Abstract: Compounds used as labels with properties comparable to known fluorescent compounds. The compounds can be conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.
Type:
Application
Filed:
December 20, 2011
Publication date:
June 21, 2012
Applicants:
DYOMICS GMBH, PIERCE BIOTECHNOLOGY, INC.
Inventors:
Greg Hermanson, Peter T. Czerney, Surbhi Desai, Matthias S. Wenzel, Boguslawa Dworecki, Frank G. Lehmann
Abstract: The invention relates to novel oligomer analogues and their use in oligonucleotide-based therapies. More specifically, the invention concerns oligonucleotides carrying lipid molecules and their use as potential inhibitors of gene expression.
Type:
Application
Filed:
June 22, 2010
Publication date:
June 7, 2012
Applicant:
Sylentis S.A.U.
Inventors:
Ana Isabel Jimenez, Gema Panizo, Tamara Martinez, Anna Avino, Clara Caminal, Ramon Eritja, Santiago Grijalvo
Abstract: A di(pyrimidine nucleoside 5?-)polyphosphate is synthesized by converting a pyrimidine nucleoside 5?-triphosphate into a pyrimidine nucleoside 5?-cyclic triphosphate by use of a condensing agent, and subsequently reacting the pyrimidine nucleoside 5?-cyclic triphosphate with a pyrimidine nucleotide in the presence of a salt of a metal selected from among magnesium, manganese, and iron. Through the method of the invention, a di(pyrimidine nucleoside 5?-)polyphosphate can be synthesized from an unprotected pyrimidine nucleoside 5?-phosphate serving as a starting material at a synthesis yield of 50% or higher. Therefore, the method of the invention is suitable for large-scale synthesis of a di(pyrimidine nucleoside 5?-)polyphosphate.
Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:
Type:
Grant
Filed:
June 5, 2009
Date of Patent:
May 8, 2012
Assignee:
Gilead Pharmasset LLC
Inventors:
Jinfa Du, Dhanapalan Nagarathnam, Ganapati Reddy Pamulapati, Bruce S. Ross, Michael Joseph Sofia
Abstract: The present invention discloses compounds of formula (I), or its ?-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
September 11, 2009
Date of Patent:
April 24, 2012
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Yat Sun Or
Abstract: This invention is directed to a method of enhancing or facilitating the clearance or the lung mucus secretions in a subject. This invention is also directed to a method of facilitating the hydration of the lung mucus secretions in a subject. This invention is further directed to a method of preventing or treating diseases or conditions associated with impaired lung or airway function in a human or other mammal. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y6 receptor agonist compound, wherein said amount is effective to activate the P2Y6 receptors on the luminal surface of lung epithelia. The P2Y6 receptor agonist compounds useful for this invention include mononucleoside 5?-diphosphates, dinucleoside monophosphate, dinucleoside diphosphates, or dinucleoside triphosphates of general Formula I, or salts, solvates, hydrates thereof. This invention is also directed to novel P2Y6 receptor agonist compounds.
Type:
Grant
Filed:
November 4, 2010
Date of Patent:
April 17, 2012
Assignee:
Inspire Pharmaceuticals, Inc.
Inventors:
José L. Boyer, Sammy R. Shaver, James G. Douglass, III, Catherine C. Redick
Abstract: A practical high potency anti-craving oral medication or combined oral/IV drip medication is disclosed which comprises three components: a group of amino-acid substances, a group of vitamin substances, and a group of minerals, wherein each substance is selected for maximum efficacy in the body of an individual suffering from substance abuse disorder as opposed to the body of a healthy individual. The ingredients of the invention are selected to cooperate in easing metabolization in the bodies of individuals suffering the various medical conditions associated with substance abuse. The ingredients are provided orally to ease administration and to provide convenient use by patients: the oral medication may be a maintenance dosage or a corrective dosage.
