Patents Issued in August 14, 2018
  • Patent number: 10045943
    Abstract: The invention pertains to implantable medical devices for controlled delivery of therapeutic agents. Some devices according to the invention have a titanium reservoir, and a porous titanium oxide based membrane to control the rate of release of the therapeutic agent. The reservoir contains a formulation of the active agent, including a stabilizer for the active agent, wherein the stabilizer is provided in an extended release configuration.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: August 14, 2018
    Assignee: Nano Precision Medical, Inc.
    Inventor: Wouter Erik Roorda
  • Patent number: 10045944
    Abstract: The present invention provides a pharmaceutical formulation comprising clomipramine or its pharmaceutically acceptable salt (preferably, clomipramine hydrochloride) as the first active ingredient, and sildenafil or its pharmaceutically acceptable salt (preferably, sildenafil citrate) as the second active ingredient, wherein stability of clomipramine is improved, and a method for manufacturing this pharmaceutical formulation. In particular, the present invention provides a pharmaceutical formulation comprising the above two active ingredients and manufactured by using a wet granulation method, wherein stability of clomipramine is improved, and a method for manufacturing this pharmaceutical formulation.
    Type: Grant
    Filed: December 29, 2014
    Date of Patent: August 14, 2018
    Assignee: CTC BIO, INC.
    Inventors: Hong Ryeol Jeon, Bong-Sang Lee, Seong-Shin Kwak, Dong-Jin Lee, Hyun-Jung Park, Jung-Hwa Kim
  • Patent number: 10045945
    Abstract: Delivery systems and their methods of formation are generally provided. The delivery system can protect a delivery molecule (e.g., DNA/RNA) and deliver it into a cell via serum. In one embodiment, the method can include binding a delivery molecule with polyethylenimine such that an end of the delivery molecule is exposed; capping the end of the delivery molecule with a first biocompatible polymer to form a core; and encapsulating the core with a second biocompatible polymer. The resulting delivery system can include a delivery molecule bonded with polyethylenimine such that an end of the delivery molecule is exposed; a first biocompatible polymer electrostatically bonded to the end of the delivery molecule to form a core; and a second biocompatible polymer encapsulating the core.
    Type: Grant
    Filed: September 21, 2015
    Date of Patent: August 14, 2018
    Inventors: Peisheng Xu, Remant Bahadur K C
  • Patent number: 10045946
    Abstract: A unit multiparticulate dosage form for delivering one or more basic, active pharmaceutical ingredients into the body in need of such medications to achieve target PK (pharmacokinetics) profiles is described. The dosage form comprises one or more multicoated drug particles (beads, pellets, mini-/micro-tablets) having a barrier coating and a lag-time coating. Each Timed Pulsatile Release (TPR) bead population exhibits pre-determined lag-time followed by differing release characteristics. The composition and thickness of the barrier coating, composition and thickness of the lag-time coating, ratio of IR beads to one or more TPR bead populations and total dose may be varied depending on the alkalinity, pH-dependent solubility and elimination half-life of the active ingredients to achieve target PK profiles (suitable for a once or twice daily dosing regimen) in patients in need of such medications.
    Type: Grant
    Filed: January 9, 2017
    Date of Patent: August 14, 2018
    Assignee: ADARE PHARMACEUTICALS, INC.
    Inventor: Gopi M. Venkatesh
  • Patent number: 10045947
    Abstract: The invention provides polymer compositions for cell and drug delivery.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: August 14, 2018
    Assignee: President and Fellows of Harvard College
    Inventors: Sidi A. Bencherif, David J. Mooney, David Edwards, Roger Warren Sands
  • Patent number: 10045948
    Abstract: The purpose of the present invention is to provide a nonaqueous tape that is stable and has high percutaneous absorption performance, and that contains pramipexole hydrochloride, which is slightly soluble in organic solvents and has high crystallinity. The present invention could produce a nonaqueous tape that is stable and has high percutaneous absorption performance by dissolving pramipexole, using a combination of a fatty acid ionic liquid and a divalent alcohol and a fatty acid ester. As a result, it has become possible to provide a transdermal patch (tape) containing pramipexole for the treatment of Parkinson's disease with which the problems associated with a conventional water-containing poultice of discoloration of the preparation and stability of the pramipexole can be solved.
