TWI835884B - 神經活性類固醇及其使用方法 - Google Patents

神經活性類固醇及其使用方法 Download PDF

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Publication number
TWI835884B
TWI835884B TW108136955A TW108136955A TWI835884B TW I835884 B TWI835884 B TW I835884B TW 108136955 A TW108136955 A TW 108136955A TW 108136955 A TW108136955 A TW 108136955A TW I835884 B TWI835884 B TW I835884B
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TW
Taiwan
Prior art keywords
substituted
unsubstituted
compound
disorder
pharmaceutically acceptable
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TW108136955A
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English (en)
Chinese (zh)
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TW202027753A (zh
Inventor
佩拉杜 馬利亞 耶稣 巴蘭可
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美商賽吉醫療公司
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Publication of TW202027753A publication Critical patent/TW202027753A/zh
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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)
TW108136955A 2018-10-12 2019-10-14 神經活性類固醇及其使用方法 TWI835884B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862745109P 2018-10-12 2018-10-12
US62/745,109 2018-10-12

Publications (2)

Publication Number Publication Date
TW202027753A TW202027753A (zh) 2020-08-01
TWI835884B true TWI835884B (zh) 2024-03-21

Family

ID=68425315

Family Applications (2)

Application Number Title Priority Date Filing Date
TW108136955A TWI835884B (zh) 2018-10-12 2019-10-14 神經活性類固醇及其使用方法
TW113106814A TWI886813B (zh) 2018-10-12 2019-10-14 神經活性類固醇及其使用方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW113106814A TWI886813B (zh) 2018-10-12 2019-10-14 神經活性類固醇及其使用方法

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

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2016061527A1 (en) * 2014-10-16 2016-04-21 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders

Family Cites Families (12)

* 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
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.
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

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2016061527A1 (en) * 2014-10-16 2016-04-21 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders

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
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
BR112021009428A2 (pt) 2021-08-31
MX2024011494A (es) 2024-09-26

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