Abstract: Boron-based prodrugs of phenol- or aromatic hydroxyl group-containing therapeutic molecules (“original drugs”), uses thereof, and methods of making the same, are provided for achieving, for example, improved bioavailability, prolonged retention (e.g., in a circulatory system) and, in particular, significantly lowered therapeutically effective dosage in order to reduce adverse effects while maintaining the desired therapeutic effects of the original drugs.
Abstract: A method of combating infectious agents, such as Pneumocystis pneumonia, and a method of treating a subject in need of such treatment is disclosed. The method comprises administering to the subject a bis-benzamidoxime of formula I wherein the linker is a di-substituted cyclic moiety of any ring size and may contain at least one heteroatom; the aromatic group is 1,2-; 1,3-; or 1,4-disubstituted; R is selected from the group consisting of a hydrogen, a linear or branched alkyl group, containing from 1 to 20 carbon atoms; R? is selected from the group consisting of a hydrogen, a linear or branched alkyl group containing from one to twenty carbon atoms, an aromatic ring, a cycloalkyl group containing three to eight carbon atoms, or a hydroxyl group; alternatively, R and R? may form a cyclic structure that can be fused to another cyclic system; or a pharmaceutically acceptable salt thereof. Pharmaceutical formulations and active compounds useful in the practice of the present invention are also disclosed.
Type:
Grant
Filed:
March 17, 2011
Date of Patent:
December 16, 2014
Assignees:
University of Cincinnati, Xavier University
Inventors:
Peter D. Walzer, Melanie T. Cushion, Annie Mayence, Tien Liang Huang, Jean Jacques Vanden Eynde