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US20090291967 |
SMALL MOLECULE MODULATORS OF CELL ADHESION
Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure:
or a pharmaceutically acceptable salt, stereoisomer or prodrug...
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US20090286800 |
Glucokinase Activators
Compounds are provided for use with glucokinase that comprise the formula:
wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of...
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US20090286791 |
Amide Compounds
The present invention provides compounds represented by the formula (Ia):
the formula (Ib):
the formula (Ic):
and the formula (Id):
wherein each symbol is as defined in the specification....
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US20090286786 |
Compounds having a 4-pyridylalkylthio group as a substituent
A compound having the following formula [I] or a pharmaceutically acceptable salt thereof:
wherein A is benzene or an aromatic five-membered heterocycle which optionally is fused with a...
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US20090286767 |
SUBSTITUTED QUINOLIN-4-YLAMINE ANALOGUES
Substituted quinolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the...
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US20090285756 |
11C/18 F-LABELED INHIBITORS OF GLYCOGEN SYNTHASE KINASE-3
The present invention relates to new 11 C/ 18 F-labeled inhibitor compounds for over-expressed GSK-3 prepared from the GMP synthesis method. The present invention provides novel 11 C/ 18 F...
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US20090281099 |
SUBSTITUTED PYRAZINONE DERIVATIVES FOR USE AS A MEDICINE
The present invention concerns substituted pyrazinone derivatives according to the general Formula (I)
a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically...
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US20090281060 |
HETEROCYCLIC DERIVATIVES AS GPCR RECEPTOR AGONISTS
Compounds of Formula (I), R 1 -A-V—B—R 2 ; or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful as regulators of satiety, e.g. for the treatment of obesity, and...
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US20090275609 |
Carboxamide Compounds and Methods for Using The Same
Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure
in which R 1 , R 2 , R 3 , R 4 , D, J, Z, T, p,...
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US20090274655 |
2-CARBOXY THIOPHENE DERIVATIVES AS ANTI VIRAL AGENTS
Anti-viral agents of compounds of Formula (I): wherein A, R 1 , R 2 and R 3 are as defined in the specification, processes for their preparation and their use in HCV treatment are provided.
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US20090274652 |
Hepatitis C Virus Inhibitors
Hepatitis C virus inhibitors having the general formula
are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
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US20090270418 |
PYRAZOLE PYRAZINE AMINE COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS THEREOF AND METHODS OF TREATMENT THEREWITH
Provided herein are Pyrazole Pyrazine Amine Compounds having the following structure:
Wherein Q and R 1 -R 3 are as defined herein, compositions comprising an effective amount of a...
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US20090270416 |
N-OXIDES OF DIARYLUREA DERIVATIVES AND THEIR USE AS Chk1 INHIBITORS FOR THE TREATMENT OF CANCER
The invention provides a Chk-1 kinase inhibiting compound of the formula (I) or a salt, solvate or tautomer thereof, wherein: G is CH 2 , O, NH, NHCO or CONH; A is a group (CH 2 ) n where n is 1...
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US20090270415 |
COMPOUNDS THAT INHIBIT PROTEASE CATHEPSIN S AND HCV REPLICATION
The present invention is directed to compounds that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating...
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US20090270407 |
FUNGICIDAL ISOXAZOLIDINES
Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof,
wherein
A, B, D, R 1 , R 2 , R 3 , X and m are as defined in the disclosure....
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US20090264653 |
USEFUL INDOLE COMPOUNDS
Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.
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US20090264445 |
PYRROLIDINONE GLUCOKINASE ACTIVATORS
Provided herein are compounds of the formula (I):
as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and...
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US20090264444 |
Organic compounds
The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase...
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US20090258884 |
Substituted amides
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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US20090253906 |
ARYL- AND HETEROARYL-SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN
The compounds of the present invention are represented by the chemical structure found in Formula (I):
wherein:
the carbon atom designated * is in the R or S configuration; and X is a fused...
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US20090247550 |
3-TRIFLUOROMETHYL-PYRAZINE-2-CARBOXYLIC ACID AMIDE DERIVATIVES AS HDL-CHOLESTEROL RAISING AGENTS
The present invention relates to pyrazine derivatives of the formula
and pharmaceutically acceptable salts thereof, wherein R 1 to R 8 are as defined in the description and claims for use as...
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US20090247547 |
HYDROXAMATE-BASED INHIBITORS OF DEACETYLASES B
The present teachings relate to compounds of Formula I:
and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R 1 , R 2 , R 3 , Y, Z, and are as defined...
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US20090239877 |
NOVEL 1,2,4-TRIAZOLE DERIVATIVES AND PROCESS OF MANUFACTURING THEREOF
The invention provides 1,2,4-triazole compounds, compositions containing those compounds, methods of treating diseases and/or disorders with those compounds and processes of manufacturing...
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US20090239847 |
Organic compounds
The present invention concerns a compound of formula (I)
or a salt, suitably a pharmaceutically acceptable salt, or solvate thereof, wherein the groups R 1 , R 2 , Ar′, A and Y are defined in...
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US20090233944 |
PYRAZINE-2-CARBOXYAMIDE DERIVATIVES
The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I)
wherein R 1 , R 2 and R 3 are as defined in the specification. These compounds are useful for...
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US20090227601 |
Bradykinin 1 Receptor Antagonists
The invention encompasses novel compounds and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for treatment of diseases mediated by B1 bradykinin receptor.
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US20090227600 |
4-(PYRAZINE-2-YL) -PYRROLIDINE -2-CARBOXYLIC ACID COMPOUNDS AND DERIVATIVES THEREOF AS HEPATITIS C VIRUS INHIBITORS
Anti-viral agents of Formula (Ia)
wherein:
A represents hydroxy; B represents C(O)R 3 wherein R 3 is 4-tert-butyl-3-methoxyphenyl; D represents 1,3-thiazol-2-yl or 5-methyl-1,3-thiazol-2-yl;...
