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公开(公告)号：US10730911B2
公开(公告)日：2020-08-04
申请号：US15564539
申请日：2016-04-06
申请人： POLYPHOR AG , Universität Zürich
发明人： Daniel Obrecht , Christian Bisang , Anatol Luther , Steffen Weinbrenner , John Anthony Robinson , Kerstin Moehle , Christian Steuer , William J. Drury, III
IPC分类号： A61K38/08 , A61K38/12 , C07K7/54 , C07K7/64 , C07K14/72 , A61K38/02 , C07K1/04 , C07K14/00 , C07K14/47 , C07K14/655 , C07K14/705 , C40B50/14 , A61K38/00
摘要： Novel backbone-cyclized peptidomimetics of the general formula cyclo[-P1-P2-P3-P4-P5-P6-P7-P8-T1-T2-] (I) wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to modulate the GLP-1 receptor. They can be used as medicaments to treat, prevent, or delay the onset of diseases, disorders or conditions in which modulation of the human GLP-1 receptor is beneficial, such as type 2 diabetes. These backbone-cyclized peptidomimetics can be manufactured by a process which is based on a mixed solid—and solution phase synthetic strategy.
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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
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.
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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
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.
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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
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.
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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
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.
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公开(公告)号：US09850284B2
公开(公告)日：2017-12-26
申请号：US14781229
申请日：2014-03-28
申请人： POLYPHOR AG
CPC分类号： C07K7/64 , A61K38/00 , Y02A50/473
摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo(P1-p2-p3-p4-p5-p6-p7p8p9-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.
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公开(公告)号：US10829520B2
公开(公告)日：2020-11-10
申请号：US15560200
申请日：2016-03-23
申请人： POLYPHOR AG
摘要： Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, T, 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. 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.
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公开(公告)号：US10370411B2
公开(公告)日：2019-08-06
申请号：US15791087
申请日：2017-10-23
申请人： POLYPHOR AG
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.
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公开(公告)号：US10259847B2
公开(公告)日：2019-04-16
申请号：US15515445
申请日：2015-09-29
申请人： POLYPHOR AG
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.
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