The N-hereto Ring Is Six-membered And Monocyclic (e.g., Uridine-5-mono- Phosphate, Etc.) Patents (Class 536/26.8)
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Publication number: 20140248242Abstract: 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: ApplicationFiled: March 3, 2014Publication date: September 4, 2014Inventors: Cyril B. DOUSSON, Benjamin Alexander MAYES, David DUKHAN, Adel M. MOUSSA, Alistair James STEWART
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Publication number: 20140248241Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3?-deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Base1 and Base2 are as provided herein.Type: ApplicationFiled: March 3, 2014Publication date: September 4, 2014Inventors: Alistair James STEWART, Adel M. MOUSSA, Benjamin Alexander MAYES, Francois-Rene ALEXANDRE, Dominique SURLERAUX, Christophe Claude PARSY, Claire PIERRA, David DUKHAN, Gilles GOSSELIN
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Patent number: 8822671Abstract: A 2?-modified ribonucleoside having an alkoxymethyl protective group can be imparted with a high duplex-forming ability by introducing, as a substituent, a halogen atom into the protective group moiety. A modified form of RNA having a halogen-substituted alkoxymethyl protective group exhibits a high duplex-forming ability that is comparable to the duplex-forming ability of a 2?-O-methyl modified nucleic acid.Type: GrantFiled: November 28, 2011Date of Patent: September 2, 2014Assignees: The University of Tokyo, Chiralgen, Ltd.Inventors: Mamoru Shimizu, Takeshi Wada, Kouichiro Arai
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PYRIMIDINE NUCLEOSIDES AND THEIR MONOPHOSPHATE PRODRUGS FOR TREATMENT OF VIRAL INFECTIONS AND CANCER
Publication number: 20140235566Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, cytomegalovirus (CMV), herpes viruses (HSV-1, HSV-2), Dengue virus, Yellow fever, or HBV in human patients or other animal hosts. The compounds are certain N4-hydroxycytidine nucleosides derivatives, modified monophosphate and phosphonates prodrugs analogs, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, cytomegalovirus (CMV), herpes viruses (HSV-1, HSV-2), Dengue virus, Yellow fever, and HBV.Type: ApplicationFiled: October 29, 2013Publication date: August 21, 2014Applicants: Emory University, RFS Pharma, LLCInventors: Franck Amblard, Steven J. Coats, Raymond F. Schinazi -
Publication number: 20140221304Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.Type: ApplicationFiled: July 10, 2012Publication date: August 7, 2014Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
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Publication number: 20140213543Abstract: The invention provides a compound of formula (1), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.Type: ApplicationFiled: March 28, 2014Publication date: July 31, 2014Applicant: Regents of the University of MinnesotaInventor: Carston R. Wagner
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Publication number: 20140206640Abstract: The present invention relates to 2?-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: April 11, 2012Publication date: July 24, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Frank Bennett, Vishal Verma, Ashok Arasappan, Kevin X. Chen, Ying Huang, Angela Kerekes, Latha Nair, Dimitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
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Publication number: 20140206856Abstract: The invention provides a glucoside compound, which is capable of providing a phosphoramidite, which can be produced at low cost and can produce a nucleic acid in high yield and with high purity. The glycoside compound has the formula wherein B, R1, R2, and R3 are as described herein.Type: ApplicationFiled: August 24, 2012Publication date: July 24, 2014Applicant: BONAC CORPORATIONInventors: Eriko Aoki, Hiroshi Suzuki, Akihiro Itoh
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Publication number: 20140187511Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.Type: ApplicationFiled: August 29, 2013Publication date: July 3, 2014Applicant: GILEAD PHARMASSET LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
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Publication number: 20140179627Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.Type: ApplicationFiled: December 19, 2013Publication date: June 26, 2014Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
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Publication number: 20140179910Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.Type: ApplicationFiled: December 19, 2013Publication date: June 26, 2014Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
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Publication number: 20140178338Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are according to Formula 1501: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, PD, RA, RB, RC, L, M and Z are as described herein.Type: ApplicationFiled: December 17, 2013Publication date: June 26, 2014Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART, Gilles GOSSELIN
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Patent number: 8759508Abstract: The compounds are of class of chromophoric 1,2,3-triazolyl equipped silyl linking groups that are useful in the chemical synthesis of RNA.Type: GrantFiled: May 16, 2008Date of Patent: June 24, 2014Assignee: GE Healthcare Dharmacon, Inc.Inventor: Michael Oren Delaney
