N-glycoside Patents (Class 514/42)
  • Publication number: 20130237490
    Abstract: The present invention relates to novel therapeutics with antibacterial activity, processes for their preparation, and pharmaceutical, veterinary and nutritional compositions containing them as active ingredients. The present invention also relates to uses of the novel therapeutics, for example, as medicants or food additives in the treatment of bacterial infections or to aid body mass gain in a subject.
    Type: Application
    Filed: September 17, 2010
    Publication date: September 12, 2013
    Applicant: Albany Molecular Research, Inc.
    Inventors: Grant J. CARR, David D. MANNING, Zhicai YANG, Cheng GUO, Jun-Ho MAENG, John RABENSTEIN, Peter C. MICHELS, Matthew W. CHASE
  • Patent number: 8530445
    Abstract: A first aspect of the invention relates to a combination comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof. A second aspect of the invention relates to a pharmaceutical product comprising a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a DNA methyltransferase inhibitor and 1-(2-C-cyano-2-dioxy-?-D-arabino-pentofuranosyl)-N4-palmitoyl cytosine, or a metabolite thereof, to a subject.
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: September 10, 2013
    Assignee: Cyclacel Limited
    Inventors: Simon Richard Green, Ruth Mackay, Ian Neil Fleming
  • Patent number: 8518930
    Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of alkylating or alkylating-like agents, antimetabolite agents and topoisomerase I inhibitors, wherein the active ingredients are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
    Type: Grant
    Filed: July 29, 2009
    Date of Patent: August 27, 2013
    Assignee: Nerviano Medical Sciences S.r.l.
    Inventors: Marina Ciomei, Aurelio Marsiglio, Valter Domenico Croci, Enrico Pesenti
  • Patent number: 8507411
    Abstract: The present invention provides methods of producing libraries of compounds with enhanced desirable properties and diminished side effects as well as the compounds produced by the methods. In preferred embodiments, methods of the present invention use a universal chemical glycosylation method that employs reducing sugars and requires no protection or activation. In a preferred embodiment, the invention provides a library of neoglycoside digitoxin analogs that includes compounds with significantly enhanced cytotoxic potency toward human cancer cells and tumor-specificity, but are less potent Na+/K+-ATPase inhibitors in a human cell line than digitoxin.
    Type: Grant
    Filed: August 25, 2008
    Date of Patent: August 13, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventor: Joseph M. Langenhan
  • Publication number: 20130203975
    Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: April 12, 2012
    Publication date: August 8, 2013
    Applicant: NOVARTIS AG
    Inventors: Gregory Raymond Bebernitz, Mark Gary Bock
  • Patent number: 8501701
    Abstract: The invention relates to methods of use for compounds in treating, reducing the incidence, reducing the severity or pathogenesis of an intestinal disease or condition in a subject, including, inter alia, inflammatory bowel disease, Crohn's disease, ulcerative colitis, or a combination thereof.
    Type: Grant
    Filed: November 14, 2006
    Date of Patent: August 6, 2013
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventors: Saul Yedgar, Moshe Ligumski, Miron Krimsky
  • Patent number: 8492352
    Abstract: The present invention relates to novel synthetic polysaccharides with antithrombotic activity, having at least one covalent bond with an amino chain, and to the preparation method thereof and to the therapeutic use thereof.
    Type: Grant
    Filed: August 24, 2009
    Date of Patent: July 23, 2013
    Assignee: Sanofi
    Inventors: Joseph Schofield, Dave Smith, Patrick Soubayrol
  • Publication number: 20130178431
    Abstract: The present invention provides glycoside compounds, methods of preparing such compounds, pharmaceutical compositions comprising such compounds, and a method for the treatment of hyperproliferative diseases using the same.
    Type: Application
    Filed: December 27, 2012
    Publication date: July 11, 2013
    Applicants: CENTROSE, LLC
    Inventor: Jill Hutchinson-Bollettieri
  • Patent number: 8481503
    Abstract: The invention relates to combination anticancer therapy with certain Akt inhibitor and other anticancer agents such as anticancer antimetabolites, anticancer antibiotics, plant-derived anticancer agents, anticancer platinum-coordinated complex compounds, anticancer camptothecin derivatives and anticancer tyrosine kinase inhibitors.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: July 9, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Mark E. Layton, Hiroshi Hirai, Hidehito Kotani
  • Patent number: 8476241
    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.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: July 2, 2013
    Assignee: University of South Florida
    Inventor: Jin Q. Cheng
  • Publication number: 20130137653
    Abstract: The present invention relates to a theanine derivative, a preparation method thereof, and a use thereof for anti-acne treatment, having a selective inhibitory effect on Propionibacterium acnes in the skin.
    Type: Application
    Filed: August 9, 2011
    Publication date: May 30, 2013
    Applicant: AMOREPACIFIC CORPORATION
    Inventors: Jae Won Yoo, Yu Na Yun, Seo Young Kim, Jin Young Lee, Jun Oh Kim, Jun Cheol Cho
  • Patent number: 8450467
    Abstract: The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z?)(Z?)O-nucleoside, —P(Z?)(Z?)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z?)(Z?)O-Linker-OP(Z??)(Z??)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z?)(Z?)-formula (I), —P(Z?)(Z?)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: May 28, 2013
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Narayanannair K. Jayaprakash, Martin Maier
  • Publication number: 20130131003
    Abstract: It was an object of the present invention to provide an orally disintegrating tablet (ODT) for the glycosidase inhibitor acarbose. The object is achieved with an orally disintegrating tablet containing 1-30% acarbose and 40-90% water-soluble carrier. In order to obtain the desired properties, the ingredients have to be precompacted and to be premixed with an insoluble carrier.
    Type: Application
    Filed: April 26, 2011
    Publication date: May 23, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Axel Schneeweis, Tobias Laich
  • Publication number: 20130131004
    Abstract: A method for directly inhibiting proliferation of Helicobacter pylori bacteria, that includes administering to a subject infected with Helicobacter pylori an N-acetylglucosaminyl beta-linked monosaccharide represented by: GlcNAcl-beta-O—Y where Y is an alkyl group, an alkoxyl group, an alkenyl group, an alkynyl group, an aralkyl group, an aryl group, a heteroaryl group, a carboxyl group, or an alkoxycarbonyl group.
    Type: Application
    Filed: January 9, 2013
    Publication date: May 23, 2013
    Applicant: THE NOGUCHI INSTITUTE
    Inventor: THE NOGUCHI INSTITUTE
  • Patent number: 8445458
    Abstract: A composition comprising (a) one or more ?-3 fatty acids selected from DHA, DPA and EPA, (b) uridine or its equivalent, and (c) a methyl donor, useful in the treatment of a person having characteristics of a prodromal dementia patient. The characteristics include e.g. a level of more than 350 ng Total-tau per liter cerebrospinal fluid (CSF), and a weight ratio of abeta-42/Phospho-tau-181 of less than 6.5 in CSF.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: May 21, 2013
    Assignee: N. V. Nutricia
    Inventors: Robert Johan Joseph Hageman, Patrick Joseph Gerardus Hendrikus Kamphuis, Ladislaus Maria Broersen
  • Patent number: 8440638
    Abstract: Compositions and methods are disclosed which are effective for modulating glucose homeostasis, calcium ion flux and cell death in target cells.
    Type: Grant
    Filed: July 20, 2005
    Date of Patent: May 14, 2013
    Assignees: Wisconsin Alumni Research Foundation, University of Washington
    Inventors: John M. Denu, Andrew M. Scharenberg
  • Patent number: 8435959
    Abstract: The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat tumors and cancer 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.
    Type: Grant
    Filed: March 29, 2005
    Date of Patent: May 7, 2013
    Assignee: University of South Florida
    Inventors: Jin Q. Cheng, Said M. Sebti
  • Publication number: 20130108573
    Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2012
    Publication date: May 2, 2013
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventor: Lumena Pharmaceuticals, Inc.
