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
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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)
  • 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)
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) EP3864022B1 (enExample)
JP (3) JP7671244B2 (enExample)
CN (2) CN113166193B (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) TWI886813B (enExample)
WO (1) WO2020077255A1 (enExample)

Families Citing this family (10)

* 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
RS62761B1 (sr) 2012-08-21 2022-01-31 Sage Therapeutics Inc Alopregnanolon za lečenje refraktornog epileptičkog statusa
SMT202100509T1 (it) 2013-04-17 2021-11-12 Sage Therapeutics Inc Steroide di c21-n-pirazolile 19-nor c3,3-disostituito per l'uso in terapia
US10246482B2 (en) 2014-06-18 2019-04-02 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
WO2018013613A1 (en) 2016-07-11 2018-01-18 Sage Therapeutics, Inc. C17, c20, and c21 substituted neuroactive steroids and their methods of use
TW202604538A (zh) 2016-08-23 2026-02-01 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
US20200291059A1 (en) 2017-12-08 2020-09-17 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
AU2019357040B2 (en) 2018-10-12 2025-03-27 Sage Therapeutics, Inc. Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders

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 (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
DK1038880T3 (da) * 1994-02-14 2008-03-03 Euro Celtique Sa Androstaner og pregnaner til allosterisk modulering af GABA-receptor
BR9509764A (pt) 1994-11-23 1998-07-07 Cocensys Inc Série androstano e pregnano para modulação alostérica de receptor de gaba
PT837874E (pt) 1995-06-06 2005-03-31 Euro Celtique Sa Esteroides neuroactivos da serie androstano e pregnano
UA73736C2 (en) 1999-04-29 2005-09-15 Euro Celtic S A Method for alleviating or preventing insomnia and inducing anesthesia
DK2935307T3 (en) 2012-12-18 2018-07-30 Univ Washington NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS USED IN METHODS OF TREATMENT
CA3086299A1 (en) 2017-12-22 2019-06-27 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
EP3728285B1 (en) 2017-12-22 2026-04-08 Sage Therapeutics, LLC Compositions and methods for treating cns disorders
US12139508B2 (en) 2018-02-11 2024-11-12 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Steroid derivative regulators, method for preparing the same, and uses thereof
AU2019357040B2 (en) 2018-10-12 2025-03-27 Sage Therapeutics, Inc. Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of CNS disorders
CA3143545A1 (en) 2019-06-27 2020-12-30 Sage Therapeutics, Inc. Compounds for treating cns disorders
BR112021026447A2 (pt) * 2019-06-27 2022-04-12 Sage Therapeutics Inc Composições e métodos para tratamento de distúrbios de cns
AU2021238346A1 (en) 2020-03-18 2022-09-29 Sage Therapeutics, Inc. Neuroactive steroids and their methods of use
CN115768781A (zh) 2020-06-24 2023-03-07 萨奇治疗股份有限公司 3.α.-羟基,17.β.-C(O)-N-芳基取代的神经活性类固醇及其组合物

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
IL282183A (en) 2021-05-31
US20240376144A9 (en) 2024-11-14
AU2019357040A1 (en) 2021-05-20
CN113166193B (zh) 2025-08-19
CA3115805A1 (en) 2020-04-16
TWI886813B (zh) 2025-06-11
TW202448479A (zh) 2024-12-16
JP7899241B2 (ja) 2026-08-03
ES2966055T3 (es) 2024-04-18
BR112021009428A2 (pt) 2021-08-31
EP4321519A2 (en) 2024-02-14
JP2022504607A (ja) 2022-01-13
TWI835884B (zh) 2024-03-21
CN113166193A (zh) 2021-07-23
CN121045302A (zh) 2025-12-02
US20210340172A1 (en) 2021-11-04
EP4321519B1 (en) 2026-04-08
JP2026126430A (ja) 2026-08-04
EP3864022B1 (en) 2023-09-20
JP7671244B2 (ja) 2025-05-01
US20240051987A1 (en) 2024-02-15
DK3864022T3 (da) 2023-12-18
WO2020077255A1 (en) 2020-04-16
EP4321519A3 (en) 2024-05-01
MX2024011494A (es) 2024-09-26
AU2025200422A1 (en) 2025-02-13
US11634453B2 (en) 2023-04-25
JP2024040444A (ja) 2024-03-25
MX2021004159A (es) 2021-09-08
US12686700B2 (en) 2026-07-21
AR116695A1 (es) 2021-06-02
TW202027753A (zh) 2020-08-01
EP3864022A1 (en) 2021-08-18

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