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5500230 |
Method for treatment of glaucoma with nitrogen containing guanylate cyclase activators
The present invention relates to a method of treating cranial fluid volume dysfunctions such as glaucoma in an individual, comprising administering compounds which effect an increase in cyclic GMP...
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5482936 |
Imidazo[4,5-C]quinoline amines
Compounds and pharmaceutically acceptable salts thereof formally derived by bridging the 1- and 2-positions of 1H-imidazo[4,5-c]quinolin-4-amines. Also, methods of using such compounds and...
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5478825 |
5-(substituted amino)-1,2,4-triazolo (1,5-A) pyrimidine derivatives
The disclosed compounds have the formula ##STR1## wherein Q is a 6-membered saturated heterocyclic group or a group S(O)pR 3 , wherein p is 0, 1, or 2, and R 3 is alkyl, alkenyl, or phenyl-,...
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5441955 |
Indolo[2,1-biquinazoline-6,12-dione antibacterial compounds and methods of use thereof
Methods, compounds and compositions are provided form inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic mycobacterial infections in vivo using...
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5420129 |
Phenylsulfonylamide pyrimidine
The invention is concerned with novel sulphonamides and their use as medicaments. In particular, the invention is concerned with compounds of the formula ##STR1## wherein R 1 is hydrogen,...
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5418252 |
Method for inhibiting cartilage degradation
A method of inhibiting cartilage degradation comprising administering to a human or other mammal in need of treatment an effective amount of a compound having the formula ##STR1## wherein R 1 and...
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5393755 |
Polycyclic guanine derivatives
Novel polycylic guanine derivatives of the formula: ##STR1## wherein J is oxygen or sulfur, R 1 is hydrogen, alkyl or alkyl substituted with aryl or hydroxy; R 2 is hydrogen, aryl, heteroaryl,...
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5368864 |
Formulation of oxypurinol and/or its alkali and alkaline earth salts
Formulations of oxypurinol and/or its alkali or alkaline earth salts in non-crystalline form, containing the active substance in the form of a solids dispersion with pharmacologically harmless...
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5302589 |
Heterocyclic inhibitors of 5-α-testosterone reductase
The present invention relates to certain substituted 17 β-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R 1 and R 2 are i) independently hydrogen or lower...
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5292741 |
Macrocycles incorporating quinazolinones
Macrocyclic compounds of general Structure I: ##STR1## Wherein M is C or N are angiotensin II receptor (A-II) antagonists useful in the treatment of certain cardiovascular dysfunctions and ocular...
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5284854 |
2-aminopyrimidinone derivatives
2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and anti-histaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects...
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5268375 |
Dinitrogen heterocyclic derivatives N-substituted by a biphenylmethyl group, and the pharmaceutical compositions in which they are present
This invention relates to compounds of formula ##STR1## in which: R 1 and R 2 are similar or different and are each independently hydrogen or a group selected from CO 2 NC(NH 2 ) 2 ,...
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5260298 |
Imidazatriazoloquinazoline compounds and their use
Imidazotriazoloquinazoline compounds having the general formula ##STR1## wherein A together with the α-marked carbon atom and the β-marked nitrogen atom is one of the groups ##STR2## cyano or CO...
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5232915 |
9α-hydroxy-19,11β-bridged steroids, their production and pharmaceutical preparations containing these steroids
9α-Hydroxy-19,11β-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R 1 , R 2 , G, Z, R 4 --Y and R 4 ' --Y' follows from the description. The...
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5227387 |
Quinoline nematicidal method
A method of inhibiting a nematode population which comprises applying to the locus of a nematode, a nematode inactivating amount of a compound of the formula (1): Het--X--CH 2 --CH 2 --Ar ...
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5214047 |
Tetracyclic quinazoline derivatives, effective as antiarrythmic agents
A tetracyclic quinazoline derivative of the formula I: ##STR1## wherein A is C 2 -3 -alkylene or C 2 -3 -alkylene which is substituted by one or two C 1 -4 -alkyl radicals or A is cyclohexylene; X...
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5188833 |
Freeze-dried pharmaceutical preparations for parenteral use
Freeze-dried pharmaceutical preparation containing antibacterial quinolinecarboxylic acid derivatives are provided. These preparations are characterized by their stability against light and heat...
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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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5137888 |
N,N- substituted amines and use thereof in hair growth promotion
Novel compounds are provided having the general formula RB n wherein R is a multi-functional amine moiety having at least n amine-functional nitrogen sites, n equals 2 to about 8, and B are...
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5126339 |
Anti-allergic bicyclic heterocyclyl-containing N-(bicyclic heterocyclyl)-4-piperidinamines
Bicyclic heterocyclyl containing N-(bicyclic heterocyclyl)-4-piperidinamines having antihistaminic and serotonin-antagonistic properties which compounds are useful agents in the treatment of...
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5100895 |
Heterocyclic compounds and their preparation and use
New imidazoquinazoline compounds having the general formula ##STR1## wherein A together with the α-marked carbon atom and the β-marked nitrogen atom is one of the groups ##STR2## wherein R 4 , R...
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5084457 |
Benzoylaminoquinazolinones
This invention is compounds of the formula: ##STR1## and a method of treating cognitive and related neuronal behavioral problems in mammals using the compounds.
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5077288 |
4-fluorobenzoic compounds with 5-HT.sub.2 - and α.sub.1 -antagonistic activities
The invention relates to the compounds of general formula I: ##STR1## in which: m represents an integer from 2 to 4, n and p, which may be identical or different, each represent an integer from...
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5070086 |
Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds
Imidazo- and pyrimido-quinoline, naphthyridine and pyridopyrazine compounds, methods of making said compounds and their use as anti-allergy, antiinflammatory and/or agents for the treatment of...
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5008279 |
Circulation-active fluoromethoxyphenyl dihydropyridine compounds
Circulation-active fluoromethoxyphenyldihydropyridines of the formula ##STR1## in which X stands for hydrogen or fluorine and R stands for straight-chain, branched or cyclic alkyl or alkenyl...
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4925846 |
2-thiazolyl-imidazo[1,2,-a]pyrimidines
A compound selected from the group consisting of a compound of the formula ##STR1## wherein R 1 is thiazol-2-yl optionally substituted by 1 or 2 alkyl of 1 to 3 carbon atoms optionally substituted...
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4873247 |
Derivatives of paraherquamide isolated from a fermentation broth active as antiparasitic agents
Paraherquamide is a fungal metabolite isolated from the known fungus Penicillium paraherquei, and from a newly isolated strain of the fungus Penicillium charlesii. Additional compounds are...
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4831013 |
2-substituted-e-fused-[1,2,4]triazolo[1,5-c]pyrimidines, pharmaceutical compositions, and uses thereof
Compounds of the formula ##STR1## wherein R 1 is optionally substituted phenyl, pyridyl, thienyl, furyl, pyrrolyl, thiazolyl, or ribofuranosyl; X is oxygen, NR, or sulfur; R is hydrogen, lower...
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4824849 |
α.sub.2 -adrenoceptor antagonistic arylquinolizines
Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective α 2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives,...
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4814335 |
Antiviral compounds
In one aspect, compounds having antiviral activity and having the general formula: ##STR1## wherein each R 2 , independently, is H or lower (fewer than 6 carbon atoms) alkyl; each R 3 ,...
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4806525 |
Formulation comprising gelatin and glycine for treating the dryness of skin
A formulation comprised of soft gelatin and glycine in a proportion of about 3:1 to 2:1 by weight, to which can be added mineral oligoelements and vitamins, which, when administered orally, exerts...
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4778511 |
Fluorine-containing N-sulphenylated indazoles for use as bactericides and fungicides
Novel fluorine-containing N-sulfenylated indazoles are prepared by reacting the corresponding indazoles with sulfenyl halides in the presence of a solvent and/or diluent and in the presence of an...
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4772622 |
3,5-diamino-1,2,4-oxidiazoles as gastric secretion inhibitors
Novel diamino oxadiazoles, wherein one of the amine functions is connected to a basicly-substituted heterocyclic group through a linear or cyclic connecting group, which are useful for the...
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4760065 |
Trifluoromethyl substituted tetracyclic quinazolin-ones having tranquilizing activity
Trifluoromethyl substituted tetracyclic compounds including optical isomers thereof having the formula: ##STR1## wherein n is 1 or 2 and p is 0 or 1, are useful as CNS agents with tranquilizing...
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4757072 |
Carcinostatic agent
A carcinostatic composition useful in inhibiting the growth of colon and/or rectal tumors comprising 8-amino-12-oxo-10, 12-dihydroindolo [1,2-b]-quinazoline of the formula: ##STR1##
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4720496 |
Pyridotriazoloquinazolines and triazolopyridoquinazolines useful as antiallergics
Compounds of the formula ##STR1## wherein (a) R 1 is hydrogen, lower alkyl, lower alkoxy or 8-halo; R 2 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; and R 3 and R 4 ,...
