JP2015512937A5 - - Google Patents
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- JP2015512937A5 JP2015512937A5 JP2015505762A JP2015505762A JP2015512937A5 JP 2015512937 A5 JP2015512937 A5 JP 2015512937A5 JP 2015505762 A JP2015505762 A JP 2015505762A JP 2015505762 A JP2015505762 A JP 2015505762A JP 2015512937 A5 JP2015512937 A5 JP 2015512937A5
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- Prior art keywords
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- subject
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- 150000001875 compounds Chemical class 0.000 claims description 41
- 238000000034 method Methods 0.000 claims description 26
- 239000008194 pharmaceutical composition Substances 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 15
- AKEJUJNQAAGONA-UHFFFAOYSA-N sulfur trioxide Chemical compound O=S(=O)=O AKEJUJNQAAGONA-UHFFFAOYSA-N 0.000 claims description 15
- 239000000203 mixture Substances 0.000 claims description 12
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims description 10
- 150000002632 lipids Chemical class 0.000 claims description 8
- 239000007788 liquid Substances 0.000 claims description 8
- DTGDZMYNKLTSKC-HKQCOZBKSA-N cholest-5-ene Chemical compound C1C=C2CCCC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 DTGDZMYNKLTSKC-HKQCOZBKSA-N 0.000 claims description 6
- DTGDZMYNKLTSKC-UHFFFAOYSA-N cholest-5-ene Natural products C1C=C2CCCCC2(C)C2C1C1CCC(C(C)CCCC(C)C)C1(C)CC2 DTGDZMYNKLTSKC-UHFFFAOYSA-N 0.000 claims description 6
- 239000003085 diluting agent Substances 0.000 claims description 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
- 239000007787 solid Substances 0.000 claims description 6
- 201000001320 Atherosclerosis Diseases 0.000 claims description 5
- 208000031226 Hyperlipidaemia Diseases 0.000 claims description 5
- 235000012000 cholesterol Nutrition 0.000 claims description 5
- 206010012601 diabetes mellitus Diseases 0.000 claims description 5
- 208000010706 fatty liver disease Diseases 0.000 claims description 5
- 208000027866 inflammatory disease Diseases 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 5
- 206010061218 Inflammation Diseases 0.000 claims description 4
- 239000003708 ampul Substances 0.000 claims description 4
- 230000015572 biosynthetic process Effects 0.000 claims description 4
- 230000037396 body weight Effects 0.000 claims description 4
- 230000004054 inflammatory process Effects 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 4
- -1 sulfur trioxide amine Chemical class 0.000 claims description 3
- 239000004067 bulking agent Substances 0.000 claims description 2
- 239000002775 capsule Substances 0.000 claims description 2
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 238000002347 injection Methods 0.000 claims description 2
- 239000007924 injection Substances 0.000 claims description 2
- 238000010255 intramuscular injection Methods 0.000 claims description 2
- 239000007927 intramuscular injection Substances 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 238000007911 parenteral administration Methods 0.000 claims description 2
