Joshua Close - Franklin MA, US Jonathan Grimm - Newton MA, US Solomon Kattar - Arlington MA, US Thomas A. Miller - Brookline MA, US Karin M. Otte - Newton Center MA, US Scott Peterson - Somerville MA, US Phieng Siliphaivanh - Brookline MA, US Paul J. Tempest - Brookline MA, US Kevin J. Wilson - West Newton MA, US David J. Witter - Norfolk MA, US
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.
Richard Heidebrecht - Brookline MA, US Joey Methot - Westwood MA, US Dawn Mampreian - Boston MA, US Thomas Miller - Brookline MA, US Phieng Siliphaivanh - Newton MA, US
The present invention relates to a novel class of disubstituted aniline compounds. These compounds can 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 compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
Jonathan Grimm - Newton MA, US Paul Harrington - Camarillo CA, US Richard Heidebrecht, Jr. - Brookline MA, US Thomas Miller - Brookline MA, US Karin Otte - Newton Center MA, US Phieng Siliphaivanh - Brookline MA, US David Sloman - Boston MA, US Matthew Stanton - Medfield MA, US Kevin Wilson - West Newton MA, US David Witter - Norfolk MA, US Solomon Kattar - Arlington MA, US Paul Tempest - Brookline MA, US
The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate 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 modified malonate derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the modified malonate derivatives in vivo.
Jonathan B. Grimm - Newton MA, US Jed L. Hubbs - Cambridge MA, US Thomas Miller - Brookline MA, US Karin M. Otte - Newton Centre MA, US Phieng Siliphaivanh - Newton MA, US Matthew G. Stanton - Medfield MA, US Kevin Wilson - West Newton MA, US David Witter - Norfolk MA, US Hua Zhou - Waltham MA, US
Assignee:
Merck Sharp & Dohme Corp. - Rahway NJ
International Classification:
A61K 31/4412 C07D 409/12
US Classification:
514336, 5462804
Abstract:
The present invention relates to a novel class of compounds. These compounds can 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 compounds of the instant invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of these compounds in vivo.
Cycloalkyl-Fused Tetrahydroquinolines As Crthreceptor Modulators
Xianhai Huang - Warren NJ, US Jason Brubaker - Cambridge MA, US Scott L. Peterson - Salem MA, US John W. Butcher - Berlin MA, US Joshua T. Close - Franklin MA, US Michelle Martinez - Medford MA, US Rachel Nicola MacCoss - Oxford, GB Joon O. Jung - Newton MA, US Phieng Siliphaivanh - Newton MA, US Hongjun Zhang - Newton MA, US Robert G. Aslanian - Rockaway NJ, US Purakkattle Johny Biju - Piscataway NJ, US Li Dong - Roselle Park NJ, US Ying Huang - Berkeley Heights NJ, US Kevin D. McCormick - Basking Ridge NJ, US Anandan Palani - Bridgewater NJ, US Ning Shao - Watchung NJ, US Wei Zhou - Scotch Plains NJ, US
Jed Lee Hubbs - Cambridge MA, US Sam Kattar - Medford MA, US Joey Methot - Boston MA, US Thomas Miller - Brookline MA, US Phieng Siliphaivanh - Brookline MA, US Matthew Stanton - Medfield MA, US Kevin Wilson - West Newton MA, US David J. Witter - Norfolk MA, US
The present invention relates to a novel class of hydroxamic acid derivatives. The hydroxamic acid compounds can be used to treat cancer. The hydroxamic acid 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 are also 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 hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.
Jed Lee Hubbs - Cambridge MA, US Dawn M. Mampreian - Boston MA, US Joey L. Methot - Boston MA, US Thomas A. Miller - Brookline MA, US Karin M. Otte - Newton Center MA, US Phieng Siliphaivanh - Brookline MA, US David L. Sloman - Boston MA, US Matthew G. Stanton - Medfield MA, US Kevin J. Wilson - West Newton MA, US David J. Witter - Norfolk MA, US
The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide 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 hydroxamic acid derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the hydroxamic acid derivatives in vivo.
N-Hydroxy-Naphthalene Dicarboxamide And N-Hydroxy-Biphenyl-Dicarboxamide Compounds As Histone Deacetylase Inhibitors
Solomon Kattar - Arlington MA, US Thomas A. Miller - Brookline MA, US Karin M. Otte - Natick MA, US Phieng Siliphaivanh - Newton MA, US Laura Surdi - Natick MA, US Paul Tempest - Brookline MA, US Anna A. Zabierek - Salem MA, US
The present invention relates to a novel class of N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide compounds can be used to treat cancer. The N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide 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 N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the N-hydroxy-naphthalene dicarboxamide and N-hydroxy-biphenyl-dicarboxamide derivatives in vivo.