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| Number | Title | Issue Date |
| 8106183 | Process for preparing an A-adenosine receptor agonist and its polymorphs Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph. ... | 01/31/2012 |
| 8039614 | 4' -C-substituted-2-haloadenosine derivative The present invention provides a method for producing a 4′-C-substituted-2-haloadenosine derivative represented by the following formula [I], [II], or [III]: wherein X represents a halogen atom, R1 represents a... | 10/18/2011 |
| 7994310 | Process for preparing 2′-deoxy-2′, 2′-difluorocytidine Disclosed is a method for preparing 2′-deoxy-2′,2′-difluorocytidine of Formula I comprising, preparing an optically pure 3R-hydroxypropane amide compound of Formula VIII from an optical ester compound of Formula IX using an optically active chiral amine, prepa... | 08/09/2011 |
| 7956179 | Process for preparing an A2A-adenosine receptor agonist and its polymorphs Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph. ... | 06/07/2011 |
| 7884202 | Nucleobase having perfluoroalkyl group and process for producing the same Nucleobases are perfluoroalkylated in a one step process with a perfluoroalkyl halide in the presence of a sulfoxide, a peroxide and an iron compound. Compounds so produced are useful as medicinal drugs, intermediates for medicinal drugs and agricultural chemicals. | 02/08/2011 |
| 7799907 | Method for the preparation of 2′-deoxy-2′,2′-difluorocytidine Provided is an improved method for stereoselectively preparing 2′-deoxy-2′,2′-difluorocytidine of formula (I), which includes reacting a 1-halo ribofuranose compound with a nucleobase of formula (IV) in a solvent to obtain a nucleo side of formula (II) with re... | 09/21/2010 |
| 7741473 | Process for the preparation of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles The present invention is directed to a processes for the synthesis of trans isomer of 4,6-disubstituted-tetrahydro-furo, thieno, pyrrolo and cyclopenta-[3,4][1,3]dioxoles (Formula I). The process comprises the steps of: (a) obtaining a compound of Formula II, which ... | 06/22/2010 |
| 7732595 | Process for preparing an A-adenosine receptor agonist and its polymorphs Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph. The A2A-adenosine receptor agonist has the fo... | 06/08/2010 |
| 7714123 | Crystalline forms of an antiviral benzimidazole compound The invention relates to crystalline forms of 5,6-dichloro-2-(isopropylamino)-1-β-L-ribofuranosyl-1Hbenzimidazole, pharmaceutical compositions comprising the same, processes for preparing the same, and their use in medical therapy. ... | 05/11/2010 |
| 7671192 | Process for preparing an A-adenosine receptor agonist and its polymorphs Synthesis methods suitable for large scale manufacture of the A2A-adenosine receptor agonist (1-{9-[(4S,2R,3R,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-6-aminopurin-2-yl}pyrazol-4-yl)-N-methylcarboxamide and precursors thereof. ... | 03/02/2010 |
| 7595390 | Industrially scalable nucleoside synthesis An industrially scalable two-step process for preparing a β-L-2′-deoxy-nucleoside that results in a predominance of the β- over the α-anomeric form of the compound is described. An optional third step may be used to prepare 3′-prodrugs of desirable β-L-2′-... | 09/29/2009 |
| 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 |
| 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 |
| 7388094 | Processing for producing 2′-deoxy-2′-fluorouridine 1-β-D-Arabinofuranosyluracil in 3′,5′-hydroxyl-protected form is reacted with a trifluoromethanesulfonylating agent in the presence of an organic base to convert it into a 2′-triflate form, and then it is reacted with a fluorinating agent containing “a salt... | 06/17/2008 |
| 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 |
| 7345164 | Production method of 5′-acyloxynucleoside compound A production method for conveniently producing a 5′-acyloxynucleoside compound shown by the formula [A] in a good yield while suppressing formation of by-products, including subjecting a 2′,3′,5′-triacyloxynucleoside compound represented by the formula [I] t... | 03/18/2008 |
| 7342003 | Synthesis of 2-aralkyloxyadenosines, 2-alkoxyadenosines, and their analogs Provided is a method for the synthesis of an aralkyloxyadenosine or an alkoxyadenosine. The method includes protecting the hydroxyl sugar groups with a protecting group to produce a protected halogenated adenosine. The protected halogenated adenosine is alkoxylated,... | 03/11/2008 |
| 7339054 | Process for preparing branched ribonucleosides from 1,2-anhydroribofuranose intermediates A process is provided for the preparation of branched-chain ribonucleosides of formula (I): from the 1,2-anhydroderivatives of formula (II). wherein PG is a hydroxyl protecting gr... | 03/04/2008 |
| 7297787 | Process for preparing N6 substituted aminopurine ribofuranose nucleosides An improved process for preparing N6 -substituted aminopurine ribofuranose nucleosides. Compounds of this type are known to be usefull in the prepartation of compounds having activitity at adenosine receptors, e.g. Adenosine A1 receptor. The process comprises the st... | 11/20/2007 |