Type:
Grant
Filed:
September 14, 2006
Date of Patent:
March 27, 2012
Inventors:
Tamea Rae Sisco, Keith Kenneth Skinner, Theodore Keller
Abstract: A practical high potency anti-craving medication is disclosed which comprises three components: an amino-acid component, a vitamin component, and a mineral component, wherein each component is selected for maximum efficacy in the body of an individual suffering from substance abuse disorder as opposed to the body of a healthy individual. Additionally, the active agents are received by means of a prolonged administration, preferably by means of an IV drip, thus assuring a period of time in which the active agents are present in desired concentrations, and more preferably a prolonged time during which they are simultaneously present in desired concentrations. The agents of each component are also selected so as to allow easy administration of the medication to patients in three vials of medication rather than as a large number of individual vials.
Type:
Grant
Filed:
August 20, 2005
Date of Patent:
March 27, 2012
Inventors:
Tamea Rae Sisco, Keith Kenneth Skinner, Theodore R Keller
Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
Type:
Application
Filed:
August 25, 2011
Publication date:
March 8, 2012
Applicant:
Pacific Biosciences of California, Inc.
Abstract: The invention provides a novel class of cyanine dyes that are functionalized with a linker moiety that facilitates their conjugation to other species and substituent groups which increase the water-solubility, and optimize the optical properties of the dyes. Also provided are conjugates of the dyes, methods of using the dyes and their conjugates and kits including the dyes and their conjugates.
Type:
Application
Filed:
August 25, 2011
Publication date:
March 8, 2012
Applicant:
Pacific Biosciences of California, Inc.
Abstract: The present invention relates to methods and reagents for detecting analytes, e.g. nucleic acids. The new methods and reagents allow a simple and sensitive detection even in complex biological samples.
Type:
Grant
Filed:
April 28, 2006
Date of Patent:
March 6, 2012
Assignee:
Baseclick GmbH
Inventors:
Thomas Carell, Anja Schwögler, Glenn A. Burley, Johannes Gierlich, Mohammad Reza Mofid
Abstract: The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z?)(Z?)O-nucleoside, —P(Z?)(Z?)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z?)(Z?)O-Linker-OP(Z??)(Z??)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z?)(Z?)-formula (I), —P(Z?)(Z?)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g.
Type:
Grant
Filed:
December 4, 2008
Date of Patent:
January 31, 2012
Assignee:
Alnylam Pharmaceuticals, Inc.
Inventors:
Muthiah Manoharan, Kallanthottathil G. Rajeev, Jayaprakash K. Narayanannair, Martin Maier
Abstract: The present invention provides oligomeric compounds and uses thereof. In certain embodiments, such oligomeric compounds are useful as antisense compounds. Certain such antisense compounds are useful as RNase H antisense compounds, as RNAi compounds, and/or as modulators of splicing.
Type:
Application
Filed:
February 5, 2010
Publication date:
January 26, 2012
Inventors:
Eric E. Swayze, Andrew M. Siwkowski, Balkrishen Bhat, Thazha P. Prakash, Charles Allerson, Punit P. Seth
Abstract: Methods and compositions are provided for treating lung diseases, including but not limited to infections and small cell and non-small cell lung cancer, by conjugating a drug of interest to glycerol ethers or glycerol phosphate ethers.
Type:
Grant
Filed:
December 15, 2005
Date of Patent:
January 24, 2012
Assignee:
The Regents of the University of California
Abstract: Embodiments of the invention include nucleotide and nucleoside monomers protected at the 5?- or 3?-hydroxyls with thioether substituted aryl carbonate protecting groups. In certain cases, the carbonate protecting groups include an aryl moiety, e.g., a phenyl group, attached to the carbonate, where the aryl moiety further includes a thioether group, e.g., an alkyl or aryl thioether group, bound directly to the aryl ring. Aspects of the invention further include methods of synthesizing nucleic acids, e.g., oligonucleotides, using such protected nucleoside monomer monomers, as well as nucleic acids produced using methods of the invention and compositions thereof.
Type:
Grant
Filed:
August 31, 2007
Date of Patent:
January 17, 2012
Assignee:
Agilent Technologies, Inc.
Inventors:
Zoltan Timar, Zoltan Kupihar, Douglas J. Dellinger, Marvin H. Caruthers
Abstract: The present invention relates to antisense oligonucleotides that modulate the expression of and/or function of Brain derived neurotrophic factor (BDNF), in particular, by targeting natural antisense polynucleotides of Brain derived neurotrophic factor (BDNF). The invention also relates to the identification of these antisense oligonucleotides and their use in treating diseases and disorders associated with the expression of BDNF.
Type:
Application
Filed:
February 12, 2010
Publication date:
December 29, 2011
Applicant:
OPKO CuRNA, LLC
Inventors:
Joseph Collard, Olga Khorkova Sherman, Carlos Coito
Abstract: The present invention discloses compounds of formula (I): which exhibit antiviral properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of anti-HBV treatment. The invention also relates to methods of treating a HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
December 12, 2006
Date of Patent:
December 13, 2011
Assignee:
Spring Bank Pharmaceuticals, Inc.
Inventors:
Radhakrishnan P. Iyer, Seetharamaiyer Padmanabhan
Abstract: The present invention describes novel compounds and methods for capping reactive groups on support and during multistep synthesis. These new capping reagents are also useful for high quality synthesis on solid supports and surfaces used as microarrays, biosensors, or in general as biochips. The compounds are also useful for controlling surface density of reactive groups on a support. The compounds may also be used to modify the hydrophilic/hydrophobic characteristics of a surface or a molecule. The compounds have functional utility in various applications in the fields of genomics, proteomics, diagnostics and medicine.
Abstract: Processes are disclosed that use 3?-reversibly terminated nucleoside triphosphates to analyze DNA for purposes other than sequencing using cyclic reversible termination. These processes are based on the unexpected ability of terminal transferase to accept these triphosphates as substrates, the unexpected ability of polymerases to add reversibly and irreversibly terminated triphosphates in competition with each other, the development of cleavage conditions to remove the terminating group rapidly, in high yield, and without substantial damage to the terminated oligonucleotide product, and the ability of reversibly terminated primer extension products to capture groups. The presently preferred embodiments of the disclosed processes use a triphosphate having its 3?-OH group blocked as a 3?-ONH2 group, which can be removed in buffered NaNO2 and use variants of Taq DNA polymerase, including one that has a replacement (L616A).
Type:
Grant
Filed:
March 27, 2009
Date of Patent:
October 11, 2011
Inventors:
Steven Albert Benner, Daniel Hutter, Nicole Aurora Leal, Fei Chen
Abstract: The present invention provides 5?-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5?-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.
Type:
Grant
Filed:
March 31, 2010
Date of Patent:
October 4, 2011
Assignee:
Isis Pharmaceuticals, Inc.
Inventors:
Punit P. Seth, Eric E. Swayze, Balkrishen Bhat
Abstract: Hydrazino, oxyamino and carbonyl-based monomers and methods for incorporation into oligonucleotides during enzymatic synthesis are provided. Modified oligonucleotides are provided that incorporate the monomers provided herein. Immobilized oligonucleotides and oligonucleotide conjugates that contain covalent hydrazone or oxime linkages are provided. Methods for preparation of surface bound oligonucleotides are provided. Methods for the preparation of oligonucleotide conjugates are also provided.
Abstract: The invention provides compounds of formula (I) and salts thereof: R1-L-R2—B wherein R1, L, R2, and B have any of the values defined herein, as well as compositions comprising such compounds, and therapeutic methods comprising the administration of such compounds or salts. The compounds block siderophore production in bacteria and are useful as antibacterial agents.
Type:
Grant
Filed:
December 6, 2006
Date of Patent:
August 2, 2011
Assignee:
Regents of the University of Minnesota
Inventors:
Courtney Aldrich, Ravindranadh Venkata Somu
Abstract: Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2?-arabino-fluoronucleoside and an internucleoside 3?-NH—P(?O)(OR)—O-5? linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2?-arabino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.
Abstract: The present invention describes a composition comprising at least 55% w/w (on sodium chloride free dry matter weight) of 5?-ribonucleotides and a process for the production of this composition comprising the steps of: (i) treating microbial cells to release the cell contents comprising RNA; (ii) separating the RNA present in the released cell content from other soluble cell material; and (iii) converting the separated RNA into 5?-ribonucleotides.
Abstract: Provided are novel nucleotides, nucleoside, and their derivatives described herein, that can be used in DNA sequencing technology and other types of DNA analysis. In one embodiment, the nucleotide or nucleoside with an unprotected 3?-OH group is derivatized at the nucleobase to include a fluorescent dye attached via a linker to a photocleavable terminating group. The photocleavable-fluorescent group is designed to terminate DNA synthesis as well as be cleaved so that DNA oligomers can be sequenced efficiently in a parallel format. The design of such rapidly cleavable fluorescent groups on nucleotides and nucleosides can enhance the speed and accuracy of sequencing of large oligomers of DNA in parallel, to allow rapid whole genome sequencing, and the identification of polymorphisms and other valuable genetic information, as well as allowing further manipulation and analysis of nucleic acid molecules in their native state following cleavage of the fluorescent group.
Type:
Grant
Filed:
November 11, 2008
Date of Patent:
June 21, 2011
Assignee:
LaserGen, Inc.
Inventors:
Weidong Wu, Vladislav A. Litosh, Brian P. Stupi, Michael L. Metzker
Abstract: The present invention provides for reagents for the introduction of colorimetric-oxycarbonyl protecting groups, compounds bearing colorimetric-oxycarbonyl protecting groups, and the use thereof in solid-supported organic syntheses of oligonucleotides, polypeptides, polysaccharides, and combinatorial libraries.
Type:
Grant
Filed:
March 30, 2009
Date of Patent:
June 14, 2011
Assignee:
Berry and Associates, Inc.
Inventors:
John C. Hodges, Yam Foo Poon, William H. Pearson
Abstract: One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such modified nucleosides. Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
Type:
Application
Filed:
March 26, 2009
Publication date:
June 2, 2011
Applicant:
ALNYLAM PHARMACEUTICALS, INC.
Inventors:
Muthiah Manoharan, Kallanthottathil G. Rajeev
Abstract: Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may be substituted at the 5-position. The phosphoramidate moiety has attached to the P atom an aryl-O moiety and an ?-amino acid moiety. The ?-amino acid moiety may correspond to or be derived from either a naturally occurring or a non-naturally occurring amino acid.
Abstract: A protecting group for 1-nitrogen atom of an indole group including a sulfonylethyl carbamate group, wherein the protecting group is represented by the following General Formula (I) and capable of being removed from the 1-nitrogen atom of the indole group in an aprotic solvent: where R represents an alkyl group, a derivative of the alkyl group, a phenyl group or a derivative of the phenyl group.
Abstract: 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.
Type:
Grant
Filed:
September 24, 2010
Date of Patent:
May 3, 2011
Assignee:
Medivir AB
Inventors:
Nils-Gunnar Johansson, Genaidy Kalyanov, Joseph Armstrong Martin, David Bernard Smith, Anna Winqvist
Abstract: This invention describes a simple method useful for the excision and isolation of maize immature embryos. The embryos are useful for plant tissue culture and transformation methods.
Abstract: The invention relates to a compound suited as entity carrier, having the general formula (I) wherein X is an amine-containing residue further defined herein. The invention further relates to the use of such compounds, a nanocarrier system, a kit comprising such compounds and methods for gene silencing and anti-cancer treatment.
Type:
Application
Filed:
May 22, 2009
Publication date:
April 7, 2011
Applicants:
Ramot at Tel-Aviv University Ltd., Freie Universitat Berlin
Inventors:
Rainer Haag, Wiebke Fischer, Mohiuddin Abdul Quadir, Paula Ofek
Abstract: The present invention relates to a DNA sequencing method using a nucleoside triphosphate with a fluorescent blocking group on its 3?-OH end as a reversible terminator. Further, the present invention relates to sequencing-by-synthesis method using the mono-modified reversible terminator (MRT), the novel nucleotide monomer having a reversible fluorescent blocking group removable chemically or enzymatically at its 3?-OH end. The sequencing method of the present invention facilitates sequencing of bases inserted by terminating extension of a nucleotide chain by the nucleotide monomer and then detecting fluorescence signal from 3?-OH end. At this time, after analyzing the fluorescence signal, the blocking group conjugated to the 3?-OH end can be effectively removed, indicating that a free 3?-OH functional group can be successfully restored, so that the next monomer insertion is possible, making continuous sequencing possible.
Type:
Application
Filed:
October 26, 2009
Publication date:
March 31, 2011
Applicant:
KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
Abstract: The invention is related to phosphorus substituted nucleoside compounds and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Type:
Application
Filed:
April 9, 2008
Publication date:
March 24, 2011
Inventors:
Constantine G. Boojamra, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Christopher P. Lee, David A. Oare, Vidya K. Prasad, Adrian S. Ray, Sundaramoorthi Swaminathan, William J. Watkins
Abstract: Provided are novel nucleotides, nucleoside, and their derivatives described herein, that can be used in DNA sequencing technology and other types of DNA analysis. In one embodiment, the nucleotide or nucleoside with an unprotected 3?-OH group is derivatized at the nucleobase to include a fluorescent dye attached via a linker to a photocleavable terminating group. The photocleavable-fluorescent group is designed to terminate DNA synthesis as well as be cleaved so that DNA oligomers can be sequenced efficiently in a parallel format. The design of such rapidly cleavable fluorescent groups on nucleotides and nucleosides can enhance the speed and accuracy of sequencing of large oligomers of DNA in parallel, to allow rapid whole genome sequencing, and the identification of polymorphisms and other valuable genetic information, as well as allowing further manipulation and analysis of nucleic acid molecules in their native state following cleavage of the fluorescent group.
Type:
Grant
Filed:
December 5, 2006
Date of Patent:
March 1, 2011
Assignee:
LaserGen, Inc.
Inventors:
Weidong Wu, Vladislav A. Litosh, Brian P. Stupi, Michael L. Metzker
Abstract: Provided are novel nucleotides, nucleoside, and their derivatives described herein, that can be used in DNA sequencing technology and other types of DNA analysis. In one embodiment, the nucleotide or nucleoside with an unprotected 3?-OH group is derivatized at the nucleobase to include a fluorescent dye attached via a linker to a non-cleavable terminating group. The non-cleavable-fluorescent group is designed to terminate DNA synthesis so that DNA oligomers can be sequenced efficiently in a parallel format. These reagents and methods will lead to more accurate identification of polymorphisms and other valuable genetic information.
Type:
Grant
Filed:
December 5, 2006
Date of Patent:
February 22, 2011
Assignee:
LaserGen, Inc.
Inventors:
Weidong Wu, Vladislav A. Litosh, Brian P. Stupi, Michael L. Metzker
Abstract: The invention provides short interfering nucleic acids, either single-stranded or double-stranded, that cause RNAi-induced degradation of mRNA from the Nav1.8 sodium channel gene; to pharmaceutical compositions comprising such short interfering nucleic acids; recombinant vectors comprising such short interfering nucleic acids; a method for inhibiting translation of an mRNA; a method for inhibiting expression of a polypeptide; a method for blocking the membrane potential in a cell; a method for blocking the sodium current in a cell; and a method for inhibiting chronic pain.
Type:
Application
Filed:
May 28, 2010
Publication date:
December 2, 2010
Applicants:
SCHERING CORPORATION, CANJI, INC.
Inventors:
SAMEER GOREGAOKER, JOHN C. HUNTER, TONY PRIESTLEY
Abstract: The present disclosure is directed to fluorogenic schiff base-forming dyes capable of detecting analytes containing aldehyde and ketone groups. The dyes contain nucleophilic hydrazinyl appendages and are capable of binding and detecting analytes in situ.
Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble, non-peptidic oligomer. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.
Type:
Application
Filed:
September 18, 2008
Publication date:
November 11, 2010
Applicant:
Nektar Therapeutics
Inventors:
Zhongxu Ren, Jennifer Riggs-Sauthier, Timothy A. Riley, Laurie A. Vander Veen, Aaron S. Hammons
Abstract: A method for modifying nucleic acid bases by a chemical means, which enables the discrimination of every base species in plural species of bases in a nucleic acid comprising plural nucleotide units, while retaining the base sequence information of the nucleic acid. A nucleic acid base-modified product provided by the method. The nucleic acid base-modified product is essentially a single strand. In accordance with the invention, a novel means for sequencing a nucleic acid by a microscopic means is provided.
Abstract: The purpose of the invention is to develop a silyl linker that can be efficiently introduced on a solid-phase support used for the synthesis of nucleic acid oligomers such as DNA. The present invention relates to a silyl linker for use in the solid-phase synthesis of nucleic acid, comprised of a compound of the general formula or its ester or salt: H—(R1)Si(R2)-(C6H4)—CONH-(A)-COOH??(I) wherein each of R1 and R2 is an alkyl or aryl group, and (A) represents a spacer moiety; a 3?-end nucleoside unit having said compound linked via an oxygen atom to the 3-position of a sugar of the nucleoside or its derivative, a solid-phase support having the 3?-end nucleoside unit, and a method for synthesis of nucleic acid oligomer with the use of said solid-phase support.
Abstract: A class of nucleoside derivatives of formula (I), as defined herein, that are useful as inhibitors of RNA-dependent RNA viral replication and in particular HCV replication, are provided. Also provided are processes for the synthesis and use of such compounds for treating or preventing HCV infection.
Type:
Application
Filed:
September 16, 2008
Publication date:
August 19, 2010
Applicant:
Istitute de Ricerche di Biologia Molecolare P. Angeletti
Inventors:
Maria Emilia Di Francesco, Vincenzo Summa, Gabriella Dessole
Abstract: Reactions of Group 16 elements involving the addition of atoms such as sulfur, selenium or tellurium to organic or inorganic molecules comprising use of an ionic liquid as a reaction medium.
Type:
Application
Filed:
August 21, 2006
Publication date:
July 15, 2010
Applicant:
THE QUEEN'S UNI IONIC LIQUID LAB RESEARCH CENTRE
Inventors:
Martin John Earle, Eva Boros, Kenneth Richard Seddon, Manuela A. Gilea, Joseph S. Vyle
Abstract: The current invention provides methods (e.g., large-scale processes) for the production of nucleotide sugars, which are modified with a polymeric modifying group, such as poly(alkylene oxide) moieties (e.g., poly(ethylene glycol) or poly(propylene glycol)) moieties. A typical process of the invention includes anion exchange chromatography followed by an ultrafiltration procedure, such as tangential flow filtration. The process of the invention provides modified nucleotide sugars in unexpectedly high purity and high overall yields.
Abstract: Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III) wherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy, halogen, SH, NH2, azide or DL wherein D is O, S or NH and L is a heteroatom-protecting group, unsubstituted hydrocarbyl, substituted hydrocarbyl, heteroatom-containing hydrocarbyl, or substituted heteroatom-containing hydrocarbyl; B is a nucleobase; and one of R11 and R12 is a blocking group and the other is (IV) or (VI) in which W, X, Y, Z, R1 and n are as defined herein.
