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5395847 |
Imidazolyl-alkenoic acids
Angiotensin II receptor antagonists having tile formula: ##STR1## or a pharmaceutically acceptable salt thereof which are useful in regulating hypertension and in the treatment of congestive heart...
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5395849 |
Hybrid antitumor compounds containing a cyclic enediyne and a DNA-binder
The present invention provides novel antitumor agents which are hybrid molecules consisting of a cyclic enediyne unit attached to a DNA-binding unit via a linker unit, and having the general...
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5393762 |
Pharmaceutical agents for treatment of emesis
The present invention relates to a method of treating or preventing emesis in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane derivatives...
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5391367 |
Antifungal nail solution
A composition useful in the treatment of onychomycosis comprises tioconazole, a gel-forming agent and a hydro-alcoholic vehicle.
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5389661 |
Imidazole and 1,2,4-triazole derivatives with angiotensin II antagonist properties
This invention relates to novel substituted imidazole and triazole derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of...
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5385927 |
Hydroxy-3-[1-(1H-imidazol-4-yl)alkyl]-benzenecarboximidamides and their use in treating glaucoma
New 2-hydroxyl-3-[1-(1H-imidazol-4-yl)alkyl]-benzenecarboximidam
ides as well as their salts, having the formula ##STR1## wherein R 1 is hydrogen or an alkyl radical having 1 to 4 carbon atoms, ...
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5385919 |
Imidazolinyl indole derivatives useful in the treatment of diabetes
The invention relates to compound of formula I: ##STR1## wherein R 1 is hydrogen or hydroxy; R 2 is hydrogen or methyl; R 3 is hydrogen or methyl; and R is 2-pyridyl, 3-pyridyl or --C 6 H 4 ...
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5380742 |
4H-thieno[3,4-c]pyrrole derivatives
Pyrrole derivatives of formula: ##STR1## in which R 1 represents a hydrogen or halogen atom, a linear or branched C 1 -6 alkyl group, a C 3 -6 alkenyl group, a C 1 -4 alkoxymethyl group, benzyl, a...
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5376666 |
Angiotension-II receptor blocking, azacycloalkyl or azacycloalkenyl
Novel heterocycle substituted azocycloalkane benzylimidazoles of Formula (I), which are useful as angiotensin-II antagonists, are disclosed: ##STR1##
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5374615 |
Indole- and benzimidazole-substituted imidazole and benzimidazole derivatives
Novel compounds are disclosed having the formula ##STR1## wherein X, R 1 , R 2 , R 3 , R 4 , and R 5 are substituents. These compounds inhibit the action of angiotensin II and are useful,...
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5374642 |
Hydroquinone diethers, their preparation and their use
Hydroquinone diethers of the general formula I ##STR1## where R 1 is hydrogen, halogen or C 1 -C 6 -alkyl, A and B are each unsubstituted or substituted methylene, ethylene or propylene and X...
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5374643 |
Aryl urea (thiourea) and cyanoguanidine derivatives
Novel compounds useful, for example, in the treatment of ischemic conditions and arrhythmia having the formula I ##STR1## wherein X is oxygen, sulfur or --NCN and the R groups are as defined herein.
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5369125 |
Cholesterol-lowering agents
This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds...
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5366990 |
Method for treating alcohol abuse and alcoholism
A method for decreasing appetite for alcohol in humans which comprises the steps of providing an effective dosage of an alpha-2-adrenergic antagonist to the subject.
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5364875 |
Imidazoles linked to bicyclic heterocyclic groups for the treatment of atherosclerosis
Disclosed are imidazoles linked to bicyclic heterocyclic groups, as inhibitors of acyl-CoA:cholesterol acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and...
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5360801 |
Pharmacological stimulation of eye growth
A method of inducing axial elongation of an eye of an animal comprising contacting a first open animal eye with a cholinergic agonist, detecting the change in axial growth of the first eye,...
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5358946 |
Heterocycle-substituted amides, carbamates and ureas as agents for the treatment of atherosclerosis
This invention relates to imidazoles, namely, heterocycle-substituted amides, carbamates and ureas as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), pharmaceutical compositions...
