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

    • 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)
  • Biomedical Technology (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)
  • Neurosurgery (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
CA2848212C (en) 2011-09-08 2022-03-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
EP3572417B1 (en) 2011-10-14 2025-12-17 Sage Therapeutics, LLC 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
EP2806877B2 (en) 2012-01-23 2025-01-29 Sage Therapeutics, Inc. Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin
CA2882708A1 (en) 2012-08-21 2014-02-27 Sage Therapeutics, Inc. Methods of treating epilepsy or status epilepticus
AU2013352141B2 (en) 2012-11-30 2018-04-05 The Regents Of The University Of California Anticonvulsant activity of steroids
PT2968369T (pt) 2013-03-13 2018-12-05 Sage Therapeutics Inc Esteroides neuroativos e métodos para o seu uso
KR102396328B1 (ko) 2013-04-17 2022-05-10 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
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
EP2986624B1 (en) 2013-04-17 2020-03-25 Sage Therapeutics, Inc. 19-nor neuroactive steroids for methods of treatment
US20160068563A1 (en) 2013-04-17 2016-03-10 Boyd L. Harrison 19-nor neuroactive steroids and methods of use thereof
SI3021852T1 (sl) 2013-07-19 2021-07-30 Sage Therapeutics, Inc. Nevroaktivni steroidi, sestavki in uporabe le-teh
AU2014308621C1 (en) 2013-08-23 2022-01-06 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
US10259840B2 (en) 2014-06-18 2019-04-16 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses 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
ME03809B (me) 2014-10-16 2021-04-20 Sage Therapeutics Inc KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a
CN117024501A (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
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
CA2991311C (en) 2015-07-06 2025-05-06 Sage Therapeutics, Inc. OXYSTEROLS AND THEIR METHODS OF USE
HUE071964T2 (hu) 2015-07-06 2025-10-28 Sage Therapeutics Inc Oxiszterolok és alkalmazási eljárásaik
EP3828194B1 (en) 2015-07-06 2025-04-16 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
KR20240157128A (ko) * 2016-03-08 2024-10-31 세이지 테라퓨틱스, 인크. 신경활성 스테로이드, 조성물, 및 그의 용도
SMT202200300T1 (it) 2016-04-01 2022-09-14 Sage Therapeutics Inc Ossisteroli e relativi metodi d'uso
WO2017193046A1 (en) 2016-05-06 2017-11-09 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
WO2018013615A1 (en) 2016-07-11 2018-01-18 Sage Therapeutics, Inc. C7, c12, and c16 substituted neuroactive steroids and their methods of use
EP3504189A1 (en) 2016-08-23 2019-07-03 Sage Therapeutics, Inc. A crystalline 19-nor c3, 3-disubstituted c21-n-pyrazolyl steroid
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
RU2019115113A (ru) 2016-10-18 2020-11-24 Сейдж Терапьютикс, Инк. Оксистеролы и способы их применения
KR20230051723A (ko) 2016-10-18 2023-04-18 세이지 테라퓨틱스, 인크. 옥시스테롤 및 그의 사용 방법
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
WO2019154257A1 (zh) * 2018-02-11 2019-08-15 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
SG11202112391UA (en) 2019-05-31 2021-12-30 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

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

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
KR101345473B1 (ko) 헤테로 화합물
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
CA3020310A1 (en) Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
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
JP2020519651A (ja) アミン又は（チオ）アミド含有ｌｘｒモジュレーター
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

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