BR112015026380A2 - esteróides 19-nor-c3,3-c21-n-pirazolil dissubstituídos e métodos de utilização dos mesmos - Google Patents

esteróides 19-nor-c3,3-c21-n-pirazolil dissubstituídos e métodos de utilização dos mesmos

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Publication number
BR112015026380A2
BR112015026380A2 BR112015026380A BR112015026380A BR112015026380A2 BR 112015026380 A2 BR112015026380 A2 BR 112015026380A2 BR 112015026380 A BR112015026380 A BR 112015026380A BR 112015026380 A BR112015026380 A BR 112015026380A BR 112015026380 A2 BR112015026380 A2 BR 112015026380A2
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Brazil
Prior art keywords
disorders
disubstituted
steroids
methods
pyrazolyl
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BR112015026380A
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English (en)
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BR112015026380A8 (pt
Inventor
Jean Robichaud Albert
L Harrison Boyd
G Salituro Francesco
Martinez Botella Gabriel
Thomas Beresis Richard
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Sage Therapeutics Inc
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Application filed by Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Publication of BR112015026380A2 publication Critical patent/BR112015026380A2/pt
Publication of BR112015026380A8 publication Critical patent/BR112015026380A8/pt

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    • 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
    • A61K31/58—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
    • 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
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J15/00—Stereochemically pure steroids containing carbon, hydrogen, halogen or oxygen having a partially or totally inverted skeleton, e.g. retrosteroids, L-isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • C07J5/0046—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 substituted in position 17 alfa
    • C07J5/0053—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 substituted in position 17 alfa not substituted in position 16
    • 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
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane 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
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • 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
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074—Esters
    • 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
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • 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
    • 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
    • C07J7/0065—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 an OH group free esterified or etherified
    • C07J7/007—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 an OH group free esterified or etherified not substituted in position 17 alfa
    • 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
    • C07J7/0085—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 an halogen atom

Abstract

resumo “esteróides 19-nor-c3,3-c21-n-pirazolil dissubstituídos e métodos de utilização dos mesmos” são aqui fornecidos 19-nor c3,3-dissubstituídas esteróides c21-pirazolilo de fórmula geral (i): e seus sais farmaceuticamente aceitáveis; em que, r1, r2, r3a, r3b, r4a, r4b, r5, r6, e r7are como aqui definido. tais compostos estão contemplados útil para a prevenção e tratamento de uma variedade de condições relacionadas com o snc, por exemplo, o tratamento de distúrbios do sono, transtornos de humor, transtornos do espectro da esquizofrenia, perturbações convulsivas, perturbações de memória e / ou cognição, perturbações do movimento, distúrbios de personalidade , desordens do espectro autista, dor, lesão cerebral traumática, doenças vasculares, distúrbios de abuso de substâncias e / ou síndromes de abstinência, e zumbido.
