US 7,371,773 B2
	Breast cancer resistance protein (BCRP) inhibitor
Ryuta Yamazaki, Tokyo (Japan); Yukiko Nishiyama, Tokyo (Japan); Tomio Furuta, Tokyo (Japan); Takeshi Matsuzaki, Tokyo (Japan); Hiroshi Hatano, Tokyo (Japan); Oh Yoshida, Tokyo (Japan); Masato Nagaoka, Tokyo (Japan); Ritsuo Aiyama, Tokyo (Japan); Shusuke Hashimoto, Tokyo (Japan); and Yoshikazu Sugimoto, Chiba (Japan)
Assigned to Kabushiki Kaisha Yakult Honsha, Tokyo (Japan)
Appl. No. 10/544,064 PCT Filed Feb. 03, 2004, PCT No. PCT/JP2004/001067 § 371(c)(1), (2), (4) Date Aug. 02, 2005, PCT Pub. No. WO2004/069243, PCT Pub. Date Aug. 19, 2004.
Claims priority of application No. 2003-026856 (JP), filed on Feb. 04, 2003.
Prior Publication US 2006/0128636 A1, Jun. 15, 2006
Int. Cl. A61K 31/415 (2006.01)

U.S. Cl. 514—388  [514/402]

9 Claims

1. A method of inhibiting a breast cancer resistance protein (BCRP) comprising administering to a patient an effective amount of a diphenylacrylonitrile derivative represented by the following formula (1) or a salt thereof: 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 (—NHCOCH3 group), a cyano group (—CN group), a formyl group (—CHO group), —COOR1 (R1 is hydrogen or C1-C4 alkyl), —O(CH2)nCOOR2 (n=1-7: R2 is hydrogen or C1-C4 alkyl), —OOCCH2CH2COOR3 (R3 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 (—OP(O)(OH)2) or a salt thereof, a sulfate group (—OSO3H) 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.