The Bicyclic Ring System Consists Of A 1,3-diazine Ring, Which May Be Hydrogenated, Fused To A Five-membered N-hetero Ring (e.g., Purine Isoesters Like Tubercidin, Toyocamycin, Sangivamycin, Sparsomycin A, Etc.) Patents (Class 536/27.2)
  • Patent number: 10040815
    Abstract: The present invention relates to compounds of formula (I), wherein R1, R2 and R3 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: July 11, 2016
    Date of Patent: August 7, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Dongdong Chen, Song Feng, Lu Gao, Chao Li, Baoxia Wang, Lisha Wang, Hongying Yun, Xiufang Zheng
  • Patent number: 9441008
    Abstract: The present invention relates to compounds of formula (I), wherein R1, R2 and R3 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: December 3, 2015
    Date of Patent: September 13, 2016
    Assignee: Hoffmann-LA Roche Inc.
    Inventors: Dongdong Chen, Song Feng, Lu Gao, Chao Li, Baoxia Wang, Lisha Wang, Hongying Yun, Xiufang Zheng
  • Patent number: 8987437
    Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: March 24, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Richard Hung Chiu Yu, Brandon Heath Brown, Richard P. Polniaszek, Benjamin R. Graetz, Keiko Sujino, Duong Duc-Phi Tran, Alan Scott Triman, Kenneth M. Kent, Steven Pfeiffer
  • Patent number: 8969545
    Abstract: Alkynyl-derivatized cap analogs, alkynyl-modified capped RNA, 1,4-disubstituted triazole-derivatized capped RNA, methods of preparation, methods of isolation, and uses thereof are provided. The “click” modification facilitates detection and isolation of capped RNAs and the 1,4-disubstituted triazole derivatives formed by the “click” reaction are useful for producing RNA transcripts and encoded protein.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: March 3, 2015
    Assignee: Life Technologies Corporation
    Inventors: Anilkumar R. Kore, Shanmugasundaram Muthian, Kyle Gee
  • Patent number: 8927520
    Abstract: The present invention relates to compounds of formula (I): wherein Rj, R2, R3, R4, Xi, X2, X3 and Z are as defined in claim 1. The compounds are useful in the prevention and/or treatment of bacterial infections.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: January 6, 2015
    Assignees: Institut Pasteur, Institut Curie
    Inventors: Sylvie Pochet, Gilles Labesse, Muriel Gelin, Liliane Assairi, Olivier Dussurget, Guillaume Poncet-Montange
  • Publication number: 20140303106
    Abstract: Compounds having methyltransferase inhibitory activity are disclosed. The compounds have the structure and are useful in the treatment of cancer and similar diseases associated with inappropriate methyltransferase activity.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Weihong Zheng, Minkui Luo, Glorymar del Valle Ibanzen Sanchez
  • Publication number: 20140256668
    Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.
    Type: Application
    Filed: May 23, 2013
    Publication date: September 11, 2014
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
  • Publication number: 20140235567
    Abstract: The present invention relates to 5?-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Derivative, and methods of using the 5?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 10, 2012
    Publication date: August 21, 2014
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Vinay Girijavallabhan, Stephane L. Bogen, Qun Dang, David B. Olsen
  • Publication number: 20140148403
    Abstract: The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is acetyl salicylic acid, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a such a co-crystal.
    Type: Application
    Filed: May 31, 2012
    Publication date: May 29, 2014
    Applicant: AstraZeneca UK Limited
    Inventors: Stephen David Cosgrove, David Thomas Jonaitis, Jonathan Charles Derrick Sutch
  • Publication number: 20140113282
    Abstract: Nucleosides and nucleotides are disclosed that are linked to detectable labels via a cleavable linker group.
    Type: Application
    Filed: December 2, 2013
    Publication date: April 24, 2014
    Applicant: ILLUMINA CAMBRIDGE LIMITED
    Inventors: SHANKAR BALASUBRAMANIAN, COLIN BARNES, XIAOHAI LIU
  • Publication number: 20140099283
    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 2?-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.
