The Hetero Ring Is Five-membered Patents (Class 514/461)
  • Publication number: 20140323562
    Abstract: The present application provides compound of Formula X wherein A is an optionally substituted aliphatic or an optionally substituted aryl, and B is a moiety that stabilizes the partial positive charge at the carbon adjacent the divalent sulfur. The compound of Formula X is useful as a reversible antioxidant in a variety of applications. Also provided are methods of synthesizing the compound of Formula X.
    Type: Application
    Filed: November 23, 2012
    Publication date: October 30, 2014
    Inventors: Philip Jessop, Paul David Thornton, Shannon Marie Decker, Derek Pratt, Feng Zheng, Donna Lynn Leger
  • Patent number: 8871802
    Abstract: The present invention discloses novel naphtho[2,3-b]furan-4,9-diones and naphtho[2,3-b]thiophene-4,9-diones and methods of making and using the same. The present invention also discloses pharmaceutical compositions comprising novel naphtho[2,3-b]furan-4,9-dione or naphtho[2,3-b]thiophene-4,9-diones for the treatment of various indications including proliferative diseases.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: October 28, 2014
    Assignee: Zhoushan HaiZhongZhou Xinsheng Pharmaceuticals Co., Ltd.
    Inventors: Zhiwei Jiang, Aijin Wang, Xian Li, Qingrong Li, Hongwei Hu, Jiali Xu, Yuesong Hu, Yan Ye
  • Patent number: 8871801
    Abstract: A method of treating acquired perforating dermatosis. The method has the step of applying an amount of cantharidin to an area of skin in need of treatment thereof.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: October 28, 2014
    Inventor: Jacob Levitt
  • Patent number: 8871679
    Abstract: Fungicidal mixtures, comprising as active components 1) at least one 1-methylpyrazol-4-ylcarboxanilide of the formula I where R1?C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, X=hydrogen or halogen, Q=direct bond, a cyclopropylene or an anellated bicyclo[2.2.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: October 28, 2014
    Assignee: BASF SE
    Inventors: Markus Gewehr, Ulf Groeger, Egon Haden, Michael Vonend
  • Publication number: 20140309274
    Abstract: Compounds, methods, and compositions are provided for the treatment of cancer, neurological disorders, and fibrotic disorders. Specifically, the invention includes administering an effective amount of a compound of Formula I, II, or III, or a pharmaceutically acceptable composition, salt, isotopic analog, prodrug, or combination thereof, to a subject suffering from a cancer, neurological disorder, or fibrotic disorder.
    Type: Application
    Filed: March 28, 2014
    Publication date: October 16, 2014
    Applicant: Avoscience, LLC
    Inventor: Richard Huber
  • Patent number: 8859616
    Abstract: The present invention provides a method for stimulating hair growth in a mammalian species or converting vellus hair or intermediate hair to terminal hair or stimulating hair follicles to increase hair growth and one or more properties selected from the group consisting of luster, sheen, brilliance, gloss, glow, shine or patina of hair associated with the follicles or increasing one or more of: length, thickness, number, and density, of eyelash hair or eyebrow hair comprising applying to the skin of a patient a composition comprising an effective amount of an EP3 agonist or an EP4 agonist prodrug or a mixture thereof. Such compositions which are used in treating the skin or scalp of a human or non-human animal may comprise an effective amount of 3, 7 or 3 and 7 thia prostanoic acid. A mixture of 3,7-dithia PGE1 and 3,7-dithia PGE1-isopropyl ester is preferred for this treatment.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: October 14, 2014
    Assignee: Allergan, Inc.
    Inventors: Jenny W. Wang, David F. Woodward
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Publication number: 20140302564
    Abstract: A method for sterilizing microbial cells is provided. According to the method, microbial cells or a culture containing microbial cells are treated with a polyethylene glycol-based nonionic surfactant so that almost all of the microbial cells are sterilized while the enzyme activity expressed in the microbial cells is maintained at a high level. A method for sterilizing microbial cells and a material containing the sterilized microbial cells, in which the microbial cells are sterilized using a polyethylene glycol-based nonionic surfactant, can be used for foods so that the microbial cells are sterilized to be used in food production. Further, a material containing sterilized microbial cells can be used in processes for preparing tagatose, in which Corynebacterium genus microbial cells that produce Galactose and/or Arabinose isomerase are sterilized using a polyethylene glycol-based nonionic surfactant.
