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5707988 |
Benzo d! isoxazole derivatives, compositions containing them and their use in therapy
Compounds of formula (I) ##STR1## in which X represents a group >O, >S, >CO or >NR wherein R is hydrogen, C 1 -6 alkyl, phenyl or C 7 -12 phenalkyl, R 1 and R 2 each represent...
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5688791 |
Aryl group-or aromatic heterocyclic group-substituted aminoquinolone derivatives and anti-hiv agent
Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the...
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5686095 |
Method of treating canker sores
A method of treating canker sores is disclosed by which a fluoroquinolone is topically applied to the ulcerous area. The fluoroquinolone is shown to be applied in solution form, and also as a...
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5672599 |
Compounds containing a fused bicycle ring
Compounds of the formula ##STR1## wherein X is O or S--(O) t ; n is one; m is zero or one; Y is CH 2 , O, or S--(O) t provided that Y is O or S--(O) t only when m is one; and A is ##STR2## are...
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5672600 |
Antimicrobial dithiocarbamoyl quinolones
Antimicrobial dithiocarbamoyl quinolone compounds of the general formula: ##STR1## wherein (1) A 1 , A 2 , A 3 , R 1 , R 3 , R 4 , and R 6 form any of a variety of quinolone and related...
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5622950 |
Pyrrolo-pyridine derivatives
A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a...
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5610158 |
4-oxo- and 4H-imidazo(5,1-c)(1,4)benzoxazines useful as benzodiazepine receptor-binding agents
Imidazo-benzoxazines of Formula (I) and pharmaceutically acceptable salts thereof. ##STR1## where Q is selected from (A) through (H) ##STR2## or pharmaceutically acceptable salts thereof wherein...
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5589476 |
Imidazol-4-ylpiperidine derivatives, their preparation and their application in therapeutics
A compound of formula (I): ##STR1## in which R 1 represents a hydrogen atom or a straight or branched (C 1 -C 4 )alkyl group; and A represents a 5,6-dihydro-4H-imidazo[4,5,1-ij]quinol-2-yl...
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5512566 |
Tricyclic compounds having affinity for the 5-HT1A receptor
Compounds represented by the general formula I: ##STR1## are disclosed as useful in treating diseases of the central nervous system.
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5494909 |
Substituted oxazinoisoquinoline derivatives, pharmaceutical compositions containing them and process for preparing same
New compounds with the ability to inhibit calcium uptake in the brains of mammals are disclosed of the Formula (I) ##STR1## wherein R 1 is hydrogen, C 1 to C 4 alkyl, phenyl, or phenyl-C 1 to C...
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5474988 |
5-phenylpyrrolo-1,4-benzoxazine and 5-phenylpyrrolo-1,4-benzothiazine compounds, process and intermediates for their production and pharmaceutical compositions containing them
Pharmacologically active compounds of formula I ##STR1## which can be substituted in the phenyl rings and in which R 1 denotes hydrogen or lower alkyl, R 2 denotes hydrogen or lower alkyl, ...
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5462938 |
Arthropodicidal oxadiazinyl, thiadiazinyl and triazinyl carboxanilides
Arthropodicidal carboxanilides of Formula I and II ##STR1## wherein Q is selected from the group ##STR2## A, E, G, X, X 1 , Y, Z, Z 1 , R 2 , R 3 , R 4 , R 5 , R 6 and n are as defined in the...
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5436240 |
Heterocyclic amines having central nervous system activity
Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R 1 , R 2 , and R...
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5416096 |
7-(1-pyrrolidinyl)-3-quinolone carboxylic acid derivatives as antibacterial agents and feed additives
7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X 1 is halogen, X 2 is hydrogen,...
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5409924 |
Benzo-fused oxazobicyclo terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
Compounds characterized generally as benzo-fused oxazobicyclo-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension....
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5401741 |
Topical preparation for treating otopathy
A topical preparation for treating otophathy which contains ofloxacin or a salt thereof as an active ingredient is disclosed.
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5380718 |
Arthropodicidal fused tetrahydropyridazines
Arthropodicidal tetrahydropyridazines of Formulae I and II, ##STR1## wherein Q,X,X 1 Y, and G are as defined in the text, compositions containing them and their use in the control of arthropods.
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5364854 |
Derivatives of substituted imidazo benzoxazin-1-one and process for their preparation
Derivatives of 2,3,3a,4-tetrahydro-2-azabicyclo alkyl-1H-imidazo[5,1,-c][1,4]benzoxazin-1-one are provided of general formula (I) ##STR1## in which inter alia R 3 represents ##STR2## wherein n is...
