JP2005519893A5 - - Google Patents
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- Publication number
- JP2005519893A5 JP2005519893A5 JP2003559519A JP2003559519A JP2005519893A5 JP 2005519893 A5 JP2005519893 A5 JP 2005519893A5 JP 2003559519 A JP2003559519 A JP 2003559519A JP 2003559519 A JP2003559519 A JP 2003559519A JP 2005519893 A5 JP2005519893 A5 JP 2005519893A5
- Authority
- JP
- Japan
- Prior art keywords
- beta
- hydroxy
- pregnane
- 5alpha
- 3beta
- 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
Links
- 150000003431 steroids Chemical class 0.000 claims 24
- 239000000203 mixture Substances 0.000 claims 15
- AURFZBICLPNKBZ-GRWISUQFSA-N 3beta-hydroxy-5beta-pregnan-20-one Chemical compound C([C@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-GRWISUQFSA-N 0.000 claims 10
- YWYQTGBBEZQBGO-HUTKLZKUSA-N 5beta-pregnane-3beta,20alpha-diol Chemical compound C([C@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](O)C)[C@@]2(C)CC1 YWYQTGBBEZQBGO-HUTKLZKUSA-N 0.000 claims 10
- 238000000034 method Methods 0.000 claims 10
- DUHUCHOQIDJXAT-YUUPMBNKSA-N (3s,5s,8s,9s,10s,13s,14s,17s)-17-acetyl-3-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-11-one Chemical compound C([C@@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1=O DUHUCHOQIDJXAT-YUUPMBNKSA-N 0.000 claims 9
- GFHOQCXDABGYAL-POBGKJHXSA-N 3beta-Hydroxy-5alpha-pregnan-20-one acetate Chemical compound C1C[C@@H]2[C@@]3(C)CC[C@H](OC(=O)C)C[C@@H]3CC[C@H]2[C@@H]2CC[C@H](C(C)=O)[C@]21C GFHOQCXDABGYAL-POBGKJHXSA-N 0.000 claims 9
- 208000015114 central nervous system disease Diseases 0.000 claims 8
- 230000027758 ovulation cycle Effects 0.000 claims 8
- 230000000694 effects Effects 0.000 claims 7
- AURFZBICLPNKBZ-FZCSVUEKSA-N 3beta-hydroxy-5alpha-pregnan-20-one Chemical compound C([C@@H]1CC2)[C@@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-FZCSVUEKSA-N 0.000 claims 6
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 206010015037 epilepsy Diseases 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 102000004300 GABA-A Receptors Human genes 0.000 claims 4
- 108090000839 GABA-A Receptors Proteins 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 238000001990 intravenous administration Methods 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 208000019695 Migraine disease Diseases 0.000 claims 3
- 206010027940 Mood altered Diseases 0.000 claims 3
- 208000019022 Mood disease Diseases 0.000 claims 3
- 229940000406 drug candidate Drugs 0.000 claims 3
- 206010025482 malaise Diseases 0.000 claims 3
- 206010027599 migraine Diseases 0.000 claims 3
- 230000007510 mood change Effects 0.000 claims 3
- 229940127234 oral contraceptive Drugs 0.000 claims 3
- 239000003539 oral contraceptive agent Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 238000012216 screening Methods 0.000 claims 3
- CYKYBWRSLLXBOW-PFIRBALFSA-N 2-hydroxy-1-[(3s,5r,8r,9s,10s,13s,14s,17s)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-17-yl]ethanone Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CC[C@@H]21 CYKYBWRSLLXBOW-PFIRBALFSA-N 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 206010009696 Clumsiness Diseases 0.000 claims 2
- 206010056465 Food craving Diseases 0.000 claims 2
- 206010061296 Motor dysfunction Diseases 0.000 claims 2
- 206010036618 Premenstrual syndrome Diseases 0.000 claims 2
- 206010039897 Sedation Diseases 0.000 claims 2
- 230000000903 blocking effect Effects 0.000 claims 2
- 230000037396 body weight Effects 0.000 claims 2
- 230000006735 deficit Effects 0.000 claims 2
- 230000006866 deterioration Effects 0.000 claims 2
- 238000002657 hormone replacement therapy Methods 0.000 claims 2
- 230000005032 impulse control Effects 0.000 claims 2
- 206010021654 increased appetite Diseases 0.000 claims 2
- 206010027175 memory impairment Diseases 0.000 claims 2
- 230000036651 mood Effects 0.000 claims 2
- 230000036280 sedation Effects 0.000 claims 2
- 230000035945 sensitivity Effects 0.000 claims 2
- 208000019116 sleep disease Diseases 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 201000006152 substance dependence Diseases 0.000 claims 2
- 208000011117 substance-related disease Diseases 0.000 claims 2
- 208000028698 Cognitive impairment Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- 206010022998 Irritability Diseases 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- 206010029216 Nervousness Diseases 0.000 claims 1
- 206010033799 Paralysis Diseases 0.000 claims 1
- 208000027030 Premenstrual dysphoric disease Diseases 0.000 claims 1
- 208000013200 Stress disease Diseases 0.000 claims 1
- TWPQBSANBKHSLJ-FRSYEEISSA-N acetic acid 1-[(8R,9S,10S,13S,14S,17S)-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]ethanone Chemical compound C(C)(=O)O.[C@@H]12CC[C@H](C(C)=O)[C@@]1(C)CC[C@H]1[C@H]2CCC2CCCC[C@]12C TWPQBSANBKHSLJ-FRSYEEISSA-N 0.000 claims 1
- 230000001195 anabolic effect Effects 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 239000007795 chemical reaction product Substances 0.000 claims 1
- 208000010877 cognitive disease Diseases 0.000 claims 1
- 230000001419 dependent effect Effects 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000005713 exacerbation Effects 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000021090 palsy Diseases 0.000 claims 1
- 230000001953 sensory effect Effects 0.000 claims 1
- 159000000000 sodium salts Chemical class 0.000 claims 1
- 239000003270 steroid hormone Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 238000003786 synthesis reaction Methods 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0104423A SE0104423D0 (sv) | 2001-12-27 | 2001-12-27 | Pregnane steroids and their use in the treatment of CNS disorders |
| PCT/SE2002/002423 WO2003059357A1 (en) | 2001-12-27 | 2002-12-20 | Pregnane steroids for use in the treatment of cns disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009256620A Division JP5289281B2 (ja) | 2001-12-27 | 2009-11-10 | Ｃｎｓ疾患の治療において使用するためのプレグナンステロイド |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005519893A JP2005519893A (ja) | 2005-07-07 |
| JP2005519893A5 true JP2005519893A5 (https=) | 2006-01-19 |
Family
ID=20286518
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003559519A Pending JP2005519893A (ja) | 2001-12-27 | 2002-12-20 | Ｃｎｓ疾患の治療において使用するためのプレグナンステロイド |
| JP2009256620A Expired - Fee Related JP5289281B2 (ja) | 2001-12-27 | 2009-11-10 | Ｃｎｓ疾患の治療において使用するためのプレグナンステロイド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009256620A Expired - Fee Related JP5289281B2 (ja) | 2001-12-27 | 2009-11-10 | Ｃｎｓ疾患の治療において使用するためのプレグナンステロイド |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US7960367B2 (https=) |
| EP (2) | EP2275109B1 (https=) |
| JP (2) | JP2005519893A (https=) |
| CN (3) | CN101601675A (https=) |
| AU (3) | AU2002359202C1 (https=) |
| CA (1) | CA2468248C (https=) |
| DK (1) | DK1458399T3 (https=) |
| ES (1) | ES2394639T3 (https=) |
| SE (1) | SE0104423D0 (https=) |
| WO (1) | WO2003059357A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2413516C2 (ru) * | 2004-11-18 | 2011-03-10 | Умекрин Аб | Гамк-стероидные антагонисты и их применение в лечении нарушений цнс |
| CN101076340B (zh) * | 2004-11-18 | 2011-01-12 | 梅克芳股份公司 | Gaba-类固醇拮抗剂及其治疗cns障碍的用途 |
| DK2792681T3 (en) | 2006-11-21 | 2017-01-23 | Umecrine Ab | Use of Pregnancy and Androstan Steroids in the Preparation of a Pharmaceutical Composition for the Treatment of CNS Disorders. |
| US20090269795A1 (en) * | 2007-03-09 | 2009-10-29 | The Research Foundation Of State University Of New York | Mutant alpha4betadelta GABAA receptor and methods of treating anxiety or irritability |
| CN101585862B (zh) * | 2008-05-20 | 2014-12-17 | 梅克芳股份公司 | 甾族化合物 |
| RU2012133627A (ru) | 2010-01-14 | 2014-04-20 | Умекрине Муд Аб | Фармацевтическая композиция, содержащая 3-бета-гидрокси-5-альфа-прегнан-20-он, с улучшенными свойствами хранения и растворимости |
| PL2709631T3 (pl) | 2011-05-20 | 2017-07-31 | Inserm - Institut National De La Santé Et De La Recherche Médicale | Antagoniści receptora cb1 |
| ES2621528T3 (es) | 2012-11-28 | 2017-07-04 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Derivados de 3-(4-sustituido)-bencil éter de pregnenolona |
| RU2684616C2 (ru) | 2014-01-29 | 2019-04-10 | Умекрин Когнишн Аб | Стероидное соединение для применения в лечении печеночной энцефалопатии |
| JOP20200195A1 (ar) * | 2014-09-08 | 2017-06-16 | Sage Therapeutics Inc | سترويدات وتركيبات نشطة عصبياً، واستخداماتها |
| AR103384A1 (es) | 2015-01-12 | 2017-05-03 | Umecrine Cognition Ab | 3a-ETINILO, 3b-HIDROXI, 5a-PREGNAN-20-OXIMA COMO MODULADOR DE GABA |