BR112015026380A 2013-04-17 2014-04-17 esteróides de c21-n-pirazolil 19-nor c3,3-dissubstituídos e métodos de uso destes BR112015026380A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN2013074323 2013-04-17
PCT/CN2014/075594 WO2014169833A1 (en) 2013-04-17 2014-04-17 19-nor c3,3-disubstituted c21-n-pyrazolyl steroids and methods of use thereof

Publications (2)

Publication Number Publication Date
BR112015026380A2 true BR112015026380A2 (pt) 2017-07-25
BR112015026380A8 BR112015026380A8 (pt) 2019-12-31

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BR112015026380A BR112015026380A8 (pt) 2013-04-17 2014-04-17 esteróides de c21-n-pirazolil 19-nor c3,3-dissubstituídos e métodos de uso destes

Country Status (26)

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US (5) US9512165B2 (pt)
EP (3) EP3498725B1 (pt)
JP (6) JP6470258B2 (pt)
KR (4) KR20230172622A (pt)
CN (3) CN108440633B (pt)
AU (4) AU2014256229B2 (pt)
BR (1) BR112015026380A8 (pt)
CA (1) CA2909545A1 (pt)
CY (2) CY1121228T1 (pt)
DK (2) DK3498725T3 (pt)
ES (2) ES2709434T3 (pt)
HK (1) HK1224301A1 (pt)
HR (2) HRP20190232T1 (pt)
HU (2) HUE055554T2 (pt)
IL (4) IL286794B1 (pt)
LT (2) LT3498725T (pt)
MX (2) MX362543B (pt)
PL (2) PL2986623T3 (pt)
PT (2) PT3498725T (pt)
RS (2) RS58297B1 (pt)
RU (1) RU2675855C2 (pt)
SG (2) SG11201508550XA (pt)
SI (2) SI3498725T1 (pt)
TR (1) TR201901745T4 (pt)
WO (1) WO2014169833A1 (pt)
ZA (1) ZA201507740B (pt)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101405545B1 (ko) 2005-11-28 2014-07-03 마리누스 파마슈티컬스 ｇａｎａｘｏｌｏｎｅ 제형, 이의 제조방법 및 용도
CN108976272B (zh) 2011-10-14 2021-05-25 萨奇治疗股份有限公司 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
EP4295908A3 (en) 2012-01-23 2024-03-20 Sage Therapeutics, Inc. Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin
US10039777B2 (en) 2012-03-20 2018-08-07 Neuro-Lm Sas Methods and pharmaceutical compositions of the treatment of autistic syndrome disorders
US20160068563A1 (en) 2013-04-17 2016-03-10 Boyd L. Harrison 19-nor neuroactive steroids and methods of use thereof
PL2986623T3 (pl) * 2013-04-17 2019-04-30 Sage Therapeutics Inc 19-nor C3,3-dipodstawione steroidy C21-n-pirazolilowe i sposoby ich stosowania
US9725481B2 (en) 2013-04-17 2017-08-08 Sage Therapeutics, Inc. 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof
EP2986624B1 (en) 2013-04-17 2020-03-25 Sage Therapeutics, Inc. 19-nor neuroactive steroids for methods of treatment
CN105555277B (zh) 2013-07-19 2022-01-11 萨奇治疗股份有限公司 神经活性类固醇化合物、组合物及其用途
RU2696585C2 (ru) 2013-08-23 2019-08-05 Сейдж Терапьютикс, Инк. Нейроактивные стероиды, их композиции и применение
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
WO2016061537A1 (en) 2014-10-16 2016-04-21 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
MX2021004492A (es) 2014-10-16 2022-12-05 Sage Therapeutics Inc Composiciones para el tratamiento de trastornos del snc.
EP3719029A1 (en) 2014-11-27 2020-10-07 Sage Therapeutics, Inc. Compositions for inducing sedation
CN104558092B (zh) * 2014-12-29 2017-01-18 北京理工大学 一种甾体皂苷化合物及其制备方法和用途
HUE054092T2 (hu) 2015-01-26 2021-08-30 Sage Therapeutics Inc Központi idegrendszeri zavarok kezelésére szolgáló kompozíciók és eljárások
WO2016134301A2 (en) 2015-02-20 2016-08-25 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
MA45276A (fr) 2015-06-18 2018-04-25 Sage Therapeutics Inc Solutions de stéroïdes neuroactifs et leurs méthodes d'utilisation
CN104910236B (zh) * 2015-06-26 2016-08-17 西北农林科技大学农药研究所 吡唑基甾体衍生物及其制备方法、用途
EA036155B1 (ru) 2015-10-16 2020-10-06 Маринус Фармасьютикалс, Инк. Инъекционные составы нейростероида, содержащие наночастицы
KR102408399B1 (ko) 2016-03-08 2022-06-13 세이지 테라퓨틱스, 인크. 신경활성 스테로이드, 조성물, 및 그의 용도
US11396525B2 (en) 2016-07-11 2022-07-26 Sage Therapeutics, Inc. C17, C20, and C21 substituted neuroactive steroids and their methods of use
US20180042903A1 (en) 2016-08-11 2018-02-15 Ovid Therapeutics Inc. Methods and compositions for treatment of epileptic disorders
PE20190915A1 (es) * 2016-08-23 2019-06-26 Sage Therapeutics Inc Un esteroide 19-nor-c21-n-pirazolilo c3,3-disustituido cristalino
US10391105B2 (en) 2016-09-09 2019-08-27 Marinus Pharmaceuticals Inc. Methods of treating certain depressive disorders and delirium tremens
CN110520131A (zh) * 2017-04-18 2019-11-29 马瑞纳斯制药公司 缓释可注射的神经类固醇制剂
IL303250A (en) * 2017-09-07 2023-07-01 Sage Therapeutics Inc Neuroactive steroids and methods of using them
MX2020002889A (es) * 2017-09-14 2020-10-01 Sage Therapeutics Inc Un esteroide c21-n-pirazolilo 19-nor c3,3-disustituido, y métodos de uso del mismo.
