The Five-membered N-hetero Ring Is 1,3-diazole, Which May Be Hydrogenated (e.g., 6-chloropurine Nucleoside, Nebularin, Etc.) Patents (Class 536/27.21)
  • Publication number: 20150080564
    Abstract: Synthesis and uses of conformationally restricted nucleomonomers (CRN) to prepare nucleic acid compounds. Methods for preparing nucleomonomers for nucleic acid compounds in high yields and in multi-gram scale for therapeutic modalities useful for treating or preventing diseases or disorders by up- or down-regulating the expression of genes and other nucleic acid based regulatory systems in a cell.
    Type: Application
    Filed: September 7, 2012
    Publication date: March 19, 2015
    Applicant: Marina Biotech, Inc.
    Inventors: Tracy J. Matray, Iwona M. Maciagiewicz, Michael E. Houston, JR.
  • Patent number: 8969545
    Abstract: Alkynyl-derivatized cap analogs, alkynyl-modified capped RNA, 1,4-disubstituted triazole-derivatized capped RNA, methods of preparation, methods of isolation, and uses thereof are provided. The “click” modification facilitates detection and isolation of capped RNAs and the 1,4-disubstituted triazole derivatives formed by the “click” reaction are useful for producing RNA transcripts and encoded protein.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: March 3, 2015
    Assignee: Life Technologies Corporation
    Inventors: Anilkumar R. Kore, Shanmugasundaram Muthian, Kyle Gee
  • 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: 20140286903
    Abstract: This invention is directed to compounds of Formula (I) having the structure that are useful in the treatment of viral infections in mammals, particularly in humans, mediated, at least in part, by a virus in the Flaviviridae family of viruses.
    Type: Application
    Filed: November 8, 2012
    Publication date: September 25, 2014
    Applicants: INHIBITEX, INC., UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
    Inventors: Stanley Chamberlain, John Vernachio, Srinivas K. Battina, Changalvala V.S. Ramamurty, C. Srinivas Rao, Chris McGuigan, Andrea Brancale
  • Publication number: 20140113282
    Abstract: Nucleosides and nucleotides are disclosed that are linked to detectable labels via a cleavable linker group.
    Type: Application
    Filed: December 2, 2013
    Publication date: April 24, 2014
    Applicant: ILLUMINA CAMBRIDGE LIMITED
    Inventors: SHANKAR BALASUBRAMANIAN, COLIN BARNES, XIAOHAI LIU
  • Patent number: 8686130
    Abstract: The present invention relates to novel unnatural fluorescent nucleic acid bases, that is, a purine base, a 1-deazapurine base, and a 1,7-deazapurine base each having a functional group which consists of two or more heterocyclic moieties linked together, at the 6-position thereof (the 6-position of purine ring). The present invention also relates to a compound containing the unnatural base, a derivative thereof, and a nucleic acid containing a nucleotide having the unnatural base. The present invention also relates to a method of preparing the nucleic acid. The unnatural base of the present invention has excellent fluorescence characteristics and also has excellent properties as a universal base.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: April 1, 2014
    Assignees: Riken, Tagcyx Biotechnologies
    Inventors: Ichiro Hirao, Michiko Hirao, Shigeyuki Yokoyama, Tsuneo Mitsui
  • 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
  • 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
  • Publication number: 20130130922
    Abstract: A method for labeling unmethylated CpG dinucleotides within a DNA fragment, and use of the method in profiling of genomic DNA methylation. The present invention further provides modified DNA methyltransferase enzymes and compounds which are capable of being used by the enzymes as cofactors for use in the labeling method.
    Type: Application
    Filed: November 16, 2012
    Publication date: May 23, 2013
    Applicants: Centre for Addiction and Mental Health, Vilnius University
    Inventors: Vilnius University, Centre for Addiction and Mental Health
  • 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: 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
  • Publication number: 20130018010
    Abstract: The present invention relates to polymeric conjugates of adenine nucleoside analogs. In particular, the invention relates to multi-arm polyethylene glycol conjugates of adenine nucleoside analogs and use thereof. The present invention, more specifically, provides polymeric conjugates of toyocamycin and its derivatives. Furthermore, the present invention provides a method for preparing the polymeric conjugates of adenine nucleoside analogs and a method of using the same for treating a cancer, inhibiting the growth or proliferation of cancer cells, treating a viral infection, treating a disease or condition associated with abnormal expression of VEGF. Most polymeric conjugates of toyocamycin was stable in PBS but released toyocamycin in vivo to provided inhibition of cancer cell growth.
