Sophie Barthélémy,Christian Bisang,Frank Otto Gombert,Alexander Lederer,Daniel Obrecht,Barbara Romagnoli,Jürg Zumbrunn,Tobias Remus,Guillaume Lemercier
申请号:
US13513550
公开号:
US08716242B2
申请日:
2009.12.04
申请国别(地区):
US
年份:
2014
代理人:
摘要:
β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), and pharmaceutically acceptable salts thereof, with Xaa 1-Xaa 16 being amino acid residues of certain types which are defined in the description 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.