    Type: Application
    Filed: October 7, 2013
    Publication date: April 10, 2014
    Inventors: Gilles GOSSELIN, Christophe Claude PARSY, Francois-Rene ALEXANDRE, Houcine RAHALI, Jean-Francois GRIFFON, Julien MILHAU, Dominique SURLERAUX, Cyril B. DOUSSON, Claire PIERRA, Adel M. MOUSSA, Benjamin Alexander MAYES
  • Patent number: 8686130
    Abstract: The present invention relates to novel unnatural fluorescent nucleic acid bases, that is, a purine base, a 1-deazapurine base, and a 1,7-deazapurine base each having a functional group which consists of two or more heterocyclic moieties linked together, at the 6-position thereof (the 6-position of purine ring). The present invention also relates to a compound containing the unnatural base, a derivative thereof, and a nucleic acid containing a nucleotide having the unnatural base. The present invention also relates to a method of preparing the nucleic acid. The unnatural base of the present invention has excellent fluorescence characteristics and also has excellent properties as a universal base.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: April 1, 2014
    Assignees: Riken, Tagcyx Biotechnologies
    Inventors: Ichiro Hirao, Michiko Hirao, Shigeyuki Yokoyama, Tsuneo Mitsui
  • Publication number: 20140073597
    Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransferases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.
    Type: Application
    Filed: September 4, 2013
    Publication date: March 13, 2014
    Applicant: EPIZYME, INC.
    Inventors: Richard Chesworth, Kevin Wayne Kuntz, Edward James Olhava, Michael A. Patane
  • Publication number: 20140051654
    Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: October 16, 2013
    Publication date: February 20, 2014
    Applicant: EPIZYME, INC.
    Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott R. Daigle
  • Publication number: 20130338094
    Abstract: The present disclosure relates to compounds of formula (I-A) using the compounds wherein Ring A and the variables X, Y, R3a, R3b, R3c, R3d, R4, R5, R5?, and m are defined herein, to pharmaceutical compositions comprising the compounds, and methods of using the compounds.
    Type: Application
    Filed: May 23, 2013
    Publication date: December 19, 2013
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Stephen CRITCHLEY, Thomas G. Gant, Steven P. Langston, Edward J. Olhava, Stephane Peluso
  • Patent number: 8609627
    Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: December 17, 2013
    Assignees: RFS Pharma, LLC, Emory University
    Inventors: Jong Hyun Cho, Steven J. Coats, Raymond F. Schinazi, Hongwang Zhang, Longhu Zhou
  • Publication number: 20130310334
    Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, uses of the compounds and compositions as modulators of histone methyltransferases, and methods for treating diseases influenced by modulation of histone methyltransferase activity.
    Type: Application
    Filed: December 5, 2011
    Publication date: November 21, 2013
    Applicant: EPIZYME, INC.
    Inventors: Richard Chesworth, Kevin Wayne Kuntz, Edward James Olhava, Michael A. Patane
  • 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
  • Patent number: 8551966
    Abstract: 3-(2?,3?-dideoxy-ribo-?-L-furanosyl)[2,3-d]pyrimidin-2(3H)-one derivatives comprising 6-substitutents on the base moiety are shown to have anti-viral properties, particularly with respect to vaccinia and measles. The compounds have unnatural L ribose stereochemistry.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: October 8, 2013
    Assignee: University College Cardiff Consultants Limited
    Inventors: Christopher McGuigan, Joachim J. Bugert, Arwyn T. Jones, Ranjith Pathirana, Laura E. Farleigh
  • Patent number: 8551965
    Abstract: A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; R8 and R9 can be hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY2, where Y may be H, alkyl or halogens; X can be O, NH, S, N-alkyl, (CHR2)m where m is 1 to 10, and CY2; Z can be O, S, NH, or N-alkyl; U? is H and U? can be H or CH2; wherein: T can be OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2. or N3; T? and T? can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: October 8, 2013
    Assignees: University College Cardiff Consultants Limited, Rega Foundation
    Inventors: Christopher McGuigan, Jan Balzarini
  • Patent number: 8541569
