Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
Type:
Application
Filed:
December 17, 2008
Publication date:
June 25, 2009
Applicant:
Dr. Karl Thomae GmbH
Inventors:
Klaus RUDOLF, Wolfgang EBERLEIN, Wolfhard ENGEL, Helmut PIEPER, Henri DOODS, Gerhard HALLERMAYER, Michael ENTZEROTH, Wolfgang WIENEN
Abstract: The present invention relates to modified amino acids of general formula
wherein
A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
Type:
Grant
Filed:
October 12, 1999
Date of Patent:
February 5, 2002
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Klaus Rudolf, Wolfgang Eberlein, Wolfhard Engel, Helmut Pieper, Henri Doods, Gerhard Hallermayer, Michael Entzeroth, Wolfgang Wienen
Abstract: The invention relates to a sampling device, in which the site of separation from the microbiologically contaminated environment is constructed as a sterile protective gas current according to the laminar air-flow principle under a housing bell (7), the site of connection of the inner tube (11) to the sample tube (10) being so designed that it occurs inside to just below the housing bell (7), fixedly or with no fixed connection, and for automatic operation occurs just below the housing bell (7), with no fixed connection.
Abstract: The invention relates to a strong homologous promoter from hamsters. In particular, it relates to the promoter of a gene which codes for the Ubiquitin-S27a-fusion protein. The promoter can be used in processes for preparing heterologous gene products in culture cells, particularly CHO cells.
Type:
Grant
Filed:
September 30, 1998
Date of Patent:
May 16, 2000
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Barbara Enenkel, Frank Gannon, Klaus Bergemann, Wolfgang Noe
Abstract: The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
Type:
Grant
Filed:
May 29, 1998
Date of Patent:
March 21, 2000
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfgang Eberlein, Wolfhard Engel, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim
Abstract: The specification describes a pharmaceutical combination consisting of dipyridamole or mopidamol and acetylsalicylic acid or the physiologically acceptable salts thereof, processes for preparing this pharmaceutical combination and the use thereof for the controlled prevention of clot formation.
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 oncoses, and their preparation. Exemplary compounds are:(a) 4-(5-indolylamino)-6-morpholinopyrimido[5,4-d]pyrimidine;(b) 4-(5-indolylamino)-6-[trans-(4-hydroxycyclohexyl)amino]pyrimido[5,4-d]pyri midine;(c) 4-[(3-chloro-4-fluorophenyl)amino]-6-[4-(morpholinocarbonylmethyl)-1-piper azinyl]pyrimido[5,4-d]pyrimidine;(d) 4-[(3-chloro-4-fluorophenyl)amino]-6-[(4-morpholinyl)amino]pyrimido[5,4-d] pyrimidine;(e) 4-[(3-chloro-4-fluorophenyl)amino]-6-(4-picolylamino)pyrimido[5,4-d]pyrimi dine;(f) 4-[(3-chloro-4-fluorophenyl)amino]-6-[1-trifluoroacetyl-4-piperidinylamino ]pyrimido[5,4-d]pyrimidine;(g) 4-[(3-chloro-4-fluorophenyl)amino]-6-(endo-tropinylamino)pyrimido[5,4-d]py rimidine; and,(h) 4-[(3-chloro-4-fluorophenyl)amino]-6-(exo-tropinylamino)pyrimido[5,4-d]pyr imidine.
Type:
Grant
Filed:
March 5, 1997
Date of Patent:
November 2, 1999
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Georg Dahmann, Thomas von Ruden, Thomas Metz
Abstract: Compounds that inhibit the enzyme 2,3-epoxysqualene-lanosterol-cyclase and cholesterol biosynthesis, of the 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 the denote 5- to 7-membered saturated, monocyclic or heterocyclic rings which may optionally also be interrupted by an oxygen or sulfur 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 having up to 17 carbon atoms.
