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7589126 |
5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation
The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula:
wherein R 1 is a hydrogen atom or an optionally substituted lower alkyl...
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7563822 |
Agents for the prevention or treatment of renal diseases
The present invention relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2-
hydroxybenzenesulfonamide derivative represented...
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7547716 |
Sulfonamide derivatives
A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a...
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7544637 |
2-cyano-3(halo)alkoxy-benzenesulfonamide compounds for combating animal pests
The invention relates to 2-cyano-3-(halo)alkoxy-benzenesulfonamide compounds I
where the variables Alk and R 1 to R 5 are as defined in claim 1 , and/or to their agriculturally useful...
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7511175 |
Inhibitors of the 11-beta-hydroxysteroid dehydrogenase type 1 enzyme
The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of...
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7511076 |
Nitrosation-inducible inhibitors biological macromolecules
Biomacromolecules such as proteins are inactivated by hydrophobic ANSA derivatives of the formula:
wherein R 1 and R 2 are hydrophobic or affinity groups and R 3 is selected from the group...
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7459585 |
Benzene derivatives and pharmaceutical use thereof
The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory...
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7417059 |
Substituted aromatic-ring compounds, process for producing the same and use
The present invention is directed to a class of cyclohexene derivatives bearing sulfamoyl and ester groups which have an inhibitory activity on nitric oxide (NO) production and cytokine production,...
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7393873 |
Arylsulfonamide derivatives
N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin...
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7375120 |
Peptide deformylase inhibitors
Novel PDF inhibitors and novel methods for their use are provided.
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7345095 |
Sulfonamide compounds for the treatment of neurodegenerative disorders
The present invention relates to compounds of the Formula I
wherein R 1 , R 2 , R 3 , m, and n are as defined. Compounds of the Formula I have activity inhibiting production of Aβ-peptide. The...
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7314638 |
Preparing method for controlled released type tablet tamsulosin HCL and the tablet thereof
The present invention relates to a simple and effective method for preparing a tamsulosin HCl sustained-release tablet and a tamsulosin HCl sustained-release tablet produced thereby. The method...
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7265130 |
NPY Y5 antagonist
The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I):
wherein R 1 is lower alkyl, cycloalkyl or the...
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7262223 |
Amidine derivatives for treating amyloidosis
The present invention relates to the use of amidine compounds in the treatment of amyloid-related diseases. In particular, the invention relates to a method of treating or preventing an...
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7256204 |
Amine compounds, their production and use
A compound of the formula:
wherein Ar is an aromatic ring assembly group which may be substituted or a fused aromatic group which may be substituted; X is (i) a bond, (ii) —S—, —SO— or...
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7250447 |
Acylsulfamide inhibitors of factor VIIa
Compounds having the general formula I are useful for inhibiting serine protease enzymes, such as Tissue Factor VIIa, factor Xa, thrombin and kallikrein and have improved permeability properties....
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7244755 |
Hydroxypropylamines
Disclosed are compounds of formula I:
and the pharmaceutically acceptable salts thereof wherein the variables R N , R 1 , R 2 , R 3 , R P and R C are defined herein. These compounds are...
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7214711 |
Method of treating migraine headache without aura
The present invention relates to methods and compositions for treating selected conditions of the central and peripheral nervous systems employing non-synaptic mechanisms. More specifically, one...
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7211599 |
Use of etodolac to treat hyperplasia
The present invention provides a therapeutic method to treat non-malignant diseases characterized by the excessive tissue growth, e.g., hyperplastic diseases, comprising administering to a mammal...
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7208528 |
Polyamine analogues as therapeutic and diagnostic agents
Novel inhibitors of polyamine transport having inhibition constants two orders of magnitude lower than those of known compounds are disclosed. These polyamine analogues are useful pharmaceutical...
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7208526 |
Styrylsulfonamides
The present invention relates to the compounds of formula I:
their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above...
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7135487 |
Sulphonamide derivatives
The present invention relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.
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7122571 |
Substituted hydrazones as inhibitors of cyclooxygenase-2
Compounds useful as inhibitors of cyclooxygenase-2 activity have the formulae I or Ia:
wherein: Q 1 , Q 2 , n, m, X, Y and R are as defined herein.
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7115632 |
Sulfonyl aryl or heteroaryl hydroxamic acid compounds
A sulfonyl aromatic or heteroaromatic ring 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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7109243 |
Inhibitors of cathepsin S
The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at...
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7074832 |
Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use
Topical compositions which include urea and an antimicrobial agent, particularly sulfacetamide or metronidazole, are described. Sulfacetamide compositions further including sulfur are also...
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7067556 |
Compositions containing antimicrobials and urea for the treatment of dermatological disorders and methods for their use
Topical compositions which include urea and an antimicrobial agent, particularly sulfacetamide, are described. Sulfacetamide compositions further including sulfur are also described. Methods for...
