Patents Issued in March 5, 2019
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Patent number: 10219987Abstract: A cosmetic composition for coating keratin fibers including: an aqueous phase, a surfactant system present at an amount greater than or equal to 15% by weight relative to the total weight of the composition including: i) at least one nonionic surfactant with an HLB value at 25° C. of less than 8, and ii) at least one nonionic surfactant with an HLB value at 25° C. of greater than or equal to 8, together forming a lamellar paracrystalline phase L?, and at least one aqueous dispersion of particles of at least one film-forming polymer, as well as methods of using these compositions are provided.Type: GrantFiled: September 23, 2014Date of Patent: March 5, 2019Assignee: L'OREALInventors: Philippe Ilekti, Nathalie Jager Lezer
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Patent number: 10219988Abstract: An oral care composition containing a gel network phase, potassium nitrate, an abrasive and a fluoride ion source. The gel network phase contains a fatty amphiphile and a secondary surfactant. The oral care composition contains at least about 12% fatty amphiphile and phase separation is not visually perceptible.Type: GrantFiled: March 31, 2017Date of Patent: March 5, 2019Assignee: The Procter & Gamble CompanyInventors: Sanjeev Midha, Lawrence Edward Dolan
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Patent number: 10219989Abstract: A method of producing mixtures of interference pigments having special effects comprises mixing at least one large particle size interference pigment with at least one normal size interference pigment of predetermined colors and in proportions desired to obtain a unique effect.Type: GrantFiled: March 28, 2016Date of Patent: March 5, 2019Assignee: MERCK PATENT GMBHInventors: Qinyun Peng, Philip Linz
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Patent number: 10219990Abstract: The present invention relates to the use of the compounds (A) corresponding to formula wherein R1 is hydrogen; a linear or branched C1-C30 aliphatic hydrocarbon residue comprising 0, 1, 2 or 3 double bonds; R2 independently from each other are hydrogen; methyl; ethyl; —OH; —COOR4; —CH2—OH; and —CH2—COOR4; R4 is hydrogen; or a linear or branched C1-C30 aliphatic hydrocarbon residue comprising 0, 1, 2 or 3 double bonds; R3 independently from each other are hydrogen; methyl; ethyl; —OH; —COOR5; —CH2—OH; and —CH2—COOR5; R5 is hydrogen; or a linear or branched C1-C30 aliphatic hydrocarbon residue comprising 0, 1, 2 or 3 double bonds; n is at least 0.Type: GrantFiled: December 9, 2015Date of Patent: March 5, 2019Assignee: BASF SEInventors: Laurence Pottie, Ansgar Behler, Stanislaw Krus, Jochen Giesinger
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Patent number: 10219991Abstract: The present invention relates to a composition comprising particles of at least one polymer that is surface-stabilized with a stabilizer, the polymer of the particles being a C1-C4 alkyl (meth)acrylate polymer; the stabilizer being an isobornyl (meth)acrylate polymer chosen from isobornyl (meth)acrylate homopolymer and statistical copolymers of isobornyl (meth)acrylate and of C1-C4 alkyl (meth)acrylate present in an isobornyl (meth)acrylate/C1-C4 alkyl (meth)acrylate weight ratio of greater than 4, at least one hydrocarbon-based oil and at least one silicone resin, and a mixture thereof. The invention also relates to a process for making up and/or caring for keratin materials, in which said composition is applied.Type: GrantFiled: December 11, 2015Date of Patent: March 5, 2019Assignee: L'OREALInventors: Laure Daubersies, Nathalie Gavache, Stephane Douezan
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Patent number: 10219992Abstract: The present disclosure relates to cosmetic compositions comprising an organosilane (A) having the formula: (R1)n(R2O)(3-n)SiR3O(CH2CH2O)a(C3H6O)bR4 where n is 1, 2, or 3, a?1, b may vary from 0 to 30, with the proviso a?b, R1 is a hydrocarbon group containing 1 to 12 carbon atoms, R2 is hydrogen or an alkyl group containing 1 to 6 carbon atoms, R3 is a divalent hydrocarbon group containing 2 to 12 carbon atoms, R4 is hydrogen, R1, or an acetyl group; and a cosmetic ingredient (B), and optionally in a cosmetically acceptable medium.Type: GrantFiled: November 4, 2016Date of Patent: March 5, 2019Assignee: Dow Corning CorporationInventors: Michael Salvatore Ferritto, Lenin James Petroff
