Zhaoning Zhu;Andrew Stamford;Elizabeth M. Smith;Brian McKittrick
发明人:
Brian McKittrick,Zhaoning Zhu,Andrew Stamford,Elizabeth M. Smith
申请号：
US11451262
公开号：
US08110682B2
申请日:
2006.06.12
申请国别(地区):
US
年份:
2012
代理人:
摘要：
Disclosed are compounds of the formula Ior a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof,whereinA is a bond, —C(O)—, or —C(R3′)(R4′)—；X is —N(R1)— or —C(R6)(R7)—；Y is —S(O)2—, —C(═O)—, —PO(OR9) or —C(R6′R7′)—； is a single or double bondand R, R1, R2, R3, R4, R3′, R4′, R5, R6, R6′, R7 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.
