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7618976 Methods for the production of sildenafil base and citrate salt  
Provided are processes for the preparation of sildenafil base and the citrate salt of sildenafil. Also provided are sildenafil citrate water adduct and a method of preparing pharmaceutical...
7615558 6-arylmethylprazolo[3,4-d]pyrimidines  
Described are 6-arylmethylpyrazolo[3,4-d]pyrimidines of the following formula: processes for their preparation and their use for producing medicaments for improving perception, concentration,...
7608603 Substituted pyrazolo[3,4-D]pyrimidines as p38 MAP kinase inhibitors  
Compounds of formula Ia, Ib, Ic, Id, Ie, If, Ig or Ih: wherein X and Y are nitrogen or one of X and Y is nitrogen and the other is CR g , and W, D, E, R 4 , R 5 , R 6 and R g are as defined...
7601726 Substituted pyrazolo[3,4-d]pyrimidines as p38 MAP kinase inhibitors  
Compounds of formula Ia or Ib: wherein A, W, X, Y, R 1 , R 2 , R 3 and R 4 are as defined herein. Also disclosed are methods of making the compounds and methods of using the compounds for...
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...
7598244 [1,2,4]triazolo[1,5,a]pyrimidin-2-ylurea derivative and use thereof  
Novel [1,2,4]triazolo[1,5-a]pyrimidine derivative of the general formula (1): (1) its prodrug or a pharmaceutically acceptable salt thereof, which exhibits an antigen presentation inhibiting...
7589086 Substituted pyrazolo[3,4-D]pyrimidines as anti-tumor agents  
The present invention provides a compound of pyrazolo[3,4-d]pyrimidine having the formula wherein: X=N; R=H, alkylthio, or aminoalkylthio; R 1 =NHcyclopropyl, NHC 3 H 7 , NHC 4 H 9 , N(CH 2 CH...
7585868 Substituted pyrazolo[3,4-D]pyrimidines as kinase antagonists  
The present invention provides novel compounds that can be used as antagonists of a lipid kinase such as a PI3 kinase, protein tyrosine kinase, and/or protein serine-threonine kinases such as mTOR....
7579355 Inhibitors of Akt activity  
The present invention is directed to compounds which contain a substituted pyridine moeity which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to...
7572799 Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors  
This invention relates to compounds of formula (I)
7569572 Pyrazolo[4,3-D]pyrimidines  
This invention relates to compounds of formula (I).
7569571 Substituted pyrazolo [3,4-d]pyrimidines as cytokine modulators  
Provided are bicyclic heterocycle-based p38 kinase, including p38α and p38β kinase, inhibitors. Pharmaceutical compositions containing the compounds are also provided. Methods of use of the...
7566708 Substituted pyrazolo{3,4-D}pyrimidines as p38 map kinase inhibitors  
Compounds effective as p38 MAP kinase inhibitors, methods of making the compounds, and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
7563800 Substituted pyrazolo[3,4-D]pyrimidines as p38 map kinase inhibitors  
Compounds of formula Ia or Ib: wherein R 1 , R 2 , R 3 and R 4 are as defined herein. Also disclosed are methods of making the compounds and methods of using the compounds for treatment of...
7563799 Substituted pyrazolo[3,4-D]pyrimidines as p38 map kinase inhibitors  
Compounds of the formula Ia or Ib: wherein X and Y are N or one of X and Y is N and the other is CR g , and A, D, E, G, W, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Also disclosed...
7553839 5h-pyrrolo[3,2-D] pyrimidine inhibitors of nucleoside phosphorylases and nucleosidases  
The present invention relates to compounds of the general formula (I) which are inhibitors of purine muclioside phosphorylases (PNP), purine phosphoribosyltransferases (PPRT),...
7528140 Substituted pyrrolo[3,2-d]pyrimidines as glycogen synthase kinase (GSK) inhibitors  
The invention provides pyrrolo[3,2-d]pyrimidine derivatives represented by formula (I), and their medically acceptable salts. The compounds of the invention exhibit GSK-3 inhibiting activity and...
7524845 Azaindazole compounds and methods of use  
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in...
7470693 Oxalamide derivatives as kinase inhibitors  
The invention is directed to compounds having the following Formula I: and methods of using them for the treatment of proliferative diseases.
7452893 4-cycloakylaminopyrazolo pyrimidine NMDA/NR2B antagonists  
Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are effective as NMDA/NR2B antagonists useful for treating neurological conditions such as, for example, pain,...
7452880 Substituted pyrazolo [3,4-d] pyrimidines and methods of using the same  
Compounds of the formula I: where A, B, X, Y, Z, k, R 1 , R 2 and R 3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing...
7439345 Supramolecular pairing system, its preparation and use  
The invention relates to conjugates including at least one linker, a biomolecule coupled to the linker, and cyclohexane derivatives of the following formula: and oligomers thereof.
7439246 Fused heterocyclic kinase inhibitors  
In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase...
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...
