Abstract: This invention relates to pyridyl derivatives of the formula ##STR1## wherein X, Y, A, n and R.sub.3 to R.sub.8 are defined hereinbelow, the enantiomers thereof, the cis- and trans-isomers thereof, which have antithrombotic pharmaceutical activity.
Type:
Grant
Filed:
July 5, 1994
Date of Patent:
January 9, 1996
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Rainer Soyka, Thomas Muller, Johannes Weisenberger
Abstract: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
Type:
Grant
Filed:
October 28, 1993
Date of Patent:
December 26, 1995
Assignee:
Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Wolfgang Eisert
Abstract: Pharmaceutical compositions are described which contain 1,5,6,7-tetrahydro-4H-indazol-4-ones of the formula ##STR1## some of these substances themselves being new. The pharmaceutical compositions may be used as analgesics, antipyretics and antiphlogistics.
Type:
Grant
Filed:
September 29, 1993
Date of Patent:
November 21, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Klaus Rudolf, Gunther Engelhardt
Abstract: The invention relates to arylidene-1-azacycloalkanes and arylalkyl-1-azacycloalkanes of the general formula ##STR1## (wherein n, m, p, A, W.sup.1, W.sup.2, X, Y, and R.sup.1 to R.sup.11 are as defined in claim 1) and the isomers, isomer mixtures and salts thereof, which have useful properties, in particular an inhibitory effect on cholesterol biosynthesis.
Type:
Grant
Filed:
March 25, 1994
Date of Patent:
November 14, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
Abstract: Compounds of the formula ##STR1## wherein X.sub.1 to X.sub.5 are as defined herein, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases. The compounds are useful for inhibiting undesirable cell aggregation.
Type:
Grant
Filed:
November 8, 1993
Date of Patent:
October 31, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Guenter Linz, Volkhard Austel, Helmut Pieper, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
Abstract: The invention relates to substituted benzimidazolyl derivatives of the general formula ##STR1## wherein A and R.sub.a to R.sub.c are defined as in claim 1, the mixtures of position isomers thereof and the salts thereof which have valuable properties.These compounds have valuable pharmacological properties, particularly angiotensin-antagonistic effects and preferably angiotensin-II-antagonistic effects.
Type:
Grant
Filed:
May 3, 1994
Date of Patent:
October 17, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Norbert Hauel, Uwe Ries, Berthold Narr, Jacques van Meel, Wolfgang Wienen, Michael Entzeroth
Abstract: Compounds of formula ##STR1## where the substituents are as defined herein, are disclosed, which compounds are useful in the treatment of diabetes and obesity, among other uses.
Type:
Grant
Filed:
March 12, 1993
Date of Patent:
October 10, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Manfred Reiffen, Rudolph Hurnaus, Robert Sauter, Wolfgang Grell, Eckhard Rupprecht
Abstract: The invention relates to N,N-disubstituted arylcycloalkylamines of general formula ##STR1## wherein n, m, A, X and R.sup.1 to R.sup.7 are defined as in claim 1, the isomers, isomer mixtures and salts thereof, which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis.
Type:
Grant
Filed:
November 19, 1993
Date of Patent:
October 3, 1995
Assignee:
Karl Thomae GmbH
Inventors:
Roland Maier, Peter Muller, Eberhard Woitun, Rudolf Hurnaus, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
Abstract: The invention relates to carboxylic acid derivatives of general formulaA--B--C--D--E--F--G (I)whereinA to G are defined as in claim 1, the tautomers thereof, the stereoisomers thereof including the mixtures thereof and the addition salts thereof, particularly the physiologically acceptable salts with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably inhibitory effects on aggregation, and to pharmaceutical compositions containing the compounds and processes for preparing them.
Type:
Grant
Filed:
October 12, 1993
Date of Patent:
August 15, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Helmut Pieper, Gunter Linz, Frank Himmelsbach, Volkhard Austel, Thomas Muller, Johannes Weisenberger, Brian Guth
Abstract: The invention relates to cyclic imino derivatives of general formula ##STR1## wherein A to G, R.sub.1, Z.sub.1 to Z.sub.6, X and Y are defined as in claim 1, the tautomers, stereoisomers and mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting properties, pharmaceutical compositions which contain these compounds and processes for preparing them.
Type:
Grant
Filed:
August 28, 1992
Date of Patent:
July 18, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Volhard Austel, Helmut Pieper, Frank Himmelsbach, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
Abstract: The invention relates to new arylsulphonamides of the formula ##STR1## (wherein A, B and R.sub.1 to R.sub.6 are as defined in claim 1, the enantiomers, the cis- and trans-isomers thereof where R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof, more particularly for pharmaceutical use the physiologically acceptable addition salts thereof with inorganic or organic bases, if R.sub.6 represents a hydroxy group) which have useful pharmacological properties, particularly antithrombotic activities and thromboxane-mediating activities. Furthermore, the new compounds are also thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH). They also have an effect on PGE.sub.2 production.