    Type: Application
    Filed: June 20, 2014
    Publication date: October 9, 2014
    Inventors: Jin Ha Kim, Yong Mi Lee, Seong Bo Kim, Taek Beom Kim, Yang Hee Kim, Seung Won Park
  • Patent number: 8853262
    Abstract: A pKa buffered vitamin C composition which includes a base alkalizer composition mixed with vitamin C (calcium ascorbate or ascorbic acid). The base alkalizer composition can be approximately 24% to 40% and the ascorbic acid or calcium ascorbate can be approximately 76% to 60% by weight of the vitamin C composition. When this vitamin C composition is orally administered to an individual (in capsule or tablet form), a rapid neutralization of his stomach acid occurs followed by a sustained pH of 6.0 to 7.5 for a thirty minute to two hour period. This allows the ingredients to be absorbed in his stomach, while preventing unpleasant reactions in his stomach. The base alkalizer composition can include the combination of a calcium carbonate carrier which acts as a mild alkalizer, an hydroxide (magnesium or potassium) which acts as a fast alkalizer, and a phosphate (dicalcium or tricalcium) which acts as a moderate alkalizer and which also maintains the pH fairly stable over a twenty to forty minute time period.
    Type: Grant
    Filed: February 14, 2007
    Date of Patent: October 7, 2014
    Assignee: Scientific Food Solutions, LLC
    Inventors: Ricky L. Falkenberg, Harold L. Archibald
  • Patent number: 8853282
    Abstract: A topical liquid formulation is provided which contains a combination of three active ingredients for treating fleas and ticks in domestic animals. Total concentration of the active hydrophobic and hydrophilic ingredients can exceed 60 weight percent. In contrast to commonly available flea treatments, the new insecticidal composition is safe and effective for both felines and canines and a single topical application can be effective for at least several weeks.
    Type: Grant
    Filed: May 22, 2014
    Date of Patent: October 7, 2014
    Assignee: Sumitomo Corporation
    Inventor: Ian Cottrell
  • Publication number: 20140294782
    Abstract: Disclosed are membrane-anchored polynucleotides, and compositions comprising the membrane-anchored polynucleotides. Also disclosed are the processes for the synthesis of these compounds, compositions comprising such compounds, and the use of such compounds and compositions in research and therapeutic applications.
    Type: Application
    Filed: November 1, 2012
    Publication date: October 2, 2014
    Inventors: Zev Jordan Gartner, Nicholas Scott Selden, Michael E. Todhunter, Samantha Isabel Liang, Robert Joseph Weber, Noel Youngho Jee, Jennifer S. Liu
  • Patent number: 8841332
    Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogs, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: September 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Samir Bennabi, Jurgen Benting, Stephane Brunet, Philippe Desbordes, Peter Dahmen, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Rachel Rama, Philippe Rinolfi, Valerie Toquin, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Patent number: 8840923
    Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: September 23, 2014
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Vincenzo Russo, Elisa Liberati, Nicola Cazzolla, Leonardo Marchitto, Lorella Ragni
  • Publication number: 20140271537
    Abstract: The present invention generally relates to deuterium-enriched aldehydes, compositions comprising deuterium-enriched aldehydes, and methods for slowing the rate of aldehyde autoxidation. In one aspect, the present invention provides a composition comprising a compound of structure 1: wherein: there are at least 6×1018 molecules of the aldehyde and Rx is hydrogen, wherein the deuterium isotope in Rx is in an amount greater than 0.10 percent of the hydrogen atoms present in Rx.
