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6593340 |
Pharmaceutical compositions containing N-propargylphentermine and related analogs to treat neurodegeneration and/or depression
The present invention relates to N-propargylphentermine and its derivatives and the neuroprotective and anti-depressant activity of such compounds as well as therapeutic methods for such compounds.
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6593352 |
Substituted anthranilic acids, their use as a medicament or diagnostic, and medicament comprising them, and a pharmaceutical combination preparation containing a sodium/hydrogen exchange (NHE) blocker
Substituted anthranilic acids of the formula I their use as a medicament or diagnostic, and medicament comprising them, and a pharmaceutical combination preparation containing a sodium/hydrogen...
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6589967 |
Oxime O-ether compounds and fungicides for agricultural and horticultural use
The present invention relates to novel oxime O-ether compounds represented by a general formula [I]; wherein R 1 represents C 1-6 alkyl, C 3-6 cycloalkyl, C 1-6 alkoxy, etc., m represents an...
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6586466 |
Carbohydrazide-protease inhibitors
The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or...
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6583182 |
Compounds with chelation affinity and selectivity for first transition series elements: use in medical therapy and diagnosis
This invention involves synthesis and use of a class of compounds with chelation affinity and selectivity for first transition series elements. Administration of the free or conjugated compound, or...
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6573284 |
Method of treating melanoma
Novel pro-drugs and assay reagents are provided which are useful as therapeutic agents especially for delivery and targetting therapeutically active agents to melanoma cells. The pro-drugs and...
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6555562 |
Phenylalanine derivatives
Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L 1 is a linker atom or group; Ar is an optionally substituted aromatic group;...
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6548522 |
Method for treating conditions related to the glutamate receptor using carboxylic acid amide derivatives
The present invention is concerned with the use of carbonylamino derivatives of the formula wherein R signifies lower alkyl, lower alkenyl, lower alkinyl, cycloalkyl, lower alkoxy or CF 3 ; R 1 ...
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6548519 |
Pyridoxine and pyridoxal analogues: novel uses
The invention provides pyridoxal and pyridoxine analogues, pharmaceutical compositions containing pyridoxine and pyridoxal analogues, and methods of administering pharmaceutical compositions...
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6548523 |
Process for the preparation of arylethanolamine derivatives having an anti-obesity and anti-diabetic properties
The present invention is a process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: that includes preparing a diamide of Formula (II) or a...
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6545029 |
Phenylserine derivatives as integrin antagonists
The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and...
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6541520 |
Treatment of addiction and addiction-related behavior
The present invention provides a highly efficient method for treating substance addiction and for changing addiction-related behavior of a mammal suffering from substance addiction. The method...
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6534546 |
Aniline derivatives possessing an inhibitory effect of nitric oxide synthase
Compounds represented by the general formula (1): (where R 1 is SR 6 or NR 7 R 8 , where R 6 is typically an alkyl group having 1-6 carbon atoms, R 7 is a hydrogen atom, an alkyl group...
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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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6525036 |
Compounds and compositions as protease inhibitors
The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and...
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6525078 |
Compound for the treatment of atherosclerotic-thrombotic pathological conditions
4-Methoxy-N 1 -(4-trans-nitrooxycyclohexyl)-N 3 -(3-pyridinylmethyl)-1,3-benzenedicarboxamide and acid addition salts thereof with pharmaceutically acceptable organic and inorganic acids, and a...
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6525099 |
N-substituted sulfonamide derivatives
The present invention provides certain N-substituted sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of...
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6521626 |
Thiocarboxamide derivatives
Compounds of formula (1): wherein R 1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or...
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6518272 |
Cycloalkyl-substituted aryl-piperazines, piperidines and tetrahydropyridines as serotonergic agents
This invention relates to compounds which have activity as 5-HT 1A agonists and antagonists which may be useful for the treatment of anxiety, depression, cognitive deficits, and prostate cancer,...
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6518267 |
Protease inhibitors
The present invention provides bis-aminomethyl carbonyl protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K,...
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6503928 |
Arylpiperidine and aryl-1,2,5,6-tetrahydropyridine amide derivatives
Compounds of the formula wherein R 1 , R 2 , R 3 , R 4 , X and n are defined in the specification, are useful for the treatment of anxiety, depression and related CNS disorders, and other...
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6500865 |
Sulfonamide derivatives
The present invention provides certain sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such...
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6500849 |
1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino 1,3-propanediols and related compounds
Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and...
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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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6498172 |
Prostaglandin agonists and their use to treat bone disorders
This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such...
