Patent ID: 6440942
Filing Date: 2002-08-27
Classification: A61P,C07H

Abstract:
A compound represented by the Formula: or a pharmaceutically acceptable salt, ester and prodrug thereof, whereinA is: (1) CHO; (2) CH2-X, where X is selected from the group consisting of a. hydroxy or protected hydroxy, b. halogen, c. NR7R8 wherein R7 and R8 are each independently selected from the group consisting of hydrogen and C1-C6-alkyl optionally substituted with aryl, or heterocyclic groups; or R7and R8 taken together with the nitrogen atom to which they are connected form a 3- to 7-membered ring which, may optionally contain a hetero function selected from the group consisting of â€”Oâ€”, â€”NHâ€”, â€”N(C1-C6-alkyl)-, â€”N(aryl)-, â€”N(heteroaryl)- , â€”Sâ€”, â€”S(O)â€” and â€”S(O)2-, d. NR7C(O)â€”R9, where R7 is as previously defined and R9 is selected from the group consisting of i. C1-C6-alkyl optionally substituted with aryl, substituted aryl, heterocyclic or substituted heterocyclic, ii. aryl, iii. substituted aryl, iv. heterocyclic, and v. substituted heterocyclic, e. S(O)n-(C1-C6-alkyl) optionally substituted with aryl or a heterocyclic group where n=0, 1 or 2, f. S(O)n-(aryl or heterocyclic group) where n=0, 1 or 2, and g. O-(aryl or heterocyclic group); (3) an aldehyde protecting group (4) substituted or unsubstituted imidazole, arylimidazole or heteroarylimidazole (5) substituted or unsubstituted oxazole, aryloxazole or heteroaryloxazole (6) substituted or unsubstituted thioxazole, arylthioxazole or heteroarylthioxazole (7) substituted or unsubstituted imidazoline, arylimidazoline or heteroarylimidazoline (8) substituted or unsubstituted oxazoline, aryloxazoline or heteroaryloxazoline or (9) substituted or unsubstituted thioxazoline, arylthioxazoline or heteroarylthioxazoline R1 and R2 are each independently selected from the group consisting of (1) hydrogen, (2) hydroxy, (3) protected hydroxy, (4) OC(O)â€”C1-C12 alkyl, optionally substituted with aryl, substituted aryl, heterocyclic, substituted heterocyclic, (5) Oâ€”R7 where R7 is as previously defined, (6) halogen, and (7) R1and R2 taken together are oxo; R3, R4 and R5 are each independently selected from the group consisting of (1) hydrogen, (2) a hydroxy protecting group, and (3) C(O)â€”C1-C12 alkyl, optionally, substituted with aryl, substituted aryl, heterocyclic, substituted heterocyclic. Oâ€”R7 or NR7R8 where R7 and NR7R8 are as previously defined; and RP) is hydrogen or a hydroxy protecting group.