- 239000002953 phosphate buffered saline Substances 0.000 claims description 2
- 239000008227 sterile water for injection Substances 0.000 claims description 2
- 238000010254 subcutaneous injection Methods 0.000 claims description 2
- 239000007929 subcutaneous injection Substances 0.000 claims description 2
- 239000003826 tablet Substances 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- INBGSXNNRGWLJU-ZHHJOTBYSA-N 25-hydroxycholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@@H](CCCC(C)(C)O)C)[C@@]1(C)CC2 INBGSXNNRGWLJU-ZHHJOTBYSA-N 0.000 description 7
- INBGSXNNRGWLJU-UHFFFAOYSA-N 25epsilon-Hydroxycholesterin Natural products C1C=C2CC(O)CCC2(C)C2C1C1CCC(C(CCCC(C)(C)O)C)C1(C)CC2 INBGSXNNRGWLJU-UHFFFAOYSA-N 0.000 description 4
- 238000002560 therapeutic procedure Methods 0.000 description 4
- 239000003814 drug Substances 0.000 description 3
- 102100039164 Acetyl-CoA carboxylase 1 Human genes 0.000 description 2
- 108010018763 Biotin carboxylase Proteins 0.000 description 2
- 102000015303 Fatty Acid Synthases Human genes 0.000 description 2
- 108010039731 Fatty Acid Synthases Proteins 0.000 description 2
- 102000004286 Hydroxymethylglutaryl CoA Reductases Human genes 0.000 description 2
- 108090000895 Hydroxymethylglutaryl CoA Reductases Proteins 0.000 description 2
- 108010074436 Sterol Regulatory Element Binding Protein 1 Proteins 0.000 description 2
- 102100026839 Sterol regulatory element-binding protein 1 Human genes 0.000 description 2
- VFNGKCDDZUSWLR-UHFFFAOYSA-L disulfate(2-) Chemical compound [O-]S(=O)(=O)OS([O-])(=O)=O VFNGKCDDZUSWLR-UHFFFAOYSA-L 0.000 description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate group Chemical group S(=O)(=O)([O-])[O-] QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 1
- 108090000790 Enzymes Proteins 0.000 description 1
- 229930182558 Sterol Natural products 0.000 description 1
- 108010074438 Sterol Regulatory Element Binding Protein 2 Proteins 0.000 description 1
- 102100026841 Sterol regulatory element-binding protein 2 Human genes 0.000 description 1
- 102000004896 Sulfotransferases Human genes 0.000 description 1
- 108090001033 Sulfotransferases Proteins 0.000 description 1
- PIUZYOCNZPYXOA-ZHHJOTBYSA-N [(3s,8s,9s,10r,13r,14s,17r)-17-[(2r)-6-hydroxy-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1h-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate Chemical compound C1C=C2C[C@@H](OS(O)(=O)=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@@H](CCCC(C)(C)O)C)[C@@]1(C)CC2 PIUZYOCNZPYXOA-ZHHJOTBYSA-N 0.000 description 1
- 150000001841 cholesterols Chemical class 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 230000037356 lipid metabolism Effects 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 150000003432 sterols Chemical class 0.000 description 1
- 235000003702 sterols Nutrition 0.000 description 1
- 230000019635 sulfation Effects 0.000 description 1
- 238000005670 sulfation reaction Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261623203P | 2012-04-12 | 2012-04-12 | |
