Breast cancer resistance protein (bcrp) inhibitor

C - Chemistry – Metallurgy – 07 – C

Patent

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Details

C07C 255/34 (2006.01) A61K 31/277 (2006.01) A61P 35/00 (2006.01) C07H 17/04 (2006.01)

Patent

CA 2515174

A drug which inhibits BCRPs. It is a breast cancer resistance protein inhibitor which contains as an active ingredient either a diphenylacrylonitrile derivative represented by the following formula (1): (1) {wherein the eight R's are the same or different and each independently represents hydrogen, hydroxy, nitro, amino, acetylamino (-NHCOCH3), cyano (- CN), formyl (-CHO), -COOR1 (R1 is hydrogen or C1-4 alkyl), -O(CH2)nCOOR2 (n is 1 to 7 and R2 is hydrogen or C1-4 alkyl), -OOCH2CH2COOR3 (R3 is hydrogen, C1-4 alkyl, (Z)-2-(3,4-dimethoxyphenyl)-3-(4-hydroxyphenyl)acrylonitrile, or glycopyranosyl), C1-8 alkoxy, C1-4 alkyl, halogeno, ((C1-4 alkoxy)C1-4 alkoxy)C1-4 alkoxy, C2-8 acyloxy, C2-8 halogenoacyloxy, methylenedioxy, trifluoromethyl, phosphate group (-OP(O)(OH)2) or salt thereof, sulfate group (-OSO3H) or salt thereof, glycopyranosyl or salt thereof, a glycopyranosyl phosphate or salt thereof, glycopyranosyl sulfate or salt thereof, or piperidinopiperidinocarbonyloxy} or an ester or salt of the derivative.

L'invention concerne un médicament inhibant les BCRP. L'invention concerne un inhibiteur de protéine de résistance de cancer du sein contenant, en tant que principe actif, soit un diphénylacrylonitrile de formule (1) (dans laquelle les huit R sont identiques ou différents, et chacun représente indépendamment hydrogène, hydroxy, nitro, amino, acétylamino (-NHCOCH¿3?), cyano (-CN), formyle (-CHO), -COOR¿1? (R¿1? désigne hydrogène ou alkyle C¿1-4?), -O(CH¿2?)¿n?COOR¿2? (n est compris entre 1 et 7 et R¿2? désigne hydrogène ou alkyle C¿1-4?), -OOCH¿2?CH¿2?COOR¿3? (R¿3? désigne hydrogène, alkyle C¿1-4?, (Z)-2-(3,4-diméthoxyphényl)-3-(4-hydroxyphényl)acrylonitrile ou glycopyranosyl), alcoxy C¿1-8?, alkyle C¿1-4?, halogène, ((alcoxy C¿1-4?)alcoxy C¿1-4?)alcoxyC¿1-4?, acyloxy C¿2-8?, halogenoacyloxy C¿2-8?, méthylènedioxy, trifluorométhyle, un groupe phospate (-OP(O)(OH)¿2?) ou un sel de celui-ci, un groupe sulfate (-OSO¿3?H) ou un sel de celui-ci, du glycopyranosyle ou un sel de celui-ci, un phosphate de glycopyranosyle ou un sel de celui-ci, du sulfate de glycopyranosyle ou un sel de celui-ci, ou du pipéridinopipéridinocarbonyloxy), ou un ester, ou un sel de ce dérivé.

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