Exactly Two Phosphorus Atoms In The Chain (e.g., Coenzyme A, Etc.) Patents (Class 536/26.23)
  • Patent number: 10065973
    Abstract: The present invention relates to compounds of formula (I), wherein R1 to R5 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: November 10, 2017
    Date of Patent: September 4, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Baoxia Wang, Lisha Wang, Hongying Yun, Xiufang Zheng
  • Patent number: 9249177
    Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.
    Type: Grant
    Filed: June 27, 2014
    Date of Patent: February 2, 2016
    Assignee: K.U. Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
  • Patent number: 9107879
    Abstract: A method of treating cancer in a subject in need thereof, comprising administering to the subject a first amount of a compound of the HAT inhibitor of the following formula: wherein R is chosen from coenzyme A, (CH2)2NHCO(CH2)2NHCOR2; (CH2)2NHCOR3; (CH2)2NHCO(CH2)2NHCOR4; R1 is H, NH2, NH, N, and R1 can optionally cyclize with at least one other X2 to form a C3-8 membered ring containing C, O, S, or N; R2 is chosen from alkyl, cycloalkyl, aryl, heteroaryl; R3 is chosen from an alkyl, cycloalkyl, aryl, heteroaryl; R4 is chosen from CH(OH)C(CH3)2CH2)OCOR2; X1 is chosen from H or can cyclize with one other X2 or R1 to form a C3-8 membered ring containing C, O, S, or N; and X2 is chosen from C, N, NH, and can optionally cyclize with at least one other X2 or R1 to form a C3-8 membered ring containing C, O, S, or N; or a pharmaceutically acceptable salt or hydrate thereof, thereby treating the cancer.
    Type: Grant
    Filed: April 1, 2011
    Date of Patent: August 18, 2015
    Assignee: Vanderbilt University
    Inventors: Joseph Parello, Keya Bandyopadhyay, Jean-Louis Baneres, Casimir Blonski, Ruth Anne Gjerset, Aimee Martin
  • Patent number: 8980865
    Abstract: Disclosed herein are phosphorothioate nucleotide analogs, such as thiophosphoroamidate prodrugs and thiophosphates (including ?-thiomonophosphates, ?-thiodiphosphates, and ?-thiotriphosphates), methods of synthesizing phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates and methods of treating viral infections, such as HCV, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs, such as thiophosphoramidate prodrugs, and thiophosphates.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: March 17, 2015
    Assignee: Alios BioPharma, Inc.
    Inventors: Guangyi Wang, Leonid Beigelman
  • Publication number: 20140378408
    Abstract: Particular nucleoside 5?-phosphorothioate analogues, such as, adenosine or uridine 5?-di- or tri-phosphorothioate analogues in which at least one of the bridging oxygen atoms of the phosphorothioate is replaced by a group such as —CH2— or —CCl2—, and at least one of the non-bridging atoms or negatively-charged atoms of the phosphorothioate is either a sulfur atom or a sulfur ion can be formulated into pharmaceutical compositions. These compounds are useful for treatment of osteoarthritis/calcium pyrophosphate dihydrate (CPPD) deposition disease.
    Type: Application
    Filed: September 5, 2014
    Publication date: December 25, 2014
    Inventors: Bilha FISCHER, Ortal SHIMON, Yael NADEL, Uri ARAD
  • Publication number: 20140371417
    Abstract: The invention provides non-naturally occurring microbial organisms having a 4-hydroxybutyrate, gamma-butyrolactone, 1,4-butanediol, 4-hydroxybutanal, 4-hydroxybutyryl-CoA and/or putrescine pathway and being capable of producing 4-hydroxybutyrate, wherein the microbial organism comprises one or more genetic modifications. The invention additionally provides methods of producing 4-hydroxybutyrate, gamma-butyrolactone, 1,4-butanediol, 4-hydroxybutanal, 4-hydroxybutyryl-CoA and/or putrescine or related products using the microbial organisms.
    Type: Application
    Filed: April 25, 2014
    Publication date: December 18, 2014
    Applicant: Genomatica, Inc.
