CN113166193B - 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 - Google Patents

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

Info

Publication number
CN113166193B
CN113166193B CN201980079330.5A CN201980079330A CN113166193B CN 113166193 B CN113166193 B CN 113166193B CN 201980079330 A CN201980079330 A CN 201980079330A CN 113166193 B CN113166193 B CN 113166193B
Authority
CN
China
Prior art keywords
compound
substituted
disorder
unsubstituted
pharmaceutically acceptable
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CN201980079330.5A
Other languages
English (en)
Chinese (zh)
Other versions
CN113166193A (zh
Inventor
M.J.布兰科-皮拉多
F.G.萨利图罗
M.L.莫宁斯塔
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
Priority to CN202511082220.8A priority Critical patent/CN121045302A/zh
Publication of CN113166193A publication Critical patent/CN113166193A/zh
Application granted granted Critical
Publication of CN113166193B publication Critical patent/CN113166193B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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)
CN201980079330.5A 2018-10-12 2019-10-11 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 Active CN113166193B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202511082220.8A CN121045302A (zh) 2018-10-12 2019-10-11 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

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
CN202511082220.8A Division CN121045302A (zh) 2018-10-12 2019-10-11 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

Publications (2)

Publication Number Publication Date
CN113166193A CN113166193A (zh) 2021-07-23
CN113166193B true CN113166193B (zh) 2025-08-19

Family

ID=68425315

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201980079330.5A Active CN113166193B (zh) 2018-10-12 2019-10-11 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
CN202511082220.8A Pending CN121045302A (zh) 2018-10-12 2019-10-11 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 Applications After (1)

Application Number Title Priority Date Filing Date
CN202511082220.8A Pending CN121045302A (zh) 2018-10-12 2019-10-11 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

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
CN107404877A (zh) * 2014-10-16 2017-11-28 萨奇治疗股份有限公司 靶向cns 障碍的组合物和方法

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
CN107404877A (zh) * 2014-10-16 2017-11-28 萨奇治疗股份有限公司 靶向cns 障碍的组合物和方法

Also Published As

Publication number Publication date
IL282183A (en) 2021-05-31
US20240376144A9 (en) 2024-11-14
AU2019357040A1 (en) 2021-05-20
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
AU2019357040B2 (en) 2025-03-27
TW202027753A (zh) 2020-08-01
EP3864022A1 (en) 2021-08-18

Similar Documents

Publication Publication Date Title
AU2022200247B2 (en) C7, C12, and C16 substituted neuroactive steroids and their methods of use
US11147877B2 (en) Compositions and methods for treating CNS disorders
CN113227114B (zh) 9(11)-不饱和神经活性类固醇及其使用方法
JP6875996B2 (ja) 神経刺激性ステロイド、組成物、およびその使用
JP2024114787A (ja) Ｃ１７、ｃ２０、およびｃ２１置換神経刺激性ステロイドおよびそれらの使用方法
CN121045302A (zh) 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
JP2021506890A (ja) Ｃｎｓ障害の処置のための組成物および方法
RU2796006C2 (ru) Нейроактивные стероиды, замещенные в положении 10 циклической группой, для использования при лечении расстройств цнс
HK40106568A (en) Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders
RU2828261C2 (ru) С17-, с20- и с21-замещенные нейроактивные стероиды и способы их применения
HK40059417B (en) Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders
HK40059417A (en) Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders
BR112019000578B1 (pt) Compostos esteróides neuroativos c17, c20 e c21 substituídos, suas composições farmacêuticas e seus usos
BR122022005119B1 (pt) Compostos esteróides neuroativos c17, c20 e c21 substituídos, suas composições farmacêuticas, seus usos e kits
HK1242201B (en) Compositions and methods for treating cns disorders

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant