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
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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
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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 UCSD
Original Assignee
University of California San Diego UCSD
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 UCSD filed Critical University of California San Diego UCSD
Publication of CA2843436A1 publication Critical patent/CA2843436A1/en
Abandoned legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0044Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal 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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AU2012304412A1 (en) 2011-09-08 2014-03-27 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
PT2766380T (pt) 2011-10-14 2019-07-29 Sage Therapeutics Inc Compostos de 19-nor pregnano 3,3-dissubstituídos, composições e seus usos
RS59734B1 (sr) 2012-01-23 2020-02-28 Sage Therapeutics Inc Formulacije neuroaktivnog steroida koje uključuju kompleks alopregnanolona i sulfobutil etar beta-ciklodekstrina
EP2887944B1 (en) 2012-08-21 2021-10-06 Sage Therapeutics, Inc. Allopregnanolone for treating refractory status epilepticus
EP2925327B1 (en) 2012-11-30 2024-01-10 The Regents of The University of California Allopregnanolone for treating, reducing or mitigating symptoms of post-partum depression
PT2968369T (pt) 2013-03-13 2018-12-05 Sage Therapeutics Inc Esteroides neuroativos e métodos para o seu uso
KR102614507B1 (ko) 2013-04-17 2023-12-19 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
PL2986624T3 (pl) 2013-04-17 2020-11-16 Sage Therapeutics, Inc. Neuroaktywne steroidy 19-NOR do stosowania w sposobach leczenia
WO2014169831A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21-c-bound heteroaryl steroids and methods of use thereof
CA3199003A1 (en) 2013-07-19 2015-01-22 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
HUE052308T2 (hu) 2013-08-23 2021-04-28 Sage Therapeutics Inc Neuroaktív szteroidok, készítmények és alkalmazásuk
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
WO2015195967A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
WO2016036724A1 (en) 2014-09-02 2016-03-10 The Texas A&M University System Method of treating organophosphate intoxication
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
EP3206493B1 (en) 2014-10-16 2020-05-06 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
CN117024502A (zh) 2014-10-16 2023-11-10 萨奇治疗股份有限公司 靶向cns障碍的组合物和方法
EP3719029A1 (en) 2014-11-27 2020-10-07 Sage Therapeutics, Inc. Compositions for inducing sedation
ES2857082T3 (es) 2015-01-26 2021-09-28 Sage Therapeutics Inc Composiciones y métodos para el tratamiento de trastornos del SNC
JP6875996B2 (ja) 2015-02-20 2021-05-26 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、組成物、およびその使用
CN113292623A (zh) 2015-07-06 2021-08-24 萨奇治疗股份有限公司 孕甾醇及其使用方法
EP3319610A4 (en) 2015-07-06 2019-03-06 Sage Therapeutics, Inc. OXYSTEROLS AND METHOD OF USE THEREOF
PT3319612T (pt) 2015-07-06 2021-08-24 Sage Therapeutics Inc Oxisteróis e métodos de utilização dos mesmos
AU2017229656B2 (en) 2016-03-08 2022-09-29 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
US10752653B2 (en) 2016-05-06 2020-08-25 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
ES2884071T3 (es) 2016-07-07 2021-12-10 Sage Therapeutics Inc 24-hidroxiesteroles sustituidos en 11 para el tratamiento de afecciones relacionadas con NMDA
AU2017296295B2 (en) 2016-07-11 2022-02-24 Sage Therapeutics, Inc. C7, C12, and C16 substituted neuroactive steroids and their methods of use
MA45599A (fr) 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
KR20230079470A (ko) 2016-08-23 2023-06-07 세이지 테라퓨틱스, 인크. 결정질 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드
ES2935057T3 (es) 2016-09-30 2023-03-01 Sage Therapeutics Inc C7 oxisteroles sustituidos y estos compuestos para su uso como moduladores de la NMDA
EP4105223B1 (en) 2016-10-18 2025-04-30 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
BR112019008032A2 (pt) 2016-10-18 2019-09-03 Sage Therapeutics, Inc. oxiesteróis e métodos de uso dos mesmos
CN114805462B (zh) * 2018-02-11 2024-06-18 江苏豪森药业集团有限公司 一种甾族类衍生物调节剂及其制备方法和应用
AU2019217320B2 (en) * 2018-02-11 2023-12-21 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Steroid derivative regulators, method for preparing the same, and uses thereof
WO2020243488A1 (en) 2019-05-31 2020-12-03 Sage Therapeutics, Inc. Neuroactive steroids and compositions thereof
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
PL185523B1 (pl) * 1995-06-06 2003-05-30 Cocensys Inc Neuroaktywne steroidy z grupy pochodnych androstanu i pregnanu oraz kompozycja farmaceutyczna
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
US20090209504A1 (en) * 2006-03-23 2009-08-20 Yissum Research Development Company Of The Hebrew University Of Jerusalem Use of Digitalis-Like Compounds in the Treatment of Affective Disorders

Also Published As

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

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20170801