Massachusetts Institute of Technology

The United States of America, As Represented by the Secretary, Department of Health and Human Services

Harvard College

The Broad Institute, Inc.

Mitsubishi Tanabe Pharma Corporation

Tanabe Seiyaku Company, Limited

Marshall Morningstar

John M Essigmann

Ila Sircar

Kevin J Yarema

Robert G Croy

Nicholas D Smith

Bradley Teegarden

Christopher J Michejda

Ronald Griffith

Eamon Comer

Nobutaka Kato

Paul Furth

Bruno Melillo

Thomas Roth

Takayuki Kawaguchi

Masatoshi Kakushima

Toshiyuki Kume

Hidefumi Kaji

Provided herein are compounds useful for the treatment of various parasitic diseases. These compounds, as well as pharmaceutically acceptable salts thereof may be formulated in pharmaceutical compostions, veterinary compositions and may be used in methods of treatment and/or prophylaxis of diseases spread by parasites, including malaria and cryptosporidiosis.

Compounds and methods for the treatment of parasitic diseases

The present invention relates to a compound of formula (I): wherein R is hydrogen atom, hydroxyl group or carbamoyl group, and n is 1 or 2, or a pharmaceutically acceptable salt thereof. 

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The present invention relates to a compound of the following formula: or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of preparing and using the compounds. The compounds of the invention are useful in treating &#x3b1;&#x3b2;adhesion mediated conditions in a mammal.

The compositions and methods disclosed herein provide heterobifunctional programmable genotoxic compounds that can be designed to kill selected cells present in a heterogenous cell population. The present compounds comprise a first agent that inflicts damage on cellular DNA, and a second agent that attracts a macromolecular cell component such as a protein, which in turn shields genomic lesions from repair. Unrepaired lesions therefore persist in the cellular genome and contribute to the death of selected cells. In contrast, lesions formed in nonselected cells, which lack the cell component, are unshielded and thus are repaired. As a result, compounds described herein are less toxic to nonselected cells. Compounds of this invention can be designed to cause the selective killing of transformed cells, viral-infected cells and the like.

Programmable genotoxic agents and uses therefor

The present invention relates to a compound of the following formula:or a pharmaceutically acceptable salt thereof. Also disclosed are compositions containing the compound and methods of preparing and using the compounds. The compounds of the invention are useful in treating &#x3b1;&#x3b2;adhesion mediated conditions in a mammal.

Inhibitors of &#x3b1;L&#x3b2;2 mediated cell adhesion

The present invention provides compositions and methods for the treatment of HIV infection. In particular, the present invention provides non-nucleoside inhibitors of reverse transcriptase (RT), as well as methods to treat HIV infection using these non-nucleoside inhibitors of RT. In preferred embodiments, the present invention provides a novel class of substituted benzimidazoles, effective in the inhibition of human immunodeficiency virus (HIV) RT.

Substituted benzimidazoles as non-nucleoside inhibitors of reverse transcriptase

Substituted benzimidazoles, and methods of use thereof, for the inhibition of HIV reverse transcription and for the treatment of HIV infection

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San Diego, CA, United States of America

Marshall Morningstar