Novel salts and polymorphs of desazadesferrothiocin polyether analogues as metal chelation agents
AssigneeFerrokin Biosciences, Inc.
InventorsAmy E. Tapper, Hugh Y. Rienhoff, JR., Stephan D. Parent, Patricia Andres, Jason A. Hanko, Huamin Zhang
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Abstract
Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.
Claims59
A solid salt of Formula I:
- wherein:
- R1, R2, R3, R4, and R5 are independently chosen from hydrogen, hydroxy, alkyl, arylalkyl, alkoxy, and CH3O((CH2)n—O)m—, any of which may be optionally substituted;
- R6, R7, and R8 are independently chosen from hydrogen, halogen, hydroxy, lower alkyl, and lower alkoxy;
- m is an integer from 0 to 8;
- n is an integer from 0 to 8;
- and
- X is a counterion;
- or a polymorph thereof.
Magnesium 3′-desazadesferrithiocin polyether hydroxide or a polymorph thereof.
Tromethamine 4′-desazadesferrithiocin polyether hydroxide, or a polymorph thereof.
A pharmaceutical composition comprising magnesium 3′-desazadesferrithiocin polyether hydroxide, or a polymorph thereof, together with at least one pharmaceutically acceptable excipient.
A pharmaceutical composition comprising tromethamine 4′-desazadesferrithiocin polyether hydroxide or a polymorph thereof, together with at least one pharmaceutically acceptable excipient.
Dependencies are inferred from the claim text.