  • Publication number: 20130102555
    Abstract: Methods are provided for treating diabetes, lowering plasma level of HbA1c, glucose plasma levels, total cholesterol plasma level, and/or triglyceride plasma level while increasing HDL cholesterol levels and delaying onset of diabetic retinopathy in a diabetic, pre-diabetic, or non-diabetic mammal while minimizing undesirable side effects.
    Type: Application
    Filed: October 18, 2012
    Publication date: April 25, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Patent number: 8415095
    Abstract: Nucleoside analogues comprising a citrate group can be used to obtain immunogens designed to produce antibodies having an affinity for triphosphorylated nucleosides. Such antibodies are useful for implementing sensitive immunologic assays for triphosphorylated nucleoside derivatives.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: April 9, 2013
    Assignee: Centre National de la Recherche-Scientifique-CNRS
    Inventors: Anny Cupo, Cecile Le Saint, Jean-Pierre Vincent, Fatima Akeb, Daniele Duval, Roger Guedj
  • Publication number: 20130079296
    Abstract: The present invention relates to a reliable method of prediction of lower respiratory tract infection or inflammation in humans, wherein the level of pancreatic stone protein/regenerating protein (PSP/reg) is determined in serum, and a high level is indicative of the development and the severity of the disease, allowing the classification of patients according to risk.
    Type: Application
    Filed: May 31, 2011
    Publication date: March 28, 2013
    Applicants: SEPSTONE DIAGNOSTICS SARL, UNIVERSITY HOSPITAL OF BASEL
    Inventors: Daiana Stolz, Frederic Lajaunias
  • Publication number: 20130072427
    Abstract: Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.
    Type: Application
    Filed: July 22, 2010
    Publication date: March 21, 2013
    Inventors: Cristiano Guimaraes, Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
  • Publication number: 20130058998
    Abstract: A method for treating a disorder characterized by hyposialylation in a subject that includes administering to the subject an effective amount of (i) a composition comprising N-acetylmannosamine, or a derivative thereof, encapsulated within a liposome, or (ii) a composition comprising N-acetylneuraminic acid, or a derivative thereof, encapsulated within a liposome, wherein the liposome comprises 1,2-dioleoyl-3-trimethylammonium-propane and cholesterol.
    Type: Application
    Filed: September 6, 2012
    Publication date: March 7, 2013
    Inventors: Marjan Huizing, Tal Yardeni, Christopher M. Jay, Nancy Smyth Templeton, William A. Gahl
  • Publication number: 20130059808
    Abstract: The present invention relates to antimicrobial agents. Some embodiments include compounds, compositions, methods of preparation, and methods of treatment using new aminoglycosides and aminoglycoside derivatives.
    Type: Application
    Filed: May 12, 2011
    Publication date: March 7, 2013
    Applicant: Rempex Pharmaceuticals, Inc.
    Inventors: Tomasz W. Glinka, Olga Rodny
  • Publication number: 20130059807
    Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.
    Type: Application
    Filed: February 22, 2012
    Publication date: March 7, 2013
    Applicant: Satiogen Pharmaceuticals, Inc.
    Inventors: Bronislava Gedulin, Andrew A. Young, Howard E. Greene
  • Publication number: 20130045290
    Abstract: The present invention relates, e.g., to a system for treating damaged skin, comprising a cosmeceutical formulation comprising about 1-10% of a mixture of perfluorocarbons (PFC's) of at least three different molecular weights, and about 0.001-5% hyaluronic acid (HA) of molecular weight about 100 kDa or less, packaged in an aerosol spray container.
    Type: Application
    Filed: August 16, 2012
    Publication date: February 21, 2013
    Applicant: Kate Somerville Skincare, LLC
    Inventors: Kate Somerville, Fred Khoury
  • Patent number: 8372815
    Abstract: In one embodiment, the invention provides a method of suppressing, inhibiting, preventing, or treating conjunctivitis in a subject, comprising the step of administering an effective amount of a lipid or phospholipid moiety bound via an ester or amide bond to a physiologically acceptable monomer, dimer, oligomer, or polymer, and/or a pharmaceutically acceptable salt or a pharmaceutical product thereof to a subject with conjunctivitis.
