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7220760 |
Quinoline derivatives as CRTH2 antagonists
The invetion relates to compounds of formula (I)
wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined in the description, their use as medicament, pharmaceutical...
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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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7211671 |
Substituted 1,3-dihydro-imidazol-2-one and 1,3-dihydro-imidazol-2-thione derivatives as inhibitors of matrix metalloproteinases and/or TNF-α converting enzyme (TACE)
The present invention describes novel 1,3-dihydro-imidazol-2-one or 1,3-dihydro-imidazol-2-thione compounds of formula (I):
or a stereoisomer or pharmaceutically acceptable salt or solvate...
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7202362 |
Transition metal complexes from solid state synthesis
Methods and compositions related to the synthesis of photosensitizers of titanium dioxide performed in situ, stepwise, in the solid state, and directly on the surface of the titanium dioxide...
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7176314 |
Inflammation modulators
Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular,...
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7141581 |
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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7138412 |
Tetrahydroquinoline derivatives useful as serine protease inhibitors
The present invention provides compounds of Formula (I):
or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, B, L 1 , L 2 , X 1 , X 2 , X 3 , X 4 , R 4...
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7125878 |
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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7094790 |
Fused bicyclic-substituted amines as histamine-3 receptor ligands
Compounds of formula (I)
are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising...
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7091348 |
Fluorescent dyes, energy transfer couples and methods
Fluorescent dyes, fluorescence energy transfer dye couples, multi-color dye sets, can be employed in art-recognized assays and certain novel methods, such as in proximity assays.
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7071177 |
P-(sulfonyl) aryl and heteroarylamines as anti-inflammatory agents
This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use,...
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7060832 |
Nitrogen-containing fused heterocyclic carboxylic acids having an absolute configuration of “R”
Nitrogen-containing fused heterocyclic carboxylic acid having an absolute configuration of “R” of the formula [XIX]:
wherein Y is substituted or unsubstituted arylsulfonyl group or an...
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7041829 |
Antagonists of the magnesium binding defect as therapeutic agents and methods for treatment of abnormal physiological states
This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential...
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7041667 |
CCR5 modulators
Compounds of Formula 1
[R egion α]—[R egion β]—[R egion γ]—[R egion δ] (1)
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7030139 |
Compounds
Compounds of general formula (I), are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in...
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7030063 |
Cyclohexenonquinolinoyl-derivatives as herbicidal agents
Cyclohexenonequinolinoyl derivatives of the formula I
where:
R 1 is hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxyiminomethyl, alkoxy, haloalkoxy, alkylthio, C 1 –C 6...
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7030133 |
Inhibitors of formation of advanced glycation endproducts (AGEs)
The nonenzymatic glycation and crosslinking of proteins is a part of the aging process with the glycation endproducts and crosslinking of long-lived proteins increasing with age. This process is...
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7026478 |
Iron catalyzed cross coupling reactions of aromatic compounds
A process for the production of compounds Ar—R 1 by means of a cross-coupling reaction of an organometallic reagent R 1 -M with an aromatic or heteroaromatic substrate Ar—X catalyzed by one or...
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7022857 |
Preparation of substituted aromatic compounds
A process for preparing compounds of the formula (II),
where the substituents R 1 to R 5 are each independently H, CH 3 , straight-chain or branched C 1 –C 8 -alkyl, CH(OC 1 –C 5 -alkyl)...
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7019005 |
3 (5)-heteroaryl substituted pyrazoles as p38 kinase inhibitors
A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula I
wherein R 1 , R 2 , Ar 1 and HetAr 2 ...
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7018987 |
Synthesis of combretastatin A-4 prodrugs and trans-isomers thereof
The present invention relates to novel water-soluble, stable derivatives of combretastatin A-4, and novel synthesis methods therefore. The combretastatin A-4 prodrugs described herein appear to be...
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6995181 |
Modulators of the glucocorticoid receptor and method
Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as...
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6989447 |
Compounds
Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
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6989446 |
Process for the preparation of 3-aryl-benzofuranones
Process for the preparation of compounds of formula I
wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula V
wherein the general...
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6987122 |
2-(1H-indol-3-yl)-2-oxo-acetic acid amides with antitumor activity
2-(1H-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.
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6977265 |
Piperidine CCR-3 receptor antagonists
The invention provides compounds of Formula (I):
wherein: R 1 -R 5 , A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical...
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6974823 |
Hydantoin derivative compounds, pharmaceutical compositions, and methods of using same
The present invention relates generally to novel hydantoin derivative compounds, pharmaceutical compositions containing such compounds, and methods for their use in preventing and/or treating...
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6960599 |
Heterocyclic aminoalkylpyridine derivatives as psychopharmaceuticals
The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I:
where
R 1 is the radical of a heterocycle having 1 to 3 ring structures, where each ring structure is...
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6949563 |
(2-carboxamido)(3-amino)thiophene compounds
Compounds represented by Formula (I):
or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1 is
R2 is
and R3 is C 0-4 alkyl, are useful in the treatment of cancer.
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6946466 |
Aromatic sulfonamides as peroxynitrite-rearrangement catalysts
The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the...
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6909003 |
Process for the manufacture of organic compounds
The invention relates to a process for the manufacture of a compound of formula
or a salt, especially a pharmaceutically acceptable salt with a base, thereof or a lactone thereof wherein the...
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6906193 |
N-type calcium channel antagonists for the treatment of pain
Compounds useful for the treatment of pain in accord with the following structural diagram,
wherein R 1 , R 2 , R 3 , R 4 and R 5 are any of a number of groups as defined in the...
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6903114 |
Derivatives of naphthalene with COMT inhibiting activity
Compounds of formula (I′), wherein A, R 1 to R 3 and t are as defined in the disclosure, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.
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6894041 |
Oxazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic...
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6878720 |
VEGF receptor tyrosine kinase inhibitors
Described are compunds of formula (I), wherein W is O or S; X is NR 8 ; Y is CR 9 R 10 —(CH 2 )n wherein R 9 and R 10 are independently of each other hydrogen or lower alkyl, and n is an...
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6875769 |
Substituted6,6-hetero-bicyclicderivatives
This invention relates to compounds of the formula
wherein A, B, D, E, K, G, R 3 and R 5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.
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6852748 |
Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide
Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-sulfonyl]-pyrrolid
ine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are...
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6844087 |
Material for use in a light-emitting device and highly efficient electroluminescent device
A material is provided that can be used for a light-emitting device. The base unit of said material is tris(8-quinolinolato)aluminum(III) (Alq3). This Alq3 is substituted in the said 3- or...
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6844342 |
Heterocyclic substituted 2-methyl-benzimidazole antiviral agents
The present invention concerns antiviral compounds, their methods of preparation and their compositions, and use in the treatment of viral infections. More particularly, the invention provides...
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6841555 |
Lavendamycin analogs, quinoline-5,8-diones and methods of using them
The invention provides novel lavendamycin analogs having the following general formula:
and quinoline-5,8-diones having the following formula:
Methods of making and using and compositions...
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6821988 |
3-cyanoquinolines as inhibitors of EGF-R and HER2 kinases
This invention provides compounds of Formula (I), represented by the structure wherein G 1 , G 2 , G 3 , G 4 , Z, X and n are defined herein, or a pharmaceutically acceptable salt thereof which...
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6818777 |
Intermediates for synthesis of vinblastine compound and method for synthesizing the intermediate
Intermediates A, which are important in the whole synthesis of vindoline; and a method of synthesizing intermediates respectively represented by the general formulae B and C. By the method, the...
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6809097 |
Quinoline derivatives inhibiting the effect of growth factors such as VEGF
Compounds of the formula (I): wherein: R 2 represents hydroxy, halogeno, C 1-3 alkyl, C 1-3 alkoxy, C 1-3 alkanoyloxy, trifluoromethyl, cyano, amino or nitro; n is an integer from 0 to 5; Z...
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6800618 |
Chemosensitizing agents against chloroquine resistant plasmodium falciparum and methods of making and using thereof
A compound having the structural formula or a pharmaceutically acceptable salt or prodrug thereof, wherein X is a substituted or unsubstituted alkyl or a heteroatom; n is 4, 5 or 6; Y is a...
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6800652 |
Diaryl compounds
The invention relates to compounds of formula I
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6787534 |
Sulfonamide-containing heterocyclic compounds
The present invention provides a sulfonamide- or sulfonylurea-containing heterocyclic compounds. Specifically, it provides a heterocyclic compound represented by the formula (I), a...
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6784190 |
Integrin receptor antagonists
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are...
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6753335 |
Quinolinyl-piperidin-4-ylidene-methyl-benzamide derivatives for the treatment of pain
Compounds of general formula I R 1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, and triazolyl; where each R 1 phenyl ring and R 1 heteroaromatic ring may...
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6689770 |
Aryl sulfonyls as factor Xa inhibitors
The present application describes aryl sulfonyls of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein D, E, and M are defined below, are effective factor Xa...
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6689771 |
Amide derivatives as inhibitors of matrix metalloproteinases, TNF-α, and aggrecanase
The present application describes novel amides and derivatives thereof of formula I: or pharmaceutically acceptable salt forms thereof, wherein these compounds are useful as inhibitors of matrix...
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