POLYMER CONJUGATES OF DRUGS WITH CENTRAL NERVOUS SYSTEM (CNS) EFFECTS AND PERIPHERAL NMDAR BLOCKING ACTIVITY AND/OR IMMUNE SYSTEM MODULATING EFFECTS

The present invention discolses novel molecules consisting of N-methyl-D-aspartate receptor (NMDAR) antagonists-polymer conjugates having a general structure D-(X-Poly-T)n, wherein D is an high affinity, i.e., (+)-, (-)-, or (±)-dizocilpine, or a low affinity, i.e., (+)-, (-)-, or (±)-methadone, CNS...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: COMAI, Stefano, MANFREDI, Paolo L, MATTAREI, Andrea, PASUT, Gianfranco, BANZATO, Marco, INTURRISI, Charles E, DE MARTIN, Sara
Format: Patent
Sprache:eng
Schlagworte:
Online-Zugang:Volltext bestellen
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:The present invention discolses novel molecules consisting of N-methyl-D-aspartate receptor (NMDAR) antagonists-polymer conjugates having a general structure D-(X-Poly-T)n, wherein D is an high affinity, i.e., (+)-, (-)-, or (±)-dizocilpine, or a low affinity, i.e., (+)-, (-)-, or (±)-methadone, CNS active NMDAR antagonist, n is an integer comprised between 1 and 6. X is a stable (enzymatically and/or hydrolytically under physiological conditions) linker comprising a covalent bond or a chain of atoms that covalently attaches a small molecule NMDAR antagonist drug moiety to the Poly derivative. Poly is a covalently bonded chain of repeating monomer units that form a polymer or an oligomer backbone of synthetic or natural origin. T, if present, is either another molecule of D, or a terminal group of Poly, represented by any suitable chemical group which, depending upon preference, is unreactive or reactive with other chemical moieties, or has a targeting property.