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    Melanin production inhibitor
    2.
    发明授权
    Melanin production inhibitor 有权
    黑色素生成抑制剂

    公开(公告)号：US08846012B2

    公开(公告)日：2014-09-30

    申请号：US13131827

    申请日：2009-12-22

    申请人： Kouji Yokoyama ,  Makoto Kimura ,  Masashi Tamai ,  Yuko Saitoh ,  Tomomi Kato ,  Yu Ikeda

    发明人： Kouji Yokoyama ,  Makoto Kimura ,  Masashi Tamai ,  Yuko Saitoh ,  Tomomi Kato ,  Yu Ikeda

    IPC分类号： A61K8/49 ,  C07D233/58 ,  C07D401/06 ,  A61K8/44 ,  A61K8/41 ,  A61K8/34 ,  C07D207/404 ,  A61Q19/02 ,  C07D213/38 ,  C07D213/30 ,  C07D295/03 ,  C07D207/12 ,  C07D295/096

    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 is 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. 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. When one of R1 and R2 is an oxo group, the other is not present. 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. 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： 公开了一种黑色素产生抑制剂，其对黑色素的生成具有优异的抑制活性，并且是高度安全的。 黑色素产生抑制剂由通式（1）表示（不包括克霉唑）和/或其药理学上可接受的盐。 在该式中，A1，A2和A3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。 A1，A2和A3中的至少一个选自芳基和芳族杂环基，A1，A2和A3中所含的碳原子总数为6〜50，A1，A2和A3中的至少2个 表示芳基或芳族杂环基，相邻的两个芳基或芳族杂环基可以通过烷基链或烯基链彼此结合形成环; m表示0〜2的整数。 X表示杂原子，氢原子或碳原子; R 1和R 2独立地选自氢原子和氧代基。 当R1和R2中的一个是氧代基时，另一个不存在。 R3选自氢原子和碳原子数为1〜8的烃基，其中一个或几个氢原子或碳原子可以被杂原子或杂原子取代。 化合物中存在的R3的数目对应于X，并且当存在两个或更多个R 3时，R 3独立地存在，并且相邻的两个R 3可以彼此结合形成与X一起形成环，并且末端 的R3可以结合到与A1，A2和A3结合的碳原子上，从而形成环。

    Biphenyl derivatives
    3.
    发明授权
    Biphenyl derivatives 失效
    联苯衍生物

    公开(公告)号：US07531576B2

    公开(公告)日：2009-05-12

    申请号：US10451408

    申请日：2001-12-05

    申请人： Takayuki Namiki ,  Kenichi Kishii ,  Masaki Mitani ,  Masashi Tamai ,  Naoki Hiyama ,  Makoto Kimura ,  Satoshi Ichinomiya

    发明人： Takayuki Namiki ,  Kenichi Kishii ,  Masaki Mitani ,  Masashi Tamai ,  Naoki Hiyama ,  Makoto Kimura ,  Satoshi Ichinomiya

    IPC分类号： A01N47/28 ,  A01N41/02 ,  A01N41/06 ,  A01N37/18 ,  C07C273/00 ,  C07C333/00 ,  C07C303/00 ,  C07C233/00

    CPC分类号： C07D257/04 ,  C07C275/30 ,  C07C311/09 ,  C07C311/60

    摘要： Biphenyl derivatives represented by the following formula (1): wherein R1 represents a C5-7 alkyl group, R2 represents a substituted or unsubstituted aromatic hydrocarbon, or cycloalkyl group, R3 represents a tetrazolyl group, —NHCOCF3, —NHSO2CF3 or —SO2NHCONHR4 in which R4 represents a substituted or unsubstituted aromatic hydrocarbon group, and Z represents a single bond, a C1-4 alkylene group or —SO2NH—, and salts thereof; and ACAT inhibitors and medicines containing them as active ingredients. The compounds according to the present invention possess excellent ACAT inhibitory activities, and are useful as preventives and/or therapeutics for diseases cased by the enhancement of ACAT activity, for example, hypercholesterolemia, atherosclerosis and the like.

    摘要翻译： 由下式（1）表示的联苯衍生物：其中R1表示C5-7烷基，R2表示取代或未取代的芳族烃或环烷基，R3表示四唑基，-NHCOCF3，-NHSO2CF3或-SO2NHCONHR4，其中 R4表示取代或未取代的芳族烃基，Z表示单键，C1-4亚烷基或-SO2NH-，及其盐; 和ACAT抑制剂和含有它们作为活性成分的药物。 根据本发明的化合物具有优异的ACAT抑制活性，并且可用作通过增强ACAT活性（例如高胆固醇血症，动脉粥样硬化等）而引起的疾病的预防剂和/或治疗剂。

    MELANIN PRODUCTION INHIBITOR
    5.
    发明申请
    MELANIN PRODUCTION INHIBITOR 有权
    MELANIN生产抑制剂

    公开(公告)号：US20110243865A1

    公开(公告)日：2011-10-06

    申请号：US13131827

    申请日：2009-12-22

    申请人： Kouji Yokoyama ,  Makoto Kimura ,  Masashi Tamai ,  Yuko Saitoh ,  Tomomi Kato ,  Yu Ikeda

    发明人： Kouji Yokoyama ,  Makoto Kimura ,  Masashi Tamai ,  Yuko Saitoh ,  Tomomi Kato ,  Yu Ikeda

    IPC分类号： A61K8/49 ,  C07D233/58 ,  C07D401/06 ,  A61K8/44 ,  C07C229/36 ,  A61K8/34 ,  C07C43/178 ,  A61K8/41 ,  C07C215/20 ,  C07C43/205 ,  C07C43/23 ,  C07C211/03 ,  C07D207/04 ,  C07D211/70 ,  C07D213/36 ,  C07D207/40 ,  C07D265/30 ,  C07D241/04 ,  A61Q19/02

    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 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 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 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.

    摘要翻译： 公开了一种黑色素产生抑制剂，其对黑色素的生成具有优异的抑制活性，并且是高度安全的。 黑色素生成抑制剂包含通式（1）表示的化合物（克霉唑除外）和/或其药理学上可接受的盐。 在该式中，A1，A2和A3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A1，A2和A3中的至少一个选自 芳基和芳香族杂环基时，A1，A2，A3中含有的碳原子总数为6〜50，A1，A2，A3中的至少2个为芳基或芳香族杂环基时， 两个芳基或芳族杂环基可以通过烷基链或烯基链彼此结合形成环; m表示0〜2的整数。 X表示杂原子，氢原子或碳原子; R 1和R 2独立地选自氢原子和氧代基，其中当R 1和R 2之一是氧代基时，另一个不存在; 和R3选自氢原子，其中一个或几个氢原子或碳原子可以被杂原子或杂原子取代的C1-8烃基，其中存在于化合物中的R3的数目对应于 X的数目，当存在两个或更多个R3时，R3独立地存在，并且相邻的两个R 3可以彼此结合形成与X一起形成环，并且R 3的末端可以与碳结合 与A1，A2和A3结合的原子，从而形成环。