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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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5488057 |
2-oxindole compounds which have useful tyrosine kinase activity
The present invention provides novel aryl- and heteroarylethenylene derivatives which are useful as tyrosine kinase activity inhibitors.
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5484804 |
Perhydroisoindole derivatives as antagonists of substance P
This invention relates to novel perhydroisoindole derivatives of general formula (I), ##STR1## wherein radicals R are phenyl radicals optionally 2- or 3-substituted by a halogen atom or a methyl...
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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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5472962 |
Benzothiophene derivative
A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial...
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5462934 |
Condensed heterocyclic ketone derivatives and their use
A compound of the formula: ##STR1## wherein R 1 is H or an optionally substituted hydrocarbon or acyl group; ring A is an optionally further substituted benzene ring; n is an integer of 1 to 10; R...
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5459149 |
Penta-2,4-dienamides and use as pesticides
The present Application discloses pesticidally active compounds of formula (I): Q(CH 2 ) a (O) b Q 1 CR 2 =CR 3 CR 4 =CR 5 CXNR 1 R x or a salt or propesticide thereof, wherein Q is an...
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5446043 |
Isoquinolyl, quinoxalinyl and quinazolinyl derivatives as inhibitors of 5-lipoxygenase
The invention concerns a heterocyclic cycloalkane of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one...
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5446051 |
Aryl-spaced decahydroisoquinoline-3-carboxylic acids as excitatory amino acid receptor antagonists
The present invention provides novel decahydroisoquinoline derivatives which are useful as excitatory amino acid antagonists. The invention also provides for methods of using these derivatives to...
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5446071 |
Methods for lowering serum cholesterol
The present invention provides methods for lowering serum cholesterol comprising administering to a mammal in need of treatment a serum cholesterol lowering amount of a compound of formula I or...
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5444056 |
Aminoalkoxyphenyl derivatives, process for their preparation and compositions containing them
An aminoalkoxyphenyl derivative of general formula: Cy--B--Ph--O--A--Am (1) as well as a pharmaceutically acceptable salt thereof in which B represents a...
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5434162 |
Quinolinyl/isoquinolinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
Compounds characterized as quinolinyl- or isoquinolinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension and are of...
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5424323 |
Sterilant composition
A biocidal, aqueous composition for killing bacteria, spores, fungi, and viruses on nonabsorbent surfaces comprises at least one quaternary ammonium compound, at least one aliphatic dialdehyde...
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5416094 |
Antiarrhythmic and cardioprotective substituted -1(2H)isoquinolines, medicament containing them, and their use for combating heart failures
Described are guanidinocarbonyl isoquinolines of the formula I, ##STR1## wherein R(1) is hydrogen, (amino) (cyclo) (aryl)alk(en)yl (heteroaryl); R(2) is hydrogen, halogen, alkyl, or aryl; G is a...
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5411960 |
Substituted pyrroloanthracenes and -diones
Substituted pyrroloanthracenes are prepared by reacting either furanoanthracenes or N-unsubstituted pyrroloanthracenes with appropriately substituted alkylamines. The compounds can be employed as...
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5409929 |
Hydroisoindolines and hydroisoquinolines as psychotropic drugs
There are provided novel nitrogen-containing bicyclic compounds which are useful in the treatment of physiological or drug induced psychosis or dyskinesia in a mammal. These novel compounds are...
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5409938 |
Antimalarial korupensamines and pharmaceutical compositions and medical uses thereof
The present invention provides new antimalarial compounds called korupensamines, korupensamine derivatives, and pharmacologically acceptable salts thereof, methods for isolating such antimalarial...
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5407946 |
Pyrrolidine compounds which are useful as thromboxane AZ-inhibitors
Components of formula (I): ##STR1## in which: R 1 represents optionally substituted phenylsulfonyl, naphthylsulfonyl, quinolyl, or isoquinolyl, R 2 represents hydrogen, optionally substituted...
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5405845 |
(Pyrrolidinyl)phenyl carbamate derivatives and use
Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and...
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5401752 |
Tetrahydroisoquinoline derivatives, processes for producing the same and fungicides containing the same
Tetrahydroisoquinoline derivatives useful as fungicides are disclosed of formula [I]: ##STR1## wherein R 1 represents C 1 -C 5 linear or branched alkyl, C 2 -C 5 linear or branched alkenyl, C...
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5401751 |
Isoquinoline derivatives suitable for use in leukotriene mediated disease
The invention concerns a heterocycle of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two...
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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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5393764 |
Cyclic phenolic thioethers
The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R 1 and R 2 are the same or different and independently represent...
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5389661 |
Imidazole and 1,2,4-triazole derivatives with angiotensin II antagonist properties
This invention relates to novel substituted imidazole and triazole derivatives which antagonize the binding of angiotensin II to its receptors. The compounds are useful in the treatment of...
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5389638 |
Tetrahydroisoquinolines as alpha-2 antagonists and biogenic amine uptake inhibitors
The present invention provides a tetrahydroisoquinoline compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof which is an antagonist for alpha-2 adrenoreceptors and/or...
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5389644 |
1,4-dihydropyridine compounds
The compounds are 2,4-disubstituted 3-ethoxycarbonyl 5-methoxycarbonyl 6-methyl 1,4-dihydropyridines in their dextrorotatory form, useful to potentiate the activity of cytotoxic agents and to...
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5389649 |
Oxathiane derivatives
Oxathiane derivatives of formula ##STR1## in which R represents alkyl and A represents optionally substituted phenyl or a heteroaromatic group containing 1 or 2 nitrogen atoms optionally...
