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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.:

US 8871796 B1

PDFFull Text
Date of Patent:
Oct. 28, 2014

Filed:

Oct. 05, 2010

Diaryl ether derivatives as notch sparing gamma secretase inhibitors

Applicants:

William Colby Brown, Cleveland Heights, OH (US);

Jason Brubaker, Cambridge, MA (US);

Christian Fischer, Natick, MA (US);

Richard W. Heidebrecht, Brookline, MA (US);

John T. Hendrix, Charlottesville, VA (US);

Elizabeth H. Kelley, Lynnfield, MA (US);

Rachel N. Maccoss, Brookline, MA (US);

Joey L. Methot, Westwood, MA (US);

Thomas Miller, Brookline, MA (US);

Karin M. Otte, Natick, MA (US);

Phieng Siliphaivanh, Newton, MA (US);

Thomas Reger, Lansdale, PA (US);

Peter D. Williams, Harleysville, PA (US);

Catherine M. Wiscount, Allentown, PA (US);

Inventors:

William Colby Brown, Cleveland Heights, OH (US);

Jason Brubaker, Cambridge, MA (US);

Christian Fischer, Natick, MA (US);

Richard W. Heidebrecht, Brookline, MA (US);

John T. Hendrix, Charlottesville, VA (US);

Elizabeth H. Kelley, Lynnfield, MA (US);

Rachel N. MacCoss, Brookline, MA (US);

Joey L. Methot, Westwood, MA (US);

Thomas Miller, Brookline, MA (US);

Karin M. Otte, Natick, MA (US);

Phieng Siliphaivanh, Newton, MA (US);

Thomas Reger, Lansdale, PA (US);

Peter D. Williams, Harleysville, PA (US);

Catherine M. Wiscount, Allentown, PA (US);

Assignee:

Merck Sharp & Dohme Corp., Rahway, NJ (US);

Attorneys:

J. Eric Thies

John C. Todaro

Primary Examiner:

Jeffrey S Lundgren

Assistant Examiner:

Michael Schmitt

Int. Cl.
CPC ...
A61K 31/415 (2006.01); C07D 401/00 (2006.01); C07D 421/00 (2006.01); C07D 405/10 (2006.01); C07D 413/12 (2006.01); C07D 409/12 (2006.01); C07D 417/12 (2006.01); C07D 231/22 (2006.01); C07D 413/14 (2006.01); C07D 491/113 (2006.01); C07D 405/12 (2006.01); C07D 401/04 (2006.01); C07D 405/14 (2006.01); C07D 401/12 (2006.01);
U.S. Cl.
CPC ...
C07D 231/22 (2013.01); C07D 405/10 (2013.01); C07D 413/12 (2013.01); C07D 409/12 (2013.01); C07D 417/12 (2013.01); C07D 413/14 (2013.01); C07D 491/113 (2013.01); C07D 405/12 (2013.01); C07D 401/04 (2013.01); C07D 405/14 (2013.01); C07D 401/12 (2013.01);
Abstract

The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative γ-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.

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