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Class 536/28.54 - Alkyl, or substituted alkyl, bonded directly to the 5-position of the diazine ring (e.g., thymidine, 5-methyl uridine, etc.)


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein an alkyl group, or a substituted alkyl
No. of applications: 29
Last issue date: 03/22/2012


Application No.Application TitleIssue Date
20120071641NUCLEIC ACID CHEMICAL MODIFICATIONS
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 ... 		03/22/2012
20120053337SYNTHESIS OF 2'-Deoxy-2'-[18F]FLUORO-5-METHYL-1-B-D-ARABINOFURANOSYLURACIL (18F-FMAU)
The present invention relates to methods of synthesizing 18F-FMAU. In particular, 18F-FMAU is synthesized using one-pot reaction conditions in the presence of Friedel-Crafts catalysts. The one-pot reaction conditions are incorporated into a fully a... 		03/01/2012
20120004404RADIOLABELLING METHODS
The present invention relates to the field of [18F] radiofluorination chemistry for the preparation of Positron Emission Tomography (PET) radioligands and [18F] radiofluorinating reagents. The invention further provides kits for preparation of the ... 		01/05/2012
20110294122Synthesis of 2', 3'-Dideoxynucleosides for Automated DNA Synthesis and Pyrophosphorolysis Activated Polymerization
Methods for preparation of 2′,3′-dideoxynucleotides support structures, such as 2′,3′-dideoxyguanosine, 2′,3′-dideoxyadenosine, and 3′-deoxythymidine support structures are disclosed. Various methods of using such structures are also provided, such as thei... 		12/01/2011
20110269709PRODRUGS CONTAINING NOVEL BIO-CLEAVABLE LINKERS
The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable c... 		11/03/2011
20110184159PROCESS FOR PRODUCTION OF RADIOPHARMACEUTICALS
The present invention relates to novel processes for the production of F-18 labeled radiotracers for Positron Emission Tomography (PET). The invention also comprises radiopharmaceutical kits using these processes.... 		07/28/2011
20110166096URACIL DERIVATIVES AND USE THEREOF
Disclosed are uracil derivatives of the formula (I):

wherein R1, R2, R3, and X are as defined herein, and use thereof as therapeutic agents. The uracil derivatives are used in...

07/07/2011
20110130440NON-NATURAL RIBONUCLEOTIDES, AND METHODS OF USE THEREOF
One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such modified nucleosides. Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oli... 		06/02/2011
20110082286Method for Generating Aptamers with Improved Off-Rates
The present disclosure describes improved SELEX methods for producing aptamers that are capable of binding to target molecules and improved photoSELEX methods for producing photoreactive aptamers that are capable of both binding and covalently crosslinking to target mol... 		04/07/2011
20110059180Method for Preparing Nanoparticles Based on Functional Amphiphilic Molecules or Macromolecules, and the Use Thereof
The invention relates to a method for preparing nanoparticles based on functional amphiphilic molecules or macromolecules, optionally in the presence of at least one colipide, enabling the encapsulation of therapeutic agents, especially anti-tumoral agents, and the use ... 		03/10/2011
20110054164PRODUCTION PROCESS OF ETHYNYLTHYMIDINE COMPOUNDS FROM 5-METHYLURIDINE AS A STARTING MATERIAL
The present invention provides a process for producing 2′,3′-didehydro-3′-deoxy-4′-ethynylthymidine, which is useful as a medicine, in an efficient and industrially advantageous manner, and more specifically, provides a process for producing 2′,3′-didehydro-... 		03/03/2011
20110040083PHOTORESPONSIVE NUCLEIC ACID MANUFACTURING METHOD
The present invention provides a manufacturing method that can easily manufacture a compound known as photoresponsive (photocoupling) nucleic acids at high yield in a shorter period of time than that of the conventional technology. The present invention relates to a met... 		02/17/2011
20110009607METHOD FOR PREPARING DNA FRAGMENT HAVING STICKY END
The present invention provides a method for preparing a DNA fragment, in which a desired double-stranded DNA fragment having a sticky end is directly and easily obtained from an amplification product (an amplified fragment) after PCR without a restriction enzyme digesti... 		01/13/2011
20100292458NOVEL PHOTOLABILE PROTECTIVE GROUPS FOR IMPROVED PROCESSES TO PREPARE OLIGONUCLEOTIDE ARRAYS
The present invention discloses novel and improved nucleosidic and nucleotidic compounds that are useful in the light-directed synthesis of oligonucleotides, as well as, methods and reagents for their preparation. These compounds are characterized by novel photolabile p... 		11/18/2010
20100280235METHOD FOR PRODUCING 4'ETHYNYL d4T
Disclosed is a method for mass-producing 4′-ethynyl d4T (4′-ethynyl-2′,3′-didehydro-3′-deoxythymidine) by a simpler process at low cost. Specifically disclosed is a method for producing 4′-ethynyl d4T, which is characterized by comprising a step for introduc... 		11/04/2010
20100137573SYNTHESIS OF SELENIUM-DERIVATIZED NUCLEOSIDES, NUCLEOTIDES, PHOSPHORAMIDITES, TRIPHOSPHATES AND NUCLEIC ACIDS
The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids and methods for their synthesis. Selenium derivatives of both ribonucleic ... 		06/03/2010
20100130440ANTIVIRAL NUCLEOSIDES
Disclosed are nucleosides which are useful in diagnosing and treating viral infections, for example, infections caused by hepatitis B virus (HBV), and herpes viruses including Epstein Barr virus.... 		05/27/2010
20100113763METHOD FOR PREPARATION OF ORGANOFLUORO COMPOUNDS IN ALCOHOL SOLVENTS
The present invention relates to a method for preparation of organofluoro compounds containing radioactive isotope fluorine-18. More particularly, the present invention relates to a method for preparation of organofluoro compound [18F]florbetaben or [18<... 		05/06/2010
20100092971COMPOUND HAVING STRUCTURE DERIVED FROM MONONUCLEOSIDE OR MONONUCLEOTIDE, NUCLEIC ACID, LABELING SUBSTANCE, AND METHOD AND KIT FOR DETECTION OF NUCLEIC ACID
The present invention provides, for example, a labeling substance that allows the double helix structure of a nucleic acid to be detected effectively. The present invention provides a compound having a structure derived from mononucleoside or mononucleotide, with the st... 		04/15/2010
20100068786METHODS AND COMPOSITIONS FOR REVERSING P-GLYCOPROTEIN MEDICATED DRUG RESISTANCE
A method for inhibiting therapeutic drug resistance within a cell over-expressing a membrane protein is provided. The method comprises synthesizing a dimeric prodrug inhibitor of a monomeric therapeutic agent; administering the dimeric prodrug inhibitor to the membrane ... 		03/18/2010
20100048504CRYSTALLINE AND AMORPHOUS FORMS OF BETA-L-DEOXYTHYMIDINE
Physical forms of beta-L-2′-deoxythymidine are disclosed that can be characterized by physical appearance, purity levels, Infra-Red and Raman spectroscopy, X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These forms of beta-L-2′-de... 		02/25/2010
20100009353Dye Compounds and the Use of their Labelled Conjugates
Novel rhodamine dye compounds, labelled conjugates comprising the dyes are described, together with methods for their use. The dyes and labelled conjugates are useful as molecular probes in a variety of applications, such as in assays involving staining of cells, protei... 		01/14/2010
20090258931CHIMERIC OLIGOMERIC COMPOUNDS COMPRISING ALTERNATING REGIONS OF NORTHERN AND SOUTHERN CONFORMATIONAL GEOMETRY
The present invention relates to novel chimeric oligomeric compounds having a plurality of alternating regions having either RNA like having northern or 3′-endo conformational geometry (3′-endo regions) or DNA like having southern or C2′-endo/O4′-endo conformati... 		10/15/2009
20090082306DEUTERIUM-ENRICHED TELBIVUDINE
The present application describes deuterium-enriched telbivudine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.... 		03/26/2009
20090018325PROCESS FOR PREPARING L-NUCLEIC ACID DERIVATIVES AND INTERMEDIATES THEREOF
A novel method has been found to produce 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine. According to these methods,... 		01/15/2009
20080292548COMPOUNDS AND METHODS FOR 18F LABELED AGENTS
The present invention relates to novel compounds suitable for or already radiolabeled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging. Such labeled compounds are characterized by Formula II, wherein the substituents... 		11/27/2008
20080064868Novel Dideoxynucleoside Derivatives
The present invention discloses a 5′-amino-2′-fluoro-2′,5′-dideoxynucleoside derivative represented by the following formula [1]:

(wherein R1 represents a nucleic acid base which may have a...

03/13/2008
200800396203'-End Nucleoside Unit Comprising Phosphoramidite
The purpose of the present invention is therefore to provide a method for binding a 3′-end nucleoside unit comprising any base to a hydroxyl group on a solid-phase support under completely the same condition as in DNA chain elongation reaction. The present invention r... 		02/14/2008
20070265224Nucleotide mimics and their prodrugs
The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a ... 		11/15/2007
 
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