AU2019357040B2 - Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders - Google Patents

Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders Download PDF

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Publication number
AU2019357040B2
AU2019357040B2 AU2019357040A AU2019357040A AU2019357040B2 AU 2019357040 B2 AU2019357040 B2 AU 2019357040B2 AU 2019357040 A AU2019357040 A AU 2019357040A AU 2019357040 A AU2019357040 A AU 2019357040A AU 2019357040 B2 AU2019357040 B2 AU 2019357040B2
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AU
Australia
Prior art keywords
substituted
unsubstituted
alkyl
compound
independently hydrogen
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Active
Application number
AU2019357040A
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English (en)
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AU2019357040A1 (en
Inventor
Maria Jesus Blanco-Pillado
Marshall Lee Morningstar
Francesco G. Salituro
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sage Therapeutics Inc
Original Assignee
Sage Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Publication of AU2019357040A1 publication Critical patent/AU2019357040A1/en
Priority to AU2025200422A priority Critical patent/AU2025200422A1/en
Application granted granted Critical
Publication of AU2019357040B2 publication Critical patent/AU2019357040B2/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • 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
    • A61P25/22—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
    • A61P25/24—Antidepressants
    • 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
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Neurology (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)
AU2019357040A 2018-10-12 2019-10-11 Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders Active AU2019357040B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2025200422A AU2025200422A1 (en) 2018-10-12 2025-01-22 Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2025200422A Division AU2025200422A1 (en) 2018-10-12 2025-01-22 Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders

Publications (2)

Publication Number Publication Date
AU2019357040A1 AU2019357040A1 (en) 2021-05-20
AU2019357040B2 true AU2019357040B2 (en) 2025-03-27

Family

ID=68425315

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2019357040A Active AU2019357040B2 (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
AU2025200422A Pending AU2025200422A1 (en) 2018-10-12 2025-01-22 Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2025200422A Pending AU2025200422A1 (en) 2018-10-12 2025-01-22 Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders

Country Status (14)

Country Link
US (2) US11634453B2 (enExample)
EP (2) EP4321519B1 (enExample)
JP (2) JP7671244B2 (enExample)
CN (2) CN121045302A (enExample)
AR (1) AR116695A1 (enExample)
AU (2) AU2019357040B2 (enExample)
BR (1) BR112021009428A2 (enExample)
CA (1) CA3115805A1 (enExample)
DK (1) DK3864022T3 (enExample)
ES (1) ES2966055T3 (enExample)
IL (1) IL282183A (enExample)
MX (2) MX2021004159A (enExample)
TW (2) TWI835884B (enExample)
WO (1) WO2020077255A1 (enExample)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SMT202000008T1 (it) 2012-01-23 2020-03-13 Sage Therapeutics Inc Formulazione di steroide neuroattivo comprendente un complesso di allopregnanolone e solfobutil eter beta-ciclodestrina
PL2887944T3 (pl) 2012-08-21 2022-02-21 Sage Therapeutics, Inc. Allopregnanolon do leczenia lekoopornego stanu padaczkowego
CN113527400B (zh) 2013-04-17 2024-06-28 萨奇治疗股份有限公司 19-去甲c3,3-二取代的c21-n-吡唑基类固醇及其使用方法
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
ME03749B (me) 2014-11-27 2021-04-20 Sage Therapeutics Inc KOMPOZICIJE I POSTUPCIZA LEČENJE POREMEĆAJA CNS-a
CN115974956A (zh) 2016-08-23 2023-04-18 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
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
DK3864022T3 (da) * 2018-10-12 2023-12-18 Sage Therapeutics Inc Neuroaktive steroider substitueret i Position 10 med en cyklisk gruppe til anvendelse til behandlingen af CNS-lidelser

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
DK0752860T3 (da) * 1994-02-14 2000-11-13 Euro Celtique Sa Androstaner og pregnaner til allosterisk modulering af GABA-receptor
AP653A (en) 1994-11-23 1998-07-21 Cocensys Inc Androstane and pregnane series for allosteric modulations of gaba receptor.
TR201808616T4 (tr) 2012-12-18 2018-07-23 Sage Therapeutics Inc Nöroaktif 19-alkoksi-17-ikameli steroidler, bunların ön ilaçları ve bunları kullanan tedavi yöntemleri.
US20220315621A1 (en) 2017-12-22 2022-10-06 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
IL275562B2 (en) 2017-12-22 2024-07-01 Sage Therapeutics Inc Compositions and methods for treating cns disorders
KR102917075B1 (ko) 2018-02-11 2026-01-26 장쑤 한서 파마슈티칼 그룹 캄파니 리미티드 스테로이드 유도체 조절제, 그의 제조 방법 및 그의 용도
DK3864022T3 (da) * 2018-10-12 2023-12-18 Sage Therapeutics Inc Neuroaktive steroider substitueret i Position 10 med en cyklisk gruppe til anvendelse til behandlingen af CNS-lidelser
WO2020264495A1 (en) * 2019-06-27 2020-12-30 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
EP3990468A1 (en) 2019-06-27 2022-05-04 Sage Therapeutics, Inc. Compounds for treating cns disorders
IL296371A (en) 2020-03-18 2022-11-01 Sage Therapeutics Inc Neuroactive steroids and methods of using them
EP4172171A1 (en) 2020-06-24 2023-05-03 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
JP7671244B2 (ja) 2025-05-01
US20210340172A1 (en) 2021-11-04
EP4321519B1 (en) 2026-04-08
US20240051987A1 (en) 2024-02-15
US20240376144A9 (en) 2024-11-14
ES2966055T3 (es) 2024-04-18
IL282183A (en) 2021-05-31
WO2020077255A1 (en) 2020-04-16
DK3864022T3 (da) 2023-12-18
MX2021004159A (es) 2021-09-08
CN121045302A (zh) 2025-12-02
TW202448479A (zh) 2024-12-16
CA3115805A1 (en) 2020-04-16
AU2019357040A1 (en) 2021-05-20
EP3864022A1 (en) 2021-08-18
CN113166193B (zh) 2025-08-19
BR112021009428A2 (pt) 2021-08-31
AU2025200422A1 (en) 2025-02-13
JP2024040444A (ja) 2024-03-25
EP4321519A3 (en) 2024-05-01
TWI835884B (zh) 2024-03-21
EP3864022B1 (en) 2023-09-20
EP4321519A2 (en) 2024-02-14
TW202027753A (zh) 2020-08-01
US11634453B2 (en) 2023-04-25
AR116695A1 (es) 2021-06-02
JP2022504607A (ja) 2022-01-13
TWI886813B (zh) 2025-06-11
MX2024011494A (es) 2024-09-26
CN113166193A (zh) 2021-07-23

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