7435731 Substituted pyrazolo[3,4-d]pyrimadines and methods of using the same  
Compounds of the formula Ia or Ib: wherein A, B, X, Y, Z, W, k, R 1 , R 2 , R 3 , R 4 and R 5 are those defined herein, and compositions comprising the same. The present invention also...
7425630 Processes for preparing pyrazolo[3,4-d]pyrimidine ethers  
The present invention relates to processes for preparing pyrazolo[3,4-d]pyrimidine ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic...
7407962 Heteroaryl compounds useful as inhibitors or protein kinases  
The present invention provides compounds that are inhibitors of protein kinase, particularly inhibitors of ERK2, GSK3, PKA, CDK2 protein kinases, mammalian protein kinases involved in proliferative...
7405220 Pyrazolopyrimidines  
Novel pyrazolopyrimidines of formula (I): are discussed. These pyrazolopyrimidines are capable of inhibiting the activity of cyclin-dependent kinases, most particularly cyclin-dependent kinase...
7384952 Pyrazolopyrimidine compound and a process for preparing the same  
The present invention provides a novel pyrazolopyrimidine compound of the formula [I]: wherein R′ is (A) a substituted aryl group, (B) an optionally substituted nitrogen-containing aliphatic...
RE40332 Fungicidal trifluoromethylalkylamino-triazolopyrimidines  
The novel compounds of formula I: wherein (R 1 , R 2 , Hal and L 1 through L 5 are defined in the specification) show selective fungicidal activity. The new compounds may be processed with...
7351826 Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds  
The invention provides compounds of Formula (I) that bind to GABA A receptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABA A ...
7339054 Process for preparing branched ribonucleosides from 1,2-anhydroribofuranose intermediates  
A process is provided for the preparation of branched-chain ribonucleosides of formula (I): from the 1,2-anhydroderivatives of formula (II). wherein PG is a hydroxyl protecting group, B is...
7332497 Pyrazolopyrimidines as therapeutic agents  
The present invention provides compounds of Formula I, including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R a , R 2 , and R 3 are defined as described herein.
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.
7268133 Cannabinoid receptor ligands 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
7268128 1,3,5-trisubstituted-5-phenyl and 5-pyridyl pyrazolopyrimidinone derivatives having PDE7 inhibiting action  
Pyrazolopyrimidinone derivatives expressed by the following general formula (IA) or (IB): where the symbols are as disclosed in the specification, are provided as desired compounds. These...
7262192 Substituted pyrazolo[4,3-d]pyrimidines and their use as PDE-5 inhibitors  
The present invention comprises a class of 5,7-diaminopyrazolo[4,3-d]pyrimidine compounds. These compounds are useful as phosphodiesterase type 5 inhibitors. The present invention further comprises...
7259165 Heterocyclyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands  
The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.
7259157 N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B Antagonists  
Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
7230100 Stereoselective method for the preparation of nucleosides  
A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): wherein R1 is a pyrimidine base or a pharmaceutically acceptable derivative thereof...
7217710 Substituted pyrazolopyrimidines  
Pyrazolo-pyrimidine derivatives are described herein. The described invention also includes methods of making such derivatives as well as methods of using the same in the treatment of diseases.
7176311 Process for preparing pharmaceutically active compounds  
A process for the preparation of Compounds of the formula (1): wherein R 1 , R 2 , R 4 and R 13 are as defined or a pharmaceutically or veterinarily acceptable salt or polymorph thereof, or a...
7173039 Protein kinase inhibitors  
Disclosed are compounds which inhibit or modulate the activity of protein kinases and pharmaceutical compositions containing such compounds. The disclosed compound contain two or more ligand...
7148350 Compounds in the form of homodimeric or heterodimeric pro-drugs; process for obtaining these pro-drugs and their acceptable pharmaceutical salts and use of compounds in the treatment of phosphodiesterases-mediated diseases or dysfunction  
The present invention describes new homo or heterodimer prodrugs wherein both active monomeric units are compounds of the formula: where R 1 and R 2 are each independently —H, —C 1 –C 6...
7148228 Pyrazolopyrimidines and related analogs as HSP90-inhibitors  
A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R 1 is halogen, —OR 1 , —SR 11 or...
7141669 Cannabiniod receptor ligands 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
7135493 HDAC inhibitor  
A compound having the following formula (I): wherein R 1 is N-containing heterocyclic ring optionally substituted with one or more suitable substituent(s), R 2 is hydroxyamino, R 3 is...
7132426 Fused-aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto  
The present invention relates to certain fused aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the...
7101884 Tyrosine kinase inhibitors  
The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to...
7087754 Pyrazolo[3,4-d]pyrimidine derivatives and their use as purinergic receptor antagonists  
Use of a compound of formula (I): wherein R 1 is selected from alkyl, alkoxy, aryloxy, alkylthio, arylthio, aryl, halogen, CN, NR 6 R 7 , NR 5 COR 6 , NR 5 CONR 6 R 7 , NR 5 CO 2 R 8 and NR 5 SO...
Matches 1 - 50 out of 215 1 2 3 4 5 >