    Type: Grant
    Filed: February 18, 2015
    Date of Patent: August 14, 2018
    Assignee: MEDRX CO., LTD.
    Inventors: Noboru Tatsumi, Makiko Takemoto, Hidetoshi Hamamoto
  • Patent number: 10045949
    Abstract: The present invention relates to the administration of compositions comprising polyethylene glycol, for improving the general gastrointestinal health of an animal increasing growth performance and treating osteopenia, osteoporosis and other bone disorders.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 14, 2018
    Assignees: MIDWAY PHARMACEUTICALS, INC, BOARD OF TRUSTEES OF MICHIGAN STATE UNIVERSITY
    Inventors: Rifat Pamukcu, Laura Rae McCabe
  • Patent number: 10045950
    Abstract: Methods and compounds are disclosed for wound healing by modulating autophagy. A formulation for modulating autophagy comprises a first modulating compound (FAM) selected from compounds having the general structure (I): wherein: L represents a linker selected from —C?C—, (a tolan), —CH?CH— (a stilbene, preferably trans); or —CRa?CRb— a stilbene derivative; where Ra and Rb are independently H or phenyl optionally substituted with —(R3)p or —(R4)q; R1 to R4 are independent substituents at any available position of the phenyl rings, preferably at 3, 3?, 4, 4?, and/or 5, 5?; and m, n, p, and q are independently 0, 1, 2, or 3 representing the number of substituents of the rings, respectively, but at least one of m or n must be ?1. Each R1 to R2 is independently selected from substituents described herein, including but not limited to hydroxyl, alkoxy, halo, halomethyl and glycosides. The formulation may also include an auxiliary autophagy modulating compound (AAM) as described herein.
    Type: Grant
    Filed: April 7, 2016
    Date of Patent: August 14, 2018
    Assignee: BIOMENDICS, LLC
    Inventors: Chun-che Tsai, Karen M. McGuire, James M. Jamison, Jack L. Summers
  • Patent number: 10045951
    Abstract: The invention relates compositions and methods for treating pathological lung conditions using whole-grain flaxseed or flaxseed lignans. Specifically, the invention relates to the dietary use of flaxseed lignans.
    Type: Grant
    Filed: April 11, 2011
    Date of Patent: August 14, 2018
    Assignee: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventor: Melpo Christofidou-Solomidou
  • Patent number: 10045952
    Abstract: A use of polygodial or a structural derivative thereof, or a plant extract containing polygodial or a structural derivative thereof for the manufacture of a medicament for treating or preventing a viral infection, or a condition or disease resulting from a viral infection.
    Type: Grant
    Filed: June 25, 2014
    Date of Patent: August 14, 2018
    Assignee: Forest Herbs Research Limited
    Inventor: Peter Scott Butler
  • Patent number: 10045953
    Abstract: A method for treating and preventing diseases associated with neutrophil infiltration, particularly ocular diseases, is provided, which method comprises administering to a subject in need thereof an effective amount of ceramide or a derivative thereof. Also provided is a composition for treating diseases associated with neutrophil infiltration, the composition comprising ceramide or a derivative thereof.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: August 14, 2018
    Assignees: Case Western Reserve University, The Penn State Research Foundation
    Inventors: Eric Pearlman, Mark Kester
  • Patent number: 10045954
    Abstract: The invention discloses a use of paracetamol and a pharmaceutical preparation containing the same in preparation of anti-HPV drugs. The novel anti-HPV pharmaceutical preparation of the invention has a significant anti-HPV effect and low toxicity, and can be used for preventing and treating clinical symptoms caused by HPV infection, especially common warts, plane warts, plantar wart, vulvar cancer, penile neoplasms, anal carcinoma, prostate cancer, bladder cancer, cervical cancer, rectal cancer, oral cancer, tonsil cancer and the like.
    Type: Grant
    Filed: July 14, 2014
    Date of Patent: August 14, 2018
    Assignee: INSTITUTE OF BIOMEDICAL ENGINEERING, CHINESE ACADEMY OF MEDICAL SCIENCE
    Inventors: Tianjun Liu, Shuai Meng, Lihui Zhao, Ge Hong
  • Patent number: 10045955
    Abstract: The present invention is directed to an aqueous gel composition containing a local anesthetic, a lubricating agent, and a preservative and methods of treating vulvovaginal pain, such as dyspareunia by topically administering said composition.
    Type: Grant
    Filed: January 22, 2018
    Date of Patent: August 14, 2018
    Assignee: ELLE PHARMACEUTICAL, LLC
    Inventors: Elias Reichel, Lauren Oshry
  • Patent number: 10045956
    Abstract: It is provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis. It is also provided a catechol-O-methyltransferase (COMT) inhibitor for use in the prevention and/or treatment of transthyretin-associated amyloidosis in combination therapy with another COMT inhibitor, a benzoxazole derivative, iododiflunisal, diflunisal, resveratrol, tauroursodeoxycholic acid, doxocycline, or epigallocatechin-3-gallate.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: August 14, 2018
    Assignee: SOM Innovation Biotech, S.L.
    Inventors: Marc Centellas Casado, Raúl Insa Boronat, Núria Reig Bolano, Nuria Gavaldà Batalla
  • Patent number: 10045957
    Abstract: A GIP-increase inhibitor, which may be utilized for producing a medicine, a food, or the like, is provided. The GIP-increase inhibitor contains triacylglycerol in which ?-linolenic acid accounts for 10% by mass or more of the constituent fatty acid, as an effective ingredient.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: August 14, 2018
    Assignee: KAO CORPORATION
    Inventors: Chika Suzukamo, Koji Onizawa, Noriko Osaki
  • Patent number: 10045958
    Abstract: The present disclosure provides methods for evaluating daily ammonia exposure based on a single fasting ammonia blood level measurement, as well as methods that utilize this technique to adjust the dosage of a nitrogen scavenging drug, determine whether to administer a nitrogen scavenging drug, and treat nitrogen retention disorders.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: August 14, 2018
    Assignee: Horizon Therapeutics, LLC
    Inventors: Bruce Scharschmidt, Masoud Mokhtarani
  • Patent number: 10045959
    Abstract: The present disclosure provides methods for evaluating daily ammonia exposure based on a single fasting ammonia blood level measurement, as well as methods that utilize this technique to adjust the dosage of a nitrogen scavenging drug, determine whether to administer a nitrogen scavenging drug, and treat nitrogen retention disorders.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: August 14, 2018
    Assignee: Horizon Therapeutics, LLC
    Inventors: Bruce Scharschmidt, Masoud Mokhtarani
  • Patent number: 10045960
    Abstract: A coating composition for drug-eluting medical devices, which enables a medical device to be delivered to a target tissue for the purpose of treating an affected blood vessel part such as restenosis, without easy separation of a drug from the medical device during the delivery process is provided. The coating composition for drug-eluting medical devices contains a water-insoluble drug and at least one selected from the group consisting of ester compounds of amino acids, which have a hydropathy index of the amino acid of zero or less than zero, and salts thereof. A drug coating layer, a drug-eluting medical device and a method of treatment are also provided.
