JP2015527386A5 - - Google Patents
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- JP2015527386A5 JP2015527386A5 JP2015530461A JP2015530461A JP2015527386A5 JP 2015527386 A5 JP2015527386 A5 JP 2015527386A5 JP 2015530461 A JP2015530461 A JP 2015530461A JP 2015530461 A JP2015530461 A JP 2015530461A JP 2015527386 A5 JP2015527386 A5 JP 2015527386A5
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- Prior art keywords
- omega
- derivative
- composition according
- fatty acid
- acid
- 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.)
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- 239000000203 mixture Substances 0.000 claims 20
- 235000020660 omega-3 fatty acid Nutrition 0.000 claims 8
- 235000020777 polyunsaturated fatty acids Nutrition 0.000 claims 8
- MBMBGCFOFBJSGT-KUBAVDMBSA-N Docosahexaenoic acid Chemical compound CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCC(O)=O MBMBGCFOFBJSGT-KUBAVDMBSA-N 0.000 claims 7
- 239000007788 liquid Substances 0.000 claims 7
- 150000001335 aliphatic alkanes Chemical class 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 210000001519 tissues Anatomy 0.000 claims 4
- ZCDMRPMKAQLWAO-PZLFCYFRSA-N (5Z,8Z,11Z,14Z)-icosa-5,8,11,14-tetraenoic acid;(9Z,12Z)-octadeca-9,12-dienoic acid Chemical class CCCCC\C=C/C\C=C/CCCCCCCC(O)=O.CCCCC\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O ZCDMRPMKAQLWAO-PZLFCYFRSA-N 0.000 claims 3
- JAZBEHYOTPTENJ-JLNKQSITSA-N Eicosapentaenoic acid Chemical class CC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CCCC(O)=O JAZBEHYOTPTENJ-JLNKQSITSA-N 0.000 claims 3
- 229940012843 Omega-3 Fatty Acids Drugs 0.000 claims 3
- 229940033080 Omega-6 Fatty Acids Drugs 0.000 claims 3
- 150000002148 esters Chemical class 0.000 claims 3
- 210000004877 mucosa Anatomy 0.000 claims 3
- 235000020665 omega-6 fatty acid Nutrition 0.000 claims 3
- 229960005135 Eicosapentaenoic Acid Drugs 0.000 claims 2
- 235000014113 dietary fatty acids Nutrition 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 229960004363 doconexent Drugs 0.000 claims 2
- 235000020669 docosahexaenoic acid Nutrition 0.000 claims 2
- 229940090949 docosahexaenoic acid Drugs 0.000 claims 2
- 235000020673 eicosapentaenoic acid Nutrition 0.000 claims 2
- 239000000194 fatty acid Substances 0.000 claims 2
- 150000004665 fatty acids Chemical class 0.000 claims 2
- 150000002194 fatty esters Chemical class 0.000 claims 2
- 239000006014 omega-3 oil Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- 229940064701 Corticosteroid nasal preparations for topical use Drugs 0.000 claims 1
- 229960001334 Corticosteroids 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
- 206010013774 Dry eye Diseases 0.000 claims 1
- SSQPWTVBQMWLSZ-AAQCHOMXSA-N Ethyl eicosapentaenoic acid Chemical compound CCOC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/C\C=C/CC SSQPWTVBQMWLSZ-AAQCHOMXSA-N 0.000 claims 1
- 229920000064 Ethyl eicosapentaenoic acid Polymers 0.000 claims 1
- AXISYYRBXTVTFY-UHFFFAOYSA-N Isopropyl myristate Chemical compound CCCCCCCCCCCCCC(=O)OC(C)C AXISYYRBXTVTFY-UHFFFAOYSA-N 0.000 claims 1
- 206010023332 Keratitis Diseases 0.000 claims 1
- 229940057917 Medium chain triglycerides Drugs 0.000 claims 1
- 210000002850 Nasal Mucosa Anatomy 0.000 claims 1
- 210000003491 Skin Anatomy 0.000 claims 1
- 239000004164 Wax ester Substances 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000005907 alkyl ester group Chemical group 0.000 claims 1
- 230000003110 anti-inflammatory Effects 0.000 claims 1
- 150000001840 cholesterol esters Chemical class 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- -1 ester derivative of omega-3 fatty acid Chemical class 0.000 claims 1
- TYLNXKAVUJJPMU-PWQIQEKYSA-N ethyl (2Z,4Z,6Z,8Z,10Z,12E)-docosa-2,4,6,8,10,12-hexaenoate Chemical compound CCCCCCCCC\C=C\C=C/C=C\C=C/C=C\C=C/C(=O)OCC TYLNXKAVUJJPMU-PWQIQEKYSA-N 0.000 claims 1
- 150000002191 fatty alcohols Chemical class 0.000 claims 1
- 150000002327 glycerophospholipids Chemical class 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 230000002584 immunomodulator Effects 0.000 claims 1
- 229940121354 immunomodulators Drugs 0.000 claims 1
- 230000004968 inflammatory condition Effects 0.000 claims 1
- 229940074928 isopropyl myristate Drugs 0.000 claims 1
- 201000010666 keratoconjunctivitis Diseases 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 239000002480 mineral oil Substances 0.000 claims 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims 1
- 239000003921 oil Substances 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 150000003408 sphingolipids Chemical class 0.000 claims 1
- 230000000087 stabilizing Effects 0.000 claims 1
- 150000003445 sucroses Chemical class 0.000 claims 1
- 229940083878 topical for treatment of hemorrhoids and anal fissures Corticosteroids Drugs 0.000 claims 1
- 150000003626 triacylglycerols Chemical class 0.000 claims 1
- 235000019386 wax ester Nutrition 0.000 claims 1
Claims (19)
- 多価不飽和脂肪酸またはその誘導体を含む安定液体組成物であって、前記多価不飽和脂肪酸またはその誘導体が、式
F(CF2)n(CH2)mH
または式
F(CF2)n(CH2)m(CF2)oF
(式中、n、mおよびoは、3〜20の範囲から独立して選択される整数である)の半フッ素化アルカンを含む液体ビヒクルに溶解、分散または懸濁されており、前記液体ビヒクルが水を含まない、安定液体組成物。 - 前記多価不飽和脂肪酸の誘導体がエステル誘導体である、請求項1に記載の組成物。
- 前記多価不飽和脂肪酸またはその誘導体が、オメガ−3もしくはオメガ−6脂肪酸もしくはそれらの誘導体であるか、またはオメガ−3もしくはオメガ−6脂肪酸もしくはそれらの誘導体の混合物である、請求項1または請求項2に記載の組成物。
- 前記多価不飽和脂肪酸またはその誘導体がオメガ−3脂肪酸またはその誘導体であり、前記オメガ−3脂肪酸またはその誘導体のみを活性成分として含む、請求項3に記載の組成物。
- 前記オメガ−3脂肪酸が、α−リノレン酸、ドコサヘキサエン酸、エイコサペンタエン酸、またはそれらのエステル誘導体から選択される、請求項3に記載の組成物。
- 前記オメガ−3脂肪酸が、ドコサヘキサエン酸誘導体、エイコサペンタエン酸誘導体、レゾルビンまたはニューロプロテクチンから選択される、請求項3に記載の組成物。
- 前記オメガ−3脂肪酸のエステル誘導体が、ドコサヘキサエン酸エチルエステルまたはエイコサペンタエン酸エチルエステルから選択される、請求項5に記載の組成物。
- 液体半フッ素化アルカンに溶解または分散された1つ以上のオメガ−3脂肪酸またはそのエステル誘導体からなる、請求項4または請求項5に記載の組成物。
- F(CF2)6(CH2)8Hに溶解または分散されたドコサヘキサエン酸および/もしくはエイコサペンタエン酸またはそれらのアルキルエステル誘導体からなる、請求項8に記載の組成物。
- 0.01〜10wt%の前記多価不飽和脂肪酸またはその誘導体を含む、請求項1〜9のいずれか一項に記載の組成物。
- 前記半フッ素化アルカンが、F(CF2)4(CH2)5H、F(CF2)4(CH2)6H、F(CF2)4(CH2)8H、F(CF2)6(CH2)4H、F(CF2)6(CH2)6H、F(CF2)6(CH2)8H、F(CF2)6(CH2)10H、F(CF 2 ) 8 (CH 2 ) 10 HおよびF(CF 2 ) 10 (CH 2 ) 12 Hから選択される、請求項1〜10のいずれか一項に記載の組成物。
