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8163761 |
Methods and compositions for treating disorders
Compounds and compositions for treating disorders related to TRPA1 are described herein.
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8163762 |
Purine derivatives having, in particular, anti-proliferative properties, and their biological uses
This invention provides 2-, 6, and 9-substituted purine derivatives, particularly 2(1-R hydroxymethylpropylamino)-6-benzylamino-9-isopropyl purine, having, in particular, antiproliferative...
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8163754 |
Purine derivatives for use as adenosine A-2A receptor agonists
Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine...
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8153640 |
HIV inhibiting bicyclic pyrimdine derivatives
HIV replication inhibitors of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein-a1=a2-a3=a4- is —CH═CH—CH═CH—, —N═CH—CH═...
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8153628 |
Pyrazolyl substituted xanthines
The present invention provides compounds and pharmaceutical compositions that are substituted xanthines of formula I: or pharmaceutically acceptable salts thereof, wherein: Z is selected from the...
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8143249 |
Prodrugs of A2B adenosine receptor antagonists
Disclosed are prodrugs of A2B adenosine receptor antagonists of the formula: wherein R1 and R2 are independently lower alkyl; R4 is optionally substituted phenyl; X is hydrogen or methyl; and Y is...
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8143264 |
Xanthine derivatives as selective HM74A agonists
The present invention relates to a xanthine compound derivative which is 3-butyl-8-chloro-1-(3-{5-[(4-fluorophenyl)methyl]-2H-tetrazo
l-2-yl}propyl)-3,7-dihydro-1H-purine-2,6-dione: a...
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8138172 |
8-oxoadenine derivatives acting as modulators of TLR7
The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as...
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8114877 |
Organic compounds
Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine...
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8071565 |
Purine derivatives as a2a agonists
Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating...
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8071609 |
Unsaturated heterocyclic derivatives
This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable...
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8067413 |
9-substituted-8-oxo-adenine compounds as toll-like receptor (TLR7 ) modulators
The present invention provides compounds of formula (I) wherein R1, Y1, X1, L and R2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for...
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8067411 |
Compounds
The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions...
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8063051 |
9-substituted-8-oxo-adenine compounds as toll-like receptor (TLR7) modulators
The present invention provides compounds of formula where n, R1, R2, A, X1, Y1, Z1, X2 and Y2 are as defined in the specification, processes for their preparation, pharmaceutical compositions...
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8058281 |
Use of adenine-derived compounds for the treatment of lupus
The present invention is directed to a method of treating systemic lupus erythematosus comprising administering a compound of formula (I) whereinR1 is selected from the group consisting of CF3, a...
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8044056 |
Adenine compound
A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated...
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8044061 |
8-alkynylxanthines and derivatives
Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the...
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8026244 |
Thioxanthine derivatives and their use as inhibitors of MPO
There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their...
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7989459 |
Purinones and 1H-imidazopyridinones as PKC-theta inhibitors
A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKCθ. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I: whereinR1 is ...
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7968544 |
Modulators of toll-like receptor 7
The present application includes a compound of Formula I or II: or a pharmaceutically acceptable-salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods...
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7968556 |
Heteroaryl compounds, compositions thereof, and methods of treatment therewith
Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl...
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7919490 |
6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection....
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7915268 |
8-substituted 2-(benzimidazolyl)purine derivatives for immunosuppression
The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory diseases, mast cell mediated disease and transplant rejection. The...
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7902187 |
6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection....
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7888343 |
Substituted, bicyclic 8-pyrrolidinoxanthines, and methods for their use as inhibitors of dipeptidyl peptidase
The present invention involves substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are defined herein. The present invention also comprises...
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7884109 |
Purine and imidazopyridine derivatives for immunosuppression
The present invention provides novel purine and imidazopyridine derivatives useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and...
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7879864 |
Substituted 8-aminoalkoxy-xanthine compounds and compositions useful in the treatment of hyperlipidemia and diabetes
Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed which are inhibitors of the enzyme dipeptidyl peptidase IV...
