The N-hetero Ring Is Part Of A Purine Ring System Patents (Class 536/26.12)
  • Patent number: 10836783
    Abstract: Though 3?,5?-cyclic diadenylic acid was conventionally provided only as a freeze-dried product, a solid material other than a freeze-dried product and a manufacturing method thereof is provided. By a step of adding acid to an aqueous solution of 3?,5?-cyclic diadenylic acid so as to lower pH to 1 to 3, an inclusion compound of 3?,5?-cyclic diadenylic acid can be obtained. Said manufacturing method is an extremely simple and easy method and does not need a special machine or the like.
    Type: Grant
    Filed: June 25, 2019
    Date of Patent: November 17, 2020
    Assignee: Yamasa Corporation
    Inventors: Hisaki Tanaka, Kazuya Ishige
  • Patent number: 10787479
    Abstract: A crystal of free acid of 3?,5?-cyclic diguanylic acid containing no metal salt with cobalt, magnesium or the like is provided. A method is sought for obtaining said crystal in a large amount and with ease. By a manufacturing method comprising a step of adding acid to an aqueous solution of 3?,5?-cyclic diguanylic acid so as to lower pH to 1 to 3, crystals of 3?,5?-cyclic diguanylic acid can be obtained in a large amount with ease. Said crystals are free acid crystals which do not contain a metal salt with cobalt, magnesium or the like.
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: September 29, 2020
    Assignee: Yamasa Corporation
    Inventors: Hisaki Tanaka, Kazuya Ishige
  • Patent number: 10429397
    Abstract: A cell permeable ATP analog has the following formula: or a physiologically acceptable salt thereof, wherein: R0 is n, o, p are each independently 1, 2, 3, 4, 5, or 6, m is 0, 1, 2, 3, 4, or 5; X is O, S, NH, or CH2. R1 is H or C1-6 alkyl, R2 is H, C1-6 alkyl, C6-30 aryl, C5-32 heteroaryl, or C7-32 alkylaryl; R3, R4 are each independently H, C1-6 alkyl, C6-30 aryl, C5-32 heteroaryl, or C7-32 alkylaryl, wherein R3, and R4 can be combined together to form a ring structure.
    Type: Grant
    Filed: June 20, 2016
    Date of Patent: October 1, 2019
    Assignee: WAYNE STATE UNIVERSITY
    Inventor: Mary Kay Pflum
  • Patent number: 10322087
    Abstract: The invention relates to means and methods of targeted drug delivery of therapeutic agent to and across the blood-ocular barrier. In particular, the invention relates to cyclic guanosine-3?, 5?-monophosphate analogs as therapeutic agent for treating retinal diseases. The cGMPSs targeted to the blood-ocular barrier by glutathione-based ligands that facilitate the specific binding to and enhanced internalization by glutathione transporters present on the blood-ocular barrier. The glutathione-based ligands are conjugated to nanocontainers such as liposomes encapsulating the cGMPSs.
