Spa Societa Prodotti Antibiotici S.p.a.

Franco Ottoni

Tiberio Bruzzese

Holger H Van Den Heuvel

Ernani Dell'Acqua

Giuseppe Ghielmetti

Massino Signorini

Derivatives of partricin and of its individual components, partricin A and B, wherein the mycosamine primary amino group forms an amide bond with the carboxy group of acids containing in addition a basic nitrogen group, the carboxy group at C-18 of macrolide ring being either free or in form of ester or neutral amide or containing in the chain a basic nitrogen moiety, their pharmaceutically acceptable salts, a process for preparing the same and pharmaceutical formulations containing the same.

Partricin derivatives

The present invention is directed towards a series of secondary and tertiary amide derivatives of Partricin A & Partricin B attached at the C-18 carboxyl group. The compounds can be used in the treatment of hypercholesteremia and hyperlipemia conditions, of steroidal imbalances, and as antifungal and antiprotozoan agents.

Amide derivatives of Partricin A & Partricin B

Compounds of the following general structure (I) ##STR1## where R.sub.1 stands for an acyl radical of the following structure (II) ##STR2## where p1 X.sup.- is a halogen atom and R.sub.4 is a C.sub.1 -C.sub.4 acyl radical or a hydrogen atom

Pantothenyl derivatives

The process for the preparation of derivatives of 2-methyl-N-(2-pyridyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide of the formula ##STR1## wherein R represents hydroxy (Ia) or substituted hydroxy OR.sub.1 in which R.sub.1 is the cinnamoyl radical --CO--CH.dbd.CH--C.sub.6 H.sub.5 (Ib) consists in reacting a strong base salt of 4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxylic acid 1,1-dioxide with an acyl chloride R.sub.1 Cl, in which R.sub.1 is the cinnamoyl radical, or R.sub.2 Cl, in which R.sub.2 is an aromatic or aliphatic C.sub.2 -C.sub.6 acyl radical to give the corresponding mixed anhydride, optionally esterified at position 4, which is then reacted with 2-aminopyridine to give the desired amide.

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Pieve Emanuele, Italy

Franco Ottoni