C-glycosides Wherein The Sugar Ring Is Bonded Directly To Carbon Of An N-hetero Ring (e.g., 9-deazaadenosines, Etc.) Patents (Class 536/29.2)
  • Patent number: 11149049
    Abstract: Disclosed herein are compounds of the Formula (I) and pharmaceutically acceptable salts thereof: (I) where the variables in Formula (I) are described herein. Methods of synthesizing such compounds and methods of using them to treat diseases and/or conditions such as a Picornaviridae, Flaviviridae, Filoviridae, Pneumoviridae and/or Coronaviridae viral infections are also disclosed.
    Type: Grant
    Filed: September 18, 2018
    Date of Patent: October 19, 2021
    Assignee: JANSSEN BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Jerome Deval, Marija Prhavc
  • Publication number: 20150133395
    Abstract: Provided herein are formulations, methods and substituted tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of tetrahydrofuranyl-pyrrolo[1,2-f][1,2,4]triazine-4-amine compounds.
    Type: Application
    Filed: November 6, 2014
    Publication date: May 14, 2015
    Inventors: Michael O'Neil Hanrahan Clarke, Edward Doerffler, Richard L. Mackman, Dustin Siegel
  • Patent number: 9024009
    Abstract: The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
    Type: Grant
    Filed: September 9, 2008
    Date of Patent: May 5, 2015
    Assignees: Janssen Pharmaceutica N.V., Mitsubishi Tanabe Pharma Corporation
    Inventors: Ahmed F. Abdel-Magid, Maureen Chislom, Steven Mehrman, Lorraine Scott, Kenneth M. Wells, Fan Zhang-Plasket, Sumihiro Nomura, Mitsuya Hongu, Yuichi Koga
  • Publication number: 20150111839
    Abstract: Provided are methods for treating Paramyxoviridae virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Human parainfluenza and Human respiratory syncytial virus infections.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Richard L. Mackman, Jay P. Parrish, Adrian S. Ray, Dorothy A. Theodore
  • Patent number: 8952139
    Abstract: The present invention provides processes (e.g., arylation reaction) for stereoselectively preparing C-arylglucosides that can be useful as synthetic building block or drugs, including SGLT2 inhibitors.
    Type: Grant
    Filed: November 7, 2012
    Date of Patent: February 10, 2015
    Assignee: ScinoPharm Taiwan, Ltd
    Inventors: Julian Paul Henschke, Chen-Wei Lin, Ping-Yu Wu, Chi-Nung Hsiao, Jyh-Hsiung Liao, Tsung-Yu Hsiao
  • Patent number: 8946397
    Abstract: This invention provides compounds that are of the class of nucleoside analogs, and more specifically nucleoside analogs that have a non-standard nucleobase, and more specifically analogs where a side chain is appended to said non-standard nucleobase, where said side chain can be cleaved so as to leave behind no more than five atoms appended to the nucleobase as a “scar”. The claimed compounds are useful as intermediates in processes that transiently introduce tags, labels, fluorescent molecules, or other species into oligonucleotides, as in sequencing using cyclic reversible termination, in in vitro selection using functionalized nucleotides that must later be PCR amplified, or in nucleotide capture protocols used in diagnostics.
    Type: Grant
    Filed: April 4, 2012
    Date of Patent: February 3, 2015
    Inventor: Steven A. Benner
  • Patent number: 8853171
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, 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, wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: October 7, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Thomas Butler, Aesop Cho, Choung U. Kim, Jay P. Parrish, Oliver L. Saunders, Lijun Zhang
  • Patent number: 8802840
    Abstract: The invention relates to the use of bicyclic nucleosides and nucleotides based on formula (II) for the treatment of infectious diseases, and in particular, viral infections.
    Type: Grant
    Filed: March 8, 2006
    Date of Patent: August 12, 2014
    Assignee: Biota Scientific Management Pty Ltd.
    Inventors: Paula Francom, Roland Henry Nearn, Alistair George Draffan, John Nicholas Lambert, Silas Bond
  • Publication number: 20140200188
    Abstract: Provided are methods for treating Orthomyxoviridue virus infections by administering ribosides, riboside phosphates and prodrugs thereof, of Formula I: wherein R2 is halogen. The compounds, compositions, and methods provided are particularly useful for the treatment of Human Influenza virus infections.