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5308843 |
Method of inhibiting mammalian topoisomerase II and malignant cell growth in mammals, with substituted (S)-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4 ]-benzoxazine(and-benzothiazine)-6-carboxylic acids
A method of inhibiting mammalian topoisomerase II and inhibiting the growth and inducing the regression of malignant cells in mammals by the action of a...
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5276039 |
Substituted indazole arthropodicides
Indazole arthropodicides, compositions containing them and a method for controlling arthropods employing these indazoles as the active ingredient. The indazoles have the following general formula...
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5175160 |
Antimicrobial agent for animals
An antimicrobial agent for animals is disclosed. The agent comprises as an effective component a racemate of a 3S-type compound of a pyrido[1,2,3-de][1,4]benzoxazine derivative represented by the...
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5164400 |
Pyrroloquinoline compounds
The invention relates to a compound of the formula: ##STR1## in which R 1 and R 2 are each hydrogen or lower alkyl, R 3 is aryl or unsaturated, 5- or 6-membered heterocyclic group containing...
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5153203 |
Quinolone derivatives and salts thereof, preparation processes thereof, and antibacterial agents containing the same
Antibacterial quinolone derivatives represented by the following formula and salts thereof are disclosed. ##STR1## wherein R 1 meawns a substituted or unsubstituted lower alkyl group, a...
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5147873 |
Amino-substituted bridged azabicyclic quinolone carboxylic acids and esters
Compounds of the formula ##STR1## wherein R 1 is hydrogen, C 1 -C 6 alkyl, or a pharmaceutically acceptable cation; Y is cyclopropyl, ethyl or p-fluorophenyl, and X is hydrogen or fluoro, or...
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5112820 |
Anti-glaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-(1,2,3-de)-1,4-benzoxazines and method of use thereof
Antiglaucoma compositions containing 2- and 3-aminomethyl-6-arylcarbonyl- or 6-phenylthio-2,3-dihydropyrrolo-[1,2,3-de]-1,4-benzoxazines as the active component thereof and the method of use...
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5104868 |
Tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and esters
This invention relates to novel tricyclic derivatives of 7-substituted-6-fluoro-1,4-dihydroquinol-4-one-3-carboxylic acids and certain esters and cation salts thereof. The compounds of this...
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5059597 |
7-(4-oxa or 4-thia-2,7-diazabicyclo[3.3.0]oct-2-en-3-yl)-3-quinolone-and-naphthyrido ne-carboxylic acid derivatives as antibacterial agents and feed additives
7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridone-carboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X 1 is halogen, X 2 is hydrogen,...
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5053407 |
Optically active pyridobenzoxazine derivatives and anti-microbial use
An optically action pyridobenzoxazine derivative, a process for preparing the same and a novel intermediate useful for preparing the optically active pyridobenzoxazine derivative are disclosed. The...
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5023257 |
Intramuscular injection forms of gyrase inhibitors
Ciprofloxacin and related gyrase inhibitors are tolerated well if administered intramuscularly in the form of an aqueous suspension of the betaine form having an approximate neutral pH value or in...
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5001129 |
Oxazoloquinoline compounds and therapeutic application thereof
The present invention relates to tricyclic carbamates coplying with the formula ##STR1## in which n=0, 1 or 2, p=0 or 1, R 1 represents a hydrogen atom; a group which is alkyl in C 1 -C 4 ...
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4990508 |
Pyridone carboxylic acid derivatives and salts thereof, process for producing the same and antibacterial agents comprising the same
This invention relates to a novel pyridone carboxylic acid derivative having a substituted or unsubstituted cyclopropyl group at the 10-position of pyridobenzoxazine, pyridobenzothiazine or...
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4990517 |
7-(1-pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives
7-(1-Pyrrolidinyl)-3-quinolone- and -naphthyridonecarboxylic acid derivatives as antibacterial agents and feed additives, of the formula ##STR1## in which X 1 is halogen, X 2 is hydrogen,...
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4988709 |
Quinolone-carboxylic acids as antibacterial agents
Novel pyridonecarboxylic acids of the formula: ##STR1## or the pharmaceutically acceptable salts thereof having a more potent and longer lasting antibacterial activities against gram-positive and...
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4980287 |
4H-3,1-benzoxazin-4-one compounds and pharmaceutical compositions thereof for the inhibition of serine proteases
A 4H-3,1-benzoxazin-4-one compound of the formula (I): ##STR1## wherein R is a hydrogen atom or alkyl radical, A is an amino acid residue or a peptide having 2 to 3 amino acid residues, which amino...
