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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...
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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...
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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...
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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...
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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,...
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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...
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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,...
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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...
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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...
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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...
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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.
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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...
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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...
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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...
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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.
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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...
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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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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...
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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...
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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...
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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...
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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...
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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...
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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.
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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,...
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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...
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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...
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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...
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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...
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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,...
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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;...
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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...
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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,...
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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.
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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