Chalcogen Bonded Directly To The 2- And 4-positions Of The Diazine Ring (e.g., Uridine, Etc.) Patents (Class 536/28.53)
  • Patent number: 11124536
    Abstract: This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside 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, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.
    Type: Grant
    Filed: January 27, 2020
    Date of Patent: September 21, 2021
    Assignee: Tufts University
    Inventors: Philip G. Haydon, Jinbo Lee
  • Patent number: 10544183
    Abstract: This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside 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, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: January 28, 2020
    Assignee: TUFTS UNIVERSITY
    Inventors: Philip G. Haydon, Jinbo Lee
  • Patent number: 9885352
    Abstract: A delivery system for a sensor chip includes a plurality of selectable ports arranged on a first assembly. Each of the selectable ports is in communication with a separate channel. The delivery system includes a second assembly movable in relation to the first assembly. The second assembly has a channel that is mechanically connectable to different ones of the plurality of selectable ports on the first assembly by motion of the second assembly relative to the first assembly. The delivery system includes a mechanical interface configured to engage a separate actuator so that relative motion of the first assembly and the second assembly is affected by the actuator.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: February 6, 2018
    Assignee: Genia Technologies, Inc.
    Inventor: Robert A. Yuan
  • Publication number: 20150141365
    Abstract: The present invention relates to compounds of the formula I: including any possible stereoisomers thereof, wherein R9 has the meaning as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Application
    Filed: May 24, 2013
    Publication date: May 21, 2015
    Applicant: Janssen R&D Ireland
    Inventors: Ioannis Nicolaos Houpis, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
  • Patent number: 9012428
    Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: April 21, 2015
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Publication number: 20150105341
    Abstract: Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 16, 2015
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Marija Prhavc, Christian Andreas Jekle, Jerome Deval
  • Patent number: 9006209
    Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: April 14, 2015
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
  • Publication number: 20150094462
    Abstract: A novel method of simultaneously protecting two functions which are same or different, namely hydroxyl, amine, or thiol ones, particularly in sugars, polyalcohols, nucleosides, nucleotides, peptides, and nucleic acids during an organic synthesis, and to novel compounds for implementing this method, as well as to the method of obtaining these compounds. Method of simultaneously protecting two hydroxyl, amine, or thiol functions according to the invention by carrying out a protecting reaction between a compound having at least two free hydroxyl, amine, or thiol groups, and the disilane of formula 1, where R stands for Cl or Br, or I, or a substituent of formula 2, where X1, X2, X3, X4 are the same or different.
    Type: Application
    Filed: April 23, 2013
    Publication date: April 2, 2015
    Inventors: Wojciech Tadeusz Markiewicz, Marcin Krzysztof Chmielewski, Sylwia Maria Musial, Hieronim Franciszek Maciejewski, Grzegorz Hreczycho
  • Patent number: 8951988
    Abstract: The invention provides the Zidovudine-conjugated quinoline compound N-((1-(2-(hydroxy-methyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-tetrahydrofuran-3-yl)-1H-1,2,3-triazol-4-yl)methyl)-6-(4b,8,8-trimethyl-4b,5,6,7,8,8a-hexahydrodibenzo[a,c]phenazin-2-yloxy)hexanamide. The compound can selectively kill hepatoma cells, especially hepatoma cells with hepatitis B, and inhibit the growth of subcutaneous tumors in mice, but has no significant toxicity to normal liver cells. Experiments confirm that the compound has an anti-hepatoma effect and can be used in preparation of anti-hepatoma drugs.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: February 10, 2015
    Assignee: Huazhong University of Science and Technology
    Inventor: Qibing Zhou
  • Publication number: 20150005251
    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 paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 1, 2015
    Inventors: Natalia Dyatkina, Guangyi Wang, Leonid Beigelman, Vivek Kumar Rajwanshi
  • 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: 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: 20140323427
    Abstract: The present invention relates to the new indications of chronic obstructive pulmonary disease (COPD) and idiophathic lung fibrosis (IPF) for uridine and uridine analogues.
