Abstract: The present invention discloses novel macrocyclic 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 macrocycles as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
April 17, 2001
Date of Patent:
July 5, 2005
Assignee:
Schering Corporation
Inventors:
Srikanth Venkatraman, Kevin X. Chen, Ashok Arasappan, F. George Njoroge, Viyyoor Moopil Girijavallabhan, Ashit K. Ganguly, Tin-Yau Chan, Brian Alexander Mc Kittrick, Nanhua Hugh Yao, Andrew Joseph Prongay, Vincent Stewart Madison
Abstract: The present invention is directed to certain diaryl amide compounds as NS3-Serine protease inhibitors of hepatitis C virus.
Type:
Grant
Filed:
December 10, 2001
Date of Patent:
June 28, 2005
Assignee:
Schering Corporation
Inventors:
Zhaoning Zhu, Zhong-Yue Sun, Srikanth Venkatraman, F. George Njoroge, Ashok Arasappan, Bruce A. Malcolm, Viyyoor M. Girijavallabhan, Raymond G. Lovey, Kevin X. Chen
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:
September 5, 2002
Date of Patent:
June 7, 2005
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: 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:
January 21, 2003
Date of Patent:
May 17, 2005
Assignee:
Schering Corporation
Inventors:
Ashok Arasappan, Frank Bennett, Stephane L. Bogen, Kevin X. Chen, Edwin Jao, Yi-Tsung Liu, Raymond G. Lovey, Vincent S. Madison, Latha G. Nair, F. George Njoroge, Anil K. Saksena, Mousumi Sannigrahi, Srikanth Venkatraman, Viyyoor M. Girijavallabhan
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:
April 10, 2002
Date of Patent:
May 3, 2005
Assignee:
Pharmacopeia Drug Discovery, Inc.
Inventors:
Douglas W. Hobbs, Tao Guo, Rachael C. Hunter, Huizhong Gu, Suresh D. Babu, Yuefei Shao
Abstract: In an illustrative embodiment, the present invention describes the synthesis of the following compound and similar compounds, in high stereochemical purity by a novel stereoselective alkylation process:
Type:
Grant
Filed:
March 27, 2003
Date of Patent:
March 29, 2005
Assignee:
Schering Corporation
Inventors:
Wenxue Wu, Hongbiao Liao, David J. S. Tsai, David R. Andrews, Dinesh Gala, Gary M. Lee, Martin Lawrence Schwartz, Timothy L. McAllister, Xiaoyong Fu, Donal Maloney, Tiruvettipuram K. Thiruvengadam, Chou-Hang Tann
Abstract: The present invention discloses novel macrocyclic 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 macrocycles as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
April 3, 2001
Date of Patent:
January 25, 2005
Assignee:
Schering Corporation
Inventors:
Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Tejal Parekh, Haining Gu, George F. Njoroge, Viyyoor Moopil Girijavallabhan, Ashit Ganguly, Anil Saksena, Edwin Jao, Nanhua Hugh Yao, Andrew Joseph Prongay, Vincent Stewart Madison, Bancha Vibulbhan
Abstract: The present invention discloses novel imidazolidinones which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazolidinones as well as methods of using them to treat disorders associated with the HCV protease.
Type:
Grant
Filed:
July 19, 2001
Date of Patent:
January 4, 2005
Assignee:
Schering Corporation
Inventors:
Ashok Arasappan, Tejal Parekh, F. George Njoroge, Viyyoor Moopil Girijavallabhan, Ashit K. Ganguly
Abstract: A xanthine phosphodiesterase V inhibitor having the formula (I), with the variables defined herein, which is especially useful for treating male (erectile) and female sexual dysfunction and other physiological disorders:
For example, a representative compound of the invention is:
Type:
Grant
Filed:
August 28, 2001
Date of Patent:
November 23, 2004
Assignee:
Schering Corporation
Inventors:
Samuel Chackalamannil, Yuguang Wang, Craig D. Boyle, Andrew W. Stamford
Abstract: In one embodiment, the present invention describes the synthesis of 4-[(Z)-(4-bromophenyl)(ethoxyimino)methyl]-1′-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbonyl]-4′-methyl-1,4′-bipiperidine, and intermediates therefor from easily available starting materials by a simple route.
Type:
Grant
Filed:
October 11, 2002
Date of Patent:
November 16, 2004
Assignee:
Schering Corporation
Inventors:
Minzhang Chen, Bosco Anthony D'Sa, William W. Leong, Tong Gan, George S. K. Wong, Suhan Tang, Christopher Michael Nielsen
Abstract: The present invention discloses novel peptide 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 peptides as well as methods of using them to treat disorders associated with the HCV protease.
