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7601835 Preparation of famciclovir and other purine derivatives  
Purine derivatives of formula I, substituted at the 9-position, are prepared from a chloro substituted purine starting material, first making an alkyl substitution at the 9-position, then forming...
7595401 Therapeutic compounds and their use in cancer  
The invention relates to compounds of Formula I and their therapeutic uses, wherein substituent A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carboxylic...
7498334 Pyrrolopyrimidines as phosphodiesterase VII inhibitors  
Pyrrolopyrimidine derivatives of the formula I in which R 3 , R 4 , R 5 , R 6 and X are as defined in claim 1 , act as phosphodiesterase VII inhibitors and can be employed for the treatment...
7470784 Methods for synthesizing 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin-6-amine  
2-Chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-9H-purin -6-amine is synthesized by reacting a 2-chloro-6-substituted purine with a protected and activated 2-deoxy-2-fluoro-D-arabinofiranose;...
7452894 Purine derivatives as purinergic receptor antagonists  
Use of a compound of formula (I) wherein R 1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR 5 R 6 , NR 4 COR 5 , NR 4 CONR 5 R 6 , NR 4 CO 2 R 7 and NR 4 SO 2 R...
7439359 Small molecule compositions for binding to hsp90  
Structural differences in binding pockets of members of the HSP90 family can be exploited to achieve differential degradation of kinases and other signaling proteins through the use of designed...
7439240 Purine-or pyrrolol[2,3-d]pyrimidine-2-carbonitiles for treating diseases associated with cysteine protease activity  
The present invention therefore provides a compound of formula (I) and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of...
7393855 2,2-bis-(hydroxymethyl)cyclopropylidenemethyl-purines and pyrimidines as antiviral agents  
Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include...
7388002 Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases  
Compounds represented by the formula: A is (CH 2 ) n R 2 , —CH═CH 2 , CH 2 —CH═CH 2 , O(CH 2 ) n R 2 , CH(OH)CH 3 , CH(OH)CH 2 OH, CH 2 —CH(OH)CH 3 , CH 2 CH(OH)CH 2 OH, or...
7358235 Analogs 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...
7351827 Substituted oxetanes, method of making, and method of use thereof  
Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog...
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...
7285558 Pyrazolo[3,4-d]pyrimidines inhibiting H. pylori infections  
Compounds having the general formula and pharmaceutical compositions containing them, and their use in the treatment or prophylaxis of H. pylori infection.
7256196 Purine cytokine inhibitors  
The present invention relates to 2,8,9-substituted purines which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian...
7253154 Substituted thiazolopyrimidines as xanthine oxidase inhibitors  
The invention relates to compounds of the following formula (I) or their salts: in which R 1 represents OR 4 or others, in which R 4 is an alkyl group having 1-8 carbon atoms which may have...
7241890 Purine analogs having HSP90-inhibiting activity  
Novel purine compounds of Formula I. and tautomers, pharmaceutically acceptable salts, and prodrugs thereof, wherein X is S, S(O), or S(O) 2 ; and O is selected from alkyl, cycloalkyl,...
7176312 Kinase inhibitor scaffolds and methods for their preparation  
General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic...
7129239 Purine compounds and uses thereof  
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein. ...
RE39112 Purine derivatives and adenosine A2 receptor antagonists serving as preventives/remedies for diabetes  
The present invention provides a preventive or therapeutic agent of a new type for diabetes mellitus and diabetic complications on the basis of an adenosine A2 receptor antagonist action. A purine...
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...
6991902 Nucleobase heterocyclic combinatorialization  
Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic...
6974815 Hexahydro-benzimidazolone compounds useful as anti-inflammatory agents  
The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K is O or S; Q is —C(═O)— or optionally substituted C...
6962921 Dementia remedies containing 2-aryl-8-oxodihydropurine derivatives as the active ingredient  
Medicines for treatment or prevention of dementia comprising 2-aryl-8-oxodihydropurine derivatives of the formula (I): wherein W is H, C 1-6 alkyl, halogen, C 1-6 alkoxy, or the like; X is...
6949640 Method 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;...
6949535 Inhibitors of human phosphatidyl-inositol 3-kinase delta  
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role...
6936602 Benzazepine derivatives, process for the preparation of the same and uses thereof  
Compounds of the general formula (I): or salts thereof, which exhibit CCR5 antagonism and exert preventive and therapeutic effects against HIV infections: wherein R 1 is a 5- to 6-membered...
