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| Number | Title | Issue Date |
| 7781576 | Process for preparing a synthetic intermediate for preparation of branched nucleosides A process is provided for the preparation of a key intermediate in the preparation of 2′-branched nucleoside compounds. The process includes contacting a protected precursor 3,4-O-isopropylidene-2-C-substituted-D-arabinono-1,5-lactone with a... | 08/24/2010 |
| 7723512 | Oligonucleotides comprising a non-phosphate backbone linkage One aspect of the present invention relates to a ribonucleoside substituted with a phosphonamidite group at the 3′-position. In certain embodiments, the phosphonamidite is an alkyl phosphonamidite. Another aspect of the present invention relates to a double-strand... | 05/25/2010 |
| 7615628 | Imidazopyridine derivatives The present invention relates to a novel imidazo[4,5-b]pyridine derivative compound represented by Formula (I) and a pharmaceutically acceptable salt thereof. The present invention also relates to a method for preparing the above compound. The present invention furt... | 11/10/2009 |
| 7439351 | 2′ or 3′ -deoxy and 2′, 3′-dideoxy-β-L-pentofuranonucleo-side compounds, method of preparation and application in therapy, especially as anti-viral agents Method for the sterospecific preparation of 2′ or 3′ deoxy and 2′,3′-dideoxy-β-L-pentafuranonucleoside compounds. 2′ or 3′ deoxy and 2′,3′-dideoxy-β-L-pentofuranonucleoside compounds are also described. Finally, the invention concerns the use of th... | 10/21/2008 |
| 7432272 | Antiviral analogs The application relates to 4′-substituted nucleoside derivatives of Formula I: wherein B and R1 have any of the values described in the application, as well as to compositions comprising such compounds, to meth... | 10/07/2008 |
| 7405204 | Nucleoside compounds for treating viral infections Disclosed are compounds, compositions and methods for treating viral infections caused by a Flaviviridae family virus, such as hepatitis C virus. ... | 07/29/2008 |
| 7399754 | N-quinoline or isoquinoline substituted purine derivatives Novel compound having the following formula: wherein W represents a hydrogen, an optionally substituted C1-6 alkyl, an optionally substituted C3-6 cycloalkyl, or an optionally substituted C1-6 | 07/15/2008 |
| 7393954 | Process for the production of pentostatin aglycone and pentostatin A novel, scaleable and improved process for preparing pentostatin and its analogs is disclosed. The method comprises the diastereospecific synthesis of the nucleobase from commercially available L-Dialkyl tartarates. ... | 07/01/2008 |
| 7371737 | 2-substituted-6-trifluoromethyl purine derivatives with adenosine-Aantagonistic activity The present invention relates to 2-substituted-6-trifluoromethyl purine derivatives as selective adenosine antagonists, in particular adenosine-A3 receptor antagonists, to methods for the preparation of these compounds and to novel intermediates useful fo... | 05/13/2008 |
| 7321033 | 3-B-D-ribofuranosylthiazolo [4,5-] pyrimidine 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... | 01/22/2008 |
| 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 |
| 7294486 | Enzymatic process for the synthesis of organo-fluorine compounds There is described a process for the synthesis of a fluoronucleoside compound, said process comprising mixing a substrate and an enzyme from Streptomyces cattelya as catalyst. The process may be used to produce an 18F labelled fluoronucleoside comp... | 11/13/2007 |
| 7282581 | Oligonucleotide labeling reactants based on acyclonucleosides and conjugates derived thereof The invention relates to a labeling reactant of formula (I) useful for labeling an oligonucleotide wherein: R is a temporary protecting group. A is either a phosphorylating moiety or a solid support tethered to Z... | 10/16/2007 |
| 7268119 | Tricyclic nucleosides or nucleotides as therapeutic agents Nucleosides and nucleotides containing a tricyclic base portion thereof are useful for treating infectious diseases and proliferative disorders, such as viral infections or cancer respectively. ... | 09/11/2007 |
| 7244732 | Prodrugs of heteroaryl compounds The present invention provides hydrophobic prodrugs of bases, nucleosides, and nucleotides as well as methods of using the prodrugs as antiviral and anti-cancer chemotherapeutic agents. ... | 07/17/2007 |
| 7227019 | Process for the preparation of rebeccamycin and analogs thereof The present invention relates to a method for making an indolopyrrolocarbazole of the general formula [I], where the method includes the step of reacting a bisindolylmaleimide compound with an oxidizing agent in the presence of an oxygen containing gas at a temperat... | 06/05/2007 |
| 7217805 | Bicyclonucleoside analogues Bicyclonucleoside analogues which exhibit anti-AIDS activity and intermediates to produce oligonucleotide analogues which have anti-sense or anti-gene activity as well as in vivo stability. Compounds of the following formula (1) or their pharmaceutically acceptable ... | 05/15/2007 |
