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| Number | Title | Issue Date |
| 8097722 | Inhibitors of polyisoprenylated methylated protein methyl esterase Inhibitors of the enzyme prenylated methylated protein methyl esterase (PMPMEase), the last step in the prenylation process for many eukaryotic proteins, having the general structure R1-X-A-B(R2)-Y or R1-X-A(R2)-B-Y, where... | 01/17/2012 |
| 8063209 | Phosphonyl ester conjugates as prodrugs Cidofovir or foscarnet based compounds having an amino acid or dipeptide esters are provided as prodrugs. ... | 11/22/2011 |
| 7674900 | Chiral tertiary aminoalkylnaphthols The present invention provides bipyrimidinyl diphosphine compounds of the formula wherein R is optionally substituted alkyl, cycloalkyl, aryl or heteroaryl; R′ and R″ ... | 03/09/2010 |
| 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, R1, R2, R3 and R4 are as defined herein. The ... | 10/14/2008 |
| 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 their preparation and their use in therapy. | 08/05/2008 |
| 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 compounds, and therapeutic methods that include the administration of s... | 08/05/2008 |
| 7321828 | System of components for preparing oligonucleotides Interative, preferably computer based iterative processes for generating synthetic compounds with desired physical, chemical and/or bioactive properties, i.e., active compounds, are provided. During iterations of the processes, a target nucleic acid sequence is prov... | 01/22/2008 |
| 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, aryl or arylalkyl, R | 12/25/2007 |
| 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 solvates, to compo... | 08/21/2007 |
| 7214701 | Active substance combinations having insecticidal and acaricdal properties The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising (a) compounds of the formula (I) ... | 05/08/2007 |
| 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 described. ... | 04/17/2007 |
| 7176310 | Pyrimidinecarboxamide derivatives and their use as anti-inflammatory agents This invention is directed to compound of the following formula (I): wherein R1, R2, R3 and R4 are as described herein. These compounds and pharmaceutical compositions ... | 02/13/2007 |
| 7169916 | Chloral-free DCA in oligonucleotide synthesis A process of manufacturing oligonucleotides includes a 5′-deblocking step in which the 5-blocking group is removed with dichloroacetic acid that is essentially free of chloral. The process is useful for making oligonucleotides that are substantially free of chlora... | 01/30/2007 |
| 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 can be used, for example, to produce amino-modified linkers that spac... | 01/16/2007 |
| 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 useful as an antivi... | 01/02/2007 |
| 7144866 | Avermectin derivatives Provided is a compound represented by the general formula (I) or a salt thereof: wherein, —XY— represents —CH═CH— and the like, between R2 and the carbon atom at 5-posi... | 12/05/2006 |
| 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 infection-combating amount of a phospholipid or phospholipid derivative. | 10/31/2006 |
| 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 effect purifications, ... | 10/03/2006 |
| 7115592 | Phosphonate substituted pyrimidine compounds and methods for therapy Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods for use and processes f... | 10/03/2006 |
| 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, these derivatives are potent inhibitors of HIV reverse transcriptase.... | 07/04/2006 |
| 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 unsubstituted alkyl, (ii) substituted or unsubstituted alkenyl, (iii) substitute... | 06/13/2006 |
| 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 inhibitors, which are structurally unrelated to the natural product and... | 04/18/2006 |
| 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 polar phase, adding a portion of water to the polar phase, contacting t... | 04/18/2006 |
| 7018989 | Chemical compounds Aryl substituted phosphoryl derivatives of the formula In which Ar is phenyl, naphthyl, or pyridyl, Y is O or S, X1 is O, NR3, S, CR3R4, CR3W1 or CW... | 03/28/2006 |
| 7002006 | Protection of nucleosides A process of manufacturing protected nucleosides comprises reacting a nucleoside with a protecting reagent in the presence of a regioselective activator to produce a regioselectively protected nucleoside. In some embodiments of the inventive method, an optionally su... | 02/21/2006 |
| 7001903 | Synergistic insecticidal mixtures The invention relates to insecticidal mixtures of spinosyns and agonists or antagonists of nicotinic acetylcholine receptors for protecting plants against attack by pests. ... | 02/21/2006 |
| 6967079 | Pyrimidine derivatives for labeled binding partners Compounds having particular interest as labels and various novel uses in diagnostics and therapeutics are provided which have structure (1) wherein R1 is a binding partner, a linker or H; | 11/22/2005 |
| 6964968 | Method for the treatment or prevention of viral infection using nucleoside analogues Viral infections selected from the group consisting of herpes simplex virus, varicella zoster virus, respiratory syncytial virus and cytomegalovirus can be treated by administering to the host a therapeutically effective amount of a compound of formula I or a pharma... | 11/15/2005 |
| 6958214 | Polymorphic kinase anchor proteins and nucleic acids encoding the same Polymorphic A-kinase anchor proteins (AKAPs) and nucleic acids encoding the proteins are provided herein. Methods of detecting polymorphic AKAPs and nucleic acids encoding the AKAPs, and kits for use in the detection methods are also provided. Further provided herei... | 10/25/2005 |
| 6943173 | 5-substituted 2-aryl-4-pyrimidinones Arylpyrimidinone compounds that act as selective modulators of CRF 1 receptors are provided. These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating diso... | 09/13/2005 |
| 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 R1 is a 5- to 6-membered aromatic ring which... | 08/30/2005 |
| 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. ... | 07/19/2005 |
| 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 toward the host cells. In particular, the compounds according to the pres... | 07/05/2005 |
| 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) infections, in human patients or other animal hosts, comprising the admi... | 06/21/2005 |
| 6878697 | Phenylamino-pyrimidines and uses thereof This invention relates to compounds of the general formula: in which RA, RB, RC, RD, w, x, y, and z are as defined herein, and to their preparation a... | 04/12/2005 |
| 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 density lipoproteins and very low density lipoproteins) and for lowering... | 03/29/2005 |
| 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, especially fluorescently labeled versions thereof. The invention furth... | 02/22/2005 |
| 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 (E)-(6-[2-4-(4-flourophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]vinyl)-(4R,6S)-2,2-dimethyl[1,3]-dioxan-4-yl)acetate, the novel starting material used in said process and the u... | 01/18/2005 |
| 6833364 | Substituted pyrazole derivatives The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R1, R2, R3, A, X and Y are each as defined, and to processes... | 12/21/2004 |
| 6818633 | Antiviral compounds and methods for synthesis and therapy Novel compounds are provided having formula (I) where R1, R2, R3, R4, Z, X and * are defined herein. Also provided are antiviral methods fo... | 11/16/2004 |
