The Phosphorus Is Part Of A Ring Patents (Class 536/26.11)
  • Patent number: 9504705
    Abstract: Described herein is a combination that includes compound (A) of the formula and compound (B) of the formula or a pharmaceutically acceptable salt(s) of the foregoing, for ameliorating and/or treating a hepatitis C viral infection.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: November 29, 2016
    Assignee: Alios BioPharma, Inc.
    Inventors: Julie Krop, Margaret James Koziel, Lawrence M. Blatt, John Fry, Sushmita Mukherjee Chanda
  • Publication number: 20150080457
    Abstract: The present invention provides nucleosides and oligonucleotides comprising a 5? phosphate mimics of formula (IVc) or (Vc), One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such dinucleotide of formula (Ia). 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: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Muthiah MANOHARAN, Kallanthottathil G. RAJEEV, Marija PRHAVC, Ivan ZLATEV
  • Patent number: 8846638
    Abstract: The present invention provides nucleoside phosphoramidate compounds of Formula I, where R1, R2a, R2b, R3, R4, R5a, R5b, R6, R7, R8a, R8b, M and W are as defined herein. The invention further includes pharmaceutical compositions comprising a compound of Formula I, methods of use of these compounds for treating a viral infection, and methods of producing these compounds.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: September 30, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yat Sun Or, Jun Ma, Guoqiang Wang
  • Patent number: 8772474
    Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: July 8, 2014
    Assignee: Alios BioPharma, Inc.
    Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
  • Patent number: 8759510
    Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: June 24, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Ganapati Reddy Pamulapati, Bruce S. Ross, Michael Joseph Sofia
  • Patent number: 8716263
    Abstract: A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: May 6, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Byoung-Kwon Chun, Jinfa Du, Suguna Rachakonda, Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Wonsuk Chang, Hai-Ren Zhang, Dhanapalan Nagarathnam
  • Patent number: 8629265
    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: Grant
    Filed: August 6, 2009
    Date of Patent: January 14, 2014
    Assignee: Universitaet Hamburg
    Inventors: Chris Meier, Saskia Wolf, Svenja Warnecke
  • Patent number: 8507460
    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.
    Type: Grant
    Filed: October 12, 2012
    Date of Patent: August 13, 2013
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Dominique Surleraux, Cyril B. Dousson, Christophe Claude Parsy
  • Publication number: 20130184450
    Abstract: A method for preparing a phosphorothioate RNA based on the oxazaphospholidine method, wherein cyanoethoxymethyl group is used instead of tert-butyldimethylsilyl group as a protective group of 2?-hydroxyl group of RNA.
    Type: Application
    Filed: March 4, 2011
    Publication date: July 18, 2013
    Applicant: THE UNIVERSITY OF TOKYO
    Inventors: Takeshi Wada, Yohei Nukaga
  • Publication number: 20130178612
    Abstract: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.
    Type: Application
    Filed: September 22, 2011
    Publication date: July 11, 2013
    Applicant: CHIRALGEN, LTD.
    Inventors: Takeshi Wada, Mamoru Shimizu
  • Patent number: 8450293
    Abstract: The invention provides analogs cyclic diguanosine monophosphate (c-di-GMP) having different substituents at the guanine C8 position.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: May 28, 2013
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Roger A. Jones, Elizabeth Veliath
  • Publication number: 20120237480
    Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.
    Type: Application
    Filed: March 16, 2012
    Publication date: September 20, 2012
    Inventors: YAT SUN OR, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
  • Publication number: 20120165286
    Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.
    Type: Application
    Filed: December 20, 2011
    Publication date: June 28, 2012
    Applicant: ALIOS BIOPHARMA, INC.
    Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
  • Publication number: 20120157511
    Abstract: The present invention provides nucleosides and oligonucleotides comprising a 5? phosphate mimics of formula (IVc) or (Vc). One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such dinucleotide of formula (Ia). 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: July 7, 2010
    Publication date: June 21, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Marija Prhavc, Ivan Zlatev
  • Patent number: 8173621
    Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: May 8, 2012
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Ganapati Reddy Pamulapati, Bruce S. Ross, Michael Joseph Sofia
  • Patent number: 8153787
    Abstract: The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: April 10, 2012
    Assignees: K.U. Leuven Research & Development, Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech Republic
    Inventors: Antonin Holy, Marcela Krecmerova, Alois Piskala, Graciela Andrei, Robert Snoeck, Erik De Clercq, Johan Neyts, Lieve Naesens
  • Publication number: 20110212437
    Abstract: Methods, Compositions, and Systems are provided for nucleic acid sequencing where the sequential incorporation of nucleotides uses two distinct chemical steps. A plurality of nucleotide analogs, each having a labeled leaving group at its 3? hydroxyl can be sequentially added to a growing strand in the presence of a selective cleaving activity that cleaves the 3? hydroxyl leaving group preferentially after it has been incorporated. The selective cleaving agent can comprise an exonuclease activity, and the exonuclease activity can be a polymerase-associated exonuclease activity. Nucleotide analogs having labels on both a cleavable polyphosphate portion and on a 3? hydroxyl leaving group can provide signals characteristic of nucleotide analog incorporation. Systems having illumination optics, collection optics, and substrates observe signals from the labels as they are being incorporated into a growing nucleic acid strand, allowing for the sequencing of template nucleic acids.
