Chalcogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 514/369)
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Patent number: 8653115Abstract: The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on.Type: GrantFiled: June 13, 2007Date of Patent: February 18, 2014Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Fajun Nan, Jianping Zuo, Haijun Chen, Guifeng Wang, Min Gu, Fenghua Zhu, Wei Tang
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Publication number: 20140044783Abstract: A pharmaceutical composition comprises a combination of thiazolidinedione or a pharmaceutically acceptable salt thereof as a first pharmaceutically active ingredient and a second pharmaceutically active ingredient different from thiazolidinedione, wherein the amount of said second pharmaceutically ingredient is larger than that of the first pharmaceutically active ingredient, and wherein the combination of said first and second pharmaceutically active ingredients are provided by a first granulate comprising the first and second pharmaceutically active ingredients and optionally at least one excipient, said first granulate being present in a second granulate comprising a further pharmaceutical excipient.Type: ApplicationFiled: October 7, 2011Publication date: February 13, 2014Applicant: LEK PHARMACEUTICALS D.D.Inventors: Tijana Stanic Ljubin, Rok Staric, Simon Skubin
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Publication number: 20140039004Abstract: The development of agents for gastroesophageal reflux disease, in which existing treatment is not effective, is strongly demanded. An object of the present invention is to provide an agent for preventing or relapse-preventing, treating or ameliorating such gastroesophageal reflux disease. 4-[({6-[Isobutyl(1,3-thiazol-2-ylsulfonyl)amino]-2,3-dihydro-1H-inden-5-yl}oxy)methyl]-3-methyl benzoic acid, a salt thereof or a prodrug thereof is effective in the prevention or relapse prevention, treatment or amelioration of gastroesophageal reflux disease.Type: ApplicationFiled: July 26, 2013Publication date: February 6, 2014Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiroki OKADA, Takashi KONEMURA
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Publication number: 20140038962Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.Type: ApplicationFiled: September 20, 2013Publication date: February 6, 2014Applicant: GEORGETOWN UNIVERSITYInventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
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Publication number: 20140038970Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A??I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: October 2, 2013Publication date: February 6, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: HUBERT B. JOSIEN, John W. Clader, William J. Greenlee, Michael J. Mayer, Jason L. Davis, Shuangyi Wan
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Publication number: 20140030223Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: September 25, 2013Publication date: January 30, 2014Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Martzman, Philip Anthony Morganelli, William J. Watkins, Hong Ye
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Patent number: 8637556Abstract: Provided herein are compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell.Type: GrantFiled: January 15, 2010Date of Patent: January 28, 2014Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, Georgetown UniversityInventors: Steven J. Metallo, Edward V. Prochownik, Ariele Viacava Follis
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Patent number: 8637558Abstract: The present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and the uses thereof. More specifically, the present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and a pharmaceutical composition comprising the same. The novel thiazolidinedione derivatives of formula (I) according to the present invention can be effectively used for the prevention or treatment of cardiovascular disease, gastrointestinal disease and renal disease by inhibiting the activity of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) that decomposes prostaglandins as well as useful for the prevention of hair loss and the stimulation of hair growth, and osteogenic stimulation and wound healing.Type: GrantFiled: December 30, 2009Date of Patent: January 28, 2014Assignee: Industry-Academic Cooperation Foundation, Chosun UniversityInventors: Hoon Cho, Ying Wu, Cheol-Hee Choi
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Publication number: 20140023615Abstract: The present invention provides thermo-sensitive, mucoadhesive biopolymer formulations that enhance the penetration of therapeutics across the skin or mucosal surfaces. In a preferred embodiment, the biopolymer formulation comprises co-polymer of poloxamer 188 and propylene glycol, laurocapram and, optionally, one or more therapeutic agents. Also provided are uses of the biopolymer formulations for topical therapy of cancer including cervical cancer.Type: ApplicationFiled: March 29, 2012Publication date: January 23, 2014Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.Inventor: Stephen I-Hong Hsu
