JP2021523156A - マラセチア由来の化合物および/またはその化学的類縁体を含有する光保護組成物 - Google Patents
マラセチア由来の化合物および/またはその化学的類縁体を含有する光保護組成物 Download PDFInfo
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- JP2021523156A JP2021523156A JP2020562712A JP2020562712A JP2021523156A JP 2021523156 A JP2021523156 A JP 2021523156A JP 2020562712 A JP2020562712 A JP 2020562712A JP 2020562712 A JP2020562712 A JP 2020562712A JP 2021523156 A JP2021523156 A JP 2021523156A
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- melanin
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/06—Fungi, e.g. yeasts
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4906—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
- A61K8/4913—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid
- A61K8/492—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having five membered rings, e.g. pyrrolidone carboxylic acid having condensed rings, e.g. indol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9728—Fungi, e.g. yeasts
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
- A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
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- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/12—Radicals substituted by oxygen atoms
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Abstract
Description
本発明は、2018年5月7日に出願された米国仮出願第62/668,007号、2018年6月15日に出願された米国仮出願第62/685,800号、2018年6月19日に出願された米国仮出願第62/686,912号、2018年8月24日に出願された米国仮出願第62/722,412号および2018年10月8日に出願された米国仮出願第62/742,657号の恩典を主張する。先述の出願の内容全体が、参照により組み込まれる。さらに、2016年3月10日に出願された米国仮出願第62/306,468号、2018年4月12日に出願された米国仮出願第62/656,769号、現在米国特許第10,131,631号である2017年3月10日に出願された米国特許出願第15/455,932号および2019年4月12日に出願された米国特許出願第16/382,891号の内容全体が、参照により本明細書に組み込まれる。
Xは、NR14およびOからなる群から選択され;Yは、共有結合、CR5R6、OまたはNR15であり;R1、R2、R3、R4、R7、R8、R9、R10およびR11は、水素、ハロゲン、CN、ヒドロキシル、R16またはOR16からなる群から独立に選択され;R13、R14およびR15は、独立に、水素またはR16であり;R5およびR6は、水素、ヒドロキシル、OR16、R16およびC3〜6シクロアルキルからなる群から独立に選択されるか;またはR5およびR6は結合してオキソ(=O)基またはC3〜6シクロアルキルを形成し;R12は、水素、−CORaおよびR16からなる群から選択され;各R16は、独立に、ホルミル、C1〜9アルキル、C2〜9アルケニルまたはC2〜9アルキニルであり;ならびにRaは、水素、ヒドロキシルおよびOR16からなる群から選択される]
の構造を有する化合物、
あるいはその結晶形、水和物または美容的にもしくは薬学的に許容され得る塩と、
美容的にまたは薬学的に許容され得る、ビヒクル、希釈剤または担体とを含む。
R1、R4、R5、R6、R9およびR10は、水素、ヒドロキシル、ハロゲン、CN、R13、OR13、OCOR13および−CHOからなる群から独立に選択され;R2およびR3は、水素、ヒドロキシル、ハロゲン、CN、R13、OR13、OCOR13および−CHOからなる群から独立に選択されるか、またはR2およびR3は結合して5員もしくは6員のヘテロシクリルを形成し;R7およびR8は、水素、ヒドロキシル、ハロゲン、CN、R13、OR13、OCOR13および−CHOからなる群から独立に選択されるか、またはR7およびR8は結合して5員もしくは6員のヘテロシクリルを形成し;R11およびR12は、独立に、水素またはR13であり;ならびに、各R13は、独立に、C1〜9アルキル、C2〜9アルケニルまたはC2〜9アルキニルである]
の構造を有する化合物
あるいはその結晶形、水和物または美容的にもしくは薬学的に許容され得る塩と、
美容的にまたは薬学的に許容され得る、ビヒクル、希釈剤または担体とを含む。
美容的にまたは薬学的に許容され得る、ビヒクル、希釈剤または担体とを含む。
Xは、NR14およびOからなる群から選択され;Yは、共有結合、CR5R6、OまたはNR15であり;R1、R2、R3、R4、R7、R8、R9、R10およびR11は、水素、ハロゲン、CN、ヒドロキシル、R16またはOR16からなる群から独立に選択され;R13、R14およびR15は、独立に、水素またはR16であり;R5およびR6は、水素、ヒドロキシル、OR16、R16およびC3〜6シクロアルキルからなる群から独立に選択されるか;またはR5およびR6は結合してオキソ(=O)基またはC3〜6シクロアルキルを形成し;R12は、水素、−CORaおよびR16からなる群から選択され;各R16は、独立に、ホルミル、C1〜9アルキル、C2〜9アルケニルまたはC2〜9アルキニルであり;ならびにRaは、水素、ヒドロキシルおよびOR16からなる群から選択される]
