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5466704 |
N-substituted imidazole and benzimidazole derivatives useful as angiotenson II antagonists
Compounds are disclosed having the formula ##STR1## These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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5464854 |
Method of modifying ovarian hormone-regulated AT1 receptor activity as treatment of incapacitating symptom(s) of P.M.S.
The method of treatment moderating, blocking and/or eliminating premenstrual syndrome embodies the intermittent administering of an AT1 antagonist to a female having menstrual cycles characterized...
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5462954 |
Substituted phenyl phenol leukotriene antagonists
Antagonists having a substituted phenyl phenol or a substituted phenolic biphenyl structure, and various derivatives thereof, are specific leukotriene antagonists. Their structures, use and...
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5462963 |
Chelator compositions comprising α-diamine compounds
The present invention involves photoprotective compositions which are useful for topical application to prevent damage to skin caused by acute or chronic exposure to ultraviolet light comprising...
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5461049 |
Amide tetrazole ACAT inhibitors
Amide tetrazoles of the formula ##STR1## wherein aryl includes phenyl and naphthyl, unsubstituted or substituted, X is O, N--R 5 , or --NR 3 R 4 , where R 2 , R 4 , and R 5 include alkyl...
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5459148 |
Biphenyl derivatives and their use for the treatment of hypertension and cardiac disease
Compounds of formula (I): ##STR1## [wherein: A represents a group (IIa), (IIb) or (IIc): ##STR2## R 1 is alkyl, alkenyl, cycloalkyl or a group of formula R 4 --Y--R 5 --, where: R 4 is...
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5459134 |
(Fused) benz (thio) amides
A novel (fused) benz(thio)amide of the general formula: ##STR1## or a non-toxic salt thereof, wherein R 4 represents: (i) when B represents a closed ring, a group of the general formula: ##STR2##...
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5457114 |
Amidinophenylalanine derivatives, a process for the preparation thereof, use thereof and agents containing these as anticoagulants
Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
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5455222 |
1-substituted-5-thiomethylthiocyanato-1H-tetrazoles, compositions containing them and their use as antimicrobial and marine antifouling agents
Disclosed are substituted-5-thiomethylthiocyanato-1H-tetrazole compounds corresponding to the formula ##STR1## wherein R represents a C 1 -C 6 straight or branched chain alkyl radical, a C 3 -C...
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5451597 |
Treatment of circulatory disorders using n-substituted (α-imidazolyl-toluyl) pyrrole angiotensin II antagonists
A class of N-substituted (α-imidazolyltoluyl)pyrrole compounds is described for use in treatment of circulatory disorders. Compounds of particular interest are angiotensin II antagonists of the...
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5449682 |
Angiotensin II antagonists incorporating a substituted benzyl element
Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. ##STR1## wherein the substituents are...
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5444081 |
Substituted histidines having angiotension II receptor antagonist activity
Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma,...
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5444080 |
Substituted [1H-imidazol-5-ylialkanoic acids having angiotension II receptor antagonist activity
Angiotensin II receptor antagonists having the formula: ##STR1## which are useful in regulating hypertension and in the treatment of congestive heart failure, renal failure, and glaucoma,...
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5436260 |
Angiotensin II receptor antagonists
Substituted 1-benzylimidazole-5-methylidene hydantoins are disclosed as well as methods of preparing them, pharmaceutical compositions containing them, and methods of using them. Intermediates...
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5434167 |
Imidazolines N-substituted by a biphenylmethyl group, their medical use and the pharmaceutical compositions therefor
The invention relates to compounds of the formula ##STR1## in which X and R 1 -R 5 are defined in the specification and their salts where appropriate, all of which are useful as angiotensin II...
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5430047 |
Neurotensin antagonists
Neurotensin antagonists are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as central nervous system agents and are particularly useful...
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5426114 |
ω-[2-(tetrazolylalkyl)cyclohexyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors
The present invention pertains to antagonists of excitatory amino acid receptors, their method or preparation as well as compositions pertaining to them, which have the general formula: ##STR1##...
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5426105 |
Conformationally restricted angiotensin II antagonists
Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders. Compounds of particular interest...
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5426113 |
Method of preventing ulcer formation caused by nonsteroidal antiinflammatory drugs employing tetrazol-benzothiophene carboxamide compounds
Tetrazol-benzothiophenes carboxamides or a pharmaceutically acceptable salt thereof are useful in preventing ulcer formation caused by nonsteroidal antiinflammatory drugs in mammals.
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5414008 |
Imidazolyl-substituted phenylpropionic and cinnamic acid derivatives
Imidazolyl-substituted phenylpropionic and cinnamic acid derivatives are prepared by reacting appropriate benzyl compounds with imidazoles and optionally varying the substituents. The...
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5409947 |
Cycloheptimidazole derivatives, method of manufacturing the same and therapeutic agents containing these compounds
New therapeutic agents of cycloheptimidazole derivatives are disclosed, which are represented by the following formula or its alkali-addition salts. ##STR1## (wherein R 1 represents H or isopropyl...
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RE34918 |
Azaazulene compounds which are useful as antiallergic and antiinflammatory agents
An azaazulene derivative having the general formula (I): ##STR1## wherein R 1 is hydrogen atom or isopropyl group; the bond C N between C at the 2-position and N at the 1-position is single bond...
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5407951 |
Sulphonamidocycloalkane compounds, pharmaceutical compositions containing them, and methods of use thereof
The present invention provides sulphonamides of the general formula: ##STR1## wherein R 1 and R 2 , which can be the same or different, are hydrogen or halogen atoms or C 1 -C 6 -alkyl,...
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5401764 |
Benzimidazole derivative compositions and medical use thereof
1-Acetoxyethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl]benzi
midazole-7-car boxylate or a pharmaceutically acceptable salt thereof has potent angiotensin II antagonistic activity and...
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5395840 |
Heterocyclically substituted phenyl-cyclohexane-carboxylic acid derivatives
Heterocyclically substituted phenyl-cyclohexanecarboxylic acid derivatives are prepared by reacting appropriate heterocyclic compounds with cyclohexanebenzyl halides. The compounds can be employed...
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5393768 |
Leukotriene antagonists
This invention provides novel benzene derivatives which are leukotriene antagonists, formulations of those derivatives, intermediates for preparing the derivatives, and a method of using those...
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5393767 |
Insect control with substituted triazole and tetrazole compounds
Insects, especially sucking insects, such as brown planthoppers, and phytophageous mites, such as two-spotted spider mites, are controlled by applying an triazole or tetrazole compound substituted...
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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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5389634 |
Imidazole derivatives having angiotensin II receptor antagonistic activity
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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5389641 |
Fused heterocyclic compounds, having angiotensin II antagonistic activity
Fused heterocyclic compounds of the formula (I): ##STR1## wherein R 1 is an optionally substituted hydrocarbon residue which may be attached through a hetero atom; R 2 is a group capable of...
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5389663 |
1-(1h-1,2,4-triazole-yl)-2-propanol compounds
An azole compound represented by the formula (I): ##STR1## wherein X is a nitrogen atom; Ar is a phenyl group substituted by halogen or a halogenated C 1 -4 alkyl group; R 1 and R 2 independently...
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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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5389659 |
C-linked pyrazole derivatives
The invention provides compounds of the general formula (I): ##STR1## or a physiologically acceptable salt, solvate (e.g. hydrate) or a metabolically labile ester thereof. The compounds may be used...
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5380739 |
Substituted indole derivatives
Compounds of the Formula (I), (II), or (III): ##STR1## wherein the variables are as defined in the specification and the pharmaceutically acceptable salts thereof, exhibit useful pharmacological...
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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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5374638 |
Six membered ring fused imidazoles substituted with phenoxyphenylacetic acid derivatives used to treat asthma
Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as...
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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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5371100 |
Optically active tetrazole compounds, and fungicidal compositions thereof
An optically active azole compound of the formula (I): ##STR1## wherein R 1 and R 2 are independently a hydrogen atom, a halogen atom, a haloalkyl group, a haloalkoxy group or an optionally...
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5364876 |
Omega-[2-(alkyl)phenyl]-2-aminoalkanoic acids as antagonists of excitatory amino acid receptors
The present invention pertains to antagonists of excitatory amino acid receptors, their method of preparation as well as compositions pertaining to them, which have the general formula: ##STR1##...
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5362744 |
Tetrazole-substituted urea acat inhibitors
Novel ACAT inhibitors useful in the treatment of atherosclerosis which are tetrazole-substituted ureas,
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5356919 |
Leukotriene B.sub.4 synthesis inhibitors
This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CHCH--, or --CHN--; wherein R 1 is --CO 2 R 2 or...
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5352690 |
1,2,4-trioxygenated benzene derivatives useful as leukotriene antagonists
This invention provides 1,2,4-trioxygenated benzene derivatives which are leukotriene B 4 antagonists, formulations of those derivatives, and a method of using those derivatives for the treatment...
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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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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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5338740 |
Angiotensin II receptor antagonists
The present invention relates to novel heterocyclic derivatives of the formula Ar--W--Het wherein Ar, W and Het are as defined below, and related compounds, pharmaceutical compositions comprising...
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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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5328919 |
Pivaloyloxymethyl 2-ethoxy-1-[[2'-(1H-tetrazol-5-yl) biphenyl-4-yl] benzimidazole-7-carboxylate or a pharmaceutically acceptable salt thereof and compositions and method of pharmaceutical use thereof
Pivaloyloxymethyl2-ethoxy-1-[['-(1H-tetrazol-5-yl)biphenyl-4
-yl]methyl]benz imidazole-7-carboxylate or a pharmaceutically acceptable salt thereof has potent angiotensin II antagonistic activity...
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5318981 |
Cholecystokinin antagonists useful in the treatment of panic attacks
Unnatural dipeptoids of α-substituted Try-Phe derivatives are useful as agents in the treatment of panic disorders. These dipeptoids are Cholecystokinin-B Receptor (CCK B ) antagonists having...
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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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