6919332 N-substituted-heteroaryloxy-aryloxy-pyrimidine-2,4,6-trione metalloproteinase inhibitors  
The present invention relates to N-substituted-heteroaryloxy-aryloxy-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, A, Y, B, G, and R 1 are as defined in the...
6919455 Purine derivative dihydrate, drugs containing the same as the active ingredient and intermediate in the production thereof  
A compound represented by the following formula (I), or a salt thereof: where X is a halogen atom or a group represented by —S—(CH 2 ) n —A, —SO—(CH 2 ) m —B, —SO 2 —(CH 2 ) m ...
6906190 Inhibitors for de novo-RNA polymerases and methods of identifying targets for same  
A polymerase inhibitor has first moiety coupled to a second moiety via an optional linker in which the first moiety binds to an initiation nucleotide binding site of a polymerase and forms at least...
6897201 Compositions and methods for the treatment of glaucoma or ocular hypertension  
The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a...
6894045 Tetrahydropurinones and derivatives thereof as corticotropin releasing factor receptor ligands  
Compounds provided herein are novel substituted tetrahydropurinones of Formula (I): wherein R 3 is aryl substituted with 0-5 X Ar or heteroaryl substituted with 0-4 X hAr . Such compounds...
6864254 Inhibitor for 20-hete-yielding enzyme  
An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is...
6855821 Processes for preparing 1,3-dioxolane nucleosides  
Disclosed are novel processes for preparing 1,3-dioxolane nucleosides of general formula I and II: wherein B is a purine or pyrimidine base or an analog or derivative thereof. The invention...
6849735 Methods of synthesis for 9-substituted hypoxanthine derivatives  
An improved method of synthesis of a 9-substituted hypoxanthine derivative comprises the steps of: (1) reacting aminocyanacetamide with triethyl orthoformate to form an imidoester derivative of...
6800620 Inhibitors of human phosphatidylinositol 3-kinase delta  
Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3Kδ plays a role...
6790841 2-hydroxymethylcyclopropylidenemethylpurines and -pyrimidines as antiviral agents  
Compounds which are active against viruses have the following Formulas: wherein B is a purine or pyrimidine heterocyclic ring and is preferably selected from the group consisting of...
6770645 Pharmaceutically active compounds  
Compound of general formula I: wherein R 1 , R 2 , R 3 , R 4 , X, Y and R 5 have the meanings given herein which are useful in the curative and prophylactic treatment of a medical condition for...
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, W a , G and G a have the meanings given in the patent claims, and their physiologically tolerable salts and...
6713623 Tetraphosphonate bicyclic trisanhydrides  
Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.
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,...
6590107 Synthesis, anti-human immunodeficiency virus, and anti-hepatitis B virus activities of 1,3-oxaselenolane nucleosides  
A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an...
6562969 Ricin inhibitors and methods for use thereof  
Ricin A-chain is an N-glycosidase that attacks ribosomal RNA at a highly conserved adenine residue. Crystallographic studies show that not only adenine and formycin, but also pterin-based rings can...
6555545 Adenosine A2A receptor antagonists for treating and preventing hepatic fibrosis, cirrhosis and fatty liver  
Hepatic cirrhosis and fibrosis and fatty liver can be prevented and treated by administering to a subject in need thereof an effective amount of at least one adenosine A 2A receptor antagonist or...
6489333 Integrin antagonists  
This invention relates to novel heterocycles which are useful as antagonists of the α v β 3 integrin, the α 2b β 3 integrin, and related cell surface adhesive protein receptors, to...
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 wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH 2 , O,...
6437125 Process for the production of purine derivatives  
The invention provides a method of rearranging a compound of formula (I), wherein R and R′ are selected independently from hydrogen and C 1-12 alkyl; and R 1 and R 2 are selected independently...
6436989 Prodrugs of aspartyl protease inhibitors  
The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl...
6433134 Peptide nucleic acid precursors and methods of preparing same  
Novel and efficient syntheses create novel piperazinone intermediates which facilitate the production and use of PNAs. Such syntheses and the products enhance the feasibility of a system which...
6407237 Crystal forms of 9-substituted hypoxanthine derivatives  
The bifunctional compound N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide monopotassium salt occurs in a number of crystal forms which differ in their stability. Of these forms, the most...
6372740 2-aryl-8-oxodihydropurine derivative, process for the producing the same, medicinal compositions containing the same, and intermediates thereof  
2-Aryl-8-oxodihydropurine derivative of the following formula (I): wherein W is H, lower alkyl, halogen, lower alkoxy, amino, mono- or di-lower alkylamino, or substituted or unsubstituted...
Matches 1 - 50 out of 255 1 2 3 4 5 6 >