Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
Type:
Grant
Filed:
February 14, 2014
Date of Patent:
October 6, 2015
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Adam D. Hughes, Erik Fenster, Melissa Fleury, Roland Gendron, Edmund J. Moran
Abstract: The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat esophogeal adenocarcinoma by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.
Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransferases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.
Type:
Grant
Filed:
December 5, 2011
Date of Patent:
September 29, 2015
Assignee:
Epizyme, Inc.
Inventors:
Richard Chesworth, Kevin W. Kuntz, Edward J. Olhava, Michael A. Patane
Abstract: A solute is precipitated from a solution of a solute, a solvent, and a non-solvent by preparing the solution and introducing the solution into a precipitation chamber contain a supercritical fluid.
Type:
Grant
Filed:
November 22, 2010
Date of Patent:
September 22, 2015
Assignee:
HONG KONG POLYTECHNIC UNIVERSITY
Inventors:
Yi Li, Footim Chau, Aizheng Chen, Junyan Hu, Tsuiyan Lau
Abstract: The present invention provides compositions methods for treating susceptible viral infections, especially hepatitis C viral (HCV) infections as well as co infections of HCV with other viruses such as HBV and/or HIV. In one embodiment, the present invention provides compositions having the formula (I) and their use in treating viral infections: or a pharmaceutically acceptable salt, ester, stereoisomer, tautomers, solvate, prodrug, or combination thereof.
Type:
Grant
Filed:
March 13, 2013
Date of Patent:
September 22, 2015
Assignee:
SPRING BANK PHARMACEUTICALS, INC.
Inventors:
Radhakrishnan P. Iyer, Seetharamaiyer Padmanabhan
Abstract: The present invention relates to the use of a taste masking agent selected from the group of starch; cellulose; xanthan gum; gellan gum; alginate; galactomannans such as fenugreek, guar gum, tara gum, locust bean gum, and cassia gum; gum karaya; gum tragacanth; carrageenan; and mixture thereof, for improving one or more of mouth feel, taste, aftertaste and smell of a liquid aqueous nutritional composition comprising a nucleoside and/or a nucleotide. It also relates to a nutritional composition comprising an unsavoury nucleoside and/or nucleotide component, having improved sensory characteristics such as improved mouth feel, taste, aftertaste and smell. In particular, it relates to a composition comprising said unsavoury nucleoside and/or nucleotide component, in particular comprising an uridine-containing nucleoside and/or a nucleotide in combination with an unsavoury edible oil, such as a fish oil.
Type:
Grant
Filed:
December 3, 2013
Date of Patent:
September 15, 2015
Assignee:
N. V. Nutricia
Inventors:
Esther Jacqueline De Kort, Martine Groenendijk, Patrick Joseph Gerardus Hendrikus Kamphuis
Abstract: Kits and methods for treating disordered tissue caused by a virus in a mammal involve co-administration of a systemic anti-virus drug and topically administering an anti-infective composition. The systemic anti-virus drug is internally administered and disrupts or inhibits virus replication systemically within the mammal. Examples include nucleoside analogues, nucleoside analogue precursors, and nucleotide analogues. The topically administered anti-infective composition includes at least one anti-infective agent, such as an organohalide (e.g., benzalkonium chloride), and is formulated to penetrate below the disordered tissue surface and allow the anti-infective agent to kill viruses at the disordered tissue site. The anti-infective composition reduces the time and/or number of dosages required for the systemic anti-virus drug to treat the disordered tissue in the absence of topically administering the anti-infective composition. It also reduces or eliminates incidences of post-treatment neuralgia.
Abstract: An object of the present invention is to provide an agent for suppressing the formation of skin cells induced by exposure to light such as ultraviolet light. The object is achieved by using a purine nucleic acid for suppressing the formation of abnormal skin cells caused by exposure to light.
Abstract: A plant disease control agent comprising at least one member selected from the group consisting of saccharides and substances each having a bactericidal and/or fungicidal activity. The plant disease control agents are effective for the control of cucumber, grape and cabbage downy mildew, damping-off in seedlings caused by Pythium spp, cucumber and barley powdery mildew, wheat stem rust, potato and tomato late blight, and others.
Type:
Grant
Filed:
August 18, 2009
Date of Patent:
September 8, 2015
Assignees:
MITSUI CHEMICALS AGRO, INC., NATIONAL UNIVERSITY CORPORATION KAGAWA UNIVERSITY
Abstract: Provided herein are methods for treating subjects having a cancer, such as a relapsed or refractory solid tumor, wherein the method comprises administering to the subject a cytidine analog. In certain of the methods, the cytidine analog is administered alone or in combination with one or more anti-cancer agents. Also provided are methods for using a cytidine analog, to treat diseases and disorders including disorders related to abnormal cell proliferation, hematologic disorders, and immune disorders, among others. In certain of the methods, the cytidine analog is formulated in an oral dosage form and administered orally.
