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)
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Patent number: 11149049Abstract: 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: GrantFiled: September 18, 2018Date of Patent: October 19, 2021Assignee: JANSSEN BIOPHARMA, INC.Inventors: Leonid Beigelman, Jerome Deval, Marija Prhavc
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Publication number: 20150133395Abstract: 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: ApplicationFiled: November 6, 2014Publication date: May 14, 2015Inventors: Michael O'Neil Hanrahan Clarke, Edward Doerffler, Richard L. Mackman, Dustin Siegel
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Patent number: 9024009Abstract: 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: GrantFiled: September 9, 2008Date of Patent: May 5, 2015Assignees: Janssen Pharmaceutica N.V., Mitsubishi Tanabe Pharma CorporationInventors: Ahmed F. Abdel-Magid, Maureen Chislom, Steven Mehrman, Lorraine Scott, Kenneth M. Wells, Fan Zhang-Plasket, Sumihiro Nomura, Mitsuya Hongu, Yuichi Koga
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Publication number: 20150111839Abstract: 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: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Inventors: Richard L. Mackman, Jay P. Parrish, Adrian S. Ray, Dorothy A. Theodore
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Patent number: 8952139Abstract: 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: GrantFiled: November 7, 2012Date of Patent: February 10, 2015Assignee: ScinoPharm Taiwan, LtdInventors: Julian Paul Henschke, Chen-Wei Lin, Ping-Yu Wu, Chi-Nung Hsiao, Jyh-Hsiung Liao, Tsung-Yu Hsiao
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Patent number: 8946397Abstract: 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: GrantFiled: April 4, 2012Date of Patent: February 3, 2015Inventor: Steven A. Benner
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Patent number: 8853171Abstract: 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: GrantFiled: October 11, 2012Date of Patent: October 7, 2014Assignee: Gilead Sciences, Inc.Inventors: Thomas Butler, Aesop Cho, Choung U. Kim, Jay P. Parrish, Oliver L. Saunders, Lijun Zhang
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Patent number: 8802840Abstract: 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: GrantFiled: March 8, 2006Date of Patent: August 12, 2014Assignee: Biota Scientific Management Pty Ltd.Inventors: Paula Francom, Roland Henry Nearn, Alistair George Draffan, John Nicholas Lambert, Silas Bond
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Publication number: 20140200188Abstract: 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: ApplicationFiled: January 24, 2014Publication date: July 17, 2014Inventors: Michael O'Neil Hanrahan Clarke, Choung U. Kim, Willard Lew
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Patent number: 8778636Abstract: 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: GrantFiled: May 19, 2010Date of Patent: July 15, 2014Assignee: Euticals S.p.A.Inventors: Paride Grisenti, Shahrzad Reza Elahi, Elisa Verza
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Patent number: 8697658Abstract: 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: GrantFiled: December 13, 2012Date of Patent: April 15, 2014Assignee: National Health Research InstitutesInventors: Jinq-Chyi Lee, Yu-Sheng Chao
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Publication number: 20130344028Abstract: 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: ApplicationFiled: October 11, 2012Publication date: December 26, 2013Inventors: Thomas BUTLER, Aesop CHO, Choung U. KIM, Jay P. PARRISH, Oliver L. SAUNDERS, Lijun ZHANG
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Patent number: 8501699Abstract: 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: GrantFiled: September 7, 2012Date of Patent: August 6, 2013Assignee: Biota Scientific Management Pty LtdInventors: 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
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Patent number: 8455451Abstract: 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: GrantFiled: March 17, 2011Date of Patent: June 4, 2013Assignee: Gilead Sciences, Inc.Inventors: Aesop Cho, Choung U. Kim, Adrian S. Ray
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Patent number: 8440813Abstract: 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: GrantFiled: January 11, 2008Date of Patent: May 14, 2013Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, V. Satish Kumar, Pravin L. Kotian, Minwan Wu
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Publication number: 20130090298Abstract: 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: ApplicationFiled: June 10, 2011Publication date: April 11, 2013Applicant: GREEN CROSS CORPORATIONInventors: 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
