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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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7410992 |
Ophthalmic compositions for treating ocular hypertension
This invention relates to potent potassium channel blocker compounds of Formula (I) or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular...
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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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7312199 |
Process for the production of (−)-epigallocatechin gallate
A process is provided for making (−)-epigallocatechin gallate (EGCG) by subjecting a green tea extract to chromatography on a macroporous polar resin, eluting EGCG from the resin with a polar...
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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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7253201 |
Small molecule inhibitors of necrosis
The invention features methods for decreasing necrosis. The invention also features methods for treating a subject with a condition in which necrosis occurs. The invention further features chemical...
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7250436 |
Indazole-aminoacetonitrile derivatives having special pesticidal activity
The invention relates to compounds of the general formula
wherein Ar 1 , Ar 2 , R 4 , R 5 , R 6 , R 7 , R 8 , W, X, a and b have the significances given in the specification, and optionally the...
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7250435 |
Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents
The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I):
that are potent inhibitors of the class of enzymes known as cyclin dependent...
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7241791 |
Substituted 4-(indazol-3-yl)phenols
This invention provides compound of formulae I or II having the structure
wherein
R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , and R 10 are as defined in the specification or a...
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RE39681 |
1-(4-sulfamyaryl)-3-substituted-5-aryl-2-pyrazolines and inhibitors of cyclooxygenase-2
Compounds of the formula
wherein:
X is selected from the group consisting of trihalomethyl, C 1 -C 6 alkyl, and a group of formula II:
wherein:
R 3 and R 4 are...
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7226941 |
Compound for treating angiogenesis
The present invention provides methods and pharmaceutical compositions for inhibiting expressions of HIF and HIF regulated genes, inhibiting angiogenesis, inducing cell cycle arrest in tumor cells,...
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7220771 |
Methods of using indazole derivatives as JNK inhibitors
Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure:
wherein R 1 , R 2 and A are as...
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7217728 |
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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7217706 |
Propanolamine derivatives
This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]:
Wherein each symbol is as defined in the specification or salts thereof which...
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7214699 |
Indazole derivatives as CRF antagonists
This invention relates to compounds which are generally CRF-1 receptor antagonists and which are represented by Formula I or Formula II:
wherein R 3 is optionally substituted aryl or...
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7211594 |
Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith
This invention is generally directed to Indazole Derivatives having the following structure:
or pharmaceutically acceptable salt thereof, wherein R 1 , R 2 and A are as defined herein. Such...
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7208513 |
Indazole compounds and compositions thereof as JNK inhibitors and for the treatment of diseases associated therewith
Compounds having activity as selective inhibitors of JNK are disclosed. The compounds of this invention are indazole derivatives having the following structure:
wherein R 1 , R 2 and A are as...
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7196111 |
Pyrazolo[1,5a]pyrimidine compounds as antiviral agents
The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA...
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7196109 |
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...
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7192953 |
Antibacterial agents
Compounds of formula (I) have antibacterial activity; wherein Q represents a radical of formula —N(OH)CH(═O) or formula —C(═O)NH(OH); Y represents —C(═O)—, —C(═S)—,...
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7186741 |
Neurotensin active 2,3,diaryl-pyrazolidine derivatives
The invention relates to a group of novel 2,3 diaryl-pyparazolidine derivatives having formula (1). The symbols used in formula (1) have the meanings given in the specification. The compounds have...
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7186738 |
Antibacterial oxalidinones
Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereo Formula (I): wherein N-HeT is for example triazolyl; Q is for example phenyl or pyridyl,...
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7183316 |
Treatment of HPV caused diseases
Human papillomavirus (HPV) protein expression is downregulated in patients infected with HPV by administration of PPARγ ligand, selective inhibitor of cyclooxygenase-2 (COX-2), diaryl heterocycle,...
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7157482 |
Antibacterial 1,3-oxazolidin-2-one derivatives
Compounds of the formula (I), or a pharmaceutically-acceptable salts, or in-vivo-hydrolysable esters thereof, wherein: N—HET is for example triazolyl substituted with R 1 ; R 1 is for example...
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7153881 |
Compounds acting as melanocortin receptor ligands
The present invention provides novel compounds and use of compounds of general formula (I) as ligands to the melanocortin receptors and/or for treatment of disorders in the melanocortin system:...
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7148240 |
Aminoalkoxybenzoyl-benzofuran or benzothiophene derivatives, method for preparing same and compositions containing same
The invention relates to benzofuran or benzothiophene derivatives of general formula:
These compounds are of use as medicinal products, in particular in the treatment of pathological syndromes...
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7144883 |
Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful...
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7144570 |
Sunscreen compositions and methods of use thereof
Disclosed herein are novel methods for reducing or preventing the harmful effects of solar radiation on skin. Also disclosed are novel sunscreen compositions comprising thaizolium, thiadiazolium or...
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7141587 |
Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating...
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7138418 |
Pentafluorobenzenesulfonamides and analogs
The invention provides methods and compositions relating to novel pentafluorophenylsulfonamide derivatives and analogs and their use as pharmacologically active agents. The compositions find...
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7129257 |
Pyrazolo[3,4- e]benzoxazoles for the treatment of glaucoma
Pyrazolo[3,4-e]benzoxazoles and analogues thereof for lowering intraocular pressure and treating glaucoma are disclosed.
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7119114 |
Pyrazoloanthrone and derivatives thereof as JNK inhibitors and compositions and methods related thereto
Compounds having activity as selective inhibitors of JNK are disclosed The compounds of this invention are pyrazoloanthrone and derivatives thereof having the following structure:
wherein R 1 ...
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7115624 |
Method of inhibiting protein tyrosine phosphatase 1B and/or T-cell protein tyrosine phosphatase 4 and/or other PTPases with an Asp residue at position 48
The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTPα, PTPε, PTPμ, PTPδ,...
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