CN112823164A - 神经甾体衍生物和其用途 - Google Patents

神经甾体衍生物和其用途 Download PDF

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Publication number
CN112823164A
CN112823164A CN201980033110.9A CN201980033110A CN112823164A CN 112823164 A CN112823164 A CN 112823164A CN 201980033110 A CN201980033110 A CN 201980033110A CN 112823164 A CN112823164 A CN 112823164A
Authority
CN
China
Prior art keywords
pharmaceutical composition
ganaxolone
mixture
subject
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
Application number
CN201980033110.9A
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English (en)
Chinese (zh)
Inventor
N·布莱森
A·C·莎尔玛
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Akeros Pharmaceutical Co
Original Assignee
Akeros Pharmaceutical Co
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 Akeros Pharmaceutical Co filed Critical Akeros Pharmaceutical Co
Publication of CN112823164A publication Critical patent/CN112823164A/zh
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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (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)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Otolaryngology (AREA)
  • Dispersion Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
CN201980033110.9A 2018-05-04 2019-05-03 神经甾体衍生物和其用途 Pending CN112823164A (zh)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
CN112823164A true CN112823164A (zh) 2021-05-18

Family

ID=68384780

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980033110.9A Pending CN112823164A (zh) 2018-05-04 2019-05-03 神经甾体衍生物和其用途

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
EP2806877B2 (en) 2012-01-23 2025-01-29 Sage Therapeutics, Inc. Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin
CA2882708A1 (en) 2012-08-21 2014-02-27 Sage Therapeutics, Inc. Methods of treating epilepsy or status epilepticus
KR102396328B1 (ko) 2013-04-17 2022-05-10 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
US20160068563A1 (en) 2013-04-17 2016-03-10 Boyd L. Harrison 19-nor neuroactive steroids and methods of use thereof
AU2014308621C1 (en) 2013-08-23 2022-01-06 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
US10246482B2 (en) 2014-06-18 2019-04-02 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
CN117024501A (zh) 2014-10-16 2023-11-10 萨奇治疗股份有限公司 靶向cns障碍的组合物和方法
ME03809B (me) 2014-10-16 2021-04-20 Sage Therapeutics Inc KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a
RS61530B1 (sr) 2015-01-26 2021-04-29 Sage Therapeutics Inc Kompozicije i postupci za lečenje poremećaja cns
KR20240157128A (ko) 2016-03-08 2024-10-31 세이지 테라퓨틱스, 인크. 신경활성 스테로이드, 조성물, 및 그의 용도
WO2018013615A1 (en) 2016-07-11 2018-01-18 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
SG11202112391UA (en) 2019-05-31 2021-12-30 Sage Therapeutics Inc Neuroactive steroids and compositions thereof
IL295362A (en) * 2020-02-05 2022-10-01 Puretech Lyt Inc Lipid drug inhibitors of neurosteroids
IL295902A (en) * 2020-02-27 2022-10-01 Brii Biosciences Inc Drug inhibitors of neuroactive steroids
EP4493574A1 (en) * 2022-03-18 2025-01-22 Marinus Pharmaceuticals, Inc. Prodrugs of ganaxolone

Citations (6)

* 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
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
WO2015081170A2 (en) * 2013-11-26 2015-06-04 Systamedic Inc. Ganaxolone derivatives for treatment of central nervous systems disorders
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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2296594T3 (es) * 1994-02-14 2008-05-01 Euro-Celtique S.A. Androstanos y pregnanos para la modulacion alosterica del receptor de gaba.
FR2973031B1 (fr) * 2011-03-23 2013-11-29 Univ Strasbourg Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique
CA3068462A1 (en) * 2017-06-23 2019-12-27 The Board Of Trustees Of The University Of Illinois Treatment of neuropsychiatric disorders with neurosteroids and analogues thereof

Patent Citations (6)

* 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
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
WO2015081170A2 (en) * 2013-11-26 2015-06-04 Systamedic Inc. Ganaxolone derivatives for treatment of central nervous systems disorders
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

Also Published As

Publication number Publication date
EP3788055A2 (en) 2021-03-10
JP2021523938A (ja) 2021-09-09
UY38213A (es) 2019-10-31
WO2019211668A3 (en) 2019-12-12
TW202014192A (zh) 2020-04-16
CA3099089A1 (en) 2019-11-07
AR116659A1 (es) 2021-06-02
WO2019211668A2 (en) 2019-11-07
AU2019264032A1 (en) 2020-12-03
US20190337975A1 (en) 2019-11-07
EP3788055A4 (en) 2022-03-30
PY1934080A (es) 2019-11-08
US20210363173A1 (en) 2021-11-25

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WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20210518

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