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7060729 |
Composition and method for treating skin
The present invention relates to a composition and method for treating individuals afflicted with rosacea by combining a dicarboxylic acid, at least an antimicrobial agent, and a pharmaceutically...
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7008962 |
IL-8 receptor antagonists
This invention relates to the novel use of dianilino squarates in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
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6998419 |
3,4,5-trisubstituted aryl nitrone compounds and pharmaceutical compositions containing the same
Disclosed are 3,4,5-trisubstituted aryl nitrone compoundsd and pharmaceutical compositions containing such compounds. The 3,4,5-trisubstituted aryl nitrone compounds have formula (I); where R 1...
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6958331 |
Bradykinin receptor antagonists
The invention relates to sulfonyl amine derivatives of formula IA
wherein R 5A , X 1 , X 2 , R 9 and R 10 are as defined herein, which derivatives are useful as bradykinin B 1 receptor...
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6949567 |
Compounds for the treatment of protozoal diseases
The invention relates to new diphenylurea having the formula (I)
or a salt thereof, where
Y is C═O, C═S, C═NH, (C═O) 2 or SO 2 ; and to processes for the preparation of these...
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6943170 |
N-cycloalkylglycines as HIV protease inhibitors
This invention relates generally to N-cycloalkylglycines of the Formula (I):
or a stereoisomeric form, a mixture of stereoisomeric forms, or a pharmaceutically acceptable salt thereof, which...
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6919369 |
Serine protease inhibitors
Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of...
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6908947 |
Sulfonamide-substituted fused 7-membered ring compounds, their use as a medicament, and pharmaceutical preparations comprising them
The present invention relates to compounds of formula I,
in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and...
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6906092 |
Method of inhibiting matrix metalloproteinases
The present invention relates to a method of inhibiting matrix metalloproteinases using compounds that are dibenzofuran sulfonamide derivatives having the Formula I
More particularly, the...
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6897209 |
Labelled factor XIIIa substrates
A complex of a radiometal or paramagnetic metal ion with a metal chelating agent such as a diaminedioxime has attached thereto a substituent of formula (Y) m -A-NHR) k can function as a substrate...
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6890942 |
Acyl sulfonamides as inhibitors of HIV integrase
The present invention relates a series of compounds of Formula I
wherein R 1 , R 2 , R 3 , and B are as defined in the specification. The compounds are useful for the inhibition of HIV...
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6872716 |
Antipsychotic sulfonamide-heterocycles, and methods of use thereof
One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds...
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6852484 |
Methods for the identification of inhibitors of asparagine synthase as antibiotics
The present inventors have discovered that Asparagine Synthase is essential for fungal pathogenicity. Specifically, the inhibition of Asparagine Synthase gene expression in fungi results in no...
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6849648 |
Phenylene alkyne matrix metalloproteinase inhibitors
A compound of Formula I
or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G 1 , G 2 , and B are as defined in the application, are selective inhibitors of...
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6825231 |
Substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics, and a medicament comprising them
The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them Substituted...
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6822001 |
Combination therapy using pentafluorobenzenesulfonamides and antineoplastic agents
Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.
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6812252 |
Acylsulfonamide derivatives
The present invention provides new acylsulfonamide derivatives such as 4-(3-trifluoromethyl)phenylethynyl-N-(2-(5-ketohexanoylamino
)sulfonylphenyl)benzamide,...
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6809119 |
Branched chain amino acid-dependent aminotransferase inhibitors and their use in the treatment of neurodegenerative diseases
The invention relates to BCAT inhibitors and the use thereof for treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating...
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6794414 |
Method and compositions for treating diseases mediated by transglutaminase activity
Diseases Mediated by transglutaminase, such as Huntington's Disease, spinobulbar atrophy, spinocerebellar ataxia, and dentatorubralpallidoluysian atrophy, as well as inflammatory diseases of the...
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6750217 |
Benzenesulfonamide derivatives and their use as MEK inhibitors
Benzenesulfonamides of formula (I), in which W is OR 1 , NR 2 OR 1 , NR A R B , NR 2 NR A R B , or NR 2 (CH 2 ) 2-4 NR A R B and the other variables as defined in the claims, are inhibitors of MEK...
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6747027 |
Thiol sulfonamide metalloprotease inhibitors
This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfonamide inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors,...
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6734182 |
Aryl sulfonamides and sulfamide derivatives and uses thereof
This invention is directed to novel aryl sulfonamide and sulfamide compounds which bind selectively to and inhibit the activity of the human Y5 receptor. This invention is also related to uses of...
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6733963 |
Methods for the identification of inhibitors of 3-isopropylmalate dehydratase as antibiotics
The present inventors have discovered that 3-Isopropylmalate dehydratase is essential for fungal pathogenicity. Specifically, the inhibition of 3-Isopropylmalate dehydratase gene expression in...
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