To provide heterocyclic aspartyl protease inhibitors, pharmaceutical compositions comprising the compounds, their use in the treatment of cardiovascular diseases, cognitive and neurodegenerative diseases, and their use as inhibitors of the Human Immunodeficiency Virus, plasmepsins, cathepsin D and protozoal enzymes.
Disclosed are compounds of the formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof; 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 m1 agonist or m2 antagonist.
MCKITTRICK BRIAN
SUN ZHONG-YUE
YE YUANZAN C
VOIGT JOHANNES H
STRICKLAND COREY
SMITH ELIZABETH M
STAMFORD ANDREW
GREENLEE WILLIAM J
MAZZOLA JR ROBERT D
CALDWELL JOHN
CUMMING JARED N
WANG LINGYAN
WU YUSHENG
ISERLOH ULRICH
LIU XIAOXIANG
HUANG YING
LI GUOQING
PAN JIANPING
MISIASZEK JEFFREY A
GUO TAO
LE THUY X H
SAIONZ KURT W
BABU SURESH D
HUNTER RACHAEL C
MORRIS MICHELLE L
GU HUIZHONG
QIAN GANG
TADESSE DAWIT
LAI GAIFA
DUO JINGQI
QU CHUANXING
SHAO YUEFEI
PHARMACOPEIA LLC
Natsuki Morishita