    Abstract: The present invention provides building blocks and methods for synthesizing very pure RNA in a form that can efficiently be modified at the 3? end. Reverse RNA monomer phosphoramidites have been developed for RNA synthesis in 5??3? direction, leading to very clean oligo synthesis that allows for the introduction of various modifications at the 3?-end cleanly and efficiently. Higher coupling efficiency per step have been observed during automated oligo synthesis with the reverse RNA amidites disclosed herein, resulting in a greater ability to achieve higher purity and produce very long oligonucleotides. The use of the reverse RNA phosphoramidites in the synthetic process of this invention leads to oligonucleotides free of N+1 species.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: September 24, 2013
    Assignee: ChemGenes Corporation
    Inventors: Suresh C. Srivastava, Naveen P. Srivastava
  • Publication number: 20130237495
    Abstract: The present invention relates to a CDK-inhibiting pyrrolopyrimidinone carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing same as an active ingredient for preventing or treating liver cell cancer, and the composition containing the pyrrolopyrimidinone carboxamide derivative of the present invention suppresses the cell growth of SNU-354 cell, which is a liver cancer stem cell in humans, by inhibiting CDK1 and CDK2, and induces cell apoptosis of the cell by inhibiting CDK7 and CDK 7, and thus can be effective in use for preventing or treating liver cell cancer.
    Type: Application
    Filed: November 2, 2010
    Publication date: September 12, 2013
    Applicant: SNU R&DB FOUNDATION
    Inventors: Seung Ki Lee, Byeong Moon Kim, Seun Ju Cho, Young Jong Kim
  • Patent number: 8461128
    Abstract: Many pathogens, including Mycobacterium tuberculosis and Yersinia pestis, rely on an iron acquisition system based on siderophores, secreted iron-chelating compounds with extremely high Fe(III) affinity. The compounds of the invention are inhibitors of domain salicylation enzymes, which catalyze the salicylation of an aroyl carrier protein (ArCP) domain to form a salicyl-ArCP domain thioester intermediate via a two-step reaction. The compounds include the intermediate mimic 5?-O—[N-(salicyl)sulfamoyl]-adenosine (salicyl-AMS) and analogs thereof. These compounds are inhibitors of the salicylate activity of MbtA, YbtE, PchD, and other domain salicylation enzymes involved in the biosynthesis of siderophores. Therefore, these compounds may be used in the treatment of infection caused by microorganisms which rely on siderphore-based iron acquisition systems.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: June 11, 2013
    Assignees: Sloan-Kettering Institute for Cancer Research, Cornell Research Foundation, Inc.
    Inventors: Derek Shieh Tan, Luis E. N. Quadri, Jae-Sang Ryu, Justin Scott Cisar, Julian Alberto Ferreras, Xuequan Lu
  • Patent number: 8440812
    Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: May 14, 2013
    Assignee: Nogra Pharma Limited
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Publication number: 20130078217
    Abstract: The present invention relates to 2?-chloroacetylenyl-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.
    Type: Application
    Filed: September 21, 2012
    Publication date: March 28, 2013
    Inventors: Guoqiang Wang, In Jong Kim, Yat Sun Or
  • Publication number: 20130018010
    Abstract: The present invention relates to polymeric conjugates of adenine nucleoside analogs. In particular, the invention relates to multi-arm polyethylene glycol conjugates of adenine nucleoside analogs and use thereof. The present invention, more specifically, provides polymeric conjugates of toyocamycin and its derivatives. Furthermore, the present invention provides a method for preparing the polymeric conjugates of adenine nucleoside analogs and a method of using the same for treating a cancer, inhibiting the growth or proliferation of cancer cells, treating a viral infection, treating a disease or condition associated with abnormal expression of VEGF. Most polymeric conjugates of toyocamycin was stable in PBS but released toyocamycin in vivo to provided inhibition of cancer cell growth.
    Type: Application
    Filed: April 15, 2011
    Publication date: January 17, 2013
    Applicant: ENZON PHARMACEUTICALS, INC.
    Inventors: Hong Zhao, Jing Xia
  • Publication number: 20120258927
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: June 19, 2012
    Publication date: October 11, 2012
    Applicant: Millenium Pharmaceuticals, Inc.