    Type: Application
    Filed: July 24, 2012
    Publication date: October 30, 2014
    Applicant: Universitaetsklinikum Freiburg
    Inventors: Marco Idzko, Stephan Sorichter
  • Publication number: 20140309412
    Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 16, 2014
    Inventors: Balkrishen Bhat, Anne B. El drup, Thazha P. Prakash, Phillip Dan Cook, Robert L. LaFemina, Amy L. Simcoe, Carrie A. Rutkowski, Mario A. Valenciano
  • Patent number: 8846636
    Abstract: The disclosure provides nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moieties with quaternary centers at the 3? position, the pharmaceutical formulations comprising the analogues, and methods of using the analogues and formulations for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: September 30, 2014
    Assignee: LCB Pharma Inc.
    Inventor: Yvan Guindon
  • Publication number: 20140275511
    Abstract: This invention relates to an improved method of purifying Nikkomycin Z, an antifungal compound shown to be particularly useful in treating Valley Fever, coccidioidomycosis. The improvement of this invention lies in the choice of resins and elution conditions, chosen to minimize handling of the material.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventor: David J. Larwood
  • Publication number: 20140256670
    Abstract: The invention provides Zidovudine conjugated quinoline compound N-((1-(2-(Hydroxy-methyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-tetrahydrofuran-3-yl)-1H-1,2,3-triazol-4-yl)methyl)-6-(4b,8,8-trimethyl-4b,5,6,7,8,8a-hexahydrodibenzo[a,c]phenazin-2-yloxy)hexanamide. The compound can selectively kills the hepatoma cells especially the hepatoma cells with hepatitis B, and inhibit the growth of subcutaneous tumors in mice, but has no significant toxicity to normal liver cells. Experiments confirm the compound has anti-hepatoma effect, and can be used in preparation of anti-hepatoma drugs.
    Type: Application
    Filed: June 15, 2012
    Publication date: September 11, 2014
    Applicant: Huazhong University of Science and Technology
    Inventor: Qibing Zhou
  • Publication number: 20140248241
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3?-deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Base1 and Base2 are as provided herein.
    Type: Application
    Filed: March 3, 2014
    Publication date: September 4, 2014
    Inventors: Alistair James STEWART, Adel M. MOUSSA, Benjamin Alexander MAYES, Francois-Rene ALEXANDRE, Dominique SURLERAUX, Christophe Claude PARSY, Claire PIERRA, David DUKHAN, Gilles GOSSELIN
  • Publication number: 20140235563
    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: April 30, 2014
    Publication date: August 21, 2014
    Applicants: Gilead Sciences, Inc., Gilead Pharmasset LLC
    Inventors: Michael Joseph Sofia, Jinfa Du
  • Patent number: 8809520
    Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 19, 2014
    Assignee: K.U. Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
  • Publication number: 20140219958
    Abstract: In one aspect, the invention provides compounds represented by Formula I, and pharmaceutically acceptable salts, esters, stereoisomers, tautomers, solvates, and combinations thereof, pharmaceutical compositions comprising these compounds and the use of these compounds for treating a viral infection in a subject.