WO2019075362A1 (en) * 2017-10-12 2019-04-18 Sage Therapeutics, Inc. METHOD OF TREATING CENTRAL NERVOUS SYSTEM DISORDERS WITH NEUROSTEROIDS AND GABAERGIC COMPOUNDS
MA51046A (fr) 2017-12-08 2021-03-17 Sage Therapeutics Inc Dérivés de 21-[4-cyano-pyrazol-1-yl]-19-nor-pregan-3. alpha-ol-20-one deutérés pour le traitement de troubles du snc
BR112020012761A2 (pt) 2017-12-22 2021-02-17 Sage Therapeutics, Inc. composições e métodos para o tratamento de distúrbios do snc
US11718642B2 (en) 2018-01-12 2023-08-08 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
US11661437B2 (en) * 2018-02-11 2023-05-30 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Steroid derivative regulators, method for preparing the same, and uses thereof
CN114656514A (zh) * 2018-02-11 2022-06-24 江苏豪森药业集团有限公司 一种甾族类衍生物调节剂及其制备方法和应用
KR20210021005A (ko) * 2018-06-12 2021-02-24 세이지 테라퓨틱스, 인크. 19-nor c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
CN111040015B (zh) * 2018-10-15 2022-03-18 南京诺瑞特医药科技有限公司 19-去甲-c21取代类固醇衍生物
CN109503694A (zh) * 2018-11-21 2019-03-22 苏州闻天医药科技有限公司 一种新型gabaa受体调节剂及其用途
BR112021010996A2 (pt) 2018-12-05 2021-08-31 Sage Therapeutics, Inc. Esteroides neuroativos e seus métodos de uso
US11266662B2 (en) 2018-12-07 2022-03-08 Marinus Pharmaceuticals, Inc. Ganaxolone for use in prophylaxis and treatment of postpartum depression
US20220089637A1 (en) * 2019-01-08 2022-03-24 Chengdu kanghong pharmaceutical co ltd Steroid compound, and use thereof and preparation method therefor
CN113301901B (zh) * 2019-01-14 2022-09-09 北京轩义医药科技有限公司 四唑啉酮取代的类固醇及其用途
CN111454318A (zh) 2019-01-20 2020-07-28 浙江易众化工有限公司 抗抑郁药物sage-217的晶型及其制备方法
WO2020155057A1 (zh) * 2019-01-31 2020-08-06 深圳仁泰医药科技有限公司 γ-氨基丁酸调节剂的晶型X及其制备方法和应用
US20220220149A1 (en) 2019-05-28 2022-07-14 Teva Czech Industries S.R.O Solid state forms of sage-217 and processes for preparation thereof
JOP20210293A1 (ar) 2019-05-31 2023-01-30 Sage Therapeutics Inc ستيرويدات ذات فعالية عصبية وتركيبات منها
EP3990467A1 (en) * 2019-06-27 2022-05-04 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
MX2021015854A (es) 2019-06-27 2022-04-18 Sage Therapeutics Inc Composiciones y métodos para tratar trastornos del snc.
