Patents Assigned to Dr. Karl Thomae GmbH
  • Patent number: 5707989
    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
  • Patent number: 5681961
    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
  • Patent number: 5677466
    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
  • Patent number: 5650424
    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
  • Patent number: 5641772
    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
  • Patent number: 5624690
    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
  • Patent number: 5618814
    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.
    Type: Grant
    Filed: August 2, 1994
    Date of Patent: April 8, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Armin Heckel, Uwe Bamberger, Annerose Mauz
  • Patent number: 5610155
    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
  • Patent number: 5604225
    Abstract: Substituted thiazoles, oxazoles and 2-hydroxy morpholine compounds useful in the treatment of diabetes mellitus and obesity are described.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: February 18, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Manfred Reiffen, Rudolf Hurnaus, Robert Sauter, Wolfgang Grell, Eckhard Rupprecht
  • Patent number: 5597825
    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: May 16, 1994
    Date of Patent: January 28, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, G unter Linz, Thomas M uller, Wolfgang Eisert, Johannes Weisenberger
  • Patent number: 5594003
    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 compound is:4'-[(2-Ethyl-4-methyl-6-(5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl)-ben zimidazol-1-yl)-methyl]-biphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: January 14, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5591762
    Abstract: Disclosed herein are 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:(a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl] methyl]-biphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: January 7, 1997
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5587393
    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: September 1, 1994
    Date of Patent: December 24, 1996
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Berthold Narr, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth, Uwe Ries
  • Patent number: 5576444
    Abstract: Cyclic imino derivatives of the formulaB--X.sub.2 --X.sub.1 --A--Y--E (I)wherein A, B, E, X.sub.1, X.sub.2 and Y are as defined herein, the stereoisomers, tautomers, mixtures and addition salts thereof, pharmaceutical compositions containing these compounds and processes for preparing them. The cyclic imino derivatives are useful as inhibitors of cell-cell and cell-matrix interactions, e.g., thrombocyte aggregation.
    Type: Grant
    Filed: April 26, 1993
    Date of Patent: November 19, 1996
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Austel Volkhard, Helmut Pieper, Guenter Linz, Johannes Weisenberger, Thomas Mueller
  • Patent number: 5565469
    Abstract: Angiotensin-II inhibiting benzimidazoles, useful for the treatment of hypertension.
    Type: Grant
    Filed: March 13, 1995
    Date of Patent: October 15, 1996
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Gerhard Mihm, Norbert Hauel, Uwe Ries, Jacobus C. Antonius van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5563268
    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: January 19, 1995
    Date of Patent: October 8, 1996
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Guenter Linz, Helmut Pieper, Frank Himmelsbach, Volkhard Austel, Thomas Mueller, Johannes Weisenberger, Elke Seewaldt-Becker
  • Patent number: 5560122
    Abstract: The invention relates to a one-pot mixer/granulator/dryer constituting a single step or one-pot production apparatus for successively mixing, moist-granulating and drying solid pharmaceutical products, for example in the manufacture of powdered products, pellets or granules. The dryer according to the invention has a substantially improved drying performance compared with conventional production equipment. The high efficiency of drying is achieved by the simultaneous use of four different drying mechanisms.
    Type: Grant
    Filed: May 19, 1994
    Date of Patent: October 1, 1996
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Kurt Bauer, Wolfram Carius, Gerold Duschler
  • Patent number: 5552161
    Abstract: Low viscosity, highly concentrated surfactant suspensions for replacement therapy In diseases of the respiratory tract are described. The suspensions are characterised in that they contain calcium and/or magnesium ions bound to the surfactant and unbound in the suspension agent, as well as containing a certain amount of common salt.
    Type: Grant
    Filed: May 1, 1995
    Date of Patent: September 3, 1996
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Bernd Disse, Eberhard Weller, Robert Becker
  • Patent number: 5541229
    Abstract: The invention relates to benzimidazoles of the formula ##STR1## in which R.sub.1 to R.sub.2 are as defined in claim 1,1 and 3 isomer mixtures thereof and addition salts thereof which have valuable properties.In particular, the novel compounds are angiotensin II antagonists.
    Type: Grant
    Filed: April 13, 1994
    Date of Patent: July 30, 1996
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Berthold Narr, Andreas Bomhard, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth
  • Patent number: 5521177
    Abstract: The invention relates to benzimidazoles of general formula ##STR1## Exemplary compounds are: (a) 4'-[[2-Ethyl-4-methyl-6-[(2-dimethylamino-3,4-dioxo-1-cyclobuten-1-yl)amin o]-1H-benzimidazol-1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl,(b) 4'-[[2-n-Propyl-4-methyl-6-(2-cyano-3,3-dimethyl-guanidino)-1H-benzimidazo l-1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl,(c) 4'-[[2-n-Propyl-4-methyl-6-(2,2-dicyano-1-dimethylamino-etheneamino)-1H-be nzimidazol -1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl,(d) 4'-[[2-n-Propyl-4-methyl-6-(1-morpholino-2-nitro-etheneamino)-1H-benzimida zol -1 -yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl, and(e) 4'-[[2-n-Propyl-4-methyl-6-(1,1-dimethylamino-2-nitro-etheneamino)-1H-benz imidazol -1-yl]-methyl]-2-(1H-tetrazol-5-yl)-biphenyl.The new compounds are angiotensin-antagonists.
    Type: Grant
    Filed: October 4, 1993
    Date of Patent: May 28, 1996
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Uwe Ries, Norbert Hauel, Jacques van Meel, Wolfgang Wienen, Michael Entzeroth