Nitrogen, Other Than Nitro Or Nitroso, Bonded Directly To The 6-position Of A Purine Ring System (e.g., Adenosine, Etc.) Patents (Class 536/27.6)
  • Patent number: 9163056
    Abstract: The present disclosure relates to the field of nucleic acid chemistry, specifically to 5-position modified uridines as well as phosphoramidite and triphosphate derivatives thereof. The present disclosure also relates to methods of making and using the same.
    Type: Grant
    Filed: November 1, 2013
    Date of Patent: October 20, 2015
    Assignee: SomaLogic, Inc.
    Inventors: John Rohloff, Nebojsa Janjic, Jeffrey D. Carter, Catherine Fowler
  • 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
  • Publication number: 20150094462
    Abstract: A novel method of simultaneously protecting two functions which are same or different, namely hydroxyl, amine, or thiol ones, particularly in sugars, polyalcohols, nucleosides, nucleotides, peptides, and nucleic acids during an organic synthesis, and to novel compounds for implementing this method, as well as to the method of obtaining these compounds. Method of simultaneously protecting two hydroxyl, amine, or thiol functions according to the invention by carrying out a protecting reaction between a compound having at least two free hydroxyl, amine, or thiol groups, and the disilane of formula 1, where R stands for Cl or Br, or I, or a substituent of formula 2, where X1, X2, X3, X4 are the same or different.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventors: Wojciech Tadeusz Markiewicz, Marcin Krzysztof Chmielewski, Sylwia Maria Musial, Hieronim Franciszek Maciejewski, Grzegorz Hreczycho
  • Publication number: 20150094275
    Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.
    Type: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • 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
  • Patent number: 8957201
    Abstract: A method for the prevention or treatment in a mammal of a disease preventable or treatable by the pharmacologically useful antisense or antigene activity of an oligonucleotide analogue or a pharmacologically acceptable salt thereof in the body of said mammal, which method comprises administering to said mammal in need of such prevention or treatment a pharmaceutically effective amount of an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of said nucleoside units is a structure of the formula (2): wherein A is methylene; and B is an unsubstituted purin-9-yl, an unsubstituted 2-oxo-pyrimidin-1-yl or a substituted purin-9-yl; or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: February 17, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masakatsu Kaneko, Koji Morita, Takeshi Imanishi
  • Publication number: 20140377743
    Abstract: This invention provides a nucleotide analogue comprising (i) a base selected from the group consisting of adenine, guanine, cytosine, thymine and uracil, (ii) a deoxyribose, (iii) an allyl moiety bound to the 3?-oxygen of the deoxyribose and (iv) a fluorophore bound to the base via an allyl linker, and methods of nucleic acid sequencing employing the nucleotide analogue.
    Type: Application
    Filed: August 4, 2014
    Publication date: December 25, 2014
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Jingyue Ju, Lanrong Bi, Dae Hyun Kim, Qinglin Meng
  • Publication number: 20140370108
    Abstract: Compositions and methods to improve the pharmacokinetic profile of S-Adenosylmethionine (SAMe) are provided, as are methods of treating various disorders using SAMe formulations with improved pharmacokinetic profiles. More specifically, the invention is directed to methods of treating a disease or disorder in a subject and/or improving the nutritional status of a subject by administering formulations exhibiting improved pharmacokinetic profiles of exogenous SAMe. The method also includes the step of orally administering compositions of the invention to the subject once per day after overnight fast; that is prior to food intake in the morning.
    Type: Application
    Filed: August 28, 2014
    Publication date: December 18, 2014
    Inventors: Nancy HARRISON, I. David MacDonald, Aniko Takacs-Cox, Robert Miller
  • Publication number: 20140357594
    Abstract: This invention relates to heteroaryl compounds, containing a purinyl moiety, that inhibit DNA methyltransferase (DNMT) activity—including DNMT1, DNMT3a, or DNMT3b—useful in the treatment of cancer and hyperproliferative diseases.
    Type: Application
    Filed: October 23, 2012
    Publication date: December 4, 2014
    Applicant: GlaxoSmithkline Intellectual Property (No.2) Limited
    Inventors: Thomas Francis Hendrickson, Koc-Kan Ho, Michael David Saunders, Brian John Stevens, Krzysztof Swierczek, Kevin Bret Wright
  • Patent number: 8877731
    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. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: November 4, 2014
    Assignee: Alios Biopharma, Inc.
    Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
  • Patent number: 8871981
    Abstract: A method for oxidizing an alcohol, wherein oxidation is performed in the presence of a compound represented by the following formula (I) and a bulk oxidant, which enables efficient oxidation of secondary alcohols as well as primary alcohols, and can attain high reaction efficiency even when air is used as a bulk oxidant.
    Type: Grant
    Filed: May 30, 2011
    Date of Patent: October 28, 2014
    Assignee: Tohoku University
    Inventors: Yoshiharu Iwabuchi, Masaki Hayashi
  • Patent number: 8846636
    Abstract: The disclosure provides nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moieties with quaternary centers at the 3? position, the pharmaceutical formulations comprising the analogues, and methods of using the analogues and formulations for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: September 30, 2014
    Assignee: LCB Pharma Inc.
    Inventor: Yvan Guindon
  • Publication number: 20140248241
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3?-deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Base1 and Base2 are as provided herein.
    Type: Application
    Filed: March 3, 2014
    Publication date: September 4, 2014
    Inventors: Alistair James STEWART, Adel M. MOUSSA, Benjamin Alexander MAYES, Francois-Rene ALEXANDRE, Dominique SURLERAUX, Christophe Claude PARSY, Claire PIERRA, David DUKHAN, Gilles GOSSELIN
  • Patent number: 8809520
    Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 19, 2014
    Assignee: K.U. Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
  • Publication number: 20140194614
    Abstract: A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.
    Type: Application
    Filed: March 15, 2013
    Publication date: July 10, 2014
    Applicant: Santaris Pharma A/S
    Inventors: Signe M. Christensen, Nikolaj Dam Mikkelsen, Miriam Frieden, Henrik Frydenlund Hansen, Troels Koch, Daniel Sejer Pedersen, Christoph Rosenbohm, Charlotte Albaek Thrue, Majken Westergaard
  • Patent number: 8771310
    Abstract: The present invention relates to compositions and methods for improving outcomes in vascular interventional procedures. In particular, the present invention relates to compositions and methods for improving outcomes in vascular interventional procedures using an anti-no-reflow guide wire that attenuates the “no-reflow” phenomenon that is associated with negative outcomes.
    Type: Grant
    Filed: May 28, 2008
    Date of Patent: July 8, 2014
    Assignee: Adenopaint, LLC
    Inventors: Mervyn B. Forman, Edwin K. Jackson, Jianying Zhang, Zaichuan Mi
  • Patent number: 8658616
    Abstract: Compounds having the general formula (I): are provided which have enhanced inhibitory potency and are thus useful in methods of prophylaxis or treatment of a viral infection such as hepatitis C virus. The compounds are phosphoramidate derivatives of nucleoside compounds derived from bases such as adenine and guanine. The glycoside moiety of the nucleoside compound can be substituted at the ss-2? position with methyl and the phosphoramidate group can be 1-naphthyl linked by —O— to the P atom. These compounds can be administered as pharmaceutical compositions, and methods for their preparation are also provided.
    Type: Grant
    Filed: November 23, 2007
    Date of Patent: February 25, 2014
    Assignees: University College Cardiff Consultants Limited, K.U. Leuven Research and Development
    Inventors: Christopher McGuigan, Plinio Perrone, Johan Neyts
  • Publication number: 20140051848
    Abstract: The present invention relates generally to labeled and unlabeled cleavable terminating groups and methods for DNA sequencing and other types of DNA analysis. More particularly, the invention relates in part to nucleotides and nucleosides with chemically cleavable, photocleavable, enzymatically cleavable, or non-photocleavable groups and methods for their use in DNA sequencing and its application in biomedical research.
    Type: Application
    Filed: June 27, 2013
    Publication date: February 20, 2014
    Inventors: Vladislav A. LITOSH, Megan N. HERSH, Brian P. STUPI, Weidong WU, Michael L. METZKER
  • Publication number: 20140005136
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Application
    Filed: July 30, 2013
    Publication date: January 2, 2014
    Applicant: Ardea Biosciences, Inc.
    Inventors: Barry D. QUART, Jean-Luc GIRARDET, Esmir GUNIC, Li-Tain YEH
  • Publication number: 20130337581
    Abstract: Embodiments are disclosed herein that involve C5-functionalized nucleic acids, which can be used for detecting a target in a nucleic acid. Particular embodiments disclose methods for making these compounds, wherein the compounds can be formed by coupling of an intermediate with a linker. Certain embodiments disclose the use of these compounds for detecting single nucleotide polymorphisms, and for increasing the thermal affinity of nucleic acid complements as compared to unmodified nucleic acid complements. In addition, the disclosed compounds can decrease enzymatic degradation of nucleic acids.
    Type: Application
    Filed: June 19, 2013
    Publication date: December 19, 2013
    Applicant: University of Idaho
    Inventors: Patrick Jerzy Hrdlicka, Pawan Kumar, Michael E. Østergaard
  • Publication number: 20130309188
    Abstract: The present invention has an object to provide an external dermal agent with a sustainable anti-wrinkle action, which has both the action of enhancing the proliferation and differentiation of keratinocytes in the skin and the action of enhancing the collagen production in the skin, and which assists the maintenance and the improvement of tissue structures and physiological functions of the epidermis and the dermis, whereby providing a remarkable skin improvement effect. The present invention solves the above abject by providing an external dermal agent containing ?-D-glucopyranosyl-(1?3?)-adenosine and/or ?-D-glucopyranosyl-(1?5?)-adenosine as an effective ingredient(s).
    Type: Application
    Filed: January 31, 2012
    Publication date: November 21, 2013
    Applicant: HAYASHIBARA CO., LTD.
    Inventors: Tatsuya Ishihara, Shimpei Ushio, Rohko Yamamoto, Takanori Ohkura, Shigeharu Fukuda
  • Patent number: 8580762
    Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: December 2, 2011
    Date of Patent: November 12, 2013
    Assignee: Epizyme, Inc.
    Inventors: Edward James Olhava, Richard Chesworth, Kevin Wayne Kuntz, Victoria M. Richon, Roy Macfarlane Pollock, Scott Richard Daigle
  • Patent number: 8580949
    Abstract: The disclosure concerns the enzymatic synthesis of stable analogues of nicotinamide adenine dinucleotide NAD/NADH and nicotinamide adenine dinucleotide phosphate NADP/NADPH, the so-called “carba-NADs”, i.e. analogues of NAD/NADH or NADP/NADPH, respectively, comprising a carbacyclic sugar instead of ribose.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: November 12, 2013
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Hartmut Duefel, Dieter Heindl, Carina Horn, Thomas Meier, Rainer Schmuck
  • Patent number: 8575331
    Abstract: An improved method of preparing a sugar modified nucleoside analog includes a protocol in which a hydroxy group of a sugar is selectively deprotected and oxidized prior to nucleophilic modification of the corresponding carbonyl group. The modified sugar is then coupled to a heterocyclic base that is modified with a dual nucleophilic reagent in a further step that provides N6-modified adenosine analogs with high stereoselectivity.
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: November 5, 2013
    Assignee: Valeant Pharmaceuticals North America
    Inventors: Haoyun An, Kanda Ramasamy, Stephanie Shaw
  • Publication number: 20130261073
    Abstract: The present invention provides a novel compound capable of inhibiting cardiac adenylyl cyclase. The present invention relates to a compound represented by the following formula (I) or a pharmaceutically acceptable salt, ester or solvate thereof: where R1, R2 and R3 each independently represent a hydrogen atom or an acyl group having an acidic or basic substituent, provided that all of R1, R2 and R3 are not simultaneously a hydrogen atom. The present invention also provides a modulator of adenylyl cyclase activity, a pharmaceutical composition and a food composition, all of which comprise the above-described compound or a pharmaceutically acceptable salt, ester or solvate thereof.
    Type: Application
    Filed: October 20, 2011
    Publication date: October 3, 2013
    Applicants: National Univeristy Corporation Yokohama National University, Public University Corporation Yokohama City University
    Inventors: Yoshihiro Ishikawa, Satoshi Okumura, Yujiro Hoshino, Seiichi Inoue
  • Publication number: 20130237491
    Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: April 12, 2013
    Publication date: September 12, 2013
    Applicant: Roche Palo Alto LLC
    Inventors: Rene Robert Devos, Christopher John Hobbs, Wen-Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
  • Patent number: 8513214
    Abstract: The invention provides for novel 2-Deoxyadenosine compounds, which can treat HIV infection at low cytotoxicity values. Substitution at the 4?-position provided compounds which demonstrated low cytotoxicity values in an ATP-based cytotoxicity assay.
    Type: Grant
    Filed: November 10, 2008
    Date of Patent: August 20, 2013
    Assignee: The United States of America as Represented by the Secretary of the Dept. of Health and Human Services
    Inventors: Bao-Han C. Vu, Maqbool A. Siddiqui, Victor E. Marquez, Stephen H. Hughes, Paul L. Boyer
  • Publication number: 20130172543
    Abstract: A method for oxidizing an alcohol, wherein oxidation is performed in the presence of a compound represented by the following formula (I) and a bulk oxidant, which enables efficient oxidation of secondary alcohols as well as primary alcohols, and can attain high reaction efficiency even when air is used as a bulk oxidant.
    Type: Application
    Filed: May 30, 2011
    Publication date: July 4, 2013
    Applicant: TOHOKU UNIVERSITY
    Inventors: Yoshiharu Iwabuchi, Masaki Hayashi
  • Publication number: 20130165399
    Abstract: The present invention has an object to provide an effective and safe therapeutic agent for inflammatory diseases such as sepsis, hepatitis, and inflammatory bowel disease, and solves the above object by providing a therapeutic agent for inflammatory diseases containing adenosine N1-oxide or a derivative thereof as an effective ingredient.
    Type: Application
    Filed: June 16, 2011
    Publication date: June 27, 2013
    Applicant: HAYASHIBARA CO., LTD.
    Inventors: Keizo Kohno, Emiko Ohashi, Hajime Kusano, Shigeharu Fukuda, Tatsuya Ishihara
  • Patent number: 8461128
    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: April 14, 2006
    Date of Patent: June 11, 2013
    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
  • Patent number: 8461124
    Abstract: Conformationally locked 2?,4?-carbocylic nucleosides with improved thermal and nuclease stability are disclosed. Oligonucleotides incorporating the locked nucleosides, and methods of treating disease states, are also disclosed.
    Type: Grant
    Filed: March 11, 2008
    Date of Patent: June 11, 2013
    Inventor: Jyoti Chattopadhyaya
  • Publication number: 20130131006
    Abstract: The present invention relates to a method for inhibiting the induction of cell death by inhibiting the synthesis or secretion of AGE-albumin in cells of the mononuclear phagocyte system, to an AGE-albumin synthesis inhibitor, and to a pharmaceutical composition comprising the AGE-albumin synthesis inhibitor for preventing or treating degenerative disease and autoimmune disease. The AGE-albumin of the present invention is synthesized and secreted in human microglia or human macrophages in an Alzheimer's model, stroke model, Parkinson's disease model and rheumatoid arthritis model. The AGE-albumin synthesis and secretion are caused by oxidative stress. The expression of RAGE increases in first-order human neurons or cartilage cells to which AGE-albumin is administered, whereupon a MAPK signaling pathway is activated and the expression of Bax increases to induce an increase in calcium in mitochondria, thus finally inducing cell death.
    Type: Application
    Filed: April 28, 2011
    Publication date: May 23, 2013
    Applicant: Gachon University of Industry-Academic Cooperation Foundation
    Inventors: Bong Hee Lee, Kyung Hee Byun
  • 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
  • Publication number: 20130078217
    Abstract: The present invention relates to 2?-chloroacetylenyl-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.
    Type: Application
    Filed: September 21, 2012
    Publication date: March 28, 2013
    Inventors: Guoqiang Wang, In Jong Kim, Yat Sun Or
  • Publication number: 20130052710
    Abstract: An RNA of the present invention is an RNA containing a 5? cap structure and a coding region having a 5? initiation codon and a 3? stop codon on both ends of the coding region, the RNA having a nucleoside compound introduced at a site selected from among the 5? cap structure and 10 bases from a 5? end of the RNA, wherein the nucleoside compound is such that a group is attached to (i) a carbon atom at position 8 of a purine nucleus or (ii) a carbon atom at position 5 or 6 of a pyrimidine nucleus, the group being represented by formula (I): A-X?X-#??(I) where A represents an aryl group or a heteroaryl group, # represents a site where the group represented by the formula (I) is attached to the carbon atom at the position 8 of the purine nucleus or the carbon atom at the position 5 or 6 of the pyrimidine nucleus, and two Xs, which are identical to or different from each other, each represents a nitrogen atom or CH whose H may be substituted by alkyl.
    Type: Application
    Filed: February 18, 2011
    Publication date: February 28, 2013
    Applicant: RIKEN
    Inventors: Shinji Ogasawara, Mizuo Maeda
  • Publication number: 20130045475
    Abstract: This disclosure provides novel reversibly terminated ribonucleotides which can be used as a reagent for DNA sequencing reactions. Methods of sequencing nucleic acids using the disclosed nucleotides are also provided.
    Type: Application
    Filed: October 23, 2012
    Publication date: February 21, 2013
    Applicant: ALERE SAN DIEGO, INC.
    Inventor: Alere San Diego, Inc.
  • Publication number: 20130045942
    Abstract: The present invention provides N6-substituted adenosine derivatives and N6-substituted adenine derivatives, manufacturing methods thereof, a pharmaceutical composition comprising the said compounds above, and uses of these compounds in manufacturing medicaments and health-care products for treating insomnia, convulsion, epilepsy, and Parkinson's diseases, and preventing and treating dementia.
    Type: Application
    Filed: December 10, 2009
    Publication date: February 21, 2013
    Applicant: INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Jiangong Shi, Jianjun Zhang, Zhenggang Yue, Min Li, Chenggen Zhu, Ying Zhang, Jiachen Zi, Yafang Wang, Xiaona Fan, Ruiming Xu, Sheng Lin, Yan Li, Yongchun Yang, Li Sheng
  • Publication number: 20130017171
    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: Application
    Filed: September 20, 2012
    Publication date: January 17, 2013
    Applicants: UNIVERSITA DEGLI STUDI DI CAGLIARI, IDENIX PHARMACEUTICALS, INC.
    Inventors: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari
  • Patent number: 8334364
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose. [Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: December 18, 2012
    Assignee: Nipon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Publication number: 20120309705
    Abstract: The present invention includes novel 3?-deoxy-3?-methylidene-?-L-nucleosides, pharmaceutical composition comprising such compounds, as well as the methods to treat or to prevent viral infections and in particular HBV and/or HIV infections.
    Type: Application
    Filed: December 14, 2010
    Publication date: December 6, 2012
    Applicant: NOVADEX PHARMACEUTICALS AB
    Inventors: Xiao Xiong Zhou, Staffan Torssell, Olov Wallner, Piaoyang Sun
  • Publication number: 20120295863
    Abstract: The present invention provides therapeutic agents for preventing and treating neurodegenerative diseases. These agents synergistically target both the adenosine A2A receptor (A2AR) and the equilibrative nucleoside transporter 1 (ENT1).
    Type: Application
    Filed: November 12, 2010
    Publication date: November 22, 2012
    Inventors: Yun-Lian Lin, Yijuang Chern, Jim-Min Fang, Jung-Hsing Lin, Nai-Kuei Huang
  • 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: 20120245335
    Abstract: The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2?R)-2?-deoxy-2?-fluoro-2?-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: GILEAD PHARMASSET LLC
    Inventor: Jeremy Clark
  • Publication number: 20120237480
    Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.
    Type: Application
    Filed: March 16, 2012
    Publication date: September 20, 2012
    Inventors: YAT SUN OR, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
  • Publication number: 20120232029
    Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
    Type: Application
    Filed: December 13, 2011
    Publication date: September 13, 2012
    Applicant: Pharmasset, Inc.
    Inventors: MICHAEL JOSEPH SOFIA, Jinfa Du
  • Patent number: 8263762
    Abstract: Provided herein are alkoxy-carbonyl-amino-alkynyl-adenosine compounds and derivatives thereof 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: June 30, 2010
    Date of Patent: September 11, 2012
    Assignee: Dogwood Pharmaceuticals, Inc.
    Inventors: Anthony R. Beauglehole, Frank W. Schmidtmann, Jayson M. Rieger, Robert Thompson
  • Publication number: 20120220546
    Abstract: 5?-methylthioadenosine (MTA) is described as a compound that is susceptible to inhibiting and/or blocking the epithelial-mesenchymal transition (EMT), a process whereby epithelial cells become mesenchymal cells. The periodical intake of MTA [every 24 h for 21 days] significantly improves fibrosis and the markers for hepatic cellular damage in KO-Mdr2 mice with MTA (28 mg/kg). Following the daily oral administration of MTA, both the expression of EMT markers in the total liver and appreciable signs of fibrosis are significantly reduced, indicating the beneficial effect of MTA on the liver affected by the lack of Mdr2. MTA is proposed to be a safe drug, suitable for oral formulation and without secondary effects, to be used in the prevention and/or treatment of diseases associated with EMT, including chronic cholestatic diseases, fibrosis and cholangiocarcinoma.
    Type: Application
    Filed: May 3, 2012
    Publication date: August 30, 2012
    Inventors: Matías Antonio Avila Zaragoza, Jesús Maria Bañales Asurmendi, Maria Carmen Berasain Lasarte, Fernando José Corrales Izquierdo, MarÍa del Carmen Gil Puig, María Ujue Latasa Sada, Jon Lecanda Cordero, Jesús Maria Prieto Valtueña, Carlos Manuel Rodríguez Ortigosa
  • 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: 8222229
    Abstract: A peritoneal dialysate containing adenosine triphosphate or a salt thereof, and a peritoneal dialysis method using the dialysate. The peritoneal dialysate is safe and causes less peritoneal injuries even when employed in peritoneal dialysis over a long period of time.
    Type: Grant
    Filed: November 20, 2003
    Date of Patent: July 17, 2012
    Assignee: Kowa Co., Ltd.
    Inventors: Kei Kiribayashi, Noriaki Yorioka
  • Patent number: RE44779
    Abstract: An oligo- or polynucleotide analogue having one or more structures of the general formula where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is disclosed. The use of this analogue provides an oligonucleotide analogue antisense molecule, which is minimally hydrolyzable with an enzyme in vivo, has a high sense strand binding ability, and is easily synthesized.
    Type: Grant
    Filed: June 26, 2012
    Date of Patent: February 25, 2014
    Assignees: Santaris Pharma A/S, Exiqon A/S
    Inventors: Takeshi Imanishi, Satoshi Obika