Back to results
US 2003/0158125 A1Published application
Polysaccharidic esters of n-derivatives of glutamic acid
AssigneeEurand Pharmaceuticals Ltd.
InventorsGiuliana Miglierini, Luca Stucchi, Alessandro Rastrelli
Life of this patent
Estimating the term…
Abstract
The present invention is related to polysaccharide esters of N-derivatives of glutamic acid (N-GA derivatives). These polysaccharidic esters have antiproliferative activity and are characterized by a low systemic toxicity. The esters of the invention are used in the prevention and therapy of diseases caused by cellular hyperproliferation, particularly psoriasis, tumors, rheumatoid arthritis, or intestinal inflammatory pathologies.
Claims33
Polysaccharidic ester of the compound of formula (I)
- 3
- wherein:
- R2 and R4 independent from one another, are selected in the group consisting of:
- —NH2, —OH, —OCH3, C1-C5 alkyl, ═O and the 6-membered ring containing the two nitrogen atoms is optionally aromatic;
- X and Y are selected in the group consisting of:
- —C(R5)═, —CH(R5)—, —NH—, —N═, wherein R5 represents:
- —H, C1-C5 alkyl, and the ring including X and Y is optionally aromatic;
- Z is selected in the group consisting of:
- —O—, —CH(R10)—, —N(R10)—, wherein R10 represents —H, C1-C5 alkyl, C1-C5 alkenyl, C1-C5 alkynyl, 5-6 membered heterocyclic ring with 1-3 heteroatoms selected in the group consisting of nitrogen, sulphur and oxygen.
- Ar is 1,4phenyl, possibly condensed with one or more 5-6-membered aromatic rings, optionally heterocycles, optionally substituted with R2 as defined above;
- characterized in that only the primary hydroxy groups present on the monosaccharid units of the polysaccharide are either partially or totally esterified with the γ-carboxylic group of the compounds of formula (I).
8 more elements
Dependencies are inferred from the claim text.