The N-hetero Ring Is A Diazine Or A Diazole Ring, Including Hydrogenated Patents (Class 536/26.14)
  • 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
  • Publication number: 20140356325
    Abstract: Compositions and methods relating to 2?-C-methyl nucleoside 5?-monophosphate derivative compounds are provided. In some embodiments, the novel compounds are useful to treat viral infections. In particular, 2?-C-methyl nucleoside 5?-monophosphate derivative compounds, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of viral infection are described.
    Type: Application
    Filed: January 8, 2013
    Publication date: December 4, 2014
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Lin Zhi, K. Raja Reddy, Mark David Erion, Scott Hecker
  • Publication number: 20140303108
    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: June 23, 2014
    Publication date: October 9, 2014
    Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
  • Publication number: 20140206640
    Abstract: The present invention relates to 2?-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: July 24, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Frank Bennett, Vishal Verma, Ashok Arasappan, Kevin X. Chen, Ying Huang, Angela Kerekes, Latha Nair, Dimitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • 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
  • Publication number: 20140161770
    Abstract: The present invention relates to 2?-Cyano Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Cyano Substituted Nucleoside Derivative, and methods of using the 2?-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: June 12, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Angela Kerekes, Frank Bennett, Ying Huang, Latha Nair, Dmitri Pissarnitski, Vishal Verma, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • 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: 20140155345
    Abstract: The invention provides new biotinylated compounds and methods for their use.
    Type: Application
    Filed: December 4, 2013
    Publication date: June 5, 2014
    Applicant: Rutgers, the State University of New Jersey
    Inventors: Roger A. Jones, Barbara L. Gaffney
  • Patent number: 8742094
    Abstract: The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method, a cyclosaligenyl nucleotide is produced first, to which a linker is added, which is used to perform the immobilization on a solid phase. A subsequent reaction with corresponding nucleophiles results in the desired phosphate-bridged nucleoside conjugates, which can then again be cleaved from the solid phase-bound linker.
    Type: Grant
    Filed: May 6, 2010
    Date of Patent: June 3, 2014
    Assignee: Universitaet Hamburg
    Inventors: Chris Meier, Viktoria Caroline Tonn
  • 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
  • Publication number: 20130315867
    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: Application
    Filed: May 21, 2013
    Publication date: November 28, 2013
    Inventors: Christophe Claude PARSY, Francois-Rene ALEXANDRE, Cyril B. DOUSSON, David DUKHAN, Gilles GOSSELIN, Houcine RAHALI, Dominique SURLERAUX
  • Publication number: 20130315864
    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: Application
    Filed: May 17, 2013
    Publication date: November 28, 2013
    Applicant: ENANTA PHARMACEUTICALS, INC.
    Inventors: Yat Sun Or, Jun Ma, Guoqiang Wang
  • 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
  • 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.
  • Publication number: 20120269725
    Abstract: Method of using androgen receptor and/or butyrylcholinesterase targeted radiolabeled compounds, e.g., cycloSalingenyl pyrimidine nucleoside monophosphates, for the treatment and diagnosis of cancer.
    Type: Application
    Filed: December 23, 2010
    Publication date: October 25, 2012
    Inventors: Janine Baranowska-Kortylewicz, Zbigniew P. Kortylewicz
  • Publication number: 20120263678
    Abstract: Provided are compounds of Formula I: nucleosides, nucleoside phosphates and prodrugs thereof, wherein R6 is CN, ethenyl, 2-haloethen-1-yl, or (C2-C8)-alkyn-1-yl. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.
    Type: Application
    Filed: April 13, 2012
    Publication date: October 18, 2012
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Aesop Cho, Choung U. Kim, Thorsten A. Kirschberg, Michael R. Mish, Neil Squires
  • Publication number: 20120258928
    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: Application
    Filed: April 5, 2012
    Publication date: October 11, 2012
    Applicant: GILEAD PHARMASSET LLC
    Inventors: JINFA DU, DHANAPALAN NAGARATHNAM, GANAPATI REDDY PAMULAPATI, BRUCE S. ROSS, MICHAEL JOSEPH SOFIA
  • 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: 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
  • Publication number: 20120116067
    Abstract: The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method, a cyclosaligenyl nucleotide is produced first, to which a linker is added, which is used to perform the immobilization on a solid phase. A subsequent reaction with corresponding nucleophiles results in the desired phosphate-bridged nucleoside conjugates, which can then again be cleaved from the solid phase-bound linker.