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US20090227594 |
ALIPHATIC AMIDE & ESTER PYRAZINOYLGUANIDINE SODIUM CHANNEL BLOCKERS
The present invention relates to sodium channel blockers. The present invention also includes a variety of methods of treatment using these inventive sodium channel blockers.
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US20090227592 |
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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US20090221824 |
ENANTIOSELECTIVE PROCESS
A process for the production of compounds comprising the enantioselective hydrogenation of 2-substituted acrylic acid derivatives.
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US20090221591 |
Selective Inhibitors of Human Corticosteroid Synthases
The invention relates to compounds for selectively inhibiting human corticosteroid synthases CYP1 1 B1 and CYP1 1 B2, and to the production and use thereof for treating hypercortisolism, diabetes...
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US20090221564 |
Heterocyclic Compounds and Their Use in the Treatment of Cardiovascular Disease
Heterocyclic compounds of the formula (I) are provided: wherein ring A, ring B, R 1 , R 2 , R 3 , R 4 , Y, m, n and q are as identified herein. R 1 is in particular amidino. The invention further...
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US20090214444 |
POLY AROMATIC SODIUM CHANNEL BLOCKERS
Polyaromatic sodium channel blockers represented by the formula:
are provided where the structural variables are defined herein. The invention also includes a variety of compositions,...
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US20090209759 |
AUTOMATED ITERATIVE DRUG DISCOVERY AND SYNTHESIS
The present invention relates to methods and systems for de novo iterative synthesis, an automated iterative drug discovery method and system providing for rapid identification and synthesis of...
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US20090209556 |
SOLUBLE GUANYLATE CYCLASE ACTIVATORS
A compound having the structure
useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, angina pectoris,...
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US20090209555 |
2-PYRAZINONE DERIVATIVES FOR THE TREATMENT OF DISEASE OR CONDITION IN WHICH INHIBITION OF NEUTROPHIL ELASTASE ACTIVITY IS BENEFICIAL
The invention provides compounds of formula
wherein R 1 , R 3 , R 4 , R 5 , R 14 , X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and...
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US20090209554 |
Thiazoliums as transketolase inhibitors
The present invention provides N-3′-pyridyl-methyl or N-2′-pyrazinylmethyl thiazolium derivatives of formula (I) which are useful as transketolase inhibitors wherein R 1 , R 2 , R 3 , Y, R 5 -R...
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US20090203715 |
NOVEL 2-HETARYLTHIAZOLE-4-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND USE AS PHARMACEUTICALS
The present invention relates to 2-hetarylthiazole-4-carboxamide derivatives of the formula (I), the use thereof as medicament for the treatment of various disorders, and processes for the...
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US20090203700 |
Azolylmethyloxiranes, Their Use for Controlling Phytopathogenic Fungi, and Compositions Comprising Them
The present invention relates to azolylmethyloxiranes of the general formula I
in which
A or B is a 6-membered heteroaryl selected from the group consisting of pyridinyl, pyrimidinyl,...
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US20090197927 |
JASMONATE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF
The present invention relates to novel jasmonate derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and...
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US20090197897 |
Novel Oxadiazole Derivatives and Their Use as Positive Allosteric Modulators of Metabotropic Glutamate Receptors
The present invention relates to new compounds which are Oxadiazole derivatives of formula (I) wherein B, P, Q, W, R 1 and R 2 are defined in the description. Invention compounds are useful in...
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US20090197860 |
BIARYL SUBSTITUTED DIAZABICYCLOALKANE DERIVATIVES
The invention relates biaryl substituted diazabicycloalkanes, and more particularly bicycloheteroaryl substituted fused diazabicycloalkane derivatives, compositions comprising such compounds, and...
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US20090192146 |
SUBSTITUTED ORGANOSULFUR COMPOUNDS AND METHODS OF USING THEREOF
The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative...
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US20090186907 |
Pyrazinones As Cellular Proliferation Inhibitors
This invention pertains to a method of inhibiting undesired animal cellular proliferation said method comprising contacting an animal cell with a compound of Formula 1 and all pharmaceutically...
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US20090181968 |
Novel 3-Bicyclocarbonylaminopyridine-2-Carboxamides or 3-Bicyclocarbonylaminopyrazine-2-Carboxamides
The present invention relates to compounds of formula (I) [Chemical formula should be inserted here. Please see paper copy] as well as pharmaceutically acceptable salts and pharmaceutical...
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US20090176799 |
PHOSPHODIESTERASE 4 INHIBITORS
Selective PDE4 inhibition is achieved by 4-(substituted-phenyl)-2-pyrrolidinone compounds. The compounds exhibit improved PDE4 inhibition as compared to compounds like rolipram and show selectivity...
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US20090170874 |
Triazole-substituted arylamides as P2X3 and P2X2/3 antagonists
Compounds of the formula I:
or a pharmaceutically acceptable salt thereof, wherein, R 1 is optionally substituted triazolyl, and R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined...
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US20090170873 |
Pyrazole-substituted arylamides as P2X3 and P2X2/3 antagonists
Compounds of the formula I:
or a pharmaceutically acceptable salt thereof, wherein, R 1 is optionally substituted pyrazolyl, and R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are as defined...
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US20090170872 |
Compounds and Their Pharmaceutical Use
The present invention relates to novel compounds of the general formula (I), their analogs, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable...
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US20090163515 |
Compounds Which Bind to the Active Site of Protein Kinase Enzymes
The present invention relates to a compound and a group of compounds which are inhibitors of Rho kinase (ROK, ROCK). In addition, the invention relates to methods of treatment and use of the...
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