NZ739760A - Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same - Google Patents

Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

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Publication number
NZ739760A
NZ739760A NZ739760A NZ73976013A NZ739760A NZ 739760 A NZ739760 A NZ 739760A NZ 739760 A NZ739760 A NZ 739760A NZ 73976013 A NZ73976013 A NZ 73976013A NZ 739760 A NZ739760 A NZ 739760A
Authority
NZ
New Zealand
Prior art keywords
neuroactive
alkoxy
prodrugs
treatment
methods
Prior art date
Application number
NZ739760A
Other languages
English (en)
Inventor
Douglas Covey
Albert Robichaud
Original Assignee
Univ Washington
Sage Therapeutics Inc
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 Univ Washington, Sage Therapeutics Inc filed Critical Univ Washington
Publication of NZ739760A publication Critical patent/NZ739760A/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • 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
    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/566—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
    • 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
    • A61K31/57—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
    • A61K31/573—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 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0029—Ethers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/006—Ketals at position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/008—Ketals at position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0016—Oximes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • 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
    • 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
    • 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
    • C07J9/005—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 containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton

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  • 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Addiction (AREA)
  • Toxicology (AREA)
  • Pulmonology (AREA)
  • Psychology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
NZ739760A 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same NZ739760A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261738822P 2012-12-18 2012-12-18
NZ709211A NZ709211A (en) 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

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NZ739760A true NZ739760A (en) 2020-05-29

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NZ739760A NZ739760A (en) 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
NZ709211A NZ709211A (en) 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

