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8163758 |
Phenyl substituted pyrazinoylguanidine sodium channel blockers possessing beta agonist activity
Provided is class of sodium channel blockers. One example of such a compound is shown by the following formula: The compounds are useful for promoting hydration of mucosal surfaces and treating a...
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8143256 |
Cyclic amide and ester pyrazinoylguanidine sodium channel blockers
The present invention provides compounds represented by formula (I): where the structural variables are defined herein. The compound of the present invention are useful as sodium channel blockers.
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8124607 |
Poly aromatic pyrazinoylguanidine 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, combinations...
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8114881 |
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 R1, R3, R4, R5, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically...
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8114871 |
3-amido-pyrrolo[3,4-C]pyrazole-5(1H,4H,6H) carbaldehyde derivatives
The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to...
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8110579 |
5,6-bisaryl-2-pyridine-carboxamide derivatives, preparation and application thereof in therapeutics as urotensin II receptor antagonists
The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.
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8093252 |
Crystalline polymorphic form of glucokinase activator
A new polymorphic form of 3-{[5-(azetidin-1-ylcarbonyl)pyrazin-2-yl]oxy}-5-{[(1S)-1-me
thyl-2-(methyloxy)ethyl]oxy}-N-(5-methylpyrazin-2-yl)benzami
de, processes for making it and its use as an...
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8084456 |
Pyrazine-based tubulin inhibitors
A compound of general formula (I) or pharmaceutically acceptable prodrugs, salts, hydrates, solvates, crystal forms or diastereomers thereof is described. A method of treating a...
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8076341 |
Compounds and use thereof
A compound of formula (I) wherein R1 is selected from H, F, Cl, Br, CF3, C1-C6 alkoxy and OH; R2 is selected from H and C1-C6 alkyl; n is 1-12; m is O or 1; Y is selected from CH2, NR3, (NR3R4)+X,...
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8071594 |
Substituted diketopiperazines and their use as oxytocin antagonists
Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the notrogen atom to which they are attached represents...
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8071606 |
Substituted pyrazinone amides useful for activation of glucokinase
The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated...
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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...
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8058278 |
Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes
The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium...
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8048886 |
Substituted pyrazine-3-one-derivatives as IAP inhibitors
The present invention relates to novel IAP inhibitor compounds of formula I:
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8039475 |
Co-crystals and pharmaceutical compositions comprising the same
The invention relates to compositions and co-crystals each comprising...
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8034819 |
Glucokinase activator
A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a...
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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...
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8003654 |
N-glycinsulfonamide derivatives and uses as orexin receptor antagonists
The invention relates to novel sulfonamide compounds of the formula (I) and their use as orexin receptor antagonists.
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7998965 |
Glutamate aggrecanase inhibitors
The present invention relates to modulators of metalloproteinase activity.
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7994179 |
Carbamoyl compounds as DGAT1 inhibitors 190
DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use...
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7994178 |
Crystalline rosuvastatin calcium and compositions thereof for treatment of hyperlipidaemia
The present invention provides a crystalline form of rosuvastatin calcium characterized by an X-ray powder diffraction pattern having peaks at about 4.7, 19.4 and 22.3° 2θ±0.2° 2θ. The crys...
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7989456 |
Pyrazine kinase inhibitors
The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of...
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7981898 |
Methods of enhancing mucosal hydration and mucosal clearance by treatment with sodium channel blockers and osmolytes
The present invention relates to methods and compositions for treating diseases ameliorated by increased mucociliary clearance and mucosal hydration by administering an effective amount of a sodium...
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7968577 |
Modulators of glucocorticoid receptor, AP-1, and/or NF-κB activity and use thereof
Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-κB activity including inflammatory and ...
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7956059 |
Aliphatic amide and ester pyrazinoylguanidine sodium channel blockers
The present invention relates to pyrazinoylguanidine compounds represented by formula (I): where the structural variables are defined herein. The compounds are useful as, for example, sodium...
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7932256 |
(S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile: a pyrazinone modulator of corticotropin-releasing factor receptor activity
The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-
2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-c
arbonitrile, pharmaceutical...
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7928138 |
Marine actinomycete taxon for drug and fermentation product discovery
The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature...
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7923448 |
Purine receptor inhibition as a therapeutic strategy in spinal cord and brain
The present invention is directed to a method of treating a subject with acute spinal cord injury by administering a purine receptor antagonist to the subject under conditions effective to treat...
