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8183216 |
Nucleoside derivatives as inhibitors of viral polymerases
A class of nucleoside derivatives of formula (I), as defined herein, that are useful as inhibitors of RNA-dependent RNA viral replication and in particular HCV replication, are provided. Also...
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8178510 |
Preparation of thioarabinofuranosyl compounds and use thereof
Patients suffering from cancer are treated by being administered a compound represented by the following formula: wherein each R individually is H or an aliphatic or aromatic acyl group;A is...
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8178502 |
Effective treatment of esophogeal adenocarcinoma using triciribine and related compounds
The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat esophogeal adenocarcinoma by one or a combination of (i) administering...
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8173620 |
BHQ-caged nucleotide probes photolysable by two-photon excitation
The disclosure encompasses caged compounds such as caged nucleoside phosphoesters (caged nucleotides). In an embodiment, the caged nucleotides include compounds corresponding to those described by...
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8163707 |
4′-allene-substituted nucleoside derivatives
The present invention discloses compounds of formula (I), or its β-L enantiomer, or a pharmaceutically acceptable salt, ester, stereoisomer, tautomer, solvate, prodrug, or combination thereof: ...
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8158605 |
Azacytidine analogues and uses thereof
The present invention is directed toward compounds of Formula (I) as follows: wherein, R is H, R5C(O);R1 is where the crossing dashed line illustrates the bond formed joining R1 to the molecule of...
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8158606 |
β-L-2′-deoxynucleosides for the treatment of resistant HBV strains and combination therapies
It has been discovered that β-L-2′-deoxynucleosides are active against drug-resistant hepatitis B virus with mutations. A method for treating lamivudine resistant HBV (M552V) in a host is pr...
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8147818 |
Hepatitis C virus inhibitors
The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such...
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8133872 |
Use of nicotinic acid adenine dinucleotide phosphate or derivative thereof as agent for treating type-2 diabetes
The administration of nicotinic acid adenine dinucleotide phosphate (NAADP) or a pharmaceutically acceptable salt thereof to a host in need thereof for the treatment of type-2 diabetes has been...
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8114847 |
Selective inhibitors of translesion DNA replication
An agent for inhibiting translesion DNA replication comprises a non-natural adenine ribose analog represented by those as set forth in FIG. 1.
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8106023 |
1,4-benzothiepin-1, 1-dioxide derivatives with improved properties method for producing the same, drugs containing said compounds and the use thereof
This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives with improved properties, method for producing the same, drugs containing said compounds and use thereof.
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8106022 |
Carbohydrate conjugates as delivery agents for oligonucleotides
The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein:A and B are each independently for each occurrence O, N(RN) or S;X and Y are each...
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8101583 |
1,4-benzothiepin-1,1-dioxide derivatives which are substituted with fluorine, method for producing the same, drugs containing said compounds and use thereof
This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives which are substituted with fluorine, method for producing the same, drugs containing said compounds and use thereof.
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8097595 |
Modulation of telomere length in telomerase positive cells and cancer therapy
Induction of telomere shortening, G2 arrest and apoptosis in telomerase positive cancer cells using acyclic nucleoside analogs has been disclosed. In addition, methods for impairment or prevention...
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8093226 |
Cytostatic 7-deazapurine nucleosides
The invention provides compounds of formula I: wherein R1 and R2 have any of the values defined in the specification and salts thereof, as well as compositions comprising such compounds and...
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8093220 |
Combination of an HDAC inhibitor and an antimetabolite
The invention relates to a combination which comprises: (a) a HDAI; and(b) an anti-metabolite, for simultaneous, concurrent, separate or sequential use, especially for use in the treatment of...
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8088746 |
Bis-modified bicyclic nucleic acid analogs
The present disclosure describes bis-modified bicyclic nucleosides and oligomeric compounds that can be prepared comprising at least one of these bis-modified bicyclic nucleosides. More...
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8088368 |
Antiviral compounds
The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and...
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8076303 |
Nucleotide and oligonucleotide prodrugs
The present invention discloses compounds of formula (I): which exhibit antiviral properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned...
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8076311 |
Compositions and methods for modulating the immune system
The present invention provides methods and compositions for the prophylaxis of blood cell disorders such as neutropenia, thrombocytopenia, lymphocytopenia, and anaemia. The invention provides...
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8071535 |
Guanidinium derivatives for improved cellular transport
Reagents and methods useful for the synthesis of conjugates comprising guanidinylated cyclic acetals are provided. Also provided are methods for increasing the cellular uptake of various...
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8067392 |
Compositions and methods for treatment of mitochondrial diseases
Compounds, compositions, and methods are provided for treatment of disorders related to mitochondrial dysfunction. The methods comprise administering to a mammal a composition containing pyrimidien...
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8067391 |
ODCase inhibitors for the treatment of malaria
The present invention includes methods of treating or preventing malaria by administering an anti-malarial effective amount of 6-substituted uridine derivatives to a subject need thereof. The...
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8063025 |
Nucleoside prodrugs and uses thereof
Compounds having the formula I or II wherein R1, R2, B, and V are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV...
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8058261 |
3′-ethynylcytidine derivative
To provide a compound which exhibits excellent anti-tumor activity and excellent oral absorption and which is a useful anti-tumor drug. The invention provides a 3′-ethynylcytidine derivative r...
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8058258 |
Methods for cancer therapy and stem cell modulation
The present invention relates to a method of inducing apoptosis in a tumour cell as well as modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method...
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8058259 |
Substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters as A2AR agonists
The present invention provides substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-pur
in-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters and pharmaceutical compositions...
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8048862 |
Macrocyclic inhibitors of hepatitis C virus replication
The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The...
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8044033 |
Fluorocytidine derivatives and COX-2 inhibitors for the treatment of cancer
The present invention provides, in certain embodiments, methods for the treatment of colorectal cancer comprising administering a COX-2 inhibitor and fluorocytidine derivative to a human patient....
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8044034 |
Nanoparticle derivatives of gemcitabine
The use of squalenic acid or a derivative thereof in formulating at least one polar active principle with a molecular weight of 100 Da or more, in the form of nanoparticles, and pharmaceutical...
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8034802 |
Administration of TLR7 ligands and prodrugs thereof for treatment of infection by hepatitis C virus
This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention...
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8034396 |
Bioadhesive composition formed using click chemistry
The present disclosure provides compositions which may be utilized as adhesives or sealants in medical and surgical applications. The compositions may, in embodiments, be formed from the...
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8017594 |
Agent against psychosocial stresses
To provide a novel anti-psychosocial stress agent which is highly safety and can be continuously taken, more particularly, a novel anti-psychosocial stress agent which prevents or alleviates...
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8003324 |
Modulation of sodium channels by nicotinamide adenine dinucleotide
The present invention relates to the use of oxidized nicotinamide adenine dinucleotide (NAD+) or of its reduced form, NADH, as sodium channel modulators. The present invention also relates to the...
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7994143 |
Metabolically stable alkoxyalkyl esters of antiviral or antiproliferative phosphonates, nucleoside phosphonates and nucleoside phosphates
The present invention relates to phosphonate, nucleoside phosphonate or nucleoside phosphate compounds, compositions containing them, processes for obtaining them, and their use in treating a...
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7994142 |
Agents containing folic acid, vitamin B6 and vitamin B12, and the use thereof
The invention relates to agents that contain folic acid, vitamin B6 and vitamin B12, and to the use thereof in hyperhomocysteinemia for controlling homocysteine levels. The agents are mainly...
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7989430 |
Antibacterial agents
The invention provides compounds of formula (I) and salts thereof: R1-L-R2—B wherein R1, L, R2, and B have any of the values defined herein, as well as compositions comprising such compounds, and t...
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7989422 |
Antibacterial agents
The present invention, in one aspect, provides a method of inhibiting bacterial growth by contacting bacteria with an effective amount of at least one monosaccharide compound of formula (1) as...
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7985737 |
Compositions and methods for the regulation of homocysteine levels within the body
Described herein is a method for reducing levels of the harmful metabolic waste product of S-adenosylmethionine (SAMe), homocysteine, and provide vitamin and other nutritional co-factors that...
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7985738 |
Cytosine nucleoside analogs and isoflavones and uses thereof
Methods, uses, compositions and kits relating to the inhibition and/or prevention of undesirable cell proliferation, and prevention and/or treatment of diseases or disorders associated with such...
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7981930 |
Compositions and kits for treating influenza
Kits comprising an M2 inhibitor selected from amantadine and rimantadine; ribavirin, and a neuraminidase inhibitor (NAi) in an amount that is antivirally effective in the combination, an oral...
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7977320 |
Method of increasing efficacy of tumor cell killing using combinations of anti-neoplastic agents
The present invention provides compositions and methods for increasing the amount of active Syk protein kinase and or SHP-1 protein phosphatase in a cell. The compositions and methods are useful...
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7964181 |
Amino acid surrogates for peptidic constructs
Ring-constrained amino acid surrogates of formula I: where R1, R2, R3, R4, R5, R6a, R6b, R7, and y are as defined in the specification, methods for synthesizing ring-constrained amino acid...
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7964580 |
Nucleoside phosphoramidate prodrugs
Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt),...
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7951789 |
Compounds and pharmaceutical compositions for the treatment of viral infections
Provided herein are compounds, compositions and methods for the treatment of liver disorder, including HCV and/or HBV infections. Specifically, compound and compositions of nucleoside derivatives...
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7951788 |
Method of treating cancer and other conditions or disease states using L-cytosine nucleoside analogs
The present invention relates to the use of the compound according to formula (I) Where S is (A) or (B); X is H or F; R1 is H, an acyl group, a C1-C20 alkyl or ether group, a phosphate,...
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7951787 |
Phosphoramidate compounds and methods of use
Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may...
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7947661 |
Compounds for the treatment of marihuana dependence, withdrawal, and usage
The invention provides methods for treating or suppressing marihuana usage, withdrawal, or dependence involving administration of a therapeutically-effective amount of a cytosine-containing or...
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7935674 |
Indole derivatives
Novel indole derivatives of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is halogen, or alkyl, R2 is hydrogen, or halogen, Ar is phenyl, or thienyl, which may be...
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7935681 |
Antiviral nucleosides
4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3
-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C (HCV) polymerase inhibitors. Also disclosed...
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