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1. 发明公开

EP4380689A1 ANTIMICROBIAL PEPTIDOMIMETICS 审中-实审
公开(公告)号：EP4380689A1
公开(公告)日：2024-06-12
申请号：EP22764328.5
申请日：2022-08-04
申请人： Basilea Pharmaceutica International AG, Allschwil , Universität Zürich
发明人： OBRECHT, Daniel , LUTHER, Anatol , UPERT, Grégory , DESJONQUERES, Nicolas , BRABET, Emile , ZBINDEN, Peter , JUNG, Françoise , ZERBE, Oliver , MÖHLE, Kerstin
IPC分类号： A61P31/02 , A61K38/00 , C07K7/08 , C07K14/47
CPC分类号： C07K7/08 , A61P31/02 , A61K38/00 , C07K14/43563 , Y02A50/30

2. 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.

3. 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.

4. 发明授权

EP1856140B1 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：EP1856140B1
公开(公告)日：2013-12-25
申请号：EP05707463.5
申请日：2005-02-17
申请人： Polyphor Ltd. , Universität Zürich
发明人： DE MARCO, 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

5. 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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