The N-hetero Ring Is Part Of A Bicyclic Ring System Patents (Class 536/26.7)
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Publication number: 20130018013Abstract: 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: ApplicationFiled: September 7, 2012Publication date: January 17, 2013Applicant: 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: 20130017171Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: ApplicationFiled: September 20, 2012Publication date: January 17, 2013Applicants: UNIVERSITA DEGLI STUDI DI CAGLIARI, IDENIX PHARMACEUTICALS, INC.Inventors: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari
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Publication number: 20130018011Abstract: The application provides methods for treatment or prophylaxis of dengue virus mediated diseases with compounds of Formula I wherein R1, R2a, R2b, R3, R4, R5 R6, R8a, R9 and R10 are as defined herein. The application further discloses methods for treatment or prophylaxis of dengue virus mediated diseases with pharmaceutical compositions comprising compounds of Formula I.Type: ApplicationFiled: June 5, 2012Publication date: January 17, 2013Inventors: Hassan Javanbakht, Klaus G. Klumpp, Suping Ren, Zhuming Zhang
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Publication number: 20120316327Abstract: A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.Type: ApplicationFiled: June 7, 2012Publication date: December 13, 2012Applicant: GILEAD PHARMASSET LLCInventors: Byoung-Kwon Chun, Jinfa Du, Suguna Rachakonda, Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Wonsuk Chang, Hai-Ren Zhang, Dhanapalan Nagarathnam
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Publication number: 20120316328Abstract: 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: February 7, 2012Publication date: December 13, 2012Applicant: Girindus AGInventors: Meinolf Lange, Andreas Schönberger, Christina Kirchhoff, Olaf Grössel, Nadja Knaub, Andreas Hohlfeld, Fritz Link
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Publication number: 20120296076Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.Type: ApplicationFiled: May 18, 2012Publication date: November 22, 2012Inventors: Richard Hung Chiu Yu, Brandon Heath Brown, Richard P. Polniaszek, Benjamin R. Graetz, Keiko Sujino, Duong Duc-Phi Tran, Alan Scott Triman, Kenneth M. Kent, Steven Pfeiffer
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Patent number: 8309707Abstract: Novel technology for RNA synthesis in the reverse direction, involving a new class of products, 3?-DMT-5’-CE ribonucleoside phosphoramidites and 3?-DMT-5’-succinyl ribonucleoside solid supports, with per step coupling efficiency surpassing 99% in the RNA synthesis. This leads to high purity RNA. Examples of a large number of 20-21 mers and a few examples of long chain oligonucleotides are demonstrated. The data indicates dramatic improvement in coupling efficiency per step during oligonucleotide synthesis using the reverse RNA monomers (5??? direction) as compared to 3?-CE ribonucleoside phosphoramidites used in the conventional method of RNA synthesis (3??5? direction). The new process requires shorter coupling cycle time, approx. 4 minutes as compared to approx. 10 minutes using conventional RNA synthesis method (3??5? direction). Furthermore, almost complete absence of M+1 impurities in the reverse RNA synthesis methodology were observed, even when the last phosphoramidite was a macromolecule.Type: GrantFiled: September 8, 2009Date of Patent: November 13, 2012Assignee: ChemGenes CorporationInventors: Suresh C. Srivastava, Divya Pandey, Satya P Bajpai, Naveen P Srivastava
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Patent number: 8299225Abstract: To provide an excellent amidite for synthesizing modified nucleic acid, which enables a protective group therein to be removed under a moderate condition, thereby stably producing a hydroxyl group-containing modified nucleic acid, and a method for synthesizing modified nucleic acid using the amidite. Specifically, an amidite for synthesizing modified nucleic acid, expressed by General Formula (I): where X represents a base, Y represents a substituent, Z represents a protective group for protecting a hydroxyl group in the substituent, and Q represents one of a hydrogen atom, a hydroxyl group and a hydroxyl group protected by a protective group, wherein the protective group can be removed in an aprotic solvent, and when the protective group is removed, the hydroxyl group emerges in the substituent, and a method for synthesizing modified nucleic acid using the amidite.Type: GrantFiled: October 12, 2010Date of Patent: October 30, 2012Assignee: Fujitsu LimitedInventor: Tsuyoshi Fujihara
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Patent number: 8293215Abstract: The present invention relates to the field of improving the flavor of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. More particularly, the present invention provides flavor modulating substances selected from the group represented by formula (I): and edible salts thereof and edible esters thereof, which can advantageously be used for modulating the flavor of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. These flavor modulating substances can be used to impart desirable taste attributes in a wide variety of applications and products. In addition, the present flavor modulating substances are capable of modulating the taste and/or aroma impact of other, flavor imparting, substances contained within these same products, thereby improving the overall flavor quality of these products.Type: GrantFiled: December 13, 2007Date of Patent: October 23, 2012Assignee: Givaudan Nederland Services B.V.Inventors: Adri De Klerk, Marieke Baalbergen, Harry Renes, Chris Winkel
