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
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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 (https=)
EP (1) EP2736919A4 (https=)
JP (1) JP2014521662A (https=)
CA (1) CA2843436A1 (https=)
WO (1) WO2013019711A2 (https=)

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CN119192266A (zh) 2011-10-14 2024-12-27 萨奇治疗股份有限公司 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
SG10201606063RA (en) 2012-01-23 2016-09-29 Sage Therapeutics Inc Neuroactive steroid formulations and methods of treating cns disorders
MX2015002252A (es) 2012-08-21 2015-07-21 Sage Therapeutics Inc Metodos para tratar epilepsia o estado de epilepsia.
DK2925327T3 (da) 2012-11-30 2024-03-25 Univ California Allopregnanolon til behandling, reduktion eller lindring af symptomer på fødselsdepression
SMT201800657T1 (it) 2013-03-13 2019-01-11 Sage Therapeutics Inc Steroidi neuroattivi e loro metodi di utilizzo
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
JP6470258B2 (ja) 2013-04-17 2019-02-13 セージ セラピューティクス, インコーポレイテッド 19−ノルc3,3−ジ置換c21−n−ピラゾリルステロイドおよびその使用方法
ES2807264T3 (es) 2013-04-17 2021-02-22 Sage Therapeutics Inc Esteroides neuroactivos 19-nor para métodos de tratamiento
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
WO2015010054A2 (en) 2013-07-19 2015-01-22 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
ES2848823T3 (es) 2013-08-23 2021-08-12 Sage Therapeutics Inc Esteroides neuroactivos, composiciones y usos de los mismos
WO2015195967A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
WO2015195962A1 (en) 2014-06-18 2015-12-23 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
US10577390B2 (en) 2014-10-16 2020-03-03 Sage Therapeutics, Inc. Compositions and methods for treating CNS disorders
ME03809B (me) 2014-10-16 2021-04-20 Sage Therapeutics Inc KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a
WO2016082789A1 (en) 2014-11-27 2016-06-02 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
WO2016123056A1 (en) * 2015-01-26 2016-08-04 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
EP4155314A1 (en) 2015-02-20 2023-03-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
MX382122B (es) 2015-07-06 2025-03-13 Sage Therapeutics Inc Oxiesteroles y metodos de uso de los mismos.
AU2016289965B2 (en) 2015-07-06 2021-09-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
PL3319611T3 (pl) 2015-07-06 2021-07-12 Sage Therapeutics, Inc. Oksysterole i sposoby ich stosowania
HK1258616A1 (zh) * 2016-03-08 2019-11-15 Sage Therapeutics, Inc. 神经活性类固醇、组合物、及其用途
EP3436022B1 (en) 2016-04-01 2022-03-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US10752653B2 (en) 2016-05-06 2020-08-25 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
US20190233465A1 (en) 2016-07-11 2019-08-01 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
TWI904593B (zh) 2016-08-23 2025-11-11 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
PT3519422T (pt) 2016-09-30 2022-12-05 Sage Therapeutics Inc Oxisteróis substituídos em c7 e métodos como moduladores nmda
DK4105223T3 (da) 2016-10-18 2025-07-07 Sage Therapeutics Inc Oxysteroler og fremgangsmåder til anvendelse deraf
CA3041088C (en) 2016-10-18 2024-05-21 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
CN114656514B (zh) * 2018-02-11 2024-05-14 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
EP3750909B1 (en) * 2018-02-11 2025-03-05 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Steroid derivative regulators, method for preparing the same, and uses thereof
CR20240234A (es) 2019-05-31 2024-07-09 Sage Therapeutics Inc ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629)
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
FI972202L (fi) * 1994-11-23 1997-07-17 Cocensys Inc Androstaanit ja pregnaanit GABA-reseptoreiden allosteeriseen muunteluun
RU2194712C2 (ru) * 1995-06-06 2002-12-20 Коукенсис, Инк. НЕЙРОАКТИВНЫЕ СТЕРОИДЫ, ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ, СПОСОБ ЛЕЧЕНИЯ ИЛИ ПРОФИЛАКТИКИ РАЗЛИЧНЫХ НАРУШЕНИЙ, СПОСОБ ИНДУКЦИИ СНА И СПОСОБ ИНДУКЦИИ АНЕСТЕЗИИ С ИХ ИСПОЛЬЗОВАНИЕМ, СПОСОБ МОДУЛИРОВАНИЯ КОМПЛЕКСА РЕЦЕПТОР ГАМКa-ХЛОРИДНЫЙ ИОНОФОР
AU3967297A (en) * 1996-08-01 1998-02-25 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
EP2736919A4 (en) 2015-01-14
WO2013019711A3 (en) 2013-04-04
WO2013019711A2 (en) 2013-02-07
US20140148412A1 (en) 2014-05-29
JP2014521662A (ja) 2014-08-28
EP2736919A2 (en) 2014-06-04

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FZDE Discontinued

Effective date: 20170801