Alkyl, Or Substituted Alkyl, Bonded Directly To The 5-position Of The Diazine Ring (e.g., Thymidine, 5-methyl Uridine, Etc.) Patents (Class 536/28.54)
  • Patent number: 10626083
    Abstract: A method of manufacturing 2-(1-{6-[(2-[F-18]fluoroethyl)(methyl)amino]-2-naphthyl}ethylidene)-malononitrile ([F-18]FDDNP) utilizes a semi-automated module that is used to perform fluorination, pre-purification, separation, product extraction, and formulation. The method is able to produce [F-18]FDDNP with high yields and ready for human administration under existing FDA regulations, and without the need for hazardous organic solvents such as dichloromethane (DCM), methanol (MeOH), and tetrahydrofuran (THF). The method also improves the speed with which [F-18]FDDNP can be synthesized with the method being able to generate a final product within about 90 to 100 minutes. This synthesis method is easily adaptable to FDA registered and approved automated synthesis systems.
    Type: Grant
    Filed: June 28, 2019
    Date of Patent: April 21, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Nagichettiar Satyamurthy, Jie Liu, Jorge R. Barrio
  • Patent number: 10027048
    Abstract: An electrical component includes a connection portion that is to be in contact with other electrical component and is to establish an electrical connection with the other electrical component. The connection portion includes a plating film that defines a surface of the connection portion. The plating film includes a metal as a main constituent and an aromatic compound that is dispersed in the plating film. The aromatic compound has pi-acceptability and causes ligand field splitting equal to or greater than that of 2,2?-bipyridyl in spectrochemical series. A content of the aromatic compound in the plating film is equal to or greater than 0.1 weight percent, in terms of carbon atoms, with respect to the metal of the plating film.
    Type: Grant
    Filed: June 8, 2017
    Date of Patent: July 17, 2018
    Assignee: DENSO CORPORATION
    Inventor: Kenji Ochi
  • Patent number: 9212174
    Abstract: The invention provides a process for producing a ?-dihydrofuran derivative represented by formula (1) or a ?-tetrahydrofuran derivative represented by formula (4), characterized in that the process includes causing a dialkyl dicarbonate, a diaralkyl dicarbonate, or a halide to act on a diol compound represented by formula (2) or (3). The invention also provides a process for producing 4?-ethynyl-2?,3?-didehydro-3?-deoxythymidine or an analog thereof, the process including glycosylation and deprotection.
    Type: Grant
    Filed: February 7, 2011
    Date of Patent: December 15, 2015
    Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Yusuke Iriyama, Tsutomu Higashiyama
  • Publication number: 20150141637
    Abstract: The present invention provides novel tricyclic nucleosides and oligomeric compounds prepared therefrom. Incorporation of one or more of the tricyclic nucleosides into an oligomeric compound is expected to enhance one or more properties of the oligomeric compound. Such oligomeric compounds can also be included in double stranded compositions. 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: Application
    Filed: March 15, 2013
    Publication date: May 21, 2015
    Applicant: UNIVERSITÄT BERN
    Inventors: Christian Leumann, Branislav Dugovic, Jory Liétard
  • Publication number: 20150112055
    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: Application
    Filed: March 20, 2013
    Publication date: April 23, 2015
    Applicant: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze, Stephen Hanessian, Benjamin R. Schroeder, Robert D. Giacometti, Bradley L. Merner
  • Publication number: 20150076062
    Abstract: The present invention relates to the use of a supramolecular system in order to remove particles from a liquid medium containing same. According to the invention, the supramolecular system includes at least one molecule having a low molecular weight and/or an organic compound from living organisms, preferably from jellyfish, said compound being selected from among collagen, a polysaccharide, a proteoglycan or a mixture of two of said organic compounds, and said molecule having a low molecular weight and formula (I) as defined herein. The invention also relates to a method for removing particles from a liquid medium containing same. The invention is particularly suitable for use in water decontamination and biotechnology.
    Type: Application
    Filed: January 25, 2013
    Publication date: March 19, 2015
    Inventors: Philippe Barthelemy, Alain Thiery, Amit Patwa
  • 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.