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Publication number: 20120258891Abstract: 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: March 29, 2012Publication date: October 11, 2012Applicant: NIMBLEGEN SYSTEMS GMBHInventor: Klaus-Peter Stengele
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Publication number: 20120251487Abstract: 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: ApplicationFiled: March 30, 2012Publication date: October 4, 2012Inventor: Dominique SURLERAUX
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Publication number: 20120245335Abstract: The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2?R)-2?-deoxy-2?-fluoro-2?-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Applicant: GILEAD PHARMASSET LLCInventor: Jeremy Clark
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Publication number: 20120245029Abstract: This invention provides phosphate-modified nucleosides represented by the structural formula (I): wherein W is O or S, and wherein B, R1; R3 and R2. are as defined herein. These compounds are useful as substrates for DNA/RNA polymerases, and as anti-viral agents in particular against HIV-1.Type: ApplicationFiled: May 12, 2010Publication date: September 27, 2012Applicant: Katholieke Universiteit LeuvenInventors: Piet Herdewijn, Philippe Marlière
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Publication number: 20120238737Abstract: Aspects of the invention include 2? protected nucleoside monomers that are protected at the 2? site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.Type: ApplicationFiled: May 31, 2012Publication date: September 20, 2012Applicant: Agilent Technologies, Inc.Inventors: Douglas J. Dellinger, Agnieszka Sierzchala, John Turner, Joel Myerson, Zoltan Kupihar, Fernando Ferreira, Marvin H. Caruthers, Geraldine F. Dellinger
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Publication number: 20120237480Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.Type: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Inventors: YAT SUN OR, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
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Patent number: 8263575Abstract: The compounds are phosphoramidate derivatives of nucleoside compounds such as cladribine, isocladribine, fludarabine and clofarabine useful in the treatment of cancer.Type: GrantFiled: March 16, 2006Date of Patent: September 11, 2012Assignee: Nucana Biomed LimitedInventors: Christopher McGuigan, Kenneth Mills, Costantino Congiatu
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Publication number: 20120220922Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.Type: ApplicationFiled: December 23, 2011Publication date: August 30, 2012Applicants: Universidad de Buenos Aires, THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Rafael YUSTE, Roberto Etchenique, Luis Baraldo
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Patent number: 8242258Abstract: Aspects of the invention include 2? protected nucleoside monomers that are protected at the 2? site with orthoester-type protecting groups. The 2? protected monomers also include a second, aryl carbonate-type, protecting group. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.Type: GrantFiled: December 3, 2007Date of Patent: August 14, 2012Assignees: Agilent Technologies, Inc., The Regents of the University of ColoradoInventors: Douglas J. Dellinger, Brian Stell, Marvin H. Caruthers
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Publication number: 20120202983Abstract: This invention features conjugates, compositions, methods of synthesis, and applications thereof, including folate derived conjugates of nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids and antisense nucleic acid molecules.Type: ApplicationFiled: April 26, 2012Publication date: August 9, 2012Applicant: Sirna Therapeutics, Inc.Inventors: Jasenka Matulic-Adamic, Leonid Beigelman
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Publication number: 20120189597Abstract: Nutritional compositions and methods of making and using the nutritional compositions are provided. In a general embodiment, the present disclosure provides a nutritional composition including one or more exogenous nucleotides.Type: ApplicationFiled: August 9, 2010Publication date: July 26, 2012Applicant: NESTEC S.A.Inventors: Norman Alan Greenberg, Douglas Richard Bolster
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Publication number: 20120190098Abstract: Fluorophores derived from photoactivatable azide-pi-acceptor fluorogens or from a thermal reaction of an azide-pi-acceptor fluorogen with an alkene or alkyne are disclosed. Fluorophores derived from a thermal reaction of an alkyne-pi-acceptor fluorogen with an azide are also disclosed. The fluorophores can readily be activated by light and can be used to label a biomolecule and imaged on a single-molecule level in living cells.Type: ApplicationFiled: March 1, 2012Publication date: July 26, 2012Applicants: LELAND STANFORD JUNIOR UNIVERSITY, KENT STATE UNIVERSITYInventors: ROBERT J. TWIEG, WILLIAM E. MOERNER, SAMUEL J. LORD, NA LIU, REICHEL SAMUEL
