JP6796601B2 - 脂肪を低減させるための美容上の方法及び治療用途 - Google Patents
脂肪を低減させるための美容上の方法及び治療用途 Download PDFInfo
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Description
本願は、2015年4月30日に提出された米国特許仮出願第62/154,926号に基づく利益を主張するものであり、この仮出願は、参照により、その全体が本明細書に援用されるとともに、本願における優先権及び/または利益の主張の基礎としての役割を果たす。
この実施例では、式I及びIIによる化合物に活性がないことが示されている。概して、インビトロインピーダンスアッセイにおいて、ビマトプロストまたは式Iの化合物を10-5〜10-12Mの濃度で、ヒト毛乳頭細胞とともにインキュベートした。ビマトプロストによって、下方信号(緩和)、すなわちインピーダンスの低下がもたらされたのに対して、式Iの化合物によって、検出可能な作用は全くもたらされなかった。独立した実験を3回行った。
この実施例では、式Iの化合物が、完全に発育毛するまでの時間を短縮しないことが示されている。概して、式Iの化合物及びビマトプロストをミノキシジル製剤(50%プロピレングリコール、30%エチルアルコール)中に、いずれの化合物も0.03%の濃度で調製した。いずれの化合物も、(Khidhir et al.FASEB J.2013 27(2):557−567に記載されているように、)マウスの剃毛背部に局所投与した。
この実施例では、式I及びIIの化合物が前脂肪細胞を刺激することが示されている。概して、式I及びIIの化合物、ならびにビマトプロストをxCelligenceインピーダンスアッセイで試験した。ビマトプロストも、式I及びIIの化合物も、ヒト前脂肪細胞のプロスタミドレセプターを刺激する。
この実施例では、式Iの化合物を毎日、経口投与すると、体重増加が緩やかになり、平均体重が低下することが示されている。概して、雄のラット(n=17〜20)及び雌のラット(n=17〜20)に毎日、6カ月間、下記の用量で経口投与(強制投与)した。式Iの化合物は、5mg/kg/日で雌雄両方、0.3mg/kg/日で雌の体重増加を抑制した(p<0.05)。薬物の投与を中止した後には、この作用は、多少可逆的であった。
〔1〕
対象の体脂肪の低減方法であって、体脂肪を低減させる必要のある対象に、下記の式Iの化合物、下記の式IIの化合物、またはこれらの混合物を有効量投与することを含む前記方法。
〔2〕
前記式Iの化合物を有効量投与する、〔1〕に記載の方法。
〔3〕
前記式IIの化合物を有効量投与する、〔1〕に記載の方法。
〔4〕
脂肪低減部位で実質的な発育毛を引き起こすことなく脂肪を低減させるのに有効な量で、前記化合物または化合物の混合物を投与する、〔1〕〜〔3〕のいずれか1項に記載の方法。
〔5〕
脂肪低減部位で追加的な発育毛を引き起こすことなく脂肪を低減させるのに有効な量で、前記化合物または化合物の混合物を投与する、〔1〕〜〔3〕のいずれか1項に記載の方法。
〔6〕
約0.05mg/kg〜約5mg/kgの量で、前記化合物または化合物の混合物を投与する、〔1〕〜〔5〕のいずれか1項に記載の方法。
〔7〕
約0.3mg/kg〜約5mg/kgの量で、前記化合物または化合物の混合物を投与する、〔1〕〜〔5〕のいずれか1項に記載の方法。
〔8〕
前記化合物または化合物の混合物を局所投与する、注射によって投与する、経皮投与する、または経口投与する、〔1〕〜〔7〕のいずれか1項に記載の方法。
〔9〕
対象の顎下領域、大腿部、腹部または胴部のうちの少なくとも1つに、前記化合物または化合物の混合物を投与する〔1〕〜〔7〕のいずれか1項に記載の方法。
〔10〕
前記化合物または化合物の混合物を全身投与する、〔1〕〜〔7〕のいずれか1項に記載の方法。
〔11〕
前記化合物または化合物の混合物を脂肪沈着部に局所投与する、〔1〕〜〔7〕のいずれか1項に記載の方法。
〔12〕
脂肪を低減させるのに用いる医薬組成物であって、有効量の下記の式Iの化合物、下記の式IIの化合物またはこれらの混合物、及び1つ以上の製薬学的に許容可能な賦形剤を含む前記医薬組成物。
〔13〕
前記式Iの化合物を有効量含む、〔12〕に記載の医薬組成物。
〔14〕
前記式IIの化合物を有効量含む、〔12〕に記載の医薬組成物。
〔15〕
脂肪低減部位で実質的な発育毛を引き起こすことなく脂肪を低減させる、〔12〕〜〔14〕のいずれか1項に記載の医薬組成物。
〔16〕
脂肪低減部位で追加的な発育毛を引き起こすことなく脂肪を低減させる、〔12〕〜〔14〕のいずれか1項に記載の医薬組成物。
〔17〕
約0.05mg/kg〜約5mg/kgの量で、前記化合物または化合物の混合物を含む、〔12〕〜〔16〕のいずれか1項に記載の組成物。
〔18〕
約0.03mg/kg〜約5mg/kgの量で、前記化合物または化合物の混合物を含む、〔12〕〜〔16〕のいずれか1項に記載の医薬組成物。
〔19〕
局所投与、注射による投与、経皮投与、または経口投与に適する、〔12〕〜〔18〕のいずれか1項に記載の医薬組成物。
〔20〕
対象の顎下領域、大腿部、腹部、または胴部のうちの少なくとも1つに投与するのに適する、〔12〕〜〔18〕のいずれか1項に記載の医薬組成物。
〔21〕
全身投与に適する、〔12〕〜〔18〕のいずれか1項に記載の医薬組成物。
〔22〕
脂肪沈着部への局所投与に適する、〔12〕〜〔18〕のいずれか1項に記載の医薬組成物。
Claims (18)
- 体脂肪の低減に用いるための局所投与又は経皮投与用医薬の製造における、下記の式Iの化合物、下記の式IIの化合物、またはこれらの混合物の使用。
- 前記式Iの化合物の使用である、請求項1に記載の使用。
- 前記式IIの化合物の使用である、請求項1に記載の使用。
