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8183245 Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1  
The present invention relates to pyrazine substituted pyrrolopyridines having formula (I) useful as inhibitors of JAK kinases (JAK1, JAK2, JAK3 and/or TYK2) and/or PDK1 and for the treatment of...
8183371 Pyrazines as delta opioid receptor modulators  
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein...
8183275 Substituted imidazoles as bombesin receptor subtype-3 modulators  
Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful...
8178131 Pyrrolopyridines as kinase inhibitors  
Compounds of Formula (I) are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula (I) and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in...
8163757 Immuno inhibitory pyrazolone compounds  
The present invention relates to compounds of formula (IA) or (IB) or pharmaceutically or veterinarily acceptable salt thereof:
8158647 Substituted pyrrolopyridines and pyrazolopyridines as kinase modulators  
Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said...
8153634 Carbinol derivatives having cyclic linker  
[Object] To provide a novel LXRβ agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; ...
8153635 Compounds and compositions as modulators of GPR119 activity  
The invention provides compounds of Formula I: wherein A, L, m, q, Q, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention. The invention further provides for pharmaceutical...
8153638 Metabotropic glutamate-receptor-potentiating isoindolones  
Compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation,...
8148380 Antibacterial amide and sulfonamide substituted heterocyclic urea compounds  
The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and...
8138189 Substituted benzene compounds as modulators of the glucocorticoid receptor  
The present invention relates to compounds of formula I wherein R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds...
8133908 Heteroaryl derivatives of N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]hept-4-yl]methyl}-2-amine  
Disclosed are N-{[(1S,4S,6S)-3-(2-pyridinylcarbonyl)-3-azabicyclo[4.1.0]he pt-4-yl]methyl}-2-heteroarylamine derivatives having the following formula: wherein m, n, Het, R1, R2 and R3 are as...
8129389 Substituted oxindole derivatives, medicaments containing the latter and use thereof  
The invention relates to novel oxindole derivatives of general formula (I), in which the substituents A, B, R1, R2 and R3 are defined as cited in claim 1, to medicaments containing said derivatives...
8129372 Compounds having NPY Y5 receptor antagonistic activity  
This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or...
8129415 Fungicide hydroximoyl-tetrazole derivatives  
The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L1 and L2 represent various...
8124789 Method for producing glycosylated indole compound and antibody against the compound  
This invention provides a method of producing a large amount of an α-form or β-form of N-pyranosyl-tryptophan having a specified structure and preparing an antibody therefrom. The method c...
8119644 Thiadiazole-substituted arylamides as P2X3 and P2X2/3 antagonists  
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted thiadiazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also...
8119643 Benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses  
Biologically active chemical compounds, namely benzoimidazolyl-pyrazine derivatives and structurally related compounds, are disclosed herein. Such compounds include those represented by structural...
8114893 Compounds and methods of use  
In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In...
8106048 Heterocyclic NF-κB inhibitors  
The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, (I) wherein R1 is independently hydrogen, alkyl, cycloalkyl,...
8101620 Heterocyclic sulfonamides  
Provided is a compound of the following formula: wherein: R3 is an aryl or heteroaryl group, which is optionally substituted with a halogen, lower alkoxy, aryl or heteroaryl group;R4 is halogen;R5...
8093275 Oxazolone and pyrrolidinone-substituted pryidine amides as P2X3 and P2X2/3 antagonists  
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, X, Y, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of using the compounds for...
8093241 Acid amide derivatives, process for their production and pesticides containing them  
The present invention relates to an acid amid derivative of the formula (I) or a salt thereof: wherein A is phenyl which may be substituted by X, benzyl which may be substituted by X, naphthyl...
8088771 Cycloalkylidene and heterocycloalkylidene inhibitor compounds  
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to...
8067420 Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods  
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are...
8063044 Pyrazole derivatives  
This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, wherein R1 to R4 are defined in the description, and to...
8058045 Pyrazin-2-yl-pyridin-2-yl-amine and pyrazin-2-yl-pyrimidin-4-yl-amine compounds and their use  
The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain biarylamine compounds (referred to herein as BAA compounds), and especially certain...
8049016 Thiazole derivatives which inhibit stearoyl-CoA desaturase enzymes  
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...
8039623 Inhibitors of serine proteases, particularly HCV NS3-NS4A protease  
The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C...
8030316 Malate salt of (2R)-methyl-1-{3-[2-(3-pyridinyloxy)ethoxy]-2-pyrazinyl}piperazine  
The present invention relates to a process for the preparation of compounds which are therapeutically active in the central nervous system. In one aspect, the invention relates to a process for the...
8030309 Viral polymerase inhibitors  
An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as...
8026370 Carboxylic acid derivative containing thiazole ring and pharmaceutical use thereof  
According to the present invention, a compound represented by the following formula (I) having a superior PPARα agonist action and concurrently showing a hypolipidemic action can be provided, and ...
8022210 Soluble amide and ester pyrazinoylguanidine sodium channel blockers  
The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where X, Y and R1-R4 are as defined herein. The compounds of the present invention are useful as sodium...
8022221 Aurora kinase modulators and method of use  
The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating...
8017610 Phenylpyrrole derivative  
The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or...
8017601 Bis-aryl kinase inhibitors and method  
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
8017608 5-Phenylthiazole derivatives and their use as p13 kinase inhibitors  
Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol...
8012984 Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods  
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R2, R3, R8, and R9 are...
8012989 Substituted pyrimidine compounds and their utility as CETP inhibitors  
A compound represented by the following general formula (I), wherein R1, R2, R3, R4 and R5 represent hydrogen atom, a halogen atom, a lower alkyl group and the like, R6 represents an alkyl group, a...
8012956 Tropane compounds  
A compound according to Formula I or II: wherein R1, R1b, R2, L1, and L2 and L2b are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
8008481 Indazole compounds  
Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are...
8008494 Soluble amide and ester pyrazinoylguanidine sodium channel blockers  
The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where X, Y and R1-R4 are as defined herein. The compounds of the present invention are useful as sodium...
7998959 Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same  
The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1 and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of ...
7994177 Therapeutic agents useful for treating pain  
The present invention discloses a compound of formula: where Ar1, Ar2, X, Z1, Z2, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Pyridylene Compound”); com...
7989621 Method for producing substituted imidazo[1,2-A]pyrazines of (s)-1-(3-(2-sec-butyl-6-(1h-indol-3-yl)-3-oxo-3,7-dihydroimadazo[1,2-a]pyrazin-8-yl)propyl)guanidine  
The present invention relates to a method for producing marine ostracod crustacean luciferin or a derivative thereof represented by a general formula (4), characterized by reacting a compound...
7989637 Triazole-substituted arylamides as P2X3 and P2X2/3 antagonists  
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted triazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed...
7985762 Inhibitors of serine proteases  
The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C...
7981925 Compounds that modulate intracellular calcium  
Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of...
7977367 Substituted imidazole propanamide glucokinase activators  
The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by...
7977340 Antibacterial compositions  
Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical...
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