DEMARCO, STEVEN J.,MUKHERJEE, RESHMI,MOEHLE, KERSTIN,ROBINSON, JOHN ANTHONY,HENZE, HEIKO,ROMAGNOLI, BARBARA,OBRECHT, DANIEL,GOMBERT, FRANK,LUDIN, CHRISTIAN,VRIJBLOED, JAN WIM
申请号:
CA2679414
公开号:
CA2679414C
申请日:
2007.02.28
申请国别(地区):
CA
年份:
2014
代理人:
摘要:
The template-fixed ß-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro- Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, 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 fromCXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or, in particular, for stem cell mobilisation of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These .beta.-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.