    Inventors: Steven P. Langston, Edward J. Olhava, Stepan Vyskocil
  • Patent number: 8278282
    Abstract: This invention relates to novel compounds that have various medicinal applications, e.g. for the treatment and/or prevention of viral infections.
    Type: Grant
    Filed: February 7, 2008
    Date of Patent: October 2, 2012
    Assignee: Novartis AG
    Inventors: Zheng Yin, Jeyaraj Duraiswamy, Yen Liang Chen
  • Publication number: 20120232029
    Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
    Type: Application
    Filed: December 13, 2011
    Publication date: September 13, 2012
    Applicant: Pharmasset, Inc.
    Inventors: MICHAEL JOSEPH SOFIA, Jinfa Du
  • Patent number: 8258115
    Abstract: The present invention refers to new salts of S-adenosyknethionine (SAMe) with improved stability and containing at least 70% by weight of SAMe.
    Type: Grant
    Filed: October 22, 2007
    Date of Patent: September 4, 2012
    Assignee: Gnosis SpA
    Inventors: Ermanno Valoti, Daniele Giovannone, Marco Berna
  • Publication number: 20120190838
    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: Application
    Filed: March 2, 2012
    Publication date: July 26, 2012
    Applicant: BASECLICK GMBH
    Inventors: Thomas CARELL, Anja SCHWOEGLER, Glenn A. BURLEY, Johannes GIERLICH, Mohammad Reza MOFID
  • Publication number: 20120172582
    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: Application
    Filed: March 2, 2012
    Publication date: July 5, 2012
    Applicant: BASECLICK GMBH
    Inventors: Thomas CARELL, Anja SCHWÖGLER, Glenn A. BURLEY, Johannes GIERLICH, Mohammad Reza MOFID
  • Publication number: 20120142625
    Abstract: The present invention relates to substituted purine and 7-deazapurine compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Application
    Filed: December 2, 2011
    Publication date: June 7, 2012
    Applicant: EPIZYME, INC.
    Inventors: Edward J. Olhava, Richard Chesworth, Kevin W. Kuntz, Victoria M. Richon, Roy M. Pollock, Scott R. Daigle
  • Patent number: 8188055
    Abstract: Disclosed are compounds that are AGT inactivators that include a folate residue, e.g., a compound of formula (I), wherein X1, X2, R1, and R2 are as described herein. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells and inactivating AGT in a tumor cell. The methods comprise, inter alia, administering a compound or pharmaceutically acceptable salt of formula (I).
    Type: Grant
    Filed: March 12, 2008
    Date of Patent: May 29, 2012
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, The Penn State Research Foundation
    Inventors: Robert C. Moschel, Matthew Karl Moschel, legal representative, Anthony E. Pegg, Sahar Javanmard, Natalia Loktionova, Gary Pauly
  • Patent number: 8173797
    Abstract: The present invention is directed to new therapeutic compounds isolated from spider venom and methods of using these new compounds. The compounds are sulfated nucleoside derivatives including ribonucleoside mono- and disulfates derived from guanine, adenosine, and cytidine. Some of these compounds are glycosylated or fucosylated bearing one or more sugar residues.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: May 8, 2012
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Jerrold Meinwald, Andrew Edmund Taggi, Frank Clemens Schroeder
  • Patent number: 8153781
    Abstract: Disclosed are conjugates comprising a dendrimer and a ligand, which is a functionalized congener of an agonist or antagonist of a receptor of the G-protein coupled receptor (GPCR) superfamily, for example, wherein the functionalized congener is an A1 adenosine receptor agonist having a purine nucleoside moiety and a functional group at the N6 position of the purine nucleoside moiety, wherein the functional group has the formula (I): N6H—Ar1—CH2—C(?O)NH—R1 (I), wherein Ar1 and R1 as defined herein. Also disclosed are pharmaceutical compositions, methods of treating various diseases, and a diagnostic method employing such conjugates.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: April 10, 2012
    Assignees: The United States of America as represented by the Secretary, Department of Health and Human Services, Inserm
    Inventors: Kenneth A. Jacobson, Yoonkyung Kim, Athena Klutz, Beatrice Hechler, Christian Gachet
  • Patent number: 8114986
    Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).
