EA201270241A1 - СПОСОБ ПОЛУЧЕНИЯ 3α-ГИДРОКСИ, 3β-МЕТИЛ-5α-ПРЕГНАН-20-ОНА (ГАНАКСОЛОНА) - Google Patents

СПОСОБ ПОЛУЧЕНИЯ 3α-ГИДРОКСИ, 3β-МЕТИЛ-5α-ПРЕГНАН-20-ОНА (ГАНАКСОЛОНА)

Info

Publication number
EA201270241A1
EA201270241A1 EA201270241A EA201270241A EA201270241A1 EA 201270241 A1 EA201270241 A1 EA 201270241A1 EA 201270241 A EA201270241 A EA 201270241A EA 201270241 A EA201270241 A EA 201270241A EA 201270241 A1 EA201270241 A1 EA 201270241A1
Authority
EA
Eurasian Patent Office
Prior art keywords
pregnan
hydroxy
methyl
hanaxolon
obtaining
Prior art date
Application number
EA201270241A
Other languages
English (en)
Other versions
EA024269B1 (ru
Inventor
Кеннес Шо
Алан Хатчисон
Original Assignee
ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "НоваМедика"
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "НоваМедика" filed Critical ОБЩЕСТВО С ОГРАНИЧЕННОЙ ОТВЕТСТВЕННОСТЬЮ "НоваМедика"
Publication of EA201270241A1 publication Critical patent/EA201270241A1/ru
Publication of EA024269B1 publication Critical patent/EA024269B1/ru

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)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Описан способ стереоселективного и региоселективного синтеза 3α-гидрокси, 3β-метил-5α-прегнан-20-она (ганаксолона), включающий реагирование 5α-прегнан-3,20-диона с органометаллическим метилирующим агентом в инертном растворителе и получение соединения формулы
EA201270241A 2009-08-13 2010-08-11 СПОСОБ ПОЛУЧЕНИЯ 3α-ГИДРОКСИ-3β-МЕТИЛ-5α-ПРЕГНАН-20-ОНА (ГАНАКСОЛОНА) EA024269B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23355309P 2009-08-13 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)

Publication Number Publication Date
EA201270241A1 true EA201270241A1 (ru) 2013-09-30
EA024269B1 EA024269B1 (ru) 2016-09-30

Family

ID=43586809

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201270241A EA024269B1 (ru) 2009-08-13 2010-08-11 СПОСОБ ПОЛУЧЕНИЯ 3α-ГИДРОКСИ-3β-МЕТИЛ-5α-ПРЕГНАН-20-ОНА (ГАНАКСОЛОНА)

Country Status (15)

Country Link
US (1) US8362286B2 (ru)
EP (1) EP2464653B1 (ru)
JP (1) JP5745517B2 (ru)
KR (1) KR101778603B1 (ru)
CN (1) CN102549007B (ru)
AU (1) AU2010282570B2 (ru)
BR (1) BR112012003085B1 (ru)
CA (1) CA2769820C (ru)
EA (1) EA024269B1 (ru)
ES (1) ES2524724T3 (ru)
HK (1) HK1171761A1 (ru)
IL (1) IL217857A (ru)
MX (1) MX2012001728A (ru)
NZ (1) NZ597940A (ru)
WO (1) WO2011019821A2 (ru)

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
CZ2015130A3 (cs) * 2015-02-25 2016-03-30 Vysoká škola chemicko - technologická v Praze (3α,5β,20S)-3-Nitrooxy-pregnan-20-karboxylová kyselina
EA036155B1 (ru) 2015-10-16 2020-10-06 Маринус Фармасьютикалс, Инк. Инъекционные составы нейростероида, содержащие наночастицы
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
EP4233861A3 (en) 2016-08-11 2023-10-11 Ovid Therapeutics, Inc. Compositions for treatment of essential tremor
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
MX2022001553A (es) 2019-08-05 2022-04-18 Marinus Pharmaceuticals Inc Ganaxolona para su uso en el tratamiento del estado epileptico.
CN114828889A (zh) 2019-12-06 2022-07-29 马瑞纳斯制药公司 用于治疗结节性硬化症的加奈索酮
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)

* 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
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.
GEP20002033B (en) * 1994-11-23 2000-04-10 Cocensys Inc Us Androstane and Pregnane Series Compounds for Allosteric Modulation of GABA Receptor
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.