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Patent number: 10219993Abstract: The invention relates to systems and methods for improving the appearance of the skin. The systems comprise 1) a skin-tightening composition comprising (a) at least one film former; (b) at least one polyvalent silicate thickener; (c) at least one anionic associative polymeric thickener; (d) at least one plasticizer; and (e) optionally, at least one cosmetic powder, and 2) a long-wear cosmetic composition comprising at least one silicone-polyamide copolymer, at least one silicone film former, and at least one volatile oil. Methods comprise applying the compositions of the systems on to the skin sequentially after a drying period.Type: GrantFiled: December 27, 2016Date of Patent: March 5, 2019Assignee: L'OREALInventors: Catherine Chiou, Angelike A. Galdi
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Patent number: 10219994Abstract: A method for the permanent shaping and color modification of keratinic in a single process includes the following steps. First, an aqueous composition, including at least one keratin-reducing compound and at least one alkalizing agent, is applied to the keratinic fibers and is left on the keratinic fibers for a period of 5 to 50 minutes at a temperature of 20 to 45° C. The keratinic fibers are rinsed, and optionally dried. Next, a composition including at least one oxidation dye precursor and at least one oxidizing agent is applied to the keratinic fibers and the keratinic fibers are deformed. That composition is allowed to act for 10 to 35 minutes. An aqueous composition including at least one oxidizing agent, is applied to the keratinic fibers for 30 seconds to 15 minutes. The keratinic fibers are rinsed out, along with removal of the deformation aids.Type: GrantFiled: April 14, 2017Date of Patent: March 5, 2019Assignee: Henkel AG & Co. KGaAInventors: Torsten Lechner, Yvonne Lissner, Birgit Rautenberg-Groth
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Patent number: 10219995Abstract: Described herein are methods and compositions for increasing the efficacy and decreasing the irritancy of topical formulations of hydroquinone.Type: GrantFiled: April 23, 2018Date of Patent: March 5, 2019Assignee: SHAMROC, INC.Inventors: Ronald M. Gurge, Mark W. Trumbore, Nupoor Devrajbhai Hirani
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Patent number: 10219996Abstract: The invention provides a composition suitable for topical skin application comprising isolated queen bee venom. The queen bee venom has been found to be significantly superior for treating skin conditions relative to the normal bee venom. Therefore the invention also provides a method of treatment or prevention of a skin condition, comprising the topical application of the composition onto the skin of a subject afflicted with the skin condition, or at risk of being afflicted with the skin condition. The skin condition could be skin ageing, elastosis, laxity (sagging), rhytids (wrinkles), skin infection, skin damage, skin burn, pain, and muscle tightness, or combinations thereof.Type: GrantFiled: August 23, 2013Date of Patent: March 5, 2019Inventor: Deborah Mitchell
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Patent number: 10219997Abstract: The present invention provides a novel radiosensitizer or anti-cancer chemotherapy sensitizer. In particular, the invention provides a radiosensitizer or anti-cancer chemotherapy sensitizer that can relieve the irritation of an affected area caused by hydrogen peroxide, is safe when injected into a human body, and can delay or reduce the degradation of hydrogen peroxide and thereby can efficiently exert a radiation sensitizing effect and an anti-cancer chemotherapy sensitizing effect. The radiosensitizer or anti-cancer chemotherapy sensitizer comprises a combination of (a) hydrogen peroxide and (b) hyaluronic acid or salt thereof.Type: GrantFiled: September 21, 2007Date of Patent: March 5, 2019Assignee: KOCHI UNIVERSITYInventor: Yasuhiro Ogawa
