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:
October 5, 2010
Assignee:
Schering Corporation
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
Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.
Type:
Grant
Filed:
February 14, 2006
Date of Patent:
July 27, 2010
Assignee:
Schering Corporation
Inventors:
Wensheng Yu, Seong Heon Kim, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Bandarpalle B. Shankar, Brian F. McGuinness, Douglas W. Hobbs, Yuefei Shao
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:
October 3, 2006
Date of Patent:
July 20, 2010
Assignee:
Schering Corporation
Inventors:
Srikanth Venkatraman, F. George Njoroge, Melissa L. Blackman, Wanil Wu, Latha G. Nair, Ashok Arasappan, Stephane L. Bogen, Kevin X. Chen, Mousumi Sannigrahi, Frank Bennett, Viyyor 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:
October 3, 2006
Date of Patent:
May 18, 2010
Assignee:
Schering Corporation
Inventors:
Srikanth Venkatraman, F. George Njoroge, Melissa L. Blackman, Wanil Wu, Latha G. Nair, Ashok Arasappan, Stephane L. Bogen, Kevin X. Chen, Mousumi Sannigrahi, Frank Bennett, Viyyor M. Girijavallabhan
Abstract: The use of CCR3 antagonists of the formula I or a pharmaceutically acceptable salt thereof for the treatment of asthma is disclosed, as well as novel compounds of the formula II, pharmaceutical compositions comprising them, and their use in the treatment of asthma, wherein R, Ra, X, Xa, R1, R2, R2a, R14, R14a, R16 and n are as defined in the specification.
Type:
Grant
Filed:
February 2, 2005
Date of Patent:
April 27, 2010
Assignee:
Schering Corporation
Inventors:
Pauline C. Ting, Jianhua Cao, Youhao Dong, Eric J. Gilbert, Ying Huang, Joseph M. Kelly, Stuart McCombie, Neng-Yang Shih
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.
Type:
Grant
Filed:
October 4, 2006
Date of Patent:
January 12, 2010
Assignee:
Schering Corporation
Inventors:
Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer
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.
Type:
Grant
Filed:
October 4, 2006
Date of Patent:
January 5, 2010
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:
December 22, 2009
Assignee:
Schering Corporation
Inventors:
Stephane L. Bogen, Weidong Pan, Sumie Ruan, F. George Njoroge
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:
November 20, 2006
Date of Patent:
November 17, 2009
Assignee:
Schering Corporation
Inventors:
Kevin X Chen, F George Njoroge, Mousumi Sannigrahi, Latha G Nair, Weiying Yang, Bancha Vibulbhan, Srikanth Venkatraman, Ashok Arasappan, Stephane L. Bogen, Frank Bennett, Viyyoor M. Girijavallabhan
Abstract: In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), 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 4, 2006
Date of Patent:
October 20, 2009
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc Labroli, Kartik M. Keertikar
Abstract: In its many embodiments, the present invention provides a class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), 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 4, 2006
Date of Patent:
October 13, 2009
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer
Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.
Type:
Grant
Filed:
October 20, 2005
Date of Patent:
October 6, 2009
Assignee:
Schering Corporation
Inventors:
Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
Abstract: The present invention discloses novel 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. The novel compounds typically include a 15-20 member macrocycle and have the general structure of structural Formula 1: wherein Z?, L?, M?, R1, X and D are defined herein.
Type:
Grant
Filed:
September 23, 2004
Date of Patent:
September 22, 2009
Assignee:
Schering Corporation
Inventors:
Srikanth Venkatraman, F. George Njoroge, Wanli Wu, Viyyoor M. Girijavallabhan, Brian McKittrick, Jing Su, Francisco Velazquez, Patrick A. Pinto
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:
March 6, 2007
Date of Patent:
September 22, 2009
Assignee:
Schering Corporation
Inventors:
F. George Njoroge, Ashok Arasappan, Srikanth Venkatraman, Stephane L. Bogen, Kevin X. Chen, Frank Bennett
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:
November 10, 2005
Date of Patent:
August 18, 2009
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Lianyun Zhao, Patrick J. Curran, David B. Belanger, Blake Hamann, Panduranga A. Reddy, M. Arshad Siddiqui
Abstract: In its many embodiments, the present invention provides a class of pyrazolo [1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases (CDKs), 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 4, 2006
Date of Patent:
July 21, 2009
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, M. Arshad Siddiqui, Panduranga Adulla P. Reddy, David B. Belanger, Blake Hamann, Patrick J. Curran
Abstract: In its many embodiments, the present invention provides a novel class of imidazopyrazine 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.
Type:
Grant
Filed:
June 5, 2007
Date of Patent:
July 7, 2009
Assignee:
Schering Corporation
Inventors:
Lianyun Zhao, Panduranga Adulla P. Reddy, Neng-Yang Shih, Kamil Paruch, Timothy J. Guzi, M. Arshad Siddiqui
Abstract: The present invention discloses compounds of Formula I wherein V, W, Y, Z, R1, R2, R3, R4, d, m, n, p and r 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:
October 11, 2005
Date of Patent:
June 23, 2009
Assignee:
Schering Corporation
Inventors:
Tao Guo, Huizhong Gu, Douglas Walsh Hobbs
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:
August 25, 2005
Date of Patent:
June 23, 2009
Assignee:
Schering Corporation
Inventors:
Mousumi Sannigrahi, 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:
March 31, 2006
Date of Patent:
April 7, 2009
Assignees:
Schering Corporation, Pharmacopeia, Inc.
Inventors:
Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Carmen S. Alvarez, Tin Yau Chan, Chad Knutson, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park