The University of Arizona

University of Texas System

Eugene A Mash

Garth Powis

Daruka Mahadevan

Shuxing Zhang

Emmanuelle J Meuillet

Vijay Gokhale

Pawel R Kiela

Robert J Gillies

David L Morse

Gary V Martinez

Parastou Foroutan

Fayez K Ghishan

Bhumasamudram Jagadish

Vijay M Gohkale

Suryakiran Navath

Vijay M Gokhale

The present invention provides a nitroreductase-releasable pro-drug of the formula: where Ar, m, n, Z, Y, L, and A are as defined herein, and methods for using and producing the same. Compound of formula I is useful in oral administration of the active pharmaceutical ingredient to the distal gut region of a subject to treat a wide variety of clinical conditions associated with distal gut region of a subject, such as colorectal cancer, inflammatory bowel disease (IBD), infectious diarrhea, bacterial infections, and bacterial overgrowth.

Nitroreductase-releasable pro-drugs and methods for using the same

Disclosed is CT or MR contrast agent which comprises a base or carrier scaffold formed of a polyhydroxol compound having a linker to which a Gd-DOTA is covalently bonded. Also disclosed is a method of screening a patient for colon cancer using a CT or MR contrast, which method comprises administering to a patient undergoing screening a compound as above described.

Method and compositions for orally administered contrast agents for MR imaging

The present invention provides a process for nitrating aromatic compounds without the need for a solid catalyst and/or any organic solvents and/or any other additives. A typical process includes combining or admixing a nitric acid and an anhydride compound under conditions sufficient to produce a reactive intermediate. The aromatic compound to be nitrated is then added to this reactive intermediate to produce a nitroaromatic compound. The nitroaromatic compound can be substituted with one or more, typically, one to three, and often one or two nitrate (&#x2014;NO) groups.

Nitration of aromatic compounds

A composition and method for targeted delivery of substances to the lower GI tract comprises a base or scaffold carrier to which a drug or prodrug is fixed or covalently attached. Compound, when taken orally travels through the GI tract of a patient to the lower GI where bacterial azo reductace enzymes cleave the bonds, releasing the drug or prodrug from the base or scaffold carrier permitting the delivery of the drug to the vicinity of a target cell type in the GI tract. The base or scaffold, which remains as a by-product passes out of the GI tract in the feces.

Method and compositions for targeted drug delivery to the lower GI tract

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.

Small molecule inhibitors of the pleckstrin homology domain and methods for using same

Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein. 

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Tucson, AZ, United States of America

Eugene A Mash