The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jul. 24, 2012

Filed:

Apr. 05, 2005
Applicants:

Thomas A. Miller, New York, NY (US);

David J. Witter, Putnam Valley, NY (US);

Sandro Belvedere, New York, NY (US);

Inventors:

Thomas A. Miller, New York, NY (US);

David J. Witter, Putnam Valley, NY (US);

Sandro Belvedere, New York, NY (US);

Assignee:

Merck HDAC Research, LLC, Boston, MA (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07C 69/02 (2006.01); A61K 31/22 (2006.01);
U.S. Cl.
CPC ...
Abstract

The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (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.


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