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7632825 |
Methods of decreasing or preventing pain using spicamycin derivatives
Methods of providing pain relief by administering a water-soluble derivative of spicamycin. Methods of using pain mediation agents are also provided.
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7629447 |
Dideoxynucleoside derivatives
The invention provides a 5′-amino-2′-fluoro-2′,5′-dideoxynucleoside compound represented by the formula [1]:
wherein R 1 represents a nucleic acid base which may have a protecting...
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7605143 |
2-propynyl adenosine analogs with modified 5′-ribose groups having A2A agonist activity
The invention provides compounds having the following general formula (I):
wherein X, R 1 , R 2 , R 7 and Z are as described herein.
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7553823 |
C-pyrazole A2A receptor agonists
2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for...
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7514417 |
A1 adenosine receptor agonists
Disclosed are novel compounds that are partial and full A 1 adenosine receptor agonists having the structure of Formula I:
which are useful for treating various disease states, in particular...
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7511133 |
Adenosine A3 receptor agonists
The compounds of the following formula:
wherein Ar, R and R 1 have the meanings given in the specification. This series of sulfonamido derivatives with a conserved uronamide group at the...
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7470784 |
Methods for synthesizing 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin
-6-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofiranose;...
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7427679 |
Precursors for two-step polynucleotide synthesis
Precursors for use in the synthesis of polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl...
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7423144 |
Purine Derivatives as adenosine A1 receptor agonists and methods of use thereof
The invention relates to Purine Derivatives; compositions comprising an effective amount of a Purine Derivative; and methods for reducing an animal's rate of metabolism, protecting an animal's...
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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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7300923 |
Partial and full agonists of A1 adenosine receptors
Disclosed are syntheses suitable for large scale manufacture of novel compounds that are partial and full A 1 adenosine receptor agonists, useful for treating various disease states, in particular...
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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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7262176 |
Adenosine A3 receptor agonists
Disclosed are novel compounds that are A 3 adenosine receptor agonists, useful for treating various disease states, including cancer, cardiac ischemia, leukopenia, and neutropennia.
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7238676 |
Purine derivatives
The present invention relates to compounds of the formula
and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation...
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7217815 |
2-beta -modified-6-substituted adenosine analogs and their use as antiviral agents
Various 2′-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and...
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7214665 |
2-propynyl adenosine analogs having A2A agonist activity and compositions thereof
The invention provides compounds having the following general formula (I):
wherein X, R 1 , R 2 , R 7 and Z are as described here.
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7199127 |
Purine nucleosides
Disclosed are purine nucleoside compounds that are selective to A 3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the...
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7196071 |
Methods of decreasing or preventing pain using spicamycin derivatives
Methods of providing pain relief by administering a water-soluble derivative of spicamycin. Methods of using pain mediation agents are also provided.
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7182939 |
Hair tonic composition
A hair tonic composition containing adenosine, adenosine 5′-phosphate, and/or an adenosine 5′-phosphate salt as an active ingredient.
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7163928 |
Partial and full agonists of A1 adenosine receptors
Disclosed are novel compounds that are partial and full A 1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and...
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7148223 |
4′-thio-L-xylo furanosyl 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 is...
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7141553 |
A3AR agonists for the treatment of inflammatory arthritis
The present invention concerns a method for the treatment of inflammatory arthritis, and in particular rheumatoid arthritis, by administering to the subject specific low dosages of...
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7109180 |
C-pyrazole A2A receptor agonists
2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for...
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6995148 |
Adenosine cyclic ketals: novel adenosine analogues for pharmacotherapy
The present invention relates to novel compounds that are novel adenosine receptor analogues. Specifically, the compounds of the present invention preferably function as both adenosine receptor...
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6972330 |
Chemical synthesis of methoxy nucleosides
Process for chemical synthesis of methoxy nucleosides.
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6951932 |
Synthesis of 2-aralkoxyadenosines and 2-alkoxyadenosines
The invention provides new methods for synthesis of 2-aralkyloxyadenosines and 2-alkoxyadenosines. The invention is particularly useful for synthesis of 2-[2-(4-chlorophenyl)ethoxy]adenosine....
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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;...
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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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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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6906190 |
Inhibitors for de novo-RNA polymerases and methods of identifying targets for same
A polymerase inhibitor has first moiety coupled to a second moiety via an optional linker in which the first moiety binds to an initiation nucleotide binding site of a polymerase and forms at least...
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6903079 |
Nucleoside compounds and compositions thereof
The invention provides a novel class of substituted nucleoside derivatives having the formula:
A-Z1-L-Z2-G
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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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6831072 |
Compositions and methods of synthesis and use of novel nucleic acid structures
The present invention is directed to a method to produce 8-amino-2′deoxyadenosine by treating 8-azido-2′deoxyadenosine with an aqueous solution of methylamine or dimethylamine.
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6713623 |
Tetraphosphonate bicyclic trisanhydrides
Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.
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6699978 |
Linker nucleoside, and production and use of the same
The present invention relates to a linker nucleoside, its preparation and use for the covalent bonding of biomolecules to oligonucleotides, in particular p-RNA oligonucleotides.
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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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6680052 |
Methods of inhibiting tumor growth using adenosine receptor activated cells
Methods of treating and/or imaging tumors utilize A 1 adenosine-receptor activated cells (such as monocytes and macrophages) are described. Activated cells may be administered systemically or...
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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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6596858 |
Process for the production of 2-halo-6-aminopurine derivatives
A novel process for preparing 2-halo-6-aminopurine derivatives and their analogs is disclosed. The method comprises halogenation of 2,6-diaminopurine derivatives at the C-2 position in a specific...
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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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6576619 |
Orally active A1 adenosine receptor agonists
Esters of N 6 -oxa, thia, thioxa and azacycloalkyl substituted adenosine derivatives having the following formula; wherein the compounds are selective adenosine type 1 receptor agonists that are...
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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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6548486 |
Fatty acid esters of nucleoside analogs
New compounds of the general formula (I): Nu-O-Fa, wherein O represents an oxygen, Nu is a nucleoside or nucleoside analogue, and Fa is an acyl group of a mono-unsaturated C18 or 20 fatty acid. The...
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6545134 |
Method for the production of pentopyranosyl nucleosides
Processes for the preparation of 3′,4′-cyclic acetals of pentopyranosylnucleosides, in which the pentopyranosyl nucleoside is reacted with an aldehyde, ketone, acetal, or ketal under reduced...
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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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6528042 |
Compositions of flavonoids for use as cytoprotectants and methods of making and using them
Non-naturally-occurring compositions for use in amelioration of disruption of energy metabolism secondary to stress are described. These compositions comprise a flavonoid or derivative thereof and...
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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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