Abstract: Carbazolylmethane compounds of the formula ##STR1## wherein one of Y.sub.1, Y.sub.2 and Q represents a 3-carbazolyl radical of the formula ##STR2## and each of the other two independently represents an amino-substituted phenyl radical of the formula ##STR3## a 3-indolyl radical of the formula ##STR4## a 3-carbazolyl radical of the formula ##STR5## or a 3-carbazolyl radical of the formula (1a), and Q also represents hydrogen, alkyl of 1 to 12 carbon atoms, alkenyl containing not more than 12 carbon atoms, aryl, aralkyl or a further heterocyclic radical, while each of X.sub.1 and X.sub.2 independently represents hydrogen, alkyl containing not more than 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxyl, cyano or lower alkoxy, or represents cycloalkyl, phenyl, benzyl, or phenyl or benzyl which is substituted by halogen, lower alkyl or lower alkoxy, or X.sub.1 and X.sub.2 together with the nitrogen atom to which they are attached represent a 5- or 6-membered heterocyclic radical, X.sub.
Abstract: 2-Amino- and 2-(substituted amino)-tetrahydro- and -cis-hexahydro-carbazoles useful for alleviating depression in mammals or as intermediate compounds thereto.
Abstract: Morpholinyl acetamide derivatives are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl, lower alkenyl or lower alkanoyl, R.sup.1 and R.sup.2 may be the same or different and are lower alkyl, lower alkenyl, phenyl-lower alkyl or lower alkoxy, or ##STR2## may be taken together to form a 5- to 7-membered heterocyclic ring optionally containing one other hetero atom, such as nitrogen, sulfur or oxygen; Y is hydroxyl, OR wherein R is as defined above, or ##STR3## wherein R.sup.1 and R.sup.2 and R.sup.1 and R.sup.2 taken together with the nitrogen to which they are attached are as defined above, and n is 1 to 6.These compounds are useful as anti-arrhythmia agents and have been found to be effective in the treatment of acute myocardial infarction.
Abstract: A process for the preparation of benzothiazole-sulfenamides in which a benzothiazyl disulfide is reacted with a mixture comprising an amine halogenhydrate and an N-halogen amine derivative.
Type:
Grant
Filed:
October 5, 1979
Date of Patent:
February 24, 1981
Assignee:
Produits Chimiques Ugine Kuhlmann
Inventors:
Michel Alicot, Laurent Ciccotto, Adrien Tignol
Abstract: Compounds are disclosed of general formula (I): ##STR1## wherein R.sub.1 and R.sub.2 each independently represents a hydrogen atom, or an aryl, aralkyl, cycloalkyl, fluoroalkyl or alkyl group, which alkyl group is optionally substituted by an alkenyl group or by a group -OR.sub.7 or by ##STR2## where R.sub.7 and R.sub.8 each independently represents a hydrogen atom, an alkyl, aryl or aralkyl group; or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a saturated monocyclic 5 to 7 membered ring which may contain a further hetero function (viz--O--, --NH or ##STR3## R.sub.3 and R.sub.4 have the same meanings as R.sub.1 and R.sub.2 and may together form an aralkylidene group;R.sub.5 represents a hydrogen atom or an alkyl or aralkyl group;R.sub.6 represents a hydrogen atom or an aryl or C.sub.1 -C.sub.3 alkyl group;Alk represents an C.sub.1 -C.sub.4 alkylene group optionally substituted at one or more of its carbon atoms by one to three C.sub.1 -C.sub.
Abstract: Compounds of the formula ##STR1## wherein R is 2-bromo-4,5-dihydroxy-phenyl; 3-chloro-4-hydroxy-phenyl; 4-bromo-2,5-dihydroxy-phenyl; 3,5-dihydroxy-phenyl; 5-chloro-2,4-dihydroxy-phenyl; 3-hydroxy-4-methyl-phenyl; 2,6-dibromo-4-hydroxymethyl-phenyl; 3,5-dibromo-4-amino-phenyl; 3-methylmercapto-phenyl; 3,4,5-trihydroxy-phenyl; or 3-bromo-4-fluoro-phenyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
Type:
Grant
Filed:
February 16, 1979
Date of Patent:
February 10, 1981
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Helmut Stahle, Herbert Koppe, Werner Kummer, Wolfgang Hoefke, Wolfram Gaida, Ludwig Pichler
Abstract: Alcohol, thiol, epoxylated alcohol, epoxylated thiol and benzyloxy derivatives of benzodioxane, benzodioxole and benzodioxepine are useful as intermediates for preparing certain useful cinnamoyl piperazines and homopiperazines.
Type:
Grant
Filed:
April 13, 1979
Date of Patent:
February 3, 1981
Assignee:
Delalande S.A.
Inventors:
Guy R. Bourgery, Alain P. Lacour, Gerard H. Moinet, Bernard M. Pourrias, Anne-Marie P. Ruch
Abstract: New-pyrrolyl-3-pyridazineamines having a further aminic substituent in the position 6. The compounds are useful as antihypertensive agents and may be prepared from 6-amino substituted-3-hydrazino pyridazines and .beta.-dicarbonyl compounds. The use of the novel compounds as antihypertensives and compositions containing the novel compounds as active ingredients are also claimed.
Type:
Grant
Filed:
September 17, 1979
Date of Patent:
January 27, 1981
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Elvio Bellasio, Nunzio Di Mola, Ambrogio Campi, Emiliana Baldoli
Abstract: Fominoben/theophylline complex is disclosed having the formula: ##STR1## In pharmaceutical oral preparations (dragees or syrup) the complex is usable in dosages corresponding to those of Fominoben hydrochloride, without exhibiting, however, a bitter nauseating taste.The complex is prepared by refluxing a solution of Fominoben hydrochloride and theophylline sodium salt in equimolar proportions in an alcoholic solvent while at the same time dehydrating the reflux stream.
