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5516784 |
Anti-HIV (AIDS) agents
Compounds of formula ##STR1## wherein Ar, W, Z, Q, R 1 , U, and T are as set forth herein, are described. These compounds are active as agents against retroviruses and in particular against HIV.
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5506227 |
Pyridine-substituted benzyl alcohols as leukotriene antagonists
Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents....
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5506257 |
Aminocyclohexylamides for antiarrhythmic and anaesthetic uses
The present invention provides methods for blocking sodium channels in cardiac or neuronal tissue using aminocyclohexylamides. This invention also provides kits including aminocyclohexylamides and...
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5496844 |
Indole derivatives
The present invention provides indole derivatives of the general formula: ##STR1## The indole derivatives of the invention have potent antiestrogen activity and are useful as drugs for the...
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5489583 |
2-substituted 3-(4-amidinophenyl)propionic acid derivatives
2-Substituted 3-(4-amidinophenyl)propionic acid derivatives of the formula ##STR1## in which A, Ar and B have the meanings stated in the description, and the preparation thereof are described. The...
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5475007 |
1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes and the use thereof
Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease,...
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5468742 |
8-vinyl- and 9-ethinyl-quinolone-carboxylic acids
The invention relates to new 8-vinyl- and 8-ethinylquinolonecarboxylic acids, process for their preparation, and antibacterial agents and feed additives containing them.
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5457104 |
Quinolone- and naphthyridonecarboxylic acid derivatives
The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which have hydrogen in the 6-position, to processes for their preparation, and to antibacterial compositions and...
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5447929 |
Method of treating joint disorders using hydroxamic derivatives
Hydroxamic acid derivatives of the fdrrnula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint...
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5428033 |
Saturated hydroxyalkylquinoline acids as leukotriene antagonists
Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and...
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5428036 |
Sertindole prodrugs, compositions and use
Reaction products of sertindole with an acid or an activated acid, with formaldehyde alone, formaldehyde in the presence of an alcohol or an amine, or with an acyloxymethylene halide, and having...
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5401766 |
Aminoacid derivatives, a process for their preparation, agents containing these compounds, and the use thereof
Aminoacid derivatives of the formula I ##STR1## A , n, R 1 , R 2 and R 3 have the meanings given, and salts thereof, a process for their preparation, pharmaceutical preparations based on these...
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5401740 |
Carbostyril derivative
The novel carbostyril derivative represented by the general formula (1) ##STR1## [in the formula, A, R 1 , R 2 and the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton...
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5399559 |
Fungicidal indole derivatives
The invention relates to fungicidal compositions which comprise a carrier and, as active ingredient, an indole derivative of the formula ##STR1## in which R is a substituted phenyl group; R 3 and...
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5380722 |
Indole carboxamides
Novel indole-carboxamides of the formula ##STR1## and their non-toxic pharmaceutically acceptable acid addition salts having remarkable anti-arrhytmic properties.
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5373008 |
Phenylamidine and phenylguanidine derivatives and their use as anti-diabetic agents
Compounds of formula I ##STR1## and their salts in which n=0 or 1, R 1 and R 2 are each aliphatic or cycloalkyl or NR 1 R 2 is an optionally substituted heterocyclic ring, R 3 is alkyl,...
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5358949 |
Carbostyril derivatives and salts thereof and anti-arrhythmic agents containing the carbostyril derivatives
Carbostyril derivatives or salt thereof, including novel compounds, having activities for curing and/or improving arrhythmia. Some carbostyril derivatives having similar chemical structural formula...
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5356907 |
1-cycloalkylpyridones as analgesics
A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected...
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5354749 |
Sulfonylbenzyl-substituted benzo- and pyridopyridones
Sulfonylbenzyl-substituted benzo- and pyridopyridones are prepared by reacting corresponding benzo- and pyridopyridones with sulphonylbenzyl compounds. The sulphonylbenzyl-substituted benzo- and...
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5350747 |
Heteroaryl piperazine antipsychotic agents
Compounds of the formula ##STR1## and pharmaceutical compositions comprising them, wherein R 1 , Z, X, W and Y are as defined below. The compounds are useful in the treatment of psychosis and anxiety.
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5334589 |
Quinolone carboxylic acid--metal ion--acid complexes
Compositions of a quinolone carboxylic acids useful for oral or parenteral administration to a human or veterinary patient are disclosed which comprise quinolone carboxylic acid--metal ion--acid...
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5330997 |
1H-indazole-3-acetic acids as aldose reductase inhibitors
Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic...
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5326760 |
Aminobutanoic acid compounds having metalloprotease inhibiting properties
Aminobutanoic acids of the following formula (I): ##STR1## where R 1 -R 5 are a variety of substituents, novel intermediates, a pharmaceutical composition for treating inflammatory diseases,...
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5318964 |
Hydroxamic derivatives and pharmaceutical compositions
Hydroxamic acid derivatives of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are collagenase inhibitors useful for the control or prevention of degenerative joint...
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5310744 |
Quinolylmethoxyphenyl-acetamides
Quinolylmethoxyphenyl-acetamides of the formula: ##STR1## in which A, B, D, E, G, L and M are hydrogen, hydroxyl, halogen, cyano, carboxyl, nitro, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy...