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Patent number: 10219998Abstract: Pharmaceutical formulations with a tropomyosin-related kinase inhibitor (“Trk inhibitor”) are disclosed. The pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine in microcrystalline suspension formulations in its monohydrate form, which shows improved characteristics over the anhydrate form, and in extended release formulations. The extended release pharmaceutical formulations comprise 3-(3-methoxy-4-((4-methoxybenzyl)oxy)benzyl)-6-(1-methyl-1H-pyrazol-4-yl)-3H-imidazo[4,5-b]pyridin-2-amine-loaded microspheres.Type: GrantFiled: December 17, 2015Date of Patent: March 5, 2019Assignee: Genzyme CorporationInventors: Harvey Lieberman, Donglai Yang, C. Michael Philbrook, Michael Santos, Chris Ho
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Patent number: 10219999Abstract: Use of a nicotine-cellulose combination for the preparation of a snuff composition for achievement of a fast onset of action of nicotine after application of the snuff composition to the oral cavity of a subject, wherein the composition has a high release rate so that when subjected to an in vitro dissolution test about 45% or more of the total content of nicotine is released within 30 minutes. Moreover, the invention relates to an improved snuff composition for application to the oral cavity.Type: GrantFiled: November 30, 2012Date of Patent: March 5, 2019Assignee: Niconovum USA, Inc.Inventors: Anders Axelsson, Arne Kristensen, Henri Hansson
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Patent number: 10220000Abstract: Compositions including pH sensitive lipid vesicles comprised of a lipid layer, an agent, and an organic halogen such that the agent is released from the vesicles after exposure to ionizing radiation. Methods of delivering the agent to a target in a subject using the compositions provided herein are also described. The methods allow for controlled release of the agent. The timing of release of the agent from the lipid vesicle may be controlled as well as the location of release by timing and localizing the exposure to ionizing radiation exposure.Type: GrantFiled: December 19, 2017Date of Patent: March 5, 2019Assignees: The Board of Trustees of the University of Arkansas, BioVentures, LLCInventors: Daniel Fologea, Ralph Henry, Greg Salamo, Yuriy Mazur, Michael J. Borrelli
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Patent number: 10220001Abstract: Methods and compositions are provided that load and encapsulate an agent, such as a protein, in a porous self-healing polymer. A delivery system includes a porous self-healing polymer, an ionic affinity trap within the pores of the self-healing polymer, and an agent associated with the ionic affinity trap. Methods of encapsulating an agent in a polymer include providing a porous self-healing polymer comprising an ionic affinity trap within the pores. The polymer is incubated with an agent having an affinity for the ionic affinity trap. At least a portion of the pores in the polymer are then healed. Active encapsulation of macromolecules at low concentrations may be achieved due to affinity of the agent for the ionic affinity trap within the pores.Type: GrantFiled: January 6, 2015Date of Patent: March 5, 2019Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Steven P. Schwendeman, Kashappa-Goud Desai
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Patent number: 10220002Abstract: Controlled-release formulations of carboxy-terminal C5a analogs (such as sustained-release formulations of the analogs), and their use in methods for treating and preventing an infection or a disease such as cancer, for directly killing microorganisms, for vaccine preparation, for inducing an immune response and for targeting antigen-presenting cells and other cells bearing a C5a receptor, are provided.Type: GrantFiled: November 30, 2012Date of Patent: March 5, 2019Assignee: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKAInventors: Joseph A. Vetro, Sam D. Sanderson
