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6576630 |
Compounds and compositions as protease inhibitors
The present invention relates to novel alkanoyl-substituted heterocyclic derivatives which are cysteine protease inhibitors; the pharmaceutically acceptable salts and N-oxides thereof; their uses...
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6566375 |
Elevation of HDL cholesterol by 4-&lsqb (aminothioxomethyl)-hydrazono&rsqb -N-(substituted)-4-arylbutanamides
Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis. These...
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6566376 |
Diphenyl-piperidine derivative
The invention provides compounds of general formula (I) wherein R 1 , R 2 , R 3 , R 4 , A, Q, U, V, W, X, Y and n are as defined in the specification, processes for their preparation,...
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6562828 |
Amidine compounds
A compound of the formula [I] wherein R 1 , R 2 and R 3 are the same or different and each is hydrogen atom, wherein each symbol is as defined in the specification, a salt thereof or a prodrug...
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6559146 |
Aminophenoxyacetic acid derivatives as neuroprotectants
There is provided an aminophenoxyacetic acid derivative of the following formula (I): wherein, R 1 , R 2 , R 3 and R 4 are, independent from each other, alkoxy group, alkyl group or aryl...
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6552046 |
Materials and methods for the treatment of gastroesophageal reflux disease
The subject invention provides novel compounds and compositions for the safe and effective treatment of gastroesophageal reflux and related conditions. In a preferred embodiment, the compositions...
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6552041 |
Cyclized amide derivatives
The present invention relates to cyclized amide derivatives of formula (I) These cyclized amide derivatives are useful for treating or preventing neuronal damage associated with neurological...
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6548520 |
Substituted imidazoles having anti-cancer and cytokine inhibitory activity
The present invention is related to novel 2-alkyl substituted imidazoles of formula (I) useful for the treatment of CSBP kinase mediated diseases.
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6545021 |
Use of substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds for treating hepatitis virus infections
N-Substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds of Formula I are effective in treatment of hepatitis infections, including hepatitis B and hepatitis C. In treating hepatitis infections,...
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6544987 |
Compounds, compositions, and methods for stimulating neuronal growth and elongation
The present invention concerns methods, pharmaceutical compounds, and compositions for stimulating neuroite outgrowth in nerve cells leading to nerve regeneration. These methods, compounds and...
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6537996 |
Modulators of p38 MAP kinase
Compounds of formula 1 are effective modulators of p38 MAP kinase. wherein R 1 is H, lower alkyl, or OR 5 , where R 5 is aryl, heterocyclyl, acyl, N—R 6 -4-piperidinyl, N—R 6...
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6531494 |
Gem-substituted αvβ3 antagonists
The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula...
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6528532 |
Urea derivatives as HIV aspartyl protease inhibitors
The present invention provides HIV aspartyl protease inhibitors of the formula: and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof,...
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6528531 |
Aliphatic hydroxy substituted piperidyl diaryl pyrrole derivatives as antiprotozoal agents
Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
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6511990 |
Class of 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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6511993 |
Metalloprotease inhibitors
Compounds of formula (I) and pharmaceutically-acceptable derivatives thereof, are matrix metalloprotease inhibitors, useful in treatment of conditions mediated by matrix metalloproteases, such as...
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6509337 |
Arylsulfonyl Hydroxamic Acid derivatives as MMP and TNF inhibitors
A compound of the formula wherein R 1 -R 9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration,...
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6500823 |
Unsaturated hydroximic acid derivatives as per abstract inhibitors
The object of the invention consists of novel unsaturated hydroximic acid derivatives, the process for their preparation and as active substance such as compounds containing pharmaceutical...
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6498161 |
Pyrrolidine modulators of chemokine receptor activity
The present invention is directed to pyrrolidine compounds of the formula I: (wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and n are defined herein) which are useful as modulators of chemokine...
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6495568 |
Hydroxamic acid derivatives as matrix metalloprotease (MMP) inhibitors
Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line...
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6492392 |
2-piperidone compounds
The present invention provides 2-piperidone compounds or pharmaceutically acceptable salts thereof, which have a potent activity of inhibiting the proliferation of tumor cells and thus are useful...
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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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6479482 |
Alkylamine derivatives of dihydropyridine NPY antagonists
A series of non-peptidergic antagonists of NPY have been synthesized and are comprises of amino and piperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula 1. where X is CH or N As...
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6476054 |
Cyclic amine modulators of chemokine receptor activity
The present invention is directed to cyclic amines of the formula I: (wherein R 1 , R 2 , R 3 , m and n are defined herein) which are useful as modulators of chemokine receptor activity. In...
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6472392 |
Triazole compounds and the use thereof as dopamine-D3 -ligands
Triazole compounds of the following formula: where Ar 1 , A, B and Ar 2 have the meanings given in the description, possess a high affinity for the dopamine D 3 receptor and can therefore be...
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6465484 |
Angiogenesis inhibitors
The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to...
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6465491 |
6-phenylpyridyl-2-amine derivatives
The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and...
