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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...
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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...
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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...
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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;...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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.
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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...
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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...
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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,...
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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...
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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. ...
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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...
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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...
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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...
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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...
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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...
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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;...
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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...
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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...
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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...
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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 ...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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.
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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,...
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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...
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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...
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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...
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