Class / Patent application number | Description | Number of patent applications / Date published |
536280100 | N-glycosides wherein the N is part of a six-membered hetero ring (e.g., diazines, etc.) | 88 |
20090131652 | CAPRAZENE AS A NOVEL COMPOUND AND DERIVATIVES THEREOF, AND CAPRAZOL AS A NOVEL COMPOUND AND DERIVATIVES THEREOF - Caprazene and caprazol could be synthesized by hydrolysis of a caprazamycin. There could be synthesized a caprazene-1′″-amide derivative of the formula (II) | 05-21-2009 |
20120172584 | NICOTYL RIBOSIDE COMPOSITIONS AND METHODS OF USE - The invention relates to compositions of nicotinoyl ribosides and nicotinamide riboside derivatives and their methods of use. In some embodiments, the invention relates to methods of making nicotinoyl ribosides. In some embodiments, the invention relates to pharmaceutical compositions and nutritional supplements containing a nicotinoyl riboside. In further embodiments, the invention relates to methods of using nicotinoyl ribosides and nicotinamide riboside derivatives that promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for improving cell and tissue survival. | 07-05-2012 |
20160168184 | METHODS OF PREPARING NICOTINAMIDE RIBOSIDE AND DERIVATIVES THEREOF | 06-16-2016 |
536280200 | Multideoxy or didehydro | 13 |
20080312428 | Process for the Large Scale Production of Stavudine - The present invention provides a method for preparing pure Stavudine having purity more than 99.5% comprises: i) Converting 3′,5′-anhydrothymidine to crude Stavudine, ii) Converting crude Stavudine to stable solvates of Stavudine, iii) Desolvation of the solvates to give pure Stavudine. The present invention also disclosed novel solvates of Stavudine and conversion of novel Stavudine solvates to Stavudine. | 12-18-2008 |
20090264637 | PROCESS FOR PREPARING DISULPHIDES AND THIOSULPHINATES AND COMPOUNDS PREPARED - Process for preparing a compound of the formula (I) R1-S(O) | 10-22-2009 |
20100105887 | PROCESS FOR THE PREPARATION OF GEMCITABINE HYDROCHLORIDE - Disclosed is the preparation of 2-deoxy-D-erythro-2,2-difluoro-ribofuranose-3,5-dibenzoate: | 04-29-2010 |
20100179314 | Novel and Highly Stereoselective Process for Preparing Gemcitabine and Intermediates Thereof - The present invention provides a novel and highly stereoselective process for preparing gemcitabine, which is suitable for industrial production, wherein, it includes the following reactions. Additionally, the invention discloses the key intermediates. The definition for the groups of G1, G2, G3, G4, and G5 are described in the specification. | 07-15-2010 |
20110054164 | PRODUCTION 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-3′-deoxy-4′-ethynylthymidine as shown below. | 03-03-2011 |
20110172410 | ANTIVIRAL NUCLEOSIDES - 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process. | 07-14-2011 |
20110224421 | PREPARATION OF INTERMEDIATES USEFUL IN THE SYNTHESIS OF 2'-CYANO-2'-DEOXY-N4-PALMI-TOYL-1-BETA-D-ARABINOFURANOSYLCYTOSINE - The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2′ into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2′-cyano-2′-deoxy-N | 09-15-2011 |
20120238740 | NON-POLAR AND POLAR LEAVING GROUPS - The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group L | 09-20-2012 |
20120322995 | beta-DIHYDROFURAN DERIVING COMPOUND, METHOD FOR PRODUCING beta-DIHYDROFURAN DERIVING COMPOUND OR beta-TETRAHYDROFURAN DERIVING COMPOUND, beta-GLYCOSIDE COMPOUND, METHOD FOR PRODUCING beta GLYCOSIDE COMPOUND, AND METHOD FOR PRODUCING 4'-ETHYNYL D4T AND ANALOGUE COMPOUNDS THEREOF - The invention provides a process for producing a β-dihydrofuran derivative represented by formula (1) or a β-tetrahydrofuran derivative represented by formula (4), characterized in that the process includes causing a dialkyl dicarbonate, a diaralkyl dicarbonate, or a halide to act on a diol compound represented by formula (2) or (3). The invention also provides a process for producing 4′-ethynyl-2′,3′-didehydro-3′-deoxythymidine or an analog thereof, the process including glycosylation and deprotection. | 12-20-2012 |
