ZUMBRUNN, JUERG,DEMARCO, STEVEN J.,MUKHERJEE, RESHMI,MOEHLE, KERSTIN,ROBINSON, JOHN ANTHONY,HENZE, HEIKO,ROMAGNOLI, BARBARA,LOCIURO, SERGIO,VRIJBLOED, JAN WIM,GOMBERT, FRANK,OBRECHT, DANIEL,LUDIN, CHR
申请号:
CA2524253
公开号:
CA2524253C
申请日:
2004.04.29
申请国别(地区):
CA
年份:
2016
代理人:
摘要:
Template-fixed .beta.-hairpin peptidomimetics of the general formula (I)wherein Z is a template-fixed chain of 12, 14 or 18 .alpha.-amino acidresidues which, depending on their positions in the chain (counted startingfrom the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, or of certaintypes which, as the remaining symbols in the above formula, are defined in thedescription and the claims, and salts thereof, have CXCR4 antagonizingproperties and can be used for preventing HIV infections in healthyindividuals or for slowing and halting viral progression in infected patients;or where cancer is mediated or resulting from CXCR4 receptor activity; orwhere immunological diseases are mediated or resulting from CXCR4 receptoractivity; or for treating immuno suppression; or during apheresis collectionsof peripheral blood stem cells. These .beta.-hairpin peptidornimetics can bemanufactured by a process which is based on a mixed solid- and solution phasesynthetic strategy.