Patent ID: 6613747
Filing Date: 2003-09-02
Classification: A61P,C07H

Abstract:
A compound of Formula 1whereinR1 and R2 are independently selected from hydrogen, optionally substituted â€”CRfRg(C1-C8)alkyl, optionally substituted â€”CRfRg(C2-C8)alkenyl, optionally substituted â€”CRfRg(C2-C8)alkynyl, optionally substituted cycloalkyl, and optionally substituted (C5-C7)-cycloalkenyl, provided that R1 and R2 are not both hydrogen, wherein the substituents are 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€”CONaRb, 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; and Rf and Rg are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, heterocyclo, COORa, and CONRaRb; or R1 and R2, together with the nitrogen atom to which they are attached, form an optionally substituted nitrogen-containing heterocycle, wherein the substituents are 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€”CONaRb, â€”OCONRaRb, â€”NHCORa, â€”NHCOORa, and â€”NHCONRaRb; R3 is hydrogen or â€”Wâ€”V, wherein W is selected from the group consisting of (a) â€”NHâ€”(CH2)pâ€”, (b) â€”(CH2)qâ€”, (c) â€”Oâ€”(CH2)râ€”, (d) â€”NHâ€”C1-C6alkenyl-, (e) â€”C1-C6alkenyl-, (f) â€”Oâ€”C1-C6alkenyl-, (g) â€”NHâ€”C1-C6alkynyl-, (h) â€”C1-C6alkynyl-, and (i) â€”Oâ€”C1-C6alkynyl-; p is 0 to 5; q is 0 to 5; and r is 0 to 5; and V is selected from the group consisting of (a) hydrogen, (b) aryl, (c) substituted aryl, (d) heteroaryl, (e) substituted heteroaryl, and (f) Ar1-Ar2, wherein Ar1 and Ar2 are independently selected from the group consisting of (i) aryl, (ii) substituted aryl, (iii) heteroaryl, and (iv) substituted heteroaryl; R4 is selected from hydrogen, halogen, and hydroxy; R5 is hydrogen or a hydroxy protecting group; R6 is selected from hydrogen, 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; 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 Y and Yâ€², together with the carbon atom to which they are attached, form C&boxH;O, â€”CHOH, C&boxH;NRc, or C&boxH;NORc, wherein Rc is independently selected from hydrogen, alkyl, alkenyl and alkynyl; or an optical isomer, enantiomer, diastereomer, racemate or racemic mixture thereof, or a pharmaceutically acceptable salt, esters or pro-drugs thereof.