Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Application
Filed:
April 8, 2011
Publication date:
October 13, 2011
Inventors:
Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Yat Sun Or
Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
Type:
Application
Filed:
October 6, 2009
Publication date:
October 13, 2011
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Adandan Palani, Michael Y. Berlin, Robert G. Aslanian
Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, processes for their preparation, pharmaceutical compositions containing these compounds, and their use in the treatment of allergic disorders, such as allergic rhinitis and asthma.
Type:
Application
Filed:
December 16, 2009
Publication date:
October 6, 2011
Inventors:
Ian Baxter Campbell, Simon Peace, John Martin Pritchard, Daniel Tape, Robert Charles Wheeler
Abstract: Described herein is the finding that polymerase ? (Pol?) and N-methylpurine DNA glycosylase (MPG) can be used as biomarkers to evaluate the sensitivity of a subject to combination therapy that includes treatment with either temozolomide (TMZ) and methoxyamine, or TMZ and a poly(ADP-ribose) polymerase (PARP) inhibitor. Thus, provided herein is a method of determining if a subject will be sensitive to TMZ and methoxyamine, or TMZ and a PARP inhibitor by measuring expression of Pol? and MPG in a sample from the subject and comparing expression of Pol? and MPG in the sample to a control. A decrease in expression of Pol? and an increase in expression of MPG relative to the control indicates the subject is sensitive to TMZ and methoxyamine, or sensitive to TMZ and the PARP inhibitor.
Abstract: The present invention relates to methods of improving a treatment outcome comprising administering a heat shock protein (HSP) preparation or an ?-2-macroglobulin (?2M) preparation with a non-vaccine treatment modality. In particular, an HSP preparation or an ?2M preparation is administered in conjunction with a non-vaccine treatment modality for the treatment of cancer or infectious diseases. In the practice of the invention, a preparation comprising HSPs such as but not limited to, hsp70, hsp90 and gp96 alone or in combination with each other, noncovalently or covalently bound to antigenic molecules or ?2M, noncovalently or covalently bound to antigenic molecules is administered in conjunction with a non-vaccine treatment modality.
Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-?]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
Type:
Application
Filed:
November 20, 2008
Publication date:
September 15, 2011
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Antonio Jose del Moral Barbosa, Joerg Martin Benzien, Steven Richard Brunette, Zhidong Chen, Derek Cogan, Donghong A. Gao, Alexander Heim-Riether, Joshua Courtney Horan, Jennifer A. Kowalski, Michael David Lawlor, Rene Marc Lemieux, Weimin Liu, Bryan Mckibben, Craig Andrew Miller, Neil Moss, Matt Aaron Tschantz, Zhaoming Xiong, Hui Yu, Yang Yu
Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
Type:
Application
Filed:
November 3, 2009
Publication date:
September 1, 2011
Inventors:
Peter J. Manley, Kausik K. Nanda, B. Wesley Trotter
Abstract: The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.
Type:
Grant
Filed:
December 8, 2006
Date of Patent:
August 30, 2011
Assignee:
Novartis AG
Inventors:
Peter Herold, Robert Mah, Vincenzo Tschinke, Michael Quirmbach, Christiane Marti, Aleksandar Stojanovic, Stefan Stutz
Abstract: The present invention relates to new quinoline inhibitors of tyrosine kinases, pharmaceutical compositions thereof, and methods of use thereof.
Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Application
Filed:
January 25, 2011
Publication date:
August 4, 2011
Inventors:
Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Hui Cao, Yat Sun Or
Abstract: The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.
Abstract: Described are methods for treating cancers, e.g., glioblastoma, including administering an inhibitor of Notch signalling, e.g., a gamma secretase inhibitor, in combination with a chemotherapeutic agent.
