Purines (including Hydrogenated) (e.g., Adenine, Guanine, Etc.) Patents (Class 514/45)
  • Patent number: 10292951
    Abstract: This disclosure features chemical entities (e.g., a compound exhibiting activity as a mitochondrial uncoupling agent or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as niclosamide or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof; e.g., a compound, such as a niclosamide analog, or a pharmaceutically acceptable salt and/or hydrate and/or cocrystal thereof) that are useful, e.g., for treating one or more symptoms of a pathology characterized by an abnormal inflammatory response (e.g., inflammatory bowel diseases) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: September 1, 2016
    Date of Patent: May 21, 2019
    Assignee: First Wave Bio, Inc.
    Inventors: Gary D. Glick, Luigi Franchi, Giancarlo Santus
  • Patent number: 9968628
    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: November 13, 2012
    Date of Patent: May 15, 2018
    Assignees: Idenix Pharmaceuticals LLC, Universita Degli Studi Di Cagliari
    Inventors: Jean-Pierre Sommadossi, Paolo LaColla
  • Patent number: 9969802
    Abstract: Provided is a detection method for a malignant tumor cell, including measuring a protein marker expressed on a malignant tumor cell surface. The detection method for a malignant tumor cell includes measuring LR11 on a cell surface in a sample to be tested.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: May 15, 2018
    Assignee: SEKISUI MEDICAL CO., LTD.
    Inventors: Hiroyuki Ebinuma, Kohei Takubo, Isamu Fukamachi, Saishu Yoshida, Hideaki Bujo, Chiaki Nakaseko, Yasushi Saito
  • Patent number: 9861811
    Abstract: Apparatus and methods for treating back pain are provided in which electrical stimulation therapy is designed to cause muscle contraction to rehabilitate the muscle, restore neural drive and restore spinal stability. In accordance with one aspect, electrical stimulation is applied through at least one electrode to stimulate efferent motor nerve fibers to cause muscle contraction to facilitate rehabilitation without targeting stimulation of afferent nerve fibers. In accordance with another aspect, a stimulator further includes one or more of a number of additional therapeutic modalities, including a module that provides analgesic stimulation; a module that monitors muscle performance and adjusts the muscle stimulation regime; and/or a module that provides longer term pain relief by selectively and repeatedly ablating nerve fibers.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: January 9, 2018
    Assignee: Mainstay Medical Limited
    Inventors: Peter Andrew Crosby, Dan Sachs, Prashant Brijmohansingh Rawat, Jason Alan Shiroff, Johannes Petrus Heemels
  • Patent number: 9737512
    Abstract: Certain embodiments are directed to methods of treating pain, e.g., chronic or neuropathic pain, comprising administering an effective amount of an EPAC inhibitor.
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: August 22, 2017
    Assignee: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Xiaodong Cheng, Fang Mei, Annemieke Kavelaars, Cobi J. Heijnen
  • Patent number: 9732111
    Abstract: The present invention relates to 2?-Alkynyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Alkynyl Substituted Nucleoside Derivative, and methods of using the 2?-Alkynyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: November 14, 2013
    Date of Patent: August 15, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Frank Bennett, Yuhua Huang, Lingyan Wang, Stephane L. Bogen, Angela D. Kerekes, Vinay M. Girijavallabhan, Gabor Butora, Quang Truong, Ian Davies, Ann E. Weber
  • Patent number: 9730944
    Abstract: The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: August 15, 2017
    Assignee: Katholieke Universiteit Leuven, K.U. Leuven R&D
    Inventors: Steven De Jonghe, Ling-Jie Gao, Piet Herdewijn, Jean Herman, Miyeon Jang, Pieter Leyssen, Thierry Louat, Johan Neyts, Christophe Pannecouque, Bart Vanderhoydonck
  • Patent number: 9713622
    Abstract: The present invention relates to a pharmaceutical composition for treating the human immunodeficiency virus (HIV) in humans, including three or four active principles selected as: a nucleoside reverse transcriptase inhibitor (NRTI) selected from lamivudine and emtricitabine; a nucleoside or nucleotide reverse transcriptase inhibitor (NRTI) selected from didanosine, abacavir and tenofovir; and the combination of a boosted or unboosted protease inhibitor (PI) selected from lopinavir, fosamprenavir, atazanavir and darunavir; or an non-nucleoside reverse transcriptase inhibitor (NNRTI) selected from efavirenz and etravirine; or an integrase inhibitor; for daily administration to said human being one to four days per week.
    Type: Grant
    Filed: June 23, 2015
    Date of Patent: July 25, 2017
    Assignee: UNIVERSITÉ VERSAILLES SAINT-QUENTIN-EN-YVELINES
    Inventor: Jacques Leibowitch
  • Patent number: 9632090
    Abstract: The subject matter relates to newly discovered nucleic acid molecules and proteins associated with thymic lymphoma and hamartomatous tumors. Compositions and methods for detecting, characterizing, preventing, and treating human thymic lymphoma and hamartomatous tumors are provided.
    Type: Grant
    Filed: August 26, 2010
    Date of Patent: April 25, 2017
    Assignee: Dana-Farber Cancer Institute, Inc.
    Inventors: Ronald A. DePinho, Ji-Hye Paik, Ramya Kollipara
  • Patent number: 9631240
    Abstract: Nucleotide and amino acid variations associated with tumors are provided. Methods for detecting variations and for diagnosing and treating tumors are provided.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: April 25, 2017
    Assignee: Genentech, Inc.
    Inventors: Zhengyan Kan, Denise M. Kenski, Brock Peters, Somasekar Seshagiri
  • Patent number: 9586986
    Abstract: Compounds of Formula I and a pharmaceutically acceptable salt thereof, an optical isomer thereof, or a mixture of optical isomers thereof, as well as compositions which include such compounds and therapeutic methods that utilize such compounds and/or compositions.
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: March 7, 2017
    Assignees: INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I., PALACKY UNIVERSITY IN OLOMOUC
    Inventors: Michal Hocek, Petr Naus, Olga Caletkova, Marian Hajduch, Petr Dzubak
  • Patent number: 9579337
    Abstract: The present invention relates to a pharmaceutical or dietary composition comprising deoxyuridine and a pharmaceutically or dietetically suitable carrier. Another aspect of the present invention relates to a method of supplementing the dietary needs of a subject. This method includes administering to the subject a dietary supplementing effective amount of deoxyuridine. Yet another aspect of the present invention relates to a method of treating cancer in a subject. This method includes selecting a subject having cancer and administering to the selected subject a therapeutically effective amount of uridine, thereby treating the cancer in the selected subject.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: February 28, 2017
    Assignee: Cornell University
    Inventors: Patrick J. Stover, Martha S. Field
  • Patent number: 9567627
    Abstract: The invention relates in particular to an in vitro or ex vivo method for predicting the response of a patient to treatment with at least one HER2-blocking agent, said method including the steps of: i) identifying the nucleotide at the rs3746083 polymorphic site, for at least one allele, in particular the two alleles of the gene coding the tristetraprolin protein, in a biological sample from said patient; and/or ii) determining the concentration of the tristetraprolin protein in a biological sample from said patient, wherein said patient is suffering from HER2-positive cancer.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: February 14, 2017
    Assignees: UNIVERSITE DE NICE SOPHIA ANTIPOLIS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)
    Inventor: Gilles Pages
  • Patent number: 9505796
    Abstract: A phosphorylated A2A receptor agonist providing agonist properties on the A2A receptor after dephosphorylation the phosphorylated A2A receptor agonist comprises a ribosyl moiety and a purine moiety and being phosphorylated at the 5?-position of the ribose moiety except adenosine monophosphate (AMP), adenosine diphosphate (ADP) or adenosine triphosphate (ATP), a medicament containing the compound of the invention including ADP and the use of the compound of the invention including ATP and ADP for several medical indications e.g. inflammatory events. In particular, compounds of formula (I) are also disclosed.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: November 29, 2016
    Assignee: Crozet Medical GmbH
    Inventors: Jurgen Schrader, Christa Muller, Ali El-Tayeb, Jamshed Iqbal
  • Patent number: 9464326
    Abstract: Toll-like receptors (TLR) are expressed by a variety of cancers, including melanoma and T-ALL. TLR signaling plays an important role in T cell malignancies and melanoma. The effects of stimulating or inhibiting the TLR/IL-1 receptor-associated kinases IRAK-1 and IRAK-4 in melanoma and T-ALL cells were evaluated. Pharmacological treatment with an IRAK-1,-4 inhibitor delays tumor growth and prolongs survival in vitro and in vivo, indicating that TLR signaling contributes to T-ALL and melanoma progression and interfering with this signaling is a novel therapeutic strategy to control T-ALL and melanoma proliferation.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: October 11, 2016
    Assignee: University of Maryland, Baltimore
    Inventor: Eduardo Davila
  • Patent number: 9456629
    Abstract: An infant and/or toddler nutrition comprising non-viable Bifidobacterium breve and a non-digestible oligosaccharide and its use are disclosed.
