申请人:Yokoyama Kouji
公开号:US20110243865A1
公开(公告)日:2011-10-06
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 and A3 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 C
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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 the number of X's 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.
披露了一种黑色素生产抑制剂,它对黑色素的生产具有出色的抑制活性且高度安全。该黑色素生产抑制剂包括由通用公式(1)表示的化合物(不包括克霉唑)和/或其药理上可接受的盐。在公式中,A1、A2和A3独立地选自氢原子、可能带有取代基的芳基团和可能带有取代基的芳香杂环团,其中至少A1、A2和A3之一选自芳基团和芳香杂环团,A1、A2和A3中包含的碳原子总数为6至50,并且当至少两个A1、A2和A3表示芳基团或芳香杂环团时,相邻的两个芳基或芳香杂环团可以通过烷基链或烯基链相互连接形成环;m代表0至2的整数;X代表异原子、氢原子或碳原子;R1和R2独立地选自氢原子和氧代基,其中当R1和R2之一是氧代基时,另一个不出现;R3选自氢原子和C
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碳氢化合物组,其中一些或所有的氢原子或碳原子可能被异原子或异原子取代,其中化合物中存在的R3的数量对应于X的数量,并且当存在两个或更多R3时,R3独立地存在,并且相邻的两个R3可以相互连接以与X一起形成环,并且R3的末端可以与A1、A2和A3连接的碳原子结合,从而形成环。