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6395768 |
Uses for indole-3-propionic acids and salts and esters thereof
The cytotoxic effects of amyloid beta protein on cells are prevented by contacting the cells with an effective amount of an indole-3-propionic acid or a salt or ester thereof. Furthermore, a...
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6395764 |
2-imidazolinylaminoindole compounds useful as alpha-2 adrenoceptor agnonists
This invention involves compounds having the following structure: wherein: a) R 1 is hydrogen; or alkyl; bond (a) is a single or a double bond; b) R 2 and R 3 are each independently selected...
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6376531 |
Method of treatment using deuterium compounds
The present invention provides organic deuterium compounds which can be therapeutic compounds to treat manic depression. In particular, the present invention relates to deuterated methionine,...
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6369109 |
Betulinic acid and derivatives thereof useful for the treatment of neuroectodermal tumor
The present invention is, generally, directed to the use of betulinic acid and derivatives thereof for the treatment of neuroectodermal tumors. The present invention is based on the discovery that...
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6348486 |
Methods for modulating bladder function
This invention provides methods and pharmaceutical compositions for maintaining bladder control or treating urinary incontinence in a mammal utilizing agonists of KCNQ potassium channels, including...
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6337344 |
Indole derivatives as inhibitors or factor Xa
The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R 1a , R 1b , R 1c R 1d , R 2 , R 3 , R 4 and A...
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6319918 |
Substituted indolinones with kinase inhibitory activity
Substituted indolinones of general formula ##STR1## having effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells. Exemplary compounds are: ...
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6306873 |
Substituted β-thiocarboxylic acids
This invention relates to compounds of general formula (I): ##STR1## in which Ar is a group selected from: ##STR2## A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and...
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6302837 |
Benzothiophene, benzofuran and indole compounds
A compound selected from those of formula (I): ##STR1## wherein: X represents oxygen, sulphur, or NR 3 wherein R 3 is as defined in the description, Y represents oxygen, sulphur, NR 3 , or...
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6300364 |
Medicinal compositions with cholesterol-lowering effect
Pharmaceutical compositions having a cholesterol-lowering effect which comprises as the active ingredient a compound having a PPAR (peroxisome proliferator-activated receptor)δ activating effect...
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6300365 |
Use of dopamine D2/D3 receptor agonists to treat fibromyalgia
The present invention is directed to methods for the treatment of human patients afflicted with fibromyalgia using a non-ergot dopamine receptor D2/D3 agonist. In particular, patients are treated...
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6268391 |
Benzylidene-1,3-dihydro-indol-2-one derivatives a receptor tyrosine kinase inhibitors, particularly of Raf kinases
Compounds of general formula (I) wherein: R 1 is H or optionally joined with R 2 to form a fused ring selected from the group consisting of five to ten membered aryl, heteroaryl or heterocyclyl...
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6245761 |
Indolyl neuropeptide Y receptor antagonists
This invention provides a series of substituted indoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides the novel...
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6235769 |
Methods of preventing and treating neurological disorders with compounds that modulate the function of the C-RET receptor protein tyrosine kinase
The invention relates in part to a method of preventing or treating an abnormal condition caused by an aberration in the function of the C-RET receptor, and specifically to the treatment and...
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6228880 |
4-amino-(ethylamino)-oxindole dopamine autoreceptor agonists
Compounds having dopaminegic activity are provided, having the formula: ##STR1## wherein R 1 and R 2 are each, independently, hydrogen, C 1 -10 alkyl, or (CH 2 ) m R 4 , wherein R 4 is phenyl...
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6221377 |
Administration media for analgesic, anti-inflammatory and anti-pyretic drugs containing nitrous oxide and pharmaceutical compositions containing such media and drugs
Administration mediums comprising solutions of nitrous oxide in water, alcohols, ethers or oils, and optionally including essential fatty acids or C 1 -C 6 alkyl esters thereof enhance the action...
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6214857 |
Substituted alkanohydroxamic acids and method of reducing TNFα levels
Imido and amido substituted alkanohydroxamic acids reduce the levels of TNFα and inhibit phosphodiesterase in a mammal. A typical embodiment is...
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6207686 |
Endothelin antagonists
A compound of formula (I), in which: R 1 is lower alkyl, cyclo(lower)alkyl, optionally substituted aryl, optionally substituted heterocyclic group, cyclo(lower)alkyl(lower)alkyl, or...
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6174883 |
3-substituted-2-oxindoles derivatives
This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the phamaceutically-accepted salts thereof which are inhibitors of prostaglandin H 2 synthase,...
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6169106 |
Indolinones having kinase inhibitory activity
The present invention relates to substituted indolinones of general formula ##STR1## wherein R 1 to R 5 , and X are defined as in claim 1, the isomers thereof and the salts thereof, particularly...
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6166023 |
1,5- and 3-O-substituted 1H-indazoles having anti-asthmatic, anti-allergic, anti-inflammatory, immunomodulating and neuroprotective action, process for their preparation and their use as medicaments
The invention relates to 1,5- and 3-O-substituted 1H-indazoles of formula (I) ##STR1##
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6166055 |
Benzoisothiazole compounds useful as IL-8 receptor antagonists
This invention relates to compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8). ##STR1##
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6160005 |
Medicament for circadian rhythm sleep disorder
A preventive and/or therapeutic medicament for circadian rhythm sleep disorders such as jet lag syndrome which comprises as an active ingredient an alkylenedioxybenzene derivative represented by...
