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| Number | Title | Issue Date |
| 7378402 | Anti-viral nucleosides 4-Amino-1-((2R,3S,4S,5R)-5-azido-3,4-dihydroxy-5-hydroxymethyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (I:R1=R2=R3=R4=H) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions an... | 05/27/2008 |
| 7365188 | Process for producing N-Acyl-5′-deoxy-5-fluorocytidine The present invention provides a process for producing a N4-acyl-5′-deoxy-5-fluorocytidine compound of the formula: where R2 is alkyl, cycloalkyl, aralkyl, aryl, or alkoxy. ... | 04/29/2008 |
| 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 |
| 7276228 | Methods for treating hematological disorders through inhibition of DNA methylation and histone deacetylase Methods are provided for treating hematological disorders by inhibition of DNA hypomethylation and histone deacetylase. Such disorders include, for example, acute promyelocytic leukemia, acute lymphoblastic leukemia, chronic myelogenous leukemia, myelodysplastic syn... | 10/02/2007 |
| 6936709 | Method for purifying protected 2′-deoxycytidines and hydrated crystals thereof A protected 2′-deoxycytidine is purified by precipitating the protected 2′-deoxycytidine represented by general formula (3) in the form of a hydrated crystal from a solution containing the protected 2′-deoxycytidine and water, and by recovering the protected 2... | 08/30/2005 |
| 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 |
| 6908906 | Crystalline forms of pyrimidine nucleoside derivative The present invention provides crystalline forms and compositions thereof, of a pyrimidine nucleoside derivative of formula (I) having anti-tumour activity, wherein formula (I) is: ... | 06/21/2005 |
| 6905669 | Compositions and methods for reestablishing gene transcription through inhibition of DNA methylation and histone deacetylase Compositions and methods are provided for treating diseases associated with aberrant silencing of gene expression such as cancer by reestablishing the gene expression through inhibition of DNA hypomethylation and histone deacetylase. The method comprises: administer... | 06/14/2005 |
| 6894159 | Process for the preparation of 2′-fluoro-5-methyl-beta-L-arabino-furanosyluridine The present invention relates to a novel and improved process for preparing 2′-fluoro-5-methyl-β-L-arabinofuranosyluridine represented by formula (1) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus and Epstein-Barr... | 05/17/2005 |
| 6870048 | Process for the preparation of 2'-halo-β-L-arabinofuranosyl nucleosides The present invention is directed to the process for the preparation of 2′-deoxy-2′-halo-β-L-arabinofuranosyl nucleosides, and in particular, 2′-deoxy-2′-fluoro-β-L-arabinofuranosyl thymine (L-FMAU), from L-arabinose, which is commercially available and le... | 03/22/2005 |
| 6864244 | Anhydrous crystalline 1-[4(S)-azido-2(S),3(R)-dihydroxy-4-(hydroxymethyl)-1(R)-cyclopentyl]cytosine hemisulfate as useful as an antiviral agent The present invention relates to the hemisulfate salt of 1-[4(S)-azido-2(S),3(R)-dihydroxy-4-(hydroxymethyl)-1(R)-cyclopentyl]cytosine (Ia) with improved stability and physical properties which facilitate manufacturing, handling and formulating I and polymorphic cry... | 03/08/2005 |
| 6846810 | Antiviral nucleoside derivatives The present invention relates to nucleoside derivatives for the treatment of Hepatitis C viral infections including compounds of formula I, pharmaceutical compositions comprising these compounds and methods for treatment or prophylaxis of Hepatitis C Virus mediated ... | 01/25/2005 |
| 6617437 | 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) ##STR1## wherein R1 is a binding partner, a linker or H; a and b are 0 or 1, provided that the total ... | 09/09/2003 |
| 6579976 | Process for producing 2',3'-diethyl substituted nucleoside derivatives There can be provided an excellent industrial process for producing compounds having sugar-moiety hydroxyl groups or halogen atoms reduced in nucleic acids or in derivatives thereof by allowing O-thiocarbonyl derivatives of sugar-moiety hydroxyl groups or... | 06/17/2003 |
| 6566344 | ଲ-L-2'-deoxy-nucleosides for the treatment of hepatitis B This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2'-deoxy-ଲ-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or ... | 05/20/2003 |
| 6512107 | Process for the preparation of 2'-fluoro-5-methyl-ଲ-L-arabinofuranosyluridine The present invention relates to a novel and improved process for preparing 2'-fluoro-5-methyl-ଲ-L-arabinofuranosyluridine represented by formula (I) which shows anti-viral activity, especially potent anti-viral activity against hepatitis B-virus an... | 01/28/2003 |
| 6403568 | 4'-C-ethynyl pyrimidine nucleosides and pharmaceutical compositions thereof The invention provides 4'-C-ethynyl pyrimidine nucleosides (other than 4'-C-ethynylthymidine) represented by formula [I]: ##STR1## wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydroge... | 06/11/2002 |
| 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 |
| 6291670 | 4'-C-ethynyl pyrimidine nucleoside compounds and pharmaceutical compositions The invention provides 4'-C-ethynyl pyrimidine nucleosides (other than 4'-C-ethynylthymidine) represented by formula [I]: ##STR1## wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydroge... | 09/18/2001 |