    Type: Application
    Filed: March 15, 2014
    Publication date: September 18, 2014
    Inventor: Anthony W. Czarnik
  • Patent number: 8835659
    Abstract: The present invention refers to compounds of formula (I): as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or chemoprevention of cancer, aging related diseases or processes, diabetes and neurodegenerative diseases.
    Type: Grant
    Filed: May 10, 2011
    Date of Patent: September 16, 2014
    Assignees: Ikerchem, S.L., Universidad del Pais Vasco
    Inventors: Fernando Pedro Cossio Mora, Leire Lidia Arias Echeverría, Yosu Ion Vara Zalazar, Eneko Aldaba Arévalo, Eider San Sebastián Larzabal, Aizpea Zubia Olascoaga
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Patent number: 8815924
    Abstract: Novel heterocyclic compounds of the formula (I), in which R1, D, W, T and T? have the meanings indicated in Claim 1, are SGK inhibitors and can be used for the treatment of SGK-induced diseases and conditions, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in fibroses and inflammatory processes of any type.
    Type: Grant
    Filed: April 4, 2005
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang
  • Patent number: 8808774
    Abstract: The described pKa process creates a unique combination of active ingredients. The calcium carbonate carrier is impregnated with various proportions of active ingredients and the compounds are made more effective by the sheer and absorption action as they are combined in the described process. The calcium carrier is adjusted to incorporate small amounts of highly efficient/effective pH adjusters. No natural solution exists in Nature with a pH of 10.6 that is optimal for adjusting the pKa naturally in foods. The present invention effects a change in the pKa of most acids and therefore impacts pH which can positively affect flavor, color and taste. The reduced moisture process in combination with the invention solution applied as a treatment results in fruits and vegetables that exhibit cleaner flavors, better texture, enhanced color and lower microbial counts than is found in standard IQF vegetables currently available.
    Type: Grant
    Filed: June 17, 2006
    Date of Patent: August 19, 2014
    Assignee: Scientific Food Solutions, LLC
    Inventors: Ricky L. Falkenberg, Harold L. Archibald, Danford Wilkinson, Lisa L. Trexler
  • Patent number: 8808755
    Abstract: A skin disinfectant in ready-to-use concentrated liquid or dry powdered form. Ready-to-use liquid forms have a pH of from about 2 to about 6 and include: (a) hydrogen peroxide in a concentration of from about 0.01 to about 4% w/w of the solution; (b) at least one surfactant chosen from imidazoline derivatives, alkyl betaines, alkyl amidopropyl betaine amides, alkyl amidopropyl betaines, alkylsulfo betaines, amine oxides and derivatives thereof in a concentration of from about 0.01 to about 15% w/w of the solution; (c) at least one hydrogen peroxide stabilizer in a concentration of from about 0.01 to about 4% w/w of the solution; (d) at least one member chosen from cyclic carboxylic acids and salts thereof in a concentration of from about 0.01 to about 4% w/w of the solution; and (e) at least one skin conditioning agent in a concentration of from about 0.01 to about 10% w/w of the solution.
    Type: Grant
    Filed: February 8, 2011
    Date of Patent: August 19, 2014
    Assignee: Virox Technologies Inc.
    Inventor: Navid Omidbakhsh
  • Publication number: 20140228375
    Abstract: The present invention involves new and original sigma receptors ligands: (Mono-or dialkylaminoalkyl)-?-butyrolactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)benzyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or diastereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Asteinizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, antimetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotective and cytoregenerative activity against the cytodegenerative diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: August 14, 2014
    Applicant: Anavex Life Sciences Corp.
    Inventor: Alexandre Vamvakides
  • Patent number: 8796326
    Abstract: A fire ant killer chemical composition (the “FAK Composition”) for effective killing of fire ants where the FAK Composition utilizes a minimal amount of active ingredients thereby significantly reducing safety concerns with respect to the use of said active ingredients, the FAK composition having a dish detergent composition and an insecticide composition.
