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6569873 |
Azolidines as beta-3 adrenergic receptor agonists
This invention provides compounds of Formula I having the structure wherein, A, X, Y, Z, W, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as defined hereinbefore or a pharmaceutically acceptable...
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6569877 |
Therapeutic and prophylactic agents for neoplasms
This invention relates to therapeutic and prophylactic agents for neoplasms which comprise a fused heterocyclic compound or a pharmaceutically acceptable salt thereof as an active ingredient; to...
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6562820 |
Method for treatment and prevention of mastitis
The invention is directed to a method of treatment or prevention of mastitis in mammals with known oxazolidinone anti-bacterial agents, either alone or in combination with exogenous lactoferrins.
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6552058 |
Oxazolidinedione derivatives and their use
Novel 2,4-oxazolidinedione compounds of the formula: wherein R is a hydrocarbon residue or a heterocyclic group each of which may be substituted; Y is —CO—, —CH(OH)— or —NR 3 —...
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6552054 |
Chromone derivatives, process for the preparation of the same and uses thereof
The invention provides chromone derivatives of the following general formula, a process for preparing such chromone derivatives and a prophylactic and therapeutic agent comprising such chromone...
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6544991 |
Compositions and methods for treating bacterial infections
A composition having antibacterial activity is disclosed. More particularly, a mixture of an oxazolidinone compound, sulbactam, and ampicillin active agents, demonstrating activity against...
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6534533 |
Fungicidal compositions based on metalaxyl
Metalaxyl having a high content of R-enantiomer of more than 70% by weight, or pure R-metalaxyl, in admixture with 4-[3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl)acryloyl]-morph
oline...
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6518285 |
Piperidinyloxy and pyrrolidinyloxy oxazolidinone antibacterials
Piperidinyloxy, pyrrolidinyloxyl and azetidinyloxy compounds of the formula: wherein R 1 is a piperidinyl, pyrrolidinyl or azetidinyl moiety as described herein and in which the substituents...
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6512004 |
Promoters of neural regeneration
The invention provides methods and compositions for promoting neural cell growth and/or regeneration. The general methods involve contacting with an activator of a cyclic nucleotide dependent...
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6509379 |
Phenylacetic acid derivatives, process and intermediate products for their preparation, and their use as fungicides and pesticides
Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful...
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6503950 |
Triple drug therapy for the treatment of narcotic and alcohol withdrawal symptoms
A triple drug, pharmaceutical kit, composition, and method of treatment containing a combination of effective amounts of at least one anxiolytic agent, at least one centrally acting alpha...
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6500847 |
Inhibition of matrix metalloproteases by substitued biaryl oxobutyric acids
Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the...
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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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6498174 |
Substituted oxazoles and thiazoles derivatives as hPPAR&ggr and hPPARα activators
The present invention discloses compounds of formula (I), and tautomeric forms, pharmaceutically acceptable salts, or solvates thereof. Preferably, the compounds of the invention are dual...
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6497886 |
1,3-bis-(N-lactamyl) propane and the pharmaceutical and cosmetic use thereof
The present invention relates to a 1,3-bis-(N-lactamyl)propane of general formula (I), wherein radicals R 1 , R 2 , R 3 , R 4 , R 5 and R 6 independently stand for hydrogen, alkyl, cycloalkyl,...
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6469036 |
Peptidyl heterocyclic ketones useful as tryptase inhibitors
The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment...
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6465501 |
Azolidines as β3 adrenergic receptor agonists
This invention provides compounds of Formula I having the structure wherein, A, X, Y, Z, W, R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as defined hereinbefore or a pharmaceutically acceptable...
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6465500 |
Indole derivatives as 5-HT1 agonists
Compounds of the formula where W is n is 0, 1, or 2; m is 0, 1, 2, or 3: Y and G are each independently oxygen or sulfur; Z is —O—, —S—, —NH, or —CH 2 ; R 1 is hydrogen, C 1 to C...
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6455559 |
Phenylacetamido-pyrazole derivatives, process for their preparation and their use as antitumor agents
Compounds represented by formula (I) wherein R is a C 3 -C 5 cycloalkyl group, R 1 is a hydrogen atom or a methyl group, or a pharmaceutically acceptable salt thereof; are useful in the...
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6448240 |
Synergistic fungicidal and/or bactericidal composition
The invention concerns a synergetic fungicide and/or bactericide composition comprising famoxadone and a phosphorous acid derivative; and a method for fighting, for cure or prevention, against...
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6448286 |
Imino pyrrolidine 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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6448278 |
Procollagen C-proteinase inhibitors
Compounds of formula (I): and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in...
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6441005 |
Oxazolidinone compounds and compositions, and methods of using the same
Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising...
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6441013 |
Sulphonyloxazolamines as therapeutic active ingredients
The present invention relates to sulphonylexazolamines of general formula (I), wherein R 1 , R 2 represent independently from each other H, A, —(CH 2 ) n —Ar or alkenyl with 2-6 C atoms, R 1 ...
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6423731 |
Indole derivatives as prodrugs of 5-HT1-like receptor agonists
A method for the prophylaxis or treatment of conditions for which 5-HT 1 -like agonists are indicated comprising the administration of therapeutically-effective amount of compounds of formula (I) ...
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6417184 |
Triple drug therapy for the treatment and prevention of acute or chronic pain
A triple drug therapy, pharmaceutical kit, composition, and method of treatment regimen utilized as a combination of effective amounts of an anxiolytic agent, centrally acting alpha antiadrenergic...
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6414003 |
Oxazolone derivatives and their use as anti-helicobacter pylori agents
An anti- Helicobacter pylori agent comprising a compound represented by the formula: wherein A represents an aromatic ring group which may be substituted; R 1 and R 2 , whether identical or...