    Type: Grant
    Filed: February 1, 2017
    Date of Patent: August 14, 2018
    Assignee: TERUMO KABUSHIKI KAISHA
    Inventors: Keiko Yamashita, Shigenori Nozawa
  • Patent number: 10045961
    Abstract: Provided herein are methods of treating a subject having hepatitis B viral (HBV) infection. More specifically, disclosed herein are methods of stimulating the innate cytokine response in macrophages, dendritic cells and/or liver non-parenchymal cells with small molecular agonists of STING to suppress HBV replication in hepatocytes. The methods are especially suitable for use in the treatment of chronic HBV infections. Also disclosed herein are methods of identifying compounds useful in the treatment of HBV infection.
    Type: Grant
    Filed: April 10, 2017
    Date of Patent: August 14, 2018
    Assignee: Drexel University
    Inventors: Jinhong Chang, Fang Guo, Timothy M. Block, Ju-Tao Guo
  • Patent number: 10045962
    Abstract: Provided in the present invention are uses of duloxetine hydrochloride in preparing a pharmaceutical composition for treatment of cancer.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: August 14, 2018
    Assignee: LAUNX BIOMEDICAL CO., LTD.
    Inventors: Chiu-Hung Chen, Show-Mei Chuang, Tzong-Der Way, Nai-Wan Hsiao
  • Patent number: 10045963
    Abstract: Disclosed are methods for the preparation of amorphous N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Also disclosed are methods for the preparation of amorphous solid dispersion of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide.
    Type: Grant
    Filed: January 2, 2018
    Date of Patent: August 14, 2018
    Assignee: SIGA TECHNOLOGIES, INC.
    Inventors: Shanthakumar R. Tyavanagimatt, N K Peter Samuel, Joseph Paz, Ying Tan, Dennis E. Hruby
  • Patent number: 10045964
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: July 27, 2017
    Date of Patent: August 14, 2018
    Assignee: Siga Technologies Inc.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William C. Weimers, Dylan Nelson, Tove' C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Patent number: 10045965
    Abstract: Disclosed are gel compositions suitable for the topical administration of an active compound having poor solubility and skin penetration, for example, of a COX-2 inhibitor compounds, processes of preparation thereof and methods of use thereof for the treatment of indications treatable by the active compound.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: August 14, 2018
    Assignee: EGIS Pharmaceuticals PLC
    Inventors: Endre Mikulásik, Tamás Spaits, Ágota Szakályné Sinka
  • Patent number: 10045966
    Abstract: Embodiments of the presently-disclosed subject matter include activators of HssRS that induce endogenous heme biosynthesis by perturbing central metabolism. These molecules are toxic to fermenting S. aureus, including clinically relevant small colony variants (SCVs). The utility of targeting fermenting bacteria is exemplified by the fact that this compound prevents the emergence of antibiotic resistance, enhances phagocyte killing, and reduces S. aureus pathogenesis. This small molecule is a powerful tool not only for studying bacterial heme biosynthesis and central metabolism, but also establishes targeting of fermentation as a viable antibacterial strategy.
    Type: Grant
    Filed: April 21, 2017
    Date of Patent: August 14, 2018
    Assignee: Vanderbilt University
    Inventors: Eric P. Skaar, Laura Anzaldi Mike, Gary Sulikowski, Alex Waterson, Paul Reid
  • Patent number: 10045967
    Abstract: The present invention relates to novel liquid compositions and formulations containing a thioureylene compound, a polysaccharide and a liquid vehicle. The compositions and formulations of the invention are useful for dealing with diseases and conditions associated with abnormally high thyroid hormone levels in mammals, such as humans and cats.
    Type: Grant
    Filed: June 23, 2015
    Date of Patent: August 14, 2018
    Assignee: Norbrook Laboratories Limited
    Inventors: Louise Reynolds, Manish Umrethia
  • Patent number: 10045968
    Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atom; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: August 14, 2018
    Assignee: TOBIRA THERAPEUTICS, INC.
