Abstract: The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in Claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.
Type:
Grant
Filed:
April 10, 2009
Date of Patent:
December 28, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Gerald Juergen Roth, Armin Heckel, Thorsten Lehmann-Lintz, Joerg Kley, Frank Hilberg, Jacobus C. A. Van Meel, Ulrike Tontsch-Grunt
Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.
Type:
Application
Filed:
September 1, 2010
Publication date:
December 23, 2010
Applicant:
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
Inventors:
Matthias HOFFMANN, Matthias GRAUERT, Martin STEEGMAIER, Gisela SCHNAPP, Anke BAUM, Jens Juergen QUANT, Flavio SOLCA, Florian COLBATZKY
Abstract: A pharmaceutical composition comprising: (a) a salt of formula 1 wherein: X? is an anion with a single negative charge; and (b) a steroid 2, processes for preparing such pharmaceutical composition, and their use in the treatment of respiratory complaints.
Type:
Grant
Filed:
April 20, 2006
Date of Patent:
December 14, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Rolf Banholzer, Helmut Meissner, Gerd Morschhaeuser, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck, Christopher John Montague Meade, Michel Pairet
Abstract: A pharmaceutical composition comprising an anticholinergic and at least one additional active ingredient selected from among corticosteroids, dopamine agonistes, PDE-IV inhibitors, NK1-antagonists, endothelin antagonists, antihistamines, and EGFR-kinase inhibitors, processes for preparing them and their use in the treatment of respiratory diseases.
Type:
Application
Filed:
August 13, 2010
Publication date:
December 9, 2010
Applicant:
Boehringer Ingelheim Pharma GmbH & Co. Kg.
Inventors:
Michel Pairet, Michael P. Pieper, Christopher John Montague Meade, Richard Reichl, Christel Schmelzer, Birgit Jung
Abstract: The invention relates to DNA-sequences, especially transcription- or expression-enhancing elements (TE elements) and their use on an expression vector in conjunction with an enhancer, a promoter, a product gene and a selectable marker. The invention describes Sequence No. 1 and TE elements TE-01, -02, -03, -04, -06, -07, -08, -10, -11 or -12. Because of their small size, TE-06, TE-07 or TE-08 are particularly preferred. Sequence No. 1 originates from a sequence region located upstream from the coding region of the Ub/S27a gene from CHO cells. TE elements bring about an increase in the expression of the product gene, particularly when stably integrated in the eukaryotic genome, preferably the CHO-DG44 genome. Chromosomal positional effects are thereby overcome, shielded or cancelled out. In this way the proportion of high producers in a transfection mixture and also the absolute expression level are increased up to seven-fold.
Abstract: The invention relates to a method for producing 1,3-dioxolane-2-ones of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1 to R5 have the meanings indicated in the claims and the description. The invention further relates to a method for producing 2-hydroxy carboxylic acid esters of general formula (5) with or without isolation of the intermediate in the form of a derivative of the 1,3-dioxolane-2-one of general formula (3) in basic reaction conditions by reesterifying the respective ester of general formula (1) in which R1, R2, and R6 have the meanings indicated in the claims and the description. The method according to the invention allows the reaction to take place in very gentle basic conditions, causing fewer secondary reactions and providing a greater yield than reactions in highly polar aprotic solvents. Acid-sensitive and/or temperature-sensitive compounds can be synthesized.
Type:
Application
Filed:
September 3, 2008
Publication date:
December 2, 2010
Applicant:
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
Abstract: The invention relates to methods of increasing the titre of a protein of interest in a cell as well as the improved production and purification of optimised biomolecules, one component of which is the domain CH3. A frequently observed effect in biomolecules is the cleaving of the C-terminal amino acid(s), e.g. the C-terminal lysine. The usually incomplete processing of the heavy chain of antibodies for example leads to product heterogeneity. To prevent this product heterogeneity the corresponding codon of the C-terminal lysine of the heavy antibody chain has been deleted by recombinant DNA technology. These optimised antibodies lead to a product titre which is higher than in the wild-type. In addition, they prove advantageous during purification by having better elution characteristics as a result of the reduced charge heterogeneity.
Type:
Application
Filed:
August 28, 2008
Publication date:
November 25, 2010
Applicant:
BOEHRINGER INGELHEIM PHARMA GMBH & CO KG
Inventors:
Dorothee Ambrosius, Barbara Enenkel, Christian Eckermann
Abstract: A new method for selecting clones and recloning mammalian cells which are of importance for the production of biopharmaceuticals, preferably hamster or mouse myeloma cells, with a high degree of automation and throughput. The invention relates to methods of depositing and replicating single cell clones of the cells in question. The invention also relates to methods of preparing proteins using cells which have been obtained and replicated by single cell deposition as well as compositions which allow the replication of single cells.
Type:
Grant
Filed:
August 19, 2004
Date of Patent:
November 16, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Ralf Otto, Barbara Enenkel, Juergen Fieder, Thomas Krieg
Abstract: The present invention relates to a process for preparing tablets of pramipexole dihydrochloride. In particular, the present invention relates to a process for preparing tablets of pramipexole dihydrochloride wherein the tablets exhibit enhanced storage stability properties.
Type:
Application
Filed:
July 1, 2010
Publication date:
October 21, 2010
Applicant:
Boehringer Ingelheim Pharma GmbH & Co. KG
Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.
