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7592338 |
Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I)
useful for treating p38 kinase-associated conditions, where W, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and m are as...
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7576116 |
PDK-1/Akt signaling inhibitors
A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of formula I:
wherein X is selected from the group consisting of alkyl and haloalkyl; Ar is an aryl radical selected from...
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7576115 |
Heterocyclic compounds and thrombopoietin receptor activators
A compound represented by the formula (1):
wherein A is a nitrogen atom or CR 4 , B is an oxygen atom, a sulfur atom or NR 9 (provided that when A is a nitrogen atom, B is not NH), R 1 is a C...
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7531669 |
Methods for treating neural disorders and conditions, and compounds useful therefor
In accordance with the present invention, there are provided novel compounds that protect neurons and/or promote neuroregeneration and/or promote memory formation. Such compounds are useful for...
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7491748 |
Carboxylic acid derivative compounds and drugs comprising these compounds as the active ingredient
A carboxylic acid derivative of formula (I):
wherein R 1 is —COOH, —COOR 6 , etc.; A is a single bond, alkylene, etc.; R 2 is alkyl, alkoxy, etc.; B is a carbocyclic ring or a...
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7476744 |
Polymorphic crystalline forms of celecoxib
Pharmaceutical compositions are provided comprising one or more orally deliverable dose units, each comprising a selective cyclooxygenase-2 inhibitory compound of low water solubility in a...
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7442802 |
Cyclooxygenase-2 selective inhibitors, compositions and methods of use
The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least...
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7432285 |
Nitrosated and nitrosylated cyclooxygenase-2 inhibitors, compositions and methods of use
The present invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase...
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7399765 |
Substituted diazabicycloalkane derivatives
Compounds of formula (I)
Z-Ar 1 —Ar 2 (I)
wherein Z is a diazabicyclic...
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7361769 |
Heterocyclyls as selective melanin concentrating hormone receptor antagonists for the treatment of obesity and related disorders
The present invention discloses compounds of formula I
wherein m, n, p, R 1 , R 2 and X, are herein defined, the compounds being novel antagonists for melanin-concentrating hormone (MCH), as...
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7358371 |
Process for the preparation of 1,5—carboxylic acid derivatives
The present invention comprises a process for the preparation of compounds that possess an affinity for the cannabinoid receptor in the human brain. These compounds are useful as immunomodulators...
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7358359 |
Antibacterial agents
Antibacterial compounds of formula I are provided:
As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such...
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7351825 |
Cyclopropane compounds and pharmaceutical use thereof
The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the...
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7332608 |
Anthranilamides and methods of their use
The present invention is related to a process for preparing anthranilamides of formula I,
in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as...
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7297710 |
Derivatives of N-[(1,5-diphenyl-1H-pyrazol-3-yl)methyl]sulfonamide, their preparation and their application in therapeutics
The present invention relates to compounds corresponding to the formula (I):
In which R 1 , R 2 , R 3 , R 4 and R 5 are as described herein. The invention also relates to the method of...
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7294645 |
Derivatives of N′-(1,5-diphenyl-1H-pyrazol-3-yl) sulfonamide with CB1 receptor affinity
The invention relates to compounds of formula (I):
Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 are as defined herein. The invention also relates to the preparation method...
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7271191 |
Pyrazole derivatives as gamma-secretase inhibitors useful in the treatment of Alzheimer's disease
The compounds of formula I:
inhibit gamma secretase and hence are of utility in the treatment or prevention of Alzheimer's Disease.
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7253170 |
Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I)
useful for treating p38 kinase-associated conditions, where W, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and m are as...
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7247628 |
Cannabinoid receptor ligands and uses thereof
Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment diseases, conditions and/or disorders herein.
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7241793 |
Phenyloxyalkanonic acid derivatives as hPPAR activators
A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrolysable ester thereof, wherein:
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7220867 |
Solid-state form of celecoxib having enhanced bioavailability
The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable...
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7211598 |
Oxime and/or hydrozone containing nitrosated and/or nitrosylated cyclooxygenase-2 selective inhibitors, compositions and methods of use
The invention describes novel cyclooxygenase 2 (COX-2) selective inhibitors having at least one oxime group or hydrazone group and novel compositions comprising at least one cyclooxygenase 2...
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7208528 |
Polyamine analogues as therapeutic and diagnostic agents
Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical...
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7192906 |
Substituted pyrazole derivatives, production process thereof, and herbicide compositions containing the derivatives
Substituted pyrazole compounds of the formula (1). The compounds are synthesized from a pyrazole derivative and a haloalkyleneoxime ester derivative, and have excellent herbicidal effects....
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7183306 |
Pyrazole derivatives
A compound of the formula (I):
wherein R 1 is hydrogen or lower alkyl;
R 2 is lower alkyl, etc.; R 3 is lower alkoxy, etc.; R 4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is...
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7179825 |
Retinoic acid mimetic anilides
The present invention is concerned with compounds of formula
the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents...
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7151113 |
Pyrazole-amine compounds useful as kinase inhibitors
The present invention provides pyrazole derived compounds of formula (I)
useful for treating p38 kinase-associated conditions, where W, X, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and m are as...
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7138414 |
Heterocyclically substituted benzoylureas, process for their preparation and their use as pharmaceuticals
The invention relates to heterocyclically substituted benzoylureas and also to their physiologically tolerated salts and physiologically functional derivatives. Compounds are described of the...
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7122547 |
Anthranilic acid amides and the use thereof as medicaments
The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products...
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7109349 |
Process for obtaining Cizolirtine and its enantiomers
A process is described for the preparation of a precursor alcohol of Cizolirtine, (±)-2-[phenyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethy
lethanamine and its enantiomers. The process involves...
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7056932 |
Heterocyclyl substituted 1-alkoxy acetic acid amides
The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I)
wherein R 1 to R 6 and A are as defined in the description and in the claims, as...
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7045532 |
ACE-2 modulating compounds and methods of use thereof
ACE-2 inhibitors for the treatment of body weight and related disorders are disclosed. ACE-2 inhibitors include peptides and small molecules. Examples of small molecule ACE-2 inhibitors include...
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7041833 |
3-step synthesis of pyrazolotriazole couplers and coupler intermediates
A process and intermediate useful for forming a 1H-Pyrazolo[1,5-b][1,2,4]triazole compounds comprise the step of reacting a 1,5-diaminopyrazole bearing a substituent, bonded to one and only one of...
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7030239 |
Compounds to treat Alzheimer's disease
The present invention is directed toward substituted hydroxyethylene compounds of formula (XII)
useful in treating Alzheimer's disease and other similar diseases.
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7009056 |
Blockade of voltage dependent sodium channels
Compounds of formula (I), and pharmaceutically acceptable salts thereof, are capable of blockading voltage-dependent sodium channels and are useful in particular, in treating glaucoma and multiple...
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7001917 |
Pyrazole compounds as anti-inflammatory and analgesic agents
This invention provides a compound of the formula (I):
wherein:
R 1 represents a hydrogen atom, an alkyl group, etc.; R 2 represents a hydrogen atom, a halogen atom, etc.; R 3 represents...
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6987112 |
Organic compound having cyano group and insecticides/miticides
The present invention is directed to compounds represented by Formula (1);
wherein A, R, X, Y and n are as defined in the description, the salts thereof, and insecticide/acaricide compositions...
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6972287 |
Method of inhibiting amyloid protein aggregation and imaging amyloid deposits
The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound...
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6967196 |
Sulfonamide compounds and uses thereof
In accordance with the present invention, there is provided a novel class of sulfonamide compounds. Compounds of the invention contain a core sulfonamide group. Variable moieties connected to the...
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6949578 |
Cycloalkyl alkanoic acids as integrin receptor antagonists
The present invention relates to a class of compounds represented by the Formula I
or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the...
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6906196 |
Processes for the preparation of 1,5-diaryl-3-substituted-pyrazoles
Provided are processes and chemical intermediates useful for preparing a compound of the formula I
wherein X is selected from the group consisting of C 1 -C 6 trihalomethyl; C 1 -C 6 ...
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6903092 |
Naphthamide neurokinin antagonists for use as medicaments
Compounds having the general formula
wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 and X 2 are as defined in the specification, methods of using such compounds for the treatment of diseases and...
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6884821 |
Carboxylic acid derivatives and drugs containing the same
Novel carboxylic acid derivatives of general formula (I), salts of the same, esters thereof, or hydrates of them, which are useful as insulin resistance improvers; and drugs containing the...
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6872711 |
β-substituted β-aminoethyl phosphonate derivatives
The present invention relates to novel β-substituted-β-aminoethylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a), apo B, apo B associated lipoproteins (low...
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6864254 |
Inhibitor for 20-hete-yielding enzyme
An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is...
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6770597 |
Benzohydrazide derivatives as herbicides and desiccant compositions containing them
The compound of the formula: wherein Y, X, Z, T and Q are defined in the specification,
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6759538 |
Substituted diphenyl heterocycles useful for treating HCV infection
The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the...
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6706743 |
β3 adrenergic receptor agonists and uses thereof
The instant invention provides β 3 adrenergic receptor agonists of structural Formula (I), the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds,...
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6686318 |
Heterocyclically substituted aromatic amino compounds with a herbicidal effect
The invention relates to new substituted aromatic amino compounds of the general formula (I) in which R 1 , R 2 , R 3 , R 4 and Z have the meanings given in the description, to a process for...
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6677353 |
Substituted N-phenyl-N-heteroaralkyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity
The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer...
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