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    TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY
    2.
    发明申请
    TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY 审中-公开

    公开(公告)号：US20170107259A1

    公开(公告)日：2017-04-20

    申请号：US15392586

    申请日：2016-12-28

    申请人： POLYPHOR LTD. ,  UNIVERSITAET ZUERICH

    发明人： Steven J. DEMARCO ,  Wim VRIJBLOED ,  Ricardo DIAS ,  John Anthony ROBINSON ,  Nityakalyani SRINIVAS ,  Frank GOMBERT ,  Daniel OBRECHT

    IPC分类号： C07K7/64

    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.

    Dye conjugates of template-fixed peptidomimetics
    3.
    发明授权
    Dye conjugates of template-fixed peptidomimetics 有权
    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。

    Template-fixed peptidomimetics
    4.
    发明授权
    Template-fixed peptidomimetics 有权
    模板固定肽模拟物

    公开(公告)号：US08921325B2

    公开(公告)日：2014-12-30

    申请号：US13764099

    申请日：2013-02-11

    申请人： Universitaet Zuerich ,  Polyphor Ltd.

    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 ,  C07K7/56

    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 mobilization 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 Gys11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。

    Template-fixed peptidomimetics with antimicrobial activity
    5.
    发明授权
    Template-fixed peptidomimetics with antimicrobial activity 有权
    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。

    Template fixed β-hairpin loop mimetics and their use in phage display
    6.
    发明授权
    Template fixed β-hairpin loop mimetics and their use in phage display 有权
    模板固定β-发夹环模拟物及其在噬菌体展示中的应用

    公开(公告)号：US08642560B2

    公开(公告)日：2014-02-04

    申请号：US13196658

    申请日：2011-08-02

    申请人： Jan Wim Vrijbloed ,  Daniel Obrecht ,  Sergio Locurio ,  Frank Otto Gombert ,  Christian Ludin ,  Françoise Jung

    发明人： Jan Wim Vrijbloed ,  Daniel Obrecht ,  Sergio Locurio ,  Frank Otto Gombert ,  Christian Ludin ,  Françoise Jung

    IPC分类号： A61K38/10 ,  A61K38/08

    CPC分类号： C07K1/047 ,  C12N15/1037 ,  C40B40/02

    摘要： Template-fixed β-hairpin mimetics and libraries including a plurality of these mimetics are provided. The template-fixed β-hairpin mimetics are of the following general formula: R1-Cys-Z-Cys-R2  I wherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; R1 and R2 are di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-α-amino acid.

    摘要翻译： 提供了模板固定的β-发夹模拟物和包括多个这些模拟物的文库。 模板固定的β-发夹模拟物具有以下通式：R1-Cys-Z-Cys-R2I，其中两个半胱氨酸残基通过二硫键桥连，由此形成环肽; R1和R2是如本文所定义的某些类型的二肽或三肽部分; 并且Z是n个氨基酸残基的链，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。

    Template Fixed Beta-Hairpin Loop Mimetics and Their Use in Phage Display
    7.
    发明申请
    Template Fixed Beta-Hairpin Loop Mimetics and Their Use in Phage Display 有权
    模板固定β-发夹环模拟物及其在噬菌体展示中的应用

    公开(公告)号：US20090118134A1

    公开(公告)日：2009-05-07

    申请号：US10579104

    申请日：2003-11-15

    申请人： Jan Wim Vrijbloed ,  Daniel Obrecht ,  Sergio Locurio ,  Frank Otto Gombert ,  Christian Ludin ,  Francoise Jung

    发明人： Jan Wim Vrijbloed ,  Daniel Obrecht ,  Sergio Locurio ,  Frank Otto Gombert ,  Christian Ludin ,  Francoise Jung

    IPC分类号： C40B30/04 ,  C07K7/00 ,  C40B40/10 ,  C40B40/02

    CPC分类号： C07K1/047 ,  C12N15/1037 ,  C40B40/02

    摘要： Template-fixed β-hairpin mime tics of the general formula R1-Cys-Z-Cys-R2 (1) wherein the two Cys residues are bridged by a disulfide bond thereby forming a cyclic peptide; R1 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.

    摘要翻译： 通式R1-Cys-Z-Cys-R2（1）的模板固定β-发夹制剂，其中两个Cys残基用二硫键桥接，从而形成环肽; R1和R2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，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。