公开(公告)号：US08563552B2

公开(公告)日：2013-10-22

申请号：US12866250

申请日：2009-02-06

申请人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

发明人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

IPC分类号： A61K31/535

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 pharmacologically acceptable salt thereof: wherein X1, X2, and X3 are each CR2 or N; R1, R2, and R3 are each H, C1-6 alkyl, C1-6 alkoxy, SH, OH, or NRbRc, wherein Rb and Rc are each H, C1-6 alkyl, or hydroxy-C1-6 alkyl, or NRbRc 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 R1, R3, R4, and R6 is a group other than C1-3 alkyl in the case where X1═X2═Y1═N and X3═CR2.

摘要翻译： 本发明提供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）表示的化合物或其药理学上可接受的盐：其中，X1，X2，X3各自为CR2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X1 = X2 = Y1 = N和X3 = CR2的情况下，R 1，R 3，R 4和R 6中的至少一个为不是C 1-3烷基的基团。

公开(公告)号：US08324234B2

公开(公告)日：2012-12-04

申请号：US12866062

申请日：2009-02-06

申请人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

发明人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

IPC分类号： A01N43/54 ,  C07D401/00

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 pharmacologically acceptable salt thereof: wherein, R1, R3, R4, and R6 are each independently C1-3 alkyl; and R2 and R5 are each independently a hydrogen atom or C1-3 alkyl.

摘要翻译： 本发明提供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）表示的化合物或其药理学上可接受的盐：其中，R 1，R 3，R 4和R 6各自独立地为C 1-3烷基; 并且R 2和R 5各自独立地为氢原子或C 1-3烷基。

公开(公告)号：US20110003817A1

公开(公告)日：2011-01-06

申请号：US12866250

申请日：2009-02-06

申请人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

发明人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

IPC分类号： A61K8/49 ,  C07D401/04 ,  C07D413/14 ,  C07D403/04 ,  C07D231/12 ,  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 pharmacologically acceptable salt thereof: wherein X1, X2, and X3 are each CR2 or N; R1, R2, and R3 are each H, C1-6 alkyl, C1-6 alkoxy, SH, OH, or NRbRc, wherein Rb and Rc are each H, C1-6 alkyl, or hydroxy-C1-6 alkyl, or NRbRc 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 R1, R3, R4, and R6 is a group other than C1-3 alkyl in the case where X1═X2═Y1═N and X3═CR2.

摘要翻译： 本发明提供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）表示的化合物或其药理学上可接受的盐：其中，X1，X2，X3各自为CR2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X1 = X2 = Y1 = N和X3 = CR2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。

公开(公告)号：US20100324096A1

公开(公告)日：2010-12-23

申请号：US12866472

申请日：2009-02-06

申请人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

发明人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

IPC分类号： A61K8/49 ,  C07D277/18 ,  C07D417/12 ,  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 C1-6 alkyl, C5-6 cycloalkyl, benzyl, benzylcarbonyl, benzoyl, phenyl, pyridyl or pyrimidyl; Ra is H, C1-6 alkyl, or C2-6 alkenyl; “” represents a single bond or a double bond wherein n=1 or 2; Y is S or O; and R3 and R4 are each independently H, C1-6 alkyl, hydroxy-C1-6 alkyl, C2-7 acyl, phenyl, pyridyl, pyrimidyl, etc.;with the proviso that at least one R3 is a group other than C1-3 alkyl in the case where: the hetero ring containing Y is a thiazoline ring; R4═Ra═H; X1═X2═CH; and either p =0 or R5═C1-6 alkyl.

摘要翻译： 本发明提供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C1-6烷基，C5-6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; 并且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是除C1- 3烷基，其中：含有Y的杂环是噻唑啉环; R4 = R = X1 = X2 = CH; 和p = 0或R5 = C1-6烷基。

公开(公告)号：US20120134944A1

公开(公告)日：2012-05-31

申请号：US13367577

申请日：2012-02-07

申请人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

发明人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

IPC分类号： A61K8/49 ,  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 R1, R2, and R2′ are each independently C1-3 alkyl; Y is S or O; and p is an integer of 0 to 3, wherein when p is 2 or 3, R1 may be the same or different.

摘要翻译： 本发明提供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R1，R2和R2'各自独立地为C1-3烷基; Y为S或O; p为0〜3的整数，p为2或3时，R 1可以相同或不同。

公开(公告)号：US20110003838A1

公开(公告)日：2011-01-06

申请号：US12866062

申请日：2009-02-06

申请人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

发明人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

IPC分类号： A61K8/49 ,  C07D403/04 ,  A61Q19/00

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 pharmacologically acceptable salt thereof: wherein, R1, R3, R4, and R6 are each independently C1-3 alkyl; and R2 and R5 are each independently a hydrogen atom or C1-3 alkyl.

摘要翻译： 本发明提供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）表示的化合物或其药理学上可接受的盐：其中，R 1，R 3，R 4和R 6各自独立地为C 1-3烷基; 并且R 2和R 5各自独立地为氢原子或C 1-3烷基。

公开(公告)号：US20100316584A1

公开(公告)日：2010-12-16

申请号：US12866460

申请日：2009-02-06

申请人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

发明人： Naoto Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

IPC分类号： A61K8/49 ,  C07D277/18 ,  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 R1, R2, and R2′ are each independently C1-3 alkyl; Y is S or O; and p is an integer of 0 to 3, wherein when p is 2 or 3, R1 may be the same or different.

摘要翻译： 本发明提供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R1，R2和R2'各自独立地为C1-3烷基; Y为S或O; p为0〜3的整数，p为2或3时，R 1可以相同或不同。

公开(公告)号：US08211412B2

公开(公告)日：2012-07-03

申请号：US13367577

申请日：2012-02-07

申请人： Naota Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

发明人： Naota Hanyu ,  Tomoko Saito ,  Takako Shibata ,  Kiyoshi Sato ,  Kimihiro Ogino

IPC分类号： A61K8/00 ,  C07D277/00 ,  C07D263/00

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 R1, R2, and R2′ are each independently C1-3 alkyl; Y is S or O; and p is an integer of 0 to 3, wherein when p is 2 or 3, R1 may be the same or different.

摘要翻译： 本发明提供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R1，R2和R2'各自独立地为C1-3烷基; Y为S或O; p为0〜3的整数，p为2或3时，R 1可以相同或不同。