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    Beta-hairpin peptidomimetics
    1.
    发明授权
    Beta-hairpin peptidomimetics 有权

    公开(公告)号：US11629171B2

    公开(公告)日：2023-04-18

    申请号：US16762394

    申请日：2018-11-12

    申请人： POLYPHOR AG

    发明人： Daniel Obrecht ,  Anatol Luther ,  Francesca Bernardini ,  Glenn E. Dale ,  Nicolas Desjonqueres ,  Emile Brabet ,  Grégory Upert

    IPC分类号： C07K7/64 ,  C07K1/06 ,  A61K38/00

    摘要： Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, X, Q., and optionally L being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli and/or Pseudomonas aeruginosa and/or Enterobacter cloacae. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    β-hairpin peptidomimetics
    3.
    发明授权
    β-hairpin peptidomimetics 有权

    公开(公告)号：US10654897B2

    公开(公告)日：2020-05-19

    申请号：US15515417

    申请日：2015-09-29

    申请人： POLYPHOR AG

    发明人： Daniel Obrecht ,  Anatol Luther ,  Francesca Bernardini ,  Peter Zbinden ,  Sophie Barthelemy ,  Alexander Lederer

    IPC分类号： C07K7/64 ,  A61K38/00

    摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2] and pharmaceutically acceptable salts thereof, with P1 to P12, T1 and T2 being elements as defined in the description and the claims, have Gramnegative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    Beta-hairpin peptidomimetics
    5.
    发明授权
    Beta-hairpin peptidomimetics 有权

    公开(公告)号：US10370412B2

    公开(公告)日：2019-08-06

    申请号：US15816955

    申请日：2017-11-17

    申请人： Polyphor AG

    发明人： Daniel Obrecht ,  Anatol Luther ,  Francesca Bernardini ,  Peter Zbinden

    IPC分类号： A61K38/00 ,  C07K7/64

    摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo[P1—P2—P3—P4—P5—P6—P7—P8—P9—P10—P11—P12-T1-T2], and pharmaceutically acceptable salts thereof, with P1 to P12, T1 and T2 being elements as defined in the description and the claims, have broad spectrum Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials.These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    β-hairpin peptidomimetics
    6.
    发明授权
    β-hairpin peptidomimetics 有权

    公开(公告)号：US10363284B2

    公开(公告)日：2019-07-30

    申请号：US15444045

    申请日：2017-02-27

    申请人： POLYPHOR AG

    发明人： Frank Otto Gombert ,  Daniel Obrecht ,  Alexander Lederer ,  Johann Zimmermann ,  Christian Oefner

    IPC分类号： C07K7/54 ,  A61K38/00 ,  A61K38/12 ,  C07K7/08

    摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8, Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological 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 immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair.These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    Beta-hairpin peptidomimetics as selective elastase inhibitors
    7.
    发明授权
    Beta-hairpin peptidomimetics as selective elastase inhibitors 有权

    公开(公告)号：US10273267B2

    公开(公告)日：2019-04-30

    申请号：US15107575

    申请日：2013-12-27

    申请人： POLYPHOR AG

    发明人： Frank Otto Gombert ,  Daniel Obrecht ,  Odile Sellier-Kessler ,  Alexander Lederer ,  Christian Ludin ,  Manuella Schmitt-Billet ,  Steffen Weinbrenner

    IPC分类号： C07K7/64 ,  C07K14/81 ,  A61K38/00

    摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Xaa1-Xaa2-Thr3-Xaa4-Ser5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-) and pharmaceutically acceptable salts thereof, with Xaa1, Xaa2, Xaa4, Xaa6, Xaa7, Xaa8, Xaa9, Xaa10, Xaa11, Xaa12 and Xaa13 being amino acid residues of certain types which are defined in the description and the claims, have elastase inhibitory properties, especially against human neutrophil elastase, and can be used for preventing infections or diseases related to such infections in healthy individuals or for slowing infections in infected patients. The compounds of the invention can further be used where cancer, or immunological diseases, or pulmonary diseases, or cardiovascular diseases, or neurodegenerative diseases, or inflammation, or diseases related to inflammation, are mediated or resulting from elastase activity. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    β-hairpin peptidomimetics
    8.
    发明授权
    β-hairpin peptidomimetics 有权

    公开(公告)号：US09938322B2

    公开(公告)日：2018-04-10

    申请号：US14781247

    申请日：2014-03-28

    申请人： POLYPHOR AG

    发明人： Daniel Obrecht ,  Anatol Luther ,  Francesca Bernardini ,  Peter Zbinden

    IPC分类号： A61K38/00 ,  C07K7/64 ,  C07K7/08

    CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K7/08 ,  Y02A50/473

    摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo[P1-p2-p3-p4-p5-p6-p7-p8-p9-p10-p11-p12-T1-T2], and pharmaceutically acceptable salts thereof, with P1 to P12, T1 and T2 being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.