TW202114700A (zh) * 2019-06-27 2021-04-16 美商賽吉醫療公司 用於治療cns病症之組合物及方法
MX2022001553A (es) 2019-08-05 2022-04-18 Marinus Pharmaceuticals Inc Ganaxolona para su uso en el tratamiento del estado epileptico.
US20220275020A1 (en) 2019-08-07 2022-09-01 Shanghai Hansoh Biomedical Co., Ltd. Salt and crystal form of steroid derivative regulator
US10857163B1 (en) 2019-09-30 2020-12-08 Athenen Therapeutics, Inc. Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof
IL291835A (en) * 2019-09-30 2022-06-01 Athenen Therapeutics Inc Preparations which preferentially increase subtypes of GABA receptors and methods of using them
MX2022006014A (es) 2019-12-06 2022-06-22 Marinus Pharmaceuticals Inc Ganaxolona para uso en el tratamiento del complejo de esclerosis tuberosa.
AR123018A1 (es) * 2020-07-20 2022-10-26 Sage Therapeutics Inc Formulaciones del esteroide c21-n-pirazolilo 19-nor c3,3-disustituido y métodos de uso de este
IL304080A (en) 2021-01-28 2023-08-01 Sage Therapeutics Inc Use of neuroactive steroids to treat sexual dysfunction
JP2024510436A (ja) 2021-03-17 2024-03-07 セージ セラピューティクス， インコーポレイテッド 大うつ病性障害の処置のための１９－ノルｃ３，３－２置換ｃ２１－ｎ－ピラゾリルステロイド
WO2022232504A1 (en) 2021-04-29 2022-11-03 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21 -n-pyrazolyl steroid for use in treating major depressive disorder and postpartum depression
EP4329769A1 (en) 2021-04-29 2024-03-06 Sage Therapeutics, Inc. Neuroactive steroid for use in treating major depressive disorder and postpartum depression in a lactating female
WO2023158668A1 (en) 2022-02-16 2023-08-24 Sage Therapeutics, Inc. Neuroactive steroids for treatment of cns-related disorders
WO2023163879A1 (en) 2022-02-28 2023-08-31 Sage Therapeutics, Inc. Neuroactive steroids for treatment of gastrointestinal diseases or conditions

Family Cites Families (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2856415A (en) 1957-11-13 1958-10-14 Searle & Co 3,19-dihydroxy-5-androstene derivatives
FR1380417A (fr) 1962-05-15 1964-12-04 Roussel Uclaf Nouveaux androstanyl-pyrazoles et procédé de préparation
NL297205A (pt) * 1962-08-28
US3206459A (en) 1962-10-19 1965-09-14 Syntex Corp 10alpha-pregnan-19-ol derivatives
US3169134A (en) 1963-03-21 1965-02-09 Searle & Co 2, 3-oxygenated-17alpha-methyl-5alpha-androstan-17beta-ols
US3511860A (en) * 1966-09-26 1970-05-12 Syntex Corp Synthesis of 19-nor and ring a aromatic steroids and intermediates therefor
NL6801449A (pt) * 1968-02-01 1969-08-05
BE754111A (fr) 1969-07-29 1971-01-29 Upjohn Co Nouveaux 7alpha- et 7beta-methyl-3alpha,5alpha- cycloandrostanes et composes analogues 19-nor et leur procede de preparation
GB1434919A (en) 1972-06-15 1976-05-12 Glaxo Lab Ltd 3alpha-hydroxy androstanes
