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1. 发明申请

WO2010015287A2 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定的多形性
公开(公告)号：WO2010015287A2
公开(公告)日：2010-02-11
申请号：PCT/EP2008/060494
申请日：2008-08-08
申请人： POLYPHOR AG , UNIVERSITÄT ZÜRICH , ROBINSON, John Anthony , MÖHLE, Kerstin , SEITZ, Markus , MAILLARD, Ludovic T. , MOUNME, Roba , GOMBERT, Frank Otto , SELLIER-KESSLER, Odile , HENZE, Heiko , OBRECHT, Daniel , BISANG, Christian , LEDERER, Alexander
发明人： ROBINSON, John Anthony , MÖHLE, Kerstin , SEITZ, Markus , MAILLARD, Ludovic T. , MOUNME, Roba , GOMBERT, Frank Otto , SELLIER-KESSLER, Odile , HENZE, Heiko , OBRECHT, Daniel , BISANG, Christian , LEDERER, Alexander
CPC分类号： C07K1/02 , C07K7/56 , C07K7/64
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) 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 GIy 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.
摘要翻译：通式（I）的模板固定的β-发夹肽模拟物，其中Z是8个α-氨基酸残基的模板固定链，取决于它们在链中的位置（从 N-末端氨基酸）是Gly或Pro或某些类型的化合物，作为上式中剩余的符号，如说明书和权利要求书中所定义的，及其盐具有对抗尾加压素II的激动或拮抗活性或显示抑制STAT6 / NCoA-1相互作用，并可用于预防或治疗与尾加压素II，STAT6和NCoA-1相关的疾病或病症。这些β-发夹肽模拟物可以通过基于混合固相和液相合成策略的方法来制造。

2. 发明授权

EP2324047B1 Template-fixed peptidomimetics 有权
标题翻译：在支架固定肽
公开(公告)号：EP2324047B1
公开(公告)日：2015-02-25
申请号：EP08787073.9
申请日：2008-08-08
申请人： Polyphor AG , Universität Zürich
发明人： ROBINSON, John Anthony , MÖHLE, Kerstin , SEITZ, Markus , MAILLARD, Ludovic T. , MOUNME, Roba , GOMBERT, Frank Otto , SELLIER-KESSLER, Odile , HENZE, Heiko , OBRECHT, Daniel , BISANG, Christian , LEDERER, Alexander
IPC分类号： C07K7/56 , C07K7/64 , C07K1/02
CPC分类号： C07K1/02 , C07K7/56 , C07K7/64
摘要： Template-fixed &bgr;-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 &bgr;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

3. 发明公开

EP2324047A2 TEMPLATE-FIXED PEPTIDOMIMETICS 有权
标题翻译：在支架固定肽
公开(公告)号：EP2324047A2
公开(公告)日：2011-05-25
申请号：EP08787073.9
申请日：2008-08-08
申请人： Polyphor Ag , Universität Zürich
发明人： ROBINSON, John Anthony , MÖHLE, Kerstin , SEITZ, Markus , MAILLARD, Ludovic T. , MOUNME, Roba , GOMBERT, Frank Otto , SELLIER-KESSLER, Odile , HENZE, Heiko , OBRECHT, Daniel , BISANG, Christian , LEDERER, Alexander
IPC分类号： C07K7/56 , C07K7/64 , C07K1/02
CPC分类号： C07K1/02 , C07K7/56 , C07K7/64
摘要： Template-fixed &bgr;-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 &bgr;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

4. 发明申请

WO2010127704A1 BETA-HAIRPIN PEPTIDOMIMETICS HAVING CXCR4 ANTAGONIZING ACTIVITY 审中-公开
标题翻译：具有CXCR4拮抗活性的BETA-HAIRPIN PEPTIDOMIMETICS
公开(公告)号：WO2010127704A1
公开(公告)日：2010-11-11
申请号：PCT/EP2009/055563
申请日：2009-05-07
申请人： POLYPHOR AG , OBRECHT, Daniel , GOMBERT, Frank, Otto , LEDERER, Alexander , ROMAGNOLI, Barbara , BISANG, Christian
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： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa 1 -Xaa 2 -Xaa 3 -Cys 4 -Xaa 5 -Xaa 6 -Xaa 7 -Xaa 8 -Arg 9 -Tyr 10 -Cys 11 - Xaa 12 -Xaa 13 -Xaa 14 -Xaa 15 -Xaa 16 -), disulfide bond between Cys 4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa 1 , Xaa 2 , Xaa 3 , Xaa 5 , Xaa 6 , Xaa 7 , Xaa 8 , Xaa 12 , Xaa 13 , Xaa 14 , Xaa 15 and Xaa 16 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： ß-通式为（Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的发夹肽模拟物，Cys4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拮抗性，可用于预防健康个体的艾滋病毒感染，或用于缓解和停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。