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7919497 |
Analogs of dehydrophenylahistins and their therapeutic use
Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and...
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7884108 |
Certain substituted pyrazinones
Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable...
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7875619 |
Hetero substituted sodium channel blockers
The present invention relates to group of butylphenyl-pyrazinoylguanidine compounds useful as sodium channel blockers. The compounds may be used to promote promoting hydration of mucosal surfaces.
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7868010 |
Capped pyrazinoylguanidine sodium channel blockers
The invention relates to substituted pyrazinoylguanidine compounds. These compounds are useful as sodium channel blockers, and may be effective in treating a variety of conditions including chronic...
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7851476 |
Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine
Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)
-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2
-dioxoethyl]-piperazine its salts and solvates thereof...
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7842697 |
Soluble amide and ester pyrazinoylguanidine sodium channel blockers
The present invention relates to pyrazinoylguanidine compounds represented by the formula: where the structural variables are defined herein. The compounds are useful as sodium channel blockers.
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7824698 |
Lyophilized formulations of Salinosporamide A
Lyophilized formulations comprising Salinosporamide A or analogs thereof are provided. In some aspects, lyophilized formulations comprising Salinosporamide A or analogs thereof and bulking agents...
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7820678 |
Sodium channel blockers
Provided are methods of increasing hydration of mucosal surfaces by topically administering sodium channel blocking pyrazinoylguanidine compounds.
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7812028 |
3-pyridinecarboxamide derivatives as HDL-cholesterol raising agents
The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in...
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7803804 |
Substituted pyrazines for use in the treatment of inflammatory or allergic conditions
Disclosed herein are substituted pyrazine compounds and tautomers, stereoisomers, solvates, or pharmaceutically acceptable salts thereof for the treatment of conditions mediated by the blockade of...
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7772228 |
Method for treatment of bacterial infections with once or twice-weekly administered rifalazil
A method for treatment of bacterial infections with rifalazil administered once-weekly, or twice-weekly. A method for treatment of tuberculosis caused by Mycobacterium tuberculosis, infections...
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7745444 |
Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life...
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7745442 |
Methods of reducing risk of infection from pathogens
Prophylactic treatment methods are provided for protection of individuals and/or populations against infection from airborne pathogens. In particular, prophylactic treatment methods are provided...
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7737151 |
Pyrazine kinase inhibitors
The present invention relates to compounds useful as inhibitors of protein kinases of the following formula: or a pharmaceutically acceptable salt thereof. The invention also provides...
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7737152 |
6-carboaryl-oxy-pyrazin-2-yl-carboaryl-amines and compositions comprising said compounds
The present invention pertains to certain 6-carboaryloxy-pyrazin-2-yl-carboaryl-amines of the following formula, and pharmaceutically acceptable salts thereof, which, inter alia, inhibit RAF (e.g.,...
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7727991 |
Substituted melanocortin receptor-specific single acyl piperazine compounds
Melanocortin receptor-specific compounds of the general formula and pharmaceutically acceptable salts thereof, where J is a substituted or unsubstituted monocyclic or bicyclic ring structure, W is...
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7709478 |
Acylated 6,7,8,9-tetrahydro-5H-benzocycloheptenyl amines and their use as pharmaceutical agents
The present invention relates to compounds according to the general formula (I), wherein R1-R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1-C3-alkyl), B, C and D are i...
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7704995 |
Protein kinase modulators and methods of use
This invention relates to compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and...
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7662825 |
N-pyrazinyl-phenylsulphonamides and their use in the treatment of chemokine mediated diseases
The invention provides N-pyrazinyl-phenyl-sulphonamides of formula (I) for use in the treatment of chemokine mediated diseases. Particularly inflammatory diseases, such as asthma.
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7629346 |
Pyrazinecarboxamide derivatives as CB1 antagonists
The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful...
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7608618 |
Urea or thiourea substituted 1,4-pyrazine compounds useful as anti-cancer agents and for inhibiting Chk1
Compounds of the formula wherein: Y′ is O or S, W′ is optionally substituted, Z′ is selected from the group consisting of wherein Q′ is OR7 and R7 is C1-3alkyleneC3-8heterocycloalkyl useful in the ...
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7598241 |
Carboxamide derivatives and their use as factor Xa inhibitors
Novel compounds of the formula (I) in which R1, D, X, W, Y and T have the meaning indicated in Patent Claim (1), e.g. (II), are inhibitors of coagulation factor Xa and can be employed for the...
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