Type:
Application
Filed:
November 10, 2010
Publication date:
July 21, 2011
Applicant:
UNIVERSITY OF MASSACHUSETTS
Inventors:
Alonzo H. Ross, Candace Gilbert, Richard Moser
Abstract: Methods and compositions are provided for treating a urinary tract infection (UTI). The methods involve administering to a subject in need thereof a cAMP elevator or agent that mimics cAMP, particularly a labdane diterpene such as forskolin or a derivative or analog thereof in a therapeutically effective amount to treat a UTI. The methods may further include administration of at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs. Compositions of the invention include pharmaceutical compositions and kits for treating a UTI in a subject in need thereof that include therapeutically effective amounts of at least two cAMP elevators, particularly where one of the cAMP elevators is a labdane diterpene such as forskolin or a derivative or analog thereof.
Type:
Application
Filed:
June 12, 2008
Publication date:
July 14, 2011
Applicant:
Duke University
Inventors:
Soman N. Abraham, Brian L. Bishop, Matthew J. Duncan, K. Ranga Rama Krishnan, Jeongmin Song, Guojie Li, David A. Zaas
Abstract: The invention relates to methods of predicting the clinical outcome of brain cancer patients based on the LOH levels of the PTEN gene and on the expression levels or the polysomy/amplification levels of EGFR gene in a sample from said patients.
Type:
Application
Filed:
December 7, 2010
Publication date:
July 7, 2011
Inventors:
Michael J. Donovan, Anna Colomer Valero, Nadina Erill Sagales, Isidre Ferrer Abizanda, Susana Boluda Casas
Abstract: The present invention relates to methods for treating, preventing or controlling vasomotor symptoms such as hot flashes comprising administering specific norepinephrine/serotonin reuptake inhibitors.
Abstract: A strip, which is both edible and dissolvable, is provided comprising a film and a dosage of at least 2% of the reference daily intake (RDI) of at least one dietary supplement for malnutrition or to prevent/treat alcohol induced hangovers. A method for treating malnutrition and/or preventing and treating alcohol-induced hangovers using a dissolvable orally administered strip.
Abstract: The invention features compositions and methods that are useful for the treatment of neoplasia (e.g., breast cancer) by increasing DNA damage and reducing base excision repair (BER).
Type:
Application
Filed:
June 29, 2009
Publication date:
June 23, 2011
Applicant:
UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
Inventors:
Satya Narayan, Aruna S. Jaiswal, David A. Ostrov
Abstract: The present invention relates to the treatment of protozoal diseases by administering cytotoxic and/or cytostatic compounds, in particular those used in anticancer therapy, to patients. In particular, the invention relates to the use of anticancer agents that can penetrate into the CNS for treatment of late stage African sleeping sickness or cerebral malaria.
Abstract: The invention provides compositions and methods for the treatment of neoplasias that are cytotoxic to neoplastic cells or that modulate JAZ expression, subcellular localization, or biological activity.
Type:
Application
Filed:
September 11, 2008
Publication date:
May 12, 2011
Applicant:
UNIVERSITY OF FLORIDA RESEARCH FOUNDATION
Inventors:
Jingxin Qiu, Mingli Yang, David A. Ostrov, W. Stratford May
Abstract: The present invention relates to novel compounds which are antagonist or inverse agonists at an opioid receptor. Such compounds are useful in the treatment of obesity and related diseases and/or conditions in mammals, particularly humans. Methods of making and using such compounds are also disclosed.
Type:
Grant
Filed:
October 12, 2006
Date of Patent:
May 10, 2011
Assignee:
GlaxoSmithKline LLC
Inventors:
Kevin Karl Barvian, Jason Daniel Speake, David John Cowan, Andrew Lamont Larkin, Jerzy Ryszard Szewczyk
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: The subject invention concerns materials and methods for treating oncological disorders in a person or animal using any agent or compound that inhibits uptake of glucose into a cell. The subject invention also concerns methods for inducing apoptosis and inhibiting the proliferation or survival of a cell. In one embodiment, the methods comprise administering an effective amount of an agent or compound that inhibits the activity of one or more glucose transporter proteins, such as Glut-1. An antibody that binds to and inhibits a glucose transporter protein can be used in the present methods.
