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Class 544/266 - At 2-,6-, and 8-positions


Subclass of Class 544 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein chalcogens (i.e., oxygen, sulfur, selenium,
No. of patents: 53
Last issue date: 09/23/2008


1    
NumberTitleIssue Date
7427616Condensed pyridines and pyrimidines with tie2 (TEK) activity
A compound of the Formula (I), wherein A together with the carbon atoms to which it is attached forms a fused 5-membered heteroaryl ring, wherein said heteroaryl ring contains 1 or 2 heteroatoms selected from O, N and S, and wherein the 5-membered ring containing G ...
09/23/2008
7307166Oxpurine nucleosides and their congeners, and acyl, derivatives thereof, for improvement of hematopoiesis
The invention relates to certain oxypurine nucleosides, congeners of such oxypurine nucleosides, and acyl derivatives thereof, and compositions which contain at least one of these compounds. The invention also relates to methods of treating or preventing hematopoiet...
12/11/2007
RE390564-Azasteroids for treatment of hyperandrogenic conditions
Compounds of structural Formula (I) and pharmacologically acceptable salts and esters thereof possess 5α-reductase inhibitory activity. These compounds inhibit 5α-reductase type 1 and type 2. The compounds of structural Formula...
04/04/2006
6723727Substituted purine derivatives, processes for their preparation, their use, and compositions comprising them
The present invention relates to compounds of the formulae I and Ia in which X, Y, W, Wa, G and Ga have the meanings given in the patent claims, and their physiologically tolerable salts and their p...
04/20/2004
6600044Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucl...
07/29/2003
6518425Method of manufacture of 1,3-oxathiolane nucleosides
Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the process...
02/11/2003
6489344Inhibitors of glycogen synthase kinase 3
New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the in...
12/03/2002
6465650Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids
The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof ##STR1## wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B' is a base customary in nucleot...
10/15/2002
6333331Substituted O6-benzylguanines
The present invention provides AGT inactivating compounds such as substituted O6 -benzylguanines of the formula ##STR1## 7- or 9-substituted 8-aza-O6 -benzylguanines, 7,8-disubstituted O6 -benzylguanines, 7,9-disubstituted...
12/25/2001
62588096-aryloxy and arylthiopurines
Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: ...
07/10/2001
6175008Processes for preparing substituted 1,3-oxathiolanes with antiviral properties
Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: ##STR1## wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S.dbd.O or SO2...
01/16/2001
6166019Piperazinyl pyrimidine dione compounds selective for adrenoceptors
Compounds of Formula I and II and their pharmaceutically acceptable, salts, esters and prodrugs thereof are selective alpha-1D adrenoceptor anatagonists and may be useful for treating disease states....
12/26/2000
6143743Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders
Corticotropin releasing factor (CRF) antagonists of formula (I): ##STR1## and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders a...
11/07/2000
61037079-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)purine derivatives
The present invention relates to 9-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)purine derivatives having antiviral activity, represented by formula [I]: ##STR1## wherein B represents a base selected from the group consisting of purine, azap...
08/15/2000
6075143Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids
There are described N-ethylglycine derivatives of the formula I ##STR1## in which PG is a urethane-type or trityl-type amino protective group which is labile to weak acids, X is NH, O or S, Y is CH2, NH or O, and B' are bases customary in ...
06/13/2000
6046207Benzopyranopyrrole and benzopyranopyridine ଱-1 adrenergic compounds
The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are ଱-1 adrenergic antagonists and are useful in the treatment of BPH; also ...
04/04/2000
6004966Use of xanthine oxidase inhibitors as anti-ischaemic agents
The use of a compound of formula I ##STR1## in which R1 and R2 are N, X1 and X2 which may be the same or different are hydrogen, hydroxy, or an optionally substituted alkyl, and Z1 and Z2
12/21/1999
60018444-Azasteroids for treatment of hyperandrogenic conditions
Compounds of structural Formula (I) ##STR1## and pharmacologically acceptable salts and esters thereof possess 5଱-reductase inhibitory activity. These compounds inhibit 5଱-reductase type 1 and type 2. The compounds of structural Formula ...
12/14/1999
5998456Benzimidazole compounds containing 1,2,4-triazole ring, and compositions and methods of use containing the same
Benzimidazole compounds represented by the formula set out below and analogs thereof, wherein Y represents a single bond or sulfur atom; Z represents oxygen atom, sulfur atom, or N--R4 ; R1 and R2 independently represent h...
12/07/1999
5994361Substituted purinyl derivatives with immunomodulating activity
The present invention comprises a compound of formula I: ##STR1## R1 of Formula I is substituted amino represented by formula NR5 R6 wherein R5 and R6 are independently selected from the group co...
