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 20, 2004
Date of Patent:
March 18, 2008
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
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:
June 27, 2006
Date of Patent:
February 26, 2008
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: 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.
Type:
Grant
Filed:
July 29, 2004
Date of Patent:
February 12, 2008
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Zhidong Chen, John David Ginn, Eugene Richard Hickey, Weimin Liu, Can Mao, Tina Marie Morwick, Peter Allen Nemoto, Denice Spero, Sanxing Sun
Abstract: 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 diseases.
Type:
Grant
Filed:
March 1, 2004
Date of Patent:
February 5, 2008
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Eugene R. Hickey, Weimin Liu, Sanxing Sun, Yancey David Ward, Erick Richard Roush Young
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:
April 15, 2003
Date of Patent:
January 22, 2008
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 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 other diseases.
Type:
Grant
Filed:
August 26, 2004
Date of Patent:
December 25, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
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:
January 13, 2005
Date of Patent:
December 4, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Disclosed are substituted tricyclic heterocycle compounds of the formulas (I), (II) and (III) shown below, wherein R1, R2, R3 and R4 are described herein, which are active as anti-inflammatory agents.
Type:
Grant
Filed:
October 7, 2004
Date of Patent:
November 6, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Charles Lawrence Cywin, Roman Wolfgang Fleck, Eugene Richard Hickey, Weimin Liu, Tina Marie Morwick, John Robert Proudfoot, Denice M. Spero
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:
April 29, 2005
Date of Patent:
October 23, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Derek Cogan, Daniel R. Goldberg, Ming-Hong Hao, Zhaoming Xiong, Ronald A. Aungst, Amy L. Davis
Abstract: Disclosed are compounds of formula(I): wherein R1, R2, W and X 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:
September 14, 2004
Date of Patent:
October 9, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Pier Francesco Cirillo, Abdelhakim Hammach, Victor Kamhi, Neil Moss, Paul S Riska, Christopher Pargellis
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:
September 9, 2004
Date of Patent:
October 9, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Michel Jose Emmanuel, Leah L. Frye, Eugene R. Hickey, Weimin Liu, Tina Marie Morwick, Denice Mary Spero, Sanxing Sun, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
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:
March 21, 2003
Date of Patent:
September 11, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Younes Bekkali, Mario G. Cardozo, Christian Hanke Justus Joachim Harcken, Thomas M. Kirrane, Daniel Kuzmich, John Robert Proudfoot, Hossein Razavi, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell
Abstract: Disclosed is a process of making compounds of formula(I): wherein R1, R2, R3, R4 and Ra of formula(I) are defined herein. The product compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation. Also disclosed are intermediates useful in making such compounds.
Type:
Grant
Filed:
June 30, 2004
Date of Patent:
September 4, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: Disclosed are 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:
September 9, 2004
Date of Patent:
September 4, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals Inc.
Inventors:
Michel Jose Emmanuel, Leah L. Frye, Eugene R. Hickey, Weimin Liu, Tina Marie Morwick, Denice Mary Spero, David S. Thomson, Yancey David Ward, Erick Richard Roush Young
Abstract: 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 another reducing agent comprising: (i) an R1R2AlH moiety, wherein R1 and R2 are each an alkyl species or oxygen, and wherein at least one of R1 or R2 comprises at least 2 carbon atoms, or (ii) an R1R2R3Al moiety, wherein R1, R2, and R3 are not hydrogen, and wherein at least one of R1, R2, and R3 is an alkyl species comprising a ?-hydrogen, not including triethylaluminum. Preferred reducing agents for the present invention include: diisobutylaluminum hydride, triisobutyldialiuminoxane, triisobutylaluminum, tetraisobutyldialuminoxane, and combinations thereof.
Type:
Grant
Filed:
January 12, 2005
Date of Patent:
August 14, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Abstract: A process for stereoselective synthesis of a compound of Formula (X) or Formula (X?) wherein R1, R2, and R3 are as defined herein, the process comprising: (a) reacting the starting material of formula A with a chiral sulfoxide anion source in a suitable solvent to prepare a compound of formula C or C?; (b) reducing the sulfoxide of formula C or C? in a suitable solvent to obtain the compound of formula D or D?; and (c) cyclizing the compound of formula D or D? in a suitable solvent to form the epoxide compound of Formula (X) or Formula (X?), 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:
March 15, 2005
Date of Patent:
August 14, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
Inventors:
Thomas Wai-Ho Lee, John Robert Proudfoot
Abstract: Disclosed are novel aromatic compounds of the formula (I) wherein G, X, Ar, L and Q are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.
Type:
Grant
Filed:
October 15, 2002
Date of Patent:
July 10, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.
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:
December 8, 2003
Date of Patent:
June 26, 2007
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc.