JP2008542372A - 発毛の低減 - Google Patents
発毛の低減 Download PDFInfo
- Publication number
- JP2008542372A JP2008542372A JP2008514674A JP2008514674A JP2008542372A JP 2008542372 A JP2008542372 A JP 2008542372A JP 2008514674 A JP2008514674 A JP 2008514674A JP 2008514674 A JP2008514674 A JP 2008514674A JP 2008542372 A JP2008542372 A JP 2008542372A
- Authority
- JP
- Japan
- Prior art keywords
- agent
- acid
- farnesoid
- hair growth
- skin
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- 230000003779 hair growth Effects 0.000 title claims abstract description 38
- 230000009467 reduction Effects 0.000 title claims description 10
- 102100038495 Bile acid receptor Human genes 0.000 claims abstract description 38
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 claims abstract description 36
- 239000003795 chemical substances by application Substances 0.000 claims description 53
- 238000000034 method Methods 0.000 claims description 52
- 239000000203 mixture Substances 0.000 claims description 48
- 150000001875 compounds Chemical class 0.000 claims description 30
- 210000003491 skin Anatomy 0.000 claims description 30
- 239000003613 bile acid Substances 0.000 claims description 23
- HSINOMROUCMIEA-FGVHQWLLSA-N (2s,4r)-4-[(3r,5s,6r,7r,8s,9s,10s,13r,14s,17r)-6-ethyl-3,7-dihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]-2-methylpentanoic acid Chemical group C([C@@]12C)C[C@@H](O)C[C@H]1[C@@H](CC)[C@@H](O)[C@@H]1[C@@H]2CC[C@]2(C)[C@@H]([C@H](C)C[C@H](C)C(O)=O)CC[C@H]21 HSINOMROUCMIEA-FGVHQWLLSA-N 0.000 claims description 13
- 230000015572 biosynthetic process Effects 0.000 claims description 11
- 239000002537 cosmetic Substances 0.000 claims description 11
- 210000003780 hair follicle Anatomy 0.000 claims description 11
- 241000124008 Mammalia Species 0.000 claims description 9
- 241000282414 Homo sapiens Species 0.000 claims description 8
- 150000002148 esters Chemical class 0.000 claims description 8
- 230000014509 gene expression Effects 0.000 claims description 7
- 239000013543 active substance Substances 0.000 claims description 6
- 239000000833 heterodimer Substances 0.000 claims description 5
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- KXGVEGMKQFWNSR-UHFFFAOYSA-N deoxycholic acid Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 KXGVEGMKQFWNSR-UHFFFAOYSA-N 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
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- 238000002360 preparation method Methods 0.000 claims description 4
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- 238000010998 test method Methods 0.000 claims description 3
- BHQCQFFYRZLCQQ-UHFFFAOYSA-N (3alpha,5alpha,7alpha,12alpha)-3,7,12-trihydroxy-cholan-24-oic acid Natural products OC1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)C(O)C2 BHQCQFFYRZLCQQ-UHFFFAOYSA-N 0.000 claims description 2
- 239000004380 Cholic acid Substances 0.000 claims description 2
- SMEROWZSTRWXGI-UHFFFAOYSA-N Lithocholsaeure Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(CCC(O)=O)C)C1(C)CC2 SMEROWZSTRWXGI-UHFFFAOYSA-N 0.000 claims description 2
- 239000003098 androgen Substances 0.000 claims description 2
- 229960001091 chenodeoxycholic acid Drugs 0.000 claims description 2
- RUDATBOHQWOJDD-BSWAIDMHSA-N chenodeoxycholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 RUDATBOHQWOJDD-BSWAIDMHSA-N 0.000 claims description 2
- BHQCQFFYRZLCQQ-OELDTZBJSA-N cholic acid Chemical compound C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 BHQCQFFYRZLCQQ-OELDTZBJSA-N 0.000 claims description 2
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- KXGVEGMKQFWNSR-LLQZFEROSA-N deoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 claims description 2
- 229960003964 deoxycholic acid Drugs 0.000 claims description 2
- RUDATBOHQWOJDD-UZVSRGJWSA-N ursodeoxycholic acid Chemical compound C([C@H]1C[C@@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)CC1 RUDATBOHQWOJDD-UZVSRGJWSA-N 0.000 claims description 2
- 229960001661 ursodiol Drugs 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims 4
- ABLZXFCXXLZCGV-UHFFFAOYSA-N phosphonic acid group Chemical group P(O)(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 4
- CRDAMVZIKSXKFV-YFVJMOTDSA-N (2-trans,6-trans)-farnesol Chemical compound CC(C)=CCC\C(C)=C\CC\C(C)=C\CO CRDAMVZIKSXKFV-YFVJMOTDSA-N 0.000 claims 3
- 239000000260 (2E,6E)-3,7,11-trimethyldodeca-2,6,10-trien-1-ol Substances 0.000 claims 3
- 229930002886 farnesol Natural products 0.000 claims 3
- 229940043259 farnesol Drugs 0.000 claims 3
- CRDAMVZIKSXKFV-UHFFFAOYSA-N trans-Farnesol Natural products CC(C)=CCCC(C)=CCCC(C)=CCO CRDAMVZIKSXKFV-UHFFFAOYSA-N 0.000 claims 3
- 206010040844 Skin exfoliation Diseases 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- 125000002573 ethenylidene group Chemical group [*]=C=C([H])[H] 0.000 claims 2
- 125000000219 ethylidene group Chemical group [H]C(=[*])C([H])([H])[H] 0.000 claims 2
- NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical compound [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- YHRUHBBTQZKMEX-YFVJMOTDSA-N (2-trans,6-trans)-farnesal Chemical compound CC(C)=CCC\C(C)=C\CC\C(C)=C\C=O YHRUHBBTQZKMEX-YFVJMOTDSA-N 0.000 claims 1
