Patent ID: 6825172
Filing Date: 2004-11-30
Classification: A61P,C07H

Abstract:
A compound of Formula 1whereinR1 is selected from hydrogen, optionally substituted C1-C8-alkyl, optionally substituted C2-C8-alkenyl, and optionally substituted C2-C8-alkynyl, wherein the substituents are independently selected from halogen, alkyl, alkenyl, alkynyl, cycloalkyl, oxo, aryl, heteroaryl, heterocyclo, CN, nitro, â€”COORa, â€”OCORa, â€”ORa, â€”SRa, â€”SORa, â€”SO2Ra, â€”NRaRb, â€”CONRaRb, â€”OCONRaRb, â€”NHCORa, â€”NHCOORa, and â€”NHCONRaRb, wherein Ra and Rb are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclo, aralkyl, heteroaralkyl, and heterocycloalkyl; R2 is selected from hydrogen, alkoxy, optionally substituted C1-C8-alkyl, optionally substituted C2-C8-alkenyl, and optionally substituted C2-C8-alkynyl, wherein the substituents are independently selected from halogen, alkyl, alkenyl, alkynyl, cycloalkyl, oxo, aryl, heteroaryl, heterocyclo, CN, nitro, â€”COORa, â€”OCORa, â€”ORa, â€”SRa, â€”SORa, â€”SO2Ra, â€”NRaRb, â€”CONRaRb, â€”OCONRaRb, â€”NHCORa, â€”NHCOORa, and â€”NHCONRaRb, wherein Ra and Rb are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclo, aralkyl, heteroaralkyl, and heterocycloalkyl; R3 is selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, cycloalkyl, optionally substituted aryl, and optionally substituted heteroaryl; R4 is hydrogen or a hydroxy protecting group; R5 is selected from hydrogen, C1-C8-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, aryl, heteroaryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl, C3-C6-cycloalkyl, C5-C8-cycloalkenyl, alkoxyalkyl containing 1-6 carbon atoms in each alkyl or alkoxy group, and alkylthioalkyl containing 1-6 carbon atoms in each alkyl or thioalkyl group; L is absent or C(O); W is O; X and Xâ€², together with the carbon atom to which they are attached, form C&boxH;O, C&boxH;NRc, or C&boxH;NORc, wherein Rc is independently selected from hydrogen, alkyl, alkenyl and alkynyl; and Z is selected from C(O), C(O)â€”O, C(O)â€”NR2, and SO2; and R6 is selected from optionally substituted aryl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted cycloalkyl, optionally substituted C1-C8-alkyl, optionally substituted C2-C8-alkenyl, and optionally substituted C2-C8-alkynyl, wherein the substituents are selected from halogen, alkyl, alkenyl, alkynyl, cycloalkyl, oxo, alkoxyimino, aryl, heteroaryl, heterocyclo, CN, nitro, â€”COORa, â€”OCORa, â€”ORa, â€”SRa, SORa, â€”SO2Ra, â€”NRaRb, â€”CONRaRb, â€”OCONRaRb, â€”NHCORa, â€”NHCOORa, and â€”NHCONRaRb, wherein Ra and Rb are independently selected from hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclo, aralkyl, heteroaralkyl, and heterocycloalkyl, or NR2R6 taken together form heterocyclyl having at least one N atom; or an optical isomer, enantiomer, diastereomer, racemate or racemic mixture thereof, or a pharmaceutically acceptable salt, esters or pro-drugs thereof.