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Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.


Location: Ridgefield, CT
No. of patents: 261

1              
NumberTitleIssue Date
7932392Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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 composi...
04/26/2011
7914770Formulation for a metered dose inhaler using hydro-fluoro-alkanes as propellants
An improved suspension formulation for use in a metered-dose inhaler having a hydro-fluoro-alkane propellant is described, the improvement being the controlled addition of a small quantity of water. ...
03/29/2011
7741361Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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; pharmaceu...
06/22/2010
7714127Process for making heteroaryl amine intermediate compounds
Disclosed are processes to produce a compound of the formula (I): ...
05/11/2010
7709480Pyrimidine derivatives
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 ...
05/04/2010
77051511,6 Naphthridines useful as inhibitors of SYK kinase
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...
04/27/2010
76789111,6 naphthyridines useful as inhibitors of SYK kinase
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...
03/16/2010
7622594Glucocortioid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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 ...
11/24/2009
7608407Fluorescence polarization assay for determining histidine decarboxylase activity
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 an...
10/27/2009
7601714Pyrimidine derivatives useful as inhibitors of PKC-theta
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 dis...
10/13/2009
7592332Cytokine inhibitors
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 in...
09/22/2009
7589115Derivatives of [6,7-dihydro-5-imidazo[1,2-α]imidazole-3-sulfonylamino]-propionamide
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. ...
09/15/2009
7588899Fluorescent probes for use in protein kinase inhibitor binding assay
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 K
09/15/2009
7579469Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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 s...
08/25/2009
7569568Cytokine inhibitors
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 infl...
08/04/2009
7553966Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
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,...
06/30/2009
7550494Small molecules useful in the treatment of inflammatory disease
Compounds of the formula I which are useful for treating or preventing inflammatory and immune cell-mediated diseases. Exemplary are: ...
06/23/2009
7550473Pyrimidine derivatives useful as inhibitors of PKC-theta
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 ...
06/23/2009
7550461Benzofuran and benzothiophene compounds useful in treating cytokine mediated diseases
Disclosed are amide compounds of formula (I): wherein Ar1, Q, Y and R3-R6 of formula (I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes ...
06/23/2009
7531560Anti-cytokine heterocyclic compounds
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 in...
05/12/2009
7514458Anti-cytokine heterocyclic compounds
Disclosed 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 inflam...
04/07/2009
7511042Triazole compounds
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 and are thus u...
03/31/2009
7507843Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
A process for stereoselective synthesis of compounds of Formula X wherein: R1 is an aryl or heteroaryl group, each optionally independently substituted with one to three substit...
03/24/2009
7491851Method for generating secondary phosphines
This invention provides a method for generating secondary phosphines from secondary phosphine oxides in the presence of a reducing agent, such as diisobutylaluminum hydride (DIBAL-H), triisobutyldialuminoxane, triisobutylaluminum, tetraisobutyldialuminoxane, or anot...
02/17/2009
7485657Anti-cytokine heterocyclic compounds
Disclosed are compounds of formula (I) The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as ch...
02/03/2009
7470795Synthesis of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid amides
Disclosed is a multi-step process for preparing a compound of Formula I: wherein R1 to R3 are as defined herein. The compounds of formula I inhibit the binding of human intercellular adhesion molecules...
12/30/2008
7470692Cytokine inhibitors
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 in...
12/30/2008
7465745Cathepsin S inhibitors
This invention relates to peptidyl compounds of the formulas (I) and (II) active as cathepsin S, a cysteine protease, inhibitors. The compounds are selective, reversible inhibitors of the cathepsin S are therefore useful in the treatment of autoimmune and other dise...
12/16/2008
7462637Derivatives of [6,7-dihydro-5-imidazo[1,2-]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide
Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonyl]-pyrrolidine-2-carboxylic acid amide which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease. ...
12/09/2008
7425629Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
A process for stereoselective synthesis of a compound of Formula (I) wherein R1, R2, R3, R4, and R5 are as described herein. ...
09/16/2008
7417127Antibodies specific for CD44v6
The present invention belongs to the field of oncology. The invention relates to antibodies with specified sequence which are specific for an epitope which is coded by the variant exon v6 of the CD44 gene and to derivatives of said antibody. The invention also provi...
08/26/2008
7405225Substituted 3-amino-thieno[2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses
Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the IκB kinase (IKK) complex. The compounds are therefore useful ...
07/29/2008
7375220Method of treating diseases and conditions associated with an altered level of amyloid β peptides and new enolcarboxamide compounds
A method of treating or preventing of a disease or condition associated with an increased level of isoforms of amyloid β peptides (Aβ) and/or with a changed ratio of levels of Aβ isoforms and/or with the formation of plaques containing amyloid β peptide (Aβ) is...
05/20/2008
7345074Derivatives of [6,7-dihydro-5H-imidazol[1,2-a]imidazole-3-sulfonylamino]-propionamide
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. ...
03/18/2008
7335657Cytokine inhibitors
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 ...
02/26/2008
7329764Substitute benzothiophene compounds
Disclosed are compounds of the formula I shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents. Also disclosed are methods of using and making such compounds ...
02/12/2008
7326719Cathepsin S inhibitors
This invention relates to peptidyl compounds of the formulas (I) and (II) active as cathepsin S, a cysteine protease, inhibitors. The compounds are selective, reversible inhibitors of the cathepsin S are therefore useful in the treatment of autoimmune and other dise...
02/05/2008
73210411,6 Naphthyridines useful as inhibitors of SYK kinase
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 disease...
01/22/2008
7312211Pryanone compounds useful as reversible inhibitors of cysteine proteases
Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and othe...
12/25/2007
7304067Derivatives of [6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonylamino]-propionamide
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. ...
12/04/2007
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