Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
December 21, 2006
Date of Patent:
September 16, 2008
Assignee:
Schering Corporation
Inventors:
Ashok Arasappan, F. George Njoroge, Angela I. Padilla-Acevedo, Kevin X. Chen, Frank Bennett, Mousumi Sannigrahi, Stephane L. Bogen, Srikanth Venkatraman, Edwin E. Jao, Anil K. Saksena, Viyyoor M. Girijavallabhan
Abstract: The present invention provides compounds, which, are novel antagonists for D1 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
Type:
Grant
Filed:
December 21, 2004
Date of Patent:
September 9, 2008
Assignee:
Schering Corporation
Inventors:
Duane A. Burnett, Wen-Lian Wu, Martin S. Domalski, Mary Ann Caplen, Richard Spring, Jean E. Lachowicz
Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
December 21, 2006
Date of Patent:
September 9, 2008
Assignee:
Schering Corporation
Inventors:
Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
May 18, 2005
Date of Patent:
July 15, 2008
Assignee:
Schering Corporation
Inventors:
Ashok Arasappan, F. George Njoroge, Viyyoor M. Girijavallabhan
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the kinases using such compounds or pharmaceutical compositions.
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
March 31, 2006
Date of Patent:
December 18, 2007
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
Abstract: The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.
Type:
Grant
Filed:
August 24, 2005
Date of Patent:
December 18, 2007
Assignee:
Schering Corporation
Inventors:
Andrew Stamford, Youhao Dong, Stuart W. McCombie, Yusheng Wu
Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17?-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17?-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
February 23, 2006
Date of Patent:
September 18, 2007
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Yi-Tsung Liu, Ronald J. Doll, Anil Saksena, Viyyoor Girijavallabhan, Jonathan A. Pachter
Abstract: The present invention provides a method for identifying a member of a mass-coded combinatorial library which is a ligand for biomolecule and assessing the effect of the binding of the ligand to the biomolecule. The mass-coded molecular library comprises compounds of the general formula XYn, wherein n is an integer from 2 to about 6, X is a scaffold and each Y is, independently, a peripheral moiety. The mass-coded combinatorial library is produced by reacting a scaffold precursor with a sufficient number of distant peripheral moiety precursors such that there exist at least about 250 distinct combinations of n peripheral moieties derived from the peripheral moiety precursors.
Type:
Grant
Filed:
March 11, 2003
Date of Patent:
September 11, 2007
Assignee:
Schering Corporation
Inventors:
Huw M. Nash, Seth Birnbaum, Edward A. Wintner, Krishna Kalghatgi, Gerald Shipps, Satish Jindal
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
October 6, 2005
Date of Patent:
April 17, 2007
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer
Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
February 24, 2005
Date of Patent:
April 17, 2007
Assignee:
Schering Corporation
Inventors:
Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
October 6, 2005
Date of Patent:
March 27, 2007
Assignee:
Schering Corpoartion
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc Labroli, Kartik M. Keertikar
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
October 6, 2005
Date of Patent:
March 27, 2007
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer
Abstract: The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.
Type:
Grant
Filed:
June 2, 2003
Date of Patent:
March 27, 2007
Assignee:
Schering Corporation
Inventors:
Gerald W. Shipps, Kristin E. Rosner, Janet Popovici-Muller, Yongqi Deng, Tong Wang, Patrick J. Curran
Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
February 24, 2005
Date of Patent:
March 20, 2007
Assignee:
Schering Corporation
Inventors:
Srikanth Venkatraman, F. George Njoroge, Melissa L. Blackman, Wanli Wu, Latha G. Nair, Ashok Arasappan, Stephane L. Bogen, Kevin X. Chen, Mousumi Sannigrahi, Frank Bennett, Viyyoor M. Girijavallabhan
Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
February 24, 2005
Date of Patent:
March 6, 2007
Assignee:
Schering Corporation
Inventors:
Ashok Arasappan, F. George Njoroge, Angela I. Padilla-Acevedo, Kevin X. Chen, Frank Bennett, Mousumi Sannigrahi, Stephane L. Bogen, Srikanth Venkatraman, Edwin Jao, Anil K. Saksena, Viyyoor M. Girijavallabhan
Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a] pyrazine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
September 19, 2003
Date of Patent:
March 6, 2007
Assignee:
Schering Corporation
Inventors:
Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan
Abstract: Methods for identifying a member of a mass-coded molecular library, which is a ligand for a biomolecule and binds to the biomolecule at the binding site of a known second ligand for the biomolecule are described. The methods includes contacting a mass-coded molecular library with a biomolecule; separating the biomolecule-ligand complexes from the unbound members of the mass-coded molecular library; contacting the biomolecule-ligand complexes with a second ligand to dissociate biomolecule-ligand complexes in which the ligand binds to the biomolecule at the binding site of the second ligand, thereby forming biomolecule-second ligand complexes and dissociated ligands; separating the dissociated ligands and biomolecule-second ligand complexes; and determining the molecular mass of each dissociated ligand.
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]triazine compounds as inhibitors of kinases such as, for example, cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the kinases using such compounds or pharmaceutical compositions.
Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
September 3, 2003
Date of Patent:
January 9, 2007
Assignees:
Schering Corporation, Pharmacopeia Drug Discovery, Inc.
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin-Yau Chan, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Paradkar, Douglas Walsh Hobbs