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7618974 Gyrase inhibitors and uses thereof  
The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions...
7618969 Compounds which potentiate glutamate receptor and uses thereof in medicine  
Compounds of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof, are disclosed: wherein R 1 is C 1-6 alkyl, haloC 1-6 alkyl, C 2-6 alkenyl, amino, monoC 1-4...
7608618 Urea or thiourea substituted 1,4-pyrazine compounds useful as anti-cancer agents and for inhibiting Chk1  
Compounds of the formula wherein: Y′ is O or S, W′ is optionally substituted, Z′ is selected from the group consisting of wherein Q′ is OR 7 and R 7 is C 1-3 alkyleneC 3-8...
7605156 Methods for the use of inhibitors of cytosolic phospholipase A2  
This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the...
7595317 Barbituric acid derivatives as inhibitors of TNF-α converting enzyme (TACE) and/or matrix metalloproteinases  
The present application describes novel barbituric acid derivatives of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, L, R 1 , R 2 , R 3 , R 4 , R 5 , n,...
7592353 Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses  
Disclosed are compounds of formula (I): wherein R 1 and R 4 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are...
7592337 Di-aryl substituted tetrazole modulators of metabotropic glutamate receptor-5  
Tetrazole compounds substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring,...
7589115 Derivatives of [6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-sulfonylamino]-propionamide  
Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-pro pionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the...
7589096 Azole derivatives  
The present invention relates to a compound of the formula (I): wherein Az is a group comprising a monocyclic azole or a bicyclic aromatic ring of the same or different fused azoles; T, U, V...
7589095 4-phenyl-pyrimidine-2-carbonitrile derivatives  
The invention relates to 4-phenyl-pyrimidine-2-carbonitrile derivatives having the general formula I wherein each of the substituents is given the definition as set forth in the specification...
7589088 Pyrimidine-based inhibitors of dipeptidyl peptidase IV and methods  
Compounds are provided having the formula (I) wherein R, B, X and Y are as defined herein.
7585866 Protein tyrosine kinase inhibitors  
The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal...
7582641 Gyrase inhibitors and uses thereof  
The present invention relates to methods of treating, preventing, or lessening the severity of resistant bacterial infections in mammals, utilizing compounds of formula I or formula VII or...
7582640 Vitronectin receptor antagonist derivatives, method for preparing same, use thereof as medicines and pharmaceutical compositions containing same  
A subject of the invention is the compounds of formula (I): in which R 1 , R 2 , R 3 , R 4 and G have the meanings indicated in the description, their preparation process, their use as...
7582632 Tri(cyclo) substituted amide compounds  
Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
7579465 Antiviral agents  
This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the...
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...
7579353 Pyridinone derivatives against malaria  
4-pyridone derivatives of Formula (I) and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations thereof and their use in chemotherapy of...
7576209 Inhibitors of Akt activity  
The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The...
7576089 3-cycloalkylaminopyrrolidine derivatives as modulators of chemokine receptors  
The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , X, Y and Z are as defined herein) which are useful...
7576053 Methods and compositions for treating degenerative bone disorders  
The present disclosure provides methods and compositions using Syk inhibitory compounds for treating degenerative bone disorders and as prophylactic treatment to prevent bone loss. These treatments...
7572793 3-Substituted-4-pyrimidone derivatives  
A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R 1 represents...
7569688 Propane-1, 3-dione derivative  
Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione...
7569604 Heterocyclic derivatives for modulation of calcium channels  
Heterocyclic derivatives act as Ca channel antagonists. The compositions are useful for treating or relieving Ca channel mediated conditions.
7569591 Gyrase inhibitors and uses thereof  
The present invention relates to compounds that inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions...
7569590 Use of thianecarboxamides as dgat inhibitors  
The present application describes methods of treating obesity using DGAT-1 inhibitors according to Formula I: including all prodrugs, solvates, pharmaceutically acceptable salts and...
7566730 Substituted aminoethers for the treatment of Alzheimer's disease  
The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful...
7563807 Removal of aldehyde impurity by reactive polystyrene resini  
A purification method in the preparation of a substituted 8-arylquinoline, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, utilizes a polystyrene-based...
7563787 Substituted pyrazole compounds  
Disclosed are protein kinase inhibitors, compositions comprising such inhibitors, and methods of use thereof. More particularly, disclosed are inhibitors of Aurora A (Aurora-2) protein kinase. Also...
7560464 Polycyclic pyrimidines as potassium ion channel modulators  
The present invention provides a genus of polycyclic pyrimidines that are useful as modulators of potassium ion channels. The modulators of the invention are of use in both therapeutic and...
7547700 Aryl-[4-halo-4(heteroarylmethylamino)-methyl]-piperidin-1-1yl]-methanone derivatives, methods for production and use thereof as medicaments  
The invention relates to compounds of general formula (1) in which X and Y=a carbon with a bonded hydrogen atom (CH) or a nitrogen atom, A=a methyl, fluoromethyl, cyano, hydroxyl, methoxy group, or...
7544688 Hetereoaryl nitrile derivatives  
The invention provides compounds of Formula (I) or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use...
7544675 Chemical compounds with dual activity, processes for their preparation and pharmaceutical compositions  
The present invention concerns chemical compounds combining affinity and antagonism against the human m3 muscarinic receptor with activity as selective phosphodiesterase IV (PDE IV) inhibitors,...
7541361 N-[4,5-diphenylpyrimidin-2-yl)methyl]amine derivatives, the preparation thereof and their therapeutic use  
The invention relates to compounds of formula (I): Wherein X, R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. The invention also relates to a method for preparing the aforementioned...
7541357 Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin  
The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused...
7538138 Amines as histamine-3 receptor ligands and their therapeutic applications  
Compounds of formula (I) or a pharmaceutically acceptable salts or prodrug thereof which are useful for the modulation of the histamine-3 receptors in mammals and which are useful for the...
7534798 Vanilloid receptor ligands and their use in treatments  
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster...
7531541 Partial mGluR5 antagonists for treatment of anxiety and CNS disorders  
Provided is a method of treating conditions and disorders for which full mGluR5 antagonists are potentially effective, such as, e.g., anxiety, epilepsy, schizophrenia and other psychotic disorders,...
7528149 Respiratory syncytial virus replication inhibitors  
This invention concerns compounds of formula (I) prodrugs, addition salts, or stereochemically isomeric forms thereof for use as, inter alia, respiratory syncytial virus replication inhibitors;...
7528133 Use of thiazolidinediones derivatives for preventing uterine contractions in premature labour or lactation  
The present invention provides methods of preventing or reducing oxytocin-mediated action by using a thiazolidinedione, such as troglitazone, or thiazolidinedione-like compounds. These methods...
7524849 5-arylpyrimidines as anticancer agents  
This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof,...
7517902 Substituted indazoles, compositions containing the same, and the preparation and use thereof  
Disclosed are novel substituted indazole compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising such compounds.
7514446 Pyrimidine compounds  
The present invention provides compounds of formula (I): wherein all variables are as defined herein, pharmaceutical compositions containing the same, processes for preparing the same and their...
7511125 Pyrimidine derivatives for labeled binding partners  
Compounds having structure (1) wherein R 1 is —H a protecting group, a linker or a binding partner; and R 2 and R 34 are as defined in the specification. The invention also provides...
7511034 Dialkylhydroxybenzoic acid derivatives containing metal chelating groups and their therapeutic uses  
Novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups are disclosed. The novel compounds are used as therapeutics for treating and/or preventing various medical...
7507738 5-protected aminopyrimidine compound, production method thereof and intermediate therefor  
The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with...
7507733 11b-HSD1 inhibitors for the treatment of diabetes  
Compounds of the formula (I): as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 to R 5 have the significance given in claim 1 can be used in the form of...
7504501 Antiprotozoal imidazopyridine compounds  
Compounds described by the Formula (I): (I) or pharmaceutically acceptable salts, or N-oxides thereof. The compounds are useful for the treatment and prevention of protozoal diseases in mammals and...
7504402 Triazole derivatives as inhibitors of 11-β-hydroxysteroid dehydrogenase-1  
Triazole derivatives of structural formula I are selective inhibitors of the 11β-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as...
7501407 Pyrimidine A2B selective antagonist compounds, their synthesis and use  
The subject invention provides compounds having the structure: wherein R 1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5...