| 7291726 | 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... | 11/06/2007 |
| 7235647 | Intermediate and process for preparing of β- anomer enriched 21-deoxy,21,21-difluoro-D-ribofuranosyl nucleosides The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 21-deoxy-21,21-D-ribofuranosyl difluoronucleosides of formula (II), and physiologically accept... | 06/26/2007 |
| 7226913 | Pharmaceutical compositions having Aadenosine receptor agonist activity The present invention provides compositions for oral administration of compounds having A2A adenosine receptor agonist activity. These compositions are useful for treatment of inflammatory conditions. ... | 06/05/2007 |
| 7214665 | 2-propynyl adenosine analogs having Aagonist activity and compositions thereof The invention provides compounds having the following general formula (I): wherein X, R1, R2, R7 and Z are as described here. ... | 05/08/2007 |
| 7183264 | N-pyrazole A2A receptor agonists 2-adenosine N-pyrazole compounds having the following formula: and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes... | 02/27/2007 |
| 7144872 | N-pyrazole Areceptor agonists This specification discloses 2-adenosine N-pyrazole compounds having the following formula: and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeu... | 12/05/2006 |
| 7101994 | Process for preparing substituted benzimidazole compounds The invention relates to new methods of preparing substituted benzimidazole compounds, such as 2-bromo-5,6-dichlorobenzimidazole, which are useful in the preparation of compounds having antiviral activity. ... | 09/05/2006 |
| 7038039 | Process for selectively producing 1-phosphorylated sugar derivative anomer and process for producing nucleoside A desired isomer is selectively prepared by phosphorolyzing and isomerizing an anomer mixture of a 1-phosphorylated saccharide derivative while crystallizing one of the isomers to displace the equilibrium. Furthermore, using the action of a nucleoside phosphorylase,... | 05/02/2006 |
| 7034161 | Process for producing a ribofuranose A method of converting pure α-anomer or β/α-anomer mixtures of 1,2,3,5-tetra-O-acetyl-L-ribofuranose to methyl-1-(2,3,5-tri-O-acetyl-β-L-ribofuranosyl)-1,2,4-triazole-3-carboxylate an intermediate for levovirin, as well as, the novel pure α-anomer, alpha 1,2,3,... | 04/25/2006 |
| 7019128 | Propargylethoxyamino nucleotides Propargylethoxyamino nucleosides are disclosed having the structure wherein R1 and R2 are —H, lower alkyl, or label; B is a 7-deazapurine, purine, or pyrimidine nucleoside base; W1 is ... | 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 |
| 6972330 | Chemical synthesis of methoxy nucleosides Process for chemical synthesis of methoxy nucleosides. ... | 12/06/2005 |
| 6933114 | Nucleic acid ligands to the prostate specific membrane antigen Methods are provided for generating nucleic acid ligands of Prostate Specific Membrane Antigen (PSMA). The methods of the invention use the SELEX method for the isolation of nucleic acid ligands. The invention also includes nucleic acid ligands to PSMA, and methods ... | 08/23/2005 |
| 6914061 | 4′-thio-L-xylofuranosyl 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 acyl, Y is X, N3,... | 07/05/2005 |
| 6914138 | Urea 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 pyrimidine ring, wit... | 07/05/2005 |
| 6897302 | Method for synthesizing β-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (β-L-FD4C) The invention provides a method of synthesizing β-L-5-fluoro-2′,3′-dideoxy-2′,3′-didehydrocytidine (β-L-FD4C). The method allows for large-scale production of β-L-FD4C in an efficient, cost-effective, and environmentally sound manner. ... | 05/24/2005 |
| 6884881 | 2′-Substituted RNA preparation A process for the preparation of a compound of formula (1): is provided, which comprises the reaction a compound of formula (2): with a compound of formula Al(OR)3 | 04/26/2005 |
| 6884880 | Process for the preparation of 9-β-anomeric nucleoside analogs A process for substantially enhancing the regio and stereoselective synthesis of 9-β-anomeric nucleoside analogs is described. The introduction of the sugar moiety onto a 6-substituted purine base was preformed so that only the 9-β-D- or L-purine nucleoside analog... | 04/26/2005 |
| 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 |
| 6770439 | Sets of generalized target-binding e-tag probes Probe sets for the multiplexed detection of the binding of, or interaction between, one or more ligands and target antiligands are provided. Detection involves the release of identifying tags as a consequence of target recognition. The probe sets include electrophor... | 08/03/2004 |
| 6696555 | 3'-Desoxypentopyranosyl nucleic acid, its production and its use The invention relates to a 3'-deoxypentopyranosylnucleic acid consisting essentially of 3'-deoxypentopyranosylnucleosides of the formulae (I) or of the formulae (II) ##STR1## their preparation and use for the production of a therapeutic, diagnostic a... | 02/24/2004 |
