Merck Sharp + Dohme Corp.

Paul J Tempest

Thomas Allen Miller

David James Witter

Kevin J Wilson

Phieng Siliphaivanh

Joshua Close

Solomon D Kattar

Jonathan B Grimm

Scott Peterson

Richard W Heidebrecht, Jr

Karin M Otte

The present invention relates to a novel class of phosphorus derivatives. The phosphorus compounds can be used to treat cancer. The phosphorus compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases. The present invention further provides pharmaceutical compositions comprising the phosphorus derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the phosphorus derivatives in vivo.

Phosphorus derivatives as histone deacetylase inhibitors

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Brookline, MA, United States of America

Paul J Tempest