Patents Issued in November 12, 2019
  • Patent number: 10471014
    Abstract: Disclosed herein are compositions comprising a drug such as a triptan (e.g. rizatriptan) and/or an NSAID (e.g. meloxicam) in combination with a cyclodextrin and/or a carbonate or a bicarbonate. These compositions may be orally administered, for example, to improve the bioavailability, solubility, or pharmacokinetics of the drug for the treatment of conditions such as pain.
    Type: Grant
    Filed: June 6, 2018
    Date of Patent: November 12, 2019
    Assignee: AXSOME THERAPEUTICS, INC.
    Inventor: Herriot Tabuteau
  • Patent number: 10471015
    Abstract: The present invention relates generally to abuse-deterrent formulations containing dextroamphetamine sulfate.
    Type: Grant
    Filed: April 2, 2018
    Date of Patent: November 12, 2019
    Assignee: Vallon Pharmaceuticals, Inc.
    Inventors: Yaron Daniely, David Baker, Hanna Ron, David Siner
  • Patent number: 10471016
    Abstract: The invention relates to microparticles comprising a crosslinked gel and methods for making and using same.
    Type: Grant
    Filed: March 8, 2018
    Date of Patent: November 12, 2019
    Assignee: President and Fellows of Harvard College
    Inventors: David J. Mooney, David A. Weitz, Stefanie Utech, Radivoje Prodanovich, Esther Amstad, Raluca Ostafe, Angelo S. Mao, Connie Chang Wilking, Huanan Wang
  • Patent number: 10471017
    Abstract: There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more task-masked active pharmaceutical ingredient(s), rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates on contact with saliva in the buccal cavity forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing the active), coated with a taste-masking membrane comprising a water-insoluble polymer and one or more gastrosoluble inorganic or organic pore-formers (practically insoluble in water and saliva, but soluble in an acidic buffer), exhibit acceptable taste-masking when placed in the oral cavity and provide rapid, substantially-complete release of the dose on entry into the stomach.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: November 12, 2019
    Assignee: ADARE PHARMACEUTICALS, INC.
    Inventors: Jin-Wang Lai, Gopi M. Venkatesh, Ken Kangyi Qian
  • Patent number: 10471018
    Abstract: A computer-implemented method for image-guided delivery of a nanoparticle mixture to a target tumor located in a region of interest includes selecting a non-hypoxic delivery location within the region of interest for delivery of a non-bacteria-associated nanoparticle component included in the nanoparticle mixture and selecting a hypoxic delivery location within the region of interest for delivery of a bacteria-associated nanoparticle component included in the nanoparticle mixture. An image-guided delivery and monitoring process may then be performed.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: November 12, 2019
    Assignee: Siemens Medical Solutions USA, Inc.
    Inventors: Ankur Kapoor, Dorin Comaniciu
  • Patent number: 10471019
    Abstract: Provided is a monodisperse agglomerate of a substance-containing vesicle filled with a substance at a concentration higher than conventionally possible. A mixed solution, in which a target substance is included in an aqueous medium, is mixed with a monodisperse agglomerate of a crosslinked vesicle comprising a prescribed polymer which includes a first polymer, i.e. a block copolymer having uncharged hydrophilic segments and first charged segments, and a second polymer having second charged segments carrying a charge opposite to that of the first charged segments, and in which the first polymer and/or the second polymer are/is crosslinked. As a result, the crosslinked vesicle is made to contain the target substance.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: November 12, 2019
    Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Kazunori Kataoka, Akihiro Kishimura, Yasutaka Anraku, Akinori Goto
  • Patent number: 10471020
    Abstract: The present invention generally relates to particles, including nanoparticles, for example, for drug delivery or other applications. Certain aspects of the present invention are generally directed to particles, such as nanoparticles, comprising an inner portion and a coating. The inner portion may contain insulin or other therapeutic molecules for delivery to a living organism. In some cases, the molecules may be electrostatically complexed with an oppositely-charged peptide, such as an oligoarginine, or other species. The therapeutic molecules may also be water soluble. In some cases, the peptide may be conjugated to a hydrophobic portion, such as cholesterol, lauric acid, or a fatty acid chain. This hydrophobic modification may facilitate complex formation with the therapeutic molecule and the stability of the resulting complex. The complex typically is surrounded by a coating, which may protect the complex. For example, the coating may include polymers such as poly(glutamic acid) and poly(ethylene glycol).
