Oregon Health & Science University

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

University of South Florida

Interlab Inc.

Medicines for Malaria Venture

The United States of America

State of Oregon

Michael Kevin Riscoe

Rolf W Winter

David J Hinrichs

Jane Xu Kelly

Aaron Nilsen

Martin J Smilkstein

Sovitj Pou

Dennis Edward Kyle

Roman Manetsch

David Lawrence Flanigan

Richard Matthew Cross

Yuexin Li

Rozalia Dodean

Galen Miley

Jeremy Burrows

Andrii Monastyrskyi

John H Fitchen

Adolph J Ferro

Disclosed are derivative compounds of ELQ-300 that include an ester at position 4. These compounds have enhanced properties relative to ELQ-300. Also disclosed are pharmaceutical compositions comprising the compounds and methods of treating and preventing malaria infections involving administering the pharmaceutical compositions to the subject.

Quinolone-3-diarylethers

Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.

Compounds, compositions and associated methods comprising 3-aryl quinolines

(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.

A compound, particularly an antimalarial compound, according to formula I: 

Compounds for treating parasitic disease

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

Therapeutic compounds and compositions for the treatment of infectious diseases are disclosed. The compounds are xanthones and xanthone derivatives, such as 3,5-bis-&egr;-(N,N-diethylamino)amyloxyxanthone. The described compositions include such compounds and a pharmaceutical carrier. These compositions also can include additional materials conventionally used to form therapeutic compositions. 3,5-bis-&egr;-(N,N-diethylamino)amyloxyxanthone has an IC for of about 0.15 &mgr;M, and an IC for of <<0.5 &mgr;M. These compositions are additionally useful for forming soluble complexes with heme and porphyrins.

Xanthone analogs for treating infectious diseases and complexation of heme and porphyrins

Therapeutic compositions for the treatment of infectious diseases are disclosed. These compositions comprise xanthones and xanthone derivatives, such as 2,3,4,5,6-pentahydroxyxanthone. Also disclosed are methods for the treatment of infectious diseases using such compounds.

Xanthone analogs for the treatment of infectious diseases

Compounds of the formula: ##STR1## wherein R is H, Cl, F, Br, I or R.sub.1 S--, in which R.sub.1 is C.sub.1 -C.sub.10 linear or branched chain alkyl or halogenated linear or branched chain alkyl, and

Growing community of inventors

Tualatin, OR, United States of America

Michael Kevin Riscoe