Gruppo Lepetit S.p.a.

Vicuron Pharmaceuticals Inc.

Merrell Dow Pharmaceuticals

Naicons S.c.a.r.l.

Adriano Malabarba

Bruno Cavalleri

Paolo Strazzolini

Romeo Ciabatti

Carolina Coronelli

Angelo Borghi

Aldo Trani

Giorgio Tarzia

Ambrogio Magni

Pietro Ferrari

Giorgio Mosconi

Daniela Jabes

Marco Cavaleri

Jurgen K Kettenring

Martin Stogniew

Timothy Henkel

Richard J White

Gianbattista Panzone

Pierfausto Seneci

Alessandra Maria Marazzi

Gabriela Romano

J Urgen Kettenring

Use of the compound of formula (I) and the pharmaceutically acceptable addition salts thereof for the manufacture of a medicament for topical treatment or 5 prevention of acne formula (I) wherein: R represents methoxymethyl, R1 represents methyl, Rz represents methyl, Y represents the group formula (II) The compound of formula (I) and the pharmaceutically acid addition salts thereof show selective activity againstand are suitable for use in a method of treatment or prevention of acne. 

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The invention provides methods and compositions for treatment of bacterial infections. Methods of the invention include administration of dalbavancin for treatment of a bacterial infection, in particular a Gram-positive bacterial infection of skin and soft tissue. Dosing regimes include once weekly administration of dalbavancin, which often remains at therapeutic levels in the bloodstream for at least one week, providing prolonged therapeutic action against a bacterial infection.

Stable pharmaceutical compositions of dalbavancin and methods of administration

Methods of administering dalbavancin for treatment of bacterial infections

The present invention is directed to novel 38-decarboxy-38-hydroxymethyl derivatives of teicoplanin antiobiotics and a process for preparing them which includes submitted the corresponding lower alkyl ester precursor to a reduction reaction in the presence of an alkali metal borohydride. The compounds of the invention show an improved antibacterial activity against some clinical isolates of Staphylococci somewhat resistant to teicoplanin. The teicoplanin derivatives of the present invention are represented by the following formula: ##STR1## wherein: X represents hydroxymethyl;

38-decarboxy-38-hydroxymethyl derivatives of teiocoplanin antibiotics

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

Tetrapeptides of general formula (I) deriving from dalbaheptide antibiotics ##STR1## wherein: W and Z represent the relative portions of the aglycon of an antibiotic of the dalbaheptide group (aglucodalbaheptides);

Tetrapeptides deriving from dalbaheptide antibiotics

Synthetic aglucodalbaheptide antibiotics

Pentapeptide antibiotics of the formula ##STR1## wherein W, Z, X.sub.1, X.sub.2 and T represent the relative portions of an antibiotic of the dalbaheptide group (glyccpeptide antibiotics), Y represents a carboxyacid group, a functional derivative of said carboxyacid group or a hydroxymethyl group. The invention includes the salts of the above represented pentapeptide antibiotics with acids or bases as well as their inner salts. The compounds are obtained by reductive cleavage of the peptidic bond between the second and the third aminoacid of the seven aminoacid chain of dalbaheptides (glycopeptide antibiotics). The inventions concerns also the reductive cleavage process which implies using an alkali metal borohydride as the reagent. The compounds show antibacterial activity against staphylococcal and streptococcal strains.

Pentapeptide antibiotics

Pentapeptide antibiotics of the formula ##STR1## wherein W, Z, X.sub.1, X.sub.2 and T represent the relative portions of an antibiotic of the dalbaheptide group (glycopeptide antibiotics), Y represents a carboxyacid group, a functional derivative of a carboxyacid group or a hydroxymethyl group. The invention includes the salts of the above represented pentapeptide antibiotics with acids or bases as well as their inner salts.

The present invention is directed to an amide derivative of the glycopeptide, teicoplanin. This compound is an antibiotic that is active against gram positive bacteria. This compound is produced by subjecting teicoplanin to an amidation reaction.

Amides of teicoplanin compounds

The present invention is directed to new C.sup.63 amide derivatives of teicoplanin wherein the amide moiety is derived from a di- or poly-alkylamine, and to a process for preparing them. The derivatives are prepared by reacting a teicoplanin-like product with an active ester forming reagent such as chloroacetonitrile and then contacting said active ester with the appropriate di- or poly-alkylamine. The amide derivatives of the invention are active against gram positive and gram negative bacteria.

Substituted alkylamide derivatives of teicoplanin

Hexapeptides of formula (I) deriving from aglucoteicoplanin and their salts with acids and bases as well as their inner salts wherein R is hydrogen or a protecting ##STR1## group of the amino function. The products of formula (I), wherein R is hydrogen, possess antimicrobial activity in particular against coagulase-negative strains and some S. aureus and S. epidermidis strains which have low sensitivity toward teicoplanin. The hexapeptides are produced by reductive cleavage of aglucoteicoplanin with alkali metal borohydrides in the presence of a hydroalcoholic mixture as solvent.

Hexapeptides deriving from aglucoteicoplanin and a process for preparing

The present invention is directed to teicoplanin derivatives in which position 63 of the glycopeptide core is substituted with a substituted alkylamide.

Substituted alkylamides of teicoplanin compounds

C.sup.63 -Amide derivatives of 34-de(acetylglucosaminyl)-34-deoxy-teicoplanin wherein the amide moiety is derived from a di- or poly-amine. The derivatives are prepared by reacting 34-de(acetylglucosaminyl)- 34-deoxy-teicoplanins with an active esters forming reagent such as chloroacetonitrile and then contacting the resulting active esters with the appropriate di- or poly-amine. The amide derivatives which are active against Gram-positive microorganisms, in particular against Group A Streptococci were found to be active also against bacteria which are resistant to glycopeptide antibiotics.

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Binasco, Italy

Adriano Malabarba