Abstract: This invention relates to a pharmaceutical tablet containing active substance prone to hydrolysis and having a long shelf life which comprises (1) one or more layers free from active substance and (2) a layer containing said active substance in a concentration sufficient to inhibit hydrolysis.
Abstract: Compounds of the formula ##STR1## wherein W and X, which may be identical to or different from each other, are each hydrogen, fluorine, chlorine, bromine, iodine, nitro, alkyl of 1 to 4 carbon atoms, fluoro-substituted alkyl of 1 to 4 carbon atoms or chloro-substituted alkyl of 1 to 4 carbon atoms;Y is hydrogen, fluorine, chlorine, bromine, alkyl of 1 to 4 carbon atoms, fluoro-substituted alkyl of 1 to 4 carbon atoms or chloro-substituted alkyl of 1 to 4 carbon atoms;Z is fluorine, chlorine, bromine, alkyl of 1 to 4 carbon atoms, fluoro-substituted alkyl of 1 to 4 carbon atoms, chloro-substituted alkyl of 1 to 4 carbon atoms, --COOH or --COO-(alkyl of 1 to 4 carbon atoms); andn is 0 or 1;and, when Z is COOH, salts thereof, especially their alkali metal salts. The compunds as well as the salts are useful as selective herbicides.
Type:
Grant
Filed:
September 5, 1986
Date of Patent:
November 22, 1988
Assignee:
Celamerck GmbH & Co. KG
Inventors:
Rudolf Mengel, Ludwig Schroder, Werner Stransky, Gerbert Linden, Sigmund Lust
Abstract: The invention relates to novel N-alkylnorscopines wherein the alkyl group may have 2 to 10 carbon atoms, which are useful in the preparation of valuable pharmaceutical compositions. These compounds may be prepared from the corresponding N-alkylnorscopolamines by hydrogenolysis with complex hydrides, which reaction is preferably carried out with sodium borohydride in ethanol at ambient temperature.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.2 is 2-, 3- or 4-pyridyl, phenyl or mono- or di- substituted phenyl, where the substituents are each individually alkoxy of 1 to 2 carbon atoms, fluorine, chlorine, bromine, trifluoromethyl, alkyl or 1 to 4 carbon atoms, hydroxyl or nitro; andR.sub.3 and R.sub.4 are each independently hydrogen or alkyl of 1 to 4 carbon atoms; orR.sub.3 and R.sub.4, together with each other and the nitrogen atom to which they are attached, form an unsubstituted or methyl-substituted, saturated 5- or 6-membered heterocycle which may contain an additional oxygen or nitrogen heteroatom, or form an imidazole ring;where the aminomethyl substituent is attached to the 4- or 5-position or the pyrrolidine ring, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as the salts are useful as nootropics and antihypoxics.
Type:
Grant
Filed:
June 26, 1986
Date of Patent:
August 30, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr
Abstract: Compounds of the formula ##STR1## wherein A, B, C and D are --N.dbd., HN.dbd., R.sub.3 N.dbd., O.dbd.C.dbd., HC.tbd., HO--C.tbd. or R.sub.3 SO.sub.2 --O--C.tbd.; andR.sub.1 and R.sub.2 are substituents of various types.The compounds are useful as hypotensives and cardiotonics.
Type:
Grant
Filed:
January 28, 1987
Date of Patent:
August 23, 1988
Assignee:
Celamerck GmbH & Co. KG
Inventors:
Volkhard Austel, Joachim Heider, Norbert Hauel, Manfred Reiffen, Jacobus C. A. van Meel, Willi Diederen
Abstract: 5,6,-dihydro-pyrrolo[2,1-a]isoquinolines of the formula ##STR1## are prepared by heating a 1-(3-furyl)-3,4-dihydro-isoquinoline of the formula ##STR2## in a primary or secondary amine to at least 80.degree. C. for several hours, the amine is removed, the reaction product is treated with dilute acid, and the reaction product is purified and isolated.
Type:
Grant
Filed:
June 16, 1987
Date of Patent:
August 23, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Walter Losel, Otto Roos, Gerd Schnorrenberger
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.2 is hydrogen, alkyl of 1 to 4 carbon atoms or phenyl(alkyl of 1 to 6 carbon atoms);R.sub.3 is hydrogen or alkyl of 1 to 6 carbon atoms;n and m are each independently 0, 1 or 2, the sum of n and m being 1 or 2;X, Y and Z are each independently oxygen, sulfur, --NR.sub.4 --, .dbd.CR.sub.5 --, --CHR.sub.5 --, ##STR2## provided that only one of X, Y and Z is O, S, ##STR3## and one or two of X, Y and Z are --R.sub.4 --; R.sub.4 is hydrogen or alkyl of 1 to 4 carbon atoms; andR.sub.5 is hydrogen or, together with a vicinal radical R.sub.5, a phenyl ring, or when m and n are both 1, the dihydro form with its double bond in conjugation with the C-terminal carboxylic group;or a non-toxic, pharmacologically acceptable salt thereof. The compounds as well as their salts are useful as antihypertensives.
Type:
Grant
Filed:
May 6, 1987
Date of Patent:
August 23, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Gerd Schnorrenberg, Otto Roos, Walter Losel, Ingrid Wiedemann, Wolfram Gaida, Wolfgang Hoefke
Abstract: The invention is directed to a process and apparatus for dotting molding tools with droplets of liquid or suspended lubricant in the production of shaped articles in the pharmaceutical, food, or catalyst fields. Pressurized lubricant solutions or suspensions and pressurized gas are alternately passed through capillaries, in conjunction with alternating single-substance nozzles, in such a way that drops are formed on the nozzle surface, in between the jets of gas, and are then detached from this surface and directed to specific zones of pressing tools. The apparatus comprises fast-acting valves for the brief release of pressurized gases and lubricant liquids or suspensions. The delivery lines of a gas valve and a liquid valve combine upstream of a capillary, and single-substance nozzles are mounted at the end of the capillaries.