20130005956 | Synthesis of 18F-labeled Tracers in Hydrous Organic Solvents - A method for synthesizing an | 01-03-2013 |
20130023657 | SYSTEM FOR RADIOPHARMACEUTICAL PREPARATION INVOLVING SOLID AND LIQUID PHASE INTERACTIONS - A system and method for radiopharmaceutical production involving solid and liquid phase interactions are provided, the system including a module for facilitating solid and liquid phase interactions by performing techniques including high pressure, low pressure, and solid phase extraction. The system includes various modular components, each of which performs steps in the process of preparing radiopharmaceuticals, and one or more radiation detectors monitor the radiation level and path of various products. The modular components may be added to and removed from the system easily to allow for flexibility in the operation of the system. An HPLC module may be included to purify radiopharmaceuticals. | 01-24-2013 |
20130102772 | SYSTEMS, METHODS AND DEVICES FOR PRODUCING, MANUFACTURING AND CONTROL OF RADIOPHARMACEUTICALS-FULL - Systems, methods, and devices for generating radionuclides for use in production of radiopharmaceuticals; synthesizing the radionuclides generated and removing any unwanted products; measuring the quantity and activity level of the synthesized radionuclides; distributively delivering the radionuclides in appropriate quantities to modular cassette synthesis units in a modular cassette subsystem for contemporaneous/parallel production of radiopharmaceutical output and that allow reuse and/or quick, safe, and disposable replacement of portions of the subsystem; delivering non-radionuclide components to the modular cassette synthesis units as part of production of radiopharmaceutical output; measuring the quantity and activity level of each stream of radiopharmaceutical output; purifying the radiopharmaceutical output; dispensing individual doses in sterile vial(s); automatically producing labeling and dose related information; performing automated quality control on extracted samples of produced radiopharmaceutical output; and providing software and hardware controls for overall and sub-portion operation for optional remote data collection, communication, and/or control. | 04-25-2013 |
20150045548 | METHOD FOR PREPARING FLUORINE-18 ELUENT WITH ADJUSTED PH, AND METHOD FOR LABELLING FLUORINE-18 USING SAME - The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [ | 02-12-2015 |
536280300 | The N-hetero ring is a triazine ring, including hydrogenated (e.g., 6-azauridine, etc.) | 16 |
20090005551 | SYNTHESIS OF 5-AZACYTIDINE - The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: | 01-01-2009 |
20100036112 | Process for Making 5-Azacytosine Nucleosides and Their Derivatives - A process of synthesizing a 5-azacytosine nucleoside, such as azacitidine and decitabine, comprises coupling a silylated 5-azacytosine with a protected D-ribofuranose of formula in the presence of a sulfonic acid catalyst. | 02-11-2010 |
20100087637 | Synthesis of Decitabine - A method for producing a β-enriched protected decitabine comprising:
| 04-08-2010 |
20100222565 | METHOD OF PRODUCING 2'-DEOXY-5-AZACYTIDINE (DECITABINE) - Method of producing 2′-deoxy-5-azacytidine (Decitabine) by providing a compound of formula (I): | 09-02-2010 |
20100249394 | PROCESSES FOR PRODUCING DECITABINE - New processes for producing decitabine are provided. | 09-30-2010 |
20110092694 | SYNTHESIS OF 5-AZACYTIDINE - The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: | 04-21-2011 |
20110201800 | AZACITIDINE PROCESS AND POLYMORPHS - Processes for preparing azacitidine. Further included are processes for the preparation of crystalline azacitidine crystalline Form (I) and mixtures of azacitidine crystalline Forms (I) and (II). | 08-18-2011 |
20110245485 | PROCESS FOR THE SYNTHESIS OF AZACITIDINE AND DECITABINE - Described herein is a process for the synthesis of azacitidine or decitabine, comprising the silylation of azacytosine in the presence of N,O-bis-trimethylsilyl-trifluoroacetamide. Such reaction is performed in an organic solvent, preferably aprotic, even more preferably selected from among dichloromethane, dichloroethane and/or acetonitrile. According to a further aspect of the process, 2 to 3 moles of N,O-bis-trimethylsilyl-trifluoroacetamide are used per mole of azacytosine, preferably from 2.2 to 2.5. | 10-06-2011 |
20120046457 | PREPARATION OF DECITABINE - The present application relates to processes for the preparation and purification of decitabine structurally represented by formula (I): | 02-23-2012 |
20120245342 | METHODS FOR ISOLATING CRYSTALLINE FORM I OF 5-AZACYTIDINE - The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: | 09-27-2012 |
20130274459 | METHODS FOR ISOLATING CRYSTALLINE FORM I OF 5-AZACYTIDINE - The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: | 10-17-2013 |
20140094598 | METHOD FOR THE PURIFICATION OF DECITABINE - A method of preparing purified decitabine comprises mixing crude decitabine with solvent, such as dimethylacetamide, to form a solution or suspension and forming the purified decitabine from the solution or suspension. The forming step comprises adding an anti-solvent, such as ethanol, to the solution or suspension. The forming step may further comprise after adding ethanol to provide a mixture of dimethylacetamide and ethanol: cooling the mixture; isolating the solid decitabine present in the cooled mixture; and evaporating residual dimethylacetamide and ethanol from the solid decitabine to provide the purified decitabine. The mixture of dimethylacetamide and ethanol may be heated. The purification method preferably results in decitabine having a ratio of the β-anomer of decitabine to the α-anomer of decitabine of at least about 99.9:0.1. | 04-03-2014 |
20140128593 | SYNTHESIS OF 5-AZACYTIDINE - Provided herein are processes for the preparation of 5-azacytidine, useful for treating, preventing, and/or managing diseases or conditions including cancer, disorders related to abnormal cell proliferation, hematologic disorders, and myelodysplastic syndromes (MDS), wherein 5-azacytidine is represented by the structure: | 05-08-2014 |
20140135490 | SYNTHESIS OF NUCLEOSIDES - A process for the preparation of nucleosides, derivatives and analogues thereof by coupling reaction of a protected suitable nitrogeneous purine or pyrimidine base, a derivative or analogue thereof and a protected suitable sugar in the presence of SnCl | 05-15-2014 |
20140155588 | AZACITIDINE PROCESS AND POLYMORPHS - Processes for preparing azacitidine. Further included are processes for the preparation of crystalline azacitidine crystalline Form I and mixtures of azacitidine crystalline Forms I and II. | 06-05-2014 |
20160168182 | METHOD FOR THE PURIFICATION OF DECITABINE | 06-16-2016 |
536280400 | The N-hetero ring is a 1,3-diazine ring, including hydrogenated (e.g., pyrimidines, etc.) | 56 |
20090124797 | NOVEL SYNTHESIS OF BETA-NUCLEOSIDES - This invention relates to a process of stereoselectively synthesizing β-nucleoside, e.g., 2′-deoxy-2,2′-difluorocytidine. | 05-14-2009 |
20110082289 | Nucleic Acid Labeling Compounds - Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection. | 04-07-2011 |
20130324709 | PROCESS FOR THE PREPARATION OF 2-DEOXY-2-FLUORO-2-METHYL-D-RIBOFURANOSYL NUCLEOSIDE COMPOUNDS - An improved process for the preparation of ( | 12-05-2013 |
536280500 | Nitrogen, other than nitro or nitroso, bonded directly to the 4-position, and chalcogen bonded directly to the 2-position of the diazine ring (e.g., cytidines, etc.) | 32 |
20080262215 | GEMCITABINE PRODUCTION PROCESS - Provided is a process for preparing gemcitabine or a salt thereof, which preferably includes selectively precipitating the β-anomer of a 3′,5′-di-O-protected-N | 10-23-2008 |
20090221811 | PROCESS FOR PREPARING GEMCITABINE AND ASSOCIATED INTERMEDIATES - The present invention provides processes for preparing intermediates useful in the preparation of gemcitabine and other nucleosides, and processes for preparing gemcitabine therewith. Exemplary intermediates include mixtures of D-erythro and D-threo isomers of 3-(hydroxy)-2,2-difluoro-3-(2,2-dimethyldioxolan-4-yl)-propionic acid salts. Also provided is a process for selectively isolating the D-erythro and D-threo isomers of D-erythro and D-threo isomers of 3-(hydroxy)-2,2-difluoro-3-(2,2-dimethyldioxolan-4-yl)-propionic acid salts, and processes for using such isomers in the preparation of nucleoside analogs such as, e.g., gemcitabine, intermediates thereof, and analogs thereof. | 09-03-2009 |
20090281300 | HIGH-MOLECULAR WEIGHT DERIVATIVE OF NUCLEIC ACID ANTIMETABOLITE - [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose. | 11-12-2009 |
20090326214 | Crystalline Polymorphs of Gemcitabine Base - The present application provides several crystalline forms of gemcitabine base and methods of making the same. | 12-31-2009 |
20100056770 | PREPARATION OF NUCLEOSIDES RIBOFURANOSYL PYRIMIDINES - The present process provides an improved method for the preparation of 4-amino-1-((2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-hydrox-ymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one of the formula (IV) which is a potent inhibitor of Hepatitis C Virus (HCV) NS5B polymerase. | 03-04-2010 |
20100069625 | PROCESS FOR PREPARING OF 2'-DEOXY-2'2'-DIFLUOROCYTIDINE - Disclosed is a method for preparing 2′-deoxy-2′,2′-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compound of Formula IX using an optically active chiral amine, preparing an optically pure D-erythro-2,2-difluoro-2-deoxy-1-oxoribose compound of Formula V from the compound of Formula VIII, glycosylating the compound of Formula V with a nucleobase to prepare the 2′-deoxy-2′,2′-difluorocytidine of Formula I as a β-nucleoside. With the present invention, it is possible to prepare an optically pure compound of Formula I in a high purity and a high yield. In the Formulae, R | 03-18-2010 |
20100093992 | Macromolecular Nucleotide Compounds and Methods for Using the Same - The invention relates to the structure, production and use of modified nucleotide and nucleoside building blocks, (nuc-macromolecules). | 04-15-2010 |
20100204463 | Preparation Of Synthetic Nucleosides via Pi-Allyl Transition Metal Complex Formation - This invention provides highly regioselective and stereoselective processes for preparing synthetic nucleosides. A process for the preparation of synthetic nucleosides is provided that comprises a) preparing a bicycloamide derivative, b) reacting the bicycloamide derivative with a nucleic acid base or heterocyclic base or salt thereof in the presence of a transition metal catalyst to form a cyclopentenecarboxamide, and c) cleaving a carboxamide group from the cyclopentenecarboxamide to form the synthetic nucleoside. The processes according to the invention can be used for the synthesis of a variety of anti-viral agents, including Abacavir, Carbovir, and Entecavir, as well as derivatives thereof. | 08-12-2010 |
20100234585 | PREPARATION OF ALKYL-SUBSTITUTED 2-DEOXY-2-FLUORO-D-RIBOFURANOSYL PYRIMIDINES AND PURINES AND THEIR DERIVATIVES - The present invention provides (i) a process for preparing a 2-deoxy-2-fluoro-2-methyl-D-ribonolactone derivative, (ii) conversion of the lactone to nucleosides with potent anti-HCV activity, and their analogues, and (iii) a method to prepare the anti-HCV nucleosides containing the 2-deoxy-2-fluoro-2-C-methyl-β-D-ribofuranosyl nucleosides from a preformed, preferably naturally-occurring, nucleoside. | 09-16-2010 |
20110092695 | CELL CULTURE MODEL FOR ACQUIRED CHEMORESISTANCE OF CHRONIC MYELOGENOUS LEUKEMIA AND RELATED METHODS FOR IDENTIFYING AGENTS TO OVERCOME RESISTANCE - A method of generating a chronic myelogenic leukemia (CML) acquired chemoresistant culture model is provided. Such a method may comprise providing a naïve blast crisis CML cell line; administering/contacting the cell line with a mutation-inducing dose of imatinib; maintaining a culture of the treated cell line for a period of time until the treated cell line relapses and repopulates the culture; and determining the repopulated cell culture is a CML acquired chemoresistant cell line by detecting a BCR-ABL mutation, wherein the acquired chemoresistance is achieved by a BCR-ABL mutation. | 04-21-2011 |
20110282046 | PROCESS FOR PREPARATION OF CIS-NUCLEOSIDE DERIVATIVE - The present invention relates to a novel and stereoselective synthetic process for the preparation of optically active cis-nucleoside derivatives of compound of Formula (I), wherein R | 11-17-2011 |
20120029182 | NOVEL STABLE CRYSTAL OF 1-(2'-CYANO-2'-DEOXY-BETA-D-ARABINOFURANOSYL)CYTOSINE MONOHYDROCHLORIDE - Disclosed is a stable crystal of 1-(2′-cyano-2′-deoxy-β-D-arabinofuranosyl)cytosine monohydrochloride. There is provided a crystal of 1-(2′-cyano-2′-deoxy-β-D-arabinofuranosyl)cytosine monohydrochloride having characteristic peaks at 13.7°, 15.7°, 16.0°, 18.6°, 20.3°, and 22.7° as diffraction angles (2θ±0.1°) measured by powder X-ray diffraction, and having a melting point of 192° C. to 197° C. | 02-02-2012 |
20120065387 | SYNTHESIS 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 acids and deoxyribonucleic acids, as well as methods for their synthesis, crystallization and uses in structural determinations, particularly by X-ray crystallographic techniques are disclosed. The selenium derivatives of the present invention are also useful as food supplements. | 03-15-2012 |
20120088908 | Prodrugs Based on Gemcitabine Structure and Synthetic Methods and Applications Thereof - Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N | 04-12-2012 |
20120178919 | RADIOLABELED NUCLEOSIDE ANALOGUE, AND PREPARATION METHOD AND USE THEREOF - A radiolabeled nucleoside analogue is provided, which includes radioactive iodine | 07-12-2012 |
20120259106 | ASYNTHESIS OF B-NUCLEOSIDES - A process of stereoselectively synthesizing β-nucleoside, e.g., 2′-deoxy-2,2′-difluorocytidine, is described. The process includes reacting a tetrahydrofuran compound of the following formula: | 10-11-2012 |
20130217871 | CONJUGATES COMPRISING HYDROXYALKYL STARCH AND A CYTOTOXIC AGENT AND PROCESS FOR THEIR PREPARATION - The present invention relates to hydroxyalkyl starch conjugates and a method for preparing the same, the hydroxyalkyl starch conjugate comprising a hydroxyalkyl starch derivative and a cytotoxic agent, the cytotoxic agent comprising at least one primary hydroxyl group, wherein the hydroxyalkyl starch is linked via said primary hydroxyl group to the cytotoxic agent. The conjugates according to the present invention have a structure according to the following formula HAS′(-L-M) | 08-22-2013 |
20130303747 | PYRIMIDINE NUCLEOSIDE DERIVATIVES, SYNTHESIS METHODS AND USES THEREOF FOR PREPARING ANTI-TUMOR AND ANTI-VIRUS MEDICAMENTS - The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, and preparation methods and uses thereof. The structural formula is as shown (I). These compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value. | 11-14-2013 |
20140221639 | RADIOLABELED NUCLEOSIDE ANALOGUE, AND PREPARATION METHOD AND USE THEREOF - A radiolabeled nucleoside analogue is provided, which includes radioactive iodine | 08-07-2014 |
20150031872 | METHOD FOR SCREENING ANTICANCER DRUGS, AND ANTICANCER DRUG THAT INDUCES CELL DEATH AND USES SUBSTANCE THAT INCREASES GRANZYME M ACTIVITY AS ACTIVE INGREDIENT - The purpose of the present invention is to provide a method for screening anticancer drugs that use novel treatment mechanisms, and an anticancer drug that induces cell death and uses a substance that increases the activity of granzyme M as an active ingredient. This method for screening anticancer drugs comprises: a step for administering test substances to cancer cells; a step for detecting the activity of granzyme M in which cancer cells are expressed, and selecting test substances for which an increase in activity has been verified; and/or a step for detecting the presence or absence of cancer cell death induced by the activation of granzyme M in which cancer cells are expressed, and selecting test substances for which cell death has been verified. | 01-29-2015 |
20160115190 | METHODS OF PREPARING SUBSTITUTED NUCLEOSIDE ANALOGS - Disclosed herein are methods of preparing a nucleoside analog, which are useful in treating diseases and/or conditions such as viral infections, and intermediates thereof. | 04-28-2016 |
536280510 | Having chalcogen, carbonyl, or thiocarbonyl bonded directly to the 4-position substituent nitrogen | 9 |
20080300399 | PROCESSES RELATED TO MAKING CAPECITABINE - An intermediate (2) useful in making capecitabine can be formed without the use, or presence, of a silylation agent. | 12-04-2008 |
20090069557 | PREPARATION OF GEMCITABINE - A process for preparation of gemcitabine hydrochloride and purification thereof. | 03-12-2009 |
20090209754 | Process for the preparation of capecitabine - The present application relates to an improved process for the preparation of capecitabine. | 08-20-2009 |
20100130734 | PROCESS FOR PREPARING CAPECITABINE - There is provided processes for the preparation of capecitabine and intermediates thereof. | 05-27-2010 |
20100240883 | Lipid-drug conjugates for drug delivery - New prodrugs are derived from highly water soluble parent drugs that exist as primary or secondary amines in their parent form. Lipophilic carrier groups are bonded to the parent drug via an amide linkage with additional linker elements between the amide group and the carrier group. | 09-23-2010 |
20100249395 | METHODS FOR PREPARING CAPECITABINE AND BETA-ANOMER-RICH TRIALKYL CARBONATE COMPOUND USED THEREIN - The present invention relates to a method for preparing capecitabine and a method for preparing a β-anomer-rich trialkyl carbonate compound used therein, and a highly pure capecitabine can be efficiently prepared with a high yield by the method of the present invention using the β-anomer-rich trialkyl carbonate compound as an intermediate. | 09-30-2010 |
20110021769 | Process for Producing Fluorocytidine Derivatives - A process for making a capecitabine or its derivative comprising (a) reacting a compound of the formula (II): | 01-27-2011 |
20110224422 | PREPARATION OF CAPECITABINE - The present invention relates to substantially pure capecitabine and processes for the preparation thereof. | 09-15-2011 |
20130184451 | NOVEL SYNTHESIS OF 5-DEOXY-5'-FLUOROCYTIDINE COMPOUNDS - This invention relates to a process of synthesizing a β-nucleoside compound of formula (I): | 07-18-2013 |
536280520 | Halogen or alkyl group of 1-5 carbon atoms bonded directly to the 5-position of the diazine ring | 2 |
20110054165 | XANTHENE DYES - The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates. | 03-03-2011 |
20150376143 | Prodrugs of NH-Acidic Compounds - The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment. | 12-31-2015 |
536280530 | Chalcogen bonded directly to the 2- and 4-positions of the diazine ring (e.g., uridine, etc.) | 21 |
20090281301 | Manufacturing Process of 2' ,2' - Difluoronucleoside and Intermediate - The present invention relates to more improved process for preparing 2′-deoxy-2′,2′-difluoronucleoside and its intermediate. The present invention provide a process for preparing an erythro enantiomer in greater than 98% purity, comprising forming a lactone ring by hydrolyzing ethyl (3RS)-2,2-difluoro-3-hydroxy-3-(2,2-dimethyloxolan-4-yl)propionate is hydrolyzed in the presence of hydrolysis reagents selected from acetic acid or chloroacetic acid, water and a mixture of organic solvents selected from the group comprising acetonilrile, dioxane, tetrahydrofuran or toluene, introducing a substituted benzoyl protecting group at the 3-position and 5-position, and recrys- tallizing said erythro enantiomer. Further, the present invention provides a process for selectively preparing, in greater than 99% purity, a beta-anomer 2′-deoxy-2′,2′-difluoronucleoside at the 3′-position and 5′-position that are protected by a substituted benzoyl in a 2:3 alpha/beta anomeric ratio. | 11-12-2009 |
20100056771 | Process of Making 2-Deoxy-2,2-Difluoro-D-Ribofuranosyl Nucleosides and Intermediates Therefor - A compound of formula (A) or salt thereof: | 03-04-2010 |
20100105888 | SEPARATION PROCESS - The present invention relates to a process for separating a target radiolabelled compound from an impurity, apparatus for performing such a process and a removable cassette for use in such apparatus. Also provided are methods for using the target radiolabelled compound obtained by a method comprising the separating process of the invention. | 04-29-2010 |
20100113762 | Apparatus and Method Using Rotary Flow Distribution Mechanisms - Methods and apparatus for facilitating the synthesis of compounds in a batch device are presented. Application of the batch type microfluidic devices to the synthesis of radiolabeled compounds is described. These methods and apparatus enable the selective introduction of multiple reagents via an enhanced rotary flow distribution valve through a single inlet port of the synthetic device. The sequential introduction of multiple reagents through a single inlet port allows an optimal delivery of highly concentrated reagents into the reactor and facilitates the synthesis of the desired products with a minimal loss of materials during transfers, which is critical to the synthesis of radiolabeled biomarkers. | 05-06-2010 |
20100130735 | ANTIVIRAL NUCLEOSIDES - 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process. | 05-27-2010 |
20110105743 | IMPROVED METHOD AND PROCESS FOR SYNTHESIS OF 2',3'-DIDEHYDRO-2',3'-DIDEOXYNUCLEOSIDES - A method is disclosed for synthesizing 2′,3′-didehydro-2′,3′-dideoxynucleosides (d4Ns) from a nucleophile-mediated elimination, such as a telluride-mediated elimination reaction. After substitution of 2,2′-anhydronucleosides with a nucleophile, such as a telluride monoanion, a telluride intermediate is formed, and its elimination leads to formation of the olefin products (d4Ns). This disclosure describes this telluride-assisted (or nucleophile-assisted) reaction and how to facilitate the substitution and elimination in order to form d4Ns. | 05-05-2011 |
20130281687 | METHODS OF PREPARING SUBSTITUTED NUCLEOTIDE ANALOGS - Disclosed herein are methods of preparing a phosphorothioate nucleotide analog, which are useful in treating diseases and/or conditions such as viral infections. | 10-24-2013 |
20130289266 | Spiroannulated Nucleosides and Process for the Preparation Thereof - We claim a simple strategy for the synthesis of a collection of C(3′)-spirodihydroisobenzo- furannulated and C(3′)-spirodihydroisobenzo-furannulated nucleosides featuring a [2+2+2]-cyclotrimerization as the key reaction. The cyclotrimerization reactions are facile with the unprotected nucleosides having a diyne unit. When both alkynes of the diyne are terminal, the regioselectivity is poor. However, when one of the terminal alkynes is additionally substituted, the cyclotrimerizations are highly diaste reoselective. Since the key bicycloannulation is the final step, this strategy provides flexibility in terms of the alkynes and is thus amenable for the synthesis of a focussed small molecule library. | 10-31-2013 |
20140066613 | URIDINE DIPHOSPHATE DERIVATIVES, COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISORDERS - This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P | 03-06-2014 |
20140275511 | PURIFICATION OF NIKKOMYCIN Z - This invention relates to an improved method of purifying Nikkomycin Z, an antifungal compound shown to be particularly useful in treating Valley Fever, coccidioidomycosis. The improvement of this invention lies in the choice of resins and elution conditions, chosen to minimize handling of the material. | 09-18-2014 |
536280540 | Alkyl, or substituted alkyl, bonded directly to the 5-position of the diazine ring (e.g., thymidine, 5-methyl uridine, etc.) | 9 |
20090018325 | PROCESS 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, synthesis of various L-nucleic acid derivatives, synthesis of which has been difficult till now, is possible. | 01-15-2009 |
20100113763 | METHOD 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 [ | 05-06-2010 |
20100280235 | METHOD 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 introducing a triple bond-containing group into a furfuryl alcohol derivative or a levoglucosenone, by reacting the furfuryl alcohol derivative or levoglucosenone with a certain compound, and a step for reacting a compound represented by the formula (III), which is obtained by the aforementioned step, with thymine. | 11-04-2010 |
20120004404 | RADIOLABELLING METHODS - The present invention relates to the field of [ | 01-05-2012 |
20120322996 | Novel Method for the Preparation of Stavudine Polymorphic Form I and Form II - A novel method for the preparation of stavudine polymorphic form I and form II is described. 5′-acetate-2′,3′-diacetyl-5-methyluridine is reacted with catalytic amounts of sodium methoxide in a C | 12-20-2012 |
20130211067 | NOVEL SELENY-METHYLURACIL COMPOUNDS, RADIOSENSITIZER AND PHARMACEUTICAL COMPOSITION USING THEM - Provided are novel selenyl-methyluracil compounds and a pharmaceutical composition for enhancing the effect of radiation treatment. The composition contains at least one compound selected from the group consisting of the selenyl-methyluracil compounds or pharmaceutically acceptable salts thereof, as an active ingredient. | 08-15-2013 |
20150112055 | TRICYCLIC NUCLEIC ACID ANALOGS - The present disclosure provides tricyclic nucleosides and oligomeric compounds prepared therefrom. The tricyclic nucleosides each have a tricyclic ribosyl sugar moiety wherein a bridge between the 2′ and 4′ ribosyl ring carbon atoms further comprises a fused carbocyclic or heterocyclic ring. The tricyclic nucleosides are expected to be useful for enhancing properties of oligomeric compounds including for example binding affinity and nuclease resistance. | 04-23-2015 |
20160107951 | DIGITAL MICROFLUIDIC PLATFORM FOR RADIOCHEMISTRY - Disclosed herein are methods of performing microchemical reactions and electro-wetting-on-dielectric devices (EWOD devices) for use in performing those reactions. These devices and method are particularly suited for preparing radiochemical compounds, particularly compounds containing | 04-21-2016 |
20160185811 | Spiroannulated nucleosides and process for the preparation thereof - We claim a simple strategy for the synthesis of a collection of C(3′)-spirodihydroisobenzo-furannulated and C(3′)-spirodihydroisobenzo-furannulated nucleosides featuring a [2+2+2]-cyclotrimerization as the key reaction. The cyclotrimerization reactions are facile with the unprotected nucleosides having a diyne unit. When both alkynes of the diyne are terminal, the regioselectivity is poor. However, when one of the terminal alkynes is additionally substituted, the cyclotrimerizations are highly diastereoselective. Since the key bicycloannulation is the final step, this strategy provides flexibility in terms of the alkynes and is thus amenable for the synthesis of a focussed small molecule library. | 06-30-2016 |
536280550 | Halogen bonded directly to the 5-position of the diazine ring (e.g., 5-fluorouridine, etc.) | 2 |
20140066614 | PROBE OF IODINE-123 MARKER THYMIDINE (FLT)ANALOGUE [123I]-IARAU - A tumor radiation probe of iodine-123 marker thymidine (FLT) analogue [ | 03-06-2014 |
20150291649 | 5-Fluorouracil Derivatives - The present invention relates to 5-fluorouracil derivatives represented by formula (i), pharmaceutical compositions comprising said derivative and their use in the treatment of cancer as well as a process for preparing the 5-fluorouracil derivative represented by formula (I). | 10-15-2015 |