    Type: Application
    Filed: February 8, 2011
    Publication date: September 1, 2011
    Applicant: Pacific Biosciences of California, Inc.
    Inventors: Robin Emig, Lei Jia, Jeremiah Hanes, Lubomir Sebo
  • Patent number: 7217815
    Abstract: Various 2?-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and combinatorial library approaches. Contemplated compounds are particularly useful as therapeutic agents, and especially as antiviral agents.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: May 15, 2007
    Assignee: Valeant Pharmaceuticals North America
    Inventors: Haoyun An, Yili Ding, Stephanie Z. Shaw, Zhi Hong
  • Patent number: 6965041
    Abstract: The present invention provides a compound of formula (I), (II), or (III), wherein R1, R2, R2?, R3, and R3? are the same or different and each is H an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl, or an aralkyl. Alternatively, either of R2 or R2? combined with either of R3 or R3? comprises a ring. R4 is a protecting group or a solid support R5 is H or an alkyl. R6 is a protecting group, an amidoalkyl, an alkyl, an alkyl ketone, an alkenyl, an alkynyl, a cycloalkyl, an aryl, or an aralkyl. R15 is H or a protecting group. Q and Q1 are the same or different and each is a nucleoside, an oligonucleotide comprising a nucleoside, or an oligomer comprising a nucleoside, which is of formula (a) or (b), wherein B is a labeling group, an alkyl, an alkenyl, an alkynyl, a cyclic group optionally containing one or more heteroatoms, or an amino; and, E is H, a halogen, a hydroxy, an alkoxy, an ester, an amino or a protecting group. X and X1 are independently O, S, or Se, and n is an integer from 1 to about 300.
    Type: Grant
    Filed: February 16, 2000
    Date of Patent: November 15, 2005
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventors: Serge L. Beaucage, Andrzej Wilk, Andrzej Grajkowski
  • Patent number: 6875859
    Abstract: The invention concerns compounds of the general formula (I) in which the residues R1 to R7 have the meanings given in the application as well as methods for their preparation.
    Type: Grant
    Filed: March 11, 2002
    Date of Patent: April 5, 2005
    Assignee: Roche Diagnostics GmbH
    Inventors: Klaus M├╝hlegger, Herbert Von Der Eltz
  • Patent number: 6812342
    Abstract: The present invention is directed to the field of organic chemistry in general and specifically to the preparation of hydrophobic derivatives of cyclic ADP ribose. One form of the present invention is the composition of one or more hydrophobic derivatives of cyclic ADP ribose. In another form of the present invention, a method for preparing a hydrophobic composition is described. Compositions of the present invention are useful for the study of in vivo calcium metabolism.
    Type: Grant
    Filed: June 20, 2002
    Date of Patent: November 2, 2004
    Assignee: Board of Regents, The University of Texas System
    Inventor: Wen Hong Li
  • Patent number: 6593307
    Abstract: The present invention provides a compound of formula I: wherein A, D, R1, and R2 are as defined in the specification; or a salt or a detectably labeled derivative thereof. The invention also provides methods of using the compound of formula I or a salt or a detectably labeled derivative thereof for promoting the proliferation of hemopoietic progenitor cells without cell differentiation.
    Type: Grant
    Filed: October 27, 2000
    Date of Patent: July 15, 2003
    Assignee: Regents of the University of Minnesota
    Inventors: Timothy F. Walseth, Antonio De Flora, Elena Zocchi, Marina Podesta, Long Wong, Robert A. Aarhus, Hon Cheung Lee
  • Publication number: 20030114660
    Abstract: Methods and Intermediates for the Preparation of Oligomers Containing Diastereomerically Enriched Phosphorothioate Linkages are Disclosed.
    Type: Application
    Filed: September 24, 2002
    Publication date: June 19, 2003
    Inventors: George Just, Zhili Xin, Eric Marsault, Yi Jin, Jianchao Wang
  • Publication number: 20030013869
    Abstract: The present invention is directed to the field of organic chemistry in general and specifically to the preparation of hydrophobic derivatives of cyclic ADP ribose. One form of the present invention is the composition of one or more hydrophobic derivatives of cyclic ADP ribose. In another form of the present invention, a method for preparing a hydrophobic composition is described. Compositions of the present invention are useful for the study of in vivo calcium metabolism.
    Type: Application
    Filed: June 20, 2002
    Publication date: January 16, 2003
    Inventor: Wen Hong Li