Patents Represented by Law Firm Weissenberger, Hammond & Littell
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Patent number: 4786507Abstract: 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.Type: GrantFiled: March 31, 1987Date of Patent: November 22, 1988Assignee: Boehringer Ingelheim KGInventor: Michael Schmidt
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Patent number: 4786317Abstract: 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: GrantFiled: September 5, 1986Date of Patent: November 22, 1988Assignee: Celamerck GmbH & Co. KGInventors: Rudolf Mengel, Ludwig Schroder, Werner Stransky, Gerbert Linden, Sigmund Lust
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Patent number: 4783534Abstract: 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.Type: GrantFiled: March 31, 1987Date of Patent: November 8, 1988Assignee: Boehringer Ingelheim KGInventor: Rolf Banholzer
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Patent number: 4767759Abstract: 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: GrantFiled: June 26, 1986Date of Patent: August 30, 1988Assignee: Boehringer Ingelheim KGInventors: Karl-Heinz Weber, Gerhard Walther, Claus Schneider, Dieter Hinzen, Franz J. Kuhn, Erich Lehr
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Patent number: 4766130Abstract: 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: GrantFiled: January 28, 1987Date of Patent: August 23, 1988Assignee: Celamerck GmbH & Co. KGInventors: Volkhard Austel, Joachim Heider, Norbert Hauel, Manfred Reiffen, Jacobus C. A. van Meel, Willi Diederen
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Patent number: 4766217Abstract: 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: GrantFiled: June 16, 1987Date of Patent: August 23, 1988Assignee: Boehringer Ingelheim KGInventors: Walter Losel, Otto Roos, Gerd Schnorrenberger
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Patent number: 4766129Abstract: 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: GrantFiled: May 6, 1987Date of Patent: August 23, 1988Assignee: Boehringer Ingelheim KGInventors: Gerd Schnorrenberg, Otto Roos, Walter Losel, Ingrid Wiedemann, Wolfram Gaida, Wolfgang Hoefke
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Patent number: 4758142Abstract: 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: GrantFiled: September 12, 1986Date of Patent: July 19, 1988Assignee: Dr. Karl Thomae GmbHInventors: Gunther M. Voss, Volker I. Glasel, Peter Gruber, Walter Bubeck
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Patent number: 4755603Abstract: Norscopine is prepared from norscopolamine by hydrogenation cleavage with a complex hydride in an inert solvent at room temperature.Type: GrantFiled: May 26, 1987Date of Patent: July 5, 1988Assignee: Boehringer Ingelheim KGInventor: Rolf Banholzer
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Patent number: 4753934Abstract: 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: GrantFiled: September 29, 1986Date of Patent: June 28, 1988Assignee: Celamerck GmbH & Co. KGInventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
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Patent number: 4746658Abstract: 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: GrantFiled: July 9, 1987Date of Patent: May 24, 1988Assignee: Dr. Karl Thomae GmbHInventors: Volkhard Austel, Norbert Hauel, Joachim Heider, Manfred Reiffen, Jacobus C. A. Van Meel, Willi Diederen
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Patent number: 4735959Abstract: 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: GrantFiled: May 14, 1985Date of Patent: April 5, 1988Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
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Patent number: 4728646Abstract: 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: GrantFiled: January 28, 1987Date of Patent: March 1, 1988Assignee: Dr. Karl Thomae GmbHInventors: Josef Roch, Erich Muller, Berthold Narr, Josef Nickl, Walter Haarmann, Johannes M. Weisenberger
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Patent number: 4723989Abstract: 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: GrantFiled: December 18, 1986Date of Patent: February 9, 1988Assignee: Celarmerck GmbH & Co. KGInventors: Wolfgang Buck, Manfred Garrecht, Gerhart Schneider, Christo Drandarevski
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Patent number: 4722929Abstract: 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: GrantFiled: December 20, 1984Date of Patent: February 2, 1988Assignee: Dr. Karl Thomae GmbHInventors: Volkhard Austel, Joachim Heider, Norbert Hauel, Manfred Reiffen, Josef Nickl, Jacobus C. A. van Meel, Willi Diederen
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Patent number: 4720496Abstract: 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: GrantFiled: June 4, 1986Date of Patent: January 19, 1988Assignee: Boehringer Ingelheim KGInventors: Kurt Schromm, Anton Mentrup, Ernst-Otto Renth, Armin Fugner
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Patent number: 4708868Abstract: 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: GrantFiled: May 31, 1984Date of Patent: November 24, 1987Assignee: Dr. Karl Thomae GmbHInventors: Rolf Brickl, Gottfried Schepky, Eckhard Rupprecht, Andreas Greischel
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Patent number: 4705803Abstract: This invention relates to a method of improving the resorption of injected antibacterially active substances or combinations. More specifically, this invention relates to a method of increasing the resorption of an antibacterially active substance or combination which does not have optimum resorbability and which is administered parenterally into tissue, which comprises administering to a host at least one benzylamine derivative of the formula ##STR1## wherein R.sub.1 is a hydroxyl group in the 2- or 4-position or an amino group in the 2-position;R.sub.2 is a hydrogen atom or an alkyl group having from 1 to 3 carbon atoms; andR.sub.3 is a cyclohexyl group optionally substituted by a hydroxyl group,or a non-toxic, pharmacologically acceptable acid addition salt thereof with an inorganic or organic acid, in conjunction with said antibacterially active substance or combination.Type: GrantFiled: February 3, 1986Date of Patent: November 10, 1987Assignee: Boehringer Ingelheim Vetmedica GmbHInventors: Otto Kern, Franz Wilhelm, Ernst Salamon
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Patent number: 4705191Abstract: A re-usable mixing and spraying device in which the fill opening and the hand pump used to discharge the spray solution are arranged at different heights, and a concentrate and a diluent may be mixed together in the device which is tightly sealed off from the outside, the concentrate being enclosed in a sealing cap which can be ruptured by the device, so that the reservoir enclosing the concentrate is closed when the sealing cap and fill opening are loosely connected and opened toward the diluent when the sealing cap and fill opening are tightly connected.Type: GrantFiled: July 29, 1985Date of Patent: November 10, 1987Assignee: Celamerck GmbH & Co. KGInventors: Hanshelmut Itzel, Volker Barth
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Patent number: D298577Type: GrantFiled: February 28, 1986Date of Patent: November 15, 1988Inventor: Sheila H. Faxon