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7837998 |
Anti-cancer activity of an anti-thymidine kinase monoclonal antibody
Monoclonal antibodies to thymidine kinase 1 are disclosed which are useful in methods of detecting, diagnosing, and treating cancer.
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7838528 |
Substituted bicyclic 8-pyrrolidinoxanthines, methods for their production, pharmaceutical formulations and their use
Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed and comprise novel substituted bicyclic...
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7795269 |
A2B adenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal...
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7795268 |
Method of treating hepatic disease using A2B adenosine receptor antagonists
The invention is related to methods of treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment of liver damage caused by alcohol abuse, surgical...
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7790730 |
Imidazo[4,5-d]pyrimidines, their uses and methods of preparation
The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one compound having the general formula...
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7781432 |
Analogs of nitrobenzylthioinosine
Analogs or derivatives of nitrobenzylthioinosine corresponding to formula I: in which R represents an unsubstituted or mono- or polysubstituted phenyl, benzyl or heteroaryl group or a phenyl group...
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7772226 |
Condensed imidazole derivatives
The present invention is related to compounds represented by the following formula, or salts or hydrates thereof wherein,T1 represents a 4- to 12-membered heterocyclic group containing one or two...
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7767685 |
Adenosine A2B receptor antagonists
The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the...
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7767670 |
Substituted 3-carboxamido isoxazoles as kinase modulators
The invention provides methods and compositions for treating conditions mediated by various kinases wherein substituted 3-carboxamido isoxazoles compounds are employed. The invention also provides...
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7763625 |
Agents for treating migraine
A method for treating migraine comprising administering, as an active ingredient, a xanthine derivative represented by the following formula or a pharmaceutically acceptable salt thereof.
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7759355 |
Adenosine A2A receptor antagonists for treating restless legs syndrome or nocturnal myoclonus
The present invention provides methods of treating restless legs syndrome or related disorders, comprising administering an effective amount of at least one adenosine A2A receptor antagonist to a...
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7754728 |
Adenine compound and use thereof
A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the...
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7741331 |
A2B adenosine receptor antagonists
Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal...
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7732455 |
Substituted 8-heteroaryl xanthines
Selective antagonists of A2B adenosine receptors like those of formula I are provided. These compounds and compositions are useful as pharmaceutical agents.
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7723340 |
Haloaryl substituted aminopurines, compositions thereof, and methods of treatment therewith
Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and...
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7662827 |
Pyrazole derivatives having tyrosine kinase inhibitory activity
Compounds of the formula (I), in which R, X, R1, R2, R3 and R4 have the meanings indicated in Claim (1), are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be...
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7659278 |
Use of low molecular weight compounds for preparing a medicament useful in treating mutant p53 mediated diseases
The present invention provides novel compounds, corresponding to formulae I and II, respectively, which are able to reactivate the apoptosis-inducing function of mutant p53 proteins. This...
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7642267 |
Benzimidazole and pyridylimidazole derivatives
This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. The invention is particularly related to such...
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7625881 |
Prodrugs of A2B adenosine receptor antagonists
Disclosed are prodrugs of A2B adenosine receptor antagonists, having the following structure and their use in treating mammals for various disease states.
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7618962 |
Pyrazolyl substituted xanthines
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula I which are selective antagonists of A2B adenosine receptors (ARs)....
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7601713 |
Kinase inhibitors and their uses
The present disclosure provides compounds that inhibit protein kinases, such as JAK, Axl, or Syk kinases, compositions comprising the compounds and methods of using the compounds to inhibit protein...
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7579348 |
Derivatives of 8-substituted xanthines
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I which are selective antagonists of A2B adenosine receptors (ARs)....
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7572800 |
Combination therapy to treat hepatitis B virus
The present invention is directed to a method for treating hepatitis B virus infection in humans comprising administering a synergistically effective amount of agents having known anti-hepatitis B...
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