JP5745517B2 - ３α−ヒドロキシ−３β−メチル−５α−プレグナン−２０−オン（ガナキソロン）の製造法 - Google Patents
３α−ヒドロキシ−３β−メチル−５α−プレグナン−２０−オン（ガナキソロン）の製造法 Download PDFInfo
- Publication number
- JP5745517B2 JP5745517B2 JP2012524841A JP2012524841A JP5745517B2 JP 5745517 B2 JP5745517 B2 JP 5745517B2 JP 2012524841 A JP2012524841 A JP 2012524841A JP 2012524841 A JP2012524841 A JP 2012524841A JP 5745517 B2 JP5745517 B2 JP 5745517B2
- Authority
- JP
- Japan
- Prior art keywords
- ganaxolone
- halide
- methyl
- organometallic
- methylating agent
- 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.)
- Active
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
- C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
- C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
- C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
- C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
- C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
- C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
- C07J7/004—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
- C07J7/0045—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US23355309P | 2009-08-13 | 2009-08-13 | |
| US61/233,553 | 2009-08-13 | ||
| PCT/US2010/045176 WO2011019821A2 (en) | 2009-08-13 | 2010-08-11 | METHOD FOR MAKING 3α-HYDROXY, 3β- METHYL-5α-PREGNAN-20-ONE (GANAXOLONE) |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013501803A JP2013501803A (ja) | 2013-01-17 |
| JP2013501803A5 JP2013501803A5 (enExample) | 2013-09-26 |
| JP5745517B2 true JP5745517B2 (ja) | 2015-07-08 |
Family
ID=43586809
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012524841A Active JP5745517B2 (ja) | 2009-08-13 | 2010-08-11 | ３α−ヒドロキシ−３β−メチル−５α−プレグナン−２０−オン（ガナキソロン）の製造法 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8362286B2 (enExample) |
| EP (1) | EP2464653B1 (enExample) |
| JP (1) | JP5745517B2 (enExample) |
| KR (1) | KR101778603B1 (enExample) |
| CN (1) | CN102549007B (enExample) |
| AU (1) | AU2010282570B2 (enExample) |
| BR (1) | BR112012003085B1 (enExample) |
| CA (1) | CA2769820C (enExample) |
| EA (1) | EA024269B1 (enExample) |
| ES (1) | ES2524724T3 (enExample) |
| IL (1) | IL217857A (enExample) |
| MX (1) | MX2012001728A (enExample) |
| NZ (1) | NZ597940A (enExample) |
| WO (1) | WO2011019821A2 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2008006888A (es) | 2005-11-28 | 2008-09-30 | Marinus Pharmaceuticals | Formulas y metodos para la manufactura y uso de la ganaxolona. |
| US9629853B2 (en) | 2014-05-21 | 2017-04-25 | Wisconsin Alumni Research Foundation | Uses of ganaxolone |
| CZ305837B6 (cs) * | 2015-02-25 | 2016-03-30 | Vysoká škola chemicko - technologická v Praze | (3α,5β,20S)-3-Nitrooxy-pregnan-20-karboxylová kyselina |
| US10780099B2 (en) * | 2015-10-16 | 2020-09-22 | Marinus Pharmaceuticals, Inc. | Injectable neurosteroid formulations containing nanoparticles |
| CN106279326A (zh) * | 2016-08-09 | 2017-01-04 | 南京臣功制药股份有限公司 | 一种醋酸甲羟孕酮胶囊的有关物质及其分析检测方法 |
| CN106366149B (zh) * | 2016-08-09 | 2018-01-23 | 南京臣功制药股份有限公司 | 一种醋酸甲羟孕酮分散片的有关物质及其分析检测方法 |
| JP2019524816A (ja) | 2016-08-11 | 2019-09-05 | オービッド・セラピューティクス・インコーポレイテッドＯｖｉｄ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | てんかん性障害の処置のための方法および組成物 |
| US10391105B2 (en) | 2016-09-09 | 2019-08-27 | Marinus Pharmaceuticals Inc. | Methods of treating certain depressive disorders and delirium tremens |
| IT201800009683A1 (it) * | 2018-10-22 | 2020-04-22 | Ind Chimica Srl | Processo per la preparazione di 3α-idrossi-5α-pregnan-20-one (brexanolone) |
