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AssigneeAccess Pharmaceuticals, Inc.
InventorDavid F. Ranney
Estimating the term…
This application concerns novel agents comprising cationic or chemically basic metal chelators in association with hydrophilic carriers of anionic or chemically acidic saccharides, sulfatoids and glycosaminoglycans. In certain embodiments, the agents comprise metals and metal ions. Covalent and non-covalent chemical and physical means are described for stabilizing the binding of the metal chelators to the carriers. Novel non-covalently bound compositions are described which give uniquely high payloads and ratio of metal chelator to carrier, ranging from a low of about 15% metal chelator by weight, to a characteristic range of 70% to 90% metal chelator by weight. Specific embodiments are described comprising deferoxamine, ferrioxamine, iron-basic porphine, iron-triethylenetetraamine, gadolinium DTPA-lysine, gadolinium DOTA-lysine and gadolinium with basic derivatives of porphyrins, porphines, expanded porphyrins, Texaphyrins and sapphyrins as the basic or cationic metal chelators, which are in turn, bound to acidic or anionic carriers, including one or more of acidic or anionic saccharides, and including sulfated sucrose, pentosan polysulfate, dermatan sulfate, essentially purified dermatan sulfate with a sulfur content of up to 9% and with selective oligosaccharide oversulfation, chondroitin sulfate, oversulfated chondroitin sulfate, heparan sulfate, beef heparin, porcine heparin, non-anticoagulant heparins, and other native and modified acidic saccharides and glycosaminoglycans.
An agent comprising a metal-ion chelate, said chelate having at least one excess basic or cationic group not involved in metal-ion chelation and being bound to an anionic, hydrophilic, water-soluble glycosaminoglycan carrier with selective saccharide oversulfation and a sulfur content between about 4% (w/w) and about 9% (w/w).
An agent comprising a metal-ion chelate, said chelate having at least one excess basic or cationic group not involved in metal-ion chelation being noncovalently bound to an anionic, hydrophilic, water-soluble glycosaminoglycan carrier with selective saccharide oversulfation and a sulfur content between about 4% (w/w) and about 9% (w/w) by paired ion electrostatic binding.
An agent comprising a metal-ion chelate, said chelate having at least one excess basic or cationic group not involved in metal-ion chelation and being covalently bound to an anionic, hydrophilic, water-soluble glycosaminoglycan carrier with selective saccharide oversulfation and a sulfur content between about 4% (w/w) and about 9% (w/w).
An agent comprising a metal-ion chelate, said chelate having at least one excess basic or cationic group not involved in metal-ion chelation and being bound to essentially purified dermatan sulfate carrier with a sulfur content between about 4% (w/w) and about 9% (w/w) and with selective oligosaccharide oversulfation.
A spectral-enhancing agent to enhance images arising from induced magnetic resonance signals, the agent comprising Gd(III)diethylenetriaminepentaacetate covalently conjugated to heparin or essentially purified dermatan sulfate with a sulfur content of from about 4% to about 9% (w/w) and with selective oligosaccharide oversulfation.
An agent comprising ferrioxamine bound by non-covalent electrostatic binding to essentially purified dermatan sulfate with a sulfur content between about 4% (w/w and about 9% (w/w) and with selective oligosaccharide oversulfation.
An agent comprising N-methyl-1,3-propanediamine-DTPA bound to essentially purified dermatan sulfate with a sulfur content between about 4% (w/w) and about 9% (w/w) and with selective oligosaccharide oversulfation.
An agent comprising gadolinium (III):N-methyl-1,3-propanediamine-DTPA bound to essentially purified dermatan sulfate with a sulfur content between about 4% (w/w) and about 9% (w/w) and with selective oligosaccharide oversulfation.
Dependencies are inferred from the claim text.