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5451605 |
1,2-epoxycyclohexanyl and bicyclic aromatic substituted ethyne compounds having retinoid-like biological activity
Compounds of the formula ##STR1## where R 1 -R 5 are hydrogen, lower alkyl of 1-6 carbons, or halogen; A is (CH 2 ) n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl...
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5441984 |
Urea, thiourea and guanidine derivatives
The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.
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5432195 |
Benzofuran derivative and pharmaceutical composition
The present invention relates to a compound expressed by the following general formula (I), pharmacologically-acceptable salt thereof and pharmaceutical composition mainly comprising the same....
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5432174 |
Treatment of ocular hypertension
A method for the treatment of ocular hypertension which comprises administering, to a subject in need of such treatment, (a) a β-adrenergic blocker at the enhancement phase of aqueous humor...
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5430056 |
Substituted 2-aminotetralins
Optically active or racemic compounds are provided having the formula ##STR1## where R 1 is ##STR2## where Y is hydrogen, halogen or C 1 to C 6 linear or branched alkyl; R 6 is C 1 to C 4 ...
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5416117 |
Cyclopropenone derivatives
A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent...
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5407961 |
α-substituted benzenemethanamine derivatives and pharmaceutical use
The present invention is concerned with antiretroviral (e.g. anti HIV-1) compounds having the formula ##STR1## Pharmaceutical compositions containing said compounds of formula (I-a) or (I-b), and...
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5385931 |
Sulfonamides derived from benzocyclic or benzoheterocyclic acids, their preparation and application in therapeutics
The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or...
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5376679 |
Bicyclic or tricyclic biocidal compounds
Compounds of the general formula ##STR1## where R 2 and R 3 together, or R 3 and R 4 together, represent an optionally substituted hydrocarbyloxy chain; the ring is optionally substituted at...
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5376681 |
Aminocoumaran derivatives, their production and use
A novel aminocoumaran derivatives of the general formula (I): ##STR1## wherein R 1 and R 2 are a hydrogen atom, an acyl group, an alkoxycarbonyl group, an aliphatic group or aromatic group; R 3 ...
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5371105 |
Aqueous formulations and their use
The invention relates to aqueous formulations containing 1 to 70% by weight of an agrochemical active substance which is sparingly soluble in water, besides an amount which inhibits crystallization...
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5358962 |
Antihypertensive method
An antihypertensive method comprising administering to a hypertensive patient a pharmaceutical agent containing lithospermic acid B represented by the formula: ##STR1## and/or the pharmaceutically...
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5348976 |
Condensed heterocyclic derivatives and agricultural or horticultural fungicides containing the same
The present invention provides a condensed heterocyclic derivative represented by a formula: ##STR1## wherein R 1 represents a lower alkyl group, an alkenyl group, or the like, R 2 , R 3 , R 4 , R...
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RE34712 |
Pharmaceutically useful (+)-1-(3-dimethylaminopropyl)-1-(4'-fluorophenyl)-1,3-dihydroiso benzofuran-5-carbonitrile and non-toxic acid addition salts thereof
The two enantiomers of the anti-depressant drug of the formula I ##STR1## are disclosed. Methods for resolving intermediates and their steroselective stereoselective conversion to a...
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5328927 |
Hetercyclic compounds, processes for their preparation and pharmaceutical compositions containing them
Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein Q 1 is halo substituted phenyl; naphthyl; indolyl; benzthiophenyl; benzofuranyl; benzyl; or fluorenyl; . . is an...
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5314910 |
Ester inhibitors
2-Heteroaromatic alkanoate esters which are useful as inhibitors of human leukocyate or neutrophil elastase.
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5308866 |
Benzofuran ethylamine compounds
The invention relates to a compound selected from those of formula (I): ##STR1## in which Ar', R 1 and R 2 are as defined in the specification, an optical isomer, and an addition salt thereof...
