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41. 发明申请

WO2013050346A1 TEMPLATE -FIXED PEPTIDOMIMETICS AS INHIBITORS OF FPR1 审中-公开
标题翻译：作为FPR1的抑制剂的模板化混合肽
公开(公告)号：WO2013050346A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069412
申请日：2012-10-02
申请人： POLYPHOR AG
发明人： JUNG, Françoise , OBRECHT, Daniel , LÖWE, Ralf , ZIMMERMANN, Johann , LEMERCIER, Guillaume , CHEVALIER, Eric
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： C07K7/08 , C07K7/64
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I): cyclo[P 1 -P 2 -P 3 -P 4 -P 5 -P 6 -P 7 -P 8 -P 9 -P 10 -P 11 -P 12 -P 13 -P 14 -T 1 -T 2 ] 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.
摘要翻译：通式（I）：环[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2]的新型模板固定β-发夹肽模拟物其中单个元件T或P是沿任一方向连接的α-氨基酸残基，根据其在链中的位置如说明书和权利要求及其盐中所定义，其具有拮抗生物效应的性质受体FPR1。它们可以用作治疗或预防炎性疾病，过敏性疾病，免疫学障碍，神经炎症，神经障碍，阻塞性气道疾病，传染病，缺血再灌注损伤和增殖性疾病如疾病或疾病的疾病或病症的药物。癌症。这些β-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。

42. 发明申请

WO2017063755A1 CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS 审中-公开
标题翻译：构象约束的大环化合物
公开(公告)号：WO2017063755A1
公开(公告)日：2017-04-20
申请号：PCT/EP2016/025111
申请日：2016-10-12
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel , ERMERT, Philipp
IPC分类号： C07D498/18 , A61K31/429 , A61P35/00
CPC分类号： C07D498/18
摘要： Formula (I); Conformationally constrained macrocyclic compounds of formula (I), including substituents E with at least one ester moiety, G and Q, as defined in the description and the claims, and salts thereof, can be metabolized to compounds that have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerase Pin1. In addition, they show antiproliferative activity on various cancer cell lines. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
摘要翻译：式（I）;式（I）式（I）的构象约束的大环化合物，包括具有至少一个酯部分的取代基E，如说明书和权利要求书中定义的G和Q及其盐，可被代谢成具有调节活性的性质的化合物的肽基 - 脯氨酰顺/反异构酶Pin1。另外，它们显示出对各种癌细胞系的抗增殖活性。因此，含有所述化合物的这些化合物和药物组合物可以用于治疗和/或预防增殖性疾病和疾病领域中的疾病或病症，例如，癌症，炎性疾病，移植排斥，病毒感染，溶骨性骨疾病，心脏疾病，心血管疾病，呼吸系统疾病，急性神经疾病，神经退行性疾病，免疫疾病和淋巴增生性泰勒氏菌病。

43. 发明申请

WO2017063754A1 CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS AS PIN1 MODULATORS 审中-公开
公开(公告)号：WO2017063754A1
公开(公告)日：2017-04-20
申请号：PCT/EP2016/025110
申请日：2016-10-12
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel , Ermert, Philipp , GOSALBES, Jean-Frangois , SHELKE, Sachin V.
IPC分类号： C07D498/18 , A61K31/429 , A61P35/00 , C07D498/04
CPC分类号： C07D498/04
摘要： Conformationally constrained macrocyclic compounds of formula (I), including substituents E, G, and Q, as defined in the description and the claims, and salts thereof, have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerases Pin1. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.

44. 发明申请

WO2015096873A1 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：WO2015096873A1
公开(公告)日：2015-07-02
申请号：PCT/EP2013/078073
申请日：2013-12-27
申请人： POLYPHOR AG
发明人： GOMBERT, Frank Otto , OBRECHT, Daniel , SELLIER-KESSLER, Odile , LEDERER, Alexander , LUDIN, Christian , SCHMITT-BILLET, Manuela , WEINBRENNER, Steffen
IPC分类号： C07K14/81
CPC分类号： C07K7/64 , A61K38/00 , C07K14/811
摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Xaa 1 -Xaa 2 -Thr 3 -Xaa 4 -Ser 5 -Xaa 6 -Xaa 7 -Xaa 8 -Xaa 9 -Xaa 10 -Xaa 11 -Xaa 12 -Xaa 13 -) and pharmaceutically acceptable salts thereof, with Xaa 1 , Xaa 2 , Xaa 4 , Xaa 6 , Xaa 7 , Xaa 8 , Xaa 9 , Xaa 10 , Xaa 11 , Xaa 12 and Xaa 13 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。

