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7625888 |
Fused triazole derivatives as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
The present invention is directed to novel fused triazole derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or...
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7612083 |
Urea substituted imidazoquinoline ethers
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and urea functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the...
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7608716 |
Pyrazolonaphthyridine derivative
The target is to provide PDE IV inhibitors which have a highly potent anti-asthmatic and/or COPD-prophylactic/therapeutic profile with unexpectedly excellent safety. A compound of the formula (1): ...
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7589101 |
Compounds and compositions as protein kinase inhibitors
The invention provides a novel class of compounds of formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders...
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7579359 |
1-alkoxy 1H-imidazo ring systems and methods
Imidazo-containing compounds (e.g., imidazonaphthyridines, imidazopyridines, imidazoquinolines, and imidazote-trahydroquinolines) with an alkoxy substituent at the 1-position, pharmaceutical...
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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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7569580 |
Heterotricyclic compounds for use as HCV inhibitors
The present invention comprises tetrazoloquinoline-compounds that are inhibitors of HCV. Compositions comprising the compounds in combination with a pharmaceutically acceptable carrier are also...
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7557211 |
8H-imidazo[4,5-D]thiazolo[4,5-B]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
The present invention provides for thiazolopyridine-based tricyclic compounds having the formula (I),
wherein R 1 , R 2 , R 5 and R 6 are as described herein. The present invention further...
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7544697 |
Pyrazolopyridines and analogs thereof
Pyrazolopyridin-4-amines, pyrazoloquinolin-4-amines, pyrazolonaphthyridin-4-amines, and 6,7,8,9-tetrahydropyrazoloquinolin-4-amines, pharmaceutical compositions containing the compounds,...
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7521459 |
Method for treating damaged skin
The invention relates to a method and composition for treating aged or photo-damaged skin. In one embodiment, the invention includes using a composition comprising about 1% to about 2% of...
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7495000 |
Variolin derivatives and their use as antitumor agents
Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X 2 , R 1 , R 2 , R 3 , R 6 , R 7 and R 12 are each independently selected from the group consisting of...
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7465742 |
Heterocyclic compounds having anti-HBV activity
This application relates to novel fused tricyclic thienopyridines of Formulas I and II, which useful for treating Hepatitis B infection and other diseases. This application also relates to...
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7465741 |
C-substituted tricyclic isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted tricyclic isoxazoline derivatives according to Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric...
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7462717 |
C6-and C9-substituted chromeno[4,3-c]isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and...
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7456194 |
Imidazo-fused oxazolo [4,5-b]pyridine and imidazo-fused thiazolo[4,5-b]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I),
wherein R 1 , R 2 , R 3 , and R 6 are as described herein. The present invention further...
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7439253 |
Heterocyclic compounds, their preparation and their use as medicaments, in particular as antibacterials and beta-lactamase inhibitors
The invention relates to novel heterocyclic compounds of general formula (I), and their salts with a base or an acid:
The invention also relates to a method for preparing these compounds, and to...
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7407963 |
Cyclopropane CGRP antagonists, medicaments containing these compounds, and method for the production thereof
A compound of general formula (I)
wherein R and R 1 are as defined herein, or a tautomer, diastereomer, enantiomer, or salt thereof, particularly the physiologically acceptable salts thereof,...
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7393860 |
Tetrahydropyridoethers
The compound (7R,8R,9R)-2,3-Dimethyl-8-hydroxy-7-(2-methoxyethoxy)-9-phen
yl-7,8,9,10-tetrahydro-imidazo-[1,2-h] [1,7] naphthyridine inhibits the secretion of gastric acid.
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7393859 |
Amide substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain amide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the invention...
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7390819 |
Imidazo[4,5-b]quinoline-derivatives and their use as no-synthase inhibitors
The compounds of formula I
in which R1, R2, R3 and A have the meanings as given in the description are novel effective INOS inhibitors.
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RE40245 |
Gyrase inhibitors and uses thereof
The present invention relates to compounds of the formula I:
or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase...
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7358259 |
HCV inhibitors and methods of using them
The present invention comprises tetrazoloquinoline-compounds that are inhibitors of HCV. Compositions comprising the compounds in combination with a pharmaceutically acceptable carrier are also...
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7348324 |
Cyclic amine compounds as CCR5 antagonists
A compound of formula (I) (wherein R 1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R 2 is a hydrocarbon group...
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7307084 |
Cyclic benzimidazoles
The invention relates to cyclic benzimidazoles of formula 1,
in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion...
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7291612 |
Immunomodulatory compounds
The present invention relates to novel heterocyclic compounds, to methods for their preparation, to compositions containing them, and to methods and use for clinical treatment of medical conditions...
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7288549 |
Heterocyclic compounds, method for preparing same and use thereof as medicines, in particular as antibacterial agents
The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid:
The invention also relates to a process for the preparation of these...
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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,...
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7288550 |
Thioether substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain thioether functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the...
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7285561 |
Imidazo-substituted compounds as p38 kinase inhibitors
The present invention discloses compounds corresponding to formula I:
wherein A, Z, Z 1 , Y, R 1 and R 2 are as defined in the specification, as well as pharmaceutical formulations, methods...
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7265103 |
Substituted amino isoxazoline derivatives and their use as anti-depressants
The invention concerns substituted amino isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisozazoline, dihydronaphthalenoisoxazoline and...
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7238699 |
Imidazolyl derivatives as corticotropin releasing factor inhibitors
The present invention relates to novel heterocyclic antagonists of Formula (I) and pharmaceutical compositions comprising said antagonists of the corticotropin releasing factor receptor (“CRF...
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7226928 |
Methods for the treatment of periodontal disease
The disclosure provides methods for the treatment and prevention of periodontal disease. In preferred embodiments, the invention provides for local treatment of periodontal tissues with a...
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7199131 |
Sulfonamide and sulfamide substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and...
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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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7189736 |
Prodrugs of imidazopyridine derivatives
Compounds of formula 1, in which the substituents have the meanings mentioned in the description are suitable for the prevention and treatment of gastrointestinal diseases.
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7176214 |
Imidazo-fused oxazolo[4,5-β]pyridine and imidazo-fused thiazolo[4,5-β]pyridine based tricyclic compounds and pharmaceutical compositions comprising same
The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I),
wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as described herein. The present invention...
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7169786 |
Isoxazoline derivatives as anti-depressants
The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R 7 , S or O, R 1 , R 2 and R 3 are certain specific substituents, Pir is an...
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7163947 |
1-Amino 1H-imidazoquinolines
1-Amino 1H-imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of making and methods of use of these compounds as immunomodulators, for...
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7157453 |
Urea substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain urea, thiourea, acylurea, or sulfonylurea functionality at the 1-position are useful as immune response modifiers. The...
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7148232 |
Oxazolo, thiazolo and selenazolo [4,5-c]-quinolin-4-amines and analogs thereof
Thiazolo-, oxazolo- and selenazolo[4,5-c]quinolin-4-amines and analogs thereof are described including methods of manufacture and the use of novel intermediates. The compounds are immunomodulators...
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7135468 |
Antibacterial compounds
Bacterial protein synthesis-inhibiting compounds having formula (I)
and salts, prodrugs, salts of prodrugs, and metabolites thereof, processes for making the compounds and intermediates in the...
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7132429 |
Sulfonamido ether substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and sulfonamide or sulfamide functionality at the 1-position are useful as immune response modifiers. The compounds and...
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7132428 |
Pyrazoloisoquinoline derivative as kinase inhibitors for the treatment of various disorders
Compounds of the formula I
are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.
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7115622 |
Amido ether substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain ether and amide functionality at the 1-position are useful as immune response modifiers. The compounds and compositions of the...
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7091214 |
Aryl substituted Imidazoquinolines
Aryl substituted imidazoquinoline compounds, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing or...
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7064131 |
Compounds and methods for inhibiting MRP1
The present invention relates to a compound of formula (I) which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.
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7060710 |
Isoxazole pyrazoloindane derivatives as cognition enhancing GABAA α5 subtype ligands
The present invention provides compounds of formula I:
in which:
one of X and Y is a nitrogen atom substituted by a group R 6′ and the other is a carbon atom substituted by an isoxazole...
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7053093 |
Bicyclic and tricyclic hetroaromatic compounds
Disclosed are compounds of the formula:
and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X 1 , Y and Z are as defined herein. These compounds bind with high selectivity...
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7037921 |
Compounds and methods for inhibiting MRP1
The present invention relates to a compound of Formula (I), which are useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.
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7030131 |
Sulfonamide substituted imidazoquinolines
Imidazoquinoline and tetrahydroimidazoquinoline compounds that contain sulfonamide or sulfonamide functionality at the 1-position are useful as immune response modifiers. The compounds and...
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