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7385050 |
Cleavable linker for polynucleotide synthesis
Functionalized supports for polynucleotide synthesis are disclosed. The supports have linker moieties that are stable to conditions used in polynucleotide synthesis, but may be cleaved to release...
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7335765 |
Nucleoside and oligonucleotide analogues
A compound of the formula (1):
wherein R 1 and R 2 are the same or different and represent a hydrogen atom, a hydroxyl protecting group, a phosphate group, or —P(R 3 )R 4 , wherein R 3 and...
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7307166 |
Oxpurine nucleosides and their congeners, and acyl, derivatives thereof, for improvement of hematopoiesis
The invention relates to certain oxypurine nucleosides, congeners of such oxypurine nucleosides, and acyl derivatives thereof, and compositions which contain at least one of these compounds. The...
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7271258 |
Methods of synthesizing oligonucleotides using carbonate protecting groups and alpha-effect nucleophile deprotection
The invention provides methods for synthesizing oligonucleotides using nucleoside monomers having carbonate protected hydroxyl groups that are deprotected with α-effect nucleophiles. The α-effect...
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7179896 |
Method of making PNA oligomers
This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA...
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7101993 |
Oligonucleotides containing 2′-O-modified purines
Compounds are provided containing purine nucleotides that bear moieties X at the 2′ position thereof wherein X is R 1 —(R 2 ) n ; R 1 is C 3 -C 20 alkyl, C 4 -C 20 alkenyl or C 2 -C 20 ...
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7101992 |
Nucleic acid base pair
A novel artificial nucleic acid base pair which is obtained by forming a selective base pair by introducing a group having steric hindrance (preferably a group having steric hindrance and static...
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6972330 |
Chemical synthesis of methoxy nucleosides
Process for chemical synthesis of methoxy nucleosides.
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6924271 |
3-β-D-ribofuranosylthiazolo[4-5-d]pyridimine nucleosides and uses thereof
The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention...
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6914138 |
Urea nucleosides as therapeutic and diagnostic agents
Modified nucleosides and methods of making and using the nucleosides are disclosed. The compounds can be prepared by reacting nucleoside starting materials that contain a suitable leaving group at...
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6914061 |
4′-thio-L-xylofuranosyl nucleosides, precursors thereof, preparation and use thereof
Compounds represented by the formula 1:
A is selected from the group consisting of
wherein each R individually is H or acyl, Y is X, N 3 , NH 2 , monoalkylamino, or dialkylamino; Z...
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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...
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6762170 |
2-(purin-9-yl)-tetrahydrofuran-3,4-diol derivatives
There are provided according to the invention, novel compounds of formula (I) wherein R 1 , R 2 and R 3 are as described in the specification, processes for preparing them, formulations...
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RE38416 |
Cross-linking oligonucleotides
This invention is directed to novel substituted nucleotide bases with a crosslinking arm which accomplish crosslinking between specific sites on adjoining strands of oligonucleotides a...
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6677345 |
Cyclin dependent kinase inhibitors
A range is disclosed of pyrimidine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDK's) and which thereby can provide useful therapeutic compounds for use in treatment of...
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6646118 |
Solid phase synthesis
The present invention relates to a support system for solid phase synthesis of oligomers, such as oligonucleotides, wherein the starting compound is bound to the support via a disiloxyl linkage....
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6593466 |
Guanidinium functionalized nucleotides and precursors thereof
The present invention provides oligomers which are specifically hybridizable with a selected sequence of RNA or DNA wherein at least one of the nucleoside moieties of the oligomer is modified to...
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6579976 |
Process for producing 2′,3′-diethyl substituted nucleoside derivatives
There can be provided an excellent industrial process for producing compounds having sugar-moiety hydroxyl groups or halogen atoms reduced in nucleic acids or in derivatives thereof by allowing...
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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...
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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...
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6534486 |
2-(purin-9-yl)-Tetrahydrofuran-3,4-diol derivatives
A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2a...
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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...
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6506888 |
2′-O-amino-containing nucleoside analogs and polynucleotides
Novel nucleoside or nucleotide analogs comprising 2′-O-amino residues, processes for their synthesis and incorporation into polynucleotides.
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6504024 |
Propargylethoxyamino nucleotide primer extensions
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...
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6498241 |
2-deoxy-isoguanosines isosteric analogues and isoguanosine derivatives as well as their synthesis
2′-Deoxyisoguanosine, isosteric analogues and isoguanosine derivatives of formulae I-V, processes for their production via compounds of the general formulae a or b and reaction with aroyl...
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6498149 |
Natural antitumor or antiviral substances and use of the same
The present invention provides substances having an efficacy against tumors and viruses on which the conventional anti-tumor agents and anti-virus agents exhibit only insufficient effects, and...
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6495528 |
2-(Purin -9-yl)-tetrahydrofuran-3,4-diol derivatives
A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2...