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6147073 |
Substituted tetralymethylen-Oxindoles analogues as tyrosine kinase inhibitors
A tetralylmethylene-2-oxindole derivative having the following formula (I) ##STR1## wherein one or two of R, R 1 , R 2 and R 3 the said two being the same or different, are selected from: a)...
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6133306 |
Methods of inhibiting neurodegerative diseases
Methods for inhibiting a nitric oxide-mediated pathological condition and a neurodegenerative disease such as Parkinson's disease, Huntington's disease, Alzheimers's disease, and amyotrophic...
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6127404 |
Tissue selective compounds in the treatment of endometrial proliferation
The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment...
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6103752 |
Therapeutic heterocyclic compounds
Compounds of formula (I) ##STR1## wherein R and R 1 are hydrogen, C 1 -4 alkyl or are linked to form a ring, A is a cycloalkyl or alkyl-cycloalkyl group, n is an integer from 0 to 3, W is...
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6090839 |
Antidiabetic agents
The instant invention is concerned with aryl and heteroaryl oxyacetic acid type compounds which are useful antidiabetic compounds. Compositions and methods for the use of the compounds in the...
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6090818 |
Indolin-2-one derivatives, method for preparing them and pharmaceutical compositions containing them
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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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6071949 |
Use of lipoxygenase inhibitors as anti-cancer therapeutic and intervention agents
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6066663 |
Oxidation derivatives of indolylalkylamines and their use as drugs
The invention relates to derivatives of general formula I ##STR1## The invention also relates to pharmaceutical and cosmetic compositions comprising derivatives of general formula I.
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6051593 |
3-(cycloalkanoheteroarylidenyl)-2- indolinone protein tyrosine kinase inhibitors
The present invention relates to novel 3-(cycloalkanoheteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity...
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6028085 |
Indole derivatives as 5-HT receptor antagonist
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6001866 |
Method for treating and preventing inflammation and atherosclerosis
This invention provides a method for treating or preventing inflammation or atherosclerosis in mammals comprising administering an effective amount of a 15-LO inhibitor of Formula I: ##STR1##...
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5998463 |
Glycogen phosphorylase inhibitors
This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with...
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5994388 |
Cytochalasin and isoindolinone derivatives as inhibitors of angiogenesis
The present invention relates to inhibition of angiogenesis and the treatment of diseases mediated by angiogenesis. Particularly, the invention relates to the inhibition of neovascularization and...
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5985926 |
Method for inhibiting intracellular viral replication
There is disclosed a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans by administering an...
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5977130 |
Intimal hypertrophy inhibitors
The present invention is directed to an intimal hypertrophy inhibitor containing as the active ingredient an oxyindole derivative represented by the following formula (I) or a salt thereof:...
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5972988 |
Method for treatment of chronic bronchitis using indole compounds
A method is disclosed for the treatment of chronic bronchitis by administering to a mammal in need thereof a therapeutically effective amount of a 1H-indole-3-glyoxylamide compound.
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5948808 |
Indole-3-carbinol, diindolylmethane and substituted analogs as antiestrogens
Provided in the present invention are compounds and compositions of substituted indole-3-carbinols and diindolylmethane suitable for treating estrogen-dependent tumors. Also provided are methods of...
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5945413 |
Aspartyl protease inhibitors
This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized...
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5919809 |
3-substituted-2-oxindole derivatives
This invention relates to novel 3-substituted-2-oxindole derivatives of the formula ##STR1## and the pharmaceutically-acceptable salts thereof which are inhibitors of prostaglandin H 2 synthase,...
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5919790 |
Hydroxamate inhibitors of interleukin-1β converting enzyme
The present invention relates to compounds that are inhibitors of interleukin-1β converting enzyme that have the Formula II ##STR1## This invention also relates to a method of treatment of stroke,...
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5891902 |
Indole derivatives
The present invention relates to indole derivatives represented by formula (I): ##STR1## wherein R 1 and R 2 independently represent hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen,...
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5886020 |
3-(4'-dimethylaminobenzylidenyl)-2-indolinone and analogues thereof for the treatment of disease
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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5883116 |
3-(2'-alkoxybenzylidenyl)-2-indolinone and analogues thereof for the treatment of disease
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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5880141 |
Benzylidene-Z-indoline compounds for the treatment of disease
The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
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5861426 |
Nitro compounds of the formula A-X.sub.i -NO.sub.2 and their compositions having anti-inflammatory, analgesic and anti-thrombotic activities
New compounds and their compositions having anti-inflammatory, analgesic and anti-thrombotic activities, of the general formula: A--X 1 --NO 2 or their salts, wherein: A is R(COX u ) t , wherein...
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5859017 |
Method for inhibiting mast cell and basophil activation
In a method for treating or preventing allergy or allergic disorders an effective amount of a compound that inhibits intracellular generation of phosphatidic acid and diacylglycerol is...
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