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5306719 |
Carbostyril derivatives and salts thereof
Novel carbostyril derivatives and salts thereof having useful pharmacological activities such as myocardial contraction increasing activity (positive inotropic activity), coronary blood flow...
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5304554 |
4-[(alkyl or dialkyl)amino]quinolines and their method of preparation
Novel 4-[(alkyl or dialkyl)amino]quinolines are disclosed that are prepared by condensin BACKGROUND OF THE INVENTION The United States government has rights in this invention as a result of a...
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5296499 |
Indole derivatives, their production and use
An agent for inhibiting bone resorption comprising an indole derivative of the formula (I): ##STR1## wherein each ring of A and B is optionally substituted, R is a hydrogen atom, a lower alkyl...
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5296478 |
1-substituted oxindoles as cognition enhancers
Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetlcholine, and thus may be useful as chemical intermediates and as pharmacological agents in the treatment...
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5292736 |
Morpholinoalkylindenes as antiglaucoma agents
Compounds of the formula ##STR1## wherein Alk is lower-alkylene; R 1 is hydrogen, lower-alkyl, Ar or ArCOO; R 2 is hydrogen or lower-alkyl; R 3 and R 4 are the same or different...
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5270309 |
Kynurenic acid derivatives useful in the treatment of neurodegenerative disorders
4-Oxo-1,4-dihydroquinoline compounds having a 2-acidic group or a group convertible thereto in vivo, and their pharmaceutically acceptable salts, are potent specific antagonists of...
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5270331 |
Prodrugs of antiinflammatory 3-acyl-2-oxindole-1-carboxamides
Antiinflammatory and analgesic oxindole prodrugs of the formula ##STR1## wherein R 10 , R 11 , R 12 and R 13 are hydrogen, alkyl or halogen and R is methyleneoxyalkanoyl, methyleneoxyalkenoyl or...
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5268378 |
Dioxo-tetrahydroquinoline derivatives
A class of 2,4-dioxo-1,2,3,4-tetrahydroquinoline derivatives, substituted at the 3-position by a range of carbonyl-containing substituents or by a five- or six-membered heteroaromatic moiety, are...
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5266568 |
Hydroxyalkylquinoline ether acids as leukotriene antagonists
Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and...
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5256657 |
Succinamide derivative matrix-metalloprotease inhibitors
Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH 2 R 1 has the R-configuration, the carbon atom bearing CH 2 R 2 has...
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5254566 |
Decahydroquinoline compounds
A compound selected from the group consisting of racemates, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein R 1 and R 2 are individually selected from the...
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5250533 |
Fungicidal pyridinylpyrimidines
Fungicidal pyridinylpyrimidines of the formula ##STR1## in which R 1 represents hydrogen, halogen, alkoxy, alkylthio, halogenoalkyl, amino or dialkylamino, where, in the case of dialkylamino, the...
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5242939 |
Anilide derivatives with angiotensin II antagonist properties
This invention relates to anilide derivatives of Formula I ##STR1## which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of hypertension, heart...
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5225413 |
pH-neutral aqueous solutions of quinolone-carboxylic acids
A pH-neutral aqueous solution of a quinolonecarboxylic acid of the formula ##STR1## in which R 1 represents halogen, C 1 -4 -alkyl or C 2 -4 -alkenyl, R 2 and R 3 represent hydrogen, C 1 -4...
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5223505 |
Pyrimidine derivatives
This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R 1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R 2 and R 6 is a...
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5189054 |
3-amidoindolyl derivatives and pharmaceutical compositions thereof
The present invention is directed to a new class of 3-amido and 3-sulfamido-indolyl NMDA antagonists and their use in the treatment of a number of disease states.
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5182282 |
4-Benzyl-1H-indole derivatives
Novel 4-benzyl-1H-indoles of the formula ##STR1## in all diastereoisomeric forms and mixtures thereof having anti-arhythmic activity.
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5182275 |
Dihydro-4(hydroxyalkyeneamino)quinolines
There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R 1 is hydrogen or loweralkyl; R 2 is...
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5179093 |
Quinoline-diones
Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C 1 -C 6 ) alkyl, N(C 1 -C 6 alkyl/aryl) 2 , OH, O--(C 1 -C 6 ) alkyl/aryl, CH 2 OH,...
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5179089 |
Isoquinoline compounds, compositions and use
The invention relates to novel compounds of the general formula (I), ##STR1## wherein R means hydrogen or a straight or branched chain C 1 -6 alkoxy group; R 1 stands for hydrogen or a straight...
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5177088 |
Substituted 3-(pyridinylamino)-indoles
There are disclosed various compounds of the formula below, ##STR1## where R 1 , W, X, Y and Z are as defined in the specification; which are useful for alleviating various memory dysfunctions such...
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5175002 |
Amantadine hydrochloride syspension with enhanced dissolution characteristics for use in soft gelatin capsules
There are provided, novel no or low wax formulations for amantadine hydrochloride and methods for preparing such formulations.
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5158959 |
Decahydroisoquinoline carboxylic acids
What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds;...
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5149702 |
Cycloheptenopyridine derivatives, process for preparation thereof and antiulcer agents containing the same
Provided are cycloheptenopyridine derivatives represented by the general formula ##STR1## [wherein R represents a hydrogen atom or lower alkyl group; R 1 represents a hydrogen atom, halogen atom,...
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5124327 |
HIV reverse transcriptase
Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds or pharmaceutical...
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