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7368437 Bicyclic heterocycles, processes for their preparation and their use as herbicides and pharmaceutical agents  
Methods and compounds for inhibiting the enzymes adenosine monophosphate deaminase or adenoside deaminase are provided. Such methods and compounds are useful in agriculture, horticulture and/or...
7176305 Production method for purine nucleotide derivative disodium crystals and alcohol removing method  
Purine nucleotide derivative disodium crystals having a minimized amount of remaining alcohol such as methanol, ethanol or a mixture thereof are produced by overdrying purine nucleotide derivative...
7153840 Aqueous fludarabine phosphate composition  
This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which...
7148207 Oral fludara of high-purity formulation with quick release of active ingredient  
This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants.
7125982 Microbial production of nuclease resistant DNA, RNA, and oligo mixtures  
The present method describes the use of thio-phosphate as a feed source for micro-organisms and multi-cellular organisms. This compound enters into nucleotide pools and ultimately into polymers of...
7019128 Propargylethoxyamino nucleotides  
Propargylethoxyamino nucleosides are disclosed having the structure wherein R 1 and R 2 are —H, lower alkyl, or label; B is a 7-deazapurine, purine, or pyrimidine nucleoside base; W 1 is...
6949640 Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine  
2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin -9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose;...
6884880 Process for the preparation of 9-β-anomeric nucleoside analogs  
A process for substantially enhancing the regio and stereoselective synthesis of 9-β-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base...
6812342 Esters of cyclic ADP ribose derivatives  
The present invention is directed to the field of organic chemistry in general and specifically to the preparation of hydrophobic derivatives of cyclic ADP ribose. One form of the present invention...
6794142 Amplification using modified primers  
The present invention provides modified primers for use in the amplification of a nucleic acid sequence. Amplifications carried out using the modified primers result in less template-independent...
6610841 Nucleotide-based prodrugs  
This invention relates to nucleotide-based prodrugs and their drug-delivery applications. The nucleotide-based prodrugs of the present invention comprise a drug component covalently attached via...
6555676 Biologically active phosphotriester-type compounds  
Compounds of formula RS—P(═O)(QR)—Nu where: R is a radical —(CH 2 )n—W—X; X is a radical —C(═Z)(Y) or —S—U; Z is O or S; W is O or S; Q is O or S; Y and U are an alkyl, aryl or...
RE38090 3′-substituted nucleoside derivative  
The invention relates to a 3′-substituted nucleoside derivative represented by the following general formula (1): wherein B means a nucleic acid base which may have a substituent, Z represents...
6531589 Base protecting groups and synthons for oligonucleotide synthesis  
The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotides under more mild conditions than existing methods. The invention further...
6506896 Use of a pentopyranosyl nucleoside for producing an electronic component, and conjugates of said pentopyranosyl nucleoside  
The invention relates to a pentopyranosylnucleoside of the formula (I) or of the formula (II) their preparation and use for the production of a therapeutic, diagnostic and/or electronic component.
6420546 Oligoribonucleotide and ribozyme analogs with terminal 3′—3′ and/or 5′—5′ linkages  
The invention relates to oligoribonucleotide analogs with terminal 3′—3′ and/or 5′—5′ internucleotide linkages. This modification stabilizes the molecules altered in this way, including...
6407223 Process for the synthesis of modified P-chiral nucleotide analogues  
The process of the instant invention is drawn to the synthesis of modified P-chiral nucleotide analogues in the form of pure diastereomers possessing preselected configuration at the P-atom....
6329519 Intermediates for oligonucleotide synthesis  
A compound of formula (I) wherein B 1 is a radical of a nucleoside base, R 1 is hydrogen or a hydroxy-protecting group, R 2 is hydrogen, hydroxy or a 2'-nucleoside-modifying atom or group, R 3 ...
6320035 C-nucleoside derivatives and their use in the detection of nucleic acids  
The invention concerns pyrrolo-[3,2-d]pyrimidine, pyrazolo-[4,3-d]pyrimidine and pyrimidine-furanosides i.e. so-called C-nucleosides of the general formulae I-V ##STR1## or appropriate derivatives...
6252060 Antiviral liponucleosides: treatment of hepatitis B  
Compounds for treating hepatitis B infections. The compounds consist of nucleoside analogues having anti-hepatitis B activity which are linked, commonly through a 5' phosphate of the pentose...
6232465 Compositions for enzyme catalyzed template-independent creation of phosphodiester bonds using protected nucleotides  
A method for the stepwise creation of phosphodiester bonds between desired nucleosides resulting in the synthesis of polynucleotides having a predetermined nucleotide sequence by preparing an...
6200757 Method for controlling the extension of an oligonucleotide  
The present invention relates to a method for selectively extending an oligonucleotide primer along a specific target polynucleotide sequence in a mixture of polynucleotides. A combination is...
6140310 Phosphorous prodrugs  
The composition and methods of synthesis of phosphorus prodrugs are described. These methods can be used to convert negatively charged phosphorus bearing drugs into neutrally charged; lipid soluble...
6133438 Process for the preparation of 2'-O-alkyl purine phosphoramidites  
Processes for preparing 2'-O-alkylated guanosine, uridine, cytidine, and 2,6-diaminopurine 3'-O-phosphoramidites include the steps of alkylating nucleoside precursors, adding suitable blocking...
6124445 Phosphotriester oligonucleotides, amidities and method of preparation  
Oligonucleotides having bioreversible phosphate blocking groups can be used as pro drugs for the oligonucleotides. The bio-reversible blocking groups can be removed by intercellular enzymes,...
6048975 Process for the chemical synthesis of oligonucleotides  
A process for the chemical synthesis of oligonucleotides Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable...
6020482 Phosphotriester type biologically active compounds  
Phosphotriester compound of general formula (I); ##STR1## wherein R is a radical --(CH 2 ) n --S--X in which X is a radical (a) or --S--U, Z being O or S, and Y and U denote an alkyl, aryl or...
6001611 Modified nucleic acid amplification primers  
The present invention provides modified primers for use in the amplification of a nucleic acid sequence. Amplifications carried out using the modified primers result in less non-specific...
5990303 Synthesis of 7-deaza-2'deoxyguanosine nucleotides  
The present invention provides 7-deaza-2'-deoxy-guanosine nucleotides of the general formula: ##STR1## wherein R is a --PO 3 H 2 , --P 2 O 6 H 3 or --P 3 O 9 H 4 residue or an alkali metal,...
5977343 Synthesis, deprotection, analysis and purification of RNA and ribozymes  
Method for purification and synthesis of RNA molecules and enzymatic RNA molecules in enzymatically active form.
5955591 Phosphotriester oligonucleotides, amidites and method of preparation  
Oligonucleotides having bioreversible phosphate blocking groups can be used as pro drugs for the oligonucleotides. The bio-reversible blocking groups can be removed by intercellular enzymes,...
5872243 Caged nucleotides  
The present invention describes a family of photolabile caged nucleotides, including cyclic nucleotides. The compounds of the present invention are caged analogs and derivatives of NAD + , NADH,...
5849905 Biologically active phosphotriester-type nucleosides and methods for preparing same  
Compounds of formula RS--P(O) (QR)--Nu where: R is a radical --(CH 2 )n-W--X; X is a radical --C(Z) (Y) or --S--U; Z is O or S; W is O or S; Q is O or S; Y and U are an alkyl, aryl or...
5808035 Protected nucleoside and method for its synthesis  
The present invention relates to a nucleoside having the formula: ##STR1## where R 1 is a hydrogen or a protecting group; R 2 is a hydrogen or a coupling group; R 3 and R 4 are each...
5780617 Synthesis of liponucleotides  
A process for the preparation of glycerol di- or triphosphate derivatives comprising coupling the phosphate group of a glycerol monophosphate derivative in which one of the phosphate hydroxyls is...
5763418 3'-substituted nucleoside derivatives  
The invention relates to a 3'-substituted nucleoside derivative represented by the following general formula (1): ##STR1## wherein B means a nucleic acid base which may have a substituent, Z...
5750676 Process for preparing nucleosides with unprotected sugars  
A novel process for nucleoside synthesis, which process comprises reacting the free sugar with heterocyclic bases in the presence of silylating agents in an inert solvent containing a Lewis acid.
5750674 Methods and compounds for the stereoselective enrichment of oligonucleotide diastereomers and oligonucleotides thereby produced  
The present invention provides new mononucleotide synthons useful in the synthesis of oligonucleotides having from one to all P-chiral centers that are predominantly and independently in the R or S...
5744595 Propargyl modified nucleosides and nucleotides  
The present invention describes a novel 2'-O-alkylation reaction to produce a novel series of nucleosides carrying the 2'-O-propargyl group, using propargyl bromide, dibutyl tin oxide and...
5734042 Process for the production of asymmetrical phosphoric acid diesters  
The present invention concerns a process for the production of asymmetrical phosphoric acid diesters. The process is characterized in that a phosphoric acid ester is condensed with a compound...
5700666 Process for the production of arabinonucleotides  
A process for the production of arabinonucleotides of general formula I ##STR1## in which X represents a hydrogen atom or a fluorine atom, is described, which is characterized in that an...
5696255 Process for the production of 2-fluoropurine derivatives  
This invention relates to a process for the production of 2-fluoropurine derivatives from 2-aminopurine derivatives, which are reacted in HF/pyridine or HF/pyridine/H 2 O in the presence of a...
5668270 Process for the preparation of fludarabine or fludarabine phosphate from guanosine  
A process for the production of fludarabine or fludarabine phosphate is provided, wherein the nucleoside guanosine or a suitable derivative is employed as the starting material. The guanosine...
5659027 Boronated compounds  
A novel class of pharmaceutically active boronated compounds are provided. The boronated compounds include boronated purine and pyrimidine bases and boronated nucleosides, as well as phosphate...
5646265 Process for the preparation of 2'-O-alkyl purine phosphoramidites  
2'-O-alkylated guanosine, uridine, cytidine, and 2,6-diaminopurine 3'-O-phosphoramidites are prepared by alkylating nucleoside precursors, adding suitable blocking groups and phosphitylating....
5639867 TTTr as protective group in nucleotide synthesis  
The invention relates to nucleosides, nucleotides and oligonucleotides carrying in their basic structure a primary hydroxyl group protected by tris-4,4',4"-tert-butylphenylmethyl, to processes for...
5627165 Phosphorous prodrugs and therapeutic delivery systems using same  
The composition and methods of synthesis of phosphorus prodrugs are described. These methods can be used to convert negatively charged phosphorous bearing drugs into neutrally charged; lipid...
5623069 Method for producing 5'-nucleotide  
A method of producing 5'-nucleotide, which comprises maintaining a nucleoside suspension in an organic solvent at a temperature not lower than about 20° C., and then subjecting the resultant...
5621086 Sialic acid derivative and method of manufacturing it  
The present invention is drawn to methods of manufacturing a sialic acid derivative suitable for industrial production. With a method of the present invention, Tetra-O-acetylsialic acid (4a) and...
5614622 5-pentenoyl moiety as a nucleoside-amino protecting group, 4-pentenoyl-protected nucleotide synthons, and related oligonucleotide syntheses  
The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotide under more mild conditions than existing methods. The invention further...
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