| US201261623414P | 2012-04-12 | 2012-04-12 | |
| US61/623,414 | 2012-04-12 | ||
| US61/623,203 | 2012-04-12 | ||
| PCT/US2013/031861 WO2013154752A1 (en) | 2012-04-12 | 2013-03-15 | A NOVEL CHOLESTEROL METABOLITE, 5-CHOLESTEN, 3β-25-DIOL, DISULFATE (25HCDS) FOR THERAPY OF METABOLIC DISORDERS, HYPERLIPIDEMIA, DIABETES, FATTY LIVER DISEASES AND ATHEROSCLEROSIS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017074866A Division JP2017160213A (ja) | 2012-04-12 | 2017-04-05 | 代謝障害、高脂血症、糖尿病、脂肪性肝疾患及びアテローム性動脈硬化症の治療のための新規コレステロール代謝物、５−コレステン−３β，２５−ジオールジスルファート（２５ＨＣＤＳ） |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015512937A JP2015512937A (ja) | 2015-04-30 |
| JP2015512937A5 true JP2015512937A5 (https=) | 2016-12-15 |
| JP6125610B2 JP6125610B2 (ja) | 2017-05-10 |
Family
ID=49328028
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015505762A Expired - Fee Related JP6125610B2 (ja) | 2012-04-12 | 2013-03-15 | 代謝障害、高脂血症、糖尿病、脂肪性肝疾患及びアテローム性動脈硬化症の治療のための新規コレステロール代謝物、５−コレステン−３β，２５−ジオールジスルファート（２５ＨＣＤＳ） |
| JP2017074866A Pending JP2017160213A (ja) | 2012-04-12 | 2017-04-05 | 代謝障害、高脂血症、糖尿病、脂肪性肝疾患及びアテローム性動脈硬化症の治療のための新規コレステロール代謝物、５−コレステン−３β，２５−ジオールジスルファート（２５ＨＣＤＳ） |
| JP2019002297A Withdrawn JP2019089777A (ja) | 2012-04-12 | 2019-01-10 | 代謝障害、高脂血症、糖尿病、脂肪性肝疾患及びアテローム性動脈硬化症の治療のための新規コレステロール代謝物、５−コレステン−３β，２５−ジオールジスルファート（２５ＨＣＤＳ） |
| JP2021082520A Pending JP2021138713A (ja) | 2012-04-12 | 2021-05-14 | 代謝障害、高脂血症、糖尿病、脂肪性肝疾患及びアテローム性動脈硬化症の治療のための新規コレステロール代謝物、５−コレステン−３β，２５−ジオールジスルファート（２５ＨＣＤＳ） |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017074866A Pending JP2017160213A (ja) | 2012-04-12 | 2017-04-05 | 代謝障害、高脂血症、糖尿病、脂肪性肝疾患及びアテローム性動脈硬化症の治療のための新規コレステロール代謝物、５−コレステン−３β，２５−ジオールジスルファート（２５ＨＣＤＳ） |
| JP2019002297A Withdrawn JP2019089777A (ja) | 2012-04-12 | 2019-01-10 | 代謝障害、高脂血症、糖尿病、脂肪性肝疾患及びアテローム性動脈硬化症の治療のための新規コレステロール代謝物、５−コレステン−３β，２５−ジオールジスルファート（２５ＨＣＤＳ） |
| JP2021082520A Pending JP2021138713A (ja) | 2012-04-12 | 2021-05-14 | 代謝障害、高脂血症、糖尿病、脂肪性肝疾患及びアテローム性動脈硬化症の治療のための新規コレステロール代謝物、５−コレステン−３β，２５−ジオールジスルファート（２５ＨＣＤＳ） |
Country Status (20)
| Country | Link |
|---|---|
| US (6) | US20150072962A1 (https=) |
| EP (2) | EP2836502B1 (https=) |
| JP (4) | JP6125610B2 (https=) |
| KR (1) | KR102180485B1 (https=) |
| CN (2) | CN104220450B (https=) |
| AU (2) | AU2013246435B2 (https=) |
| BR (1) | BR112014025081B1 (https=) |
| CA (1) | CA2867694C (https=) |
| DK (1) | DK2836502T3 (https=) |
| EA (1) | EA026683B1 (https=) |
| ES (1) | ES2641841T3 (https=) |
| HU (1) | HUE035073T2 (https=) |
| IL (1) | IL234892B (https=) |
| IN (1) | IN2014KN02366A (https=) |
| MX (1) | MX357046B (https=) |
| PL (1) | PL2836502T3 (https=) |
| PT (1) | PT2836502T (https=) |
| SI (1) | SI2836502T1 (https=) |
| WO (1) | WO2013154752A1 (https=) |
| ZA (1) | ZA201406981B (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006047022A1 (en) | 2004-10-25 | 2006-05-04 | Virginia Commonwealth University | Nuclear sulfated oxysterol, potent regulator of cholesterol homeostasis, for therapy of hypercholesterolemia, hyperlipidemia, and atherosclerosis |
| US9034859B2 (en) | 2011-04-06 | 2015-05-19 | Virginia Commonwealth University | Sulfated oxysterol and oxysterol sulfation by hydroxysterol sulfotransferase promote lipid homeostasis and liver proliferation |
| US20150072962A1 (en) * | 2012-04-12 | 2015-03-12 | Virgini Commonwealth University | Novel cholesterol metabolite, 5-cholesten, 3beta-25-diol, disulfate (25hcds) for therapy of metabolic disorders, hyperlipidemia, diabetes, fatty livers diseases and atherosclerosis |
| HRP20220112T1 (hr) * | 2013-12-24 | 2022-04-15 | Virginia Commonwealth University | Upotreba oksidacijskog sulfata kolesterola (ocs) za liječenje akutne insuficijencije jetre |
| TWI547280B (zh) * | 2014-04-24 | 2016-09-01 | 長弘生物科技股份有限公司 | 穩定醫藥組合物 |
| US10238664B2 (en) | 2014-07-09 | 2019-03-26 | Duke University | Compositions and methods for the repair of myelin |
| EP3204013A1 (en) * | 2014-10-10 | 2017-08-16 | Virginia Commonwealth University | Oxygenated cholesterol sulfates for therapy of disorders caused by at least one of attenuated leptin activity and a lipid storage disorder |
| JP6784963B2 (ja) * | 2014-12-24 | 2020-11-18 | 国立大学法人京都大学 | ビタミンｄ３誘導体及びその薬学的用途 |
| EP3493810A4 (en) | 2016-08-02 | 2020-04-08 | Durect Corporation | COMPOSITIONS WITH OXYGENOUS CHOLESTERINSULFATE AND AT LEAST POLYALKYLENE GLYCOL, CARBOXYMETHYLCELLULOSE OR POLYOXYL GLYCERIDE |
| EP3494125B1 (en) * | 2016-08-02 | 2022-06-22 | Virginia Commonwealth University | Compositions comprising 5-cholesten-3, 25-diol, 3-sulfate (25hc3s) or pharmaceutically acceptable salt thereof and at least one cyclic oligosaccharide |
| KR20230124756A (ko) * | 2016-08-02 | 2023-08-25 | 버지니아 커먼웰스 유니버시티 | 염증성 피부 질환 및 피부 병변을 치료하기 위한 산소첨가된콜레스테롤 술페이트 (ocs) 의 용도 |
| EP4537847A3 (en) * | 2017-01-13 | 2025-07-30 | Duke University | Compositions and methods for the treatment of myelin related and inflammation related diseases or disorders |
| KR101892577B1 (ko) | 2017-04-21 | 2018-08-28 | 부산대학교 산학협력단 | 레블라스타틴 유도체 또는 이의 약학적으로 허용가능한 염을 유효성분으로 포함하는 죽상동맥경화증 예방 또는 치료용 조성물 |
| CN107286160A (zh) * | 2017-06-05 | 2017-10-24 | 毛佳婧 | 一种抗肝炎药物的哌啶并吡啶并吡唑‑锌配合物的制备方法 |
| US20200197471A1 (en) * | 2017-08-31 | 2020-06-25 | Ariel Scientific Innovations Ltd | S. spinosum extract for treating fatty liver disease |
| JP7830313B2 (ja) * | 2019-09-30 | 2026-03-16 | デュレクト コーポレーション | アルコール性肝炎の処置 |
| JP2023532286A (ja) * | 2020-06-26 | 2023-07-27 | デュレクト コーポレーション | 炎症状態を処置するための酸素化コレステロールスルフェート類の使用 |
| CN112294827B (zh) * | 2020-11-12 | 2021-12-24 | 四川大学华西医院 | 5-胆甾烯 -3β-醇硫酸酯盐的用途 |
| KR102732697B1 (ko) | 2021-10-29 | 2024-11-25 | 부산대학교 산학협력단 | 크산틴 유도체를 유효성분으로 포함하는 죽상동맥경화증 예방 또는 치료용 약학적 조성물 |
| WO2024008614A1 (en) * | 2022-07-08 | 2024-01-11 | Société des Produits Nestlé S.A. | Use of 25-hydroxycholesterol for diabetic treatment and/or prevention |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1187364C (zh) * | 1999-04-30 | 2005-02-02 | 亚其发展公司 | 类固醇衍生物 |
| WO2006047022A1 (en) * | 2004-10-25 | 2006-05-04 | Virginia Commonwealth University | Nuclear sulfated oxysterol, potent regulator of cholesterol homeostasis, for therapy of hypercholesterolemia, hyperlipidemia, and atherosclerosis |