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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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6495577 |
Pesticidal composition
Pesticidal compositions comprising deltamethrin and acetamiprid.
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6489364 |
Antiviral protease inhibitors
Compounds of formula (I), wherein A′ and A″ are independently the same or different group of formula (II) wherein: R′ is H, CH 3 , C(CH 3 ) 2 , —OR a , —N(R a ) 2 , —N(R a )OR a or...
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6489349 |
Pharmaceutical compositions for inhibition of cytokine production and secretion
Pharmaceutical compositions incorporate compounds that affect cytokine production and/or secretion. Such compounds include aryl substituted olefinic amine compounds, pyridyloxylalkylamines and...
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6486193 |
3-substituted pyrrolidines useful as inhibitors of matrix metalloproteinases
The present invention provides novel 3-substituted pyrrolidines of the formula useful in as inhibitors of matrix metallo-proteinases (MMPs). Pharmaceutical compositions containing said compounds...
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6482859 |
Microbicidal N-sulfonylglycin alkynyloxyphenethyl amide derivatives
The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R 1 is...
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6479493 |
Methods for treatment of type I diabetes
Substituted condensation products of -benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of type I diabetes.
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6479550 |
α-sulfenimino acid derivatives
α-Sulfenimino acid derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally...
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6476027 |
N-hydroxy 4-sulfonyl butanamide compounds
An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy...
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6476056 |
Heterocycle substituted aryloxyaniline derivatives and their use as MDR ligands
An aryloxyaniline derivative represented by the formula: wherein Ar 1 and Ar 2 are the same or different, and are each a substituted or unsubstituted phenyl group, a substituted or...
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6472413 |
Heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives, their preparation, their use and pharmaceutical preparations comprising them
One embodiment of the present invention relates to heteroarylacryloylaminoalkyl-substituted benzenesulfonamide derivatives of the formula (I), in which R(1), R(2), R(3), R(4), Het, X, Y and Z...
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6465471 |
Cinnamic acid derivatives
Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk 1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative...
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6465493 |
Triarylimidazoles
Compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R 1 , R 2 and R 3 are various substituent groups; and one of X 1 and X 2 is N or CR′, and the other is NR′...
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6455539 |
Squaric acid derivates
Squaric acid derivatives of formula (1) are described: wherein R 1 is a group Ar 1 Ar 2 Alk- in which Ar 1 is an optionally substituted aromatic or heteroaromatic group; Ar 2 is an optionally...
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6455554 |
Oxopyridinyl pharmaceutical compositions and methods for use
Pharmaceutical compositions incorporate aryl substituted olefinic amine compounds. Representative compounds are (2S)-(4E)-N-methyl-5-[3-(5-isopropoxy-1-oxopyridin)yl)]-4-pe
nten-2-amine,...
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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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6448254 |
Substituted amides, their production and their use
Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, as well as possible physiologically tolerable salts, in which the...
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6448276 |
Method for treating vaginal dryness with nicotinic acetylcholine receptor agonists
The invention provides a method for treating vaginal dryness by increasing hydration and lubrication of vaginal and cervical tissues in a subject in need of such treatment. The method comprises...
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6436969 |
Dialysis solutions and methods
The present invention provides improved dialysis compositions and methods for dialysis comprising utilizing the disclosed AGE inhibitors, together with methods to reduce dialysis-related...
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6436925 |
Substituted benzamides, their production and their use as cysteine protease inhibitors
Benzamides 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...
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6432990 |
2-methoxyimino-2-(pyridinyloxymethyl) phenyl acetamides with polyether derivatives on the pyridine ring
The present invention provides novel 2-methoxyimino-2-(pyridinyloxymethyl)phenyl acetamide compounds with polyether substituents on the pyridine ring, their use as fungicidal compounds, and their...
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6426348 |
Diphenyl heterocyclic thioamide derivatives
It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4...
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6423728 |
Heterocyclic thioamide derivatives
It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4...
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6420397 |
Heteroaryl protease inhibitors and diagnostic imaging agents
Ketothiazole alkoxyguanidine and aminoguanidine analogs are described, including compounds of the Formula I: wherein X is O or NR 9 and Het, A, R 1 , R 7 , R 8 , R 12 , R 13 , R a , R b , R c ,...
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6420398 |
Urea derivatives having nitrogen aromatic heterocycle
An object of the present invention is to provide novel urea derivatives which have TNF-α production inhibitory effects and are useful as therapeutic agents for various diseases, particularly as...
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