    Inventors: Priti PHARKYA, Anthony P. BURGARD, Stephen J. VAN DIEN, Robin E. OSTERHOUT, Mark J. BURK, John D. TRAWICK, Michael P. KUCKINSKAS, Brian STEER
  • Patent number: 8877731
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: November 4, 2014
    Assignee: Alios Biopharma, Inc.
    Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
  • Publication number: 20140235565
    Abstract: The present invention provides N-alkylthio ?-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.
    Type: Application
    Filed: May 1, 2014
    Publication date: August 21, 2014
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: EDWARD TUROS, KEVIN D. REVELL
  • Patent number: 8809520
    Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 19, 2014
    Assignee: K.U. Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
  • Patent number: 8759316
    Abstract: A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.
    Type: Grant
    Filed: June 28, 2013
    Date of Patent: June 24, 2014
    Assignee: The Medicines Company
    Inventors: Lisa Ruderman Chen, Simona Skerjanec, Dawn Bell, Jayne Prats, Meredith Todd, Clive Arthur Arculus-Meanwell, Diane Mould
  • Publication number: 20140099262
    Abstract: The present invention provides CDP-Choline (Citicoline) and any salt thereof comprising at least one isotopically labeled carbon atom directly bonded to at least one deuterium atom, a composition comprising said CDP-Choline, uses thereof, methods for diagnosing and evaluating a state, condition, or disease in a subject utilizing CDP-Choline of the invention and kits comprising CDP-Choline of the invention.
    Type: Application
    Filed: May 31, 2012
    Publication date: April 10, 2014
    Applicant: BRAIN WATCH LTD.
    Inventors: Rachel Katz-Brull, Moshe Gomori
  • Publication number: 20130323283
    Abstract: Methods for treating or preventing a Foxp3+ T regulatory cell (Treg) related disease in a subject in need thereof comprise administering to the subject an effective amount of a pharmaceutical composition comprising an inhibitor of a histone/protein acetyltransferase (HAT). Methods for identifying an agent useful for treating or preventing a Foxp3+ T regulatory cell (Treg) related disease comprise (a) contacting a candidate agent with a test sample comprising Foxp3+ T regulatory cells (Tregs), and (b) comparing a function of the Foxp3+ Tregs in the test sample with that in a control sample, wherein inhibition of the function of the Foxp3+ Tregs in the test sample when compared with the control sample indicates that the candidate agent is an agent useful for treating or preventing a Foxp3+ Treg related disease.
    Type: Application
    Filed: December 1, 2011
    Publication date: December 5, 2013
    Applicants: THE CHILDREN'S HOSPITAL OF PHILADELPHIA, THE JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: Wayne W. Hancock, Steven M. Albelda, Philip A. Cole
  • Patent number: 8598141
    Abstract: This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: December 3, 2013
    Assignee: Tufts University
    Inventors: Philip Haydon, Jinbo Lee, Jinghui Dong, Stephen Moss, Raquel Revilla-Sanchez
  • Publication number: 20130224177
    Abstract: The present invention relates to a pharmaceutical composition for promoting fertilization comprising cyclic ADP-ribose or its derivative, CD38 and to a method of promoting fertilization by promoting the synthesis of cyclic ADP-ribose to increase sperm motility. Also, the present invention relates to a pharmaceutical composition for contraception and a method for inhibiting fertilization, which can inhibit the expression or function of cyclic ADP-ribose to reduce sperm motility, thereby inhibiting fertilization.
    Type: Application
    Filed: March 4, 2013
    Publication date: August 29, 2013
    Applicant: Industrial Cooperation Foundation Chonbuk National University
    Inventor: Industrial Cooperation Foundation Chonbuk National University
  • Patent number: 8501709
    Abstract: The invention is directed to phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base, as well as pharmaceutical compositions thereof. These compounds, which can be described by general formula (II), are useful for the treatment of retroviral infection, e.g., HIV (Human Immunodeficiency Virus) infection in a mammal. The invention also features synthetic intermediates for the preparation of phosphonate nucleosides.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: August 6, 2013
    Assignee: K.U.Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
  • Publication number: 20130184168
    Abstract: The present invention relates to immunoreactive Francisella tularensis antigens and their uses as correlates of protection against tularemia. In one aspect, the invention provides a set of biomarkers for tularemia. In another aspect the invention provides a method of evaluating immunity against tularaemia in a subject, using the biomarkers.
    Type: Application
    Filed: January 13, 2012
    Publication date: July 18, 2013
    Inventors: Mary Katherine HART, Robert Victor HOUSE, Shannon MARTIN
  • Publication number: 20130183712
    Abstract: The invention provides methods and compositions for the rapid and sensitive detection of post-translationally modified proteins, and particularly of those with posttranslational glycosylations. The methods can be used to detect O-GlcNAc posttranslational modifications on proteins on which such modifications were undetectable using other techniques. In one embodiment, the method exploits the ability of an engine˜red mutant of ?-1,4-galactosyltransferase to selectively transfer an unnatural ketone functionality onto O-GlcNAc glycosylated proteins. Once transferred, the ketone moiety serves as a versatile handle for the attachment of biotin, thereby enabling detection of the modified protein. The approach permits the rapid visualization of proteins that are at the limits of detection using traditional methods. Further, the preferred embodiments can be used for detection of certain disease states, such as cancer, Alzheimer's disease, neurodegeneration, cardiovascular disease, and diabetes.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 18, 2013
    Applicant: CALIFORNIA INSTITUTE OF TECHNOLOGY
    Inventor: California Institute of Technology
  • Publication number: 20130109850
    Abstract: Provided herein are modified 5? diphosphate nucleosides and oligomeric compounds prepared therefrom. More particularly, modified 5? diphosphate nucleosides are provided that can be further modified at the 2? and 5? positions. In some 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. The oligomeric compounds are also expected to be useful as primers and probes in diagnostic applications.
    Type: Application
    Filed: April 26, 2011
    Publication date: May 2, 2013
    Applicant: Isis Pharmaceuticals, Inc
    Inventors: Thazha P. Prakash, Punit P. Seth, Muthiah Manoharan, Eric E. Swayze, Kallanthottathil G. Rajeev, Ivan Zlatev
  • Publication number: 20130102771
    Abstract: An object of the present invention is to provide a non-peptidic nerve axon and/or neurite outgrowth agent for allowing a nerve axon and a neurite to elongate. 3-(Aminocarbonyl)-1-[5-O-[[1-(6-amino-9H-purin-9-yl)-1-deoxy-?-D-ribofuranos-5-O-yl]phosphonyloxy(oxylato)phosphinyl]-?-L-ribofuranosyl]pyridinium that is an analogue of nicotinamide adenine dinucleotide (NAD) comprising ?-L-ribose as the sugar component is used as a nerve axon and/or neurite outgrowth agent or composition, a cancer cell growth suppressing and/or apoptosis inducing agent, or a cancer cell growth suppressing and/or apoptosis inducing composition.
    Type: Application
    Filed: April 20, 2011
    Publication date: April 25, 2013
    Inventors: Hidenori Kaminishi, Junei Kinjo, Ryota Tsuchihashi, Tsuyoshi Ikeda, Akihiro Sakamoto
  • Publication number: 20130102034
    Abstract: The present disclosure provides modified nucleosides, nucleotides, and nucleic acids, and methods of using thereof.
    Type: Application
    Filed: May 25, 2012
    Publication date: April 25, 2013
    Inventor: Jason P. Schrum
  • Publication number: 20130065248
    Abstract: The invention provides a method of preparing a sirtuin complex. The invention also provides a method of detecting a sirtuin in a sample comprising use of the aforesaid sirtuin complex.
    Type: Application
    Filed: May 18, 2011
    Publication date: March 14, 2013
    Applicant: CORNELL UNIVERSITY
    Inventors: Anthony A. SAUVE, Yana CEN
  • Publication number: 20120302519
    Abstract: Disclosed herein are substituted fluoromethanes; pharmaceutical compositions comprising a therapeutically effective amount of the same; processes for preparing these fluoromethanes; and methods of using the same in alleviating infection and parasitism. Also disclosed are methods for identifying substituted fluoromethanes for modulating the activity of receptors and enzymes that bind and/or modify phosphate containing ligands and substrates.
    Type: Application
    Filed: February 3, 2011
    Publication date: November 29, 2012
    Applicant: MEH ASSOCIATES, INC.
    Inventor: Mark E. Hediger
  • Publication number: 20120108535
    Abstract: Disclosed are halogenated 2-deoxy-lactone, 2?-deoxy-nucleosides, and derivatives thereof, for example, a compound of formula (I). Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, and a method of treating a disorder is selected from the group consisting of an abnormal cellular proliferation, a viral infection, and an autoimmune disorder.
    Type: Application
    Filed: July 1, 2010
    Publication date: May 3, 2012
    Applicant: CORNELL UNIVERSITY
    Inventors: Anthony A. Sauve, Yana Cen
  • Patent number: 8153779
    Abstract: Described are modified mononucleotides and processes for their production. The nucleotides have a structure in which B is a purine or pyrimidine, S is a sugar unit, Y is an OH, a monophosphate, or a diphosphate, and Acc is an electron acceptor selected from the group consisting of (a) —CN and (b) —SO2—R? in which R? contains one amino-substituted alkyl or one optionally substituted aryl.
    Type: Grant
    Filed: October 16, 2009
    Date of Patent: April 10, 2012
    Assignee: Roche Diagnostics Operations, Inc.
    Inventor: Dieter Heindl
  • Publication number: 20120052507
    Abstract: In various embodiments, the present invention provides fluorescent dyes that are linked to another species through an amino acid or peptide linker. In an exemplary embodiment, the dye is linked to a polyphosphate nucleic acid through an amino acid or peptide linker. These conjugates find use in single molecule DNA sequencing and other applications. In various embodiments, the dye moiety is a cyanine dye. Cyanine dyes that are highly charged, such as those including muliple sulfonate, alkylsulfonate, carboxylate and/or alkylcarboxylate moieties are examples of cyanine dyes of use in the compounds of the invention.
    Type: Application
    Filed: August 25, 2011
    Publication date: March 1, 2012
    Applicant: Pacific Biosciences of California, Inc.
    Inventor: Gene Shen
  • Publication number: 20120052532
    Abstract: The sialic acid-like sugar legionaminic acid is found as a virulence-associated surface glyco-conjugate in Legionella pneumophila and Campylobacter coli. In this work, we have purified and biochemically characterized eleven candidate biosynthetic enzymes from C. jejuni, thereby fully reconstituting the biosynthesis of legionaminic acid and its CMP-activated form, starting from fructose-6-P. This pathway involves unique GDP-linked intermediates and provides a facile means for the efficient large-scale synthesis of an important sialic acid mimic and novel precursors.
    Type: Application
    Filed: December 16, 2009
    Publication date: March 1, 2012
    Inventors: Ian C. Schoenhofen, Susan M. Logan
  • Publication number: 20120041185
    Abstract: Provided is a dTDP-?-D-fucofuranose, which is also referred to as dTDP-?-6-deoxy-D-galactofuranose. The dTDP-?-D-fucofuranose is synthesized by using reductase Fcf1 and mutase Fcf2 in the gram-negative bacteria. Also provided are the preparation method of the dTDP-?-D-fucofuranose and use of the dTDP-?-D-fucofuranose for manufacturing a medicament for the treatment of tumors.