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Patent number: 10220003Abstract: Embodiments provide swallowable devices, preparations and methods for delivering viable cells (VC) into the GI tract including GI wall tissue or other tissue site. Particular embodiments provide a swallowable device such as a capsule for delivering VC into an intestinal wall or other site. The VC can be contained within a tissue-penetrating shell disposed in the capsule that protects the VC as they pass through the GI tract until they are inserted into GI tract tissue or other location. The shell desirably has shape, size and material consistency to be contained in a swallowable capsule, delivered from the capsule into solid tissue by the application of force on the shell and biodegrade within the solid tissue to release the VC into the tissue. Within the shell or other structure the VC can be maintained in a viability-sustaining gel that preserves the viability of the VC for selected time periods.Type: GrantFiled: March 9, 2017Date of Patent: March 5, 2019Assignee: InCube Labs, LLCInventors: Mir Imran, Joel Harris
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Patent number: 10220004Abstract: A method for controlled delivery of a substance into a body includes administering a plurality of containment vessels into the body, in which each of the plurality of containment vessels includes a quantity of the substance loaded therein prior to the administering; and providing a time-varying magnetic field such that the plurality of containment vessels are exposed thereto to cause a release of at least a portion of the substance from the plurality of containment vessels. Each of the plurality of containment vessels has an average outer diameter less than about 1 ?m.Type: GrantFiled: July 16, 2012Date of Patent: March 5, 2019Assignee: The Regents of the University of CaliforniaInventors: Jeffrey I. Zink, Courtney R. Thomas, Monty Liong, Sarah Ann Henscheid, Jinwoo Cheon, Jae-Hyun Lee, Daniel P. Ferris
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Patent number: 10220005Abstract: The present invention relates to a method of treating newborn hypoxic-ischemic encephalopathy (NHIE). Such method comprises administering the phytocannabinoid cannabidiol (CBD) in combination with therapeutic hypothermia to a newborn subject suffering from NHIE. Preferably the CBD is in the form of a plant extract, alternatively the CBD is in a pure or isolated form.Type: GrantFiled: June 10, 2013Date of Patent: March 5, 2019Assignee: GW Research LimitedInventors: Jose Martinez-Orgado, Geoffrey Guy
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Patent number: 10220006Abstract: A method of treating a host of neuromuscular, neurodegenerative, developmental, autoimmune and metabolic diseases/disorders related to aging, such as traumatic injury, stroke, Huntington's disease, Epilepsy, Multiple Sclerosis (MS), Lupus, Type-1 and Type-2 diabetes, Maturity Onset Diabetes of the Young (MODY), myasthenia gravis (MG), rheumatoid arthritis (RA), Graves' disease, Guillain-Barré syndrome (GB S), metabolic syndrome, Muscular Dystrophy or Duchenne Muscular Dystrophy (DMD), severe burns, aging, Amyotrophic Lateral Sclerosis (ALS), Friedreich's Ataxia, Batten Disease, Alzheimer's disease, optic neuritis, Leber's hereditary optic neuropathy (LHON), autism, Rett syndrome, Batten Disease, Angelman's Syndrome, Leigh disease, Fragile-X Syndrome, depression, Parkinson's disease, mitochondrial diseases, developmental disorders, metabolic disease disorders and/or autoimmune disorders by inducing endogenous BDNF expression with DNP treatment to protect from neuromuscular dysfunction/disorders and/or neurodegType: GrantFiled: September 18, 2017Date of Patent: March 5, 2019Assignee: Mitochon Pharmaceuticals, Inc.Inventors: Robert Alonso, John Gerard Geisler
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Patent number: 10220007Abstract: Provided herein are compositions and methods for preparing foods and beverages that contain additives, such as nutraceuticals, pharmaceuticals, and supplements, such as essential fatty acids, including omega-3 fatty acids, omega-6 fatty acids, conjugated fatty acids, and other fatty acids; phytochemicals, including phytosterols; other oils; and coenzymes, including Coenzyme Q10, and other oil-based additives.Type: GrantFiled: September 14, 2012Date of Patent: March 5, 2019Assignee: Virun, Inc.Inventor: Philip J. Bromley
