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7514425 |
Short-acting sedative hypnotic agents for anesthesia and sedation
The invention provides compounds compositions and methods useful for inducing or maintaining general anesthesia or sedation in mammals.
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7405209 |
Protease inhibitors
The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K,...
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7351702 |
Caspase inhibitors and uses thereof
This invention provides compounds of formula I:
wherein Z is oxygen or sulfur; R 1 is hydrogen, —CHN 2 , R, CH 2 OR, CH 2 SR, or —CH 2 Y; next to R 3 represents a single or double bond;...
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7351703 |
Sulfonylamino carboxylic acid N-arylamides as guanylate cyclase activators
The present invention relates to compounds of the formula I
in which A 1 , A 2 , R 2 and R 3 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds for...
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7285547 |
Amidinophenylalanine derivatives as thrombin inhibitors
The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein...
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7235647 |
Intermediate and process for preparing of β- anomer enriched 21-deoxy,21,21-difluoro-D-ribofuranosyl nucleosides
The present invention provides a highly stereoselective, simple and economical glycosylation process for preparation of β-anomer enriched 2 1 -deoxy-2 1 ,2 1 -D-ribofuranosyl difluoronucleosides...
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7160874 |
Phenylalanine derivatives
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.
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7132451 |
Inhibition of TNF-α-initiated neutrophil response
The impact of lipoxin A 4 (LXA 4 ) and aspirin-triggered-lipoxins (ATL) was investigated in tumor necrosis factor (TNFα)-initiated neutrophil (PMN) responses in vitro and in vivo using...
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7071184 |
Protease inhibitors
The present invention provides C 1-6 alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin...
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6953789 |
Thiol compounds, their production and use
The present invention provides a compound represented by Formula:
wherein ring A and ring B may be same or different and each is an optionally substituted homocyclic or heterocyclic ring and...
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6906059 |
Pharmaceutical composition with protective action against oxidative/toxic substances, especially cardiotoxic substances
The use of benzazepin-N-acetic acid derivatives which contain an oxo group in the a position to the nitrogen atom and are substituted in the 3 position by a...
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6887864 |
Azepane derivatives
This invention provides novel azepane derivatives or pharmaceutically acceptable salts thereof, according to the general formula (I)
wherein the symbols are defined in the specification, as...
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6787560 |
Serotonin reuptake inhibitor
A serotonin reuptake inhibitor containing a cyclic amine represented by the following formula, a prodrug thereof, or a pharmaceutically acceptable salt of said cyclic amine or prodrug as an active...
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6579889 |
Substituted isonipecotyl derivatives as inhibitors of cell adhesion
Compounds of Formula I are antagonists of VLA-4 and/or α 4 β 7 , and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds...
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6534536 |
Alkylsulfonamido heterocyclic thrombin inhibitors
Alkylsulfonamido heterocyclic thrombin inhibitors are provided which have the structure wherein G is wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; R is hydrogen, hydroxyalkyl,...
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6506802 |
Disulfide derivatives useful for treating allergic diseases
Novel disulfide derivatives useful for preventing or treating allergic diseases of the eye, nose, skin, ear, gastrointestinal tract, airways or lung and preventing or treating manifestations of...
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6495544 |
Homoiminopiperidinyl hexanoic acid inhibitors of inducible nitric oxide synthase
Homoiminopiperidinyl Hexanoic Acid derivatives and pharmaceutically acceptable salts thereof useful in the inhibition of the inducible isoform of nitric oxide synthase are disclosed.
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6486151 |
N-oxides of heterocyclic esters, amides, thioesters, and ketones
This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their...
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6462073 |
N-hydroxy-2-(alkyl, aryl, or heteroaryl sulfanyl, sulfinyl or sulfonyl)-3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors
Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases...
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6455520 |
Benzamide derivatives and their use as cytokine inhibitors
The invention concerns amide derivatives of formula (I) wherein R 3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R 1 and R 2 is a group such as hydroxy, halogeno,...
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6451817 |
Alpha-substituted-1-benzyl-napthyls
This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are α-substituted with ether, thioether, amino, hydrazino, cyano or halo...
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6403584 |
Substituted nipecotyl derivatives as inhibitors of cell adhesion
Compounds of Formula I are antagonists of VLA-4 and/or α 4 β 7 , and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds...
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6376468 |
Protein:prenyl transferase inhibitors
The invention pertains to novel peptide analogs suitable for inhibiting protein:prenyl transferases. As such they are therapeutically useful in e.g. inhibiting oncogenesis and other unwanted cell...
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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,...
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6346547 |
N-substituted amino acids, antioxidant pharmaceutical compositions containing n-substituted amino acids and methods for preventing cardiovascular diseases and/or preventing and/or treating antioxidant responsive diseases therewith
Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general...
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6344466 |
Benzamide and sulfonamide substitued aminoguanidines and alkoxyguanidines as protease inhibitors
The present invention is directed to aminoguanidine and alkoxyguanidine compounds, including compounds of Formula I: wherein X is O or NH, L is —O— or —SO 2 —, and R 1 -R 4 , R 9 -R 19 ,...
