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7414131 Bicycloheteroarylamine compounds as ion channel ligands and uses thereof  
Amine compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of...
7407964 Caspase inhibitors and uses thereof  
This invention provides novel caspase inhibitors of formula I: wherein R 1 is hydrogen, CHN 2 , R, or —CH 2 Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group,...
7407957 Phthalazinone derivatives  
A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic...
7407955 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions  
The present invention relates to substituted xanthines of general formula wherein R 1 to R 3 are defined as in claims 1 to 16 , the tautomers, the stereoisomers, the mixtures, the prodrugs...
7407950 N-(heteroaryl)-1H-indole-2-carboxamide derivatives and their use as vanilloid TRPV1 receptor ligands  
The invention concerns compounds of general formula (I), wherein n, X 1 , X 2 , X 3 , X 4 , Z 1 , Z 2 , Z 3 , Z 4 , Z 5 and W are as defined herein. Said compounds are ligands of the TRPV 1 ...
7405215 Indole acetic acids exhibiting CRTH2 receptor antagonism and uses thereof  
The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of...
7402580 Fused pyridazine derivative compounds and drugs containing these compounds as the active ingredient  
Fused pyridazine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof (wherein each symbol has the meaning as defined in the specification.). Because of...
7393847 Imidazopyridazinediones, their preparation and their use as pharmaceutical compositions  
The invention relates to substituted imidazopyridazinediones of general formula wherein R 1 and R 4 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures...
7390808 Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes  
The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of...
7390806 Antibiotics containing borinic acid complexes and methods of use  
The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of...
7388006 Non-steroidal progesting  
The present invention relates to non-steroidal progestins of the general formula (I) wherein R 1 and R 2 are independently of each other —H or —F, R 3 is —CH 3 or —CF 3 , and Ar is...
7384942 Pyrazine based inhibitors of glycogen synthase kinase 3  
New bicyclic based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The...
7378420 Urea derivatives as calcium channel blockers  
Derivatives of urea that contain piperazine rings and additional substitution with aromatic groups are effective in ameliorating conditions associated with unwanted calcium ion channel activity.
7378418 Azabicyclic heterocycles as cannabinoid receptor modulators  
The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional...
7365072 Inhibitors of p38  
The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods...
7365071 Heterocyclic compounds, preparation process and intermediates, and use as medicaments, in particular as β-lactamase inhibitors and antibacterials  
The invention relates to novel heterocyclic compounds of general formula (I) and to their salts with a base or an acid: The invention also relates to processes and to intermediates for the...
7348326 Heteroaryl fused aminoalkyl imidazole derivatives: selective modulators of GABAa receptors  
Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein the A, B, C, D, X, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 , are variables defined...
7344702 Contrast agents for myocardial perfusion imaging  
The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds...
7338954 Compounds useful as motilin agonists and method  
A method is provided for treating disorders of gastrointestinal motility which include the steps of administering to a patient in need of treatment of a compound having the structure or a...
7332498 Modulation of KSP kinesin activity with heterocyclic-fused pyrimidinone derivatives  
A method of modulating KSP kinesin activity in vitro comprising contacting KSP kinesin with at least one chemical entity chosen from compounds represented by Formula I: and pharmaceutically...
7329660 Phthalazine derivatives for treating inflammatory diseases  
The invention relates to the treatment of leukemias with an inhibitor of the activity of VEGF receptor tyrosine kinase of the formula I, the substituents being defined in the...
7329659 Substituted-1-phthalazinamines as vr-1 antagonists  
The present invention provides a compound of formula (I): in which Ar and R 1 are phenyl or a heteroaromatic group, R 2 is generally hydrogen, R 3 is hydrogen or alkyl and X, Y and Z are...
7326690 Modulation of cell fates and activities by phthalazinediones  
Phthalazinediones that function as intracellular redox modulators are useful in treating cells in various disease states where intracellular redox status is impaired. By buffering aberrant redox...
7323467 3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics  
The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R 1 , R 2 and R 3 are as described herein. The invention further discloses processes for...
7319105 Cytotoxic agents  
The invention provides compounds of the invention pharmaceutical compositions comprising a compound of the invention, processes for preparing compounds of the invention, intermediates useful for...
7317009 Pyrrolopyridazine derivatives  
The invention relates to compound of the formula (I) or its salt, in which R 1 , R 2 , R 3 and R 4 are as defined in the description, their use of as medicament, the process for their preparation...
7312214 1, 1-disubstituted cycloalkyl derivatives as factor Xa inhibitors  
The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.
7312211 Pryanone compounds useful as reversible inhibitors of cysteine proteases  
Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R 2 , R 3 , R 4 , R 6 , R 8 and Y are defined herein. The compounds are useful for...
7307080 Compounds, methods and pharmaceutical compositions for treating cellular damage, such as neural or cardiovascular tissue damage  
The disclosure relates to compounds, pharmaceutical compositions and methods for inhibiting PARP by use of the disclosed compositions. The compounds of the disclosure have the following structures...
7300932 Pyrrolo[1,2-b]pyridazine derivatives  
Compounds, pharmaceutical compositions and methods that are useful in the treatment or prevention of metabolic and cell proliferative diseases or conditions are provided herein. In particular, the...
7294625 Pyrazole compounds  
The present invention relates to pyrazole compounds represented by the formula (I): wherein R 1 represents phenyl which may be substituted, R 2 represents H, halogen, alkyl, alkoxy,...
7288543 Opioid receptor antagonists  
A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3′, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate,...
7285533 Apo-2 ligand  
A novel cytokine, designated Apo-2 ligand, which induces mammalian cell apoptosis is provided. The Apo-2 ligand is believed to be a member of the TNF cytokine family. Compositions including Apo-2...
7279473 Pyrazolopyridazine derivatives  
Fused pyradazine derivatives which are usefule as CDK inhibitors are described herein. The described invention alos includes methods of making such fused pyradazine derivatives as wells as methods...
7276505 Immunomodulating heterocyclic compounds  
Compounds of formula (I) are inhibitors of CD80 and useful in immunomodulation therapy: wherein R 1 and R 3 independently represent H; F; CI; Br; —NO 2 ; —CN; C 1 -C 6 alkyl optionally...
7271168 Piperazine derivatives having SST1 antagonistic activity  
The invention provides compounds of formula ( 1 ) wherein X, R 1 and R 2 are as defined in the specification, their, preparation and to their use in treating, e.g., depression, anxiety and...
7268136 Compositions useful as inhibitors of protein kinases  
The present invention provides a compound of formula (I): or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of...
7265116 Aryl and heteroaryl substituted tetrahydroisoquinolines and use thereof  
Provided herein are compounds of the formula (I): wherein R 1 -R 8 are as described herein, R 4 being phthalazinyl, pyrazinyl, pyridazinyl, or quinoxalinyl. Such compounds are particularly...
7265115 Diazabicyclic CNS active agents  
Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
7235554 3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b] indole-1-acetamide derivatives, preparation and use thereof in medicaments  
The invention provides compounds of general formula (I) in which X represents a hydrogen or halogen atom; R 1 represents a hydrogen atom or a (C 1 -C 4 )alkyl group; R 2 and R 3 each...
7232823 Cannabinoid receptor ligands and uses thereof  
Compounds of Formula (I) or (II) 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...
7226923 Phthalazinone derivatives  
Compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates are disclosed. Also disclosed are methods for the preparation of the...
7226922 Imidazo[1,2-b]pyridazine analogues as anxiolytics and cognition enhancers  
The present invention provides a compound of formula I: wherein X 1 represents hydrogen, halogen, C 1-6 alkyl, trifluoromethyl or C 1-6 alkoxy; X 2 represents hydrogen or halogen; Y...
7223759 Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds  
The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of...
7220757 Compositions and methods for topical administration of 2-NH-heteroarylimidazoles  
Compounds of formula (I): are inhibitors of bacterial methionyl tRNA synthetase and are of use in treating bacterial infections.
7220746 Pyrrolidinedione substituted piperidine-phthalazones as PDE4 inhibitors  
The compounds of formula I in which the substituents have the meanings as indicated in the description, are novel effective PDE4 inhibitors.
7217711 Piperazin-1-yl and 2-([1,4]diazepan-1-yl)-imidazo[4,5-d]-pyridazin-4-ones, the preparation thereof and their use as pharmaceutical compositions  
The present invention relates to substituted imidazo[4,5-d]pyridazin-4-ones of general formula wherein R 1 to R 3 and n are defined as in claims 1 to 8 , the tautomers, enantiomers,...
7211572 Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor  
The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically...
7208492 Topoisomerase-targeting agents  
The invention provides compounds of formula I or formula II: wherein: the bond represented by --- is a single bond or a double bond, and R 1 –R 5 , X, and Y have any of the meanings defined...
7205312 N-[4-(heteroarylmethyl)phenyl]-heteroarylamines  
The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R 1 is...
Matches 1 - 50 out of 841 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 >