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Publication number: 20120184724Abstract: A nucleoside monomer that is protected by a thionocarbamate protecting group and contains one or more 2H, 13C, or 15N isotopes in the ribose and/or base part is provided, as well as a method for making a polynucleotide that uses the same. Also provided is a polynucleotide synthesis method that employs a diamine to deprotect a protected polynucleotide.Type: ApplicationFiled: December 28, 2011Publication date: July 19, 2012Applicant: AGILENT TECHNOLOGIES, INC.Inventors: Agnieszka B. Sierzchala, Brian Phillip Smart, Douglas J. Dellinger, Geraldine Dellinger, Joel Myerson, Zoltan Timar
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Publication number: 20120178638Abstract: The present invention is directed to RNA monomers comprising O-acetal levulinyl protecting groups at the 2? and/or the 5?-hydroxy functionalities of the ribose moiety. Said monomers may be incorporated into oligoribonucleotides or RNA polynucleotides. Furthermore, the invention is directed to methods for the synthesis of said RNA monomers, oligoribonucleotides and RNA polynucleotides, as well as methods for their deprotection and methods for the use of said compounds and compositions comprising said compounds. In particular, such compounds and compositions comprising them are used in methods for light-directed synthesis of RNA microarrays.Type: ApplicationFiled: September 4, 2009Publication date: July 12, 2012Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Masad Damha, Jeremy Lackey, Debbie Mitra, Marvin Wickens, Franco Cerrina, Saima A. Akhtar, Mark Somoza
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Publication number: 20120165515Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.Type: ApplicationFiled: February 2, 2007Publication date: June 28, 2012Inventors: Balkrishen Bhat, Anne B. Eldrup, Thazha P. Prakash, Phillip Dan Cook, Robert L. LaFemina, Amy L. Simcoe, Carrie A. Rutkowski, Mario A. Valenciano
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Publication number: 20120149888Abstract: The present invention relates to synthesis, purification and methods to obtain high purity novel 2?-arabino-O-methyl nucleosides and the corresponding phosphoramidites of various arabinonucleoside bases and introduction of such units into defined sequence synthetic DNA and RNA. Various synthetic oligonucleotides, such as HIV integrase inhibitor 14-mer and thrombin binding oligonucleotide, thrombin-1, bearing ara-2?-omethyl modification have been synthesized. It is anticipated the oligonucleotides incorporating these monomers will exhibit biological activities related to antisense approach approach, design of better SiRNA's, diagnostic agents. Similarly, it is anticipated that oligonucleotides incorporating such novel nucleosides will be useful to develop therapeutic candidates designing stable G-quadruplexes and Aptamers for oligonucleotide structure, folding topology, evaluation of biochemical properties and design and develop as therapeutic agents.Type: ApplicationFiled: February 23, 2010Publication date: June 14, 2012Inventors: Suresh C. Srivastava, Divya Pandey, Naveen P. Srivastava, Alok Srivastava
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Publication number: 20120142908Abstract: The present invention provides for compounds of Formula I: wherein X—N and R1-R4 have any of the values disclosed in the specification. The compounds of Formula I are useful as reagents to introduce N-alkyl nucleosides into DNA oligonucleotides. The present invention also provides for methods of synthesizing the compounds of Formula I.Type: ApplicationFiled: November 29, 2011Publication date: June 7, 2012Applicant: Berry and Associates, Inc.Inventors: David A. Berry, Lana L. Berry, John C. Hodges
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Publication number: 20120142763Abstract: This disclosure relates to nucleic acid constructs modified to have a reduced net anionic charge. The constructs comprise phosphotriester and/or phosphothioate protecting groups. The disclosure also provides methods of making and using such constructs.Type: ApplicationFiled: June 1, 2010Publication date: June 7, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Steven F. Dowdy, Bryan R. Meade, Khirud Gogoi
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Publication number: 20120135951Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing viral infections, in particular, HIV, and HBV, in human patients or other animal hosts. The compounds are 3?-azido-2?,3?-dideoxy purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1 and HBV.Type: ApplicationFiled: December 9, 2009Publication date: May 31, 2012Inventors: Raymond F. Schinazi, Ph.D., John W. Mellors, Nicolas Paul Sluis-Cremer, Steven J. Coats, Ph.D., Richard Anthony Whitaker, Brian David Herman, Jong Hyun Cho, Longhu Zhou, Hongwang Zhang
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Publication number: 20120122811Abstract: 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: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Applicant: Biota Scientific Management Pty LtdInventors: Paula Francom, Barbara Frey, Silas Bond, Jianmin Duan, Richard Bethell, George Kukolj
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Patent number: 8173621Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:Type: GrantFiled: June 5, 2009Date of Patent: May 8, 2012Assignee: Gilead Pharmasset LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Ganapati Reddy Pamulapati, Bruce S. Ross, Michael Joseph Sofia