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Patent number: 8759316Abstract: A method for reducing or maintaining platelet inhibition in a patient by administering cangrelor prior to an invasive procedure is described. The method of this invention can be used for patients in need of antiplatelet therapy or at risk of thrombosis. The method can further be used in patients who were previously treated with long-acting platelet inhibitors without increasing the risk of excessive bleeding.Type: GrantFiled: June 28, 2013Date of Patent: June 24, 2014Assignee: The Medicines CompanyInventors: Lisa Ruderman Chen, Simona Skerjanec, Dawn Bell, Jayne Prats, Meredith Todd, Clive Arthur Arculus-Meanwell, Diane Mould
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Publication number: 20140161770Abstract: 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: ApplicationFiled: April 11, 2012Publication date: June 12, 2014Applicant: 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
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Publication number: 20140154210Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.Type: ApplicationFiled: March 11, 2013Publication date: June 5, 2014Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
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2'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
Publication number: 20140154211Abstract: 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: ApplicationFiled: April 11, 2012Publication date: June 5, 2014Inventors: 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: 20140140951Abstract: 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, provided herein is an isolated compound according to Formula Ia: or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Inventors: Adel M. MOUSSA, Benjamin Alexander MAYES, Cyril B. DOUSSON, David DUKHAN
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Publication number: 20140140952Abstract: 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, provided herein is an isolated compound according to Formula Ib: or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Inventors: Adel M. MOUSSA, Benjamin Alexander MAYES, Cyril B. DOUSSON, David DUKHAN
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Publication number: 20140128339Abstract: The present invention relates to 2?-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2?-Methyl Substituted Nucleoside Derivative, and methods of using the 2?-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: October 15, 2013Publication date: May 8, 2014Inventors: Vinay Girijavallabhan, Stephane Bogen, Quang T. Truong, Ping Chen, Angela Kerekes, Frank Bennett, Sara Esposite, Qingmei Hong, Ian Davies
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Publication number: 20140121366Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.Type: ApplicationFiled: January 10, 2014Publication date: May 1, 2014Applicant: GILEAD PHARMASSET LLCInventors: Byoung-Kwon Chun, Ganapati Reddy Pamulapati, Suguna Rachakonda, Bruce Ross, Michael Joseph Sofia, Peiyuan Wang, Hai-Ren Zhang
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Publication number: 20140106451Abstract: Provided herein are novel bicyclic nucleosides, oligomeric compounds that include such bicyclic nucleosides and methods of using the oligomeric compounds. More particularly, the novel bicyclic nucleosides comprise a furanose ring system having a bridge comprising a 4?-methylene group attached to a 2?-sulfoxide or sulfone group and optionally including one or more substituent groups attached to the 4?-methylene and or the 5?-position. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: ApplicationFiled: October 9, 2013Publication date: April 17, 2014Inventors: Thazha P. Prakash, Eric E. Swayze
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Publication number: 20140099283Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2?-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Gilles GOSSELIN, Christophe Claude PARSY, Francois-Rene ALEXANDRE, Houcine RAHALI, Jean-Francois GRIFFON, Julien MILHAU, Dominique SURLERAUX, Cyril B. DOUSSON, Claire PIERRA, Adel M. MOUSSA, Benjamin Alexander MAYES
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Publication number: 20140100186Abstract: 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: ApplicationFiled: May 7, 2012Publication date: April 10, 2014Inventors: Charles E. McKenna, Boris A. Kashemirov, Ivan S. Krylov, Valeria M. Zakharova
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Patent number: 8691972Abstract: Disclosed are compounds of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Also disclosed are methods of preparing compound of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Further disclosed are methods of counducting drug discovery and research comprises applying the compound of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer in an investigation.Type: GrantFiled: July 20, 2012Date of Patent: April 8, 2014Inventor: Zhen Huang
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Patent number: 8691971Abstract: Disclosed herein are compositions and methods for generating ribo-nucleic neutral (RNN) or deoxyribo-nucleic-neutral (DNN) polynucleotides with reduced anionic charge, for improved intracellular delivery. Also disclosed herein are methods of using RNN and DNN compositions.Type: GrantFiled: September 23, 2009Date of Patent: April 8, 2014Inventor: Scott G. Petersen
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Patent number: 8680071Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: GrantFiled: March 31, 2011Date of Patent: March 25, 2014Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche ScientifiqueInventors: Dominique Surleraux, Gilles Gosselin
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Publication number: 20140065101Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is defined herein, which is a 2?-branched nucleoside useful for the treatment or prevention of viral infections, particularly dengue virus, yellow fever virus, West Nile virus, Japanese encephalitis virus, tick-borne encephalitis virus, Kunjin virus, Murray Valley encephalitis, St Louis encephalitis, Omsk hemorrhagic fever virus, bovine viral diarrhea virus, Zika virus and Hepatitis C virus.Type: ApplicationFiled: August 27, 2013Publication date: March 6, 2014Applicant: Novartis AGInventor: Fumiaki Yokokawa
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Publication number: 20140066398Abstract: The invention provides compounds of the formula: which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.Type: ApplicationFiled: October 10, 2013Publication date: March 6, 2014Applicant: Medivir, ABInventors: Anders ENEROTH, Bjorn Klasson, Magnus Nilsson, Pedro Pinho, Bertil Samuelsson, Christian Sund
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Publication number: 20140058076Abstract: The present disclosure relates to the field of nucleic acid chemistry, specifically to 5-position modified uridines as well as phosphoramidite and triphosphate derivatives thereof. The present disclosure also relates to methods of making and using the same.Type: ApplicationFiled: November 1, 2013Publication date: February 27, 2014Inventors: John Rohloff, Nebojsa Janjic, Jeffrey D. Carter, Catherine Fowler
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Publication number: 20140057866Abstract: Phosphoramidate derivatives of 5-fluoro-2?-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.Type: ApplicationFiled: September 7, 2012Publication date: February 27, 2014Inventors: Christopher McGuigan, Jan Balzarini, Magdalena Slusarczyk, Blanka Gonczy, Paola Murziani
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Publication number: 20140051605Abstract: The present disclosure relates to photoactivable protecting groups containing a diarylsulfide chromophore, a method for the synthesis thereof and their use as photoactivable protecting groups using maskless photolithography based array synthesis.Type: ApplicationFiled: October 23, 2013Publication date: February 20, 2014Applicant: NimbleGen Systems GmbHInventor: Klaus-Peter Stengele
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Publication number: 20140046021Abstract: The molecular structures of metal-salen complexes which exerts pharmacological effects are clarified and the metal-salen complexes having such molecular structures and their derivatives are provided. A metal-salen complex compound is characterized in that a metal atom part in each of multiple molecules of the metal-salen complex or its derivative is multimerized via water.Type: ApplicationFiled: January 19, 2012Publication date: February 13, 2014Applicants: IHI CORPORATIONInventors: Yoshihiro Ishikawa, Haruki Eguchi
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Publication number: 20140039179Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.Type: ApplicationFiled: July 11, 2013Publication date: February 6, 2014Inventors: Piet HERDEWIJN, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
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Publication number: 20140038916Abstract: This application discloses novel phosphoramidate and phosphonoamidate prodrugs of nucleosides, nucleotides, C-nucleosides, C-nucleotides, phosphonates, and other alcohol-containing drugs; use of these prodrugs for treatment of infectious diseases and cancers, in particular, liver infections and cancers; and methods of preparing these novel phosphoramidate and phosphonoamidate prodrugs.Type: ApplicationFiled: December 30, 2011Publication date: February 6, 2014Applicant: Nanjing Molecular Research, Inc.Inventors: Zheng Wang, Suping Zhou
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Patent number: 8642756Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.Type: GrantFiled: May 20, 2010Date of Patent: February 4, 2014Assignee: Gilead Pharmasset LLCInventors: Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
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Patent number: 8618076Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.Type: GrantFiled: March 31, 2011Date of Patent: December 31, 2013Assignee: Gilead Pharmasset LLCInventors: Bruce S. Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
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Publication number: 20130337581Abstract: Embodiments are disclosed herein that involve C5-functionalized nucleic acids, which can be used for detecting a target in a nucleic acid. Particular embodiments disclose methods for making these compounds, wherein the compounds can be formed by coupling of an intermediate with a linker. Certain embodiments disclose the use of these compounds for detecting single nucleotide polymorphisms, and for increasing the thermal affinity of nucleic acid complements as compared to unmodified nucleic acid complements. In addition, the disclosed compounds can decrease enzymatic degradation of nucleic acids.Type: ApplicationFiled: June 19, 2013Publication date: December 19, 2013Applicant: University of IdahoInventors: Patrick Jerzy Hrdlicka, Pawan Kumar, Michael E. Østergaard
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Publication number: 20130323836Abstract: The present invention provides compounds of formula (1). 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: April 22, 2011Publication date: December 5, 2013Applicant: Isis Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Ivan Zlatev, Eric E. Swayze, Thazha P. Prakash, Walter F. Lima
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Publication number: 20130324591Abstract: Disclosed herein are double stranded RNA molecules which have been modified to exhibit one of the following, increased activity, enhanced nuclease stability, reduced off target activity and or reduced immunogenicity, to pharmaceutical compositions comprising such compounds and to methods of use. Further disclosed is a method for the synthesis of threose nucleic acid phosphoramidites and methods of use thereof.Type: ApplicationFiled: December 6, 2011Publication date: December 5, 2013Applicant: QUARK PHARMACEUTICALS, INC.Inventors: Sharon Avkin-Nachum, Elena Feinstein, Leonid Beigelman
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Publication number: 20130317207Abstract: The present invention provides novel fluorescent dyes and kits containing the same, which are useful for labeling a wide variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis and/or treatment of disease conditions.Type: ApplicationFiled: November 20, 2012Publication date: November 28, 2013Applicant: PROMEGA CORPORATIONInventor: Promega Corporation
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Publication number: 20130315868Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disease and conditions, 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: ApplicationFiled: May 21, 2013Publication date: November 28, 2013Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART
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Publication number: 20130316969Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 21, 2013Publication date: November 28, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130310551Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.Type: ApplicationFiled: July 8, 2013Publication date: November 21, 2013Inventors: Bruce S. Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
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Publication number: 20130289263Abstract: A compound is represented by the following formula (1), (2), or (3) (where, in the above formulae (1), (2), and (3), Z11 and Z12 independently have a fluorescent property and are an uncharged atomic group exhibiting an exciton effect).Type: ApplicationFiled: December 28, 2011Publication date: October 31, 2013Applicant: RIKENInventors: Akimitsu Okamoto, Shuji Ikeda
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Publication number: 20130288997Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.Type: ApplicationFiled: June 24, 2013Publication date: October 31, 2013Inventors: Bruce S. Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
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Patent number: 8569478Abstract: Compounds, methods and compositions for treating a host infected with human immunodeficiency virus and hepatitis B virus comprising administering an effective amount of a described 4?-C-substituted ?-D- and ?-L-nucleoside or a pharmaceutically acceptable salt or prodrug thereof, are provided.Type: GrantFiled: September 26, 2006Date of Patent: October 29, 2013Assignee: Gilead Pharmasset LLCInventors: Jinfa Du, Phillip Furman, Michael Joseph Sofia
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Publication number: 20130281682Abstract: A method for preparing a phosphitylated compound comprising the step of:—reacting a hydroxyl containing compound with a phosphitylating agent in the presence of an activator having the formula (I) wherein R=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl R1, R2=either H or form a 5 to 6-membered ring together. X1, X2=independently either N or CH Y=H or Si(R4)3, with R4=alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl B=deprotonated acid. The hydroxyl containing compound is preferably a sugar moiety or a nucleoside or an oligomer derived therefrom.Type: ApplicationFiled: June 20, 2013Publication date: October 24, 2013Applicant: Girindus AGInventors: Meinholf Lange, Andreas Schönberger, Christina Kirchhoff, Olaf Grössel, Nadja Omelcenko, Andreas Hohlfeld, Fritz Link
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Publication number: 20130281686Abstract: Provided are methods and intermediates for preparing diastereomerically pure phosphoramidate prodrugs of nucleosides of Formulas Ia and Ib: The compounds of Formula Ia and Ib are useful for the treatment Hepatitis C infections.Type: ApplicationFiled: July 19, 2011Publication date: October 24, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Aesop Cho, Michael O'Neil Hanrahan Clarke, Scott Alan Wolckenhauer
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Publication number: 20130266538Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.Type: ApplicationFiled: March 11, 2013Publication date: October 10, 2013Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent