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Class 536/27.22 - Carbonyl, thiocarbonyl, or nitrogen, other than as nitro or nitroso, bonded directly to the sugar ring


Subclass of Class 536 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein the sugar ring of the nucleoside is bonded
No. of patents: 52
Last issue date: 09/09/2008


1    
NumberTitleIssue Date
7423025L-nucleosides as ligands to adenosine receptors
Disclosed herein are compounds having Formula I, which are non-natural L-adenosine analogs. Also disclosed are their methods of making. Still further, disclosed are the uses of the disclosed compounds to treat cardiovascular disease, ischemia related injuries; and n...
09/09/2008
7381714A1 adenosine receptor agonists
Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists having the structure of Formula I: which are useful for treating various disease states, in particular tachycardia and atrial...
06/03/2008
7358235Analogs of nitrobenzylthioinosine
Analogs or derivatives of nitrobenzylthioinosine compounds. The use of these new analogs of nitrobenzylthioinosine and methods for the treatment of pain and various other indications using these analogs of nitrobenzylthioinosine as well as pharmaceutical composition...
04/15/2008
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
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
7132409Adenosine derivatives and use thereof
2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5′-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and pro...
11/07/2006
7078499Nucleotide analogues comprising a reporter moiety and a polymerase enzyme blocking moiety
Nucleotides comprising a reporter moiety and a polymerase enzyme blocking moiety in which the reporter moiety does not also act as a polymerase enzyme blocking moiety are described. Also described are compounds of Formula (I): wherein W is a phosphate group, B is a ...
07/18/2006
7022727Crystalline drug form
The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing a...
04/04/2006
7005425Method for treating arrhythmias
Methods are provided for treating arrhythmia in a manner that minimizes undesirable side effects, comprising administration of a therapeutically effective minimal dose of an A1 adenosine receptor agonist with a therapeutically effective minimal dose of a ...
02/28/2006
6936596Adenosine derivatives and use thereof
2-(6-Cyano-1-hexyn-1-yl)adenosine, 2-(6-cyano-1-hexyn-1-yl)adenosine 5′-monophosphate, or salts thereof; and drugs containing the same as an active ingredient. The compounds have excellent effects of lowering ocular tension, promoting blood flow in retina, and pro...
08/30/2005
6903079Nucleoside compounds and compositions thereof
The invention provides a novel class of substituted nucleoside derivatives having the formula: A-Z1-L-Z2-G wherein: A and G are connected via Z1 and Z2 respectively, to a linker, L; and A i...
06/07/2005
6852746Crystalline drug form
The present invention relates to a crystalline form of 6-[(2,2-diphenylethyl)amino]-9-(N-ethyl-β-D-ribofuranosyluronamide)-N-(2-{N′-[1-(2-pyridyl)-4-piperidyl]ureido}ethyl)-9H-purine-2-carboxamide and to a process for the preparation of, compositions containing a...
02/08/2005
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
6784165Treatment of heart rhythm disturbances with N6-substituted-5′-(N-substituted) carboxamidoadenosines
The present invention discloses a method for treating heart rhythm disturbances in a mammal in need thereof by the administration of N6-substituted-5′(N-substituted)carboxamidoadenosines. More particularly, the invention is directed to a method for trea...
08/31/2004
6541626Process for selective N-acylation of purine nucleosides
Methods for selectively protecting the exocyclic amino function of a purine nucleoside are provided using activating agents to effect acylation at the exocyclic amino site. Methods are also provided for recycling polymer bound coupling supports from the r...
04/01/2003
6232297Methods and compositions for treating inflammatory response
Compounds and methods are provided to treat inflammatory conditions with certain A2A adenosine receptor antagonists....
05/15/2001
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
6072051Nucleoside derivatives and process for preparing the same
According to the present invention, provided are novel nucleoside derivatives having antiviral activity, in particular, anti-HBV (anti-Hepatitis-B Virus) activity, represented by general formula (I), wherein R1 represents hydrogen, phosphate, p...
06/06/2000
59256242,6-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
58891782-6-diaminopurine precursors
The present invention relates to compounds of formula (IV): ##STR1## wherein Ra and Rb each represent a hydrogen atom or together form an alkylidene group....
03/30/1999
5773423A3 adenosine receptor agonists
The present invention provides N6 -benzyladenosine-5'-N-uronamide and related substituted compounds, particularly those containing substituents on the benzyl and/or uronamide groups, and modified xanthine ribosides, as well as pharmaceutical co...
06/30/1998
5721356Orally active adenosine kinase inhibitors
This invention relates to adenosine kinase inhibitors and to nucleoside analogs, specifically to orally active, substituted 5-aryl pyrrolo›2,3-d!pyrimidine and 3-aryl pyrazolo›3,4-d! pyrimidine nucleoside analogs having activity as adenosine kinase inhi...
02/24/1998
5714599Process for the preparation of ste specific 1'-spiro-nucleosides
The invention relates to a novel process for stereocontrolled preparation of 1',1'-disubstituted and 1'-spiro-nucleosides of the formula I ##STR1## in which the substituents A, R8 and R9 are as defined in claim 1, and to novel i...