  • 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
  • Patent number: 8916538
    Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: December 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
  • Patent number: 8912319
    Abstract: The present invention relates to methods of synthesizing 18F-FMAU. In particular, 18F-FMAU is synthesized using one-pot reaction conditions in the presence of Friedel-Crafts catalysts. The one-pot reaction conditions are incorporated into a fully automated cGMP-compliant radiosynthesis module, which results in a reduction in synthesis time and simplifies reaction conditions. The one-pot reaction conditions are also suitable for the production of 5-substituted thymidine or cytidine analogs. The products from the one-pot reaction (e.g. the labeled thymidine or cytidine analogs) can be used as probes for imaging tumor proliferative activity. More specifically, these [18F]-labeled thymidine or cytidine analogs can be used as a PET tracer for certain medical conditions, including, but not limited to, cancer disease, autoimmunity inflammation, and bone marrow transplant.
    Type: Grant
    Filed: July 15, 2011
    Date of Patent: December 16, 2014
    Assignee: University of Southern California
    Inventors: Zibo Li, Hancheng Cai, Peter S. Conti
  • Patent number: 8877734
    Abstract: Provided are novel selenyl-methyluracil compounds and a pharmaceutical composition for enhancing the effect of radiation treatment. The composition contains at least one compound selected from the group consisting of the selenyl-methyluracil compounds or pharmaceutically acceptable salts thereof, as an active ingredient.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: November 4, 2014
    Assignee: Kongju National University Industry-University Cooperation Foundation
    Inventors: In Seok Hong, Sung Hee Hong, Marc M. Greenberg
  • Publication number: 20140221639
    Abstract: A radiolabeled nucleoside analogue is provided, which includes radioactive iodine 123I/131I, and a nucleoside analogue selected from a group consisting of cytidine, thymidine, uridine, and a derivative thereof. A method for preparing the radiolabeled nucleoside analogue, and a use thereof are further provided. The nucleoside analogue, prepared through the preparation method with a short synthesis time and a high radiochemical yield, has a long in vivo physiological half life and a high stability in serum, and, as a radiopharmaceutical composition, is useful in development of tumor proliferation diagnosis or therapy prognosis evaluation, and further assists in observation of long-time in vivo metabolism of a drug.
    Type: Application
    Filed: April 8, 2014
    Publication date: August 7, 2014
    Applicants: Institute of Nuclear Energy Research Atomic Energy Council, Executive Yuan, NATIONAL YANG-MING UNIVERSITY
    Inventors: HSIN-ELL WANG, CHIH-YUAN LIN, WEI-TI KUO, CHUAN-LIN CHEN, MEI-HUI WANG, HUNG-MAN YU, MAO-CHI WENG, YU CHANG, WUU-JYH LIN
  • Patent number: 8779118
    Abstract: Provided herein are novel base modified bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel pyrimidine bicyclic nucleosides are provided wherein each pyrimidine base is substituted at the 5 position with an optionally substituted, aromatic or heteroaromatic ring system comprising from 5 to 7 ring atoms selected from C, N, O and S. In certain embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: July 15, 2014
    Assignee: Isis Pharmaceuticals, Inc.
    Inventors: Charles Allerson, Balkrishen Bhat, Eric E. Swayze
  • 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
  • Publication number: 20140128338
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and 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: November 8, 2013
    Publication date: May 8, 2014
    Applicant: ARDEA BIOSCIENCES, INC.
    Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
  • Patent number: 8691972
    Abstract: Disclosed are compounds of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Also disclosed are methods of preparing compound of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Further disclosed are methods of counducting drug discovery and research comprises applying the compound of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer in an investigation.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: April 8, 2014
    Inventor: Zhen Huang
  • Publication number: 20140058076
    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: Application
    Filed: November 1, 2013
    Publication date: February 27, 2014
    Inventors: John Rohloff, Nebojsa Janjic, Jeffrey D. Carter, Catherine Fowler
  • Patent number: 8658776
    Abstract: Methods for preparation of 2?,3?-dideoxynucleotides support structures, such as 2?,3?-dideoxyguanosine, 2?,3?-dideoxyadenosine, and 3?-deoxythymidine support structures are disclosed. Various methods of using such structures are also provided, such as their use for automated DNA synthesis and pyrophosphorolysis activated polymerization.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: February 25, 2014
    Assignee: Life Technologies Corporation
    Inventors: Zhaochun Ma, Khairuzzaman Bashar Mullah, Robert G. Eason
  • Publication number: 20140051605
    Abstract: The present disclosure relates to photoactivable protecting groups containing a diarylsulfide chromophore, a method for the synthesis thereof and their use as photoactivable protecting groups using maskless photolithography based array synthesis.