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6455690 |
L-8-oxo-7-propyl-7,8-dihydro-(9H)-guanosine
Novel nucleosides having the structure of Formula 1 and Formula 2 are contemplated. In one aspect of the invention, controlled release dosage forms are particularly contemplated. Further,...
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6414137 |
Selective solvent extraction for the purification of protected nucleosides
A process for the purification of nucleosides, and more particularly to a selective solvent extraction method for purifying protected nucleosides. In the purification process, solid particles of...
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6355787 |
Purine nucleoside modifications by palladium catalyzed methods and compounds produced
This invention discloses a method for the preparation of 2′-modified nucleosides, using a palladium catalyst and an alkene functionalized with a heteroatom. Included in the invention are the...
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6333315 |
4'-C-ethynyl purine nucleoside compounds
The invention provides 4'-C-ethynyl purine nucleosides represented by formula [I]: ##STR1## wherein B represents a base selected from the group consisting of purine and derivatives thereof; X...
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6320040 |
4-desmethyl nucleoside analogs and oligomers thereof
Tetrahydrofuranyl compounds are provided that are functionalized to include pendant conjugate groups, and which are useful in diagnosis assays and as research reagents. Novel intermediates for the...
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6274725 |
Activators for oligonucleotide synthesis
The present invention relates to improved methods for the preparation of nucleoside phosphoramidites and oligonucleotides. In one aspect, the methods of the invention are used to prepare...
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6271358 |
RNA targeted 2'-modified oligonucleotides that are conformationally preorganized
2'-O-modified ribosyl nucleosides and modified oligonucleotides containing such nucleotides are disclosed. Oligonucleotides are disclosed that have increased binding affinity as shown by molecular...
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6265558 |
Thiol-derivatized nucleosides and oligonucleosides
Nucleosides and linked nucleosides functionalized to include alkylthiol chemical functionality at ribofuranosyl positions, nucleosidic base positions, or on internucleoside linkages. In certain...
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6262254 |
8-fluoropurine compounds
An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred...
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6194390 |
Procedure to block the replication of reverse transcriptase dependent viruses by the use of inhibitors of deoxynucleotides synthesis
A method for inhibiting replication of reverse transcriptase dependent virus in plant or animal cells, comprising the step of administering to said cells a compound that depletes the intracellular...
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6187914 |
Nucleoside derivatives, and their use in oligonucleotide synthesis
The invention relates to nucleoside derivatives bearing electrolabile protector groupings and their use in an oligonucleotide synthesis method comprising at least one step of electronic deprotection.
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6172209 |
Aminooxy-modified oligonucleotides and methods for making same
Oligonucleotides and other macromolecules are provided which have increased nuclease resistance, substituent groups (such as 2'-aminooxy groups) for increasing binding affinity to complementary...
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6166199 |
N-2 substituted purines
This invention presents novel purine-based compounds for inclusion into oligonucleotides. The compounds of the invention, when incorporated into oligonucleotides are especially useful as...
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6153594 |
5'-O-acylated antiviral nucleosides
A monoester compound of formula I: Nu--O--Fa wherein O is oxygen, Nu is a nucleoside analog, Fa is an acyl group of a mono-unsaturated C18 or C20 omega-9 fatty acid, which fatty acid is...
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6147200 |
2'-O-acetamido modified monomers and oligomers
Nucleosidic monomers and oligomeric compounds prepared therefrom are provided. Also provided is a novel method of deprotection of oligomeric compounds. Oligomeric compounds having at least one...
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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...
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6127533 |
2'-O-aminooxy-modified oligonucleotides
Nucleotide compositions containing aminooxy moieties are provided. In accordance with preferred embodiments, oligonucleotides and oligonucleotide analogs are provided which are specifically...
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6121431 |
Nucleoside derivatives
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6117988 |
Nucleotides and oligonucleotides preparable therefrom
Analogues of RNA and DNA compounds contain a neutral, stereoregular linking group based on replacement of the phosphoryl with a sulfonyl group. Precursors to the analogues are also described, as...
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6096724 |
Pyrimidine derivatives and guanine derivatives, and their use in treating tumor cells
The present invention provides certain 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR1## wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring,...
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6054442 |
Methods and compositions for modulation and inhibition of telomerase in vitro
It was found that normal human stem cells produce a regulated non-processive telomerase activity, while cancer cells produce a processive telomerase activity. Nucleotide analogs, such as...
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6043228 |
O.sup.6 -substituted guanine derivatives, a process for their preparation and their use in treating tumor cells
O 6 -hetarylalkyl- or naphthylalkylguanine derivatives of the formula ##STR1## wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR', wherein X is O or S, R" and R"' are alkyl, or substituted...
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6001817 |
Pharmaceutical composition comprised of cisplatin, and processes for making and using same
A pharmaceutical composition, comprising cisplatin, a special carrier and, optionally, customary pharmaceutical excipients, is disclosed. The preparation of this pharmaceutical composition is also...
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