JPWO2020146666A5 - - Google Patents
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- JPWO2020146666A5 JPWO2020146666A5 JP2021540019A JP2021540019A JPWO2020146666A5 JP WO2020146666 A5 JPWO2020146666 A5 JP WO2020146666A5 JP 2021540019 A JP2021540019 A JP 2021540019A JP 2021540019 A JP2021540019 A JP 2021540019A JP WO2020146666 A5 JPWO2020146666 A5 JP WO2020146666A5
- Authority
- JP
- Japan
- Prior art keywords
- agent
- formulated
- skin
- damage
- radiation
- 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.)
- Pending
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- 239000003795 chemical substances by application Substances 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 6
- 229960004308 ACETYLCYSTEINE Drugs 0.000 claims 4
- UJCHIZDEQZMODR-SCSAIBSYSA-N Acetylcysteinamide Chemical compound CC(=O)N[C@H](CS)C(N)=O UJCHIZDEQZMODR-SCSAIBSYSA-N 0.000 claims 4
- PWKSKIMOESPYIA-BYPYZUCNSA-N L-N-acetyl-Cysteine Chemical compound CC(=O)N[C@@H](CS)C(O)=O PWKSKIMOESPYIA-BYPYZUCNSA-N 0.000 claims 4
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
- 229940095259 Butylated Hydroxytoluene Drugs 0.000 claims 2
- 239000004322 Butylated hydroxytoluene Substances 0.000 claims 2
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 claims 2
- LNTHITQWFMADLM-UHFFFAOYSA-N Gallic acid Chemical compound OC(=O)C1=CC(O)=C(O)C(O)=C1 LNTHITQWFMADLM-UHFFFAOYSA-N 0.000 claims 2
- 206010040829 Skin discolouration Diseases 0.000 claims 2
- GEHJYWRUCIMESM-UHFFFAOYSA-L Sodium sulfite Chemical compound [Na+].[Na+].[O-]S([O-])=O GEHJYWRUCIMESM-UHFFFAOYSA-L 0.000 claims 2
- 201000004569 blindness Diseases 0.000 claims 2
- 235000010354 butylated hydroxytoluene Nutrition 0.000 claims 2
- 201000004624 dermatitis Diseases 0.000 claims 2
- 231100000406 dermatitis Toxicity 0.000 claims 2
- KCXVZYZYPLLWCC-UHFFFAOYSA-N edta Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(O)=O)CC(O)=O KCXVZYZYPLLWCC-UHFFFAOYSA-N 0.000 claims 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 230000037380 skin damage Effects 0.000 claims 2
- 230000036559 skin health Effects 0.000 claims 2
- 230000002087 whitening Effects 0.000 claims 2
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-N 0.000 claims 2
- JLPULHDHAOZNQI-ZTIMHPMXSA-N 1-hexadecanoyl-2-(9Z,12Z-octadecadienoyl)-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCC\C=C/C\C=C/CCCCC JLPULHDHAOZNQI-ZTIMHPMXSA-N 0.000 claims 1
- DVOVBGJJSFSOPZ-UHFFFAOYSA-N 2-acetamidopropanamide Chemical compound NC(=O)C(C)NC(C)=O DVOVBGJJSFSOPZ-UHFFFAOYSA-N 0.000 claims 1
- 208000009043 Chemical Burns Diseases 0.000 claims 1
- 229960001305 Cysteine Hydrochloride Drugs 0.000 claims 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 229940074391 Gallic acid Drugs 0.000 claims 1
- QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 claims 1
- 239000011786 L-ascorbyl-6-palmitate Substances 0.000 claims 1
- 229940067606 Lecithin Drugs 0.000 claims 1
- FEWJPZIEWOKRBE-XIXRPRMCSA-N Mesotartaric acid Chemical compound OC(=O)[C@@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-XIXRPRMCSA-N 0.000 claims 1
- 108009000578 Oxidative Stress Proteins 0.000 claims 1
- 229940100996 SODIUM BISULFATE Drugs 0.000 claims 1
- 210000003491 Skin Anatomy 0.000 claims 1
- 208000006641 Skin Disease Diseases 0.000 claims 1
- WBHQBSYUUJJSRZ-UHFFFAOYSA-M Sodium bisulfate Chemical compound [Na+].OS([O-])(=O)=O WBHQBSYUUJJSRZ-UHFFFAOYSA-M 0.000 claims 1
- 206010053615 Thermal burn Diseases 0.000 claims 1
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Vitamin C Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 1
- QIJRTFXNRTXDIP-JIZZDEOASA-N [(1R)-1-carboxy-2-sulfanylethyl]azanium;chloride;hydrate Chemical compound O.Cl.SC[C@H](N)C(O)=O QIJRTFXNRTXDIP-JIZZDEOASA-N 0.000 claims 1
- 229940087168 alpha Tocopherol Drugs 0.000 claims 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 claims 1
- 235000010323 ascorbic acid Nutrition 0.000 claims 1
- 229960005070 ascorbic acid Drugs 0.000 claims 1
- 239000011668 ascorbic acid Substances 0.000 claims 1
- 235000010385 ascorbyl palmitate Nutrition 0.000 claims 1
- 235000019282 butylated hydroxyanisole Nutrition 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 235000004515 gallic acid Nutrition 0.000 claims 1
- 239000000787 lecithin Substances 0.000 claims 1
- 235000010445 lecithin Nutrition 0.000 claims 1
- 239000007788 liquid Substances 0.000 claims 1
- 239000008185 minitablet Substances 0.000 claims 1
- 230000004297 night vision Effects 0.000 claims 1
- 230000036542 oxidative stress Effects 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 229910000342 sodium bisulfate Inorganic materials 0.000 claims 1
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 claims 1
- 235000010262 sodium metabisulphite Nutrition 0.000 claims 1
- 235000010265 sodium sulphite Nutrition 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 230000036561 sun exposure Effects 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 229960001367 tartaric acid Drugs 0.000 claims 1
- 239000011975 tartaric acid Substances 0.000 claims 1
- 235000002906 tartaric acid Nutrition 0.000 claims 1
- 230000036575 thermal burns Effects 0.000 claims 1
- 229960000984 tocofersolan Drugs 0.000 claims 1
- 230000000007 visual effect Effects 0.000 claims 1
- 230000004393 visual impairment Effects 0.000 claims 1
- 201000006083 xeroderma pigmentosum Diseases 0.000 claims 1
- 239000002076 α-tocopherol Substances 0.000 claims 1
- 235000004835 α-tocopherol Nutrition 0.000 claims 1
Claims (8)
- 放射線皮膚炎、皮膚ライトニング、放射線による皮膚への損傷のうちの少なくとも1つの予防及び治療、ホワイトニング、又は皮膚の健康の改善を必要とするヒト対象における放射線皮膚炎、皮膚ライトニング、放射線による皮膚への損傷のうちの少なくとも1つの予防及び治療、ホワイトニング、又は皮膚の健康の改善のための薬剤であって、治療有効量のN-アセチルシステイン(NAC)、N-アセチルシステインアミド(NACA)、又は(2R、2R')-3,3'-ジスルファンジイルビス(2-アセトアミドプロパンアミド)(diNACA)を含む、前記薬剤。
- NAC、NACA、又はdiNACAが、以下の少なくとも1つに該当するように製剤化された、請求項1に記載の薬剤。
薬学的に許容される担体中において、又は薬学的に許容される担体と共に製剤化された;
経口、静脈内、筋肉内、経腸、眼内、網膜下、硝子体内、局所、眼、舌下、皮膚、皮下、又は直腸内に投与されるように製剤化された;
約0.5~150mg/Kgの1日用量で製剤化された;
1日2回又は3回の投与用に製剤化された;
第2の活性薬剤と共に製剤化された;
1用量当たり100、150、150、300、333、400、500、600、700、750、800、900、1,000、2,500、5,000、7,500、又は10,000mgで製剤化された;
ミニ錠剤、カプセル、錠剤、発泡剤、デュアル放出、混合放出、サシェ、粉末、又は液剤に製剤化された; - NAC、NACA、又はdiNACAが、アスコルビン酸、システイン塩酸塩、硫酸水素ナトリウム、二亜硫酸ナトリウム、亜硫酸ナトリウム、パルミチン酸アスコルビル、ブチル化ヒドロキシアニソール(BHA)、ブチル化ヒドロキシトルエン(BHT)、レシチン、没食子酸プロピル、α-トコフェロール、クエン酸、エチレンジアミン四酢酸(EDTA)、ソルビトール、酒石酸、又はリン酸のうちの少なくとも1つから選択される第2の活性薬剤と共に投与される、請求項2に記載の薬剤。
- 治療有効量が、好ましくは、夜間視力の欠損、全体的な視力の欠損、視野の欠損のうちの少なくとも1つを、2週間、1カ月、2カ月、3カ月、6カ月、1年、2年、又は5年のうちの少なくとも1つから選択される規定された期間にわたり、未治療の対照対象と比較して少なくとも10%、少なくとも15%、少なくとも20%、少なくとも25%、少なくとも30%、少なくとも35%、少なくとも40%、少なくとも45%、少なくとも50%、少なくとも55%、少なくとも60%、少なくとも65%、少なくとも70%、少なくとも75%、少なくとも80%、少なくとも85%、少なくとも90%、少なくとも95%、又はそれ以上減少させる治療薬の量を意味する、請求項1に記載の薬剤。