| 6211166 | 5'-deoxy-cytidine derivative administration to treat solid tumors Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1## wherein R1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R2 is a hydrogen atom, or --CO--OR4 group [wh... | 04/03/2001 |
| 6187914 | Nucleoside derivatives, and their use in oligonucleotide synthesis The invention relates to nucleoside derivatives bearing electrolabile protector groupings and their use in an oligonucleotide synthesis method comprising at least one step of electronic deprotection.... | 02/13/2001 |
| 6133438 | Process for the preparation of 2'-O-alkyl purine phosphoramidites Processes for preparing 2'-O-alkylated guanosine, uridine, cytidine, and 2,6-diaminopurine 3'-O-phosphoramidites include the steps of alkylating nucleoside precursors, adding suitable blocking groups and phosphitylating. For the guanosine 2'-O-alkylated 3... | 10/17/2000 |
| 6114520 | 5'-deoxy-cytidine derivatives Novel 5'-deoxy-cytidine derivatives represented by the general formula (I) ##STR1## wherein R1 is a hydrogen atom or a group easily hydrolyzable under physiological conditions; R2 is a hydrogen atom, or --CO--OR4 grou... | 09/05/2000 |
| 6060592 | Pyrimidine nucleoside compounds and oligonucleoside compounds containing same Novel 2- and 4-substituted pyrimidine nucleosides and oligonucleosides are provided, as are methods and intermediates useful in preparing same. In preferred embodiments, one of the 2- and 4-substituents is .dbd.O, .dbd.NH, or .dbd.NH2+ | 05/09/2000 |
| 6020483 | 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 ... | 02/01/2000 |
| 6005098 | 5'deoxycytidine derivatives Compounds of the formula (I) ##STR1## wherein R1 is each independently hydrogen or a group easily hydrolyzable under physiological conditions; R2 is --(CH2)n -cycloalkyl wherein cycloalkyl contains 3 to 5 c... | 12/21/1999 |
| 5977325 | 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease stat... | 11/02/1999 |
| 5968910 | Compositions containing two or three inhibitors of different HIV reverse transcriptases A composition and method for the prevention or treatment of HIV-1 infection comprising an HIV-1 reverse transcriptase-inhibiting heterocyclyl carb(ox/thio)anilide compound, a second HIV-1 reverse transcriptase inhibitor compound which does not select for ... | 10/19/1999 |
| 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 one or more of the carbon atoms in the purine or pyrimidin... | 09/28/1999 |
| 5945527 | Palladium catalyzed nucleoside modification methods using nucleophiles and carbon monoxide This invention discloses a method for the preparation modified nucleosides and nucleotides using a palladium catalyst, a nucleophile and carbon monoxide.... | 08/31/1999 |
| 5859234 | 2'-O-methyl cytidine monomer useful in oligonucleotide synthesis Methods of preparing N4 -alkanoyl, aroyl and aralkanoyl 2'-O-methylcytidine derivatives are provided. Also provided are cytidine derivatives and nucleoside monomers comprising these cytidine derivatives which are useful in the synthesis of Olig... | 01/12/1999 |
| 5852027 | Antiviral 1,3-dioxolane nucleoside analogues This invention includes the compounds 2'-deoxy-5-fluoro-3'-oxacytidine, (-)-2'-deoxy-5-fluoro-3'-oxacytidine, and (+)-2'-deoxy-5-fluoro-3+-oxacytidine, and pharmaceutically acceptable salts thereof for use in medical therapy, for example for the treatment... | 12/22/1998 |
| 5808047 | Process for the preparation of 2,2'-anhydro- and 2'-keto-1-(3',5'-di-O-protected-ଲ-D-arabinofuranosyl) nucleosides A process for the preparation of compounds of the formula: ##STR1## wherein Pg and R are protecting groups and B is a nucleobase. The process uses protected nucleobases to form 2,2'-anhydro nucleosides having the formula ##STR2## which are ... | 09/15/1998 |
| 5798340 | Nucleotide analogs Nucleotide analogs characterized by the presence of an amidate lirked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is h... | 08/25/1998 |
| 5792841 | 2'-halomethylidene, 2'-ethenylidene and 2'-ethynl cytidine, uridine and guanosine derivatives This invention relates to certain novel 2'-halomethylidene, 2'-ethenylidene and 2'-ethynyl cytidine, uridine and guanosine derivatives, and compositions thereof, which are useful in the treatment of patients afflicted with neoplastic or viral disease stat... | 08/11/1998 |
| 5763418 | 3'-substituted nucleoside derivatives The invention relates to a 3'-substituted nucleoside derivative represented by the following general formula (1): ##STR1## wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may... | 06/09/1998 |
| 5756707 | Method of making 2'-O-alkyl pyrimidine ribonucleosides Method for production of 2'-O-derivatized uridine and cytosine RNA synthons comprising derivatizing the 2'-hydroxyl group of a partially protected cytosine ribonucleoside to preferentially produce a partially protected 2'-O-derivatized nucleoside, which i... | 05/26/1998 |
| 5726301 | CAC H-phosphonate and its use in the synthesis of oligonucleotides Disclosed herein are N4 protected deoxycytidines for use in the synthesis of oligonucleotides, the protecting groups being represented by the formula: --CO--(CH2)0-9 --CH3. Preferred embodiments are N4 | 03/10/1998 |
| 5719273 | Palladium catalyzed nucleoside modifications methods using nucleophiles and carbon monoxide This invention discloses a method for the preparation modified nucleosides using a palladium catalyst, a nucleophile and carbon monoxide.... | 02/17/1998 |
