Abstract: One object of the present invention are novel substituted piperidyl-propane-thiols of the formula (1), wherein R1, R2, R3 and R4 are defined as below. Another object of the present invention is to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, 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:
October 25, 2007
Date of Patent:
April 10, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Domnic Martyres, Matthias Hoffmann, Peter Seither, Thierry Bouyssou
Abstract: One object of the present invention are novel substituted piperidyl-propane-thiols of the formula (1), wherein R1, R2, R3 and D are defined as below. Another object of the present invention is to provide agonists or antagonists of CCR-3, or pharmaceutically acceptable salts thereof, 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:
October 25, 2007
Date of Patent:
April 3, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Domnic Martyres, Matthias Hoffmann, Peter Seither, Thierry Bouyssou
Abstract: Disclosed are pharmaceutical compositions for the treatment of diseases which involve cell proliferation. Also disclosed are methods for the treatment of said diseases, comprising co-administration of a compound 1 of Formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given herein and of an effective amount of an active compound 2 and/or co-treatment with radiation therapy, in a ratio which provides an additive and synergistic effect, and to the combined use of a compound 1 of Formula (I) and of an effective amount of an active compound 2 and/or radiotherapy for the manufacture of corresponding pharmaceutical combination preparations.
Type:
Grant
Filed:
May 7, 2009
Date of Patent:
March 27, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Gerd Munzert, Martin Steegmaier, Anke Baum
Abstract: Disclosed are processes and intermediate compounds for preparing dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and in the specification.
Type:
Grant
Filed:
June 4, 2010
Date of Patent:
March 20, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Guenter Linz, Gerd Kraemer, Ludwig Gutschera, Geert Asche
Abstract: Disclosed are processes for preparing dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and in the specification.
Type:
Grant
Filed:
June 4, 2010
Date of Patent:
March 20, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Guenter Linz, Gerd Kraemer, Ludwig Gutschera, Geert Asche
Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are as defined herein, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
Type:
Grant
Filed:
June 20, 2008
Date of Patent:
February 21, 2012
Assignee:
Boehringer Ingelheim Pharma GmbH & Co. KG
Inventors:
Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf Lotz
Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.
Type:
Grant
Filed:
August 8, 2011
Date of Patent:
February 21, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Guenther Huchler, Werner Rall, Uwe Reis
Abstract: The invention relates to a process for preparing the compound of formula 1, a valuable intermediate product in the synthesis of the pharmaceutical active substance dabigatran etexilate.
Abstract: An improved method for recovering the protein expressed by open reading frame 2 from porcine circovirus type 2 is provided. Also provided is recombinant PCV2 ORF2 protein, and immunogenic compositions comprising PCV2 ORF2 protein. Moreover, multivalent combination vaccines are provided which include an immunological agent effective for reducing the incidence of or lessening the severity of PCV2 infection, preferably PCV2 ORF2 protein, or an immunogenic composition comprising PCV2 ORF2 protein, and at least one immunogenic active component of another disease-causing organism in swine.
Type:
Grant
Filed:
June 11, 2008
Date of Patent:
February 21, 2012
Assignee:
Boehringer Ingelheim Vetmedica, Inc.
Inventors:
Michael Roof, Phillip Hayes, Marc Eichmeyer, Greg Nitzel
Abstract: The present invention relates to the field of animal health and in particular to Lawsonia intracellularis. In particular, the invention relates to a method of diagnosing Lawsonia intracellularis infection and a diagnostic test kit using Lawsonia intracellularis-specific antibodies. The invention also relates to the use of the method or test kit for diagnosing Lawsonia intracellularis infections.
Abstract: The present invention relates to the field of animal health and in particular to Lawsonia intracellularis. In particular, the invention relates to a method of diagnosing Lawsonia intracellularis infection and a diagnostic test kit using Lawsonia intracellularis-specific antibodies. The invention also relates to the use of the method or test kit for diagnosing Lawsonia intracellularis infections.
