Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-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 17, 2003
Date of Patent:
December 19, 2006
Assignee:
Schering Corporation
Inventors:
Michael P. Dwyer, Timothy J. Guzi, Kamil Paruch, Ronald J. Doll, Kartik M. Keertikar, Viyyoor M. Girijavallabhan
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:
January 28, 2005
Date of Patent:
November 21, 2006
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Kamil Paruch, Alan K. Mallams, Jocelyn D. Rivera, Ronald J. Doll, Viyyoor M. Girijavallabhan, Jonathan A. Pachter, Yi-Tsung Liu, Anil K. Saksena
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:
February 11, 2004
Date of Patent:
October 10, 2006
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. Hobbs, Douglas Walsh Hobbs
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:
August 1, 2006
Assignees:
Schering Corporation, Pharmacopeia Drug Discovery, Inc.
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: 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:
July 18, 2006
Assignees:
Schering Corporation, Pharmacopeia Drug Discovery, Inc.
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:
September 3, 2003
Date of Patent:
July 11, 2006
Assignees:
Schering Corporation, Pharmacopeia Drug Discovery, Inc.
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 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. In one embodiment, the present invention discloses a compound having the general structure shown in Formula I: wherein the various moieties are as defined herein.
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:
June 27, 2006
Assignees:
Schering Corporation, Pharmacopeia Drug Discovery, 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
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 one embodiment, this invention provides a novel class of compounds as antagonists of the MCH receptor, methods of preparing such compounds, pharmaceutical compositions containing one or more of the compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention or amelioration or one or more of diseases associated with the MCH receptor.
Type:
Grant
Filed:
March 19, 2002
Date of Patent:
April 25, 2006
Assignee:
Pharmacopeia Drug Discovery, inc.
Inventors:
Douglas Walsh Hobbs, Tao Guo, Rachael C. Hunter, Huizhong Gu
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:
November 19, 2003
Date of Patent:
April 25, 2006
Assignee:
Schering Corporation
Inventors:
Zhaoning Zhu, Robert Mazzola, Zhuyan Guo, Brian J. Lavey, Lisa Sinning, Joseph Kozlowski, Brian McKittrick, Neng-Yang Shih
Abstract: In one embodiment, the present application relates to a process of making a compound of formula I: and to certain intermediate compounds that are made within the process of making the compound of formula I.
Type:
Grant
Filed:
June 15, 2004
Date of Patent:
January 31, 2006
Assignee:
Schering Corporation
Inventors:
Minzhang Chen, Michael D. Green, Fucheng Zhang
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 17, 2003
Date of Patent:
January 31, 2006
Assignee:
Schering Corporation
Inventors:
Michael P. Dwyer, Timothy J. Guzi, Kamil Paruch, Ronald J. Doll, Kartik M. Keertikar, Viyyoor M. Girijavallabhan
Abstract: In its several embodiments, this invention discloses novel processes to prepare the compounds of formula II and formula IV:
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
January 31, 2006
Assignee:
Schering Corporation
Inventors:
William Leong, Minzhang Chen, Bosco A. D'sa, Man Zhu, Tong Xiao, Xiongwei Shi, Suhan Tang, Dinesh Gala, Andrew J. Goodman, Christopher M. Nielsen, Gary M. Lee, Juan A. Gamboa, Andrew D. Jones
Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.
Type:
Grant
Filed:
February 21, 2003
Date of Patent:
January 17, 2006
Assignee:
Schering Corporation
Inventors:
Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
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.
Abstract: In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of rotamers of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing specific rotamers of pharmaceutically useful salts in desired preponderance.
Type:
Grant
Filed:
November 26, 2002
Date of Patent:
September 13, 2005
Assignee:
Schering Corporation
Inventors:
Dinesh Gala, Andrew J. Goodman, Gary Lee, Hongbiao Liao, Martin L. Schwartz, Suhan Tang, David Js Tsai, Wenxue Wu
Abstract: In one embodiment, the present invention discloses a process to directly prepare an unequal ratio of specific, preferred rotamer or rotameric pair of an acid salt from a basic compound, by creative choice of a solvent medium. The process is particularly useful in preparing desired rotamers of pharmaceutically useful salts.
Type:
Grant
Filed:
November 26, 2002
Date of Patent:
August 30, 2005
Assignee:
Schering Corporation
Inventors:
Minzhang Chen, Bosco D'sa, William Leong, Suhan Tang
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:
July 19, 2005
Assignee:
Schering Corporation
Inventors:
Kamil Paruch, Timothy J. Guzi, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams
Abstract: In one embodiment, the present invention describes the synthesis of (4-bromophenyl) (4-piperidyl)methanone-(Z)—O-ethyloxime and its acid salts, and similar compounds, in high stereochemical purity.
Type:
Grant
Filed:
October 11, 2002
Date of Patent:
July 5, 2005
Assignee:
Schering Corporation
Inventors:
George S. K. Wong, Jeonghan Park, Weidong Tong, Ramani Raghavan