| 7217815 | 2-beta -modified-6-substituted adenosine analogs and their use as antiviral agents Various 2′-beta-methyl-6-substituted adenosine analogs (including 2,6-disubstituted adenosine, 8-aza-6-substituted adenosine, and 2-aza-6-substituted adenosine) are prepared by conventional and combinatorial library approaches. Contemplated compounds are particula... | 05/15/2007 |
| 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 |
| 7163928 | Partial and full agonists of Aadenosine receptors Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction. ... | 01/16/2007 |
| 7157440 | Partial and full agonists of A1 adenosine receptors Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, and myocardial infarction. ... | 01/02/2007 |
| 7148223 | 4′-thio-L-xylo furanosyl nucleosides, precursors thereof, preparation and use thereof Compounds represented by the formula 1: A is selected from the group consisting of wherein each R individually is H or... | 12/12/2006 |
| 7148042 | Method of preparing a guanosine-group compound and an intermediate thereof A glyoxal-guanosine-group compound is prepared either by reacting glyoxal-guanine with any one of ribose-1-phosphate and 2-deoxyribose-1-phosphate in the presence of purine nucleoside phosphorylase, or by reacting glyoxal-guanine with any one selected from the group... | 12/12/2006 |
| 7141397 | Method of preparing a guanosine-group compound and an intermediate thereof A glyoxal-guanosine-group compound is prepared either by reacting glyoxal-guanine with any one of ribose-1-phosphate and 2-deoxyribose-1-phosphate in the presence of purine nucleoside phosphorylase, or by reacting glyoxal-guanine with any one selected from the group... | 11/28/2006 |
| 7141396 | Method of preparing a guanosine-group compound and an intermediate thereof A glyoxal-guanosine-group compound is prepared either by reacting glyoxal-guanine with any one of ribose-1-phosphate and 2-deoxyribose-1-phosphate in the presence of purine nucleoside phosphorylase, or by reacting glyoxal-guanine with any one selected from the group... | 11/28/2006 |
| 7138377 | Topoisomerase inhibitors The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells. ... | 11/21/2006 |
| 7125983 | L-nucleic acid derivatives and process for the synthesis thereof A novel method has been found to produce 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine as a novel useful intermediate compound. A novel method has been further found to produce thymidine from 2,2′-anhydro-1-(β-L-arabinofuranosyl)thymine. A novel method has been... | 10/24/2006 |
| 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 |
| 7094769 | 2-aminocarbonyl-9H-purine derivatives The present invention relates to compounds of the formula: and pharmaceutically acceptable salts and solvates thereof, and to processes for the preparation of, intermediates used in the preparation of, compositio... | 08/22/2006 |
| 7087732 | Nucleotides and analogs having photoremovable protecting groups A synthetic strategy for the creation of large scale chemical diversity. Solid-phase chemistry, photolabile protecting groups, and photolithography are used to achieve light-directed spatially-addressable parallel chemical synthesis. Binary masking techniques are ut... | 08/08/2006 |
| 7074923 | Process for preparing xanthine phosphodiesterase V inhibitors and precursors thereof A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to sy... | 07/11/2006 |
| 7071173 | 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 ... | 07/04/2006 |
| 7070928 | Evolving new molecular function Nature evolves biological molecules such as proteins through iterated rounds of diversification, selection, and amplification. The present invention provides methods, compositions, and systems for synthesizing, selecting, amplifying, and evolving non-natural molecul... | 07/04/2006 |
| 7067641 | Phosphinoamidite carboxylates and analogs thereof in the synthesis of oligonucleotides having reduced internucleotide charge Nucleoside phosphinoamidite carboxylates and analogs are provided that have the structure of formula (III) wherein A is hydrogen, hydroxyl, lower alkoxy, lower alkoxy-substituted lower alkoxy, halogen, SH, NH | 06/27/2006 |
| 7056894 | Inhibitors of ADP-ribosyl transferases, cyclases, and hydrolases, and uses thereof The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C... | 06/06/2006 |
| 7022680 | Inhibitors of ADP-ribosyl transferases, cyclases, and hydrolases The present invention provides compounds having the formula: wherein A is a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group, the group being further substituted with an electron contribut... | 04/04/2006 |
| 6979676 | Pharmaceutical composition containing and indolopyrrolocarbazole derivative The present invention is directed to a pharmaceutical composition comprising a compound of Formula I dissolved in propylene glycol and water. The present invention also relates to a pharmaceutical composition containing a compound of Formula I dissolved in propylene... | 12/27/2005 |