US3943124A (en) 1970-12-17 1976-03-09 Gordon Hanley Phillipps Chemical compounds
GB1380246A (en) 1970-12-17 1975-01-08 Glaxo Lab Ltd 3alpha-hydroxy-androstanes and esters thereof
GB1430942A (en) 1972-05-05 1976-04-07 Glaxo Lab Ltd 21-substituted 3alpha-hydroxy pregnanes
US3983111A (en) 1972-05-05 1976-09-28 Glaxo Laboratories Limited Steroidal anaesthetics of the pregnane and 19-norpregnane series
GB1436324A (en) 1972-05-12 1976-05-19 Glaxo Lab Ltd Anaesthetic 3alpha-hydroxy pregnanes
DK134348C (da) 1973-11-30 1977-03-21 Schering Ag Analogifremgangsmade til fremstilling af d-homo-20-ketopregnaner
US4071625A (en) 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
DE2438020A1 (de) 1974-08-05 1976-02-26 Schering Ag 18-methyl-19-nor-20-keto-pregnane und verfahren zu ihrer herstellung
IL48628A0 (en) 1974-12-23 1976-02-29 Schering Ag D-homo-20-keto-pregnanes and process for their manufactur
DE2526373C2 (de) 1975-06-11 1983-11-10 Schering AG, 1000 Berlin und 4709 Bergkamen Verfahren zur Herstellung von Δ↑9↑↑(↑↑1↑↑1↑↑)↑-5α-20-Ketosteroiden
US4192871A (en) 1976-01-06 1980-03-11 Glaxo Laboratories Limited Chemical compounds
GB1570394A (en) 1976-01-06 1980-07-02 Glaxo Lab Ltd 11-acyloxy-3-hydroxy steroids
GB1581234A (en) 1976-04-05 1980-12-10 Glaxo Operations Ltd 11a - amino - 3a - hydroxysteroids
DE2632677A1 (de) 1976-07-16 1978-01-26 Schering Ag Verfahren zur herstellung von androstan-17-on-derivaten und deren verwendung
GB1581235A (en) 1977-04-04 1980-12-10 Glaxo Operations Ltd 11a-amino-3a-hydroxy-steroids
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
US5319115A (en) 1987-08-25 1994-06-07 Cocensys Inc. Method for making 3α-hydroxy, 3β-substituted-pregnanes
US5120723A (en) 1987-08-25 1992-06-09 University Of Southern California Method, compositions, and compounds for modulating brain excitability
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
WO1993005786A1 (en) 1991-09-13 1993-04-01 Cocensys, Inc. Novel gabaa receptor with steroid binding sites
DE4232681C2 (de) 1992-09-29 1994-11-24 Sigma Tau Ind Farmaceuti 17-Phenyl- und 17-Furyl-14beta,5alpha-androstan- und androsten- Derivate, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Zusammensetzung
EP0701444B1 (en) 1993-05-24 2010-04-07 Purdue Pharma Ltd. Methods and compositions for inducing sleep
EP0656365B1 (en) 1993-12-02 1997-04-09 Akzo Nobel N.V. Substituted 2beta-morpholinoandrostane derivatives
CZ300694A3 (en) 1993-12-02 1996-05-15 Akzo Nobel Nv Substituted 2beta-morpholinandrostane derivatives, process of their preparation, their use for preparing pharmaceutical preparations and pharmaceutical compositions containing thereof
ES2151593T3 (es) 1994-02-14 2001-01-01 Euro Celtique Sa Androstanos y pregnanos para modulacion alosterica del receptor de gaba.