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Patent number: 8632808Abstract: A solid preparation sufficiently masking the unpleasant taste of pioglitazone or a salt thereof; a solid preparation sufficiently masking the unpleasant taste of pioglitazone or a salt thereof and having superior properties of superior disintegration property in the oral cavity, appropriate preparation strength, long-term preservation stability and the like is provided. The present invention provides a solid preparation comprising particles comprising (i) core particles comprising an excipient, and (ii) pioglitazone or a salt thereof and an acid-soluble polymer both coating the core particles.Type: GrantFiled: April 26, 2007Date of Patent: January 21, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Kazuhiro Okochi, Arisa Maeda
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Publication number: 20140018377Abstract: This application claims priority to European Patent Application No. 09173304.8, filed Oct. 16, 2009, and the benefit of U.S. Provisional Application No. 61/253,091, filed Oct. 20, 2009, the disclosure of each of which is incorporated by reference herein in its entirety. The present invention relates to aminopropenoate derivatives, the process of their preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.Type: ApplicationFiled: June 12, 2013Publication date: January 16, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Christophe Dubost, Jacky Vadal, Philippe Rinolfi, Marie-Claire Grosjean-Cournoyer, Mazen Es-Sayed, Jürgen Benting, Ulrike Wachendorff-Neumann, Shinichi Narabu, Koichi Ishikawa, Hiroyuki Hadano, Pierre Genix, Jean-Pierre Vors, Angela Becker, Ulrich Görgens
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Publication number: 20140011822Abstract: This document provides methods and materials for reducing venous stenosis formation of an arteriovenous fistula or graft. For example, methods and materials for using VEGF inhibitors to reduce venous stenosis formation of arteriovenous fistulas or grafts are provided.Type: ApplicationFiled: March 16, 2012Publication date: January 9, 2014Inventor: Sanjay Misra
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Publication number: 20140011748Abstract: This present invention provides methods of treating of accessing/monitoring the responsiveness of a cancer cell to JNK inhibitor therapy.Type: ApplicationFiled: January 19, 2012Publication date: January 9, 2014Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Lynda Chin, Ronald A. Depinho, Giulio Draetta, Timothy P. Heffernan
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Publication number: 20130345267Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.Type: ApplicationFiled: May 30, 2013Publication date: December 26, 2013Inventors: Ronen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee
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Publication number: 20130345268Abstract: The instant disclosure relates to compositions that may be useful as therapeutic agents for the treatment of disorders associated or caused by Ras deregulation or dysregulation, for example, disorders associated with alterations in the NF1 gene such as neurofibromatosis type I, fungal infections such as those caused by Candida albicans, and proliferative disorders such as glioblastoma.Type: ApplicationFiled: August 20, 2013Publication date: December 26, 2013Applicants: The Trustees of Dartmouth College, Children's Hospital Medical CenterInventors: Nancy Ratner, Yolanda Sanchez, Gunnar Johansson, William Seibel
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Patent number: 8614229Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: GrantFiled: August 27, 2008Date of Patent: December 24, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20130338158Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification.Type: ApplicationFiled: July 19, 2013Publication date: December 19, 2013Applicant: Allergan, Inc.Inventors: Richard L. Beard, John E. Donello, Tien T. Duong, Xiaoxia Liu, Haiging Yuan
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Publication number: 20130338165Abstract: Methods of treating Parkinson's Disease comprising administering compounds that up-regulate cystine-glutamate exchange (system Xc?) and/or increase glutathione levels in the brain cells. Preferred compounds are cysteine/cystine prodrugs or N-acetyl cysteine (NAC) prodrugs.Type: ApplicationFiled: June 17, 2013Publication date: December 19, 2013Inventors: David A. Baker, Daniel G. Lawton, Chad Beyer, Michael Neary
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Publication number: 20130338117Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.Type: ApplicationFiled: August 27, 2013Publication date: December 19, 2013Applicant: The Trustees of the University of PennsylvaniaInventor: Robert P. RICCIARDI
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Publication number: 20130331380Abstract: Compounds of formula (I): wherein: m and n represent 1 or 2, A represents a pyrrolyl group, X represents a C(O), S(O) or SO2 group, R1 and R2 represent an alkyl group or, together with the nitrogen atom carrying them, form a heterocyclic group, R3 and R4, together with the atoms carrying them, form a heterocyclic group, R5 represents a hydrogen atom or an alkyl group, R6 represents a hydrogen atom or a halogen atom. Medicinal products containing the same which are useful in treating cancer.Type: ApplicationFiled: February 21, 2013Publication date: December 12, 2013Applicant: LES LABORATOIRES SERVIERInventors: Vincent Lacoste, Pauline Lacoste, LES LABORATOIRES SERVIER
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Publication number: 20130330365Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20130331386Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, irritable bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.Type: ApplicationFiled: August 15, 2013Publication date: December 12, 2013Inventors: Robert Shalwitz, Kevin Gene Peters