    Type: Grant
    Filed: November 14, 2016
    Date of Patent: November 12, 2019
    Assignee: Universidade de Santiago de Compostela
    Inventors: Maria Josefa Alonso Fernandez, Zhigao Niu, Manuel Jesus Santander Ortega
  • Patent number: 10471021
    Abstract: The invention relates to a transdermal therapeutic system (TTS), which is suited for the administration of a peptide to a patient through skin treated with ablation. The transdermal therapeutic system includes a back layer and an active substance-containing layer that contains at least one peptide and a carrier substance, preferably as a textile web material.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: November 12, 2019
    Assignee: LTS Lohmann Therapie-Systeme AG
    Inventors: Michael Horstmann, Gerd Hoffmann, Sandra Wiedersberg
  • Patent number: 10471022
    Abstract: The present technology relates to a method of treating one or more behavioral symptoms of Fragile X Syndrome in a subject by transdermally administering an effective amount of cannabidiol (CBD) to the subject wherein one or more behavioral symptoms of Fragile X Syndrome are treated in the subject.
    Type: Grant
    Filed: January 16, 2019
    Date of Patent: November 12, 2019
    Assignee: ZYNERBA PHARMACEUTICALS, INC.
    Inventors: Marcel Bonn-Miller, Nancy Tich, Donna Gutterman, John Messenheimer, Terri Sebree
  • Patent number: 10471023
    Abstract: Compounds having a structure of Formula I, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, L1, L2, L3, X, a, b, c, n, and m are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity and uses as therapeutics as well as methods for treatment of subjects in need thereof, including prostate cancer are also provided.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: November 12, 2019
    Assignees: British Columbia Cancer Agency Branch, The University of British Columbia
    Inventors: Raymond John Andersen, Kunzhong Jian, Marianne Dorothy Sadar, Nasrin R. Mawji, Carmen Adriana Banuelos
  • Patent number: 10471024
    Abstract: The invention is an increased effectiveness of allylamine drug compounds for topical treatment of fungal infections of skin and skin appendages. The allylamine active ingredient is prepared in an acidic environment; the acidic environment altering the physiochemical properties of the active ingredient resulting in the active ingredient having a positive charge. The positive charge and enhancers used in the formula allow for increased penetration of the active ingredient through skin and skin appendages. The positively charged active ingredients are either dissolved in the vehicle directly or dissolved in a plurality of beads suspended in the vehicle.
    Type: Grant
    Filed: January 11, 2017
    Date of Patent: November 12, 2019
    Assignee: BIOPHILE CORPORATION, LTD.
    Inventors: Nardo Zaias, Pichit Suvanprakorn, Panida Vayumhasuwan
  • Patent number: 10471025
    Abstract: The present invention relates to methods of treating and managing Parkinson's disease and related disorders. The methods especially find use in managing motor symptoms, including gait problems, particularly during advanced stages when effectiveness of standard medications wear off or side effects become problematic, as seen in Parkinson's disease, other disorders treated with dopaminergic agents, and other conditions associated with motor problems, such as aging or stroke. The treatment also may include disease-modifying effects, neuroprotection of, or neurorescue effects on neuronal cells in patients with Parkinson's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: November 12, 2019
    Inventors: Nuno Afonso, Sara Sousa, Rita Vaz, Diana Chapela, Sofia Côrte-Real
  • Patent number: 10471026
    Abstract: The inventive subject matter is directed to compositions and methods for ready-to-inject norepinephrine compositions with improved stability. Most preferably, compositions presented herein are substantially antioxidant free and exhibit less than 10% isomerization of R-norepinephrine and exhibit less than 5% degradation of total norepinephrine.
    Type: Grant
    Filed: October 17, 2018
    Date of Patent: November 12, 2019
    Assignee: Nevakar Inc.
