MX2015007900A - Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos. - Google Patents

Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos.

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Publication number
MX2015007900A
MX2015007900A MX2015007900A MX2015007900A MX2015007900A MX 2015007900 A MX2015007900 A MX 2015007900A MX 2015007900 A MX2015007900 A MX 2015007900A MX 2015007900 A MX2015007900 A MX 2015007900A MX 2015007900 A MX2015007900 A MX 2015007900A
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Mexico
Prior art keywords
neuroactive
alkoxy
treatment
prodrugs
methods
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MX2015007900A
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English (en)
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MX365644B (es
Inventor
Douglas Covey
Albert Jean Robichaud
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Univ Washington
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Publication date
Application filed by Univ Washington filed Critical Univ Washington
Publication of MX2015007900A publication Critical patent/MX2015007900A/es
Publication of MX365644B publication Critical patent/MX365644B/es

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    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
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    • 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
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Abstract

La descripción actual se dirige generalmente a esteroides neuroactivos sustituidos con 19-alcoxi-17 como se hace referencia en la presente, y sales farmacéuticamente aceptables de los mismos, para uso como, por ejemplo, un anestésico, y/o en el tratamiento de trastornos relacionados a la función y actividad GABA. La descripción actual se dirige además a composiciones farmacéuticas que comprenden tales compuestos.
MX2015007900A 2012-12-18 2013-12-18 Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos. MX365644B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261738822P 2012-12-18 2012-12-18
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

Publications (2)

Publication Number Publication Date
MX2015007900A true MX2015007900A (es) 2016-02-05
MX365644B MX365644B (es) 2019-06-10

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MX2015007900A MX365644B (es) 2012-12-18 2013-12-18 Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos.
MX2019006739A MX2019006739A (es) 2012-12-18 2015-06-18 Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos.

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WO (1) WO2014100228A1 (es)

Families Citing this family (49)

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Publication number Priority date Publication date Assignee Title
CA2631233C (en) 2005-11-28 2011-11-08 Marinus Pharmaceuticals Ganaxolone formulations and methods for the making and use thereof
CN103958540B (zh) 2011-09-08 2017-12-05 萨奇治疗股份有限公司 神经活性类固醇、组合物、及其用途
CA3152410A1 (en) 2011-10-14 2013-04-18 Sage Therapeutics, Inc. 3,3-disubstituted 19-nor pregnane compounds, compositions, and uses thereof for the treatment of cns related disorders
IL298436B1 (en) 2012-01-23 2024-03-01 Sage Therapeutics Inc Pharmaceutical preparations that include allopregnanolone
IL310501A (en) * 2012-12-18 2024-03-01 Washington University St Louis Neuroactive steroids converted at the 19th position to the 17th position, their prodrugs, and methods of treatment using them
SI3461834T1 (sl) 2013-03-13 2021-11-30 Sage Therapeutics, Inc. Nevroaktivni steroidi
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
RS60420B1 (sr) 2013-04-17 2020-07-31 Sage Therapeutics Inc 19-nor neuroaktivni steroidi za metode lečenja
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
IL286794B2 (en) 2013-04-17 2024-06-01 Sage Therapeutics Inc 19- NOR C3, 3- dimomer C21- N- pyrazole Steroids and methods of using them
RU2754534C2 (ru) 2013-07-19 2021-09-03 Сейдж Терапьютикс, Инк. Нейроактивные стероиды, композиции и их использование
DK3488852T3 (da) 2013-08-23 2021-02-01 Sage Therapeutics Inc Neuroaktive steroider, sammensætninger og anvendelser deraf
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
WO2016061537A1 (en) 2014-10-16 2016-04-21 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
CN107404877A (zh) 2014-10-16 2017-11-28 萨奇治疗股份有限公司 靶向cns 障碍的组合物和方法
SI3224269T1 (sl) 2014-11-27 2020-10-30 Sage Therapeutics, Inc. Sestavki in metode za zdravljenje CNS motenj
PL3250210T3 (pl) * 2015-01-26 2021-07-26 Sage Therapeutics, Inc. Kompozycje i sposoby leczenia zaburzeń OUN
JP6875996B2 (ja) * 2015-02-20 2021-05-26 セージ セラピューティクス， インコーポレイテッド 神経刺激性ステロイド、組成物、およびその使用
MA45276A (fr) 2015-06-18 2018-04-25 Sage Therapeutics Inc Solutions de stéroïdes neuroactifs et leurs méthodes d'utilisation
JP6882996B2 (ja) 2015-07-06 2021-06-02 セージ セラピューティクス， インコーポレイテッド オキシステロールおよびそれらの使用の方法
CA2991214C (en) 2015-07-06 2024-04-30 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
WO2017007840A1 (en) 2015-07-06 2017-01-12 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
CA3001722A1 (en) 2015-10-16 2017-04-20 Marinus Pharmaceuticals, Inc. Injectable neurosteroid formulations containing nanoparticles
WO2017087864A1 (en) * 2015-11-20 2017-05-26 Sage Therapeutics, Inc. Compounds and methods of their use
RU2022102537A (ru) 2016-03-08 2022-03-30 Сейдж Терапьютикс, Инк. Нейроактивные стероиды, их композиции и применения
PL3436022T3 (pl) 2016-04-01 2022-08-08 Sage Therapeutics, Inc. Oksysterole i sposoby ich stosowania
US10752653B2 (en) 2016-05-06 2020-08-25 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
EP3919502A1 (en) 2016-07-07 2021-12-08 Sage Therapeutics, Inc. 11-substituted 24-hydroxysterols for use in the treatment of nmda related conditions
AU2017297375B2 (en) 2016-07-11 2022-09-15 Sage Therapeutics, Inc. C17, C20, and C21 substituted neuroactive steroids and their methods of use
EP3481844B1 (en) 2016-07-11 2024-04-17 Sage Therapeutics, Inc. C7, c12, and c16 substituted neuroactive steroids and their methods of use
KR102518846B1 (ko) 2016-08-11 2023-04-05 오비드 테라퓨틱스 인크. 간질 장애의 치료를 위한 방법 및 조성물
CN110088091A (zh) 2016-08-23 2019-08-02 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
MA46351A (fr) 2016-09-30 2021-06-02 Sage Therapeutics Inc Oxystérols substitués en c7 et procédés en tant que modulateurs nmda
WO2018075698A1 (en) 2016-10-18 2018-04-26 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
MA46566A (fr) 2016-10-18 2019-08-28 Sage Therapeutics Inc Oxystérols et leurs procédés d'utilisation
KR20200096596A (ko) 2017-12-08 2020-08-12 세이지 테라퓨틱스, 인크. Cns 장애의 치료를 위한 중수소화 21 -[4-시아노-피라졸-1 -일]-19-노르-프레간-3. 알파-올-20-온 유도체
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
SG11202112391UA (en) 2019-05-31 2021-12-30 Sage Therapeutics Inc Neuroactive steroids and compositions thereof
WO2021026124A1 (en) 2019-08-05 2021-02-11 Marinus Pharmaceuticals, Inc. 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
MX2022006014A (es) 2019-12-06 2022-06-22 Marinus Pharmaceuticals Inc Ganaxolona para uso en el tratamiento del complejo de esclerosis tuberosa.
AU2021241622A1 (en) 2020-03-25 2022-10-20 Sage Therapeutics, Inc. Use of agents for treatment of respiratory conditions
CN117801047A (zh) * 2023-01-19 2024-04-02 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 (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB820779A (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
NL292848A (es) * 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
US4071625A (en) 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
US4139617A (en) * 1974-05-13 1979-02-13 Richardson-Merrell Inc. 19-Oxygenated-androst-5-enes for the enhancement of libido
US4022769A (en) * 1974-05-13 1977-05-10 Richardson-Merrell Inc. Androst-4-en-19-ones
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
ATE284895T1 (de) * 1995-06-06 2005-01-15 Euro Celtique Sa Neuroaktive steroide der androstan- und pregnanreihe
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
US6844456B2 (en) 2000-11-03 2005-01-18 Washington University Modified, hydroxy-substituted aromatic structures having cytoprotective activity
GR1003861B (el) 2000-12-29 2002-04-11 Νεα νευροστεροειδη που αλληλεπιδρουν με τον υποδοχεα gabaa.
DK1608671T3 (da) 2003-03-24 2010-05-10 Sterix Ltd Østrogenderivater som inhibitorer af steroidsulfatase
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
WO2005000869A1 (en) 2003-05-29 2005-01-06 Washington University Neuroactive 13,24-cyclo-18,21-dinorcholanes and structurally-related pentacyclic steroids
US20070099880A1 (en) * 2003-11-24 2007-05-03 Blizzard Timothy A Estrogen receptor modulators
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
WO2008157460A1 (en) * 2007-06-15 2008-12-24 Cook, Kevin, M. 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
US20130303500A1 (en) 2010-07-30 2013-11-14 Medexis S.A. Compounds and methods for treating neoplasia
US20120214987A1 (en) 2010-12-15 2012-08-23 Yu Ge Methods and compounds for preparing 3alpha-oxygen substituted steroids
WO2012116290A2 (en) 2011-02-25 2012-08-30 Washington University Neuroactive 17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
US9851309B2 (en) 2011-03-23 2017-12-26 Satoshi Watabe Ultra-high-sensitive assay of protein and nucleic acid and kit, and novel enzyme substrate
WO2013188792A2 (en) * 2012-06-15 2013-12-19 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
IL310501A (en) 2012-12-18 2024-03-01 Washington University St Louis Neuroactive steroids converted at the 19th position to the 17th position, their prodrugs, and methods of treatment using them
US9562026B2 (en) * 2013-03-14 2017-02-07 Washington University Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors
DK3488852T3 (da) 2013-08-23 2021-02-01 Sage Therapeutics Inc Neuroaktive steroider, sammensætninger og anvendelser deraf

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