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...Chester Carlson was a patent agent who tired of having to make multiple copies of patent applications using the only duplication method available at the time: carbon paper. In 1959 he came up with a new copying system and took it to IBM for evaluation. The "experts" at IBM determined potential sales to be only 5,000 units because people wouldn't want to use a bulky machine when they had carbon paper. Carlson's invention was the xerography process, the company founded on the system is Xerox.

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Class 536/28.55 - Halogen bonded directly to the 5-position of the diazine ring (e.g., 5-fluorouridine, etc.)


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein halogen is bonded directly to the 5-position
No. of patents: 135
Last issue date: 06/26/2007


1        
NumberTitleIssue Date
7235647Intermediate 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
7148207Oral 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
7119096Uracil reductase inactivators
Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 ...
10/10/2006
6884880Process 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
6699978Linker nucleoside, and production and use of the same
The present invention relates to a linker nucleoside, its preparation and use for the covalent bonding of biomolecules to oligonucleotides, in particular p-RNA oligonucleotides....
03/02/2004
6593467Process for the preparation of a deoxyuridine derivative
A process for the preparation of 5'-deoxy-5-fluorouridine, which comprises the transformation of 2',3'-O-isopropylidene-5-fluorouridine in the corresponding 5'-O-sulfonyl derivative, subsequent reaction with alkaline or earth-alkaline iodides and, after h...
07/15/2003
6569837ଲ-L-2'-deoxy pyrimidine 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 ...
05/27/2003
6482805AZT derivatives exhibiting spermicidal and anti-viral activity
Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient conta...
11/19/2002
6458772Prodrugs
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
6407078AZT derivatives exhibiting spermicidal and anti-viral activity
Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient conta...
06/18/2002
6392032Heavily fluorinated sugar analogs
Heavily fluorinated sugar analogs of formula ##STR1## wherein R1 is selected from alkyl, alkenyl, aryl, --CH2 --O-alkyl, --CH2 --O-aryl, --CH2 OPO3 H, --CH2 --O-carbohydrate, --CH2
05/21/2002
6339151Enzyme catalyzed therapeutic agents
This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous, intracellular enzyme in the cell which is enhanced in its expres...
01/15/2002
6297223Uracil reductase inactivatores
Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-fluorouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, iodo, cyano, halo-substituted C
10/02/2001
6258360Prodrugs activated by targeted catalytic proteins
Prodrugs that are activated by and conjugated to a catalytic antibody conjugated to a moiety that binds to a tumor cell population are provided....
07/10/2001
6225450DNA 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
62111665'-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
6191120Spermicidally active 5-halo-6-alkoxy-5,6-dihydro-2',3'-dideoxy-uridines and their pharamaceutical compositions
Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient conta...
02/20/2001
6175001Functionalized 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
6060592Pyrimidine 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
6040298Methods 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
6020483Nucleoside 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
6013790Heavily fluorinated sugar analogs
Heavily fluorinated sugar analogs of formula ##STR1## wherein R1 is selected from alkyl, alkenyl, aryl, CH2 OH, --CH2 --O-alkyl, --CH2 --O-aryl, --CH2 OPO3 H, --CH2 --O-carb...
01/11/2000
5985849Phosphate compounds and their use as medicaments
A compound of the formula (I) or salts thereof: ##STR1## wherein X, R1, Q1 and Q2 are as defined in the specification. The compounds have been found to be P2 7-TM G-protein receptor antagonists, especially to the P2 Y...
11/16/1999
5968910Compositions 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
5959100Pyrimidine 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
5945527Palladium 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
58694642'-Deoxy-5-fluorouridine derivatives, a process for their preparation, antitumor agents containing same and methods for using said agents
The compounds of the invention are a 2'-deoxy-5-fluorouridine derivative represented by the formula ##STR1## wherein one of R1 and R2 is a hydrogen atom or a group easily hydrolyzable in vivo, the other is a benzyl group which m...
02/09/1999
58439175-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
5817639Purine 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
58115405-O-pyrimidyl-2,3-dideoxy-1-thiofuranoside derivative, and production method and use thereof
Disclosed is a 5-O-pyrimidyl-2,3-dideoxy-1-thio-D-furanoside derivative represented by the following formula (I) or an L-form isomer thereof: ##STR1## wherein X represents a hydrogen atom, a fluorine atom or an azido group; R1 represents a...
09/22/1998
5808049Stereospecific 5-fu esters and methods for preparing same
There is disclosed an ester compound that is resistant to decomposition in blood, but is quickly hydrolyzed in cancer cells, and functions as an anticancer agent. The ester compound has a structure represented by formula (I) or formula (II): ##STR1##...
09/15/1998
5798340Nucleotide 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
57928412'-halomethylidene, 2'-ethenylidene and 2'-ethynl 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...
08/11/1998
5792773L-ଲ-dioxolane uridine analog administration for treating Epstein-Barr virus infection
The present invention relates to the discovery that certain ଲ-L-dioxolane nucleoside analogs which contain a uracil base, and preferably, a 5-halosubstituted uracil base, exhibit unexpectedly high activity against Epstein-Barr virus (EBV). In partic...
08/11/1998
5789387Methods and compositions for treating fungal infections in mammals
Methods of treating fungal infections are disclosed. The methods comprise administering a chitin synthesis inhibitor to a mammal in a continuous fashion so that at least a minimum effective concentration is maintained in the mammal's plasma or in a target...
08/04/1998
5783689Antibacterial and antifungal nucleosides
5'-O-Acyl-5-fluorouridines and 5'-O-acyl-5-sluorocytidines are prepared by the direct acylation of the 5'-hydroxyl group with amino acids under Mitsunobu conditions and the amino acyl derivatives are coupled with other amino acids or peptides to provide a...
07/21/1998
57634183'-substituted nucleoside derivatives
The invention relates to a 3'-substituted nucleoside derivative represented by the following general formula (1): ##STR1## wherein B means a nucleic acid base which may have a substituent, Z represents a lower alkynyl or lower alkenyl group which may...
06/09/1998
5719132Compositions and methods of treating HIV with d4T, 5-fluorouracil/tegafur, and uracil
The present invention is directed to the use of pharmaceutical compositions containing anti-retroviral effective amounts of (a) d4T and (b) 5-fluorouracil or a prodrug, or salt thereof....
02/17/1998
5719273Palladium catalyzed nucleoside modifications methods using nucleophiles and carbon monoxide
This invention discloses a method for the preparation modified nucleosides using a palladium catalyst, a nucleophile and carbon monoxide....
02/17/1998
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