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

Info

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
Other languages
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

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)
  • 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)
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=)

Families Citing this family (39)

* 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
RS61530B1 (sr) 2015-01-26 2021-04-29 Sage Therapeutics Inc Kompozicije i postupci za lečenje poremećaja cns
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
MA45599A (fr) * 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
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

Family Cites Families (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
NZ298567A (en) * 1994-11-23 2000-01-28 Cocensys Inc Androstane and pregnane derivatives, pharmaceutical compositions and methods of treatment
ATE284895T1 (de) * 1995-06-06 2005-01-15 Euro Celtique Sa Neuroaktive steroide der androstan- und pregnanreihe
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
EP2156862A1 (en) * 2006-03-23 2010-02-24 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
EP2736919A2 (en) 2014-06-04
JP2014521662A (ja) 2014-08-28
WO2013019711A3 (en) 2013-04-04
WO2013019711A2 (en) 2013-02-07
US20140148412A1 (en) 2014-05-29

Similar Documents

Publication Publication Date Title
CA2843436A1 (en) Novel 17.beta.-heteroaryl-substituted steroids as modulators of gaba a receptors
JP7269911B2 (ja) 向神経活性ステロイド、組成物、及びその使用
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
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
CN114656514B (zh) 一种甾族类衍生物调节剂及其制备方法和应用
AU2007236707C1 (en) Hetero compound
RU2194699C2 (ru) 1-фенил-бензимидазольные соединения, фармацевтическая композиция и способ лечения расстройства или заболевания, чувствительного к модуляции гамка-рецепторного комплекса центральной нервной системы
JP5815765B2 (ja) イソオキサゾール誘導体及び代謝型グルタミン酸受容体ポテンシエーターとしてのその使用
JP2020183410A (ja) 置換ピラゾロ[1,5−a]ピリミジンおよび医療疾患の治療におけるその使用
KR20180043247A (ko) Tgr5 조절제 및 이를 사용하는 방법
BRPI0806245B1 (pt) Compostos de fórmula i e seus usos
JP2014509316A (ja) RORγT阻害薬
CA2966581A1 (en) Substituted pyrrolo[1,2-a]pyrimidines and their use in the treatment of medical disorders
JP5809172B2 (ja) プロゲステロン受容体アンタゴニスト
CA3020287A1 (en) Pyrazolo[1,5-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
CA3020310A1 (en) Pyrrolo[1,2-a]pyrimidinyl carboxamide compounds and their use in the treatment of medical disorders
AU2018303186B2 (en) Amine or (thio)amide containing LXR modulators
CN113727973B (zh) 可用作类法尼醇x受体调节剂的取代酰胺化合物
TW201943711A (zh) 一種吡咯並胺基噠嗪酮化合物的製備方法及其中間體
CN109265471B (zh) Fxr受体激动剂
EP0567472B1 (de) D-homo-(16-en)-11 beta-aryl-4-estrene,verfahren zu ihrer herstellung sowie deren verwendung als arzneimittel.
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
CN113801061A (zh) 一种螺环甲酰胺类衍生物的制备方法
DE4417880A1 (de) 19,11beta-Überbrückte 18-Nor-Steroide, Verfahren zu ihrer Herstellung, diese Steroide enthaltende Arzneimittel sowie deren Verwendung zur Herstellung von Arzneimitteln
HK40079963A (en) Pyridone-containing fused ring derivative inhibitor, preparation method therefor, and use thereof

Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20170801