Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
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Patent number: 8658618Abstract: Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme in both nervous and non-nervous tissues within the patient and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU generated from a prodrug is in substantial excess of DPD inhibitor in the patient.Type: GrantFiled: October 14, 2010Date of Patent: February 25, 2014Assignee: Adherex Technologies, Inc.Inventor: Thomas Spector
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Patent number: 8658660Abstract: This present disclosure is related to the field of 5-fluoro-4-imino-3-(substituted)-3,4-dihydropyrimidin-2(1H)ones and their derivatives and to the use of these compounds as fungicides.Type: GrantFiled: August 15, 2012Date of Patent: February 25, 2014Assignee: Dow AgroSciences, LLC.Inventors: Timothy A. Boebel, Beth Lorsbach, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
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Publication number: 20140051708Abstract: The present invention relates to pyrazolyl-pyrimidine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: April 3, 2012Publication date: February 20, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Francesco Casuscelli, Maria Gabriella Brasca, Marina Caldarelli, Giovanni Cervi, Teresa Disingrini, Francesca Quartieri
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Patent number: 8653002Abstract: The present invention relates to aqueous suspension concentrate formulation for plant protection comprising: 2-chloro-5-[3,6-dihydro-3-methyl-2,6-dioxo-4-(trifluoromethyl)-1-(2H)pyrimidinyl]-4-fluoro-N-[[methyl(1-methylethyl)amino]sulfonyl]benzamide in the form of its crystalline anhydrate; at least one non-ionic surfactant selected from polyoxyethylene-polyoxy-C3-C4-alkylene block copolymers; at least one anionic surfactant comprising at least one arylsulfonate group; and water; wherein the pH value of the formulation is in the range of 3 to 7.Type: GrantFiled: August 26, 2010Date of Patent: February 18, 2014Assignee: BASF SEInventors: Michael Krapp, Wolfgang Gregori, Klaus Kolb, Bernd Sievernich, Heidi Emilia Saxell, Joerg Steuerwald, Steven Bowe, Rex Liebl, Terrance M. Cannan
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Publication number: 20140045812Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: August 7, 2013Publication date: February 13, 2014Inventors: Michael Mortimore, Stephen Clinton Young, Simon Robert Lorrie Everitt, Ronald Knegtel, Joanne Louise Pinder, Alistair Peter Rutherford, Steven Durrant, Guy Brenchley, Jean-Damien Charrier, Michael O'Donnell
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Publication number: 20140045869Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: October 17, 2013Publication date: February 13, 2014Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
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Publication number: 20140045872Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, A and n are as defined herein. A deuteriated derivative of the compound of Formula (I) is also provided.Type: ApplicationFiled: September 14, 2011Publication date: February 13, 2014Applicant: NOVARTIS AGInventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Henrik Moebitz, Saumitra Sengupta
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Publication number: 20140045873Abstract: The present invention provides compounds of formula (I) wherein A1, A2, R1, D1, D2, Y3 and X are as defined in the claims. The invention further relates to compositions which comprise these compounds and to their use in agriculture or horticulture for controlling or preventing infestation of plants by phytopathogenic microorganisms, preferably fungi.Type: ApplicationFiled: November 10, 2011Publication date: February 13, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Stephan Trah, Werner Zambach, Daniel Stierli, Kurt Nebel, Andrea Bortolato
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Publication number: 20140045758Abstract: Cardiac dysfunction during sepsis is due, at least in part, to cardiac energy deficiency. It has been discovered that lipopolysaccharide (LPS)-mediated cardiac dysfunction is prevented or treated by treatments that improve FA oxidation (FAO), despite the persistence of inflammation. The present invention relates to methods for increasing or maintaining cardiac function in a subject, by administering to the subject a therapeutically effective amount of an agent that increases fatty acid oxidation in the heart.Type: ApplicationFiled: February 21, 2012Publication date: February 13, 2014Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Ira J. Goldberg, Konstantinos Drosatos
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Publication number: 20140044806Abstract: The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine ?7 receptor.Type: ApplicationFiled: October 16, 2013Publication date: February 13, 2014Applicant: H. Lundbeck A/SInventors: Jørgen Eskildsen, Anette Graven Sams, Ask Püschl
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Publication number: 20140045802Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: September 12, 2012Publication date: February 13, 2014Applicant: Bayer Intellectual Property GmbHInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
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Publication number: 20140038971Abstract: Crystalline salts of 5-ethyl-2-{4-[4-(4-tetrazol-1-yl-phenoxymethyl)-thiazol-2-yl]-piperidin-1-yl}-pyrimidine, compositions thereof, methods for their preparation, and methods for their use are disclosed.Type: ApplicationFiled: March 28, 2013Publication date: February 6, 2014Applicant: Metabolex, Inc.Inventors: Jiangao SONG, Charles A. McWherter, Fang Ma, Mark Andres, Igor Ivanisevic, Ekaterina Albert, Patricia Andres
