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US 5,296,597 AGranted
Amide derivatives of Partricin A & Partricin B
AssigneeSPA-Societa Prodotti Antibiotici S.p.A.
InventorsTiberio Bruzzese, Franco Ottoni, Giuseppe Ghielmetti
Life of this patent
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Abstract
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.
Claims25
A compound of the formula ##STR2## wherein:
- R is the residue of partricin A or partricin B molecule, which is bound to the C-18 carboxyl;
- R.sub.1 is a dimethylamino-substituted cyclohexyl or phenyl group;
- or an alkyl group with 1 to 6 carbon atoms substituted with an N-methyl- or N-ethyl-cycloalkyleneamine with 4 to 5 carbon atoms, with a pyridyl group or with a primary amine group NH.sub.2, a secondary amine group NHR.sub.3 or a tertiary amine group NR.sub.3 R.sub.4, wherein R.sub.3 and R.sub.4 are alkyl groups with 1 to 4 carbon atoms, or NR.sub.3 R.sub.4 together form a basic nitrogen heterocycle, said heterocycle being 5- or 6-membered and optionally containing one or more further heteroatoms chosen from N or O or S;
- R.sub.2 is a hydrogen atom, a methyl group, or has the same meanings as R.sub.1 ;
- or
- NR.sub.1 R.sub.2 together form a basic nitrogen heterocycle, said heterocycle being 5- or 6-membered and optionally containing one or more further N atoms;
- n is an integer of from 0 to 2,
- X is the residue of a pharmacologically and pharmaceutically acceptable organic or inorganic acid.
5 more elements
Dependencies are inferred from the claim text.