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1. 发明授权

US11235024B2 Beta-hairpin peptidomimetic with elastase inhibitory activity and aerosol dosage forms thereof 有权
公开(公告)号：US11235024B2
公开(公告)日：2022-02-01
申请号：US16305714
申请日：2017-05-31
申请人： POLYPHOR AG
发明人： Christian Ludin , Manfred Keller , Piet Bruijnzeel , Johann Zimmermann , Philip Barth , Eric Chevalier
IPC分类号： A61K38/12 , A61P11/08 , A61K9/00
摘要： The present invention relates to pharmaceutical aerosols comprising a β-hairpin peptidomimetic of formula cyclo(-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-DPro-Pro-), or a pharmaceutically acceptable salt thereof, having inhibitory activity against human neutrophil elastase. It further relates to solid or liquid pharmaceutical compositions and kits for preparing and administering such aerosols. The invention can be used for the prevention, management or treatment of pulmonary diseases, such as alpha-1 antitrypsin deficiency (AATD), cystic fibrosis (CF), non-cystic fibrosis bronchiactasis (NCFB), or chronic obstructive pulmonary disease (COPD), or infections, or diseases, or conditions of the lungs, being mediated by or resulting from human neutrophil elastase activity. Thus, the invention further relates to a pharmaceutical composition or a pharmaceutical aerosol comprising the active compound cyclo(-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-DPro-Pro-), or any pharmaceutically acceptable salt thereof, for use in a method for the prevention, management or treatment of diseases or conditions of the lungs being mediated by or resulting from human neutrophil elastase activity in a subject.

2. 发明申请

US20200230202A1 BETA-HAIRPIN PEPTIDOMIMETIC WITH ELASTASE INHIBITORY ACTIVITY AND AEROSOL DOSAGE FORMS THEREOF 审中-公开
公开(公告)号：US20200230202A1
公开(公告)日：2020-07-23
申请号：US16305518
申请日：2017-05-31
申请人： POLYPHOR AG
发明人： Christian LUDIN , Manfred KELLER
IPC分类号： A61K38/12 , A61K9/00 , A61P11/08
摘要： The present invention relates to pharmaceutical aerosols comprising a β-hairpin peptidomimetic of formula cyclo(-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-DPro-Pro-), or a pharmaceutically acceptable salt thereof, having inhibitory activity against human neutrophil elastase. It further relates to solid or liquid pharmaceutical compositions and kits for preparing and administering such aerosols. The invention can be used for the prevention, management or treatment of pulmonary diseases, such as alpha-1 antitrypsin deficiency (AATD), cystic fibrosis (CF), non-cystic fibrosis bronchiactasis (NCFB), or chronic obstructive pulmonary disease (COPD), or infections, or diseases, or conditions of the lungs, being mediated by or resulting from human neutrophil elastase activity. Thus, the invention further relates to a pharmaceutical composition or a pharmaceutical aerosol comprising the active compound cyclo(-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-DPro-Pro-), or any pharmaceutically acceptable salt thereof, for use in a method for the prevention, management or treatment of diseases or conditions of the lungs being mediated by or resulting from human neutrophil elastase activity in a subject.

3. 发明授权

US10370412B2 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.

4. 发明授权

US10363284B2 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.

5. 发明授权

US10273267B2 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.

6. 发明授权

US09938322B2 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.

7. 发明申请

US20180072776A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：US20180072776A1
公开(公告)日：2018-03-15
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： 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 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.

8. 发明申请

US20160333053A1 BETA-HAIRPIN PEPTIDOMIMETICS AS SELECTIVE ELASTASE INHIBITORS 审中-公开
标题翻译： BETA-HAIRPIN PEPTIDOMIMETICS作为选择性弹性酶抑制剂
公开(公告)号：US20160333053A1
公开(公告)日：2016-11-17
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
CPC分类号： C07K7/64 , A61K38/00 , C07K14/811
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.
摘要翻译：通式为（Xaa1-Xaa2-Thr3-Xaa4-Ser5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-）的β-发夹肽模拟物及其药学上可接受的盐与Xaa1，Xaa2，Xaa4 作为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Xaa6，Xaa7，Xaa8，Xaa9，Xaa10，Xaa11，Xaa12和Xaa13具有弹性蛋白酶抑制性质，特别是针对人嗜中性粒细胞弹性蛋白酶，并且可用于预防感染或与健康个体感染有关的疾病或感染患者感染减缓。本发明的化合物可以进一步用于由弹性蛋白酶活性介导或由弹性蛋白酶活性介导的癌症或免疫疾病或肺部疾病或心血管疾病或神经变性疾病或炎症或与炎症有关的疾病。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造。

9. 发明申请

US20160052971A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
公开(公告)号：US20160052971A1
公开(公告)日：2016-02-25
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： 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-p8p9-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），环[P1-p2-p3-p4-p5-p6-p7-p8p9-p10-p11-p12-T1-T2]的β-发夹肽模拟物及其药学上可接受的盐，其中P1至 P12，T1和T2是描述和权利要求中定义的元件，具有革兰氏阴性的抗微生物活性，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。它们可用作治疗或预防感染的药物，或用作食品，化妆品，药物或其他含营养材料的消毒剂。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造。

10. 发明申请

US20110312879A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 有权
标题翻译：具有CXCR4拮抗活性的模板固定的BETA-HAIRPIN PEPTIDOMIMETICS
公开(公告)号：US20110312879A1
公开(公告)日：2011-12-22
申请号：US13131205
申请日：2008-11-26
申请人： Frank Gombert , Daniel Obrecht , Alexander Lederer , Barbara Romagnoli
发明人： Frank Gombert , Daniel Obrecht , Alexander Lederer , Barbara Romagnoli
IPC分类号： A61K38/15 , A61P7/00 , A61P31/18 , A61P35/00 , A61P35/04 , A61P29/00 , C07K7/54 , A61P9/10
CPC分类号： C07K7/64 , C07K1/047 , C07K7/08
摘要： Template-fixed peptidomimetics formula (Ia) formula (Ib) wherein Z is a template-fixed chain of 14 α-amino and/or α-hydroxy acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Pro, Gly, a glycolic acid residue or of certain types which, as the remaining symbols in the above formulae, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties and can be used for preventing HIV infections in non-infected 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 immuno suppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These depsipeptides can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译：模板固定肽模拟物式（Ia）式（Ib）其中Z是14个α-氨基和/或α-羟基酸残基的模板固定链，其取决于其在链中的位置（从N-末端计数氨基酸）是Pro，Gly，乙醇酸残基或某些类型，其作为上述式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，其盐具有CXCR4拮抗特性，并且可用于预防未感染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/或作为诱导干细胞动员以调节组织修复的试剂。这些脱肽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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