Patent ID: 6680299
Filing Date: 2004-01-20
Classification: A61P,C07H

Abstract:
A compound represented by the Formula: wherein A is selected from the group consisting of; (1) CHO or a protected aldehyde, (2) CH2X, wherein 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 hydrogen, C1-C6-alkyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, C2-C6-alkynyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic or R7R8 taken 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)2â€”, 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 one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, ii. C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, iii. C2-C6-alkynyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, iv. aryl, v. substituted aryl, vi. heterocyclic, and vii. substituted heterocyclic e. NR7C(O)â€”NR8R9, where R7, R8, and R9 are as previously defined, f. S(O)nâ€”R10, where R10 is selected from the group consisting of aryl, substituted aryl, heterocyclic and substituted heterocyclic and where n=0, 1 or 2, g. S(O)nâ€”(C1-C6-alkyl), optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined, h. S(O)nâ€”(C2-C6-alkenyl), optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined i. S(O)nâ€”(C2-C6-alkynyl), optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, where n is as previously defined, and j. Oâ€”Mâ€”Y, where M is (i) absent, (ii) â€”C(O)â€”(iii) â€”C(O)N(R7)-, where R7 is as previously defined, (iv) C1-C6-alkyl-N(R7)-, where R7 is as previously defined, (v) C2-C6-alkenyl-N(R7)-, where R7 is as previously defined, and (vi) C2-C6-alkynyl-N(R7)-, where R7 is as previously defined and where Y is (i) hydrogen (ii) C2-C6-alkyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, (iii) C2-C6-alkenyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted hetreocyclic, (iv) C2-C6-alkynyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic and substituted heterocyclic, (v) aryl, (vi) substituted aryl, (vii) heterocyclic, or (viii) substituted heterocyclic, provided that when M is absent, Y is not hydrogen; (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 and (9) 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-C 12-alkyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, Oâ€”R7 and NR7R8 where R7 and R8 are as previously defined, (5) Oâ€”R7, where R7 is as previously defined, (6) halogen, (7) R1 and R2 taken together are oxo, and (8) NR7R8, where R7 and R8 are as previously defined; R3 is selected from the group consisting of; (1 ) hydrogen, (2) a hydroxy protecting group, and (3) C(O)â€”C1-C12 alkyl, optionally substituted with one or more substituents selected from the group consisting of halogen, aryl, substituted aryl, heterocyclic, substituted heterocyclic, Oâ€”R7 and NR7R8 where R7 and R8 are as previously defined; R4 is Oâ€”Mâ€”Y, where M and Y are as previously defined, and Rp is hydrogen or a hydroxy protecting group.