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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

WO2004018503A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIBACTERIAL ACTIVITY 审中-公开
标题翻译：具有抗菌活性的模板固定化肽酶
公开(公告)号：WO2004018503A1
公开(公告)日：2004-03-04
申请号：PCT/EP2002/009278
申请日：2002-08-20
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , VRIJBLOED, Jan, Wim , OBRECHT, Daniel , ROBINSON, John, Anthony , SELLIER, Odile , KESSLER, Marc
发明人： VRIJBLOED, Jan, Wim , OBRECHT, Daniel , ROBINSON, John, Anthony , SELLIER, Odile , KESSLER, Marc
IPC分类号： C07K7/64
CPC分类号： C07K5/06165 , A61K38/00 , C07K1/047 , C07K7/64 , Y02A50/473
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 and Acinetobacter. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. In a specific embodiment, the template is based on the D-Pro-L-Pro dipeptide. 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，其作为上述式中的其余符号在说明书和权利要求及其盐中定义，并且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和不动杆菌。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。在具体实施方案中，模板基于D-Pro-L-Pro二肽。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

WO02070547A8 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：WO02070547A8
公开(公告)日：2003-10-30
申请号：PCT/EP0201711
申请日：2002-02-18
申请人： POLYPHOR LTD , UNIV ZUERICH , OBRECHT DANIEL , ROBINSON JOHN ANTHONY , VRIJBLOED JAN WIM
发明人： OBRECHT DANIEL , ROBINSON JOHN ANTHONY , VRIJBLOED JAN WIM
IPC分类号： A23L3/3544 , A61K38/00 , A61K38/08 , A61K38/10 , A61P31/00 , A61P35/00 , C07K1/04 , C07K1/06 , C07K1/10 , C07K7/06 , C07K7/08 , C07K7/64 , C07K14/00
CPC分类号： C07K7/06 , A61K38/00 , C07K1/047 , C07K7/08
摘要： Template-fixed beta -hairpin peptidomimetics of the general formulae (I) and (II) wherein Z, Z1 and Z2 are template-fixed chains of 8 to 16 alpha -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 formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit the growth of or to kill microorganisms and cancer cells. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials or as medicaments to treat or prevent infections or diseases related to such infections and/or cancer. These beta -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）和（II）的模板固定β-螺旋肽模拟物，其中Z，Z1和Z2是8至16个α-氨基酸残基的模板固定链，这取决于它们在链中的位置（计数开始来自N-末端氨基酸）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中定义，及其盐具有抑制生长的性质或杀死微生物和癌细胞。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，或用作治疗或预防与这种感染和/或癌症有关的感染或疾病的药物。这些β-螺旋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。

4. 发明申请

WO2003054000A1 TEMPLATE-FIXED PEPTIDOMIMETICSAS INHIBITORS OF SERINE PROTEASES 审中-公开
标题翻译：模板固定肽酶抑制剂丝氨酸蛋白酶抑制剂
公开(公告)号：WO2003054000A1
公开(公告)日：2003-07-03
申请号：PCT/EP2001/014528
申请日：2001-12-11
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , OBRECHT, Daniel , ROBINSON, John, Anthony , DESCOURS, Anne
发明人： OBRECHT, Daniel , ROBINSON, John, Anthony , DESCOURS, Anne
IPC分类号： C07K7/06
CPC分类号： C07K7/06 , A61K38/00 , C07K7/08 , C07K7/64
摘要： Template-fixed β-hairpin peptidomimetics of the general formulae (1), wherein Z is a template-fixed chain of 7 to 11 α-amino acid residues which, depending on their positions in the chain (counted starting formteh N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining symbols in the aove formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit proteases, in particular serine proteases. 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（1）的模板固定的β-螺旋肽模拟物，其中Z是7至11个α-氨基酸残基的模板固定链，其取决于其在链中的位置（计数的起始形式N-末端氨基酸）是Gly或Pro，或某些类型，其作为酰基配方中的其余符号在说明书和权利要求书及其盐中定义，具有抑制蛋白酶，特别是丝氨酸蛋白酶的性质。这些β-螺旋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。

5. 发明申请

WO2007079597A1 TEMPLATE - FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY 审中-公开
标题翻译：模板 - 具有抗微生物活性的固定肽
公开(公告)号：WO2007079597A1
公开(公告)日：2007-07-19
申请号：PCT/CH2006/000036
申请日：2006-01-16
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , ROBINSON, John, Anthony , SRINIVAS, Nityakalyani , GOMBERT, Frank , OBRECHT, Daniel , VRIJBLOED, Wim , DIAS, Ricardo , DEMARCO, Steve, J.
发明人： ROBINSON, John, Anthony , SRINIVAS, Nityakalyani , GOMBERT, Frank , OBRECHT, Daniel , VRIJBLOED, Wim , DIAS, Ricardo , DEMARCO, Steve, J.
IPC分类号： C07K7/06 , C07K7/08 , C07K7/64 , C07K14/00 , A61K38/04
CPC分类号： C07K7/64 , A01N43/36 , A61K38/00 , C07K1/10 , C07K7/06 , C07K7/08 , C07K14/001
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）为 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。

6. 发明申请

WO2002070547A1 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：WO2002070547A1
公开(公告)日：2002-09-12
申请号：PCT/EP2002/001711
申请日：2002-02-18
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , OBRECHT, Daniel , ROBINSON, John, Anthony , VRIJBLOED, Jan, Wim
发明人： OBRECHT, Daniel , ROBINSON, John, Anthony , VRIJBLOED, Jan, Wim
IPC分类号： C07K7/06
CPC分类号： C07K7/06 , A61K38/00 , C07K1/047 , C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formulae (I) and (II) wherein Z, Z1 and Z2 are template-fixed chains of 8 to 16 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 formulae, are defined in the description and the claims, and salts thereof, have the property to inhibit the growth of or to kill microorganisms and cancer cells. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials or as medicaments to treat or prevent infections or diseases related to such infections and/or 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）和（II）的模板固定β-螺旋肽模拟物，其中Z，Z1和Z2是8至16个α-氨基酸残基的模板固定链，这取决于它们在链中的位置（计数开始来自N-末端氨基酸）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中定义，及其盐具有抑制生长的性质或杀死微生物和癌细胞。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，或用作治疗或预防与这种感染和/或癌症有关的感染或疾病的药物。这些β-螺旋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。

7. 发明申请

WO2008092281A8 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定蛋白质
公开(公告)号：WO2008092281A8
公开(公告)日：2009-09-03
申请号：PCT/CH2007000038
申请日：2007-01-29
申请人： POLYPHOR LTD , OBRECHT DANIEL , GOMBERT FRANK , DEMARCO STEVE J , LUDIN CHRISTIAN , SELLIER-KESSLER ODILE , JUNG FRANCOISE , MUKHERJEE RESHMI , ROMAGNOLI BARBARA , HENZE HEIKO , LEDERER ALEX , BISANG CHRISTIAN
发明人： OBRECHT DANIEL , GOMBERT FRANK , DEMARCO STEVE J , LUDIN CHRISTIAN , SELLIER-KESSLER ODILE , JUNG FRANCOISE , MUKHERJEE RESHMI , ROMAGNOLI BARBARA , HENZE HEIKO , LEDERER ALEX , BISANG CHRISTIAN
IPC分类号： C07K5/10 , A61K38/04 , C07K7/06 , C07K7/08
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 ß-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 4 a-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 ß-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4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）为 Gly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及其盐中定义，具有激动或拮抗GPCR受体如CXCR3，尿素调节素和CCR10的性质。它们可以用作治疗或预防心血管疾病，皮肤病，内分泌系统和激素失调，代谢疾病，炎性疾病，神经疾病，呼吸系统疾病，血液病和癌症等疾病的药物。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。

8. 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。

9. 发明申请

WO2007079605A3 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY 审中-公开
公开(公告)号：WO2007079605A3
公开(公告)日：2007-07-19
申请号：PCT/CH2007/000017
申请日：2007-01-15
申请人： POLYPHOR LTD. , UNIVERSITÄT ZÜRICH , GOMBERT, Frank , OBRECHT, Daniel , VRIJBLOED, Wim , DIAS, Ricardo , DEMARCO, Steve, J. , ROBINSON, John, Anthony , SRINIVAS, Nityakalyana
发明人： GOMBERT, Frank , OBRECHT, Daniel , VRIJBLOED, Wim , DIAS, Ricardo , DEMARCO, Steve, J. , ROBINSON, John, Anthony , SRINIVAS, Nityakalyana
IPC分类号： C07K7/06 , C07K7/08 , C07K7/64 , C07K14/00 , A61K38/04
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 firom 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.

10. 发明申请

WO2007079605A2 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定蛋白质
公开(公告)号：WO2007079605A2
公开(公告)日：2007-07-19
申请号：PCT/CH2007000017
申请日：2007-01-15
申请人： POLYPHOR LTD , UNIV ZUERICH , GOMBERT FRANK , OBRECHT DANIEL , VRIJBLOED WIM , DIAS RICARDO , DEMARCO STEVE J , ROBINSON JOHN ANTHONY , SRINIVAS NITYAKALYANA
发明人： GOMBERT FRANK , OBRECHT DANIEL , VRIJBLOED WIM , DIAS RICARDO , DEMARCO STEVE J , ROBINSON JOHN ANTHONY , SRINIVAS NITYAKALYANA
IPC分类号： C07K7/06 , A61K38/04 , C07K7/08 , C07K7/64 , C07K14/00
CPC分类号： C07K7/64 , A01N43/36 , A61K38/00 , C07K1/10 , C07K7/06 , C07K7/08 , C07K14/001
摘要： Template-fixed ß-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12 a-amino acid residues which, depending on their positions in the chain (counted starting firom 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 ß-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）为 Gly或Pro，或某些类型，其作为上述公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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