Nicholas G Bacopoulos

US Patent:

7148257, Dec 12, 2006

Filed:

Aug 26, 2003

Appl. No.:

10/650025

Inventors:

Nicholas G. Bacopoulos - New York NY, US
Judy H. Chiao - Berkeley Heights NJ, US
Thomas A. Miller - New York NY, US
Carolyn M. Paradise - Cortland Manor NY, US
Victoria M. Richon - Rye NY, US

Assignee:

Merck HDAC Research, LLC - Boston MA
Sloan-Kettering Institute for Cancer Research - New York NY

International Classification:

A61K 31/165

US Classification:

514616

Abstract:

Methods for treating mesothelioma comprising administering the histone deacetylase inhibitor suberoylanilide hydroxamic acid (SAHA) are disclosed.

US Patent:

7375137, May 20, 2008

Filed:

Mar 28, 2006

Appl. No.:

11/391971

Inventors:

Nicholas G. Bacopoulos - New York NY, US
Judy H. Chiao - Berkeley Heights NJ, US
Thomas A. Miller - New York NY, US
Carolyn M. Paradise - Cortland Manor NY, US
Victoria M. Richon - Rye NY, US

Assignee:

Merck HDAC Research, LLC - Boston MA

International Classification:

A61K 31/165

US Classification:

514616

Abstract:

The present invention provides methods of treating cancers, chemoprevention, selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

US Patent:

7399787, Jul 15, 2008

Filed:

Jul 9, 2003

Appl. No.:

10/616649

Inventors:

Judy H. Chiao - Berkeley Heights NJ, US
Nicholas G. Bacopoulos - New York NY, US
Thomas A. Miller - New York NY, US
Carolyn M. Paradise - Cortland Manor NY, US
Victoria M. Richon - Rye NY, US

Assignee:

Merck HDAC Research, LLC - Boston MA

International Classification:

A61K 31/19

US Classification:

514575

Abstract:

The present invention provides methods of treating cancers, chemoprevention, selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

US Patent:

20040127523, Jul 1, 2004

Filed:

Sep 16, 2003

Appl. No.:

10/665079

Inventors:

Nicholas Bacopoulos - New York NY, US
Judy Chiao - Berkeley Heights NJ, US
Thomas Miller - New York NY, US
Carolyn Paradise - Cortland Manor NY, US
Victoria Richon - Rye NY, US

International Classification:

A61K031/44
A61K031/19

US Classification:

514/352000, 514/575000

Abstract:

The present invention relates to methods of treating cancers, e.g., lymphoma. More specifically, the present invention relates to methods of treating diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

US Patent:

20040132825, Jul 8, 2004

Filed:

Oct 24, 2003

Appl. No.:

10/692523

Inventors:

Nicholas Bacopoulos - New York NY, US
Judy Chiao - Berkeley Heights NJ, US
Thomas Miller - New York NY, US
Carolyn Paradise - Cortland Manor NY, US
Victoria Richon - Rye NY, US

International Classification:

A61K031/19

US Classification:

514/575000

Abstract:

The present invention relates to methods of treating cancers, e.g., leukemia. More specifically, the present invention relates to methods of treating acute and chronic leukemias including Acute Lymphocytic Leukemia (ALL), Acute Myeloid Leukemia (AML), Chronic Lymphocytic leukemia (CLL), Chronic myeloid leukemia (CML) and Hairy Cell Leukemia, by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

US Patent:

20060276547, Dec 7, 2006

Filed:

Jul 24, 2006

Appl. No.:

11/492478

Inventors:

Nicholas Bacopoulos - New York NY, US
Judy Chiao - Berkeley Heights NJ, US
Thomas Miller - New York NY, US
Carolyn Paradise - Cortland Manor NY, US
Victoria Richon - Rye NY, US

International Classification:

A61K 31/19
A61K 38/12

US Classification:

514575000, 514009000

Abstract:

The present invention relates to methods of treating cancers, e.g., lymphoma. More specifically, the present invention relates to methods of treating diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

US Patent:

20070060614, Mar 15, 2007

Filed:

Aug 26, 2004

Appl. No.:

10/567952

Inventors:

Nicholas Bacopoulos - New York NY, US
Judy Chiao - Berkeley Heights NJ, US
Thomas Miller - New York NY, US
Carolyn Paradise - Cortland Manor NY, US
Victoria Richon - Rye NY, US

International Classification:

A61K 31/445
A61K 31/44
A61K 31/426
A61K 31/19

US Classification:

514315000, 514352000, 514365000, 514575000

Abstract:

The present invention relates to methods of treating cancers, e.g., mesothelioma or lymphoma. More specifically, the present invention relates to methods of treating mesothelioma or diffuse large B-cell lymphoma (DLBCL), by administration of pharmaceutical compositions comprising HDAC inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The oral formulations of the pharmaceutical compositions have favorable pharmacokinetic profiles such as high bioavailability and surprisingly give rise to high blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.

US Patent:

20070190022, Aug 16, 2007

Filed:

Aug 12, 2004

Appl. No.:

10/567953

Inventors:

Nicholas Bacopoulos - Stonington CT, US
Judy Chiao - Berkeley Heights NJ, US
Paul Marks - Washington CT, US
Thomas Miller - Brookline MA, US
Carolyn Paradise - Cortland Manor NY, US
Victoria Richon - Wellesley MA, US
Richard Rifkind - New York NY, US

International Classification:

A61K 38/20
A61K 38/19
A61K 38/09
A61K 31/7072
A61K 31/57
A61K 31/522
A61K 31/19

US Classification:

424085100, 514015000, 424085200, 424155100, 514575000, 514049000, 514251000, 514263310, 424094630, 514269000, 514254070, 514102000, 514171000

Abstract:

The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor or a pharmaceutically acceptable salt or hydrate thereof, in a first treatment procedure, and a second amount of an anti-cancer agent in a second treatment procedure. The first and second amounts together comprise a therapeutically effective amount. The effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic.