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7615542 |
Dioxolane thymine and combinations for use against 3TC/AZT resistant strains of HIV
The present invention relates to the use of a dioxolane thymine compound according to the chemical structure of Formula (I): where R 1 is H, an acyl group, a C 1 -C 20 alkyl or ether group, a...
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7605147 |
Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same
The present invention relates to an acyclic nucleoside phosphonate derivative represented by the following formula (1):
in which represents single bond or double bond, R 1 , R 2 , R 3 , R 7 ...
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7579332 |
Nucleobase phosphonate analogs for antiviral treatment
The invention provides compounds with activity against infectious diseases. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication, of the...
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7544672 |
Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs as HSP90-inhibitors
Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of...
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7511051 |
Cidofovir peptide conjugates as prodrugs
Cidofovir-based compounds having an amino acid, dipeptide or tripeptide attached to a cidofovir or cyclic cidofovir framework. The compounds show enhanced oral bioavailability and increased binding...
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7435739 |
Substituted pyrrolopyrimidines useful in the treatment of cancer
The invention relates to compounds of the formula 1
or a pharmaceutically acceptable salt, prodrug or hydrates thereof, wherein X, L, R 1 , R 2 , R 3 and R 4 are as defined herein. The...
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7407965 |
Phosphonate analogs for treating metabolic diseases
The invention is related to phosphorus substituted compounds with activity for treating metabolic diseases and/or disorders, e.g., diabetes and hypercholesterolemia, compositions containing such...
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7407946 |
Quinazoline compounds
Quinazoline derivatives of formula (I) wherein A is 5-membered heteroaryl containing a sulphur atom and optionally containing one or more nitrogen atoms; compositions containing them, processes for...
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7312329 |
Process for the preparation of pyrimidine derivatives
An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula
wherein R is an alkyl of from 1 to 10 carbon atoms,...
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7259154 |
Pyrrolopyrimidines
Compounds of the formula
and N-oxides, prodrugs, acid bioisosteres, pharmaceutically acceptable salts or solvates of such compounds, or N-oxides, prodrugs, or acid bioisosteres of such salts or...
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7205404 |
Phosphorus-containing prodrugs
Novel cyclic phosphoramidate prodrugs of drugs of formula I
in their use in delivery of drugs to the liver, their use in enhancing oral bioavailability, and their method of preparation are...
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7176310 |
Pyrimidinecarboxamide derivatives and their use as anti-inflammatory agents
This invention is directed to compound of the following formula (I):
wherein R 1 , R 2 , R 3 and R 4 are as described herein. These compounds and pharmaceutical compositions containing the...
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7164014 |
Protected linker compounds
The invention features linker molecules that have at one terminus a amino-protecting group and at the other terminus a phosphorous activating group, typically phosphoramidite. The linker molecules...
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7157448 |
Acyclic nucleoside phosphonate derivatives, salts thereof and process for the preparation of the same
The present invention relates to a nucleoside phosphonate derivative represented by formula (1):
pharmaceutically acceptable salts, and stereoisomers. This nucleoside phosphonate derivative is...
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7144866 |
Avermectin derivatives
Provided is a compound represented by the general formula (I) or a salt thereof:
wherein, —X Y— represents —CH═CH— and the like, between R 2 and the carbon atom at 5-position...
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7129227 |
Lipid analogs for treating viral infections
A method of treating viral infections, and in particular HIV-1, hepatitis B virus, and herpesviruses, is disclosed. The method comprises administering to a subject in need of such treatment an...
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7115738 |
Hydroxyproline/phosphono oligonucleotide analogues, methods of synthesis and methods of use
Compounds are described and claimed comprising general formula:
The compounds have substituents as described herein and are useful, e.g., for their ability to bind nucleic acids and thereby...
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7115592 |
Phosphonate substituted pyrimidine compounds and methods for therapy
Novel compounds are provided having formula (I)
where
R 1 , R 2 , R 3 , R 4 , Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the...
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7098341 |
Process for preparing haptens for immunoassay of phosphorothioate pesticides
The present invention relates to a process for preparing haptens for immunoassay of phosphorothioate pesticides, which comprises the steps of reacting O-methyl(ethyl) dichlorothiophosphate with a...
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7071176 |
Aryl phosphate derivatives of AZT 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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7060290 |
Phosphocholine linked prodrug derivatives
Disclosed are compounds of general formula (I) that function as prodrugs, thereby increasing bioavailabilities of the linked therapeutic agents, wherein the LINKER is (i) substituted or...
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7030230 |
Process of purifying phosphoramidites
A process of purifying phosphoramidite precursors useful in inter alia synthesis of oligonucleotides comprises dissolving a crude phosphoramidite in a polar phase, adding a basic compound to the...
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7030103 |
Sulfonamidomethyl phosphonate inhibitors of β-lactamase
The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel β-lactamase...
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7018989 |
Chemical compounds
Aryl substituted phosphoryl derivatives of the formula
In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X 1 is O, NR 3 , S, CR 3 R 4 , CR 3 W 1 or CW 1 W 2 , X 2 and X 6 are a bond...
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6936602 |
Benzazepine derivatives, process for the preparation of the same and uses thereof
Compounds of the general formula (I):
or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R 1 is a 5- to 6-membered...
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6919322 |
Phenyl Phosphonate Fructose-1,6-Bisphosphatase Inhibitors
Novel FBPase inhibitors of the formula I
are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
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6914052 |
Selective anti-viral nucleoside chain terminators
The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity...
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6908924 |
N4-acylcytosine-1,3-dioxolane nucleosides for treatment of viral infections
The present invention is directed to a compound, method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV)...
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6878697 |
Phenylamino-pyrimidines and uses thereof
This invention relates to compounds of the general formula:
in which R A , R B , R C , R D , w, x, y, and z are as defined herein, and to their preparation and use.
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6872711 |
β-substituted β-aminoethyl phosphonate derivatives
The present invention relates to novel β-substituted-β-aminoethylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low...
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6858393 |
Chain terminators for DNA synthesis
The invention relates to acyclic chain terminator nucleotide analogs. More particularly, the invention relates to phosphonomethoxyethyl nucleotide analogs and detectably labeled versions thereof,...
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6844437 |
Process for the production of tert-butyl (E)-(6-[2-[4-(4-flurophenyl)-6-isopropyl-2-[methyl(methylsufonyl)amino]pyrimidin-5-yl]vinyl]4R,6S)-2,2-dimethyl[1,3]dioxan-4-yl)acetate
The invention concerns a process for the manufacture of tert-butyl...
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6833364 |
Substituted pyrazole derivatives
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R 1 , R 2 , R 3 , A, X and Y are each as defined, and to processes...
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6818633 |
Antiviral compounds and methods for synthesis and therapy
Novel compounds are provided having formula (I) where R 1 , R 2 , R 3 , R 4 , Z, X and * are defined herein. Also provided are antiviral methods for use and processes for synthesis of the...
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6812231 |
Benzamidine derivative
Benzamidine derivatives of the following formula, analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an effect of inhibiting activated...
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6787525 |
Glyceryl nucleotides, method for the production thereof and their use
The invention relates to glyceryl nucleotides of the formula Ia in which a) one of the radicals A 1 , A 2 and A 3 is a hydrogen atom or a radical selected from hydroxyl, mercapto, alkyl,...
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6774121 |
Phospholipid prodrugs of anti-proliferative drugs
The invention discloses prodrugs comprising anti-proliferative drugs covalently linked, via bridging group, to a phospholipid moiety such that the active species is preferentially released,...
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6750340 |
Bisphosphonate conjugates and methods of making and using the same
The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and...
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6743798 |
Substituted pyrazole derivatives condensed with six-membered heterocyclic rings
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R 1 , R 2 , R 3 and A are each as defined, and to processes for their preparation and...
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6723711 |
Propanoic acid derivatives that inhibit the binding of integrins to their receptors
A compound of the structure A method for the inhibition of the binding of α 4 β 1 integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin;...
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6706698 |
α-Substituted β-aminoethyl phosphonate derivatives
The present invention relates to novel α-substituted-β-aminoethylphosphonate and α-substituted-β-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a),...
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6653296 |
Antiretroviral enantiomeric nucleotide analogs
Resolved enantiomers of the formula (IA) and (IB) wherein B is a purine or pyrimidine base or aza and/or deaza analogs thereof are useful in antiviral pharmaceutical compositions to treat...
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RE38333 |
Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure —OC(R 2 ) 2 OC(O)X(R) a , wherein R 2 ...
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6649622 |
Tetrahydropyrimidone inhibitors of fatty acid binding protein and method
aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II...
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6620796 |
Combinatorial library synthesis and pharmaceutically active compounds produced thereby
The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications,...
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6596865 |
Method of purifying thiamine phosphates
The invention relates to a method for removing phosphoric acid, thiamine triphosphate and higher thiamine phosphates from solutions that contain phosphoric acid, thiamine monophosphate, thiamine...
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6576760 |
Processes for synthesis of cyclic and linear polyamine chelators containing N-monosubstituted coordinating arms
Polyamines containing at least two nitrogen atoms monosubstituted with pendant arms capable of coordinating metal cations, or with precursors of such pendant arms, all nitrogen atoms of the...
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6531581 |
Purines and pyrimidines linked to a quencher
Compounds are described comprising purines substituted at the C-8 position and pyrimidines substituted at the C-4 position with a linker and quencher. These compounds, when incorporated into...
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6500811 |
Sulfonylaminophosphinic and sulfonylaminophosphonic acid derivatives, methods for their preparation and use
Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading...
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6498151 |
Aryldifluoromethylphosphonic acids with sulfur-containing substituents as PTP-1B inhibitors
The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and...
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