The N-hereto Ring Is Five-membered (e.g., 1- -d-riboburanosyl-1, 2,3- Triazole-4-carboxamide-5-phosphate, Etc.) Patents (Class 536/26.9)
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Patent number: 10450334Abstract: The present invention provides a new photoreactive compound which can be used in technologies for photoreactions of nucleic acid, and also provides a photoreactive crosslinking agent comprising the above photoreactive compound. A photoreactive compound represented by the following formula I can be used.Type: GrantFiled: March 27, 2014Date of Patent: October 22, 2019Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCYInventors: Kenzo Fujimoto, Takashi Sakamoto, Yuya Tanaka
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Patent number: 10127349Abstract: The invention provides methods to identify pRNA- and pDNA oligomer affinity pairs. Affinity pairs comprised of nucleic acid oligomers which demonstrate no cross-reactivity (“orthogonal”) are designed using software and empirically verified by thermodynamic study and lateral flow testing. The design software uses a semi-random algorithm to build such sequences of nucleic acid oligomers based on user-input parameters for affinity strength and orthogonal stringency. These pairs can be applied for use in multi-analyte solid support and lateral flow diagnostic tests.Type: GrantFiled: July 18, 2011Date of Patent: November 13, 2018Assignee: ELITECHGROUP B.V.Inventors: Noah Scarr, Eugeny A. Lukhtanov
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Patent number: 8981078Abstract: An agent for inhibiting translesion DNA replication comprises a non-natural adenine ribose analog represented by those as set forth in FIG. 1.Type: GrantFiled: January 4, 2012Date of Patent: March 17, 2015Assignee: Case Western Reserve UniversityInventors: Anthony J. Berdis, Irene Lee, Xuemei Zhang
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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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Patent number: 8481714Abstract: The present invention provides a photoreactive crosslinking agent that is capable of crosslinking a sequence which cannot be photo-crosslinked by psoralen, and is capable of photo-crosslinking using a light having a longer wavelength, as compared with psoralen. The present invention also provides a compound having a group represented by formula (I) coupled with a group represented by formula (II).Type: GrantFiled: November 19, 2008Date of Patent: July 9, 2013Assignee: Japan Advanced Institute of Science and TechnologyInventors: Kenzo Fujimoto, Yoshinaga Yoshimura, Shinya Toba, Yukari Nitta
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Patent number: 8426569Abstract: The present invention relates to unnatural base pairs of Ds (a 7-(2 thienyl)-3H-imidazo[4,5-b]pyridine-3-yl group) and a Pa derivative (a 2-nitro-1H-pyrrole-1-yl group bearing a substituent having a ?-electron system attached at position 4) that can be replicated with high selectivity/high efficiency, and methods for replicating nucleic acids containing the unnatural base pairs. The present invention also relates to methods for incorporating an unnatural base bearing a functional substituent attached thereto into DNA by a nucleic acid replication reaction. The present invention also relates to methods for replicating and selectively collecting a nucleic acid containing an unnatural base pair from a nucleic acid pool. The present invention also relates to methods for determining a sequence of natural bases in the proximity of an unnatural base in DNA for achieving highly efficient and highly selective replication of a nucleic acid containing the unnatural base.Type: GrantFiled: March 31, 2009Date of Patent: April 23, 2013Assignees: Riken, Tagcyx BiotechnologiesInventors: Ichiro Hirao, Michiko Hirao, Shigeyuki Yokoyama
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Publication number: 20110286962Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: ApplicationFiled: May 26, 2011Publication date: November 24, 2011Inventors: Jean-Pierre SOMMADOSSI, Gilles Gosselin, Claire Pierra, Christian Perigaud, Suzanne Peyrottes
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Publication number: 20100316594Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: ApplicationFiled: June 2, 2008Publication date: December 16, 2010Inventors: Jean-Pierre Sommadossi, Paolo LaColla, Richard Storer, Gilles Gosselin
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Publication number: 20100298256Abstract: Lipid-modified phosphodiester nucleoside prodrugs are described herein. The prodrugs can be used to treat viral infections and cancer.Type: ApplicationFiled: December 23, 2008Publication date: November 25, 2010Inventors: Steven Dong, Mel C. Schroeder
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Publication number: 20100286084Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble, non-peptidic oligomer. The conjugates of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered compounds.Type: ApplicationFiled: September 18, 2008Publication date: November 11, 2010Applicant: Nektar TherapeuticsInventors: Zhongxu Ren, Jennifer Riggs-Sauthier, Timothy A. Riley, Laurie A. Vander Veen, Aaron S. Hammons
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Publication number: 20100286386Abstract: Nucleotide analogues comprising a reactive hydrazide function (formula II) used as initial synthons for preparing compounds (formula I) capable of inducing mutations or capable of inhibiting a DNA polymerase or a kinase provided. Nucleic acids comprising the nucleotide and nucleoside analogues are also provided. Methods of using the compounds are also provided.Type: ApplicationFiled: November 14, 2007Publication date: November 11, 2010Inventors: Philippe Marliere, Sylvie Pochet
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Publication number: 20100274000Abstract: The present invention provides a photoreactive crosslinking agent that is capable of crosslinking a sequence which cannot be photo-crosslinked by psoralen, and is capable of photo-crosslinking using a light having a longer wavelength, as compared with psoralen. The present invention also provides a compound having a group represented by formula (I) coupled with a group represented by formula (II).Type: ApplicationFiled: November 19, 2008Publication date: October 28, 2010Applicant: JAPAN ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGYInventors: Kenzo Fujimoto, Yoshinaga Yoshimura, Shinya Toba, Yukari Nitta
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Publication number: 20100240604Abstract: Disclosed herein are nucleotide analogs with protected phosphates, methods of synthesizing nucleotide analogs with protected phosphates and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with protected phosphates.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: Alios BioPharma, Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Harri Lonnberg
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Publication number: 20100113381Abstract: The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat esophogeal adenocarcinoma by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.Type: ApplicationFiled: September 8, 2008Publication date: May 6, 2010Inventor: Jin Q. CHENG
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Publication number: 20100104532Abstract: The invention provides unsaturated phosphonates of Formula I or a tautomer or pharmaceutically accepatble salt thereof, as described herein, as well as pharmaceutical compositions comprising the compounds, and therapeutic methods comprising administering the compounds. The compounds have anti-viral properties and are useful for treating viral infections (e.g. HCV) in animals (e.g. humans).Type: ApplicationFiled: February 8, 2008Publication date: April 29, 2010Applicant: GILEAD SCIENCES, INC.Inventors: James M. Chen, Alan X. Huang, Richard L. Mackman, Jay Parrish, Jason K. Perry, Oliver L. Saunders, David Sperandio
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Patent number: 7638496Abstract: Novel nucleoside analog compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.Type: GrantFiled: August 22, 2002Date of Patent: December 29, 2009Assignee: Valeant Pharmaceuticals North AmericaInventors: Robert Tam, Kandasamy Ramasamy, Zhi Hong, Johnson Lau
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Patent number: 7608599Abstract: The invention provides novel nucleoside compounds of formula I wherein R1, R2a, R2b, R3, R4, R5 R6, R8a, R9 and R10 are as defined herein which are useful for the treatment of Hepatitis C Virus (HCV) mediated diseases.Type: GrantFiled: August 11, 2006Date of Patent: October 27, 2009Assignee: Roche Palo Alto LLCInventors: Klaus Klumpp, Joseph Armstrong Martin, Christopher McGuigan, David Bernard Smith
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Patent number: 7560435Abstract: The present disclosure relates to a method of treatment of a human patient suffering from a B-cell lymphoproliferative disorders such as B-cell chronic lymphocytic leukemia (B-CLL), splenic marginal zone lymphoma (SMZL), mantle cell lymphoma (MCL), follicular lymphoma (FL), lymphoplasmacytic lymphoma (LPL), and Waldenström syndrome (WS), by the administration of a therapeutically effective amount of 5-aminoimidazole-4-carboxamide riboside (acadesine) or its precursors (eg. its mono-, di- and tri-5?-phosphates). This makes acadesine and its bioprecursors (eg. its mono-, di- and tri-5?-phosphates) useful as therapeutic agents for B-cell lymphoproliferative disorders in humans. The surprising feature that T cells are virtually not affected means that the side effect (immunosuppression) is minor, what represents a therapeutical advantage of acadesine over cladribine, fludarabine and other nucleosides known in the art.Type: GrantFiled: March 20, 2003Date of Patent: July 14, 2009Assignee: Advanced In Vitro Cell Technologies, S. A.Inventors: José Manuel López Blanco, Clara Campás Moya, Juan Gil Santano
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Publication number: 20090176732Abstract: Disclosed herein are nucleotide analogs with one or more protecting groups, methods of synthesizing nucleotide analogs with one or more protecting groups and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the nucleotide analogs with one or more protecting groups.Type: ApplicationFiled: December 19, 2008Publication date: July 9, 2009Applicant: Alios BioPharma Inc.Inventors: Leonid Beigelman, Lawrence Blatt, Harri Lonnberg
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Patent number: 7501506Abstract: The invention relates to compounds including at least one pentopyranosyl nucleic acid and a biomolecule conjugated through a covalent linkage to the at least one pentopyranosyl nucleic acid. The pentopyranosyl nucleic acid has at least two pentopyranosyl nucleotide subunits covalently linked between carbon 4 and carbon 2 of their respective pentopyranosyl rings. The pentopyranosyl nucleic acid does not non-covalently bond or hybridize to naturally occurring DNA or RNA. The invention also relates to compounds comprising a biotin molecule and a pentopyranosyl nucleic acid conjugated through a covalent linkage to the biotin molecule. Processes for preparing conjugates are also described.Type: GrantFiled: August 3, 2006Date of Patent: March 10, 2009Assignee: Nanogen Recognomics GmbHInventors: Christian Miculka, Norbert Windhab, Tilmann Brandstetter, Gerhard Burdinski
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Patent number: 7268119Abstract: 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: GrantFiled: February 14, 2007Date of Patent: September 11, 2007Assignee: Biota Scientific Management Pty LtdInventors: Phillip Dan Cook, Deborah K. Ewing, legal representative, Yi Jin, John Lambert, Marija Prhavc, Vasanthankumar Rajappan, Vivek K. Rajwanshi, Kandasamy Sakthivel, Gregory Ewing, deceased
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Patent number: 7153955Abstract: The invention relates to a pentopyranosylnucleoside of the formula (I) or of the formula (II) their preparation and use for the production of a therapeutic, diagnostic and/or electronic component.Type: GrantFiled: May 16, 2002Date of Patent: December 26, 2006Assignee: Nanogen Recognomics GmbHInventors: Christian Miculka, Norbert Windhab, Tilmann Brandstetter, Gerhard Burdinski
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Patent number: 7056895Abstract: Novel heterocyclic aromatic compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.Type: GrantFiled: March 11, 2002Date of Patent: June 6, 2006Assignee: Valeant Pharmaceuticals InternationalInventors: Kanda Ramasamy, Robert Tam
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Patent number: 7053199Abstract: Nucleoside analogues expressed by the following general formula where B represents an aromatic base having carbonyl oxygen at the 2-position, or a 2-hydroxyphenyl group, or oligonucleotide derivatives containing one or more of the nucleoside analogues are provided. The oligonucleotide derivatives are triplex-forming oligonucleotide derivatives which bind specifically to target double-stranded DNA with high affinity in the antigene method to form triplexes, and can thereby control and inhibit the expression of relevant genes efficiently, and which show high resistance to nucleases.Type: GrantFiled: August 29, 2001Date of Patent: May 30, 2006Inventors: Takeshi Imanishi, Satoshi Obika
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Patent number: 6777394Abstract: The present invention relates to methods and compositions for regulating the activity of imidazoline receptors. In particular, the invention relates to pharmaceutical compositions comprising imidazoleacetic acid-ribotide (IAA-RP), imidazoleacetic acid-riboside (IAA-R) and its related congeners such as pros-linked ribotide and riboside. The invention is based on the discovery that IAA-RP and to a lesser extent IAA-P bind with a high affinity to imidazoline receptors. Antibodies to IAA-RP, IAA-R are additionally provided, as well as screening methods for identification of compounds that either promote or antagonize the activity of IAA-RP, IAA-R and its related congeners. The invention further relates to diagnostic and prognostic methods for detection of abnormalities in levels or activity of IAA-RP and IAA-R. The invention encompasses treatment of disorders related to the imidazoline system, including hypertension, glaucoma, psychiatric (e.g., depression), neurological (e.g.Type: GrantFiled: July 15, 1999Date of Patent: August 17, 2004Inventor: George D. Prell
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Patent number: 6770748Abstract: An oligo- or polynucleotide analogue having one or more structures of the general formula where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is disclosed. The use of this analogue provides an oligonucleotide analogue antisense molecule, which is minimally hydrolyzable with an enzyme in vivo, has a high sense strand binding ability, and is easily synthesized.Type: GrantFiled: December 28, 2001Date of Patent: August 3, 2004Inventors: Takeshi Imanishi, Satoshi Obika
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Patent number: 6756496Abstract: Novel hydrogen-phosphonodithioate compositions are provided which are particularly useful for forming internucleotide and internucleoside linkages in oligonucleosides or oligonucleotides. The oligonucleotides and analogs thereof made by using the hydrogen-phosphonodithioate compositions may be therapeutically useful as antiviral and anticancer agents and may have other therapeutic or diagnostic uses. A method for making the hydrogen-phosphonodithioates is provided as well as a method for converting same to an activated intermediate for substitution on the phosphorus atom.Type: GrantFiled: November 19, 1997Date of Patent: June 29, 2004Assignee: ISIS Pharmaceuticals, Inc.Inventors: Brian C. Froehler, Chris A. Buhr
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Publication number: 20040002596Abstract: Nucleosides, novel nucleoside analog compounds and their novel prodrug forms are disclosed. The novel compounds, prodrugs, or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.Type: ApplicationFiled: December 13, 2002Publication date: January 1, 2004Inventors: Zhi Hong, Jean-Luc Girardet, Kanda Ramasamy, Johnson Lau
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Patent number: 6531589Abstract: The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotides under more mild conditions than existing methods. The invention further provides a nucleoside base protecting group that is stable under oligonucleotide synthesis conditions, but which can be removed under more mild conditions than existing protecting groups, as well as nucleoside synthons having such base protecting groups.Type: GrantFiled: February 8, 1996Date of Patent: March 11, 2003Assignee: Hybridon, Inc.Inventors: Radhakrishnan P. Iyer, Theresa Devlin, Ivan Habus, Dong Yu, Sudhir Agrawal, Nan-Hui Ho
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Patent number: 6518254Abstract: The present invention is a novel Ribonucleoside TRIBOSE. A process to prepare the nucleoside is also disclosed. The Ribonucleoside is a new chemical entity (NCE) not previously described. The preparation of the nucleoside portion of the molecule, also not previously described involves a thermal rearrangement of 3-Isoxazolecarboxylic acid, 5-methyl-,2-(phenylmethyl)-hydrazide, The resulting 1,2,3 ribonucleoside has anti-viral and anti-neoplastic activity potential.Type: GrantFiled: April 11, 2002Date of Patent: February 11, 2003Inventor: Henry Joseph Niemczyk
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Patent number: 6506896Abstract: The invention relates to a pentopyranosylnucleoside of the formula (I) or of the formula (II) their preparation and use for the production of a therapeutic, diagnostic and/or electronic component.Type: GrantFiled: July 11, 2000Date of Patent: January 14, 2003Assignee: Nanogen Recognomics GmbHInventors: Christian Miculka, Norbert Windhab, Tilmann Brandstetter, Gerhard Burdinski
