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7465734 |
Methods and compositions for overcoming resistance to biologic and chemotherapy
This invention provides a method for identifying potential therapeutic agents by contacting a target cell with a candidate therapeutic agent which is a selective substrate for an endogenous,...
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7410956 |
Caspase inhibitor prodrugs
The present invention relates to compounds of formula I which are prodrugs of caspase inhibitors and pharmaceutically acceptable salts thereof. This invention further relates to the release of...
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7402557 |
Combined treatment with keratinocyte growth factor and epidermal growth factor inhibitor
The present invention relates to compositions and methods for treating the epithelial toxicity caused by administering to a human cancer patient an epidermal growth factor receptor (EGFR)...
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7259155 |
Phosphonic diester derivatives
The present invention provides a phosphonic acid diester compound represented by General Formula
wherein R 1 , R 2 , R 3 and R 4 are the same or different, and represent hydrogen, halogen,...
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7253169 |
Aza compounds, pharmaceutical compositions and methods of use
The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
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7214701 |
Active substance combinations having insecticidal and acaricdal properties
The invention relates to insecticidal mixtures for protecting plants against attack by pests comprising
(a) compounds of the formula (I)
in which W, X, Y, Z, A, B, D and G...
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7115591 |
Prostaglandin endoperoxide H synthase biosynthesis inhibitors
The present invention describes pyridazinone compounds of formula I
which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2), COX-2 is...
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RE39264 |
Pharmaceutical combination
The invention relates to pharmaceutical compositions for topical administration comprising a topically acceptable antiviral substance and an antiinflammatory glucocorticoid in a pharmaceutically...
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7067501 |
Aryloxyphenyl and arylsulfanylphenyl derivatives
The invention provides compounds of the formula
wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.
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7053055 |
Compounds of unstable DP IV-inhibitors
Novel compounds of unstable inhibitors of the serine peptidase dipeptidyl peptidase IV, are used in the treatment of various disorders, especially of metabolic disorders. The compounds can be used...
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7001895 |
Prostaglandin endoperoxide H synthase biosynthesis inhibitors
The present invention describes pyridazinone compounds of formula I
which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is...
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6998391 |
Method for treating diseases associated with abnormal kinase activity
Methods are provided for treating diseases associated with abnormal activity of kinases. The method comprises: administering a DNA methylation inhibitor to the patient in therapeutically effective...
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6930097 |
Matrix metalloproteinase and tumor necrosis factor inhibitors
A compound of formula 1-[3,4-dihydroxy-5-(2-hydroxyethyl)tetrahydrofuran-2-yl]pryi
midine-2,4(1H,3H)-dione has inhibitory effects of matrix metalloproteinase-2 (gelatinase A) enzyme and binding of...
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6919323 |
Pyridazinone inhibitors of fatty acid binding protein and method
aP2 inhibiting compounds are provided having the formula
wherein A, X, R and Z are as described herein.
A method is also provided for treating diabetes and related diseases, especially Type...
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6919322 |
Phenyl Phosphonate Fructose-1,6-Bisphosphatase Inhibitors
Novel FBPase inhibitors of the formula I
are useful in the treatment of diabetes and other conditions associated with elevated blood glucose.
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6916797 |
α-arylethylpiperazine derivatives as neurokinin antagonists
The invention relates to new α-arylethylpiperazine of the formula
wherein
Z represents 0 or S; n′ represents 1 or 2; R 2 represents a hydrogen atom or a methyl group; W, Ar 1 and...
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6914052 |
Selective anti-viral nucleoside chain terminators
The present invention relates to dideoxynucleoside analog compounds containing a dideoxy ribofuranosyl moiety that exhibit selective anti-viral activity coupled with substantially low toxicity...
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6833364 |
Substituted pyrazole derivatives
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R 1 , R 2 , R 3 , A, X and Y are each as defined, and to processes...
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6756391 |
Antiviral compounds
The present invention is drawn to novel antiviral compounds, pharmaceutical compositions and their use. More specifically this invention is drawn to derivatives of monocyclic polyamines which have...
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6743798 |
Substituted pyrazole derivatives condensed with six-membered heterocyclic rings
The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which R 1 , R 2 , R 3 and A are each as defined, and to processes for their preparation and...
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6706698 |
α-Substituted β-aminoethyl phosphonate derivatives
The present invention relates to novel α-substituted-β-aminoethylphosphonate and α-substituted-β-aminovinylphosphonate derivatives and their uses for lowering plasma levels of apo (a), Lp(a),...
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6699855 |
Inhibitors of hepatitis C virus NS3 protease
The present invention relates to compounds of Formula (I): wherein A 1 is methylene, ethylene or propylene group and A 2 is N or CR 5 , or stereoisomeric forms, stereoisomeric mixtures, or...
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6649605 |
Treatment of tension-type headaches with NMDA receptor antagonists
NMDA receptor antagonists, especially mirtazapine, can be used to treat tension-type headaches.
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6608067 |
Inhibitors of serine proteases, particularly HCV NS3 protease
The present invention relates to compounds, methods and pharmaceutical compositions for inhibiting proteases, particularly serine proteases, and more particularly HCV NS3 proteases. The compounds,...
