Patents Assigned to Thomas GmbH
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Patent number: 4870076Abstract: The invention relates to new sulphonamido-ethyl compounds having the following structure: ##STR1## wherein R.sub.1 is substituted or unsubstituted phenyl, benzyl, nitrophenyl, acetamidophenyl or thienyl, R.sub.2 is hydroxycarbonyl or alkoxycarbonyl bonded via alkylene or alkenylene, or a 4,5-dihydro-pyridazin-3-one-6-yl or pyridazin-3-on-6-yl group optionally substituted on a ring carbon by C.sub.1 -C.sub.3 alkyl and X is substituted or unsubstituted imino, oxygen or sulphur, which compounds may be used to prevent arteriosclerosis or tumor metastasis, and are antitrombotic and thromboxane antagonists.Type: GrantFiled: September 3, 1987Date of Patent: September 26, 1989Assignee: Karl Thomae GmbHInventors: Armin Heckel, Josef Nickl, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
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Patent number: 4863724Abstract: Galenic compositions containing an oral antidiabetic agent and having an improved release of active substance are provided, as well as processes for producing these compositions. The 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 the metabolism and the associated proper release of insulin. A basic or acidic excipient in a solvent is added to the antidiabetic active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. Polyvinylpyrrolidone is dissolved as carrier in this solution, but the carrier may simultaneously serve as the solubilizing adjuvant. This solution is further processed with other excipients to form pharmaceutical compositions.Type: GrantFiled: July 23, 1987Date of Patent: September 5, 1989Assignee: Dr. Karl Thomae GmbHInventors: Gottfried Schepky, Rolf Brickl, Eckhard Rupprecht, Andreas Greischel
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Patent number: 4831027Abstract: The invention relates to new imidazo-benzoxazinones of formula ##STR1## wherein the substituents are defined herein below, which compounds are useful in the treatment of cardiovascular disorders.Type: GrantFiled: October 5, 1987Date of Patent: May 16, 1989Assignee: Dr. Karl Thomae GmbHInventors: Berthold Narr, Norbert Hauel, Klaus Noll, Joachim Heider, Manfred Psiorz, Andreas Bomhard, Jacques van Meel, Willi Diederen
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Patent number: 4829058Abstract: Disclosed are substituted bis(4-aminophenyl)-sulfones of general formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or cycloalkyl; group,R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl,R.sub.3 is nitrile, C.sub.1 -C.sub.3 alkylaminocarbonyl, di C.sub.1 -C.sub.3 alkylaminocarbonyl, C.sub.3 -C.sub.7 N-cycloalkyl-C.sub.1 -C.sub.3 alkylaminocarbonyl C.sub.1 -C.sub.3 alkylamino, C.sub.1 -C.sub.3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C.sub.1 -C.sub.3 alkylaminono, diC.sub.1 -C.sub.3 alkylaminosulfonyl, hydroxy C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkylcarbonyl, amino C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy C.sub.1 -C.sub.3 alkyl groupor, when R.sub.1 and R.sub.2 are each hydrogen, R.sub.3 can be hydroxy, hydroxycarbonyl C.sub.1 -C.sub.3 alkoxy or di C.sub.1 -C.sub.3 aminocarbonylalkoxy;or, when R.sub.1 is C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 cycloalkyl and R.sub.2 is hydrogen or C.sub.1 -C.sub.3 alkyl, R.sub.Type: GrantFiled: June 15, 1987Date of Patent: May 9, 1989Assignee: Dr. Karl Thomae GmbHInventors: Joachim K. Seydel, Helmut Pieper, Gerd Kruger, Klaus Noll, Johannes Keck, Uwe Lechner
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Patent number: 4820705Abstract: The invention relates to new benzenesulphonamidoindanyl compounds having the following formula ##STR1## wherein the substituents are defined herein useful in the treatment and prophylaxis of thromboembolic diseases, arteriosclerosis and tumor metastasis.Type: GrantFiled: July 16, 1987Date of Patent: April 11, 1989Assignee: Dr. Karl Thomae GmbHInventors: Josef Nickl, Armin Heckel, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
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Patent number: 4820638Abstract: A novel species of alpha interferon is taught. The alpha interferon amino acid sequence is disclosed and a gene corresponding thereto. The alpha interferon gene is expressed in Escherichia coli.Type: GrantFiled: May 19, 1983Date of Patent: April 11, 1989Assignee: Dr. Karl Thomae GmbHInventors: Peter Swetly, Eva Dworkin-Rastl, Peter Meindl
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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: 4755385Abstract: There is described a solid pharmaceutical preparation for oral administration which produces high and long-lasting blood and tissue levels, containing 9-deoxo-11-deoxy-9,11-[imino[2-(2-methoxyethoxy)-ethylidene]oxy]-(9S)-eryt hromycin as active substance, in which the active substance must be intimately mixed with a basic excipient in a ratio of 1 mol of active substance to at least 2 gram-equivalents of basic excipient, and the preparations are coated with a gastric juice-resistant lacquer which is soluble in a pH range of between 5.5 and 6.8, and processes for preparing them. The solid pharmaceutical preparations include tablets, pellets or granules and a syrup can be produced from the latter.Type: GrantFiled: July 8, 1986Date of Patent: July 5, 1988Assignee: Dr. Karl Thomae, GmbHInventors: Alain Etienne, Peter Gruber, Ulrich Busch
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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: 4731374Abstract: This invention relates to new tetrahydrobenzthiazoles of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom, an alkyl group, an alkenyl or alkynylk group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the above mentioned phenyl nuclei may each be substituted by 1 or 2 halogen atoms,R.sub.2 represents a hydrogen atom or an alkyl group,R.sub.3 represents a hydrogen atom, an alkyl group a cycloalkyl group, an alkenyl or alkynyl group, an alkanoyl group, a phenyl alkyl or phenyl alkanoyl group, while the phenyl nucleus may be substituted by flurorine, chlorine or bromine atoms,R.sub.4 represents a hydrogen atom, an alkyl group, an alkyl or alkenyl group, orR.sub.3 and R.sub.4 together with the nitrogen atom between them represent a pyrrolidino, piperidino, hexamethyleneimino or morpholino group, the enantiomers and the acid addition salts thereof.The compounds of general formula I above in which one of the groups R.sub.1 or R.sub.3 or both groups R.sub.1 and R.sub.Type: GrantFiled: December 19, 1985Date of Patent: March 15, 1988Assignee: Dr. Karl Thomae GmbHInventors: Gerhart Griss, deceased, Rudolf Hurnaus, Walter Kobinger, Ludwig Pichler, Rudolf Bauer, Joachim Mierau, Dieter Hinzen, Gunter Schingnitz
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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: 4724236Abstract: Compounds of general formula I are described, ##STR1## wherein X represents the group .dbd.CHR, .dbd.NR or an oxygen atom andA represents the groups --NR.sup.1 R.sup.2,wherein R.sup.1 and R.sup.2 represent alkyl, cycloalkyl or phenylalkyl groups, n represents the number 0, 1 or 2, R.sup.3 represents a hydrogen atom, a hydroxy or alkyl group or a group --(CH.sub.2).sub.n --N--R.sup.5 R.sup.6 (R.sup.5 and R.sup.6 being lower alkyl groups) and R.sup.4 is an alkyl or phenylalkyl group; two processes for preparing these compounds and the salts thereof are also described.The compounds have favourable effects on heart rate and can be used as vagal pacemakers for treating bradycardia and bradyarrhythmia in human and veterinary medicine. Some of these compounds also have very good antithrombotic effects.Type: GrantFiled: December 19, 1986Date of Patent: February 9, 1988Assignee: Karl Thomae GmbHInventors: Wolfgang Eberlein, Gunter Trummlitz, Wolfhard Engel, Gerhard Mihm, Rudolf Hammer, Norbert Mayer, Antonio Giachetti, Adriaan de Jonge
