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7601702 |
Dutpase Inhibitors
Deoxyuridine derivatives of Formula (I′); where A is O, S or CH 2 ; B is O, S or CHR 3 ; R 1 is H, or various substituents; R 2 is H, F; R 3 is H, F, OH, NH 2 ; or R 2 and R 3 together form...
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7589078 |
Anti-viral nucleoside analogs and methods for treating viral infections, especially HIV infections
The present invention relates to compounds according to the general formula:
wherein B is
or
and the remaining variables are defined in the specification, and compositions comprising...
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7429572 |
Modified fluorinated nucleoside analogues
The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a...
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7192936 |
Modified 2′ and 3′-nucleoside prodrugs for treating Flaviviridae infections
2′ and/or 3′ prodrugs of 1′, 2′, 3′ or 4′-branchednucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and...
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7169766 |
Methods and compositions for treating hepatitis C virus
A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1′, 2′ or 3′-modified nucleoside or a...
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7163929 |
Methods and compositions for treating flaviviruses and pestiviruses
A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or...
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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.
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7144874 |
Aryl phosphate derivatives of d4T having activity against resistant HIV strains
Methods of inhibiting virus replication of in a cell infected with a resistant strain of HIV that includes administering to the infected cell a virus replication inhibiting amount of an aryl...
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7119096 |
Uracil reductase inactivators
Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent...
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7101861 |
Methods and compositions for treating flaviviruses and pestiviruses
A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or...
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6974802 |
Treatment of viral infections using prodrugs of 2′,3-dideoxy,3′-fluoroguanosine
A method of treating HBV or HIV infections comprising administering to an individual an effective amount of the compound of formula IId′:
wherein R 2 is the residue of an aliphatic...
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6960568 |
Nucleosides and related processes, pharmaceutical compositions and methods
The invention provides novel nucleosides and related processes, pharmaceutical compositions, and methods. The novel nucleosides are useful in a wide variety of antiviral, antineoplastic, and...
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6930097 |
Matrix metalloproteinase and tumor necrosis factor inhibitors
A compound of formula 1-[3,4-dihydroxy-5-(2-hydroxyethyl)tetrahydrofuran-2-yl]pryi
midine-2,4(1H,3H)-dione has inhibitory effects of matrix metalloproteinase-2 (gelatinase A) enzyme and binding of...
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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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6846918 |
Nucleoside modifications by palladium catalyzed methods
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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6841675 |
Piperazine-based nucleic acid analogs
A novel nucleoside analog is disclosed which comprises a piperazine ring in the place of the ring ribose or deoxyribose sugar. Monomers utilizing a broad variety of nucleobases are disclosed, as...
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6822089 |
Preparation of deoxynucleosides
Methods for preparing deoxynucleosides from their corresponding ribonucleosides by forming 3-tert-butylphenoxythiocarbonylderivatives of the ribonucleosides and subsequently effecting radical...
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6812219 |
Methods and compositions for treating flaviviruses and pestiviruses
A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1′, 2′ or...
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6784161 |
Method for the treatment or prevention of flavivirus infections using nucleoside analogues
The present invention relates to a method for the treatment or prevention of Flavivirus infections using nucleoside analogues in a host comprising administering a therapeutically effective amount...
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6680303 |
3′,5-difluoro-2′,3′-didehydropyrimidine nucleosides and methods of treatment therewith
A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or...
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6670336 |
Aryl phosphate derivatives of d4T having anti-HIV activity
Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular,...
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6635753 |
Process for the preparation of substantially pure stavudine and related intermediates useful in the preparation thereof
There are disclosed novel Stavudine solvates as follows: Stavudine NN-dimethyllacetamide solvates; Stavudine NN-dimethylacrylamide solvates and Stavudine NN-dimethylpropionamide solvates and...
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6602664 |
3′-azido-2′,3′-dideoxyuridine in an anti-HIV effectiveness test protocol
It has been discovered that 3′-azido-2′,3′-dideoxyuridine (CS-87) induces a transient mutation in HIV-1 at the 70 th codon (K to R, i.e., lysine to arginine) of the reverse transcriptase...
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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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6482805 |
AZT derivatives exhibiting spermicidal and anti-viral activity
Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or...
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6458772 |
Prodrugs
Compounds of the formula I or corresponding monohydroxynucleoside derivatives wherein: R 1 is hydroxy, amino or carboxy: optionally having esterified/amide bonded thereon; a C 4 -C 22 ...
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6458773 |
Nucleoside with anti-hepatitis B virus activity
Compounds and pharmaceutical compositions active against hepatitis B virus are provided, as is a method for the treatment of hepatitis B virus infection in humans and other host animals is provided...
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6392032 |
Heavily fluorinated sugar analogs
Heavily fluorinated sugar analogs of formula wherein R 1 is selected from alkyl, alkenyl, aryl, —CH 2 —O-alkyl, —CH 2 —O-aryl, —CH 2 OPO 3 H, —CH 2 —O-carbohydrate, —CH 2...
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6384019 |
Gemcitabine derivatives
The invention provides Gemcitabine esters or amides in which the 3′- and/or 5′-OH group and/or the N 4 -amino group is derivatised with a C 18 - and/or C 20 -saturated or mono-unsaturated acyl...
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6297223 |
Uracil reductase inactivatores
Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-fluorouracil and find use particularly in the treatment of cancer. The 5-substituent...
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6268374 |
Uracil reductase inactivators
The present invention relates to a group of 5-substituted uracil derivatives which are inactivators of uracil reductase and which are particularly useful in cancer chemotherapy, especially in...
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6232300 |
Treatment of HIV by administration of β-D-2', 3'-didehydro-2',3'-dideoxy-5-fluorocytidine (D4FC)
A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or...
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6211349 |
Protonated/acidified nucleic acids and methods of use
The novel discovery that protonated nucleic acids inhibit bacterial growth is reported and methods for the preparation and therapeutic use of nuclease resistant and acid resistant...
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6207650 |
Antiviral, highly water soluble, stable, crystalline salts of 2', 3'-dideoxyinosine, 2', 3'-dideoxy-2', 3'-didehydrothymidine and 2', 3'-dideoxy-2'-fluoroinosine
Provided are very highly water soluble, stable, crystalline salts of 2',3'-dideoxy-2',3'-didehydrothymidine ("d4T"), 2',3'-dideoxyinosine ("ddI"), and 2',3'-dideoxy-2'-fluoroinosine ("F-ddI"). Such...
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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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6191120 |
Spermicidally active 5-halo-6-alkoxy-5,6-dihydro-2',3'-dideoxy-uridines and their pharamaceutical compositions
Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or...
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6184364 |
High affinity nucleic acid ligands containing modified nucleotides
Nucleic acid ligands containing modified nucleotides are described as are methods for producing such oligonucleotides. Such ligands enrich the chemical diversity of the candidate mixture for the...
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6156737 |
Use of dideoxy nucleoside analogues in the treatment of viral infections
The present invention is directed to a method of treating hepatitis B viral infections in mammals comprising the administration of β-L-5-fluoro-2',3'-dideoxycytidine and pharmaceutically...
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6117849 |
S-(+)-adenosylmethionine and 3'-azido-2', 3'-dideoxy-nucleoside complexes as potent inhibitors of HIV-replication
Molecular Complexes, comprising of S-(+)-adenosylmethionine and 3'-azido-2',3'-dideoxy nucleosides are prepared, and shown to have synergistic inhibitory effects on the replication of...
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6107288 |
Antiviral nucleoside combination
Synergistic combinations of nucleoside derivatives, pharmaceutical formulations containing said combinations and use of the combinations in the treatment of retroviral infections are disclosed.
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6093702 |
Mixtures of dideoxy-nucleosides and hydroxycarbamide for inhibiting retroviral spread
A method and composition for inhibiting the spread of a retrovirus such as HIV in a human cell population in which a retrovirus such as HIV is present has been found. The spread of the retrovirus...
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6025482 |
Backbone modified oligonucleotide analogs and preparation thereof through reductive coupling
Methods for preparing oligonucleotide analogs which have improved nuclease resistance and improved cellular uptake are provided. In preferred embodiments, the methods involve reductive coupling of...
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6005097 |
Processes for high-yield diastereoselective synthesis of dideoxynucleosides
The present invention relates to methods for substantially enhancing the stereoselective synthesis of β-anomeric nucleoside analogs. In methods according to the present invention, the introduction...
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5959100 |
Pyrimidine 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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5905070 |
5--Caboxamido or 5--fluoro!-- 2', 3'--unsaturated or 3'--modified!--pyrimidine nucleosides
A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a 5-carboxamido or...
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5831075 |
Amino acid ester of nucleoside analogues
A process for the preparation of an amino acid ester of a nucleoside analogue comprises reacting a nucleoside analogue having an esterifiable hydroxy group with a 2-oxa-4-aza-cycloalkane-1,3-dione....
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5817799 |
2'-Fluorofuranosyl derivatives and methods for preparing 2'-fluoropyrimidine and 2'-fluoropurine nucleosides
A method of preparing a 2'-fluoro compound of the formula ##STR1## where B is selected from the group consisting of purines and pyrimidines, both of which may be substituted, comprises reacting a...
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5811540 |
5-O-pyrimidyl-2,3-dideoxy-1-thiofuranoside derivative, and production method and use thereof
Disclosed is a 5-O-pyrimidyl-2,3-dideoxy-1-thio-D-furanoside derivative represented by the following formula (I) or an L-form isomer thereof: ##STR1## wherein X represents a hydrogen atom, a...
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5808048 |
Process for preparing 1-(2'-deoxy-2',2'-difluoro-D-ribofuranosyl)-4-aminopyrimidin-2-one) hydrochloride
This invention provides a process for preparing gemcitabine hydrochloride which comprises deblocking β-1-(2'-deoxy-2',2'-difluoro-3',5'-di-O-benzoyl-D-ribofuran
osyl)-4-am inopyrimidin-2-one with...
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5770716 |
Substituted propargylethoxyamido nucleosides, oligonucleotides and methods for using same
Substituted propargylethoxyamido nucleosides are disclosed having the structure ##STR1## wherein X is selected from the group consisting of amino alkanoic acid, alkylamino benzoic acid, α-amino...
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