Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Grant
Filed:
September 21, 2011
Date of Patent:
January 8, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.
Type:
Grant
Filed:
April 8, 2010
Date of Patent:
January 8, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Claudio Sturino, Patrick Deroy, Martin Duplessis, Paul J. Edwards, Anne-Marie Faucher, Teddy Halmos, Clint James, Jean-Eric Lacoste, Eric Malenfant, Joannie Minville, Louis Morency, Sebastien Morin, Martin Tremblay, Christiane Yoakim
Abstract: The invention relates to a method of finding suitable parameters for the chromatographic purification of biomolecules. The method consists of equilibration, charging, washing and eluting steps, this sequence of steps being carried out by the partial batch method. The parameters determined in small, preferably numerous parallel test batches provide conclusions as to the chromatography conditions under which a given biomolecule can be purified optimally by column chromatography, optionally even on a larger scale.
Type:
Grant
Filed:
June 13, 2007
Date of Patent:
January 8, 2013
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Christian Eckermann, Sybille Ebert, Stefanie Rubenwolf, Dorothee Ambrosius
Abstract: The present invention relates methods for treating disease conditions selected from the list consisting of benign or malignant tumors, diseases of the airways and lungs, diseases of the gastrointestinal tract, the bile duct and the gall bladder by administration to a patient in need thereof of a therapeutically effective amount of a bicyclic heterocyclic groups of general formula wherein said substituents are as defined herein.
Type:
Grant
Filed:
December 6, 2010
Date of Patent:
January 1, 2013
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Frank Himmelsbach, Birgit Jung, Flavio Solca
Abstract: The invention relates to modified neomycin phosphotransferase genes and their use in a selection method for high-producing recombinant cells. The invention further relates to expression vectors which contain a modified neomycin phosphotransferase gene and a gene of interest functionally linked to a heterologous promoter and a method of preparing heterologous gene products using these expression vectors.
Type:
Grant
Filed:
January 4, 2008
Date of Patent:
December 25, 2012
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Barbara Enenkel, Juergen Fieder, Ralf Otto, Kerstin Sautter, Klaus Bergemann
Abstract: The invention relates to biparatopic A-beta binding polypeptides and, more specifically, to biparatopic A-beta binding polypeptides comprising at least two immunoglobulin single variable domains binding to different epitopes of A-beta. The invention also relates to specific sequences of such polypeptides, methods of their production, and methods of using them, including methods of treatment of diseases such as Alzheimer's Disease.
Type:
Grant
Filed:
March 2, 2011
Date of Patent:
December 25, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
John E. Park, Cornelia Dorner-Ciossek, Stefan Hoerer, Lothar Kussmaul, Martin Lenter, Katharina Zimmermann, Gerald Beste, Toon Laeremans, Pascal Merchiers, Jo Vercammen
Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.
Type:
Grant
Filed:
October 13, 2009
Date of Patent:
December 25, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Alexander Heim-Riether, Shuang Liang, Sabine Schlyer
Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are intermediates thereof, and methods of making and methods of using same.
Type:
Grant
Filed:
February 8, 2012
Date of Patent:
December 25, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Daniel Kuzmich, Pingrong Liu, Hossein Razavi
Abstract: The present invention relates to a method of making pyrimidines of formula (III), wherein X1, X2, R1 and R2 have the meanings as defined herein.
Type:
Grant
Filed:
March 19, 2009
Date of Patent:
December 18, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Adil Duran, Stefan Goepper, Joerg Halmer, Michael Konrad
Abstract: Disclosed are thiazolyl-dihydro-quinazolines of general formula (I) wherein the groups R1 to R4 have the meanings given in the claims and specification, the isomers thereof, and processes for preparing these compounds and their use as pharmaceutical compositions.