    Type: Application
    Filed: September 14, 2007
    Publication date: February 16, 2012
    Applicant: TIANJIN BIOCHIP TECHNOLOGY CORPORATION
    Inventors: Lei Wang, Quan Wang, Lu Feng
  • Publication number: 20110257376
    Abstract: Methods are provided for labeling cellular glycans bearing azide groups via fluorescent labeling comprising Cu(I)-catalyzed [3+2] cycloaddition of a probe comprising alkynyl group. Generation of fluorescent probes from a nonfluorescent precursor, 4-ethynyl-N-ethyl-1,8-naphthalimide, by Cu(I)-catalyzed [3+2] cycloaddition of the alkyne group of the probe to an azido-modified sugar are provided. Incorporation of azido-containing fucose analog into glycoconjugates via the fucose salvage pathway are disclosed. Fluorescent visualization of fucosylated cells by flow cytometry of cells treated with 6-azidofucose labeled with click-activated fluorogenic probe or biotinylated alkyne is disclosed. Visualization of intracellular location of fucosylated glycoconjugates by fluorescence microscopy are disclosed.
    Type: Application
    Filed: March 21, 2011
    Publication date: October 20, 2011
    Applicant: ACADEMIA SINICA
    Inventors: Chi-Huey Wong, Tsui-Ling Hsu, Sarah R. Hanson, Masaaki Sawa
  • Publication number: 20110229918
    Abstract: The invention relates to a precursor for producing sintered metallic components, a method for producing the precursor and the production of the components. The object of the invention is to disclose possibilities of being able to produce sintered metallic components, which render possible an increased physical density and a reduced shrinkage on the fully sintered component. With a precursor according to the invention for the production of sintered metallic components, a coating layer is formed on a core, which is formed from respectively one particle of a first metallic powder. The coating layer is formed with a second powder and a binder. The first powder thereby has a particle size d90 of at least 50 ?m and the second powder has a particle size d90 of less than 25 ?m. The precursor is powdery.
    Type: Application
    Filed: November 7, 2008
    Publication date: September 22, 2011
    Applicant: COVALYS BIOSCIENCES AG
    Inventors: Nicole Schneider-Han-Marra, Andreas Brecht
  • Publication number: 20110177029
    Abstract: The present invention provides covalent conjugates between a polypeptide and a modifying group, such as a water-soluble polymer (e.g., PEG). The amino acid sequence of the polypeptide includes one or more O-linked glycosylation sequence, each being a substrate for a GIcNAc transferase. The modifying group is covalently linked to the polypeptide via a glycosyl-linking group interposed between and covalently linked to both the polypeptide and the modifying group. In one embodiment, a glucosamine linking group is directly attached to an amino acid residue of the O-linked glycosylation sequence. The invention further provides methods of making polypeptide conjugates. The present invention also provides non-naturally occurring polypeptides that include at least one O-linked linked glycosylation sequence of the invention, wherein each glycosylation sequence is a substrate for a GIcNAc transferase. The invention further provides pharmaceutical compositions that include a polypeptide conjugate of the invention.
    Type: Application
    Filed: June 4, 2008
    Publication date: July 21, 2011
    Applicant: NOVO NORDISK A/S
    Inventor: Shawn DeFrees
  • Publication number: 20110137023
    Abstract: The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method a nucleophile is first dissolved in a non-aqueous solvent and dried, and a cyclosaligenyl phosphate compound is subsequently added to the solution.
    Type: Application
    Filed: August 6, 2009
    Publication date: June 9, 2011
    Applicant: Universitaet Hamburg
    Inventors: Chris Meier, Saskia Wolf, Svenja Warnecke
  • 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: 20110014196
    Abstract: The invention relates to compounds comprising a plurality of enzyme substrates suitably linked and further carrying one or more cargo entities. In particular such compounds have the structure (substrate)n-linker-(cargo)m wherein “substrate” is a substrate specific for an enzyme-type protein; n is 2 or more; “linker” is a linking unit consisting of 1 to 300 atoms; “cargo” is a drug, a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraphy, or a functional group which can be transformed into a drug or a detectable label; and m is 1 or more. The invention further relates to a corresponding molecular shuttles having the structure (fusion protein)n-linker-(cargo)m wherein “fusion protein” is a proteinaceous binding entity fused to an enzyme-type protein for which specific substrates exist. The proteinaceous binding entity is designed to bind to a target structure in vitro or in vivo, for example a cellular receptor.
