|7378446||Compound having anti-HCV activity and process for producing the same|
The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its having a high degree of replication inhibitory activity against HCV,...
|7378409||Substituted cycloalkylamine derivatives as modulators of chemokine receptor activity|
The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.
|7378448||Diphenylether amide derivatives as opioid receptor antagonists|
A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3′, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mi...
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α4 integrin. They are used as therapeutic agents for various diseases concerning α4 integrin. ...
|7153822||Compositions and methods for modulating connexin hemichannels|
Disclosed are compositions and methods for modulating hemichannel function in a cell, tissue or organ. The invention also relates to useful screens for detecting such compounds, particularly those capable of modulating connexin phosphorylation. Further provided are ...
|7141560||Alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics|
The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of th...
|7129238||Mandelic acid derivatives|
The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acc...
|7060683||Hydroxamate-containing cysteine and serine protease inhibitors|
The present invention is directed to hydroxamate-containing inhibitors of cysteine and serine proteases. Methods for the use of the protease inhibitors are also described. ...
|7026510||Quaternary ammonium salts of omega-aminoalkylamides of r-2-aryl-propionic acids and pharmaceutical compositions containing them|
(R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: where R, R1, R2, R3, X and Z are as defined in the description. The process for their preparati...
|7001907||Peptide-containing α-ketoamide cysteine and serine protease inhibitors|
This invention relates to peptide-containing α-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same. ...
|6992081||Compounds to treat Alzheimer's disease|
The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) useful in treating Alzheimer's disease and other similar diseases. ...
|6916802||Amino ceramide-like compounds and therapeutic methods of use|
The present invention provides amino ceramide-like compounds which inhibit glucosyl ceramide (GlyCer) formation by inhibiting the enzyme GlyCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer sy...
Specified phenylalanine derivatives and analogues thereof have an antagonistic activity to α 4 integrin. They are used as therapeutic agents for various diseases concerning α 4 integrin. ...
|6844299||Polyol ester derivatives of polyamines and use in turbine oils to improve cleanliness|
This invention generally relates to new polyol ester derivatives of polyamines for use as dispersant additives compatible in synthetic ester-based turbo oils. The dispersant additives of the present invention consist of a hydrocarbon acid, a polyol, an amine carrier...
|6831080||Cinnamide derivatives as KCNQ potassium channel modulators|
There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-ben...
|6812229||Carbamate derivative and agricultural/horticultural fungicide|
It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops. A carbamate derivative represented by the general formula [I]
|6770644||Hydroxamic acid derivatives, process for the production thereof and drug containing the same as the active ingredient|
Hydroxamic acid derivatives of the formula (I) (wherein all the symbols have the same meaning as defined in the specification.), non-toxic salt thereof or prodrugs thereof. The compounds of the formula (I) ...
|6753327||Substituted amides, their preparation and use|
An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: ...
|6740741||Diazo derivatives and process for their preparation|
Novel diazo derivatives useful for the deacidification of paper material and the process for their preparation comprising three steps starting from an amine and ethyl chlorocarbonate, are described. ...
|6730784||Urea derivatives useful as synthetic intermediates|
Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-α production inhibitory effects. The pre...
|6635621||Cysteine protease inhibitors|
This invention relates to derivatives of alpha-amino acid amides, to pharmaceutical compositions containing such compounds, and to their use in medicine as inhibitors of cysteine proteases, particularly the cathepsins. A compound of formula (I) is describ...
|6613743||Sulfonamide inhibitors of aspartyl protease|
The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and phy...
|6576628||3-aryl-succinamido-hydroxamic acids, methods for producing said acids and medicaments containing the same|
The invention relates to inhibitors of matrix metalloproteases, more specifically a 3-aryl-succinamido-hydroxamic acid of formula (I) ##STR1## and its salt, ester and derivative thereof, along with methods of producing a compound of formula (I) and pharma...
|6562963||Process for the preparation of macrocyclic metalloprotease inhibitors|
The present invention is directed to a process for the preparation of a compound of formula (X-a) ##STR1## or a pharmaceutically acceptable salt form thereof, wherein: R1 is selected from the group consisting of: C1-5 alkyl substituted wi...
|6534499||N-substituted-N'-substituted urea derivatives and the use thereof as TNF- production inhibitory agents|
N-Substituted-N'-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF- production inhibitory activity. ##STR1##...
|6525036||Compounds and compositions as protease inhibitors|
The present invention relates to novel cysteine protease inhibitors of Formula I: ##STR1## the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them....
|6500983||Hydroxamic acid derivatives|
Novel hydroxamic acid compounds, e.g., of formula I, ##STR1## wherein R1, R2, R3 and R4 are as defined, are found to be useful as pharmaceuticals, e.g., for the suppression of TNF release and the treatment of au...
|6479491||Disubstituted morpholine, oxazepine or thiazepine derivatives, their preparation and their use as dopamine d4 receptor antagonists|
The present invention relates to compounds of formula (I), any of it enantiomers, or any mixture thereof, or a pharmaceutically acceptable acid addition salt thereof, wherein R1, R2, R3, R4, R11, R
|6455502||Compounds and compositions as protease inhibitors|
The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making....
|6452012||3-phenyl-2,6-dioxopiperidin-3-ylpropionamide derivatives and method for preparing same|
This invention relates to 3-(3-phenyl-2,6-dioxopiperidin-3-yl) propionamide derivatives, and to processes for preparing the same....
|6448229||Gamma secretase inhibitors|
The invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CH2, O or S. The compounds inhibit gamma secretase without affecting Notch signalling, and hence find use in the treatment or ...
The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted histidine residues, o...
|6423689||Peptidyl calcium channel blockers|
The present invention provides compounds that block calcium channels having the Formula I shown below. ##STR1## The present invention also provides methods of using the compounds of Formula I to treat stroke, cerebral ischemia, head trauma, or epilepsy an...
|6407064||Aminoalcohol derivative and medicament comprising the same|
An aminoalcohol derivative which is a ceramide analogue, and a medicament, especially an agent for treating neuronal diseases and an agent for protecting brain, comprising the same....
|6407107||Derivatives of butyric acid and uses thereof|
The present invention provides a series of compounds having structural formulas ##STR1## wherein n1 is 1 to 5, n2 is 1 to 4 and m is 1 to 3; X is O or NH; Y is CH2, O, S, NH, NR; R is selected from the group consisting a straigh...
|6384220||Para-aryl or heterocyclic substituted phenyl glucokinase activators|
Para-aryl or heteroaryl substituted phenyl amides which are active as glucokinase activators to increase insulin secretion which makes them useful for treating type II diabetes....
|6380223||Glucocorticoid receptor modulators|
The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compos...
|6372885||Solid-phase technology for the preparation of amides|
Method for preparing a combinatorial chemistry library of compounds of the formula R1--C(.dbd.O)--NH--R2, wherein R1 and R2 are as defined in the specification, which comprises acylating a combinatorial chemistry intermediate of the formula 1A ##STR1...
|6362174||Reduced dipeptide analogues as calcium channel antagonitsts|
The present invention provides novel N-type calcium channel blockers, compositions comprising them, and methods of their use. The compounds of the invention are useful in the treatment of stroke, cerebral ischemia, pain, epilepsy, and head trauma. The nov...
|6344457||Amino acid derivatives inhibiting extracellular matrix metalloproteinase and TNF alpha release|
The invention concerns compounds of general formula (X) in which Y represents in particular --CONHOH, R1 represents in particular a C1 -C5 alkyl group, AA represents an amino acid, or an amino acid sequence, and R3