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7625900 |
Sutstituted tetrahydropyrrolopyrazine compounds and the use thereof in the treatment and/or inhibition of pain
Substituted tetrahydropyrrolopyrazine compounds corresponding to the formula I:
processes for their preparation, pharmaceutical compositions comprising these compounds and the use of these...
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7618978 |
Amides as BACE inhibitors
The present invention provides BACE inhibitors of Formula (I): methods for their use, and intermediates and methods for their preparation.
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7618966 |
Abnormal Cannabidiols as agents for lowering intraocular pressure
The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular...
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7595329 |
Benzimidazolone carboxylic acid derivatives
This invention relates to compounds of the formula (I):
wherein R 1 , R 2 , R 3 , A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions...
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7582766 |
Inhibitors of papilloma virus
The use of a compound of formula (II):
or its enantiomers or diastereoisomers thereof, or salts or pharmaceutically-acceptable esters thereof, in the treatment or prevention of a papilloma...
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7572792 |
Azetidine glycine transporter inhibitors
The present invention is directed to azetidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with...
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7569588 |
Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I:
wherein a, b, c, m, p, r, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , W and X 1 are as defined in the specification. The compounds of formula I are...
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7531664 |
Flame retarding compounds
Novel flame retarding compounds that comprise at least one sterically hindered nitroxyl, hydroxylamine or hydrocarbyloxyamine moiety and at least one conventional organohalogen or organophosphorus...
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7528154 |
Polyarylcarboxamides useful as lipid lowering agents
Polyarylcarboxamide compounds of formula (I)
are useful as lipid lowering agents.
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7528153 |
Deoxynojirimycin analogues and their uses as glucosylceramidase inhibitors
The invention provides a new class of deoxynojirimycin analogues, or pharmaceutically acceptable salts thereof which can suitably be used for the treatment of a disease selected from the group...
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7524963 |
Synthesis of (4-bromophenyl)(4-piperidyl)methanone-(Z)-O-ethyloxime and salts
In one embodiment, the present invention describes the synthesis of (4-bromophenyl) (4-piperidyl)methanone-(Z)-O-ethyloxime and its acid salts, and similar compounds, in high stereochemical purity.
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7524867 |
Tetrasubstituted imidazole derivatives as cannabinoid CB1 receptor modulators with a high CB1/CB2 receptor subtype selectivity
The present invention relates to 1,2,4,5-tetrasubstituted imidazole derivatives as selective cannabinoid CB 1 receptor modulators, in particular CB 1 receptor antagonists or inverse agonists...
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7507767 |
Cannabinoid receptor ligands
There are disclosed compounds of the formula
a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit...
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7498344 |
Arylpiperidinol and arylpiperidine derivatives and pharmaceuticals containing the same
A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and...
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7498328 |
Derivatives of sulphonamides, their preparation and use as medicaments
The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their...
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7435824 |
Prodrugs of potassium channel inhibitors
Compounds useful as prodrugs of potassium channel inhibitor compounds, in particular as prodrugs of Kv1.5 channel inhibitors.
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7432284 |
Estrogen receptor modulators
The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen...
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7425631 |
Compounds and methods of use
Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically...
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7423061 |
Substitute thiophenes and uses thereof
This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical salts, compositions and methods of use. These novel compounds provide a treatment or...
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7423012 |
Phosphinyloxy, oxime and carboxylic acid derivatives which are useful as carboxypeptidase U inhibitors
The present invention relates to compounds of Formula I, and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts,
which compounds inhibit carboxypeptidase U and...
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7417059 |
Substituted aromatic-ring compounds, process for producing the same and use
The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production,...
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7414054 |
3-(arylamino)methylene-1, 3-dihydro-2H-indol-2-ones as kinase inhibitors
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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7408067 |
Aza-cyclic compounds as modulators of acetylcholine receptors
Compounds comprising an aza-cyclic portion and an aromatic portion linked via a sulphur atom are disclosed. The compounds disclosed are selective modulators of beta 4 subtype nicotinic...
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7408066 |
Carbon-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists
Disclosed are compounds of the formula
or a pharmaceutically acceptable salt thereof, wherein:
M 1 and M 3 are CH or N; M 2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH 2...
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7405229 |
Cathepsin cysteine protease inhibitors
This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These...
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7388007 |
Gamma-lactams as beta-secretase inhibitors
There is provided a series of novel substituted gamma-lactams of Formula (I)
or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 4 , R 5 and R 6 as defined...