Type:
Grant
Filed:
September 12, 1986
Date of Patent:
July 19, 1988
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Gunther M. Voss, Volker I. Glasel, Peter Gruber, Walter Bubeck
Abstract: Compounds of the formula ##STR1## wherein A, B, R.sub.1, X and Q are substituents of various types, and acid addition salts thereof. The compounds are useful as fungicides.
Type:
Grant
Filed:
September 29, 1986
Date of Patent:
June 28, 1988
Assignee:
Celamerck GmbH & Co. KG
Inventors:
Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
Abstract: Compounds of the formula ##STR1## wherein A, B, C and D are each independently --N.dbd. or --CH.dbd., provided, however, that at least two of them must be --N.dbd., and when A and C are both --N.dbd., at least one or both of B and D must be --N.dbd.; andR.sub.1, R.sub.2 and R.sub.3 are substituents of diverse types;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds are useful as cardiotonics.
Type:
Grant
Filed:
July 9, 1987
Date of Patent:
May 24, 1988
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Volkhard Austel, Norbert Hauel, Joachim Heider, Manfred Reiffen, Jacobus C. A. Van Meel, Willi Diederen
Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.
Type:
Grant
Filed:
May 14, 1985
Date of Patent:
April 5, 1988
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted alkoxy group, or an optionally substituted mercapto or amino group,R.sub.2 is a cyclic imino group,R.sub.3 is hydrogen, phenyl, alkyl or acyl, andn is 2 or 3,and non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as antithrombotics.
Type:
Grant
Filed:
January 28, 1987
Date of Patent:
March 1, 1988
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann, Johannes M. Weisenberger
Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.9 and R.sub.10 have diverse meanings. They are useful as herbicides.
Type:
Grant
Filed:
December 18, 1986
Date of Patent:
February 9, 1988
Assignee:
Celarmerck GmbH & Co. KG
Inventors:
Wolfgang Buck, Manfred Garrecht, Gerhart Schneider, Christo Drandarevski
Abstract: The invention relates to novel 2-phenyl-imidazoles of the formula ##STR1## and the tautomers and acid addition salts thereof, particularly the pharmacologically acceptable acid addition salts, which exhibit valuable pharmacological properties, particularly an effect on the contractility of the heart muscle. The compounds of Formula I may be prepared by methods conventionally used for similar compounds.
Type:
Grant
Filed:
December 20, 1984
Date of Patent:
February 2, 1988
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Volkhard Austel, Joachim Heider, Norbert Hauel, Manfred Reiffen, Josef Nickl, Jacobus C. A. van Meel, Willi Diederen
Abstract: Compounds of the formula ##STR1## wherein (a)R.sub.1 is hydrogen, lower alkyl, lower alkoxy or 8-halo;R.sub.2 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring; andR.sub.3 and R.sub.4, together with each other, are --N.dbd.N--NH--; or(b)R.sub.1 and R.sub.2, together with each other, are --N.dbd.N--NH--;R.sub.3 is hydrogen, lower alkyl, lower alkoxy, 2-halo, 3-halo or 4-halo; andR.sub.4 is hydrogen, lower alkyl, lower alkoxy or a fused benzene ring;and non-toxic, pharmacologically acceptable salts thereof formed with an inorganic or organic base. The compounds as well as their salts are useful as antiallergics.
Type:
Grant
Filed:
June 4, 1986
Date of Patent:
January 19, 1988
Assignee:
Boehringer Ingelheim KG
Inventors:
Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner
Abstract: Gold values are obtained from gold cyanidation tailings or gold bearing ores by treating the same with a flotation collector consisting of 5 to 20% xanthate collector and 80 to 95% fatty acid collector of a pulp pH range from 5 to 8.
Abstract: This invention is directed to novel galenic preparation forms for providing an oral anti-diabetic agent having an improved release of active substance and to processes for producing these preparation forms. The pharmaceutical compositions are characterized in that the onset of the activity and the duration of activity are adapted to the particular needs of diabetics with regard to proper control of metabolism and the associated proper release of insulin. A basic or acidic excipient in a solvent is added to the anti-diabetically active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. The solution is applied to a water-insoluble carrier, the solvent is evaporated, and the residue is further processed to yield the various preparation forms.
Type:
Grant
Filed:
May 31, 1984
Date of Patent:
November 24, 1987
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Rolf Brickl, Gottfried Schepky, Eckhard Rupprecht, Andreas Greischel
Abstract: The invention is directed to a process for dotting molding tools with droplets of liquid or suspended lubricant in the production of shaped articles in the pharmaceutical, food, or catalyst fields. Pressurized lubricant solutions or suspensions and pressurized gas are alternately passed through capillaries, in conjunction with alternating single-substance nozzles, in such a way that drops are formed on the nozzle surface, in between the jets of gas, and are then detached form this surface and directed to specific zones of pressing tools. The apparatus comprises fast-acting valves for the brief release of pressurized gases and lubricant liquids or suspensions. The delivery lines of a gas valve and a liquid valve combine upstream of a capillary, and single-substance nozzles are mounted at the end of the capillaries.
Type:
Grant
Filed:
March 27, 1984
Date of Patent:
November 17, 1987
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Gunther M. Voss, Volker I. Glasel, Peter Gruber, Walter Bubeck