    Type: Application
    Filed: April 15, 2011
    Publication date: January 17, 2013
    Applicant: ENZON PHARMACEUTICALS, INC.
    Inventors: Hong Zhao, Jing Xia
  • Publication number: 20120295862
    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: March 9, 2012
    Publication date: November 22, 2012
    Inventors: Patrick J. Hrdlicka, Pawan Kumar, Michael E. Østergaard
  • Publication number: 20120264706
    Abstract: The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's rate of metabolism, protecting an animal's heart against myocardial damage during cardioplegia; or for treating or preventing a cardiovascular disease, a neurological disorder, an ischemic condition, a reperfusion injury, obesity, a wasting disease, or diabetes, comprising administering an effective amount of a Purine Derivative to an animal in need thereof.
    Type: Application
    Filed: April 20, 2012
    Publication date: October 18, 2012
    Applicant: INOTEK PHARMACEUTICALS CORPORATION
    Inventors: Prakash JAGTAP, Csaba SZABO, Andrew L. SALZMAN
  • Patent number: 8288526
    Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 16, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takayoshi Torii, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
  • Publication number: 20120245340
    Abstract: The present invention relates to novel unnatural fluorescent nucleic acid bases, that is, a purine base, a 1-deazapurine base, and a 1,7-deazapurine base each having a functional group which consists of two or more heterocyclic moieties linked together, at the 6-position thereof (the 6-position of purine ring). The present invention also relates to a compound containing the unnatural base, a derivative thereof, and a nucleic acid containing a nucleotide having the unnatural base. The present invention also relates to a method of preparing the nucleic acid. The unnatural base of the present invention has excellent fluorescence characteristics and also has excellent properties as a universal base.
    Type: Application
    Filed: October 6, 2010
    Publication date: September 27, 2012
    Applicants: TAGCYX Biotechnologies, Riken
    Inventors: Ichiro Hirao, Michiko Hirao, Shigeyuki Yokoyama, Tsuneo Mitsui
  • 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: 20120238520
    Abstract: The present invention relates to a compound which is (2R,3R,4S,5R)-2-(6-amino-2-{[(1S)-2-hydroxy-1-(phenylmethyl)ethyl]amino}-9H-purin-9-yl)-5-(2-ethyl-2H-tetrazol-5-yl)tetrahydro-3,4-furandiol or a pharmaceutically acceptable salt thereof for use in the treatment or prevention of inflammatory and non-inflammatory diseases abd conditions associated with alveolar filling.
    Type: Application
    Filed: December 3, 2010
    Publication date: September 20, 2012
    Inventor: David Lipson
  • Patent number: 8258115
    Abstract: The present invention refers to new salts of S-adenosyknethionine (SAMe) with improved stability and containing at least 70% by weight of SAMe.
    Type: Grant
    Filed: October 22, 2007
    Date of Patent: September 4, 2012
    Assignee: Gnosis SpA
    Inventors: Ermanno Valoti, Daniele Giovannone, Marco Berna
  • Patent number: 8252920
    Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: August 28, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takayoshi Torii, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
  • Publication number: 20120142626
    Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.
    Type: Application
    Filed: November 30, 2011
    Publication date: June 7, 2012
    Applicant: Pharmasset, Inc.
    Inventors: JINFA DU, Michael Joseph Sofia
  • Patent number: 8188055
    Abstract: Disclosed are compounds that are AGT inactivators that include a folate residue, e.g., a compound of formula (I), wherein X1, X2, R1, and R2 are as described herein. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells and inactivating AGT in a tumor cell. The methods comprise, inter alia, administering a compound or pharmaceutically acceptable salt of formula (I).
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: May 29, 2012
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, The Penn State Research Foundation
    Inventors: Robert C. Moschel, Matthew Karl Moschel, legal representative, Anthony E. Pegg, Sahar Javanmard, Natalia Loktionova, Gary Pauly
  • Patent number: 8173797
    Abstract: The present invention is directed to new therapeutic compounds isolated from spider venom and methods of using these new compounds. The compounds are sulfated nucleoside derivatives including ribonucleoside mono- and disulfates derived from guanine, adenosine, and cytidine. Some of these compounds are glycosylated or fucosylated bearing one or more sugar residues.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: May 8, 2012
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Jerrold Meinwald, Andrew Edmund Taggi, Frank Clemens Schroeder
  • Patent number: 8168766
    Abstract: A compound of formula (A) or salt thereof: wherein each of R1, R2, and R3 independently represents hydrogen, alkyl, aryl, acyl, sulfonyl, or silyl; P represents hydrogen or a hydroxy protective group. This compound may be used an intermediate for making a 2-deoxy-2,2-difluoro-D-ribofuranosyl nucleosides, such as gemcitabine.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: May 1, 2012
    Assignee: ScnioPharm Taiwan Ltd.
    Inventors: Julian Paul Henschke, Yung Fa Chen, George Charles Schloemer
  • Patent number: 8153781
    Abstract: Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A1 adenosine receptor agonist having a purine nucleoside moiety and a functional group at the N6 position of the purine nucleoside moiety, wherein the functional group has the formula (I): N6H—Ar1—CH2—C(?O)NH—R1 (I), wherein Ar1 and R1 as defined herein. Also disclosed are pharmaceutical compositions, methods of treating various diseases, and a diagnostic method employing such conjugates.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: April 10, 2012
    Assignees: The United States of America as represented by the Secretary, Department of Health and Human Services, Inserm
    Inventors: Kenneth A. Jacobson, Yoonkyung Kim, Athena Klutz, Beatrice Hechler, Christian Gachet
  • Publication number: 20120071646
    Abstract: There is a demand for a convenient production method of an NC type purine nucleoside. The present invention relates to a method of producing a purine nucleoside represented the formula (I?) or a salt thereof, which comprising reacting a pyrimidine nucleoside represented by the formula (I) or a salt thereof with a purine nucleobase represented by the formula B?H in the presence of a Lewis acid.
    Type: Application
    Filed: March 30, 2010
    Publication date: March 22, 2012
    Inventors: Tadashi Umemoto, Yoji Hayase, Shumpei Murata, Kenichi Miyata
  • Publication number: 20120040345
    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: August 10, 2011
    Publication date: February 16, 2012
    Applicant: ALERE SAN DIEGO, INC.
    Inventors: Olaf Piepenburg, Derek L. Stemple, Niall A. Armes
  • Patent number: 8114986
    Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: February 14, 2012
    Assignee: Giuliani International Limited
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Patent number: 8076310
    Abstract: Disclosed herein are novel phosphonate nucleosides and thiophosphonate nucleosides comprising a phosphonalkoxy-substituted or phosphonothioalkyl-substituted five-membered, saturated or unsaturated, oxygen-containing or sulfur-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.
    Type: Grant
    Filed: March 4, 2005
    Date of Patent: December 13, 2011
    Assignee: K.U.Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clerq
  • Publication number: 20110293719
    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: June 30, 2011
    Publication date: December 1, 2011
    Applicant: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Jean-Luc Girardet, Esmir Gunic, Li-Tain Yeh
  • Publication number: 20110257120
    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: Application
    Filed: June 27, 2011
    Publication date: October 20, 2011
    Applicants: Idenix Pharmaceuticals, Inc., L'Universite Montpellier II, Centre National de la Recherche Scientifique
    Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
  • Publication number: 20110250699
    Abstract: The present teachings generally relate to fluorescent dyes, linkable forms of fluorescent dyes, energy transfer dyes, reagents labeled with fluorescent dyes and uses thereof.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 13, 2011
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Ronald J. Graham, Ruiming Zou, Krishna G. Upadhya, Scott C. Benson
  • Publication number: 20110195922
    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: Application
    Filed: December 8, 2009
    Publication date: August 11, 2011
    Applicants: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier II
    Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
  • Patent number: 7982030
    Abstract: The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids and methods for their synthesis. Selenium derivatives of both ribonucleic acids and deoxyribonucleic acids, as well as methods for their synthesis, crystallization and uses in structural determinations, particularly by X-ray crystallographic techniques are disclosed. The selenium derivatives of the present invention are also useful as food supplements.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: July 19, 2011
    Assignee: Georgia State University Research Foundation, Inc.
    Inventor: Zhen Huang
  • Publication number: 20110087015
    Abstract: The object of the present invention is to provide a nucleoside or a nucleotide, or a derivative thereof, which has an unnatural base. The nucleoside and others of the present invention are characterized by having a 2-amino-6-(2-thiazolyl)purin-9-yl group or a 2-amino-6-(2-oxazolyl)purin-9-yl group as a base, wherein the 4- and/or 5-position of the thiazolyl or oxazolyl group may be substituted.
    Type: Application
    Filed: September 10, 2004
    Publication date: April 14, 2011
    Applicant: RIKEN
    Inventors: Ichiro Hirano, Shigeyuki Yokoyama
  • Patent number: 7915232
    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 which inhibit HCV polymerase and are useful for treating a patient suffering from a HCV infection and to pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: March 29, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Rene Robert Devos, Christopher John Hobbs, Wen Rong Jiang, Nobuo Shimma, Takuo Tsukuda
  • Publication number: 20110053154
    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: June 21, 2010
    Publication date: March 3, 2011
    Applicant: TwistDx, Inc.
    Inventors: Olaf Piepenburg, Derek L. Stemple, Niall A. Armes
  • Patent number: 7897759
    Abstract: Disclosed are structurally modified, metabolically stable nucleosides having antitumor activity wherein the formation of toxic metabolites is blocked and antimicrobial activity. The disclosure further relates to pharmaceutical compositions comprising one or more disclosed modified nucleosides and to methods of use thereof.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: March 1, 2011
    Assignee: MUSC Foundation for Research Development
    Inventors: Giuseppe Gumina, Roger L. White
  • Publication number: 20100323980
    Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).
    Type: Application
    Filed: July 24, 2006
    Publication date: December 23, 2010
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Publication number: 20100316704
    Abstract: The subject invention concerns platinum complexes that exhibit antitumor cell and/or antiparasitic activity. The subject invention also concerns the use of platinum complexes of the invention to treat oncological and inflammatory disorders. The platinum complexes of the invention can also be used to treat or prevent infection by a virus or a bacterial or parasitic organism in vivo or in vitro.
    Type: Application
    Filed: July 13, 2010
    Publication date: December 16, 2010
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: HEIDI KAY, JAY W. PALMER, JOSEPH A. STANKO
  • Patent number: 7816513
    Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
    Type: Grant
    Filed: December 16, 2005
    Date of Patent: October 19, 2010
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takayoshi Torii, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
  • Patent number: 7816333
    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 27, 2007
    Date of Patent: October 19, 2010
    Assignees: Daiichi Sankyo Company, Limited, Mitsubishi-Kagaku Foods Corporation
    Inventors: Masakatsu Kaneko, Koji Morita, Takeshi Imanishi
  • Publication number: 20100249053
    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: Application
    Filed: October 22, 2008
    Publication date: September 30, 2010
    Applicant: Can-Fite Biopharma Ltd.
    Inventors: Pnina Fishman, Shira Cohen
  • Patent number: 7799908
    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: January 15, 2004
    Date of Patent: September 21, 2010
    Assignee: Valeant Pharmaceuticals North America
    Inventors: Haoyun An, Kanda Ramasamy, Stephanie Shaw
  • Patent number: 7795236
    Abstract: The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.
    Type: Grant
    Filed: March 13, 2007
    Date of Patent: September 14, 2010
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Yoshinori Nonaka, Norihiko Kikuchi
  • Publication number: 20100190972
    Abstract: The present invention relates to stable anti-parallel heteropolynucleotide duplexes, comprising a plurality of complementary purine-purine nucleobase dyads, wherein the nucleobase is coupled to a pentose sugar backbone. The present invention further relates to methods of hybridizing two heteropolynucleotide molecules to form such purine-purine nucleobase dyads, as well as kits and solid supports comprising such purine-purine nucleobase dyads.
    Type: Application
    Filed: December 21, 2007
    Publication date: July 29, 2010
    Applicant: SIEMENS HEALTHCARE DIAGNOSTICS INC.
    Inventors: Thomas Battersby, Maria Albalos, Michel Friesenhahn, Edward Brooks
  • Publication number: 20100179312
    Abstract: The present invention is directed to convertible nucleosides and polymer supported convertible nucleosides for use in SNAP displacement reactions. The convertible nucleosides can be used to synthesize numerous substituted purine and pyrimidine derivatives.
    Type: Application
    Filed: October 12, 2007
    Publication date: July 15, 2010
    Inventors: Mahesh K. Lakshman, Suyeal Bae
  • Publication number: 20100166780
    Abstract: The invention relates to oligonucleotides including at least one lipophilic substituted nucleotide analog and a pyrimidine-purine dinucleotide. The invention also relates to pharmaceutical compositions and methods of use thereof.
    Type: Application
    Filed: September 27, 2007
    Publication date: July 1, 2010
    Inventors: Harald Debelak, Eugen Uhlmann, Marion Jurk
  • Publication number: 20100152126
    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: Application
    Filed: December 8, 2009
    Publication date: June 17, 2010
    Applicants: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier II
    Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant