US 7,332,615 B2
Hydrophilic analogs of 4,8-dihydrobenzodithiophene-4,8-diones as anticancer agents
Pi-Tsan Huang, Hsinchu (Taiwan); Yen-Fang Wen, Hsinchu (Taiwan); Wuu-Chian Shin, Hsinchu (Taiwan); Mei-Hwai Chen, Hsinchu (Taiwan); Sheng-Chu Kuo, Taichung (Taiwan); and Kuo-Hsiung Lee, Chapel Hill, N.C. (US)
Assigned to Industrial Technology Research Institute, Hsinchu (Taiwan); and Yung Shin Pharm. Ind. Co., Ltd., Taichung (Taiwan)
Filed on Sep. 28, 2005, as Appl. No. 11/236,730.
Claims priority of provisional application 60/613225, filed on Sep. 28, 2004.
Prior Publication US 2006/0069041 A1, Mar. 30, 2006
Int. Cl. A61K 31/38 (2006.01); C07D 333/74 (2006.01)
U.S. Cl. 549—43  [549/44; 549/45; 549/48; 514/443] 19 Claims
 
1. A derivative of 4,8-dihydrobenzodithiophene-4,8-dione having the formulas (D) or (E):

OG Complex Work Unit Drawing
wherein Y and Z independently are O, S, —NH— or Se;
A1 and A2 independently are O, S, and NR5, wherein R5 is H or alkyl;
R1, R2, R3, and R4 independently are H, alkyl, —CR5R6—X—C (O)—(CH2)nCOOH, —CR5R6—X—(CH2)nCOOH, —CR5R6—X—(CH2)nNR5R6, —C (O)—NR6—(CR5R6)nCOOH, —C (O)—NR6—(CR5R6)nNR5R6, —CR5R6—C (O)—(CH2)nCOOH, CR5R6—X—C (O)—(CH2)nNR5R6, —C (O)—(CR5R6)nCOOH, —C (O)—(CR5R6)nNR5R6, —CR5═N—(CH2)nCOOH, —CR5═N—(CH2)nCOOH, —CR5═NO, or

OG Complex Work Unit Drawing
wherein X is O, S, or NH; R5 is defined as above; R6 is H or alkyl; and n is 1-5; subject to the proviso that at least one of R1, R2, R3, and R4 is a radical other than hydrogen and alkyl; or a pharmaceutically acceptable salt thereof.