KR101778603B1 - 3α-히드록시, 3β-메틸-5α-프레그난-20-온 (가낙솔론)의 제조 방법 - Google Patents

3α-히드록시, 3β-메틸-5α-프레그난-20-온 (가낙솔론)의 제조 방법 Download PDF

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KR101778603B1
KR101778603B1 KR1020127006429A KR20127006429A KR101778603B1 KR 101778603 B1 KR101778603 B1 KR 101778603B1 KR 1020127006429 A KR1020127006429 A KR 1020127006429A KR 20127006429 A KR20127006429 A KR 20127006429A KR 101778603 B1 KR101778603 B1 KR 101778603B1
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inert solvent
halide
methyl
methylating agent
titanium
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KR20120084715A (ko
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케네스 쇼
알랜 허치슨
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마리누스 파마슈티컬스
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    • 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

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  • 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)
KR1020127006429A 2009-08-13 2010-08-11 3α-히드록시, 3β-메틸-5α-프레그난-20-온 (가낙솔론)의 제조 방법 Active KR101778603B1 (ko)

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 (2)

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KR20120084715A KR20120084715A (ko) 2012-07-30
KR101778603B1 true KR101778603B1 (ko) 2017-09-14

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KR1020127006429A Active KR101778603B1 (ko) 2009-08-13 2010-08-11 3α-히드록시, 3β-메틸-5α-프레그난-20-온 (가낙솔론)의 제조 방법

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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)

* Cited by examiner, † Cited by third party
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)

Citations (3)

* Cited by examiner, † Cited by third party
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
US6117994A (en) 1994-06-02 2000-09-12 Hoechst Marion Roussel Intermediates for 16β-methyl steroids
WO2006010085A1 (en) 2004-07-09 2006-01-26 Roxro Pharma, Inc. Use of neurosteroids to treat neuropathic pain

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
DE69519945T2 (de) * 1994-11-23 2001-06-07 Cocensys, Inc. Androstan- und pregnanserien für die allosterische modulation des gaba-rezeptors
MX2008006888A (es) * 2005-11-28 2008-09-30 Marinus Pharmaceuticals Formulas y metodos para la manufactura y uso de la ganaxolona.

Patent Citations (3)

* Cited by examiner, † Cited by third party
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
US6117994A (en) 1994-06-02 2000-09-12 Hoechst Marion Roussel Intermediates for 16β-methyl steroids
WO2006010085A1 (en) 2004-07-09 2006-01-26 Roxro Pharma, Inc. Use of neurosteroids to treat neuropathic pain

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
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
JP5745517B2 (ja) 2015-07-08
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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