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Publication number: 20140037622Abstract: Methods of treating a head and neck cancer are disclosed.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Applicants: UCL BUSINESS PLC, FOUNDATION MEDICINE, INC.Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Roman Yelensky, Garrett Michael Frampton
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Publication number: 20140038919Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: December 16, 2011Publication date: February 6, 2014Applicant: AbbVie Inc.Inventors: Clarence J. Maring, John K. Pratt, William A. Carroll, Dachun Liu, David A. Betebenner, Douglas K. Hutchinson, Michael D. Tufano, Todd W. Rockway, Uwe Schoen, Axel Pahl, Andreas Witte
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Publication number: 20140037746Abstract: Disclosed is a sustained release system that includes a polymer and a pharmaceutically active agent dispersed in the polymer. The agent is in granular or particulate form, and has a rate of release from the system that is limited primarily by the rate at which the agent dissolves from the granules into the polymer matrix. Advantageously, the polymer is permeable to the agent and is non-release-rate-limiting with respect to the rate of release of the agent from the polymer.Type: ApplicationFiled: July 9, 2013Publication date: February 6, 2014Applicant: pSivida US, Inc.Inventors: Paul Ashton, Jianbing Chen, Hong Guo
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Publication number: 20140031321Abstract: The current invention is directed to methods of inducing the negative chemotaxis of a migratory cell comprising contacting the cell with a compound selected from the group consisting of idebenone, benazepril, rolipram, moxonidine, lamivudine, loxoprofen, terbinafine, synephrine, 6-aminoindazole, and a Vitamin D analog, or a pharmaceutically acceptable salt of any of thereof.Type: ApplicationFiled: January 14, 2013Publication date: January 30, 2014Applicant: CELTAXSYS, INC.Inventor: Erica Brook Goodhew
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Publication number: 20140031376Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: October 3, 2013Publication date: January 30, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Shigeyuki ITOH, Atsushi IWATA
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Publication number: 20140030356Abstract: There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment.Type: ApplicationFiled: July 30, 2013Publication date: January 30, 2014Applicant: Gilead Sciences, Inc.Inventors: Hunter Campbell Gillies, Tobias Peschel, David J. Pizzuti
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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: 8637536Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.Type: GrantFiled: December 5, 2011Date of Patent: January 28, 2014Assignee: Glaxo Group LimitedInventors: Yun Jin, Zehong Wan, Qing Zhang
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Patent number: 8637535Abstract: Solid phases of (?)-cis-FTC, which are designated herein as amorphous (?)-FTC and Forms II and III (?)-cis-FTC) are provided that can be distinguished from Form I (?)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (±)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.Type: GrantFiled: June 9, 2009Date of Patent: January 28, 2014Assignees: Gilead Sciences, Inc., Abbvie, Inc.Inventors: Yuerong Hu, Kenneth R. Phares, Devalina Law
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Patent number: 8637511Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: June 8, 2010Date of Patent: January 28, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sham Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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Patent number: 8637509Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: GrantFiled: May 5, 2011Date of Patent: January 28, 2014Assignee: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis LaFrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
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Publication number: 20140024666Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: September 13, 2013Publication date: January 23, 2014Applicant: GlaxoSmithKline LLCInventors: Duke M. Fitch, Antony N. Shaw, Kenneth Wiggall
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Publication number: 20140024616Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: September 19, 2013Publication date: January 23, 2014Applicant: DOW AGROSCIENCES LLCInventors: Timothy Boebel, Kristy Bryan, Carla J.R. Klittich, Beth Lorsbach, Timothy P. Martin, Mark A. Pobanz, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, W. John Owen
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Publication number: 20140024665Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: June 5, 2013Publication date: January 23, 2014Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
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Publication number: 20140024613Abstract: In one aspect, the present invention features HCV therapies comprising administering to a patient in need thereof an HCV protease inhibitor and ritonavir, wherein ritonavir is used as a pharmacokinetic booster to improve the pharmacokinetics of the HCV protease inhibitor. The HCV therapies do not require the testing of total cholesterol and triglyceride levels prior to and after the therapies.Type: ApplicationFiled: June 26, 2013Publication date: January 23, 2014Inventors: Daniel E. COHEN, Thomas J. PODSADECKI, Barry M. BERNSTEIN, Martin S. KING