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Patent number: 8415309Abstract: 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: GrantFiled: January 11, 2012Date of Patent: April 9, 2013Assignee: Biota Scientific Managment Pty LtdInventors: Paula Francom, Barbara Frey, Jianmin Duan, Richard Bethell, George Kukolj
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Patent number: 8415308Abstract: 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: GrantFiled: May 26, 2011Date of Patent: April 9, 2013Assignee: Gilead Sciences, Inc.Inventors: Aesop Cho, Choung U. Kim, Adrian S. Ray, Lijun Zhang
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Patent number: 8394949Abstract: 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: GrantFiled: March 6, 2009Date of Patent: March 12, 2013Assignee: Enzo Life Sciences, Inc.Inventors: Elazar Rabbani, Jannis G. Stavrianopoulos, James J. Donegan
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Multisignaling oligomeric or polymeric compositions comprising labeled moieties and binding partners
Patent number: 8389701Abstract: 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: GrantFiled: June 24, 2010Date of Patent: March 5, 2013Assignee: Enzo Life Sciences, Inc.Inventors: Elazar Rabbani, Jannis G. Stavrianopoulos, James J. Donegan -
Patent number: 8389702Abstract: 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: GrantFiled: June 24, 2010Date of Patent: March 5, 2013Assignee: Enzo Life Sciences, Inc.Inventors: Elazar Rabbani, Jannis G. Stavrianopoulos, James J. Donegan
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Publication number: 20130034521Abstract: 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: ApplicationFiled: October 11, 2012Publication date: February 7, 2013Applicant: GILEAD SCIENCES, INC.Inventor: GILEAD SCIENCES, INC.
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Patent number: 8354225Abstract: 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: GrantFiled: March 9, 2006Date of Patent: January 15, 2013Inventors: Steven Albert Benner, Albert Michael Sismour
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Patent number: 8318682Abstract: 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: GrantFiled: August 2, 2011Date of Patent: November 27, 2012Assignee: Gilead Sciences, Inc.Inventors: Thomas Butler, Aesop Cho, Choung U. Kim, Jay P. Parrish, Oliver L. Saunders, Lijun Zhang
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Patent number: 8242085Abstract: 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: GrantFiled: May 8, 2008Date of Patent: August 14, 2012Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand
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Publication number: 20120142617Abstract: 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: ApplicationFiled: July 12, 2011Publication date: June 7, 2012Applicant: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin Kotian, Minwan Wu, V. Satish Kumar
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Patent number: 8163703Abstract: 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: GrantFiled: March 6, 2009Date of Patent: April 24, 2012Assignee: 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
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Publication number: 20120064575Abstract: 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: ApplicationFiled: May 19, 2010Publication date: March 15, 2012Inventors: Paride Grisenti, Shahrzad Reza Elahi, Elisa Verza
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Patent number: 8133870Abstract: 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: GrantFiled: October 28, 2005Date of Patent: March 13, 2012Assignee: 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
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Patent number: 8119607Abstract: 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: GrantFiled: July 1, 2009Date of Patent: February 21, 2012Assignee: Biota Scientific Management Pty LtdInventors: 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
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Publication number: 20120020921Abstract: 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: ApplicationFiled: May 26, 2011Publication date: January 26, 2012Applicant: Gilead Sciences, Inc.Inventors: Aesop CHO, Choung U. Kim, Adrian S. Ray, Lijun Zhang
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Publication number: 20120009147Abstract: 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: ApplicationFiled: March 17, 2011Publication date: January 12, 2012Applicant: Gilead Sciences, Inc.Inventors: Aesop Cho, Choung U. Kim, Adrian S. Ray
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Publication number: 20110293563Abstract: 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: ApplicationFiled: August 2, 2011Publication date: December 1, 2011Applicant: Gilead Sciences, Inc.Inventors: Thomas Butler, Aesop Cho, Choung U. Kim, Jay P. Parrish, Oliver L. Saunders, Lijun Zhang
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Patent number: 8053212Abstract: 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: GrantFiled: March 9, 2006Date of Patent: November 8, 2011Inventor: Steven Albert Benner
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Publication number: 20110230654Abstract: 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: ApplicationFiled: September 20, 2010Publication date: September 22, 2011Applicant: 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
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Patent number: 8012941Abstract: 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: GrantFiled: April 22, 2009Date of Patent: September 6, 2011Assignee: Gilead Sciences, Inc.Inventors: Aesop Cho, Choung U. Kim, Jay Parrish, Jie Xu
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Patent number: 8013147Abstract: 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: GrantFiled: March 2, 2005Date of Patent: September 6, 2011Assignee: Roche Molecular Systems, Inc.Inventors: Klaus Muhlegger, Herbert Von Der Eltz
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Patent number: 8008264Abstract: 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: GrantFiled: April 22, 2009Date of Patent: August 30, 2011Assignee: Gilead Sciences, Inc.Inventors: Thomas Butler, Aesop Cho, Choung U. Kim, Jay Parrish, Oliver L. Saunders, Lijun Zhang
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Patent number: 7994139Abstract: 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: GrantFiled: March 5, 2009Date of Patent: August 9, 2011Assignee: BioCryst Pharmaceuticals, Inc.Inventors: Yarlagadda S. Babu, Pooran Chand, Pravin Kotian, Minwan Wu, V. Satish Kumar
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Patent number: 7973012Abstract: 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: GrantFiled: May 18, 2007Date of Patent: July 5, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Hiroyuki Kakinuma, Yohei Kobashi, Yuko Hashimoto, Takahiro Oi, Hitomi Takahashi, Hideaki Amada, Yuki Iwata
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Patent number: 7973013Abstract: 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: GrantFiled: September 20, 2010Date of Patent: July 5, 2011Assignee: Gilead Sciences, Inc.Inventors: Aesop Cho, Choung U. Kim, Samuel E. Metobo, Adrian S. Ray, Jie Xu
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Patent number: 7968521Abstract: 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: GrantFiled: June 21, 2006Date of Patent: June 28, 2011Assignee: Yamasa CorporationInventor: Kenji Kitano
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Publication number: 20110130440Abstract: 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: ApplicationFiled: March 26, 2009Publication date: June 2, 2011Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev
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Publication number: 20110070194Abstract: 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: ApplicationFiled: September 20, 2010Publication date: March 24, 2011Applicant: Gilead Sciences, Inc.Inventors: Aesop Cho, Choung U. Kim, Samuel E. Metobo, Adrian S. Ray, Jie Xu
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Patent number: 7910561Abstract: 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: GrantFiled: December 9, 2005Date of Patent: March 22, 2011Assignee: 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
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Patent number: 7902157Abstract: 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: GrantFiled: September 13, 2007Date of Patent: March 8, 2011Assignee: Schering CorporationInventors: Duane A. Burnett, Brian A. McKittrick
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Patent number: 7884080Abstract: 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: GrantFiled: September 13, 2007Date of Patent: February 8, 2011Assignee: Schering Plough CorporationInventors: 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
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Publication number: 20110028414Abstract: Novel compounds of the formula (I), in which X has the meaning indicated in Patent Claim 1, are suitable as antidiabetics.Type: ApplicationFiled: March 17, 2009Publication date: February 3, 2011Inventors: Christos Tsaklakidis, Norbert Beier
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Publication number: 20100311684Abstract: 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: ApplicationFiled: May 10, 2010Publication date: December 9, 2010Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: Phillip Dan Cook, Gregory Ewing, Deborah K. Ewing, Yi Jin, John Lambert, Marija Prhavc, Vasanthankumar Rajappan, Vivek K. Rajwanshi, Kandasamy Sakthivel
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Publication number: 20100216985Abstract: 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: ApplicationFiled: June 21, 2006Publication date: August 26, 2010Applicant: YAMASA CORPORATIONInventor: Kenji Kitano