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5686455 |
Imidazole derivatives and their use as cytokine inhibitors
As cytokine inhibitors 2,4,5-triarylimidazole compounds and compositions for use as cytokine inhibitors.
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5684028 |
Sulphorous derivatives of imidazole, their preparation process, the new intermediates obtained, their use as medicaments and the pharmaceutical compositions
Novel compounds of the formula ##STR1## wherein the, substituents are defined as in the specification and their non-toxic, pharmaceutically acceptable salts which inhibit the effects of angiotensin...
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5681838 |
Substituted amino compounds, their preparation and their use as inhibitors of thrombocyte-aggregation
The present invention relates to novel substituted amino compounds of the formula I: R 1 -(A) a -(B) b -(D) c -(CH 2 ) m -N(R 2 )-(CH 2 ) n -R 3 as defined in the present application, and...
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5681843 |
Parabanic acid derivatives
Parabanic acid derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component are useful pharmaceuticals for the treatment of...
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5674858 |
Medicaments for treating gastrointestinal disorders
The use is described of both (i) ranitidine bismuth citrate and (ii) one or more Helicobacter pylori-inhibiting antibiotics in treating or preventing gastrointestinal disorders. Pharmaceutical...
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5668130 |
Medicament for treating gastrointestinal disorders
The use is described of both (i) ranitidine bismuth citrate and (ii) one or more Helicobacter pylori-inhibiting antibiotics in treating or preventing gastrointestinal disorders. Pharmaceutical...
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5663053 |
Inhibition of inflammatory lipid mediators
Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme...
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5656651 |
Androgenic directed compositions
Substituted phenylthiohydantoins are provided for use in detecting the presence of tumor cells having androgenic receptors and providing for cytostatic and cytotoxic activity toward such cells. The...
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5652255 |
Potentiation of bioreductive agents
A human or animal subject having a solid tumour is treated by administering to the subject therapeutically effective amounts of a nitric oxide (NO) synthase inhibitor and a compound which is an...
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5650428 |
Arylsulfonamide derivative and pharmaceutical compositions and use thereof
An arylsulfonamide derivative of the formula (I): ##STR1## wherein R 1 is unsubstituted phenyl or naphthyl, or phenyl substituted by 1 to 3 same or different substituents selected from the group...
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5648373 |
CoA-IT and PAF inhibitors
Coenzyme A-independent transacylase is required for the release of free arachidonic acid, and the production of arachidonic acid metabolites and platelet activation factor. Blocking of this enzyme...
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5635522 |
Immunosuppressive agents
A suppression of the human immune system is accomplished by administering to the person an effective amount of a non-toxic thioheterocycle compound having the formula ##STR1## wherein R1 is a...
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5633237 |
Imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds for treatment of neurotoxic injury
A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac...
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5627200 |
β.sub.3 -Adrenoceptor agonists and antagonists for the treatment of intestinal motility disorders, depression, prostate disease and dyslipidemia
This invention relates to methods for treating intestinal motility disorders, intestinal ulcerations, including inflammatory bowel disease, ulcerative colitis, Crohn's disease and proctitis, and...
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5624947 |
Phenyl derivatives useful as tachykinin antagonists
Compounds of formula (I), or a salt or prodrug thereof are tachykinin antagonists.
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5620999 |
Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation
A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R 1 is...
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5618564 |
Composition for the treatment of helicobacter pylori infection
The present invention is directed to a method for the treatment of Helicobacter pylori infection wherein a composition containing protease and an antibacterial agent as active ingredients, which...
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5616600 |
Griseolic acid compounds and their use as a phosphodiesterase inhibitor
A compound of the formula (I) is provided ##STR1## wherein A represents a group of the formula: ##STR2## R 1 and R 2 are independently hydrogen, halogen or a group of the formula --OR 9 ; R 9 ...
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5616601 |
1,2-aryl and heteroaryl substituted imidazolyl compounds for the treatment of inflammation
A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R 1 -R...
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5614519 |
(1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-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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5614545 |
Topical composition for treatment of blepharitis
A pharmaceutical composition for treating blepharitis or blepharoconjunctivitis is disclosed for topical administration comprising a nitroimidazole, as metronidazole, in a suitable ophthalmic...
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5612365 |
Angiotensin II receptor antagonists for the treatment and prophylaxis of coronary heart disease
Angiotensin II receptor antagonists for the treatment and prophylaxis of coronary heart disease. Antagonists for angiotensin II receptors of the AT 1 subtype can be employed for the prophylaxis...
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5607953 |
Butenoic or propenoic acid derivative
A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are...
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5604246 |
2-aminoalkyl-5-aminoalkylamino substituted-isoquinoindazole-6(2H)-ones
This invention is directed to 2-aminoalkyl-5-aminoalkylamino substituted isoquino[8,7,6-cd]indazole-6-(2H)-ones and to 2-aminoalkyl-5-aminoalkylamino...
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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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5602156 |
Method for inhibiting metalloproteinase expression
Calcium homeostasis is an important regulator of MMP-2 transcription, activation and activity. Disclosed herein are compounds which inhibit the expression of matrix metalloproteinases in cells....
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5599795 |
Method for treatment of idiopathic inflammatory bowel disease (IIBD)
A new method for the prevention and treatment of Idiopathic inflammatory Bowel Disease (IIBD), including Crohn's Disease and Ulcerative Colitis, in human patients is provided. The key steps include...
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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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5594003 |
Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biph enyls 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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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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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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5563159 |
Dithiocarbonimide derivatives useful as acaricidal, fungicidal, and insecticidal agents
There is disclosed a dithiocarbonimide derivative of the formula: ##STR1## wherein B is a C 1 -C 6 alkyl group; X is an NH group or an oxygen atom and Y is a nitrogen atom or a CH group, A is a...
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5552427 |
Glutaminase inhibitory compounds, compositions, and methods of use
There is disclosed a pharmaceutical composition for inhibiting glutaminase which comprises a imidazole derivative or a salt thereof. This compound selectively inhibits the proliferation of tumor...
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5550145 |
Potentiation of antimicrobial effects
An antimicrobial composition comprising an antimicrobially effective amount of a combination of: A) a monoglyceride of lauric acid, a monoglyceride of monomyristic acid or a mixture of these...
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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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5538988 |
Benzocycloalkylazolethione derivatives
The present invention relates to novel benzocycloalkylazolethione compounds which are dopamine β-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from...
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5536749 |
Method for attenuation of sympathetic nervous system activity or onset of migraine by selectively metabolized beta-blocking agents
Disclosed is a method for attenuating sympathetic nervous system hyperactivity or onset of migraine in a patient in need of such treatment, by the sublingual, buccal or intranasal administration to...
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5523317 |
Method of reducing blood pressure
Disclosed is a method of reducing blood pressure which comprises administering to a patient an imidazole derivative of the formula: ##STR1## wherein: each of R 1 and R 2 is hydrogen, substituted...
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5514698 |
Antifungal vaginal cream composition
A long-lasting antifungal vaginal cream composition having stable viscosity at human body temperature is disclosed.
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5510344 |
Acrylate fungicides
Compounds of formula I ##STR1## wherein X is oxygen or sulphur, W is CH or N, m is 0 or 1, and either a) n is 1 and Q is a non-aromatic heterocyclic ring of 3 to 10 ring atoms, containing one to...
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5506263 |
Benzyl derivatives and pesticides containing them
Benzyl derivatives of the formula I ##STR1## where A is CH 2 , CHCl, CH-alkyl, CH-alkoxy, CH-alkylthio or N-alkoxy, B is OH, alkylthio, alkoxy or alkylamino, U, V, W are hydrogen, halogen,...
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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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5494934 |
Guanidine compounds
A compound of formula (I): ##STR1## in which: R 1 represents substituted or unsubstituted phenyl or (C 3 -C 7 ) cycloalkyl, R 2 represents trifluoromethyl or (C 3 -C 4 ) cycloalkyl, A...
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5482954 |
Signal transduction inhibitor triazole and diazole compounds
A discovery underlying this invention is the concordance between particular cellular signaling mechanisms and cancer cell growth and metastasis. It has now been discovered that certain compounds...
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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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5476669 |
Method for treatment of gastro intestinal disorders
A method is disclosed for preventing the recurrence of duodenal ulcer associated with Campylobacter pylori (Helicobacter pylori) infection in a patient suffering from duodenal ulcer disease...
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5472956 |
Phosphoramidates useful as antitumor agents
Cyclophosphamide analogs are provided of the general formula: ##STR1## wherein R 1 and R 2 are each (C 2 -C 6 )alkyl, substituted with a leaving group such as halo or alkylsulfonyl, R 3 and R 4...
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5464857 |
2-phenyl-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide derivatives and their use as therapeutic agents for maintaining blood pressure
(1) The imidazoline derivative represented by the following general formula (1) ##STR1## where R 1 is a substituent endowed with water solubility or fat solubility, particularly carboxyl group or...
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5462946 |
Nitroxides as protectors against oxidative stress
The instant invention is directed to the use of a biologically compatible composition, containing an effective amount of a metal independent nitroxide compound which is preferably represented by...
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5446065 |
Sulfonamides of phenylalkylamines or phenoxyalkylamines processes for their preparation and medicaments containing these compounds
Compounds of the formula I ##STR1## in which R 1 signifies an aryl, aralkyl or an aralkenyl group, the aryl radical of which can, in each case, be substituted one or more times by halogen, cyano,...
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