の構造を有する化合物、
あるいはその結晶形、水和物または美容的にもしくは薬学的に許容され得る塩と、
美容的にまたは薬学的に許容され得る、ビヒクル、希釈剤または担体とを含む。
R1、R4、R5、R6、R9およびR10は、水素、ヒドロキシル、ハロゲン、CN、R13、OR13、OCOR13および−CHOからなる群から独立に選択され;R2およびR3は、水素、ヒドロキシル、ハロゲン、CN、R13、OR13、OCOR13および−CHOからなる群から独立に選択されるか、またはR2およびR3は結合して5員もしくは6員のヘテロシクリルを形成し;R7およびR8は、水素、ヒドロキシル、ハロゲン、CN、R13、OR13、OCOR13および−CHOからなる群から独立に選択されるか、またはR7およびR8は結合して5員もしくは6員のヘテロシクリルを形成し;R11およびR12は、独立に、水素またはR13であり;ならびに、各R13は、独立に、C1〜9アルキル、C2〜9アルケニルまたはC2〜9アルキニルである]
の構造を有する化合物
あるいはその結晶形、水和物または美容的にもしくは薬学的に許容され得る塩と、
美容的にまたは薬学的に許容され得る、ビヒクル、希釈剤または担体とを含む。
美容的にまたは薬学的に許容され得る、ビヒクル、希釈剤または担体とを含む。
定義
実験の方法
アネキシンVアッセイおよびカスパーゼ3/7アッセイの結果
実施例3
インジルビンおよびインジルビン誘導体への曝露後の細胞生存率
試薬
実験の方法
結果
実施例4
インジルビンおよびインジルビン誘導体のアリール炭化水素受容体活性化能
アッセイ手順
結果
実施例5
MelanoDerm(商標)Assay
試験物質およびアッセイ対照の特定
試験系
実験のデザインおよび方法論
培地および試薬
被験物質の調製および送達
投与経路
pH決定
対照
直接的な被験物質によるMTTの還元の査定
MelanoDerm(商標)の受領
確定的アッセイ
残存する被験物質によるMTTの還元の査定のための死滅対照
補正された被験物質曝露OD550=被験物質曝露OD550−ブランク平均OD550
各被験物質KCについての正味のOD550=生のOD550被験物質KC−生のOD550陰性/溶媒対照KC
最終的な補正されたOD550=補正された被験物質OD550(生きた)−正味のOD550被験物質(KC)
%生存率=[(被験物質または陽性対照の最終的な補正されたOD550)/(陰性/溶媒対照(単数または複数)の補正された平均OD550)]×100
結果
実施例6
インジルビンおよびインジルビン誘導体のメラニン形成能
材料および試薬
プロトコール
結果
実施例7
インビトロでの効力
実施例8
インビボでの効力
実施例9
マラセチア由来の化合物および/またはその化学的類縁体を含有する組成物のアポトーシス誘導活性
試薬
実験の方法
アネキシンVアッセイおよびカスパーゼ3/7アッセイの結果
実施例10
マラセチア由来の化合物および/またはその化学的類縁体を含有する組成物への曝露後の細胞生存率
試薬
実験の方法
結果
実施例11
マラセチア由来の化合物および/またはその化学的類縁体を含有する組成物のアリール炭化水素受容体活性化能
アッセイ手順
結果
実施例12
MelanoDerm(商標)Assay
試験物質およびアッセイ対照の特定
試験系
実験のデザインおよび方法論
培地および試薬
被験物質の調製および送達
投与経路
pH決定
対照
直接的な被験物質によるMTTの還元の査定
MelanoDerm(商標)の受領
確定的アッセイ
残存する被験物質によるMTTの還元の査定のための死滅対照
データ解析
補正された被験物質曝露OD550=被験物質曝露OD550−ブランク平均OD550
各被験物質KCについての正味のOD550=生のOD550被験物質KC−生のOD550陰性/溶媒対照KC
最終的な補正されたOD550=補正された被験物質OD550(生きた)−正味のOD550被験物質(KC)
%生存率=[(被験物質または陽性対照の最終的な補正されたOD550)/(陰性/溶媒対照(単数または複数)の補正された平均OD550)]×100
結果
実施例13
マラセチア由来の化合物および/またはその化学的類縁体を含有する組成物のメラニン形成能
材料および試薬
プロトコール
結果
実施例14
インビトロでの効力
実施例15
インビボでの効力
実施例16
マラセジンおよびインジルビンの化学的類縁体の合成
AB17590の合成
AB17653の合成
AB17654の合成
AB17655の合成
AB17656の合成
AB17657の合成
AB17658の合成
実施例17
マラセジン、他のマラセチア由来化合物およびこれらの化学的類縁体の光保護特性のインビボ査定
マラセジン1%製剤
実験のデザイン
結果
結論
文献
Claims (11)
Priority Applications (1)
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JP2022076475A JP2022093689A (ja) | 2018-05-07 | 2022-05-06 | マラセチア由来の化合物および/またはその化学的類縁体を含有する光保護組成物 |
Applications Claiming Priority (11)
Application Number | Priority Date | Filing Date | Title |
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US201862668007P | 2018-05-07 | 2018-05-07 | |
US62/668,007 | 2018-05-07 | ||
US201862685800P | 2018-06-15 | 2018-06-15 | |
US62/685,800 | 2018-06-15 | ||
US201862686912P | 2018-06-19 | 2018-06-19 | |
US62/686,912 | 2018-06-19 | ||
US201862722412P | 2018-08-24 | 2018-08-24 | |
US62/722,412 | 2018-08-24 | ||
US201862742657P | 2018-10-08 | 2018-10-08 | |
US62/742,657 | 2018-10-08 | ||
PCT/US2019/031072 WO2019217387A1 (en) | 2018-05-07 | 2019-05-07 | Photoprotective compositions containing malassezia-derived compounds and/or chemical analogs thereof |
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JP2022076475A Pending JP2022093689A (ja) | 2018-05-07 | 2022-05-06 | マラセチア由来の化合物および/またはその化学的類縁体を含有する光保護組成物 |
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US (1) | US20190337927A1 (ja) |
EP (2) | EP3957639A1 (ja) |
JP (2) | JP2021523156A (ja) |
KR (1) | KR20210070949A (ja) |
CN (1) | CN113015732A (ja) |
AU (1) | AU2019267554A1 (ja) |
BR (1) | BR112020022708A2 (ja) |
CA (1) | CA3099418A1 (ja) |
MX (1) | MX2020011919A (ja) |
PH (1) | PH12020551845A1 (ja) |
SG (1) | SG11202010991RA (ja) |
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WO2019241706A1 (en) * | 2018-06-15 | 2019-12-19 | Einziger Michael | Photoprotective compositions containing malassezia-derived compounds and/or chemical analogs thereof |
MX2021002170A (es) | 2018-08-24 | 2021-04-28 | Michael EINZIGER | Composiciones fotoprotectoras que contienen compuestos derivados de malassezia y/o analogos quimicos de los mismos. |
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KR20160128764A (ko) * | 2015-04-29 | 2016-11-08 | 주식회사 엘지생활건강 | 피부 개선용 조성물 |
WO2017156424A1 (en) * | 2016-03-10 | 2017-09-14 | Einziger Michael | Malassezin and analogs thereof as skin brightening agents |
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FR2901471B1 (fr) * | 2006-05-24 | 2010-06-04 | Oreal | Procede de defrisage des fibres keratiniques avec un moyen de chauffage et un derive d'acide |
KR20110062159A (ko) * | 2009-12-02 | 2011-06-10 | (주)더페이스샵 | 장뇌삼 캘러스 추출물을 함유하는 피부 미백용 화장료 조성물 |
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2019
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- 2019-05-07 MX MX2020011919A patent/MX2020011919A/es unknown
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- 2019-05-07 JP JP2020562712A patent/JP2021523156A/ja active Pending
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- 2019-05-07 CN CN201980045590.0A patent/CN113015732A/zh active Pending
- 2019-05-07 TW TW108115720A patent/TW201946620A/zh unknown
- 2019-05-07 AU AU2019267554A patent/AU2019267554A1/en not_active Abandoned
- 2019-05-07 SG SG11202010991RA patent/SG11202010991RA/en unknown
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KR20160128764A (ko) * | 2015-04-29 | 2016-11-08 | 주식회사 엘지생활건강 | 피부 개선용 조성물 |
WO2017156424A1 (en) * | 2016-03-10 | 2017-09-14 | Einziger Michael | Malassezin and analogs thereof as skin brightening agents |
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EP3790880A1 (en) | 2021-03-17 |
TW201946620A (zh) | 2019-12-16 |
PH12020551845A1 (en) | 2021-06-28 |
CA3099418A1 (en) | 2019-11-14 |
CN113015732A (zh) | 2021-06-22 |
US20190337927A1 (en) | 2019-11-07 |
SG11202010991RA (en) | 2020-12-30 |
MX2020011919A (es) | 2021-03-29 |
JP2022093689A (ja) | 2022-06-23 |
AU2019267554A1 (en) | 2020-12-03 |
KR20210070949A (ko) | 2021-06-15 |
WO2019217387A1 (en) | 2019-11-14 |
BR112020022708A2 (pt) | 2021-05-04 |
EP3957639A1 (en) | 2022-02-23 |
TW202123933A (zh) | 2021-07-01 |
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