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| Number | Title | Issue Date |
| 7825238 | Antiviral methods employing double esters of 2′, 3′-dideoxy-3′-fluoroguanosine A method for treatment of HBV and HIV infections comprising administering the compound or salt of formula Ig ... | 11/02/2010 |
| 6713623 | Tetraphosphonate bicyclic trisanhydrides Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates. ... | 03/30/2004 |
| 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 |
| 6531589 | Base protecting groups and synthons for oligonucleotide synthesis The invention provides new methods for synthesizing oligonucleotides that allow for deprotection of the oligonucleotides under more mild conditions than existing methods. The invention further provides a nucleoside base protecting group that is stable und... | 03/11/2003 |
| 6399589 | 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 w... | 06/04/2002 |
| 6329519 | Intermediates for oligonucleotide synthesis A compound of formula (I) wherein B1 is a radical of a nucleoside base, R1 is hydrogen or a hydroxy-protecting group, R2 is hydrogen, hydroxy or a 2'-nucleoside-modifying atom or group, R3 is an unsubstituted or... | 12/11/2001 |
| 6326490 | Tetraphosphonate bicyclic trisanhydrides Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biolologically active compounds, and the compounds which may be synthesized from such intermediates.... | 12/04/2001 |
| 6232465 | Compositions for enzyme catalyzed template-independent creation of phosphodiester bonds using protected nucleotides A method for the stepwise creation of phosphodiester bonds between desired nucleosides resulting in the synthesis of polynucleotides having a predetermined nucleotide sequence by preparing an initiation substrate containing a free and unmodified 3'-hydrox... | 05/15/2001 |
| 6147205 | Photocleavable protecting groups and methods for their use Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be remo... | 11/14/2000 |
| 6140310 | Phosphorous prodrugs The composition and methods of synthesis of phosphorus prodrugs are described. These methods can be used to convert negatively charged phosphorus bearing drugs into neutrally charged; lipid soluble prodrugs which are able to passively diffuse into cells a... | 10/31/2000 |
| 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 |
| 6124445 | Phosphotriester oligonucleotides, amidities and method of preparation Oligonucleotides having bioreversible phosphate blocking groups can be used as pro drugs for the oligonucleotides. The bio-reversible blocking groups can be removed by intercellular enzymes, particularly carboxyesterases, to provide the unprotected oligon... | 09/26/2000 |
| 6111086 | Orthoester protecting groups Novel orthoesters are provided which can be used as a 2'-hydroxyl protecting groups or 2'-modification in the synthesis of polymers containing ribonucleic acid (RNA) nucleotides. The RNA comprising the orthoester can be handled and analyzed while 2'-modif... | 08/29/2000 |
| 6048975 | Process for the chemical synthesis of oligonucleotides A process for the chemical synthesis of oligonucleotides Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes. The ease of detection of the dansyl protective g... | 04/11/2000 |
| 6020482 | Phosphotriester type biologically active compounds Phosphotriester compound of general formula (I); ##STR1## wherein R is a radical --(CH2)n --S--X in which X is a radical (a) or --S--U, Z being O or S, and Y and U denote an alkyl, aryl or osidic radical, optionally substituted ... | 02/01/2000 |
| 5990303 | Synthesis of 7-deaza-2'deoxyguanosine nucleotides The present invention provides 7-deaza-2'-deoxy-guanosine nucleotides of the general formula: ##STR1## wherein R is a --PO3 H2, --P2 O6 H3 or --P3 O9 H4 residue o... | 11/23/1999 |
| 5955591 | Phosphotriester oligonucleotides, amidites and method of preparation Oligonucleotides having bioreversible phosphate blocking groups can be used as pro drugs for the oligonucleotides. The bio-reversible blocking groups can be removed by intercellular enzymes, particularly carboxyesterases, to provide the unprotected oligon... | 09/21/1999 |
| 5871947 | Method for the determination of low concentrations of heavy metals The present invention provides a highly effective method for determining very low concentrations of heavy metals such as lead, cadminum, mercury, and copper in body fluids. Ratios of d-5'-N/Pyr-5'-N activities which display greater deviation and stronger ... | 02/16/1999 |
| 5849905 | Biologically active phosphotriester-type nucleosides and methods for preparing same 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 w... | 12/15/1998 |
| 5808035 | Protected nucleoside and method for its synthesis The present invention relates to a nucleoside having the formula: ##STR1## where R1 is a hydrogen or a protecting group; R2 is a hydrogen or a coupling group; R3 and R4 are each either a hydrogen or an alkyl group, w... | 09/15/1998 |
| 5808045 | Compositions for enzyme catalyzed template-independent creation of phosphodiester bonds using protected nucleotides A method for the stepwise creation of phosphodiester bonds between desired nucleosides resulting in the synthesis of polynucleotides having a predetermined nucleotide sequence by preparing an initiation substrate containing a free and unmodified 3'-hydrox... | 09/15/1998 |
| 5780617 | Synthesis of liponucleotides A process for the preparation of glycerol di- or triphosphate derivatives comprising coupling the phosphate group of a glycerol monophosphate derivative in which one of the phosphate hydroxyls is replaced by a leaving group, with the terminal phosphate gr... | 07/14/1998 |
| 5770725 | Phosphotriester type biologically active compounds Compounds of formula RO--P(.dbd.O)(OR)--Nu where: each R is, independently, --(CH2)n --S--X; X is --C(.dbd.Z) (Y) or --S--U; Z is O or S; Y and U are alkyl, aryl or saccharide groups optionally substituted with OH, SH or NH groups; n... | 06/23/1998 |
| 5750674 | Methods and compounds for the stereoselective enrichment of oligonucleotide diastereomers and oligonucleotides thereby produced The present invention provides new mononucleotide synthons useful in the synthesis of oligonucleotides having from one to all P-chiral centers that are predominantly and independently in the R or S configuration. The invention also provides methods of syn... | 05/12/1998 |
| 5734042 | Process for the production of asymmetrical phosphoric acid diesters The present invention concerns a process for the production of asymmetrical phosphoric acid diesters. The process is characterized in that a phosphoric acid ester is condensed with a compound containing hydroxy groups in the presence of an arylsulfonic ac... | 03/31/1998 |
| 5693521 | Membrane-permeant second messengers Acyloxyalkyl esters of phosphate-containing second messengers which are capable of permeating cell membranes. Once inside the cell, the ester derivatives undergo enzymatic conversion to the biologically active form of the second messenger. Acyloxyalkyl es... | 12/02/1997 |
| 5681702 | Reduction of nonspecific hybridization by using novel base-pairing schemes Methods are provided for substantially reducing background signals encountered in nucleic acid hybridization assays. The method is premised on the elimination or significant reduction of the phenomenon of nonspecific hybridization, so as to provide a dete... | 10/28/1997 |
| 5646265 | Process for the preparation of 2'-O-alkyl purine phosphoramidites 2'-O-alkylated guanosine, uridine, cytidine, and 2,6-diaminopurine 3'-O-phosphoramidites are prepared by alkylating nucleoside precursors, adding suitable blocking groups and phosphitylating. Alkylation is effected on 2,6-diamino-9-(ଲ-D-ribofuranosy... | 07/08/1997 |
| 5646269 | Method for oligonucleotide analog synthesis The present invention is directed to improved methods to synthesize oligonucleotide analogs having an acetal linkage, such as a 3',5'-formacetal (3' --O--CH2 --O-- 5'), 3',5'-thioformacetal (3' --S--CH2 --O-- 5') or an analogous 2',5... | 07/08/1997 |
| 5639867 | TTTr as protective group in nucleotide synthesis The invention relates to nucleosides, nucleotides and oligonucleotides carrying in their basic structure a primary hydroxyl group protected by tris-4,4',4"-tert-butylphenylmethyl, to processes for the preparation of said nucleosides and nucleotides, to a ... | 06/17/1997 |
| 5627165 | Phosphorous prodrugs and therapeutic delivery systems using same The composition and methods of synthesis of phosphorus prodrugs are described. These methods can be used to convert negatively charged phosphorous bearing drugs into neutrally charged; lipid soluble prodrugs which are able to passively diffuse into cells ... | 05/06/1997 |
| 5623069 | Method for producing 5'-nucleotide A method of producing 5'-nucleotide, which comprises maintaining a nucleoside suspension in an organic solvent at a temperature not lower than about 20° C., and then subjecting the resultant suspension to a phosphorylatipon of the nucleoside(s). Accordin... | 04/22/1997 |
| 5621086 | Sialic acid derivative and method of manufacturing it The present invention is drawn to methods of manufacturing a sialic acid derivative suitable for industrial production. With a method of the present invention, Tetra-O-acetylsialic acid (4a) and acetylcytidine-5'-O-amidite (5a) are condensed in the presen... | 04/15/1997 |
| 5506351 | Process for the preparation of 2'-O-alkyl guanosine and related compounds An improved process for preparing 2'-O-substituted guanosine comprising reacting an unprotected 2,6-diaminopurine riboside with an alkyl halide in the presence of a sodium hydride or a base of equal strength followed by a deamination step with adenosine d... | 04/09/1996 |
| 5449664 | Antiviral agents Nucleoside compounds of the formula ##STR1## wherein: B is a purine or a pyrimidine; X and X' are H, OH or F, provided that at least one is H; Y and Y' are H, OH, OCH3 or F, provided that at least one is H; Y' and Z together form a cyclic phosphate ... | 09/12/1995 |
| 5420265 | Separation of phosphorothioate oligonucleotides by capillary gel electrophoresis A method for separating a mixture of 5'-phosphorothioate mononucleotides, a mixture of 5'-phosphorothioate oligonucleotides, or a mixture of both 5'-phosphorothioate mononucleotides and 5'-phosphorothioate oligonucleotides comprising electro- phoresis thr... | 05/30/1995 |
| 5218103 | Nucleoside thiophosphoramidites The present invention relates to new and useful nucleside thiophosphoramidite, polynucleotide dithioate phosphoramidite and polynucleotide phosphorothioamidate phosphoramidite compounds as well as the process whereby these compounds can be used for synthe... | 06/08/1993 |
| 5218102 | Nucleic acid probe containing a terminal carbamyl linking non-radioactive labeling and preparating processes The subject of the present invention is a nucleic acid probe containing a nucleic acid sequence, wherein the said sequence is linked at its 5' end, via a divalent bifunctional chemical "arm" L, to a "labeling component" M, M being a synthetic or natural m... | 06/08/1993 |
| 5194599 | Hydrogen phosphonodithioate compositions Novel hydrogen-phosphonodithioate compositions are provided which are particularly useful for forming internucleotide and internucleoside linkages in oligonucleosides or oligonucleotides. The oligonucleotides and analogs thereof made by using the hydrogen... | 03/16/1993 |
| 5043437 | 5'phosphonates of 3'-azido-2',3'dideoxynucleosides The compounds of the invention are 5'-phosphonates of 3'-azido-2',3'-dideoxynucleosides having the following general formula: ##STR1## where B is thymin-1-yl, cytosin-1-yl, adenin-9-yl, or guanin-9-yl. The compounds according to the present invention... | 08/27/1991 |