Type:
Grant
Filed:
December 5, 1997
Date of Patent:
October 5, 1999
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Eberhard Woitun, Roland Maier, Peter Muller, Rudolf Hurnaus, Michael Mark, Bernard Eisele, Ralph-Michael Budzinski, Gerhard Hallermayer
Abstract: The invention relates to new amino acid derivatives of general formula ##STR1## wherein R, U, V, Y, n, m and R.sup.1 to R.sup.3 are defined as in claim 1, their tautomers, diastereomers, enantiomers, mixtures thereof and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly selective NPY-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
Type:
Grant
Filed:
May 29, 1998
Date of Patent:
October 5, 1999
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Wolfhard Engel, Wolfgang Eberlein, Klaus Rudolf, Henri Doods, Heike-Andrea Wieland, Klaus-Dieter Willim
Abstract: The present invention relates to phenyl amidines of general formula (I), ##STR1## in which R.sup.1 to R.sup.5 are as defined in claim 1, their tautomers, their stereoisomers and their mixtures and their salts, especially their physiologically acceptable salts with inorganic or organic acids or bases also having valuable pharmacological properties, preferably aggregation-limiting effects, producing them.
Type:
Grant
Filed:
December 17, 1997
Date of Patent:
September 28, 1999
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Volkhard Austel, Gunther Linz, Helmut Pieper, Brian Guth, Johannes Weisenberger
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:
November 26, 1997
Date of Patent:
July 13, 1999
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
Abstract: The present invention relates to piperazine derivatives of the general formula ##STR1## in which R.sub.a, Y.sub.1 to Y.sub.3 and E are defined herein, tautomers thereof, stereoisomers thereof, including their mixtures, and salts thereof, and in particular physiologically tolerated salts thereof with inorganic or organic acids or bases. These compounds have valuable pharmacological properties, such as aggregation-inhibiting activity. This invention also relates to medicaments comprising these compounds and to processes for the preparation of these compounds.
Type:
Grant
Filed:
December 21, 1995
Date of Patent:
July 13, 1999
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Helmut Pieper, Volkhard Austel, Frank Himmelsbach, Gunter Linz, Brian Guth, Johannes Weisenberger
Abstract: The invention relates to benzothiazoles and benzoxazoles of general formula ##STR1## wherein R.sup.1 to R.sup.3, X, Z and n are defined as in claim 1, the enantiomers, diastereomers and salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
Type:
Grant
Filed:
October 28, 1997
Date of Patent:
July 6, 1999
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Peter Muller, Rudolph Hurnaus, Roland Maier, Michael Mark, Bernhard Eisele, Ralph-Michael Budzinski, Leo Thomas, Gerhard Hallermayer
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:
May 28, 1997
Date of Patent:
March 9, 1999
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Volkhard Austel, Gunter Linz, Helmut Pieper, Brian Guth, 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:
May 1, 1997
Date of Patent:
December 22, 1998
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Guenter Linz, Johannes Weisenberger, Wolfgang Eisert, Thomas Mueller
Abstract: A bacterial host is described which is transformed by a plasmid coding for a polypeptide precursor wherein the host comprises a multi-enzyme complex capable of reacting with the expressed polypeptide precursor to produce a polypeptide comprising at least one dehydroamino acid and/or at least one lanthione bridge. A process for producing a polypeptide comprising at least one dehydroamino acid and/or at least one lanthione bridge, such as gallidermin, is also described. A plasmid capable of transforming a bacterial host is additionally described.Also disclosed are recombinant DNA molecules which specify Epi B, Epi C, Epi D, Epi P and Epi Q, enzymes which are involved in the biosynthesis of lantibiotic epidermin.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
December 1, 1998
Assignee:
Dr. Karl Thomae GmbH
Inventors:
Karl-Dieter Entian, Friedrich Gotz, Norbert Schnell, Johannes Augustin, Germar Engelke, Ralf Rosenstein, Cortina Kaletta, Cora Klein, Bernd Wieland, Thomas Kupke, Gunther Jung, Roland Kellner
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