BR112021009428A2 - Esteroides neuroativos substituídos na posição 10 por um grupo cíclico para uso no tratamento de distúrbios do cns - Google Patents

Esteroides neuroativos substituídos na posição 10 por um grupo cíclico para uso no tratamento de distúrbios do cns Download PDF

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Publication number
BR112021009428A2
BR112021009428A2 BR112021009428-8A BR112021009428A BR112021009428A2 BR 112021009428 A2 BR112021009428 A2 BR 112021009428A2 BR 112021009428 A BR112021009428 A BR 112021009428A BR 112021009428 A2 BR112021009428 A2 BR 112021009428A2
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BR
Brazil
Prior art keywords
substituted
unsubstituted
alkyl
compound according
compound
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BR112021009428-8A
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English (en)
Portuguese (pt)
Inventor
Maria Jesus Blanco-Pillado
Francesco G. Salituro
Marshall Lee Morningstar
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Sage Therapeutics, Inc.
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Publication date
Application filed by Sage Therapeutics, Inc. filed Critical Sage Therapeutics, Inc.
Publication of BR112021009428A2 publication Critical patent/BR112021009428A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00Anaesthetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001Normal 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
    • C07J7/0015Normal 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
    • C07J7/002Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0011Androstane derivatives substituted in position 17 by a keto group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J13/00Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007Normal 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)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005Ketals
    • C07J21/008Ketals at position 17
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/0065Normal 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
    • C07J7/007Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0085Normal 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
BR112021009428-8A 2018-10-12 2019-10-11 Esteroides neuroativos substituídos na posição 10 por um grupo cíclico para uso no tratamento de distúrbios do cns BR112021009428A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862745109P 2018-10-12 2018-10-12
US62/745,109 2018-10-12
PCT/US2019/055926 WO2020077255A1 (en) 2018-10-12 2019-10-11 Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders

Publications (1)

Publication Number Publication Date
BR112021009428A2 true BR112021009428A2 (pt) 2021-08-31

Family

ID=68425315

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021009428-8A BR112021009428A2 (pt) 2018-10-12 2019-10-11 Esteroides neuroativos substituídos na posição 10 por um grupo cíclico para uso no tratamento de distúrbios do cns

Country Status (14)

Country Link
US (2) US11634453B2 (https=)
EP (2) EP4321519B1 (https=)
JP (2) JP7671244B2 (https=)
CN (2) CN113166193B (https=)
AR (1) AR116695A1 (https=)
AU (2) AU2019357040B2 (https=)
BR (1) BR112021009428A2 (https=)
CA (1) CA3115805A1 (https=)
DK (1) DK3864022T3 (https=)
ES (1) ES2966055T3 (https=)
IL (1) IL282183A (https=)
MX (2) MX2021004159A (https=)
TW (2) TWI835884B (https=)
WO (1) WO2020077255A1 (https=)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10201606063RA (en) 2012-01-23 2016-09-29 Sage Therapeutics Inc Neuroactive steroid formulations and methods of treating cns disorders
MX2015002252A (es) 2012-08-21 2015-07-21 Sage Therapeutics Inc Metodos para tratar epilepsia o estado de epilepsia.
JP6470258B2 (ja) 2013-04-17 2019-02-13 セージ セラピューティクス, インコーポレイテッド 19−ノルc3,3−ジ置換c21−n−ピラゾリルステロイドおよびその使用方法
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
WO2016082789A1 (en) 2014-11-27 2016-06-02 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
TWI904593B (zh) 2016-08-23 2025-11-11 美商賽吉醫療公司 結晶19-去甲c3,3-二取代之c21-n-吡唑類固醇
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
CN113166193B (zh) * 2018-10-12 2025-08-19 萨奇治疗股份有限公司 用于治疗cns病症的在位置10处被环状基团取代的神经活性类固醇

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
KR100338287B1 (ko) * 1994-02-14 2002-11-30 푸르듀 파머 리미티드 감마-아미노부티르산a수용체의알로오스테리조절용안드로스탄및프레그난
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
FI972202L (fi) 1994-11-23 1997-07-17 Cocensys Inc Androstaanit ja pregnaanit GABA-reseptoreiden allosteeriseen muunteluun
MX365644B (es) 2012-12-18 2019-06-10 Univ Washington Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos.
US10577390B2 (en) * 2014-10-16 2020-03-03 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
CN111741965B (zh) 2017-12-22 2024-06-25 萨奇治疗股份有限公司 治疗中枢神经系统疾病的组合物和方法
EP3728284B1 (en) 2017-12-22 2024-08-21 Sage Therapeutics, Inc. 19-homo, 3.alpha.-hydroxy-steroid-20-one compounds for treating cns disorders
CN114656514B (zh) 2018-02-11 2024-05-14 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
CN113166193B (zh) * 2018-10-12 2025-08-19 萨奇治疗股份有限公司 用于治疗cns病症的在位置10处被环状基团取代的神经活性类固醇
AU2020304673A1 (en) * 2019-06-27 2022-01-20 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
US20230257415A1 (en) 2019-06-27 2023-08-17 Sage Therapeutics, Inc. Compounds for treating cns disorders
TW202143976A (zh) 2020-03-18 2021-12-01 美商賽吉醫療公司 神經活性類固醇及其使用方法
IL299176A (en) 2020-06-24 2023-02-01 Sage Therapeutics Inc 3.alpha.-hydroxy, 17.beta.-c(o)-n-aryl substituted neuroactive steroids and compositions thereof

Also Published As

Publication number Publication date
EP4321519A3 (en) 2024-05-01
TW202448479A (zh) 2024-12-16
EP3864022A1 (en) 2021-08-18
IL282183A (en) 2021-05-31
US20210340172A1 (en) 2021-11-04
US20240051987A1 (en) 2024-02-15
CN113166193A (zh) 2021-07-23
ES2966055T3 (es) 2024-04-18
EP4321519A2 (en) 2024-02-14
JP7671244B2 (ja) 2025-05-01
CN113166193B (zh) 2025-08-19
DK3864022T3 (da) 2023-12-18
JP2022504607A (ja) 2022-01-13
WO2020077255A1 (en) 2020-04-16
JP2024040444A (ja) 2024-03-25
MX2021004159A (es) 2021-09-08
US11634453B2 (en) 2023-04-25
AR116695A1 (es) 2021-06-02
AU2025200422A1 (en) 2025-02-13
US20240376144A9 (en) 2024-11-14
AU2019357040A1 (en) 2021-05-20
TWI835884B (zh) 2024-03-21
CA3115805A1 (en) 2020-04-16
EP4321519B1 (en) 2026-04-08
TWI886813B (zh) 2025-06-11
TW202027753A (zh) 2020-08-01
CN121045302A (zh) 2025-12-02
AU2019357040B2 (en) 2025-03-27
EP3864022B1 (en) 2023-09-20
MX2024011494A (es) 2024-09-26

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