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5646170 |
Tetrazole alkyl amide acat inhibitors
Pharmaceutically useful compounds having ACAT inhibitory activity of the formula ##STR1## wherein n is 0, 1, or 2, for X other than tetrazole and n=2 then R 2 R 3 H; R 1 is phenyl,...
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5641798 |
Bicyclic compounds and their use as excitatory amino acid receptor antagonists
This invention provides novel bicyclic compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides...
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5631281 |
N-substituted cycloalkyl and polycycloalkyl α-substituted Trp-Phe- and phenethylamine derivatives
Novel unnatural dipeptoids of α-substituted Trp-Phe derivatives useful as agents in the treatment of obesity, hypersecretion of gastric acid in the gut, gastrin-dependent tumors, colorectal...
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5629331 |
Process for the preparation of a tetrazole derivative in two crystalline forms and novel the crystalline forms thereof
The present invention relates to a process for the preparation of the 2-n.butyl-3-[[2'-(tetrazol-5-yl)biphenyl-4-yl]methyl]-1,3-di
azaspiro [4.4]-non-1-en-4-one by reaction of the corresponding...
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5616599 |
Angiotensin II antagosist 1-biphenylmethylimidazole compounds and their therapeutic use
Compounds of the following formula (I) or the formula (I) p : ##STR1## wherein R 1 is alkyl or alkenyl; R 2 and R 3 are hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl, or aryl fused to...
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5607956 |
1-heteroazolyl-1-heterocyclyl alkane derivatives and their use and their use as neuroprotective agents
The present invention relates to novel heterocyclic compounds having the general formula (1) ##STR1## geometric and optical isomers and racemates thereof where such isomers exist, as well as...
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5607957 |
Imidazole, triazole and tetrazole 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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5605917 |
Method of treating dysmenorrhea employing an interphenylene 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analog
A method is provided for treating dysmenorrhea (menstrual cramps) employing an interphenylene 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analog thromboxane A 2 receptor...
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5604251 |
Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain and their use as angitensin II receptors
Imidazole derivatives with a biphenylsulfonylurea or biphenylsulfonylurethane side chain, process for their preparation and their use Compounds of the formula (I) ##STR1## in which R 1 is, for...
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5602161 |
Tetrazolylphenyl pivalate derivatives and medicinal composition containing the same as effective component
The tetrazolylphenyl pivalate of the the following general formula or a pharmaceutically acceptable salt thereof: ##STR1## wherein R 1 and R 2 each represents a hydrogen atom, a lower alkyl group...
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5602127 |
(Alkanesultam-1-yl)-benzimidazol-1-yl)-1yl)-methyl-biphenyls useful as angiotensin-II antagonists
Angiotensin-II antagonists of the formula ##STR1## wherein R 1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R 2 is, inter alia, optionally substituted...
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5599830 |
Sulphorous derivatives of imidazole and their use as medicaments
The invention relates to the products: ##STR1## in which: R 1 =alkyl, alkenyl, alkynyl, alkylthio, R 2B , R 3B representing: hydrogen, mercapto, formyl, acyl, carboxy nitro, cyano, --PO...
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5594016 |
Naphthalene derivatives
Naphthalene derivatives represented by the formula (I): ##STR1## wherein the symbol ##STR2## --X-- represents --O-- or --S--, Y-- represents N-- or CR 5 --, R 1 , C 2 , R 3 , R 4 and R 5...
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5591762 |
Benzimidazoles useful as angiotensin-11 antagonists
Disclosed herein are angiotensin-II antagonists of the formula ##STR1## wherein R 1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R 2 is, inter alia, optionally...
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5587390 |
Imidazole derivatives having a II antagonist activity
Imidazole derivatives having A II antagonist activity, of Formula I, the processes for the preparation thereof, pharmaceutical compositions containing them and the use thereof as therapeutic...
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5585394 |
1-benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives
The present invention relates to 1-benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives of the formula: ##STR1## to their preparation and to the pharmaceutical compositions in which they...
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5583152 |
Method for treating vasospastic cardiovascular diseases heterocyclic amide derivatives
The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts...
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5583128 |
Contraception in female primates without affecting the menstrual cycle
The invention relates to the use of aromatase inhibitors for contraception in female primates and to a method for contraception in female primates using such substances and to the use of those...
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5580896 |
Treatment of pain and colorectal cancer with dipeptoids of α-substituted Trp-Phe derivatives
This invention relates to the treatment of pain and inhibiting the growth of colorectal cancer with dipeptoids of α-substituted Trp-Phe derivatives.
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5580542 |
Method of testing for nephritis
Disclosed is an acetyltransferase activity measuring agent which contains an arylamine derivative. As the arylamine derivative, sodium p-aminohippurate can be used preferably. Use of the...
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5578634 |
1H-indole-3-acetic acid hydrazide sPLA.sub.2 inhibitors
A class of novel 1H-indole-3-acetic acid hydrazides is disclosed together with the use of such indole compounds for inhibiting sPLA 2 mediated release of fatty acids (e.g., arachidonic acid) for...
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5565485 |
Biphenyl compounds useful or endothelin antagonists
Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension,...
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5565480 |
Substituted histidines
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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5563164 |
Phospholipase A.sub.2 inhibitors
This invention provides methods for the treatment or prevention of Alzheimer's disease in a mammal which comprises administering to a mammal in need thereof an effective amount of an inhibitor of...
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5556788 |
Fructosmaine reagent and calibrator system
A system for determining the concentration of fructosamine in sera which consists of a first reagent in which a tetrazolium salt which reduces all reactive substances in sera including fructosamine...
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5554633 |
Substituted amines as tachykinin receptor antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR 9 , where R 9 is...