    Type: Grant
    Filed: June 13, 2008
    Date of Patent: October 4, 2016
    Assignee: N.V. NUTRICIA
    Inventors: Sander Hougee, Adrianus Johannes Maria Vriesema, Johan Garssen, Jan Knol
  • Patent number: 9452217
    Abstract: Compositions and methods including at least one PNP inhibitor or at least one PNP inhibitor in combination with one or more agents identified as endogenous adjuvants useful in the treatment of pathogen infection and cancer are disclosed. The compositions may be formulated as pharmaceutical dosage forms and components may be assembled as kits. Methods for increasing levels of endogenous adjuvants to enhance an immune response and to potentiate/augment antiviral, antibacterial or anticancer effects of therapeutic agents are also disclosed.
    Type: Grant
    Filed: June 19, 2014
    Date of Patent: September 27, 2016
    Assignee: Nitor Therapeutics
    Inventor: Shanta Bantia
  • Patent number: 9422321
    Abstract: The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: Also disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: August 23, 2016
    Assignees: High & New Technology Research Center, Henan Academy of Sciences, Zhengzhou Granlen Pharmatech Ltd., Zhengzhou University
    Inventors: Junbiao Chang, Haoyun An, Xuejun Yu, Xiaohe Guo
  • Patent number: 9423405
    Abstract: Methods of characterizing a test subject's risk of having or developing cardiovascular disease are provided. The methods include using an analytic device to determine levels of choline-related trimethylamine-containing compounds such as trimethylamine N-oxide, choline, or betaine in a biological sample obtained from the subject and comparing the levels of the choline-related trimethylamine-containing compound in the subject's biological sample to a control value. The test subject's risk of having cardiovascular disease is then characterized as higher if the levels of the choline-related trimethylamine-containing compound are higher than the control value. Also provided are methods of identifying a subject at risk of experiencing a complication of atherosclerotic cardiovascular disease, and methods of evaluating the efficacy of a cardiovascular therapeutic agent in a subject with cardiovascular disease using levels of choline-related trimethylamine-containing compounds.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: August 23, 2016
    Assignee: The Cleveland Clinic Foundation
    Inventors: Stanley L. Hazen, Zeneng Wang, Bruce S. Levison
  • Patent number: 9387220
    Abstract: The present application provides methods and compositions for inducing hepatocyte proliferation and liver regeneration, the latter being mainly dependent on hepatocyte proliferation even if all the other cell types divide to reconstitute the organ specific-lobular-architecture. The methods and compositions provided herein make use of an A3AR agonist. A preferred A3AR agonist disclosed herein is Cl-IB-MECA.
    Type: Grant
    Filed: August 21, 2014
    Date of Patent: July 12, 2016
    Assignee: CAN-FITE BIOPHARMA LTD.
    Inventors: Pnina Fishman, Shira Cohen
  • Patent number: 9315545
    Abstract: Compounds and methods are described herein that can be used to treat subjects for conditions related to hepcidin activity, such as but not limited diseases of iron metabolism, beta thalassemia, hemochromatosis, iron-loading anemias, alcoholic liver disease, or chronic hepatitis C.
    Type: Grant
    Filed: April 7, 2015
    Date of Patent: April 19, 2016
    Assignee: MERGANSER BIOTECH, INC.
    Inventor: Gene Scott Merutka
  • Patent number: 9315535
    Abstract: The present invention provides compounds shown by the formula: wherein Y1 is CR6 or N, Y2 is CR7 or N, Y3 is CR8 or N, R6, R7 and R8 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, Bx is a nucleic acid base moiety, Z1 and Z2 are each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group, R1 to R5 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, and n is an integer of 0 to 3, or salts thereof, that are novel nucleosides or nucleotides that can be useful as materials for synthesizing nucleic acid pharmaceuticals.
    Type: Grant
    Filed: February 17, 2014
    Date of Patent: April 19, 2016
    Assignee: SHIONOGI & CO., LTD.