    Type: Grant
    Filed: October 26, 2009
    Date of Patent: February 12, 2013
    Assignee: Yissum Research Development Company
    Inventor: Saul Yedgar
  • Publication number: 20130034536
    Abstract: Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.
    Type: Application
    Filed: August 3, 2012
    Publication date: February 7, 2013
    Applicant: Lumena Pharmaceuticals, Inc.
    Inventor: Bronislava GEDULIN
  • Publication number: 20130012466
    Abstract: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.
    Type: Application
    Filed: July 9, 2012
    Publication date: January 10, 2013
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Jon S. Thorson, Ahmed Aqeel
  • Publication number: 20130011411
    Abstract: Methods and compositions for diagnosing and treating cancer, such as breast cancer are provided. In particular, methods and compositions relating to nucleic acids encoding DACH1 and DACH1 proteins are provided.
    Type: Application
    Filed: January 6, 2011
    Publication date: January 10, 2013
    Inventors: Richard G. Pestell, Kongming Wu, Xuanmao Jiao, Sanjay Katiyar, Vladimir M. Popov, Mathew Casimiro
  • Patent number: 8344133
    Abstract: The present invention provides methods of producing compounds with enhanced desirable properties and diminished side effects as well as the compounds produced by the methods. In preferred embodiments, methods of the present invention use a universal chemical glycosylation method that employs reducing sugars and requires no protection or activation. In a preferred embodiment, the invention provides neoglycoside digitoxin analogs that include compounds with significantly enhanced cytotoxic potency toward human cancer cells and tumor-specificity, but are less potent Na+/K+-ATPase inhibitors in a human cell line than digitoxin.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: January 1, 2013
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Jon S. Thorson, Joseph M. Langenhan
  • Patent number: 8343937
    Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: January 1, 2013
    Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari
    Inventors: Jean-Pierre Sommadossi, Paulo LaColla
  • Publication number: 20120309672
    Abstract: Pharmaceutical compositions are provided. The compositions comprise a compound comprising the hyaluronan-containing structure A-(low molecular weight hyaluronan domain)-B. The compositions also comprise a pharmaceutically acceptable excipient. A is hydrogen, a substituent that does not comprise a binding site for tumor necrosis factor stimulated gene-6 (“TSG-6”) protein, a substituent that interferes with binding of TSG-6 protein immediately adjacent thereto, or chondroitin. B is hydroxyl, a substituent that does not comprise a binding site for TSG-6 protein, a substituent that interferes with binding of TSG-6 protein immediately adjacent thereto, or chondroitin. The composition is suitable for administration by injection, inhalation, topical rub, or ingestion.
    Type: Application
    Filed: June 6, 2012
    Publication date: December 6, 2012
    Applicant: THE CLEVELAND CLINIC FOUNDATION
    Inventors: Anthony Calabro, Mark Lauer, Vincent Hascall
  • Patent number: 8324373
    Abstract: The present invention provides a novel and highly stereoselective process for preparing gemcitabine, which is suitable for industrial production, wherein, it includes the following reactions. Additionally, the invention discloses the key intermediates. The definition for the groups of G1, G2, G3, G4, and G5 are described in the specification.
    Type: Grant
    Filed: September 7, 2007
    Date of Patent: December 4, 2012
    Assignee: Nanjing Cavendish Bio-Engineering Technology Co., Ltd.
    Inventors: Yongxiang Xu, Hao Yang, Wen Hou
  • Patent number: 8304395
    Abstract: The invention relates to methods of use for compounds in treating, reducing the incidence, reducing the severity or pathogenesis of an intestinal disease or condition in a subject, including, inter alia, inflammatory bowel disease, Crohn's disease, ulcerative colitis, or a combination thereof.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: November 6, 2012
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd.
