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    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN
    1.
    发明公开
    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN 审中-公开
    HAUTBLEICHMITTEL UND EXTERNESPRÄPARATFÜRDIE HAUT

    公开(公告)号：EP2251001A1

    公开(公告)日：2010-11-17

    申请号：EP09709400.7

    申请日：2009-02-06

    申请人： Shiseido Company, Ltd.

    发明人： HANYU, Naoto ,  SAITO, Tomoko ,  SHIBATA, Takako ,  SATO, Kiyoshi ,  OGINO, Kimihiro

    IPC分类号： A61K8/49 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4439 ,  A61K31/506 ,  A61P17/00 ,  A61Q19/02

    CPC分类号： A61K31/4439 ,  A61K8/4946 ,  A61K31/506 ,  A61Q19/02

    摘要： The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a heterocyclic compound represented by formula (1) or a pharmacologically acceptable salt thereof:

    wherein A is C 1-6 alkyl, C 5-6 cycloalkyl, benzyl, benzylcarbonyl, benzoyl, phenyl, pyridyl or pyrimidyl; Ra is H, C 1-6 alkyl, or C 2-6 alkenyl; " - - - " represents a single bond or a double bond whereinn = 1 or 2; Y is S or O; and R 3 and R 4 are each independently H, C 1-6 alkyl, hydroxy-C 1-6 alkyl, C 2-7 acyl, phenyl, pyridyl, pyrimidyl, etc.;with the proviso that at least one R 3 is a group other than C 1-3 alkyl in the case where: the hetero ring containing Y is a thiazoline ring; R 4 = Ra = H; X 1 = X 2 = CH; and either p = 0 or R 5 = C 1-6 alkyl.

    摘要翻译： 本发明提供了对黑素生成具有优异抑制作用并可用作增白剂的化合物和含有该化合物的皮肤外用制剂。 本发明的增白剂作为活性成分，含有式（1）表示的杂环化合物或其药理学上可接受的盐：其中A为C 1-6烷基，C 5-6环烷基，苄基，苄基羰基，苯甲酰基 ，苯基，吡啶基或嘧啶基; R a是H，C 1-6烷基或C 2-6烯基; “ - - - ”表示单键或双键，其中n = 1或2; Y为S或O; R 3和R 4各自独立地为H，C 1-6烷基，羟基-C 1-6烷基，C 2-7酰基，苯基，吡啶基，嘧啶基等;条件是至少一个R 3为 在含有Y的杂环是噻唑啉环的情况下是C 1-3烷基以外的基团; R 4 = Ra = H; X 1 = X 2 = CH; p = 0或R 5 = C 1-6烷基。

    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN
    4.
    发明授权
    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN 有权
    皮肤美白剂和皮肤外用制剂

    公开(公告)号：EP2250999B1

    公开(公告)日：2016-04-13

    申请号：EP09707883.6

    申请日：2009-02-06

    申请人： Shiseido Company, Ltd.

    发明人： HANYU, Naoto ,  SAITO, Tomoko ,  SHIBATA, Takako ,  SATO, Kiyoshi ,  OGINO, Kimihiro

    IPC分类号： A61K8/49 ,  A61K31/4439 ,  A61K31/506 ,  A61P17/00 ,  A61Q19/02

    CPC分类号： A61K31/4439 ,  A61K8/4946 ,  A61K31/506 ,  A61Q19/02

    摘要： The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a heterocyclic compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein A is C 1-6 alkyl, C 5-6 cycloalkyl, benzyl, benzylcarbonyl, benzoyl, phenyl, pyridyl or pyrimidyl; Ra is H, C 1-6 alkyl, or C 2-6 alkenyl; " - - - " represents a single bond or a double bond whereinn = 1 or 2; Y is S or O; and R 3 and R 4 are each independently H, C 1-6 alkyl, hydroxy-C 1-6 alkyl, C 2-7 acyl, phenyl, pyridyl, pyrimidyl, etc.;with the proviso that at least one R 3 is a group other than C 1-3 alkyl in the case where: the hetero ring containing Y is a thiazoline ring; R 4 = Ra = H; X 1 = X 2 = CH; and either p = 0 or R 5 = C 1-6 alkyl.

    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN
    7.
    发明公开
    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN 有权
    HAUTAUFHELLUNGSMITTEL EXTERNE ZUBEREITUNGFÜRDIE HAUT

    公开(公告)号：EP2251000A1

    公开(公告)日：2010-11-17

    申请号：EP09709047.6

    申请日：2009-02-06

    申请人： Shiseido Company, Ltd.