Type:
Grant
Filed:
November 18, 1993
Date of Patent:
June 20, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Armin Heckel, Josef Nickl, deceased, Rainer Soyka, Wolfgang Eisert, Thomas Muller, Johannes Weisenberger, Christopher Meade, Gojko Muacevic
Abstract: Heterobiaryl derivatives of the formulaR.sub.1 NH--X.sub.1 --X.sub.2 --X.sub.3 --Y.sub.1 --Y.sub.2 --Y.sub.3 --Y.sub.4 --E (I)whereinR.sub.1, X.sub.1 to X.sub.3 and Y.sub.1 to Y.sub.4 are as defined herein, the tautomers, stereoisomers and mixtures thereof, and the salts, particularly the physiologically acceptable salts, thereof with organic or inorganic acids or bases. The derivatives have valuable pharmacological properties, such as inhibiting cell-cell aggregation and cell-matrix interactions.
Type:
Grant
Filed:
October 14, 1992
Date of Patent:
May 23, 1995
Assignee:
Karl Thomae GmbH
Inventors:
Guenter Linz, Helmut Pieper, Frank Himmelsbach, Austel: Volkhard, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
Abstract: The invention relates to benzimidazolyl derivatives of general formula ##STR1## wherein R.sub.1 to R.sub.3 are defined as in claim 1, the mixtures of position isomers thereof and the salts thereof, which have valuable pharmacological properties, particularly the effect of extending the thrombin time, a thrombin inhibiting effect and an inhibiting effect on related serine proteases such as trypsin, pharmaceutical compositions containing this compound and processes for the preparation thereof.
Type:
Grant
Filed:
February 8, 1993
Date of Patent:
February 21, 1995
Assignee:
Karl Thomae GmbH
Inventors:
Armin Heckel, Robert Sauter, Manfred Psiorz, Klaus Binder, Thomas Mueller, Rainer Zimmermann
Abstract: The invention relates to benzimidazoles of general formula ##STR1## wherein R.sub.1 to R.sub.4 are as defined herein, the 1-, 3-isomer mixtures thereof and the addition salts thereof. The new compounds are useful, in particular, as angiotensin antagonists.
Type:
Grant
Filed:
March 30, 1994
Date of Patent:
January 31, 1995
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Berthold Narr, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth, Uwe Ries
Abstract: A method for the prevention of adhesions to body organs and parts of organs caused by therapeutic intervention by applying a pharmaceutical composition of tissue plasminogen activator and an aqueous hydroxyethylcellulose hydrogel.
Type:
Grant
Filed:
October 13, 1993
Date of Patent:
November 15, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Helmut Franz, Thomas Muller, Wolfgang Eisert
Abstract: Pharmaceutical forms of pimobendan for oral administration comprising citric acid, whereby a constant, satisfactory resorption is ensured even when there are major pH fluctuations in the gastrointestinal tract.
Type:
Grant
Filed:
March 16, 1993
Date of Patent:
November 15, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Peter Gruber, Willy Roth, Gottfried Schepky
Abstract: The invention relates to a process and apparatus for the controlled release of metered quantities of finely divided solids with one or more regulated venturi nozzles for the purpose of applying lubricant or separating compound to the stressed surfaces of pressing tools in tablet making machines or for applying finely divided solids to solid carrier materials particularly in the fields of pharmaceuticals, foodstuffs or catalysts.
Type:
Grant
Filed:
May 21, 1993
Date of Patent:
October 18, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Josef Boldis, Volker I. Glasel, Ekkehard Flaischlen, Gunther M. Voss
Abstract: The present application relates to the uses of phenylacetic acid benzylamides and new (S)(+)-2-ethoxy-4-[N-[1-2-piperidino-phenyl)-3-methyl-1-butyl]-aminocarbon ylmethyl]benzoic acid and the salts thereof, which have valuable pharmacological properties, namely an effect on the intermediate metabolism, but particularly the effect of lowering blood sugar.
Type:
Grant
Filed:
July 24, 1992
Date of Patent:
May 17, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, deceased, Robert Sauter, Manfred Reiffen, Eckhard Ruprecht
Abstract: New pyridyl derivatives of the formula ##STR1## wherein R.sub.1 to R.sub.6, A, X and n are as defined herein, the enantiomers thereof, the cis- and trans-isomers thereof if R.sub.4 and R.sub.5 together represent a carbon-carbon bond, and the addition salts thereof. The new pyridyl derivatives have antithrombotic activity and thromboxane-mediated activities. The new compounds are also simultaneously thromboxane antagonists (TRA) and thromboxane synthesis inhibitors (TSH). They also have an effect on PGE.sub.2 -production.
Type:
Grant
Filed:
January 19, 1993
Date of Patent:
February 15, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Rainer Soyka, Wolfgang Eisert, Thomas Mueller, Johannes Weisenberger
Abstract: The invention relates to cyclic urea derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
Type:
Grant
Filed:
March 11, 1992
Date of Patent:
January 4, 1994
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Wolfgang Eisert