The Phosphorus Is Part Of A Ring Patents (Class 536/26.11)
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Patent number: 9504705Abstract: Described herein is a combination that includes compound (A) of the formula and compound (B) of the formula or a pharmaceutically acceptable salt(s) of the foregoing, for ameliorating and/or treating a hepatitis C viral infection.Type: GrantFiled: April 3, 2014Date of Patent: November 29, 2016Assignee: Alios BioPharma, Inc.Inventors: Julie Krop, Margaret James Koziel, Lawrence M. Blatt, John Fry, Sushmita Mukherjee Chanda
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Publication number: 20150080457Abstract: The present invention provides nucleosides and oligonucleotides comprising a 5? phosphate mimics of formula (IVc) or (Vc), One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such dinucleotide of formula (Ia). 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: November 24, 2014Publication date: March 19, 2015Inventors: Muthiah MANOHARAN, Kallanthottathil G. RAJEEV, Marija PRHAVC, Ivan ZLATEV
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Patent number: 8846638Abstract: The present invention provides nucleoside phosphoramidate compounds of Formula I, where R1, R2a, R2b, R3, R4, R5a, R5b, R6, R7, R8a, R8b, M and W are as defined herein. The invention further includes pharmaceutical compositions comprising a compound of Formula I, methods of use of these compounds for treating a viral infection, and methods of producing these compounds.Type: GrantFiled: May 17, 2013Date of Patent: September 30, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Jun Ma, Guoqiang Wang
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Patent number: 8772474Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.Type: GrantFiled: December 20, 2011Date of Patent: July 8, 2014Assignee: Alios BioPharma, Inc.Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Patent number: 8759510Abstract: 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: April 5, 2012Date of Patent: June 24, 2014Assignee: Gilead Pharmasset LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Ganapati Reddy Pamulapati, Bruce S. Ross, Michael Joseph Sofia
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Patent number: 8716263Abstract: 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: GrantFiled: December 23, 2009Date of Patent: May 6, 2014Assignee: 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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Patent number: 8629265Abstract: The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method a nucleophile is first dissolved in a non-aqueous solvent and dried, and a cyclosaligenyl phosphate compound is subsequently added to the solution.Type: GrantFiled: August 6, 2009Date of Patent: January 14, 2014Assignee: Universitaet HamburgInventors: Chris Meier, Saskia Wolf, Svenja Warnecke
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Patent number: 8507460Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: GrantFiled: October 12, 2012Date of Patent: August 13, 2013Assignee: Idenix Pharmaceuticals, Inc.Inventors: Dominique Surleraux, Cyril B. Dousson, Christophe Claude Parsy
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Publication number: 20130184450Abstract: A method for preparing a phosphorothioate RNA based on the oxazaphospholidine method, wherein cyanoethoxymethyl group is used instead of tert-butyldimethylsilyl group as a protective group of 2?-hydroxyl group of RNA.Type: ApplicationFiled: March 4, 2011Publication date: July 18, 2013Applicant: THE UNIVERSITY OF TOKYOInventors: Takeshi Wada, Yohei Nukaga
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Publication number: 20130178612Abstract: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.Type: ApplicationFiled: September 22, 2011Publication date: July 11, 2013Applicant: CHIRALGEN, LTD.Inventors: Takeshi Wada, Mamoru Shimizu
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Patent number: 8450293Abstract: The invention provides analogs cyclic diguanosine monophosphate (c-di-GMP) having different substituents at the guanine C8 position.Type: GrantFiled: August 10, 2011Date of Patent: May 28, 2013Assignee: Rutgers, The State University of New JerseyInventors: Roger A. Jones, Elizabeth Veliath
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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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Publication number: 20120165286Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Publication number: 20120157511Abstract: The present invention provides nucleosides and oligonucleotides comprising a 5? phosphate mimics of formula (IVc) or (Vc). One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such dinucleotide of formula (Ia). 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: July 7, 2010Publication date: June 21, 2012Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Marija Prhavc, Ivan Zlatev
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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: 8153787Abstract: The present invention provides 5-azacytosine derivatives with antiviral activity, specifically having viral replication inhibiting properties, more particularly in DNA viruses such as pox-, papilloma- and herpes viruses in humans. The invention also provides pharmaceutical compositions comprising such 5-azacytosine derivatives as active ingredients in combination with pharmaceutically acceptable carriers, which are useful for the treatment of subjects suffering from viral infections.Type: GrantFiled: December 8, 2006Date of Patent: April 10, 2012Assignees: K.U. Leuven Research & Development, Institute of Organic Chemistry and Biochemistry Academy of Sciences of the Czech RepublicInventors: Antonin Holy, Marcela Krecmerova, Alois Piskala, Graciela Andrei, Robert Snoeck, Erik De Clercq, Johan Neyts, Lieve Naesens
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Publication number: 20110212437Abstract: Methods, Compositions, and Systems are provided for nucleic acid sequencing where the sequential incorporation of nucleotides uses two distinct chemical steps. A plurality of nucleotide analogs, each having a labeled leaving group at its 3? hydroxyl can be sequentially added to a growing strand in the presence of a selective cleaving activity that cleaves the 3? hydroxyl leaving group preferentially after it has been incorporated. The selective cleaving agent can comprise an exonuclease activity, and the exonuclease activity can be a polymerase-associated exonuclease activity. Nucleotide analogs having labels on both a cleavable polyphosphate portion and on a 3? hydroxyl leaving group can provide signals characteristic of nucleotide analog incorporation. Systems having illumination optics, collection optics, and substrates observe signals from the labels as they are being incorporated into a growing nucleic acid strand, allowing for the sequencing of template nucleic acids.Type: ApplicationFiled: February 8, 2011Publication date: September 1, 2011Applicant: Pacific Biosciences of California, Inc.Inventors: Robin Emig, Lei Jia, Jeremiah Hanes, Lubomir Sebo
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Patent number: 7217815Abstract: Various 2?-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and combinatorial library approaches. Contemplated compounds are particularly useful as therapeutic agents, and especially as antiviral agents.Type: GrantFiled: October 23, 2002Date of Patent: May 15, 2007Assignee: Valeant Pharmaceuticals North AmericaInventors: Haoyun An, Yili Ding, Stephanie Z. Shaw, Zhi Hong
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Patent number: 6965041Abstract: The present invention provides a compound of formula (I), (II), or (III), wherein R1, R2, R2?, R3, and R3? are the same or different and each is H an alkyl, an alkenyl, an alkynyl, a cycloalkyl, an aryl, or an aralkyl. Alternatively, either of R2 or R2? combined with either of R3 or R3? comprises a ring. R4 is a protecting group or a solid support R5 is H or an alkyl. R6 is a protecting group, an amidoalkyl, an alkyl, an alkyl ketone, an alkenyl, an alkynyl, a cycloalkyl, an aryl, or an aralkyl. R15 is H or a protecting group. Q and Q1 are the same or different and each is a nucleoside, an oligonucleotide comprising a nucleoside, or an oligomer comprising a nucleoside, which is of formula (a) or (b), wherein B is a labeling group, an alkyl, an alkenyl, an alkynyl, a cyclic group optionally containing one or more heteroatoms, or an amino; and, E is H, a halogen, a hydroxy, an alkoxy, an ester, an amino or a protecting group. X and X1 are independently O, S, or Se, and n is an integer from 1 to about 300.Type: GrantFiled: February 16, 2000Date of Patent: November 15, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Serge L. Beaucage, Andrzej Wilk, Andrzej Grajkowski
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Patent number: 6875859Abstract: 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.Type: GrantFiled: March 11, 2002Date of Patent: April 5, 2005Assignee: Roche Diagnostics GmbHInventors: Klaus Mühlegger, Herbert Von Der Eltz
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Patent number: 6812342Abstract: The present invention is directed to the field of organic chemistry in general and specifically to the preparation of hydrophobic derivatives of cyclic ADP ribose. One form of the present invention is the composition of one or more hydrophobic derivatives of cyclic ADP ribose. In another form of the present invention, a method for preparing a hydrophobic composition is described. Compositions of the present invention are useful for the study of in vivo calcium metabolism.Type: GrantFiled: June 20, 2002Date of Patent: November 2, 2004Assignee: Board of Regents, The University of Texas SystemInventor: Wen Hong Li
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Patent number: 6593307Abstract: The present invention provides a compound of formula I: wherein A, D, R1, and R2 are as defined in the specification; or a salt or a detectably labeled derivative thereof. The invention also provides methods of using the compound of formula I or a salt or a detectably labeled derivative thereof for promoting the proliferation of hemopoietic progenitor cells without cell differentiation.Type: GrantFiled: October 27, 2000Date of Patent: July 15, 2003Assignee: Regents of the University of MinnesotaInventors: Timothy F. Walseth, Antonio De Flora, Elena Zocchi, Marina Podesta, Long Wong, Robert A. Aarhus, Hon Cheung Lee
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Publication number: 20030114660Abstract: Methods and Intermediates for the Preparation of Oligomers Containing Diastereomerically Enriched Phosphorothioate Linkages are Disclosed.Type: ApplicationFiled: September 24, 2002Publication date: June 19, 2003Inventors: George Just, Zhili Xin, Eric Marsault, Yi Jin, Jianchao Wang
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Publication number: 20030013869Abstract: The present invention is directed to the field of organic chemistry in general and specifically to the preparation of hydrophobic derivatives of cyclic ADP ribose. One form of the present invention is the composition of one or more hydrophobic derivatives of cyclic ADP ribose. In another form of the present invention, a method for preparing a hydrophobic composition is described. Compositions of the present invention are useful for the study of in vivo calcium metabolism.Type: ApplicationFiled: June 20, 2002Publication date: January 16, 2003Inventor: Wen Hong Li