Abstract: Disclosed are methods of synergistically inhibiting growth of a glioma cell comprising contacting the cell with temozolomide and TNF?, or with temozolomide, TNF?, and radiation. Also disclosed are methods of synergistically inhibiting growth of a glioma in a human cancer patient comprising administering temozolomide and TNF?, or with temozolomide, TNF?, and radiation. Pharmaceutical combinations and therapeutic combinations suitable for use in the methods of the invention are also disclosed.
Type:
Application
Filed:
December 17, 2010
Publication date:
April 21, 2011
Applicants:
THE UNIVERSITY OF CHICAGO, DANA-FARBER CANCER INSTITUTE, INC.
Inventors:
Ralph R. Weichselbaum, Donald W. Kufe, Bakhtiar Yamini
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Methods of treating IL-6 involved diseases with EP4 receptor ligands, including EP4 receptor antagonists. Assays to determine the effect of test compounds on PGE2-induced whole blood cells activation.
Abstract: The present invention describes nanoprodrugs of non-steroidal anti-inflammatory drug (NSAIDs) and nanoprodrugs of ?-lipoic acid-containing and NSAIDs. These nanoprodrugs have antioxidant properties and stimuli-responsiveness, which can be used to treat various disease conditions.
Abstract: The invention relates to the use of one or more cannabinoids, particularly THC and/or CBD in combination with a non-cannabinoid chemotherapeutic agent in the manufacture of a medicament for use in the treatment of cancer. In particular the cancer to be treated is a brain tumour, more particularly a glioma, more particularly still a glioblastoma multiforme (GBM). The non-cannabinoid chemotherapeutic agent may be a selective estrogen receptor modulator or an alkylating agent.
Type:
Application
Filed:
June 4, 2009
Publication date:
April 14, 2011
Inventors:
Guillermo Velasco Diez, Manuel Guzman Pastor, Mar Lorente, Sofia Torres
Abstract: This invention relates to novel benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.
Type:
Grant
Filed:
December 4, 2006
Date of Patent:
April 12, 2011
Assignee:
Neurosearch A/S
Inventors:
Janus S. Larsen, Lene Teuber, Philip K. Ahring, Elsebet Østergaard Nielsen, Naheed Mirza
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: An anti-hepatitis C virus agent or anti-HIV agent comprising, as an active ingredient, a fullerene derivative which has a nitrogen atom forming a ring together with adjacent bonded carbon atom pairs constituting the carbon cluster skeleton of the fullerene or a quaternary amine salt thereof is provided.
Abstract: The invention relates to a sustained release pharmaceutical composition, containing mebicar, for the treatment of anxiety, depression and other psychiatric and neurological disorders.
Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, including, e.g., neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as, e.g., histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical compositions containing the compounds and their methods of use are also provided herein.
Type:
Application
Filed:
September 9, 2010
Publication date:
March 17, 2011
Inventors:
Milan Chytil, Sharon R. Engel, Qun Kevin Fang
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: The present invention is directed to novel substituted aminocyclohexanes which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Type:
Grant
Filed:
May 19, 2006
Date of Patent:
March 15, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Ann E. Weber, Jason Cox
Abstract: Methods for treating an allergic or inflammatory disease or other Syk-mediated disease or Syk-mediated condition characterized by administering a composition which contains a therapeutically effective amount of a 3,6-substituted imidazol[1,2-b]pyridazine compound.
Type:
Grant
Filed:
March 10, 2010
Date of Patent:
March 15, 2011
Assignee:
Alcon, Inc.
Inventors:
Mark R. Hellberg, Steven T. Miller, Andrew Rusinko
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin ? and rifaximin ?, and a poorly crystalline form referred to as rifaximin ?, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.
Type:
Grant
Filed:
May 13, 2008
Date of Patent:
March 15, 2011
Assignee:
Alfa Wassermann, S.p.A.
Inventors:
Giuseppe Claudio Viscomi, Manuela Campana, Dario Braga, Donatella Confortini, Vincenzo Cannata, Paolo Righi, Goffredo Rosini
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.
Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.