    Type: Application
    Filed: January 24, 2014
    Publication date: July 17, 2014
    Inventors: Michael O'Neil Hanrahan Clarke, Choung U. Kim, Willard Lew
  • Patent number: 8778636
    Abstract: Processes for preparing pimecrolimus starting from ascomycin, exploiting the selectivity characteristics of the purified enzymatic systems particularly regarding the selective functionalization of the hydroxyl groups present in position 24 and 33 of ascomycin. Such method represents the first example of chemoenzymatic synthesis for preparing pimecrolimus.
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: July 15, 2014
    Assignee: Euticals S.p.A.
    Inventors: Paride Grisenti, Shahrzad Reza Elahi, Elisa Verza
  • Patent number: 8697658
    Abstract: Compounds of formula (I): wherein X, Y, and Z are defined herein. Also disclosed are pharmaceutical compositions and therapeutical methods related to these compounds.
    Type: Grant
    Filed: December 13, 2012
    Date of Patent: April 15, 2014
    Assignee: National Health Research Institutes
    Inventors: Jinq-Chyi Lee, Yu-Sheng Chao
  • Publication number: 20130344028
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, 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, wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: October 11, 2012
    Publication date: December 26, 2013
    Inventors: Thomas BUTLER, Aesop CHO, Choung U. KIM, Jay P. PARRISH, Oliver L. SAUNDERS, Lijun ZHANG
  • Patent number: 8501699
    Abstract: The present disclosure relates to the use and methods of manufacture of bicyclic nucleosides and nucleotides for the treatment and prevention of infectious and proliferative diseases, including microbial infections and cancer.
    Type: Grant
    Filed: September 7, 2012
    Date of Patent: August 6, 2013
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Paula Francom, Barbara Frey, Silas Bond, Alistair George Draffan, Michael Harding, Richard Hufton, Saba Hangiri, Michael John Lilly, Edward Tyndall, Jianmin Duan, Richard Bethell, George Kukolj
  • Patent number: 8455451
    Abstract: Provided are select imidazo[1,2-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2? position of the nucleoside sugar is substituted with halogen and carbon substituents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: June 4, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Adrian S. Ray
  • Patent number: 8440813
    Abstract: The invention provides compounds of Formula (I), as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.
    Type: Grant
    Filed: January 11, 2008
    Date of Patent: May 14, 2013
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, V. Satish Kumar, Pravin L. Kotian, Minwan Wu
  • Publication number: 20130090298
    Abstract: The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.
    Type: Application
    Filed: June 10, 2011
    Publication date: April 11, 2013
    Applicant: GREEN CROSS CORPORATION
    Inventors: Jinhwa Lee, Jeongmin Kim, Suk Ho Lee, Junwon Lee, Kwang-Seop Song, Eun-Jung Park, Min Ju Kim, Hee Jeong Seo, Sung-Han Lee, Eun Jung Son, Jong Yup Kim, Suk Youn Kang, Younggyu Kong
  • Patent number: 8415308
    Abstract: Provided are prodrugs of pyrrolo[1,2-f][1,2,4]triazin-7-yl nucleoside phosphates wherein the 1? position of the nucleoside sugar is substituted with CN. The compounds, compositions, and methods provided are useful for the treatment Hepatitis C infections.
    Type: Grant
    Filed: May 26, 2011
    Date of Patent: April 9, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Adrian S. Ray, Lijun Zhang
  • Patent number: 8415309
    Abstract: The present disclosure relates to the use and methods of manufacture of bicyclic nucleosides and nucleotides for the treatment and prevention of infectious and proliferative diseases, including microbial infections and cancer.
    Type: Grant
    Filed: January 11, 2012
    Date of Patent: April 9, 2013
    Assignee: Biota Scientific Managment Pty Ltd
    Inventors: Paula Francom, Barbara Frey, Jianmin Duan, Richard Bethell, George Kukolj
  • Patent number: 8394949
    Abstract: The present invention provides multisignal labeling reagents and these are useful in a number of biochemical applications, including the manufacture of biomolecular probes and their use in detecting or amplifying analyte-specific moieties.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: March 12, 2013
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Elazar Rabbani, Jannis G. Stavrianopoulos, James J. Donegan
  • Patent number: 8389702
    Abstract: The present invention provides multisignal labeling reagents and these are useful in a number of biochemical applications, including the manufacture of biomolecular probes and their use in detecting or amplifying analyte-specific moieties.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: March 5, 2013
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Elazar Rabbani, Jannis G. Stavrianopoulos, James J. Donegan
  • Patent number: 8389701
    Abstract: The present invention provides multisignal labeling reagents and these are useful in a number of biochemical applications, including the manufacture of biomolecular probes and their use in detecting or amplifying analyte-specific moieties.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: March 5, 2013
    Assignee: Enzo Life Sciences, Inc.