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6605602 |
Method of treating BK virus nephropathy
Provided are oligonucleotides for the quantitation of BK virus (BKV) viral loads in a sample and methods for the diagnosis and management of BKV-associated nephropathy using PCR or QPCR methods. In...
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6562783 |
Phosphinylmethyl and phosphorylmethyl succinic and glutauric acid analogs as β-secretase inhibitors
The invention provides a compound of formula (I): or salts or hydrates thereof, useful as beta-secretase inhibitors. The invention further relates to a method of reducing plaque formation,...
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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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6455530 |
2R,4S,S,S- and 2S,4R,S,S-hydroxyitraconazole
A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (S,S)-isomer, and to phosphate and sulfate derivatives...
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6362172 |
Water soluble prodrugs of azole compounds
Water-soluble prodrugs of triazole antifungal compounds having a secondary or tertiary hydroxy group are provided. More particularly, new water-soluble triazole antifungal compounds are provided...
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6310051 |
Use of chelating agents in the treatment of atherosclerotic conditions
The invention provides the use of dipyridoxyl or aminopolycarboxylic acid based chelating agents, metal chelates and salts thereof, in the manufacture of a therapeutic agent for use in the...
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6300356 |
Method for decreasing QT dispersion or inhibiting the progression of QT dispersion with an angiotensin II receptor antagonist
Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in...
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6248729 |
Combination of an ADP-receptor blocking antiplatelet drug and antihypertensive drug and a method for preventing a cerebral infarction employing such combination
A method is provided for preventing a cerebral infarction by administering to a patient a combination of an ADP-receptor blocking antiplatelet drug, such as clopidogrel, in combination with an...
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6201002 |
Method for reducing mortality with an angiotensin II antagonist
Angiotensin II receptor antagonists are useful in reducing and preventing mortality and sudden cardiac death in symptomatic heart failure patients. Losartan potassium has been shown to reduce...
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6200961 |
Concentrates of organophosphorous insecticides
A low volatile organic compound co-solvent system is disclosed for preparing emulsion concentrates of low melting organophosphorous insecticides wherein the bioefficacy of the insecticide active is...
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6143733 |
Quinoxalinedione derivatives, their production and use in pharmaceutical agents
Quinoxalinedione derivatives ##STR1## as well as their production and use in pharmaceutical agents are described.
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6121251 |
Dihydropyridazinones and pyridazinones and their use as fungicides and insecticides
Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is ##STR2## n is 0 or 1; Y is O, S, NR 1 , or R 6 ; the ring bond containing R 4 and R 5 is a single...
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6043245 |
Tetrahydrofuran antifungal phosphate
A compound of the formula I ##STR1## wherein G is H or PO 3 H 2 or a pharmaceutical acceptable salt thereof, pharmaceutical compositions containing such compounds and method of using such...
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6015800 |
Substituted quinoxaline-2-ones as glutamate receptor antagonists
A novel series of substituted quinoxaline 2-ones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds...
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5985858 |
Phosphonic diester derivatives
A phosphonic diester derivative represented by the following formula (1): ##STR1## wherein R 1 represents a cycloalkyl group; a phenyl group which may have 1 to 3 substituents selected from the...
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5985856 |
Water soluble prodrugs of secondary and tertiary amine containing drugs and methods of making thereof
The present invention is drawn to water soluble derivatives aliphatic acid aromatic secondary and tertiary amine containing drugs. The present invention is further drawn to methods of making water...
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5914351 |
Anti-viral aromatic hydrazones
Compounds of the formula ##STR1## wherein Q is a hydrazone derivative; R 1 is hydrogen, halogen, alkyl or alkoxy; R 2 is hydrogen, halogen, alkyl, alkoxy, alkenoxy, alkynyloxy, halomethyl,...
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5880111 |
Therapeutic derivations of diphosphonates
Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by...
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5856323 |
Compounds and methods for the treatment of disorders mediated by platelet activating factor or products of 5-lipoxygenase
2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl...
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5854227 |
Therapeutic derivatives of diphosphonates
Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, infectious urinary tract stones, and bone cancer, are...
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5846971 |
Oral antifungal composition
A pharmaceutical composition comprising: i) substantially inert beads; wherein said beads are coated with ii) an antifungal agent which is (-)-(2R-cis)-4- 4- 4- 4- ...
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5837702 |
4-arylamino-benzopyran and related compounds
Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH 2 --, --C(O)--, --O--, --S-- or --N(R 8 )-- where R 8 is hydrogen,...
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5824679 |
Phosphanoxides--preparation and use
The invention concerns novel phosphanoxides of formula 1 in which R 1 means aryl or heteroaryl group. The invention further concern the optically active forms, racemates and diastereomers mixtures...
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5767119 |
Method of treating neurodegenerative diseases using an AMPA excitatory amino and an uricosuric agent
The present invention is a pharmaceutical composition having a combination of an uricosuric agent such as probenecid or the like and an excitatory amino acid antagonist useful for treating a...
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5741784 |
Benzopyran derivatives and their use
This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more...
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5714490 |
Tetrahydrofuran antifungals
A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R 1 is a straight or branched chain (C...
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