    Type: Grant
    Filed: July 24, 2006
    Date of Patent: February 14, 2012
    Assignee: Giuliani International Limited
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Patent number: 8097718
    Abstract: The invention is directed to 3,5-disubstituted and 3,5,7-trisubstituted-3H-oxazolo and 3H-thiazolo[4,5-d]pyrimidin-2-one compounds and prodrugs thereof that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and pharmaceutical compositions containing them, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds and prodrugs.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: January 17, 2012
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Gregory J. Haley, Joseph R. Lennox, Alan X. Xiang, Erik J. Rueden
  • Publication number: 20120010164
    Abstract: Compounds of structural formula (I): and pharmaceutically acceptable salts thereof; as defined herein, are described for use in the prevention and/or treatment of HCV infections. Novel compounds of the formula (I) and pharmaceutical formulations containing them are also described.
    Type: Application
    Filed: January 19, 2010
    Publication date: January 12, 2012
    Inventors: Vincenzo Surnma, Maria Emilia Di Francesco, Marco Pompei
  • Publication number: 20110306573
    Abstract: Compounds of structural formula (I): and pharmaceutically acceptable salts thereof; wherein R1; R2; R3; Q1 and Q2 are as defined herein, processes for their preparation; pharmaceutical compositions containing them and their use in medicine, in particular the treatment or prevention of HCV infections, are disclosed.
    Type: Application
    Filed: September 2, 2009
    Publication date: December 15, 2011
    Inventors: Salvatore Avolio, Maria Emilia Di Francesco, Marco Pompei, Vincenzo Summa
  • Publication number: 20110275124
    Abstract: This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions of matter that comprise triphosphates of modified 2?-deoxynucleosides and oligonucleotides that are formed when these are appended to the 3?-end of a primer, wherein said modifications comprise NH2 moiety attached to their 3?-hydroxyl group and a fluorescent species in a form of a tag affixed to the nucleobase via a linker that can be cleaved. Such compositions and their associated processes enable and improve the sequencing of oligonucleotides using a strategy of cyclic reversible termination, as outlined in U.S. Pat. No. 6,664,079. Most specifically, the invention concerns compositions of matter that are 5?-triphosphates of ribo- and 2?-deoxyribonucleosides carrying detectable tags and oligonucleotides that might be derived from them.
    Type: Application
    Filed: March 23, 2009
    Publication date: November 10, 2011
    Inventors: Steven A. Benner, Daniel Hutter, Nicole Aurora Leal, Fei Chen
  • Publication number: 20110275589
    Abstract: The invention is directed to 3,5-disubstituted and 3,5,7-trisubstituted-3H-oxazolo and 3H-thiazolo[4,5-d]pyrimidin-2-one compounds and prodrugs thereof that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and pharmaceutical compositions containing them, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds and prodrugs.
    Type: Application
    Filed: July 1, 2009
    Publication date: November 10, 2011
    Applicant: Anadys Pharmaceuticals, Inc.
    Inventors: Stephen E. Webber, Gregory J. Haley, Joseph R. Lennox, Alan X. Xiang, Erik J. Rueden
  • Publication number: 20110250699
    Abstract: The present teachings generally relate to fluorescent dyes, linkable forms of fluorescent dyes, energy transfer dyes, reagents labeled with fluorescent dyes and uses thereof.
    Type: Application
    Filed: June 21, 2011
    Publication date: October 13, 2011
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Ronald J. Graham, Ruiming Zou, Krishna G. Upadhya, Scott C. Benson
  • Patent number: 8034924
    Abstract: Crystals of a purine nucleoside compound, particularly crystals of 2?,3?-dideoxyinosine, which have excellent storage stability and have a concentration of phosphate attached to the crystal of 25 ppm or more, may be produce by: (1) preparing an aqueous solution containing phosphate ion (PO43?) and a purine nucleoside compound; and (2) crystallizing the purine nucleoside compound from the aqueous solution.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: October 11, 2011
    Assignee: Ajinomoto Co., Inc.