| US10278977B2 (en) | 2016-06-06 | 2019-05-07 | Umecrine Cognition Ab | Methods for treating hypersomnolence |
| RS67063B1 (sr) * | 2017-01-09 | 2025-08-29 | Relmada Therapeutics Inc | Injektabilne suspenzije |
| WO2018147792A1 (en) | 2017-02-10 | 2018-08-16 | Asarina Pharma Ab | 3-beta-hydroxy-5-alpha-pregnan-20-one for use in medical treatment |
| WO2018147791A1 (en) | 2017-02-10 | 2018-08-16 | Asarina Pharma Ab | 3-beta-hydroxy-5-alpha-pregnan-20-one for use in treatment of essential tremor |
| JP2021519799A (ja) * | 2018-04-05 | 2021-08-12 | アサリナ ファーマ エーピーエス | 物質離脱障害を治療するためのｇａｂａ−ａアンタゴニスト |
| US11969434B1 (en) | 2022-08-29 | 2024-04-30 | Lipocine Inc. | Oral allopregnanolone compositions and methods of use |
| CA3237550A1 (en) | 2021-11-10 | 2023-05-19 | Umecrine Ab | 3.alpha.-substituted 3.beta.-hydroxy 17-oximated androstane compound for modulation of the alpha-3 subtype of the gaba-a receptor |
| US20250387409A1 (en) * | 2021-11-10 | 2025-12-25 | Umecrine Cognition Ab | 3-beta-hydroxy-3-alpha-ethyl steroids for modulation of the alpha-3 subtype of the gabaa receptor |
| WO2023083980A1 (en) | 2021-11-10 | 2023-05-19 | Umecrine Ab | Steroid as a modulator of gabaa receptor |
| US12186327B2 (en) | 2022-08-29 | 2025-01-07 | Lipocine Inc. | Oral allopregnanolone compositions and methods of use |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5232917A (en) | 1987-08-25 | 1993-08-03 | University Of Southern California | Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series |
| US5439900A (en) * | 1993-02-25 | 1995-08-08 | Bukusoglu; Cuneyt | Methods and compositions for providing analgesia and enhanced anesthesia |
| US5939545A (en) | 1994-02-14 | 1999-08-17 | Cocensys, Inc. | Method, compositions, and compounds for allosteric modulation of the gaba receptor by members of the androstane and pregnane series |
| US5767117A (en) | 1994-11-18 | 1998-06-16 | The General Hospital Corporation | Method for treating vascular headaches |
| BR9809376A (pt) * | 1997-05-02 | 2000-07-04 | American Home Prod | Pregnan-3-ol-20-onas |
| ATE246705T1 (de) | 1997-05-02 | 2003-08-15 | Wyeth Corp | Pharamezeutische anwendbare sälze von 5.alpha.- pregn-16-en-3.beta.-ol-20-on 3-sulphate ester mit gestagen aktivität und verwendbar zur behandlung von störungen des zns |
| CA2289096A1 (en) * | 1997-05-02 | 1998-11-12 | Reinhold H. W. Bender | Pharmaceutically acceptable salts of 5alpha-pregnan-3beta, 16alpha-diol-20-one 3-sulfate useful as progestins and cns disorders |
| AU756001B2 (en) * | 1998-03-11 | 2003-01-02 | Umecrine Mood Ab | Epiallopregnanolone in the treatment of CNS disorders |
| IL142441A0 (en) | 1998-10-13 | 2002-03-10 | American Home Prod | Pregnane glucuronides |
| US20020072509A1 (en) * | 2000-10-11 | 2002-06-13 | Stein Donald Gerald | Methods for the treatment of a traumatic central nervous system injury |
-
2001
- 2001-12-27 SE SE0104423A patent/SE0104423D0/xx unknown
-
2002
- 2002-12-20 CN CNA2009101459540A patent/CN101601675A/zh active Pending
- 2002-12-20 EP EP10183670.8A patent/EP2275109B1/en not_active Expired - Lifetime
- 2002-12-20 CN CNB028262751A patent/CN100518741C/zh not_active Expired - Fee Related
- 2002-12-20 EP EP02793723A patent/EP1458399B1/en not_active Expired - Lifetime
- 2002-12-20 WO PCT/SE2002/002423 patent/WO2003059357A1/en not_active Ceased
- 2002-12-20 ES ES02793723T patent/ES2394639T3/es not_active Expired - Lifetime
- 2002-12-20 AU AU2002359202A patent/AU2002359202C1/en not_active Ceased
- 2002-12-20 US US10/499,214 patent/US7960367B2/en not_active Expired - Fee Related
- 2002-12-20 CN CNA2009101459536A patent/CN101601674A/zh active Pending
- 2002-12-20 CA CA2468248A patent/CA2468248C/en not_active Expired - Fee Related
- 2002-12-20 DK DK02793723.4T patent/DK1458399T3/da active
- 2002-12-20 JP JP2003559519A patent/JP2005519893A/ja active Pending
-
2009
- 2009-05-18 AU AU2009201956A patent/AU2009201956B2/en not_active Ceased
- 2009-05-18 AU AU2009201951A patent/AU2009201951A1/en not_active Abandoned
- 2009-11-10 JP JP2009256620A patent/JP5289281B2/ja not_active Expired - Fee Related
-
2011
- 2011-01-07 US US12/986,937 patent/US8119619B2/en not_active Expired - Fee Related
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