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

Info

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
Other languages
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

Links

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)
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
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 (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
KR100338287B1 (ko) * 1994-02-14 2002-11-30 푸르듀 파머 리미티드 감마-아미노부티르산a수용체의알로오스테리조절용안드로스탄및프레그난
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
EP3641779B1 (en) * 2017-06-23 2024-02-28 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
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
JP2021523938A (ja) 2021-09-09
WO2019211668A2 (en) 2019-11-07
US20210363173A1 (en) 2021-11-25

Similar Documents

Publication Publication Date Title
CN112823164A (zh) 神经甾体衍生物和其用途
BE1013477A3 (fr) Formulation.
KR101083696B1 (ko) 경피 흡수 제제
US20110040113A1 (en) Pure PEG-lipid conjugates
Hong et al. Advanced formulation and pharmacological activity of hydrogel of the titrated extract of C. asiatics
HUE027707T2 (en) Prodrugs of tetrahydrocannabinol, compositions comprising prodrugs of tetrahydrocannabinol, and methods for their use
CA2908571A1 (en) Compositions of pharmaceutical actives containing diethylene glycol monoethyl ether or other alkyl derivatives
WO2022160970A1 (zh) 一种不含乙醇的难溶性药物浓缩液以及由其制备的胶束溶液
WO1996003421A1 (en) Neurologically active aminosteroids
Nadeson et al. Antinociceptive properties of neurosteroids III: experiments with alphadolone given intravenously, intraperitoneally, and intragastrically
US20200188412A1 (en) Active ester derivatives of testosterone, compositions and uses thereof
ES2470367T3 (es) Preparaciones farmacéuticas para uso transd�rmico
CN101831067A (zh) 聚乙二醇脂类缀合物及其在制备药物中的应用
JPS6341887B2 (https=)
TWI903311B (zh) 局部藥物組合物、其製備方法及其在醫藥上的用途
CN118873516A (zh) 一种酮咯酸贴剂组合物、酮咯酸贴剂及其制备方法和应用
CN111035613A (zh) 一种包含氟维司群的可注射的药物组合物及其制备方法
CN101513415A (zh) 1-羟基-齐墩果烷-28-羧酸甲酯-2,12-二烯在制备治疗皮肤疾病药物中的应用
CN101513411A (zh) 齐墩果烷-28-酸-2,11,13(18)-三烯在制备治疗皮肤疾病药物中的应用
CN101756995A (zh) 11,28-二羟基-齐墩果烷-2,12-二烯在制备治疗皮肤疾病药物中的应用
EP3192515B1 (de) Pharmazeutische zusammensetzung enthaltend 7beta-hydroxycholesterol geeignet zur intravenösen verabreichung
KR100871531B1 (ko) 테스토스테론 외용제
CN101513414A (zh) 1-乙酰氧基-齐墩果烷-28-羧酸甲酯-2,12-二烯在制备治疗皮肤疾病药物中的应用
CN101513417A (zh) 1-羟基-齐墩果烷-28-酸-2,12-二烯在制备治疗皮肤疾病药物中的应用
CN101513413A (zh) 1,11,28-三羟基-齐墩果烷-2,12-二烯在制备治疗皮肤疾病药物中的应用

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20210518

WD01 Invention patent application deemed withdrawn after publication