    发明人： HANYU, Naoto ,  SAITO, Tomoko ,  SHIBATA, Takako ,  SATO, Kiyoshi ,  OGINO, Kimihiro

    IPC分类号： A61K8/49 ,  A61K31/421 ,  A61K31/426 ,  A61P17/00 ,  A61Q19/02

    CPC分类号： A61K31/4439 ,  A61K8/4946 ,  A61K31/506 ,  A61Q19/02

    摘要： The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a heterocyclic compound represented by formula (1) or a pharmacologically acceptable salt thereof:

    wherein R 1 , R 2 , and R 2 ' are each independently C 1-3 alkyl; Y is S or O; and p is an integer of 0 to 3, whereinwhen p is 2 or 3, R 1 may be the same or different.

    摘要翻译： 本发明提供了对黑素生成具有优异抑制作用并可用作增白剂的化合物和含有该化合物的皮肤外用制剂。 作为活性成分，本发明的增白剂含有式（1）表示的杂环化合物或其药理学上可接受的盐：其中R 1，R 2和R 2'各自独立地为C 1-3烷基; Y为S或O; p为0〜3的整数，p为2或3时，R 1可以相同也可以不同。

    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN
    8.
    发明公开
    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN 有权
    皮肤美白剂和皮肤外用制剂

    公开(公告)号：EP2250999A1

    公开(公告)日：2010-11-17

    申请号：EP09707883.6

    申请日：2009-02-06

    申请人： Shiseido Company, Ltd.

    发明人： HANYU, Naoto ,  SAITO, Tomoko ,  SHIBATA, Takako ,  SATO, Kiyoshi ,  OGINO, Kimihiro

    IPC分类号： A61K8/49 ,  A61K31/4439 ,  A61K31/506 ,  A61P17/00 ,  A61Q19/02

    CPC分类号： A61K31/4439 ,  A61K8/4946 ,  A61K31/506 ,  A61Q19/02

    摘要： The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologicallyacceptable salt thereof:

    wherein, R 1 , R 3 , R 4 , and R 6 are each independently C 1-3 alkyl; and R 2 and R 5 are each independently a hydrogen atom or C 1-3 alkyl.

    摘要翻译： 本发明提供对黑色素生成具有优异的抑制作用并且可用作美白剂的化合物以及含有该化合物的皮肤外用剂。 本发明的美白剂含有式（1）所示的化合物或其药理学上可接受的盐作为有效成分，式中，R 1，R 3，R 4和R 6分别独立地为C 1-3烷基; 并且R2和R5各自独立地为氢原子或C1-3烷基。

    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN
    9.
    发明公开
    SKIN WHITENING AGENT AND EXTERNAL PREPARATION FOR THE SKIN 有权
    HAUTAUFHELLUNGSMITTEL UNDÄUSSERLICHESPRÄPARATFÜRDIE HAUT

    公开(公告)号：EP2250998A1

    公开(公告)日：2010-11-17

    申请号：EP09707325.8

    申请日：2009-02-06

    申请人： Shiseido Company, Ltd.

    发明人： HANYU, Naoto ,  SAITO, Tomoko ,  SHIBATA, Takako ,  SATO, Kiyoshi ,  OGINO, Kimihiro

    IPC分类号： A61K8/49 ,  A61K31/4439 ,  A61K31/506 ,  A61P17/00 ,  A61Q19/02

    CPC分类号： A61K31/4439 ,  A61K8/4946 ,  A61K31/506 ,  A61Q19/02

    摘要： The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologicallyacceptable salt thereof:

    wherein X 1 , X 2 , and X 3 are each CR 2 or N; R 1 , R 2 , and R 3 are each H, C 1-6 alkyl, C 1-6 alkoxy, SH, OH, or NR b R c , wherein R b and R c are each H, C 1-6 alkyl, or hydroxy-C 1-6 alkyl, or NR b R c forms a saturated or unsaturated 5- or 6-membered hetero ring; and B is a substituted or unsubstituted pyrazole, imidazole, pyridine, or piperidine; with the proviso that at least one of R 1 , R 3 , R 4 , and R 6 is a group other than C 1-3 alkyl in the case where X 1 = X 2 = Y 1 = N and X 3 = CR 2 .

    摘要翻译： 本发明提供了对黑素生成具有优异抑制作用并可用作增白剂的化合物和含有该化合物的皮肤外用制剂。 作为活性成分，本发明的增白剂含有式（1）表示的化合物或其药理学上可接受的盐：其中X 1，X 2和X 3各自为CR 2或N; R 1，R 2和R 3各自为H，C 1-6烷基，C 1-6烷氧基，SH，OH或NR b R c，其中R b和R c各自为H，C 1-6烷基 或羟基-C 1-6烷基，或NR b R c形成饱和或不饱和的5-或6-元杂环; B是取代或未取代的吡唑，咪唑，吡啶或哌啶; 条件是在X 1 = X 2 = Y 1 = N且X 3 = CR 2的情况下，R 1，R 3，R 4和R 6中的至少一个为C 1-3烷基以外的基团 。