公开(公告)号：US10730911B2

公开(公告)日：2020-08-04

申请号：US15564539

申请日：2016-04-06

申请人： POLYPHOR AG ,  Universität Zürich

发明人： Daniel Obrecht ,  Christian Bisang ,  Anatol Luther ,  Steffen Weinbrenner ,  John Anthony Robinson ,  Kerstin Moehle ,  Christian Steuer ,  William J. Drury, III

IPC分类号： A61K38/08 ,  A61K38/12 ,  C07K7/54 ,  C07K7/64 ,  C07K14/72 ,  A61K38/02 ,  C07K1/04 ,  C07K14/00 ,  C07K14/47 ,  C07K14/655 ,  C07K14/705 ,  C40B50/14 ,  A61K38/00

摘要： Novel backbone-cyclized peptidomimetics of the general formula cyclo[-P1-P2-P3-P4-P5-P6-P7-P8-T1-T2-]   (I) 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 to modulate the GLP-1 receptor. They can be used as medicaments to treat, prevent, or delay the onset of diseases, disorders or conditions in which modulation of the human GLP-1 receptor is beneficial, such as type 2 diabetes. These backbone-cyclized peptidomimetics can be manufactured by a process which is based on a mixed solid—and solution phase synthetic strategy.

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.