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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.

Patent No.:

US 9096559 B1

PDFFull Text
Date of Patent:
Aug. 04, 2015

Filed:

Jan. 28, 2013

4-carboxybenzylamino derivatives as histone deacetylase inhibitors

Applicants:

Paul Harrington, Camarillo, CA (US);

Richard W. Heidebrecht, Jr., Somerville, MA (US);

Solomon Kattar, Wakefield, MA (US);

Thomas A. Miller, Wakefield, MA (US);

Karin M. Otte, Natick, MA (US);

Phieng Siliphaivanh, Newton Highland, MA (US);

Matthew G. Stanton, Marlton, NJ (US);

Paul Tempest, Shanghai, CN;

Kevin J. Wilson, Newton, MA (US);

David J. Witter, Norfolk, MA (US);

Inventors:

Paul Harrington, Camarillo, CA (US);

Richard W. Heidebrecht, Jr., Somerville, MA (US);

Solomon Kattar, Wakefield, MA (US);

Thomas A. Miller, Wakefield, MA (US);

Karin M. Otte, Natick, MA (US);

Phieng Siliphaivanh, Newton Highland, MA (US);

Matthew G. Stanton, Marlton, NJ (US);

Paul Tempest, Shanghai, CN;

Kevin J. Wilson, Newton, MA (US);

David J. Witter, Norfolk, MA (US);

Assignee:

Merck Sharp & Dohme Corp., Rahway, NJ (US);

Attorneys:

Richard S. Parr

Laura M. Ginkel

Primary Examiner:

Samira Jean-Louis

Int. Cl.
CPC ...
C07D 333/10 (2006.01); C07C 235/76 (2006.01); C07C 235/84 (2006.01); C07D 295/155 (2006.01); C07C 237/40 (2006.01); C07C 237/42 (2006.01); C07C 271/22 (2006.01); C07C 271/38 (2006.01); C07C 271/54 (2006.01); C07D 207/08 (2006.01); C07D 207/14 (2006.01); C07D 207/16 (2006.01); C07D 209/44 (2006.01); C07D 209/48 (2006.01); C07D 211/14 (2006.01); C07D 213/30 (2006.01); C07D 213/38 (2006.01); C07D 213/40 (2006.01); C07D 213/56 (2006.01); C07D 213/74 (2006.01); C07D 217/04 (2006.01); C07D 231/12 (2006.01); C07D 233/64 (2006.01); C07D 241/12 (2006.01); C07D 263/20 (2006.01); C07D 277/28 (2006.01); C07D 295/125 (2006.01); C07D 307/22 (2006.01); C07D 333/20 (2006.01); C07D 401/04 (2006.01); C07D 409/12 (2006.01); C07D 413/12 (2006.01); C07D 213/55 (2006.01);
U.S. Cl.
CPC ...
C07D 295/155 (2013.01); C07C 237/40 (2013.01); C07C 237/42 (2013.01); C07C 271/22 (2013.01); C07C 271/38 (2013.01); C07C 271/54 (2013.01); C07D 207/08 (2013.01); C07D 207/14 (2013.01); C07D 207/16 (2013.01); C07D 209/44 (2013.01); C07D 209/48 (2013.01); C07D 211/14 (2013.01); C07D 213/30 (2013.01); C07D 213/38 (2013.01); C07D 213/40 (2013.01); C07D 213/55 (2013.01); C07D 213/56 (2013.01); C07D 213/74 (2013.01); C07D 217/04 (2013.01); C07D 231/12 (2013.01); C07D 233/64 (2013.01); C07D 241/12 (2013.01); C07D 263/20 (2013.01); C07D 277/28 (2013.01); C07D 295/125 (2013.01); C07D 307/22 (2013.01); C07D 333/10 (2013.01); C07D 333/20 (2013.01); C07D 401/04 (2013.01); C07D 409/12 (2013.01); C07D 413/12 (2013.01); C07C 2101/02 (2013.01); C07C 2101/04 (2013.01); C07C 2101/08 (2013.01); C07C 2101/14 (2013.01);
Abstract

The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino 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 4-carboxybenzylamino derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the 4-carboxybenzylamino derivatives in vivo.

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