    Type: Application
    Filed: May 6, 2010
    Publication date: May 10, 2012
    Applicant: UNIVERSITAET HAMBURG
    Inventors: Chris Meier, Viktoria Caroline Tonn
  • Patent number: 8148349
    Abstract: The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection using the compounds of formula (I).
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: April 3, 2012
    Assignees: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.P.A., Merck Sharp & Dohme Corp.
    Inventors: Malte Meppen, Frank Narjes, Barbara Pacini, Cristina Gardelli, Philippe L. Durette
  • Publication number: 20120070415
    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: Application
    Filed: September 19, 2011
    Publication date: March 22, 2012
    Applicant: ALIOS BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
  • Publication number: 20120039845
    Abstract: Compounds having the formula I or II, wherein R1, R2, B, and V are as defined herein, are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Application
    Filed: October 26, 2011
    Publication date: February 16, 2012
    Applicant: METABASIS THERAPEUTICS, INC.
    Inventors: Scott J. HECKER, K. Raja REDDY, Zhili SUN, Brett C. BOOKSER, David Bernard SMITH
  • Publication number: 20110028705
    Abstract: The present invention relates to a method for stereoselective synthesis of phosphorus compounds, whereby in the first reaction step a chiral auxiliary on the phosphorus atom of phosphoryl chloride, thiophosphoryl chloride or phosphorus trichloride is covalently bonded, the product from the first reaction step is reacted in the following step with an alcohol, thiol, or amine as the nucleophile in the presence of a base, and in the last step the chiral auxiliary is displaced from the product of the following step by a nucleophile.
    Type: Application
    Filed: April 3, 2009
    Publication date: February 3, 2011
    Applicant: UNIVERSITAET HAMBURG
    Inventors: Chris Meier, Jens O. Thomann
  • Publication number: 20100305060
    Abstract: This application provides compositions or compounds as disclosed herein that are suitable for treating hepatic viral diseases, such as hepatitis C(HCV).
    Type: Application
    Filed: November 26, 2008
    Publication date: December 2, 2010
    Applicant: Ligand Pharmaceuticals Incorporated
    Inventors: Scott J. Hecker, K. Raja Reddy
  • Publication number: 20100297079
    Abstract: The present invention describes compounds of formulae I and II and methods for treating viral infection, such as Flaviviridae virus infection, including Hepatitis C infection (HCV).
    Type: Application
    Filed: May 20, 2010
    Publication date: November 25, 2010
    Applicant: Chimerix, Inc.
    Inventors: Merrick Almond, Ernest R. Lanier, David L. Musso, Roy Ware
  • Publication number: 20100068179
    Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses theroef, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.
    Type: Application
    Filed: November 24, 2009
    Publication date: March 18, 2010
    Applicant: Institut National de la Sante et de la Recherche Medicale
    Inventors: Christian Belmant, Jean-Jacques Fournie, Marc Bonneville, Marie-Alix Peyrat
  • Publication number: 20100022468
    Abstract: The present invention provides nucleoside cyclic phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as pre-cursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside cyclic phosphoramidates 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 cyclic phosphoramidates of the present invention.
    Type: Application
    Filed: December 14, 2007
    Publication date: January 28, 2010
    Inventors: Malte Meppen, Frank Narjes, Barbara Pacini, Cristina Gardelli, Philippe L. Durette
  • Publication number: 20090317361
    Abstract: Provided are imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: April 22, 2009
    Publication date: December 24, 2009
    Applicant: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Jay Parrish, Jie Xu
  • Publication number: 20090209481
    Abstract: Compounds having the formula I or II wherein R1, R2, B, and V are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.
    Type: Application
    Filed: November 26, 2008
    Publication date: August 20, 2009
    Inventors: Scott J. Hecker, K. Raja Reddy, Zhili Sun, Brett C. Bookser, David Bernard Smith
  • Publication number: 20090117041
    Abstract: Disclosed are certain cycloSalingenyl pyrimidine nucleoside monophosphates comprising positron emitters or gamma-emitting radiohalides, uses thereof for monitoring Alzheimer's disease progression and evaluating response to therapy and process for their preparation.
