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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 9611261 B1

PDFFull Text
Date of Patent:
Apr. 04, 2017

Filed:

Nov. 04, 2015

Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use

Applicant:

Amgen Inc., Thousand Oaks, CA (US);

Inventors:

Ana Elena Minatti, Santa Monica, CA (US);

Jonathan D. Low, Reseda, CA (US);

Jennifer R. Allen, Newbury Park, CA (US);

Albert Amegadzie, Moorpark, CA (US);

James Brown, Moorpark, CA (US);

Michael J. Frohn, Thousand Oaks, CA (US);

Angel Guzman-Perez, Belmont, MA (US);

Paul E. Harrington, Camarillo, CA (US);

Patricia Lopez, Woodland Hills, CA (US);

Vu Van Ma, Oak Park, CA (US);

Nobuko Nishimura, West Hills, CA (US);

Wenyuan Qian, Newbury Park, CA (US);

Shannon Rumfelt, Camarillo, CA (US);

Robert M. Rzasa, Ventura, CA (US);

Kelvin Sham, Thousand Oaks, CA (US);

Adrian L. Smith, Simi Valley, CA (US);

Ryan White, Somerville, MA (US);

Qiufen Xue, Newbury Park, CA (US);

Assignee:

Amgen Inc., Thousand Oaks, CA (US);

Attorney:
Primary Examiner:

Kahsay Habte

Int. Cl.
CPC ...
C07D 471/04 (2006.01); C07D 265/12 (2006.01); C07D 413/14 (2006.01); C07D 413/12 (2006.01); C07D 417/14 (2006.01); C07D 417/12 (2006.01); C07D 413/10 (2006.01); C07D 491/048 (2006.01); C07D 413/04 (2006.01);
U.S. Cl.
CPC ...
C07D 413/12 (2013.01); C07D 265/12 (2013.01); C07D 413/04 (2013.01); C07D 413/10 (2013.01); C07D 413/14 (2013.01); C07D 417/12 (2013.01); C07D 417/14 (2013.01); C07D 471/04 (2013.01); C07D 491/048 (2013.01);
Abstract

The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A, A, A, A, each of R, R, R, R, Rand Rof Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.

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