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| Number | Title | Issue Date |
| 7820811 | Pro-drugs of adenosine receptor agonists The invention relates to a method of improving oral drug absorption of adenosine analogues by the use of 2′-methoxy adenosine pro-drugs and to the use of these pro-drugs as medicaments. The invention further relates to compounds that are pro-drugs of adenosine rec... | 10/26/2010 |
| 7572909 | Method for the preparation of 2-halo-2′-deoxyadenosine compounds from 2′-deoxyguanosine The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2′-deoxyadenosine, CldAdo, 4), a drug of choice against hairy-cell leukemia and other neoplasms, from 2-amino-6-oxopu... | 08/11/2009 |
| 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 |
| 7199127 | Purine nucleosides Disclosed are purine nucleoside compounds that are selective to A3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the following general formula (I), including isomers thereof: | 04/03/2007 |
| 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 |
| 7112574 | C2,8-disubstituted adenosine derivatives and their different uses Novel C2,8-disubstituted adenosine derivatives disclosed herein have been found to be potent adenosine receptor agonists, in particular for the A2A receptor. The said compounds have biological activity against conditions such as hypertension, ischemic heart disease,... | 09/26/2006 |
| 7109180 | C-pyrazole Areceptor agonists 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart ... | 09/19/2006 |
| 6995148 | Adenosine cyclic ketals: novel adenosine analogues for pharmacotherapy The present invention relates to novel compounds that are novel adenosine receptor analogues. Specifically, the compounds of the present invention preferably function as both adenosine receptor agonists and ganglionic blocking agents. To achieve this functionality, ... | 02/07/2006 |
| 6921753 | Purine derivatives The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions cont... | 07/26/2005 |
| 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 |
| 6906190 | Inhibitors for de novo-RNA polymerases and methods of identifying targets for same A polymerase inhibitor has first moiety coupled to a second moiety via an optional linker in which the first moiety binds to an initiation nucleotide binding site of a polymerase and forms at least two hydrogen bonds with an RNA template strand that is associated wi... | 06/14/2005 |
| 6900309 | 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, compositions cont... | 05/31/2005 |
| 6855818 | C-pyrazole A2A receptor agonists 2-adenosine C-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and f... | 02/15/2005 |
| 6770634 | C-pyrazole a2a receptor agonists 2-adenosine C-pyrazole compounds having formula (a) and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart. ... | 08/03/2004 |
| 6498241 | 2-deoxy-isoguanosines isosteric analogues and isoguanosine derivatives as well as their synthesis 2'-Deoxyisoguanosine, isosteric analogues and isoguanosine derivatives of formulae I-V, processes for their production via compounds of the general formulae a or b and reaction with aroyl isocyanates or from compounds of the general formulae VI-IX by phot... | 12/24/2002 |
| 6326359 | Adenosine A2A receptor agonists as antiinflammatory agents The present invention provides compounds of formula (I): ##STR1## and pharmaceutically acceptable salts and solvates thereof, together with processes for the preparation of, compositions containing, uses of and intermediates used in the preparation of suc... | 12/04/2001 |
| 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 |
| 6214807 | C-pyrazole 2A A receptor agonists 2-adenosine C-pyrazole compositions having the following formula: ##STR1## and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.... | 04/10/2001 |
| 6187286 | Tumor imaging agents, methods and kits The invention provides tumor imaging agents comprising a radionuclide in association with a nucleotide polyphosphate targeting molecule. Methods for using the tumor imaging agents and kits containing the tumor imaging agents or components suitable for pro... | 02/13/2001 |
| 6147199 | 2-deoxy-isoguanosines isoteric analogues and isoguanosine containing oligonucleotides 2'-Deoxyisoguanosine, isosteric analogues and isoguanosine derivatives of formulae I-V, processes for their production via compounds of the general formulae a or b and reaction with aroyl isocyanates or from compounds of the general formulae VI-IX by phot... | 11/14/2000 |
| 6096724 | Pyrimidine derivatives and guanine derivatives, and their use in treating tumor cells The present invention provides certain 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR1## wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fus... | 08/01/2000 |
| 6093807 | Sugar-modified 7-deaza-7-substituted oligonucleotides Functionalized nucleomonomers and oligonucleotides are provided which have increased nuclease resistance and enhanced binding affinity to target DNA or RNA molecules. The oligonucleotides of the present invention comprise at least one 7-deaza-7-iodo-2'-su... | 07/25/2000 |
| 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 |
| 5998388 | Adenosine derivatives This invention relates to novel adenosine derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. Thus the invention provides compounds of formula (I) which are agonists at the adenosin... | 12/07/1999 |
| 5994321 | Antiviral guanine analogs A series of guanine analogs and physiological salts thereof, which are useful as virus inhibitors and as antiviral agents in the treatment of viral disease, having the basic structures of: ##STR1## wherein B is H, CH3 or NH2 ; C... | 11/30/1999 |
| 5955304 | DivIB The invention provides DivIB polypeptides and DNA (RNA) encoding such DivIB, particularly those of S. aureus, and a procedure for producing such polypeptides by recombinant techniques. Also provided are methods for utilizing such DivIB for the treatment o... | 09/21/1999 |
| 5948903 | Synthesis of 3-deazapurines This invention relates to compounds based on the 3-deazapurines ring system and to methods for making such compounds. The invention also generally relates to the field of "antisense" agents, agents that are capable of specific hybridization with a nucleot... | 09/07/1999 |
| 5925624 | 2,6-Di (substitutedamino) purine ribonucleoside analogues and administration to treat respiratory inflammation The present invention relates to 2,6-diaminopurine-ଲ-D-ribofuranuronamide derivatives of the following formula (I). These compounds and their salts and solvates are useful as anti-inflammatory agents, particularly in the treatment of patients with ... | 07/20/1999 |
| 5864033 | Adenosine kinase inhibitors Novel compounds which selectively inhibit adenosine kinase and methods of preparing adenosine kinase inhibitors are provided. Also provided are methods of treating various conditions which may be ameliorated by increased local concentrations of adenosine ... | 01/26/1999 |
| 5830881 | L-2'3',dideoxy nucleoside analogs as anti-hepatitus B (HBV) agents The present invention relates to the surprising discovery that certain dideoxynucleoside analogs which contain a dideoxy ribofuranosyl moiety having an L-configuration (as opposed to the naturally occurring D- configuration) exhibit unexpected activity ag... | 11/03/1998 |
| 5817639 | Purine 4'-thioarabinonucleosides The present invention provides a novel purine 4'-thioarabinonucleoside represented by the following formula 1!: ##STR1## wherein B represents a purine base other than adenine. Also disclosed are a method for preparing the purine 4'-thioarabinonucle... | 10/06/1998 |
| 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 |
| 5795977 | Water soluble adenosine kinase inhibitors This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to water soluble, aryl substituted 4-amino pyrrolo2,3-d! pyrimidine and pyrazolo3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhi... | 08/18/1998 |
| 5763597 | Orally active adenosine kinase inhibitors This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo2,3-d! pyrimidine and 3-aryl pyrazolo3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inh... | 06/09/1998 |
| 5763596 | C-4' modified adenosine kinase inhibitors This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo2,3-d!pyrimidine and pyrazolo3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside ... | 06/09/1998 |
| 5750675 | 2'-"up" fluorinated 2'-deoxy-arabinofuranosylpurines The present invention provides a compound having the structure: ##STR1## wherein R1 is hydrogen, benzyl or a substituted benzyl group; X is hydrogen, a flouro, an amino or a substituted amino group; Y is hydrogen, a methoxy, a methylthio, a benzylth... | 05/12/1998 |
| 5750692 | Synthesis of 3-deazapurines This invention relates to compounds based on the 3-deazapurines ring system and to methods for making such compounds. The invention also generally relates to the field of "antisense" agents, agents that are capable of specific hybridization with a nucleot... | 05/12/1998 |
| 5726302 | Water soluble adenosine kinase inhibitors This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to water soluble, aryl substituted 4-amino pyrrolo2,3-d! pyrimidine and pyrazolo3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhi... | 03/10/1998 |
| 5721356 | Orally active adenosine kinase inhibitors This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo2,3-d!pyrimidine and 3-aryl pyrazolo3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhi... | 02/24/1998 |
| 5705491 | Adenosine deaminase inhibitor The present invention relates to adenosine deaminase inhibitors containing at least one O-alkylated moiety and the pharmaceutically acceptable salts thereof. The pharmaceutical compositions of the present invention include adenosine deaminase inhibitors c... | 01/06/1998 |