| US11266662B2 (en) | 2018-12-07 | 2022-03-08 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in prophylaxis and treatment of postpartum depression |
| WO2021026124A1 (en) | 2019-08-05 | 2021-02-11 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in treatment of status epilepticus |
| CA3158280A1 (en) | 2019-12-06 | 2021-06-10 | Alex Aimetti | Ganaxolone for use in treating tuberous sclerosis complex |
| IT202000021316A1 (it) | 2020-09-09 | 2022-03-09 | Ind Chimica Srl | PROCESSO PER LA PREPARAZIONE DI (3α,5α)-3-IDROSSI-3-METIL-PREGNAN-20-ONE (GANAXOLONE) |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3953429A (en) | 1970-12-17 | 1976-04-27 | Glaxo Laboratories Limited | Anaesthetic steroids of the androstance and pregnane series |
| US5319115A (en) | 1987-08-25 | 1994-06-07 | Cocensys Inc. | Method for making 3α-hydroxy, 3β-substituted-pregnanes |
| 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 |
| AU698834B2 (en) * | 1993-05-24 | 1998-11-12 | Purdue Pharma Ltd. | Methods and compositions for inducing sleep |
| FR2720747B1 (fr) * | 1994-06-02 | 1996-07-12 | Roussel Uclaf | Nouveau procédé de préparation d'un stéroïde 16béta-méthyl et nouveaux intermédiaires. |
| DE69519945T2 (de) * | 1994-11-23 | 2001-06-07 | Cocensys, Inc. | Androstan- und pregnanserien für die allosterische modulation des gaba-rezeptors |
| WO2006010085A1 (en) * | 2004-07-09 | 2006-01-26 | Roxro Pharma, Inc. | Use of neurosteroids to treat neuropathic pain |
| MX2008006888A (es) * | 2005-11-28 | 2008-09-30 | Marinus Pharmaceuticals | Formulas y metodos para la manufactura y uso de la ganaxolona. |
-
2010
- 2010-08-11 CN CN201080035660.3A patent/CN102549007B/zh active Active
- 2010-08-11 EP EP10808696.8A patent/EP2464653B1/en active Active
- 2010-08-11 CA CA2769820A patent/CA2769820C/en active Active
- 2010-08-11 EA EA201270241A patent/EA024269B1/ru active IP Right Revival
- 2010-08-11 MX MX2012001728A patent/MX2012001728A/es active IP Right Grant
- 2010-08-11 WO PCT/US2010/045176 patent/WO2011019821A2/en not_active Ceased
- 2010-08-11 NZ NZ597940A patent/NZ597940A/xx unknown
- 2010-08-11 JP JP2012524841A patent/JP5745517B2/ja active Active
- 2010-08-11 AU AU2010282570A patent/AU2010282570B2/en active Active
- 2010-08-11 BR BR112012003085-0A patent/BR112012003085B1/pt active IP Right Grant
- 2010-08-11 ES ES10808696.8T patent/ES2524724T3/es active Active
- 2010-08-11 US US12/854,226 patent/US8362286B2/en active Active
- 2010-08-11 KR KR1020127006429A patent/KR101778603B1/ko active Active
-
2012
- 2012-01-31 IL IL217857A patent/IL217857A/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| CA2769820A1 (en) | 2011-02-17 |
| EP2464653A2 (en) | 2012-06-20 |
| CN102549007B (zh) | 2015-03-18 |
| HK1171761A1 (en) | 2013-04-05 |
| KR101778603B1 (ko) | 2017-09-14 |
| AU2010282570A1 (en) | 2012-02-23 |
| US20110040112A1 (en) | 2011-02-17 |
| WO2011019821A3 (en) | 2011-06-16 |
| MX2012001728A (es) | 2012-06-01 |
| IL217857A0 (en) | 2012-03-29 |
| JP2013501803A (ja) | 2013-01-17 |
| AU2010282570B2 (en) | 2014-04-24 |
| BR112012003085A2 (pt) | 2020-12-01 |
| BR112012003085B1 (pt) | 2021-06-01 |
| US8362286B2 (en) | 2013-01-29 |
| KR20120084715A (ko) | 2012-07-30 |
| ES2524724T3 (es) | 2014-12-11 |
| CA2769820C (en) | 2017-06-27 |
| EA201270241A1 (ru) | 2013-09-30 |
| EA024269B1 (ru) | 2016-09-30 |
| EP2464653B1 (en) | 2014-10-22 |
| WO2011019821A2 (en) | 2011-02-17 |
| NZ597940A (en) | 2013-03-28 |
| EP2464653A4 (en) | 2013-01-16 |
| CN102549007A (zh) | 2012-07-04 |
| IL217857A (en) | 2016-03-31 |
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