    Type: Application
    Filed: October 2, 2008
    Publication date: January 20, 2011
    Applicant: COVALYS BIOSCIENCES AG
    Inventors: Andreas Brecht, Florent Beaufils
  • Publication number: 20110014216
    Abstract: The invention relates to coenzyme A (CoA) type compounds carrying one or more drug entities and optionally a label detectable by a fluorescence detector, magnetic resonance imaging (MRI), positron emission tomography (PET) or scintigraphy, and/or a functional group which can be transformed into a drug or a detectable label. The invention further relates to a molecular shuttle which is a fusion protein comprising a proteinaceous binding entity directed to a target and an acyl carrier protein (ACP) or a fragment thereof, and carrying one or more drug entities. The proteinaceous binding entity is designed to bind to a target structure in vitro or in vivo, for example a cellular receptor.
    Type: Application
    Filed: October 2, 2008
    Publication date: January 20, 2011
    Applicant: COVALYS BIOSCIENCES AG
    Inventors: Andreas Brecht, Florent Beaufils
  • Publication number: 20100016250
    Abstract: The present invention provides TLR9 agonists comprising, as an active ingredient, a compound represented by formula (I): (wherein a represents 0 or 1; n represents an integer of 0 to 2; m represents an integer of 0 to 5; X1 and X2 each independently represent a hydrogen atom or hydroxy; Y represents an oxygen atom or a sulfur atom; -Q1-represents —O— or the like; -Q2- represents —O— or the like; -Z- represents —O— or the like; R1, R3 and R4 each independently represent hydroxy or the like; R2 and R5 each independently represent a hydrogen atom, hydroxy or the like; and A represents 6-aminopurin-9-yl or the like) or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: April 13, 2007
    Publication date: January 21, 2010
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Hiroyuki Nagata, Michio Ichimura, Rieko Nakatsu, Shun-Ichi Ikeda, Ayako Kawabata, Toshio Ota, Masayuki Abe, Michio Takashima, Makoto Suzuki
  • Patent number: 7629328
    Abstract: Disclosed are methods for treating hepatitis C viral infections using deaza-purine compounds of Formula I: wherein W, W1, W2, Y, R1, Z, Y? and R are as defined herein.
    Type: Grant
    Filed: September 8, 2008
    Date of Patent: December 8, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Christopher D. Roberts, Jesse Keicher, Natalia B. Dyatkina
  • Patent number: 7629320
    Abstract: Disclosed are ?-D-ribofuranosyl-pyrazolo[3,4-d]pyrimidine compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Representative compounds include those having the general formula.
    Type: Grant
    Filed: May 19, 2008
    Date of Patent: December 8, 2009
    Assignee: SmithKline Beecham Corporation
    Inventors: Natalia B. Dyatkina, Christopher D. Roberts
  • Patent number: 7612047
    Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: November 3, 2009
    Assignee: Inspire Pharmaceuticals, Inc.
    Inventors: James G. Douglass, III, Benjamin R. Yerxa, Sammy R. Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean, José L. Boyer
  • Patent number: 7541455
    Abstract: A method for preparing a nucleic acid probe is provided. The method comprises forming an activated cytosine or cytidine by a bisulfite catalyzed reaction; and covalently linking a reporter molecule to the activated cytosine or cytidine, wherein said activating step, said covalently linking step, or both are conducted in the presence of microwave energy. Also provided by the invention are nucleic acid probes.
    Type: Grant
    Filed: December 21, 2004
    Date of Patent: June 2, 2009
    Assignee: Ventana Medical Systems, Inc.
    Inventors: Christopher Bieniarz, Michael Farrell, Jerome W. Kosmeder, Mark Lefever
  • Patent number: 7521432
    Abstract: Novel compositions and methods are provided for identifying agents which affect chromosomal stability and aging.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: April 21, 2009
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: John M. Denu, Kirk G. Tanner
  • Patent number: 7432248
    Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula I as follows: wherein W, W1, W2, Y, R1, Z, Y? and R are as defined herein.
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: October 7, 2008
    Assignee: Genelabs Technologies, Inc.