    Inventors: Tushar Hingorani, Prem Sagar Akasapu, Kumaresh Soppimath
  • Patent number: 10471027
    Abstract: Described herein are methods for the treatment of an ophthalmic disease or disorder comprising the administration of non-retinoid visual cycle modulators. Ophthalmic diseases and disorders which can be treated according to the methods provided herein include age-related macular degeneration (AMD), Stargardt's disease, glaucoma, and other disorders that adversely affect the retina.
    Type: Grant
    Filed: July 2, 2010
    Date of Patent: November 12, 2019
    Assignee: ACUCELA, INC.
    Inventors: Ryo Kubota, Nancy Boman, Claes Bavik, Ian L. Scott
  • Patent number: 10471028
    Abstract: Small molecule efflux pump inhibitors are provided, as well as methods for their use in treating infections. Also provided herein are methods of using the small molecule efflux pump inhibitors to restore the antibiotic susceptibility of microbes.
    Type: Grant
    Filed: June 12, 2015
    Date of Patent: November 12, 2019
    Assignee: UNIVERSITY OF ROCHESTER
    Inventors: Paul M. Dunman, Catlyn E. Blanchard
  • Patent number: 10471029
    Abstract: Disclosed herein are methods and compositions for treating, ameliorating, and/or preventing Alzheimer's disease in ApoE4-postitive patients using particular compounds and compositions thereof.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: November 12, 2019
    Assignee: Alzheon, Inc.
    Inventors: Martin Tolar, John A. Hey, Petr Kocis, Jeremy Yu
  • Patent number: 10471030
    Abstract: Disclosed herein are methods for treating cancer comprising administering CAR-modified immune cells and at least one Retinoic Acid Receptor and/or Retinoid X Receptor active agent.
    Type: Grant
    Filed: January 31, 2019
    Date of Patent: November 12, 2019
    Assignee: lo Therapeutics, Inc.
    Inventors: Roshantha A. Chandraratna, Martin E. Sanders
  • Patent number: 10471031
    Abstract: The present invention provides a simple and improved dose form that is capable of providing a controlled release of GABAB receptor agonist contained in the core thereof. The invention also provides methods of administering the dosage form and of treating conditions that are therapeutically responsive to GABAB receptor agonist.
    Type: Grant
    Filed: February 8, 2019
    Date of Patent: November 12, 2019
    Assignee: OSMOTICA KERESKEDELMI ES SZOLGALTATO KFT
    Inventors: Glenn A. Meyer, Cristian R. Franco, Gustavo A. Fischbein, Alejandro A. Aguilar, Claude E. Wright
  • Patent number: 10471032
    Abstract: The present disclosure provides compounds, compositions, and dietary supplements useful for the treatment of a body weight condition or a thyroid disorder. The compounds induce increased T3 levels while preventing thyroidal atrophy. Also provided are compounds, compositions, and dietary supplements useful for the treatment of a disease or condition that is estrogen sensitive, estrogen receptor dependent or estrogen receptor mediated such as breast cancer.
    Type: Grant
    Filed: May 30, 2017
    Date of Patent: November 12, 2019
    Assignee: THERMOLIFE INTERNATIONAL, LLC
    Inventors: Ronald Kramer, Alexander Nikolaidis
  • Patent number: 10471033
    Abstract: A method of promoting a desired oral microbiota to treat an inflammation condition related to an allergic reaction in a subject in need of such treatment including providing a preformulated edible composition including an amino acid containing ingredient comprising L-arginine, the composition configured to be present as individual molecules of L-arginine within an oral cavity of the subject; removing a biofilm from surfaces within an oral cavity including exposing the biofilm to a biofilm degrading enzyme; wherein during or following removal of the biofilm, the composition is provided contained and at least partially dissolved within an oral cavity of the subject for a period of at least from about 30 seconds to about an hour on a daily basis comprising at least one day to promote an increased concentration of selected oral microbiota, the selected microbiota including Veillonella and Streptococcus.
    Type: Grant
    Filed: June 6, 2018
    Date of Patent: November 12, 2019
    Assignee: Knoze Jr. Corporation
    Inventor: Shunsheng Han
  • Patent number: 10471034
    Abstract: This disclosure provides pharmaceutical compositions comprising amino acid entities and uses thereof. Methods for improving liver function and for treating liver diseases comprising administering an effective amount of the compositions to a subject in need thereof are also disclosed.
    Type: Grant
    Filed: December 5, 2018
    Date of Patent: November 12, 2019
    Assignee: AXCELLA HEALTH INC.
    Inventors: Michael Hamill, Raffi Afeyan, Chung-Wei Lee, Harry Luithardt
  • Patent number: 10471035
    Abstract: The invention includes compositions and methods of using meroterpene esters for effectively modulating skin cell function and remediating undesirable skin conditions, as well as the use of such compositions in the treatment of systemic diseases, such as cancer and in nutritional, dermatologic and cosmetic applications, through topical and transbuccal delivery as well as by ingestion, injection or inhalation.
    Type: Grant
    Filed: October 19, 2015
    Date of Patent: November 12, 2019
    Assignee: Sunny BioDiscovery
    Inventor: Krzysztof Bojanowski
  • Patent number: 10471036
    Abstract: Antimicrobial compositions, especially those useful when applied topically, particularly to mucosal tissues (i.e., mucous membranes), including, in particular, an antimicrobial lipid component, such as a fatty acid ester, fatty ether, or alkoxide derivative thereof. The compositions can also include an enhancer component, a surfactant, a hydrophobic component, and/or a hydrophilic component. Such compositions provide effective topical antimicrobial activity and are accordingly useful in the treatment and/or prevention of conditions that are caused, or aggravated by, microorganisms (including viruses).
    Type: Grant
    Filed: July 15, 2013
    Date of Patent: November 12, 2019
    Assignee: 3M Innovative Properties Company
    Inventors: Matthew T. Scholz, Dianne L. Gibbs, John T. Capecchi, Jeffrey F. Andrews
  • Patent number: 10471037
    Abstract: The present application in one aspect provide Fc-containing polypeptide conjugates comprising an Fc-containing polypeptide conjugated to a conjugate moiety, wherein the Fc-containing polypeptide comprises an N-glycosylated Fc region comprising an acceptor glutamine residue flanked by an N-glycosylation site and wherein the conjugate moiety is conjugated to the Fc-containing polypeptide via the acceptor glutamine residue. Also provided are methods of making such Fc-containing polypeptide conjugates by using a wildtype or engineered transglutaminases. Further provided are engineered transglutaminases specifically designed for carrying out such reactions.
    Type: Grant
    Filed: May 22, 2018
    Date of Patent: November 12, 2019
    Assignee: CSPC Dophen Corporation
    Inventors: Sean Hu, Lisha Allen
  • Patent number: 10471038
    Abstract: The present invention relates to a calpain activation inhibitor, muscle damage inhibitor, muscle endurance improver or muscle fatigue recovery agent containing an ?-methylsulfinylalkyl isothiocyanate or physiologically acceptable salt thereof as an active ingredient, foods or beverages, pharmaceuticals or cosmetics containing the same, a pharmaceutical for the prophylaxis and/or treatment of diseases related to muscle damage or diseases related to reduced muscle mass caused by aging, and a method for the use thereof.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: November 12, 2019
    Assignee: PRODUCTIVE AGING LABORATORY, CO., LTD.
    Inventors: Yo-ichi Nabeshima, Chiaki Abe, Yoshihiro Uto, Ryuji Hiramatsu
  • Patent number: 10471039
    Abstract: A method for treating skin cancer including the steps of applying an isothiocyanate functional surfactant to an area affected by skin cancer, wherein the isothiocyanate functional surfactant comprises at least one isothiocyanate functional group associated with an aliphatic and/or aromatic carbon atom of the isothiocyanate functional surfactant.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: November 12, 2019
    Assignee: The William M. Yarbrough Foundation
    Inventor: Michael E. Silver
  • Patent number: 10471040
    Abstract: The present invention relates generally to intranasal pharmaceutical compositions. In particular, the present invention is directed to sustained, enhanced delivery of pharmaceutical agents across the nasal mucosa for systemic drug delivery.
    Type: Grant
    Filed: September 30, 2015
    Date of Patent: November 12, 2019
    Assignee: Lachesis Biosciences Limited
    Inventor: Timothy Matthias Morgan
  • Patent number: 10471041
    Abstract: Use of genistein for the treatment and prevention of dry eye syndrome or LKC and corresponding compositions containing it.
    Type: Grant
    Filed: January 8, 2018
    Date of Patent: November 12, 2019
    Assignee: DSM IP ASSETS B.V.
    Inventors: Kevin Prudence, Christoph Riegger, Wolfgang Schalch
  • Patent number: 10471042
    Abstract: The present disclosure provides a composition of artesunate, a process of preparing the same, and a method of treatment.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: November 12, 2019
    Inventors: Ming Zhao, Li-Ming Zhou
  • Patent number: 10471043
    Abstract: The invention relates to compounds of Formula (I), wherein the variables are as defined in the claims, which are useful in the treatment and/or prevention of bacterial infections in a subject. The invention further relates to the use of a compound of Formula (I) in the manufacture of a medicament, and medical devices when used in a method of treating or preventing a bacterial infection in a subject, and related aspects.
    Type: Grant
    Filed: December 2, 2016
    Date of Patent: November 12, 2019
    Assignee: Ultupharma AB
    Inventors: Anders Broberg, Pierre Andersson, Jolanta Levenfors, Joakim Bjerketorp, Christer Sahlberg
  • Patent number: 10471044
    Abstract: Provided is a medicinal composition characterized by comprising an alkyl ether derivative represented by general formula [1] [wherein: R1 and R2 are the same or different and represent a hydrogen atom, a halogen atom, an optionally substituted C1-6 alkyl group, an optionally substituted aryl group, etc.; R3 represents an optionally protected hydroxyl group, etc.; and m and n are the same or different and represent an integer of 1 to 6] or a salt thereof. The medicinal composition according to the present invention is useful as a post nerve injury rehabilitation effect-enhancing agent.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: November 12, 2019
    Assignee: FUJIFILM Toyama Chemical Co., Ltd.
    Inventors: Takuya Takahashi, Tomohiro Okuda
  • Patent number: 10471045
    Abstract: Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I): The present methods include administering to a subject an effective amount of one or more compounds of Formula (I). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.
    Type: Grant
    Filed: July 22, 2018
    Date of Patent: November 12, 2019
    Assignee: The University of Hong Kong
    Inventors: Yi Tsun Richard Kao, Peng Gao, Xuechen Li, Ming Liu
  • Patent number: 10471046
    Abstract: The present invention relates to methods for treating acne and other skin infections caused or mediated by Propionibacterium acnes, Gardnerella vaginalis, or Staphylococcus aureus in a patient with a safe and effective amount of a topically applied oxazolidinone antibiotic compound.
    Type: Grant
    Filed: November 16, 2015
    Date of Patent: November 12, 2019
    Assignee: MELINTA SUBSIDARY CORP.
    Inventor: Erin M. Duffy
  • Patent number: 10471047
    Abstract: The current invention is in the field of molecular biology/pharmacology and provides methods of using compounds that modulate the effects of GPR30/GPER for treating obesity and diabetes (preferably agonists) as well as disease states and/or conditions that result from excessive formation of reactive oxygen species (preferably antagonists). These compounds may function as agonists and/or antagonists of the disclosed estrogen receptor and/or modulate the expression/upregulation of nox and nox-associated reactive oxygen species (ROS).
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: November 12, 2019
    Assignee: STC.UNM
    Inventors: Eric R. Prossnitz, Geetanjali Sharma
  • Patent number: 10471048
    Abstract: The present invention relates to methods of treatment of hepatitis C using prasugrel. The methods of the present invention can be used in patients with hepatitis C administering prasugrel in combination with one or more anti-hepatitis C drugs.
    Type: Grant
    Filed: March 6, 2018
    Date of Patent: November 12, 2019
    Assignee: Cipla Limited
    Inventors: Karl Roberts, Geena Malhotra, Dhiraj Abhyankar, Kalpana Joshi, Jeevan Ghosalkar
  • Patent number: 10471049
    Abstract: Human therapeutic treatment compositions comprise at least two of a curcumin component, a harmine component, and an isovanillin component, and preferably all three in combination. The agents are effective for the treatment of human conditions, especially human cancers.