    Inventors: Yasunori Mitsuoka, Akira Kugimiya, Aiko Yamashita
  • Patent number: 9301960
    Abstract: The invention provides compositions for inhibiting a redox-sensitive GTPase protein, including a Rho or Rab family GTPase, comprising an effective amount of a redox-sensitive purine compound and an effective amount of a redox agent. The invention further provides methods of inhibiting a redox-sensitive GTPase protein, including a Rho or Rab family GTPase, by administering compositions of the invention. Methods of screening for compounds that inhibit a redox-sensitive GTPase protein, including compounds that target and inhibit Rho or Rab family GTPases, are further provided.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: April 5, 2016
    Assignee: Board of Regents, The University of Texas Systems
    Inventor: Jongyun Heo
  • Patent number: 9290533
    Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.
    Type: Grant
    Filed: March 22, 2013
    Date of Patent: March 22, 2016
    Assignees: Novartis AG, Centre National de la Recherche Scientifique, L'Universite Montpellier II
    Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
  • Patent number: 9247875
    Abstract: A method of diagnosing a patient with age-related macular degeneration (AMD), by detecting biomarkers in the patient's Bruch's membrane, and diagnosing the patient with AMD. A method of detecting the presence of AMD in a patient, by detecting biomarkers in the patient's Bruch's membrane. A method of detecting inflammation in a patient, by detecting biomarkers in the patient's Bruch's membrane. A method of determining the progression of AMD in a patient. A method of determining efficacy of a treatment for AMD in a patient. A method of determining the presence of AMD in an animal model. A kit for detecting the presence of disease in a patient, including an assay for biomarkers 3-nitrotyrosine and nitro-A2E. An assay of the biomarkers.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: February 2, 2016
    Assignee: Board of Trustees of Northern Illinois University
    Inventors: Elizabeth R. Gaillard, James P. Dillon
  • Patent number: 9249409
    Abstract: A method for detecting a cancer(s) based on an expression of prescribed polypeptides is disclosed. These polypeptides were isolated, by the SEREX method using a cDNA library derived from canine testis and serum from a cancer-bearing dog, as a polypeptide which binds to an antibody existing in serum derived from cancer-bearing living body. Because these polypeptides react with antibodies specifically existing in serum of a cancer patient, cancers in a living body can be detected by measuring the antibody in a sample. Cancers in a living body can also be detected by measuring the antigen protein of the antibody per se or mRNA encoding it.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: February 2, 2016
    Assignee: TORAY INDUSTRIES, INC.
    Inventors: Fumiyoshi Okano, Kana Suzuki
  • Patent number: 9221864
    Abstract: The present disclosure provides tricyclic nucleosides and oligomeric compounds prepared therefrom. The tricyclic nucleosides each have a tricyclic ribosyl sugar moiety wherein a bridge between the 2? and 4? ribosyl ring carbon atoms further comprises a fused carbocyclic or heterocyclic ring. The tricyclic nucleosides are expected to be useful for enhancing properties of oligomeric compounds including for example binding affinity and nuclease resistance.
    Type: Grant
    Filed: March 20, 2013
    Date of Patent: December 29, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze, Stephen Hanessian, Benjamin R. Schroeder, Robert D. Giacometti, Bradley L. Merner
  • Patent number: 9134313
    Abstract: A tumor marker comprising diacetylspermine, and a method of evaluating the state of a tumor, comprising reacting an antibody to diacetylspermine with a biological sample to thereby detect diacetylspermine and evaluating the state of the tumor using the obtained detection results as an indicator.
    Type: Grant
    Filed: June 9, 2009
    Date of Patent: September 15, 2015
    Assignees: Tokyo Metropolitan Organization For Medical Research, CRC Inc., Tokyo Metropolitan Government, Trans Genic Inc.
    Inventors: Masao Kawakita, Kyoko Hiramatsu, Keiichi Takahashi, Naotaka Hamasaki, Koji Yamaguchi, Tsunehisa Kaku, Koichiro Muta, Munechika Enjoji, Seiji Naito, Jun Hayashi, Shoshu Mitsuyama, Hiroyuki Yamashita, Toru Inoue, Masato Kato
  • Patent number: 9090646
    Abstract: The invention provides new biotinylated compounds and methods for their use.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: July 28, 2015
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Roger A. Jones, Barbara L. Gaffney
  • Patent number: 9078910
    Abstract: The present invention relates to compositions comprising spicamycin derivatives, methods of making such compositions, and their use in the treatment and/or prevention of pain, including neuropathic pain.