    Inventors: Elazar Rabbani, Jannis G. Stavrianopoulos, James J. Donegan
  • Publication number: 20130034521
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, 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, wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: October 11, 2012
    Publication date: February 7, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventor: GILEAD SCIENCES, INC.
  • Patent number: 8354225
    Abstract: This invention relates to nucleoside, nucleotide, and oligonucleotide analogs that incorporate non-standard nucleobase analogs, defined to be those that present a pattern of hydrogen bonds to a paired nucleobase analog in a complementary strand that is different from the pattern presented by adenine, guanine, cytosine, and thymine. Most specifically, this invention discloses and claims processes for amplifying nucleic acid analogs containing non-standard nucleobases using polymerase chain reactions, and enzymes that perform this amplification.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: January 15, 2013
    Inventors: Steven Albert Benner, Albert Michael Sismour
  • Patent number: 8318682
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, 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, wherein the 1? position of the nucleoside sugar is substituted with a cyano group. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: November 27, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Thomas Butler, Aesop Cho, Choung U. Kim, Jay P. Parrish, Oliver L. Saunders, Lijun Zhang
  • Patent number: 8242085
    Abstract: The invention provides compounds of formula (I), as described herein, or pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula (I) are useful as anti-viral agents and/or as anti-cancer agents.
    Type: Grant
    Filed: May 8, 2008
    Date of Patent: August 14, 2012
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand
  • Publication number: 20120142617
    Abstract: The invention provides compounds of Formula I: as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.
    Type: Application
    Filed: July 12, 2011
    Publication date: June 7, 2012
    Applicant: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin Kotian, Minwan Wu, V. Satish Kumar
  • Patent number: 8163703
    Abstract: The invention provides methods for treating hepatitis C viral infections and related viral infections, as well as compounds and compositions that are useful for treating such infections.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: April 24, 2012
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, Minwan Wu, Pravin L. Kotian, V. Satish Kumar, Tsu-Hsing Lin, Yahya El-Kattan, Ajit K. Ghosh
  • Publication number: 20120064575
    Abstract: Processes for preparing pimecrolimus starting from ascomycin, exploiting the selectivity characteristics of the purified enzymatic systems particularly regarding the selective functionalization of the hydroxyl groups present in position 24 and 33 of ascomycin. Such method represents the first example of chemoenzymatic synthesis for preparing pimecrolimus.
    Type: Application
    Filed: May 19, 2010
    Publication date: March 15, 2012
    Inventors: Paride Grisenti, Shahrzad Reza Elahi, Elisa Verza
  • Patent number: 8133870
    Abstract: The invention provides compounds of formula I, II, and III as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula I, II, and III are useful as anti-viral agents and/or as anti-cancer agents.
    Type: Grant
    Filed: October 28, 2005
    Date of Patent: March 13, 2012
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, Minwan Wu, Pravin L. Kotian, V. Satish Kumar, Tsu-Hsing Lin, Yahya El-Kattan, Ajit K. Ghosh
  • Patent number: 8119607
    Abstract: The present disclosure relates to the use and methods of manufacture of bicyclic nucleosides and nucleotides for the treatment and prevention of infectious and proliferative diseases, including microbial infections and cancer.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: February 21, 2012
    Assignee: Biota Scientific Management Pty Ltd
    Inventors: Paula Francom, Barbara Frey, Silas Bond, Alistair George Draffan, Michael Harding, Richard Hufton, Saba Jahangiri, Michael John Lilly, Edward Tyndall, Jianmin Duan, Richard Bethell, George Kukolj
  • Publication number: 20120020921
    Abstract: Provided are prodrugs of pyrrolo[1,2-f][1,2,4]triazin-7-yl nucleoside phosphates wherein the 1? position of the nucleoside sugar is substituted with CN. The compounds, compositions, and methods provided are useful for the treatment Hepatitis C infections.
    Type: Application
    Filed: May 26, 2011
    Publication date: January 26, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Aesop CHO, Choung U. Kim, Adrian S. Ray, Lijun Zhang
  • Publication number: 20120009147
    Abstract: Provided are select imidazo[1,2-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof, wherein the 2? position of the nucleoside sugar is substituted with halogen and carbon substituents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.