Type:
Grant
Filed:
October 31, 2012
Date of Patent:
September 8, 2015
Assignee:
Celgene Corporation
Inventors:
Kyle J. MacBeth, Aaron N. Nguyen, Jorge DiMartino
Abstract: The invention relates to a dry or slurry process to prepare phosphate-crosslinked cellulose ethers from a cellulose starting material comprising the steps of adding an alkalizing agent to the cellulose starting material to achieve mercerization, adding an etherifying agent to the reaction mixture to achieve etherification of the cellulose, and adding a crosslinking agent to the reaction mixture to achieve crosslinking of the cellulose, wherein at least part of the alkalizing agent is added to the cellulose starting material before the etherification and/or crosslinking reactions take place to obtain alkalized cellulose; the crosslinking agent and the etherifying agent are added one after the other in random order or simultaneously; the crosslinking agent is an alkali metal thmetaphosphate; and the crosslinking and etherification steps are performed at an elevated temperature.
Abstract: New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil.
Type:
Grant
Filed:
October 26, 2011
Date of Patent:
August 25, 2015
Assignee:
PROMETIC BIOSCIENCES INC.
Inventors:
Lyne Gagnon, Brigitte Grouix, Lilianne Geerts, Pierre Laurin, Christopher Penney, Boulos Zacharie
Abstract: There is provided a method for producing alkali cellulose comprising efficiently removing cellulose particles which are introduced by a pulp and have accumulated in a circulating alkali metal hydroxide solution. More specifically, there is provided a method for producing alkali cellulose, comprising at least the steps of bringing a pulp into contact with an alkali metal hydroxide solution to obtain a contact product, draining the contact product by a drainer, reusing an alkali metal hydroxide solution recovered in the step of draining for contact with a pulp, and adjusting an amount of cellulose particles in the recovered alkali metal hydroxide solution to 0.5% by weight or less prior to reusing for contact with the pulp.
Abstract: The present invention provides compositions suitable for topical administration to a mammalian subject including sodium hyaluronate and a pharmaceutically acceptable excipient. The present invention also provides methods for making and using the same.
Abstract: The invention relates to a new method of preparation of a hyaluronan derivative with an aldehydic group in the position (6) of the polysaccharide glucosamine part. The hyaluronic acid oxidation can be performed by means of TEMPO/NaCIO or TEMPO/TCC systems in a protic environment with or without the presence of anorganic salts. Thus prepared aldehyde can be used for binding amines, diamines, amino acids, peptides and other compounds containing an amino group, e.g. by means of the reductive amination with NaBH3CN in water or in a water-organic solvent system. When a diamine or compounds containing three or more amino groups are used, cross-linked hyaluronan derivatives can be prepared. Cross-linked derivatives can be also prepared by a reaction of the aldehyde with a hyaluronan substituted by an amino-alkyl group HA-alkyl-NH2.
Abstract: Disclosed are methods relating to monitoring the processing of polysaccharides and, in particular, monitoring the processing of guar in order to improve guar yield and/or lower impurity concentration in the wash effluent fluid.
Type:
Grant
Filed:
November 21, 2011
Date of Patent:
August 11, 2015
Assignee:
RHODIA OPERATIONS
Inventors:
Marie-Pierre Labeau, Kraig Luczak, Vincent Monin, Serge Henrot, Aziz Boukhelifa, Simon Firkins
Abstract: The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is acetyl salicylic acid, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a such a co-crystal.
Type:
Grant
Filed:
May 31, 2012
Date of Patent:
August 11, 2015
Assignee:
AstraZeneca AB
Inventors:
Stephen David Cosgrove, David Thomas Jonaitis, Jonathan Charles Derrick Sutch
Abstract: Borocarbohydrate complex containing compositions are presented that have an improved di-complex to boric acid ratio. In some embodiments, compositions are characterized by a di-complex to boric acid ratio of at least 5:1 and more typically at least 10:1 in liquid form, and at least 20:1 in dried form. In other embodiments, compositions are characterized by a minimum content of 80 wt % di-complex and a boric acid content of less than 15 wt %, and more typically less than 5 wt %. Contemplated compositions are thought to have improved biological activity and reduced content of undesired components.
Abstract: The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least on nucleoside of formula (2):Formula (1) and Formula (2). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
Type:
Grant
Filed:
March 31, 2011
Date of Patent:
August 11, 2015
Assignee:
ALNYLAM PHARMACEUTICALS, INC.
Inventors:
Kallanthottathil G. Rajeev, Muthiah Manoharan, Eric E. Swayze, Thazha P. Prakash