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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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7291623 |
Compounds that interact with kinases
A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose...
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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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7217702 |
Selective antagonists of A2A adenosine receptors
Selective antagonists of A 2A adenosine receptors like those of formula I are provided, wherein Y forms a ring.
The novel A 2A blockers are useful for the treatment of Parkinsons disease and...
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7199127 |
Purine nucleosides
Disclosed are purine nucleoside compounds that are selective to A 3 adenosine receptors and are useful for the treatment of cancer and inflammatory diseases. The compounds are shown by the...
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7189730 |
A2A adenosine receptor antagonists
Disclosed are novel A 2A adenosine receptor antagonists of the formula:
wherein:
R 1 is optionally substituted aryl or optionally substituted heteroaryl; R 2 is optionally substituted...
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7148229 |
Sulfonamide substituted xanthine derivatives
The present invention is a sulfonamide substituted xanthine derivative of formula I:
or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl,...
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7135475 |
Amide substituted xanthine derivatives
The present invention is a 1,3,8 substituted xanthine derivative of formula I
or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and R 3 are as defined in the specification.
...
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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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7001910 |
Thiazolidinedione derivatives as antidiabetic agents
The present invention refers to compounds of the general formula (I), to their possible pharmaceutically acceptable salts and tautomeric forms. The present invention also refers to a process for...
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6969720 |
Biaryl substituted purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of...
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6964968 |
Method for the treatment or prevention of viral infection using nucleoside analogues
Viral infections selected from the group consisting of herpes simplex virus, varicella zoster virus, respiratory syncytial virus and cytomegalovirus can be treated by administering to the host a...
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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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6887880 |
Adenine based inhibitors of adenylyl cyclase, pharmaceutical compositions, and method of use thereof
The present invention relates to derivatives and analogues of adenine of the formula:
wherein L, A, Y and Z are those defined herein. Compounds of the present invention are useful in...
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6887879 |
Pharmaceutical combination of antiviral agents
In accordance with the present invention there is provided a pharmaceutical combination useful for the treatment of viral infections comprising a at least one antiviral active compound of formula...
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6812232 |
Heterocycle substituted purine derivatives as potent antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine derivatives which are inhibitors of cyclin/cdk complexes. The compounds of the current invention also are potent inhibitors of...
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6767906 |
2-amino-6-anilino-purines and their use as medicaments
This application discloses 2-amino-6-anilino-purine derivatives of the formula I in which q is 1-5, and R 1 is α) —S(═O) k —NR 6 R 7 , in which k is 1 or 2, wherein under the proviso...
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6677316 |
Adenosine derivatives and methods of administration
A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which...
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6653312 |
Amidine derivatives, their preparation and application as medicines and pharmaceutical compositions containing same
Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.
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6627633 |
6-substituted biaryl purine derivatives as potent cyclin/CDK inhibitors and antiproliferative agents
The compounds of the present invention are 2,6,9-trisubstituted purine inhibitors of cyclin/cdk complexes. The compounds also are potent inhibitors of human cellular proliferation. As such, the...
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6620796 |
Combinatorial library synthesis and pharmaceutically active compounds produced thereby
The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications,...
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6608069 |
Phenyl xanthine derivatives
The present invention relates to novel compounds of formula (I): wherein Z represents a 5 or 6 membered cycloalkyl, aryl, substituted cycloalkyl, or substituted aryl, said cycloalkyl, aryl,...
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6605600 |
Adenosine receptor antagonists and methods of making and using the same
The invention is based on the discovery that compounds of Formula I are unexpectedly highly potent and selective inhibitors of the adenosine A 1 receptor. Adenosine A 1 antagonists can be useful...
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6566365 |
Method for the treatment of Flaviviridea viral infection using nucleoside analogues
In accordance with the present invention there is provided a method for treating or preventing a Flaviviridea viral infection in a host comprising administering a therapeutically effective amount...
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6555518 |
Gemcitabine as an immunosuppressive pharmaceutical agent
The present invention provides the use of a compound of the formula I wherein: R 1 is a base defined by one of the formulae R 2 is hydrogen, C 1 -C 4 alkyl, bromo, fluoro, chloro or iodo; or...
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6537974 |
Method of treating arrhythmias
A method for treating arrhythmia in mammals is provided comprising administering a low dose of an adenosine receptor agonist of the Formula I: wherein R 1 is an optionally substituted...
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6479466 |
Compositions for treating viral infections, and methods therefor
Methods and combinations of an agent that promotes DNA synthesis in a virally-targeted cell and a nucleoside analogue having antiviral activity are provided for treating a viral infection in a...
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6469017 |
Method of inhibiting interleukin-12 signaling
A method for blocking IL-12 signaling by administration of the following compound: wherein, R 1 is H, CH 3 , sulfate, phosphate, or salt thereof; R 2 is alkyl (C 1-12 ), alkoxyalkyl (C 1-11 ),...
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6429208 |
Methods and compositions for restoring impaired cellular immune function
The effect of HIV components on lymphocytes, as exemplified by peripheral blood mononuclear cells (PBMC) in retarding their proliferation can be reversed by inhibiting the PKA/cAMP pathway. By...
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6423719 |
Method for treating benign prostate hyperplasia
A method of treating and/or preventing renal dysfunction in a patient, such as renal colic or contrast nephropathy by administering to a patient, a compound of the formula: is described herein....
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6413974 |
6,9,-disubstituted 2-&lsqb trans-(4-aminocyclohexyl) amino&rsqb purines
The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NH—, or H 2 N—R3— wherein R2 is selected from the group...
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6369066 |
Substituted 1,3-oxathiolanes with antiviral properties
This invention relates to single enantiomers of novel cis-substituted 1,3-oxathiolanes, of the formula (I): wherein; R 1 is hydrogen, and R 2 is cytosine or 5-fluorocytosine; and...
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6329381 |
Heterocyclic compounds
The present invention relates to a heterocyclic compound of the following general formula (I): ##STR1## wherein X is sulfur atom, oxygen atom or --NR 3 -- (R 3 may form a heterocyclic ring or...
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6313131 |
Method of kidney treatment
A method of treating and/or preventing renal dysfunction in a patient, such as renal colic or contrast nephropathy by administering to a patient, a compound of the formula: ##STR1## is described...
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6303618 |
Cyclin dependent kinase inhibiting purine derivatives
Method of treating a tumour or other cell proliferation disorder which comprises administering an effective amount of a purine compound which inhibits cyclic dependent kinase activity. Novel purine...
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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...
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6194391 |
3'-azido-2',3'-dideoxyuridine administration to treat HIV and related test protocol
It has been discovered that 3'-azido-2',3'-dideoxyuridine (CS-87) induces a transient mutation in HIV-1 at the 70 th codon (K to R, i.e., lysine to arginine) of the reverse transcriptase region of...
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6124288 |
Xanthines and their therapeutic use
The subject invention concerns a compound of the formula (i): ##STR1## in which Q represents heteroaryl or heterocyclo optionally substituted with one or more substituents selected from the group...
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6121270 |
Epoxide-containing compounds
Disclosed are enantiomers diastereomers, salts, solvates, hydrates and mixtures thereof, of formula I: ##STR1## The core moiety is non-cyclic or at least one five- to seven-membered ring, n is an...
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6103730 |
Amine substituted compounds
Compounds and pharmaceutical compositions, including resolved enantiomers and/or diastereomers, hydrates, salts, solvates and mixtures thereof, have the formula: CORE MOIETY--(R) j In these...
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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...
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6100271 |
Therapeutic compounds containing xanthinyl
Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula: CORE MOIETY --(R) j wherein j is an integer from one to three. The core moiety is...
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6075029 |
Xanthine modulators of metabolism of cellular P-450
A new class of xanthine compounds, variously substituted at the 1, 3, 7 and 8 positions, is characterized by an ability to modulate the activity of key enzymes involved in drug metabolism. These...
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6043250 |
Methods for using therapeutic compounds containing xanthinyl
Therapeutic compounds with at least one carboxylic acid, ester or amide-substituted side chain have the formula: CORE MOIETY --(R) j wherein j is an integer from one to three. The core moiety is...
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6043228 |
O.sup.6 -substituted guanine derivatives, a process for their preparation and their use in treating tumor cells
O 6 -hetarylalkyl- or naphthylalkylguanine derivatives of the formula ##STR1## wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR', wherein X is O or S, R" and R"' are alkyl, or substituted...
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6034087 |
Nucleoside derivatives and process for preparing thereof
Nucleoside derivatives represented by formula (I); ##STR1## wherein, R 1 represents hydrogen, phosphate or phosphonate group, R 2 represents substituted or unsubstituted pyrimidine or purine...
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6020339 |
Aryl furan derivatives as PDE IV inhibitors
The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the...
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5925643 |
Enantiomerically pure β-D-dioxolane-nucleosides
A method and composition for the treatment of humans infected with HIV that includes the administration of an HIV treatment amount of an enantiomerically pure β-D-dioxolanyl purine nucleoside of...
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5859017 |
Method for inhibiting mast cell and basophil activation
In a method for treating or preventing allergy or allergic disorders an effective amount of a compound that inhibits intracellular generation of phosphatidic acid and diacylglycerol is...
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5834474 |
Enantiomerically pure B--D--dioxolane nucleosides with selective anti-hepatitus B virus activity
A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a β-dioxolanyl purine nucleoside of the formula: ##STR1##...
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