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4980358 |
Method employing gonadal hormones and dopamine agonist intended for combined use in the improvement of lymphocyte function
A new method, useful as a pharmacologic strategy, contains a gonadal hormone in combination with a dopamine agonist such as bromocriptine, and optionally an ascorbate source. This method has a...
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4978661 |
Use of 6-halo-4-quinolone compounds and pharmaceutical compositions thereof for the preparation of a medicament for the therapeutical application in rheumatoid arthritis
The present invention relates to the use of 6-halo-4-quinolone derivatives and pharmaceutical compositions comprising them as active ingredient, for the preparation of a medicament for the...
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4973590 |
Process for the preparation of quinolonecarboxylic acids which can be administered parenterally
Known quinolone carboxylic acid derivatives of the formula ##STR1## are treated so as to become readily administrable parenterally, the treatment comprising dissolving the active compound using an...
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4965262 |
Method for treating or preventing locally periodontal disease
A method for treating or preventing periodontal disease which comprises administering ofloxacin or salts thereof locally to periodontal tissue are disclosed. The method is excellent on the...
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4923862 |
Topical preparation containing ofloxacin
A topical preparation containing, as an active ingredient, 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihy
dro-7H-pyrido[ 1,2,3][1,4]-benzoxazine-6-carboxylic acid or a salt thereof.
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4839355 |
Tricyclic-pyridinylquinoline compounds, their preparation and use
Fluorinated 10-(2,6-dimethyl-4-pyridinyl)-3-methyl-7-oxo-2,3-dihydro-7H-
pyrido[1,2,3-d e][1,4]benzoxazine-6-carboxylic acids and -benzothiazine-6-carboxylic acids of the formula ##STR1## wherein R...
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4822801 |
4-oxo-1,4-dihydroquinoline-3-carboxylic acid derivative as antibacterial agents
Novel naphthyridine-, quinoline- and benzoxazinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial...
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4816451 |
Antibacterial 1,8-bridged 4-quinolonecarboxylic acids
Antibacterially effective 1,8-bridged 4-quinolone-3-carboxylic acids and derivatives of the formula ##STR1## in which Y represents a carboxyl group, a nitrile group, an ester group --COOR 7 or an...
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4808585 |
Solutions of lactic acid salts of piperazinylquinolone- and piperazinyl-azaquinolone-carboxylic acids
The invention relates to solutions of piperazinylquinolone- and piperazinyl-azaquinolone-carboxylic acids, and in particular both ready-to-use injection and/or infusion solutions and dosage forms...
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4762831 |
Antibacterial 1,8-bridged 4-quinolone-3-carboxylic acids
A process for the preparation of a 1,8-bridged 4-quinolone-3-carboxylic acid of the formula ##STR1## wherein the substituents are defined hereinbelow. Some of the compound are new. The old and new...
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4753953 |
Pyridonecarboxylic acid derivatives and antibacterial pharmaceutical compositions thereof
Pyridonecarboxylic acid derivatives of the following formula, ##STR1## wherein R is hydrogen atom or lower alkyl group, R 1 is lower alkyl group, cycloalkyl group or haloalkyl group, Y is hydrogen...
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4735940 |
Tricyclic pyridine derivatives and pharmaceutical compositions
Compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt of a compound of formula I which has one or more basic substituents, are described. The compounds of formula I...
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4729998 |
Cyclic carbamates and fungicidal use
Fungicidally active cyclic carbamates of the formula ##STR1## in which X and Y each represent oxygen or sulfur, Z represents hydrogen, halogen, alkyl or nitro, and n is 2 or 3. Some...
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4623647 |
[1,3]oxazino[4,3-a]-isoquinoline derivatives and pharmaceutical compositions containing them
The invention relates to new [1,3]oxazino[4,3-a]-isoquinoline derivatives of the formula (I) ##STR1## wherein R 1 and R 2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms, R 3 is...
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4623650 |
Antibiotic derivatives of 7-phenyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids
1-Substituted-6-fluoro-7-aryl-(8-fluoro)-1,4-dihydroquinol-4
-one 3-carboxylic acids having antibacterial activity are prepared by reacting the corresponding alkyl...
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4605653 |
1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives and pharmaceutical compositions containing them
The invention relates to 1-(hydroxymethyl)-1,6,7,11b-tetrahydro-2H,4H-[1,3]oxazino- or -thiazino-[4,3-a]isoquinoline derivatives of the formula (I), ##STR1## wherein R 1 and R 2 are alkoxy having...
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