Technologies

Pharmaceuticals & Vitamin D

Most Recent Inventions

New Hormone Analogs for Treating Hypoparathyroidism

UW–Madison researchers have developed backbone-modified analogs of PTH(1-34). The analogs exhibit advantageous properties; they are biased toward Gs activation/cAMP production relative to β arrestin recruitment.

The analogs were generated via an unconventional strategy in which the backbone of a natural PTHR-1 agonist was altered, rather than the side-chain complement. More specifically, selected α-amino acid residues were systemically replaced with either β-amino acid residues or with unnatural D-stereoisomer α-amino acid residues.

The researchers have shown that backbone-modification can rapidly identify potent agonists with divergent receptor-state selectivity patterns relative to a prototype peptide.
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Novel Inhibitors of Pseudomonas aeruginosa Quorum Sensing

UW–Madison researchers led by Prof. Helen Blackwell have developed novel inhibitors of LasR, a quorum sensing receptor, in P. aeruginosa. The compounds are analogs of V-06-018, an inhibitor described in the scientific literature in 2006. The potency and efficacy of the compounds – measured by IC50 and maximum inhibition, respectively – were determined to exceed the parent molecule and are the most potent inhibitors of their kind reported to date.
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Nylon-3 Polymers to Treat Fungal Infections

UW–Madison researchers have found that nylon-3 polymers developed in their lab display potent antifungal activity against a broad spectrum of common fungal pathogens, with minimal toxicity towards mammalian cells. The polymers have some activity alone, and when used in combination with existing drugs provide synergistic effects against Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus strains, including some resistant strains.

Synergistic combination offers efficacy with significantly reduced amounts of drug and corresponding toxicity, which could potentially expand the relevant patient population.

The polymers were designed to resemble host-defense peptides (HDPs), which are natural molecules that exhibit antimicrobial activities.
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Analogs of Diptoindonesin G for Breast Cancer Drug Development

UW–Madison researchers have synthesized analogs of Dip G that have shown a greater ability than the parent molecule to decrease ERα expression and stabilize ERβ in cultured breast cancer cells. The compounds are active for ameliorating, attenuating and halting the growth/metastasis of breast cancers.
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Efficient In Vitro Assay for Antigen-Specific Tolerance

Building on their work, UW–Madison researchers have now developed a T cell-bound cytokine (T-CBC) assay for detecting and quantifying regulatory T cells specific to self-antigens or donor alloantigens. The new method comprises (a) culturing the subject’s T cells for 24 hours in the presence of one or more target antigens and (b) analyzing the cultured T cells for expression of a marker (EBi3; TGFβ/LAP) indicative of antigen-specific immune suppression.
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Most Recent Patents

New Compounds for Treating High Blood Cholesterol and More

UW–Madison researchers have now developed a method using a rhodium-containing catalyst to make indole compounds, specifically cyclopropyl indoles and cyclohepta[b] indoles. The compounds may be developed into new pharmaceuticals to treat a variety of conditions.
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Generic Drug to Treat and Prevent Macular Degenerative Diseases

UW–Madison researchers have identified a new treatment option for a number of macular degenerative diseases including AMD, Stargardt’s disease and juvenile macular dystrophy.

The researchers found that a class of compounds called acid sphingomyelinase inhibitors can be used to fight retinal disorders associated with abnormal accumulations of lipofuscin (a cellular waste product), cholesterol or increased inflammation. One such inhibitor, generic name desipramine, is currently sold on the market as an antidepressant. Other acid sphingomyelinase inhibitors also may be suitable.
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New and More Potent UGM Inhibitors for Treating Tuberculosis, Other Microbial Infections

UW–Madison researchers have developed a new set of UGM inhibitors to fight tuberculosis and other diseases caused by microbial infections. The compounds feature an N-acylsulfonamide motif and are more potent in vitro than inhibitors previously identified by the researchers.
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