    Inventors: Mitsuru Shiraishi, Masanori Baba, Katsuji Aikawa, Naoyuki Kanzaki, Masaki Seto, Yuji Iizawa
  • Patent number: 10045969
    Abstract: A substituted alkenylbenzene compound of formula (4): wherein X1 is selected from the group consisting of halogen atom, —SF5, C1-C6halo alkyl, hydroxy C1-C6haloalkyl, C1-C6alkoxy C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6 haloalkoxy, C1-C3haloalkoxy C1-C3haloalkoxy, C1-C6haloalkylthio, C1-C6haloalkylsulfinyl and C1-C6haloalkylsulfonyl; X3 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy and C1-C6 alkylthio; X4 is selected from the group consisting of a hydrogen atom, halogen atom, cyano, C1-C4alkyl, C1-C4alkoxy and C1-C4haloalkoxy; R3 is —C(R3a)(R3b)R3c, where R3a and R3b independently of each other are a halogen atom, or R3a and R3b together form 3- to 6-membered ring together with the carbon atom bonding them by forming a C2-C5haloalkylene chain, and R3c is selected from the group consisting of a hydrogen atom, halogen atom, C1-C5alkyl, C1-C5haloalkyl, C1-C4haloalkoxy and C1-C4haloalkylthio, with a proviso that in case where X1
    Type: Grant
    Filed: April 12, 2016
    Date of Patent: August 14, 2018
    Assignee: Nissan Chemical Industries, Inc.
    Inventors: Takeshi Mita, Takamasa Kikuchi, Takashi Mizukoshi, Manabu Yaosaka, Mitsuaki Komoda, Shinji Takii
  • Patent number: 10045970
    Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:
    Type: Grant
    Filed: May 2, 2017
    Date of Patent: August 14, 2018
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Alfredo C. Castro, Michael J. Grogan, Karen J. McGovern, Martin R. Tremblay
  • Patent number: 10045971
    Abstract: The present invention relates to compositions and methods for the treatment of amyotrophic lateral sclerosis. More specifically, the present invention relates to novel combinatorial therapies for treating amyotrophic lateral sclerosis or a related disorder.
    Type: Grant
    Filed: January 25, 2016
    Date of Patent: August 14, 2018
    Assignee: PHARNEXT
    Inventors: Daniel Cohen, Serguei Nabirochkin, Ilya Chumakov, Rodolphe Hajj
  • Patent number: 10045972
    Abstract: Provided herein are hydroxypyridone derivatives, for example, a compound of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods for treating, preventing, or ameliorating one or more symptoms of an inflammatory, neurodegenerative, or immune-mediated disease (e.g., multiple sclerosis).
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: August 14, 2018
    Assignee: BioTheryX, Inc.
    Inventors: Armen Manoukian, Fabrizio Mastronardi, Sam Scanga, Frank Mercurio, Kyle W. H. Chan
  • Patent number: 10045973
    Abstract: The present invention relates to, inter alia, pharmaceutical compositions comprising an acid labile proton pump inhibitor and a buffering agent and to use of such compositions in treating nocturnal acid breakthrough.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: August 14, 2018
    Assignee: THE CURATORS OF THE UNIVERSITY OF MISSOURI
    Inventor: Jeffrey Owen Phillips
  • Patent number: 10045974
    Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the BACE1 enzyme. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders for which the reduction of A? deposits is beneficial such as Alzheimer's disease.
    Type: Grant
    Filed: November 9, 2015
    Date of Patent: August 14, 2018
    Assignee: H. Lundbeck A/S
    Inventors: Karsten Juhl, Lena Tagmose, Mauro Marigo
  • Patent number: 10045975
    Abstract: Ophthalmic devices and methods of treating allergic conjunctivitis are disclosed herein.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: August 14, 2018
    Assignee: Johnson & Johnson Vision Care, Inc.