    Type: Grant
    Filed: August 8, 2013
    Date of Patent: July 14, 2015
    Assignee: DARA BIOSCIENCES, INC.
    Inventors: Michael Radomsky, Mary Katherine Delmedico, Linda Jett
  • Patent number: 9062046
    Abstract: The present invention relates to substituted imidazo[4,5-c]quinoline derivatives, the compounds of formula (I), wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of formula (I), and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammatory diseases and angiogenesis related disorders.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: June 23, 2015
    Assignee: Piramal Enterprises Limited
    Inventors: Sanjay Kumar, Rajiv Sharma, Robert Zahler, Bichismita Sahu, Veena R. Agarwal, Nishigandha Naik
  • Patent number: 9040498
    Abstract: The present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: May 26, 2015
    Assignee: Research Foundation of the City University of New York
    Inventor: Mahesh K. Lakshman
  • Publication number: 20150141362
    Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 21, 2015
    Inventors: Robert A. Copeland, Victoria M. Richon, Margaret D. Scott, Christopher J. Sneeringer, Kevin W. Kuntz, Sarah K. Knutson, Roy M. Pollock
  • Publication number: 20150132258
    Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
    Type: Application
    Filed: November 14, 2014
    Publication date: May 14, 2015
    Inventor: George D. Hartman
  • Patent number: 9029345
    Abstract: An agent for inhibiting P-glycoproteins comprises a non-natural adenine ribose analog.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: May 12, 2015
    Assignee: Case Western Reserve University
    Inventors: Anthony J. Berdis, Irene Lee
  • Patent number: 9029343
    Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.
    Type: Grant
    Filed: December 5, 2011
    Date of Patent: May 12, 2015
    Assignee: Epizyme, Inc.
    Inventors: Richard Chesworth, Kevin W. Kuntz, Edward J. Olhava, Michael A. Patane
  • Patent number: 9029335
    Abstract: Provided herein are novel bicyclic nucleosides, oligomeric compounds that include such bicyclic nucleosides and methods of using the oligomeric compounds. More particularly, the novel bicyclic nucleosides comprise a furanose ring system having a bridge comprising a 4?-methylene group attached to a 2?-sulfoxide or sulfone group and optionally including one or more substituent groups attached to the 4?-methylene and or the 5?-position. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 12, 2015
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Thazha P. Prakash, Eric E. Swayze
  • Publication number: 20150105341
    Abstract: Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 16, 2015
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Marija Prhavc, Christian Andreas Jekle, Jerome Deval
  • Patent number: 9006207
    Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: April 14, 2015
    Assignee: Hydra Biosciences, Inc.
    Inventors: Howard Ng, Jianfeng Hang
  • Publication number: 20150087613
    Abstract: The invention provides methods and compositions for inhibiting opioid tolerance by administering an A3AR agonist to a subject receiving opiate therapy for nociceptive pain. Also provided are methods of treating opiate withdrawal using an A3AR agonist.
    Type: Application
    Filed: September 25, 2014
    Publication date: March 26, 2015
    Inventor: Daniela SALVEMINI
  • Publication number: 20150079107
    Abstract: Provided herein are methods and assays for isolating and culturing seborrheic keratosis cells ex vivo. Also provided herein are screening assays using cultured seborrheic keratosis cells and methods for treating seborrheic keratosis in a subject.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 19, 2015
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Anna I. Mandinova, Sam W. Lee, Victor A. Neel
  • Patent number: 8980850
    Abstract: The present disclosure relates to methods for the treatment of cancer in patients in recognized need of such treatment. The methods comprise administering to such a patient an NAE inhibitor or a pharmaceutically acceptable salt thereof, such as ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) or {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate (I-216), and a hypomethylating agent or a pharmaceutically acceptable salt thereof, such as azacitidine or decitabine. Also disclosed are medicaments for use in the treatment of cancer.
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: March 17, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventor: Peter G. Smith
  • Publication number: 20150057243
    Abstract: Methods and compositions disclosed herein relate to detecting, analyzing, isolating and inhibiting methyltransferases, methyltransferase substrates, S-adenosyl-methionine-binding proteins and RNA, including for the treatment of disease.
