Invention Grant
US08110682B2 Preparation and use of compounds as aspartyl protease inhibitors
有权
制备和使用化合物作为天冬氨酰蛋白酶抑制剂
- Patent Title: Preparation and use of compounds as aspartyl protease inhibitors
- Patent Title (中): 制备和使用化合物作为天冬氨酰蛋白酶抑制剂
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Application No.: US11451262Application Date: 2006-06-12
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Publication No.: US08110682B2Publication Date: 2012-02-07
- Inventor: Brian McKittrick , Zhaoning Zhu , Andrew Stamford , Elizabeth M. Smith
- Applicant: Brian McKittrick , Zhaoning Zhu , Andrew Stamford , Elizabeth M. Smith
- Applicant Address: US NJ Kenilworth
- Assignee: Schering Corporation
- Current Assignee: Schering Corporation
- Current Assignee Address: US NJ Kenilworth
- Agent Keith D. MacMillan; Gerard M. Devlin
- Main IPC: C07D251/42
- IPC: C07D251/42 ; C07D251/16 ; C07D251/22 ; A61K31/53 ; A61P3/10

Abstract:
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein A 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 bond and 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.
Public/Granted literature
- US20070010667A1 Preparation and use of compounds as aspartyl protease inhibitors Public/Granted day:2007-01-11
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