Inventors:
Anil K. Saksena, Viyyoor Moopil Girijavallabhan, Raymond G. Lovey, Edwin Jao, Frank Bennett, Jinping L. McCormick, Haiyan Wang, Russell E. Pike, Stephane L. Bogen, Yi-Tsung Liu, Ashok Arasappan, Tejal Parekh, Patrick A. Pinto, F. George Njoroge, Ashit K. Ganguly, Terence K. Brunck, Scott Jeffrey Kemp, Odile Esther Levy, Marguerita Lim-Wilby
Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, nasal congestion, inflammatory and CNS-related diseases and others.
Type:
Grant
Filed:
September 18, 2001
Date of Patent:
July 13, 2004
Assignee:
Schering Corporation
Inventors:
Neng-Yang Shih, Robert G. Aslanian, Daniel M. Solomon, Stuart B. Rosenblum, Mwangi Wa Mutahi, Tom G. Wing, Kevin D. McCormick, John J. Piwinski, Ronald Wolin
Abstract: In one embodiment, this invention provides a novel class of aryl oxime-piperazine compounds as antagonists of the CCR5 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 of one or more of diseases associated with the CCR5 receptor.
Type:
Grant
Filed:
March 27, 2002
Date of Patent:
February 10, 2004
Assignee:
Schering Corporation
Inventors:
John W. Clader, Sue-Ing Y. Lin, Stuart W. Mc Combie, Pradeep B. Pushpavanam, Susan Vice
Abstract: This invention discloses novel gamma secretase inhibitors of the formula:
wherein: R1 is a substituted aryl or substituted heteroaryl group; R2 is an R1 group, alkyl, —X(CO)Y, —(CR32)1-4X(CO)Y; each R3A is independently H or alkyl; X is —O—, —NH, or —N-alkyl; and Y is —NR6R7, or —N(R3)(CH2)2-6NR6R7. Also disclosed is a method of treating Alzheimer's Disease.
Type:
Grant
Filed:
August 1, 2002
Date of Patent:
January 27, 2004
Assignee:
Schering Corporation
Inventors:
Theodoros Asberom, Henry S. Guzik, Hubert B. Josien, Dmitri A Pissarnitski
Abstract: In one embodiment, the present invention describes the synthesis of 4-(piperidyl)(2-pyridyl)methanone-(E)-O-methyloxime dihydrochloride, monohydrochloride and free base, and similar compounds, in high stereochemical purity.
Abstract: The present invention relates to azapeptide compounds represented by the formula:
pharmaceutical compositions containing such compounds, and the use thereof in the treatment of Hepatitis C viral infections.
Abstract: A series of imidodisulfamide derivatives have been prepared and are useful to treat antiviral infections, especially infections caused by orthopox viruses.
Abstract: Use of an antagonist selected from the group consisting of: (a) antagonists of neurokinin-1 (NK1), neurokinin-2 (NK2) and neurokinin-3 (NK3) receptors, (b) antagonists of NK1 and NK2 receptors, (c) antagonists of NK2 and NK3 receptors, (d) antagonists of NK1 and NK3 receptors, (e) antagonists of NK1 receptors, and (f) antagonists of NK2 to treat symptoms and disorders associated with a production and/or secretion of androgen. One aspect of the invention relates to the use of antagonists to suppress production/secretion of androgens in mammals suffering from an androgen-dependent disease, such as benign prostatic hyperplasia and prostatic carcinoma.
Type:
Grant
Filed:
May 7, 2002
Date of Patent:
May 27, 2003
Assignee:
Schering Corporation
Inventors:
Michael W. Leach, Mark R. Berardi, Elmer J. Mirro, Dineshwar Sinha, Jonathan A. Pachter, Mark E. Cartwright, Gregory A. Reichard
Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.
Type:
Grant
Filed:
September 18, 2001
Date of Patent:
March 4, 2003
Assignee:
Schering Corporation
Inventors:
Neng-Yang Shih, Robert G. Aslanian, John J. Piwinski, Andrew T. Lupo, Jr., Adriano Afonso
Abstract: The present invention discloses novel substituted imidazole compounds which have either or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.
Type:
Grant
Filed:
September 18, 2001
Date of Patent:
February 11, 2003
Assignee:
Schering Corporation
Inventors:
Robert G. Aslanian, Stuart Rosenblum, Mwangi Wa Mutahi, Neng-Yang Shih, John J. Piwinski