Patents Assigned to Boehringer Ingelheim Pharma GmbH & Co. KG
  • Purine derivatives, the preparation thereof and their use as pharmaceutical compositions
    Patent number: 7569574
    Abstract: The invention relates to new purine derivatives of general formula wherein R1 to R4 are defined as in the claims, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV), the preparation thereof, the use thereof for the prevention or treatment of diseases or conditions associated with an increased DPP-IV activity or capable of being prevented or alleviated by reducing the DPP-IV activity, particularly type I or type II diabetes mellitus, the pharmaceutical compositions containing a compound of general formula (I) or a physiologically acceptable salt thereof as well as processes for the preparation thereof.
    Type: Grant
    Filed: August 4, 2003
    Date of Patent: August 4, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Roland Maier, Frank Himmelsbach, Matthias Eckhardt, Elke Langkopf, Michael Mark, Ralf R. H. Lotz
  • Use of flow-cytrometric analysis to optimize cell banking strategies for CHO cells
    Patent number: 7569339
    Abstract: Production of biopharmaceuticals from CHO cells requires generation of master-, working- and post-production cell banks of high quality, partly under GMP conditions. An optimal cryopreservation strategy is needed for each new production cell line, particularly with regard to the desire to establish production processes that are completely devoid of serum or even any animal components and to ensure robust thaw performance for reliable production. Here we describe a novel strategy employing flow cytometric (FC) analysis of Annexin V-stained cells for high-throughput characterization of CHO cell banks. Our data show that this method enables evaluation of a cryopreservation procedure just 6 h after thaw.
    Type: Grant
    Filed: November 9, 2005
    Date of Patent: August 4, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co., KG
    Inventors: Hitto Kaufmann, Juergen Fieder, Ralf Otto
  • SUBSTITUTED NITROGEN-CONTAINING HETEROBICYCLES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS
    Publication number: 20090181958
    Abstract: The present invention relates to new substituted nitrogen-containing heterobicyclic compounds of general formula wherein B, X1 to X3 and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I as well as the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, and their stereoisomers have valuable pharmacological properties, particularly an antithrombotic activity and a factor Xa-inhibiting activity.
    Type: Application
    Filed: July 21, 2008
    Publication date: July 16, 2009
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Henning Priepke, Roland Pfau, Kai Gerlach, Uwe Ries, Wolfgang Wienen, Eckhart Bauer, Herbert Nar
  • Xanthine derivatives, the preparation thereof and their use as pharmaceutical compositions
    Patent number: 7560450
    Abstract: The present invention relates to substituted xanthines of general formula the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: July 14, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co., KG
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Elke Langkopf, Roland Maier, Michael Mark, Mohammad Tadayyon
  • Pyrimidine derivatives useful as inhibitors of PKC-theta
    Patent number: 7550473
    Abstract: Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: September 3, 2004
    Date of Patent: June 23, 2009
    Assignees: Boehringer Ingelheim Pharmaceuticals, Inc., Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Mario G. Cardozo, Derek Cogan, Charles Lawrence Cywin, George Dahmann, Darren DiSalvo, John David Ginn, Anthony S. Prokopowicz, III, Denice M. Spero, Erick Richard Roush Young
  • Indoline derivatives substituted in the 6-position, their preparation and their use as medicaments
    Patent number: 7547703
    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: September 7, 2006
    Date of Patent: June 16, 2009
    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
  • TWO-PIECE METAL CAPSULE FOR ACCOMMODATING PHARMACEUTICAL PREPARATIONS FOR POWDER INHALERS
    Publication number: 20090148515
    Abstract: The invention relates to novel two-piece metal capsules for accommodating pharmaceutical preparations to be used in powder inhalers as well as a method for producing said capsule. The inventive capsules are particularly impermeable to steam and oxygen.
    Type: Application
    Filed: April 13, 2007
    Publication date: June 11, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO., KG
    Inventor: Dieter Hochrainer
  • Substituted piperidines, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof
    Patent number: 7538115
    Abstract: The present invention relates to substituted piperidines of general formula wherein R, R2 to R5, A, X, Z and n are defined as in claim 1, the tautomers, diastereomers, enantiomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: May 26, 2005
    Date of Patent: May 26, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Rudolf Hurnaus, Klaus Rudolf, Stephan Georg Mueller, Dirk Stenkamp, Philipp Lustenberger, Alexander Dreyer, Kai Gerlach, Marcus Schindler, Kirsten Arndt, Eckhart Bauer
  • XANTHINE DERIVATES, THEIR PREPARATION AND THEIR USE IN PHARMACEUTICAL COMPOSITIONS
    Publication number: 20090131432
    Abstract: Compounds of formula (I) wherein R1 to R4 are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type I and type II diabetes mellitus, arthritis, obesity, allograft transplantation, or calcitonin-induced osteoporosis using these compounds.
    Type: Application
    Filed: January 16, 2009
    Publication date: May 21, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Michael MARK, Roland MAIER, Ralf R. H. LOTZ
  • Process for preparation of isochroman and derivatives thereof
    Patent number: 7534812
    Abstract: The present invention relates to an improved process for preparing compounds of formula 1 on an industrial scale, wherein R1, R2 and R3 are independently C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl or aryl; and R4 is H, OC1-6-alkyl, Oaryl, OH, C1-6-alkyl, halogen, CN or NO2.