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Patent number: 10220008Abstract: Using high-throughput screening, in an oxygen-glucose deprivation (OGD) model, isoxsuprine hydrochloride was identified as a potent neuroprotective compound. In an animal middle artery occlusion (MCAO) model of transient focal ischemia, isoxsuprine significantly reduced infarct volume compared to vehicle. The invention, therefore, provides methods of treatment and pharmaceutical compositions that are useful in the treatment and prevention of a wide-variety of ischemia-related injuries, including stroke.Type: GrantFiled: August 14, 2014Date of Patent: March 5, 2019Assignee: STC.UNMInventor: Jeff Wade Hill
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Patent number: 10220009Abstract: Formulations and methods are provided for improving the function, i.e. clinical outcome, of solid organ transplants. Lung transplantation is of particular interest. In the methods of the invention, a nanoparticle formulation comprising an effective dose of an iron chelator active agent in nanoparticle form, including without limitation, deferoxamine (DFO), deferasirox (DFX), and deferiprone (DFP), etc. suspended in a carrier compatible with the tissue of interest, is topically applied to the surface of tissues at the site of anastomosis. The nanoparticles are comprised of the active agent and a pharmaceutically acceptable stabilizer.Type: GrantFiled: August 30, 2013Date of Patent: March 5, 2019Assignees: The Board of Trustees of the Leland Stanford Junior University, The Johns Hopkins University, The United States of America as Represented by the Department of Veterans AffairsInventors: Mark R. Nicolls, Jayakumar Rajadas, Geoffrey C. Gurtner, Xinguo Jiang, Gundeep Dhillon, Gregg L. Semenza
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Patent number: 10220010Abstract: A sterile lyophilizate composition having improved stability and shelf-life. The lyophilizate includes from 30 to 100% of Mesna and 0 to 70% of an excipient. A process for the preparation of the sterile lyophilizate composition and a dosage unit formulation including the lyophilizate composition.Type: GrantFiled: January 15, 2018Date of Patent: March 5, 2019Assignee: AUXIN SURGERY SAInventor: Gilles Capart
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Patent number: 10220011Abstract: Treatment of intrahepatic cholestatic diseases by therapy with MBX-8025 or an MBX-8025 salt.Type: GrantFiled: September 29, 2017Date of Patent: March 5, 2019Assignee: CymaBay Therapeutics, Inc.Inventors: Pol Boudes, Charles A. McWherter
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Patent number: 10220012Abstract: A solution for lysis of particles and fibers that adhere to a lens capsule of the eye during cataract operations contains 0.5-3.5 wt.-% lysine, particularly L-lysine, in an isotonic to hypertonic aqueous solution.Type: GrantFiled: June 3, 2016Date of Patent: March 5, 2019Inventor: Joerg H. Krumeich
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Patent number: 10220013Abstract: The present disclosure relates to, inter alia, methods of treating mixed dyslipidemia with ethyl eicosapentaenoate.Type: GrantFiled: September 22, 2016Date of Patent: March 5, 2019Assignee: Amarin Pharmaceuticals Ireland LimitedInventors: Ian Osterloh, Pierre Wicker, Rene Braeckman, Paresh Soni, Mehar Manku
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Patent number: 10220014Abstract: The present invention relates to a method for treating and/or preventing Huntington disease and other polyglutamine diseases, comprising the step of administering an effective amount of a precursor of propionyl-CoA to an individual in need thereof.Type: GrantFiled: June 30, 2017Date of Patent: March 5, 2019Assignee: INSERM (Institut National de la Sante et de la Recherche Medicale)Inventors: Alexandra Durr, Fanny Mochel
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Patent number: 10220015Abstract: The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided.Type: GrantFiled: January 12, 2018Date of Patent: March 5, 2019Assignee: Zafgen, Inc.Inventors: Robert Zahler, James E. Vath