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6251919 |
Heterocyclic substituted aniline calcium channel blockers
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6251949 |
Oxime derivatives, hydrazone derivatives and use thereof
Compounds having fungicidal activities and represented by general formula (I) and salts and hydrates thereof ##STR1## wherein R 1 represents an optionally substituted aryl, an optionally...
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6191125 |
Small molecule pipecolic acid derivative hair growth compositions and uses
This invention relates to pharmaceutical compositions and methods for treating alopecia and promoting hair growth using pipecolic acid derivatives.
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6191144 |
Method of using angiotensin converting enzyme inhibitor to stimulate angiogenesis
The present invention is directed to the use of a group of ACE inhibitors to stimulate angiogenesis in mammals or in mammalian tissue in vitro. Specifically, the present invention is directed to...
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6140338 |
Chemokine receptor antagonists
The present invention relates to a compound of the general formula: ##STR1## wherein each of R 1 and R 2 which may be the same or different, is e.g. a hydrogen atom, a halogen atom or a lower...
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6107291 |
Azepine or larger medium ring derivatives and methods of use
Selected novel azepine and larger medium ring compounds are effective for prophylaxis and treatment of inflammation, tissue degradation and related diseases. The invention encompasses novel...
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6046211 |
Amidino derivatives useful as nitric oxide synthase inhibitors
The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.
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6034067 |
Serine protease inhibitors
The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can...
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6030971 |
Methods and compositions for controlling biofouling using amides
The present invention relates to a method to inhibit bacteria from adhering to a submergible surface. The method contacts the submergible surface with an effective amount of at least one amide to...
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5952354 |
Tris carbamic acid esters: inhibitors of cholesterol absorption
Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are...
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5939437 |
CCK and gastrin receptor ligands
Compounds of formula (I) and their pharmaceutically active salts are gastrin and CCK receptor ligands, where Ar is a monocyclic aromatic group, R 1 is halo, amino, nitro, cyano, sulphamoyl,...
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5932196 |
Buffered emulsion compositions containing actives subject to acid or base hydrolysis
The present invention are for emulsion compositions and the process for making such compositions containing biological and cosmetic actives subject to hydrolysis of actives during processing and...
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5877203 |
Treatment for atherosclerosis and other cardiovascular and inflammatory diseases
Dithiocarboxylates, and in particular, dithiocarbamates, block the induced expression of the endothelial cell surface adhesion molecule VCAM-1, and are therefor useful in the treatment of...
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5858402 |
Methods for in vivo reduction of cyanide levels and compositions useful therefor
In accordance with the present invention, there are provided in vivo methods for the reduction of cyanide levels. The present invention employs a scavenging approach whereby cyanide is bound in...
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5859002 |
HIV protease inhibitors
HIV protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These...
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5854234 |
Amidino dervatives useful as nitric oxide synthase inhibitors
The current invention discloses useful pharmaceutical compositions containing azepine derivatives useful as nitric oxide synthase inhibitors.
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5849732 |
Phenol compound having antioxidative activity and the process for preparing the same
Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R 0 represents H, alkyl or alkyloxy; R 1 represents alkyl; R 2 represents alkyl or alkyloxy; OR 3 represents OH;...
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5776927 |
Methionine sulfone and S-substituted cysteine sulfone derivatives as enzyme inhibitors
This invention relates to compounds which inhibit thrombin or factor Xa. The compounds contain an aldehyde functionality and a methionine sulfone or S-substituted cysteine sulfone residue. The...
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5773434 |
Facilitation of AMPA receptor-mediated synaptic transmission in brain as a treatment for schizophrenia
Psychotic symptoms are treated by the administration of drugs which amplify the ability of natural stimulators of AMPA receptors to enhance the mediation of excitatory synaptic response. What is...
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5741799 |
Heterocyclic thrombin inhibitors
Heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein n, R, R 1 , R 2 , R 3 , G, G x , R 6 ', Ra, Xa, R 6 , Rb, R 3 , p, Q, A and R 4 are as defined herein.
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5691356 |
Disubstituted heterocyclic thrombin inhibitors
Disubstituted heterocyclic thrombin inhibitors are provided which have the structure ##STR1## wherein G is ##STR2## wherein n is 0, 1 or 2 or 3; m is 0, 1, 2 or 3; Y is NH or S; p is 0, 1 or 2, Q...
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5677344 |
Method for treating Parkinson's disease employing an ATP-sensitive potassium channel blocker
A method is provided for treatment of Parkinson's disease or controlling movement of a Parkinsonian patient by administering an ATP-sensitive potassium channel blocker, such as a sulfonyl urea,...
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5674864 |
N-substituted derivatives of α-mercapto alkylamines, their preparation process and the intermediates obtained, their use as medicaments and the compositions containing them
Novel α-mercapto-alkylamines in all possible racemic, enantiomeric and diastereoisomeric forms of the formula ##STR1## wherein the substituents are as defined in the specification.
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5639746 |
Hydroxamic acid-containing inhibitors of matrix metalloproteases
The invention provides hydroxamic acid-containing compounds which are useful as inhibitors of matrix metalloproteases and which are effective in treating conditions associated with excess activity...
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