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5300522 |
Condensed heterocyclic compounds and pharmaceutical use thereof
The invention relates to compounds of the formula ##STR1## wherein R 1 is hydrogen. acyl, lower-alkyl or --CHO, --CH 2 OR 10 , --COR 7 or OR 13 ; R 2 , R 3 and R 4 are, independently,...
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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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5270335 |
Method of inhibiting metabolism of cholesterol
A method of inhibiting the metabolism of cholesterol, comprising administering to a subject a pharmaceutical composition comprising a dioxabicyclo[3.3.0]octane derivative represented by the...
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5260331 |
Composition for treating depression with (S- or O-heteroaryl)alkyl amines
The invention concerns compounds having formula: ##STR1## or a salt thereof, wherein E represents hydrogen, lower alkyl or a group Ar 1 --A 1 --; Ar and Ar 1 are the same or different aryl...
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5256661 |
Substituted 2-aminotetralins and pharmaceutical use
Certain novel compounds having the structural formula ##STR1## where R 2 , R 3 and R 4 are each selected from the group consisting of H and OA; A is H or is selected from the group consisting of...
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5254595 |
Aryloxypropanolaminotetralins, a process for their preparation and pharmaceutical compositions containing them
Aryloxypropanolaminotetralins with beta-antagonist activity of the formula ##STR1## wherein R is hydrogen, hydroxy or methoxy and Ar is an optionally substituted aromatic or heteroaromatic group,...
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5254582 |
Antitumor compositions and methods
This invention provides the use of N-[[(3,4-dichlorophenyl)amino]carbonyl]-2,3-dihydrobenzofura
n-5-sulfonamid e, and pharmaceutically acceptable salts thereof, in the treatment of susceptible...
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5252608 |
Inhibitors of lysyl oxidase
This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.
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5250565 |
Indole-,benzofuran-,and benzothiophene-containing lipoxygenase-inhibiting compounds
Pro-drugs of potent 5-lipoxygenase inhibiting compounds comprise compounds of the formula ##STR1## in which A is an alkylene or alkenylene group, X is oxygen, sulfur, sulfoxyl, or substituted...
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5248686 |
Substituted cyclic amines and pharmaceutical composition containing them
The invention relates to substituted arylamines and heteroarylamines, their preparation process and the pharmaceutical composition containing them. Said substituted amine is in accordance with the...
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5244918 |
Benzofuran derivative and pharmaceutical comprising the same as active ingredient
The present invention relates to a benzofuran derivative having the following general formula (I), ##STR1## wherein R 1 and R 2 may be the same or different and represent a hydrogen atom or a...
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5234949 |
Parenteral solutions containing amiodarone in acetate buffer solution
Disclosed herein are parenteral solutions containing 3-diethylaminoethoxybenzoyl-benzofurans, such as amiodarone, in acetate buffer useful in the treatment of arrhythmias.
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5232945 |
3-aryl-2-hydroxypropionic acid derivatives and analogs as antihypertensives
A method of using certain 3-aryl-2-hydroxypropionic acid derivatives and analogs in the treatment of hypertension.
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5227399 |
Pyranylphenyl naphthalene lactones as inhibitors of leukotriene biosynthesis
Compounds having the formula I: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They...
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5223510 |
Alkylaminoalkyl derivatives of benzofuran, benzothiophene, indole and indolizine, process for their preparation and compositions containing them
The subject of the invention is benzofuran, benzothiophene, indole or indolizine compounds of general formula: ##STR1## in which: Het represents one of the groups: ##STR2## in which T,T' and...
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5223534 |
Benzofuuranyl/benofuranylaklyl-N-terminal cycloalkoxy-C-terminal amino hydroxy β-amino acid derivatives
Non-peptidyl compounds characterized generally as benzofuranyl/benzofuranylalkyl-N-terminal cycloalkoxy-C-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for...
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5219886 |
Mercapto-acylamino acids
Novel mercapto-acylamino acids of the formula ##STR1## wherein Q is hydrogen or R 7 CO--; R 1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl; R 2 is hydrogen; lower alkyl; cyclolower...
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5192799 |
Coumaran group containing amine compounds and their acid addition salts and quaternary ammonium salts and the use thereof as anti arrhythmic agents and as psychotropic agents
Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid...
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5187192 |
Cyclobutyl derivatives having lipoxygenase inhibitory activity
Compounds of the structure ##STR1## where M is a pharmaceutically acceptable cation or a metabolically cleavable group, R is alkyl, cycloalkyl or --NR 1 R 2 , where R 1 and R 2 are hydrogen,...
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H001139 |
Combination of a calcium channel blocker and thromboxane A.sub.2 receptor antagonist or synthetase inhibitor and method for treating ischemia employing such combination
A method is provided for treating ischemia in a mammalian species by administering a combination of a calcium channel blocker such as diltiazem, SQ 31,765 or SQ 32,324 and a thromoboxane A 2 ...
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5182295 |
Insecticidal benzofuran derivatives
A compound of the formula ##STR1## wherein R is selected from the group consisting of hydrogen, optionally substituted alkyl, alkenyl and alkynyl of up to 8 carbon atoms, optionally substituted...
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5179112 |
Heterocyclic amide derivatives and pharmaceutical use
The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts...
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5175184 |
Benzothiophene derivatives and antihyperuricemia thereof
A new series of benzofuran and benzothiophene derivatives are disclosed. These compounds have a structure which can be obtained by substituting the third position of 2-lower alkyl-benzofuran or...
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5171751 |
Benzofuran/benzofuranalkyl-N-terminal amino hydroxy
Non-peptidyl compounds characterized generally as benzofuran/benzofuranalkyl-N-terminal amino hydroxy β-amino acid derivatives are useful as renin inhibitors for treatment of hypertension....
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5162364 |
4-aminobutyric acid compounds, compositions, and method of use for treating disorders related to a dysfunction of GABA.sub.B receptors
A compound of formula (I): ##STR1## in which R, R 1 and R 2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA B receptors.
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5162370 |
Treatment of cataract with prostacyclin compounds
A method for treatment of cataract which comprises administering, to a subject in need of such treatment, a prostacyclin compound in an amount effective in treatment of cataract.
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5152983 |
Sunscreen compositions comprising pongomol
A sunscreen composition suitable for topical application to human skin or hair, to provide protection from excessive exposure to ultra-violet rays, comprises: i) an effective amount of a...
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5145870 |
Aryloxyphenylpropylamines their preparation and use
Novel aryloxyphenylpropylamines having the formula ##STR1## wherein X is H, cyano, halogen, halogenoalkyl, C 1 -6 -alkoxy, C 1 -6 -alkyl, C 1 -5 -alkanoyl, C 3 -5 -alkylene, aryloxy or aralkoxy,...
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5130334 |
Indane sulfonamide anti-arrhythmic agents
Novel 5-alkanesulphonamido-2-[N-(alkanesulphonamidoheterocyclicmet
hyl)-N-methyla mino]indane compounds have been prepared, including their pharmaceutically acceptable salts and various key novel...
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5128348 |
Bicyclo(3.1.0)hexane amines and bicyclo(4.1.0)-heptane amines as agricultural fungicides
Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.
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5126364 |
4-amino-5-chloro-n-(2-pyrrolidinylmethyl)-2,3-dihydrobenzo[b]fura n-7-carboxamide and pharmaceutical compositions containing the same
The compound (R) (-)-4-amino-5-chloro-N-(2-pyrrolidinylmethyl)-2,3-dihydroben
zo[b]furan-7-c arboxamide; the S isomer thereof, and pharmaceutical compositions containing the same.
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5126370 |
Anti-thrombotic heterocyclic amido prostaglandin analogs
Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula ##STR1## wherein: m is 1, 2 or 3: n is 1, 2 or 3, except that n is O when Y is vinylene;...
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5124352 |
Fat emulsions containing isocarbacyclin
The fat emulsions containing the prostaglandin I 2 's expressed by the following formula (I): ##STR1## where X represents an oxygen atom to a methine group, Y is a carbon atom, Z represents a...
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