申请人:Yamazaki Ryuta
公开号:US20060128636A1
公开(公告)日:2006-06-15
The invention provides a drug which inhibits BCRP.
A breast cancer resistance protein inhibitor containing, as an active ingredient, a diphenylacrylonitrile derivative represented by the following formula (1):
[wherein, each of 8 R's, which are the same or different from one another, represents a hydrogen atom, a hydroxyl group, a nitro group, an amino group, an acetylamino group (—NHCOCH
3
group); a cyano group (—CN group); a formyl group (—CHO group), —COOR
1
(R
1
is hydrogen or C1-C4 alkyl), —O(CH
2
)
n
COOR
2
(n=1−7: R
2
is hydrogen or C1-C4 alkyl), —OOCCH
2
CH
2
COOR
3
(R
3
is hydrogen, C1-C4 alkyl, (Z)-2-(3,4-dimethoxy-phenyl)-3-(4-hydroxy-phenyl)-acrylonitrile, or glycopyranosyl), a C1-C8 alkoxy group, a C1-C4 alkyl group, a halogen atom, a C1-C4 alkoxy C1-C4 alkoxy C1-C4 alkoxy group, a C2-C8 acyloxy group, a C2-C8 halogenoacyloxy group, a methylenedioxy group, a trifluoromethyl group, a phosphate group (i.e., —OP(O) (OH)
2
) or a salt thereof, a sulfate group (i.e., —OSO
3
H) or a salt thereof, a glycopyranosyl group or a salt thereof, a phosphate ester of a glycopyranosyl group or a salt of the ester, a sulfate ester of a glycopyranosyl group or a salt of the ester, or a piperidinopiperidinocarbonyloxy group], an ester thereof, or a salt thereof.
本发明提供了一种抑制BCRP的药物。一种含有以下式(1)所表示的二苯乙烯腈衍生物作为活性成分的乳腺癌耐药蛋白抑制剂:[其中,8个R分别表示氢原子、羟基、硝基、氨基、乙酰氨基(—NHCOCH3基)、氰基(—CN基)、甲酰基(—CHO基)、—COOR1(R1为氢或C1-C4烷基)、—O(CH2)nCOOR2(n = 1-7:R2为氢或C1-C4烷基)、—OOCCH2CH2COOR3(R3为氢、C1-C4烷基、(Z)-2-(3,4-二甲氧基苯基)-3-(4-羟基苯基)-丙烯腈或葡萄糖基)、C1-C8烷氧基、C1-C4烷基、卤原子、C1-C4烷氧基C1-C4烷氧基C1-C4烷氧基、C2-C8酰氧基、C2-C8卤代酰氧基、亚甲二氧基基团、三氟甲基基团、磷酸酯基团(即—OP(O)(OH)2)或其盐、硫酸酯基团(即—OSO3H)或其盐、葡萄糖基或其盐、葡萄糖基的磷酸酯或酯的盐、葡萄糖基的硫酸酯或酯的盐,或者是它的酯或盐。