| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 536270100 | N-glycosides wherein the N is part of an N-hetero ring which hetero ring is part of a polycyclo ring system containing an N-hetero ring and an additional hetero ring (e.g., rebeccamycin, etc.) | 65 |
| 20090137791 | METHODS OF ATTACHING BIOLOGICAL COMPOUNDS TO SOLID SUPPORTS USING TRIAZINE - Disclosed are methods of attaching biologically active compounds to a solid surface, comprising modifying the solid surface using triazine chloride and attaching the biologically active compound to the triazine moiety. | 05-28-2009 |
| 20100137577 | ADENOSINE DERIVATIVES, METHOD FOR THE SYNTHESIS THEREOF, AND THE PHARMACEUTICAL COMPOSITIONS FOR THE PREVENTION AND TREATMENT OF THE INFLAMMATORY DISEASES CONTAINING THE SAME AS AN ACTIVE INGREDIENT - Disclosed are adenosine derivatives, methods for the synthesis thereof, and pharmaceutical compositions for the prevention and treatment of inflammatory diseases, comprising the same as an active ingredient. The adenosine derivatives have high binding affinity and selectivity for adenosine receptors, especially for A3 adenosine receptors and act as A3 adenosine receptor antagonists, and exhibit anti-inflammatory activity. Thus, the adenosine derivatives are useful in the prevention and treatment of inflammatory diseases. | 06-03-2010 |
| 20100292458 | NOVEL 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 protective groups that are attached to either the 5′- or the 3′-hydroxyl group of a nucleoside moiety. The photolabile protective group is comprised of a 2-(2-nitrophenyl)-ethyoxycarbonyl skeleton with at least one substituent on the aromatic ring that is either an aryl, an aroyl, a heteroaryl or an alkoxycarbonyl group. The present invention includes the use of the aforementioned compounds in light-directed oligonucleotide synthesis, the respective assembly of nucleic acid microarrays and their application. | 11-18-2010 |
| 20120157671 | PROCESS FOR THE PREPARATION OF (1S,4R)-2-OXA-3-AZABICYCLO[2,2.1]HEPT-5-ENES - Enantiomerically enriched (1S,4R)-2-oxa-3-azabicyclo[2.2.1]hept-5-ene of formula wherein PG1 is an amino-protective group, are prepared from cyclopentadiene via hetero-Diels-Alder cycloaddition with protected 1-C-nitroso-β-D-ribofuranosyl halides of formula wherein X is a halogen atom selected from fluorine, chlorine, bromine and iodine, PG2 is a hydroxyl-protective group and PG3 is a 1,2-diol-protective group. | 06-21-2012 |
| 20140011989 | PAA NANOPARTICLES FOR TUMOR TREATMENT AND IMAGING - A tetrapyrrolic photosensitizer and imaging compound having a substituent other than hydrogen at its 10 carbon atom which substituent may contain a PAA nanoparticle. | 01-09-2014 |
| 536270110 | Preparing by cleaving nucleic acids or by attaching an N-heterocyclic base to a sugar ring | 9 |
| 20080207891 | Methods For Selective N-9 Glycosylation of Purines - A process for providing regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs is described. The introduction of the sugar moiety on to 6-(azolyl)-substituted purine bases is performed so that highly stereoselective formation of the β anomers of only the 9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs, and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-halo-arabino and 2′,3′-dideoxy-2′-halo-threo purine nucleoside analogs, in high yields without formation of the 7-positional regioisomers. Processes for providing novel 6-(azolyl)purines for the regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs are described. The compounds are drugs or intermediates to drugs. | 08-28-2008 |
| 20080300398 | 2'-FLUORONUCLEOSIDES - A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: | 12-04-2008 |
| 20100093991 | METHODS FOR THE PREPARATION OF 9-DEAZAPURINE DERIVATIVES - Methods for the preparation of the β isomer of a 9-deazapurine derivatives using benzyl protecting groups as the protecting groups for the 2 and 3 hydroxyl groups in ribose are provided. | 04-15-2010 |
| 20100210833 | METHOD OF PRODUCING NUCLEOSIDES - Method of producing a free nucleoside compound, the compound 2′-deoxy-5-azacytidine (Decitabine) being excluded, by reacting a glycoside donor preferably a 1-halogen derivative, or 1-O-acyl, 1-O-alkyl, or an imidate preferably a trichloromethyl derivative, or a thio-alkyl derivative of a blocked monosaccharide or oligosaccharide preferably ribose and 2-desoxyribose derivatives with a protected nucleoside base, in a suitable anhydrous solvent and in the presence of a catalyst, and removing the protecting groups from said blocked nucleoside compound, wherein said catalyst is selected from the group comprising salts of an aliphatic sulphonic acid and/or salts a strong inorganic acid containing a non-nucleophilic anion. | 08-19-2010 |
| 20100234584 | 2'-Fluorine-4'-Substituted-Nucleoside Analogues, Preparation Methods and Uses Thereof - The present invention provides 2′-fluorine-4′-substituted-nucleoside analogues or their pro-drugs or 5′-phosphate esters (including the pro-drugs of the 5′-phosphate esters), preparation methods and uses thereof. The compounds have the general formula as follows: | 09-16-2010 |
| 20110046363 | Process for the Preparation of Cladribine - A process for the preparation of cladribine of API grade is provided by direct coupling of O-protected 2-deoxy-ribofuranose with silylated 2-chloroadenine followed by deprotection of the resultant protected nucleoside in a separate step and then a purification step. Following the coupling, the desired N-9-glycosylated β-anomer of the nucleoside is directly isolated as a solid from the coupling reaction mixture by filtration in relatively high purity and yield, and it does not require purification. | 02-24-2011 |
| 20110257387 | PROCESS FOR PREPARING AN A2A-ADENOSINE RECEPTOR AGONIST AND ITS POLYMORPHS - Disclosed is a synthesis suitable for large scale manufacture of an A | 10-20-2011 |
| 20150376219 | Selective Preparations of Purine Nucleosides and Nucleotides: Reagents and Methods - A process of regiospecific synthesis of N-9 purine nucleoside analogs in either solution or solid phase synthesis is described. The introduction of the sugar moiety or its analogue on to a 6-heteroarylium purine or its mesomeric betaine so that formation of only the N-9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific introduction of the sugar moiety allows the synthesis of purine nucleoside analogs in high yields without formation of the N-7-positional regioisomers, while the 6-heteroaryliums are leaving groups facilitated for nucleophilic displacement. Solid supported 6-heterarylium purine bases can be used for purine based library synthesis and synthesis of nucleotide monophosphates and polyphosphates. Processes for providing novel 6-heteroarylium purines and their corresponding mesomeric betaines for the regiospecific synthesis of N-9 purine nucleoside analogs and nucleotides are described. | 12-31-2015 |
| 20160068561 | Intermediate for Production of Nucleoside Analog and Method for Producing the Same - A compound represented by the general formula (III) which serves as an intermediate of an oligonucleotide analog having stable and excellent antisense or antigene activity or having excellent activity as a detection reagent (probe) for a specific gene or as a primer for the initiation of amplification of a specific gene can be produced at high yields regardless of the type of nucleobase by a method comprising reacting a compound represented by the general formula (II) or a salt thereof with a trimethylsilylated compound obtained from a compound represented by the general formula (IVb), wherein X, Y, Z, A, R, and B are as defined in claim | 03-10-2016 |
| 536270120 | Separation or purification (e.g., resolving isomeric mixtures, etc.) | 4 |
| 20090209753 | COLUMN PACKING MATERIAL, COLUMN USING THE SAME, AND METHOD OF SEPARATION USING THE SAME - Aimed at readily and exactly separate 8-hydroxy-2′-deoxyguanosine (8-OHdG) contained in a sample, a column packing material used for separating 8-OHdG, which contains a packing material composed of a material having a straight-chain hydrocarbon group having 6 or more and 30 or less carbon atoms as a functional group, and having a carbon content over the surface of carrier of 18% or less by element ratio, wherein the packing material contains 1 cumulative percent or more and 20 cumulative percent or less, on the particle-count basis, of particles having a circle-equivalent diameter, measured using a flow-type particle image analyzer, of 0.5 μm or larger and 10 μm or smaller, is used. | 08-20-2009 |
| 20120197010 | PROCESS OF MAKING CLADRIBINE - A method of making cladribine with an increased purity comprising:
| 08-02-2012 |
| 20130331561 | Method of Preparation of Antiviral Compounds and Useful Intermediates Thereof - The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The anti-viral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection. | 12-12-2013 |
| 20140323712 | POLYMORPH OF 2-[4-[(METHYLAMINO)CARBONYL]-1H-PYRAZOL-1-YL]ADENOSINE - A new polymorph of 2-[4-[(methylamino)carbonyl]-1H-pyrazol-1-yl]adenosine (designated as polymorph E), characterized by an X-ray diffraction pattern of X-RPD showing the following reflections at 2 Theta=5.8°, 12.3°, 15.9°, 17.3°, 20.5°, 22.6°, 23.6°, 27.7°, and 29.2°, and further characterized by DSC showing marked endotherm in the range of 258 to 264° C., and further characterized by IR spectra, which is prepared by a procedure comprising the following operations:
| 10-30-2014 |
| 536270130 | Bicyclic ring system consisting of the N-hetero ring fused to another hetero ring (e.g., 2-azaadenines, 6-azaadenines, etc.) | 47 |
| 20100311961 | PROCESS AND INTERMEDIATES FOR THE PREPARATION OF SUBSTITUTED 1,3-OXATHIOLANES, ESPECIALLY LAMIVUDINE - The present invention relates to process and intermediates for the preparation of substituted 1,3-oxathiolanes. The present invention specifically relates to a process for the preparation of lamivudine. | 12-09-2010 |
| 20110009609 | 2'-HYDROXY-PROTECTED RIBONUCLEOSIDE DERIVATIVE AND PRODUCTION METHOD THEREOF - The present invention relates to a method for producing a 2′-hydroxy-protected nucleoside derivative by reacting a ribonucleoside with an acylating reagent in the presence of a metal complex consisting of a copper compound and an optically active ligand. By the method according to the present invention, a 2′-hydroxy-protected ribonucleoside derivative, which is an important intermediate for producing an oligonucleoside, can be easily produced with good regioselectivity from a nucleoside derivative of which 2′,3′-hydroxy groups are not protected. | 01-13-2011 |
| 20130261294 | Novel Crystalline Forms Of An Antiviral Benzimidazole Compound - The invention relates to crystalline forms of 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1H benzimidazole, pharmaceutical compositions comprising the same, processes for preparing the same, and their use in medical therapy. | 10-03-2013 |
| 20160108078 | GLUCOPYRANOSIDE COMPOUND - A compound of the formula: | 04-21-2016 |
| 536270140 | Multideoxy or didehydro | 3 |
| 20090306360 | 2-AZAPURINE COMPOUNDS AND THEIR USE - Within oligonucleotides, 2-azapurine and especially 2-azaadenine bases form specifically base pairs with guanine. This base pair is of analogous stability as an adenine-thymine but less stable than a guanine-cytosine base pair. Therefore, the incorporation of 2-azaadenine residues into oligonucleotides instead of cytosine leads specifically to hybridization complexes with nucleic acids with homogenous stability. This is useful for the adaptation of the stabilities of different oligonucleotide sequences in all kinds of hybridization techniques, for example in oligomer chip technology. | 12-10-2009 |
| 20110028706 | INOSINE DERIVATIVES AND PRODUCTION METHODS THEREFOR - The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. | 02-03-2011 |
| 20160122381 | METHOD OF PREPARATION OF ANTIVIRAL COMPOUNDS AND USEFUL INTERMEDIATES THEREOF - The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The antiviral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection. | 05-05-2016 |
| 536270200 | The bicyclic ring system consists of a 1,3-diazine ring, which may be hydrogenated, fused to a five-membered N-hetero ring (e.g., purine isoesters like tubercidin, toyocamycin, sangivamycin, sparsomycin A, etc.) | 40 |
| 20110040083 | PHOTORESPONSIVE 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 method of manufacturing a photoresponsive nucleic acid which includes a step of reacting a nucleic acid having groups represented by the Formula I, the Formula III, the Formula IV, or the Formula V and a compound represented by the Formula II, or reacting a nucleic acid having groups represented by the Formula VI, the Formula VIII, the Formula IX, or the Formula X and a compound represented by the Formula VII by heating them by microwaves in the presence of a metal catalyst, a basic substance, and a solvent. | 02-17-2011 |
| 20120190838 | Labelling Strategies for the Sensitive Detection of Analytes - The present invention relates to methods and reagents for detecting analytes, e.g. nucleic acids. The new methods and reagents allow a simple and sensitive detection even in complex biological samples. | 07-26-2012 |
| 536270210 | The five-membered N-hetero ring is 1,3-diazole, which may be hydrogenated (e.g., 6-chloropurine nucleoside, nebularin, etc.) | 38 |
| 20100179312 | CONVERTIBLE NUCLEOSIDE DERIVATIVES - The present invention is directed to convertible nucleosides and polymer supported convertible nucleosides for use in SNAP displacement reactions. The convertible nucleosides can be used to synthesize numerous substituted purine and pyrimidine derivatives. | 07-15-2010 |
| 20100190972 | Heteropolynucleotide Duplexes With Purine-Purine Base Pairing - The present invention relates to stable anti-parallel heteropolynucleotide duplexes, comprising a plurality of complementary purine-purine nucleobase dyads, wherein the nucleobase is coupled to a pentose sugar backbone. The present invention further relates to methods of hybridizing two heteropolynucleotide molecules to form such purine-purine nucleobase dyads, as well as kits and solid supports comprising such purine-purine nucleobase dyads. | 07-29-2010 |
| 536270220 | Carbonyl, thiocarbonyl, or nitrogen, other than as nitro or nitroso, bonded directly to the sugar ring | 1 |
| 20100152434 | Protein Kinase-binding Nucleosides and Associated Methods - Therapeutically active nucleosides and associated methods are provided. In one aspect, a nucleoside molecule having a general structural similar to ATP. Such nucleosides have a structure that allows binding to, and subsequent regulation of, protein kinase molecules. As such, the nucleosides of the present invention have may be capable of treating a variety of kinase-related medical disorders. | 06-17-2010 |
| 536270230 | Carbonyl, thiocarbonyl, additional hetero ring or nitrogen, other than as nitro or nitroso, attached indirectly to the sugar ring by acyclic nonionic bonding | 5 |
| 20090069556 | METABOLICALLY STABLE PUROMYCIN ANALOGS - Disclosed are structurally modified, metabolically stable nucleosides having antitumor activity wherein the formation of toxic metabolites is blocked and antimicrobial activity. The disclosure further relates to pharmaceutical compositions comprising one or more disclosed modified nucleosides and to methods of use thereof. | 03-12-2009 |
| 20110144320 | N-PYRAZOLE A2A RECEPTOR AGONISTS - 2-adenosine N-pyrazole compounds having the following formula: | 06-16-2011 |
| 536270300 | Adenosyl | 3 |
| 20090105468 | Synthesis of Protected 3'-Amino Nucleoside Monomers - Orthogonally protected 3′-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3′-amino group in the presence of the unprotected nucleoside base. | 04-23-2009 |
| 20110282045 | PROCESS FOR PREPARING PURINE NUCLEOSIDES - The present invention for the stereoselective preparation of 2-deoxy-β-D-adenine nucleosides wherein a blocked 2-deoxy-α-D-arabinofuranosyl halide is coupled with the salt of an adenine derivative. | 11-17-2011 |
| 20160060286 | DIARYLSULFIDE BACKBONE CONTAINING PHOTOLABILE PROTECTING GROUPS - The present disclosure relates to photoactivable protecting groups containing a diarylsulfide chromophore, a method for the synthesis thereof and their use as photoactivable protecting groups using maskless photolithography based array synthesis. | 03-03-2016 |
| 536270400 | Arabinose is sugar moiety | 2 |
| 20120220762 | METHOD FOR THE MANUFACTURE OF 2-FLUORO-ARA-ADENINE - A method is described for the manufacture of pure 2-fluoro-ara-adenine of Formula (I) from 2-fluoro-ara-adenine triacetate using potassium carbonate (K | 08-30-2012 |
| 20160024137 | STABLE SOLID FORMS OF REGADENOSON - A process for the preparation of the amorphous form of Regadenoson of formula | 01-28-2016 |
| 536270600 | Nitrogen, other than nitro or nitroso, bonded directly to the 6-position of a purine ring system (e.g., adenosine, etc.) | 24 |
| 20080262214 | Synthesis of 2-Substituted Adenosines -
A method of synthesis of a 2-substituted adenosine of formula I which comprises converting a compound of formula II to a compound of formula (I), wherein: R is C 1-6 alkoxy (straight or branched), a phenoxy group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3-, cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy), a benzoyl group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3-, cyano, nitro, C1_6 alkyl, or C1_6 alkoxy), or a benzoyl group (unsubstituted, or mono-, or di-substituted by halo, amino, CF3-, cyano, nitro, C 1-6 alkyl, or C 1-6 alkoxy); R′═H, or a protecting group. | 10-23-2008 |
| 20090124796 | Nucleobase Having Perfluoroalkyl Group and Process for Producing the Same - Provided is a simple and efficient production process of a nucleobase having a perfluoroalkyl group. | 05-14-2009 |
| 20100087636 | PROCESS FOR THE SYNTHESIS OF IB-MECA - The present disclosure provides a method for the synthesis of IB-MECA. More specifically, the present disclosure provides a simple and high yield method for Good Manufacturing Production (GMP) of IB-MECA. The method involves the reaction of 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine-9-riboside with a diol protecting reagent; oxidation of the primary alcohol in the diol protected 6-halopurine; reaction of the diol protected 6-halopurine with a nucleophile (e.g. methylamine); substitution of the halogen group with iodobenzylamine and removal of the diol protecting group. | 04-08-2010 |
| 20100130733 | LUMINESCENT METAL ION COMPLEXES - The present invention provides luminescent metal ion complexes for use in a wide range of biological and chemical studies. The luminescent metal ion complexes of the invention comprise a metal ion chelating component covalently bound to a carrier molecule. Also provided are methods of making and using the luminescent metal ion complexes. | 05-27-2010 |
| 20130172543 | METHOD FOR OXIDIZING ALCOHOLS - A method for oxidizing an alcohol, wherein oxidation is performed in the presence of a compound represented by the following formula (I) and a bulk oxidant, which enables efficient oxidation of secondary alcohols as well as primary alcohols, and can attain high reaction efficiency even when air is used as a bulk oxidant. | 07-04-2013 |
| 20140194614 | AMINO-LNA, THIO-LNA AND ALPHA-L-OXY-LN - A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides. | 07-10-2014 |
| 20150094462 | METHOD FOR PROTECTING HYDROXYL OR AMINE OR THIOL FUNCTIONS, NOVEL COMPOUNDS WITH PROTECTED HYDROXYL OR AMINE OR THIOL GROUPS, AS WELL NOVEL COMPOUNDS FOR THE IMPLEMENTATION OF THIS METHOD - A novel method of simultaneously protecting two functions which are same or different, namely hydroxyl, amine, or thiol ones, particularly in sugars, polyalcohols, nucleosides, nucleotides, peptides, and nucleic acids during an organic synthesis, and to novel compounds for implementing this method, as well as to the method of obtaining these compounds. Method of simultaneously protecting two hydroxyl, amine, or thiol functions according to the invention by carrying out a protecting reaction between a compound having at least two free hydroxyl, amine, or thiol groups, and the disilane of formula 1, | 04-02-2015 |
| 20150322107 | FLUORESCENT MOLECULAR PROBES FOR USE IN ASSAYS THAT MEASURE TEST COMPOUND COMPETITIVE BINDING WITH SAM-UTILIZING PROTEINS - Assay methods may generally comprise forming homogeneous assay mixtures comprising target SAM-utilizing protein, fluorescent detection analyte, and test compound, incubating, and measuring FP or TR-FRET signal emitted in order to determine a measure of test compound-SAM-utilizing protein binding. Assay mixtures comprise a SAM-utilizing protein, and a fluorescent detection analyte that binds with the SAM-utilizing protein in the absence of test compound. Assay mixtures may further comprise a test compound. Assay mixture embodiments may generate FP or TR-FRET signal properties that are a function of the inherent binding interactions of both the test compound and the detection analyte with the SAM-utilizing protein. Fluorescent detection analytes comprise a fluorophore moiety, a covalent linker moiety, and a SAM-utilizing protein ligand moiety and could be utilized in FP or TR-FRET assays to measure test compound binding. | 11-12-2015 |
| 20150366892 | USE OF HEAT SHOCK PROTEIN INHIBITOR IN PREPARING PHARMACEUTICAL COMPOSITION FOR TREATING HEPATITIS AND HEPATOMA - The present invention is directed to a use of a heat shock protein inhibitor in preparing pharmaceutical composition for treating hepatitis by scavenging hepatitis B virus-infected cells. The heat shock protein inhibitor is selected from a group including VER-155008, Pifithrin-μ, and pharmaceutical acceptable salts thereof. The present invention is also directed to a use of a heat shock protein inhibitor in preparing pharmaceutical composition for treating hepatoma. | 12-24-2015 |
| 536270610 | Additional nitrogen bonded directly to the 2-position of the purine ring system | 8 |
| 20090131651 | Synthesis of 2-substituted adenosines - Synthesis of 2-substituted adenosines of formula (I) using 2-nitro pentabenzoyl adenosine, or 2-nitro pentaacetyl adenosine, as intermediate is described: Formula (I) wherein R=C | 05-21-2009 |
| 20100160620 | N-PYRAZOLE A2A RECEPTOR AGONISTS - 2-adenosine N-pyrazole compounds having the following formula: | 06-24-2010 |
| 20100179313 | PROCESS FOR PREPARING AN A2A-ADENOSINE RECEPTOR AGONIST AND ITS POLYMORPHS - Disclosed is a synthesis suitable for large scale manufacture of an A | 07-15-2010 |
| 20110130559 | Methods to Manufacture 1,3-Dioxolane Nucleosides - This application provides a process for preparing enantiomerically pure β-D-dioxolane nucleosides. In particular, a new synthesis of (−)-DAPD, suitable for large scale development, is described. In one embodiment the invention provides a process for preparing a substantially pure β-D- or β-L-1,3-dioxolane nucleosides comprising a) preparing or obtaining an esterified 2,2-dialkoxy ethanol; b) cyclizing the esterified 2,2-dialkoxy ethanol with glycolic acid to obtain a 1,3-dioxolane lactone; c) resolving the 1,3-dioxolane lactone to obtain a substantially pure D- or L-lactone; d) selectively reducing and activating the D- or L-chiral lactone to obtain a substantially pure D- or L-1,3-dioxolane; e) coupling the D- or L-1,3-dioxolane to an activated and/or protected purine or pyrimidine base; and f) optionally purifying the nucleoside to obtain a substantially pure protected β-D- or β-L-1,3-dioxolane nucleoside. | 06-02-2011 |
| 20140194615 | METHOD FOR THE PREPARATION OF 2-[4-[(METHYLAMINO)CARBONYL]-1-H-PYRAZOL-1-YL]ADENOSINE MONOHYDRATE - A method for the preparation of 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine monohydrate of formula I by reaction of 2-(4-methoxycarbonylpyrazol-1-yl) adenosine of formula III with a solution of methylamine in a non-aqueous solvent, optionally in combination with another inert solvent, to produce anhydrous 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yl]adenosine, which is converted to 2-[4-[(methylamino)carbonyl]-1-H-pyrazol-1-yljadenosine monohydrate of formula I by addition of water. | 07-10-2014 |
| 20140206857 | METHOD FOR THE PREPARATION OF 2-(4-METHOXYCARBONYLPYRAZOL-1-YL)ADENOSINE AND 2-(4-ETHOXYCARBONYLPYRAZOL-1-YL)ADENOSINE - A method for the preparation of 2-(4-methoxycarbonylpyrazol-1-yl)adenosine of formula 1a and 2-(4-ethoxycarbonylpyrazol-1-yl)adenosine of formula 1b by reaction of 2-hydrazinoadenosine of formula III and the sodium salt of 3,3-dimethoxy-2-methoxycarbonylpropen-1-ol of formula Va or the sodium salt of 3,3-diethoxy-2-ethoxycarbonylpropen-1-ol of formula Vb in combination with a solvent and an acidic agent. | 07-24-2014 |
| 20150353593 | Novel Process for the Preparation of (1-pyrazole-4-yl)-N-methylcarboxamide - The present invention relates to a novel process for the preparation of (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl)-6-aminopurin-2-yl}pyrazole-4-yl)-N-methylcarboxamide. | 12-10-2015 |
| 20160115191 | Novel Polymorph of Regadenoson - The invention provides a novel polymorph of Regadenoson. More particularly, the invention provides propylene glycol solvate of Regadenoson. The invention also provides a process for the preparation of propylene glycol solvate of Regadenoson. | 04-28-2016 |
| 536270620 | Nitrogen, chalcogen, or additional carbon bonded directly to the 6-position nitrogen (e.g., 6-position nitrogen is substituted, etc.) | 3 |
| 20090240045 | Organic Compounds - A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals | 09-24-2009 |
| 20120071646 | PROCESS FOR PRODUCING NUCLEOSIDE - There is a demand for a convenient production method of an NC type purine nucleoside. | 03-22-2012 |
| 20150126726 | COMPLEX COMPOUNDS OF GERMANIUM, METHODS FOR PRODUCING SAME, AND DRUGS - The invention relates to the development of drugs intended for the prophylaxis and/or treatment of viral diseases caused, in particular, by herpes viruses. What are proposed are complex compounds of germanium having the general structural formula: | 05-07-2015 |
| 536270700 | Chalcogen, halogen, or benzene bonded directly to carbon of the purine ring system (e.g., isoguanosine, 2-fluoroadenosine, etc.) | 4 |
| 20090270604 | METHOD FOR THE PREPARATION OF 2-HALO-2'-DEOXYADENOSINE COMPOUNDS FROM 2'-DEOXYGUANOSINE - The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2′-deoxyadenosine, CldAdo, 4), a drug of choice against hairy-cell leukemia and other neoplasms, from 2-amino-6-oxopurines, which are readily obtained from the naturally occurring compound 2′-deoxyguanosine. According to the methods of the present invention, the 6-oxo group of a protected 2′-deoxyguanosine (1) is converted to a 6-(substituted oxy) leaving group, or alternatively to a 6-chloro leaving group, the 2-amino group is replaced with a 2-chloro group, the 6-(substituted oxy) leaving group, or alternatively the 6-chloro leaving group, is replaced with a 6-amino group or, alternatively, a 2,6-dichloro substituted compound is selectively replaced with a 6-amino group, and the protecting groups are removed. | 10-29-2009 |
| 20120010397 | Preparation of 2-chloro-9-(2'-deoxy-2'-fluoro-Beta-D-arabinofuranosyl)-adenine - A process for making clofarabine comprising: fluorinating a compound of formula VII | 01-12-2012 |
| 20150329583 | MODULAR RADIOCHEMISTRY SYNTHESIS SYSTEM - A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the position thereof relative to the reaction vessel being controllable from a remote position. Alternatively the heat source may be fixed in location and the reaction vial is moveable into and out of the heat source. The reaction vessel has one or more sealing plugs, the positioning of which in relationship to the reaction vessel is controllable from a remote position. Also the one or more reaction vessel sealing plugs can include one or more conduits there through for delivery of reactants, gases at atmospheric or an elevated pressure, inert gases, drawing a vacuum and removal of reaction end products to and from the reaction vial, the reaction vial with sealing plug in position being operable at elevated pressures. The modular chemical production system is assembled from modules which can each include operating condition sensors and controllers configured for monitoring and controlling the individual modules and the assembled system from a remote position. Other modules include, but are not limited to a Reagent Storage and Delivery Module, a Cartridge Purification Module, a Microwave Reaction Module, an External QC/Analysis/Purification Interface Module, an Aliquotting Module, an F-18 Drying Module, a Concentration Module, a Radiation Counting Module, and a Capillary Reactor Module. | 11-19-2015 |