    Type: Application
    Filed: January 31, 2014
    Publication date: August 7, 2014
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Jay R. Luly, Jun Ma, Guoqiang Wang, Yat Sun Or
  • 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
  • Publication number: 20140221304
    Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 10, 2012
    Publication date: August 7, 2014
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
  • Patent number: 8785620
    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: November 6, 2013
    Date of Patent: July 22, 2014
    Assignee: Tufts University
    Inventors: Philip Haydon, Jinbo Lee
  • Publication number: 20140179910
    Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: ALIOS BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
  • Publication number: 20140179627
    Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: ALIOS BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
  • Publication number: 20140154211
    Abstract: The present invention relates to 2?-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Substituted Nucleoside Derivative, and methods of using the 2?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: June 5, 2014
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Vishal Verma, Frank Bennett, Angela Kereles, Ashok Arasappan, Dmitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Publication number: 20140128339
    Abstract: The present invention relates to 2?-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2?-Methyl Substituted Nucleoside Derivative, and methods of using the 2?-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: October 15, 2013
    Publication date: May 8, 2014
    Inventors: Vinay Girijavallabhan, Stephane Bogen, Quang T. Truong, Ping Chen, Angela Kerekes, Frank Bennett, Sara Esposite, Qingmei Hong, Ian Davies
  • Patent number: 8710198
    Abstract: Caprazene is provided which is the compound represented by the following formula (I) wherein Me stands for methyl group, and a 5?-N-alkoxycarbonyl or 5?-N-aralkyloxycarbonyl derivative thereof, and wherein said compound has the 1H-NMR and 13C-NMR data as set forth in Table 15.
    Type: Grant
    Filed: December 29, 2008
    Date of Patent: April 29, 2014
    Assignee: Meiji Seika Pharma Co., Ltd.
    Inventors: Toshiaki Miyake, Masayuki Igarashi, Tetsuo Shitara, Yoshiaki Takahashi, Masa Hamada
  • Publication number: 20140066613
    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: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicant: TUFTS UNIVERSITY
    Inventors: Philip Haydon, Jinbo Lee
  • Publication number: 20140051846
    Abstract: Disclosed are O-protected compounds of the formula (I): wherein B is an optionally protected nucleobase, and R1-R3 are as described herein, a method of preparing such compounds, and a method of preparing oligonucleotides such as RNA starting from such compounds. The O-protected compounds have one or more advantages, for example, the 2?-O-protected compound is stable during the various reaction steps involved in oligonucleotide synthesis; the protecting group can be easily removed after the synthesis of the oligonucleotide, for example, by reaction with tetrabutylammonium fluoride; and/or the O-protected groups do not generate DNA/RNA alkylating side products, which have been reported during removal of 2?-O-(2-cyanoethyl)oxymethyl or 2?-O-[2-(4-tolylsulfonyl)ethoxymethyl groups under similar conditions.
    Type: Application
    Filed: March 29, 2012
    Publication date: February 20, 2014
    Applicant: TheUnited ofAmerica,asrepresentedbythe Secre -tary,Department ofHealthand Human Service
    Inventors: Serge L. Beaucage, Jacek Cieslak
  • Publication number: 20140045798
    Abstract: The present invention provides a compound of Formula Ia, wherein R1 is H or phosphate and the double bond is between N1 and C1 or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N1 C1, and N3 together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: Gencia Corporation
    Inventor: Shaharyar Khan
  • Patent number: 8633309
    Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: January 21, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
  • 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: 20140005369
    Abstract: The present invention relates to a new uridine nucleoside-based amphiphilic gadolinium complex and a magnetic resonance imaging (MRI) contrast agent including the gadolinium complex. The MRI contrast agent has high relaxivity, high binding affinity for and stability in human serum albumin, pH response, and high liver specificity.
    Type: Application
    Filed: March 15, 2012
    Publication date: January 2, 2014
    Applicants: KOREA BASIC SCIENCE INSTITUTE, KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATION
    Inventors: Jong-Seung Kim, Sankarprasad Bhuniya, Sumin Lee, Kwan Soo Hong, Hyunseung Lee, Hyeyoung Moon
  • Patent number: 8618075
    Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: December 31, 2013
    Assignee: Eisai Inc.
    Inventors: Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
  • Patent number: 8603999
    Abstract: Amphiphilic prodrugs of general formula A-X are disclosed, wherein A is a biologically active agent or may be metabolised to a biologically active agent; and X is selected from the group consisting of R, or up to three R moieties attached to a linker, Y1, Y2 or Y3, wherein R is selected from a group consisting of alkyl, alkenyl, alkynyl, branched alkyl, branched alkenyl, branched alkynyl, substituted alkyl, substituted alkenyl and substituted alkynyl groups and their analogues; Y1 is a linker group which covalently attached to an R group at one site and is attached to A at a further independent site; Y2 is a linker group which is covalently attached to two R groups at two independent sites and is attached to A at a further independent site; and Y3 is a linker group which is covalently attached to three R groups at three independent sites and is attached to A at a further independent site.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: December 10, 2013
    Assignee: Commonwealth Scientific and Industrial Research Organisation
    Inventors: Calum John Drummond, Sharon Marie Sagnella, Minoo Jalili Moghaddam, Xiaojuan Gong
  • 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: 20130323836
    Abstract: The present invention provides compounds of formula (1). 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: April 22, 2011
    Publication date: December 5, 2013
    Applicant: Isis Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Ivan Zlatev, Eric E. Swayze, Thazha P. Prakash, Walter F. Lima
  • 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: 20130303747
    Abstract: The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, and preparation methods and uses thereof. The structural formula is as shown (I). These compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.
    Type: Application
    Filed: September 2, 2011
    Publication date: November 14, 2013
    Inventors: Junbiao Chang, Haoyun An, Xuejun Yu, Xiaohe Guo
  • Publication number: 20130289266
    Abstract: We claim a simple strategy for the synthesis of a collection of C(3?)-spirodihydroisobenzo- furannulated and C(3?)-spirodihydroisobenzo-furannulated nucleosides featuring a [2+2+2]-cyclotrimerization as the key reaction. The cyclotrimerization reactions are facile with the unprotected nucleosides having a diyne unit. When both alkynes of the diyne are terminal, the regioselectivity is poor. However, when one of the terminal alkynes is additionally substituted, the cyclotrimerizations are highly diaste reoselective. Since the key bicycloannulation is the final step, this strategy provides flexibility in terms of the alkynes and is thus amenable for the synthesis of a focussed small molecule library.
    Type: Application
    Filed: December 27, 2011
    Publication date: October 31, 2013
    Applicant: Council of Scientific & Industrial Research
    Inventors: Venkata Ramana Chepuri, Mangesh Pandurang Dushing
  • Publication number: 20130281687
    Abstract: Disclosed herein are methods of preparing a phosphorothioate nucleotide analog, which are useful in treating diseases and/or conditions such as viral infections.
    Type: Application
    Filed: March 18, 2013
    Publication date: October 24, 2013
    Inventors: ALIOS BIOPHARMA, INC., VERTEX PHARMACEUTICALS INC.
  • Publication number: 20130203836
    Abstract: The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least on nucleoside of formula (2):Formula (1) and Formula (2). 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 31, 2011
    Publication date: August 8, 2013
    Applicants: ISIS PHARMACEUTICALS, INC., ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Kallanthottathil G. Rajeev, Muthiah Manoharan, Eric E. Swayze, Thazha P. Prakash
  • Patent number: 8492362
    Abstract: The present invention relates to prodrug forms of ?-L-1-[5-(E-2-Bromovinyl)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)]uracil (L-BHDU) and their use to treat viral infections of Varicella Zoster Virus, including recurrent VZV (shingles), especially including drug resistant Varicella Zoster Virus and related complications of this viral infection such as rash or post-herpetic neuralgia.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: July 23, 2013
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8481510
    Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: July 9, 2013
    Assignees: Janssen Products, LP, Medivir AB
    Inventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson, Koen Vandyck, Steven Maurice Van Hoof, Lili Hu, Abdellah Tahri
  • Publication number: 20130165400
    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.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: ALIOS BIOPHARMA, INC.
    Inventor: Alios BioPharma, Inc.
  • Patent number: 8461124
    Abstract: Conformationally locked 2?,4?-carbocylic nucleosides with improved thermal and nuclease stability are disclosed. Oligonucleotides incorporating the locked nucleosides, and methods of treating disease states, are also disclosed.
    Type: Grant
    Filed: March 11, 2008
    Date of Patent: June 11, 2013
    Inventor: Jyoti Chattopadhyaya