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5356920 |
Imidazol-2-yl derivatives of substituted bicyclic compounds
Compounds having formula (I) ##STR1## wherein Z is --O-- or --CH 2 --; n is 1-6; R is hydrogen, C 1 -C 6 alkyl, phenyl or optionally substituted phenyl-C 1 -C 3 alkyl; R 2 is C 1 -C 8 ...
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5356922 |
Imidazole compounds, processes for their preparation, pharmaceuticals based on these compounds and some intermediates
Imidazole compounds of the formula I ##STR1## in which R 1 =alkyl, R 2 and R 3 =H, halogen or alkyl, X=OH or an amide radical having certain substituents, processes for their preparation...
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5356921 |
Imidazolylphenol compounds, pharmaceutical compositions containing them, and processes for preparing such compounds and compositions
3- and 4-(1H-imidazol-1-yl)phenol compounds corresponding to the formula I ##STR1## in which R 1 represents NH 2 or CH 3 , R 2 represents H or CH 3 , X represents O or S, Y represents H, OH or...
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5354769 |
Benzofuranylimidazole derivatives and therapeutical compositions containing the same
The invention relates to benzofuranylimidazole derivatives of the general formula (1) ##STR1## wherein R 1 and R 2 represent various radicals, to a process for their preparation and to...
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5352687 |
Substituted phenylacetamides
Substituted phenylacetamides can be prepared by reaction of appropriately substituted phenylacetic acids with imidazoles and subsequent amidation. The substituted phenylacetic acid derivatives can...
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5352692 |
Thiophene-2-carboxylic acid derivatives
There are described novel compounds of the general formula ##STR1## in which R in position 3 or 4 is hydrogen, methyl, chlorine or bromine and R 2 is C 1 -C 10 -alkyl, C 3 -C 7 -cycloalkyl or...
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5350751 |
Substituted imidazoles, pharmaceutical compositions containing these, and the use thereof as antagonists of angiotensin II receptors for the treatment of high blood pressure
The invention relates to compounds of the formula I ##STR1## in which X, Y and Z are identical or different and are N or CR 2 , R 1 and R 2 are as defined in the description, L is an alkylene...
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5344834 |
Functionalized vinyl azoles and methods of use
Pharmaceutical preparations comprising functionalized vinyl azoles of formula I ##STR1## wherein the substituents are as defined herein, including novel compounds, as well as methods of use and...
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5340826 |
Pharmaceutical agents for treatment of urinary incontinence
The present invention relates to a method of treating or preventing urinary incontinence in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, azanorbornane...
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5338756 |
Benzimidazole compounds
Novel imidazoles of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts with acids and bases having an antagonistic activity against angiotensin II receptors.
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5338744 |
Angiotensin II antagonists used to treat reproductive functions associated with AT.sub.2 receptors
The present invention relates to the use of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine-6-carboxylic acids and analogs thereof in antagonizing the binding of angiotensin II to AT 2 receptors.
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5336686 |
17 Methylene lactones of steroids
A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the application having antiglucocorticoid and antiprogestomimetic...
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5332736 |
Anti-convulsant aroyl aminoacylpyrroles
Aroyl aminoacyl pyrroles are pharmaceutically useful as anti-convulsants, which includes utility for the treatment of epilepsy.
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5332427 |
Wood preservatives
A wood preservative comprising a styryl triazole derivative of the formula [I] ##STR1## wherein X represents chlorine or hydrogen as an active ingredient. The present wood preservative has a...
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5324728 |
Naphthoic acid derivative
A naphthoic acid derivative represented by the following general formula or a salt thereof: ##STR1## wherein R 1 , R 2 and R 3 are each independently a hydrogen atom, a halogen atom, a hydroxyl...
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5321038 |
Cis-azole derivatives, intermediates thereof and fungicidal compositions
Disclosed herein is a process for preparing a cis-azole derivative represented by the general formula (I) ##STR1## wherein R 1 and R 2 denote each a hydrogen atom or an alkyl group, R denotes a...
