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1. 发明申请

US20090215893A1 Parakeratosis inhibitor, pore-shrinking agent,or rough skin preventing/ameliorating agent, and external composition for skin 审中-公开
标题翻译：角化不全抑制剂，孔收缩剂或粗糙皮肤防止/改善剂，以及皮肤外用组合物
公开(公告)号：US20090215893A1
公开(公告)日：2009-08-27
申请号：US11920848
申请日：2006-05-09
申请人： Mikiko Kaminuma , Masaru Suetsugu , Maki Kaneko , Toshii Iida , Shinji Inomata
发明人： Mikiko Kaminuma , Masaru Suetsugu , Maki Kaneko , Toshii Iida , Shinji Inomata
IPC分类号： A61K31/19
CPC分类号： A61K8/0212 , A61K8/44 , A61K8/46 , A61Q1/02 , A61Q19/00
摘要： The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin-inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and to further provide an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor agent, pore-shrinking agent, or rough skin preventing/amaliorating agent comprises one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof. The external composition for skin comprises the one, two, or more compounds selected from the group consisting of α-amino acid derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent.
摘要翻译：本发明提供了具有角化不全抑制，孔收缩或粗糙皮肤抑制/消瘦等功能的角化不全抑制剂，孔收缩剂或粗糙皮肤防止/缓解剂，不会引起感觉刺激等安全性问题，而且并且为了进一步提供添加了具有上述功能的化合物的皮肤的外用组合物。角化不全抑制剂，孔收缩剂或粗糙皮肤防止/改善剂包含一种，两种或更多种选自α-氨基酸衍生物及其盐的化合物。用于皮肤的外用组合物包含一种，两种或更多种选自上述角化不力抑制剂的α-氨基酸衍生物及其盐，孔收缩剂或粗糙皮肤防止/减量剂的化合物。

2. 发明授权

US08937090B2 Parakeratosis inhibitor, pore-shrinking agent and external composition for skin 有权
标题翻译：角化不全抑制剂，孔收缩剂和皮肤外用组合物
公开(公告)号：US08937090B2
公开(公告)日：2015-01-20
申请号：US11920053
申请日：2006-04-28
申请人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata
发明人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata
IPC分类号： A61K31/44 , A61K31/135 , A61K31/13 , A61Q19/00 , A61K8/02 , A61K8/44 , A61K8/49 , A61K31/136 , A61K31/137 , A61K31/131 , A61Q1/02 , A61Q1/12
CPC分类号： A61Q19/00 , A61K8/0212 , A61K8/44 , A61K8/445 , A61K8/447 , A61K8/4926 , A61K31/131 , A61K31/136 , A61K31/137 , A61Q1/02 , A61Q1/12
摘要： The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin-inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of β-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of β-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.
摘要翻译：本发明提供了具有角化不全抑制，孔收缩或粗糙皮肤抑制/消瘦等功能的角化不全抑制剂，孔收缩剂或粗糙皮肤防止/改善剂，不会引起感觉刺激等安全问题，而且非常安全，并且还提供了已经添加了具有上述功能的化合物的皮肤的外用组合物。角化不全抑制剂，孔收缩剂或粗糙皮肤防止/改善剂包含一种或多种选自β-丙氨酸衍生物及其盐的化合物。用于皮肤的外用组合物包含一种或多种选自上述的角化不全抑制剂，毛孔收缩剂或粗糙皮肤防止/改善剂的组合物，其组合物包括β-丙氨酸衍生物及其盐。