    Inventors: Masaki Naito, Yoshitomo Kimura, Hiroya Ueda, Minoru Harada
  • Patent number: 7999098
    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.
    Type: Grant
    Filed: December 11, 2006
    Date of Patent: August 16, 2011
    Assignee: Solulink Biosciences, Inc.
    Inventors: David A. Schwartz, Richard I. Hogrefe
  • Publication number: 20110171192
    Abstract: A compound represented by following general formula (I): wherein, represents a single bond or a double bond; L represents —NH— or the like; X1 represents N or C, provided that in the case where X1 is N, X2 represents C—R and in the case where X1 is C, X2 represents N—R1 or the like; Y's may be either the same or different and represent CH2 or the like; A represents a non-natural sugar residue represented by following general formula: wherein, m represents 0 to 1; represents a single bond or a double bond; X represents O or the like; R3 to R8 may be either the same or different and represent hydroxy group or the like; and B represents a group represented by following general formula: wherein, n and k represent 0 to 5; represents a single bond or a double bond; Z1 to Z16 may be either the same or different and represent CH or the like; R10 and R11 may be either the same or different and represent a lower alkoxy group having 1 to 5 carbon atoms or the like; and R15 represents a hydrogen atom or th
    Type: Application
    Filed: August 27, 2009
    Publication date: July 14, 2011
    Inventors: Hiroshi Tomiyama, Kazuo Tokuzaki, Yoshinori Iwai
  • Patent number: 7943759
    Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyrimidine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: May 17, 2011
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden, David Louis Clark, Alan Xin Xiang
  • Publication number: 20110091887
    Abstract: The present invention provides a method for detecting methylcytosine in DNA rapidly, conveniently, and with high sensitivity. The present invention relates to a method for detecting methylcytosine by using a methylcytosine photocoupling agent (a photoresponsive probe) consisting of nucleic acids having a group represented by the Formula (I), (II), (III) or (IV) as a base moiety.
    Type: Application
    Filed: March 11, 2009
    Publication date: April 21, 2011
    Applicants: JAPAN ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGY, JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Kenzo Fujimoto, Masayuki Ogino, Yuta Taya
  • Patent number: 7928085
    Abstract: The present disclosure relates to p-toluene sulfonic acid salt of 5-amino-3-(2?-O-acetyl-3?-deoxy-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and to its use in treating conditions such as viral infections, tumors, and cancer. Also disclosed is a method of preparing the p-toluene sulfonic acid salt of 5-amino-3-(2?-O-acetyl-3?-deoxy-?-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and methods for producing furanose compounds which are useful intermediates in the preparation of pharmaceutical compounds such as p-toluene sulfonic acid salt of 5-amino-3-(2?-O-acetyl-3?-deoxy-?-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.
    Type: Grant
    Filed: October 16, 2007
    Date of Patent: April 19, 2011
    Assignee: Anadys Pharmaceuticals, Inc.
    Inventors: David Kucera, Gregory J. Haley, Erik J. Rueden, Tingmin Wang, Fritz Blatter, Martin Viertelhaus
  • Publication number: 20110040083
    Abstract: The present invention provides a manufacturing method that can easily manufacture a compound known as photoresponsive (photocoupling) nucleic acids at high yield in a shorter period of time than that of the conventional technology. The present invention relates to a method of manufacturing a photoresponsive nucleic acid which includes a step of reacting a nucleic acid having groups represented by the Formula I, the Formula III, the Formula IV, or the Formula V and a compound represented by the Formula II, or reacting a nucleic acid having groups represented by the Formula VI, the Formula VIII, the Formula IX, or the Formula X and a compound represented by the Formula VII by heating them by microwaves in the presence of a metal catalyst, a basic substance, and a solvent.
    Type: Application
    Filed: February 13, 2009
    Publication date: February 17, 2011
    Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Kenzo Fujimoto, Masayuki Ogino, Yoshinaga Yoshimura