIy 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 agonizing or antagonizing activity against urotensin II or show inhibition of the STAT6/NCoA-1 interaction and can be used for preventing or treating diseases or disorders related to urotensin II, STAT6 and NCoA-1. 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8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）是Gly或Pro或某些类型的化合物，作为上式中剩余的符号，如说明书和权利要求书中所定义的，及其盐具有对抗尾加压素II的激动或拮抗活性或显示抑制STAT6 / NCoA-1相互作用，并可用于预防或治疗与尾加压素II，STAT6和NCoA-1相关的疾病或病症。这些β-发夹肽模拟物可以通过基于混合固相和液相合成策略的方法来制造。

7. 发明申请

WO2013182240A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2013182240A1
公开(公告)日：2013-12-12
申请号：PCT/EP2012/060766
申请日：2012-06-06
申请人： POLYPHOR AG , GOMBERT, Frank Otto , OBRECHT, Daniel , LEDERER, Alexander , ZIMMERMANN, Johann , OEFNER, Christian
发明人： GOMBERT, Frank Otto , OBRECHT, Daniel , LEDERER, Alexander , ZIMMERMANN, Johann , OEFNER, Christian
IPC分类号： C07K7/64
CPC分类号： A61K38/12 , A61K38/00 , C07K7/08 , C07K7/54
摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr 1 -His 2 -Xaa 3 -Cys 4 -Ser 5 -Xaa 6 -DPro 7 -Xaa 8 -Arg 9 -Tyr 10 -Cys 11 -Tyr 12 -Xaa 13 -Xaa 14 -Xaa 15 -Pro 16 -), disulfide bond between Cys 4 and Cys 11 , and pharmaceutically acceptable salts thereof, with Xaa 3 , Xaa 6 , Xaa 8 , Xaa 13 , Xaa 14 and Xaa 15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological 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 peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.
摘要翻译：通式为（-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-）的β-发夹肽模拟物，Cys4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Xaa3，Xaa6，Xaa8，Xaa13，Xaa14和Xaa15具有有利的药理学性质并可用于预防HIV感染健康个体或减慢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和/或作为诱导干细胞动员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。

8. 发明申请

WO2011095218A1 TEMPLATE-FIXED PEP TIDOMIME TICS WITH CXCR7 MODULATING ACTIVITY 审中-公开
标题翻译：模板固定PEP TIDOMIME TICS与CXCR7调节活动
公开(公告)号：WO2011095218A1
公开(公告)日：2011-08-11
申请号：PCT/EP2010/051417
申请日：2010-02-05
申请人： POLYPHOR AG , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , LÖWE, Ralf , ZIMMERMANN, Johann
发明人： GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , LÖWE, Ralf , ZIMMERMANN, Johann
IPC分类号： C07K7/64
CPC分类号： C07K7/64 , A61K38/00 , A61K38/17 , A61K38/177 , A61K38/1793 , C07K14/705 , C07K14/715 , C07K14/7158
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C=O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.
摘要翻译：通式（I）的新型模板固定β-发夹肽模拟物，其中单个元件T或P是从连接的羰基（C = O）连接到下一个元素的氮（N）连接的α-氨基酸残基顺时针方向，并且其中所述元件取决于它们在链中的位置在说明书中定义，并且权利要求书具有作用于受体CXCR7的性质。因此，这些β-发夹肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经系统疾病，心血管疾病，呼吸系统疾病，胃肠道疾病或疾病泌尿系疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。

9. 发明申请

WO2011095607A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 审中-公开
标题翻译：具有CXCR7调节活性的模板固定化肽
公开(公告)号：WO2011095607A1
公开(公告)日：2011-08-11
申请号：PCT/EP2011/051686
申请日：2011-02-04
申请人： POLYPHOR AG , GOMBERT, Frank, Otto , LEDERER, Alexander , LÖWE, Ralf , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZIMMERMANN, Johann , PATEL, Kalpana
发明人： GOMBERT, Frank, Otto , LEDERER, Alexander , LÖWE, Ralf , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZIMMERMANN, Johann , PATEL, Kalpana
IPC分类号： C07K7/64
CPC分类号： C07K7/64 , A61K38/00 , A61K38/17 , A61K38/177 , A61K38/1793 , C07K14/705 , C07K14/715 , C07K14/7158
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C=O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilisation of stem cells.
摘要翻译：通式（I）的新型模板固定的β-发夹肽模拟物，其中单个元件T或P是从下述的羰基（C = O）连接点连接到氮（N）的α-氨基酸残基元件，并且其中所述元件取决于它们在链中的位置在描述中定义，并且权利要求具有作用于受体CXCR7的性质。因此，这些β-发夹肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经疾病，心血管疾病，呼吸系统疾病，胃肠道疾病或疾病泌尿系疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。

10. 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。

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