3. 发明申请

US20070225380A1 Parakeratosis Inhibitor and Skin Preparation for External use 有权
标题翻译：角化不全抑制剂和外用皮肤准备
公开(公告)号：US20070225380A1
公开(公告)日：2007-09-27
申请号：US10580471
申请日：2004-11-22
申请人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata , Keiko Takada , Yuji Katsuta
发明人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata , Keiko Takada , Yuji Katsuta
IPC分类号： A61K47/12
CPC分类号： A61K8/0212 , A61K8/44 , A61K8/466 , A61Q1/02 , A61Q19/00
摘要： To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for external use having these capabilities. There are provide a parakeratosis inhibitor and a pore reducing agent each comprising at least one compound selected from the group consisting of a glycine derivative, an aminodicarboxylic acid derivative, an acylaminodicarboxylic acid derivative, a pyrrolidinecarboxylic acid derivative, a piperidinecarboxylic acid derivative, a hexamethyleneiminecarboxylic acid, a beta-alanine derivative and salts of these derivatives. Further, there are provided a parakeratosis inhibitor, a pore reducing agent and a skin roughness preventing/ameliorating agent each comprising at least one compound selected from the group consisting of specified glycine derivatives and salts thereof and specified aminosulfuric acid derivatives and salts thereof. Still further, there are provided skin preparations for external use comprising these compounds.
摘要翻译：提供表现角化不全抑制，减孔，皮肤粗糙度防止/改善等的角化不全抑制剂，减孔剂和皮肤粗糙度防止/改善剂，进一步提供具有这些能力的外用皮肤制剂。提供了角化不全抑制剂和孔还原剂，其各自包含至少一种选自甘氨酸衍生物，氨基二羧酸衍生物，酰氨基二羧酸衍生物，吡咯烷羧酸衍生物，哌啶羧酸衍生物，六亚甲基亚氨基羧酸，β-丙氨酸衍生物和这些衍生物的盐。此外，提供了分别含有选自特定的甘氨酸衍生物及其盐的化合物和规定的氨基硫酸衍生物及其盐中的至少一种化合物的角化不全抑制剂，减孔剂和皮肤粗糙度防止改善剂。此外，提供了包含这些化合物的外用皮肤制剂。

4. 发明申请

US20120253064A1 PARAKERATOSIS INHIBITOR AND SKIN PREPARATION FOR EXTERNAL USE 审中-公开
标题翻译： PARAKERATOSIS抑制剂和皮肤外用品的制备
公开(公告)号：US20120253064A1
公开(公告)日：2012-10-04
申请号：US13467254
申请日：2012-05-09
申请人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata , Keiko Takada , Yuji Katsuta
发明人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata , Keiko Takada , Yuji Katsuta
IPC分类号： C07C309/26
CPC分类号： A61K8/0212 , A61K8/44 , A61K8/466 , A61Q1/02 , A61Q19/00
摘要： To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for external use having these capabilities. There are provided a parakeratosis inhibitor, a pore reducing agent and a skin roughness preventing/ameliorating agent each comprising at least one compound selected from the group consisting of specified glycine derivatives and salts thereof and specified aminosulfuric acid derivatives and salts thereof. Still further, there are provided skin preparations for external use comprising these compounds.
摘要翻译：提供表现角化不全抑制，减孔，皮肤粗糙度防止/改善等的角化不全抑制剂，减孔剂和皮肤粗糙度防止/改善剂，进一步提供具有这些能力的外用皮肤制剂。提供了一种角化不全抑制剂，减孔剂和皮肤粗糙度防止/改善剂，其各自包含至少一种选自指定的甘氨酸衍生物及其盐的化合物和指定的氨基硫酸衍生物及其盐。此外，提供了包含这些化合物的外用皮肤制剂。

5. 发明申请

US20120232111A1 Parakeratosis inhibitor, pore -shrinking agent and external compositon for skin 有权
标题翻译：角化不全抑制剂，毛孔收缩剂和皮肤外用组合物
公开(公告)号：US20120232111A1
公开(公告)日：2012-09-13
申请号：US11920053
申请日：2006-04-28
申请人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata
发明人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata
IPC分类号： A61K31/197 , C07D211/34 , C07C237/06 , A61K31/164 , C07C229/08 , A61Q19/00 , A61K31/4439 , C07D211/76 , A61K31/4402 , A61K8/49 , A61K8/44 , A61P17/00 , A61K31/4453 , C07D401/04
CPC分类号： A61Q19/00 , A61K8/0212 , A61K8/44 , A61K8/445 , A61K8/447 , A61K8/4926 , A61K31/131 , A61K31/136 , A61K31/137 , A61Q1/02 , A61Q1/12
摘要： The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin—inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent comprises one or more compounds selected from the group consisting of β-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of β-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/ameliorating agent.
摘要翻译：本发明提供了具有角化不全抑制，孔收缩或粗糙皮肤抑制/消瘦等功能的角化不全抑制剂，孔收缩剂或粗糙皮肤防止/改善剂，不会引起感觉刺激等安全问题，而且非常安全，并且还提供了已经添加了具有上述功能的化合物的皮肤的外用组合物。角化不全抑制剂，孔收缩剂或粗糙皮肤防止/改善剂包含一种或多种选自β-丙氨酸衍生物及其盐的化合物。用于皮肤的外用组合物包含一种或多种选自上述的角化不全抑制剂，毛孔收缩剂或粗糙皮肤防止/改善剂的组合物，其组合物包括β-丙氨酸衍生物及其盐。