    Inventors: Christopher D. Roberts, Jesse Keicher, Natalia B. Dyatkina
  • Patent number: 7425547
    Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula IB as follows: and pharmaceutically acceptable prodrugs and salts thereof, where R, R1, R13, R14, W, W2, W3, Y and Z are as defined herein.
    Type: Grant
    Filed: September 30, 2003
    Date of Patent: September 16, 2008
    Assignee: Genelabs Technologies, Inc.
    Inventors: Christopher Don Roberts, Natalia B. Dyatkina
  • Publication number: 20080214800
    Abstract: Methods of treating sirtuin related disorders and compounds useful in treating sirtuin related disorders are described.
    Type: Application
    Filed: September 10, 2007
    Publication date: September 4, 2008
    Inventors: Manuel A. Navia, Jeffrey O. Saunders
  • Patent number: 7414031
    Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus.
    Type: Grant
    Filed: November 15, 2005
    Date of Patent: August 19, 2008
    Assignee: Genelabs Technologies, Inc.
    Inventors: Jesse D. Keicher, Christopher D. Roberts, Natalia B. Dyatkina
  • Patent number: 7371852
    Abstract: Alkyl-linked nucleotide non-homogeneous solid supports and nucleotide affinity media comprising an alkyl-linked nucleotide are provided. The linker is generally a hydrophobic linker that can be a 3, 4, 5, 6, 7, 8, 9, 10, or a longer carbon chain. Also included in the invention are methods for synthesis of an alkyl-linked nucleotide, nucleotide affinity media and methods of use thereof for affinity chromatography and screening methods.
    Type: Grant
    Filed: January 21, 2004
    Date of Patent: May 13, 2008
    Assignee: Serenex, Inc.
    Inventors: Klass P. Hardeman, Steven E. Hall, Roy W. Ware, Lindsay A. Hinkley, Matthew G. Jenks
  • Patent number: 7291606
    Abstract: Novel compositions and methods are provided for identifying agents which affect chromosomal stability and aging.
    Type: Grant
    Filed: November 13, 2001
    Date of Patent: November 6, 2007
    Assignee: Wisconson Alumni Research Foundation
    Inventors: John M. Denu, Kirk G. Tanner
  • Patent number: 7247721
    Abstract: Surfaces containing high purity silica (silicon dioxide) exhibit high loading potential for nucleic acids. Formulations containing nucleic acids and materials which mask the electrostatic interactions between the nucleic acids and surfaces are disclosed. By masking the phosphate charges of the nucleic acids, undesired interactions may be minimized or eliminated, thereby allowing the covalent bonding of the nucleic acids to the surface to proceed. The use of such formulations additionally minimizes nonspecific binding of the nucleic acids to the surface. Examples of materials to be included in such formulations include cations, xanthines, hexoses, purines, arginine, lysine, polyarginine, polylysine, and quaternary ammonium salts.
    Type: Grant
    Filed: February 14, 2005
    Date of Patent: July 24, 2007
    Inventor: Mark B. Lyles
  • Patent number: 7244713
    Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula I as follows: wherein, T, Y, W, W1 and W2 are as defined herein.
    Type: Grant
    Filed: October 21, 2004
    Date of Patent: July 17, 2007
    Assignee: Genelabs Technologies, Inc.
    Inventors: Christopher D. Roberts, Jesse D. Keicher, Natalia B. Dyatkina
  • Patent number: 7202223
    Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula I as follows: wherein, each of R, Y, W, W1 and W2 are as defined herein.
    Type: Grant
    Filed: June 4, 2004
    Date of Patent: April 10, 2007
    Assignee: Genelabs Technologies, Inc.
    Inventors: Christopher D. Roberts, Jesse D. Keicher
  • Patent number: 7157434
    Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula I as follows: wherein, Y, W, W1 and W2 are as defined herein.
    Type: Grant
    Filed: October 20, 2004
    Date of Patent: January 2, 2007
    Assignee: Genelabs Technologies, Inc.
    Inventors: Jesse D. Keicher, Christopher D. Roberts, Natalia B. Dyatkina