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

Info

Publication number
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
Authority
JP
Japan
Prior art keywords
alkyl
hydrogen
heterocycloalkyl
haloalkyl
alkenyl
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.)
Pending
Application number
JP2014523105A
Other languages
English (en)
Japanese (ja)
Other versions
JP2014521662A5 (https=
Inventor
ジェー. ホジェンカンプ,ダーク
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
Original Assignee
University of California
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 filed Critical University of California
Publication of JP2014521662A publication Critical patent/JP2014521662A/ja
Publication of JP2014521662A5 publication Critical patent/JP2014521662A5/ja
Pending legal-status Critical Current

Links

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)
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)

Publication Number Publication Date
JP2014521662A true JP2014521662A (ja) 2014-08-28
JP2014521662A5 JP2014521662A5 (https=) 2015-09-17

Family

ID=47629869

Family Applications (1)

Application Number Title Priority Date Filing Date
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

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=)

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

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20230747T1 (hr) 2011-09-08 2024-01-05 Sage Therapeutics, Inc. Neuroaktivni steroidi, pripravci i njihova uporaba
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
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
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

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

Also Published As

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

Similar Documents

Publication Publication Date Title
JP2014521662A (ja) 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
JP7269911B2 (ja) 向神経活性ステロイド、組成物、及びその使用
EP2215049B1 (en) P2x3, receptor antagonists for treatment of pain
JP4606408B2 (ja) 選択的グルココルチコイド受容体調節物質としての17−カルバモイルオキシコルチゾル誘導体
JP5099005B2 (ja) ヘテロ化合物
JP4054369B2 (ja) オルト置換アリールまたはヘテロアリールアミド化合物
EP2758050B1 (en) Acyclic cyanoethylpyrazoles as janus kinase inhibitors
EP2137181B1 (en) Oxadiazole substituted indazole derivatives for use as sphingosine 1-phosphate (s1p) agonists
CA2570780C (en) Compounds and methods for inhibiting the interaction of bcl proteins with binding partners
KR20180043247A (ko) Tgr5 조절제 및 이를 사용하는 방법
CN104136452A (zh) 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
BR112018005861B1 (pt) Compostos derivados de ácido oleanólico modificado com c4 para a inibição de il-17, composição farmacêutica e usos terapêuticos dos ditos compostos
JP5897186B2 (ja) Pgds阻害剤としてのフェニルオキサジアゾール誘導体
CA3020287A1 (en) Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
JP7664359B2 (ja) 15β-[3-プロパンアミド]-置換エストラ-1,3,5(10)-トリエン-17-オン化合物および17β-ヒドロキシステロイドデヒドロゲナ-ゼの阻害に使用するためのそれらの17-オキシム
JP2021512909A (ja) ステロイド系誘導体モジュレーター、その製造方法及び応用
JP2020023512A (ja) S1p3アンタゴニスト
CN103298807A (zh) 作为用于治疗自身免疫性疾病和血管疾病的s1p1激动剂的杂环化合物
US20200131144A1 (en) Amine or (thio)amide containing lxr modulators
JP2012501334A (ja) 置換アミノチアゾール誘導体、医薬組成物、および使用の方法
WO2019241796A1 (en) Pyrazole and imidazole compounds for inhibition of il-17 and rorgamma
TW201136922A (en) New oxadiazole derivatives
CN120607578A (zh) 17β-HSD1抑制剂化合物、药物组合物及其应用
JP2014532656A (ja) 炎症および免疫関連用途のための化合物
JP2000507969A (ja) キラル添加剤を用いる非対称コンジュゲート付加反応によるエンドセリン中間体

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20150728

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20150728

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160719

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20170307