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Publication number: 20130324545Abstract: AKR1B1 (EC 1.1.1.21) is an aldose reductase that has mainly been associated with the polyol pathway, and more recently with lipid deperoxidation. We have discovered that the primary activity of this enzyme is rather a PGFS activity, catalyzing the transformation of PGH2 into PGF2?. AKR1B1 as a therapeutic target, and method for modulating its expression and activity are provided. Methods for regulating the expression and activity of PGF2? are also provided.Type: ApplicationFiled: July 17, 2013Publication date: December 5, 2013Applicant: UNIVERSITE LAVALInventors: Michael Fortier, Pierre Chapdelaine, Eva Bresson, Éric Madore
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Publication number: 20130324529Abstract: The present invention is related to novel benzimidazole compounds of formula (I) having cannabinoid receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals, in particular humans.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: JANSSEN PHARMACEUTICA NVInventors: Henricus Jacobus Maria Gijsen, Michel Anna Jozef De Cleyn, Michel Surkyn, Bie Maria Pieter Verbist
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Publication number: 20130316906Abstract: The invention relates to novel compounds of the formula (I) in which R1, R2, R3, R4, R5, Y, Q and G have the meanings given above, to a plurality of processes and intermediates for their preparation and to their use as herbicides and/or pesticides. Moreover, the invention relates to selective herbicidal compositions comprising, firstly, the phenyl-substituted bicyclooctane-1,3-dione derivates and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to increasing the activity of crop protection compositions comprising in particular phenyl-substituted bicyclooctane-1,3-dione derivates by adding ammonium salts or phosphonium salts and, if appropriate, penetrants, to the corresponding compositions, to processes for their preparation and to their use in crop protection as pesticides and/or for preventing unwanted plant growth.Type: ApplicationFiled: October 28, 2011Publication date: November 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alfred Angermann, Stefan Lehr, Guido Bojack, Reiner Fischer, Isolde Häuser-hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Arnd Voerste, Dieter Feucht
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Publication number: 20130310432Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.Type: ApplicationFiled: July 26, 2013Publication date: November 21, 2013Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christoph Binkert, Martin Bolli, Boris Mathys, Claus Mueller, Michael Scherz, Oliver Nayler
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Publication number: 20130310431Abstract: The invention provides 11-?-hydroxysteroid dehydrogenase type 1 enzyme (11?HSD1) inhibitors, such as a compound of the formula: (A), its hydroxy and keto metabolites, and pharmaceutically acceptable salts thereof, for treating cognitive disorders, including age-related cognitive disorders, such as Alzheimer's Disease. Also provided are methods and uses for inhibiting 11?HSD1 and for reducing the concentration or preventing the elevation of concentration of cortisol in the brain of a subject by administering the compound of the formula (A); its hydroxy and keto metabolites, and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 11, 2011Publication date: November 21, 2013Inventor: Michele Wyszynski
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Patent number: 8586607Abstract: There is provided novel compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.Type: GrantFiled: July 23, 2009Date of Patent: November 19, 2013Assignee: Syddansk UniversitetInventors: Trond Ulven, Elisabeth Christiansen
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Patent number: 8580832Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: March 6, 2008Date of Patent: November 12, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Michael Gaul, Alexander Kim, Lily Lee Searle, Dionisios Rentzeperis, Gilles C. Bignan
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Publication number: 20130296386Abstract: Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease.Type: ApplicationFiled: January 26, 2012Publication date: November 7, 2013Applicants: UNIVERSITY OF ROCHESTER, TEMPLE UNIVERSITY--OF THE COMMONWEALTH SYSTEM OF HIGHER LEARNING, BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKAInventors: Paul M. Dunman, Patrick D. Olson, Wayne Childers
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Patent number: 8569302Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: GrantFiled: July 19, 2010Date of Patent: October 29, 2013Assignee: Gilead Sciences, Inc.Inventors: Eda Canales, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Qi Liu, Michael Mertzman, Philip A. Morganelli, William J. Watkins, Hong Ye
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Publication number: 20130281414Abstract: The present invention relates to thiazolidinedione analogues that are useful for treating liver afflictions such as nonalcoholic fatty liver disease (NAFLD) or nonalcoholic steatohepatitis (NASH).Type: ApplicationFiled: April 20, 2011Publication date: October 24, 2013Applicant: Metabolic Solutions Development Company, LLCInventors: Gerard R. Colca, Robert C. Gadwood, Timothy Parker
