发明名称 BENZOPYRAN COMPOUNDS AS MELANOGENESIS MODIFIERS AND USES THEREOF
摘要 Provided are benzopyran compounds of formula I, for example, pomiferin-3′,4′-dimethyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation.;;wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.
申请公布号 US2015030551(A1) 申请公布日期 2015.01.29
申请号 US201414457634 申请日期 2014.08.12
申请人 ORLOW Seth J. 发明人 ORLOW Seth J.
分类号 C07D493/04;A61K31/353;A61K8/97;A61Q19/02;A61Q5/00;A61K36/60;A61K45/06;A61K8/49 主分类号 C07D493/04
代理机构 代理人
主权项 1. A method for inhibiting melanogenesis or a method for promoting skin lightening comprising administering to a mammal an effective amount of a compound of formula I: wherein R3 is selected from H, halo, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or substituted or unsubstituted aryl; and substituted or unsubstituted heteroaryl; R4 is selected from H, halo, hydroxy, alkoxy, alkenyloxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted phenyl; each R5, R6′ and R8 is independently selected from H, halo, hydroxy, alkoxy, alkenyloxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, and substituted or unsubstituted phenyl; R7 is selected from H, halo, hydroxy, alkoxy, alkenyloxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, or heterocycloalkyl; or R7 is —P(═O)(alkoxy)2, or —P(═S)(alkoxy)2; or R6 and R7 or R7 and R8 are joined to form a 5- or 6-membered heterocycloalkyl or heterocycloalkenyl; and the heterocycloalkyl or heterocycloalkenyl is unsubstituted or substituted with one more groups selected from alkyl, alkenyl, hydroxyalkyl, acyloxyalkyl, hydroxy, and alkoxy;or pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs, isotopic variants or prodrugs thereof.
地址 New York NY US