Class / Patent application number | Description | Number of patent applications / Date published |
536260700 | The N-hetero ring is part of a bicyclic ring system | 29 |
20080207890 | Reagents for the Improved Synthesis of Isoguanosine Containing Oligonucleotides - The present invention provides the combination of the O-2 diphenylcarbamoyl (“DPC”) and N-6 dimethy-laminomethylidene (“DMF”) protecting groups for isoguanosine nucleosides that can be utilized in oligonucleotide synthesis. | 08-28-2008 |
20090281299 | OLIGONUCLEOTIDES COMPRISING A NON-PHOSPHATE BACKBONE LINKAGE - One aspect of the present invention relates to a ribonucleoside substituted with a phosphonamidite group at the 3′-position. In certain embodiments, the phosphonamidite is an alkyl phosphonamidite. Another aspect of the present invention relates to a double-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a non-phosphate linkage occurs in only one strand. In certain embodiments, a non-phosphate linkage occurs in both strands. In certain embodiments, a ligand is bound to one of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, a ligand is bound to both of the oligonucleotide strands comprising the double-stranded oligonucleotide. In certain embodiments, the oligonucleotide strands comprise at least one modified sugar moiety. Another aspect of the present invention relates to a single-stranded oligonucleotide comprising at least one non-phosphate linkage. Representative non-phosphate linkages include phosphonate, hydroxylamine, hydroxylhydrazinyl, amide, and carbamate linkages. In certain embodiments, the non-phosphate linkage is a phosphonate linkage. In certain embodiments, a ligand is bound to the oligonucleotide strand. In certain embodiments, the oligonucleotide comprises at least one modified sugar moiety. | 11-12-2009 |
20100249393 | COLORIMETRIC-OXYCARBONYL PROTECTING GROUPS FOR USE IN ORGANIC SYNTHESES - The present invention provides for reagents for the introduction of colorimetric-oxycarbonyl protecting groups, compounds bearing colorimetric-oxycarbonyl protecting groups, and the use thereof in solid-supported organic syntheses of oligonucleotides, polypeptides, polysaccharides, and combinatorial libraries. | 09-30-2010 |
20100311960 | Phosphinoamidite Carboxylates and Analogs Thereof in the Synthesis of Oligonucleotide Having Reduced Internucleotide Charge - Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III) | 12-09-2010 |
20110015382 | Synthesis of N-FMOC protected deoxy nucleosides, ribo nucleosides, modified deoxy and ribo nucleosides, and phosphoramidites, and their use in oligonucleotide synthesis - This invention relates to synthesis of novel -N-FMOC protected nucleosides, succinates, phosphoramidites, corresponding solid supports that are suitable for oligo deoxy nucleosides and RNA oligonucleotide synthesis. Our discovery using N-FMOC as nucleoside base protecting group, which is highly base labile protecting group 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 and to produce high purity therapeutic grade DNA oligonucleotides, RNA oligonucleotides, diagnostic DNA, diagnostic RNA for microarray platform. The deprotection of FMOC protecting groups of the natural deoxy and ribonucleosides occurs under very mild deprotection conditions such as mild bases, secondary and tertiary amines for removal of such groups under such conditions would allows synthesis of various DNA and RNA of highest purity for diagnostics and therapeutic application. This approach is further designed to use FMOC protecting group on various base sensitive nucleoside, and for use in oligo peptide synthesis and for support bound oligo nucleotides. DNA oligonucleotides containing 3′-end dA at the 3′-terminal will be produced using the FMOC-dA-supports would lead to much reduced M−1 deletion sequences, and thereby high purity. | 01-20-2011 |
20110015383 | DERIVATIVES OF NUCLEOSIDE-5'-O-HYPOPHOSPHATES AND THEIR MONO- AND DITHIOHYPOPHOSPHATE ANALOGUES AND THE PROCESS FOR THE MANUFACTURE THEREOF - The subject of the invention includes derivatives of nucleoside-5′-O-hypophosphates and their mono- and dithiohypophosphate analogues, in particular 5′-O-[β,β-dialkyl-(α-thiohypophosphate)]-, 5′-O-[β,β-dialkyl-(α,α-dithiohypophosphate)]-, 5′-O-[β,α-dialkyl-(α,β-dithiohypophosphate)-, 5′-O-[β-alkyl-(α-thiohypophosphate)]-, 5′-O-[β-alkyl-(α, oc-dithiohypophosphate)]-, 5′-O-(a-thiohypophosphate)]- and 5′-O-(a,a-dithiohypophosphate)nucleosides. | 01-20-2011 |
20110077390 | BICYCLIC CYCLOHEXITOL NUCLEIC ACID ANALOGS - The present disclosure provides bicyclic cyclohexitol nucleoside analogs of formula I and oligomeric compounds comprising these nucleoside analogs. These bicyclic nucleoside analogs are expected to be useful for enhancing properties of oligomeric compounds including for example nuclease resistance. | 03-31-2011 |
20120071645 | TETRAHYDROPYRAN NUCLEIC ACID ANALOGS - 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. | 03-22-2012 |
20120202983 | Conjugates and Compositions for Cellular Delivery - 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. | 08-09-2012 |
20130203978 | NUCLEOSIDES WITH ANTIVIRAL AND ANTICANCER ACTIVITY - The invention provides a compound of formula (I), 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. | 08-08-2013 |
20130281686 | METHODS FOR THE PREPARATION OF DIASTEROMERICALLY PURE PHOSPHORAMIDATE PRODRUGS - Provided are methods and intermediates for preparing diastereomerically pure phosphoramidate prodrugs of nucleosides of Formulas Ia and Ib: | 10-24-2013 |
20140163216 | COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS - 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. | 06-12-2014 |
20140288294 | ANTIVIRAL COMPOUNDS - The invention is related to phosphorus substituted anti-viral inhibitory compounds, 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. | 09-25-2014 |
20150315229 | METHOD FOR LIQUID-PHASE SYNTHESIS OF NUCLEIC ACID - In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R | 11-05-2015 |
20150337002 | NUCLEOSIDE AND NUCLEOTIDE HAVING SULFONAMIDE STRUCTURE - The present invention provides compounds shown by the formula: | 11-26-2015 |
20160075732 | RADICAL ORBITAL SWITCHING - Described herein are distonic radical anion species of formula (I): RAD-L-NEG; wherein RAD is a group comprising a radical; NEG is a group comprising an anion, which is capable of bonding to a proton or other cation; L is a linker that links NEG to RAD; and the radical of RAD is not π-conjugated to the anion of NEG. | 03-17-2016 |
20160159845 | NUCLEOSIDES WITH ANTIVIRAL AND ANTICANCER ACTIVITY - The invention provides a compound of formula I: | 06-09-2016 |
536260710 | Preparing purine nucleotides | 11 |
20090118491 | STABLE SALT OF 3'-PHOSPHOADENOSINE 5'-PHOSPHOSULFATE - The present invention provides a stable salt of 3′-phosphoadenosine 5′-phosphosulfate (PAPS) and a production method therefor. | 05-07-2009 |
20090326213 | PROCESS FOR PRODUCTION OF CRYSTAL OF PURINE NUCLEOSIDE COMPOUND - Crystals of a purine nucleoside compound, particularly crystals of 2′,3′-dideoxyinosine, which have excellent storage stability and have a concentration of phosphate attached to the crystal of 25 ppm or more, may be produce by: (1) preparing an aqueous solution containing phosphate ion (PO | 12-31-2009 |
20100036111 | METHOD FOR REPLICATING NUCLEIC ACIDS AND NOVEL UNNATURAL BASE PAIRS - The present invention relates to a method for nucleic acid replication and novel artificial base pairs. | 02-11-2010 |
20110015384 | SULFURIZATION AGENT AND ITS USE - The use of a sulfurizing agent of formula A: or a salt, hydrate, solvate, or a mixture thereof, in which all R groups, independently, represent H or an organic group, in sulfurization. The sulfurizing agent is preferably a formamidine disulfide. It is found a particularly suitable alternative to existing sulfurizing agents, since it is easy to synthesize from readily available, cheap starting materials. | 01-20-2011 |
20110245484 | STEREOSELECTIVE SYNTHESIS OF PHOSPHORUS CONTAINING ACTIVES - Disclosed herein are phosphorus-containing actives, their use as actives for treating diseases, and a stereoselective process for preparing the same. Also disclosed herein are useful synthetic intermediates and processes for preparing the same. | 10-06-2011 |
20120142908 | COMPOUNDS FOR THE SYNTHETIC INTRODUCTION OF N-ALKYL NUCLEOSIDES INTO DNA OLIGONUCLEOTIDES - The present invention provides for compounds of Formula I: | 06-07-2012 |
20140039179 | PHOSPHONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION - 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. These compounds can be described by general formula (II) | 02-06-2014 |
20140206856 | GLYCOSIDE COMPOUND, METHOD FOR PRODUCING THIOETHER, ETHER, METHOD FOR PRODUCING ETHER, METHOD FOR PRODUCING GLYCOSIDE COMPOUND, METHOD FOR PRODUCING NUCLEIC ACID - 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 | 07-24-2014 |
20140316127 | PHOSPHONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION - 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. These compounds can be described by general formula (II) | 10-23-2014 |
536260720 | Guanosine nucleotide preparation | 2 |
20100081802 | Synthesis of Phosphitylated Compounds Using a Quaternary Heterocyclic Activator - A method for preparing a phosphitylated compound comprising the step of: -reacting 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 R | 04-01-2010 |
20120316328 | SYNTHESIS OF PHOSPHITYLATED COMPOUNDS USING A QUATERNARY HETEROCYCLIC ACTIVATOR - 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 R | 12-13-2012 |
536260740 | Inosine nucleotide | 1 |
20120065386 | SYNTHESIS OF LABILE BASE PROTECTED - MODIFIED DEOXY & MODIFIED RIBO NUCLEOSIDES, CORRESPONDING PHOSPHORAMIDITES AND SUPPORTS AND THEIR USE IN HIGH PURITY OLIGONUCLEOTIDE SYNTHESIS - 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. The deprotection of acetyl protecting groups of the natural deoxy and ribonucleosides occurs under substantially reduced time in contact with mild deprotection conditions such as mild bases, secondary amines for removal of such groups under such conditions would allows synthesis of various DNA and RNA of highest purity for diagnostics and therapeutic application. This approach is designed to lead to high purity large | 03-15-2012 |