    Type: Grant
    Filed: December 7, 2018
    Date of Patent: November 12, 2019
    Assignee: Ankh Life Sciences Limited
    Inventors: Gene H. Zaid, Thomas W. Burgoyne
  • Patent number: 10471050
    Abstract: The present invention relates to compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: October 3, 2016
    Date of Patent: November 12, 2019
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO.2) LIMITED
    Inventors: Stephen John Atkinson, Emmanuel Hubert Demont, Lee Andrew Harrison, Thomas George Christopher Hayhow, Matthew J. Lindon, Alexander G. Preston, Jonathan Thomas Seal, Ian David Wall, Robert J. Watson, James Michael Woolven
  • Patent number: 10471051
    Abstract: The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, Z, J, M, and R1 to R8 are defined herein, these compounds are effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: November 12, 2019
    Assignee: Asana BioSciences, LLC
    Inventors: Aranapakam M. Venkatesan, Scott K. Thompson, Roger A. Smith, Sanjeeva P. Reddy, Raghava Reddy Kethiri, Purushottam M. Dewang, Gurulingappa Hallur, Chandrika Mulakala, Ramesh Mullangi, Mohd Zainuddin
  • Patent number: 10471052
    Abstract: A pharmaceutical composition containing isomyosmine or a pharmaceutically acceptable salt thereof is administered to an individual in need thereof for treating a substance addiction, inclusive of addiction to heroin (diacetylmorphine), cocaine, opioids, methadone, d-methamphetamine, barbiturates, alcohol, benzodiazepines, amphetamines, or buprenorphine. The isomyosmine, along with optional additional therapeutic agent(s), may be administered in a capsule, tablet, or lozenge.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: November 12, 2019
    Assignee: MyMD Pharmaceuticals, Inc.
    Inventor: Jonnie R. Williams
  • Patent number: 10471053
    Abstract: Provided are methods for treatment of Fabry disease in patients having HEK assay amenable mutations in ?-galactosidase A. Certain methods comprise administering migalastat or a salt thereof every other day, such as administering about 150 mg of migalastat hydrochloride every other day.
    Type: Grant
    Filed: February 25, 2019
    Date of Patent: November 12, 2019
    Assignee: Amicus Therapeutics, Inc.
    Inventors: Jeff Castelli, Elfrida Benjamin
  • Patent number: 10471054
    Abstract: Provided is a series of acetyl Chrysin Mannich base derivatives with the structures illustrated in the following scheme: wherein R1 is acetyl and R2 is cycloalkylamine-methyl, or R2 is acetyl and R1 is cycloalkylamine-methyl. Such derivatives are cyclin-dependent protein kinases 1 (CDK1) selective inhibitors. Base on the levels of .O2? and Fe++ are higher 5-15 times in cancer cells than in normal cells, the action mechanism of such derivatives by regulating intracellular reactive oxygen species (ROS) is activating mitochondria apoptosis pathway without the death receptor pathway, thus selectively inducing apoptosis of cancer cells and protecting normal cells. Inside, CH-j has a good druggability for the selectivity of solid cancers. Moreover, CH-f has also a good druggability for the systemic cancers.
    Type: Grant
    Filed: December 13, 2018
    Date of Patent: November 12, 2019
    Inventor: Fan Zhang
  • Patent number: 10471055
    Abstract: The present invention relates to the field of molecular biology and cancer biology. Specifically, the present invention relates to methods of treating a subject with a farnesyltransferase inhibitor (FTI) that include determining whether the subject is likely to be responsive to the FTI treatment based on genotyping and expression profiling of certain immunological genes and RAS mutation status in the subject.
    Type: Grant
    Filed: August 16, 2016
    Date of Patent: November 12, 2019
    Assignee: Kura Oncology, Inc.
