	US 7,524,883 B2
	Eponemycin and epoxomicin analogs and uses thereof
Sergei Agoulnik, Wilmington, Mass. (US); Kozo Akasaka, Belmont, Mass. (US); Frank Fang, Andover, Mass. (US); Jean-Christophe Harmange, Andover, Mass. (US); Lynn Hawkins, Concord, Mass. (US); Yimin Jiang, Londonderry, N.H. (US); Charles Johannes, Newbury, Mass. (US); Xiang-Yi Li, Andover, Mass. (US); Pamela McGuiness, Methuen, Mass. (US); Erin A. Murphy, Atkinson, N.H. (US); Shawn Schiller, Haverhill, Mass. (US); Mary Vermeulen, Ipswich, Mass. (US); and Jiayi Wu, Brookline, Mass. (US)
Assigned to Eisai R&D Management Co., Ltd., Tokyo (Japan)
Appl. No. 10/501,120 PCT Filed Jan. 08, 2003, PCT No. PCT/US03/00390 § 371(c)(1), (2), (4) Date Dec. 20, 2004, PCT Pub. No. WO03/059898, PCT Pub. Date Jul. 24, 2003.
Claims priority of provisional application 60/346711, filed on Jan. 08, 2002.
Claims priority of provisional application 60/373011, filed on Apr. 16, 2002.
Prior Publication US 2005/0101781 A1, May 12, 2005
Int. Cl. C07D 303/46 (2006.01); A61K 31/336 (2006.01)

U.S. Cl. 514—475 [514/307; 514/314; 514/414; 514/456; 514/457; 514/466; 546/146; 546/169; 548/467; 549/402; 549/405; 549/435; 549/548]

52 Claims

1. A compound having the structure (I):

or pharmaceutically acceptable derivative thereof;

wherein each occurrence of A, J, E, D and G is independently CR_A, CR_AR_B, C═O, O, S, NR_A, or N, wherein each occurrence of R_Aand R_Bis independently hydrogen, a protecting group, or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety;

A and J, J and D, D and E, and D and G are each independently linked by a single or double bond as valency permits;

w, x, y and z are each independently 0, 1, 2, 3, 4, 5 or 6, but the sum of x, y and z is 2-6;

R₁, R₂, R₃and R₄are each independently hydrogen, halogen, —CN, —OR_C, —SR_C, —NR_CR_D, —(C═O)R_Cor an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety, wherein each occurrence of R_Cand R_Dis independently hydrogen, a protecting group, or an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety, or R_Cand R_D, taken together, form a heteroalicyclic or heteroaryl moiety; or wherein any two adjacent groups R₁, R₂, R₃and R₄, taken together, form an alicyclic or heteroalicyclic moiety, or an aryl or heteroaryl moiety;

R₅and R₆are each independently an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety; and Q is an epoxycarbonyl moiety having the structure:

wherein R^Q1is hydrogen, an aliphatic, alicyclic, heteroaliphatic, heteroalicyclic, aryl or heteroaryl moiety, an oxygen protecting group or a prodrug moiety.