CA2843436A1 - Novel 17.beta.-heteroaryl-substituted steroids as modulators of gaba a receptors - Google Patents

Novel 17.beta.-heteroaryl-substituted steroids as modulators of gaba a receptors Download PDF

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Publication number
CA2843436A1
CA2843436A1 CA2843436A CA2843436A CA2843436A1 CA 2843436 A1 CA2843436 A1 CA 2843436A1 CA 2843436 A CA2843436 A CA 2843436A CA 2843436 A CA2843436 A CA 2843436A CA 2843436 A1 CA2843436 A1 CA 2843436A1
Authority
CA
Canada
Prior art keywords
alkyl
heterocycloalkyl
hydrogen
alkenyl
alkynyl
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.)
Abandoned
Application number
CA2843436A
Other languages
English (en)
French (fr)
Inventor
Derk J. Hogenkamp
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.)
University of California, San Diego
Original Assignee
University of California, San Diego
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 University of California, San Diego filed Critical University of California, San Diego
Publication of CA2843436A1 publication Critical patent/CA2843436A1/en
Abandoned legal-status Critical Current

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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
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07J41/0044—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
CA2843436A 2011-07-29 2012-07-30 Novel 17.beta.-heteroaryl-substituted steroids as modulators of gaba a receptors Abandoned CA2843436A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161513059P 2011-07-29 2011-07-29
US61/513,059 2011-07-29
PCT/US2012/048816 WO2013019711A2 (en) 2011-07-29 2012-07-30 NOVEL 17β-HETEROARYL-SUBSTITUTED STEROIDS AS MODULATORS OF GABAA RECEPTORS

Publications (1)

Publication Number Publication Date
CA2843436A1 true CA2843436A1 (en) 2013-02-07

Family

ID=47629869

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2843436A Abandoned CA2843436A1 (en) 2011-07-29 2012-07-30 Novel 17.beta.-heteroaryl-substituted steroids as modulators of gaba a receptors

Country Status (5)

Country Link
US (1) US20140148412A1 (enExample)
EP (1) EP2736919A4 (enExample)
JP (1) JP2014521662A (enExample)
CA (1) CA2843436A1 (enExample)
WO (1) WO2013019711A2 (enExample)

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EP4717314A2 (en) 2011-10-14 2026-04-01 Sage Therapeutics, LLC 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
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
US20150313915A1 (en) 2012-11-30 2015-11-05 The Regents Of The University Of California Anticonvulsant activity of steroids
FI3932932T3 (fi) 2013-03-13 2025-10-15 Sage Therapeutics Inc Neuroaktiivisia steroideja ja niiden käyttömenetelmiä
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
CN117304245A (zh) 2013-04-17 2023-12-29 萨奇治疗股份有限公司 刺激神经活性的19-去甲类固醇及其使用方法
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
US9725481B2 (en) 2013-04-17 2017-08-08 Sage Therapeutics, Inc. 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof
CA2918735C (en) 2013-07-19 2023-08-01 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
CN105579043B (zh) 2013-08-23 2021-09-14 萨奇治疗股份有限公司 神经活性类固醇、组合物和其用途
JP6628745B2 (ja) 2014-06-18 2020-01-15 セージ セラピューティクス， インコーポレイテッド オキシステロールおよびその使用方法
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
MA40498A (fr) 2014-09-02 2021-05-19 Texas A & M Univ Sys Méthode de traitement de l'intoxication par organophosphates
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
MY190408A (en) 2014-10-16 2022-04-21 Sage Therapeutics Inc Compositions and methods for treating cns disorders
US20170233433A1 (en) 2014-10-16 2017-08-17 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
WO2016082789A1 (en) 2014-11-27 2016-06-02 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
LT3250210T (lt) * 2015-01-26 2021-04-12 Sage Therapeutics, Inc. Kompozicijos ir būdai, skirti gydyti cns sutrikimus
DK3258939T3 (da) 2015-02-20 2022-12-12 Sage Therapeutics Inc Neuroaktive steroider, sammensætninger og anvendelser heraf
WO2017007832A1 (en) 2015-07-06 2017-01-12 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
PT3319611T (pt) 2015-07-06 2021-04-22 Sage Therapeutics Inc Oxisteróis e métodos de utilização dos mesmos
DK3812392T3 (da) 2015-07-06 2025-07-21 Sage Therapeutics Inc Oxysteroler og fremgangsmåder til anvendelse deraf
PH12018501923B1 (en) 2016-03-08 2024-06-28 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof
ES2921010T3 (es) 2016-04-01 2022-08-16 Sage Therapeutics Inc Oxisteroles y procedimientos de uso de los mismos
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
WO2018009867A1 (en) 2016-07-07 2018-01-11 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
CA3030420C (en) 2016-07-11 2025-11-18 Sage Therapeutics, Inc. C7, C12 AND C16 SUBSTITUTED NEUROACTIVE STEROIDS AND ASSOCIATED METHODS OF USE
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
MA46351A (fr) 2016-09-30 2021-06-02 Sage Therapeutics Inc Oxystérols substitués en c7 et procédés en tant que modulateurs nmda
KR102521573B1 (ko) 2016-10-18 2023-04-14 세이지 테라퓨틱스, 인크. 옥시스테롤 및 그의 사용 방법
DK3529257T3 (da) 2016-10-18 2023-08-07 Sage Therapeutics Inc Oxysteroler og fremgangsmåder til anvendelse deraf
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
MX2020008182A (es) * 2018-02-11 2020-09-22 Jiangsu Hansoh Pharmaceutical Group Co Ltd Reguladores de derivados esteroides, metodo para prepararlos y usos de los mismos.
JP7670626B2 (ja) 2019-05-31 2025-04-30 セージ セラピューティクス， インコーポレイテッド 神経刺激性ステロイド及びその組成物
AU2021238346A1 (en) 2020-03-18 2022-09-29 Sage Therapeutics, Inc. Neuroactive steroids and their methods of use
US12215126B2 (en) * 2020-05-21 2025-02-04 Brigham Young University Cationic steroidal antimicrobial compounds with endogenous groups
WO2023060067A1 (en) 2021-10-04 2023-04-13 Marinus Pharmaceuticals, Inc. Amorphous solid dispersion ganaxolone formulation

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US3313809A (en) * 1965-03-05 1967-04-11 Sterling Drug Inc Steroido[21, 20-d]isoxazoles
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
AU3967297A (en) * 1996-08-01 1998-02-25 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
DE602007010595D1 (de) * 2006-03-23 2010-12-30 Yissum Res Dev Co Verwendung von digitalis-artigen verbindungen bei der behandlung von affektiven störungen

Also Published As

Publication number Publication date
US20140148412A1 (en) 2014-05-29
JP2014521662A (ja) 2014-08-28
EP2736919A2 (en) 2014-06-04
WO2013019711A3 (en) 2013-04-04
WO2013019711A2 (en) 2013-02-07
EP2736919A4 (en) 2015-01-14

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20170801