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.

Date of Patent:
Jan. 20, 2015

Filed:

Feb. 22, 2012
Applicants:

Kurt W. Saionz, Cranford, NJ (US);

Tao Guo, Dayton, NJ (US);

Andrew W. Stamford, Chatham Township, NJ (US);

Zhaoning Zhu, Plainsboro, NJ (US);

Inventors:

Kurt W. Saionz, Cranford, NJ (US);

Tao Guo, Dayton, NJ (US);

Andrew W. Stamford, Chatham Township, NJ (US);

Zhaoning Zhu, Plainsboro, NJ (US);

Assignees:

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

Pharmacopeia Drug Discovery, Inc., Princeton, NJ (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A61K 31/4245 (2006.01); C07D 271/07 (2006.01); A61K 31/5377 (2006.01); C07D 233/46 (2006.01); C07D 233/70 (2006.01); C07D 233/88 (2006.01); C07D 239/22 (2006.01); C07D 239/70 (2006.01); C07D 273/00 (2006.01); C07D 401/04 (2006.01); C07D 401/08 (2006.01); C07D 401/10 (2006.01); C07D 401/12 (2006.01); C07D 403/04 (2006.01); C07D 403/06 (2006.01); C07D 403/08 (2006.01); C07D 403/10 (2006.01); C07D 403/12 (2006.01); C07D 405/10 (2006.01); C07D 409/04 (2006.01); C07D 409/10 (2006.01); C07D 409/14 (2006.01); C07D 413/10 (2006.01); C07D 413/12 (2006.01); C07D 417/06 (2006.01); A61K 31/4168 (2006.01); A61K 31/4178 (2006.01); A61K 31/4184 (2006.01); A61K 31/4439 (2006.01); A61K 31/454 (2006.01); A61K 45/06 (2006.01); C07D 295/15 (2006.01); C07D 401/06 (2006.01); C07D 405/06 (2006.01); C07D 409/06 (2006.01);
U.S. Cl.
CPC ...
A61K 31/5377 (2013.01); C07D 233/46 (2013.01); C07D 233/70 (2013.01); C07D 233/88 (2013.01); C07D 239/22 (2013.01); C07D 239/70 (2013.01); C07D 271/07 (2013.01); C07D 273/00 (2013.01); C07D 401/04 (2013.01); C07D 401/08 (2013.01); C07D 401/10 (2013.01); C07D 401/12 (2013.01); C07D 403/04 (2013.01); C07D 403/06 (2013.01); C07D 403/08 (2013.01); C07D 403/10 (2013.01); C07D 403/12 (2013.01); C07D 405/10 (2013.01); C07D 409/04 (2013.01); C07D 409/10 (2013.01); C07D 409/14 (2013.01); C07D 413/10 (2013.01); C07D 413/12 (2013.01); C07D 417/06 (2013.01); A61K 31/4168 (2013.01); A61K 31/4178 (2013.01); A61K 31/4184 (2013.01); A61K 31/4439 (2013.01); A61K 31/454 (2013.01); A61K 45/06 (2013.01); C07D 295/15 (2013.01); C07D 401/06 (2013.01); C07D 405/06 (2013.01); C07D 409/06 (2013.01);
Abstract

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W, X, U, R, R, R, and R, are as defined herein, and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.


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