    Inventors: Antonio Gualberto, Catherine Rose Scholz
  • Patent number: 10471056
    Abstract: The invention relates to a dosage form that is suitable for releasing an active ingredient over a long period of time. For this purpose, the active ingredient is released in two-stages in order to do away with an excessively frequent ingestion of the dosage form. The dosage forms according to the invention are for treating dizziness in humans. They are administered with or after a meal. The concept according to the invention provides that the pharmaceutical form has a dimensionally stable portion which, after ingestion of the dosage form by the patients, does not dissolve in the chyme-filled stomach for a number of hours. In this way, this dimensionally stable portion remains in the stomach until same is evacuated by the so-called “housekeeper waves”. Another portion of the dosage form is formed in such a way that it dissolves within a short time of the patients ingesting same. In this way, a quick invasion of the active ingredient with corresponding plasma levels is ensured.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: November 12, 2019
    Assignee: HENNIG ARZNEIMITTEL GMBH & CO. KG
    Inventors: Jan Christoph Grewe, Karl-Heinz Przyklenk
  • Patent number: 10471057
    Abstract: 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: Grant
    Filed: February 4, 2019
    Date of Patent: November 12, 2019
    Assignee: The Scripps Research Institute
    Inventors: Matthew D. Disney, Suzanne G. Rzuczek
  • Patent number: 10471058
    Abstract: The present invention relates to novel treatments of periodontal disease by administering a suitable formulation of a cyclophilin inhibitor. The present invention further relates to novel pharmaceutical compositions containing said cyclophilin inhibitor compounds.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: November 12, 2019
    Assignee: PERIOC LTD
    Inventors: Thomas Kissel, Ching Pong Mak
  • Patent number: 10471059
    Abstract: The present invention provides compositions and methods of inhibiting tyrosine phosphorylation. In one aspect, a composition comprising a low-dosage tyrosine kinase inhibitor, where the low-dosage tyrosine kinase inhibitor decreases tyrosine phosphorylation, is provided. In another aspect, a method for treating cardiovascular disease or condition associated with a RASopathy having aberrant protein tyrosine phosphorylation is described. Methods for treating congenital heart disease associated with Noonan or Noonan syndrome with multiple lentigines and decreasing aberrant levels of Protein Zero-Related (PZR) tyrosyl phosphorylation are also described.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: November 12, 2019
    Assignee: Yale University
    Inventors: Anton Bennett, Jae-Sung Yi
  • Patent number: 10471060
    Abstract: The present invention provides compounds of the formula below pharmaceutically acceptable salts of the compounds, methods of treating patients for liver disease, and processes for preparing the compounds.
    Type: Grant
    Filed: March 18, 2019
    Date of Patent: November 12, 2019
    Assignee: Eli Lilly and Company
    Inventors: Mengyang Fan, Luoheng Qin, Yi Wei, Guoqiang Zhou, Jingye Zhou
  • Patent number: 10471061
    Abstract: Disclosed are inhibitors of human galactokinase of formula (I) that are useful in treating or preventing a galactokinase mediated disease or disorder, e.g., galactosemia. Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one inhibitor of the invention, and a method of treating or preventing such disease or disorder in a mammal. Formula (I).
    Type: Grant
    Filed: October 5, 2018
    Date of Patent: November 12, 2019
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University of Utah Research Foundation
    Inventors: Matthew B. Boxer, Martin J. Walsh, Li Liu, Cordelle D. Tanega, Min Shen, Kent Lai, Manshu Tang, Douglas S. Auld
  • Patent number: 10471063
    Abstract: The invention provides a composition which comprises (a) a PDE3/PDE4 inhibitor which is 9,10-Dimethoxy-2-(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one or a pharmaceutically acceptable acid addition salt thereof and (b) a muscarinic receptor antagonist.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: November 12, 2019
    Assignee: Verona Pharma PLC
    Inventors: Michael J. A. Walker, Mario Cazzola, Luigino Calzetta
  • Patent number: 10471064
    Abstract: The invention provides a pharmaceutical composition for treating atopic dermatitis of a human that is induced by Herpes simplex virus (HSV), said pharmaceutical composition comprising an effective amount of 2-[(2-amino-6-oxo-6,9-dihydro-3H-purin-9-yl)methoxy]ethyl-2-amino-3-methylbutanoate and an effective amount of an Anti-allergic agent.
    Type: Grant
    Filed: March 7, 2018
    Date of Patent: November 12, 2019
    Inventor: Lily Hsiao