| 20160130295 | MODULAR RADIOCHEMISTRY SYNTHESIS SYSTEM - A modular chemical production system includes multiple modules for performing a chemical reaction, particularly of radiochemical compounds, from a remote location. One embodiment comprises a reaction vessel including a moveable heat source with the position thereof relative to the reaction vessel being controllable from a remote position. Alternatively the heat source may be fixed in location and the reaction vial is moveable into and out of the heat source. The reaction vessel has one or more sealing plugs, the positioning of which in relationship to the reaction vessel is controllable from a remote position. Also the one or more reaction vessel sealing plugs can include one or more conduits there through for delivery of reactants, gases at atmospheric or an elevated pressure, inert gases, drawing a vacuum and removal of reaction end products to and from the reaction vial, the reaction vial with sealing plug in position being operable at elevated pressures. The modular chemical production system is assembled from modules which can each include operating condition sensors and controllers configured for monitoring and controlling the individual modules and the assembled system from a remote position. Other modules include, but are not limited to a Reagent Storage and Delivery Module, a Cartridge Purification Module, a Microwave Reaction Module, an External QC/Analysis/Purification Interface Module, an Aliquotting Module, an F-18 Drying Module, a Concentration Module, a Radiation Counting Module, and a Capillary Reactor Module. | 05-12-2016 |
| 536270800 | Chalcogen bonded directly to the 6- or 2-position of a purine ring system (e.g., inosine, etc.) | 4 |
| 20100324279 | CRYSTAL FORMS OF 2-[2-(4-CHLOROPHENYL)ETHOXY]ADENOSINE - The present invention provides novel crystal forms of 2-[2-(4-chlorophenyl)ethoxy]adenosine of the formula processes for the production of such crystal forms, and methods for the manufacture of pharmaceutical compositions for the treatment of diseases or conditions modulated by the adenosine A2 receptors, in particular the A2A receptor, in a mammal in need thereof, by employing such crystal forms. The crystal forms of the present invention are especially useful in the preparation of topical compositions for accelerating wound healing, e.g., for the treatment of diabetic foot ulcers. | 12-23-2010 |
| 536270810 | Nitrogen, other than nitro or nitroso, bonded directly to the 2-position of the purine ring system (e.g., guanosine, etc.) | 3 |
| 20090299049 | Bicyclic Compounds and Their Use - The present invention provides fluorescent bicyclic compounds of the formula (I); wherein ring A, the broken lines -----, C | 12-03-2009 |
| 20140031539 | 6-ETHER/THIOETHER-PURINES AS TOPOISOMERASE II CATALYTIC INHIBITORS AND THEIR USE IN THERAPY - The present invention relates to certain purines, which act as topoisomerase II catalytic inhibitors. These compounds are useful in combination with topoisomerase II poisons, such as anthracyclines and epipodophyllotoxins, in the treatment of proliferative conditions (e.g., cancer). These compounds are useful in the treatment of tissue damage associated with extravasation of a topoisomerase II poison, such as an anthracycline or an epipodophyllotoxin. | 01-30-2014 |
| 20150376224 | USE OF COMPOSITIONS OBTAINED BY CALCINING PARTICULAR METAL-ACCUMULATING PLANTS FOR IMPLEMENTING CATALYTICAL REACTIONS - The use of metal-accumulating plants for implementing chemical reactions especially catalytical reactions. | 12-31-2015 |