6. 发明授权

US08586638B2 Parakeratosis inhibitor and skin preparation for external use 有权
标题翻译：角化失调抑制剂和外用皮肤制剂
公开(公告)号：US08586638B2
公开(公告)日：2013-11-19
申请号：US10580471
申请日：2004-11-22
申请人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata , Keiko Takada , Yuji Katsuta
发明人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata , Keiko Takada , Yuji Katsuta
IPC分类号： A61K47/12
CPC分类号： A61K8/0212 , A61K8/44 , A61K8/466 , A61Q1/02 , A61Q19/00
摘要： To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for external use having these capabilities. There are provide a parakeratosis inhibitor and a pore reducing agent each comprising at least one compound selected from the group consisting of a glycine derivative, an aminodicarboxylic acid derivative, an acylaminodicarboxylic acid derivative, a pyrrolidinecarboxylic acid derivative, a piperidinecarboxylic acid derivative, a hexamethyleneiminecarboxylic acid, a beta-alanine derivative and salts of these derivatives. Further, there are provided a parakeratosis inhibitor, a pore reducing agent and a skin roughness preventing/ameliorating agent each comprising at least one compound selected from the group consisting of specified glycine derivatives and salts thereof and specified aminosulfuric acid derivatives and salts thereof. Still further, there are provided skin preparations for external use comprising these compounds.
摘要翻译：提供表现角化不全抑制，减孔，皮肤粗糙度防止/改善等的角化不全抑制剂，减孔剂和皮肤粗糙度防止/改善剂，进一步提供具有这些能力的外用皮肤制剂。提供了角化不全抑制剂和孔还原剂，其各自包含至少一种选自甘氨酸衍生物，氨基二羧酸衍生物，酰氨基二羧酸衍生物，吡咯烷羧酸衍生物，哌啶羧酸衍生物，六亚甲基亚氨基羧酸，β-丙氨酸衍生物和这些衍生物的盐。此外，提供了分别含有选自特定的甘氨酸衍生物及其盐的化合物和规定的氨基硫酸衍生物及其盐中的至少一种化合物的角化不全抑制剂，减孔剂和皮肤粗糙度防止改善剂。此外，提供了包含这些化合物的外用皮肤制剂。

7. 发明申请

US20120053243A1 PARAKERATOSIS INHIBITOR AND SKIN PREPARATION FOR EXTERNAL USE 审中-公开
标题翻译： PARAKERATOSIS抑制剂和皮肤外用品的制备
公开(公告)号：US20120053243A1
公开(公告)日：2012-03-01
申请号：US13290309
申请日：2011-11-07
申请人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata , Keiko Takada , Yuji Katsuta
发明人： Mikiko Kaminuma , Masaru Suetsugu , Toshii Iida , Shinji Inomata , Keiko Takada , Yuji Katsuta
IPC分类号： A61K31/197 , C07C233/83 , C07C235/52 , A61K8/44 , A61Q19/00 , C07C309/19 , A61K31/185 , A61K8/46 , A61P17/00 , C07C311/19 , C07C309/15
CPC分类号： A61K8/0212 , A61K8/44 , A61K8/466 , A61Q1/02 , A61Q19/00
摘要： To provide a parakeratosis inhibitor, pore reducing agent and skin roughness preventing/ameliorating agent that exhibit capabilities of parakeratosis inhibition, pore reduction, skin roughness prevention/amelioration, etc., and further provide a skin preparation for external use having these capabilities. There are provide a parakeratosis inhibitor and a pore reducing agent each comprising at least one compound selected from the group consisting of a glycine derivative, an aminodicarboxylic acid derivative, an acylaminodicarboxylic acid derivative, a pyrrolidinecarboxylic acid derivative, a piperidinecarboxylic acid derivative, a hexamethyleneiminecarboxylic acid, a beta-alanine derivative and salts of these derivatives. Further, there are provided a parakeratosis inhibitor, a pore reducing agent and a skin roughness preventing/ameliorating agent each comprising at least one compound selected from the group consisting of specified glycine derivatives and salts thereof and specified aminosulfuric acid derivatives and salts thereof. Still further, there are provided skin preparations for external use comprising these compounds.
摘要翻译：提供表现角化不全抑制，减孔，皮肤粗糙度防止/改善等的角化不全抑制剂，减孔剂和皮肤粗糙度防止/改善剂，进一步提供具有这些能力的外用皮肤制剂。提供了角化不全抑制剂和孔还原剂，其各自包含至少一种选自甘氨酸衍生物，氨基二羧酸衍生物，酰氨基二羧酸衍生物，吡咯烷羧酸衍生物，哌啶羧酸衍生物，六亚甲基亚氨基羧酸，β-丙氨酸衍生物和这些衍生物的盐。此外，提供了分别含有选自特定的甘氨酸衍生物及其盐的化合物和规定的氨基硫酸衍生物及其盐中的至少一种化合物的角化不全抑制剂，减孔剂和皮肤粗糙度防止改善剂。此外，提供了包含这些化合物的外用皮肤制剂。

