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:
July 17, 2007
Date of Patent:
March 31, 2009
Assignees:
Schering Corporation, Pharmacopeia, Inc.
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Lawrence W. Dillard, Vinh D. Tran, Zhenmin He, Ray Anthony James, Haengsoon Park
Abstract: The present invention discloses compounds of formula I wherein Ar, Y, m, n, R1 and R4 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
Type:
Grant
Filed:
August 26, 2004
Date of Patent:
March 31, 2009
Assignee:
Schering Corporation
Inventors:
Duane A. Burnett, Wen-Lian Wu, Thavalakulamgara K. Sasikumar, William J. Greenlee, Mary Ann Caplen, Tao Guo, Rachael Catherine Hunter
Abstract: Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
Type:
Grant
Filed:
August 16, 2006
Date of Patent:
March 31, 2009
Assignee:
Schering Corporation
Inventors:
Yongqi Deng, Patrick J. Curran, Gerald W. Shipps, Jr., Lianyun Zhao, M. Arshad Siddiqui, Janeta Popovici-Muller, Jose S. Duca, Alan W. Hruza, Thierry O. Fischmann, Vincent S. Madison, Rumin Zhang, Charles W. McNemar, Todd W. Mayhood, William T. Windsor, Emma M. Lees, David A. Parry
Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine compounds as inhibitors of protein and/or Aurora kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or Aurora kinases using such compounds or pharmaceutical compositions.
Type:
Grant
Filed:
November 7, 2007
Date of Patent:
March 31, 2009
Assignee:
Schering Corporation
Inventors:
David B. Belanger, M. Arshad Siddiqui, Timothy J. Guzi, Patrick J. Curran, Praveen K. Tadikonda, Blake Hamann, Panduranga Adulla P. Reddy, Lianyun Zhao
Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 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:
May 20, 2004
Date of Patent:
March 17, 2009
Assignee:
Schering Corporation
Inventors:
Duane A. Burnett, William J. Greenlee, Brian McKittrick, Jing Su, Zhaoning Zhu, Thavalakulamgara K. Sasikumar, Robert Mazzola, Li Qiang, Yuanzan Ye
Abstract: The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is directed to pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes. Compounds of the invention generally have the structure: where the substituents are as defined herein.
Type:
Grant
Filed:
February 26, 2004
Date of Patent:
March 3, 2009
Assignee:
Schering Corporation
Inventors:
Thavalakulamgara K. Sasikumar, Wen-Lian Wu, Duane A. Burnett, Li Qiang
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 9, 2004
Date of Patent:
February 3, 2009
Assignee:
Schering Corporation
Inventors:
Francisco Velazquez, Srikanth Venkatraman, Ashok Arasappan, F. George Njoroge
Abstract: In its many embodiments, the present invention provides a novel class of compounds as illustrated below, wherein the various moieties are described herein, as inhibitors of type 3 17?-hydroxysteroid dehydrogenase, pharmaceutical compositions containing 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.
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 30, 2008
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: 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 23, 2008
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Chad Knutson, Brian McKittrick, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
Abstract: The present invention discloses compounds, which are novel receptor antagonists for NPY Y1 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y1 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
Type:
Grant
Filed:
April 28, 2005
Date of Patent:
December 2, 2008
Assignee:
Schering Corporation
Inventors:
Zhaoning Zhu, Zhong-Yue Sun, Yuanzan C. Ye, Deborra E. Mullins, Brian McKittrick, Andrew Stamford, William J. Greenlee
Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
Type:
Grant
Filed:
January 28, 2005
Date of Patent:
November 18, 2008
Assignee:
Schering Corporation
Inventors:
John W. Clader, Hubert B. Josien, Anandan Palani, Tin Yau Chan
Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine 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 29, 2005
Date of Patent:
November 18, 2008
Assignee:
Schering Corporation
Inventors:
Michael P. Dwyer, Timothy J. Guzi, Kamil Paruch, Ronald J. Doll, Kartik M. Keertikar, 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 protein and/or checkpoint kinases, methods of preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of preparing pharmaceutical formulations including one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the protein or checkpoint kinases using such compounds or pharmaceutical compositions. The invention also 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:
October 6, 2005
Date of Patent:
November 11, 2008
Assignee:
Schering Corporation
Inventors:
Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Gerald W. Shipps, Jr.
Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: useful in the treatment or prevention or amelioration of one or more symptoms of hepatitis C.
Type:
Grant
Filed:
August 24, 2004
Date of Patent:
November 11, 2008
Assignee:
Schering Corporation
Inventors:
Kevin X. Chen, F. George Njoroge, Weiying Yang, Bancha Vibulbhan, Viyyoor M. Girijavallabhan, Srikanth Venkatraman, Francisco Velazquez
Abstract: Inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
Type:
Grant
Filed:
August 16, 2006
Date of Patent:
November 4, 2008
Assignee:
Schering Corporation
Inventors:
Yongqi Deng, Lianyun Zhao, Gerald W. Shipps, Jr., Patrick J. Curran, M. Arshad Siddiqui, Rumin Zhang, Charles W. McNemar, Todd W. Mayhood, William T. Windsor, Emma M. Lees, David A. Parry
Abstract: The present invention discloses novel depeptidized compounds which have HCV protease inhibitory activity as well as pharmaceutical compositions comprising such compounds and methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
June 27, 2007
Date of Patent:
October 28, 2008
Assignee:
Schering Corporation
Inventors:
F. George Njoroge, Srikanth Venkatraman, 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:
January 31, 2005
Date of Patent:
October 7, 2008
Assignee:
Schering Corporation
Inventors:
Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams
Abstract: There are disclosed compounds of the formula (I): prodrugs thereof, or pharmaceutically acceptable salts of the compounds or of said prodrugs which are useful as inhibitors of Type 3 17?-Hydroxysteroid Dehydrogenase. Also disclosed are pharmaceutical compositions containing said compounds and their use for the treatment or prevention of androgen dependent diseases.
Type:
Grant
Filed:
November 14, 2005
Date of Patent:
October 7, 2008
Assignee:
Schering Corporation
Inventors:
Timothy Guzi, Kamil Paruch, Alan Mallams, Jocelyn D. Rivera, Ronald J. Doll, Viyyoor M. Girijavallabhan, Jonathan A. Pachter, Yi-Tsung Liu, Anil K. Saksena
Abstract: The present invention provides compounds of formula I wherein X, Y, R1-R7 are as defined herein. Compositions containing these compounds, and methods for inhibiting HCV RNA-dependent RNA polymerase and treating hepatitis C and related disorders using these compounds and compositions are also provided.
Type:
Grant
Filed:
October 26, 2005
Date of Patent:
September 16, 2008
Assignee:
Schering Corporation
Inventors:
Alan B. Cooper, Hugh Y. Zhu, James J-S Wang, Jagdish A. Desai, Gerald W. Shipps, Jr., Patrick J. Curran, D. Allen Annis, Huw M. Nash, Viyyoor M. Girijavallabhan