    Type: Grant
    Filed: January 4, 2012
    Date of Patent: August 5, 2014
    Inventor: Harold V. Hutchins
  • Patent number: 8785492
    Abstract: Embodiments of the invention relate to the use of a melatonin agonist in the treatment of free running circadian rhythms in patients, including light perception impaired patients, e.g., blind patients, and to methods of measuring circadian rhythm.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: July 22, 2014
    Assignee: Vanda Pharmaceuticals Inc.
    Inventors: Marlene Michelle Dressman, John Joseph Feeney, Louis William Licamele, Mihael H. Polymeropoulos
  • Publication number: 20140193346
    Abstract: Herbal composition and method for the treatment of inflammatory pain associated with tendonitis, bursitis, arthritis, carpal tunnel syndrome, tennis elbow, plantar fasciitis, sports injuries, lower back pain and overexertion, gingivitis and muscle aches, that is compliant with HPUS monographs and/or over-the-counter FDA topical analgesic monograph requirements.
    Type: Application
    Filed: January 7, 2013
    Publication date: July 10, 2014
    Applicant: DRT LABORATORIES LLC
    Inventor: Ronit Arginteanu
  • Patent number: 8765804
    Abstract: The present invention relates to a pharmaceutical composition comprising specific compounds which may be obtained from Leontopodium alpinum Cass. (Edelweiss). A preferred compound is leoligin (=(2S,3R,4R)-4-(3,4-dimethoxybenzyl) -2-(3,4-dimethoxyphenyl)tetrahydrofuran-3-yl]methyl(2Z)-2-methylbut-2-enoat]). Corresponding means and methods in respect of medical uses of the compounds are described. The present invention also provides a medical device comprising, containing or having been contacted with the compound. The compounds provided herein may particularly be used in the treatment of hyperplastic diseases, in particular intimal hyperplasia, e.g. stenosis, restenosis, atherosclerosis and the like. Also envisaged herein is the use of these compounds in the treatment of proliferative diseases, such as leukemia, prostate cancer and lung cancer.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: July 1, 2014
    Assignee: Universität Innsbruck
    Inventors: Hermann Stuppner, Stefan Schwaiger, David Bernhard, Günther Laufer
  • Patent number: 8765805
    Abstract: Novel ligand compounds having the structural formula (I): in which: Ar is a radical selected from among the radicals of formulae (a)-(c) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, or, alternatively into cosmetic compositions.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: July 1, 2014
    Assignee: Galderma Research & Development
    Inventors: Thibaud Biadatti, Jean-Marie Arlabosse
  • Patent number: 8759315
    Abstract: A ribose-related compound is added to whole blood or packed red cells which have suboptimal function as measured by decreased levels of 2,3-DPG in order to rejuvenate the red blood cells to normal function as seen by raised levels of 2,3-DPG. Two representative ribose-related compounds are D-ribose and inosine.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: June 24, 2014
    Assignee: Viacell, LLC
    Inventors: John A St. Cyr, Daniel G Ericson, Clarence A Johnson
  • Publication number: 20140171444
    Abstract: The present invention provides aryl- or heteroaryl-diketo acid compounds effective to inhibit an activity of a Mycobacterial malate synthase enzyme or to inhibit a malate synthase activity in other bacteria having the enzyme. The compounds may be phenyl- naphthyl-, or thienyl-substituted diketo acids and carboxylate derivatives thereof. Also provided are methods of treating tuberculosis or other pathophysiological conditions associated with a malate synthase enzyme with the inhibitory compounds and methods of in silico design of the inhibitory compounds. In addition, the present invention provides the inhibitory compounds designed by this method. Furthermore, three-dimensional X-ray crystal structures of the Mycobacterial malate synthase complexed with the inhibitory compounds are provided. Further still a method for stabilizing an aromatic or heteroaromatic diketo acid or its prodrug or close analog in solution by derivatizing at least the ortho position on the aromatic ring is provided.