8. 发明申请

US20110065794A1 Wrinkle-preventing and improving composition 审中-公开
标题翻译：防皱，改善成分
公开(公告)号：US20110065794A1
公开(公告)日：2011-03-17
申请号：US12926351
申请日：2010-11-12
申请人： Makoto Tsunenaga , Haruhi Iwaki , Toshii Iida , Mikiko Kaminuma , Masaru Suetsugu , Keiko Takada , Shinji Inomata
发明人： Makoto Tsunenaga , Haruhi Iwaki , Toshii Iida , Mikiko Kaminuma , Masaru Suetsugu , Keiko Takada , Shinji Inomata
IPC分类号： A61K31/197 , A61Q19/08
CPC分类号： A61K8/44 , A61K8/445 , A61Q19/08
摘要： A wrinkle-preventing and -improving composition comprising one or more than one compound selected from the group consisting of α-amino acid derivatives represented by the following general formula (1) and salts thereof: wherein, R1 represents hydrogen atom, CH3 group or CH2OH group, R2 and R3 each independently represent hydrogen atom, alkyl group having 1 to 4 carbons, provided that R2 and R3 cannot be hydrogen atom at the same time, or R2 and R3 together with N atom to which they are bound may form a ring structure having a total carbon number of 4 to 6, in which case said ring structure may optionally contain an oxygen atom as a heteroatom, R4 represents hydrogen atom, alkyl group having 1 to 18 carbons, wherein when R1 and R4 are hydrogen atom, it cannot be that one of R2 and R3 is benzyloxycarbonyl group and the other is hydrogen atom.
摘要翻译：一种防皱和改善组合物，其包含一种或多于一种选自下列通式（1）表示的α-氨基酸衍生物及其盐的化合物：其中，R 1表示氢原子，CH 3基或CH 2 OH 基团，R 2和R 3各自独立地表示氢原子，具有1至4个碳的烷基，条件是R 2和R 3不能同时为氢原子，或者R 2和R 3与它们所连接的N原子可以形成环总碳数为4〜6的结构，在这种情况下，所述环结构可任选地含有氧原子作为杂原子，R4表示氢原子，具有1至18个碳原子的烷基，其中当R 1和R 4为氢原子时，不能是R2和R3之一是苄氧基羰基，另一个是氢原子。

