Scaffolds useful to the synthesis of compounds with biological activity

摘要

Cyclic compounds of formula (I) having an azabicycloalkane structure are useful as intermediates for the synthesis of compounds with biological activity. [wherein: the symbol represents a bond above or below the plane of the page, n is the number 1 or 2, m is an integer from 1 to 5, X is OH, N3, NH2, or COOH; and R<1> is H, C1-C4 alkyl or a suitable protecting group and R<2> is H or a suitable protecting group; or a salt thereof; or racemates, single enantiomers, single diastereoisomers or mixtures of such compounds and/or of such salts] Cyclic peptides of formula (I) are claimed wherein R<1> and R<2> together are a peptide sequence, with the RGD sequence -Asp-Gly-Arg- being particularly preferred. The latter are selective antagonists for a v b 3 and/or a v b 5 integrins, and are useful for the treatment of an altered angiogenesis, or for the treatment of tumor metastasis, retinopathy, acute kidney failure or osteoporosis. The above compounds may be used as carriers for the selective delivery of drugs, the carried drug being linked by a chemical bond, eg one formed by reaction of the drug with group X. They may also be used as reverse-turn inducers.