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1. 发明授权

US08658604B2 Template-fixed beta-hairpin peptidomimetics with protease inhibitory activity 有权
标题翻译：具有蛋白酶抑制活性的模板固定β-发夹肽模拟物
公开(公告)号：US08658604B2
公开(公告)日：2014-02-25
申请号：US11816589
申请日：2005-02-17
申请人： Steven J. DeMarco , Kerstin Moehle , Heiko Henze , Odile Sellier , Françoise Jung , Frank Gombert , Daniel Obrecht , Christian Ludin
发明人： Steven J. DeMarco , Kerstin Moehle , Heiko Henze , Odile Sellier , Françoise Jung , Frank Gombert , Daniel Obrecht , Christian Ludin
IPC分类号： A61K38/10 , A61K38/12
CPC分类号： C07K7/06 , A61K38/00 , C07K1/061 , C07K7/08 , C07K7/64
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.
摘要翻译：具有通式的模板固定的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）是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，具有抑制蛋白酶，特别是丝氨酸蛋白酶，特别是组织蛋白酶G或弹性蛋白酶或Tryptase。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

US20090054345A1 Template-Fixed Beta-Hairpin Peptidomimetics With Protease Inhibitory Activity 有权
标题翻译：具有蛋白酶抑制活性的模板固定β-发夹肽模拟物
公开(公告)号：US20090054345A1
公开(公告)日：2009-02-26
申请号：US11816589
申请日：2005-02-17
申请人： Steven J. DeMarco , Kerstin Moehle , Heiko Henze , Odile Sellier , Francoise Jung , Frank Gombert , Daniel Obrecht , Christian Ludin
发明人： Steven J. DeMarco , Kerstin Moehle , Heiko Henze , Odile Sellier , Francoise Jung , Frank Gombert , Daniel Obrecht , Christian Ludin
IPC分类号： A61K38/08 , C07K7/06 , A61P31/00 , A61P35/00 , A61P37/00 , A61P29/00
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 11α-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11α-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，具有抑制蛋白酶，特别是丝氨酸蛋白酶，特别是组织蛋白酶的性质 G或Elastase或Tryptase。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

US20050239693A1 Template-fixed peptidomimetics with antibacterial activity 有权
标题翻译：具有抗菌活性的模板固定肽模拟物
公开(公告)号：US20050239693A1
公开(公告)日：2005-10-27
申请号：US11062021
申请日：2005-02-18
申请人： Jan Vrijbloed , Daniel Obrecht , John Robinson , Odile Sellier , Marc Kessler
发明人： Jan Vrijbloed , Daniel Obrecht , John Robinson , Odile Sellier , Marc Kessler
IPC分类号： A61K38/00 , A61P31/04 , C07K1/04 , C07K5/078 , C07K7/64 , A61K38/12 , C07K5/12
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 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. 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β-发夹肽模拟物，其通式如下：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书及其盐中定义，具有选择性抑制绿脓假单胞菌和不动杆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。

4. 发明申请

US20100056432A1 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肽
公开(公告)号：US20100056432A1
公开(公告)日：2010-03-04
申请号：US12506794
申请日：2009-07-21
申请人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Odile Sellier , Marc Kessler
发明人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Odile Sellier , Marc Kessler
IPC分类号： A61K38/12 , C07K5/12 , A61P11/00 , A61P17/02 , A61P1/00 , A61P27/16 , A61P35/00
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, depend 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 dipeptides. 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）的模板固定和半透明肽模拟物，其中Z是12个α-氨基酸残基的模板固定链，其取决于它们在链中的位置（从N-末端氨基酸开始计数）是Gly或Pro，或某些类型，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，其具有选择性抑制微生物生长或杀死诸如假单胞菌属（Pseudomonas）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＆bair-Hairpin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. 发明授权

US07582604B2 Template-fixed peptidomimetics with antibacterial activity 有权
标题翻译：具有抗菌活性的模板固定肽模拟物
公开(公告)号：US07582604B2
公开(公告)日：2009-09-01
申请号：US11062021
申请日：2005-02-18
申请人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Odile Sellier , Marc Kessler
发明人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Odile Sellier , Marc Kessler
IPC分类号： A61K38/12 , 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, depend 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 foodstuff, cosmetics, medicaments or other nutrient-containing materials, or as medicaments or 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，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，其具有选择性抑制微生物生长或杀死诸如假单胞菌属（Pseudomonas）铜绿假单胞菌和不动杆菌。它们可用作食品，化妆品，药物或其他含营养物质的消毒剂，或用作药物或治疗或预防感染。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。

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