Type:
Grant
Filed:
February 17, 2010
Date of Patent:
December 18, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Trixi Brandl, Udo Maier, Matthias Hoffmann, Stefan Scheuerer, Anne T. Joergensen, Alexander Pautsch, Steffen Breitfelder, Matthias Grauert, Christoph Hoenke, Klaus Erb, Michael Pieper, Ingo Pragst
Abstract: The present invention relates to a crystalline form a dihydropteridione derivative, namely a crystalline form of the free base N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.
Type:
Grant
Filed:
August 1, 2008
Date of Patent:
December 11, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Guenter Linz, Peter Sieger, Rolf Schmid, Stefan Goepper
Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Grant
Filed:
March 1, 2011
Date of Patent:
December 11, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Monika Ermann, Doris Riether, Renee M. Zindell
Abstract: The invention provides compounds according to formula (I) their use and methods for preparation wherein A, X, Y, R1, R2 and R3 are defined herein. The compounds of the invention inhibit specific serine/threonine kinases involved in inflammatory processes and aberrant cell proliferation, and are thus useful for treating associated diseases and pathological conditions such as Pim kinase-mediated diseases and pathological conditions involving inflammation, including Chron's disease, inflammatory bowel disease, rheumatoid arthritis, and chronic inflammatory disease, or aberrant cell proliferation including various cancers.
Type:
Grant
Filed:
August 15, 2007
Date of Patent:
November 27, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Wang Mao, Tina Marie Morwick, Anthony S. Prokopowicz, III
Abstract: Antibody molecules, in particular fully human antibodies that bind to human IGF-1 and cross-react with IGF-2 such that binding of IGF-1 and IGF-2 to the IGF-1 receptor is prevented and IGF-1 receptor-mediated signaling is inhibited. The antibodies do not bind to insulin and thus do not affect the mitogenic properties of insulin that are mediated by its binding to the insulin receptors. The antibodies are useful for the treatment of hyperproliferative diseases, in particular cancer.
Abstract: The object of the present invention is novel substituted pyrrolidine amides of the general formula (I) in which D, L. E, G, J, M, L1, L2, R4, and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures, and salts thereof, particularly physiologically tolerated salts with inorganic or organic acids or bases having valuable properties.
Type:
Grant
Filed:
March 26, 2008
Date of Patent:
November 13, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Kai Gerlach, Henning Priepke, Wolfgang Wienen, Annette Schuler-Metz, Georg Dahmann, Herbert Nar
Abstract: The present invention relates to compounds defined by formula (I) wherein the group R is defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases.
Type:
Grant
Filed:
July 24, 2009
Date of Patent:
November 13, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach
Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
Type:
Grant
Filed:
January 11, 2012
Date of Patent:
November 6, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Darryl McConnell, Maria Impagnatiello, Dirk Kessler, Oliver Kraemer, Siegfried Schneider, Lars Van Der Veen, Ulrike Weyer-Czernilofsky, Tobias Wunberg
Abstract: The present invention relates to a process for the manufacture of a specific indolinone derivative and a pharmaceutically acceptable salt thereof, namely 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone and its monoethanesulfonate, to new manufacturing steps and to new intermediates of this process.
Type:
Grant
Filed:
December 2, 2008
Date of Patent:
November 6, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Joern Merten, Guenter Linz, Juergen Schnaubelt, Rolf Schmid, Werner Rall, Svenja Renner, Carsten Reichel, Robert Schiffers
Abstract: The present invention relates to capsules for holding pharmaceutical preparations for powder inhalers with increased drug safety and capsules for pharmaceutical preparations for powder inhalers with improved adaptation to their use in powder inhalers. The capsules consist of water-insoluble hydrophobic synthetic materials which do not significantly affect the pharmaceutical quality of the contents themselves, but which improve the usability of the filled capsules with regard to their function, their longevity, and/or the geographic location of their use, and are advantageous at various stages from manufacture up to utilization.
Type:
Grant
Filed:
January 8, 2008
Date of Patent:
October 30, 2012
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG