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
Abstract: Methods for the diagnosis of inflammatory bowel diseases and the identification of agents useful in the treatment of such diseases based upon the agent's effect on reducing Pim-2 expression.
Type:
Application
Filed:
September 25, 2009
Publication date:
June 3, 2010
Applicant:
BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.
Inventors:
Jun LI, Xiang John LI, Randall W. BARTON
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 characterized 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 Schapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoop, Steffen Steurer
Abstract: Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
Type:
Grant
Filed:
March 6, 2009
Date of Patent:
April 27, 2010
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Charles L. Cywin, Scott E. Jakes, Joachim Heider, Mark A. Bobko, Renee L. Des Jarlais, Mark Player, James Rinker, Michael Winters, Bao-ping Zhao
Abstract: Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
Type:
Grant
Filed:
January 15, 2008
Date of Patent:
March 16, 2010
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Charles L. Cywin, Scott E. Jakes, Joachim Heider, Mark A. Bobko, Renee L. Des Jarlais, Mark Player, James Rinker, Michael Winters, Bao-ping Zhao
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:
Application
Filed:
June 3, 2009
Publication date:
December 31, 2009
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
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, Daivd Thomson
Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a tautomer, prodrug, solvate, 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:
December 16, 2005
Date of Patent:
December 22, 2009
Assignee:
Boehringer-Ingelheim Pharmaceuticals, Inc.
Inventors:
Daniel Kuzmich, Darren DiSalvo, John Robinson Regan, David S. Thomson, Rajashekhar Betageri, Jennifer A. Kowalski
Abstract: Compounds of Formula (IA) and (IB) wherein R1, R2, R3, A, B, C, D, and E are as defined herein, or a tautomer, prodrug, solvate, 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 8, 2006
Date of Patent:
November 24, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Ingo Andreas Mugge, David S. Thomson, Abdelhakim Hammach, Michael Jason Burke, Mark Stephen Ralph, Jennifer A. Kowalski, Joerg Martin Bentzien
Abstract: The present invention relates to fluorescence polarization assays for determining the HDC modulating activity of a candidate compound including providing a reaction mixture comprising a HDC, histidine, a fluorescently labeled histamine probe, a candidate compound and an anti histamine antibody having selectivity for histamine at least 10 fold greater than histidine: incubating the reaction mixture; and determining whether inhibition of HDC has occurred in the presence of the test compound, wherein an increase in fluorescence signal is an indication that the test compound inhibits the activity of the HDC.
Type:
Grant
Filed:
November 14, 2005
Date of Patent:
October 27, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Disclosed are novel compounds of formula (I): wherein X, Y, 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:
July 6, 2005
Date of Patent:
October 13, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
August 29, 2008
Date of Patent:
September 22, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Derek Cogan, Daniel R. Goldberg, Ming-Hong Hao, Zhaoming Xiong, Ronald A. Aungst, Amy L. Davis
Abstract: Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
Type:
Grant
Filed:
October 15, 2007
Date of Patent:
September 15, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: The invention provides methods relating to a screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derived based on the Kd of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.
Type:
Grant
Filed:
July 25, 2006
Date of Patent:
September 15, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Anthony S. Prokopowicz, III, Martha Priscilla Brown, Jessi Marie Wildeson, Scott Jakes, Mark E. Labadia
Abstract: Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, 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:
December 18, 2003
Date of Patent:
August 25, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Daniel Kuzmich, Thomas Wai-Ho Lee, John Robert Proudfoot, John Robinson Regan, David S. Thomson, Abdelhakim Hammach, Mark Stephen Ralph, Renee Zindell, Younes Bekkali, Thomas Martin Kirrane, Jr.
Abstract: Disclosed are compounds of formula (I) Where Ar1, X, R3, R4, R5 and R6 are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
September 7, 2006
Date of Patent:
August 4, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Derek A. Cogan, Ming-Hong Hao, Kevin Chungeng Qian, Alan David Swinamer
Abstract: Disclosed are compounds of formula (I): wherein R3, R5, R7 and R8 are defined herein, which are useful as inhibitors SYK kinase and are thus useful for treating diseases resulting from inappropriate mast cell activation, which include allergic and inflammatory diseases. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
Type:
Application
Filed:
March 6, 2009
Publication date:
July 2, 2009
Applicant:
BOEHRINGER INGELHEIM PHARMACEUTICALS, INC.
Inventors:
Charles L. CYWIN, Scott E. JAKES, Joachim HEIDER, Mark A. BOBKO, Renee L. DES JARLAIS, Mark PLAYER, James RINKER, Michael WINTERS, Bao-ping ZHAO
Abstract: Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, 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:
September 17, 2004
Date of Patent:
June 30, 2009
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Rajashehar Betageri, Thomas A. Gilmore, Christian Hanke Justus Joachim Harcken, Daniel Kuzmich, Hossein Razavi, Doris Riether, David S. Thomson, Ji Wang
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.
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