    Type: Grant
    Filed: March 16, 2016
    Date of Patent: June 18, 2019
    Assignee: Mireca Medicines GmbH
    Inventors: Per Ekström, François Paquet-Durand, Pieter Jaap Gaillard, Valeria Marigo, Hans-Gottfried Genieser, Andreas Rentsch, Dragana Trifunovic, Ayse Sahaboglu Tekgoz
  • Patent number: 9808513
    Abstract: A method of treating cancer through use of guanosine 3?,5?-cyclic monophosphate (cyclic GMP). Cyclic GMP decreases the number of human breast cancer and prostate adenocarcinoma as well as small-cell and squamous lung cells in culture by 30% (1 ?M), 84% (1 mM), 31% (1 ?M), and 30% (1 ?M), respectively. Cyclic GMP decreases DNA synthesis in human pancreatic, breast, and prostate adenocarcinomas as well as small-cell and squamous cell carcinomas of the lung at its 1 ?M concentration by 51%, 54%, 56%, 50% and 52%, respectively. Cyclic GMP when infused for one week decreases the tumor volume of human pancreatic adenocarcinomas in athymic mice 95% compared to untreated animals with human pancreatic adenocarcinomas.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: November 7, 2017
    Assignee: UNIVERSITY OF SOUTH FLORIDA
    Inventor: David L. Vesely
  • 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
  • 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: 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
  • 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
  • Publication number: 20140248242
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, the compounds are according to Formula 2001: where PD, Base, RA and RB are as provided herein. 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: March 3, 2014
    Publication date: September 4, 2014
    Inventors: Cyril B. DOUSSON, Benjamin Alexander MAYES, David DUKHAN, Adel M. MOUSSA, Alistair James STEWART
  • Publication number: 20140205566
    Abstract: A compound of Formula (I) is provided that has been shown to be useful for treating a disease caused by a viral infection: wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: November 21, 2013
    Publication date: July 24, 2014
    Applicant: NOVARTIS AG
    Inventors: Lv LIAO, Fumiaki YOKOKAWA, Gang WANG
  • Patent number: 8785619
    Abstract: This invention relates to n-alkylated synthetic nucleosides and phosphoramidites of high regio-specific purity and stability and for selective deprotection of the protecting group in oligonucleotides for the purpose of synthesis of high purity selectively n-alkylated sequence specific DNA and RNA. Such oligonucleotides are useful for study of mechanism of cytotoxic and mutagenic DNA damage, detection and reversal of cellular cytotoxic and mutagenic damages that occurs from the incorporation of methylated nucleosides, the corresponding phosphates and triphosphates and their precursors, via de novo DNA synthesis. The reagents could be extremely valuable tools as diagnostics and mutagenic reversal reagents.
    Type: Grant
    Filed: December 20, 2004
    Date of Patent: July 22, 2014
    Assignee: ChemGenes Corporation
    Inventors: Sant K. Srivastav, Suresh C. Srivastava, Satya P Bajpai
  • 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
  • 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: 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
  • Publication number: 20140112886
    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 comprise two 2?-methyl nucleotides linked according to Formula I: N1-L-N2??(I) or a pharmaceutically acceptable salt, ester, solvate, stereoisomer, isomeric form, tautomeric form or polymorphic form thereof; wherein N1, L and N2 are as described herein.
    Type: Application
    Filed: October 18, 2013
    Publication date: April 24, 2014
    Inventors: Adel M. MOUSSA, Benjamin Alexander MAYES, Jeevanandam ARUMUGASAMY, Jingyang WANG
  • Publication number: 20140100186
    Abstract: A method of modifying a nucleotide or a nucleotide analogue to increase its overall effectiveness in treating an antiviral disease is provided. In some cases, a compound comprising a base, sugar, phosphonate moiety, and amino acid residue is provided, where the base-sugar may be a nucleoside, and the amino acid residue may be a tyrosine residue. In certain cases, the tyrosine residue contains a long chain alkyl group on the carboxamide group of the residue. Methods of inhibiting viral replication and methods of treating a viral infection are also provided.
    Type: Application
    Filed: May 7, 2012
    Publication date: April 10, 2014
    Inventors: Charles E. McKenna, Boris A. Kashemirov, Ivan S. Krylov, Valeria M. Zakharova
  • Publication number: 20140088033
    Abstract: The present invention relates to novel boranophosphate analogues of cyclic nucleotides. The invention further relates to the use of such compounds as reagents for signal transduction research or as modulators of cyclic nucleotide-regulated binding proteins and isoenzymes thereof, and/or as hydrolysis- and oxidation-resistant ligands for affinity chromatography, for antibody production or for diagnostic applications e.g. on chip surfaces and/or as additive for organ transplantation storage solutions.
    Type: Application
    Filed: March 27, 2012
    Publication date: March 27, 2014
    Applicant: BIOLOG LIFE SCIENCE INSTITUTE FORSCHUNGSLABOR UND BIOCHEMICA-VERTRIEB GMBH
    Inventor: Hans-Gottfried Genieser
  • 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
  • Publication number: 20130315866
    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, Claire PIERRA, Dominique SURLERAUX, Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART
  • 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
  • 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: 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: 20130095064
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections.
    Type: Application
    Filed: October 12, 2012
    Publication date: April 18, 2013
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventor: Idenix Pharmaceuticals, Inc.
  • Publication number: 20130072462
    Abstract: The present invention provides a compound of Formula 1a, wherein R1 is H or phosphate and the double bond is between N? and C? 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 N? C?, 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: August 17, 2012
    Publication date: March 21, 2013
    Applicant: Gencia Corporation
    Inventor: Shaharyar Khan
  • Publication number: 20120316327
    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: Application
    Filed: June 7, 2012
    Publication date: December 13, 2012
    Applicant: 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
  • 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: 20120178710
    Abstract: The invention provides methods for the synthesis of cyclic dinucleotides and thiophosphate analogs thereof as well as a new family of analogs of cyclic diguanosine monophosphate that includes a series of seven phosphorothioate derivatives that includes diastereomers of mono-, di-, and trithiophosphates.
    Type: Application
    Filed: July 1, 2010
    Publication date: July 12, 2012
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Roger A. Jones, Barbara L. Gaffney
  • 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
  • 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: 20110288286
    Abstract: A process is disclosed for the production of cyclic di-guanosine monophosphate (c-di-GMP) without the use of protecting groups by means of an enzymatic synthesis. The process comprises the coupling of two guanosine triphosphate (GTP) molecules so as to form a c-di-GMP molecule. This is done under the influence of a mutant diguanylate cyclase (DGC) comprising the amino acid sequence V153M154G155G156. It has been found that the DGC is obtainable from inclusion bodies, and therewith can be made available in amounts sufficient to improve the c-di-GMP synthesis. Particularly, the latter synthesis can be conducted in a one-pot method starting from commercially available bulk chemicals and allows upscaling to a commercial production scale.
    Type: Application
    Filed: December 7, 2009
    Publication date: November 24, 2011
    Inventors: Thomas Simon Ilg, Volker Spehr, Ralf Warrass
  • Patent number: 7977343
    Abstract: Novel adenine derivatives of the formula (I), in which R1, R2, R3, X and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: July 12, 2011
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Hans-Peter Buchstaller, Hans-Michael Eggenweiler, Bertram Cezanne, Michael Wolf
  • Patent number: 7935814
    Abstract: An object of the present invention is to provide a novel compound that is an agonist of guanosine-3?,5?-cyclic monophosphate and has an effect of activating protein kinase G. The present invention provides 8-guanosine-3?,5?-cyclic monophosphate compound which is represented by the following formula, and a pharmaceutical composition, especially a protein kinase G activating agent, which contains the 8-guanosine-3?,5?-cyclic monophosphate compound as an active ingredient.
    Type: Grant
    Filed: February 28, 2006
    Date of Patent: May 3, 2011
    Assignee: Kumamoto University
    Inventors: Takaaki Akaike, Teruo Akuta
  • Publication number: 20100279973
    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: Application
    Filed: December 23, 2009
    Publication date: November 4, 2010
    Applicant: PHARMASSET, INC.
    Inventors: BYOUNG-KWON CHUN, JINFA DU, SUGUNA RACHAKONDA, BRUCE ROSS, MICHAEL JOSEPH SOFIA, GANAPATI REDDY PAMULAPATI, WONSUK CHANG, HAI-REN ZHANG, DHANAPALAN NAGARATHNAM
  • Publication number: 20100081628
    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: June 5, 2009
    Publication date: April 1, 2010
    Applicant: PHARMASSET, INC.