02/03/1998
5593975Adenosine derivatives having A2 agonist activity
Adenosine A2 agonists of the formula ##STR1## wherein R is hydrogen, alkyl, cycloalkyl or phenylalkyl; R1 is selected from the group consisting of a) optionally substituted phenyl or naphthyl; b) --(CH2)m --Het where...
01/14/1997
5498605Sulfo-derivatives of adenosine
The adenosine derivatives which contain a sulfohydrocarbon substituent, as depicted in the formula: ##STR1## wherein at least one of R1, R2, R3, R4, R5, and R6 is a sulfohydrocarbon ra...
03/12/1996
5480983Adenosine derivatives, preparation methods and pharmaceutical compositions containing them
The present invention relates to the derivatives of the formula ##STR1## and their addition salts, and to their use in therapeutics, especially as analgesics and as antihypertensives....
01/02/1996
5459132N6-[(Imidazo[1,2-a]pyridin-3-yl)ethyl]adenosines, their 5'-uronamide analogues and pharmaceutical compositions
The present invention relates to the derivatives of the formula ##STR1## and their addition salts, and to their use in therapeutics as analgesics, as antihypertensives and as drugs with antiproliferative properties....
10/17/1995
5455234Inhibition of hair growth
Mammalian hair growth is reduced by applying to the skin an inhibitor of a cysteine synthetic pathway enzyme....
10/03/1995
5310731N-6 substituted-5'-(N-substitutedcarboxamido)adenosines as cardiac vasodilators and antihypertensive agents
Compounds of the formula ##STR1## are disclosed, wherein R1, represents secondary alkyl; aralkyl; cycloalkyl; heteroaryl substituted alkyl; norbornyl; and substituted secondary alkyl, aralkyl, cycloalkyl, heteroaryl substituted alkyl, ...
05/10/1994
5283327Tri-O-acetyl-2-alkynyladenosines
The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine. The present invention also relates to a process for producing the compound and a process for pr...
02/01/1994
52800152-substituted adenosines and 2-substituted adenosine 5'-carboxamides
The present invention is directed to compounds useful as probes for characterizing and studying the adenosine A2 receptor. The present invention is also directed to methods of treating central nervous system disorders and cardiovascular disorde...
01/18/1994
5229505N6 -[3-(1-substituted)indolylethyl] adenosine 5'-carboxamides and their pharmaceutical compositions
The present invention relates to the derivatives of the formula ##STR1## and their addition salts, and to their use in therapeutics, especially in the central nervous system as analgesics, anticonvulsants, antiepileptics, anxiolytics, antidepressants...
07/20/1993
5219839Adenosine derivatives, their methods of preparation and pharmaceutical compositions in which they are present
The present invention relates to the derivatives of the formula ##STR1## and the corresponding enantiomers and diastereoisomers and, if appropriate, their addition salts, and to their use in therapeutics, especially in the central nervous system as a...
06/15/1993
5219840Antihypertensive 9-(2,N6 -disubstituted adenyl) ribofuranuronic acid derivatives
N6, 2-disubstituted or 2-substituted 1'-desoxy-1'-(6-amino-9-purinyl)-ଲ-D-ribofuranuronic acid amides, N-substituted amides, N,N-disubstituted amides, thioamides, N-substituted thioamides and N,N-disubstituted thioamides are effective aga...
06/15/1993
5206351Process for the preparation of 2-amino (2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl)adenine
A process for the preparation of 2-amino-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl) adenine (V) is described. The process uses a protected 2,6-di(tri-alkylsilylamino)-9-trialkylsilylpurine (II) which is reacted with protected chlorosugar 2,3,5-tr...
04/27/1993
5206222Methods for the reduction of myocardial reperfusion injury
This invention relates to a method to treat a heart attack victim to reduce heart muscle damage. In particular, the invention relates to a met Grant Statement This research was supported in part by the National Institute of Health, Grant R01 HL40892-01....
04/27/1993
51400152-aralkoxy and 2-alkoxy adenosine derivatives as coronary vasodilators and antihypertensive agents
Compounds are disclosed having the formulae: ##STR1## wherein R1 is selected from the group, consisting of radicals represented by the general formulae: ##STR2## wherein Y is selected from the group consisting of lower alkyl, lower ...
08/18/1992
49979245'-deoxy-4',5'-unsaturated-5'-substituted adenosines
This invention relates to certain aristeromycin/adenosine derivatives which are useful in inhibiting AdoMet-dependent transmethylation and in the treatment of patients afflicted with neoplastic or viral disease states....
03/05/1991
4977144Imidazo[4,5-b]pyridine derivatives as cardiovascular agents
Disclosed are the compounds of the formula ##STR1## wherein R represents hydrogen, lower alkyl, aryl or aryl-lower alkyl; R1 represents hydrogen, lower alkyl, C3 -C7 -alkenyl, carbocyclic or heterocyclic aryl, carbocy...
12/11/1990
49686972-substituted adenosine 5'-carboxamides as antihypertensive agents
The compounds of the formula I ##STR1## wherein R represents hydrogen or lower alkyl; R1 represents C3 -C6 -cycloalkyl optionally substituted by lower alkyl, C3 -C6 -cycloalkyl-lower alkyl option...
11/06/1990
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