5. 发明申请

WO2016150576A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2016150576A1
公开(公告)日：2016-09-29
申请号：PCT/EP2016/025027
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： Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, T, Q., and optionally L 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 and/or Pseudomonas aeruginosa . They ca n 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-发夹肽模拟物及其药学上可接受的盐与P，T，Q和任选的L是说明书和权利要求书中定义的元素，其具有革兰氏阴性的抗微生物活性。抑制生长或杀死肺炎克雷伯菌和/或鲍氏不动杆菌和/或大肠杆菌和/或铜绿假单胞菌的微生物。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造。

6. 发明申请

WO2011066869A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
标题翻译： BETA-HAIRPIN PEPTIDMIMETICS
公开(公告)号：WO2011066869A1
公开(公告)日：2011-06-09
申请号：PCT/EP2009/066462
申请日：2009-12-04
申请人： POLYPHOR AG , BARTHÉLÉMY, Sophie , BISANG, Christian , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZUMBRUNN, Jürg , REMUS, Tobias , LEMERCIER, Guillaume
发明人： BARTHÉLÉMY, Sophie , BISANG, Christian , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZUMBRUNN, Jürg , REMUS, Tobias , LEMERCIER, Guillaume
IPC分类号： C07K7/64 , C07K1/04 , A61K38/00
CPC分类号： C07K7/08 , A61K38/00 , C07K7/64
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa 1 -Xaa 2 -Xaa 3 -Xaa 4 -Xaa 5 -Xaa 6 -Xaa 7 -Xaa 8 -Xaa 9 -Xaa 10 -Xaa 11 - Xaa 12 -Xaa 13 -Xaa 14 -Xaa 15 -Xaa 16 -), and pharmaceutically acceptable salts thereof, with Xaa 1 -Xaa 16 being amino acid residues of certain types which are defined in thedescription and the claims, have CXCR4 antagonizing properties and prolonged half-lives in vivo 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： ß-通式为Cyclo（-Xaa1 -Xaa2 -Xaa3 -Xaa4 -Xaa5 -Xaa6 -Xaa7 -Xaa8 -Xaa9 -Xaa10 -Xaa11 -Xaa12 -Xaa13 -Xaa14 -Xaa15 -Xaa16 - ）的发夹肽模拟物及其药学上可接受的盐，Xaa 1 -Xaa 16是在描述和权利要求书中定义的某些类型的氨基酸残基，具有CXCR4拮抗性质和体内延长的半衰期，并且可用于预防健康个体的HIV感染或减缓和停止感染患者病毒进展; 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。

7. 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。

8. 发明申请

WO2011095607A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 审中-公开
标题翻译：具有CXCR7调节活性的模板固定化肽
公开(公告)号：WO2011095607A1
公开(公告)日：2011-08-11
申请号：PCT/EP2011/051686
申请日：2011-02-04
申请人： POLYPHOR AG , GOMBERT, Frank, Otto , LEDERER, Alexander , LÖWE, Ralf , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZIMMERMANN, Johann , PATEL, Kalpana
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
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 mobilisation of stem cells.
摘要翻译：通式（I）的新型模板固定的β-发夹肽模拟物，其中单个元件T或P是从下述的羰基（C = O）连接点连接到氮（N）的α-氨基酸残基元件，并且其中所述元件取决于它们在链中的位置在描述中定义，并且权利要求具有作用于受体CXCR7的性质。因此，这些β-发夹肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经疾病，心血管疾病，呼吸系统疾病，胃肠道疾病或疾病泌尿系疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。

9. 发明申请

WO2011095220A1 TEMPLATE - FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 审中-公开
标题翻译：模板 - 具有CXCR7调节活性的固定肽
公开(公告)号：WO2011095220A1
公开(公告)日：2011-08-11
申请号：PCT/EP2010/051440
申请日：2010-02-05
申请人： POLYPHOR AG , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , BISANG, Christian , LUDIN, Christian
发明人： GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , BISANG, Christian , LUDIN, Christian
IPC分类号： A61K38/12 , C07K7/64 , C07K14/72
CPC分类号： C07K7/64 , A61K38/00
摘要： Specific 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 mobilisation of stem cells.
摘要翻译：通式（I）的具体的模板固定的β-发夹肽模拟物，其中单个元件T或P是从连接的羰基（C = O）连接到下一元素的氮（N）连接的α-氨基酸残基顺时针方向，并且其中所述元件取决于它们在链中的位置在描述中定义，并且权利要求具有作用于受体CXCR7的性质。因此，这些β-发夹肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经疾病，心血管疾病，呼吸系统疾病，胃肠道疾病或疾病泌尿系疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。

10. 发明申请

WO2016050360A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2016050360A1
公开(公告)日：2016-04-07
申请号：PCT/EP2015/025067
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[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 ], and 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 Gramegative 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-P-P-P-P-P-P9-P10-P-P-P2-T1-T2] P1至P12，T1和T2是说明书和权利要求书中定义的元件，具有例如抗抑郁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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