申请人:Pola Chemical Industries Inc.
公开号:EP2845587A2
公开(公告)日:2015-03-11
Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole) and/or a pharmacologically acceptable salt thereof. In the formula, A1, A2 and A3 are independently selected from a hydrogen atom, an aryl group which may have a substituent, and an aromatic heterocyclic group which may have a substituent, wherein at least one of A1, A2 andA3 is selected from the aryl group and the aromatic heterocyclic group, the total number of carbon atoms contained in A1, A2 and A3 is 6 to 50 and, when at least two of A1, A2 and A3 represent the aryl groups or the aromatic heterocyclic groups, the adjacent two aryl or aromatic heterocyclic groups may be bound to each other via an alkyl chain or an alkenyl chain to form a ring; m represents an integer of 0 to 2; X represents a hetero atom, a hydrogen atom, or a carbon atom; R1 and R2 are independently selected from a hydrogen atom and an oxo group, wherein when one of R1 and R2 is an oxo group, the other is not present; and R3 is selected from a hydrogen atom, and a C1-8 hydrocarbon group in which one or some of hydrogen atoms or carbon atoms may be substituted by a hetero atom or hetero atoms, wherein the number of R3's present in the compound corresponds to X and, when two or more R3' s are present, the R3' s are independently present and the adjacent two R3's may be bound to each other to form, together with X, a ring, and the terminal of R3 may be bound to a carbon atom to which A1, A2 and A3 are bound, thereby forming a ring.
本发明公开了一种黑色素生成抑制剂,它对黑色素的生成具有极佳的抑制活性,且安全性高。黑色素生成抑制剂包括通式(1)代表的化合物(不包括克霉唑)和/或其药理上可接受的盐。式中,A1、A2 和 A3 独立选自氢原子、可具有取代基的芳基和可具有取代基的芳香杂环基团,其中 A1、A2 和 A3 中至少有一个选自芳基和芳香杂环基团、A1、A2 和 A3 所含的碳原子总数为 6 至 50,当 A1、A2 和 A3 中至少有两个代表芳基或芳香杂环基团时,相邻的两个芳基或芳香杂环基团可通过烷基链或烯基链相互结合形成一个环;m 代表 0 至 2 的整数; X 代表杂原子、氢原子或碳原子;R1 和 R2 分别独立地选自氢原子和氧代基团,其中当 R1 和 R2 中的一个是氧代基团时,另一个不存在;R3选自氢原子和C1-8烃基,其中一个或部分氢原子或碳原子可被一个或多个杂原子取代,其中化合物中存在的R3的数目与X相对应,当存在两个或多个R3's时,R3's独立存在,相邻的两个R3's可相互结合,与X一起形成一个环,R3的末端可与A1、A2和A3所结合的碳原子结合,从而形成一个环。