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6465482 |
Arylpiperazinyl-cyclohexyl indole derivatives for the treatment of depression
Compounds are provided which are useful for the treatment of serotonin-affected neurological disorders which comprise Wherein: R 1 , R 2 and R 3 are each, independently, hydrogen, halogen, CF...
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6462036 |
Tricyclic pyrazole derivatives
This invention relates to certain 3-aryl or 3-heteroaryl pyrazoles with 4,5(3,4)-bicyclic ring fusion which are inhibitors of protein kinase activity, of which some are novel compounds, to...
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6458789 |
2-aminopyridine derivatives and combinatorial libraries thereof
The present invention relates to novel 2-aminopyridine derivative compounds of the following formula: wherein R 1 to R 5 have the meanings provided herein. The invention further relates to...
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6458806 |
Aryl alkenamides derivatives as MCP-1 antagonists
Aryl alkenamides derivatives of Formula I or a pharmaceutically acceptable salt thereof are novel MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis,...
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6451791 |
Amidoaromatic ring sulfonamide hydroxamic acid compounds
An amidoaromatic ring sulfonamide hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as are a treatment process that comprises administering a...
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6451806 |
Methods and compositions involving opioids and antagonists thereof
Novel methods and compositions comprising opioids and opioid antagonists. In preferred embodiments, the methods and compositions comprise opioids and peripheral mu opioid antagonist compounds. The...
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6451816 |
Use of pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides in the treatment of tumors or for immunosuppression
The invention relates to the use of pharmacologically valuable pyridyl alkane, pyridyl alkene and/or pyridyl alkine acid amides according to general formula (I) in the treatment of tumors or for...
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6451797 |
Muscarinic antagonists
Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts and solvates) wherein wherein one of...
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6448268 |
Aryl-&lcub 4-fluoro-4-&lsqb (2-pyridin-2-yl-ethylamino)-methyl&rsqb -piperidin-1-yl&rcub -methanone derivatives as 5-ht1 receptor antagonists
The invention concerns novel ary1-{4-fluoro-4-[(2-pyridin-2-yl-ethylamino)-methyl]-piperi
din-1-yl}-methanone derivatives of formula(1) wherein X is a hydrogen, fluorine or chlorine atom useful as...
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6444675 |
4-alkyl and 4-cycloalkyl derivatives of dihydropyridine NPY antagonists
A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of 4-alkyl and cycloalkyl derivatives of dihydropyridines of Formula I. As antagonists of NPY-induced...
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6444679 |
4-phenyl-4-heteroarylpiperidine derivatives
The present invention relates to compounds of the formula I, wherein Z 1 , X, Y, ( ) n , R 1 , R 2 and R 3 are defined as in the specification, pharmaceutical compositions containing such...
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6444677 |
5-membered heteroaryl substituted 1,4-dihydropyridine compounds as bradykinin antagonists
This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein A is independently halo; Y 1 is —(CH 2 ) m —, C(O) or S(O); Y 2 is N or CH;...
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6440998 |
Pharmaceutical composition having enhanced antitumor activity and/or reduced side effects, containing an antitumor agent and an hydroximic acid derivative
Pharmaceutical compositions having enhanced antitumor activity or reduced side effects. The compositions include both (A) a known active substance having antitumor effect or a pharmaceutically...
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6436961 |
Pharmaceutical agents for the treatment of emesis
The present invention relates to a novel process for preparing and resolving 3-amino-2-phenylpiperidine and for synthesizing from the enantiomers of such compound certain pharmaceutically active...
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6432960 |
Squarate derivatives of dihydropyridine NPY antagonists
A series of antagonists of NPY have been synthesized and are comprised of squarate derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). As antagonists of NPY-induced behavior, these...
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6432980 |
Aliphatic amine substituted piperidyl diaryl pyrrole derivatives as antiprotozoal agents
Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
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6423725 |
4-(2-keto-1-benzimidazolinyl)piperidine compounds as ORL1-receptor agonists
A compound of the formula: or the pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 and R 5 are defined above are useful as ORL1-receptor agonists, and useful as...
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6420385 |
Substituted pyrimidinone and pyridone compounds and methods of use
Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other...
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6413959 |
Method of treating depression with arylglycinamide derivatives
The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R 1 and R 2 together with the N to which they are bound...
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6413987 |
Dermal anesthetic agents
The present invention relates to new aminoindane piperidine compounds, the method of using aminoindane compounds as local anesthetics, said compounds having particularly valuable properties as...
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6407120 |
Neuropeptide Y antagonists
The compound is a neuropeptide Y antagonist and is effective in treating feeding disorders, cardiovascular diseases and other physiological disorders.
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6403581 |
Method of inhibition of farnesyl-protein transferase using substituted benz (cd) indol-2-imine and-amine derivatives
The invention is a method of treating, inhibiting or controlling a ras-associated disease by inhibiting farnesyl-protein transferase(FPTase) enzyme, treating ras oncogene-dependent tumors, which...
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6399606 |
Neuroprotective agents and methods related thereto
Neuroprotective agents are disclosed having the following structure: wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. Such compounds have utility in the treatment of conditions...
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