    Type: Application
    Filed: August 8, 2008
    Publication date: May 7, 2009
    Inventors: Zbigniew P. Kortylewicz, Janina Baranowska-Kortylewicz
  • Publication number: 20090118223
    Abstract: Novel 2?-C-methyl nucleoside 5?-monophosphate and 4?-C-methyl nucleoside 5?-monophosphate derivatives, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described.
    Type: Application
    Filed: August 14, 2006
    Publication date: May 7, 2009
    Inventors: Mark D. Erion, K. Raja Reddy, Malcolm MacCoss, David B. Olsen
  • Publication number: 20030176392
    Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.
    Type: Application
    Filed: December 19, 2002
    Publication date: September 18, 2003
    Inventors: Raymond F. Schinazi, Junxing Shi, Joyce D. Fingeroth, Erik Gustafson
  • Publication number: 20030130213
    Abstract: Pyrazine derivatives represented by general formula [1]: 1
    Type: Application
    Filed: August 16, 2002
    Publication date: July 10, 2003
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Hiroyuki Egawa, Yousuke Furuta, Jun Sugita, Sayuri Uehara, Shoichi Hamamoto, Kenji Yonezawa
  • Publication number: 20030040502
    Abstract: Inosine compounds, compositions comprising an inosine compound and methods for treating or preventing an inflammation disease or a reperfusion disease comprising administering an effective amount of an inosine compound to a patient in need thereof are disclosed.
    Type: Application
    Filed: March 26, 2002
    Publication date: February 27, 2003
    Applicant: Inotek Pharmaceuticals Corporation
    Inventors: Andrew L. Salzman, Csaba Szabo
  • Publication number: 20020160980
    Abstract: A method for the treatment for hepatitis delta infection in a host, that includes administering an effective amount of a nucleoside or a nucleoside analog that suppresses the expression of the hepatitis B surface or preS1 antigen in the host 100-fold or more relative to pretreatment values in vivo; or to not more than 1 microgram per milliliter in vivo. In a preferred embodiment, the nucleoside is L-FMAU, or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Application
    Filed: March 29, 2001
    Publication date: October 31, 2002
    Inventors: John L. Casey, Brent E. Korba, Paul J. Cote, John L. Gerin, Bud C. Tennant, Chung K. Chu
  • Publication number: 20020102590
    Abstract: Provided are nucleotide-dye conjugates and related compounds in which a dye is linked to a nucleobase directly or indirectly by an anionic linker. The anionic character of the linker is provided by one or more anionic moieties which are present in the linker, such as phosphate, phosphonate, sulfonate, and carboxylate groups. When the dye is a provided as a donor/acceptor dye pair, the anionic linker can be located between the donor and the acceptor, or between the nucleobase and either the donor or acceptor, or both. In one embodiment, conjugates of the invention provide enhanced electrophoretic mobility characteristics to sequencing fragments, e.g., for dideoxy sequencing using labeled terminators.
    Type: Application
    Filed: October 11, 2001
    Publication date: August 1, 2002
    Applicant: PE Corporation (NY)
    Inventors: Meng Taing, Shaheer H. Khan, Steven M. Menchen, Barnett B. Rosenblum
  • Publication number: 20020025922
    Abstract: Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient contains a thymine ring (e.g. AZT) that has 5-halo, 6-alkoxy substitution. Additional improvements in anti-HIV activity for certain AZT derivatives are seen by providing the pentose ring of AZT with aryl phosphate substitution.
    Type: Application
    Filed: December 1, 2000
    Publication date: February 28, 2002
    Inventors: Osmond D'Cruz, Fatih M. Uckun, Taracad Venkatachalam
  • Patent number: RE38416
    Abstract: This invention is directed to novel substituted nucleotide bases with a crosslinking arm which accomplish crosslinking between specific sites on adjoining strands of oligonucleotides a oligodeoxynucleotides. The invention is also directed to oligonucleotides comprising at least one of these crosslinking agents and to the use of the resulting novel oligonucleotides for diagnostic and therapeutic purposes.
    Type: Grant
    Filed: October 19, 2000
    Date of Patent: February 3, 2004
    Assignee: Epoch Biosciences, Inc.
    Inventors: Charles R. Petrie, Rich B. Meyer, John C. Tabone, Gerald D. Hurst