申请人:Hanyu Naoto
公开号:US08563552B2
公开(公告)日:2013-10-22
The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof:
wherein X1, X2, and X3 are each CR2 or N; R1, R2, and R3 are each H, C1-6 alkyl, C1-6 alkoxy, SH, OH, or NRbRc, wherein Rb and Rc are each H, C1-6 alkyl, or hydroxy-C1-6 alkyl, or NRbRc forms a saturated or unsaturated 5- or 6-membered hetero ring; and B is a substituted or unsubstituted pyrazole, imidazole, pyridine, or piperidine; with the proviso that at least one of R1, R3, R4, and R6 is a group other than C1-3 alkyl in the case where X1═X2═Y1═N and X3═CR2.
本发明提供了一种在黑色素生成抑制方面具有优异作用并可用作美白剂的化合物,以及含有该化合物的皮肤外用制剂。本发明的美白剂包含以下化合物作为活性成分:式(1)或其药理学上可接受的盐:其中,X1、X2和X3分别为CR2或N;R1、R2和R3分别为H、C1-6烷基、C1-6烷氧基、SH、OH或NRbRc,其中,Rb和Rc分别为H、C1-6烷基或羟基-C1-6烷基,或NRbRc形成饱和或不饱和的5-或6元杂环;B为取代或未取代的吡唑、咪唑、吡啶或哌啶;在X1═X2═Y1═N且X3═CR2的情况下,R1、R3、R4和R6中至少有一个为C1-3烷基以外的基团。