Abstract: The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2 and R3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
Type:
Grant
Filed:
April 18, 2007
Date of Patent:
February 14, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Pascale Pouzet, Christoph Hoenke, Rolf Goeggel, Birgit Jung, Peter Nickolaus, Dennis Fiegen, Thomas Fox
Abstract: The present invention relates to new CGRP-antagonists of general formula I wherein U, V, X, Y, R1, R2, R3 and R4 are defined as in the description, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures thereof and the salts thereof and the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, medicaments containing these compounds, their use and processes for preparing them.
Type:
Grant
Filed:
November 21, 2008
Date of Patent:
February 7, 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
Abstract: The invention relates to 8-[3-amino-piperidin-1-yl]-xanthines and the physiologically acceptable salts thereof, particularly the hydrochlorides thereof.
Abstract: Disclosed are highly convergent processes for preparing compounds of formula (I), which compounds are potent active agents for the treatment of hepatitis C virus (HCV) infection: The disclosed processes use SNAr-type coupling reactions between peptidic compounds having a hydroxyproline moiety of the following formula: and halogenated or sulfonated bromoquinoline compounds.
Type:
Grant
Filed:
January 16, 2009
Date of Patent:
January 24, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Carl Alan Busacca, Rogelio Perez Frutos, Nizar Haddad, Suresh R. Kapadia, Jon Charles Lorenz, Anjan Saha, Chris Hugh Senanayake, Xudong Wei
Abstract: The invention relates to a novel method for producing scopine esters of the general formula (1), wherein X—, R, R1, R2, R3, R4, R3?, R4?, R6 and R6? can have the meanings indicated in the claims and in the description.
Type:
Grant
Filed:
May 9, 2008
Date of Patent:
January 24, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Waldemar Pfrengle, Werner Rall, Joerg Brandenburg, Rolf Herter
Abstract: Double chamber container for holding and combining, e.g., a lyophilizate and a liquid reconstitution medium, comprising an integral cylindrical body (15) with a closure (20, 60) at each of the two ends (5, 70), an upper movable closure (60) to the side of the reconstitution medium and a lower closure (20) to the side of the lyophilizate, a separating stopper (40) that can be moved in the cylindrical body (15) as a seal between the upper chamber (50) and the lower chamber (30), a bypass (35), arranged below the separating stopper (40), having a length L greater than the height H of the separating stopper (40), wherein at the lower end (5) in the wall of the cylindrical body (15) or in the lower stopper (20) there are provided means (21, 25, 28) that allow connection of the interior of the cylindrical body (15) to the environment during the lyophilization.
Type:
Grant
Filed:
August 14, 2006
Date of Patent:
January 17, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Stefan Bassarab, Alexander Bauer, Nicole Denkinger, Patrick Garidel, Markus Hemminger, Hans-Joachim Kern, Andreas Langer, Ingo Presser
Abstract: Substituted amide and urea derivatives useful as inhibitors of Rho kinase are described, which inhibitors can be useful in the treatment of various disorders such as cardiovascular diseases, cancer, neurological diseases, renal diseases, bronchial asthma, erectile dysfunction and glaucoma.
Type:
Grant
Filed:
January 2, 2008
Date of Patent:
January 10, 2012
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Georg Dahmann, Eugene Richard Hickey, Xiang Li, Wang Mao, Daniel R. Marshall, Tina M. Morwick, Robert Sibley, Roger John Snow, Ronald J. Sorcek, Frank Wu, Erick Richard Roush Young
Abstract: A method for modulating NF-?B dependent gene transcription in a cell comprised of modulating IKK? protein activity in the cell. The present invention also provides siRNA compositions and methods thereof for modulating NF-?B dependent gene transcription.
Type:
Grant
Filed:
October 13, 2010
Date of Patent:
January 3, 2012
Assignee:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Jun Li, Xiang Li, Jianfei Yang, Kenneth B. Marcu
Abstract: Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates thereof.