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7638533 |
Dihydro-1[1H]-quinolin-2-one derivatives as RXR agonists for the treatment of dyslipidemia, hypercholesterolemia and diabetes
The present invention relates to compounds of Formula (I),
methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating RXR mediated disorders....
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7638517 |
3-Amino-1-arylpropyl azaindoles and uses thereof
The present invention provides compounds of the formula:
or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R 1 , R 2 , R 3 , R a , R b , R c , R d and R e are...
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7635702 |
Imidazole compounds as transforming growth factor (TGF) inhibitors
Novel imidazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The...
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7625938 |
Substituted pyrazoles, compositions containing such compounds and methods of use
The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment. The compounds are glucagon receptor antagonists and thus are useful for...
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7612085 |
Sigma 2 receptor ligands and therapeutic uses therefor
A series of N-substituted 9-azabicyclo[3.3.1]nonan-3α-yl phenylcarbamate analogs are disclosed, as well as methods of their preparation. Their affinities for sigma (σ1 and σ2) receptors are...
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7612084 |
Amine derivatives for the treatment of asthma and COPD
The invention relates to compounds of formula (1)
and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives....
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7608626 |
Substituted indolizines and derivatives as CNS agents
Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided:
which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and...
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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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7585874 |
Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives
The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine derivatives of formula I:
wherein
R 1 to R 5 are as defined in the specification and pharmaceutically...
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7585974 |
Derivatives of 5-(pyridin-3-yl)-1-azabicyclo[3.2.1]octane, their preparation and their therapeutic application
Compounds complying with the general formula
in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C 1 -C 6 )alkyl, (C 1...
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7582650 |
Tricyclic opioid modulators
The invention is directed to compounds of Formula (I) useful as delta and mu opioid receptor modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and...
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7579347 |
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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7572816 |
Therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders
The present invention is directed to compounds having the structure wherein R 1 , R 2 , R 3 , R 4 , R 5 and m are as defined herein. The compounds of this invention are novel therapeutic agents...
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7569584 |
4-(2-methyl-5,6,7,8-tetrahydro-quinolin-7-ylmethyl)-1,3-dihydro-imidazole-2-thione as specific alpha2b agonist and methods of using the same
The compound of the formula
wherein the * indicates an asymmetric carbon, is specific to alpha 2B adrenergic receptors in preference over alpha 2A and alpha 2C adrenergic receptors, and...
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RE40838 |
2-azabicyclo[3.3.1]nonane derivatives
The subject invention relates to 2-azabicyclo[3.3.1]nonane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states,...
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7553845 |
Substituted indolizine 1,2,3,6,7,8 derivatives, FGFs inhibitors, a method for the preparation thereof and pharmaceutical compositions containing said derivatives
The invention is directed to a compound of formula I,
wherein R, R 1 , R 2 , R 3 and R 4 are as defined herein, or a pharmaceutically acceptable salt thereof, and its pharmaceutically...
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7550474 |
Substituted phenyl acetamides and their use as protease inhibitors
Phenyl acetamide compounds are described, including compounds of Formula I:
or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R 3 -R 6 , R 11 , B, Y and W are set forth...
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7534800 |
7-azaindoles as inhibitors of c-Jun N-terminal kinases for the treatment of neurodegenerative disorders
The present invention relates to novel 3,5-substituted 7-azaindole compounds of formula (I), their use in the inhibition of c-Jun N-terminal kinases, their use in medecine and particularly in the...
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7531661 |
Indane compounds as CCR5 antagonists
The present invention relates to compounds of formula (I), or pharmaceutically acceptable derivatives thereof, useful in the treatment of CCR5-related diseases and disorders, for example, useful in...
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7524958 |
Certain 9-aza-bicyclo[3.3.1] nonane derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
This invention relates to novel 9-aza-bicyclo[3.3.1]nonane derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these...
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7524858 |
Substituted pyrroline kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase inhibitors and methods for treating or ameliorating a kinase mediated disorder.
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7514432 |
Compounds and methods of treating cell proliferative diseases, retinopathies and arthritis
The present invention relates to compounds and their uses, particularly in the pharmaceutical industry. The invention discloses compounds having anti-proliferative and antiangiogenic activities, as...
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7511058 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula III
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 , R 9 R 10 , and W are as defined in the specification....
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7511061 |
Triazoles as farnesyl transferase inhibitors
A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein L 1 and L 2 are R 1 —Y— wherein each (R 1 —Y)— substituent is defined independently...
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7504508 |
PGD2 receptor antagonists for the treatment of inflammatory diseases
Disclosed herein are compounds represented by Structural Formula (I) and (I-A):
Also disclosed is the use of such compounds for inhibiting the G-protein coupled receptor referred to as...
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7488735 |
Quinuclidine amide derivatives
New quinuclidine amide derivatives having the chemical structure of general formula (I) and pharmaceutically acceptable salts thereof including quaternary salts of formula (II) are disclosed; as...
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7482372 |
Hydantoins and related heterocycles as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
The present application describes novel hydantoin derivatives of formula (I):
or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7...
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7449488 |
Pyrazolopyrimidines as protein kinase inhibitors
In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of protein and/or checkpoint kinases, methods of preparing such compounds,...
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7442708 |
1,2,3-substituted indolizine derivatives, inhibitors of fgfs, method for making same and pharmaceutical compositions containing same
Compounds of formula I or salts thereof:
in which
R 1 represents —OH, (C 1 -C 5 )alkoxy, carboxyl, (C 2 -C 6 )alkoxycarbonyl, —NR 5 R 6 , —NH—SO 2 -Alk, —NH—SO 2 -Ph,...
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7429664 |
Indazoles, benzothiazoles, and benzoisothiazoles, and preparation and uses thereof
The present invention relates generally to the field of ligands for nicotinic acetylcholine receptors (nAChR), activation of nAChRs, and the treatment of disease conditions associated with...
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7423030 |
1-amino-phthalazine derivatives, the preparation and the therapeutic use thereof
A 1-amino-phthalazine derivative of general formula (I)
wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such...
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7417041 |
Imidazopyrimidines as transforming growth factor (TGF) inhibitors
Novel fused heteroaromatic compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described....
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7410961 |
2,6-disubstituted piperiddines as modulators
The present invention is further directed to compounds of formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 16 , R 17 , R 18 , R 19 , R 20 , R 21 and R 22 are as...
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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 ...
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7402592 |
Pharmaceutical compositions and methods for relieving pain and treating central nervous system disorders
Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release...
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7399769 |
Aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives
The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula
wherein:
R 1 , R 2 , and R 3 are as defined herein and pharmaceutically acceptable...
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7388018 |
4-Piridinylmethylsulphonamide derivatives as fungicidal plant protein agents
Sulfonamides of the formula I
where the substituents are as follows:
R 1 is hydrogen, alkyl, alkoxy, alkenyl or alkynyl; and R 2 , R 3 , R 4 , R 5 are hydrogen, halogen, alkyl, alkoxy or...
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7384954 |
4-substituted imidazoles
Compounds of formula I:
wherein A and R 1 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in...
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7375219 |
Substituted indole compounds having NOS inhibitory activity
The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The...
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7368457 |
Bridged N-arylsulfonylpiperidines as gamma-secretase inhibitors
In an embodiment, this invention discloses novel gamma secretase inhibitors of Formulae I:
wherein the various moieties are described herein. Also disclosed is a method of treating Alzheimer's...
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7361762 |
Process for preparing acid salts of Gemifloxacin
The present invention relates to a process for preparing acid salts of Gemifloxacin, a quinolone type antibiotic agent having potent antimicrobial activity. The process according to the present...
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7358364 |
Substituted carboxylic acids
The present invention relates to compounds and pharmaceutically acceptable salts of formula (I):
which are useful in the treatment of metabolic disorders related to insulin resistance or...
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7345174 |
Cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
The present invention provides the compound having the formula:
wherein each of R 1 and R 2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino,...
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7345056 |
Bridged N-cyclic sulfonamido inhibitors of gamma secretase
The invention provides N-cyclic sulfonamido compounds and salts of Formula I:
wherein A is as described in the specification and R 1 and R 2 combine to form a [3.3.1] or a [3.2.1] ring...
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7323477 |
7-((1H-imidazol-4-yl)methyl)-5,6,7,8-tetrahydroquinoline
A compound having a structure
or a pharmaceutically acceptable salt, or a prodrug thereof is disclosed herein. Therapeutic methods, compositions, and medicaments related thereto are also...
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7314870 |
Compounds, their preparation and use
The present invention relates to novel compounds that are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due...
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7304159 |
Ligands and catalyst systems thereof for ethylene oligomerisation to linear alpha olefins
Mixed bis-imine pyridine ligands of formula (I), wherein Z 1 , which is different from Z 2 , is an optionally substituted aryl group; and Z 2 comprises an optionally substituted heterohydrocarbyl...
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7297693 |
Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac...
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7285518 |
Dibenzo[b]perhydroheterocyclic amines and lubricating oil compositions
Dibenzo[b]perhydroheterocyclic amine compounds have shown to be particularly useful as stabilizers. The compounds may serve as antioxidants, antiozoants, heat stabilizers and ultraviolet light...
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7276520 |
Bicyclic piperidine derivatives as melanocortin-4 receptor agonists
Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R)....
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