Also Published As

Publication number Publication date
IL217857A0 (en) 2012-03-29
US20110040112A1 (en) 2011-02-17
CN102549007B (zh) 2015-03-18
AU2010282570A1 (en) 2012-02-23
JP5745517B2 (ja) 2015-07-08
EA024269B1 (ru) 2016-09-30
ES2524724T3 (es) 2014-12-11
WO2011019821A2 (en) 2011-02-17
KR101778603B1 (ko) 2017-09-14
HK1171761A1 (en) 2013-04-05
BR112012003085A2 (pt) 2020-12-01
KR20120084715A (ko) 2012-07-30
NZ597940A (en) 2013-03-28
CA2769820A1 (en) 2011-02-17
CN102549007A (zh) 2012-07-04
JP2013501803A (ja) 2013-01-17
EP2464653A2 (en) 2012-06-20
CA2769820C (en) 2017-06-27
US8362286B2 (en) 2013-01-29
BR112012003085B1 (pt) 2021-06-01
MX2012001728A (es) 2012-06-01
WO2011019821A3 (en) 2011-06-16
AU2010282570B2 (en) 2014-04-24
EP2464653B1 (en) 2014-10-22
IL217857A (en) 2016-03-31
EP2464653A4 (en) 2013-01-16

Similar Documents

Publication Publication Date Title
EA201270241A1 (ru) СПОСОБ ПОЛУЧЕНИЯ 3α-ГИДРОКСИ, 3β-МЕТИЛ-5α-ПРЕГНАН-20-ОНА (ГАНАКСОЛОНА)
LTPA2020512I1 (lt) Antinksčių hormoną modifikuojančio agento panaudojimas
TR201900067T4 (tr) Ketiyapinin yağ asidi konjugatları, bunların yapılmasına ve kullanılmasına yönelik proses.
DK2542685T3 (da) Fremgangsmåde til enzymatisk syntese af fedtsyre-alkylestere
DK2247577T4 (da) Fremgangsmåde til regioselektiv syntese af 1-alkyl-3-haloalkyl-pyrazol-4-carboxylsyrederivater
EP2576585B8 (en) Modified c-3 betulinic acid derivatives as hiv maturation inhibitors
NZ600119A (en) Process and intermediates for the preparation of 5-biphenyl-4-yl-2-methylpentanoic acid derivatives
MX350211B (es) Proceso para la preparacion del etil-ester del acido n- (4-ciclohexil-3-trifluoro-metil-benciloxi) -acetimidico.
TR201903978T4 (tr) L-ornitin fenil asetat yapım yöntemleri.
EP2313841A4 (en) GRAPHIC MODELS FOR THE ANALYSIS OF ASSOCIATIONS AT THE GENOME SCALE
MX343653B (es) Síntesis de clorhidrato de metilfenidato a baja temperatura.
EA201101147A1 (ru) Новый способ синтеза ивабрадина и его солей присоединения с фармацевтически приемлемой кислотой
EP2499151A4 (en) MAMMALIAN STEROID METABOLITES
UA119435C2 (uk) Об'єднаний спосіб одержання метанолу і метилацетату
HK1124842A1 (en) Methods of preparing imidazole-based compounds
EA201200498A1 (ru) Новый способ синтеза ивабрадина и его фармацевтически приемлемых кислотно-аддитивных солей
EA201290165A1 (ru) Способ получения производного фенилаланина
AU2013269340A8 (en) Method of synthesising sulforaphane
MX337997B (es) Nuevo procedimiento de sintesis de la ivabradina y de sus sales de adicion a un acido farmaceuticamente aceptable.
ME00929B (me) NOVI POSTUPAK ZA DOBlJANJE KRISTALNOG OBLIKA V AGOMELATIN A
EA201000397A1 (ru) Новый способ синтеза ивабрадина и его солей присоединения с фармацевтически приемлемой кислотой
AR077332A1 (es) Procesos para la alquilacion de pirazoles
MX342390B (es) Proceso para preparar 3-haloalquilpirazoles.
HK1169349A1 (en) Process for producing an ethyl acetate solvent and co-production of ethanol
EA201190203A1 (ru) Способ получения сложного эфира бифенил-2-илкарбаминовой кислоты

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): MD

NF4A Restoration of lapsed right to a eurasian patent

Designated state(s): MD