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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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2.发明申请TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 有权具有CXCR4拮抗活性的模板固定的BETA-HAIRPIN PEPTIDOMIMETICS公开(公告)号：US20150087577A1
公开(公告)日：2015-03-26
申请号：US14495737
申请日：2014-09-24
申请人： Polyphor Ltd. , Universität Zürich
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
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，其作为上述结构中的其余符号在说明书和权利要求书及其权利要求书中定义，及其盐具有CXCR4拮抗性质。 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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3.发明授权Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity 有权模板固定β-发夹肽模拟物与CXCR4拮抗活性公开(公告)号：US09518092B2
公开(公告)日：2016-12-13
申请号：US14495737
申请日：2014-09-24
申请人： Polyphor Ltd. , Universität Zürich
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
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.
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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：US09775877B2
公开(公告)日：2017-10-03
申请号：US14419986
申请日：2013-08-07
申请人： POLYPHOR AG
CPC分类号： A61K38/12 , A61K31/65 , A61K38/10 , A61K47/6809 , A61L2300/406 , C07K7/08 , C07K7/50 , C07K7/64 , A61K2300/00
摘要： A novel combination comprising a β-hairpin peptidomimetic of the formula cyclo(-Thr-Trp-Ile-Dab-Orn-DDab-Dab-Trp-Dab-Dab-Ala-Ser-DPro-Pro) (I), and a compound of the glycylcycline class, especially tigecycline, that enable therapeutic control of specific bacterial infections in human or animals at doses of the individual compounds lower than either of the compounds administered alone. The combination can be used as a medicament to treat e.g. skin or soft tissue infections; eye, ear, blood stream, or intra-abdominal infections; infections related to respiratory diseases, to bone diseases, to cardiovascular diseases, to genitourinal diseases, or to gastrointestinal diseases.
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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：US10363284B2
公开(公告)日：2019-07-30
申请号：US15444045
申请日：2017-02-27
申请人： POLYPHOR AG
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.
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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
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.
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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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