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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...
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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,...
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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...
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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...
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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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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...
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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...
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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....
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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...
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7572799 |
Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors
This invention relates to compounds of formula (I)
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7569572 |
Pyrazolo[4,3-D]pyrimidines
This invention relates to compounds of formula (I).
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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...
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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.
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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...
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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...
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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),...
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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...
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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...
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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.
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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,...
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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...
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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.
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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...
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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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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...
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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...
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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...
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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...
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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...
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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...
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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 ...
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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...
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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.
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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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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
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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...
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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...
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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.
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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.
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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...
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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.
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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...
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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...
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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...
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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...
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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
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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...
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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...
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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...
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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...
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