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Publication number: 20140017195Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 9, 2013Publication date: January 16, 2014Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavole, Omar D. Lopez, Alain Martel, Nicolas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Patent number: 8629102Abstract: [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: GrantFiled: March 15, 2013Date of Patent: January 14, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
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Publication number: 20140011799Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: July 8, 2013Publication date: January 9, 2014Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
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Publication number: 20140011824Abstract: This present disclosure is related to the field of N1-substituted-5-fluoro-2-oxopyrimidinone-1-(2H)-carboxamides and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: Dow Agrosciences LLCInventors: Timothy A. Boebel, Kristy Bryan, Beth Lorsbach, Timothy P. Martin, W. John Owen, Mark A. Pobanz, Scott Thornburgh, Jeffery D. Webster, Chenglin Yao
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Publication number: 20140011798Abstract: The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.Type: ApplicationFiled: January 24, 2013Publication date: January 9, 2014Applicant: NOVARTIS AGInventors: Pascal FURET, Vito GUAGNANO, Philipp HOLZER, Joerg KALLEN, Lv LIAO, Robert MAH, Liang MAO, Keiichi MASUYA, Achim SCHLAPBACH, Stefan STUTZ, Andrea VAUPEL
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Publication number: 20140005181Abstract: The present disclosure relates to compounds and methods for treating a disease mediated by apelin.Type: ApplicationFiled: June 20, 2013Publication date: January 2, 2014Applicant: Sanford-Burnham Medical Research InstituteInventors: Layton Smith, Anthony B. Pinkerton
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Publication number: 20140004192Abstract: The present invention relates to pharmaceutical formulations that increase the solubility and bioavailability of indibulin, such as a spray-dried solid dispersion of indibulin with at least one matrix polymer. The invention further provides dosage formulations comprising the dispersion and processes for making the dispersion. The present invention also discloses a method of treating immune system based disorders, hyper-proliferative disorders, angiogenesis, malignancies, and neoplasms with the indibulin formulations disclosed herein.Type: ApplicationFiled: March 12, 2013Publication date: January 2, 2014Inventors: John C. Amedio, JR., Barbara Wallner, Marsha G. Marande
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Publication number: 20140005165Abstract: Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.Type: ApplicationFiled: March 14, 2012Publication date: January 2, 2014Inventors: Anilkumar G. Nair, Jose S. Duca, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
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Publication number: 20140005163Abstract: The invention relates to the use of 1H-imidazo[4,5-c]quinolinone derivatives and salts thereof in the treatment of protein and/or lipid kinase dependent diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases; 1H-imidazo[4,5-c]quinolinone derivatives for use in the treatment of protein and/or lipid kinase dependent diseases; a method of treatment against said diseases, comprising administering the 1H-imidazo[4,5-c]quinolinone derivatives to a warm-blooded animal, especially a human; pharmaceutical preparations comprising an 1H-imidazo[4,5-c]quinolinone derivative, especially for the treatment of a protein and/or lipid kinase dependent disease; novel 1H-imidazo[4,5-c]quinolinone derivatives; and a process for the preparation of the novel 1H-imidazo[4,5-c]quinolinone derivatives.Type: ApplicationFiled: May 24, 2013Publication date: January 2, 2014Applicant: NOVARTIS AGInventors: Pascal Furet, Frank Stephan Kalthoff, Robert Mah, Christian Ragot, Frederic Stauffer
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Publication number: 20130345219Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: August 28, 2013Publication date: December 26, 2013Applicant: Synta Pharmaceuticals Corp.Inventors: Chi-Wan Lee, Teresa Prezewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Publication number: 20130345244Abstract: A method for treating a neurofibroma, e.g. dermal neurofibroma, a subdermal neurofibroma, or a superficial plexiform neurofibroma, in a subject in need of such treatment is disclosed. The method comprises locally applying a composition to a neurofibroma either topically or intralesionally. This method does not encompass systemic administration of the composition to the subject to have an effect on the neurofibromas. Compositions useful for such treatments and methods of preparing the compositions are disclosed.Type: ApplicationFiled: June 14, 2013Publication date: December 26, 2013Inventors: Ruihong CHEN, Allan E. Rubenstein, Xiadong Shen, Scott Stewart, Jin-Chen Yu
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Publication number: 20130345222Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: May 17, 2013Publication date: December 26, 2013Inventors: Donald S. Karanewsky, Joseph R. Fotsing, Catherine Tachdjian, Melissa Arellano
