Patents Assigned to Thomas GmbH
  • Trisubstituted pyrimido [5,4-d] pyrimidines for modulating multi-drug resistance and pharmaceutical compositions containing these compounds
    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
  • Amino acid derivatives, pharmaceutical compositions containing these compounds and their use in the treatment of obesity
    Patent number: 5616620
    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
  • (1-(2,3 or 4-N-morpholinoalkyl)-imidazol-4-yl)-benizimidazol-1-yl-methyl]-biphenyls useful as angiotensin-II antagonists
    Patent number: 5614519
    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
  • Cyclic compounds and pharmaceutical compositions containing them
    Patent number: 5612335
    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
  • Condensed diazepinones, processes for preparing them and agents containing these compounds for treating diseases of the central nervous system and for promoting cerebral blood circulation
    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
  • Bicyclic heterocyclic compounds, pharmaceutical preparations containing these compounds and processes for their preparations
    Patent number: 5607944
    Abstract: The invention relates to bicyclic heterocyclic compounds of general formula ##STR1## wherein A to F, Y.sub.1 and Y.sub.2 are defined as in claim 1, the tautomers thereof, the stereoisomers thereof including their mixtures, and 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 as well as new intermediate products of general formula Ia.
    Type: Grant
    Filed: July 31, 1995
    Date of Patent: March 4, 1997
    Assignee: Karl Thomae GmbH
    Inventors: G unter Linz, Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Thomas M uller, Johannes Weisenberger, Brian Guth
  • Substituted thiazoles and oxazoles and 2-hydroxy-morpholines
    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
  • (Alkanesultam-1-yl)-benzimidazol-1-yl)-1yl)-methyl-biphenyls useful as angiotensin-II antagonists
    Patent number: 5602127
    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-(butanesultam-1-yl)benzimidazol-1-yl)-methyl]-b iphenyl-2-carboxylic acid.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: February 11, 1997
    Assignee: Karl Thomae GmbH
    Inventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
  • Biphenyl derivatives, pharmaceutical compositions containing these compounds and processes for preparing them
    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
  • Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biph enyls useful as angiotensin-II antagonists
    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
  • Cyclic imino derivatives and pharmaceutical compositions containing them
    Patent number: 5591769
    Abstract: The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: January 7, 1997
    Assignee: Karl Thomae GmbH
    Inventors: Frank Himmelsbach, Volkhard Austel, Helmut Pieper, Wolfgang Eisert, Thomas Mueller, Johannes Weisenberger, Guenter Linz, Gerd Krueger
  • Benzimidazoles useful as angiotensin-11 antagonists
    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
  • Benzimidazoles, pharmaceutical compositions containing these compounds and processes for preparing them
    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
  • Methods and preparations for preventing adhesions to organs and parts of organs
    Patent number: 5578305
    Abstract: Pharmaceutical composition for prevention of adhesions to body organs or parts of body organs within a body cavity at a site of inflammation is disclosed. The pharmaceutical composition contains t-PA and an aqueous hydroxyethylcellulose hydrogel. The method involves applying the aforementioned pharmaceutical composition to a site of inflammation in a body cavity.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: November 26, 1996
    Assignee: Karl Thomae GmbH
    Inventors: Helmut Franz, Thomas Muller, Wolfgang Fisert
  • Cyclic imino derivatives, processes for preparing them and pharmaceutical compositions containing these compounds
    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
  • Benzimidazoles and pharmaceutical compositions containing them
    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
  • Heterobiaryl derivatives
    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
  • One-pot mixer/granulator/dryer
    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
  • Low viscosity, highly concentrated surfactant suspension
    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
  • Benzimidazoles and medicaments containing these compounds
    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