申请人:The Procter & Gamble Company
公开号:US06068834A1
公开(公告)日:2000-05-30
This invention relates to compositions, compounds and methods for lightening skin, using active compounds having the structure: ##STR1## wherein: (i) each X is, independently, selected from the group consisting of halo, alkyl, substituted alkyl, aryl, OR, OCOR, COR, CONRR COOR, CN, SR, SOR, SO.sub.2 R, SO.sub.3 R and NRR, wherein X is other than hydroxy, amino and thio, if this X is attached ortho to the phenol hydroxy; (ii) m is an integer from 0 to 4; (iii) each R' and each R" is, independently, selected from the group consisting of hydrogen, halo, alkyl, substituted alkyl, aryl, OR, OCOR, OCRROR, COR, CR(OR)OR, CONRR, COOR, CRROR, CN, SR, and NRR; wherein halo, when it appears, is other than geminal to a hydroxy, NH.sub.2, or SH; (iv) R'" is alkyl or substituted alkyl; wherein when R'" is present, wherein when R'" is present and R' is also hydrogen, R" is other than hydrogen, hydroxy, halo, thio, cyano and amino; (v) each R is, independently, selected from the group consisting of hydrogen, alkyl, substituted alkyl and aryl; (vi) n is an integer from 1 to about 5, wherein at least one carbon in (C)n has other than alkyl or hydroxy as a substituent and (C)n adjacent to Z has other than amino, SH, CN or hydroxy as R'; (vii) Z is selected from the group consisting of O, NR, S, SO, SO.sub.2, PO.sub.2 R and POR; (viii) wherein any carbon, when disubstituted, having as one substituent selected from the group consisting of hydroxy, amino, cyano and thiol, has the other substituent selected from the group consisting of hydrogen, alkyl, and aryl, whether this substituent is R' or R"; and to pharmaceutically acceptable salts of these compounds, stereoisomers and enantiomers thereof free from or mixed with other enantiomers or stereoisomers; and such compounds in compositions with a pharmaceutically-acceptable carrier thereof comprising a safe and effective amount of a subject skin lightening active.
本发明涉及用具有以下结构的活性化合物的组合物、化合物和用于美白皮肤的方法:##STR1## 其中:(i) 每个X独立地选自卤素、烷基、取代烷基、芳基、OR、OCOR、COR、CONRR、COOR、CN、SR、SOR、SO.sub.2R、SO.sub.3R 和NRR 组成的群中,其中X不是羟基、氨基和硫代基,如果此X连接到苯酚羟基的正交位;(ii) m是从0到4的整数;(iii) 每个R'和每个R"独立地选自氢、卤素、烷基、取代烷基、芳基、OR、OCOR、OCRROR、COR、CR(OR)OR、CONRR、COOR、CRROR、CN、SR 和NRR 组成的群中,其中卤素在出现时不与羟基、NH.sub.2 或SH成键;(iv) R'"是烷基或取代烷基;当R'"存在时,当R'也为氢时,R"不是氢、羟基、卤素、硫代基、氰基和氨基;(v) 每个R独立地选自氢、烷基、取代烷基和芳基;(vi) n是从1到约5的整数,其中(C)n中至少有一个碳原子的取代基不是烷基或羟基,且(C)n邻近Z的取代基不是氨基、SH、CN 或羟基作为R';(vii) Z选自O、NR、S、SO、SO.sub.2、PO.sub.2R 和POR 组成的群;(viii) 当二取代的碳原子有一个取代基选自羟基、氨基、氰基和硫醇时,另一个取代基选自氢、烷基和芳基,无论这个取代基是R'还是R";以及这些化合物的药学上可接受的盐、其立体异构体和对映异构体,不含其他对映异构体或立体异构体的纯形式或混合形式;以及这种化合物与药学上可接受的载体组成的组合物,其中该组合物包含一种主题皮肤美白活性的安全有效量。