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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: 4716169Abstract: The invention relates to new imidazo derivatives of the formula ##STR1## wherein "A-D and R.sup.1 -R.sup.3 are as defined in the specification". The new compounds have valuable pharmacological properties, particularly antithrombotic and cardiovascular properties such as a cardiotonic activity and/or an effect on blood pressure, and can be prepared using methods known per se.Type: GrantFiled: December 17, 1985Date of Patent: December 29, 1987Assignee: Dr. Karl Thomae GmbHInventors: Joachim Heider, Norbert Hauel, Volkhard Austel, Klaus Noll, Andreas Bomhard, Jacques van Meel, Willi Diederen
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Patent number: 4714698Abstract: The invention relates to new compounds of general formula ##STR1## wherein R.sub.1 represents an alkyl group,R.sub.2 represents a hydrogen atom, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group or an allyl, phenyl or benzyl group,R.sub.3 represents an allyl group, an alkyl group optionally substituted (except at the .alpha. carbon atom) by a hydroxy group, or represents a cycloalkyl group orR.sub.2 and R.sub.3 together with the nitrogen atom between them represent a straight-chained alkyleneimino group,the acid addition salts thereof, particularly the acid addition salts thereof with physiologically acceptable inorganic or organic acids which have valuable pharmacological properties, particularly a metastasis-inhibiting effect based on their selective tumour-PDE inhibiting effect, and pharmaceutical compositions containing these compounds or the physiologically acceptable acid addition salts thereof.Type: GrantFiled: June 17, 1985Date of Patent: December 22, 1987Assignee: Dr. Karl Thomae GmbHInventors: Josef Roch, Armin Heckel, Josef Nickl, Erich Muller, Berthold Narr, Rainer Zimmermann, Johannes Weisenberger
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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: 4707309Abstract: 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: GrantFiled: March 27, 1984Date of Patent: November 17, 1987Assignee: Dr. Karl Thomae GmbHInventors: Gunther M. Voss, Volker I. Glasel, Peter Gruber, Walter Bubeck
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Patent number: 4699909Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; alkyl of 1 to 7 carbon atoms; cycloalkyl of 3 to 7 carbon atoms; monosubstituted alkyl of 1 to 3 carbon atoms, where the substituent is pyridyl, methypyridyl, phenyl, mono-, di- or trisubstituted phenyl, where the substituents on the phenyl ring, which may be identical to or different from each other, are selected from the group consisting of one amino, one dimethylamino, one to two hydroxyls, one to three methoxys and one to three halogens; .omega.-monosubstituted alkyl of 2 to 4 carbon atoms, where the substituent is hydroxyl or di(alkyl of 1 to 3 carbon atoms)amino; phenyl; monohalo-phenyl; unsubstituted or monosubstituted straight or branched alkanoyl of 1 to 6 carbon atoms, where the substituent is phenyl, methoxyphenyl or cycloalkyl of 3 to 7 carbon atoms; or unsubstituted or monosubstituted phenylsulfonyl, where the substituent is methyl or methoxy; andR.sub.Type: GrantFiled: July 24, 1986Date of Patent: October 13, 1987Assignee: Dr. Karl Thomae GmbHInventors: Norbert Hauel, Volkhard Austel, Joachim Heider, Manfred Reiffen, Willi Diederen, Walter Haarman
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Patent number: 4696931Abstract: There are disclosed novel imidazole derivatives of the formula. ##STR1## and derivatives of the formula ##STR2## the tautomers thereof, and non-toxic, pharmacologically acceptable addition salts thereof with inorganic or organic acids. The compounds described herein are useful in treating cardiac insufficiency.Type: GrantFiled: April 30, 1985Date of Patent: September 29, 1987Assignee: Dr. Karl Thomae GmbHInventors: Norbert Hauel, Volkhard Austel, Joachim Heider, Manfred Reiffen, Willi Diederen