Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.
Type:
Grant
Filed:
October 30, 2006
Date of Patent:
July 14, 2009
Assignee:
Schering Corporation
Inventors:
Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
Abstract: Nucleic acids encoding a new family of small cysteine rich soluble proteins, from a mammal, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.
Type:
Grant
Filed:
September 18, 2002
Date of Patent:
July 14, 2009
Assignee:
Schering Corporation
Inventors:
Karin Franz-Bacon, Daniel M. Gorman, Terrill K. McClanahan
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: This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising: (a) providing a substrate of Formula I containing an oxime functional group; ?wherein R1 and R2 are selected independently from linear, branched or cyclic alkyl and linear, branched or cyclic alkenyl groups, optionally substituted, with the proviso that at least one of R1 or R2 contains a carbon/carbon double bond; and (b) contacting said substrate of Formula I with a molybdenum oxidation complex, thereby oxidizing said oxime functional group to a nitro functional group to yield the structure of Formula III. Where R1 and R2 are as defined above.
Type:
Grant
Filed:
June 29, 2007
Date of Patent:
June 30, 2009
Assignee:
Schering Corporation
Inventors:
Tiruvettipuram K. Thiruvengadam, Tao Wang, John S. Chiu, Jing Liao
Abstract: This invention relates to compounds of the Formulae (I)-(IX): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, aggrecanase, ADMP, LpxC, ADAMs, TACE, TNF-? or combinations thereof.
Type:
Grant
Filed:
November 29, 2006
Date of Patent:
June 30, 2009
Assignee:
Schering Corporation
Inventors:
M. Arshad Siddiqui, Umar Faruk Mansoor, Panduranga Adulla P. Reddy, Vincent S. Madison
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: 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: Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
Type:
Application
Filed:
February 13, 2009
Publication date:
June 18, 2009
Applicant:
SCHERING CORPORATION
Inventors:
Leonard G. Presta, Brian M. Beyer, Richard N. Ingram, Peter Orth, Yan-Hui Liu
Abstract: Nucleic acids encoding mammalian, e.g., primate or rodent, genes, purified proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are provided.
Type:
Application
Filed:
September 22, 2008
Publication date:
June 18, 2009
Applicant:
SCHERING CORPORATION
Inventors:
Christi L. Parham, Daniel M. Gorman, Hirokazu Kurata, Naoko Arai, Theodore R. Sana, Jeanine D. Mattson, Erin E. Murphy, Chetan Savkoor, Jeffery Grein, Kathleen M. Smith, Terrill K. McClanahan
Abstract: Purified genes encoding proteins from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding these molecules are provided. Methods of using said reagents and diagnostic kits are also provided.
Type:
Application
Filed:
December 12, 2008
Publication date:
June 18, 2009
Applicant:
SCHERING CORPORATION
Inventors:
Constance H. Zlot, Gosse Jan Adema, Carl Figdor, Joseph H. Phillips
Abstract: The present invention provides an isolated mammalian histamine receptor, isolated or recombinant nucleic acids and recombinant vectors encoding the same, host cells comprising the nucleic acids and vectors, and methods of making the receptor using the host cells. This invention further provides antibodies and antigen binding fragments thereof which specifically bind to the receptor and are useful for treating medical conditions caused or mediated by histamine. Also provided are screening methods for identifying specific agonists and antagonists of the mammalian histamine receptor.
Type:
Grant
Filed:
January 5, 2007
Date of Patent:
June 16, 2009
Assignee:
Schering Corporation
Inventors:
Jiang X. Behan, Joseph A. Hedrick, Thomas M. Laz, Frederick James Monsma, Jr., Kelley L. Morse, Shelby P. Umland, Suke Wang
Abstract: The present invention relates to an improved process for preparing himbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer.
Type:
Grant
Filed:
January 12, 2006
Date of Patent:
June 2, 2009
Assignee:
Schering Corporation
Inventors:
Tiruvettipuram K Thiruvengadam, Tao Wang, Jing Liao, John S Chiu, David Jieh-Shyh Tsai, Hong-Chang Lee, Wenxue Wu, Xiaoyong Fu
Abstract: A method and pharmaceutical composition for the enhancement of transfer of a therapeutic agent to a cell wherein the therapeutic agent is formulated in a buffer comprising a compound of Formula I: wherein: n is an integer from 2-8; X1 is a cholic acid group or deoxycholic acid group; and X2 and X3 are each independently selected from the group consisting of a cholic acid group, a deoxycholic acid group, and a saccharide group, wherein the saccharide group is selected from the group consisting of pentose monosaccharide groups, hexose monosaccharide groups, pentose-pentose disaccharide groups, hexose-hexose disaccharide groups, pentose-hexose disaccharide groups, and hexose-pentose disaccharide groups; and wherein at least one of X2 and X3 is a saccharide group.
Type:
Grant
Filed:
February 21, 2006
Date of Patent:
May 26, 2009
Assignees:
Schering Corporation, Canji, Inc.
Inventors:
Heidrun Engler, Tattanahalli L. Nagabhushan, Stephen Kenneth Youngster
Abstract: Flt3 ligand from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding said ligand. Methods of using said reagents and diagnostic kits are also provided.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
May 26, 2009
Assignees:
Schering Corporation, Inserm
Inventors:
Charles H. Hannum, Janice A. Culpepper, Frank D. Lee, Daniel Birnbaum
Abstract: This invention provides methods and compositions for enhancing transfer of an agent into a cell. The agents can include polypeptides, polynucleotides such as genes and antisense nucleic acids, and other molecules. In some embodiments, the agents are modulating agents that can modulate a cellular activity or function when introduced into the cell. The methods and compositions are useful for introducing agents into individual cells, as well as cells that are present as a tissue or organ.
Type:
Grant
Filed:
January 22, 2002
Date of Patent:
May 19, 2009
Assignees:
Canji, Inc., Schering Corporation
Inventors:
Heidrun Engler, Tattanahalli L. Nagabhushan, Stephen Kenneth Youngster
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:
March 30, 2005
Date of Patent:
May 19, 2009
Assignee:
Schering Corporation
Inventors:
Dinesh Gala, Andrew J. Goodman, Gary Lee, Hongbiao Liao, Martin L. Schwartz, Suhan Tang, David J. S. Tsai, Wenxue Wu
Abstract: Flt3 ligand from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding said ligand. Methods of using said reagents and diagnostic kits are also provided.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
May 19, 2009
Assignees:
Schering Corporation, Inserm
Inventors:
Charles H. Hannum, Janice A. Culpepper, Frank D. Lee, Daniel Birnbaum
Abstract: The present invention discloses the compound of Formula I and pharmaceutically acceptable salts and solvates thereof. The invention also relates to pharmaceutical compositions comprising the Compound of Formula I and its use in treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease. The invention also relates to the use of a combination of the Compound of Formula I with additional therapeutic agents for treating obesity, metabolic syndrome, diabetes, hepatic lipidosis or nonalcoholic fatty liver disease.
Type:
Grant
Filed:
August 10, 2007
Date of Patent:
May 12, 2009
Assignee:
Schering Corporation
Inventors:
Manuel de Lera Ruiz, Robert G. Aslanian, Michael Y. Berlin, Kevin D. McCormick, Chander S. Celly
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:
September 10, 2007
Date of Patent:
May 12, 2009
Assignee:
Schering Corporation
Inventors:
Samuel Chackalamannil, Yuguang Wang, Craig D. Boyle, Andrew W. Stamford
Abstract: A compound having the general structure of Formula (I): or a pharmaceutically acceptable salt, solvate, or ester thereof, are useful in treating diseases, disorders, or conditions such as immunodeficiencies, cancers, cardiovascular diseases, endocrine disorders, Parkinson's disease, metabolic diseases, tumorigenesis, Alzheimer's disease, heart disease, diabetes, neurodegeneration, inflammation, kidney disease, atherosclerosis and airway disease.
Type:
Grant
Filed:
January 24, 2006
Date of Patent:
May 5, 2009
Assignee:
Schering Corporation
Inventors:
Tin-Yau Chan, Thierry O. Fischmann, Mark A. McCoy, Brian A. McKittrick, Andrew J. Prongay, Haiyan Pu, Li Wang, Li Xiao