Abstract: The invention relates to cyclic derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined in claim 1, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing the compounds and processes for preparing them.
Type:
Grant
Filed:
December 17, 1996
Date of Patent:
October 27, 1998
Assignee:
Karl Thomae GmbH
Inventors:
F. Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Brian Guth, Thomas Muller, Johannes Weisenberger
Abstract: Pyrimido?5,4-d!pyrimidines of the general formula ##STR1## which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are:4-?(3-Chloro-4-fluorophenyl)amino!-6-?1-methyl-4-piperidinylamino!pyrimido? 5,4-d!pyrimidine, and4-?(3-Chloro-4-fluorophenyl)amino!-6-?trans-4-dimethyl-aminocycohexylamino! pyrimido?5,4-d!pyrimidine.
Type:
Grant
Filed:
March 5, 1997
Date of Patent:
October 13, 1998
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Georg Dahmann, Thomas von Ruden, Thomas Metz
Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R,S)-N.sup.2 -(diphenylacetyl)-N-?(4-hydroxyphenyl)methyl!-N.sup.5 -(1H-imidazol-2-yl)-ornithinamide.
Type:
Grant
Filed:
December 11, 1996
Date of Patent:
September 15, 1998
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike Andrea Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.
Type:
Grant
Filed:
August 1, 1996
Date of Patent:
April 7, 1998
Assignee:
Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
Abstract: This document describes O-acyl-4-phenyl-cycloalkanols of general formula I ##STR1## wherein n denotes the number 0 or 1, m denotes the number 1 or 2, p denotes the number 0 or 1, R.sup.1 and R.sup.2 each denote hydrogen, lower alkyl, alkenyl or alkynyl, which may optionally also be substituted, or together with the nitrogen atom between them denote 5- to 7-membered saturated, monocyclic, heterocyclic rings which may optionally also be interrupted by an oxygen or sulphur atom or by an imino group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 denote hydrogen or lower alkyl, R.sup.5 additionally denotes lower alkoxy, R.sup.7 denotes hydrogen, cycloalkyl, phenyl or substituted phenyl, naphthyl, tetrahydronaphthyl, thienyl, furyl or pyridyl and A denotes a chemical bond or alkyl, alkenyl or alkynyl having up to 17 carbon atoms, and also processes for preparing them, pharmaceutical compositions containing these compounds and the use of these pharmaceutical compositions which intervene in cholesterol biosynthesis.
Type:
Grant
Filed:
January 17, 1997
Date of Patent:
March 10, 1998
Assignee:
Karl Thomae GmbH
Inventors:
Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
Abstract: The present invention relates to pyrimido?5,4-d!pyrimidines of the general formula ##STR1## in which R.sub.a to R.sub.c are as defined herein, their tautomers, their stereoisomers and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibiting action on signal transduction mediated by tyrosine kinases, their use for the treatment of diseases, in particular tumor diseases.
Type:
Grant
Filed:
September 7, 1995
Date of Patent:
January 13, 1998
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Thomas von Ruden, Georg Dahmann, Thomas Metz
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:
February 20, 1996
Date of Patent:
November 4, 1997
Assignee:
Karl Thomae GmbH
Inventors:
Berthold Narr, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth, Uwe Ries
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:
March 21, 1995
Date of Patent:
October 28, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Armin Heckel, Josef Nickl, deceased, Rainer Soyka, Wolfgang Eisert, Thomas Muller, Johannes Weisenberger, Christopher Meade, Gojko Muacevic
Abstract: The invention relates to cyclic urea derivatives of general formula I ##STR1## wherein R.sub.a, R.sub.b, X and Y are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation inhibiting effects, and to drugs containing the compounds and processes for preparing them.
Type:
Grant
Filed:
September 10, 1993
Date of Patent:
October 28, 1997
Assignee:
Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Volkhard Austel, Gunter Linz, Helmut Pieper, Brian Guth, Thomas Muller, Johannes Weisenberger
Abstract: The invention relates to new labelled fibrinogen receptor antagonists which have an affinity for the receptor which is comparable to or greater than that of .sup.125 I-fibrinogen and whose binding is not disrupted by foreign proteins.
Type:
Grant
Filed:
May 23, 1995
Date of Patent:
October 14, 1997
Assignee:
Dr. Karl Thomae, GmbH
Inventors:
Johannes Weisenberger, Hans-Dieter Schubert, Gunter Linz, Karl-Heinz Switek, Frank Himmelsbach
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:
August 29, 1995
Date of Patent:
July 22, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Thomas Mueller, Johannes Weisenberger, Wolfgang Eisert
Abstract: New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
Type:
Grant
Filed:
April 13, 1995
Date of Patent:
June 24, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Eberlein, Gerhard Mihm, Wolfhard Engel, Klaus Rudolf, Henri Doods, Harald Ziegler, Michael Entzeroth
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:
June 1, 1995
Date of Patent:
April 29, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Josef Boldis, Volker I. Glasel, Ekkehard Flaischlen, Gunther M. Voss
Abstract: The invention relates to trisubstituted pyrimido [5,4-d]-pyrimidines of general formula ##STR1## (wherein R.sub.a, R.sub.b and R.sub.c are defined as in claim 1) and the salts thereof, more particularly for pharmaceutical use the physiologically acceptable salts thereof, which have, inter alia, valuable pharmacological properties, particularly in chemotherapy a sensitizing effect on resistant tumors, the use thereof and processes for preparing them.
Abstract: Amino acid derivatives, suitable for the treatment of obesity. The following compound is exemplary of the class: (R)-N2-(diphenylacetyl)-N-[(4-hydroxyphenyl) methyl]-argininamide-acetate.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
April 1, 1997
Assignee:
Karl Thomae GmbH
Inventors:
Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Gerhard Mihm, Henri Doods, Heike A. Wieland, Klaus-Dieter Willim, Jurgen Krause, Horst Dollinger, Franz Esser, Gerd Schnorrenberg, Michael Entzeroth, Wolfgang Wienen
Abstract: Angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl. An exemplary compound is: 4'-[(2-n-propyl-4-methyl-6-(1-(2-N-morpholinoethyl)-imidazol-4-yl)-benzimi dazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
March 25, 1997
Assignee:
Karl Thomae GmbH
Inventors:
Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. Antonius van Meel, Wolfgang Wienen, Michael Entzeroth
Abstract: The invention relates to cyclic derivatives of general formula ##STR1## wherein R.sub.a, R.sub.b, X and Y are as defined in claim 1, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing the compounds and processes for preparing them.
Type:
Grant
Filed:
May 2, 1995
Date of Patent:
March 18, 1997
Assignee:
Karl Thomae GmbH
Inventors:
F. Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Brian Guth, Thomas Muller, Johannes Weisenberger
Abstract: New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.
Type:
Grant
Filed:
June 1, 1995
Date of Patent:
March 11, 1997
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Eberlein, Gerhard Mihm, Wolfhard Engel, Klaus Rudolf, Henri Doods, Harald Ziegler, Michael Entzeroth