abstract |
beta-hairpin peptidomimetics of the general formula cyclo (-Xaa-Xaa-Thr-Xaa-Ser-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-Xaa-) and their pharmaceutically acceptable salts, wherein Xaa, Xaa, Xaa, Xaa , Xaa, Xaa, Xaa, Xaa, Xaa, Xaa and Xaa are amino acid residues as defined in the description and in the claims that have inhibitory properties against elastase, especially against human neutrophilic elastase, and can be used to prevent infections or diseases associated with with such infections in healthy subjects, or to reduce infections in infected patients. The compounds of the invention can also be used when cancer, or immunological diseases, or lung diseases, or cardiovascular diseases, or neurodegenerative diseases, or inflammation, or diseases associated with inflammation, are mediated or result from elastase activity. These peptidomimetics can be obtained by a method that is based on a mixed strategy of solid phase synthesis and solution synthesis. |