- 脂肪低減部位で実質的な発育毛を引き起こすことなく脂肪を低減させる医薬の製造における、請求項1〜3のいずれか1項に記載の使用。
- 脂肪低減部位で追加的な発育毛を引き起こすことなく脂肪を低減させる医薬の製造における、請求項1〜3のいずれか1項に記載の使用。
- 前記医薬は、式Iの化合物、下記の式IIの化合物、またはこれらの混合物が0.05mg/kg体重〜5mg/kg体重の量で投与される医薬である、請求項1〜5のいずれか1項に記載の使用。
- 前記医薬は、式Iの化合物、下記の式IIの化合物、またはこれらの混合物が0.3mg/kg体重〜5mg/kg体重の量で投与される医薬である、請求項1〜5のいずれか1項に記載の使用。
- 前記医薬は、顎下領域、大腿部、腹部または胴部のうちの少なくとも1つに局所投与又は経皮投与される医薬である、請求項1〜7のいずれか1項に記載の使用。
- 前記医薬は、脂肪沈着部に局所投与される医薬である、請求項1〜7のいずれか1項に記載の使用。
- 脂肪低減に用いるための局所投与又は経皮投与用医薬組成物であって、下記の式Iの化合物、下記の式IIの化合物またはこれらの混合物を含み、且つ1つ以上の製薬学的に許容可能な賦形剤を含んでいてもよい、前記医薬組成物。
- 前記式Iの化合物を含む、請求項10に記載の医薬組成物。
- 前記式IIの化合物を含む、請求項10に記載の医薬組成物。
- 脂肪低減部位で実質的な発育毛を引き起こすことなく脂肪を低減させる、請求項10〜12のいずれか1項に記載の医薬組成物。
- 脂肪低減部位で追加的な発育毛を引き起こすことなく脂肪を低減させる、請求項10〜12のいずれか1項に記載の医薬組成物。
- 0.05mg/kg体重〜5mg/kg体重の量で、前記式Iの化合物、下記の式IIの化合物またはこれらの混合物が投与される、請求項10〜14のいずれか1項に記載の医薬組成物。
- 0.3mg/kg体重〜5mg/kg体重の量で、前記式Iの化合物、下記の式IIの化合物またはこれらの混合物が投与される、請求項10〜14のいずれか1項に記載の医薬組成物。
- 顎下領域、大腿部、腹部、または胴部のうちの少なくとも1つに局所投与又は経皮投与される、請求項10〜16のいずれか1項に記載の医薬組成物。
- 脂肪沈着部に局所投与される、請求項10〜16のいずれか1項に記載の医薬組成物。
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AU2014228307A1 (en) | 2013-03-15 | 2015-09-10 | Allergan, Inc. | Bimatoprost for enhancement of leptin production |
CN105101962A (zh) | 2013-04-12 | 2015-11-25 | 阿勒根公司 | 用于减脂的比马前列素、比马前列素类似物、前列腺酰胺和前列腺素的持续释放 |
NO2753788T3 (ja) * | 2013-05-10 | 2018-06-16 | ||
WO2015200425A1 (en) * | 2014-06-27 | 2015-12-30 | Topokine Therapeutics, Inc. | Topical dosage regimen |
BR112017023316A2 (pt) | 2015-04-30 | 2018-08-14 | Allergan, Inc. | método cosmético e uso terapêutico para redução de gordura |
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2016
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AU2016254208B2 (en) | 2021-07-15 |
RU2017140078A3 (ja) | 2019-08-06 |
EP3288559B1 (en) | 2020-06-24 |
US20180071308A1 (en) | 2018-03-15 |
CN107660145A (zh) | 2018-02-02 |
JP2018514554A (ja) | 2018-06-07 |
CN107660145B (zh) | 2021-04-20 |
AU2016254208A1 (en) | 2017-11-16 |
UA120775C2 (uk) | 2020-02-10 |
SG11201708827SA (en) | 2017-11-29 |
KR20170141770A (ko) | 2017-12-26 |
US20160317550A1 (en) | 2016-11-03 |
KR102159427B1 (ko) | 2020-09-24 |
EP3288559A1 (en) | 2018-03-07 |
IL255318B (en) | 2021-05-31 |
IL255318A0 (en) | 2017-12-31 |
US9795615B2 (en) | 2017-10-24 |
MX2017013819A (es) | 2018-02-21 |
US10117877B2 (en) | 2018-11-06 |
IL282473A (en) | 2021-06-30 |
WO2016176640A1 (en) | 2016-11-03 |
BR112017023316A2 (pt) | 2018-08-14 |
HK1250483A1 (zh) | 2018-12-21 |
CA2983942A1 (en) | 2016-11-03 |
EP3721885A1 (en) | 2020-10-14 |
RU2017140078A (ru) | 2019-05-30 |
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