Robert Mazzola;Yuanzan C. Ye;Zhaoning Zhu;Johannes H. Voight;Corey Strickland;William J. Greenlee;Brian McKittrick;John Caldwell;Jared N. Cumming;Elizabeth M. Smith;Andrew W. Stamford;Li;Zhong-Yue Sun
发明人:
Zhaoning Zhu,Brian McKittrick,Zhong-Yue Sun,Yuanzan C. Ye,Johannes H. Voight,Corey Strickland,Elizabeth M. Smith,Andrew W. Stamford,William J. Greenlee,Robert Mazzola,John Caldwell,Jared N. Cumming,Li
申请号：
US13402521
公开号：
US20140057910A1
申请日:
2012.02.22
申请国别(地区):
US
年份:
2014
代理人:
摘要：
Disclosed are compounds of the formula Ior a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, whereinW is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—；X is —O—, —N(R5)— or —C(R6)(R7)—； provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—；U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—； wherein b is 1 or 2； provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—； provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond；and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification；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.