- YHRUHBBTQZKMEX-UHFFFAOYSA-N (2E,6E)-3,7,11-trimethyl-2,6,10-dodecatrien-1-al Natural products CC(C)=CCCC(C)=CCCC(C)=CC=O YHRUHBBTQZKMEX-UHFFFAOYSA-N 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- ZGIGZINMAOQWLX-NCZFFCEISA-N 3,7,11-Trimethyl-2,6,10-dodecatrienyl acetate Chemical compound CC(C)=CCC\C(C)=C\CC\C(C)=C\COC(C)=O ZGIGZINMAOQWLX-NCZFFCEISA-N 0.000 claims 1
- 239000005711 Benzoic acid Substances 0.000 claims 1
- YHRUHBBTQZKMEX-FBXUGWQNSA-N E,E-Farnesal Natural products CC(C)=CCC\C(C)=C/CC\C(C)=C/C=O YHRUHBBTQZKMEX-FBXUGWQNSA-N 0.000 claims 1
- ZGIGZINMAOQWLX-UHFFFAOYSA-N Farnesyl acetate Natural products CC(C)=CCCC(C)=CCCC(C)=CCOC(C)=O ZGIGZINMAOQWLX-UHFFFAOYSA-N 0.000 claims 1
- QVJMXSGZTCGLHZ-VWADHSNXSA-N Juvenile hormone III Natural products O=C(OC)/C=C(\CC/C=C(\CC[C@H]1C(C)(C)O1)/C)/C QVJMXSGZTCGLHZ-VWADHSNXSA-N 0.000 claims 1
- NWKXNIPBVLQYAB-UHFFFAOYSA-N all-trans methylfarnesoate Natural products COC(=O)C=C(C)CCC=C(C)CCC=C(C)C NWKXNIPBVLQYAB-UHFFFAOYSA-N 0.000 claims 1
- KHBQMWCZKVMBLN-IDEBNGHGSA-N benzenesulfonamide Chemical group NS(=O)(=O)[13C]1=[13CH][13CH]=[13CH][13CH]=[13CH]1 KHBQMWCZKVMBLN-IDEBNGHGSA-N 0.000 claims 1
- 235000010233 benzoic acid Nutrition 0.000 claims 1
- RAVLTUCAFRTDRY-UHFFFAOYSA-N ethyl 3,7,11-trimethyldodeca-2,6,10-trienoate Chemical compound CCOC(=O)C=C(C)CCC=C(C)CCC=C(C)C RAVLTUCAFRTDRY-UHFFFAOYSA-N 0.000 claims 1
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- 239000002562 thickening agent Substances 0.000 description 1
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- 238000012546 transfer Methods 0.000 description 1
- LADGBHLMCUINGV-UHFFFAOYSA-N tricaprin Chemical compound CCCCCCCCCC(=O)OCC(OC(=O)CCCCCCCCC)COC(=O)CCCCCCCCC LADGBHLMCUINGV-UHFFFAOYSA-N 0.000 description 1
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Abstract
Description
bグリセリン、水、ナトリウムPCA、尿素、トレハロース、ポリクオタニウム(polyqauternium)−51、及びヒアルロン酸ナトリウム(コラボレイティブ・ラボ(Collaborative Labs)、ニューヨーク)。
解剖用スコープの下で、外科用メス及び時計製造用ピンセットを用いて、しわ取りを行った組織(形成外科医から取得したもの)からヒトの増殖期(成長期)の毛嚢を分離させた。皮膚を薄い細片にスライスし、分析しやすそうな毛嚢の2〜3列を露出させた。毛嚢に、2mMのL−グルタミン、10μg/mLのインスリン、10ng/mLのヒドロコルチゾン、100単位のペニシリン、0.1mg/mLのストレプトマイシン及び0.25μg/mLのアンホテリシンBを補充したウィリアムE培地(ライフ・テクノロジーズ(Life Technologies)(メリーランド州、ガイサーズバーグ(Gaithersburg))0.5mLに配置した。毛嚢は、5%CO2及び95%空気の雰囲気下、24ウェルプレート(1毛嚢/ウェル)において37℃でインキュベートした。化合物は、100倍の原液としてジメチルスルホキシドに溶解する。対照の毛嚢は、プロスタグランジンなしでジメチルスルホキシドで処理した。解剖用スコープの下で前記毛嚢を24ウェルプレート内で倍率10倍で撮影した。典型的には、0日目(毛嚢を培養物内に配置した日)に画像記録を行い、7日目に再度行った。画像分析ソフトウェアシステムを用いて毛嚢の長さを算定した。0日目の毛嚢の長さを7日目に測定した長さから減じることによって、毛の繊維の成長度合を算出した。
ハムスターの毛量を、先行特許(US2004/0198821)に記載されるものと同様の方法を用いて測定した。
