Inhibition of glycosidase enzyme by forming novel complex with new or known polyamine compound, useful e.g. for treating non-insulin dependent diabetes, obesity, hyperglycemia or hyperlipidemia

摘要

The use of polyamines (or derivatives) (I) is claimed: (i) for inhibiting the active site in glycosidase (GD) enzymes participating in the conversion of polysaccharides into sugars in vivo; and (ii) in the production of a medicament for the diagnosis, prevention or treatment of diseases associated with metabolic disorders involving GD's. Independent claims are included for: (a) new complexes (II) of (I) with GD's (specifically glycosyl hydrolases, especially alpha -amylase) present in living organisms and causing the conversion/hydrolysis of oligo- and poly-saccharides into simpler sugar molecules (e.g. maltose and glucose), where (I) is fixed at the active site of GD, specifically via (preferably at least four) hydrogen bonds between positive charges (corresponding to amino functions) of (I) and carboxy functions of the aminoacid side-chains of GD; and (b) new polyamines (I') which can form the complexes (II), provided that (I') is other than spermidine, spermine or Boc-NH-(CH2)3-N(Boc)-(CH2)4-NH-CH(COOH)-(CH2)3-NH-Boc.