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Class 536/27.63 - Halogen, chalcogen, or cyano bonded directly to the 2-position of the purine ring system


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogen (i.e., oxygen, sulfur, selenium,
No. of patents: 127
Last issue date: 09/16/2008


1        
NumberTitleIssue Date
7425547Nucleoside derivatives for treating hepatitis C virus infection
Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula IB as follows: and pharmaceutically...
09/16/2008
7342003Synthesis 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
7199127Purine 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
7189706C2,5′-disubstituted and N,C2,5′-trisubstituted adenosine derivatives and pharmaceutical compositions containing them
The present invention concerns novel C2,5′-disubstituted and N6,C2,5′-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in...
03/13/2007
7183264N-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
7144872N-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
7141553A3AR agonists for the treatment of inflammatory arthritis
The present invention concerns a method for the treatment of inflammatory arthritis, and in particular rheumatoid arthritis, by administering to the subject specific low dosages of N6-(3-iodobenzyl)-adenosine 5′-N-methyl-uronamide (IB-MECA) and 2-chloro-N6-(3-iodo...
11/28/2006
7112574C2,8-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
7084127C2,5′-disubstituted and N, C2,5′-trisubstituted adenosine derivatives and their different uses
The present invention concerns novel C2,5′-disubstituted and N6′,C2,5′-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value...
08/01/2006
6949640Method for synthesizing 2-chloro-9-(2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine
2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-9-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofuranose; and reacting with a base such as ammonia to provide 2-chloro-9-(2-deoxy...
09/27/2005
6946449Partial 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. ...
09/20/2005
6921753Purine 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
6914053Adenosine A3 receptor agonists
Disclosed are novel adenosine A3 receptor agonists of Formula I: wherein: R is hydrogen or lower alkyl; R1 is optionally substituted lowe...
07/05/2005
6900309Purine 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
6803457Compounds for the treatment of ischemia
A3 agonists, methods of using such A3 agonists and pharmaceutical compositions containing such A3 agonists. The A3 agonists are useful for the reduction of tissue damage resulting from tissue ischemia or hypoxia. ...
10/12/2004
6680382Process for preparing purine nucleosides
The present invention provides for the preparation ଲ-adenine nucleosides by coupling an adenine derivative containing an unprotected exocyclic amino group at the C-6 position and a blocked arabinofuranosyl derivative, in the presence of a base and s...
01/20/2004
6677316Adenosine derivatives and methods of administration
A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amoun...
01/13/2004
66422102-(N-pyrazolo)adenosines with application as adenosine A2A receptor agonists
N-pyrazole substituted 2-adenosine compounds and methods for using the compounds as A2 A-adenosine receptor agonists useful to stimulate mammalian coronary vasodilation for therapeutic purposes and as adjuncts in cardiological imaging....
11/04/2003
6576620Method of identifying partial adenosine A1 receptor agonists
The present invention provides a method for identifying partial adenosine A1 receptor agonists that are useful in the treatment of arrhythmias. Partial adenosine A1 receptor agonists and methods for using partial adenosine A1 receptor agonists to treat ar...
06/10/2003
6544960Chemical compounds
A compound of formula (I), wherein R2 represents C1-3 alkyl, halogen or hydrogen; R3 represents straight or branched alkyl group of 1-6 carbon atoms; with the proviso that, when R3 represents C1-3 alk...
04/08/2003
64982412-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
6492348Adenosine derivatives
A compound of formula (I) which is an agonist at the adenosine Al receptor, wherein Y, Z, and W represent heteroatoms, and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof for use in therapy. ##STR1##...
12/10/2002
6407076Adenosine analogues and related method of treatment
A compound of formula (I) wherein R2 represents C1-3 alkyl, halogen or hydrogen; R3 represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms; and salts and solvates thereof, in particular, physiologica...
06/18/2002
6403567N-pyrazole A2A adenosine receptor agonists
2-adenosine N-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....
06/11/2002
6355787Purine nucleoside modifications by palladium catalyzed methods and compounds produced
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 ...
03/12/2002
6326359Adenosine 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
6294522N6 heterocyclic 8-modified adenosine derivatives
N6 heterocyclic 8 modified adenosine derivatives that are selective, partial or full adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity, modifying adipocyte function, treating centr...
09/25/2001
6258793N6 heterocyclic 5' modified adenosine derivatives
N6 heterocyclic 5' modified adenosine derivatives that are adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity, modifying adipocyte function, treating central nervous system disorder...
07/10/2001
6252061Process for the production of 2-halo-6-aminopurine derivatives
A novel process for preparing 2-halo-6-aminopurine derivatives and their analogs is disclosed. The method comprises halogenation of 2,6-diaminopurine derivatives at the C-2 position in a specific combination of aprotic polar and nonpolar organic solvents ...
06/26/2001
6221851Pharmaceutical therapy for congestive heart failure
The present invention is directed to reduce elevated levels of tumor necrosis factor-alpha (TNF-଱) found in a failing heart. The present invention is directed to a composition and method of regulating TNF-଱ expression in myocardial tissue by t...
04/24/2001
6180615Propargyl phenyl ether A2A receptor agonists
2-adenosine propargyl phenyl ether 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...
01/30/2001
6093807Sugar-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
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
5998388Adenosine 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
5994321Antiviral 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
5945524Process for the chemical synthesis of oligonucleotides
Use of a dansylethoxycarbonyl group as base-labile 5'-hydroxyl protective group in the chemical synthesis of DNA and RNA and suitable synthetic processes. The ease of detection of the dansyl protective group and the ease of elimination from the sugar resi...
08/31/1999
5942497Purine compound and catecholamine compound containing compositions and methods for administration
A purine compound, which has a desired and an undesired effect when a dosage sufficient to induce the desired effect is administered to a mammal, is combined with a counteracting agent, wherein the counteracting agent can reduce the undesired effect when ...
08/24/1999
5939543Stable solid 2-octynyl adenosine and process for producing the same
The present invention provides two kinds of solid 2-octynyl adenosine products with novel properties which are stabilized with respect to temperature or temperature and humidity, one being solid 2-octynyl adenosine having a moisture content of not more th...
08/17/1999
5817641Treatment of enterotoxigenic diarrhea with 2-substituted adenosine derivatives
Methods of therapeutically treating individuals suffering from diarrhea comprising the step of administering to such individuals who are suffering from diarrhea, an effective amount of a 2-substituted adenine nucleotide or 2-substituted adenine nucleoside...
10/06/1998
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
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