    Type: Application
    Filed: March 17, 2011
    Publication date: January 12, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Adrian S. Ray
  • Publication number: 20110293563
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, 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, wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Application
    Filed: August 2, 2011
    Publication date: December 1, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Thomas Butler, Aesop Cho, Choung U. Kim, Jay P. Parrish, Oliver L. Saunders, Lijun Zhang
  • Patent number: 8053212
    Abstract: This invention relates to nucleoside, nucleotide, and oligonucleotide analogs that incorporate non-standard nucleobase analogs, defined to be those that present a pattern of hydrogen bonds to a paired nucleobase analog in a complementary strand that is different from the pattern presented by adenine, guanine, cytosine, and thymine. The invention is specifically concerned with compositions of matter that present the donor-donor-acceptor, donor-acceptor-donor, and acceptor-donor-donor non-standard hydrogen bonding patterns on pyrimidine analogs, where nucleoside analogs bearing these pyrimidine analogs do not epimerize as easily as those known in the art. The heterocycles on these nucleoside analogs are diaminopyridines and aminopyridones that have electron withdrawing groups attached to the position analogous to the 5-position of the ring in standard pyrimidines, including nitro, cyano, and carboxylic acid derivatives.
    Type: Grant
    Filed: March 9, 2006
    Date of Patent: November 8, 2011
    Inventor: Steven Albert Benner
  • Publication number: 20110230654
    Abstract: Provided are processes and intermediates for the syntheses of nucleosides of pyrrolo[1,2-f][1,2,4]triazinyl and imidazo[1,24][1,2,4]triazinyl heterocycles of Formula I.
    Type: Application
    Filed: September 20, 2010
    Publication date: September 22, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Thomas Butler, Aesop Cho, Benjamin R. Graetz, Choung U. Kim, Samuel E. Metobo, Oliver L. Saunders, Andrew W. Waltman, Jie Xu, Lijun Zhang
  • Patent number: 8012941
    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: Grant
    Filed: April 22, 2009
    Date of Patent: September 6, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Jay Parrish, Jie Xu
  • Patent number: 8013147
    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. The compounds are in particular suitable as substrates for RNA or DNA polymerases and can thus be incorporated into RNA or DNA oligonucleotides and are especially suitable for labelling and detecting nucleic acids or for DNA sequencing.
    Type: Grant
    Filed: March 2, 2005
    Date of Patent: September 6, 2011
    Assignee: Roche Molecular Systems, Inc.
    Inventors: Klaus Muhlegger, Herbert Von Der Eltz
  • Patent number: 8008264
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, 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, wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: April 22, 2009
    Date of Patent: August 30, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Thomas Butler, Aesop Cho, Choung U. Kim, Jay Parrish, Oliver L. Saunders, Lijun Zhang
  • Patent number: 7994139
    Abstract: The invention provides compounds of Formula I: as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of Formula (I) are useful as anti-viral agents and/or as anti-cancer agents.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: August 9, 2011
    Assignee: BioCryst Pharmaceuticals, Inc.
    Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin Kotian, Minwan Wu, V. Satish Kumar
  • Patent number: 7973012
    Abstract: Provided is a novel C-phenyl glycitol compound that may serve as a prophylactic or therapeutic agent for diabetes by inhibiting both SGLT1 activity and SGLT2 activity, thereby exhibiting a glucose absorption suppression action and a urine glucose excretion action.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: July 5, 2011
    Assignee: Taisho Pharmaceutical Co., Ltd
    Inventors: Hiroyuki Kakinuma, Yohei Kobashi, Yuko Hashimoto, Takahiro Oi, Hitomi Takahashi, Hideaki Amada, Yuki Iwata
  • Patent number: 7973013
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, 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, wherein the 2? position of the nucleoside sugar is substituted with halogen and carbon substitutents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.
    Type: Grant
    Filed: September 20, 2010
    Date of Patent: July 5, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Samuel E. Metobo, Adrian S. Ray, Jie Xu
  • Patent number: 7968521
    Abstract: A stable and high-purity protected pseudouridine in crystal form is provided represented by the following structural formula: wherein M represents a trityl group or a derivative thereof, which is a useful material for producing an RNA oligomer or a similar substance. A method for producing the crystalline protected pseudouridine is also provided, which method includes crystallizing a protected pseudouridine from a solution containing the protected pseudouridine, by use of an ester solvent and/or an alcoholic solvent. The method, which does not need a silica gel column treatment, can be performed in a simple manner, does not impose a load on the environment, and realizes low-cost production of a target crystalline protected pseudouridine.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: June 28, 2011
    Assignee: Yamasa Corporation
    Inventor: Kenji Kitano
  • Publication number: 20110130440
    Abstract: One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such modified nucleosides. Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
    Type: Application
    Filed: March 26, 2009
    Publication date: June 2, 2011
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev
  • Publication number: 20110070194
    Abstract: Provided are pyrrolo[1,2-f][1,2,4]triazinyl, 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, wherein the 2? position of the nucleoside sugar is substituted with halogen and carbon substitutents. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections caused by both wild type and mutant strains of HCV.
    Type: Application
    Filed: September 20, 2010
    Publication date: March 24, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Choung U. Kim, Samuel E. Metobo, Adrian S. Ray, Jie Xu
  • Patent number: 7910561
    Abstract: The present invention is directed to compounds which contain substituted naphthyridines which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention. These substituted naphthyridines have unexpected advantageous properties when compared to other naphthyridines reported in PCT publication WO2003/086394, such unexpected advantageous properties may include increased cellular potency/solubility, greater selectivity, enhanced pharmacokinetic properties, lack of off target activity and so on.
    Type: Grant
    Filed: December 9, 2005
    Date of Patent: March 22, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeannie M. Arruda, Brian T. Campbell, Nicholas D. P. Cosford, Jacob M. Hoffman, Essa H. Hu, Mark E. Layton, Yiwei Li, Jun Liang, Kevin J. Rodzinak, Tony Siu, Brian A. Stearns, Lida R. Tehrani, Mark T. Bilodeau, Peter J. Manley
  • Patent number: 7902157
    Abstract: Disclosed are compounds of the formula wherein Z1 is —CH2—or —C(O)—, R4 and R5 are carbon chains (and optionally, together can form a C2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R1 and R3 are as defined herein. Also disclosed are methods of treating pain, and methods of inhibiting the absorption of cholesterol using a compound of formula I.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: March 8, 2011
    Assignee: Schering Corporation
    Inventors: Duane A. Burnett, Brian A. McKittrick
  • Patent number: 7884080
    Abstract: The present invention relates to Azetidinone Derivatives of structural formula 1: and compositions comprising an Azetidinone Derivative and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of an Azetidinone Derivative.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: February 8, 2011
    Assignee: Schering Plough Corporation
    Inventors: Robert G. Aslanian, Chad E. Bennett, Duane A. Burnett, Tin-Yau Chan, Eugenia Y. Kiselgof, Chad E. Knutson, Joel M. Harris, Brian A. McKittrick, Anandan Palani, Elizabeth M. Smith, Henry M. Vaccaro, Dong Xiao, Hyunjin M. Kim
  • Publication number: 20110028414
    Abstract: Novel compounds of the formula (I), in which X has the meaning indicated in Patent Claim 1, are suitable as antidiabetics.
    Type: Application
    Filed: March 17, 2009
    Publication date: February 3, 2011
    Inventors: Christos Tsaklakidis, Norbert Beier
  • Publication number: 20100311684
    Abstract: Nucleosides and nucleotides containing a tricyclic base portion thereof are useful for treating infectious diseases and proliferative disorders, such as viral infections or cancer respectively.
    Type: Application
    Filed: May 10, 2010
    Publication date: December 9, 2010
    Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTD
    Inventors: Phillip Dan Cook, Gregory Ewing, Deborah K. Ewing, Yi Jin, John Lambert, Marija Prhavc, Vasanthankumar Rajappan, Vivek K. Rajwanshi, Kandasamy Sakthivel
  • Publication number: 20100216985
    Abstract: A stable and high-purity protected pseudouridine in crystal form is provided represented by the following structural formula: wherein M represents a trityl group or a derivative thereof, which is a useful material for producing an RNA oligomer or a similar substance. A method for producing the crystalline protected pseudouridine is also provided, which method includes crystallizing a protected pseudouridine from a solution containing the protected pseudouridine, by use of an ester solvent and/or an alcoholic solvent. The method, which does not need a silica gel column treatment, can be performed in a simple manner, does not impose a load on the environment, and realizes low-cost production of a target crystalline protected pseudouridine.
    Type: Application
    Filed: June 21, 2006
    Publication date: August 26, 2010
    Applicant: YAMASA CORPORATION
    Inventor: Kenji Kitano