9. 发明申请

US20110004019A1 Parakeratosis Inhibitor, Pore-Shrinking Agent, Or Rough Skin Inhibiting/Ameliorating Agent, And External Composition For Skin Containing The Same 审中-公开
标题翻译：角化不全抑制剂，孔隙收缩剂或粗糙皮肤抑制/改善剂及含有其的皮肤外用组合物
公开(公告)号：US20110004019A1
公开(公告)日：2011-01-06
申请号：US12921866
申请日：2009-03-12
申请人： Toshii Iida , Maki Kaneko , Mikiko Kaminuma , Masaru Suetsugu
发明人： Toshii Iida , Maki Kaneko , Mikiko Kaminuma , Masaru Suetsugu
IPC分类号： C07C233/01 , C07C233/47
CPC分类号： A61Q19/007 , A61K8/0212 , A61K8/44 , A61K8/442 , A61K31/16 , A61K31/185 , A61K31/195 , A61K31/198 , A61Q1/02 , A61Q1/12
摘要： The present invention provides a parakeratosis inhibitor, a pore-shrinking agent, and a rough skin inhibiting or ameliorating agent comprising, as an active ingredient, a compound that has excellent effects and high safety without safety problems such as sensory irritation, and provides an external composition for skin containing the same. The compound is selected from the glutamic acid derivatives represented by formula (1) or (2) and the salts thereof: wherein A represents a carbamoyl group, a benzyloxycarbonyl group, an alkyl group having 1 to 3 carbon atoms, an allyl group, or an amidino group; wherein Z represents an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, etc.; Y represents OH, an alkyloxy group having 1 to 3 carbon atoms, an allyloxy group, or NR3R4; R1 to R4 each independently represents H, an alkyl group having 1 to 3 carbon atoms, an allyl group, a cycloalkyl group having 3 to 7 carbon atoms, a cycloalkenyl group having 3 to 7 carbon atoms, a phenyl group, or a benzyl group, or R1 and R2, or R3 and R4, independently form a heterocycle.
摘要翻译：本发明提供一种角化不全抑制剂，孔收缩剂和粗皮肤抑制或改善剂，其包含具有优异效果和高安全性的化合物作为活性成分，没有诸如感觉刺激之类的安全问题，并且提供外部含有相同成分的皮肤。该化合物选自由式（1）或（2）表示的谷氨酸衍生物及其盐：其中A表示氨基甲酰基，苄氧基羰基，具有1至3个碳原子的烷基，烯丙基或脒基; 其中Z表示碳原子数1〜4的烷基，碳原子数2〜4的烯基等。 Y表示OH，具有1至3个碳原子的烷氧基，烯丙氧基或NR 3 R 4; R 1〜R 4各自独立地表示H，碳原子数1〜3的烷基，烯丙基，碳原子数3〜7的环烷基，碳原子数3〜7的环烯基，苯基或苄基，或R 1和R 2，或R 3和R 4独立地形成杂环。

10. 发明申请

US20120283302A1 SCCA-1 PRODUCTION INHIBITOR HAVING A CARBOXAMIDE DERIVATIVE AND/OR A SALT THEREOF AS AN ACTIVE INGREDIENT 审中-公开
标题翻译：具有作为活性成分的羧酰胺衍生物和/或其盐的SCCA-1生产抑制剂
公开(公告)号：US20120283302A1
公开(公告)日：2012-11-08
申请号：US13266663
申请日：2010-04-28
申请人： Maki Kaneko , Takuya Hiruma , Masaru Suetsugu , Chika Katagiri , Toshii Iida , Tomoko Onodera
发明人： Maki Kaneko , Takuya Hiruma , Masaru Suetsugu , Chika Katagiri , Toshii Iida , Tomoko Onodera
IPC分类号： A61K31/4166 , A61K31/17 , A61P35/00 , A61P19/04 , A61P17/08 , A61P17/12 , A61P17/06 , A61K31/4015 , A61P17/00
CPC分类号： A61K31/17 , A61K31/4015 , A61K31/4166 , C07D207/27 , C07D233/34 , C07D233/40
摘要： A SCCA-1 production inhibitor, comprising as an active ingredient, at least one carboxamide derivative selected from the group consisting of compounds represented by the following formula (I): wherein X is CR5 or N, R1, R4 and R5 each independently represent hydrogen, C1-C4 alkyl or a C1-C6 hydroxyalkyl group having 1-5 hydroxy groups, R2 and R3 each independently represent hydrogen, C1-C4 alkyl or a C1-C6 hydroxyalkyl group having 1-5 hydroxy groups, or each represents a group —(CH2)n—, wherein n represents an integer of 1 or 2, and may form a 5- to 6-membered ring together with the atoms to which they are bonded and with the carbonyl group, allantoin, and salts thereof.
摘要翻译：一种SCCA-1生产抑制剂，其包含作为活性成分的至少一种选自由下式（I）表示的化合物的羧酰胺衍生物：其中X为CR 5或N，R 1，R 4和R 5各自独立地表示氢 C1-C4烷基或具有1-5个羟基的C1-C6羟基烷基，R2和R3各自独立地表示氢，C1-C4烷基或具有1-5个羟基的C1-C6羟烷基，或各自表示基团 - （CH 2）n - ，其中n表示1或2的整数，并且可以与它们所键合的原子和羰基，尿囊素及其盐一起形成5-至6-元环。

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