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Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101583620B (zh) 2005-11-28 2016-08-17 马里纳斯医药公司 加奈索酮组合物及其制备和使用方法
US20150158903A1 (en) 2011-09-08 2015-06-11 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
ES2738526T3 (es) 2011-10-14 2020-01-23 Sage Therapeutics Inc Compuestos 19-norpregnano 3,3-disustituidos, composiciones y usos de los mismos
WO2013112605A2 (en) 2012-01-23 2013-08-01 Sage Therapeutics, Inc. Neuroactive steroid formulations and methods of treating cns disorders
IL275725B (en) 2012-08-21 2022-08-01 Sage Therapeutics Inc Treatment methods for epilepsy and status epilepticus
BR112015014397B1 (pt) 2012-12-18 2021-02-02 Washington University composto, composição farmacêutica e uso de um composto
LT2968369T (lt) 2013-03-13 2018-12-27 Sage Therapeutics, Inc. Neuroaktyvūs steroidai ir jų panaudojimo būdai
WO2014169831A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof
HRP20200995T1 (hr) 2013-04-17 2020-11-27 Sage Therapeutics, Inc. 19-nor neuroaktivni steroidi za metode liječenja
HRP20190232T1 (hr) 2013-04-17 2019-03-22 Sage Therapeutics, Inc. 19-nor c3,3-disupstituirani c21-n-pirazolil steroidi i postupci za njihovu upotrebu
US20160068563A1 (en) 2013-04-17 2016-03-10 Boyd L. Harrison 19-nor neuroactive steroids and methods of use thereof
SMT202100229T1 (it) * 2013-07-19 2021-05-07 Sage Therapeutics Inc Steroidi neuroattivi, composizioni e loro usi
SMT202100048T1 (it) 2013-08-23 2021-03-15 Sage Therapeutics Inc Steroidi neuroattivi, composizioni e loro usi
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
ES2970222T3 (es) 2014-06-18 2024-05-27 Sage Therapeutics Inc Oxiesteroles y procedimientos de uso de los mismos
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
AU2015331749A1 (en) 2014-10-16 2017-05-04 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
JP6742308B2 (ja) 2014-10-16 2020-08-19 セージ セラピューティクス， インコーポレイテッド Ｃｎｓ障害を処置するための組成物および方法
ES2793237T3 (es) 2014-11-27 2020-11-13 Sage Therapeutics Inc Composiciones y métodos para el tratamiento de trastornos del SNC
SI3250210T1 (sl) * 2015-01-26 2021-07-30 Sage Therapeutics, Inc. Sestavki in metode za zdravljenje CNS motenj
US10329320B2 (en) 2015-02-20 2019-06-25 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
AR105044A1 (es) 2015-06-18 2017-08-30 Sage Therapeutics Inc Soluciones de esteroides neuroactivos y sus métodos de uso, recipiente
MA42409A (fr) 2015-07-06 2018-05-16 Sage Therapeutics Inc Oxystérols et leurs procédés d'utilisation
MX376833B (es) 2015-07-06 2025-03-07 Sage Therapeutics Inc Oxiesteroles y metodos de uso de los mismos.
RS62220B1 (sr) 2015-07-06 2021-09-30 Sage Therapeutics Inc Oksisteroli i postupci njihovog korišćenja
EP3362042A1 (en) 2015-10-16 2018-08-22 Marinus Pharmaceuticals, Inc. Injectable neurosteroid formulations containing nanoparticles
US20200306262A1 (en) * 2015-11-20 2020-10-01 Sage Therapeutics, Inc. Compounds and methods of their use
SG11201807785VA (en) 2016-03-08 2018-10-30 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof
CN114272249A (zh) 2016-04-01 2022-04-05 萨奇治疗股份有限公司 氧甾醇及其使用方法
US10752653B2 (en) 2016-05-06 2020-08-25 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
AU2017292870B2 (en) 2016-07-07 2021-10-07 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
CN109689673B (zh) 2016-07-11 2023-03-14 萨奇治疗股份有限公司 C17、c20和c21取代的神经活性类固醇及其使用方法
AU2017296295B2 (en) 2016-07-11 2022-02-24 Sage Therapeutics, Inc. C7, C12, and C16 substituted neuroactive steroids and their methods of use
WO2018031748A1 (en) 2016-08-11 2018-02-15 Ovid Therapeutics Inc. Methods and compositions for treatment of epileptic disorders
CN115974954A (zh) 2016-08-23 2023-04-18 萨奇治疗股份有限公司 19-去甲c3,3-二取代的c21-n-吡唑基类固醇的晶体
US10391105B2 (en) 2016-09-09 2019-08-27 Marinus Pharmaceuticals Inc. Methods of treating certain depressive disorders and delirium tremens
EP3519422B1 (en) 2016-09-30 2022-08-31 Sage Therapeutics, Inc. C7 substituted oxysterols and these compounds for use as nmda modulators
ES2952106T3 (es) 2016-10-18 2023-10-27 Sage Therapeutics Inc Oxisteroles y procedimientos de utilización de los mismos
KR20250054838A (ko) 2016-10-18 2025-04-23 세이지 테라퓨틱스, 인크. 옥시스테롤 및 그의 사용 방법
EP3720867A1 (en) 2017-12-08 2020-10-14 Sage Therapeutics, Inc. Deuterated 21 -[4-cyano-pyrazol-1 -yl]-19-nor-pregan-3. alpha-ol-20-one derivatives for treating cns disorders
CN109988210B (zh) * 2017-12-30 2022-05-17 天津药业研究院股份有限公司 一种黄体酮和黄体酮中间体的制备方法
EP3864022B1 (en) 2018-10-12 2023-09-20 Sage Therapeutics, Inc. Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders
CN109289095B (zh) * 2018-11-23 2021-03-26 淮海工学院 一种含盐酸利多卡因的肠镜凝胶剂及其制备方法
WO2020118142A1 (en) 2018-12-07 2020-06-11 Marinus Pharmaceuticals, Inc. Ganaxolone for use in prophylaxis and treatment of pospartum depression
CN114206900A (zh) 2019-05-31 2022-03-18 萨奇治疗股份有限公司 神经活性类固醇及其组合物
CA3145923A1 (en) 2019-08-05 2021-02-11 David Czekai Ganaxolone for use in treatment of status epilepticus
US10857163B1 (en) 2019-09-30 2020-12-08 Athenen Therapeutics, Inc. Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof
WO2021113834A1 (en) 2019-12-06 2021-06-10 Marinus Pharmaceuticals, Inc. Ganaxolone for use in treating tuberous sclerosis complex
US20230346801A1 (en) 2020-03-25 2023-11-02 Sage Therapeutics, Inc. Use of agents for treatment of respiratory conditions
CN117801047B (zh) * 2023-01-19 2024-12-20 北京华睿鼎信科技有限公司 神经甾体衍生物及其用途

