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1. 发明申请

US20170369523A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS THAT ARE LIGANDS FOR G-PROTEIN-COUPLED RECEPTORS (GPCRS) AND ARE MODULATORS OF TRANSCRIPTION FACTORS AND COACTIVATORS 审中-公开
公开(公告)号：US20170369523A1
公开(公告)日：2017-12-28
申请号：US15701284
申请日：2017-09-11
申请人： POLYPHOR AG
发明人： John Anthony ROBINSON , Kerstin MÖHLE , Markus SEITZ , Ludovic T. MAILLARD , Roba MOUNME , Frank Otto GOMBERT , Odile SELLIER-KESSLER , Heiko HENZE , Daniel OBRECHT , Christian BISANG , Alexander LEDERER
IPC分类号： C07K1/02 , C07K7/64 , C07K7/56
CPC分类号： C07K1/02 , C07K7/56 , C07K7/64
摘要： Template-fixed β-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 β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

2. 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。

3. 发明申请

US20200317735A1 BETA-HAIRPIN PEPTIDOMIMETICS AS SELECTIVE ELASTASE INHIBITORS 审中-公开
公开(公告)号：US20200317735A1
公开(公告)日：2020-10-08
申请号：US16904920
申请日：2020-06-18
申请人： POLYPHOR AG
发明人： Frank Otto GOMBERT , Daniel OBRECHT , Odile SELLIER-KESSLER
IPC分类号： C07K7/64 , A61K38/00 , C07K1/10
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 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.

4. 发明申请

US20160318976A1 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：US20160318976A1
公开(公告)日：2016-11-03
申请号：US15107980
申请日：2013-12-27
申请人： POLYPHOR AG
发明人： Frank Otto GOMBERT , Daniel OBRECHT , Odile SELLIER-KESSLER
IPC分类号： C07K7/64 , C07K1/10
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 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疾病与健康个体中的这种感染有关或者感染患者感染减缓。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。

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