- 日光曝露からの放射線による皮膚への損傷を防ぐための薬剤である、請求項1に記載の薬剤。
- 生物兵器への曝露、化学熱傷、熱傷、摩擦によって引き起こされる接触損傷を防ぐための薬剤である、請求項1に記載の薬剤。
- 色素性乾皮症を治療するための薬剤である、請求項1に記載の薬剤。
- 酸化的ストレスによって引き起こされるその他の皮膚障害を治療するための薬剤である、請求項1に記載の薬剤。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201962791422P | 2019-01-11 | 2019-01-11 | |
US62/791,422 | 2019-01-11 | ||
PCT/US2020/012975 WO2020146666A1 (en) | 2019-01-11 | 2020-01-09 | N-acetylcysteine amide (naca) and (2r,2r')-3,3'-disulfanediyl bis (2-acetamidopropanamide) (dinaca) for the prevention and treatment of radiation dermatitis and skin lightening, skin whitening and skin improvement |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2022518174A JP2022518174A (ja) | 2022-03-14 |
JPWO2020146666A5 true JPWO2020146666A5 (ja) | 2023-01-20 |
Family
ID=71521154
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2021540019A Pending JP2022518174A (ja) | 2019-01-11 | 2020-01-09 | 放射線皮膚炎の予防及び治療、並びに皮膚ライトニング、皮膚ホワイトニング、並びに皮膚改善のためのn-アセチルシステインアミド(naca)及び(2r,2r’)-3,3’-ジスルファンジイルビス(2-アセトアミドプロパンアミド)(dinaca) |
Country Status (6)
Country | Link |
---|---|
US (1) | US20220105056A1 (ja) |
EP (1) | EP3908271A4 (ja) |
JP (1) | JP2022518174A (ja) |
KR (1) | KR20210114460A (ja) |
CN (1) | CN113573704A (ja) |
WO (1) | WO2020146666A1 (ja) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20190135741A1 (en) | 2017-11-09 | 2019-05-09 | Nacuity Pharmaceuticals, Inc. | Methods of Making Deuterium-Enriched N-acetylcysteine Amide (D-NACA) and (2R, 2R')-3,3'-Disulfanediyl BIS(2-Acetamidopropanamide) (DINACA) and Using D-NACA and DINACA to Treat Diseases Involving Oxidative Stress |
EP3908341A4 (en) | 2019-01-11 | 2022-03-02 | NaCuity Pharmaceuticals, Inc. | TREATMENT OF AGE-RELATED MACULAR DEGENERATION, GLAUCOMA AND DIABETIC RETINOPATHY WITH N-ACETYLCYSTEINE AMIDE (NACA) OR (2R,2R')-3,3'-BIS(2-ACETAMIDOPROPANAMIDE) DISULFANEDIYL (DINACA) |
EP4093389A4 (en) * | 2020-01-24 | 2024-02-21 | NaCuity Pharmaceuticals, Inc. | PRODRUG FOR THE TREATMENT OF DISEASES AND INJURIES OF OXIDATIVE STRESS |
WO2024013711A1 (en) | 2022-07-15 | 2024-01-18 | Universidade De Coimbra | Topical composition and uses thereof |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20080028357A (ko) * | 2005-04-21 | 2008-03-31 | 글렌 에이. 골드스타인 | 산화성 스트레스에 관련된 질병 및 증상 치료용n-아세틸시스테인 아미드(nac 아미드) |
WO2011044230A2 (en) * | 2009-10-06 | 2011-04-14 | Goldstein Glenn A | N-acetylcysteine amide (nac amide) for the treatment of diseases and conditions |
EP2397125A1 (en) * | 2010-06-15 | 2011-12-21 | Histocell, S.L. | Antioxidant composition |
WO2013138744A1 (en) * | 2012-03-16 | 2013-09-19 | M. Alphabet 1, Llc | Compositions for the treatment of skin disorders |
CN108618993B (zh) * | 2018-07-16 | 2021-07-27 | 广东格烯生物科技股份有限公司 | 一种美白组合物及其制备方法和应用 |
-
2020
- 2020-01-09 EP EP20738196.3A patent/EP3908271A4/en active Pending
- 2020-01-09 US US17/421,308 patent/US20220105056A1/en active Pending
- 2020-01-09 WO PCT/US2020/012975 patent/WO2020146666A1/en unknown
- 2020-01-09 JP JP2021540019A patent/JP2022518174A/ja active Pending
- 2020-01-09 KR KR1020217025541A patent/KR20210114460A/ko not_active Application Discontinuation
- 2020-01-09 CN CN202080017282.XA patent/CN113573704A/zh active Pending
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