JP2021523938A - 神経ステロイド誘導体およびその使用 - Google Patents

神経ステロイド誘導体およびその使用 Download PDF

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Publication number
JP2021523938A
JP2021523938A JP2021510564A JP2021510564A JP2021523938A JP 2021523938 A JP2021523938 A JP 2021523938A JP 2021510564 A JP2021510564 A JP 2021510564A JP 2021510564 A JP2021510564 A JP 2021510564A JP 2021523938 A JP2021523938 A JP 2021523938A
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JP
Japan
Prior art keywords
pharmaceutical composition
composition according
mixture
ganaxolone
pharmaceutically acceptable
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
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JP2021510564A
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English (en)
Japanese (ja)
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JP2021523938A5 (https=
JPWO2019211668A5 (https=
Inventor
ブライソン，ナーサン
シャーマ，アヴィナッシュ，チャンダー
Original Assignee
アセラス ファーマシュウティカルズ コーポレーション
アセラス ファーマシュウティカルズ コーポレーション
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Publication of JP2021523938A publication Critical patent/JP2021523938A/ja
Publication of JP2021523938A5 publication Critical patent/JP2021523938A5/ja
Publication of JPWO2019211668A5 publication Critical patent/JPWO2019211668A5/ja
Pending legal-status Critical Current

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Classifications

    • 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
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/009—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by only one oxygen atom doubly bound
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • 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
    • A61K31/658—Medicinal preparations containing organic active ingredients o-phenolic cannabinoids, e.g. cannabidiol, cannabigerolic acid, cannabichromene or tetrahydrocannabinol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0043—Nose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • 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
    • A61P25/24—Antidepressants
    • 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
    • C07J5/0007—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 not substituted in position 17 alfa
    • C07J5/0015—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 not substituted in position 17 alfa not substituted in position 16

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (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)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Dispersion Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Inorganic Chemistry (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2021510564A 2018-05-04 2019-05-03 神経ステロイド誘導体およびその使用 Pending JP2021523938A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862667100P 2018-05-04 2018-05-04
US62/667,100 2018-05-04
US16/403,100 2019-05-03
US16/403,100 US20190337975A1 (en) 2018-05-04 2019-05-03 Neurosteroid derivatives and uses thereof
PCT/IB2019/000517 WO2019211668A2 (en) 2018-05-04 2019-05-03 Neurosteroid derivatives and uses thereof

Publications (3)

Publication Number Publication Date
JP2021523938A true JP2021523938A (ja) 2021-09-09
JP2021523938A5 JP2021523938A5 (https=) 2022-05-02
JPWO2019211668A5 JPWO2019211668A5 (https=) 2022-05-02

Family

ID=68384780

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021510564A Pending JP2021523938A (ja) 2018-05-04 2019-05-03 神経ステロイド誘導体およびその使用

Country Status (11)

Country Link
US (2) US20190337975A1 (https=)
EP (1) EP3788055A4 (https=)
JP (1) JP2021523938A (https=)
CN (1) CN112823164A (https=)
AR (1) AR116659A1 (https=)
AU (1) AU2019264032A1 (https=)
CA (1) CA3099089A1 (https=)
PY (1) PY1934080A (https=)
TW (1) TW202014192A (https=)
UY (1) UY38213A (https=)
WO (1) WO2019211668A2 (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201606063RA (en) 2012-01-23 2016-09-29 Sage Therapeutics Inc Neuroactive steroid formulations and methods of treating cns disorders
MX2015002252A (es) 2012-08-21 2015-07-21 Sage Therapeutics Inc Metodos para tratar epilepsia o estado de epilepsia.
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
JP6470258B2 (ja) 2013-04-17 2019-02-13 セージ セラピューティクス， インコーポレイテッド １９−ノルｃ３，３−ジ置換ｃ２１−ｎ−ピラゾリルステロイドおよびその使用方法
ES2848823T3 (es) 2013-08-23 2021-08-12 Sage Therapeutics Inc Esteroides neuroactivos, composiciones y usos de los mismos
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
US10577390B2 (en) 2014-10-16 2020-03-03 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
ME03809B (me) 2014-10-16 2021-04-20 Sage Therapeutics Inc KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a
WO2016123056A1 (en) 2015-01-26 2016-08-04 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
HK1258616A1 (zh) 2016-03-08 2019-11-15 Sage Therapeutics, Inc. 神经活性类固醇、组合物、及其用途
US20190233465A1 (en) 2016-07-11 2019-08-01 Sage Therapeutics, Inc. C7, c12, and c16 substituted neuroactive steroids and their methods of use
MA45599A (fr) 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
CR20240234A (es) 2019-05-31 2024-07-09 Sage Therapeutics Inc ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629)
CN115348864A (zh) * 2020-02-05 2022-11-15 纯技术Lyt股份有限公司 神经甾体的脂质前药
MX2022010620A (es) * 2020-02-27 2022-11-30 Brii Biosciences Inc Profarmacos de esteroides neuroactivos.
IL315509A (en) * 2022-03-18 2024-11-01 Marinus Pharmaceuticals Inc Genaxolone medication matrims