US5939545A (en) * 1994-02-14 1999-08-17 Cocensys, Inc. Method, compositions, and compounds for allosteric modulation of the gaba receptor by members of the androstane and pregnane series
WO1996003421A1 (en) 1994-07-21 1996-02-08 Pharmacia & Upjohn Company Neurologically active aminosteroids
US5792757A (en) * 1994-08-04 1998-08-11 Pherin Pharmaceuticals 19-nor-pregnane steroids as neurochemical initiators of change in human hypothalamic function
JPH10509458A (ja) 1994-11-23 1998-09-14 コセンシス・インコーポレイテッド Ｇａｂａレセプターをアロステリック調節するためのアンドロスタンおよびプレグナン系列
NZ310850A (en) 1995-06-06 1999-07-29 Cocensys Inc 3 alpha hydroxy(17)-unsubstituted derivatives of androstane and 21 substituted derivatives of the pregnane series and medicaments
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
US5994334A (en) 1997-02-05 1999-11-30 University Of Maryland Androgen synthesis inhibitors
US5935545A (en) 1997-07-11 1999-08-10 E. I. Du Pont De Nemours And Company Process for producing an aqueous solution comprising ferric chloride
YU77701A (sh) 1999-04-29 2005-07-19 Euro-Celtique S.A. 3-α-HIDROKSI-3Гџ-METOKSIMETIL-21-HETEROCIKLIČNO SUPSTITUISANI STEROIDI SA ANESTETIČKIM DEJSTVOM
US7018406B2 (en) 1999-11-17 2006-03-28 Corevalve Sa Prosthetic valve for transluminal delivery
EP1172371B1 (en) 2000-02-18 2005-06-08 Taiho Pharmaceutical Company Limited Process for the preparation of steroid derivatives
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
CA2427817C (en) 2000-11-03 2009-04-14 Washington University Estrone-derivatives having cytoprotective activity
GR1003861B (el) 2000-12-29 2002-04-11 Νεα νευροστεροειδη που αλληλεπιδρουν με τον υποδοχεα gabaa.
CA2520142C (en) 2003-03-24 2011-01-04 Sterix Limited Oestrogen derivatives as inhibitors of steroid sulphatase
CA2527019A1 (en) 2003-05-29 2005-01-06 Washington University Neuroactive 13,24-cyclo-18,21-dinorcholanes and structurally-related pentacyclic steroids
WO2005051972A1 (en) 2003-11-24 2005-06-09 Merck & Co., Inc. Estrogen receptor modulators
US20090118248A1 (en) 2004-04-23 2009-05-07 Euro-Celtique S.A. 3-Alpha-hydroxy 21-n-heteroaryl-pregnane derivatives for modulation of brain excitability and a process for the production thereof
CA2578789A1 (en) * 2004-09-03 2006-03-16 Celgene Corporation Substituted heterocyclic compounds and uses thereof
WO2006037016A2 (en) 2004-09-27 2006-04-06 The Regents Of The University Of California Novel therapy for treatment of chronic degenerative brain diseases and nervous system injury
EP1807118B8 (en) 2004-09-29 2014-04-23 Harbor Therapeutics, Inc. Steroid analogs and characterization and treatment methods
US8030298B2 (en) * 2005-05-26 2011-10-04 Abbott Products Gmbh 17β-HSD1 and STS inhibitors
PT1888080E (pt) 2005-06-09 2010-07-06 Euro Celtique Sa ComposiãŽes farmac—uticas de um esterëide neuroactivo e as suas utilizaãŽes
JP2009532471A (ja) * 2006-04-05 2009-09-10 ワイス ５−ヒドロキシトリプタミン−６リガンドとしてのスルホニル−３−ヘテロシクリルインダゾール誘導体
CN101506221B (zh) * 2006-09-19 2012-09-12 索尔瓦药物有限公司 雌三烯衍生物及其作为17β-羟基类固醇脱氢酶抑制剂的用途
US20090203658A1 (en) 2007-01-08 2009-08-13 Duke University Neuroactive steroid compositions and methods of use therefor
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
CA2698172C (en) 2007-06-15 2014-02-18 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
CN101412742B (zh) 2007-10-19 2013-07-31 天津金耀集团有限公司 一种抑制血管新生的硝酸酯药物
KR100958286B1 (ko) * 2007-11-15 2010-05-19 한국과학기술원 ａ１Ｇ Ｔ―타입 칼슘 채널을 억제하여 본태성 진전증을예방 및 치료하는 방법
US20090264443A1 (en) 2008-04-18 2009-10-22 David Helton Treatment of organophosphate exposure with tetrahydroindolone arylpiperazine compounds
CN101624414B (zh) 2008-07-07 2013-02-13 天津金耀集团有限公司 一种抑制血管新生的硝酸酯药物
CZ2008434A3 (cs) 2008-07-10 2009-12-09 Ústav organické chemie a biochemie Akademie ved CR, v. v. i. Pregnanové anionické slouceniny, zpusob jejich výroby a jejich použití
US20100120733A1 (en) 2008-11-07 2010-05-13 Auspex Pharmaceuticals, Inc. Steroid modulators of glucocorticoid receptor
WO2011079047A1 (en) 2009-12-23 2011-06-30 Drugtech Corporation Methods for reducing the occurrence of preterm delivery and other pregnancy-related conditions
US20130303500A1 (en) 2010-07-30 2013-11-14 Medexis S.A. Compounds and methods for treating neoplasia
AU2011343615A1 (en) 2010-12-15 2013-05-09 Harbor Biosciences, Inc. Methods and compounds for preparing 3alpha-oxygen substituted steroids
WO2012109752A1 (en) 2011-02-15 2012-08-23 Socpra Sciences Et Génie, S.E.C. Steroid alkaloids and uses thereof as antimicrobial agents against electron transport-deficient microbes and as potentiators for antimicrobial agents against pathogenic bacteria
CZ201181A3 (cs) 2011-02-15 2012-09-12 Ústav organické chemie a biochemie Akademie ved CR, v.v.i. Deriváty pregnanolonu substituované v poloze 3alfa kationickou skupinou, zpusob jejich výroby, jejich použití a prostredek je obsahující
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
JP5265816B2 (ja) 2011-03-23 2013-08-14 悦朗 伊藤 タンパク質および核酸の超高感度測定法およびキット、並びに新規な酵素基質
EP2736919A4 (en) 2011-07-29 2015-01-14 Univ California NEW 17-BETA-HETEROARYL-SUBSTITUTED STEROIDS AS MODULATORS OF GABAA RECEPTORS
WO2013036835A1 (en) * 2011-09-08 2013-03-14 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
CN108976272B (zh) 2011-10-14 2021-05-25 萨奇治疗股份有限公司 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
US20150175651A1 (en) 2012-06-15 2015-06-25 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
DK3336097T3 (da) 2012-06-19 2020-09-28 Intercept Pharmaceuticals Inc Fremstilling af ikke-krystallinsk obeticholsyre
WO2014028398A2 (en) 2012-08-13 2014-02-20 The Regents Of The University Of California Mitigation of epileptic seizures by combination therapy using benzodiazepines and neurosteroids
US9765110B2 (en) 2012-10-08 2017-09-19 Washington University Neuroactive 19-alkoxy-17(20)-Z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
WO2014071449A1 (en) 2012-11-09 2014-05-15 Goodchild Investments Pty Ltd Neuroactive steroids and their use to facilitate neuroprotection
NZ739760A (en) 2012-12-18 2020-05-29 Univ Washington Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
US8939545B2 (en) 2012-12-20 2015-01-27 Eastman Kodak Company Inkjet printing with managed airflow for condensation control
CA2831054C (en) 2013-01-09 2016-08-30 Sapna Life Sciences Corp. Formulations, and methods for their use in treatment of neuropathology and neurodegeneration as a result of traumatic injury
WO2014108808A2 (en) 2013-01-09 2014-07-17 Henry James Lorne Pharmaceutical formulations for the treatment and prevention of trauma-induced neuropathology and neurodegeneration
GB201302368D0 (en) 2013-02-11 2013-03-27 Univ Bath Compound
US9512170B2 (en) 2013-03-01 2016-12-06 Washington University Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors
US9562026B2 (en) 2013-03-14 2017-02-07 Washington University Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors
PL2986623T3 (pl) 2013-04-17 2019-04-30 Sage Therapeutics Inc 19-nor C3,3-dipodstawione steroidy C21-n-pirazolilowe i sposoby ich stosowania
EP2986624B1 (en) 2013-04-17 2020-03-25 Sage Therapeutics, Inc. 19-nor neuroactive steroids for methods of treatment
US9725481B2 (en) 2013-04-17 2017-08-08 Sage Therapeutics, Inc. 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof
US20160068563A1 (en) 2013-04-17 2016-03-10 Boyd L. Harrison 19-nor neuroactive steroids and methods of use thereof
CN105555277B (zh) 2013-07-19 2022-01-11 萨奇治疗股份有限公司 神经活性类固醇化合物、组合物及其用途
RU2696585C2 (ru) 2013-08-23 2019-08-05 Сейдж Терапьютикс, Инк. Нейроактивные стероиды, их композиции и применение
EP3149018B1 (en) 2014-05-29 2020-04-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
MA40498A (fr) 2014-09-02 2021-05-19 Texas A & M Univ Sys Méthode de traitement de l'intoxication par organophosphates
WO2016061537A1 (en) 2014-10-16 2016-04-21 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
MX2021004492A (es) 2014-10-16 2022-12-05 Sage Therapeutics Inc Composiciones para el tratamiento de trastornos del snc.
EP3719029A1 (en) 2014-11-27 2020-10-07 Sage Therapeutics, Inc. Compositions for inducing sedation
HUE054092T2 (hu) 2015-01-26 2021-08-30 Sage Therapeutics Inc Központi idegrendszeri zavarok kezelésére szolgáló kompozíciók és eljárások
CN105985396A (zh) 2015-02-16 2016-10-05 苏州泽璟生物制药有限公司 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物
WO2016134301A2 (en) 2015-02-20 2016-08-25 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
UY36741A (es) 2015-06-21 2016-12-30 Prevacus Inc Compuesto de esteroide c-20, sus composiciones y usos para tratar la lesión cerebral traumática (tbi), que incluye las conmociones cerebrales
CA2998134A1 (en) 2015-09-08 2017-03-16 Viewpoint Therapeutics, Inc. Compounds and formulations for treating ophthalmic diseases
EA036155B1 (ru) 2015-10-16 2020-10-06 Маринус Фармасьютикалс, Инк. Инъекционные составы нейростероида, содержащие наночастицы
EP3377070A4 (en) 2015-11-20 2019-07-10 Sage Therapeutics, Inc. COMPOUNDS AND METHOD FOR THEIR USE
KR102408399B1 (ko) 2016-03-08 2022-06-13 세이지 테라퓨틱스, 인크. 신경활성 스테로이드, 조성물, 및 그의 용도
US10226550B2 (en) 2016-03-11 2019-03-12 Brigham Young University Cationic steroidal antimicrobial compositions for the treatment of dermal tissue
US11396525B2 (en) 2016-07-11 2022-07-26 Sage Therapeutics, Inc. C17, C20, and C21 substituted neuroactive steroids and their methods of use
AU2017296295B2 (en) 2016-07-11 2022-02-24 Sage Therapeutics, Inc. C7, C12, and C16 substituted neuroactive steroids and their methods of use
PE20190915A1 (es) 2016-08-23 2019-06-26 Sage Therapeutics Inc Un esteroide 19-nor-c21-n-pirazolilo c3,3-disustituido cristalino
US10391105B2 (en) 2016-09-09 2019-08-27 Marinus Pharmaceuticals Inc. Methods of treating certain depressive disorders and delirium tremens
CN108727453A (zh) 2017-04-20 2018-11-02 华东理工大学 新型pd-1抑制剂及其应用
WO2019018119A1 (en) 2017-07-18 2019-01-24 Pairnomix, Llc METHODS FOR TREATING EPILEPSY AND DISORDERS ASSOCIATED WITH KCNTI
CN111065394B (zh) 2017-08-31 2023-03-31 武田药品工业株式会社 中枢神经系统病症的治疗
IL303250A (en) 2017-09-07 2023-07-01 Sage Therapeutics Inc Neuroactive steroids and methods of using them
CA3079259A1 (en) 2017-11-10 2019-05-16 Marinus Pharmaceuticals, Inc. Ganaxolone for use in treating genetic epileptic disorders
WO2019211668A2 (en) 2018-05-04 2019-11-07 Acerus Pharmaceuticals Corporation Neurosteroid derivatives and uses thereof

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AU2018278844B2 (en) 2020-07-16

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