Patent ID: 6436906
Filing Date: 2002-08-20
Classification: A61K,A61P,C07H

Abstract:
A compound represented by the Formula: or a pharmaceutically acceptable salt, ester and prodrug thereof, whereinA is selected from the group consisting of; (1) â€”CHO, or a protected aldehyde (2) â€”CH2X, where X is selected from the group consisting of; a. hydroxy or protected hydroxy, b. halogen, c. â€”NR7R8, wherein R7 and R8 are each independently selected from hydrogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, C1-C6-alkyl, optionally substituted with aryl, substituted aryl, heterocyclic or substituted heterocyclic, C2-C6-alkenyl, optionally substituted with aryl, substituted aryl, heterocyclic or substituted heterocyclic and C2-C6-alkynyl, optionally substituted with aryl, substituted aryl, heterocyclic or substituted heterocyclic; or R7 and 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€”, â€”N(aryl), â€”N(heteroaryl), â€”Sâ€”, â€”S(O)â€” and â€”S(O)2â€”, d. â€”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. â€”S(O)nâ€”(C1-C6-alkyl), optionally substituted with aryl, substituted aryl, heterocyclic, or substituted heterocyclic, where n=0, 1 or 2, f. â€”S(O)nâ€”(C2-C6-alkenyl), optionally substituted with aryl, substituted aryl, heterocyclic or substituted heterocyclic, where n is as previously defined, g. â€”S(O)nâ€”(C2-C6-alkynyl), optionally substituted with aryl, substituted aryl, heterocyclic or substituted heterocyclic, where n is as previously defined h. â€”S(O)n-(aryl or heterocyclic), where n is as previously defined, and i. â€”O -(aryl or heterocyclic), (3) substituted or unsubstituted imidazole, arylimidazole or heteroarylimidazole, (4) substituted or unsubstituted oxazole, aryloxazole or heteroaryloxazole, (5) substituted or unsubstituted thioxazole, arylthioxazole or heteroarylthioxazole, (6) substituted or unsubstituted imidazoline, arylimidazoline or heteroarylimidazoline, (7) substituted or unsubstituted oxazoline, aryloxazoline or heteroaryloxazoline, and (8) substituted or unsubstituted thioxazoline, arylthioxazoline or heteroarylthioxazoline, One of R1 and R2 is hydrogen and the other is â€”NR7R8, where R7 and R8 are as previously defined 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, â€”Oâ€”R7 or â€”NR7R8, where R7 and R8 are as previously defined; and Rp is hydrogen or a hydroxy protecting group.