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6407128 |
Method for increasing the bioavailability of metaxalone
A method of increasing the bioavailability of metaxalone by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of...
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6403612 |
Thrombin receptor antagonists
A thrombin receptor antagonist having the formula or a pharmaceutically acceptable salt thereof, useful for inhibiting the aggregation of blood platelets. The compounds can be used in a method...
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6399640 |
Arylthiazolidinedione and aryloxazolidinedione derivatives
Substituted 5-aryl-2,4-thiazolidinediones or 5-aryl-2,4-oxazolidinediones that also carry a second substituent in the 5-position of the heterocyclic ring are potent agonists of PPAR, and are...
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6391901 |
Thrombin inhibitors
This application relates to novel compounds of formula I (and their pharmaceutically acceptable salts), as defined herein, processes and intermediates for their preparation, pharmaceutical...
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6387896 |
Bicyclic oxazolidinones as antibacterial agents
The present invention provides compounds of formula I useful as antimicrobial agents wherein W, X, Y, R 1 , R 2 and n are as defined in thereof.
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6380235 |
Benzimidazolones and analogues
The present invention provides compounds and pharmaceutical formulations useful as progesterone receptor agonists and antagonists and having the general formula: wherein: A is O, S, or NR 4 ; B...
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6380191 |
Arylthiazolidinedione and aryloxazolidinedione derivatives
Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia,...
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6365607 |
Anticachectic composition
A medicinal composition for the prophylaxis and treatment of cachexia which comprises a compound of the formula: wherein R represents a hydrocarbon group that may be substituted or a...
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6365608 |
Fungicide mixtures based on pyridine carboxamides
Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR 1 R 2 I in which A is an aryl group or an aromatic or non-aromatic, 5- or 6-membered...
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6362191 |
Aminometyl oxooxazolidinyl benzene derivatives
The invention concerns compounds of formula (I), wherein: A is a 5 membered heteroaryl ring, a bicyclic benzo system containing such a 5 membered heteroaryl ring or a bicyclic or tricyclic...
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6358983 |
Heterocyclically substituted α-hydroxycarboxylic acid derivatives, method for producing the same and their use as endothelin receptor antagonists
The present invention relates to carboxylic acid derivatives of the formula I the substituents having the meanings explained in the description, preparation and use as endothelin receptor...
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6358942 |
Phenyloxazolidinones having a c-c bond 4-8 membered heterocyclic rings
A compound of Formula (I): or pharmaceutical acceptable salts thereof wherein X is NR 1 ; R 1 is H, C 1-6 alkyl optionally substituted with one or more OH, CN, or halo, or R 1 is —(CH 2 ) h...
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6355672 |
Benzothiepin derivatives, process for the preparation of the same and uses thereof
The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R 1 is an optionally substituted non-aromatic heterocyclic group; R 2 and R 3 ...
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6353009 |
Method for the treatment and prevention of hyperuricemia
Insulin sensitivity enhancers, such as troglitazone, have the ability to treat and/or prevent hyperuricemia and may thus be used for the therapy or prophylaxis of such diseases as gout, urinary...
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6329409 |
Amine derivatives and skin preparations for external use containing the same
The invention relates to an amine derivative represented by the general formula (1): ##STR1## wherein R 1 is a C 1 -C 30 hydrocarbon group which may be interrupted by an ether linkage, with the...
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6297242 |
N-substituted amidine and guanidine oxazolidinone antibacterials and methods of use thereof
N-substituted amidine and guanidine oxazolidinone compounds of the formula: ##STR1## in which the substituents have the meaning indicated in the description. These compounds are useful as...
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6291496 |
Treating cancers associated with overexpression of class I family of receptor tyrosine kinases
Cancer associated with overexpression of class I family of receptor tyrosine kinases, e.g., with overexpresssion of HER-2/neu or overexpression of epidermal growth factor receptor, are treated with...
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6288096 |
Thiazolidinedione, oxazolidinedione and oxadiazolidinedione derivatives
Novel thiazolidinedione, oxazolidinedione and oxadiazolidinedione derivatives, process for their manufacture, pharmaceutical preparations containing them and the use of the compounds in conditions...
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6262073 |
Pharmaceutical methods of use of 5-substituted and 5,5 disubstituted-3,4-dihydroxy-2(5H)-furanones
The present invention relates to synthetic methods for the production of both optically active and racemic 5,5-disubstituted-3,4-dihydroxy-2(5H)-furanones;...
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6255332 |
Use of oxazolidinone derivatives as anti-penetrating agents in a cosmetic and/or dermatological composition
The use of oxazolidinone derivatives in a composition for topical application, especially a cosmetic or dermatological composition, in particular as anti-penetrating agents. These derivatives make...
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6251869 |
Enhancement of oxazolidinone antibacterial agents activity by using arginine derivatives
The present invention provides methods and compositions for enhancing the effectiveness of oxazolidinone antibacterial agents against gram-negative organisms infection by using an arginine derivative.
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6207690 |
Troglitazone compounds for treating climacteric and cancer
The present invention is directed toward the use of the drug Troglitazone and related thiazolidinedione compounds in the treatment of the climacteric and cancer. This use is based on the novel...
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6200997 |
Heterocyclyl-substituted phenyl compounds, processes and intermediates for their preparation and their use for controlling harmful fungi and animal pests
The present invention relates to heterocyclyl-substituted phenyl compounds of the formula I, ##STR1## where the substituents have the following meanings: Y is halogen, C 1 -C 4 -alkyl, C 1 -C...
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