    Type: Grant
    Filed: January 26, 2006
    Date of Patent: May 19, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventor: Ralf Lock
  • New method for preparing tiotropium salts
    Publication number: 20090118511
    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: January 5, 2009
    Publication date: May 7, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO., KG
    Inventors: Ralf LOCK, Werner BELZER, Rainer HAMM, Monika HOFMANN
  • MEDICAMENTS FOR THE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE
    Publication number: 20090092558
    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: Application
    Filed: October 27, 2008
    Publication date: April 9, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Ingo KONETZKI, Kurt SCHROMM, Hermann SCHOLLENBERGER, Sabine PESTEL, Andreas SCHNAPP, Thierry BOUYSSOU, Frank BUETTNER, Claudia HEINE, Philipp LUSTENBERGER, Christoph HOENKE, Klaus RUDOLF
  • XANTHINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS
    Publication number: 20090093457
    Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: December 10, 2008
    Publication date: April 9, 2009
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG
    Inventors: Frank HIMMELSBACH, Elke LANGKOPF, Matthias ECKHARDT, Roland MAIER, Michael MARK, Mohammad TADAYYON, Ralf R. H. LOTZ
  • Indolinone derivatives substituted in the 6 position, the preparation thereof and their use as pharmaceutical compositions
    Patent number: 7514468
    Abstract: The present invention relates to indolinone derivatives substituted in the 6 position of general formula wherein R1 to R6 and X are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: April 7, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Armin Heckel, Frank Hilberg, Thorsten Lehmann-Lintz, Guenter Linz, Joerg Kley, Jacobus C. A. Van Meel, Werner Rall, Gerald Juergen Roth, Peter Sieger, Ulrike Tontsch-Grunt
  • Use of Lck inhibitors for treatment of immunologic diseases
    Publication number: 20090087405
    Abstract: The invention relates to a method of treating immunologic diseases or pathological conditions involving an immunologic component using certain Lck inhibitors already known as kinase inhibitors for therapy in oncology, optionally in combination with one or more other drugs selected from NSAIDs, steroids, DMARDs, immunsuppressives, biologic response modifiers and antinfectives, pharmaceutical compositions comprising said Lck inhibitors together with said other drugs, and the use of the Lck inhibitors for the manufacture of a pharmaceutical composition for the treatment of immunologic diseases or pathological conditions involving an immunologic component.
    Type: Application
    Filed: December 12, 2008
    Publication date: April 2, 2009
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Gerald Juergen ROTH, Armin HECKEL, Rainer WALTER, Frank HILBERG, Rudolf HAUPTMANN, Martin Friedrich STEFANIC, Florian COLBATZKY, Steffen ERNST
  • Process for manufacturing of chiral lobelin
    Patent number: 7511147
    Abstract: The present invention relates to a shortened process for preparing L-lobeline by rhodium-catalysed asymmetric hydrogenation on an industrial scale.
    Type: Grant
    Filed: July 8, 2005
    Date of Patent: March 31, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Franz-Dietrich Klingler, Rainer Sobotta
  • ALKYNE COMPOUNDS WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS
    Publication number: 20090069282
    Abstract: The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
    Type: Application
    Filed: May 15, 2008
    Publication date: March 12, 2009
    Applicant: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Dirk Stenkamp, Stephan Georg Mueller, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Klaus Rudolf, Philipp Lustenberger, Kirsten Arndt, Ralf R. H. Lotz, Martin Lenter
  • Process for the Manufacture of Powders of Inhalable Medicaments
    Publication number: 20090068275
    Abstract: The invention relates to an improved process for the production of powders of an inhalable medicament by crystallization from a supersaturated fluid containing said medicament, the method comprising passing along a tubular reactor (a) a segmented flow of that fluid comprised of discrete volumes; or (b) a fluid mixture being separated by discrete volumes of a separating fluid which is substantially immiscible with said fluid, characterized in that the crystallization is initiated by application of ultrasound
    Type: Application
    Filed: November 3, 2008
    Publication date: March 12, 2009
    Applicants: ECOLE POLYTECHNIQUE FEDERALE DE LAUSANNE, Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Nathalie JONGEN, Jacques LEMAITRE, Paul BOWEN, Marcel DONNET, Joerg SCHIEWE, Bernd ZIERENBERG
  • Xanthine derivatives, their preparation and their use in pharmaceutical compositions
    Patent number: 7495005
    Abstract: Compounds of formula (I) wherein R1 is a phenylcarbonylmethyl group wherein the phenyl moiety is substituted, and R2 to R4 are defined as in the claims, or the prodrugs or salts thereof, particularly the physiologically acceptable salts thereof, pharmaceutical compositions containing these compounds, and methods of treating type I and type II diabetes mellitus, arthritis, obesity, allograft transplantation and calcitonin-induced osteoporosis using these compounds.
    Type: Grant
    Filed: August 7, 2003
    Date of Patent: February 24, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz
  • Method for preparing tiotropium salts
    Patent number: 7491824
    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: Grant
    Filed: August 23, 2005
    Date of Patent: February 17, 2009
    Assignee: Boehringer Ingelheim Pharma GmbH & Co., KG
    Inventors: Ralf Lock, Werner Belzer, Rainer Hamm, Monika Hofmann