Abstract: A novel compound, 2?/3?-O-acetyl-ADP-ribose, is provided. The compound is a mixture of the 2? and 3? regioisomers of O-acetyl-ADP ribose, and is formed nonenzymatically from 2?-O-acetyl-ADP-ribose, which is the newly discovered product of the reaction of Sir2 enzymes with acetylated peptides and NAD+. Analogs of 2?/3?-O-acetyl-ADP-ribose are also provided. Additionally, methods of preparing 2?/3?-O-acetyl-ADP-ribose, methods of determining whether a test compound is an inhibitor of a Sir2 enzyme, methods of detecting Sir2 activity in a composition, methods of deacetylating an acetylated peptide, and methods of inhibiting the deacetylation of an acetylated peptide are provided. Prodrugs of 2?/3?-O-acetyl-ADP-ribose are also provided.
Type:
Grant
Filed:
September 5, 2008
Date of Patent:
June 22, 2010
Assignees:
Albert Einstein College of Medicine of Yeshiva University, The Johns Hopkins University
Inventors:
Vern L. Schramm, Jef D. Boeke, Anthony Sauvé, Ivana Celic
Abstract: The present invention relates to the use of N-phosphonylmethoxyethyl nucleoside analogs for manufacturing a medicament for the treatment or prevention of Koi Herpes virus infections in fish, especially in carps.
Type:
Application
Filed:
May 16, 2008
Publication date:
June 3, 2010
Applicants:
Katholieke Universiteit Leuven, Universite de Liege
Inventors:
Berenice Costes, Johan Neyts, Alain Vanderplasschen
Abstract: Compositions, devices, systems and methods for reducing and/or preventing photo-induced damage of one or more reactants in an illuminated analytical reaction by addition of one or more photo-induced damage mitigating agents to the reaction mixture and allowing the reaction to proceed for a period that is less than a photo-induced damage threshold period.
Type:
Application
Filed:
November 19, 2009
Publication date:
June 3, 2010
Applicant:
Pacific Biosciences of California, Inc.
Inventors:
Xiangxu Kong, Gene Shen, Andrei Fedorov, John Lyle, Grace Lee, Lubomir Sebo, Duc Do, Robert Weber, Stephen Dudek
Abstract: The present invention relates to an acyclic nucleoside phosphonate derivative which is useful as an antiviral agent (particularly, against hepatitis B virus), pharmaceutically acceptable salts, stereoisomers, and a process for the preparation thereof.
Type:
Grant
Filed:
September 9, 2009
Date of Patent:
May 25, 2010
Assignee:
LG Life Sciences Ltd.
Inventors:
Dong-Gyu Cho, Jae-Hong Lim, Jae-Taeg Hwang, Woo-Young Cho, Hyun-Sook Jang, Chang-Ho Lee, Tae-Saeng Choi, Chung-Mi Kim, Yong-Zu Kim, Tae-Kyun Kim, Seung-Joo Cho, Gyoung-Won Kim, Jong-Ryoo Choi, Jeong-Min Kim, Kee-Yoon Roh
Abstract: To provide an amidite for nucleic acid synthesis, which enables a protective group therein to be removed under moderate conditions and can be practically used, and a nucleic acid synthesizing method using the amidite for nucleic acid synthesis. Specifically, the present invention relates to an amidite for nucleic acid synthesis represented by General Formula (I) below, and a nucleic acid synthesizing method using the amidite for nucleic acid synthesis: where X denotes a base; Y denotes a protective group formed of any one of a 4-aminobutyric acid derivative, an o-aminomethylbenzoic acid derivative, an o-aminophenylacetic acid derivative, an o-aminoethylbenzoic acid derivative, an o-aminomethylphenylacetic acid derivative, an o-aminophenylpropionic acid derivative and a 5-aminovaleric acid derivative; and Q denotes one of a hydrogen atom and a hydroxyl group.