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4710504 |
Anti-depressant spiro hexahydro arylquinolizine derivatives, composition, and method of use therefor
Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective α 2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives,...
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4656034 |
Absorption enhancing agents
The absorption of a scavenger of oxygen free radicals generated at the time of reperfusion or the absorption of an agent preventing the cytotoxic effects on healthy cells in a mammal. e.g....
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4616019 |
Naphthyridine antibacterial compounds
Naphthyridine compounds having the formula: ##STR1## wherein Z is an amine or an aliphatic heterocyclic group, R is a phenyl group or an aromatic heterocyclic group and R 1 is hydrogen or a...
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4578380 |
5H-[1]benzopyrano[2,3-d]pyrimidine derivatives useful for controlling lesions of the gastric and duodenal mucous membranes
The invention relates to 5H-[1]benzopyrano-[2,3-d]pyrimidine derivatives of the general formula I ##STR1## which may be prepared by means of a new chemical process and have a protective effect...
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4510144 |
Methods of imparting immunomodulating activity with dihydrothiazolo purine derivatives
There are prepared compounds of the formulae ##STR1## Where R 1 is H, lower alkyl S--, ##STR2## NH 2 or halogen, R 2 is OH, lower alkyl S--, halogen, NH 2 or SH, R is OH, SH, lower alkyl...
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4489078 |
Diazaheterocyclopurines used as anti-broncho spasmatics and vasodilators
Imidazopyrimidinones and other diazaheterocyclopyrimidinones having an additional fused imidazole or triazole ring have utility as bronchodilators, mediator release inhibitors, phosphodiesterase...
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4472399 |
Indolo[2',3';3,4]pyrido[2,1-b]quinazoline-5-ones, a process for the preparation thereof, and diuretic compositions and methods using them
New Rutecarpine analogs are disclosed having Rutecarpine-like activity, especially diuretic activity. Also a novel process for the preparation of the Rutecarpine analogs is disclosed.
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4451466 |
Use of pyrroloquinazolinediamines as pesticides
Certain 7H-pyrrolo[3,2-f]quinazoline-1,3-diamines are useful as pesticides.
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4412995 |
Pentacyclic phenylpyrazole compounds as anti-inflammatory agents
Compounds of the formula ##STR1## where R is hydrogen, methyl, ethyl, propyl, 2-propenyl or 2-propynyl; and R' is hydrogen or fluoro possess anti-inflammatory activity. The compounds where R is H...
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4390540 |
Imidazoquinazolines having pharmaceutical activity
Imidazoquinazolines of the formula ##STR1## wherein R 1 , R 2 and R 3 are hydrogen, halogen, C 1 -4 -alkyl, C 1 -4 -alkoxy or C 2 -5 -alkoxyalkyl; or two of R 1 , R 2 and R 3 on adjacent carbon...
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4372956 |
5, 10-Dihydroimidazo[2,1-b]quinazolines and pharmaceutical compositions containing them
A 5,10-dihydroimidazo[2,1-b]quinazoline in which at least one ring carbon atom, other than the carbon atom in the 2-position, bears a substituent, or a pharmaceutically acceptable acid addition...
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4367230 |
Novel triazafluoranthene compound and processes for preparing the same
A triazafluoranthene compound of the formula: ##STR1## wherein R 1 is hydrogen, phenyl, cycloalkyl having 3 to 6 carbon atom, (lower alkoxy)carbonyl, lower alkoxy or (lower alkyl)carbonyl, R 2 is...
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4360521 |
7[3,6-Dihydro-1(2H)-p yridyl]-2-oxo-2H-[1,2,4]oxadiazolo[2,3-c]pyrimidine-5-carbamate compounds
Oxadiazolo[2,3-c]pyrimidine derivatives of the formula ##STR1## wherein R is alkyl, alkenyl, alkynyl or alkoxyalkyl, as well as their salts, are described. The compounds of formula I have valuable,...
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4341780 |
Substituted pyrido [1,2-a] pyrimidines useful as anti-allergic, anti-ulcer and anti-diabetic agents
Substituted pyrido [1,2-a] pyrimidines and pharmaceutical compositions containing them, suitable for use as anti-allergy, anti-ulcer, and anti-diabetic agents.
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