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5552422 |
Aryl substituted 5,5 fused aromatic nitrogen compounds as anti-inflammatory agents
The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a...
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RE35321 |
Tetrazoleacetic acid derivatives having aldose reductase inhibitory activity
A tetrazoleacetic acid derivative represented by the following general formula (I): ##STR1## [in Formula (I), wherein R 1 represents a hydrogen atom or an alkyl group; R 2 represents a...
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5545651 |
Imidazole 5-position substituted angiotensin II antagonists
Novel substituted imidazoles of Formula (I), which are useful as angiotensin II antagonists, are disclosed: ##STR1##
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5543428 |
Method for treating resistant tumors
This invention provides a method of reversing multidrug resistance in a multidrug resistance tumor comprising administering a multidrug resistance reversing amount of any of a series of phenoxy...
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5543433 |
Azine-substituted phenylacetic acid derivatives and fungicides containing these
Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro, Y is an amino, methylamino or dimethylamino group, Z is a group CHCH 3 ,...
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5541163 |
Renin inhibiting N-(2-amino-2-oxoethyl)butanediamide derivatives
Disclosed herein are compounds of the formula: A--N(R 1 )C(O)CH 2 CHR 2 C(O)--B wherein A is R 3 R 4 NC(O)CH 2 wherein, for example, R 3 is hydrogen or alkyl and R 4 is hydrogen, alkyl or...
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5541209 |
Method of treating or preventing cardiac arrhythmia employing an N-substituted heterocyclic derivative
The invention relates to the use of an N-substituted heterocyclic derivative and its pharmaceutically acceptable salts for the treatment or prevention of cardiac arrhythmia. These derivatives have...
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5541229 |
Benzimidazoles and medicaments containing these compounds
The invention relates to benzimidazoles of the formula ##STR1## in which R 1 to R 2 are as defined in claim 1, 1 and 3 isomer mixtures thereof and addition salts thereof which have valuable...
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5538987 |
Imidazole ethers having a II antagonist activity
Compounds of general formula (I) ##STR1## wherein E is O or S; R is C 1 -C 5 straight, branched or cyclic alkyl or C 2 -C 5 alkenyl; X can be H, F, Cl, Br, I, CF 3 ; n is an integer 1 to 4; m...
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5534534 |
Pharmaceutical compositions for oral use and method of preparing them
A pharmaceutical composition for oral use comprising an effective amount of a compound of the formula (I) having antagonistic action to angiotensin II ##STR1## (wherein the ring W is an optionally...
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5530016 |
Substituted 2,4-imidazolidinediones
Novel substituted 2,4-imidazolidinediones are prepared either by reaction of α-aminocarboxylic acid derivatives with appropriately substituted biphenylmethyl halides and subsequent cyclization...
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5527815 |
Carboxymethylidenecycloheptimidazole derivatives, method of manufacturing the same and therapeutic agents containing these compounds
New therapeutic agent of carboxymethylidenecycloheptimidazole derivatives and method for the manufacture thereof are disclosed, which are represented by the following formula or its alkali addition...
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5523312 |
Antipicornaviral agents
Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1##...
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5521177 |
Benzimidazoles, pharmaceutical compositions containing these compounds and processes for preparing them
The invention relates to benzimidazoles of general formula ##STR1## Exemplary compounds are: (a) 4'-[[2-Ethyl-4-methyl-6-[(2-dimethylamino-3,4-dioxo-1-cyclob
uten-1-yl)amin...
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5519043 |
Fluorenyl derivatives
The compound having the formula: ##STR1## and a method of treating an inflammatory condition comprising administering to an animal in need of such treatment an effective amount of at least one...
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5510362 |
Imidazole, triazole and tetrazole derivatives
A class of substituted imidazole, triazole and tetrazole derivatives of formula (I), wherein the broken circle represents two non-adjacent double bonds in any position in the five-membered ring;...
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5508297 |
Vascular hypertrophy suppression treatment
This invention relates to a method for the prophylaxis or treatment of vascular hypertropy in a mammal by administering a pharmaceutically effective amount of a compound represented by the formula...
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5506243 |
Sulfonamide derivatives
Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as...
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5504099 |
Injection solutions of azosemide which are ready for injection
Aqueous injection solution that is ready-for-injection of a water-soluble, physiologically well-tolerated azosemide salt of an organic amide, which contains an organic solvent and if desired, a...
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5494926 |
2/3-(heterocyclic alkyl amino)-1-(subst.-phenyl-methoxy)-ethanes/propanes as tachykinin-receptor antagonists
Compounds of formula (I), and salts and prodrugs thereof, wherein Q represents phenyl or benzhydryl; X and Y each represent H or X and Y together form a group =0; Z is O, S or NR 8 (R 8 is H or C...
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5492904 |
Composition of angiotensin-II receptor antagonists and calcium channel blockers
Novel pharmaceutical compositions containing a combination of an angiotensin-II antagonist and a calcium channel blocker such as 2-butyl-4...
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5482957 |
Azole derivatives, process for their preparation and their use
Azole derivatives, process for their preparation, and their use Azole derivatives of the formula (I) ##STR1## in which A, L, O, R 1 , X, Y, Z and q have the meanings given, process for their...
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5478857 |
Use of PLA.sub.2 inhibitors as treatment for alzheimer's disease
This invention provides methods for the treatment or prevention of Alzheimer's disease in a mammal which comprises administering to a mammal in need thereof an effective amount of an inhibitor of...
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5472973 |
Fluorenyl derivatives as anti-inflammatory agents
The compound having the formula: ##STR1## and a method of treating an inflammatory condition comprising administering to an animal in need of such treatment an effective amount of at least one...
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