Abstract: Disclosed are cationic dyestuffs being coumarin or coumarinimide derivatives free from sulpho groups, bearing a 7-amino group and being characterized by having, in the 3-position, a cationic group of formula (a), ##STR1## in which A.sup..crclbar. signifies an anion,eitherR.sub.5 .degree. signifies hydrogen or optionally substituted alkyl or cycloalkyl, andR.sub.6 .degree. signifies hydrogen, or optionally substituted alkyl or cycloalkyl, or, where R.sub.5 .degree. is hydrogen, also hydroxy, naphthyl, optionally substituted amino or alkoxy, or phenyl monosubstituted by phenoxy, chlorophenoxy,benzyl, amino or C.sub.1 -C.sub.4 alkylamino,orR.sub.5 .degree. and R.sub.6 .degree., together with the nitrogen to which they are attached, signify a non-aromatic heterocycle,and the dotted line indicates that the positive charge is not localized, their productionand use for dyeing and printing basic dyeable substrates, plastics and paper, particularly acid modified polyester substrates.
Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is alkyl, cycloalkyl or aryl; R.sub.2 is acyl or sulfonyl; R.sub.3 is alkylamino, dialkylamino or a nitrogen containing heterocyclic group; R.sub.4 is alkoxy; A.sub.1 is a saturated bond or an alkylene group having 1 to 4 carbon atoms; and A.sub.2 is an alkylene group having 2 to 5 carbon atoms; have antiinflammatory activity.
Abstract: New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino groupone of R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygenone of R.sub.4 and R.sub.5 is hydrogen and the other represents alkyloxy or aralkyloxy y and y' each represent hydrogen or jointly form a bond and their pharmacologically acceptable salts, as well as pharmaceutical formulations thereof.
Type:
Grant
Filed:
September 14, 1979
Date of Patent:
December 30, 1980
Assignee:
Kali-Chemie Pharma GmbH
Inventors:
Peter W. Thies, Akiji Asai, Samuell David
Abstract: 6-[(Aryloxy)methyl]-2-morpholinemethanol derivatives are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl, phenyl-lower alkyl, or lower alkenyl, and Ar represents a monocyclic or polycyclic aromatic group including tetraindiols and their analogs. These compounds are useful as adrenergic modifiers, particularly in treating arrhythmia.
Abstract: Nitroimidazoles of the formula ##STR1## wherein R.sup.1 and R.sup.2 are as hereinafter set forth, are described. The nitroimidazoles are useful as hypoxic-cell radiosensitizers, as well as being useful as antiprotozoal agents.
Abstract: Compounds of the formulaR--A--Zwherein R is a 4-biphenylyl or 4-phenoxyphenyl or a corresponding group monosubstituted or polysubstituted by one or more of F, Cl, and Br; A is --CH(CH.sub.3)--CH.sub.2 --(CH.sub.2).sub.n --, --C(CH.sub.3).dbd.CH--(CH.sub.2).sub.n -- or --C(OH)(CH.sub.3)--CH.sub.2 --(CH.sub.2).sub.n --, Z is --NR.sup.1 R.sup.2, imidazol-1-yl, phthalimido or 4,5-dihydro-4-oxophthalazin-1-yl-amino; R.sup.1 and R.sup.2 each are H or alkyl, azaalkyl or acyl, each of 1-6 carbon atoms or collectively are alkylene of 4-7 carbon atoms, 3-oxapentamethylene or 3-R.sup.3 -3-azapentamethylene; R.sup.3 is H or alkyl or hydroxyalkyl each of up to 6 carbon atoms; and n is 0, 1, or 2, and their physiologically acceptable acid addition salts possess anti-inflammatory, anti-arteriosclerotic and serum cholesterol and trigylyceride level lowering activities.
Type:
Grant
Filed:
April 11, 1978
Date of Patent:
December 16, 1980
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Joachim Gante, Hans-Adolf Kurmeier, Erich Schacht, Werner Mehrhof, Dieter Orth, Albrecht Wild, Zdenek Simane
Abstract: The present invention is related to new basically substituted ureas having the general Formula I ##STR1## and the pharmaceutically acceptable acid addition salts thereof which produce an improved antiviral activity against DNS- and RNS-viruses. The invention is further related to the treatment of humans or animals suffering from diseases caused by viruses by administering compositions containing such ureas or salts thereof as active agent.
Abstract: Ampho-ionic compounds of the formula ##STR1## wherein, for example, R is CH.sub.2 .dbd.C(CH.sub.3)--COOCH.sub.2 --, R.sub.2 is hydrogen and B.sup..sym. is --N.sup..sym. --(CH.sub.3).sub.2 C.sub.12 H.sub.25, are prepared by reacting an oxirane compound with sulfur dioxide and a tertiary amine. These ampho-ionic compounds are useful as, for example, surfactants.
Abstract: A series of new 4,6-disubstituted 2-morpholinone derivatives were prepared either by a reaction of corresponding epoxide derivatives with phenylglycine derivatives or by the reaction of isopropanol derivatives with carboxylic acid derivatives. The new morpholinone derivatives are useful for the prevention or the treatment of arteriosclerosis.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2)is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.
Type:
Grant
Filed:
September 24, 1979
Date of Patent:
December 2, 1980
Assignee:
Pfizer Inc.
Inventors:
Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.