- トリグリセリド油、鉱油、中鎖トリグリセリド、油性脂肪酸、ミリスチン酸イソプロピル、油性脂肪アルコール、ソルビトールと脂肪酸とのエステル、油性スクロースエステル、油性コレステロールエステル、油性ワックスエステル、グリセロリン脂質、およびスフィンゴ脂質から選択される脂質または油性賦形剤をさらに含む、請求項1〜11のいずれか一項に記載の組成物。
- NSAID、コルチコステロイドおよび免疫調節剤の群から選択される抗炎症化合物をさらに含む、請求項1〜3、5または11のいずれか一項に記載の組成物。
- 医薬として使用するための、請求項1〜13のいずれか一項に記載の組成物。
- 前記医薬が、眼もしくは眼組織、皮膚または頬粘膜、肛門粘膜、膣粘膜もしくは鼻粘膜に局所投与される、医薬として使用するための請求項14に記載の組成物。
- 前記医薬が、眼または眼組織の症状または疾患の処置に使用される医薬として使用するための、請求項14または15に記載の組成物。
- 前記眼または眼組織の症状または疾患が、眼組織の炎症症状もしくは乾性角結膜炎(ドライアイ)またはそれらに関連する症候もしくは症状である、請求項16に記載の組成物。
- オメガ3−脂肪酸、オメガ−6脂肪酸、もしくはこれらのエステル誘導体またはこれらの混合物から選択される多価不飽和脂肪酸を安定化する方法であって、式
F(CF2)n(CH2)mH
または式
F(CF2)n(CH2)m(CF2)oF
(式中、n、mおよびoは、3〜20の範囲から独立して選択される整数である)の半フッ素化アルカンを含む液体ビヒクルに前記多価不飽和脂肪酸を溶解、分散または懸濁する工程を含み、前記液体ビヒクルが水を含まない、方法。 - 前記半フッ素化アルカンが、F(CF2)4(CH2)5H、F(CF2)4(CH2)6H、F(CF2)4(CH2)8H、F(CF2)6(CH2)4H、F(CF2)6(CH2)6H、F(CF2)6(CH2)8H、F(CF2)6(CH2)10H、F(CF 2 ) 8 (CH 2 ) 10 HおよびF(CF 2 ) 10 (CH 2 ) 12 Hから選択される、請求項18に記載の方法。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP12183997.1 | 2012-09-12 | ||
EP12183997 | 2012-09-12 | ||
EP13169399.6 | 2013-05-27 | ||
EP13169399 | 2013-05-27 | ||
PCT/EP2013/068909 WO2014041071A1 (en) | 2012-09-12 | 2013-09-12 | Semifluorinated alkane compositions |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016215744A Division JP6352366B2 (ja) | 2012-09-12 | 2016-11-03 | 半フッ素化アルカン組成物 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2015527386A JP2015527386A (ja) | 2015-09-17 |
JP2015527386A5 true JP2015527386A5 (ja) | 2016-10-13 |
JP6039152B2 JP6039152B2 (ja) | 2016-12-07 |
Family
ID=49150965
Family Applications (5)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2015530461A Active JP6039152B2 (ja) | 2012-09-12 | 2013-09-12 | 半フッ素化アルカン組成物 |
JP2016215744A Active JP6352366B2 (ja) | 2012-09-12 | 2016-11-03 | 半フッ素化アルカン組成物 |
JP2018108178A Active JP6640919B2 (ja) | 2012-09-12 | 2018-06-06 | 半フッ素化アルカン組成物 |
JP2018170122A Active JP6440893B1 (ja) | 2012-09-12 | 2018-09-12 | 半フッ素化アルカン組成物 |
JP2019235392A Pending JP2020073535A (ja) | 2012-09-12 | 2019-12-26 | 半フッ素化アルカン組成物 |
Family Applications After (4)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016215744A Active JP6352366B2 (ja) | 2012-09-12 | 2016-11-03 | 半フッ素化アルカン組成物 |
JP2018108178A Active JP6640919B2 (ja) | 2012-09-12 | 2018-06-06 | 半フッ素化アルカン組成物 |
JP2018170122A Active JP6440893B1 (ja) | 2012-09-12 | 2018-09-12 | 半フッ素化アルカン組成物 |
JP2019235392A Pending JP2020073535A (ja) | 2012-09-12 | 2019-12-26 | 半フッ素化アルカン組成物 |
Country Status (17)
Country | Link |
---|---|
US (5) | US9770508B2 (ja) |
EP (4) | EP4342537A3 (ja) |
JP (5) | JP6039152B2 (ja) |
KR (2) | KR102115111B1 (ja) |
CN (1) | CN104755073B (ja) |
AU (2) | AU2013314303B2 (ja) |
BR (2) | BR122019024319B1 (ja) |
CA (2) | CA2883003C (ja) |
DE (1) | DE202013012753U1 (ja) |
DK (2) | DK3181119T3 (ja) |
ES (3) | ES2621226T3 (ja) |
HK (1) | HK1210052A1 (ja) |
MX (1) | MX350588B (ja) |
MY (1) | MY165124A (ja) |
PL (3) | PL3181119T3 (ja) |
PT (2) | PT3181119T (ja) |
WO (1) | WO2014041071A1 (ja) |
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