    Type: Application
    Filed: April 2, 2013
    Publication date: February 26, 2015
    Applicant: Northern University
    Inventors: Zhaohui Sunny Zhou, Wanlu Qu, Tianyi Bai
  • Publication number: 20150051167
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 19, 2015
    Inventors: Guangyi Wang, David Bernard Smith, Leonid Beigelman, Jerome Deval, Marija Prhavc
  • Patent number: 8951985
    Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: February 10, 2015
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Dominique Surleraux, Cyril B. Dousson, David Dukhan, Claire Pierra
  • Patent number: 8946188
    Abstract: Many pathogens, including Mycobacterium tuberculosis and Yersinia pestis, rely on an iron acquisition system based on siderophores, secreted iron-chelating compounds with extremely high Fe(III) affinity. The compounds of the invention are inhibitors of domain salicylation enzymes, which catalyze the salicylation of an aroyl carrier protein (ArCP) domain to form a salicyl-ArCP domain thioester intermediate via a two-step reaction. The compounds include the intermediate mimic 5?-O—[N-(salicyl)sulfamoyl]-adenosine (salicyl-AMS) and analogs thereof. These compounds are inhibitors of the salicylate activity of MbtA, YbtE, PchD, and other domain salicylation enzymes involved in the biosynthesis of siderophores. Therefore, these compounds may be used in the treatment of infection caused by microorganisms which rely on siderphore-based iron acquisition systems.
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: February 3, 2015
    Assignees: Sloan-Kettering Institute for Cancer Research, Cornell Research Foundation, Inc.
    Inventors: Derek Shieh Tan, Luis E. N. Quadri, Jae-Sang Ryu, Justin Scott Cisar, Julian Alberto Ferreras, Xuequan Lu
  • Publication number: 20150025031
    Abstract: The present invention provides a system and method of maintaining and/or increasing cell viability by downregulating cellular metabolic rate under hypoxic conditions, wherein the availability of adenosine or derivatives thereof in the cell is increased and/or prolonged. The present invention also relates to a system and method of prolonging the survival of implanted cells that are under hypoxic condition until host neovascularization is achieved, wherein the availability of adenosine or derivatives thereof in the cell is increased and/or prolonged. The present invention also provides a system and method of maintaining and/or increasing cell viability by downregulating cellular metabolic rate under hypoxic conditions, wherein at least one purine metabolism enzyme inhibitor is applied to the cell.
    Type: Application
    Filed: March 5, 2013
    Publication date: January 22, 2015
    Inventors: James Yoo, Sang Jin Lee, Jachyun Kim, Anthony Atala
  • Publication number: 20150018297
    Abstract: The present disclosure relates to a pharmaceutical composition, a health functional food composition, and a method for preventing or treating a brain disease or diabetes. The pharmaceutical composition, health functional food composition, and method includes at least one active ingredient that is chlorhexidine, thioguanosine, mebendazole, fenbendazole, colchicine, farnesol, trimethobenzamide hydrochloride, disulfuram, azathioprine, mebeverine hydrochloride, zaprinast, tosufloxacin hydrochloride, efavirenz, thiostrepton, probenecid, entacapone, harmine hydrochloride, flunisolide, thimerosal, hexestrol, sulfaquinoxaline sodium salt, monensin sodium salt, raloxifene hydrochloride, 2-chloropyrazine, or topotecan.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITY
    Inventors: Dong Gyu JO, Jong Sung PARK, Youngkwang YOUN, Yuri CHOI, Ui Jeong YUN
  • Publication number: 20150011497
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a norovirus, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 8, 2015
    Inventors: Leonid Beigelman, Jerome Deval, Zhinan Jin
  • Publication number: 20150011496
    Abstract: The invention provides methods and compositions for stimulating or promoting bone regeneration or repairing bone fracture or for stimulating or increasing differentiation or activation of osteoblasts by administering to a subject a therapeutically effective amount of an adenosine receptor agonist, or an analog, derivative or combination thereof, an adenosine receptor antagonist, or an analog, derivative or combination thereof, or adenosine or a compound that upregulates, increases the amount of or increases the biological activity of adenosine. The invention also extends to pharmaceutical compositions such as those comprising an agent that modulates an adenosine receptor such as an adenosine A2A agonist or A1 antagonist.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 8, 2015
    Inventors: Bruce Cronstein, Aranzazu Mediero Munoz