    Inventor: Saul Yedgar
  • Patent number: 8299038
    Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
    Type: Grant
    Filed: July 16, 2009
    Date of Patent: October 30, 2012
    Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari
    Inventors: Jean-Pierre Sommadossi, Paulo LaColla
  • Patent number: 8293720
    Abstract: The present invention provides substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: October 23, 2012
    Assignee: Dogwood Pharmaceuticals, Inc.
    Inventors: Robert D Thompson, Anthony Beauglehole, Frank Schmidtmann, Jayson M. Rieger
  • Publication number: 20120258170
    Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.
    Type: Application
    Filed: March 19, 2012
    Publication date: October 11, 2012
    Applicant: Nutracryst Therapeutics Private Limited
    Inventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
  • Patent number: 8278283
    Abstract: The present disclosure describes 6-disubstituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the 6-disubstituted bicyclic nucleosides each comprise a 2?-O—C(Ri)(R2)-4? or 2?-O—C=(R3)(R.4)-4? bridge wherein each R is, independently a substituent group and Ri and R2 include H. The 6-disubstituted bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: October 2, 2012
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze
  • Patent number: 8278425
    Abstract: Provided herein are bicyeMc nucleosides comprising a substituted amino group in the bridge, oligomeric compounds having at least one of these bicyclic nucleosides and methods of using the oligomeric compounds. The bicyclic nucleosides comprising a substituted amino group in the bridge are useful for enhancing properties of oligomeric compounds including nuclease resistance, in certain embodiments, the oligomeric compounds hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: May 22, 2008
    Date of Patent: October 2, 2012
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Balkrishin Bhat, Eric E. Swayze
  • Patent number: 8278436
    Abstract: The present invention discloses a set of glycosylated warfarin analogs which are useful as anti-tumor or anti-metastatic agents and as reagents for studying sugar uptake in cells.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: October 2, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Jon S. Thorson, Shannon C. Timmons
  • Patent number: 8278282
    Abstract: This invention relates to novel compounds that have various medicinal applications, e.g. for the treatment and/or prevention of viral infections.
    Type: Grant
    Filed: February 7, 2008
    Date of Patent: October 2, 2012
    Assignee: Novartis AG
    Inventors: Zheng Yin, Jeyaraj Duraiswamy, Yen Liang Chen
  • Patent number: 8278426
    Abstract: Provided herein are saturated and unsaturated carbocyclic bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using these oligomeric compounds. The saturated and unsaturated carbocyclic bicyclic nucleosides are useful for enhancing properties of oligomeric compounds including nuclease resistance.
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: October 2, 2012
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze
  • Publication number: 20120238519
    Abstract: An ophthalmic composition that, despite containing alginic acid and/or a salt thereof, has improved tackiness during use and provides a satisfactory use feeling. The composition has an improved ability to remain on the eye mucosa. The ophthalmic composition contains (A) alginic acid and/or a salt thereof in combination with (B) hyaluronic acid and/or a salt thereof.
    Type: Application
    Filed: March 27, 2012
    Publication date: September 20, 2012
    Applicant: ROHTO PHARMACEUTICAL CO., LTD.
    Inventors: Eri MATSUMOTO, Yasuko NISHINA, Kenichi HARUNA, Harumasa ARITA, Akiko KITA
  • Patent number: 8252767
    Abstract: The present invention provides substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: December 20, 2008
    Date of Patent: August 28, 2012
    Assignee: Dogwood Pharmaceuticals, Inc.
    Inventors: Robert Thompson, Anthony Beauglehole, Frank Schmidtmann, Jayson Rieger
  • Patent number: 8252752
    Abstract: Hydrophilic transportable N-linked glycosyl dopaminergic prodrug compounds according to FORMULA V and methods of their use, wherein, Ring 1 comprises an aryl or heteroaryl ring having 4 to 8 carbon atoms, among which atoms are counted “X” and “Y”; each of X and Y is optional; X, when present is either —C(R1)2— or —C(R)2—; Y, when present, is either —CH2— or —CH2—CH2—; z, R5 and R5? are optional, and when present z, R5 and R5? together form a lower alkyl or a substituted lower alkyl moiety; N is part of either an amine or an amide linkage; E is a saccharide which forms a linkage with N through a single bond from a carbon or oxygen atom thereof; R1 and R4 are selected form the group consisting of hydrogen, hydroxyl, halogen, halo-lower alkyl, alkoxyl, alkoxyl-lower alkyl, halo-alkoxy, thioamido, amidosulfonyl, alkoxylcarbonyl, carboxamide, aminocarbonyl, and alkylamino-carbonyl; R2 and R3 are hydroxyl; R5 and R6, when present, are selected from the group consisting of hydrogen, hydroxyl, alkoxyl, carbonyl
    Type: Grant
    Filed: December 27, 2007
    Date of Patent: August 28, 2012
    Assignee: Glycon LLC
    Inventor: Samuel T. Christian
  • Patent number: 8247381
    Abstract: The present invention provides branched water-soluble polymers that allow two or more water-soluble polymers to be conjugated to another species. The branched polymers provide access to therapeutic agents that are conjugated at a single site to two or more water-soluble polymers. The branched polymers are based upon branch points that are simple branched alkyl structures, reactive side-chain amino acids and small peptides of reactive side-chain amino acids, and saccharides. Also provided is a method for preparing mono-disperse poly(ethylene glycol) of a well-defined and determinable molecular weight, and a method for the rational end-functionalization of poly(ethylene glycol). Conjugates of the branched water-soluble polymers with diverse species, e.g., peptides, lipids, glycolipids and small molecules are also provided.
    Type: Grant
    Filed: August 17, 2010
    Date of Patent: August 21, 2012
    Assignee: BioGeneriX AG
    Inventor: Shawn DeFrees
  • Publication number: 20120207737
    Abstract: The present invention relates to the use of glycan-binding polypeptides and glycans as a medicament, in particular for treating and/or preventing helminthic infections or an immune disease. Moreover, the present invention is directed to corresponding pharmaceutical compositions, food products and animal feed comprising isolated glycans and/or glycan-binding polypeptides. In addition, the present invention teaches methods for identifying anti-helminthic carbohydrate-binding polypeptides, for identifying helminthic glycan and gene targets involved in glycan-mediated toxicity, for identifying helminths susceptible to glycan-mediated toxicity, and for identifying anti-helminthic and anti-allergic substances.
    Type: Application
    Filed: October 12, 2010
    Publication date: August 16, 2012
    Applicants: UNIVERSITY OF ZURICH, ETH ZURICH
    Inventors: Markus Kunzler, Martin Walti, Alex Butschi, Markus Aebi, Michael Hengartner
  • Patent number: 8232254
    Abstract: Colchicine neoglycosides, method for their synthesis and methods for their use are disclosed. The invention provides analogs of colchicine glycosylated to include a sugar moiety on a colchicine scaffold that is generally unglycosylated in nature. The colchicine neoglycosides disclosed herein are shown to have cytotoxic effects equivalent to at least the known cytotoxins paclitaxel and doxorubicin. Further, the neoglycosides disclosed according to the invention have physiologic effects not previously recognized in the alkaloid family that includes colchicine but recognized in other cytotoxic drug families such as the taxanes which act by stabilizing tubulin formation.
    Type: Grant
    Filed: October 8, 2007
    Date of Patent: July 31, 2012
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Jon S. Thorson, Ahmed Aqeel
  • Publication number: 20120190633
    Abstract: The present invention provides for monophosphorylated lipid A derivatives and carbohydrate derivatives that are useful as agents in the treatment of diseases and conditions, including cancers. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I-IV. In addition, methods for the treatment of cancers are provided.
    Type: Application
    Filed: July 30, 2010
    Publication date: July 26, 2012
    Inventors: Zhongwu Guo, Qianli Wang, Shouchu Tang