ZHU, Zhaoning,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,CUMMI
申请号：
AU2013201438
公开号：
AU2013201438A1
申请日:
2013.03.07
申请国别(地区):
AU
年份:
2013
代理人:
摘要：
#$%^&*AU2013201438A120130328.pdf#####ABSTRACT NeR2 X N Rl I R3 I U W R4(I) 5 Disclosed are compounds of the formula (1) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, -C(=S)-, -S(O)-, -S(0) 2-, -C(=O)-, -0-, -C(R6)(R)-, -N(R5)or -C(=N(R5))- 10 X is -0-, -N(R5 )- or -C(R 6 )(R7)- provided that when X is -0-, U is not -0-, -S(O)-, -S(0) 2-, -C(=0)- or -C(=NR5)- U is a bond, -S(0)-, -S(0)2-, -C(0)-, -0-, -P(0)(OR15 )-, -C(=NR 5)-, -(C(R6)(R7))b- or -N(R5)- wherein b is 1 or 2 provided that when W is -S(0)-, -S(0) 2-, -0-, or -N(R5)-, U is not -S(0)-, -S(0) 2-, -0-, or -N(R5)- provided that 15 when X is -N(R5)- and W is -S(0)-, -S(0)2-, -0-, or -N(R5)-, then U is not a bond and R1, R2, R3, R4, R , R6, and R7 are as defined in the specification and pharmaceutical compositions comprising the compounds of formula (1). 20 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 25 using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist. 41216141 (GHM~ar) P8809.AU 1