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Patent number: 8173619Abstract: The compounds are phosphoramidate derivatives of nucleoside compounds such as cladribine, isocladribine, fludarabine and clofarabine useful in the treatment of cancer.Type: GrantFiled: March 16, 2006Date of Patent: May 8, 2012Inventors: Christopher McGuigan, Kenneth Mills, Costantino Congiatu
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Publication number: 20120108800Abstract: Provided is a new production method for the synthesis of an NC type nucleoside efficiently and conveniently in a high yield without unnecessary protecting group conversion steps. It relates to a step of producing a compound represented by the formula (II): or a salt thereof, by inverting a compound represented by the formula (I): and a method of producing a compound represented by the formula (III): or a salt thereof (wherein each symbol is as defined in the specification), which includes the step.Type: ApplicationFiled: June 22, 2010Publication date: May 3, 2012Inventors: Shumpei Murata, Tadashi Umemoto, Kenichi Miyata, Yoji Hayase
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Publication number: 20120108533Abstract: This invention provides phosphate-modified nucleosides represented by the structural formula: wherein W is O or S, and wherein B, R1; R3 and R2. are s defined herein. These compounds are useful as substrates for DNA/RNA polymerases, and as anti-viral agents in particular against HIV-1.Type: ApplicationFiled: April 30, 2010Publication date: May 3, 2012Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&DInventors: Piet Herdewijn, Philippe Marlière
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Publication number: 20120107323Abstract: The invention provides compounds capable of treating a subject suffering from or being susceptible to a cell proliferative disorder (especially, cancer), methods of identifying and using the compounds, pharmaceutical compositions and kits thereof.Type: ApplicationFiled: March 12, 2010Publication date: May 3, 2012Applicant: University of FloridaInventors: Steven N. Hochwald, David A. Ostrov, William G. Cance, Elena Kurenova
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Publication number: 20120108531Abstract: Disclosed herein are novel phosphonate nucleosides and thiophosphonate nucleosides comprising a phosphonalkoxy-substituted or phosphonothioalkyl-substituted five-membered, saturated or unsaturated, oxygen-containing or sulfur-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections.Type: ApplicationFiled: November 8, 2011Publication date: May 3, 2012Applicant: K.U.LEUVEN RESEARCH & DEVELOPMENTInventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De clercq
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Publication number: 20120094948Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).Type: ApplicationFiled: December 20, 2011Publication date: April 19, 2012Inventors: Giancarlo Naccari, Sergio Baroni
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Publication number: 20120083599Abstract: Novel biotin analogues, such as 2-Azidobiotin, comprising the ureido ring of natural biotin with the thiophene ring, optionally modified, and a modified sidechain having a functional end group, preferably selected from the group consisting of a carboxylic acid, amine, alcohol, thiol, aldehyde and a halide, and at least one bio-orthogonally reactive chemical group located elsewhere in the sidechain. The analogues are used for labelling target structures and biomolecules, such as peptides and proteins in vitro or in vivo.Type: ApplicationFiled: March 22, 2010Publication date: April 5, 2012Applicant: UNIVERSITY OF NOTTINGHAMInventors: Neil R. Thomas, Yang Yong-Qing, William C. Drewe
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Publication number: 20120071434Abstract: Disclosed herein are phosphorothioate nucleotide analogs, methods of synthesizing phosphorothioate nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs.Type: ApplicationFiled: September 19, 2011Publication date: March 22, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: David Bernard Smith, Jerome Deval, Natalia Dyatkina, Leonid Beigelman, Guangyi Wang
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Publication number: 20120071641Abstract: The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least one nucleoside of formula (2): Another aspect of the invention relates to a method of inhibiting the expression of a gene in cell, 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 2, 2010Publication date: March 22, 2012Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Alexander V. Kelin, Sudhakar Rao Takkellapati, Shigeo Matsuda
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Publication number: 20120070411Abstract: Disclosed herein are phosphoroamidate nucleotide analogs, methods of synthesizing phosphoroamidate nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the phosphoroamidate nucleotide analogs.Type: ApplicationFiled: September 19, 2011Publication date: March 22, 2012Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Guangyi Wang, Vivek Kumar Rajwanshi, Natalia Dyatkina, David Bernard Smith
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Publication number: 20120070415Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.Type: ApplicationFiled: September 19, 2011Publication date: March 22, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
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Publication number: 20120071645Abstract: The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, tetrahydropyran nucleoside analogs are provided, having one or more chiral substituents, that are useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: ApplicationFiled: December 1, 2011Publication date: March 22, 2012Applicant: Isis Pharmaceuticals, Inc.Inventors: Eric E. Swayze, Andrew M. Siwkowski, Balkrishen Bhat, Thazha P. Prakash, Charles Allerson, Punit P. Seth
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Publication number: 20120065386Abstract: This invention relates to novel method of synthesis of RNA utilizing N-2-acetyl protected guanine as nucleoside base, nucleosides, succinates, phosphoramidites, corresponding solid supports that are suitable for oligo deoxy nucleosides and RNA oligonucleotide synthesis. Our discovery using N-acetyl protected guanine as nucleoside base protecting group, which is significantly faster base labile protecting group, yet significantly more stable than commonly utilized -2-isobutyryl guanosine is a novel approach to obtain highest purity oligonucleotides. This approach is designed to lead to very high purity and very clean oligonucleotide, after efficient removal of the protecting groups, including acetyl group from guanine and to produce high purity therapeutic grade DNA oligonucleotides, RNA oligonucleotides, diagnostic DNA, diagnostic RNA for microarray platform.Type: ApplicationFiled: May 19, 2010Publication date: March 15, 2012Inventors: Suresh C. Srivastava, Naveen P. Srivastava
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Publication number: 20120052046Abstract: Phosphoramidate compounds derived from guanine bases having enhanced therapeutic potency are provided, and these compounds in particular have enhanced potency with respect to treatment of viral infections, such as hepatitis C virus. Pharmaceutical compositions, methods of preparing the compounds, and methods of using the compounds and compositions to treat viral infections are also provided.Type: ApplicationFiled: January 11, 2010Publication date: March 1, 2012Inventors: Stanley Chamberlain, Jeff Hutchins, Karolina Madela, Christopher McGuigam, John Vernachio, Mohamed Aljarah, Arnaud Gilles
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Publication number: 20120040924Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, 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, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV.Type: ApplicationFiled: February 9, 2010Publication date: February 16, 2012Applicants: EMORY UNIVERSITY, RFS PHARMA, LLC.Inventors: Jong Hyun Cho, Steven J. Coats, Raymond F. Schinazi, Hongwang Zhang, Longhu Zhou
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Publication number: 20120040345Abstract: This disclosure provides novel reversibly terminated ribonucleotides which can be used as a reagent for DNA sequencing reactions. Methods of sequencing nucleic acids using the disclosed nucleotides are also provided.Type: ApplicationFiled: August 10, 2011Publication date: February 16, 2012Applicant: ALERE SAN DIEGO, INC.Inventors: Olaf Piepenburg, Derek L. Stemple, Niall A. Armes
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Publication number: 20120029167Abstract: A drug using the magnetic properties of a metal salen complex as represented by the following general formula in order to magnetize the intended drug by chemically binding the drug to a metal salen complex so that the drug can be delivered to the target diseased site. The drug can be delivered to the diseased site using the magnetic properties of the drug per se without using a carrier made of a magnetic substance as in the conventional methods.Type: ApplicationFiled: May 20, 2011Publication date: February 2, 2012Applicants: Yoshihiro Ishikawa, IHI CorporationInventors: Yoshihiro ISHIKAWA, Haruki Eguchi
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Publication number: 20120027752Abstract: 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: July 22, 2011Publication date: February 2, 2012Applicant: Gilead Sciences, Inc.Inventors: Richard L. Mackman, Jay P. Parrish, Adrian S. Ray, Dorothy Agnes Theodore
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Publication number: 20120022014Abstract: The present disclosure describes tetrahydropyran nucleoside analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, novel tetrahydropyran nucleoside analogs are provided having at least one chiral substituent that are expected to be useful for enhancing one or more properties of oligomeric compounds such as nuclease resistance and/or binding affinity. In certain embodiments, the oligomeric compounds are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: ApplicationFiled: February 1, 2010Publication date: January 26, 2012Inventors: Thazha P. Prakash, Eric E. Swayze
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Patent number: 8101745Abstract: Methods and compositions are provided for treating lung diseases, including but not limited to infections and small cell and non-small cell lung cancer, by conjugating a drug of interest to glycerol ethers or glycerol phosphate ethers.Type: GrantFiled: December 15, 2005Date of Patent: January 24, 2012Assignee: The Regents of the University of CaliforniaInventors: Karl Y. Hostetler, James R. Beadle