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Patent number: 8563741Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.Type: GrantFiled: September 10, 2008Date of Patent: October 22, 2013Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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Publication number: 20130274283Abstract: Premature termination codons readthrough compounds, composition thereof, and methods of making and using the same are provided.Type: ApplicationFiled: February 11, 2013Publication date: October 17, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Richard A. GATTI, Liutao DU, Robert DAMOISEAUX, Chih-Hung LAI, Michael JUNG, Jin-Mo KU, Carmen BERTONI
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Patent number: 8552038Abstract: A crystalline form of a hydrate of a dihydrochloride 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by the following formula: wherein the crystalline form shows main peaks at interplanar spacings of 10.42, 5.85, 5.52, 3.84, 3.46 and 2.95 angstroms in X-ray powder diffraction obtained with Cu K? line radiation (wavelength ?=1.54 angstroms).Type: GrantFiled: May 7, 2012Date of Patent: October 8, 2013Assignee: Daiichi Sankyo Company, LimitedInventor: Hiroshi Miyamoto
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Publication number: 20130261120Abstract: The present invention relates to: *combinations of: component A: one or more omega-carboxyaryl-substituted diphenyl urea compounds of general formula (I), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; component B: one or more N-(2-arylamino) aryl sulfonamide compounds of general formula (II), or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and, optionally, component C: one or more further pharmaceutical agents; in which optionally some or all of the components are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially. dependently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route; *use of such combinations for the preparation of a medicament for the treatment or prophylaxis of a cancer; and *a kit comprising such a combination.Type: ApplicationFiled: September 29, 2011Publication date: October 3, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Florian Pühler, Marion Hitchcock
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Publication number: 20130261092Abstract: The present invention provides combinations, for treatment of subjects suffering from or at high risk of developing diseases and disorders involving expression of peroxisome proliferator-activated receptors (PPAR). The combinations include abscisic acid and one other bioactive agent, which together provide synergistic effects toward treatment or blocking of development of the disease or disorder. In exemplary embodiments, a combination of abscisic acid and a thiazolidinedione (TZD) is provided for increased insulin sensitivity and improved (i.e., reduced) obesity-induced inflammation.Type: ApplicationFiled: May 30, 2013Publication date: October 3, 2013Inventors: Josep BASSAGANYA-RIERA, Amir J. GURI, Raquel HONTECILLAS
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Patent number: 8546382Abstract: Described herein are methods for improving engraftment of hematopoietic cells in an individual following hematopoietic progenitor cell transplantation (e.g., via bone marrow or cord blood transplantation). Methods for increasing hematopoietic progenitor cell proliferation in individuals with bone marrow aplasia are also described. The methods involve administering an agent that inhibits adipogenesis, adipocyte growth, adipocyte differentiation and/or adipocyte proliferation.Type: GrantFiled: April 15, 2010Date of Patent: October 1, 2013Assignee: Children's Medical Center CorporationInventors: Olaia Naveiras, George Daley, Pamela L. Wenzel
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Publication number: 20130253007Abstract: The present invention provides methods of identifying compounds that selectively induce an oxidative stress response in a biological sample. The present invention further provides methods of treating a subject having a disease associated with oxidative stress using compounds that selectively induce an oxidative stress response in the subject. The invention further provides methods of selectively inducing an oxidative stress response in a cell.Type: ApplicationFiled: May 15, 2013Publication date: September 26, 2013Applicant: High Point Pharmaceuticals, LLCInventors: Jareer Nabeel Kassis, Otis Clinton Attucks, Matthew J. Kostura
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Publication number: 20130253021Abstract: The present invention provides methods of making and using 5-(2-(indol-3-yl)-2-oxoethylidene)-3-phenyl-2-thioxothiazolidin-4-one derivatives having HIV-1 or JSP-1 inhibitory activity.Type: ApplicationFiled: March 22, 2013Publication date: September 26, 2013Applicants: The Johns Hopkins University, Southern Methodist UniversityInventors: Edward R. Biehl, Sukanta Kamila, Ted M. Dawson
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Patent number: 8541592Abstract: The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: November 13, 2006Date of Patent: September 24, 2013Assignees: Amgen Inc., Biovitrum ABInventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle, Teresa L. Marshall
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Publication number: 20130237573Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.Type: ApplicationFiled: November 15, 2011Publication date: September 12, 2013Applicant: ELI LILLY AND COMPANYInventors: Bruce Anthony Dressman, Mark Donald Chappell, Adam Michael Fivush, Charles Howard Mitch, Paul Leslie Ornstein, Eric George Tromiczak, Tatiana Natali Vetman
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Patent number: 8524752Abstract: The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.Type: GrantFiled: August 9, 2012Date of Patent: September 3, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Christoph Binkert, Martin Bolli, Boris Mathys, Claus Mueller, Michael Scherz, Oliver Nayler
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Publication number: 20130224255Abstract: Embodiments of the present invention include methods for the treatment, prevention, or amelioration of vascular disease in diabetic patients. The methods include both implantation of a stent including a first drug. Some embodiments include additional therapy, such as the co-administration of another drug. Some embodiments involve different stent selection for a diabetic patient compared to a non-diabetic patient.Type: ApplicationFiled: February 23, 2012Publication date: August 29, 2013Applicant: Abbott Cardiovascular Systems Inc.Inventors: Syed F.A. Hossainy, Paul M. Consigny
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Publication number: 20130225629Abstract: The presently disclosed subject matter generally relates to methods and compositions for treating enteritis. More particularly, the presently disclosed subject matter relates to methods and compositions for modulating a component of a PI3K/mTOR pathway. In some embodiments, the methods and compositions of the presently disclosed subject matter generally relates to the treatment of campylobacteriosis. More particularly, the methods and compositions of the presently disclosed subject matter relate to the treatment of campylobacteriosis by modulating a component of a PI3K/mTOR pathway.Type: ApplicationFiled: February 25, 2013Publication date: August 29, 2013Applicant: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILLInventor: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL
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Publication number: 20130216625Abstract: The present invention relates to the use of a substance with the core structure of formula (I), or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the manufacture of a composition for the treatment of insulin resistance or diseases associated with insulin resistance, preferably in human subject in a daily dosage in a range of from about 5 mg to about 1500 mg. The invention furthermore relates to a method of treating insulin resistance or diseases associated with insulin resistance in a mammal, said method comprises administering to said mamma, preferably a human subject, a substance with the core structure of formula (I), preferably in a daily dosage in a range from about 5 mg to about 1500 mg. The substance is preferably isosteviol or steviol, or pharmaceutically acceptable salts, solvates or prodrugs thereof. Examples of diseases associated with insulin resistance and e.g.Type: ApplicationFiled: September 14, 2012Publication date: August 22, 2013Applicant: STEVIA APSInventors: Kjeld Hermansen, Per Bendix Jeppesen
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Publication number: 20130217690Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Mochida Pharmaceutical Co., Ltd.
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Patent number: 8513252Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X1, X2, (A)m and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: GrantFiled: July 14, 2010Date of Patent: August 20, 2013Assignee: Addex Pharma S.A.Inventor: Christelle Boléa
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Publication number: 20130209403Abstract: The invention relates to Phospholipase A2 (hereinafter also referred to as PLA2) inhibitors for use in the treatment or prevention of flavivirus infection, in particular an infection with a flavivirus of the genus Flavi or the genus Hepaci. The invention also provides a pharmaceutical formulation for use in the treatment or prevention of an infection with a flavivirus of the genus Flavi or the genus Hepaci and a method of preventing or treating an infection with a flavivirus of the genus Flavi or the genus Hepaci.Type: ApplicationFiled: September 8, 2011Publication date: August 15, 2013Applicants: Ruprecht-Karls-Universitaet, Twincore Zentrum fuer Experimentelle and Klinische Infektionsforschung GmbHInventors: Nicolas Menzel, Thomas Pietschmann, Ralf Bartenschlager, Wolfgang Fischl
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Patent number: RE44578Abstract: Pharmaceutical compositions that have excellent storage stability even though they include a active component that is susceptible to degradation in an acidic environment are disclosed. The stabilized pharmaceutical composition of the invention includes a ring-opened 7-substituted-3,5-dihydroxyheptanoic or a ring-opened 7-substituted-3,5-dihydroxyheptenoic acid, or a pharmaceutically acceptable salt thereof, as an active component and a stabilizing effective amount of at least one amido-group containing polymeric compound or at least one amino-group containing polymeric compound, or combination thereof; wherein the stabilized pharmaceutical composition does not contain a stabilizing effective amount of another stabilizer or a combination of other stabilizers.Type: GrantFiled: September 18, 2009Date of Patent: November 5, 2013Assignee: TEVA Pharmaceutical Industries, Ltd.Inventors: Michael Fox, Ivo Dorossiev