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB748846A (en) * 1953-10-28 1956-05-09 Vitamins Ltd A process for the manufacture of pregnan-3(-a)-ol-20-one and derivatives thereof
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
WO1995021617A1 (en) * 1994-02-14 1995-08-17 Cocensys, Inc. Androstanes and pregnanes for allosteric modulation of gaba receptor
US20060009432A1 (en) * 2004-07-09 2006-01-12 Roger Whiting Use of neurosteroids to treat neuropathic pain
WO2012127176A1 (fr) * 2011-03-23 2012-09-27 Université De Strasbourg Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique
US20130245253A1 (en) * 2010-03-26 2013-09-19 Department Of Veterans Affairs Conjugated Neuroactive Steroid Compositions And Methods Of Use
WO2015081170A2 (en) * 2013-11-26 2015-06-04 Systamedic Inc. Ganaxolone derivatives for treatment of central nervous systems disorders
WO2018237282A1 (en) * 2017-06-23 2018-12-27 The Board Of Trustees Of The University Of Illinois Treatment of neuropsychiatric disorders with neurosteroids and analogues thereof
CN109666055A (zh) * 2017-10-16 2019-04-23 张家口华健致远生物科技有限公司 调节中枢神经治疗抑郁症的化合物及其用途

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB748846A (en) * 1953-10-28 1956-05-09 Vitamins Ltd A process for the manufacture of pregnan-3(-a)-ol-20-one and derivatives thereof
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
WO1995021617A1 (en) * 1994-02-14 1995-08-17 Cocensys, Inc. Androstanes and pregnanes for allosteric modulation of gaba receptor
US20060009432A1 (en) * 2004-07-09 2006-01-12 Roger Whiting Use of neurosteroids to treat neuropathic pain
US20130245253A1 (en) * 2010-03-26 2013-09-19 Department Of Veterans Affairs Conjugated Neuroactive Steroid Compositions And Methods Of Use
WO2012127176A1 (fr) * 2011-03-23 2012-09-27 Université De Strasbourg Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique
WO2015081170A2 (en) * 2013-11-26 2015-06-04 Systamedic Inc. Ganaxolone derivatives for treatment of central nervous systems disorders
WO2018237282A1 (en) * 2017-06-23 2018-12-27 The Board Of Trustees Of The University Of Illinois Treatment of neuropsychiatric disorders with neurosteroids and analogues thereof
CN109666055A (zh) * 2017-10-16 2019-04-23 张家口华健致远生物科技有限公司 调节中枢神经治疗抑郁症的化合物及其用途

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
J. CHEM. SOC., vol. 4, JPN6023014089, 1954, pages 1302 - 1306, ISSN: 0005032208 *

Also Published As

Publication number Publication date
WO2019211668A3 (en) 2019-12-12
TW202014192A (zh) 2020-04-16
EP3788055A2 (en) 2021-03-10
UY38213A (es) 2019-10-31
CA3099089A1 (en) 2019-11-07
AR116659A1 (es) 2021-06-02
PY1934080A (es) 2019-11-08
AU2019264032A1 (en) 2020-12-03
EP3788055A4 (en) 2022-03-30
US20190337975A1 (en) 2019-11-07
CN112823164A (zh) 2021-05-18
WO2019211668A2 (en) 2019-11-07
US20210363173A1 (en) 2021-11-25

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