Gruppo Lepetit

Biosearch Italia S.p.a.

Alessandra Maria Marazzi

Gianbattista Panzone

Adriano Malabarba

Romeo Ciabatti

Anacleto Gianantonio

Ermenegildo Restelli

Improved chemical process for preparing the compounds of formula (I), wherein: R,represents (C,-C,)alkyl; M represents hydrogen, &agr;-D-mannopyranosyl or 6-O-acetyl-&agr;-D-mannopyranosyl and Y represents an amino group of formula &mdash;NR,-alk,-(NR,-alk,),-(NR,-alk,),-W. One aspect of the invention refers to the preparation of the intermediate compound of formula (III) (which corresponds to the above compound of formula (I)

Chemical process for preparing amide derivatives of antibiotic A 40926

The present invention is directed to novel antibiotic A 40926 derivatives characterized by having a carboxy, (C.sub.1 -C.sub.4) alkoxy-carbonyl, aminocarbonyl, (C.sub.1 -C.sub.4) alkylaminocarbonyl, di (C.sub.4 -C.sub.4)alkylaminocarbonyl or hydroxymethyl substituent on the N-acylaminoglucuronyl moiety and a hydroxy or a polyamine substituent in position 63 of the molecule. The compounds of the invention show high in vitro activity against glycopeptide resistant Enterococci and Staphylococci.

Amide derivatives of antibiotic A 40926

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Saronno, Italy

Alessandra Maria Marazzi