    Inventors: Ranganath R. Raja, Shivkumar Mahadevan, Azaam Alli, Frank F. Molock, Brian Pall
  • Patent number: 10045976
    Abstract: Nicotine liquid formulations and their use in therapy, for instance, in nicotine replacement therapy are described. More specifically, the technology relates to liquid nicotine formulations comprising nicotine, one or more diol and/or triol, and a sugar alcohol, which may be used as sprays for administration through the oral cavity, such as the palate.
    Type: Grant
    Filed: December 1, 2016
    Date of Patent: August 14, 2018
    Assignee: EURO-PHARM INTERNATIONAL CANADA INC.
    Inventors: Rolando Fusco, Leonardo Calderone
  • Patent number: 10045977
    Abstract: The present invention relates to new medical uses of morphinans such as nalmefene and naltrexone and their related derivatives, pharmaceutical formulations thereof, and use thereof for prevention and treatment of NASH, NAFLD, and/or ASH.
    Type: Grant
    Filed: April 20, 2017
    Date of Patent: August 14, 2018
    Assignee: TAIWANJ PHARMACEUTICALS CO., LTD.
    Inventors: Edwin S C Wu, Peter J. S. Chiu, May Mei-chi Hsu
  • Patent number: 10045978
    Abstract: The treatment of mastocytosis, and in particular indolent forms of mastocytosis (including smoldering systemic, indolent systemic and cutaneous mastocytosis), including the administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt or solvate thereof, in particular in an appropriate dosage regimen.
    Type: Grant
    Filed: December 2, 2015
    Date of Patent: August 14, 2018
    Assignee: AB SCIENCE
    Inventors: Alain Moussy, Jean-Pierre Kinet
  • Patent number: 10045979
    Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X6, X8, Q1, Q2, Q3, Q4, Q5, Q6, Ring A, Ring B, W, W?, R2, R3, R, R?, m, n and q are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: August 14, 2018
    Assignee: MERIAL INC.
    Inventors: Alan Long, Srinivas Reddy Gurrala
  • Patent number: 10045980
    Abstract: A dry powder pharmaceutical formulation for inhalation including a compound of formula (I): that is 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(4-((2-((6-ethylpyrazin-2-yl)amino)pyridin-4-yl)methoxy)naphthalen-1-yl)urea or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof; and lactose as a topically acceptable diluent. An inhaler device containing the dry powder pharmaceutical formulation is also described.
    Type: Grant
    Filed: March 13, 2017
    Date of Patent: August 14, 2018
    Assignee: Respivert Ltd
    Inventors: Alistair Ian Longshaw, Euan Alexander Fraser Fordyce, Stuart Thomas Onions, John King-Underwood, Jennifer Venable
  • Patent number: 10045981
    Abstract: The present disclosure relates to methods of modulating (for example, inhibiting) activity of JAK3, comprising contacting the JAK3 with a compound of Formula I or pharmaceutically acceptable salt thereof, wherein constituent members are provided hereinwith. The present disclosure further provides novel compounds and compositions as well as their methods of preparation and use. The disclosed JAK3 inhibitors may be used in the treatment of JAK3-associated diseases including, for example, inflammatory and autoimmune disorders.
    Type: Grant
    Filed: November 23, 2016
    Date of Patent: August 14, 2018
    Assignee: JAKPharm, LLC
    Inventor: Haiching Ma
  • Patent number: 10045982
    Abstract: The invention relates to new pyridopyrazine derivative compounds of formula (I-A) or formula (I-B): to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: August 14, 2018
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Valerio Berdini, Gordon Saxty, Patrick Rene Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet, Bruno Roux, Lieven Meerpoel
  • Patent number: 10045983
    Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: August 31, 2017
    Date of Patent: August 14, 2018
    Assignee: Genentech, Inc.
    Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
  • Patent number: 10045984
    Abstract: The present invention provides a composition comprising zinc and trimethoprim, particularly in a weight ration of about 1:3 to about 1:7, as well as a sustained- or prolonged-release preparation which comprises trimethoprim and zinc and a biodegradable polymer providing a clinically useful composition which has prolonged release over a long period of time.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: August 14, 2018
    Inventor: Magdi El-Habbal
  • Patent number: 10045985
    Abstract: The present invention relates to pyrimidine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: August 14, 2018
    Assignee: Merck Patent GmbH
    Inventors: Hui Qiu, Richard D. Caldwell, Lesley Liu-Bujalski
  • Patent number: 10045986
    Abstract: Embodiments provide a method for radio resource management measurement. The method includes: determining, by a UE according to a detected first reference signal, a first resource on which the detected first reference signal is located; determining, by the UE, a reference signal received power RSRP of a target cell according to a received power of the detected first reference signal carried on the first resource; determining, by the UE, a second resource; determining, by the UE, a received signal strength indicator RSSI of the target cell according to a total received power on the second resource; and determining, by the UE, reference signal received quality RSRQ or a signal to interference plus noise ratio SINR of the target cell or both according to the RSRP and RSSI. The method is applied to radio resource management measurement.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: August 14, 2018
    Assignee: Huawei Technologies Co., Ltd.
    Inventors: Lei Guan, Lixia Xue, David Jean-Marie Mazzarese
  • Patent number: 10045987
    Abstract: The present invention provides kinase inhibitor analogs with improved properties, such as improved efficacy, pharmacokinetics, safety, and specificity. In some embodiments, the present invention provides nilotinib analogs that provide therapeutic benefits.
    Type: Grant
    Filed: August 27, 2015
    Date of Patent: August 14, 2018
    Assignee: Codexis, Inc.
    Inventors: Gjalt W. Huisman, Jed Lee Hubbs, Xiyun Zhang, Robert Osborne
  • Patent number: 10045988
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Grant
    Filed: July 10, 2017
    Date of Patent: August 14, 2018
    Assignee: Roivant Sciences GmbH
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 10045989
    Abstract: The disclosure relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to inhibitors of NADPH-oxidases (Nox enzymes) and/or myeloperoxidase.
    Type: Grant
    Filed: May 5, 2016
    Date of Patent: August 14, 2018
    Assignee: Emory University
    Inventors: John David Lambeth, Thota Ganesh, Susan M. Smith, Aiming Sun
  • Patent number: 10045990
    Abstract: Disclosed herein are methods of treating diseases that exhibit over-activation of the ERBB4 pathway, such as breast cancer and lung cancer. The method comprises administering to a subject having a disease that exhibits over-activation of the ERBB4 pathway and a gene expression profile consistent with an ERBB4-sensitive profile a therapeutically effective amount of an ERBB4 inhibitor, wherein the disease is effectively treated. Gene expression profiles of ERBB4-sensitive cells and microarrays suitable for protein-tyrosine kinases are also provided.
    Type: Grant
    Filed: March 2, 2016
    Date of Patent: August 14, 2018
    Assignee: Arizona Board of Regents on Behalf of Arizona State University
    Inventors: Fernanda Festa, Joshua Labaer, Jin Park, Femina Rauf
  • Patent number: 10045991
    Abstract: A method of treating a pediatric cancer in a subject in need thereof. The method includes administering to the subject a therapeutically effective amount of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, or a pharmaceutically acceptable salt thereof, or a combination thereof.
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: August 14, 2018
    Assignee: Loxo Oncology, Inc.
    Inventors: Michael Cox, Nisha Nanda
  • Patent number: 10045992
    Abstract: This disclosure relates, at least in part, to a method of treatment. In one embodiment, the method of treatment comprises administering to a subject in need of such treatment a first therapeutic agent including compound (1): or a pharmaceutically acceptable salt thereof in combination with a second therapeutic agent, wherein the first therapeutic agent and the second therapeutic agent are administered either simultaneously or sequentially.
    Type: Grant
    Filed: June 19, 2017
    Date of Patent: August 14, 2018
    Assignee: Oncoceutics, Inc.
    Inventors: Martin Stogniew, Joshua E. Allen