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Patent number: 10220016Abstract: This document provides methods and materials involved in assessing chemotherapy responsiveness and treating cancer (e.g., breast cancer). For example, methods and materials for determining whether or not a cancer patient (e.g., a breast cancer patient) is likely to respond to chemotherapy (e.g., a taxane therapy) based at least in part on the presence of a variant in the mammal's polycystic kidney disease gene 1 (PKD1) are provided. In addition, methods and materials involved in treating mammals having cancer (e.g., breast cancer) by administering an inhibitor of ubiquitin specific peptidase 2 (USP2) polypeptide activity (e.g., NSC-632839, a 2-cyano-pyrimidine, or a 2-cyano-triazine) in combination with another chemotherapeutic agent such as a taxane therapy are provided.Type: GrantFiled: February 17, 2016Date of Patent: March 5, 2019Assignee: Mayo Foundation for Medical Education and ResearchInventors: Matthew P. Goetz, Judy C. Boughey, Liewei Wang, Krishna R. Kalari, Richard M. Weinshilboum, Vera J. Suman
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Patent number: 10220017Abstract: The invention relates to novel liquid pharmaceutical compositions comprising at least one SGLT-2 inhibitor and one or more polar organic solvents, wherein the at least one SGLT-2 inhibitor comprises 1-cyano-2-(4-cyclopropyl-benzyl)-4-(?-D-glucopyranos-1-yl)-benzene according to formula (I): as well as corresponding processes of manufacturing such liquid pharmaceutical compositions and their medical uses.Type: GrantFiled: August 24, 2016Date of Patent: March 5, 2019Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Claudius Weiler, Thomas Duch, Marbod Haase, Timothy Shane Priddy, Heike Stettler
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Patent number: 10220018Abstract: Mitigation of long and short-term detrimental effects of exposure to low dose ionizing radiation by administration of genistein in the form of a nanosuspension to a mammal in an amount effective for achieving genistein serum levels of between 1-5 ?M in the mammal throughout a time period from exposure to the ionizing radiation to twelve hours after exposure to the ionizing radiation.Type: GrantFiled: May 11, 2018Date of Patent: March 5, 2019Assignee: Humanetics CorporationInventors: Michael D. Kaytor, John L. Zenk
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Patent number: 10220019Abstract: The present invention provides an application of a dimethylamino micheliolide for preparing a pharmaceutical product for treating pulmonary fibrosis.Type: GrantFiled: January 28, 2016Date of Patent: March 5, 2019Assignees: Tianjin International Joint Academy of Biotechnology & Medicine, ACCENDATECHInventors: Tao Sun, Yue Chen, Cheng Yang, Honggang Zhou, Huijuan Liu, Yanrong Liu, Jing Wang, Chengyu Zhang, Qiang Zhang, Xiangming Zhang, Yuan Qin, Xueshuang Jing
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Patent number: 10220020Abstract: The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form.Type: GrantFiled: December 23, 2011Date of Patent: March 5, 2019Assignee: NEKTAR THERAPEUTICSInventors: Antoni Kozlowski, Sean M. Culbertson, Xiaoming Shen, Samuel P. Mcmanus, Mark A. Wilson
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Patent number: 10220021Abstract: Uses of melanin and its derivatives, analogs, and precursors for the treatment and prevention of ocular diseases, disorders, and conditions, are described. Melanin, or a derivative, analog, or precursor thereof, such as synthetic melanin or natural melanin, is applied to the eye by topical application or injection. Examples of ocular diseases, disorders, and conditions that can be treated or prevented by the methods described herein include hyperemia, leukoplakia, corneal angiogenesis, and corneal keratoconus.Type: GrantFiled: September 8, 2015Date of Patent: March 5, 2019Inventor: Arturo Solis Herrera
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Patent number: 10220022Abstract: Compositions and Methods are described in which Albendazole sulfone binds to Wolbachia FtsZ providing anti filarial activity.Type: GrantFiled: July 20, 2018Date of Patent: March 5, 2019Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Laura Serbus, Fredric Landmann, Catharina Lindley, Pamela White, William Sullivan
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Patent number: 10220023Abstract: The present invention relates to a dosing regimen for (R)-5-[3-chloro-4-(2,3-dihydroxy-propoxy)-benz[Z]ylidene]-2-([Z]-propylimino)-3-o-tolyl-thiazolidin-4-one.Type: GrantFiled: December 10, 2015Date of Patent: March 5, 2019Assignee: ACTELION PHARMACEUTICALS LTDInventors: Jasper Dingemanse, Matthias Hoch, Andreas Krause
