JP7692830B2 - ３α－ヒドロキシ－１７β－アミド神経刺激性ステロイドおよびその組成物 - Google Patents

３α－ヒドロキシ－１７β－アミド神経刺激性ステロイドおよびその組成物 Download PDF

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Publication number
JP7692830B2
JP7692830B2 JP2021535679A JP2021535679A JP7692830B2 JP 7692830 B2 JP7692830 B2 JP 7692830B2 JP 2021535679 A JP2021535679 A JP 2021535679A JP 2021535679 A JP2021535679 A JP 2021535679A JP 7692830 B2 JP7692830 B2 JP 7692830B2
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hydrogen
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JP2022514385A5 (https=
JP2022514385A (ja
JPWO2020132504A5 (https=
Inventor
マリア ヘスス ブランコ－ピヤド，
フランセスコ ジー． サリトゥロ，
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Sage Therapeutics LLC
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Sage Therapeutics LLC
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Priority to JP2024094279A priority Critical patent/JP2024107296A/ja
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    • 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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • 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
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • 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
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/008—Ketals at position 17
    • 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
    • C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0066—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by a carbon atom forming part of an amide group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Toxicology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2021535679A 2018-12-21 2019-12-20 ３α－ヒドロキシ－１７β－アミド神経刺激性ステロイドおよびその組成物 Active JP7692830B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024094279A JP2024107296A (ja) 2018-12-21 2024-06-11 ３α－ヒドロキシ－１７β－アミド神経刺激性ステロイドおよびその組成物

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862784222P 2018-12-21 2018-12-21
US201862784229P 2018-12-21 2018-12-21
US62/784,222 2018-12-21
US62/784,229 2018-12-21
PCT/US2019/067953 WO2020132504A1 (en) 2018-12-21 2019-12-20 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2024094279A Division JP2024107296A (ja) 2018-12-21 2024-06-11 ３α－ヒドロキシ－１７β－アミド神経刺激性ステロイドおよびその組成物

Publications (4)

Publication Number Publication Date
JP2022514385A JP2022514385A (ja) 2022-02-10
JP2022514385A5 JP2022514385A5 (https=) 2022-11-18
JPWO2020132504A5 JPWO2020132504A5 (https=) 2022-11-18
JP7692830B2 true JP7692830B2 (ja) 2025-06-16

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JP2021535679A Active JP7692830B2 (ja) 2018-12-21 2019-12-20 ３α－ヒドロキシ－１７β－アミド神経刺激性ステロイドおよびその組成物
JP2024094279A Pending JP2024107296A (ja) 2018-12-21 2024-06-11 ３α－ヒドロキシ－１７β－アミド神経刺激性ステロイドおよびその組成物

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JP2024094279A Pending JP2024107296A (ja) 2018-12-21 2024-06-11 ３α－ヒドロキシ－１７β－アミド神経刺激性ステロイドおよびその組成物

Country Status (12)

Country Link
US (1) US20220372067A1 (https=)
EP (1) EP3898646B1 (https=)
JP (2) JP7692830B2 (https=)
KR (1) KR20210107050A (https=)
CN (1) CN113195512A (https=)
AU (2) AU2019403415B2 (https=)
BR (1) BR112021012242A2 (https=)
CA (1) CA3124371A1 (https=)
IL (1) IL284183A (https=)
MX (2) MX2021007504A (https=)
TW (2) TWI848034B (https=)
WO (1) WO2020132504A1 (https=)

Families Citing this family (12)

* 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
IL283629B2 (en) 2018-12-05 2026-03-01 Sage Therapeutics Inc Neuroactive steroids and methods of using them
CN113195512A (zh) * 2018-12-21 2021-07-30 萨奇治疗股份有限公司 3.α.-羟基-17.β.-酰胺神经活性类固醇及其组合物
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
CN119192275B (zh) * 2024-08-22 2025-05-30 湖南玉新药业有限公司 一种3-羰基-4-氮杂-5α-雄甾-17β-羧酸化合物的制备方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018013613A1 (en) 2016-07-11 2018-01-18 Sage Therapeutics, Inc. C17, c20, and c21 substituted neuroactive steroids and their methods of use

Family Cites Families (7)

* 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
CN119192266A (zh) 2011-10-14 2024-12-27 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
US9512170B2 (en) * 2013-03-01 2016-12-06 Washington University Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors
US10577390B2 (en) * 2014-10-16 2020-03-03 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
EP4155314A1 (en) * 2015-02-20 2023-03-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
IL283629B2 (en) * 2018-12-05 2026-03-01 Sage Therapeutics Inc Neuroactive steroids and methods of using them
CN113195512A (zh) * 2018-12-21 2021-07-30 萨奇治疗股份有限公司 3.α.-羟基-17.β.-酰胺神经活性类固醇及其组合物

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018013613A1 (en) 2016-07-11 2018-01-18 Sage Therapeutics, Inc. C17, c20, and c21 substituted neuroactive steroids and their methods of use

Also Published As

Publication number Publication date
US20220372067A1 (en) 2022-11-24
EP3898646A1 (en) 2021-10-27
TWI892697B (zh) 2025-08-01
MX2021007504A (es) 2021-10-13
WO2020132504A1 (en) 2020-06-25
TWI848034B (zh) 2024-07-11
KR20210107050A (ko) 2021-08-31
AU2025267433A1 (en) 2025-12-04
EP3898646B1 (en) 2026-02-18
JP2024107296A (ja) 2024-08-08
JP2022514385A (ja) 2022-02-10
IL284183A (en) 2021-08-31
TW202438080A (zh) 2024-10-01
MX2025000126A (es) 2025-02-10
TW202038967A (zh) 2020-11-01
AU2019403415A1 (en) 2021-07-08
BR112021012242A2 (pt) 2021-09-28
AU2019403415B2 (en) 2025-08-21
CN113195512A (zh) 2021-07-30
CA3124371A1 (en) 2020-06-25

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