    Inventors: Jinfa DU, Dhanapalan NAGARATHNAM, Ganapati REDDY PAMULAPATI, Bruce S. ROSS, Michael Joseph SOFIA
  • Publication number: 20090215716
    Abstract: An object of the present invention is to provide a novel compound that is an agonist of guanosine-3?,5?-cyclic monophosphate and has an effect of activating protein kinase G. The present invention provides 8-guanosine-3?,5?-cyclic monophosphate compound which is represented by the following formula, and a pharmaceutical composition, especially a protein kinase G activating agent, which contains the 8-guanosine-3?,5?-cyclic monophosphate compound as an active ingredient.
    Type: Application
    Filed: February 28, 2006
    Publication date: August 27, 2009
    Applicant: KUMAMOTO UNIVERSITY
    Inventors: Takaaki Akaike, Teruo Akuta
  • 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
  • Patent number: 7319093
    Abstract: 2-Substituted-5?-O-(1-boranotriphosphate)adenosine derivatives having at position 2 a radical R1 selected from the group consisting of H; halogen; O-hydrocarbyl; S-hydrocarbyl; NR3R4; and hydrocarbyl optionally substituted by halogen, CN, SCN, NO2, OR3, SR3 or NR3R4; wherein R3 and R4 are each independently H or hydrocarbyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring optionally containing 1-2 further heteroatoms selected from oxygen, nitrogen and sulfur, and pharmaceutically acceptable salts or diastereoisomers thereof or a mixture of diastereoisomers, are useful for treatment of type 2 diabetes.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: January 15, 2008
    Assignees: Bar-Ilan University, University of Montpellier
    Inventors: Bilha Fischer, Victoria Kleiman-Nahum, Pierre Petit
  • Patent number: 7238476
    Abstract: The invention provides compositions and methods for performing primer extension reactions, including employment of amplification primers having 5? tags to incorporate into amplicons variant nucleotides of interest from target nucleic acids at known ratios, with or without sequences surrounding the variant nucleotides of interest. The invention provides identifying the variant nucleotides generated from the target nucleic acid and generated from the 5? tags, comparing the results, evaluating the efficiency of the primer extension reactions, and monitoring the efficacy of such reactions. The invention accounts for DNA sequence and experimental variables that may affect efficiency of incorporation of nucleotides, and provides a reference point for the interpretation of polymorphisms. The invention also provides methods of breeding scrapie-resistant sheep populations.
    Type: Grant
    Filed: August 1, 2003
    Date of Patent: July 3, 2007
    Assignee: Orchid Cellmark, Inc.
    Inventors: Brian McKeown, Roger Derbyshire, Paul Rowan, Robert Sung
  • 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: 7192700
    Abstract: The invention comprises compositions and methods for performing primer extension reactions, including employment of amplification primers having 5? tags to incorporate into amplicons variant nucleotides of interest from target nucleic acids at known ratios, along with the sequences surrounding the variant nucleotides of interest. The invention comprises identifying the variant nucleotides generated from the target nucleic acid and generated from the 5? tags, comparing the results, evaluating the efficiency of the primer extension reactions, and monitoring the efficacy of such reactions. The invention accounts for DNA sequence and experimental variables which may affect efficiency of incorporation of nucleotides, and provides a reference point for the interpretation of polymorphisms.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: March 20, 2007
    Assignee: Orchid Cellmark Inc.
    Inventor: Brian McKeown
  • Patent number: 7105499
    Abstract: The present invention provides nucleoside derivatives 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 derivatives 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 derivatives of the present invention.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: September 12, 2006
    Assignees: Merck & Co., Inc., Isis Pharmaceuticals, Inc.
    Inventors: Steven S. Carroll, David B. Olsen, Malcolm MacCoss, Balkrishen Bhat, Phillip Dan Cook, Anne B. Eldrup, Thazha P. Prakash
  • 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