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:
Apr. 08, 2014

Filed:

Mar. 08, 2012
Applicants:

Zhaoning Zhu, Plainsboro, NJ (US);

Brian Mckittrick, New Vernon, NJ (US);

Zhong-yue Sun, Parlin, NJ (US);

Yuanzan C. YE, Edison, NJ (US);

Johannes H. Voight, Cranford, NJ (US);

Corey O. Strickland, Martinsville, NJ (US);

Elizabeth M. Smith, Verona, NJ (US);

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

William J. Greenlee, Teaneck, NJ (US);

Robert D. Mazzola, Jr., Stewartsville, NJ (US);

John P. Caldwell, Ringwood, NJ (US);

Jared N. Cumming, Garwood, NJ (US);

Lingyan Wang, East Brunswick, NJ (US);

Yusheng Wu, New York, NY (US);

Ulrich Iserloh, Hoboken, NJ (US);

Xiaoiang Liu, River Vale, NJ (US);

Tao Guo, Dayton, NJ (US);

Thuy X.e. Le, Monmouth Junction, NJ (US);

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

Suresh D. Babu, Plainsboro, NJ (US);

Rachael C. Hunter, Princeton, NJ (US);

Michelle L. Morris, Lawrenceville, NJ (US);

Huizhong Gu, Monmouth Junction, NJ (US);

Gang Qian, Kendall Park, NJ (US);

Dawit Tadesse, East Windsor, NJ (US);

Ying Huang, East Brunswick, NJ (US);

Guoqing LI, Belle Mead, NJ (US);

Jianping Pan, Monmouth Junction, NJ (US);

Jeffrey A. Misiaszek, Kenilworth, NJ (US);

Gaifa Lai, Monmouth Junction, NJ (US);

Jingqi Duo, Monmouth Junction, NJ (US);

Chuanxing Qu, Scotch Plains, NJ (US);

Yuefei Shao, Princeton, NJ (US);

Inventors:

Zhaoning Zhu, Plainsboro, NJ (US);

Brian McKittrick, New Vernon, NJ (US);

Zhong-Yue Sun, Parlin, NJ (US);

Yuanzan C. Ye, Edison, NJ (US);

Johannes H. Voight, Cranford, NJ (US);

Corey O. Strickland, Martinsville, NJ (US);

Elizabeth M. Smith, Verona, NJ (US);

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

William J. Greenlee, Teaneck, NJ (US);

Robert D. Mazzola, Jr., Stewartsville, NJ (US);

John P. Caldwell, Ringwood, NJ (US);

Jared N. Cumming, Garwood, NJ (US);

Lingyan Wang, East Brunswick, NJ (US);

Yusheng Wu, New York, NY (US);

Ulrich Iserloh, Hoboken, NJ (US);

Xiaoiang Liu, River Vale, NJ (US);

Tao Guo, Dayton, NJ (US);

Thuy X.E. Le, Monmouth Junction, NJ (US);

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

Suresh D. Babu, Plainsboro, NJ (US);

Rachael C. Hunter, Princeton, NJ (US);

Michelle L. Morris, Lawrenceville, NJ (US);

Huizhong Gu, Monmouth Junction, NJ (US);

Gang Qian, Kendall Park, NJ (US);

Dawit Tadesse, East Windsor, NJ (US);

Ying Huang, East Brunswick, NJ (US);

Guoqing Li, Belle Mead, NJ (US);

Jianping Pan, Monmouth Junction, NJ (US);

Jeffrey A. Misiaszek, Kenilworth, NJ (US);

Gaifa Lai, Monmouth Junction, NJ (US);

Jingqi Duo, Monmouth Junction, NJ (US);

Chuanxing Qu, Scotch Plains, NJ (US);

Yuefei Shao, Princeton, NJ (US);

Assignees:

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

Pharmacopeia Inc., La Jolla, CA (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
A01N 43/54 (2006.01); A61K 31/505 (2006.01); C07D 239/02 (2006.01);
U.S. Cl.
CPC ...
Abstract

Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein each variable in Formula 1 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods 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 magonist or mantagonist.


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