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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. 发明授权

US09073973B2 Dye conjugates of template-fixed peptidomimetics 有权
标题翻译：模板固定肽模拟物的染料缀合物
公开(公告)号：US09073973B2
公开(公告)日：2015-07-07
申请号：US11913511
申请日：2005-05-02
申请人： Steven J. DeMarco , Frank Gombert , Daniel Obrecht , Christian Ludin , Barbara Romagnoli
发明人： Steven J. DeMarco , Frank Gombert , Daniel Obrecht , Christian Ludin , Barbara Romagnoli
IPC分类号： A61K38/10 , C07K5/00 , C07K7/64 , A61K38/48
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 abnormalities; 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）的模板固定和平滑肽模拟物的染料缀合物，其中Z是14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（从N-末端计数氨基酸）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。这些染色偶联物，可以通过基于混合固相和溶液相合成策略的方法制造。

3. 发明授权

US08685922B2 Template-fixed peptidomimetics with antimicrobial 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：US08685922B2
公开(公告)日：2014-04-01
申请号：US12161065
申请日：2007-01-15
申请人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
IPC分类号： A61K38/10 , C07K7/08 , A61P31/00
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）的模板固定和半乳糖肽模拟物，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书中定义，以及其盐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

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。

5. 发明授权

US08895695B2 Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity 有权
标题翻译：模板固定β-发夹肽模拟物与CXCR4拮抗活性
公开(公告)号：US08895695B2
公开(公告)日：2014-11-25
申请号：US12828998
申请日：2010-07-01
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
IPC分类号： C07K7/08 , C07K7/50
CPC分类号： C07K7/64 , A61K38/00 , C07K1/047 , C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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. 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）的模板固定和半乳糖肽模拟物，其中Z是12,14或18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）是Gly，NMeGly，Pro或Pip，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CXCR4拮抗性质。这些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

US20140087994A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY 有权
公开(公告)号：US20140087994A1
公开(公告)日：2014-03-27
申请号：US14074251
申请日：2013-11-07
申请人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
IPC分类号： C07K7/08
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 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.

7. 发明申请

US20130150299A1 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定蛋白质
公开(公告)号：US20130150299A1
公开(公告)日：2013-06-13
申请号：US13764099
申请日：2013-02-11
申请人： Daniel OBRECHT , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel OBRECHT , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
IPC分类号： A61K38/12
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , C07K7/64
摘要： The template-fixed β-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-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 from CXCR4 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-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro），Cys4和Gys11之间的二硫键和其药学上可接受的盐，其中X为Ala或Tyr，具有CXCR4拮抗性质，可用于预防健康个体的HIV感染或减缓和停止感染患者的病毒进展; 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移动外周血干细胞和/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来制备，该方法使用肽化学中相当熟练技术人员众所周知的方法。

8. 发明授权

US08399611B2 Template-fixed peptidomimetics 有权
标题翻译：模板固定肽模拟物
公开(公告)号：US08399611B2
公开(公告)日：2013-03-19
申请号：US12528926
申请日：2007-02-28
申请人： Daniel Obrecht , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel Obrecht , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
IPC分类号： A61K38/12 , A61K38/10 , A61K38/04
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , C07K7/64
摘要： The template-fixed β-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Cys11, 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 from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or for treating inflammation, or, in particular, for stem cell mobilization of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor.
摘要翻译：模板固定和固定肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro），Cys4和 Cys11及其药学上可接受的盐，X为Ala或Tyr，具有CXCR4拮抗性质，可用于预防健康个体的HIV感染或减缓和阻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; 或用于治疗炎症，或特别是用于干细胞移动外周血干细胞和/或间充质干细胞（MSC）和/或其它干细胞，其保留取决于CXCR4受体。

9. 发明授权

US07838496B2 Template-fixed peptidomimetics as medicaments against HIV and cancer 有权
标题翻译：模板固定的肽模拟物作为抗艾滋病毒和癌症的药物
公开(公告)号：US07838496B2
公开(公告)日：2010-11-23
申请号：US10550778
申请日：2003-05-02
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , Barbara Romagnoli , John Anthony Robinson
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , Barbara Romagnoli , John Anthony Robinson
IPC分类号： A61K38/10 , C07K7/06 , C07K7/08
CPC分类号： C07K7/06 , C07K7/08 , C07K14/001
摘要： Template-fixed β-hairpin peptidomimetics of the General Formula (I); wherein Z1 and Z2 are template-fixed chains of 4 and 6 or 5 and 7 α-amino acid residues and salts thereof. They have CXCR4-antagonizing properties and can be used as medicaments. These β-sheet 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）的模板固定和模板肽模拟物; 其中Z1和Z2是4和6或5和7个α-氨基酸残基及其盐的模板固定链。它们具有CXCR4拮抗特性，可用作药物。这些胶体蛋白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。

10. 发明申请

US20100048463A1 TEMPLATE-FIXED PEPTIDOMIMETICS 有权
标题翻译：模板固定蛋白质
公开(公告)号：US20100048463A1
公开(公告)日：2010-02-25
申请号：US12528926
申请日：2007-02-28
申请人： Daniel Obrecht , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel Obrecht , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
IPC分类号： C07K7/56 , A61K38/12 , A61P31/12 , A61P31/18
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , C07K7/64
摘要： The template-fixed B-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-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 from CXCR4 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B发夹肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro），Cys4和Gys11之间的二硫键和其药学上可接受的盐，其中X为Ala或Tyr，具有CXCR4拮抗性质，可用于预防健康个体的HIV感染或减缓和停止感染患者的病毒进展; 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移动外周血干细胞和/或间充质干细胞（MSC）和/或其它干细胞，其保留取决于CXCR4-受体。这些和包装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，使用肽化学方面熟练的技术熟知的方法来制造。

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