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Vithal I Patel, 8269 Jackson Ave, West Carteret, NJ 07008

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69 Jackson Ave, Carteret, NJ 07008    732-9394715   

Roselle, NJ   

Edison, NJ   

129 Hopkins Ave, Jersey City, NJ 07306    201-2220448    201-7144922   

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Us Patents

Water Soluble Orally Effective Iron Chelator

US Patent:
5834492, Nov 10, 1998
Filed:
Apr 7, 1997
Appl. No.:
8/765369
Inventors:
Neil Lewis - Plainsboro NJ
Vithal Patel - Plainsboro NJ
Jacek Terpinski - North Brunswick NJ
Robert Bliss - Edison NJ
Assignee:
Jacobus Pharmaceutical Co. - Princeton NJ
International Classification:
C07D40102
A61K 3144
US Classification:
514335
Abstract:
There is provided a synthesis and description of diprotonated diacid derivatives of pyridoxal isonicotinoyl hydrazone (PIH) of formula (I), wherein q is 1 or 2, DPA is 2 mols of a monoprotic acid HX or 1 mol of a diprotic acid H. sub. 2 Y wherein X is a monovalent anion and Y is a divalent anion and both HX and H. sub. 2 Y are pharmaceutically acceptable acids. The unique properties of the PIH. DPA molecule make it particularly suitable and pharmaceutically acceptable for formulation as an oral dosage form by virtue of its ready solubility in water. There are further provided methods of utilizing such chemically unique and isolable crystalline compounds, such as PIH. 2HCI, as a pharmaceutical chelator. There are further provided pharmaceutical formulations specifically for the reduction of iron overload, and related chelatable metals, in subjects susceptible to such overload.

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