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Patent number: 10220024Abstract: An object of the present invention is to provide a cancer cell inhibitory drug, particularly a cancer stem-cell inhibitory drug, or a cancer stem-cell detection probe. A cancer cell inhibitory drug containing at least a compound represented by general formula (1).Type: GrantFiled: November 15, 2016Date of Patent: March 5, 2019Assignee: CANON KABUSHIKI KAISHAInventors: Taichi Shintou, Tsuyoshi Nomoto, Kohei Watanabe, Takeshi Miyazaki, Toshio Tanaka, Yasuhito Shimada, Yuhei Nishimura
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Patent number: 10220025Abstract: A solid self-micro/nano emulsifying formulation comprising CARP-1 functional mimetics (CFM; e.g., CFM-4.16 or CFM-4.17) for oral administration, and methods of fabrication and use thereof to treat cancer (e.g., breast cancer, triple negative breast cancer, resistant lung cancer, and non-resistant lung cancer) and reduce tumor volume. Solid self-micro/nano emulsifying formulation of CFM compounds was found to have significantly enhanced drug loading, aqueous solubility, and oral bioavailability of the formulation.Type: GrantFiled: November 7, 2017Date of Patent: March 5, 2019Assignee: Florida A&M UniversityInventors: Mandip Sachdeva, Ketankumar Patel, Arun Rishi
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Patent number: 10220026Abstract: The problem addressed by the present invention is to develop a pharmaceutical having therapeutic efficacy against epirubicin-resistant tumors. The present invention provides a micelle having an anti-cancer agent disposed inside the core of the micelle formed by an epirubicin-conjugated copolymer.Type: GrantFiled: August 11, 2015Date of Patent: March 5, 2019Assignees: THE UNIVERSITY OF TOKYO, TOKYO INSTITUTE OF TECHNOLOGYInventors: Hiroaki Kinoh, Kazunori Kataoka, Horacio Cabral, Yutaka Miura, Shigeto Fukushima, Nobuhiro Nishiyama, Tsukasa Chida
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Patent number: 10220027Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.Type: GrantFiled: October 13, 2017Date of Patent: March 5, 2019Assignee: GILEAD SCIENCES, INC.Inventors: Olaf Kinzel, Christoph Steeneck, Claus Kremoser
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Patent number: 10220028Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein A, B and D are each oxygen or sulfur, provided that least one of A, B and D is sulfur; and R1-R8 are each independently hydrogen, hydroxyl, acyl, substituted acyl, acyloxy, substituted acyloxy, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, amino, substituted amino, halogen, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, substituted heteroaryl, or a thio-containing group.Type: GrantFiled: March 13, 2017Date of Patent: March 5, 2019Assignee: The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: Nigel H. Greig, Weiming Luo, David Tweedie, Harold W. Holloway, Qian-Sheng Yu, Edward J. Goetzl
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Patent number: 10220029Abstract: The present invention relates to novel biologically active glutarimide derivatives of general formula (I) or a pharmaceutically acceptable salt thereof, their use as a therapeutic agent for the treatment of eosinophilic diseases, preferably of allergic nature, in particular bronchial asthma, allergic rhinitis, polypous rhinosinusopathies, eosinophilic colitis, eosinophilic syndrome, allergic conjunctivitis, atopic dermatitis, Churg-Strauss syndrome, anaphylactic shock, Quincke's edema, eosinophilic vasculitis, eosinophilic esophagitis, eosinophilic gastroenteritis, or fibroses.Type: GrantFiled: December 18, 2017Date of Patent: March 5, 2019Assignee: OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”Inventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Anastasia Vladimirovna Rydlovskaya, Alexander Grigorievich Chuchalin
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Patent number: 10220030Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.Type: GrantFiled: November 14, 2017Date of Patent: March 5, 2019Assignee: GlaxoSmithKline Intellectual Property Development LimitedInventors: Michael Jonathan Bury, Linda N. Casillas, Adam Kenneth Charnley, Pamela A. Haile, Robert W. Marquis, Jr., John F. Mehlmann, Joseph J. Romano, Robert R. Singhaus, Jr., Gren Z. Wang
