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US 7,741,345 B2Granted
AZA-peptide protease inhibitors
AssigneeGilead Sciences, Inc.
InventorsCarina E. Cannizzaro, James M. Chen, Manoj C. Desai, Michael L. Mitchell, Sundaramoorthi Swaminathan, Lianhong Xu
Life of this patent
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Abstract
The invention is related to compounds of Formula I: or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
Claims21
A compound of formula (I),
- wherein,
- X1 and X2 are each independently —C(O)—;
- Y is —O—;
- L1 is —O—, alkylene, substituted alkylene, alkenylene, substituted alkenylene, alkynylene, or substituted alkynylene;
- L2 is a covalent bond or —NR8—;
- with the proviso that when L1 is alkylene and L2 is a covalent bond, R1 is not a substituted heterocyclyl selected from the group of heterocyclyls consisting of:
- wherein U and V are independently O, S, or NH;
- n is 1 or 2;
- L3 and L5 are each independently a covalent bond, alkylene or substituted alkylene;
- L4 and L6 are each independently a bond, or —O—;
- Ar1 and Ar3 are each independently aryl or substituted aryl;
- Ar2 is heterocyclyl or sybstituted heterocyclyl;
- R1 is cycloalkyl, substituted cycloalkyl, cycloalkenyl, substituted cycloalkenyl, heterocyclyl, substituted heterocyclyl, or —C(O)OR9;
- R2, R4 and R5 are H;
- R3 is —OH;
- R6 and R6a are each independently H, halo, cyano, alkyl, substituted alkyl, haloalkyl, substituted haloalkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, heterocyclyl, substituted heterocyclyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl;
- R8 is H, alkyl, or substituted alkyl;
- R9 is H, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, or substituted alkynyl;
- m is 0 or 1;
- n is 0, 1 or 2;
- or a pharmaceutically acceptable salt, and/or ester thereof.
18 more elements
The compound of 1, wherein Ar2 is bicyclic-heterocyclyl having from 1 to 3 heteroatoms selected from O, S, and N.
Dependencies are inferred from the claim text.