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91. 发明授权

EP2978771B1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
公开(公告)号：EP2978771B1
公开(公告)日：2019-07-24
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

92. 发明公开

EP3201219A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
标题翻译： BETA-HAIRPIN多肽
公开(公告)号：EP3201219A1
公开(公告)日：2017-08-09
申请号：EP15778876.1
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[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.
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 到P12，T1和T2是说明书和权利要求书中定义的元素，对例如具有革兰氏阴性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。

93. 发明授权

EP2764010B9 TEMPLATE-FIXED PEPTIDOMIMETICS AS INHIBITORS OF FPR1 有权转让
标题翻译：模板 - 固定剂PEPTIDOMIMETIKA ALS INHIBITOREN VON FPR1
公开(公告)号：EP2764010B9
公开(公告)日：2017-01-18
申请号：EP12768803.4
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 &bgr;-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 &bgr;-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]的新型模板固定和模板肽模拟物 ]其中单元素T或P是沿任一方向连接的α-氨基酸残基，其取决于其在链中的位置如说明书和权利要求及其盐所定义，具有拮抗生物效应的性质的受体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。这些固体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。

94. 发明公开

EP3087094A1 BETA-HAIRPIN PEPTIDOMIMETICS AS SELECTIVE ELASTASE INHIBITORS 有权转让
标题翻译： BETA发夹肽作为选择性抑制剂，弹性蛋白酶
公开(公告)号：EP3087094A1
公开(公告)日：2016-11-02
申请号：EP13815527.0
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, Manuella , 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.

95. 发明公开

EP3087087A1 BETA-HAIRPIN PEPTIDOMIMETICS AS SELECTIVE ELASTASE INHIBITORS 有权转让
标题翻译：作为选择性ELASTASE抑制剂的β-HAIRPIN多肽
公开(公告)号：EP3087087A1
公开(公告)日：2016-11-02
申请号：EP13820780.8
申请日：2013-12-27
申请人： Polyphor Ag
发明人： GOMBERT, Frank Otto , OBRECHT, Daniel , SELLIER-KESSLER, Odile
IPC分类号： C07K7/64 , A61K38/00
CPC分类号： C07K7/64 , A61K38/00 , C07K1/10
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 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：通式为环（-Xaa1-Xaa2-Thr3-Xaa4-Ser5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13- ）及其药学上可接受的盐，其中Xaa 1，Xaa 2，Xaa 4，Xaa 6，Xaa 7，Xaa 8，Xaa 9，Xaa 10，Xaa 11，Xaa 12和Xaa 13是描述中定义的氨基酸残基和权利要求具有弹性蛋白酶抑制特性，特别是针对人类嗜中性粒细胞弹性蛋白酶，并且可以用于预防与健康个体中的这种感染相关的感染或疾病或用于减缓感染患者中的感染。本发明的化合物可以进一步用于与弹性蛋白酶活性有关的癌症或免疫性疾病或肺部疾病或心血管疾病或神经退行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液相合成策略的方法制造。

96. 发明授权

EP2764010B1 TEMPLATE-FIXED PEPTIDOMIMETICS AS INHIBITORS OF FPR1 有权转让
标题翻译：模板固定的肽AS FPR 1抑制剂
公开(公告)号：EP2764010B1
公开(公告)日：2016-03-16
申请号：EP12768803.4
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 &bgr;-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 &bgr;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

97. 发明公开

EP2978772A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
标题翻译： BETA-HAIRPIN多肽
公开(公告)号：EP2978772A1
公开(公告)日：2016-02-03
申请号：EP14713473.8
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： C07K7/64 , A61K38/12
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（P 1 -P 2 -P 3 -P 4 -P 5 -P 6 -P 7P 8P 9 -P 10 -P 11 -P 12 -T 1 -T 2]及其药学上可接受的盐，其中P 1至P 12，T 1和T 2是说明书和权利要求书中定义的元素，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微生物如肺炎克雷伯菌和/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一种方法它基于混合固相和液相合成策略。

98. 发明授权

EP2718307B1 BETA-HAIRPIN PEPTIDOMIMETICS AS CXC4 ANTAGONISTS 有权
标题翻译：与CRCX4拮抗作用BETA发夹肽
公开(公告)号：EP2718307B1
公开(公告)日：2015-08-12
申请号：EP12725829.1
申请日：2012-06-06
申请人： Polyphor AG
发明人： OBRECHT, Daniel , GOMBERT, Frank, Otto , ZIMMERMANN, Johann
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： A61K38/00 , C07K7/64

99. 发明公开

EP2882770A1 COMBINATIONS WITH A BACKBONE-CYCLIZED PEPTIDE 有权
标题翻译： KOMBINATIONEN MIT EINEM BACKBONE-CYCLIERTEN PEPTID
公开(公告)号：EP2882770A1
公开(公告)日：2015-06-17
申请号：EP13745432.8
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 , A61K31/65 , 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-lle-Dab-Orn-
D Dab-Dab-Trp-Dab-Dab-Ala-Ser-
D Pro-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.
摘要翻译：包含式（-Thr-Trp-Ile-Dab-Orn-DDab-Dab-Trp-Dab-Dab-Ala-Ser-DPro-Pro）（I）的式（b）所示肽模拟物的新型组合，和甘氨酰环霉素类的化合物，特别是替加环素，其能够以比单独施用的化合物低的单独化合物的剂量治疗控制人或动物中的特异性细菌感染。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，骨骼疾病，心血管疾病，生殖器疾病或肠胃疾病有关的感染。

100. 发明公开

EP2859012A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
标题翻译： BETA-发夹PEPTIDMIMETIKA
公开(公告)号：EP2859012A1
公开(公告)日：2015-04-15
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相和溶液相合成策略的方法制造。

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