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    Melanin production inhibitor
    27.
    发明公开
    Melanin production inhibitor 审中-公开
    黑色素生成抑制剂

    公开(公告)号：EP2845587A3

    公开(公告)日：2015-07-29

    申请号：EP14188830.5

    申请日：2009-12-22

    申请人： Pola Chemical Industries Inc.

    发明人： YOKOYAMA, Kouji ,  KIMURA, Makoto ,  TAMAI, Masashi ,  SAITOH, Yuko ,  KATO, Tomomi ,  IKEDA, Yu

    IPC分类号： A61K31/045 ,  A61K8/34 ,  A61K31/065 ,  A61K31/075 ,  A61K31/085 ,  A61K31/135 ,  A61K31/137 ,  A61K31/198 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4164 ,  A61K31/4409 ,  A61K31/444 ,  A61K31/4453 ,  A61K8/41 ,  A61K8/44 ,  A61K8/49 ,  A61Q19/02 ,  A61K8/46

    CPC分类号： A61K8/4946 ,  A61K8/31 ,  A61K8/34 ,  A61K8/41 ,  A61K8/411 ,  A61K8/418 ,  A61K8/44 ,  A61K8/46 ,  A61K8/49 ,  A61K8/4913 ,  A61K8/4926 ,  A61K8/494 ,  A61K2800/74 ,  A61Q19/02 ,  C07D207/12 ,  C07D207/404 ,  C07D213/30 ,  C07D213/38 ,  C07D233/58 ,  C07D295/03 ,  C07D295/096 ,  C07D401/06

    摘要： 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 C 1-8 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.

    摘要翻译： 本发明公开了黑色素生成抑制剂，其对黑色素的生成具有优异的抑制活性，安全性高。 黑色素生成抑制剂含有通式（1）所示的化合物（克霉唑除外）和/或其药理学上可接受的盐。 在式中，A 1，A 2和A 3独立地选自氢原子，可以具有取代基的芳基和可以具有取代基的芳族杂环基，其中A 1，A 2和A 3中的至少一个选自 芳基和芳族杂环基团中，A1，A2和A3中所含的碳原子总数为6至50，并且当A1，A2和A3中的至少两个表示芳基或芳族杂环基团时，相邻的两个 芳基或芳族杂环基团可以通过烷基链或链烯基链彼此连接形成环; m表示0至2的整数; X代表杂原子，氢原子或碳原子; R 1和R 2独立地选自氢原子和氧代基团，其中当R 1和R 2中的一个是氧代基团时，另一个不存在; 且R 3选自氢原子和其中氢原子或碳原子中的一个或一些可被杂原子或杂原子取代的C 1-8烃基，其中化合物中存在的R 3的数目对应于X 并且当存在两个或更多个R 3'时，R 3独立存在并且相邻的两个R 3可以彼此结合以与X一起形成环，并且R 3的末端可以与 碳原子与A1，A2和A3结合，从而形成环。