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Patent number: 6475985Abstract: The invention provides nucleosides of formulae (I), (II), (V) and (VII) as described in the specification which possess antiviral and anticancer activity. Treatment of breast cancer is a preferred embodiment.Type: GrantFiled: September 27, 2000Date of Patent: November 5, 2002Assignee: Regents of the University of MinnesotaInventors: Carston R. Wagner, George W. Griesgraber
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Patent number: 6455508Abstract: Novel heterocyclic aromatic compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.Type: GrantFiled: October 5, 2000Date of Patent: September 24, 2002Inventors: Kanda S. Ramasamy, Robert Tam
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Patent number: 6372725Abstract: The present invention concerns new phospholipid derivatives of nucleosides of the general formula (I) in which R1 represents a straight-chained or branched, saturated or unsaturated aliphatic residue with 9-14 carbon atoms which can optionally be substituted once or several times; R2 can represent a straight-chained or branched, saturated or unsaturated aliphatic residue with 8-12 carbon atoms which can optionally be substituted once or several times; m is 2 or 3; A can represent a methylene group or an oxygen; Nuc can be a nucleoside or a residue derived from a nucleoside derivative; and tautomers thereof and their physiologically tolerated salts of inorganic and organic acids and bases as well as pharmaceutical preparations containing these compounds.Type: GrantFiled: December 4, 1998Date of Patent: April 16, 2002Inventors: Harald Zilch, Dieter Herrmann
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Patent number: 6271358Abstract: 2′-O-modified ribosyl nucleosides and modified oligonucleotides containing such nucleotides are disclosed. Oligonucleotides are disclosed that have increased binding affinity as shown by molecular modeling experiments. The 2′-O-modified nucleosides of the invention include ring structures that position the sugar moiety of the nucleosides preferentially in 3′ endo geometries.Type: GrantFiled: July 27, 1998Date of Patent: August 7, 2001Assignee: Isis Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Venkatraman Mohan, Herb Boswell
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Patent number: 6268490Abstract: An oligo- or polynucleotide analogue having one or more structures of the general formula where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is disclosed. The use of this analogue provides an oligonucleotide analogue antisense molecule, which is minimally hydrolyzable with an enzyme in vivo, has a high sense strand binding ability, and is easily synthesized.Type: GrantFiled: September 7, 1999Date of Patent: July 31, 2001Assignee: Takeshi ImanishiInventors: Takeshi Imanishi, Satoshi Obika
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Patent number: 6252060Abstract: Compounds for treating hepatitis B infections. The compounds consist of nucleoside analogues having anti-hepatitis B activity which are linked, commonly through a 5′ phosphate of the pentose residue, to one of a selected group of lipids. The lipophilic nature of these compounds provides an advantage over the use of the nucleoside analogue alone, making it possible to incorporate them into the lamellar structure of liposomes, either alone or in combination with similar lipid molecules. In the form of appropriately sized liposomes, these anti-hepatitis B agents are preferentially taken up by the liver cells which have been found to harbor the target virus.Type: GrantFiled: April 4, 1994Date of Patent: June 26, 2001Assignee: NeXstar Pharmaceuticals, Inc.Inventor: Karl Y. Hostetler
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Patent number: RE44779Abstract: An oligo- or polynucleotide analogue having one or more structures of the general formula where B is a pyrimidine or purine nucleic acid base, or an analogue thereof, is disclosed. The use of this analogue provides an oligonucleotide analogue antisense molecule, which is minimally hydrolyzable with an enzyme in vivo, has a high sense strand binding ability, and is easily synthesized.Type: GrantFiled: June 26, 2012Date of Patent: February 25, 2014Assignees: Santaris Pharma A/S, Exiqon A/SInventors: Takeshi Imanishi, Satoshi Obika