    Type: Application
    Filed: October 23, 2013
    Publication date: February 20, 2014
    Applicant: NimbleGen Systems GmbH
    Inventor: Klaus-Peter Stengele
  • Publication number: 20140039074
    Abstract: The invention generally relates to the preparation of 18F-labeled radiopharmaceuticals. In particular, this invention relates to the advanced processes for an efficient eiution of [18F]fluoride trapped in a cartridge filled with quaternary ammonium polymer which comprises inert non-basic and non-nucleophilic counter anions. The said methods and polymer cartridges allow the rapid preparation of suitable [18F]fluoride solution, which is also less basic to reduce the formation of byproducts, finally to increase radiochemical yield and purity of 18F-radiopharmaceuticals.
    Type: Application
    Filed: September 6, 2011
    Publication date: February 6, 2014
    Applicant: PIRAMAL IMAGING SA
    Inventors: Dae Yoon Chi, Byoung Se Lee, Sang Ju Lee, Jin-Sook Ryu, Seung Ju Oh
  • Patent number: 8633308
    Abstract: Described herein are compounds and methods that prevent the viral infection of cells. The compounds and methods described herein minimize viral resistance and maximize the number of targeted viruses. Additionally, the compounds and methods minimize the toxicity toward uninfected cells.
    Type: Grant
    Filed: February 27, 2008
    Date of Patent: January 21, 2014
    Assignee: The Governors of The University of Alberta
    Inventors: Luis M. Schang, Mireilli R. St. Vincent, Alexey V. Ustinov
  • Publication number: 20140011961
    Abstract: The present invention relates to a solid precursor in the form of an organic salt, the solid precursor having a solid support, a method for manufacturing same, and an application thereof. The solid precursor of the present invention enables omission of the [18F]fluoride refining process using additional cartridge, and the use of excessive phase-transfer catalyst, and can easily remove remaining substance after reaction through the solid support inside the precursor. The solid precursor of the present invention is very appropriate for an automated synthesis device as an all-in-one system that can carry out overall process of [18F]fluorosis reaction, when used by charging in a cartridge.
    Type: Application
    Filed: December 13, 2011
    Publication date: January 9, 2014
    Inventors: Dae-Yoon Chi, Byoung-Se Lee, Jae-Hak Lee, So-Young Chu, Woon-Jung Jung, Hye-Rim Kwon
  • 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: 20130324491
    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: March 22, 2013
    Publication date: December 5, 2013
    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: 20130317207
    Abstract: The present invention provides novel fluorescent dyes and kits containing the same, which are useful for labeling a wide variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis and/or treatment of disease conditions.
    Type: Application
    Filed: November 20, 2012
    Publication date: November 28, 2013
    Applicant: PROMEGA CORPORATION
    Inventor: Promega Corporation
  • Publication number: 20130211067
    Abstract: Provided are novel selenyl-methyluracil compounds and a pharmaceutical composition for enhancing the effect of radiation treatment. The composition contains at least one compound selected from the group consisting of the selenyl-methyluracil compounds or pharmaceutically acceptable salts thereof, as an active ingredient.
    Type: Application
    Filed: December 23, 2010
    Publication date: August 15, 2013
    Inventors: In Seok Hong, Sung Hee Hong, Marc M. Greenberg
  • Patent number: 8501931
    Abstract: The present invention is directed to convertible nucleosides and polymer supported convertible nucleosides for use in SNAr displacement reactions. The convertible nucleosides can be used to synthesize numerous substituted purine and pyrimidine derivatives.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: August 6, 2013
    Assignee: Research Foundation of the City University of New York
    Inventors: Mahesh K. Lakshman, Suyeal Bae
  • Patent number: 8445669
    Abstract: The present invention provides a process for producing 2?,3?-didehydro-3?-deoxy-4?-ethynylthymidine, which is useful as a medicine, in an efficient and industrially advantageous manner, and more specifically, provides a process for producing 2?,3?-didehydro-3?-deoxy-4?-ethynylthymidine as shown below. (wherein R1 and R2 independently represent a protective group for a hydroxy group, or R1 and R2 together form a protective group for two hydroxy groups, R3 and R4 independently represent a protective group for a hydroxy group, R5 represents a protective group for a hydroxy group, R6 represents a protective group for a hydroxy group, X represents a leaving group, and Y represents a halogen atom.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: May 21, 2013
    Assignee: Hamari Chemicals, Ltd.
    Inventors: Tatsunori Sato, Tetsuya Kawashima, Toshio Miwa, Kazutoyo Dokei, Chikoto Fujimoto
  • Patent number: 8404830
    Abstract: The present disclosure is directed to the field of nucleic acid chemistry, specifically to 5-position modified uridines, as well as, oligonucleotides comprising said 5-position modified uridines. The present disclosure describes methods for producing aptamers comprising said 5-position modified uridines that are capable of binding to target molecules.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: March 26, 2013
    Assignee: SomaLogic, Inc.
    Inventors: Dominic Zichi, Sheri K. Wilcox, Chris Bock, Daniel J. Schneider, Bruce Eaton, Larry Gold
  • Patent number: 8394584
    Abstract: Provided are methods for detecting, characterizing or separating DNA based on methylation. Heterogeneous DNA populations are separated based on DNA methylation by providing a membrane having a nanopore through which an electric field is applied. DNA of interest is introduced, and for a given threshold voltage across the nanopore, only DNA having a methylation parameter of interest may transit the pore, thereby facilitating detection, characterization, or separation of DNA based on methylation. The methods are optionally used to detect a disease state that is associated with DNA methylation including, but not limited to, cancer.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: March 12, 2013
    Assignees: The Board of Trustees of the University of Illinois, The Johns Hopkins University
    Inventors: Gregory Timp, Winston Timp, Andrew Feinberg, Utkur Mirsaidov
  • Publication number: 20130045949
    Abstract: Described herein are compounds that may be selectively activated to produce active anti-cancer agents in tumor cells. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of treating cancer using the compounds.
    Type: Application
    Filed: July 1, 2012
    Publication date: February 21, 2013
    Applicant: UWM RESEARCH FOUNDATION, INC.
    Inventors: Xiaohua Peng, Yunyan Kuang, Sheng Cao, Wenbing Chen, Yibin Wang
  • Publication number: 20130041104
    Abstract: The invention relates to novel chemical compounds, which can be fluorinated with 18F under especially mild conditions. The novel chemical compounds thereby enable the use of a novel fluorination method according to the invention, wherein the substrate to be fluorinated is immobilized on a polymer during the fluorination. The method is characterized in that the method requires fewer and simpler manipulations than methods of the prior art. The occupational safety in the laboratory or hospital is thereby increased especially during work with the radionuclide 18F.
    Type: Application
    Filed: January 17, 2011
    Publication date: February 14, 2013
    Applicant: APTENIA S.R.L.
    Inventor: Matteo Scabini
  • Publication number: 20130040907
    Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and 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: May 4, 2012
    Publication date: February 14, 2013
    Applicant: Ardea Biosciences Inc.
    Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
  • Patent number: 8361988
    Abstract: The present invention comprises compounds useful as antiviral or antitumor agents. The compounds comprise nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moeities with quaternary centers at the 3? position. The nucleotide analogues can be used to inhibit cancer or viruses. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses. Thus, the present invention also comprising pharmaceutical formulations comprising the compounds and methods of using the compounds and formulations to inhibit viruses or tumors and treat, prevent, or inhibit the foregoing diseases.
    Type: Grant
    Filed: January 17, 2008
    Date of Patent: January 29, 2013
    Assignee: Institut de Recherches Cliniques de Montreal
    Inventor: Yvan Guindon
  • 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: 20120322996
    Abstract: A novel method for the preparation of stavudine polymorphic form I and form II is described. 5?-acetate-2?,3?-diacetyl-5-methyluridine is reacted with catalytic amounts of sodium methoxide in a C1-C4 alcoholic solvent, resulting in crude stavudine form II. Crude stavudine form II can be converted into polymorphic stavudine form I by slurry at reflux in isopropanol, without isolating or purifying the crude stavudine form II.
    Type: Application
    Filed: February 26, 2007
    Publication date: December 20, 2012
    Inventors: Gianluca Di Lernia, Alfredo Mancini, Franco Mancini, Maurizio Serra, Domenico Vergani
  • 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
  • Patent number: 8318756
    Abstract: Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient.
    Type: Grant
    Filed: December 5, 2005
    Date of Patent: November 27, 2012
    Assignee: Adherex Technologies, Inc.
    Inventors: Thomas Spector, William Paul Peters, Donald W. Kufe, Brian Huber
  • 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
  • Patent number: 8298414
    Abstract: The present invention relates to a process for separating a target radiolabelled compound from an impurity, apparatus for performing such a process and a removable cassette for use in such apparatus. Also provided are methods for using the target radiolabelled compound obtained by a method comprising the separating process of the invention.
    Type: Grant
    Filed: February 8, 2012
    Date of Patent: October 30, 2012
    Assignee: GE Healthcare Limited
    Inventor: Mette Husbyn
  • Publication number: 20120258891
    Abstract: The present disclosure relates to photoactivable protecting groups containing a diarylsulfide chromophore, a method for the synthesis thereof and their use as photoactivable protecting groups using maskless photolithography based array synthesis.
    Type: Application
    Filed: March 29, 2012
    Publication date: October 11, 2012
    Applicant: NIMBLEGEN SYSTEMS GMBH
    Inventor: Klaus-Peter Stengele
  • Publication number: 20120238740
    Abstract: The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vector in a nucleophilic reaction which offers a convenient and time-saving way to purify the product from non-reacted precursors vector-LM and by-products LM.
    Type: Application
    Filed: July 6, 2010
    Publication date: September 20, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Keith Graham, Mathias Berndt, Dae Yoon Chi, Byoung Se Lee, Sandip S. Shinde, Hee Seup Kil, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
  • 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
  • Publication number: 20120208991
    Abstract: It is an object of the present invention to provide a novel molecule for antisense therapies which is not susceptible to nuclease degradation in vivo and has a high binding affinity and specificity for the target mRNAs and which can efficiently regulate expression of specific genes. The novel artificial nucleoside of the present invention has an amide bond introduced into a bridge structure of 2?,4?-BNA/LNA. The oligonucleotide containing the 2?,4?-bridged artificial nucleotide has a binding affinity for a single-stranded RNA comparable to known 2?,4?-BNA/LNA and has an increased nuclease resistance over LNA.
    Type: Application
    Filed: October 19, 2010
    Publication date: August 16, 2012
    Applicant: OSAKA UNIVERSITY
    Inventors: Satoshi Obika, Yoshiyuki Hari, Tetsuya Kodama, Aiko Yahara, Masaru Nishida
  • Patent number: 8236945
    Abstract: Process for preparing a compound of the formula (I) R1-S(O)x—S(O)yR2 in which R1 represents a molecular hydrocarbon radical which can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si and X, where X represents a halogen; R2, independently of R1, represents a carbon-containing group or a molecular hydrocarbon radical which can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si and X, where X represents a halogen, and x and y are selected from 0 and 1 in such a way that the sum of x and y is not more than 1, characterized in that a compound of formula (II) R1-S(O)x—R3-Si(R4)(R5)(R6) in which R3 represents a hydrocarbon chain of two carbon atoms, which is optionally unsaturated and/or substituted, and R4, R5 and R6, which are identical or different, each represent, independently of one another, a
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: August 7, 2012
    Assignee: Universite Joseph Fourier (Grenoble1)
    Inventors: Jean-Luc Decout, Beatrice Gerland, Jerome Desire
  • Patent number: 8227594
    Abstract: Disclosed are nucleosides which are useful in diagnosing and treating viral infections, for example, infections caused by hepatitis B virus (HBV), and herpes viruses including Epstein Barr virus.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: July 24, 2012
    Inventors: Rakesh Kumar, Babita Agrawal, D. Lorne J. Tyrrell
  • Publication number: 20120178919
    Abstract: A radiolabeled nucleoside analogue is provided, which includes radioactive iodine 123I/131I, and a nucleoside analogue selected from a group consisting of cytidine, thymidine, uridine, and a derivative thereof. A method for preparing the radiolabeled nucleoside analogue, and a use thereof are further provided. The nucleoside analogue, prepared through the preparation method with a short synthesis time and a high radiochemical yield, has a long in vivo physiological half life and a high stability in serum, and, as a radiopharmaceutical composition, is useful in development of tumor proliferation diagnosis or therapy prognosis evaluation, and further assists in observation of long-time in vivo metabolism of a drug.
    Type: Application
    Filed: July 29, 2011
    Publication date: July 12, 2012
    Applicants: NATIONAL YANG-MING UNIVERSITY, Institute of Nuclear Energy Research Atomic Energy Council, Executive Yuan
    Inventors: HSIN-ELL WANG, CHIH-YUAN LIN, WEI-TI KUO, CHUAN-LIN CHEN, MEI-HUI WANG, HUNG-MAN YU, MAO-CHI WENG, YU CHANG, WUU-JYH LIN
  • 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