JP2014521662A - GABAA受容体のモジュレーターとしての新規な17β−ヘテロアリール置換ステロイド - Google Patents

GABAA受容体のモジュレーターとしての新規な17β−ヘテロアリール置換ステロイド Download PDF

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JP2014521662A
JP2014521662A JP2014523105A JP2014523105A JP2014521662A JP 2014521662 A JP2014521662 A JP 2014521662A JP 2014523105 A JP2014523105 A JP 2014523105A JP 2014523105 A JP2014523105 A JP 2014523105A JP 2014521662 A JP2014521662 A JP 2014521662A
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alkyl
hydrogen
heterocycloalkyl
haloalkyl
alkenyl
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JP2014521662A5 (enExample
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ジェー. ホジェンカンプ,ダーク
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University of California
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    • 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

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  • 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)
JP2014523105A 2011-07-29 2012-07-30 GABAA受容体のモジュレーターとしての新規な17β−ヘテロアリール置換ステロイド Pending JP2014521662A (ja)

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 (2)

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JP2014521662A true JP2014521662A (ja) 2014-08-28
JP2014521662A5 JP2014521662A5 (enExample) 2015-09-17

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JP2014523105A Pending JP2014521662A (ja) 2011-07-29 2012-07-30 GABAA受容体のモジュレーターとしての新規な17β−ヘテロアリール置換ステロイド

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018502891A (ja) * 2015-01-26 2018-02-01 セージ セラピューティクス, インコーポレイテッド Cns障害を処置するための組成物および方法
JP2024114787A (ja) * 2016-07-11 2024-08-23 セージ セラピューティクス, インコーポレイテッド 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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FI2753632T3 (fi) 2011-09-08 2023-08-02 Sage Therapeutics Inc Neuroaktiivisia steroideja, koostumuksia ja niiden käyttöjä
CA3152410A1 (en) 2011-10-14 2013-04-18 Sage Therapeutics, Inc. 3,3-disubstituted 19-nor pregnane compounds, compositions, and uses thereof for the treatment of cns related disorders
SMT202000008T1 (it) 2012-01-23 2020-03-13 Sage Therapeutics Inc Formulazione di steroide neuroattivo comprendente un complesso di allopregnanolone e solfobutil eter beta-ciclodestrina
PL2887944T3 (pl) 2012-08-21 2022-02-21 Sage Therapeutics, Inc. Allopregnanolon do leczenia lekoopornego stanu padaczkowego
ES2973320T3 (es) 2012-11-30 2024-06-19 Univ California Alopregnanolona para tratar, reducir o mitigar los síntomas de la depresión posparto
RS67266B1 (sr) 2013-03-13 2025-10-31 Sage Therapeutics Inc Neuroaktivni steroidi i postupci za njihovu upotrebu
RU2019126333A (ru) 2013-04-17 2019-10-08 Сейдж Терапьютикс, Инк. 19-нор нейроактивные стероиды и способы их применения
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
US20160068563A1 (en) 2013-04-17 2016-03-10 Boyd L. Harrison 19-nor neuroactive steroids and methods of use thereof
CN113527400B (zh) 2013-04-17 2024-06-28 萨奇治疗股份有限公司 19-去甲c3,3-二取代的c21-n-吡唑基类固醇及其使用方法
WO2015010054A2 (en) 2013-07-19 2015-01-22 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
AU2014308621C1 (en) 2013-08-23 2022-01-06 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
ES2970222T3 (es) 2014-06-18 2024-05-27 Sage Therapeutics Inc Oxiesteroles y procedimientos de uso de los mismos
EP3188734A4 (en) 2014-09-02 2018-01-10 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
MX2021004492A (es) 2014-10-16 2022-12-05 Sage Therapeutics Inc Composiciones para el tratamiento de trastornos del snc.
SMT202000414T1 (it) 2014-10-16 2020-09-10 Sage Therapeutics Inc Composizioni e metodi per trattare disturbi del snc
ME03749B (me) 2014-11-27 2021-04-20 Sage Therapeutics Inc KOMPOZICIJE I POSTUPCIZA LEČENJE POREMEĆAJA CNS-a
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
MX390271B (es) 2015-07-06 2025-03-20 Sage Therapeutics Inc Oxiesteroles y metodos de uso de los mismos
FI3828194T3 (fi) 2015-07-06 2025-07-17 Sage Therapeutics Inc Oxysteroleita ja menetelmiä niiden käyttämiseksi
MA42409A (fr) 2015-07-06 2018-05-16 Sage Therapeutics Inc Oxystérols et leurs procédés d'utilisation
RU2766155C2 (ru) 2016-03-08 2022-02-08 Сейдж Терапьютикс, Инк. Нейроактивные стероиды, их композиции и применения
US20190330259A1 (en) 2016-04-01 2019-10-31 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
LT3481846T (lt) 2016-07-07 2021-08-25 Sage Therapeutics, Inc. 11-pakeistieji 24-hidroksisteroliai, skirti naudoti gydant su nmda susijusias būkles
CA3030420C (en) 2016-07-11 2025-11-18 Sage Therapeutics, Inc. C7, C12 AND C16 SUBSTITUTED NEUROACTIVE STEROIDS AND ASSOCIATED METHODS OF USE
CN115974956A (zh) 2016-08-23 2023-04-18 萨奇治疗股份有限公司 19-去甲c3,3-二取代的c21-n-吡唑基类固醇的晶体
JP7149266B2 (ja) 2016-09-30 2022-10-06 セージ セラピューティクス, インコーポレイテッド C7置換オキシステロールおよびnmdaモジュレーターとしての方法
MA46566A (fr) 2016-10-18 2019-08-28 Sage Therapeutics Inc Oxystérols et leurs procédés d'utilisation
IL293231B2 (en) 2016-10-18 2025-10-01 Sage Therapeutics Inc Oxysterols and methods of use thereof
KR102917075B1 (ko) * 2018-02-11 2026-01-26 장쑤 한서 파마슈티칼 그룹 캄파니 리미티드 스테로이드 유도체 조절제, 그의 제조 방법 및 그의 용도
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
CN114206900A (zh) 2019-05-31 2022-03-18 萨奇治疗股份有限公司 神经活性类固醇及其组合物
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3313809A (en) * 1965-03-05 1967-04-11 Sterling Drug Inc Steroido[21, 20-d]isoxazoles
WO1996016076A1 (en) * 1994-11-23 1996-05-30 Cocensys, Inc. Androstane and pregnane series for allosteric modulation of gaba receptor
WO1996040043A2 (en) * 1995-06-06 1996-12-19 Cocensys, Inc. Neuroactive steroids of the androstane and pregnane series
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
WO2007108002A2 (en) * 2006-03-23 2007-09-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Use of digitalis-like compounds in the treatment of affective disorders

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3313809A (en) * 1965-03-05 1967-04-11 Sterling Drug Inc Steroido[21, 20-d]isoxazoles
WO1996016076A1 (en) * 1994-11-23 1996-05-30 Cocensys, Inc. Androstane and pregnane series for allosteric modulation of gaba receptor
WO1996040043A2 (en) * 1995-06-06 1996-12-19 Cocensys, Inc. Neuroactive steroids of the androstane and pregnane series
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
WO2007108002A2 (en) * 2006-03-23 2007-09-27 Yissum Research Development Company Of The Hebrew University Of Jerusalem Use of digitalis-like compounds in the treatment of affective disorders

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
C.G.WERMUTH編, 『最新 創薬化学 上巻』, JPN6014041942, 15 August 1998 (1998-08-15), pages 235 - 271, ISSN: 0003360476 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2018502891A (ja) * 2015-01-26 2018-02-01 セージ セラピューティクス, インコーポレイテッド Cns障害を処置するための組成物および方法
JP2020189848A (ja) * 2015-01-26 2020-11-26 セージ セラピューティクス, インコーポレイテッド Cns障害を処置するための組成物および方法
JP2024114787A (ja) * 2016-07-11 2024-08-23 セージ セラピューティクス, インコーポレイテッド 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
JP7821842B2 (ja) 2016-07-11 2026-02-27 セージ セラピューティクス, エルエルシー 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

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EP2736919A2 (en) 2014-06-04
US20140148412A1 (en) 2014-05-29
CA2843436A1 (en) 2013-02-07
WO2013019711A3 (en) 2013-04-04
EP2736919A4 (en) 2015-01-14
WO2013019711A2 (en) 2013-02-07

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