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41. 发明公开

EP2427476A1 BETA-HAIRPIN PEPTIDOMIMETICS HAVING CXCR4 ANTAGONIZING ACTIVITY 有权
标题翻译： BET EL EL EL KA KA MCR CXCR4-ANTAGONISIERENDER WIRKUNG
公开(公告)号：EP2427476A1
公开(公告)日：2012-03-14
申请号：EP09779424.2
申请日：2009-05-07
申请人： Polyphor Ag
发明人： OBRECHT, Daniel , GOMBERT, Frank, Otto , LEDERER, Alexander , ROMAGNOLI, Barbara , BISANG, Christian
IPC分类号： C07K7/08 , C07K7/02 , A61K38/10 , A61P29/00 , A61P31/18 , A61P35/00
CPC分类号： C07K7/08 , C07K1/061 , C07K7/02
摘要： &bgr;-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的艾滋病毒感染或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/或作为诱导干细胞调动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。

42. 发明授权

EP1622930B9 TEMPLATE-FIXED PEPTIDOMIMETICS AS MEDICAMENTS AGAINST HIV AND CANCER 有权
标题翻译： MATRIZENFIXIERTE肽药物抗艾滋病和癌症
公开(公告)号：EP1622930B9
公开(公告)日：2009-10-14
申请号：EP03816774.8
申请日：2003-05-02
申请人： Polyphor AG , Universität Zürich
发明人： ZUMBRUNN, Jürg , DEMARCO, J., Steven , LOCIURO, Sergio , VRIJBLOED, Jan, Wim , GOMBERT, Frank , MUKHERJEE, Reshmi , MOEHLE, Kerstin , OBRECHT, Daniel , ROBINSON, John, Anthony , ROMAGNOLI, Barbara
IPC分类号： C07K7/06 , C07K7/08 , C07K14/00
CPC分类号： C07K7/06 , C07K7/08 , C07K14/001
摘要： Template-fixed ß-hairpin peptidomimetics of the General Formula (I); wherein Z and Z are template-fixed chains of4 and 6 or 5 and 7 alpha-amino acid residues which, depending on their positions in the chain 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 prevent or to reduce HIV infections or to inhibit the growth of cancer cells or to inhibit inflammation. They can be used as medicaments to treat or prevent HIV infections and/or cancer or inflammatory disorders. These beta-sheet peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

43. 发明公开

EP3582804A1 PHARMACEUTICAL COMBINATIONS FOR TREATING CANCER 无效
公开(公告)号：EP3582804A1
公开(公告)日：2019-12-25
申请号：EP18709923.9
申请日：2018-02-20
申请人： Polyphor AG
发明人： BAUER, Michael , HOOFTMAN, Leon , ROMAGNOLI, Barbara
IPC分类号： A61K39/00 , A61K31/357 , A61P35/00

44. 发明公开

EP3463281A1 BETA-HAIRPIN PEPTIDOMIMETIC WITH ELASTASE INHIBITORY ACTIVITY AND AEROSOL DOSAGE FORMS THEREOF 有权转让
公开(公告)号：EP3463281A1
公开(公告)日：2019-04-10
申请号：EP17733738.3
申请日：2017-05-31
申请人： Polyphor AG
发明人： BRUIJNZEEL, Piet , ZIMMERMANN, Johann , BARTH, Philip , CHEVALIER, Eric , LUDIN, Christian , KELLER, Manfred
IPC分类号： A61K8/64 , A61K38/12 , A61K9/00 , A61P11/00 , C07K7/64

45. 发明公开

EP3463280A1 BETA-HAIRPIN PEPTIDOMIMETIC WITH ELASTASE INHIBITORY ACTIVITY AND AEROSOL DOSAGE FORMS THEREOF 有权转让
公开(公告)号：EP3463280A1
公开(公告)日：2019-04-10
申请号：EP17733737.5
申请日：2017-05-31
申请人： Polyphor AG
发明人： LUDIN, Christian , KELLER, Manfred
IPC分类号： A61K8/64 , A61K38/12 , A61K9/00 , C07K7/64

46. 发明公开

EP3274361A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-实审
标题翻译： BETA-HAIRPIN多肽
公开(公告)号：EP3274361A1
公开(公告)日：2018-01-31
申请号：EP16713293.5
申请日：2016-03-23
申请人： Polyphor AG
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , ZBINDEN, Peter , LEDERER, Alexander
IPC分类号： C07K7/08 , C07K7/60 , C07K7/64
CPC分类号： C07K7/64 , A61K38/00 , C07K7/08 , C07K7/62 , C07K2319/00
摘要： These peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

47. 发明公开

EP3201218A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
标题翻译： BETA-HAIRPIN多肽
公开(公告)号：EP3201218A1
公开(公告)日：2017-08-09
申请号：EP15778875.3
申请日：2015-09-29
申请人： Polyphor AG
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , DENIAU, Gildas , LEDERER, Alexander
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.
摘要翻译：通式（I）的β-发夹肽模拟物，环[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2]及其药学上可接受的盐与 P1至P12，T1和T2是说明书和权利要求书中定义的元素，对例如，具有Gramegative抗微生物活性抑制生长或杀死微生物如肺炎克雷伯氏菌和/或鲍曼不动杆菌和/或大肠杆菌。它们可以用作治疗或预防感染的药物，或用作食品，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液相合成策略的方法制造。

48. 发明授权

EP2859012B1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
标题翻译： BETA-HAIRPIN多肽
公开(公告)号：EP2859012B1
公开(公告)日：2017-08-09
申请号：EP12725830.9
申请日：2012-06-06
申请人： Polyphor AG
发明人： GOMBERT, Frank Otto , OBRECHT, Daniel , LEDERER, Alexander , ZIMMERMANN, Johann , OEFNER, Christian
IPC分类号： C07K7/64
CPC分类号： A61K38/12 , A61K38/00 , C07K7/08 , C07K7/54
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.
摘要翻译：这些肽模拟物可以通过基于混合固体和溶液相合成策略的方法制造。

49. 发明授权

EP2531520B1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 失效
标题翻译：与CXCR7调节作用MATRIZENFIXIERTE肽
公开(公告)号：EP2531520B1
公开(公告)日：2016-05-11
申请号：EP11702229.3
申请日：2011-02-04
申请人： Polyphor AG
发明人： GOMBERT, Frank, Otto , LEDERER, Alexander , LÖWE, Ralf , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZIMMERMANN, Johann , PATEL, Kalpana
IPC分类号： C07K7/64
CPC分类号： C07K7/64 , A61K38/00 , A61K38/17 , A61K38/177 , A61K38/1793 , C07K14/705 , C07K14/715 , C07K14/7158

50. 发明公开

EP2978771A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
标题翻译： BETA-发夹PEPTIDMIMETIKA
公开(公告)号：EP2978771A1
公开(公告)日：2016-02-03
申请号：EP14714670.8
申请日：2014-03-28
申请人： Polyphor Ag
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , ZBINDEN, Peter
IPC分类号： C07K7/08 , C07K7/64
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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