Abstract: This invention relates to screening assay methods that can be applied to broad members of the protein kinase gene family and are useful in the detection and evaluation of kinase inhibitors.
Type:
Application
Filed:
April 20, 2005
Publication date:
October 26, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Jeffrey Yingling, Scott Jakes, Donna Terenzio
Abstract: The invention provides methods relating to a novel 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:
September 30, 2004
Date of Patent:
October 24, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Anthony S. Prokopowicz, III, Martha Priscilla Brown, Jessi Marie Wildeson, Scott Jakes, Mark E. Labadia
Abstract: Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry 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. The compounds are also useful for treating diseases or conditions related to oncology and anticoagulant or fibrinolytic therapy. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
Type:
Application
Filed:
June 27, 2006
Publication date:
October 19, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Pier Cirillo, Donghong Gao, Daniel Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Kamhi, Neil Moss, Matthew Netherton, Kevin Qian, Mark Ralph, Lifen Wu, Zhaoming Xiong, Ronald Aungst
Abstract: Disclosed are compounds of formula (I): wherein the variables R1, R2, R3 and Z are described herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.
Type:
Grant
Filed:
December 2, 2004
Date of Patent:
October 10, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Zhidong Chen, Pier Francesco Cirillo, Darren DiSalvo, Weimin Liu, Daniel Richard Marshall, Lifen Wu, Erick Richard Roush Young
Abstract: Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds 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.
Type:
Grant
Filed:
September 3, 2003
Date of Patent:
October 3, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Antonio Jose del Moral Barbosa, Jr., Daniel R. Goldberg, Abdelhakim Hammach, Pingrong Liu, Neil Moss, Mark Stephen Ralph, Gregory Paul Roth, Christopher Ronald Sarko, Fariba Soleymanzadeh, Andre White
Abstract: A method and system for aiding the selecting/culling or reformatting of encoded containers stored in a multi-rack array with respect to certain desired characteristics of compositions held within the containers employing a corresponding graphical interface that indicates the physical position of the containers within the array, and selection operations to be performed with respect to one or more containers in the array.
Type:
Application
Filed:
November 8, 2005
Publication date:
September 21, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
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:
Application
Filed:
December 16, 2005
Publication date:
August 24, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Daniel Kuzmich, Darren DiSalvo, John Regan, David Thomson, Rajashekhar Betageri, Jennifer Kowalski
Abstract: Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), 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:
Application
Filed:
April 25, 2006
Publication date:
August 24, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Younes Bekkali, Rajashehar Betageri, David Thomson, Doris Riether, Christian Hanke Justus Harcken, Daniel Kuzmich, John Proudfoot
Abstract: Disclosed are polymorphs of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea and processes from making the same.
Type:
Grant
Filed:
December 13, 2004
Date of Patent:
August 15, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: The invention concerns an improved therapeutic regimen for the treatment of thrombolytic disorders, such as acute myocardial infarction (AMI). In particular, the present invention concerns the treatment of thrombolytic disorders, e.g. AMI, with a combination of a tissue plasminogen activator (t-PA) variant having improved fibrin specificity and extended plasma half-life when compared with wild-type human t-PA and a low molecular weight heparin.
Inventors:
Paul Armstrong, Hal Barron, Silvano Berioli, Frederique Bigonzi, Erich Bluhmki, Richard Chin, Christopher Granger, Frans Van De Werf, Fong Wang-Clow
Abstract: Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry 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. The compounds are also useful for treating diseases or conditions related to oncology and anticoagulant or fibrinolytic therapy. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
Type:
Grant
Filed:
February 27, 2004
Date of Patent:
July 18, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Pier Francesco Cirillo, Donghong Amy Gao, Daniel R. Goldberg, Abdelhakim Hammach, Ming-Hong Hao, Victor Marc Kamhi, Neil Moss, Matthew Russell Netherton, Kevin Chungeng Qian, Mark Stephen Ralph, Lifen Wu, Zhaoming Xiong, Ronald A. Aungst, Jr.
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:
Application
Filed:
December 16, 2005
Publication date:
July 13, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Daniel Kuzmich, Darren DiSalvo, John Regan, David Thomson
Abstract: A compound of Formula (IA) or Formula (IB) wherein R1, R2, R3, R4, R5, R6, R7 and R8 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:
May 28, 2003
Date of Patent:
July 11, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Thomas Martin Kirrane, Jr., Daniel Kuzmich, John Robert Proudfoot, Hossein Razavi, David Thomson
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:
November 17, 2005
Publication date:
June 29, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: A method of treating primary dysmenorrhea which comprises administering to a human female suffering from the same a therapeutically effective amount of alpha-adrenergic blocker. Exemplary alpha-adrenergic blockers are phenoxybenzamine, alfuzosin, doxazosin, terazosin, prazosin, and tamsulosin, or a pharmaceutically acceptable salt or ester thereof. Tamsulosin HCl is preferred.
Type:
Application
Filed:
December 2, 2005
Publication date:
June 15, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (I), (II), (Ia) and (Ib) further defined herein. The compounds are useful for treating autoimmune diseases.
Type:
Grant
Filed:
April 24, 2003
Date of Patent:
June 6, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Michel Jose Emmanuel, Eugene R. Hickey, Weimin Liu, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
Abstract: A fluorescence polarization assay for determining the HDC modulating activity of a candidate compound comprising the steps of: a) 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; b) incubating the reaction mixture; c) 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:
Application
Filed:
November 14, 2005
Publication date:
May 18, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Unique multifunctional nucleotide expression cassettes comprising a nucleotide sequence encoding a human protease driven by a glucose-regulatable promoter, a nucleotide sequence encoding human proinsulin having sites at its B-C and C-A junctions altered to permit cleavage by the human protease, and a CMV promoter driving the transcription of the nucleotide sequence encoding the human proinsulin, such cassettes optionally having polyadenylation sequences after each structural gene and the nucleotide sequence encoding human proinsulin optionally carrying an H10D variant, and cells transformed thereby.
Type:
Grant
Filed:
June 10, 2002
Date of Patent:
May 16, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Revati J. Tatake, Richard Schneiderman, Randall Wilber Barton
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:
Application
Filed:
November 9, 2005
Publication date:
May 11, 2006
Applicant:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): wherein Ar, X, A, L, and Q of formula(I) are defined herein. The compounds 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:
February 19, 2003
Date of Patent:
May 9, 2006
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Pier Francesco Cirillo, Abdelhakim Hammach, John Robinson Regan