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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- JP
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- Prior art keywords
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- treatment
- pharmaceutical composition
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- subject
- 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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- 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 | |
| US61/623,203 | 2012-04-12 | ||
| US61/623,414 | 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) | EP3239163A1 (https=) |
| JP (4) | JP6125610B2 (https=) |
| KR (1) | KR102180485B1 (https=) |
| CN (2) | CN106083976B (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 |
| EA026683B1 (ru) * | 2012-04-12 | 2017-05-31 | Вирджиния Коммонвелт Юниверсити | МЕТАБОЛИТ ХОЛЕСТЕРИНА ДИСУЛЬФАТ 5-ХОЛЕСТЕН-3β,25-ДИОЛА (25HCDS) ДЛЯ ТЕРАПИИ НАРУШЕНИЙ ОБМЕНА ВЕЩЕСТВ, ГИПЕРЛИПИДЕМИИ, ДИАБЕТА, ЖИРОВЫХ БОЛЕЗНЕЙ ПЕЧЕНИ И АТЕРОСКЛЕРОЗА |
| PL3639828T3 (pl) * | 2013-12-24 | 2022-05-02 | Virginia Commonwealth University | Zastosowanie utlenowanych siarczanów cholesterolu (ocs) w leczeniu ostrej niewydolności wątroby |
| 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 |
| CN107106576A (zh) * | 2014-10-10 | 2017-08-29 | 弗吉尼亚联邦大学 | 用于因减弱的瘦蛋白活性和脂质贮积障碍中的至少一种导致的障碍的疗法的氧化胆固醇硫酸酯类 |
| 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 |
| US20200222430A1 (en) * | 2016-08-02 | 2020-07-16 | Durect Corporation | Compositions comprising oxygenated cholesterol sulfate and at least one of polyalkylene glycol, carboxymethyl cellulose and polyoxylglyceride |
| 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 |
| CA3031211A1 (en) * | 2016-08-02 | 2018-02-08 | Virginia Commonwealth University | Use of oxygenated cholesterol sulfates (ocs) to treat inflammatory skin disease and skin lesions |
| US11458146B2 (en) | 2017-01-13 | 2022-10-04 | 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 |
| RU2020110253A (ru) * | 2017-08-31 | 2021-09-30 | Ариэль Сайентифик Инновейшнз Лтд | Экстракт s. spinosum для лечения жировой болезни печени |
| BR112022005039A2 (pt) * | 2019-09-30 | 2022-06-21 | Durect Corp | Tratamento de hepatite alcoólica |
| EP4171573A4 (en) * | 2020-06-26 | 2025-04-09 | Durect Corporation | USE OF OXYGENATED CHOLESTEROL SULFATES FOR THE TREATMENT OF NEUROLOGICAL CONDITIONS, NEURODEGENERATIVE DISEASES AND ADDICTION |
| 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 |
|---|---|---|---|---|
| IL146223A0 (en) * | 1999-04-30 | 2002-07-25 | Arch Dev Corp | Steroid derivatives |
| 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 |
| CA2637884A1 (en) | 2006-02-13 | 2007-08-23 | Wellstat Therapeutics Corporation | Compounds for the treatment of metabolic disorders |
| US8003795B2 (en) | 2007-06-22 | 2011-08-23 | Cvi Pharmaceuticals Limited | Compounds and compositions for reducing lipid levels |
| WO2011077245A2 (en) * | 2009-12-23 | 2011-06-30 | Fondazione Centro San Raffaele Del Monte Tabor | Compositions |
| EA026683B1 (ru) * | 2012-04-12 | 2017-05-31 | Вирджиния Коммонвелт Юниверсити | МЕТАБОЛИТ ХОЛЕСТЕРИНА ДИСУЛЬФАТ 5-ХОЛЕСТЕН-3β,25-ДИОЛА (25HCDS) ДЛЯ ТЕРАПИИ НАРУШЕНИЙ ОБМЕНА ВЕЩЕСТВ, ГИПЕРЛИПИДЕМИИ, ДИАБЕТА, ЖИРОВЫХ БОЛЕЗНЕЙ ПЕЧЕНИ И АТЕРОСКЛЕРОЗА |
-
2013
- 2013-03-15 EA EA201491859A patent/EA026683B1/ru unknown
- 2013-03-15 MX MX2014012324A patent/MX357046B/es active IP Right Grant
- 2013-03-15 CN CN201610412359.9A patent/CN106083976B/zh not_active Expired - Fee Related
- 2013-03-15 PL PL13775974T patent/PL2836502T3/pl unknown
- 2013-03-15 SI SI201330794T patent/SI2836502T1/sl unknown
- 2013-03-15 PT PT137759742T patent/PT2836502T/pt unknown
- 2013-03-15 BR BR112014025081-2A patent/BR112014025081B1/pt not_active IP Right Cessation
- 2013-03-15 HU HUE13775974A patent/HUE035073T2/en unknown
- 2013-03-15 KR KR1020147031567A patent/KR102180485B1/ko not_active Expired - Fee Related
- 2013-03-15 EP EP17167122.5A patent/EP3239163A1/en not_active Withdrawn
- 2013-03-15 DK DK13775974.2T patent/DK2836502T3/en active
- 2013-03-15 JP JP2015505762A patent/JP6125610B2/ja not_active Expired - Fee Related
- 2013-03-15 CA CA2867694A patent/CA2867694C/en active Active
- 2013-03-15 AU AU2013246435A patent/AU2013246435B2/en not_active Ceased
- 2013-03-15 US US14/391,929 patent/US20150072962A1/en not_active Abandoned
- 2013-03-15 CN CN201380019476.3A patent/CN104220450B/zh not_active Expired - Fee Related
- 2013-03-15 WO PCT/US2013/031861 patent/WO2013154752A1/en not_active Ceased
- 2013-03-15 ES ES13775974.2T patent/ES2641841T3/es active Active
- 2013-03-15 EP EP13775974.2A patent/EP2836502B1/en active Active
-
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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