Claims (36)
- 哺乳類の発毛を低減する美容方法であって、
発毛の低減が望まれる皮膚の領域を選択する工程、及び
発毛を低減するのに有効な量でファルネソイドX受容体の作用物質を含む皮膚科学的に許容可能な組成物を前記皮膚の領域に適用する工程を含み、
前記作用物質が、E−ジフルオロメチルオルニチン及びファルネソールのカルバメート又はエステルでないことを特徴とする美容方法。 - 前記作用物質が胆汁酸であることを特徴とする請求項1に記載の方法。
- 前記作用物質が胆汁酸の類縁体であることを特徴とする請求項1に記載の方法。
- 前記作用物質が胆汁酸の誘導体であることを特徴とする請求項1に記載の方法。
- 前記作用物質がファルネソイドX受容体と強く相互作用することを特徴とする請求項1に記載の方法。
- 前記作用物質が、リトコール酸、コール酸、デオキシコール酸、ケノデオキシコール酸、ウルソデオキシコール酸、6−α−エチルケノデオキシコール酸又はこれら2種以上の混合物から選択されることを特徴とする請求項1に記載の方法。
- 前記作用物質がファルネソイドであることを特徴とする請求項1に記載の方法。
- 前記作用物質がファルネソイドの類縁体であることを特徴とする請求項1に記載の方法。
- 前記作用物質がファルネソイドの誘導体であることを特徴とする請求項1に記載の方法。
- 前記作用物質が、ファルネソール、ファルネサール、ファルネシルアセテート、ファルネシル酸、メチルファルネシルエーテル、メチルファルネソエート、エチルファルネシルエーテル、エチルファルネソエート又はこれら2種以上の混合物から選択されることを特徴とする請求項1に記載の方法。
- 前記作用物質が、7−メチル−9−(3,3−ジメチルオキシバニル)−3−メチル−2,6−ノナジエン酸メチルエステル(幼若ホルモンIII)であることを特徴とする請求項1に記載の方法。
- 前記作用物質が、7−メチル−9−(3,3−ジメチルオキシバニル)−3−メチル−2,6−ノナジエン酸エチルエステルであることを特徴とする請求項1に記載の方法。
- 前記作用物質が、3α,7α−ジヒドロキシ−6α−エチル−5p−コラン−24−酸であることを特徴とする請求項1に記載の方法。
- 前記作用物質が、3α,7α−ジヒドロキシ−6α−プロピル−5p−コラン−24−酸であることを特徴とする請求項1に記載の方法。
- 前記作用物質が、3α,7α−ジヒドロキシ−6α−アリル−5p−コラン−24−酸であることを特徴とする請求項1に記載の方法。
- 前記作用物質が、ベンゼンスルホンアミド,N−(2,2,2−トリフルオロエチル)−N−[4−[2,2,2−トリフルオロ−1−ヒドロキシ−1−(トリフルオロメチル)エチル]フェニル]−であることを特徴とする請求項1に記載の方法。
- 前記作用物質が、安息香酸,3−[2−[2−クロロ−4−[[3−(2,6−ジクロロフェニル)−5−(l−メチルエチル)−4−イソキサゾリル]メトキシ]フェニル]エテニル]−であることを特徴とする請求項1に記載の方法。
- 前記作用物質が、ホスホン酸,[[3,5−ビス(l,l−ジメチルエチル)−4−ヒドロキシフェニル]エテニリデン]ビス−,テトラエチルエステルであることを特徴とする請求項1に記載の方法。
- 前記作用物質が、ホスホン酸,[2−[3,5−ビス(l,l−ジメチルエチル)−4−ヒドロキシフェニル]エチリデン]ビス−,テトラキス(l−メチルエチル)エステルであることを特徴とする請求項1に記載の方法。
- 前記作用物質が、ホスホン酸,[2−[3,5−ビス(1,1−ジメチルエチル)−4−ヒドロキシフェニル]エチリデン]ビス−,テトラエチルエステルであることを特徴とする請求項1に記載の方法。
- 前記作用物質が、ホスホン酸,[[3,5−ビス(1,1−ジメチルエチル)−4−ヒドロキシフェニル]エテニリデン]ビス−,テトラキス(1−メチルエチル)エステルであることを特徴とする請求項1に記載の方法。
- 前記組成物中の前記作用物質の濃度が0.1%〜30%であることを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 前記組成物が、ヒトの毛嚢試験法にて試験される場合に、少なくとも30%の発毛を低減することを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 前記作用物質が、皮膚1平方センチメートル当たり前記作用物質10〜3000マイクログラムの量で前記皮膚に適用されることを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 前記皮膚領域がヒトの顔面であることを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 前記組成物が、剃毛と併せて前記皮膚領域に適用されることを特徴とする請求項25に記載の方法。
- 前記皮膚領域がヒトの脚又は腕上であることを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 前記皮膚領域が腋の下であることを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 前記皮膚領域がヒトの胴体上であることを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 前記発毛がアンドロゲン刺激発毛を含むことを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 前記組成物が、同じく発毛の低減を引き起こす第2の構成成分をさらに含むことを特徴とする請求項1〜21のいずれか1項に記載の方法。
- 哺乳類の発毛を低減する美容方法であって、
発毛の低減が所望される毛嚢を含む皮膚領域を選択する工程、及び
胆汁酸類、胆汁酸類縁体、及び胆汁酸誘導体から成る群から選択される化合物を含む皮膚科学的に許容可能な組成物を、発毛を低減するのに有効な量で前記皮膚領域に適用する工程を含むことを特徴とする方法。 - 哺乳類の発毛を低減する美容方法であって、
発毛の低減が所望される毛嚢を含む皮膚領域を選択する工程、及び
E−ジフルオロメチルオルニチン及びファルネソールのカルバメート又はエステル以外の化合物を含む皮膚科学的に許容可能な組成物を発毛を低減するのに有効な量で前記皮膚領域に適用する工程を含み、
前記化合物は、FXR−RXRヘテロ二量体の形成を増大させる化合物、コアクチベーター補充及びFXR−RXRとの相互作用を促す化合物、及びファルネソイドX受容体の発現を増大させる化合物から成る群から選択されることを特徴とする方法。 - ファルネソイドX受容体の作用物質を、肌の角質を取り除いた皮膚領域に適用する工程を含むことを特徴とする肌の角質を取り除いた皮膚領域を処置する方法。
- 前記肌の角質を取り除いた皮膚領域が、ファルネソイドX受容体の作用物質を適用する前に剃毛されていることを特徴とする請求項34に記載の方法。
- 前記薬剤を適用する領域にて発毛を阻害するための薬剤の調製におけるファルネソイドX受容体の作用物質の使用。
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US11/141,798 US7618956B2 (en) | 2005-05-31 | 2005-05-31 | Reduction of hair growth |
US11/141,798 | 2005-05-31 | ||
PCT/US2006/018663 WO2006130330A2 (en) | 2005-05-31 | 2006-05-15 | Reduction of hair growth |
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DE102009029813A1 (de) | 2009-06-18 | 2010-12-23 | Henkel Ag & Co. Kgaa | Antifalten-Kosmetikum |
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DE102009037537A1 (de) | 2009-08-17 | 2010-06-02 | Henkel Ag & Co. Kgaa | Antifalten-Kosmetikum |
DE102009037900A1 (de) | 2009-08-19 | 2010-06-02 | Henkel Ag & Co. Kgaa | Antifalten-Kosmetikum mit Baicalin |
DE102009039393A1 (de) | 2009-08-31 | 2010-06-10 | Henkel Ag & Co. Kgaa | Antifalten-Kosmetikum mit einem Extrakt aus Sommer-Knotenblumen |
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- 2006-05-15 CN CNA2006800188989A patent/CN101184532A/zh active Pending
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WO2003002077A2 (en) * | 2001-06-27 | 2003-01-09 | The Gillette Company | Reduction of hair growth |
JP2005015408A (ja) * | 2003-06-27 | 2005-01-20 | Kanebo Cosmetics Inc | 発毛抑制皮膚外用剤 |
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JP2013534218A (ja) * | 2010-08-05 | 2013-09-02 | コグニス・アイピー・マネージメント・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツング | 化粧品調製物 |
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US20060269496A1 (en) | 2006-11-30 |
BRPI0611490A2 (pt) | 2010-09-08 |
CA2729440A1 (en) | 2006-12-07 |
CN101184532A (zh) | 2008-05-21 |
AU2006252877B2 (en) | 2011-05-26 |
CA2729437A1 (en) | 2006-12-07 |
WO2006130330A3 (en) | 2007-03-22 |
CA2608053A1 (en) | 2006-12-07 |
US7618956B2 (en) | 2009-11-17 |
WO2006130330A2 (en) | 2006-12-07 |
JP4801150B2 (ja) | 2011-10-26 |
CA2729431A1 (en) | 2006-12-07 |
CA2729438A1 (en) | 2006-12-07 |
EP1888176A2 (en) | 2008-02-20 |
AU2006252877A1 (en) | 2006-12-07 |
US20100021412A1 (en) | 2010-01-28 |
MX2007015060A (es) | 2008-01-28 |
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