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| Number | Title | Issue Date |
| 7427616 | Condensed 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 |
| 7307166 | Oxpurine 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 |
| RE39056 | 4-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 |
| 6723727 | Substituted 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 |
| 6600044 | Process 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 |
| 6518425 | Method 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 |
| 6489344 | Inhibitors 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 |
| 6465650 | Substituted 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 |
| 6333331 | Substituted 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 |
| 6258809 | 6-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 |
| 6175008 | Processes 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 |
| 6166019 | Piperazinyl 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 |
| 6143743 | Imidazopyrimidines 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 |
| 6103707 | 9-(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 |
| 6075143 | Substituted 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 |
| 6046207 | Benzopyranopyrrole 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 |
| 6004966 | Use 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 |
| 6001844 | 4-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 |
| 5998456 | Benzimidazole 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 |
| 5994361 | Substituted 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 |
| 5958932 | Substitutes 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 |
| 5916894 | Substituted 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 |
| 5840729 | Xanthine 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 |
| 5807854 | Pyrimidone 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 |
| 5674998 | C-4' modified adenosine kinase inhibitors This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo2,3-d!pyrimidine and pyrazolo3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside ... | 10/07/1997 |
| 5538978 | 9-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 |
| 5527803 | 9-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 |
| 5525606 | Substituted 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 |
| 5516903 | Process 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 |
| 5506347 | Lyxofuranosyl 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 |
| 5393883 | Antiviral 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 |
| 5332814 | Process 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 |
| 5332744 | Substituted 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 |
| 5208240 | 8-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 |
| 5177074 | Angiotensin 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 |
| 5175167 | Hetarylalkenes, 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 |
| 5171353 | Sulfonamides 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 |
| 5158954 | Methyl -(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 |
| 5157026 | Oxo-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 |
| 5103007 | Lipids 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 |