SI2935307T1 - Non-reactive 19-alkoxy-17-substituted steroids useful in therapeutic procedures - Google Patents

Non-reactive 19-alkoxy-17-substituted steroids useful in therapeutic procedures Download PDF

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Publication number
SI2935307T1
SI2935307T1 SI201331092T SI201331092T SI2935307T1 SI 2935307 T1 SI2935307 T1 SI 2935307T1 SI 201331092 T SI201331092 T SI 201331092T SI 201331092 T SI201331092 T SI 201331092T SI 2935307 T1 SI2935307 T1 SI 2935307T1
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Slovenia
Prior art keywords
pharmaceutically acceptable
compound according
acceptable salt
alkyl
pharmaceutical composition
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SI201331092T
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English (en)
Slovenian (sl)
Inventor
Douglas Covey
Albert Jean Robichaud
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Washington University
Sage Therapeutics, Inc.
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Publication date
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Publication of SI2935307T1 publication Critical patent/SI2935307T1/en

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    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07J—STEROIDS
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    • 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
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    • 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
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    • 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
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    • 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
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    • 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
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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
    • C07J1/0003—Androstane derivatives
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
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    • 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)
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    • 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
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    • C07J—STEROIDS
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    • 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
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    • C07J—STEROIDS
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
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    • 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
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    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07J21/005—Ketals
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    • C07J—STEROIDS
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    • 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
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    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

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  • Biomedical Technology (AREA)
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  • Urology & Nephrology (AREA)
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  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
SI201331092T 2012-12-18 2013-12-18 Non-reactive 19-alkoxy-17-substituted steroids useful in therapeutic procedures SI2935307T1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261738822P 2012-12-18 2012-12-18
EP13865411.6A EP2935307B1 (en) 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, useful in methods of treatment
PCT/US2013/076214 WO2014100228A1 (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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SI2935307T1 true SI2935307T1 (en) 2018-08-31

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SI201331092T SI2935307T1 (en) 2012-12-18 2013-12-18 Non-reactive 19-alkoxy-17-substituted steroids useful in therapeutic procedures
SI201332021T SI3392260T1 (sl) 2012-12-18 2013-12-18 Nevroaktivni 19-alkoksi-17-substituirani steroidi, uporabni pri postopkih zdravljenja

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US (8) US9676812B2 (enExample)
EP (3) EP2935307B1 (enExample)
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CN (3) CN105026415B (enExample)
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HR (1) HRP20181048T1 (enExample)
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IL (3) IL310501A (enExample)
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PT (2) PT3392260T (enExample)
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RU (1) RU2663665C2 (enExample)
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SI (2) SI2935307T1 (enExample)
SM (1) SMT201800422T1 (enExample)
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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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