The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Aug. 05, 2014
Filed:
Jun. 26, 2012
Kristi A. Leonard, Lansdale, PA (US);
Richard Scott Alexander, Newark, DE (US);
Joseph Kent Barbay, Flourtown, PA (US);
Roger F. Bone, Bridgewater, NJ (US);
Ingrid Christa Deckman, Berwyn, PA (US);
Paul F. Jackson, Furlong, PA (US);
Lawrence C. Kuo, Gwynedd Valley, PA (US);
Frank A. Lewandowski, Philadelphia, PA (US);
Diane M. Maguire, Downingtown, PA (US);
Cynthia M. Milligan, Rutledge, PA (US);
Kenneth J. Rhodes, Belmont, MA (US);
Robert H. Scannevin, Hopkinton, MA (US);
Celine Schalk-hihi, Phoenixville, PA (US);
Barry Springer, Wilmington, DE (US);
John C. Spurlino, Downingtown, PA (US);
Matthew J. Todd, Ambler, PA (US);
Brett A. Tounge, Blue Bell, PA (US);
Aihua Wang, Jamison, PA (US);
Kristi A. Leonard, Lansdale, PA (US);
Richard Scott Alexander, Newark, DE (US);
Joseph Kent Barbay, Flourtown, PA (US);
Roger F. Bone, Bridgewater, NJ (US);
Ingrid Christa Deckman, Berwyn, PA (US);
Paul F. Jackson, Furlong, PA (US);
Lawrence C. Kuo, Gwynedd Valley, PA (US);
Frank A. Lewandowski, Philadelphia, PA (US);
Diane M. Maguire, Downingtown, PA (US);
Cynthia M. Milligan, Rutledge, PA (US);
Kenneth J. Rhodes, Belmont, MA (US);
Robert H. Scannevin, Hopkinton, MA (US);
Celine Schalk-Hihi, Phoenixville, PA (US);
Barry Springer, Wilmington, DE (US);
John C. Spurlino, Downingtown, PA (US);
Matthew J. Todd, Ambler, PA (US);
Brett A. Tounge, Blue Bell, PA (US);
Aihua Wang, Jamison, PA (US);
Janssen Pharmaceutica N.V., Beerse, BE;
Abstract
The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues. The present invention also relates to the use of small-molecule allosteric processing inhibitors for the treatment of diseases mediated by inappropriate matrix metalloproteinase (MMP) activity.