11/30/1999
5958932Substitutes O6 -benzylguanines, compositions, and methods of using same
The present invention provides AGT inactivating compounds such as substituted O6 -benzylguanines of the formula ##STR1## wherein, for example, R1 is amino, hydroxy, or alkylamino, R2 is aminoalkyl, hydroxyalkyl, or al...
09/28/1999
5916894Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
The present invention provides 8-substituted O6 -benzylguanine derivatives which have been found to be effective AGT inactivators, as well as pharmaceutical compositions comprising such derivatives along with a pharmaceutically acceptable carri...
06/29/1999
5840729Xanthine derivatives as adenosine A1 receptor antagonists
A method of attenuating a cognitive deficit in a patient in need thereof comprising administering to the patient a xanthine derivative....
11/24/1998
5807854Pyrimidone derivatives with antifungal activity
Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also prov...
09/15/1998
5674998C-4' modified adenosine kinase inhibitors
This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo›2,3-d!pyrimidine and pyrazolo›3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside ...
10/07/1997
55389789-purinyl phosphonic acid derivatives
This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immuno-suppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents....
07/23/1996
55278039-purinyl phosphonic acid derivatives
This invention relates to novel purine nucleoside phosphorylase inhibitors, to the methods and intermediates for their preparation and to their use as immuno-suppressants, antilymphoma, antileukemic, antiviral and antiprotozoal agents....
06/18/1996
5525606Substituted 06-benzylguanines and 6(4)-benzyloxypyrimidines
The present invention provides 8-substituted O6 -benzylguanines of the formula ##STR1## wherein R1, R2, and R3 are as defined in the specification, and 4(6)-substituted 2-amino-5-nitro-6(4)-benzyloxypyrimid...
06/11/1996
5516903Process for preparing [IR-(1଱,2ଲ-3଱)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclob utyl]-1,9-dihydro-6H-purin-6-one
The protected cyclobutanone of the formula ##STR1## is treated with a dialkylaluminum chloride, an alkylaluminum dichloride, a trialkylaluminum compound, hydrogen in the presence of the catalysts ruthenium black or ruthenium on alumina, diphenyl-sila...
05/14/1996
5506347Lyxofuranosyl analogues of adenosine
Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of aden...
04/09/1996
5393883Antiviral combinations and compounds therefor
The present invention relates to novel ribonucleotide reductase inhibitors and new combinations comprising an antiviral compound, such as acyclovir, and a thiocarbonohydrazone ribonucleotide reductase inhibitor for the chemotherapeutic treatment of virus ...
02/28/1995
5332814Process for the preparation of carbacyclic nucleosides, and intermediates
Process for the preparation of racemic compounds of the formula I ##STR1## or enantiomers thereof, in which B is the radical of a nucleic base from the series comprising purine, a purine analogue or a pyridine analogue, and R is H or a protective gro...
07/26/1994
5332744Substituted imidazo-fused 6-membered heterocycles as angiotensin II antagonists
Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart fail...
07/26/1994
52082408-substituted purines as selective adenosine receptor agents
The present invention relates to certain novel 8-substituted purines as selective A1 -adenosine receptor antagonists which are useful in the treatment of patients suffering from Alzheimer's disease, congestive heart failure or pulmonary broncho...
05/04/1993
5177074Angiotensin II antagonists incorporating a substituted thiophene or furan
There are disclosed substituted thiophene and furan derivatives of Formula I which are useful as angiotensin II antagonists. ##STR1##...
01/05/1993
5175167Hetarylalkenes, their preparation and intermediates for their preparation and their use
Hetarylalkenes of the general formula I ##STR1## where Ar is hetaryl, A is C1 -C6 -alkyl, C2 -C6 -alkenyl, C3 -C8 -cycloalkyl, C3 -C8 -cycloalkyl-C1 -C...
12/29/1992
5171353Sulfonamides
Sulfonamides of the general formula I ##STR1## where R1 is hydrogen of C1 -C4 -alkyl, R2 is hydrogen or substituted or unsubstituted C1 -C6 -alkyl; C3 -C4 -alkenyl; C
12/15/1992
5158954Methyl ଱-(2-substituted)pyrid-3-yl-ଲ-methoxy-acrylates, compositions containing them and their use as fungicides
Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O)n, NR4, CR1 R2...
10/27/1992
5157026Oxo-purines as angiotensin II antagonists
Substituted Imidazo-fused 6-membered heterocycles of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart fail...
10/20/1992
5103007Lipids
Lipid derivatives represented by the formula: ##STR1## wherein R1 stands for an optionally substituted higher alkyl group, R2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containin...
04/07/1992
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