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7385060 |
Method for producing salts of tolperisone
The invention relates to a method for producing an addition salt of 2,4′-dimethyl-3-piperidino-propiophenone (tolperisone) with a pharmaceutically acceptable acid, of formula (I). According to...
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7381734 |
Serine protease inhibitors
Compounds of formula (I)
where R 5 , R 6a , each X, L, Cy and Lp are as defined in the specification, are tryptase inhibitors useful as antiinflammatory agents.
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7381727 |
Pyrrole derivatives, their preparation and their therapeutic use
The invention concerns compounds of formula (I):
Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are as defined herein. The invention also concerns the method for preparing said...
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7378525 |
CCR8 inhibitors
Disclosed are CCR8 inhibitors represented by Structural Formulas (I):
The variables in Structural Formula (I) are described herein. Also disclosed are methods of treating a subject with a CCR8...
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7368443 |
2,6-disubstituted piperidines and piperazine compounds
The present invention is directed to 2,6-disubstituted piperidine and piperazine analogs having the following general formula:
which are used to treat diseases of the central nervous system,...
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7345174 |
Cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
The present invention provides the compound having the formula:
wherein each of R 1 and R 2 is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino,...
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7345059 |
Diphenylpyridine derivatives, preparation and therapeutic application thereof
The invention relates to 5,6-diphenylpyridine-3-carboxamide derivatives of general formula (I):
where:
R 1 represents hydrogen or a (C 1 -C 4 )alkyl; R 2 represents:
a monoazo...
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7332487 |
Nitrogen-containing 5-membered ring compound
The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]:
wherein symbols in the formula have the following meanings;
...
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7329755 |
CCR8 inhibitors
Disclosed is an inhibitor of CCR8 that is represented by Structural Formula (I):
Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a...
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7326716 |
Treatment of inflammatory bowel disease
The present invention provides a method of treating inflammatory bowel disease which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of...
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7320978 |
Oxazole derivatives, preparation and therapeutic use thereof
This invention 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 described herein. The invention further relates to a method for prevention...
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7312218 |
Sulfonylaminovalerolactams and derivatives thereof as factor Xa inhibitors
The present application describes sulfonylaminovalerolactams and derivatives thereof of Formula Ia-If:
or pharmaceutically acceptable salt forms thereof, wherein ring G is a mono- or bicyclic...
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7309709 |
Thiazole sulfonamide compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula:
wherein R 1 to R 6 , X, Z and A are as defined. These compounds have activity inhibiting production of Aβ-peptide. The invention...
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7291633 |
6H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands
Compounds of the formula I in which R 1 , R 2 , R 3 and R 4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the...
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7291617 |
Arylamidine derivative or salt thereof
An arylamidine derivative represented by a general formula described below or a salt thereof has an excellent antifungal action and high safety, and it is useful as an antifungal agent with good...
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7282499 |
Sigma receptor inhibitors
The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to some pyrazole derivatives, to processes of preparation of such compounds, to...
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7276607 |
5-HT7 receptor antagonists
Substituted carbocyclic sulphonamide derivatives of formula (I), in which n is 0 or 1 and the other variables are as defined in the claims, are selective 5-HT 7 receptor antagonists and are...
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7265226 |
1-alkyl-4-(3-substitutedphenyl)piperidines
8-Substituted-2,6-methano-3-benzazocines of general structure I in which A is —CH 2 —OH, —CH 2 NH 2 , —NHSO 2 CH 3 ,
and Y is O, S or
NOH are useful as analgesics, anti-diarrheal...
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7256186 |
Gamma secretase inhibitors
This invention discloses novel gamma secretase inhibitors of the formula:
wherein:
R 1 is a substituted aryl or substituted heteroaryl group; R 2 is an R 1 group, alkyl, —XC(O)Y,...
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7253205 |
Gem-disubstituted cyclohexane derivatives and their use as therapeutic agents
The present invention relates compounds of the formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 represent a variety of substituents, ring A is a phenyl or pyridyl...
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7241760 |
Heteroaryl-substituted imidazole derivatives
The present invention relates to imidazole derivatives of the general formula
wherein R 1 , R 2 , R 3 and R 4 are described hereinbelow. These compounds can be used in the treatment or...
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7238710 |
EP4 receptor agonist, compositions and methods thereof
This invention relates to potent selective agonists of the EP 4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which...
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7238709 |
Therapeutic carbamates
This invention relates to hindered carbamate derivatives that are muscarinic receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.
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7232817 |
α- and β-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors
α- and β-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
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