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Publication number: 20130345161Abstract: The application describes methods for screening subjects with breast cancer to determine if the breast cancer will be responsive to a breast cancer therapy including a taxane or a taxane derivative. The application also describes methods for treating subjects with breast cancer by screening them for the likelihood of the effectiveness of treating the cancer with a therapy including a taxane or a taxane derivative and administering the therapy in subjects when it is found that a taxane or a taxane derivative is likely to be effective.Type: ApplicationFiled: November 30, 2012Publication date: December 26, 2013Inventors: Charles M. Perou, Philip S. Bernard, Torsten O. Nielsen, Matthew J. Ellis, Joel S. Parker, Miguel Martin, Eva Carrasco, Rosalia Caballero
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Publication number: 20130338105Abstract: Compounds of the formula I in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: ApplicationFiled: August 20, 2013Publication date: December 19, 2013Inventors: Paul Anthony Worthington, Daniel Stierli, Fredrik Cederbaum, Kurt Nebel, Antoine Daina
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Publication number: 20130336965Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: May 20, 2013Publication date: December 19, 2013Applicant: Novartis AGInventors: Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
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Publication number: 20130338178Abstract: Agents and methods of inhibiting or improving the growth of viruses are provided.Type: ApplicationFiled: February 2, 2012Publication date: December 19, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Thomas Shenk, Emre Koyuncu, Ileana Cristea
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Publication number: 20130337052Abstract: Administering a therapeutically effective dose of lithium ions mitigates the side effects of a psychoactive substance such as a cannabinoid. The therapeutically effective dose of lithium ions includes greater than 4 milligrams of lithium and less than 170 milligrams of lithium, or includes between 8 and 32 milligrams of lithium ions per milligram of the psychoactive substance. The therapeutically effective dose of lithium ions is administered using lithium carbonate, lithium citrate, lithium chloride, lithium orotate, lithium aspartate, or analogs thereof using a delivery vehicle selected from pills, tablets, capsules, gelcaps, liquids, syrups, injectable liquids, powders, or foods and administered prior to, with, or after administration of the psychoactive substance. The psychoactive substance includes one or more of anandamide, 2-arachidonoyl glycerol, 2-arachidonoyl glycerol ether, tetrahydrocannabinol, cannabinol, cannabidiol, or analogs thereof and may be administered using the delivery vehicle.Type: ApplicationFiled: September 24, 2012Publication date: December 19, 2013Inventors: Patricia Linert, Kenneth J. Ouimet
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Publication number: 20130336883Abstract: The invention provides compounds that bind to deoxycytidine kinase (dCK) and compositions including pharmaceutically acceptable compositions containing the compounds. The compounds are useful in treating diseases and disorders where dCK activity is implicated such as cancer and immune disorders. The compounds also find use in clinical methodologies including positron emission tomography (PET) imaging.Type: ApplicationFiled: March 8, 2012Publication date: December 19, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Caius G. Radu, Hsiang-I Liao, Nagichettiar Satyamurthy, Johannes Czernin, Jennifer M. Murphy, David A. Nathanson
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Patent number: 8609677Abstract: This invention relates to pharmaceutical compositions comprising a sulfonated biological precursor of thymidine, such as a precursor of 4-thiothymidine (4-TT), and their use in the photodynamic treatment of skin hyperplasias, including cancer, psoriasis, actinic keratosis and keloids, by topical or systemic administration.Type: GrantFiled: March 31, 2013Date of Patent: December 17, 2013Assignee: Yagna LimitedInventor: Giuseppe Trigiante
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Patent number: 8609860Abstract: The present invention relates to a compound comprising an imine bond as an acid-labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound.Type: GrantFiled: June 21, 2010Date of Patent: December 17, 2013Assignee: KTB Tumorforschungsgesellschaft mbHInventors: André Warnecke, Ivonne Müller
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Patent number: 8609852Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.Type: GrantFiled: July 26, 2012Date of Patent: December 17, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
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Publication number: 20130324566Abstract: The invention provides pyrimidine compounds of general formula (I), which reduce simultaneously the production of nitric oxide (NO) and prostaglandin E2 (PGE2). They have no negative effect on the viability of cells in concentrations decreasing the production of these factors by up to 50%; they are not cytotoxic. Furthermore, a method of preparation of the pyrimidine compounds of general formula (I), carrying 2-formamido group, a pharmaceutical composition comprising the substituted pyrimidine compounds according to the invention, and the use of these compounds for the treatment of inflammatory and cancer diseases are provided.Type: ApplicationFiled: February 27, 2012Publication date: December 5, 2013Applicants: USTAV EXPERIMENTALNI MEDICINY AKADEMIE VED CR, V.V.I., USTAV ORGANICKE CHEMIE A BIOCHEMIE AKADEMIE VED CR, V.V.I.Inventors: Petr Jansa, Antonin Holy, Zdenek Zidek, Eva Kmonickova, Zlatko Janeba
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Publication number: 20130324494Abstract: Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders.Type: ApplicationFiled: August 8, 2013Publication date: December 5, 2013Applicant: Aposense Ltd.Inventors: Ilan ZIV, Hagit Grimberg