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5387591 |
Pyrrolidine compounds
Compounds of formula (I): ##STR1## in which: R 1 represents: optionally substituted alkyl, optionally substituted phenyl, pyridyl, optionally substituted phenylsulfonyl, acyl, ...
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5384315 |
Thiophene substituted cycloamines, compositions and use
A class of compounds having the structural formula ##STR1## in which R is C 1 -C 8 alkyl, C 3 -C 6 cycloalkyl, phenyl or substituted phenyl; N, R 1 and R 2 form a monocyclic or bicyclic...
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5384322 |
Nitrogen-containing bicyclic compounds and pharmaceutical compositions thereof
The invention relates to the compounds of formula (I): ##STR1## in which: A represents, with the nitrogen and carbon atoms to which it is bound, a heterocycle, B represents, with the nitrogen...
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5366981 |
N-acyl-substituted azacyclic compounds, processes for their preparaion, and their use as pharmaceuticals
A compound, a solvate or salt thereof, of formula (I): ##STR1## in which: A is ##STR2## p is 2; ROC-- is an acyl group linked to a substituted or unsubstituted carbocyclic aromatic ring system; ...
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5366994 |
Use of a combination of angiotensin-converting enzyme inhibitor and calcium antagonist for the treatment of proteinuria
A combination of angiotensin-converting enzyme inhibitors and calcium antagonists for the treatment of proteinuria is disclosed. The invention relates to the prevention and therapy of proteinuria...
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5362736 |
Isoquinoline derivatives
Novel isoquinoline derivatives represented by formula (I): ##STR1## wherein R 1 , R 2 , R 3 , R 4 , R 5 , X 1 and X 2 are as defined in the specification, have an anti-arrhythmic activity and...
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5356906 |
(N-phthalimidoalkyl) piperidines useful as treatments for psychosis
There is described novel (N-phthalimidoalkyl) piperidine compounds which exhibit selective sigma-receptor antagonism and therefore are useful in the treatment of physiological or drug induced...
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5350762 |
Tetrahydrocyclopent[B]indole methanamines and related compounds
There are disclosed various compounds of the formula below, ##STR1## where the various parameters R 1 , R 2 , R 3 , R 4 , X, m and n are as defined in the specification, which show activities as a...
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5344843 |
Cat-1 inhibitors, pharmaceutical compositions and methods of use
The invention relates to compounds of the formula ##STR1## wherein R 1 , R 2 , R 2 ' X, Y, Z, A, B, Q and n are as described herein. Their pharmaceutically acceptable salts, and when appropriate,...
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5340811 |
Isoquinoline-or quinoline-sulfonamide derivative and a pharmaceutical composition comprising the same
Disclosed is a sulfonamide derivative represented by following formula (I) and a medicine for the treatment of asthma comprising the sulfonamide derivative as an active ingredient which exhibits...
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5340833 |
Urokinase inhibitors
Disclosed are benzothiophene and thienothiophene derivatives useful for inhibiting urokinase activity.
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5330991 |
Tetrahydroisoquinoline compounds and fungicides containing the same
Tetrahydroisoquinoline derivatives of the following formula [I] and acid addition salts thereof, and ##STR1## (wherein in all of these formulae, R 1 represents C 1 -C 5 straight or branched...
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5328906 |
0-(3-amino-2-hydroxypropyl)-hydroximic acid halides and process for preparing the same
Hydroximic acid derivatives of the formula ##STR1## These compounds are useful for treating diabetes angiopathy.
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5322848 |
N-acyl-substituted azacyclic compounds, processes for their preparation, and their use as pharmaceuticals
A compound, or solvate or salt thereof, of formula ##STR1## R 1 is hydrogen, halogen, or C 1 -6 alkyl; R 2 and R 3 are hydrogen or C 1 -6 alkyl; R 5 together with R 4 forms a --(CH) 2 ) 2 ...
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RE34630 |
Substituted isoquinolines and methods of using same
Novel substituted isoquinoline compounds are disclosed together with novel 2-phenylethylamides useful as precursors or intermediates for the production of the isoquinolines. The substituted...
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5310750 |
Heterocyclic compounds useful as α.sub.2 -adrenoceptor antagonists
A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R 1 and R 2 may each represent hydrogen or alkyl providing that at least one of R 1 or R 2 represents...
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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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5298503 |
N-(isoquinolin-5-ylsulphonyl) azacycloalkanes
Compounds of formula (I): ##STR1## wherein R 1 , R 2 , U, X, Y, Z, n, m, p and r are as defined in the description, and medicaments containing the same.
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5296485 |
Substituted N-phenylpiperidines and drugs therefrom
Substituted N-phenylpiperidines I ##STR1## (R 1 =H, NO 2 , CN, halogen, C 1 -C 4 -alkyl, CF 3 , OCF 3 , OH, CH 2 OH, COOH, CHO, NH--CHO, NH 2 , CO--NH 2 , 5-tetrazinyl, R 4 --O--, R 4 --O--CH...
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5292755 |
USPA benzolyguanidines
Benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is equal to R(6)--S(O) n -- or R(7)R(8)N--O 2 S-- and the other substituent R(1) or R(2) is in each case equal to H, F, Cl, Br,...
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5292746 |
Cyclic nitrones, pharmaceutical compositions thereof and their use in treating shock
The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.
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5288761 |
Open chain enediyne dihydroperoxides having DNA cleaving properties
Open chain enediyne dihydroperoxides having eight carbons between the hydroperoxide groups that cleave DNA are disclosed, as are methods of making and using the same.
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5286733 |
Substituted 3-piperidinealkanoates and alkanones and compositions and method of use thereof
The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein: R 1 is hydrogen, lower-alkyl, phenyl-lower-alkyl, C 3 -C 7 -monocyclic...
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