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5382586 |
Aryl (or heteroaryl)piperazinylalkylazole derivatives, their preparation and their application as medicaments
The present invention relates to heterocyclic compounds, characterized in that they have the general formula I ##STR1## wherein Ar, n, and Z 1 and Z 6 are defined in the specification, are...
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5382584 |
Adenosine re-uptake inhibiting derivatives of diphenyl oxazoles, thiazoles and imidazoles
A series of 1-piperazinyl-N-phenylacetamide derivatives of 4,5-diphenyl-oxazoles, thiazoles, and imidazoles which are novel adenosine transport inhibitors have been found to provide effective...
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5380726 |
Substituted dialkylthio ethers
Substituted dialkylthio ethers of formula I ##STR1## wherein R 1 -R 6 , alk, X and Y are as defined in the description, and salts thereof, exhibit properties inhibiting the biosynthesis of...
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5358939 |
Fungicidal 2-aryl-2,2-disubstituted ethyl-1,2,4-triazoles
2-Aryl or 2-heterocyclyl-2,2-disubstituted ethyl-1,2,4,-triazoles have been shown to have fungicidal activity.
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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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5348955 |
N,N-diacylpiperazines
Diacylpiperazines of general structural formula: ##STR1## are: angiotensin II (A-II) antagonists with affinity for both AT 1 and AT 2 receptors useful in the treatment of hypertension, congestive...
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5340809 |
New 1-(alkoxybenzyl)piperazine amide compounds
A compound selected from those of formula (I): ##STR1## with R 1 , R 2 and n as defined in the description, and medicinal products containing the same useful in treating or in preventing a...
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5340810 |
Benzanilide derivatives
The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R 1 represents a hydrogen atom or a halogen atom or a group selected from...
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5332738 |
Imidazolidine antipsychotic agents
Compounds of the general formula I ##STR1## are disclosed as novel antipsychotic agents. Pharmaceutical compositions and methods of treating convulsions employing such compounds of formula I.
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5332742 |
Renin inhibitors
A renin inhibiting compound of the formula: ##STR1## wherein R 1 is 4-piperazinyl, 1-methyl-4-piperazinyl, 1-methyl-l-oxo-4-piperazinyl, 2-oxo-4-piperazinyl, 4-morpholinyl, 4-thiomorpholinyl or...
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5328916 |
Heterocyclic compounds useful for inhibition of renin
New heterocyclic compounds of the formula X--W--CR 1 R 2 --CO--Y--NR 3 --CHR 4 --CR 5 --CH 2 --(CR 6 R 7 ) r --Z--Het I in which R 1 to R 7 , W, X, Y, Z, r and Het...
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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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5281594 |
Substituted 1-(alkoxyphenyl)piperazines with ons and antihypertensive activity
Substituted 1-(alkoxyphenyl)piperazines are disclosed as partial dopamine agonists useful in the treatment of dopaminergic dysregulation. The compounds...
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5281614 |
Substituted 1,2,4-triazoles bearing acidic functional groups as angiotensin II antagonists
Novel substituted triazolinone, triazolinethione, and triazolinimine compounds of the formula I are useful as angiotensin II antagonists. ##STR1##
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5270312 |
Substituted piperazines as central nervous system agents
Substituted piperazines and derivatives of Formula I ##STR1## are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous...
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5266571 |
Treatment of hemorrhoids with 5-HT.sub.2 antagonists
This invention relates to a method for treating or preventing hemorrhoids, comprising administering to a susceptible animal a 5-hydroxytryptamine 2 (5-HT 2 ) receptor antagonist at an...
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5258381 |
2-substituted-2-imidazolines
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging) which contain novel 2-substituted-2-imidazolines. Accordingly, a composition is...
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5256664 |
Antidepressant 3-halophenylpiperazinylpropyl derivatives of substituted triazolones and triazoldiones
2-(3-[4-(3-Halophenyl)-1-piperazinyl]propyl derivatives of certain 4-alkyl- or 4-phenoxyalkyl-2,4-dihydro-3H-1,2,4-triazol-3-ones and triazol-3,5-diones are psychotropic agents having promise as...
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5256657 |
Succinamide derivative matrix-metalloprotease inhibitors
Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH 2 R 1 has the R-configuration, the carbon atom bearing CH 2 R 2 has...
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5254553 |
4-[4- [4-(4-hydroxyphenyl)-1-piperazinyl]phenyl]-5-methyl-3H-1,2,4-triazol-3-o ne derivatives
2-[2-(4-chlorophenyl)-2-(hydroxy or oxo)ethyl]-2,4-dihydro-4-[4-[4-(4-hydroxyphenyl)-1-piperazin
yl]phenyl]-5-m ethyl-3H-1,2,4-triazol-3-one having the formula ##STR1## wherein X represents C=O or...
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RE34299 |
1-(4'-fluorophenyl)-3,5-substituted indoles useful in the treatment of psychic disorders and pharmaceutical compositions thereof
The present invention relates to novel indole derivatives which have interesting pharmacodynamic effects indicating pronounced activity in the treatment of psychic disorders, especially psychoses...
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5219856 |
Angiotensin-II receptor blocking, heterocycle substituted imidazoles
Novel heterocycle substituted imidazoles of Formula (I), which are useful as angiotensin-II antagonists, are disclosed: ##STR1##
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5217985 |
Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension
Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs...
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5208235 |
Indole- and benzimidazole-substituted imidazole derivatives
Novel compounds having the formula ##STR1## where X R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore for...
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5208234 |
Substituted imidazole phosphonic and phosphinic acid derivatives
Novel compounds having the formula ##STR1## wherein R 1 , R 2 , R 3 , R 4 and R 5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for...
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5202346 |
Piperidinyl and piperazinyl derivatives
Compounds of the formula: ##STR1## in which R 1 is alkylsulfonamido of 1 to 6 carbon atoms, arylsulfonamido of 6 to 10 carbon atoms, --NO 2 ,--CN, 1-imidazolyl or 1,2,4-triazol-1-yl; Y is...
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5196546 |
Selective pyrazoline insecticides and fungicides
Certain pyrazolines have been found to be useful as aphicides and fungicides.
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5190942 |
Benzoxazole and related heterocyclic substituted imidazole and benzimidazole derivatives
Novel compounds are disclosed having the formula ##STR1## wherein X, Y, R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful,...
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5189048 |
Substituted 1,2,3 triazole angiotensin II antagonists
This invention includes substituted pyrroles, pyrazoles and triazoles, processes for their preparation, pharmaceutical compositions containing them, and their use as antihypertensive agents, and as...
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5189036 |
Imidazolylbenzoyl substituted heterocycles
Novel imidazolybenzoyl substituted heterocycles and their use as cardiovascular agents most especially as Class III antiarrhythmic agents is described. Pharmaceutical formulations containing such...
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5185358 |
3-heteroatom containing urea and thiourea ACAT inhibitors
Compounds useful in treating hypercholesterolemia and atherosclerosis having the formula ##STR1## wherein X is oxygen or sulfur, Het is a monocyclic heterocyclic group having three hetero atoms...
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5182284 |
Piperazine compounds, processes for preparation thereof and medical uses thereof
Disclosed are a piperazine compound of the formula below or a pharmaceutically acceptable salt thereof, medical uses thereof, and processes for preparing the same: ##STR1## wherein each of R and R'...
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5177078 |
Piperazine derivatives
Compounds of formula ##STR1## where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, R is hydrogen or lower alkyl, R 1 is an aryl or...
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5166205 |
Derivatives of 1-diphenylmethyl piperazine and their use as antihistamines
The present invention relates to novel derivatives of 1-diphenylmethyl piperazinyl, characterized in that they correspond to the general formula I, and their therapeutically acceptable salts,...
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5155118 |
Method and composition for preventing NSAID-induced renal failure
Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
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5152988 |
Imidazole compounds in compositions and methods in thrombolytic therapy
The use of imidazoles of the formula ##STR1## and imidazolium salts of the formula ##STR2## in thromobolytic therapy are described.
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5153197 |
Treatment of hypertension with angiotensin II blocking imidazoles
Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
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5135928 |
Triazolo derivatives and process for their preparation
This invention relates to novel triazolo derivatives, a process for the preparation thereof, pharmaceutical compositions comprising the same, to the use of the said triazolo derivatives for the...
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5134142 |
Pyrazole derivatives, and pharmaceutical composition comprising the same
The present invention concerns pyrazole derivatives of formula: ##STR1## used for the treatment of inflammation, pain, thrombosis and rheumatism.
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5128355 |
Treatment of congestive heart failure with angiotensin 11 receptor blocking imidazoles
Substituted imidazoles such as ##STR1## are useful as angiotensin II blockers. These compounds have activity in treating hypertension and congestive heart failure.
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5120718 |
Candida acid protease inhibiting compounds
Compounds which inhibit Candida acid protease are disclosed which have the formula: ##STR1## wherein R 1 is loweralkyl, loweralkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl,...
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5118685 |
Aminopropanol derivatives of substituted 2-hydroxy-propiophenones, and therapeutic agents containing these compounds
Aminopropanol derivatives of the formula: ##STR1## where R 1 and R 2 are identical or different and are each hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl or hydroxyalkyl, each of not more than 6...
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5116835 |
Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof
Enzyme-inhibiting urea derivatives of dipeptides, a process for the preparation thereof, agents containing these, and the use thereof. The present invention relates to compounds of the formula I...
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5106845 |
Calcium antagonists
The present invention is directed to a new class of cyclic guanidines of the formula: ##STR1## in which Q is represented by a substituent selected from the group consisting of (CH 2 ) n in which n...
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5093346 |
Substituted 1,2,4-triazole angiotensin II antagonists
Substituted pyrroles, pyrazoles and triazoles such as ##STR1## and their pharmaceutically suitable salts are useful as antihypertensive agents and for treatment of congestive heart failure.
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5081127 |
Substituted 1,2,3-triazole angiotensin II antagonists
Substituted pyrroles, pyrazoles and triazoles such as ##STR1## and their pharmaceutically suitable salts are useful as antihypertensive agents and for treatment of congestive heart failure.
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5066652 |
Thiomethyl and sulfinylmethyl derivatives having gastric acid antisectetory activity and pharmaceutical compositions containing them
Compounds of the formula Het-S(O) n -CH 2 -A (I) wherein Het is a substituted imidazolyl, purinyl, thieno-imidazolyl or imidazo-pyridyl group, n is 0 or 1, A is...
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5063220 |
Parenteral formulations of 1-diphenylmethyl-4-((2-(4-methylphenyl)-5-methyl-1H-imidazol-4-yl)methyl )piperazine
A pharmaceutical formulation suitable for parenteral (preferably intravenous) administration includes an effective amount of...
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5059601 |
Imidazolone derivatives with activity on central nervous system and antihypertensive activity, preparation methods thereof, and pharmaceutical compositions containing them
Invention concerns 4,5-bisubstituted-2-imidazolone derivatives of formula I ##STR1## and pharmaceutically acceptable salts thereof, having high affinity in vitro for D 2 , 5-HT 2 , 1 receptors...
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5055482 |
N-phenylpyrazol-4-yl ether derivatives
An N-phenylpyrazol-4-yl ether derivative of the formula: ##STR1## wherein R 1 represents halogen, alkyl or alkoxy unsubstituted or substituted by halogen, alkylthio or alkylsulphinyl substituted...
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