    Type: Application
    Filed: March 3, 2014
    Publication date: June 19, 2014
    Applicant: THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Joel S. Freundlich, James C. Sacchettini, Inna V. Kriger, Thomas R. Ioerger, Vijay Gawandi
  • Patent number: 8754242
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: June 17, 2014
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Melloney Tyte, Christopher John Matthews, Gavin John Hall, William Guy Whittingham, Jeffrey Steven Wailes, James Nicholas Scutt, Stephane André Marie Jeanmart, Russell Colin Viner
  • Publication number: 20140147691
    Abstract: The present invention relates to a preservative formulation for use in treating wood or other cellulosic materials, said formulation comprising: at least one biocidal metal compound; at least one preservative; and an aqueous carrier, wherein the preservative formulation has an uptake in the sapwood of less than about 220 l/m3 yet achieves substantially full penetration of the sapwood. Preferably, the preservative formulation is copper/tebuconazole in a ratio of about 25/1 w/w; and the wood is around 25 mm in thickness—for instance, decking timber.
    Type: Application
    Filed: June 29, 2012
    Publication date: May 29, 2014
    Applicant: ARCH WOOD PROTECTION PTY LTD
    Inventors: David Humphrey, Brett Skewes, Angelo Hrastov, Drago Bagaric, Peter Hausler, Shane McFarling, Greg Jensen, Steve Koch, Noel Koskela, Troy Justice
  • Patent number: 8735396
    Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: May 27, 2014
    Assignee: Pfizer Inc.
    Inventors: Jeffrey Allen Pfefferkorn, Anthony Lai Ling
  • Patent number: 8735445
    Abstract: Inhibitors of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), for example tetrazole, styrylpyrazole, phenylfuran, phenylthiophene, phenylpyrrazole, pyrazolecarboxamide, 2-thioacetamide and azo compounds, are useful for promoting or stimulating pigmentation of the skin and/or skin appendages and/or for preventing and/or for limiting depigmentation and/or whitening of the skin and/or skin appendages, notably for preventing and/or limiting canities.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: May 27, 2014
    Assignee: L'Oreal
    Inventors: Jean-Francois Michelet, Stephane Commo
  • Patent number: 8734772
    Abstract: Disclosed herein are cosmetic compositions comprising (a) at least one styrene-maleic anhydride copolymer bearing at least one group chosen from styrylpyridine and styrylpyridinium groups and (b) at least one co-film forming agent and/or at least one plasticizer. The cosmetic composition optionally further comprises at least one pigment and at least one solvent. Also disclosed herein are methods for making up and/or enhancing the appearance of a keratinous substrate comprising (1) forming a film on the keratinous substrate by applying to said keratinous substrate a cosmetic composition comprising (a) at least one styrene-maleic anhydride copolymer bearing at least one group chosen from styrylpyridine and styrylpyridinium groups and (b) at least one co-film forming agent and/or at least one plasticizer and (2) exposing the film to radiation chosen from UV and visible light radiation.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: May 27, 2014
    Assignee: L'Oreal
    Inventors: XianZhi Zhou, Jean-Thierry Simonnet, Hy Si Bui, Chunhua Li
  • Publication number: 20140140997
    Abstract: Provided are methods for treating or reducing the likelihood of developing a retroviral infection in a feline, decreasing retroviral virion entry into a feline cell, decreasing retroviral virion budding from a feline cell, or decreasing syncytium transmission in a feline. These methods require the administration of at least one agent that specifically binds to CD11a and/or CD18, or ICAM-1, and/or decreases or prevents the binding of LFA-1 (CD11a/CD18 heterodimer) to ICAM-1. Also provided are veterinary compositions and methods of identifying candidate agents useful for treating or reducing retroviral infection in a feline, decreasing retroviral virion entry into a feline cell, decreasing retroviral virion budding from a feline cell, or decreasing syncytium transmission in a feline.
    Type: Application
    Filed: June 15, 2012
    Publication date: May 22, 2014
    Applicant: CytoDyn Inc.
    Inventor: Richard Trauger
  • Publication number: 20140137808
    Abstract: The present invention is directed to an insect repelling device that may serve as an effective barrier against ticks. The insect repelling device may include a band of technical fabric, with the fabric being very stretchable. The insect repelling device may be worn around the ankles, wrist or head. The insect repelling device may be worn in pairs on each ankle and/or wrist. The insect repelling device may have an open, tubular design and be made of a high performance, nylon/ polyester fabric, allowing a user to easily insert the foot or hand and fit the device around the ankle or wrist area. Each insect repelling device may be pre-treated with an insecticide or insect repellant, such as Permethrin. In use, the insect repellant device may be effective at preventing biting insects, such as ticks, from crawling onto the user, for example from crawling up the legs of the user.
    Type: Application
    Filed: March 6, 2013
    Publication date: May 22, 2014
    Inventor: Simon J. WHITE
  • Publication number: 20140135374
    Abstract: Compounds are disclosed that are useful for treating ophthalmic conditions caused by or related to production of toxic visual cycle products that accumulate in the eye, such as dry adult macular degeneration, as well as conditions caused by or related to the misfolding of mutant opsin proteins and/or the mis-localization of opsin proteins. Compositions of these compounds alone or in combination with other therapeutic agents are also described, along with therapeutic methods of using such compounds and/or compositions. Methods of synthesizing such agents are also disclosed.
    Type: Application
    Filed: June 13, 2012
    Publication date: May 15, 2014
    Applicant: BIKAM PHARMACEUTICALS, INC.
    Inventor: David S. Garvey
  • Patent number: 8722910
    Abstract: A novel class of diyne compounds and diyne salts provided herein are effective and potent Ole1 protein inhibitors, useful for treating fungal pathogens. Compounds, fungicides and methods are provided as novel, potent and broad spectrum anti-fungal agents for treatment against a wide variety of fungal pathogens in humans and animals, and in the agricultural setting.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: May 13, 2014
    Assignee: Evolva AG
    Inventors: Jean-Philippe Meyer, Philipp Knechtle, Katrine Buch Greve, Alexandre M P Santana Sørenson
  • Patent number: 8722939
    Abstract: The present invention relates to the identification of provided cyclohexane-1,3-diones (CHD compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided CHD compounds.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: May 13, 2014
    Assignees: Northwestern University, Cambria Pharmaceuticals, Inc.
    Inventors: Donald R. Kirsch, Radhia Benmohamed, Anthony C. Arvanites, Richard I. Morimoto, Wei Zhang, Richard B. Silverman
  • Publication number: 20140128437
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Applicants: President and Fellows of Harvard College, TRUSTEES OF BOSTON UNIVERSITY, THE BRIGHAM AND WOMEN'S HOSPITAL, INC., Tufts University
    Inventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterrev, John A. Proco, JR.
  • Patent number: 8716322
    Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: May 6, 2014
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Han-Jie Zhou, Congcong M. Sun, Kevin D. Shenk, Guy J. Laidig
  • Patent number: 8716328
    Abstract: The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: May 6, 2014
    Inventors: James D. McChesney, John T. Henri, Sylesh Kumar Venkataraman, Mahesh Kumar Gundluru
  • Publication number: 20140105952
    Abstract: Compositions and methods for controlling and/or repelling bedbugs are provided. The compositions comprise one or more compounds having bedbug repellant activity. Such compounds may be, for example, naturally occurring semiochemicals or structural or functional analogs of naturally occurring semiochemicals. Exemplary compounds are compounds of general formula (I).
    Type: Application
    Filed: March 29, 2012
    Publication date: April 17, 2014
    Applicant: SemiosBIO Technologies Inc.
    Inventor: Michael Gilbert
  • Patent number: 8697681
    Abstract: The present invention provides an antitumor agent comprising cisplatin and a combination drug of tegafur/gimeracil/oteracil potassium that ensures an excellent life-prolongation effect in advanced gastric cancer patients that is superior to that of the standard therapy in Europe and the U.S. using an agent that contains 5-FU and does not contain a dihydropyrimidine dehydrogenase inhibitor, by way of selecting the patients based on dihydropyrimidine dehydrogenase.
