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7618971 |
Mitotic kinesin inhibitors
The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for...
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7608634 |
Substituted pyrrolines as kinase inhibitors
The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating...
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7598286 |
[(1H-indazol-3-yl)methyl]phenols and (hydroxyphenyl)(1H-indazol-3-yl)methanones
This invention provides anti-inflammatory agents of formula I, having the structure
wherein A and R 1 -R 10 are as defined in the specification, or a N-oxide thereof or a pharmaceutically...
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7598284 |
Indazole compounds as B3 adrenoceptor agonist
Compounds of the general formula (I):
or a salt thereof, wherein R 1 is a hydrogen atom or the like; R 2 is NHSO 2 R 3 or the like; R 3 is a (C 1 -C 6 )alkyl group or the like; R 5 is a...
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7589232 |
Alkynyl aryl carboxamides
The present invention is related to alkynyl aryl carboxamides of Formula (I′) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders...
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7589116 |
Biaryl substituted pyrazoles as sodium channel blockers
Biaryl substituted pyrazole compounds are sodium channel blockers useful for the treatment of pain and other conditions. Pharmaceutical compositions comprise an effective amount of the instant...
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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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7566735 |
Compounds which potentiate AMPA receptor and uses thereof in medicine
Compounds of formula (I) and salts are provided:
along with pharmaceutical compositions, uses in medicine, e.g., treating disease or condition mediated by a reduction or imbalance in glutamate...
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7560478 |
Crystal forms of substituted phenylalkanoic acids and process for producing the same
In the case of using 3-[3-amino-4-(indan-2-yloxy)-5-(1-methyl-1H-indazol-5-yl)phe
nyl]propionic acid, methyl 3-[4-(indan-2-yloxy)-3-(1-methyl-1H-indazol-5-yl)-5-nitrophe
nyl]propionate, or methyl...
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7553863 |
Ultrapure 4-methylpyrazole
Disclosed is an ultrapure 4-methylpyrazole containing less than 0.1% pyrazole and containing less than 10 ppm each of hydrazine and nitrobenzaldehyde. The ultrapure 4-methylpyrazole is prepared by...
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7544707 |
Bicyclic derivatives as PPAR modulators
The present invention is directed to compounds represented by the following structural formula, Formula (I), and stereoisomers, pharmaceutically acceptable salts, solvates and hydrates thereof,...
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7538134 |
Substituted arylpyrazoles
This invention relates to a range of 1-aryl-4-cyclopropylpyrazoles in which the cyclopropyl ring is substituted at the angular position, and pharmaceutically acceptable salts and solvates thereof,...
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7531560 |
Anti-cytokine heterocyclic compounds
Disclosed are compounds of formula (I)
which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving...
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7528162 |
4,5-dihydro-1H-pyrazole derivatives having CB1-antagonistic activity
The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB 1 ) receptor antagonists with utility for the treatment of diseases connected...
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7524957 |
Compounds effecting glucokinase
The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R 1 , R 2 , R 3 , n and m are as described in the specification, in the preparation of a...
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7521471 |
4-cyanopyrazole-3-carboxamide derivatives, preparation and application thereof
The invention relates to 4-cyanopyrazole-3-carboxamide derivatives of formula (I):
in which R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 are as described herein. Also disclosed and claimed...
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7511069 |
Indazole compounds as β3 andrenoceptor agonist
Compounds of the general formula (I):
or a salt thereof, wherein R 1 is a hydrogen atom or the like; R 2 is NHSO 2 R 3 or the like; R 3 is a (C 1 -C 6 )alkyl group or the like; R 5 is a...
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7507833 |
Therapeutic N-aryl or N-heteroaryl pyrazolidine and pyrazolidinone derivatives
A compound having a structure
and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.
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7507755 |
Inhibitors of cathepsin s
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at...
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7504519 |
Derivatives of pyrazoline, procedure for obtaining them and use thereof as therapeutic agents
The invention relates to derivatives of general formula (I), and to their pharmaceutically acceptable salts, their stereoisomeric forms, preferably their pure enantiomeric or diastereomeric forms...
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7501449 |
2H -or 3H-benzo[e]indazol-1-yl carbamate derivatives, the preparation and therapeutic use thereof
Compounds corresponding to the formula (I)
as defined in the disclosure as well as methods for making such compounds, intermediates employed in such methods, pharmaceutical compositions...
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7491741 |
Diaminopropionic acid derivatives
A compound of formula 1a
which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.
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7485730 |
Pharmaceutical compounds
Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors:
wherein:
A represents a group selected from one of the...
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7485659 |
Anticancer compositions, and methods of making and using the same
Compositions, containing a ruthenium(III) complex and a heterocycle, methods for their manufacture, medicament containing these compositions and a kit. The invention relates to a composition (A),...
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7482470 |
Cannabinoid receptor antagonists/inverse agonists useful for treating metabolic disorders, including obesity and diabetes
The present invention provides novel pyrazoles that are useful as cannabinoid receptor antagonists and pharmaceutical compositions thereof and methods of using the same for treating obesity,...
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7482375 |
Compounds useful in therapy
Compounds of formula (I),
or pharmaceutically acceptable derivatives thereof, wherein:
R 1 represents H, C 1-6 -alkyl, C 1-6 alkyloxy, C 3-8 cycloalkyl, or halo; R 2 represents H, C...
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7470717 |
Indazole derivatives
The present invention provides a compound represented by Formula (I):
[wherein R 1 represents CONR 1a R 1b (wherein R 1a and R 1b may be the same or different and each represents a hydrogen...
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7468371 |
Tricyclic pyrazole kinase inhibitors
Compounds of the present invention are useful for inhibiting protein tyrosine kinases. Also disclosed are methods of making the compounds, compositions containing the compounds, and methods of...
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7465805 |
Isoxazoline derivatives and their use as herbicides
Compounds of formula: (I) wherein the substituents are as defined in claim 1 , are suitable for use as herbicides. Also claimed are processes for the preparation of the claimed compounds, a...
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7465718 |
Ansamycins having improved pharmacological and biological properties
Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and...
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7459564 |
Substituted biaryl compounds as factor XIa inhibitors
The present invention provides compounds of Formula (I):
or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R 3 , and ring B...
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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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7446121 |
Pyrazole-based HMG CoA reductase inhibitors
Novel compounds and pharmaceutical compositions useful as hypocholesterolemic and hypolipidemic agents are described. More specifically, potent inhibitors of the enzyme...
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7432271 |
Pyrazolyl inhibitors of 15-lipoxygenase
The present invention provides pyrazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such...
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7425572 |
Use of dioxindoindazoles and dioxoloindazoles for treating glaucoma
Novel dioxinoindazole compounds and dioxoloindazole compounds are disclosed. Also disclosed are methods for the lowering and controlling of normal or elevated intraocular pressure as well as a...
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7417030 |
Indazole peptidomimetics as thrombin receptor antagonists
The invention is directed to novel indazole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis,...
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7407981 |
Aminoindazole derivatives as medicaments and pharmaceutical compositions including them
The present invention relates to the use of novel derivatives of general formula (I)
in which
R3 is a (1-6C)alkyl, aryl, aryl(1-6C)alkyl, heteroaryl, heteroaryl(1-6C)alkyl, aryl or heteroaryl...
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7399778 |
Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole
Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia:
wherein, R 1 is lower alkyl, substituted lower alkyl, phenyl, substituted...
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7396850 |
Pyrazole derivative as PPAR modulator
The present invention is directed to a compound, {2-Methyl-4-[3-methyl-1-(4-trifluoromethyl-phenyl)-1H-pyrazo
l-4-ylmethylsulfanyl]-phenoxy}-acetic acid and pharmaceutical uses thereof.
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7393868 |
AMPA receptor potentiators
The present invention relates to AMPA receptor potentiators of Formula I:
formulations comprising them, methods for their use, and intermediates useful for their preparation.
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7375126 |
Fused compounds that inhibit vanilloid receptor subtype 1 (VR1) receptor
The present invention discloses novel compounds of general formula (I)
or a pharmaceutically acceptable salt or prodrug thereof (in which X 1 -X 5 , R 5 -R 8b , Z 1 -Z 2 and Ar 1 are defined...
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7358214 |
Pyrazolyl carboxanilides for controlling unwanted microorganisms
This invention relates to novel pyrazolylcarboxanilides of the formula (I)
in which R 1 , G and n are as defined in the disclosure, to a plurality of processes for preparing these...
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7320996 |
Indolinone protein kinase inhibitors and cyclooxygenase inhibitors for use in combination therapy for the treatment of cancer
The present invention relates to methods for treatment or prevention of neoplasia disorders using protein tyrosine kinase inhibitors of the formula I:
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6...
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7307097 |
Chemical compounds
Pyrazole derivatives are described herein. The described invention also includes methods of making such pyrazole derivatives as well as methods of using the same in the treatment of diseases.
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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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7291647 |
Guanylhydrazone compounds, compositions, methods of making and using
The present invention relates to compounds having the formula:
salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of...
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7282512 |
Cycloalkyl ketoamides derivatives useful as cathepsin K inhibitors
Cycloalkyl ketoamide derivatives, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such cycloalkyl ketoamide derivatives as...
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7271190 |
Indazole compounds as β3 adrenoceptor agonist
A compound represented by the general formula I: I wherein R1 represents hydrogen, etc. R 2 represents NHSO 2 R 3 , etc., provided that R 3 represents C 1-6 alkyl, etc. R 5 represents hydrogen,...
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7265130 |
NPY Y5 antagonist
The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I):
wherein R 1 is lower alkyl, cycloalkyl or the...
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