Type:
Grant
Filed:
May 30, 2008
Date of Patent:
October 19, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Abstract: A cartridge for propellant-free administration of a liquid pharmaceutical composition by inhalation includes: an elongate displacing device including an upper end and a lower end, the lower end for at least partial insertion into a container; a cartridge chamber disposed at the lower end of the displacing device and operable store a pharmaceutical formulation, the cartridge chamber including at least one pierceably sealed opening; and a cannula guide extending from the upper end of the displacing device to the cartridge chamber, wherein insertion of a cannula through the guide pierces the sealed opening and releases the pharmaceutical formulation into a liquid solvent in the container to form the liquid pharmaceutical composition.
Type:
Grant
Filed:
July 11, 2005
Date of Patent:
September 14, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Abstract: The invention relates to the optical measurement of fill level in the aseptic bottling or packaging of biopharmaceuticals. The process according to the invention allows in particular in-process fill level measurement of primary packaging means filled with protein solution with small volumes and with considerable variations in the packaging means. The invention also relates to an apparatus according to FIG. 5B.
Type:
Application
Filed:
December 4, 2009
Publication date:
September 2, 2010
Applicant:
BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
Inventors:
Christina LICHTBLAU, Stefan BASSARAB, Karoline BECHTOLD-PETERS, Christian BRADER
Abstract: A pharmaceutical composition comprising a compound of formula 1 wherein: n is 1 or 2; R1 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R2 is hydrogen, C1-C4-alkyl, halogen, OH, or —O—C1-C4-alkyl; R3 is hydrogen, C1-C4-alkyl, OH, halogen, —O—C1-C4-alkyl, —O—C1-C4-alkylene-COOH, or —O—C1-C4-alkylene-CO—O—C1-C4-alkyl, or an acid addition salt thereof with a pharmacologically acceptable acid, or a solvate or hydrate thereof; and a pharmaceutically acceptable excipient or carrier, and methods for using the pharmaceutical formulation in the treatment of chronic obstructive pulmonary disease (COPD).
Type:
Grant
Filed:
October 27, 2008
Date of Patent:
August 31, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Ingo Konetzki, Kurt Schromm, Hermann Schollenberger, Sabine Pestel, Andreas Schnapp, Thierry Bouyssou, Frank Buettner, Claudia Heine, Klaus Rudolf, Philipp Lustenberger, Christoph Hoenke
Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.
Type:
Grant
Filed:
September 6, 2005
Date of Patent:
August 31, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Matthias Hoffmann, Matthias Grauert, Martin Steegmaier, Anke Baum, Jens Jurgen Quant, Flavio Solca, Florian Colbatzky
Abstract: The invention relates to a method for producing a micronized, virtually anhydrous form of (1?,2?,4?,5?,7?)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide, said form per se, and the use thereof for producing a medicament, especially a medicament having an anticholinergic effect.
Type:
Application
Filed:
December 7, 2006
Publication date:
August 26, 2010
Applicant:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Norbert Rasenack, Mihael Walz, Michael Trunk, Hagen Graebner
Abstract: The invention relates to a new process for preparing tiotropium salts of general formula 1 wherein X? may have the meanings given in the claims and in the specification.
Type:
Application
Filed:
April 29, 2010
Publication date:
August 19, 2010
Applicant:
BOEHRINGER INGELHEIM PHARMA GmbH & Co. KG
Abstract: A pharmaceutical composition comprising an anticholinergic and at least one additional active ingredient selected from among corticosteroids, dopamine agonistes, PDE-IV inhibitors, NK1-antagonists, endothelin antagonists, antihistamines, and EGFR-kinase inhibitors, processes for preparing them and their use in the treatment of respiratory diseases.
Type:
Grant
Filed:
December 8, 2004
Date of Patent:
August 17, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Michel Pairet, Michael P. Pieper, Christopher John Montague Meade, Richard Reichl, Christel Schmelzer, Birgit Jung
Abstract: The invention relates to powdered preparations containing tiotropium for inhalation, processes for preparing them as well as their use in preparing a pharmaceutical composition for the treatment of respiratory complaints, particularly for the treatment of COPD (chronic obstructive pulmonary disease) and asthma.
Type:
Grant
Filed:
November 20, 2003
Date of Patent:
July 27, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Mareke Hartig, Michael Trunk, Michael Walz
Abstract: Disclosed are dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the pharmaceutical compositions, isomers, intermediates thereof and processes for preparing these dihydropteridinones. The compounds are useful the treatment and/or prevention of cancer, infections, inflammatory and autoimmune diseases.
Type:
Grant
Filed:
November 16, 2007
Date of Patent:
July 6, 2010
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Matthias Hoffman, Matthias Grauert, Trixi Brandl, Steffen Breitfelder, Christian Eickmeier, Martin Steegmaier, Gisela Schnapp, Anke Baum, Jens Jurgen Quant, Flavio Solca, Florian Colbatzky
Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterised by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
Inventors:
Georg DAHMANN, Frank HIMMELSBACH, Bernd KRIST, Martin LENTER, Alexander PAUTSCH, Gisela SCHNAPP, Martin STEEGMAIER, Helmut WITTNEBEN, Anthony S. PROKOPOWICZ, Walter SPEVAK, Andreas SCHOOP, Steffen STEURER