    Type: Grant
    Filed: May 21, 2010
    Date of Patent: April 15, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventor: Toshinori Oka
  • Patent number: 8685975
    Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 1, 2014
    Assignee: Omeros Corporation
    Inventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
  • Patent number: 8669292
    Abstract: The invention provides compositions and formulations comprising catechol and/or acetogenins and various combinations thereof; including various combinations with other ingredients including botanical preparations containing acetogenin, an extract of green tea or a therapeutically active flavanoid contained in green tea; and one or more quinones. The invention includes a pharmaceutical composition including a salt of rhodizonic acid, an OH anion-generating base, a non-toxic acid, a quinone, a salt-containing sulfite, catechol and optionally, an acetogenin and an extract of green tea. The compositions and formulations demonstrate positive effects against a broad variety of cancer, autoimmune diseases, viruses and provides antioxidant protection against peroxyl hydrophilic, peroxyl lipophilic, hydroxyl, peroxynitrite and super oxide radicals. The compositions and formulations can be used for nutritional and nutraceutical uses, and used as dietary supplements.
    Type: Grant
    Filed: April 17, 2009
    Date of Patent: March 11, 2014
    Assignee: Orion Therapeutics, LLC
    Inventor: Jerome Godin
  • Patent number: 8664251
    Abstract: This invention relates to methods of treating T-cell mediated diseases or disorders in human or animal subjects, such as autoimmune diseases and chronic graft versus host disease in humans and animals. In particular, the methods comprise administering to the human or animal patient a pharmaceutical composition comprising a ryanodine receptor inhibitor.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: March 4, 2014
    Assignee: The Regents of the University of California
    Inventor: Alla F. Fomina
  • Patent number: 8658809
    Abstract: The subject of the present disclosure is a novel process for the preparation of N-[2-n-butyl-3-{4-[(3-dibutylamino)propoxy]benzoyl}-1-benzofuran-5-yl]methanesulfonamide of formula I: and the new intermediates of the preparation process.
    Type: Grant
    Filed: June 29, 2012
    Date of Patent: February 25, 2014
    Assignee: SANOFI
    Inventors: Antal Friesz, Mariann Csatarine Nagy
  • Patent number: 8658838
    Abstract: The present invention is directed to inhibitors of tyrosinase, pharmaceutical compositions comprising such tyrosinase inhibitors, and methods of making and using the same. Specifically, included in the present invention are compositions of matter comprised of at least one 2,4-dihydroxybenzene analog, which inhibit the activity of tyrosinase and which inhibit the overproduction of melanin.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: February 25, 2014
    Assignee: Unigen, Inc.
    Inventors: Sandip K. Nandy, Jiyun Liu, Alexandre Mikhailovitch Nesterov, Carmen Hertel, Abeysinghe A. Padmapriya
  • Patent number: 8648113
    Abstract: The present invention relates to a compound derived from mycelium of Antrodia camphorata. The present invention also relates to the composition or mycelium comprising the compounds of the invention. The composition of the invention decreases systolic blood pressure and increases high density lipoprotein.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: February 11, 2014
    Assignee: Simpson Biotech Co., Ltd.
    Inventors: Masao Hattori, Chia-Chin Sheu
  • Patent number: 8637496
    Abstract: The invention relates to the use of compounds having a monogalactosyldiacylglycerol (MGDG) synthase inhibitory activity as herbicide or algaecide, and to herbicide and algaecide compositions containing at least one of these compounds.
    Type: Grant
    Filed: June 2, 2008
    Date of Patent: January 28, 2014
    Assignees: Commissariat a l'Energie Atomique, Centre National de la Recherche Scientifique
    Inventors: Anne-Laure Bonneau, Cyrille Botte, Michael Deligny, Nadia Saidani, Hélène Hardre, Bernard Rousseau, Roman Lopez, Eric Marechal
  • Patent number: 8633182
    Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, R3, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: January 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dieter Hamprecht, Sara Frattini, Iain Lingard, Stefan Peters