University of South Florida

Medicines for Malaria Venture

The Penn State Research Foundation

The United States Government As Represented by the Department of Veterans Affairs

Northeastern University

Oregon Health & Science University

H. Lee Moffitt Cancer Center and Research Institute, Inc.

Roman Manetsch

Dennis Edward Kyle

David Lawrence Flanigan

Lindsey Neil Shaw

Richard Matthew Cross

Whittney Burda

Kurt Steven Van Horn

Rolf W Winter

Michael Kevin Riscoe

David J Hinrichs

Jane Xu Kelly

Aaron Nilsen

Martin J Smilkstein

Hong-Gang Wang

Megan M Barber

Alexis Nichole LaCrue

Jeremiah Dwayne Tipton

Jeremy Burrows

Andrii Monastyrskyi

Niranjan Kumar Namelikonda

Jordany Richarlson Maignan

Katya Pavlova Nacheva

Arun Babu Kumar

Renee Marie Fleeman

Raghupathi Neelarapu

Gloria C Ferreira

Cynthia L Lichorowic

Kenichiro Doi

Tina Susanna Mutka

Fabian Ernesto Saenz

Iredia David Iyamu

Xiangdong Hu

Sameer Kulkarni

Sameer Shamrao Kulkarni

Jiazhi Sun

Bosko M Stojanovski

Disclosed herein, are 5-Aminolevulinate synthase inhibitors and methods for their use in the treatment of. In at least one specific embodiment, the 5-Aminolevulinate synthase inhibitors can include compounds or salts thereof of Formulas (I-V) 

5-aminolevulinate synthase inhibitors and methods of use thereof

Methods of identifying target binding molecules by target guided synthesis are provided. The methods include providing two or more fragments capable of reacting to form the target binding molecule and mixing the fragments with the target. The methods can be used to identify target binding molecules that bind targets such as proteins or nucleic acids, including those that bind shallow binding pockets on the surface of such targets. The methods are applied to the Bcl-XL and Mcl-1 proteins from the Bcl-2 family of proteins. Using thio acid and sulfonyl azide fragments capable of reacting through sulfo-click chemistry, new acyl sulfonamides are identified that bind one or both of the Bcl-XL and Mcl-1 proteins. Pharmaceutical formulations of these target binding molecules are also provided.

Target binding molecules identified by kinetic target-guided synthesis

Described herein are quinazoline-based compounds and formulations thereof. In some embodiments, the compounds and/or formulations thereof can be effective to inhibit and/or kill. Also described herein are methods of treating a subject in need thereof by administering to the subject in need thereof a quinazoline-based compound and/or formulation thereof to the subject in need thereof.

[object Object]

Embodiments of the present disclosure, in one aspect, relate to a 2,4-diaminoquinazoline compound, pharmaceutical compositions including a 2,4-diaminoquinazoline compound, methods of treatment of a condition (e.g., infection) or disease, methods of treatment using compositions or pharmaceutical compositions, and the like.

Compositions, methods of use, and methods of treatment

Provided herein are pyridyl- and pyrimidyl-containing diazirines that can be photoactivateable probes and formulations thereof. Also provided herein are photoaffinity labels that can include the pyridyl- and pyrimidyl-containing diazirines provided herein. Also provided herein are methods of using the photoactivatable probes and photoaffinity labels provided herein in a photoaffinity labeling reaction and/or assay.

Photoactivatable probes and uses thereof

Provided herein are quinolone-based compounds that can be used for treatment and/or prevention of malaria and formulations thereof. Also provided herein are methods of treating and/or preventing malaria in a subject by administering a quinolone-based compound or formulation thereof provided herein.

Quinolone-based compounds, formulations, and uses thereof

Compounds having antiparasitic or anti-infectious activity

Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of ainfection in the recipient subject, or to reduce the likelihood of the onset or establishment of ainfection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.

4(1H)-quinolones having antimalarial activity with reduced chemical resistance

The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.

Acylsulfonamides and processes for producing the same

Growing community of inventors

Tampa, FL, United States of America

Roman Manetsch