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.
Abstract: The present invention provides methods for reducing protease activity in plant hydrolysates that are utilized in cell culture media. The method involves a combination of heating and ultrafiltration to remove proteases present in the hydrolysate prior to the addition of the hydrolysate to the cell culture medium.
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, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.
Type:
Grant
Filed:
January 16, 2007
Date of Patent:
March 23, 2010
Assignee:
Schering Corporation
Inventors:
Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong-Heon Kim, De-Yi Yang, Razia Rizvi
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, ADAMs, TACE, TNF- or combinations thereof.
Type:
Grant
Filed:
December 18, 2008
Date of Patent:
March 23, 2010
Assignee:
Schering Corporation
Inventors:
Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K. C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar
Abstract: Disclosed are compounds of formula I (Chemical formula should be inserted here as it appears on abstract in paper form) Formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R4, R14, V, W, X, Y, Z, p, and ring A are as described in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. 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 m1 agonist or m2 antagonist.
Type:
Application
Filed:
December 10, 2007
Publication date:
March 18, 2010
Applicant:
Schering Corporation
Inventors:
Zhaoning Zhu, Andrew Stamford, Mihirbaran Mandal, Xiaoxiang Liu
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:
November 19, 2008
Date of Patent:
March 16, 2010
Assignee:
Schering Corporation
Inventors:
Tiruvettipuram K. Thiruvengadam, Tao Wang, John S. Chiu, Jing Liao
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:
January 13, 2006
Date of Patent:
March 9, 2010
Assignee:
Schering Corporation
Inventors:
Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
Abstract: Disclosed are novel compounds of the formula: and the pharmaceutically acceptable salts and solvates thereof. D and E are different groups wherein one is N and the other is CR50. Examples of groups comprising Substituent A include heteroaryl, aryl, heterocycloalkyl, cycloalkyl, aryl, alkynyl, alkenyl, aminoalkyl, alkyl or amino. Examples of groups comprising Substituent B include aryl and heteroaryl. Also disclosed is a method of treating a chemokine mediated diseases, such as, cancer, angiogenisis, angiogenic ocular diseases, pulmonary diseases, multiple sclerosis, rheumatoid arthritis, osteoarthritis, stroke and cardiac reperfusion injury, pain (e.g., acute pain, acute and chronic inflammatory pain, and neuropathic pain) using a compound of formula IA.
Type:
Grant
Filed:
December 20, 2004
Date of Patent:
March 2, 2010
Assignee:
Schering Corporation
Inventors:
Arthur G. Taveras, J. Robert Merritt, John J. Baldwin, Junying Zheng, Purakkattle J. Biju, Younong Yu, Jianhua Chao, Gaifa Lai, Minglang Wu
Abstract: Nucleic acids encoding mammalian Toll-like receptors (TLRs) have been identified in human cells. Recombinantly produced TLRs are used in the preparation of antibodies that are capable of binding to the TLRs. The antibodies are advantageously used in the prevention and treatment of septic shock, inflammatory conditions, and viral infections.
Type:
Grant
Filed:
April 9, 2008
Date of Patent:
March 2, 2010
Assignee:
Schering Corporation
Inventors:
Gerard T. Hardiman, Fernando L. Rock, J. Fernando Bazan, Robert A. Kastelein, Stephen W. K. Ho, Yong-Jun Liu
Abstract: The present invention includes isolated nucleic acids encoding fully human, neutralizing, monoclonal antibodies against human Insulin-like Growth Factor Receptor-I (IGFR1). Also included are methods of using and producing the antibodies of the invention.
Type:
Grant
Filed:
November 13, 2006
Date of Patent:
February 23, 2010
Assignee:
Schering Corporation
Inventors:
Yan Wang, Robert Greenberg, Leonard Presta, Jonathan A. Pachter, Judith Hailey, Peter Brams, Denise Williams, Mohan Srinivasan, Diane Feingersh
Abstract: Purified genes encoding cytokine from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this molecule are provided. Methods of using said reagents and diagnostic kits are also provided.
Abstract: The methods and compositions provided herein relate generally to IL-10 specific antibodies and uses thereof. More specifically, the methods and compositions provided herein relate to humanized IL-10 specific antibodies and methods to use such antibodies in modulating the biological activity of IL-10, particularly in autoimmune disorders and pathogen-mediated immunopathology.
Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
Type:
Grant
Filed:
August 4, 2004
Date of Patent:
February 16, 2010
Assignee:
Schering Corporation
Inventors:
Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
Abstract: In its many embodiments, the present invention provides a novel class of compounds of structural formula IA or IB where R1-R8 are as disclosed herein as inhibitors of the CCR5 receptors, 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 CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v.
Type:
Grant
Filed:
February 21, 2006
Date of Patent:
February 9, 2010
Assignee:
Schering Corporation
Inventors:
Tze-Ming Chan, Kathleen Kox, Wenqing Feng, Michael W. Miller, Daniel Weston, Stuart W. McCombie
Abstract: The purification and isolation of various genes which encode mammalian cell surface polypeptides. Nucleic acids, proteins, antibodies, and other reagents useful in modulating development of cells, e.g., lymphoid and myeloid, are provided, along with methods for their use.
Type:
Grant
Filed:
December 19, 2007
Date of Patent:
February 9, 2010
Assignee:
Schering Corporation
Inventors:
Alexander B. H. Bakker, Joseph H. Phillips, Lewis L. Lanier
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:
Application
Filed:
April 13, 2009
Publication date:
February 4, 2010
Applicants:
Canji Inc.,, Schering Corporation,
Inventors:
Heidrun Engler, Tattanahalli L. Nagabhushan, Stephen Kenneth Youngster
Abstract: CTLA-8 related antigens from mammals, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding said antigens. Methods of using said reagents and diagnostic kits are also provided.
Type:
Grant
Filed:
December 7, 2007
Date of Patent:
February 2, 2010
Assignee:
Schering Corporation
Inventors:
Daniel M. Gorman, J. Fernando Bazan, Robert A. Kastelein, Gerard Zurawski
Abstract: A method for producing a soluble, properly folded, biologically active protein in bacteria in which the heterologous protein is coexpressed with a thioredoxin protein.
Abstract: A bilayer solid composition comprising (a) an immediate release first layer comprising an anti-allergic effective amount of desloratadine and at least one pharmaceutically acceptable excipient and (b) a sustained release second layer comprising an effective amount of a nasal decongestant, e.g. pseudoephedrine sulfate and a pharmaceutically acceptable sustained release agent wherein the composition contains less than about 2% of desloratadine decomposition products is disclosed. A solid composition comprising an anti-allergic effective amount of desloratadine and at least one, and preferably two pharmaceutically acceptable antioxidants is also disclosed.
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, ADAMs, TACE, TNF-? or combinations thereof.
Type:
Grant
Filed:
June 1, 2005
Date of Patent:
January 26, 2010
Assignee:
Schering Corporation
Inventors:
Zhuyan Guo, Peter Orth, Zhaoning Zhu, Robert D. Mazzola, Tin-Yau Chan, Henry A. Vaccaro, Brian McKittrick, Joseph A. Kozlowski, Brian J. Lavey, Guowei Zhou, Sunil Paliwal, Shing-Chun Wong, Neng-Yang Shih, Pauline C. Ting, Kristin E. Rosner, Gerald W. Shipps, Jr., M. Arshad Siddiqui, David B. Belanger, Chaoyang Dai, Dansu Li, Vinay M. Girijavallabhan, Janeta Popovici-Muller, Wensheng Yu, Lianyun Zhao