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| Number | Title | Issue Date |
| 8026356 | Process for the large scale production of Stavudine The present invention provides a method for preparing pure Stavudine having purity more than 99.5% comprises: i) Converting 3′,5′-anhydrothymidine to crude Stavudine, ii) Converting crude Stavudine to stable solvates of Stavudine, iii) Desolvation of the solvate... | 09/27/2011 |
| 7759481 | Solid state forms of 5-azacytidine and processes for preparation thereof The present invention provides novel crystalline forms of 5-deazacytidine, and pharmaceutical compositions comprising these novel forms. The invention also provides methods for the preparation of the novel forms and compositions. ... | 07/20/2010 |
| 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 host, including animals, and especially humans, using a (2′R)-2′-deo... | 09/30/2008 |
| 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 |
| 7294619 | Lipid analogs for inhibiting the activity of hepatitis B antigen The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the ... | 11/13/2007 |
| 7294620 | Lipid analogs for inhibiting HIV-1 activity The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the ... | 11/13/2007 |
| 7294621 | Lipid analogs for combating tumors The invention relates to methods of treating viral infections, and in particular hepatitis B virus. The method comprises administering to a subject in need of such treatment an infection-controlling amount of a phospholipid or phospholipid derivative to inhibit the ... | 11/13/2007 |
| 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 treatment of Flaviviridae infections, including HCV infection, and o... | 03/20/2007 |
| 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 pharmaceutically acceptable salt or prodrug thereof, is provided.... | 01/30/2007 |
| 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 |
| 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 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug... | 01/16/2007 |
| 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. ... | 12/12/2006 |
| 7122528 | Use of 5-substituted nucleosides and/or prodrugs thereof in the resistance-free treatment of infectious diseases The present invention relates to the use of 5-substituted nucleosides and/or the prodrugs thereof together with at least one active substance in order to produce a drug or combination preparation for resistance-free therapy of infectious diseases caused by bacteria ... | 10/17/2006 |
| 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 is selected from bromo, ido, cyano, halo-substituted C1-4 ... | 10/10/2006 |
| 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 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug... | 09/05/2006 |
| 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 |
| 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 R2 is the residue of an aliphatic ... | 12/13/2005 |
| 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 antibacterial applications. Preferred embodiments of the instant invention ... | 11/01/2005 |
| 6930097 | Matrix metalloproteinase and tumor necrosis factor inhibitors A compound of formula 1-[3,4-dihydroxy-5-(2-hydroxyethyl)tetrahydrofuran-2-yl]pryimidine-2,4(1H,3H)-dione has inhibitory effects of matrix metalloproteinase-2 (gelatinase A) enzyme and binding of TNFα to TNFα-RI. ... | 08/16/2005 |
| 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 is also directed to the therapeutic or prophylactic use of such compou... | 08/02/2005 |
| 6914054 | 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 pharmaceutically acceptable salt or prodrug thereof, is provided.... | 07/05/2005 |
| 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 novel pyrimidines and purines that can be prepared according to the metho... | 01/25/2005 |
| 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 well as oligomers comprising the monomers disclosed herein linked by a ... | 01/11/2005 |
| 6822089 | Preparation of deoxynucleosides Methods for preparing deoxynucleosides from their corresponding ribonucleosides by forming 3-tert-butylphenoxythiocarbonylderivatives of the ribonucleosides and subsequently effecting radical deoxygenation reactions at the carbon atoms to be deoxygenated. ... | 11/23/2004 |
| 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 3′-modified nucleoside or a pharmaceutically acceptable salt or prodrug... | 11/02/2004 |
| 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 of a compound having the formula I or a pharmaceutically acceptable sa... | 08/31/2004 |
| 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 5-fluoro]-2',3'-dideoxy-2',3'-didehydro-pyrimidine nucleoside... | 01/20/2004 |
| 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, these derivatives are potent inhibitors of HIV reverse tra... | 12/30/2003 |
| 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 processes for producing Stavudine NN-dimethylacetamide solvates,... | 10/21/2003 |
| 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 70th codon (K to R, i.e., lysine to arginine) of the reverse transcriptase region of the virus. Based on this discovery, a method and... | 08/05/2003 |
| 6555676 | Biologically active phosphotriester-type compounds Compounds of formula RS--P(.dbd.O)(QR)--Nu where: R is a radical --(CH2)n--W--X; X is a radical --C(.dbd.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 saccharide radical which is optionally substituted wi... | 04/29/2003 |
| 6528495 | 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, these derivatives are potent inhibitors of HIV reverse tra... | 03/04/2003 |
| 6503890 | Aryl phosphate derivatives of d4T having anti-HIV activity Aryl phosphate nucleoside derivatives show potent activity against HIV without undesirable levels of cytotoxic activity. Examples of aryl phosphate nucleoside derivatives include aryl phosphate derivatives of d4T with para-bromo substitution on the aryl g... | 01/07/2003 |
| 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 sperm-immobilizing activity. In one example, the active ingredient conta... | 11/19/2002 |
| 6458772 | Prodrugs Compounds of the formula I ##STR1## or corresponding monohydroxynucleoside derivatives wherein: R1 is hydroxy, amino or carboxy: optionally having esterified/amide bonded thereon; a C4 -C22 saturated or unsaturated, optionally ... | 10/01/2002 |
| 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 comprising administering an effective amount of a ଲ... | 10/01/2002 |
| 6392032 | Heavily fluorinated sugar analogs Heavily fluorinated sugar analogs of formula ##STR1## wherein R1 is selected from alkyl, alkenyl, aryl, --CH2 --O-alkyl, --CH2 --O-aryl, --CH2 OPO3 H, --CH2 --O-carbohydrate, --CH2 | 05/21/2002 |
| 6384019 | Gemcitabine derivatives The invention provides Gemcitabine esters or amides in which the 3'- and/or 5'-OH group and/or the N4 -amino group is derivatised with a C18 - and/or C20 -saturated or mono-unsaturated acyl group, preferably an acyl group ... | 05/07/2002 |
| 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 is selected from bromo, iodo, cyano, halo-substituted C | 10/02/2001 |
| 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 combination with antimetabolite antineoplastic agents such as 5... | 07/31/2001 |