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB820780A (en) * 1954-12-08 1959-09-23 Syntex Sa Cyclopentanophenanthrene derivatives
US2856415A (en) * 1957-11-13 1958-10-14 Searle & Co 3,19-dihydroxy-5-androstene derivatives
BE632431A (enExample) * 1962-05-16
US3206459A (en) 1962-10-19 1965-09-14 Syntex Corp 10alpha-pregnan-19-ol derivatives
US4239681A (en) * 1974-04-15 1980-12-16 Richardson-Merrell Inc. Androst-4-en-19-ols
US4022769A (en) * 1974-05-13 1977-05-10 Richardson-Merrell Inc. Androst-4-en-19-ones
US4139617A (en) * 1974-05-13 1979-02-13 Richardson-Merrell Inc. 19-Oxygenated-androst-5-enes for the enhancement of libido
US4071625A (en) * 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
DE2632677A1 (de) 1976-07-16 1978-01-26 Schering Ag Verfahren zur herstellung von androstan-17-on-derivaten und deren verwendung
MA18433A1 (fr) * 1978-05-26 1979-12-31 Ciba Geigy Ag Procede pour la synthese de la chaine laterale hydroxyacetyle de steroides du type pregnagne, nouveaux 21-hydroxy-20-oxo-17 alpha-pregnagnes et produits pharmaceutiques en renfermant
US4389345A (en) 1981-10-09 1983-06-21 G.D. Searle & Co. 3-Oxoestra-17-acetonitrile and unsaturated analogs
US4495102A (en) * 1982-09-03 1985-01-22 G. D. Searle & Co. Aminoalkyl steroids
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
EP0656365B1 (en) 1993-12-02 1997-04-09 Akzo Nobel N.V. Substituted 2beta-morpholinoandrostane derivatives
US5661141A (en) * 1995-03-27 1997-08-26 Petrow; Vladimir 19-oxygenated steroids as therapeutic agents
KR19990022323A (ko) * 1995-06-06 1999-03-25 씨. 랜 낸시 안드로스탄 및 프레그난 시리즈의 신경활성 스테로이드
AU3967297A (en) * 1996-08-01 1998-02-25 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
US6855836B2 (en) 2000-10-26 2005-02-15 Jenapharm Gmbh & Co. Kg 17-Methylene steroids, process for their production and pharmaceutical compositions that contain these compounds
WO2002036605A2 (en) * 2000-11-03 2002-05-10 Washington University Estrone-derivatives having cytoprotective activity
GR1003861B (el) 2000-12-29 2002-04-11 Νεα νευροστεροειδη που αλληλεπιδρουν με τον υποδοχεα gabaa.
EA011123B1 (ru) 2003-03-24 2008-12-30 Стерикс Лимитед Производные эстрогена в качестве ингибиторов стероидной сульфатазы
CN1281561C (zh) * 2003-04-23 2006-10-25 中国科学院上海有机化学研究所 一种具有1，6－亚甲基－[10]－轮烯基本骨架的化合物及其用途
US7781421B2 (en) * 2003-05-29 2010-08-24 Washington University Neuroactive 13, 24-cyclo-18, 21-dinorcholanes and structurally related pentacyclic steriods
JP2007512344A (ja) * 2003-11-24 2007-05-17 メルク　エンド　カムパニー　インコーポレーテッド エストロゲン受容体調節剤
CN100376685C (zh) * 2005-01-14 2008-03-26 天津科技大学 微生物转化法制备雌酚酮的方法
CA2604887A1 (en) * 2005-04-07 2006-10-19 Hythiam, Inc. Improved methods of and compositions for the prevention of anxiety, substance abuse, and dependence
DE102007027636A1 (de) 2007-06-12 2008-12-18 Bayer Schering Pharma Aktiengesellschaft 17ß-Cyano-18a-homo-19-nor-androst-4-en-Derivat, dessen Verwendung und das Derivat enthaltende Arzneimittel
AU2008265898B2 (en) * 2007-06-15 2013-11-28 Research Triangle Institute Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties
GB0711948D0 (en) 2007-06-20 2007-08-01 Bionature E A Ltd Neurosteriod compounds
EP2598513A1 (en) * 2010-07-30 2013-06-05 Medexis S.A. Compounds and methods for treating neoplasia
EP2667876A2 (en) 2010-12-15 2013-12-04 Harbor BioSciences, Inc. Methods and compounds for preparing 3alpha-oxygen substituted steroids
US9388210B2 (en) 2011-02-25 2016-07-12 Washington University Neuroactive 17(20)-Z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
EP2695948B1 (en) 2011-03-23 2016-12-28 Etsuro Ito Method and kit for super-high-sensitivity measurement of protein and nucleic acid, and novel enzyme substrate
US20150175651A1 (en) * 2012-06-15 2015-06-25 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
WO2014058736A1 (en) * 2012-10-08 2014-04-17 Washington University Neuroactive 19-alkoxy-17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
BR112015014397B1 (pt) 2012-12-18 2021-02-02 Washington University composto, composição farmacêutica e uso de um composto
US9562026B2 (en) * 2013-03-14 2017-02-07 Washington University Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors
SMT202100048T1 (it) * 2013-08-23 2021-03-15 Sage Therapeutics Inc Steroidi neuroattivi, composizioni e loro usi

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