45. 发明申请

WO2014161781A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2014161781A1
公开(公告)日：2014-10-09
申请号：PCT/EP2014/056278
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[P 1 -p 2 -p 3 -p 4 -p 5 -p 6 - p 7 -p 8 .p 9 - p 10 -p 11 -p 12 -T 1 -T 2 ], a nd pharmaceutically acceptable salts thereof, with P 1 to P 12 , T 1 and T 2 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-p8.p9-p10-p11-p12-T1-T2]的β-发夹肽模拟物及其药学上可接受的盐，在P1至P12中，T1和T2是描述和权利要求中定义的元件，其具有例如革兰氏阴性的抗微生物活性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。

46. 发明申请

WO2014023766A1 COMBINATIONS WITH A BACKBONE-CYCLIZED PEPTIDE 审中-公开
标题翻译：与循环肽的组合
公开(公告)号：WO2014023766A1
公开(公告)日：2014-02-13
申请号：PCT/EP2013/066551
申请日：2013-08-07
申请人： POLYPHOR AG
发明人： DALE, Glenn E. , OBRECHT, Daniel , BERNARDINI, Francesca
IPC分类号： C07K7/64 , A61K38/12
CPC分类号： A61K38/12 , A61K31/405 , A61K31/407 , A61K31/496 , A61K31/7036 , A61K31/7052 , A61K38/00 , A61K45/06 , A61K47/6809 , C07K5/12 , C07K7/64 , A61K2300/00
摘要： A novel combination comprising a β-hairpin peptidomimetic of the formula cyclo(-Thr-Trp-Ile-Dab-Orn- D Dab-Dab-Trp-Dab-Dab-Ala-Ser- D Pro-Pro) (I), and a further compound with antibiotic activity, 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.
摘要翻译：包含式（-Thr-Trp-Ile-Dab-Orn-DDab-Dab-Trp-Dab-Dab-Ala-Ser-DPro-Pro）（I）的β-发夹肽模拟物（I）的新型组合，具有抗生素活性的化合物，其能够以比单独施用的任一化合物低的个体化合物的剂量来治疗性地控制人或动物中的特定细菌感染。该组合可以用作药物，例如治疗。皮肤或软组织感染; 眼睛，耳朵，血液或腹内感染; 与呼吸系统疾病相关的感染，骨病，心血管疾病，生殖器疾病或胃肠道疾病。

47. 发明申请

WO2022028737A1 ANTIMICROBIAL PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2022028737A1
公开(公告)日：2022-02-10
申请号：PCT/EP2021/025301
申请日：2021-08-05
申请人： POLYPHOR AG , UNIVERSITÄT ZÜRICH
发明人： OBRECHT, Daniel , LUTHER, Anatol , UPERT, Grégory , DESJONQUERES, Nicolas , BRABET, Emile , ZBINDEN, Peter , ZERBE, Oliver , MÖHLE, Kerstin
IPC分类号： C07K7/08 , C07K14/47 , A61P31/04 , A61K38/00
摘要： The present invention is directed to peptidomimetics having antibacterial activity, especially against Gram-negative bacteria. The peptidomimetics of the invention are compounds of the general formula (I), P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-P15-P16 (I) and pharmaceutically acceptable salts thereof, as described in the description and in the claims. The invention is also directed to therapeutic uses of the peptidomimetics for the treatment or prevention of bacterial infections and diseases related to bacterial infections and to non-therapeutic uses of the peptidomimetics for preserving or disinfecting foodstuffs, cosmetics, medicaments or other nutrient-containing materials. In addition, the present invention provides an efficient synthetic process by which these compounds can, if desired, be made in parallel library-format. Moreover, the peptidomimetics of the invention show improved antimicrobial activity, low or no hemolysis of red blood cells and reduced cytotoxicity.

48. 发明申请

WO2017063757A1 CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS 审中-公开
标题翻译：构象约束的大环化合物
公开(公告)号：WO2017063757A1
公开(公告)日：2017-04-20
申请号：PCT/EP2016/025114
申请日：2016-10-12
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel
IPC分类号： C07D498/18 , A61K31/429 , A61P35/00
CPC分类号： C07D498/18
摘要： Conformationally constrained macrocyclic compounds of formula (I), including substituents E with at least one ester moiety, G and Q, as defined in the description and the claims, and salts thereof, can be metabolized to compounds that have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerase Pin1. In addition, they show antiproliferative activity on various cancer cell lines. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
摘要翻译：式（I）的构象约束的大环化合物（包括具有至少一个酯部分的取代基E，如说明书和权利要求书中定义的G和Q）及其盐可以代谢为化合物其具有调节肽基 - 脯氨酰顺/反异构酶Pin1的活性的性质。另外，它们显示出对各种癌细胞系的抗增殖活性。因此，含有所述化合物的这些化合物和药物组合物可以用于治疗和/或预防增殖性疾病和疾病领域中的疾病或病症，例如，癌症，炎性疾病，移植排斥，病毒感染，溶骨性骨疾病，心脏疾病，心血管疾病，呼吸系统疾病，急性神经疾病，神经退行性疾病，免疫疾病和淋巴增生性泰勒氏菌病。

49. 发明申请

WO2017063756A1 CONFORMATIONALLY CONSTRAINED MACROCYCLIC COMPOUNDS AS PIN1 MODULATORS 审中-公开
标题翻译：构象约束的大环化合物作为PIN1调节剂
公开(公告)号：WO2017063756A1
公开(公告)日：2017-04-20
申请号：PCT/EP2016/025112
申请日：2016-10-12
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel , ERMERT, Philipp , OEFNER, Christian , GOMBERT, Frank, Otto , SHELKE, Sachin, V.
IPC分类号： C07D498/18 , A61P35/00 , A61K31/429
CPC分类号： C07D498/18
摘要： Conformationally constrained macrocyclic compounds of formula (I), including substituents E, G, and Q, as defined in the description and the claims, and salts thereof, have the property to modulate the activity of the peptidyl-prolyl cis/trans isomerases Pin1. Thus, these compounds and pharmaceutical compositions containing said compounds may be useful in the treatment and/or prevention of diseases or conditions in the area of proliferative disorders and diseases, such as e.g. cancer, inflammatory diseases, transplant rejection, viral infections, osteolytic bone diseases, cardiac diseases, cardiovascular diseases, respiratory diseases, acute neurological diseases, neurodegenerative diseases, immune disorders, and lymphoproliferative theileriosis.
摘要翻译：如说明书和权利要求书中所定义的包含取代基E，G和Q的式（I）的构象约束大环化合物及其盐具有调节肽基的活性的性质 - 脯氨酰顺/反异构酶Pin1。因此，含有所述化合物的这些化合物和药物组合物可以用于治疗和/或预防增殖性疾病和疾病领域中的疾病或病症，例如，癌症，炎性疾病，移植排斥，病毒感染，溶骨性骨疾病，心脏疾病，心血管疾病，呼吸系统疾病，急性神经疾病，神经退行性疾病，免疫疾病和淋巴增生性泰勒氏菌病。

50. 发明申请

WO2016050361A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2016050361A1
公开(公告)日：2016-04-07
申请号：PCT/EP2015/025068
申请日：2015-09-29
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , ZBINDEN, Peter , BARTHELEMY, Sophie , 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[P 1 -P 2 -P 3 -P 4 -P 5 -P 6 - P 7 -P 8 -P 9 -P 10 -P 11 -P 12 -T 1 -T 2 ] a nd pharmaceutically acceptable salts thereof, with P 1 to P 12 , T 1 and T 2 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.
摘要翻译：通式（I），环[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2]的β-发夹肽模拟物及其药学上可接受的盐， P1至P12，T1和T2是描述和权利要求中定义的元件，具有例如抗菌活性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。

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