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Patent number: 10220031Abstract: Potent modulators of RNA function can be assembled in cellulo by using the cell as a reaction vessel and a disease-causing RNA as a catalyst. When designing small molecule effectors of function, a balance between permeability and potency must be struck. Low molecular weight compounds are more permeable while higher molecular weight compounds are more potent. The advantages of both types of compounds could be synergized if low molecular weight molecules could be transformed into potent, multivalent ligands via a reaction catalyzed by binding to a target in cells expressing a genetic defect. We demonstrate that this approach is indeed viable in cellulo. Small molecule modules with precisely positioned alkyne and azide moieties bind adjacent internal loops in r(CCUG)exp, the causative agent of myotonic dystrophy type 2 (DM2), and are transformed into oligomeric, potent inhibitors of DM2 RNA dysfunction via a 1,3 Huisgen dipolar cycloaddition reaction, a variant of click chemistry.Type: GrantFiled: July 17, 2015Date of Patent: March 5, 2019Assignee: The Scripps Research InstituteInventors: Matthew D. Disney, Suzanne G. Rzuczek
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Patent number: 10220032Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor sub-type 2 (“mGluR2”) of Formula I: The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such com-pounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.Type: GrantFiled: July 30, 2015Date of Patent: March 5, 2019Assignee: Janssen Pharmaceutica NVInventors: Susana Conde-Ceide, Michiel Luc Maria Van Gool, María Luz Martín-Martín
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Patent number: 10220033Abstract: Implementations of the present invention include a compound and methods for inhibiting karyopherin beta 1 activity by administering to a patient in need thereof a therapeutically effective amount of a substituted benzoxazepine. The compound of Formula II, 9-[(1-methylpiperidin-3-yl)methoxy]-4-[(6-methylpyridin-2-yl)methyl]-7-(5-methylthiophen-2-yl)-3,5-dihydro-2H-1,4-benzoxazepine or one of its salts, inhibits the import of protein and transcription factors, such as NFAT and P65/NFKB into the nucleus of a cell, and thus has anti-cancer effects enabling the compound to be used for cancer treatment.Type: GrantFiled: March 23, 2018Date of Patent: March 5, 2019Assignees: University of Cape Town, University of Louisville Research Foundation Inc.Inventors: Virna Drucille Leaner, Pauline Janet Van Der Watt, John Olaf Trent
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Patent number: 10220034Abstract: Novel assembly effector compounds having a therapeutic effect against hepatitis B viral (HBV) infection are disclosed. Assembly effector molecules described herein can lead to defective viral assembly and also may affect other viral activities associated with chronic HBV infection. Also disclosed is a process to synthesize disclosed compounds, method of treatment of HBV by administration of disclosed compounds, and use of these compounds in the manufacture of medicaments against HBV.Type: GrantFiled: October 16, 2014Date of Patent: March 5, 2019Assignee: Indiana University Research and Technology CorporationInventors: Adam Zlotnick, Lichun Li, William W. Turner, Jr., Samson Francis
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Patent number: 10220035Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: GrantFiled: June 25, 2015Date of Patent: March 5, 2019Assignee: RHIZEN PHARMACEUTICALS SAInventors: Dhanapalan Nagarathnam, Swaroop K. Vakkalanka, Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Prashant K. Bhavar
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Patent number: 10220036Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.Type: GrantFiled: December 21, 2015Date of Patent: March 5, 2019Assignee: Novartis AGInventors: Ho Man Chan, Xiang-Ju Justin Gu, Ying Huang, Ling Li, Yuan Mi, Wei Qi, Martin Sendzik, Yongfeng Sun, Long Wang, Zhengtian Yu, Hailong Zhang, Ji Yue (Jeff) Zhang, Man Zhang, Qiong Zhang, Kehao Zhao