| EP1983972A4 (en) | 2006-02-13 | 2012-01-25 | Wellstat Therapeutics Corp | COMPOUNDS FOR THE TREATMENT OF METABOLIC DISORDERS |
| WO2009002873A1 (en) | 2007-06-22 | 2008-12-31 | Cvi Pharmaceuticals Limited | Compounds, compositions and methods for reducing lipid levels |
| WO2011077245A2 (en) * | 2009-12-23 | 2011-06-30 | Fondazione Centro San Raffaele Del Monte Tabor | Compositions |
| US20150072962A1 (en) * | 2012-04-12 | 2015-03-12 | Virgini Commonwealth University | Novel cholesterol metabolite, 5-cholesten, 3beta-25-diol, disulfate (25hcds) for therapy of metabolic disorders, hyperlipidemia, diabetes, fatty livers diseases and atherosclerosis |
-
2013
- 2013-03-15 US US14/391,929 patent/US20150072962A1/en not_active Abandoned
- 2013-03-15 EP EP13775974.2A patent/EP2836502B1/en active Active
- 2013-03-15 AU AU2013246435A patent/AU2013246435B2/en not_active Ceased
- 2013-03-15 ES ES13775974.2T patent/ES2641841T3/es active Active
- 2013-03-15 MX MX2014012324A patent/MX357046B/es active IP Right Grant
- 2013-03-15 HU HUE13775974A patent/HUE035073T2/en unknown
- 2013-03-15 WO PCT/US2013/031861 patent/WO2013154752A1/en not_active Ceased
- 2013-03-15 EP EP17167122.5A patent/EP3239163A1/en not_active Withdrawn
- 2013-03-15 CN CN201380019476.3A patent/CN104220450B/zh not_active Expired - Fee Related
- 2013-03-15 CA CA2867694A patent/CA2867694C/en active Active
- 2013-03-15 PT PT137759742T patent/PT2836502T/pt unknown
- 2013-03-15 KR KR1020147031567A patent/KR102180485B1/ko not_active Expired - Fee Related
- 2013-03-15 EA EA201491859A patent/EA026683B1/ru unknown
- 2013-03-15 BR BR112014025081-2A patent/BR112014025081B1/pt not_active IP Right Cessation
- 2013-03-15 JP JP2015505762A patent/JP6125610B2/ja not_active Expired - Fee Related
- 2013-03-15 CN CN201610412359.9A patent/CN106083976B/zh not_active Expired - Fee Related
- 2013-03-15 DK DK13775974.2T patent/DK2836502T3/en active
- 2013-03-15 PL PL13775974T patent/PL2836502T3/pl unknown
- 2013-03-15 SI SI201330794T patent/SI2836502T1/sl unknown
-
2014
- 2014-09-25 ZA ZA2014/06981A patent/ZA201406981B/en unknown
- 2014-09-28 IL IL234892A patent/IL234892B/en active IP Right Grant
- 2014-10-27 IN IN2366KON2014 patent/IN2014KN02366A/en unknown
-
2016
- 2016-08-19 US US15/241,171 patent/US20160355544A1/en not_active Abandoned
-
2017
- 2017-04-05 JP JP2017074866A patent/JP2017160213A/ja active Pending
- 2017-10-10 US US15/728,827 patent/US20180127457A1/en not_active Abandoned
- 2017-11-30 AU AU2017268646A patent/AU2017268646B2/en not_active Ceased
-
2018
- 2018-09-25 US US16/140,964 patent/US20190135856A1/en not_active Abandoned
-
2019
- 2019-01-10 JP JP2019002297A patent/JP2019089777A/ja not_active Withdrawn
- 2019-10-10 US US16/599,044 patent/US20200157140A1/en not_active Abandoned
-
2020
- 2020-12-15 US US17/122,647 patent/US20210238219A1/en not_active Abandoned
-
2021
- 2021-05-14 JP JP2021082520A patent/JP2021138713A/ja active Pending
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