Abstract: The present invention provides compounds, which, are novel antagonists for D1/D5 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1/D5 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.
Type:
Grant
Filed:
May 20, 2004
Date of Patent:
March 17, 2009
Assignee:
Schering Corporation
Inventors:
Duane A. Burnett, William J. Greenlee, Brian McKittrick, Jing Su, Zhaoning Zhu, Thavalakulamgara K. Sasikumar, Robert Mazzola, Li Qiang, Yuanzan Ye
Abstract: Provided are methods for diagnosing the propensity of a subject to develop skin inflammation, in particular, psoriasis. Also provided are methods of treatment with antagonists of IL-17 and/or IL-23.
Type:
Grant
Filed:
May 2, 2005
Date of Patent:
March 10, 2009
Assignee:
Schering Corporation
Inventors:
Robert A. Kastelein, Terrill K. McClanahan, Erin Murphy
Abstract: Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.
Type:
Application
Filed:
July 28, 2008
Publication date:
March 5, 2009
Applicant:
SCHERING CORPORATION
Inventors:
Madaline Chirica, Robert A. Kastelein, Kevin W. Moore, Christi L. Parham
Abstract: The present invention relates to novel screening methods for identifying agonists and antagonists of toll-like receptor (TLR) 7, TLR8 or TLR9. Methods are disclosed for identifying agonists and antagonists of TLR7, TLR8 or TLR9 using mutant TLR proteins containing deletions in one or more extracellular leucine rich regions (LRRs). Such agonists and antagonists have utility in the prevention, treatment and/or cure of various diseases and conditions, including cancer, virus infection, allergy, asthma, and chronic obstructive pulmonary disease (COPD).
Abstract: A compound having the general structure shown in Formula 1: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
Abstract: The present invention discloses compounds which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In other aspects, the invention is directed to 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. Compounds of the invention generally have the structure: where the substituents are as defined herein.
Type:
Grant
Filed:
February 26, 2004
Date of Patent:
March 3, 2009
Assignee:
Schering Corporation
Inventors:
Thavalakulamgara K. Sasikumar, Wen-Lian Wu, Duane A. Burnett, Li Qiang
Abstract: Purified genes encoding a 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.
Type:
Grant
Filed:
June 18, 2007
Date of Patent:
February 17, 2009
Assignee:
Schering Corporation
Inventors:
Rene De Waal Malefyt, Helmut Fickenscher, Bernhard Fleckenstein, Andrea Knappe
Abstract: Provided are methods of modulating cytokine activity, e.g., for the purpose of treating immune and inflammatory disorders, including tumors and cancer. Also provided are methods of administering agonists or antagonists of IL-33 and IL-33 receptor.
Type:
Application
Filed:
September 26, 2008
Publication date:
February 12, 2009
Applicant:
SCHERING CORPORATION
Inventors:
Jochen Schmitz, Martin Oft, Robert A. Kastelein, J. Fernando Bazan
Abstract: A series of compounds represented by the structural formulas and pharmaceutically acceptable isomers, salts, solvates and polymorphs thereof are disclosed. Also disclosed are pharmaceutical compositions containing said compounds and their use as thrombin receptor antagonists and binders to cannabinoid receptors.
Type:
Grant
Filed:
September 25, 2003
Date of Patent:
February 10, 2009
Assignee:
Schering Corporation
Inventors:
Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia
Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein z,1 represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein A, B, G, M, X, J, n, Het, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
Type:
Grant
Filed:
October 5, 2005
Date of Patent:
February 10, 2009
Assignee:
Schering Corporation
Inventors:
Samuel Chackalamannil, Mariappan V. Chelliah, Yan Xia, Keith A. Eagen
Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester 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:
February 10, 2009
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, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Aneta M. Micula, Robert Feltz
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.
Type:
Grant
Filed:
August 9, 2007
Date of Patent:
February 3, 2009
Assignee:
Schering Corporation
Inventors:
Timothy J. Guzi, Yi-Tsung Liu, Ronald J. Doll, Anil Saksena, Viyyoor M. Girijavallabhan, Jonathan A. Pachter
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:
December 9, 2004
Date of Patent:
February 3, 2009
Assignee:
Schering Corporation
Inventors:
Francisco Velazquez, Srikanth Venkatraman, Ashok Arasappan, F. George Njoroge
Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1—R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
Type:
Grant
Filed:
June 14, 2005
Date of Patent:
February 3, 2009
Assignee:
Schering Corporation
Inventors:
Julius J. Matasi, Deen Tulshian, Duane A. Burnett, Wen-Lian Wu, Peter Korakas, Lisa S. Silverman, Thavalakulamgara K. Sasikumar, Li Qiang, Martin S. Domalski
Abstract: The compound of the formula or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of anxiety are disclosed.
Type:
Grant
Filed:
October 27, 2005
Date of Patent:
February 3, 2009
Assignee:
Schering Corporation
Inventors:
David G. Sawutz, Philippe Brianceau, Ana Bercovici, Ginny D. Ho, Deen Tulshian
Abstract: Provided are methods for diagnosing the propensity of a subject to develop skin inflammation, in particular, psoriasis. Also provided are methods of treatment with antagonists of IL-17 and/or IL-23.
Type:
Application
Filed:
September 2, 2008
Publication date:
January 29, 2009
Applicant:
SCHERING CORPORATION
Inventors:
Robert A. Kastelein, Terrill K. McClanahan, Erin Murphy
Abstract: Methods for treating treatment-naive as well as treatment-experienced patients having melanoma to increase the progression-free survival time involving administering a therapeutically effective amount of pegylated interferon-alpha, e.g., preferably pegylated interferon alpha-2b, as adjuvant therapy to definitive surgery are disclosed.
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:
January 27, 2009
Assignee:
Schering Corporation
Inventors:
Karin Franz-Bacon, Daniel M. Gorman, Terrill K. McClanahan
Abstract: In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.
Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: n is 2-5; R is R3-aryl, R3-heteroaryl, R3-cycloalkyl, R3-heterocycloalkyl, alkyl, haloalkyl, —OR4, —SR4 or —S(O)1-2R5; R1 and R2 are H or optionally substituted phenyl or optionally substituted and X is —O— or —S—; or R1 and R2, together with the carbon atoms to which they are attached form optionally substituted and X is —O—, —S— or —NR7—; Z is 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 allergy, allergy-induced airway responses, congestion, obesity and metabolic syndrome using the compounds of Formula I, as well as combinations with other drugs useful for treating those diseases.
Type:
Grant
Filed:
January 19, 2006
Date of Patent:
January 27, 2009
Assignee:
Schering Corporation
Inventors:
Robert G. Aslanian, Wing C. Tom, Xiaohong Zhu