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5321032 |
Peptide compounds and pharmaceutical compositions thereof
A tachykinin-antagonistic compound of the following general formula: R 1 --A 1 --D--Trp(R 2 )--A 2 --R 3 [wherein R 1 is hydrogen or amino-protective group R 2 is amino-protective...
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5318980 |
Sulphonylbenzyl-substituted imidazoles
Sulphonylbenzyl-substituted imidazoles can be prepared by first reacting imidazolylaldehydes with sulphonylbenzyl compounds and then oxidising or reducing the aldehyde function in the customary...
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5318983 |
Trisubstituted pyrrole derivatives having antifungine activity, and related pharmaceutical compositions
The pyrrole derivatives having the general formula: ##STR1## wherein X and X' represent H, alkyl, alkoxy, halogen, nitro, amino, and R is H, alkyl, aryl, arylalkyl, cycloalkylmethyl, are active...
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5312826 |
N,3-disubstituted alaninamide derivatives
Disclosed are a dicarboxylic acid compound represented by the formula (I): ##STR1## wherein R represents hydrogen atom, a lower alkyl group, phenyl group or hydroxyl group; R 1 represents a...
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5310750 |
Heterocyclic compounds useful as α.sub.2 -adrenoceptor antagonists
A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R 1 and R 2 may each represent hydrogen or alkyl providing that at least one of R 1 or R 2 represents...
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5310748 |
Imidazoles for the treatment of atherosclerosis
Disclosed are imidazoles as inhibitors of acylCoA:cholesterol acyltransferase (ACAT), processes for their preparation, pharmaceutical compositions, and their use as antihypercholesterolemics and/or...
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5308853 |
Substituted-5-methylidene hydantoins with AT.sub.1 receptor antagonist properties
Substituted 1-benzylimidazole-5-methylidene hydantoins are disclosed as well as methods of preparing them, pharmaceutical compositions containing them, and method of using them. Intermediates...
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5302613 |
Antiatheroscleroic and antithrombotic 2-amino-6-phenyl-4H-pyran-4-ones
This invention relates to compounds of Formula I ##STR1## which are useful as antiatherosclerotic agents and inhibitors of cell proliferation for the treatment of proliferative diseases. In...
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5302604 |
Cholesterol lowering compounds produced by directed biosynthesis
Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal...
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5300508 |
Method for intercepting activated species of dioxygen
A method for intercepting an activated species of dioxygen by administering an N-substituted pyrrole derivative having the formula: ##STR1## in which: R is an amino acid derivative, a non-protein...
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5298520 |
Triazole containing indole derivatives
A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT 1 -like receptors and are therefore useful in the treatment of clinical conditions, in...
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5296499 |
Indole derivatives, their production and use
An agent for inhibiting bone resorption comprising an indole derivative of the formula (I): ##STR1## wherein each ring of A and B is optionally substituted, R is a hydrogen atom, a lower alkyl...
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5294627 |
Directed biosynthesis of biologically active compounds
Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal...
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5290807 |
Method for regressing angiogenesis using o-substituted fumagillol derivatives
O-substituted fumagillol derivatives and its salts have an angiogenesis regressing activity are useful for treatment of diseases induced by abnormally stimulated neovascularization.
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5290799 |
7-oxabicycloheptyl substituted heterocyclic thioamide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula ##STR1## wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is...
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5284647 |
Mesotetraphenylporphyrin complex compounds, process for their production and pharmaceutical agents containing them
Porphyrin complex compounds, consisting of a mesotetraphenylporphyrin ligand, optionally at least one ion of an element with atomic numbers 13, 21, 32, 37-39, 42-44, 49, 50 or 57-83 as well as...
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5280033 |
Substituted 1-(alkoxy-iminoalkyl) imidazole derivatives and their use in treating disease related to an enhancement of thromboxane-A.sub.2 syntheis
1-(Alkoxy-iminoalkyl)imidazole derivatives of formula ##STR1## wherein R is hydrogen or C 1 -C 4 alkyl; A is C 1 -C 4 alkylene optionally substituted by phenyl optionally substituted by halogen...
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