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1. 发明申请

US20210187059A1 PHARMACEUTICAL COMBINATIONS FOR TREATING CANCER 有权
公开(公告)号：US20210187059A1
公开(公告)日：2021-06-24
申请号：US16486945
申请日：2018-02-20
申请人： POLYPHOR AG
发明人： Michael BAUER , Leon HOOFTMAN , Barbara ROMAGNOLI
IPC分类号： A61K38/12 , A61K9/00 , A61K31/357 , A61P35/00
摘要： The present invention relates to pharmaceutical combinations comprising a compound of formula I or a pharmaceutically acceptable salt thereof and cyclo(-Tyr-His-Ala-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro-) having a disulfide bond between Cys4 and Cys1 11 or a pharmaceutically acceptable salt thereof and their use in a method for the prevention, delay of progression or treatment of cancer in a subject.

2. 发明授权

US09957297B2 Template-fixed peptidomimetics as inhibitors of FPR1 有权
公开(公告)号：US09957297B2
公开(公告)日：2018-05-01
申请号：US14349683
申请日：2012-10-02
申请人： POLYPHOR AG
发明人： Françoise Jung , Daniel Obrecht , Ralf Löwe , Johann Zimmermann , Guillaume Lemercier , Eric Chevalier
IPC分类号： A61K38/00 , C07K14/47 , A01N37/18 , A61P31/04 , A61P23/00 , A61P17/00 , A61P29/00 , A61P35/00 , A61K38/10 , A61K38/12 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K1/00 , C07K7/08 , C07K7/64
CPC分类号： C07K7/08 , C07K7/64
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I): cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2] 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 of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions, immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. cancer. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

3. 发明申请

US20180072774A1 BACKBONE-CYCLIZED PEPTIDOMIMETICS WITH GLP-1R MODULATING ACTIVITY 审中-公开
公开(公告)号：US20180072774A1
公开(公告)日：2018-03-15
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： C07K7/54 , C40B50/14 , C07K1/04 , A61K38/02 , C07K14/00 , C07K14/705 , C07K14/47 , C07K14/655
CPC分类号： C07K7/54 , A61K38/00 , A61K38/02 , C07K1/04 , C07K7/64 , C07K14/001 , C07K14/4702 , C07K14/6555 , C07K14/705 , C07K14/723 , C40B50/14
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.

4. 发明申请

US20180044380A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：US20180044380A1
公开(公告)日：2018-02-15
申请号：US15791087
申请日：2017-10-23
申请人： POLYPHOR AG
发明人： Daniel OBRECHT , Anatol LUTHER , Francesca BERNARDINI , Peter ZBINDEN
IPC分类号： 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.

5. 发明申请

US20170369523A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS THAT ARE LIGANDS FOR G-PROTEIN-COUPLED RECEPTORS (GPCRS) AND ARE MODULATORS OF TRANSCRIPTION FACTORS AND COACTIVATORS 审中-公开
公开(公告)号：US20170369523A1
公开(公告)日：2017-12-28
申请号：US15701284
申请日：2017-09-11
申请人： POLYPHOR AG
发明人： John Anthony ROBINSON , Kerstin MÖHLE , Markus SEITZ , Ludovic T. MAILLARD , Roba MOUNME , Frank Otto GOMBERT , Odile SELLIER-KESSLER , Heiko HENZE , Daniel OBRECHT , Christian BISANG , Alexander LEDERER
IPC分类号： C07K1/02 , C07K7/64 , C07K7/56
CPC分类号： C07K1/02 , C07K7/56 , C07K7/64
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 8 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 agonizing or antagonizing activity against urotensin II or show inhibition of the STAT6/NCoA-1 interaction and can be used for preventing or treating diseases or disorders related to urotensin II, STAT6 and NCoA-1.These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

6. 发明申请

US20170253634A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：US20170253634A1
公开(公告)日：2017-09-07
申请号：US15515445
申请日：2015-09-29
申请人： POLYPHOR AG
发明人： Daniel OBRECHT , Anatol LUTHER , Francesca BERNARDINI , Gildas DENIAU , Alexander LEDERER
IPC分类号： C07K7/64
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-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.

7. 发明申请

US20170218026A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：US20170218026A1
公开(公告)日：2017-08-03
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
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-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.

8. 发明授权

US09637520B2 Template-fixed peptidomimetics with CXCR7 modulating activity 有权
公开(公告)号：US09637520B2
公开(公告)日：2017-05-02
申请号：US14795694
申请日：2015-07-09
申请人： POLYPHOR AG
发明人： Frank Otto Gombert , Alexander Lederer , Ralf Löwe , Daniel Obrecht , Barbara Romagnoli , Johann Zimmermann , Kalpana Patel
IPC分类号： C07K7/64 , A61K38/12 , C07K14/715 , C07K14/705 , A61K38/00 , A61K38/17
CPC分类号： C07K7/64 , A61K38/00 , A61K38/17 , A61K38/177 , A61K38/1793 , C07K14/705 , C07K14/715 , C07K14/7158
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I) wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells.

9. 发明授权

US09284352B2 Beta-hairpin peptidomimetics having CXCR4 antagonizing activity 有权
标题翻译：具有CXCR4拮抗活性的β-发夹肽模拟物
公开(公告)号：US09284352B2
公开(公告)日：2016-03-15
申请号：US14466709
申请日：2014-08-22
申请人： POLYPHOR AG
发明人： Daniel Obrecht , Frank Otto Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
IPC分类号： C07K7/08 , C07K7/02 , C07K1/06
CPC分类号： C07K7/08 , C07K1/061 , C07K7/02
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa1, Xaa2, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa12, Xaa13, Xaa14, Xaa15 and Xaa16 being amino acid residues of certain types which are defined in the description and the claims, 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 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 peptides can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译：通式为（Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物，Cys4之间的二硫键和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa1，Xaa2，Xaa3，Xaa5，Xaa6，Xaa7，Xaa8，Xaa12，Xaa13，Xaa14，Xaa15和Xaa16，具有CXCR4拮抗特性，可用于预防健康个体中的HIV感染，或用于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; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员以调节组织修复的试剂。这些肽可以通过基于混合固相和溶液相合成策略的方法制造。

10. 发明申请

US20160060298A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
公开(公告)号：US20160060298A1
公开(公告)日：2016-03-03
申请号：US14781229
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： C07K7/64
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.
摘要翻译：通式（I）的β-发夹肽模拟物，环（P1-p2-p3-p4-p5-p6-p7p8p9-p10-p11-p12-T1-T2）及其药学上可接受的盐与P1至P12， T1和T2是描述和权利要求中定义的元件，具有广谱的革兰氏阴性抗微生物活性，例如抑制生长或杀死肺炎克雷伯杆菌和/或鲍氏不动杆菌和/或大肠杆菌等微生物，可以使用它们作为治疗或预防感染的药物或作为食品，化妆品，药物或其他含营养物质的消毒剂，这些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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