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7563928 |
Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone...
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7485752 |
Diacylglycerol acyltransferase inhibitors
Provided herein are compounds of the formula (I):
as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds,...
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7482379 |
Propenoyl hydrazides
The present disclosure provides compositions for inhibiting proteases, methods for synthesizing the compositions, and methods of using the disclosed protease inhibitors. Aspects of the disclosure...
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7449315 |
Bifunctional energy-reversible acyl-compositions
Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed. In preferred aspects, examples of such compositions include:
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7432286 |
Pharmaceutically active sulfonyl hydrazide derivatives
The present invention is related to sulfonyl hydrazide derivatives for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonyl hydrazide...
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7419972 |
2-substituted estra-1,3,5(10)-trien-17-ones as inhibitors of 17β-hydroxy steroid dehydrogenase type 1
The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I
as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for...
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7414037 |
Hydrazide-containing CFTR inhibitor compounds and uses thereof
The invention provides compositions, pharmaceutical preparations and methods for inhibition of cystic fibrosis transmembrane conductance regulator protein (CFTR) that are useful for the study and...
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7368473 |
Paclitaxel enhancer compounds
One embodiment of the present invention is a compound represented by the Structural Formula (I):
Y is a covalent bond of a substituted or unsubstituted straight chained hydrocarbyl group. In...
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7236236 |
Methods for detecting malaria parasites and reagent kits therefor
Methods for detecting a malaria parasite are described that include: releasing the malaria parasite by allowing an erythrocyte in a specimen to undergo hemolysis; staining the released malaria...
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7173063 |
Topoisomerase poisons for the treatment of proliferative disorders
Methods for the treatment of a proliferative disorder are provided in which a subject in need of such treatment is administered an effective amount of a compound selected from: compounds of formula...
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7056945 |
Selective inhibition of neuronal nitric oxide synthase
Compositions, prodrugs and methods for inhibiting neural Nitric Oxide Synthase (nNOS). By inhibiting nNOS, the compounds, prodrugs and methods of the presnet invention are useable to treat or...
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7045315 |
Methods for modulating expression of exogenous genes in mammalian systems
In accordance with the present invention, there are provided various methods for modulating the expression of an exogenous gene in an isolated cell and in a mammalian subject employing modified...
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7001924 |
Inhibitors of RNase P proteins as antibacterial compounds
The present invention features compounds useful for inhibiting RNase P activity. These compounds can be used as therapeutics for treating or preventing a variety of bacterial infections. The...
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6893659 |
Pharmaceutical composition for oral administration of a N-piperidino-3- pyrazolecarboxamide derivative, its salts and their solvates
The pharmaceutical compositions for oral administration according to the invention contain 0.5% to 20% of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-met
hylpyrazole-3-carboxamide in...
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6887863 |
Hydrazide and alkoxyamide angiogenesis inhibitors
Compounds having the formula
are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods...
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6774116 |
Prodrugs via acylation with cinnamate
A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have...
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6703424 |
Dispersible compositions containing L-DOPA ethyl ester
The present invention relates to a dispersible pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester, a therapeutically effective amount of a decarboxylase...
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6673777 |
Guanylhydrazones useful for treating diseases associated with T cell activation
There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection, using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target...
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6610715 |
Cathecol hydrazone derivatives, process for preparing the same and pharmaceutical composition containing the same
The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R 1 is C 1-7 alkyl or C 3-7 cycloalkyl; R 2 is hydrogen,...
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6521663 |
Aminoguanidinyl- and Alkoxyguanidinyl-substituted phenyl acetamides as protease inhibitors
Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R 3 -R 6 , R 11 , B, Y and W are set forth...
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6433017 |
Amphiphilic polyamine compounds
In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and...
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6410574 |
Fungicidal composition and method for using the same
The present invention relates to a fungicidal composition obtained by mixing a 1,2,3-thiadiazole derivative of general formula (I) useful as a plant disease controller with at least one fungicide...
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6399659 |
Hydrazine oxoacetamide derivative and insecticide
The present invention relates to a hydrazine oxoacetamide derivative or its salt which exhibits an excellent insecticidal effect even at a low concentration. The hydrazine oxoacetamide derivative...
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6348499 |
Amphiphilic polyamide compounds
Amphiphilic polyamide compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.
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6346547 |
N-substituted amino acids, antioxidant pharmaceutical compositions containing n-substituted amino acids and methods for preventing cardiovascular diseases and/or preventing and/or treating antioxidant responsive diseases therewith
Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general...
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6297275 |
Method for controlling fungi using phenylhydrazine derivatives
A method for controlling fungi using a phenylhydrazine derivative compound of the formula: ##STR1## wherein: X is phenyl, phenylalkoxy, phenoxy, or benzyl, alone or in combination with one or...
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6291464 |
Aminopiperazine derivatives
This invention relates to new aminopiperazine derivatives having the potentiation of the cholinergic activity, etc., and represented by general formula [I]. ##STR1## wherein R 1 is lower alkyl,...
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6248787 |
Guanylhydrazones and their use to treat inflammatory conditions
This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with...
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6172108 |
Hydrazide compounds
Compounds of formula (I): R--NH--A--CO--NH--NH--(W) n --Z (I) wherein: n is 0 or 1, W represents --CO-- or S(O) r wherein r is 0, 1 or 2, Z represents a group selected from aryl,...
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6140368 |
Naphthols useful in antiviral methods
The present invention relates to a novel class of compounds that are potent inhibitors of HIV reverse transcriptase and HIV integrase. In addition to being multienzyme inhibitors, the inventive...
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6117910 |
Bicyclic fibrinogen antagonists
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6075044 |
Heterocyclic derivatives as inhibitors of purine salvage phosphoribosyltransferases
The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.
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6031003 |
Calcium receptor-active molecules
The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more...
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6028110 |
Succinyl hydroxamic acid, N-formyl-N-hydroxy amino carboxylic acid and succinic acid amide derivatives as metalloprotease inhibitors
A pharmaceutical or veterinary composition comprising a compound of formula I ##STR1## wherein X is a --CO 2 H group and R 1 , R 2 , R 3 , R 4 , R 5 are as defined in the specification, or a...
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5990171 |
Hydrazonoacetic acid amides and the use thereof as pesticides
The invention concerns hydrazonoacetic acid amides of general formula (I), a process for producing them, and the use of the said amides as pesticides. In the formula shown, the following meanings...
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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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5877217 |
N-acylaminoalkyl-hydrazinecarboximidamides
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) using compounds of the following formula I ##STR1## wherein alk is a straight or...
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5866610 |
Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical as inhibitors of the cellular NA+/H+ exchange or as a diagnostic, and pharmaceutical containing them
Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them. Described are benzoylguanidines of the formula I...
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5840756 |
Pharmaceutical composition of L-DOPA ester
The present invention provides a pharmaceutical composition contains a thpeutically effective amount of L-DOPA ethyl ester and a carrier which comprises from 5.5 to 98.5% hydroxypropylmethyl...
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5753652 |
Antiretroviral hydrazine derivatives
The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.
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5656669 |
Restorative neuropharmacological agent for motor and speech disturbance
A restorative neuropharmacological method of treating motor or speech disturbance comprising administration of L- or DL-threo-DOPS or its pharmaceutically acceptable acid-addition-salt to a patient...
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5589510 |
Method for inhibiting retroviral infection by administering a naphthalenesulfonic acid compound
A method for inhibiting retroviral infection in a subject comprising administering to said subject a therapeutically effective amount of a naphthalenesulfonic acid compound or a pharmaceutically...
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5576353 |
Method of treating memory disorders using R-enantiomers of N-propargyl-aminoindan compounds
R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's...
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5567723 |
Miticidal hydrazine compounds and their intermediates
Compounds having the structural formula ##STR1## wherein R is C 1 -C 6 alkoxy or C 1 -C 6 alkyl; R 1 is fluorenyl, thienyl, pyridyl or thiazolyl, unsubstituted or substituted by one or more...
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5540931 |
Methods for inducing site-specific immunosuppression and compositions of site specific immunosuppressants
The present invention provides methods and formulations for site-specific immune suppression of immune/inflammatory responses with localized or topical application of immunosuppressants including...
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5478821 |
Method of accelerating the proliferation of emdothelial cells with inhibition of no synthases
A method of accelerating the proliferation of endothelial cells with inhibition of NO synthases in warm-blooded animals comprising administering to warm-blooded animals an amount of at least one...
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5457133 |
R-enantiomers of N-propargyl-aminoindan compounds, their preparation and pharmaceutical compositions containing them
R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's...
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5424055 |
Ultraviolet screening composited oxide and process for producing the same
The composite oxide comprises, by weight, 100 parts of zinc oxide and at least one member, incorporated therein, selected from seven specific oxides in their specific amounts such as 0.001 to 5.0...
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5399589 |
Oxalyl hydrazide-hydroxamic acid derivatives, their preparation and their use as fungicides
Oxalyl hydrazide-hydroxamic acid derivatives of the formula I ##STR1## where the substituents have the following meanings: R, R 1 , R 2 and R 3 independently of one another are hydrogen,...
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5288727 |
Hydrazone compounds, processes for their production, intermediates useful for their production and pesticidal compositions containing them
The present invention relates to a hydrazone compound of the formula (I) or its salt, a process for its preparation, an intermediate of the formula (II-5), a pesticidal composition containing said...
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