Oregon Health & Science University

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

University of South Florida

Medicines for Malaria Venture

The United States of America

Martin J Smilkstein

Rolf W Winter

Michael Kevin Riscoe

David J Hinrichs

Jane Xu Kelly

Dennis Edward Kyle

Roman Manetsch

Aaron Nilsen

David Lawrence Flanigan

Richard Matthew Cross

Andrii Monastyrskyi

Jeremy Burrows

(A1) A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.

Acridone compounds

Compounds having antiparasitic or anti-infectious activity

A class of acridone compounds has been discovered that exhibits chemosensitizing and antiparasitic activity. Described herein are pharmaceutical compositions and methods for their use to treat parasitic infections, such as malaria and toxoplasmosis, and to sensitize resistant cells, such as multidrug resistant cells to other therapeutic agents. The pharmaceutical compositions and methods may also be used to treat and/or prevent psychotic diseases such as schizophrenia.

Aromatic ketones having an extended fluoro-alkyl or fluoro-alkoxy moiety are disclosed. In particular aspects, the compounds comprise substituted 9-acridone, 9-xanthone, 4(1H)-quinolone, 4(1H) pyridone, 1,4-naphthoquinone, 9,10-anthraquinone derivatives. These preparations possess potent pharmacological activity for inhibiting malaria and mosquito-borne () diseases. The haloalkyl/alkoxy aromatic compounds possess significant pharmacological activity, with ICvalues in the nanomolar and sub-nanomolar range, and reduced toxicity against host derived cells and tissues. Methods of using the fluoro-alkyl/alkoxy aromatic compounds in the treatment of malaria and other human and animal diseases are also disclosed. Agricultural uses of the fluoro-alkyl/alkoxy aromatic compounds, such as in control of fungal diseases and in the production of important commercial crops (apples, etc.), are also presented.

Aromatic ketones and uses thereof

Growing community of inventors

Portland, OR, United States of America

Martin J Smilkstein