Patents Represented by Attorney Michael P. Morris
  • Patent number: 8299111
    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: November 30, 2010
    Date of Patent: October 30, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, David S. Thomson, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Nigel Blumire
  • Patent number: 8297477
    Abstract: A dosing device for dispensing small-particulate pharmaceutical preparations has at least one chamber for receiving a larger amount of the preparation and a dosing unit. A rotary valve has at least one dosing chamber for receiving a defined dose of the preparation. The dosing chamber is moveable between a filling position and a dispensing position. The rotary valve rotates about a substantially horizontal axis, and has an adjustment device for setting the volume in the dosing chamber and a twisting device. The twisting device constitutes the actuator for the adjustment device. The device is made of a plastic material carefully selected to assure that no softening agents or other volatile components will be released, which prevents drug contamination.
    Type: Grant
    Filed: December 31, 2005
    Date of Patent: October 30, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rolf-Stefan Brickl, J├╝rgen Schraivogel
  • Patent number: 8299123
    Abstract: The invention relates to a compound of formula (I): or a tautomer thereof or a pharmaceutically acceptable salt thereof, wherein R1 to R11, W, X, Y, Z, and n are as defined herein. The invention also relates to methods of using the compounds of formula (I) and compositions thereof to treat various diseases and disorders in a patient. The invention also relates to processes for preparing the compounds of formula (I) and intermediates useful in these processes.
    Type: Grant
    Filed: October 14, 2008
    Date of Patent: October 30, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kaka Dey, Donghong Amy Gao, Daniel R. Goldberg, Alexander Heim-Riether, John Edward Mangette, Ingo Andreas Mugge, Roger John Snow, Alan David Swinamer, Jiang-Ping Wu, Zhaoming Xiong, Yu Yang
  • Patent number: 8299103
    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: June 1, 2010
    Date of Patent: October 30, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Eugene Richard Hickey, Doris Riether
  • Patent number: 8293917
    Abstract: Disclosed are compounds of the formula (I) which block the interaction of CCR1 and its ligands and are thus 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 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: May 1, 2009
    Date of Patent: October 23, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Christian Harcken, Thomas Wei-Ho Lee, Pingrong Liu, Jord Lord, Can Mao, Wang Mao, Brian Christopher Raudenbush, Hossein Razavi, Christopher Ronald Sarko, Alen David Swinamer
  • Patent number: 8293729
    Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.
    Type: Grant
    Filed: June 23, 2010
    Date of Patent: October 23, 2012
    Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences Inc.
    Inventors: Brian Dyck, Joe A. Tran, Junko Tamiya, Florence Jovic, Troy Vickers, Chen Chen, Nicole Harriott, Timothy Coon, Neil J. Ashweek
  • Patent number: 8288379
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 and X 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: April 20, 2010
    Date of Patent: October 16, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Lars Van Der Veen, Maria Impagnatiello, Darryl McConnell, Siegfried Schneider, Tobias Wunberg
  • Patent number: 8288531
    Abstract: A process for preparing compounds of the formula (I) in which R1 and R2 are as defined in the description.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: October 16, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Juergen Schnaubelt, Thomas Fachinger, Michael Konrad, Thomas Krueger, Joern Merten, Carsten Reichel, Svenja Renner, Rolf Schmid, Emanuel Stehle, Bianca Werner
  • Patent number: 8283326
    Abstract: The invention relates to a crystalline form of 4-(?-D-glucopyranos-1-yl)-1-methyl-2-[4-((S)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.
    Type: Grant
    Filed: October 26, 2007
    Date of Patent: October 9, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Frank Himmelsbach, Tanja M. Butz, Hans-Juergen Martin
  • Patent number: 8281784
    Abstract: A mouthpiece for an inhaler for administering a drug in the form of substances, substance formulations or substance mixtures that can be inhaled comprises an inhalation channel (4) for coupling to a chamber for receiving the drug. At least one component (10) having an aerodynamic cross-section is arranged in the inhalation channel (4).
    Type: Grant
    Filed: April 4, 2007
    Date of Patent: October 9, 2012
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventor: Herbert Wachtel
  • Patent number: 8278336
    Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: October 2, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
  • Patent number: 8278302
    Abstract: Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: October 2, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Horst Dollinger, Riccardo Giovannini, Christoph Hoenke, Matthias Hoffmann, Jan Kriegl, Domnic Martyres, Georg Rast, Peter Seither
  • Patent number: 8268859
    Abstract: Compounds of Formula (I) wherein R1, R2, X, and Y are as defined herein, or a tautomer, optical isomer, prodrug, co-crystal, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: September 18, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Christian Harcken, Rajashekhar Betageri, Todd Bosanac, Michael Jason Burke, Soojin Kim, Daniel Kuzmich, Thomas Wai-ho Lee, Zhibin Li, Pingrong Liu, John Lord, Hossein Razavi, Jonathan Timothy Reeves, David Thomson
  • Patent number: 8267082
    Abstract: The invention is a medicament magazine having at least one medicament chamber for use in a powder inhaler, wherein the magazine is formed from two foil strips applied to one another and the at least one medicament chamber is formed between the foil strips as depicted in exemplary FIGS. 1a and 1b. The medicament chambers have an internal structure (3) which comprises in its interior a space for receiving a powdered medicament and stabilizes this inner space against external mechanical influences. In another embodiment in which the internal structure preferably also has a stabilizing function, the structure has means for opening one foil strip. In addition, the medicament chamber contains a retaining device which holds the internal structure on the medicament magazine after the medicament chamber has been opened.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: September 18, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Herbert Wachtel, Johannes Geser, Burkhard Metzger, Michael Spallek, Michael Krueger, Hubert Kunze, Achim Moser, Elmar Mock, Antonino Lanci, Andre Klopfenstein
  • Patent number: 8263768
    Abstract: The present invention relates to a process for the stereoselective preparation of compounds of general formula (I) and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: September 11, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Markus Ostermeier, Stefan Braith, Juergen Daeubler, Guenther Huchler, Waldemar Pfrengle
  • Patent number: 8263597
    Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus 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 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: July 18, 2011
    Date of Patent: September 11, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Daniel Kuzmich, Can Mao, Alan David Swinamer, David Smith Thomson
  • Patent number: 8263788
    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: Grant
    Filed: September 3, 2008
    Date of Patent: September 11, 2012
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Joerg Brandenburg, Rolf Dach, Hanfried Baltes
  • Patent number: 8258301
    Abstract: Compounds of the formula (I) wherein R1, R2, R3, R4, R5, R6, W, and Y are as described herein, or a tautomer, prodrug, solvate, or salt thereof. These compounds are useful as inhibitors of Urotensin II and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the interaction of Urotensin II with its receptor, including cardiovascular diseases. 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: May 12, 2008
    Date of Patent: September 4, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Brian Nicholas Cook, Anne Bettina Eldrup, Ingo Andreas Mugge, Fariba Soleymanzadeh, Sanxing Sun, Yunlong Zhang
  • Patent number: 8258129
    Abstract: The present invention encompasses compounds of general formula (1) wherein X and R1 to R3 are as defined in the disclosure, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: September 4, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
  • Patent number: 8252785
    Abstract: The present invention relates to compounds of general formula I wherein A, B, D, Y, R1, R2, R3, R4 and R5 are defined as in the specification, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Grant
    Filed: October 5, 2010
    Date of Patent: August 28, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Norbert Hauel, Rainer Walter, Heiner Ebel, Henri Doods, Angelo Ceci, Annette Schuler-Metz, Ingo Konetzki