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7625923 |
Bicyclic modulators of androgen receptor function
The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen...
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7625924 |
Nicotinic alpha-7 receptor ligands 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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7625922 |
Imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof as therapeutic compounds
The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit...
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7622479 |
Bicyclic derivative, its production and use
The present invention provides a heterocyclic compound having potent tyrosine kinase-inhibiting activity represented by formula:
(wherein, R 1b is a C 6-10 aryl group which has...
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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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7598236 |
Diazabicyclic central nervous system active agents
Compounds of formula I
pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.
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7592352 |
Substituted thieno and furo-pyridines
This invention relates to newly identified compounds for treating and preventing tumors and cancers, and methods for treating proliferative diseases associated with the imbalance or inappropriate...
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7576072 |
Heterocyclic inhibitors of MEK and methods of use thereof
Disclosed are compounds of the Formula I
and pharmaceutically acceptable salts and prodrugs thereof, wherein R 1 , R 2 , R 7 , R 8 and R 9 , W, X, Y and Z are as defined in the specification....
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7547709 |
Chain-breaking antioxidants
Compounds, preferably 5-pyrimidinol and 3-pyridinol derivatives, that act as effective chain breaking antioxidants of both the lipid and water-soluble variety (analogous to the natural Vitamins E...
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7538220 |
Intermediates in the preparation of homocamptothecin analogs
A compound having the formula
in racemic form, enantiomerically enriched form or enantiomerically pure form; wherein X is a radical precursor; R 5 is a C 1-10 alkyl group, an alkenyl group,...
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7514449 |
Fused furan compound
The present invention provides a condensed furan compound of the formula (I):
wherein Ring X is benzene, pyridine, or the like; Y is an optionally substituted amino, an optionally substituted...
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7498349 |
Biaryl compounds having anti-infective activity
Aromatic compounds exemplified by exhibit antimicrobial activity.
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7495101 |
Manufacture of vitamin B6
A process for manufacturing a 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 9-acyloxy-1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin (I) and optionally for manufacturing pyridoxine...
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7491733 |
Bicyclic guanidine derivatives and therapeutic uses thereof
The invention relates to compounds of general formula (I), in which A, X, Y and R1 are defined in Claim 1 . These compounds may be used in the treatment of pathologies associated with insulin...
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7470693 |
Oxalamide derivatives as kinase inhibitors
The invention is directed to compounds having the following Formula I:
and methods of using them for the treatment of proliferative diseases.
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7459468 |
Aryl sulfonic pyridoxines as antiplatelet agents
Aryl sulfonic pyridoxine compounds with antiplatelet aggregation characteristics for the treatment of cardiovascular and cardiovascular related disease, are described. The methods are directed to...
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7456192 |
3β-amino azabicyclooctane heteroaromatic amid derivatives preparation method and therapeutic uses thereof
The invention concerns compounds of general formula 1, wherein: A, B, D and E represent one or two nitrogen atoms, the others being carbon atoms; X represents a S or, a O, thereby forming a...
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7449472 |
Methods of inhibiting p38 with substituted bicyclic pyrimidines
The present invention discloses compounds corresponding to the formula
wherein A, X, Y, R, R 1 and R 2 are as defined within, pharmaceutical formulations, methods of making and uses thereof.
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7439247 |
Bicyclic pyridine and pyrimidine P38 kinase inhibitors
The present invention discloses compounds corresponding to formula
wherein A, R, X, Y, R, R 1 and R 2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.
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7439246 |
Fused heterocyclic kinase inhibitors
In general, the instant invention comprises compounds of Formulas I and II
including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase...
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7429584 |
Furo[2.3-b]pyridine derivatives for the treatment of hyper-proliferative disorders
This invention relates to a compound of Formula (I) wherein Y is CH or N; Ar 1 is phenyl or pyridyl each optionally substituted with 1 or 2 substituents each selected independently from (C 1 -C 3...
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7425562 |
Inhibitors of cruzipain and other cysteine proteases
Compounds of general formula (I) or general formula (II)
wherein R 1 , P 1 , P 2 , Q, Y, (X) o , (W) n , (V) m , Z and U are as defined in the specification, are inhibitors of cruzipain and...
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7423048 |
Compounds for treating fundic disaccomodation
The present invention concerns compounds of formula (I)
a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -a...
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7358365 |
Process for the controlled increase in the molecular weight of polyethylenes
The invention relates to novel cyclic hydroxylamine esters and to the use of known hydroxylamine esters selected from the group consisting of HALS (sterically hindered amine) compounds and the...
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7332504 |
Heterocyclic substituted aminoazacycles useful as central nervous system agents
Heterocyclic substituted aminoazacyclic compounds of formula I
Z-R 3 I,
...
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7323494 |
Compounds and methods
Disclosed is a compound of having the formula:
pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables...
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7265128 |
3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and...
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7265115 |
Diazabicyclic CNS active agents
Compounds of formula I:
or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.
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7262300 |
Polymorphic forms of a GABAA agonist
Two new crystalline monhydrates and two new crystalline anhydrates of gaboxadol are disclosed together with methods for preparing them.
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7253154 |
Substituted thiazolopyrimidines as xanthine oxidase inhibitors
The invention relates to compounds of the following formula (I) or their salts:
in which R 1 represents OR 4 or others, in which R 4 is an alkyl group having 1-8 carbon atoms which may have...
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7253165 |
Benzisoxazolyl-, pyridoisoxazolyl-and benzthienyl-phenoxy derivatives useful as D4 antagonists
The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as D 4 antagonists. Said compounds are useful for the treatment of medical...
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7205316 |
Tri- and bi-cyclic heteroaryl histamine-3 receptor ligands
Compounds of formula (I)
wherein R 1 or R 2 is a tricyclic or bicyclic ring, each of which contains at least two heteroatoms, and R 1 , R 2 , R 3 , R 3a , R 3b , R 4 , R 5 , L, X, X′, Y,...
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7199128 |
8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
The invention provides compounds and salts of Formula I and Formula II:
which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making...
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7173134 |
Selective RXR ligands
The present invention includes novel retinoid compounds that have selectivity as RXR agonists on one or more isoforms of RXR, currently, RXRα, RXRβ, or RXRγ. The present compounds, and...
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7141564 |
Nitrogen-containing bicyclic heterocycles for use as antibacterials
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly man.
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7115654 |
Caspase-1 inhibitors and methods for their use
The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and...
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7105535 |
Oxazolyl-pyrazole derivatives as kinase inhibitors
Compounds which are oxazolyl-pyrazole derivatives, as defined in the specification, and pharmaceutically acceptable salts thereof; are useful in the treatment of diseases caused by and/or...
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7102008 |
Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme
The present invention provides compounds of Formula (I):
or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, R 1 , R 2 , R 3 , R 4 , Z, U, X, Y, Z a ,...
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7091216 |
Substituted furo[2,3-b]pyridine derivatives
Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases...
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7087601 |
Metabotropic glutamate receptor-5 modulators
Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered...
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7087756 |
Isoxazolopyridinones
The invention provides compounds of formula I, wherein X, Y, R 1 , R 2 , and R 3 are as defined in the description, and the preparation thereof. The compounds of formula I are useful as...
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7067515 |
Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
The invention provides compounds of Formula I:
where in W is
These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The...
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7053219 |
Isoxazolopyridone derivatives and their use
The invention relates to isoxazolopyridone derivatives of a formula (I-a):
wherein R 1a represents an optionally-substituted heteroaryl or phenyl group, R 2a represents an...
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6992188 |
Substituted heterocyclic derivatives
Corticotropin-releasing factor (CRF) antagonists having the formula
wherein the dashed lines, A, B, D E, F, Z, G, R 3 , and R 5 having the definitions set forth in the specification...
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6987117 |
Antidepressant azaheterocyclylmethyl derivatives of 1,4-dioxino[2,3-b]pyridine
Compounds of the formula
useful for the treatment of depression, obsessive compulsive disorder, panic attacks, generalized anxiety disorder, social anxiety disorder, sexual dysfunction, eating...
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6982264 |
Substituted alcohols useful in treatment of Alzheimer's disease
The invention relates to substituted alcohol compounds of the formula (I):
wherein X, R 1 , R 2 , R 3 , R N , R 20 and R C are defined herein. The compounds are useful in the treatment or...
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6962942 |
Azacycloalkanone serine protease inhibitors
The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and...
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6951868 |
Azabicyclic-phenyl-fused-heterocyclic compounds for treatment of disease
The invention provides compounds of Formula I:
wherein Azabicyclo is any of:
These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure...
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6951863 |
Pyridoarylphenly oxazolidinone antibacterials, and related compositions and methods
Pyridoarylphenyl oxazolidinone compounds of the formula:
in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.
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6949651 |
Fused bicyclic metalloproteinase inhibitors
The present invention relates to fused bicyclic metalloproteinase inhibitors of the formula
wherein A, B, X, Y, and R 1 are as defined in the specification, and to pharmaceutical compositions...
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