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| Number | Title | Issue Date |
| 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 |
| 7335347 | Methods for purifying radiolabelled compounds One aspect of the present invention relates to a method of purifying radiolabelled compounds comprising a) loading onto a fluorous polymer a radiolabelled compound precursor comprising a fluoroalkyl tin moiety; b) reacting the radiolabelled compound precursor with a... | 02/26/2008 |
| 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 |
| 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 |
| 7148207 | Oral fludara of high-purity formulation with quick release of active ingredient This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants. ... | 12/12/2006 |
| 6933288 | Pyranosyl cytosines: pharmaceutical formulations and methods This invention is directed to novel pyranosyl cytosine compounds depicted graphically as structure I. This invention is further directed to a unique methodology for their preparation using solid-phase methodology. These hexopyranosyl cytosine derived natural product... | 08/23/2005 |
| 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 |
| 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 |
| 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 |
| 6635753 | Process for the preparation of substantially pure stavudine and related intermediates useful in the preparation thereof There are disclosed novel Stavudine solvates as follows: Stavudine NN-dimethyllacetamide solvates; Stavudine NN-dimethylacrylamide solvates and Stavudine NN-dimethylpropionamide solvates and processes for producing Stavudine NN-dimethylacetamide solvates,... | 10/21/2003 |
| 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 |
| 6458772 | Prodrugs Compounds of the formula I ##STR1## or corresponding monohydroxynucleoside derivatives wherein: R1 is hydroxy, amino or carboxy: optionally having esterified/amide bonded thereon; a C4 -C22 saturated or unsaturated, optionally ... | 10/01/2002 |
| 6458773 | Nucleoside with anti-hepatitis B virus activity Compounds and pharmaceutical compositions active against hepatitis B virus are provided, as is a method for the treatment of hepatitis B virus infection in humans and other host animals is provided comprising administering an effective amount of a ଲ... | 10/01/2002 |
| 6437118 | Vinylating of pyrimidine derivatives The invention relates to a process for the preparation of vinyl pyrimidines of the formula I ##STR1## wherein R1 is hydrogen or a carboxylic ester group, and R2 is hydrogen or a group of the formula (a) ##STR2## wherein Ra | 08/20/2002 |
| 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 |
| 6380368 | Enhanced triple-helix and double-helix formation with oligomers containing modified pyrimidines Novel oligomers are disclosed which have enhanced ability with respect to forming duplexes or triplexes compared with oligomers containing only conventional bases. The oligomers contain the bases 5-(1-propynyl)uracil, 5-(1-propynyl)cytosine or related ana... | 04/30/2002 |
| 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 |
| 6225450 | DNA sequencing by mass spectrometry The invention describes a new method to sequence DNA. The improvements over the existing DNA sequencing technologies are high speed, high throughput, no electrophoresis and gel reading artifacts due to the complete absence of an electrophoretic step, and ... | 05/01/2001 |
| 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 |
| 6175001 | Functionalized pyrimidine nucleosides and nucleotides and DNA's incorporating same Modified pyrimidine nucleotides derivatized at C5 to contain a functional group that mimics the property of a naturally occurring amino acid residues are provided. DNA molecules containing the modified nucleotides are also provided.... | 01/16/2001 |
| 6153744 | Nucleoside derivatives with photolabile protective groups The invention relates to nucleo-side derivatives with photo-unstable protective groups of the general formula (I) ##STR1## in which R1 is H, NO2, CN, OCH3, halogen, alkyl or alkoxyalkyl with 1 to 4 C atoms, R2 | 11/28/2000 |
| 6121248 | Anti-viral agent Disclosed is an anti-viral agent against varicella-zoster virus or cytomegalovirus comprising, as an active ingredient, 2-thio-5-halogenopyrimidine arabinoside of the formula (1): ##STR1## wherein B denotes a thiopyrimidine base of the formula (2) or... | 09/19/2000 |
| 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 |
| 6040298 | Methods for treatment with compositions effective against acyclovir-resistant strains of herpes viruses The present invention relates to pharmaceutical compositions useful for the treatment of subjects suffering from an infection or disease caused by herpes virus strains that are resistant to treatment with acyclovir. In particular, it has been discovered t... | 03/21/2000 |
| 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 |
| 5905070 | 5--Caboxamido or 5--fluoro!--2', 3'--unsaturated or 3'--modified!--pyrimidine nucleosides A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a 5-carboxamido or 5-fluoro!-2',3'-dideoxy-2',3'-didehydro-pyrimidine nucleosid... | 05/18/1999 |
| 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 |
| 5843917 | 5-Fluorouracil derivatives Novel compounds comprising 5-fluorouracil or 5-fluorouridine covalently linked to 5-ethynyluracil, 5-ethynyluridine or 5-propynyluracil and pharmaceutical compositions comprising such compounds are disclosed.... | 12/01/1998 |
| 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 |
