NEW (POLY)AMINOALKYLAMINOALKYLAMIDE, ALKYL-UREA, OR ALKYL-SULFONAMIDE DERIVATIVES OF EPIPODOPHYLLOTOXIN, A PROCESS FOR PREPARING THEM, AND APPLICATION THEREOF IN THERAPY AS ANTICANCER AGENTS
IMBERT, THIERRY,GUMINSKI, YVES,BARRET, JEAN-MARC,KRUCZYNSKI, ANNA
申请号：
NZ59062509
公开号：
NZ590625A
申请日:
2009.08.19
申请国别(地区):
NZ
年份:
2012
代理人:
摘要：
Discloses are compounds derived from podophyllotoxin of the general formula 1, wherein: R represents hydrogen or C1-4alkyl, A represents CO(CH2)n, or CONH(CH2)n, where n = 2, 3, 4, or 5, R1 = H, or C1-4alkyl, R2 = (CH2)m-NR3R4, where m = 2, 3, 4, or 5, R3 = H, or C1-4alkyl, R4 = H, or C1-4alkyl, or (CH2)p-NR5R6, where p = 2, 3, 4, or 5, R5 = H, or C1-4alkyl, and R6 = = H, C1-4alkyl, or (CH2)q-NH2, where q = 2, 3, 4, or 5, or a pharmaceutically acceptable salt thereof. Examples of compounds of formula 1 include: 3-(2-Dimethylaminoethylamino)-N-[9-(4-hydroxy-3,5-dimethoxyphenyl)-8 -oxo-5,5a,6, 8,8a, 9-hexahydrofuro- [3 ,4: 6, 7]-naphtho [2, 3-d][ 1,3 ]dioxol-5-yl]-propionamide, and 4-(2-Dimethylaminoethylamino )-N-[9-( 4-hydroxy-3,5-dimethoxyphenyI)-8-oxo-5,5a,6,8,8a, 9-hexahydrofuro-(3 ,4 :6, 7]-naphtho [2,3-d][ 1,3]dioxol-5-yl]-butyramide. Further disclosed is a pharmaceutical composition, a process for preparing compounds of formula 1 and their use as a medicine, particularly as a medicine for the treatment of cancer.
