AU2014308621C1 - Neuroactive steroids, compositions, and uses thereof - Google Patents

Neuroactive steroids, compositions, and uses thereof Download PDF

Info

Publication number
AU2014308621C1
AU2014308621C1 AU2014308621A AU2014308621A AU2014308621C1 AU 2014308621 C1 AU2014308621 C1 AU 2014308621C1 AU 2014308621 A AU2014308621 A AU 2014308621A AU 2014308621 A AU2014308621 A AU 2014308621A AU 2014308621 C1 AU2014308621 C1 AU 2014308621C1
Authority
AU
Australia
Prior art keywords
unsubstituted
compound
alkyl
meo
heterocyclyl
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.)
Active
Application number
AU2014308621A
Other languages
English (en)
Other versions
AU2014308621B2 (en
AU2014308621A1 (en
Inventor
Boyd L. Harrison
Robert Jason Herr
Robert Borbo Kargbo
Gabriel Martinez Botella
Albert Jean Robichaud
Francesco Gerald Salituro
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.)
Sage Therapeutics Inc
Original Assignee
Sage Therapeutics Inc
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 Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Publication of AU2014308621A1 publication Critical patent/AU2014308621A1/en
Application granted granted Critical
Publication of AU2014308621B2 publication Critical patent/AU2014308621B2/en
Priority to AU2020201948A priority Critical patent/AU2020201948B2/en
Priority to AU2021290382A priority patent/AU2021290382B2/en
Publication of AU2014308621C1 publication Critical patent/AU2014308621C1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • 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
    • A61P25/24—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/008—Ketals at position 17
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/0065—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified
    • C07J7/007—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by an OH group free esterified or etherified not substituted in position 17 alfa
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0085—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by an halogen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Anesthesiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2014308621A 2013-08-23 2014-08-22 Neuroactive steroids, compositions, and uses thereof Active AU2014308621C1 (en)

Priority Applications (2)

Application Number Priority Date Filing Date Title
AU2020201948A AU2020201948B2 (en) 2013-08-23 2020-03-18 Neuroactive steroids, compositions, and uses thereof
AU2021290382A AU2021290382B2 (en) 2013-08-23 2021-12-24 Neuroactive steroids, compositions, and uses thereof

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201361869440P 2013-08-23 2013-08-23
US201361869446P 2013-08-23 2013-08-23
US61/869,446 2013-08-23
US61/869,440 2013-08-23
US201462014018P 2014-06-18 2014-06-18
US62/014,018 2014-06-18
PCT/US2014/052417 WO2015027227A1 (en) 2013-08-23 2014-08-22 Neuroactive steroids, compositions, and uses thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2020201948A Division AU2020201948B2 (en) 2013-08-23 2020-03-18 Neuroactive steroids, compositions, and uses thereof

Publications (3)

Publication Number Publication Date
AU2014308621A1 AU2014308621A1 (en) 2016-03-10
AU2014308621B2 AU2014308621B2 (en) 2019-12-19
AU2014308621C1 true AU2014308621C1 (en) 2022-01-06

Family

ID=52484216

Family Applications (3)

Application Number Title Priority Date Filing Date
AU2014308621A Active AU2014308621C1 (en) 2013-08-23 2014-08-22 Neuroactive steroids, compositions, and uses thereof
AU2020201948A Active AU2020201948B2 (en) 2013-08-23 2020-03-18 Neuroactive steroids, compositions, and uses thereof
AU2021290382A Active AU2021290382B2 (en) 2013-08-23 2021-12-24 Neuroactive steroids, compositions, and uses thereof

Family Applications After (2)

Application Number Title Priority Date Filing Date
AU2020201948A Active AU2020201948B2 (en) 2013-08-23 2020-03-18 Neuroactive steroids, compositions, and uses thereof
AU2021290382A Active AU2021290382B2 (en) 2013-08-23 2021-12-24 Neuroactive steroids, compositions, and uses thereof

Country Status (20)

Country Link
US (3) US20160229887A1 (enExample)
EP (3) EP3831387A1 (enExample)
JP (3) JP6466942B2 (enExample)
CN (2) CN113750107B (enExample)
AU (3) AU2014308621C1 (enExample)
BR (1) BR112016003862B1 (enExample)
CA (2) CA2921512C (enExample)
CY (1) CY1124112T1 (enExample)
DK (1) DK3488852T3 (enExample)
ES (2) ES2706180T3 (enExample)
HK (1) HK1225977B (enExample)
HU (1) HUE052308T2 (enExample)
LT (1) LT3488852T (enExample)
PL (1) PL3488852T3 (enExample)
PT (2) PT3488852T (enExample)
RS (1) RS61370B1 (enExample)
RU (1) RU2696585C2 (enExample)
SI (1) SI3488852T1 (enExample)
SM (1) SMT202100048T1 (enExample)
WO (1) WO2015027227A1 (enExample)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2766380T (pt) 2011-10-14 2019-07-29 Sage Therapeutics Inc Compostos de 19-nor pregnano 3,3-dissubstituídos, composições e seus usos
EP2887944B1 (en) 2012-08-21 2021-10-06 Sage Therapeutics, Inc. Allopregnanolone for treating refractory status epilepticus
KR102400891B1 (ko) * 2012-12-18 2022-05-20 워싱톤 유니버시티 신경활성 19-알콕시-17-치환된 스테로이드, 그의 전구약물, 및 그를 사용한 치료 방법
PL2986624T3 (pl) 2013-04-17 2020-11-16 Sage Therapeutics, Inc. Neuroaktywne steroidy 19-NOR do stosowania w sposobach leczenia
KR102614507B1 (ko) 2013-04-17 2023-12-19 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
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
CA3199003A1 (en) 2013-07-19 2015-01-22 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
HUE052308T2 (hu) 2013-08-23 2021-04-28 Sage Therapeutics Inc Neuroaktív szteroidok, készítmények és alkalmazásuk
US10246482B2 (en) 2014-06-18 2019-04-02 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
EP3206493B1 (en) 2014-10-16 2020-05-06 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
CN117024502A (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
EP3719029A1 (en) 2014-11-27 2020-10-07 Sage Therapeutics, Inc. Compositions for inducing sedation
ES2857082T3 (es) 2015-01-26 2021-09-28 Sage Therapeutics Inc Composiciones y métodos para el tratamiento de trastornos del SNC
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
MA45276A (fr) 2015-06-18 2018-04-25 Sage Therapeutics Inc Solutions de stéroïdes neuroactifs et leurs méthodes d'utilisation
EA036155B1 (ru) 2015-10-16 2020-10-06 Маринус Фармасьютикалс, Инк. Инъекционные составы нейростероида, содержащие наночастицы
AU2017229656B2 (en) 2016-03-08 2022-09-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
MA45599A (fr) 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
AU2017296295B2 (en) 2016-07-11 2022-02-24 Sage Therapeutics, Inc. C7, C12, and C16 substituted neuroactive steroids and their methods of use
KR20230079470A (ko) 2016-08-23 2023-06-07 세이지 테라퓨틱스, 인크. 결정질 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드
US10391105B2 (en) 2016-09-09 2019-08-27 Marinus Pharmaceuticals Inc. Methods of treating certain depressive disorders and delirium tremens
KR20200096596A (ko) 2017-12-08 2020-08-12 세이지 테라퓨틱스, 인크. Cns 장애의 치료를 위한 중수소화 21 -[4-시아노-피라졸-1 -일]-19-노르-프레간-3. 알파-올-20-온 유도체
EP3728284B1 (en) * 2017-12-22 2024-08-21 Sage Therapeutics, Inc. 19-homo, 3.alpha.-hydroxy-steroid-20-one compounds for treating cns disorders
CN114805462B (zh) 2018-02-11 2024-06-18 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
CN109503694A (zh) * 2018-11-21 2019-03-22 苏州闻天医药科技有限公司 一种新型gabaa受体调节剂及其用途
GB201903664D0 (en) * 2019-03-18 2019-05-01 Univ Edinburgh Small, orthogonal and tunable dyes and photosensitizers
WO2020243488A1 (en) 2019-05-31 2020-12-03 Sage Therapeutics, Inc. Neuroactive steroids and compositions thereof
US20220275020A1 (en) 2019-08-07 2022-09-01 Shanghai Hansoh Biomedical Co., Ltd. Salt and crystal form of steroid derivative regulator
US10857163B1 (en) 2019-09-30 2020-12-08 Athenen Therapeutics, Inc. Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof
EP4125921A1 (en) 2020-03-25 2023-02-08 Sage Therapeutics, Inc. Use of agents for treatment of respiratory conditions

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4071625A (en) * 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
WO1995021617A1 (en) * 1994-02-14 1995-08-17 Cocensys, Inc. Androstanes and pregnanes for allosteric modulation of gaba receptor
WO2013056181A1 (en) * 2011-10-14 2013-04-18 Sage Therapeutics, Inc. 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof

Family Cites Families (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2856415A (en) 1957-11-13 1958-10-14 Searle & Co 3,19-dihydroxy-5-androstene derivatives
FR1380417A (fr) 1962-05-15 1964-12-04 Roussel Uclaf Nouveaux androstanyl-pyrazoles et procédé de préparation
US3206459A (en) 1962-10-19 1965-09-14 Syntex Corp 10alpha-pregnan-19-ol derivatives
US3169134A (en) 1963-03-21 1965-02-09 Searle & Co 2, 3-oxygenated-17alpha-methyl-5alpha-androstan-17beta-ols
BE754111A (fr) 1969-07-29 1971-01-29 Upjohn Co Nouveaux 7alpha- et 7beta-methyl-3alpha,5alpha- cycloandrostanes et composes analogues 19-nor et leur procede de preparation
US3943124A (en) 1970-12-17 1976-03-09 Gordon Hanley Phillipps Chemical compounds
GB1434919A (en) 1972-06-15 1976-05-12 Glaxo Lab Ltd 3alpha-hydroxy androstanes
GB1380246A (en) 1970-12-17 1975-01-08 Glaxo Lab Ltd 3alpha-hydroxy-androstanes and esters thereof
GB1430942A (en) 1972-05-05 1976-04-07 Glaxo Lab Ltd 21-substituted 3alpha-hydroxy pregnanes
US3983111A (en) 1972-05-05 1976-09-28 Glaxo Laboratories Limited Steroidal anaesthetics of the pregnane and 19-norpregnane series
GB1436324A (en) 1972-05-12 1976-05-19 Glaxo Lab Ltd Anaesthetic 3alpha-hydroxy pregnanes
DK134348C (da) 1973-11-30 1977-03-21 Schering Ag Analogifremgangsmade til fremstilling af d-homo-20-ketopregnaner
DE2438020A1 (de) 1974-08-05 1976-02-26 Schering Ag 18-methyl-19-nor-20-keto-pregnane und verfahren zu ihrer herstellung
IL48628A0 (en) 1974-12-23 1976-02-29 Schering Ag D-homo-20-keto-pregnanes and process for their manufactur
DE2526373C2 (de) 1975-06-11 1983-11-10 Schering AG, 1000 Berlin und 4709 Bergkamen Verfahren zur Herstellung von Δ↑9↑↑(↑↑1↑↑1↑↑)↑-5α-20-Ketosteroiden
US4192871A (en) 1976-01-06 1980-03-11 Glaxo Laboratories Limited Chemical compounds
GB1570394A (en) 1976-01-06 1980-07-02 Glaxo Lab Ltd 11-acyloxy-3-hydroxy steroids
GB1581234A (en) 1976-04-05 1980-12-10 Glaxo Operations Ltd 11a - amino - 3a - hydroxysteroids
DE2632677A1 (de) 1976-07-16 1978-01-26 Schering Ag Verfahren zur herstellung von androstan-17-on-derivaten und deren verwendung
GB1581235A (en) 1977-04-04 1980-12-10 Glaxo Operations Ltd 11a-amino-3a-hydroxy-steroids
US4389345A (en) 1981-10-09 1983-06-21 G.D. Searle & Co. 3-Oxoestra-17-acetonitrile and unsaturated analogs
US4495102A (en) 1982-09-03 1985-01-22 G. D. Searle & Co. Aminoalkyl steroids
US5319115A (en) 1987-08-25 1994-06-07 Cocensys Inc. Method for making 3α-hydroxy, 3β-substituted-pregnanes
US5232917A (en) 1987-08-25 1993-08-03 University Of Southern California Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series
US5120723A (en) 1987-08-25 1992-06-09 University Of Southern California Method, compositions, and compounds for modulating brain excitability
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
WO1993005786A1 (en) 1991-09-13 1993-04-01 Cocensys, Inc. Novel gabaa receptor with steroid binding sites
DE4232681C2 (de) 1992-09-29 1994-11-24 Sigma Tau Ind Farmaceuti 17-Phenyl- und 17-Furyl-14beta,5alpha-androstan- und androsten- Derivate, Verfahren zu deren Herstellung und diese enthaltende pharmazeutische Zusammensetzung
EP0701444B1 (en) 1993-05-24 2010-04-07 Purdue Pharma Ltd. Methods and compositions for inducing sleep
EP0656365B1 (en) 1993-12-02 1997-04-09 Akzo Nobel N.V. Substituted 2beta-morpholinoandrostane derivatives
CZ300694A3 (en) 1993-12-02 1996-05-15 Akzo Nobel Nv Substituted 2beta-morpholinandrostane derivatives, process of their preparation, their use for preparing pharmaceutical preparations and pharmaceutical compositions containing thereof
US5939545A (en) 1994-02-14 1999-08-17 Cocensys, Inc. Method, compositions, and compounds for allosteric modulation of the gaba receptor by members of the androstane and pregnane series
JP2002500616A (ja) 1994-07-21 2002-01-08 ファルマシア・アンド・アップジョン・カンパニー 神経学的に活性なアミノステロイド
BR9509764A (pt) 1994-11-23 1998-07-07 Cocensys Inc Série androstano e pregnano para modulação alostérica de receptor de gaba
PL185523B1 (pl) 1995-06-06 2003-05-30 Cocensys Inc Neuroaktywne steroidy z grupy pochodnych androstanu i pregnanu oraz kompozycja farmaceutyczna
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
US5994334A (en) 1997-02-05 1999-11-30 University Of Maryland Androgen synthesis inhibitors
US5935545A (en) 1997-07-11 1999-08-10 E. I. Du Pont De Nemours And Company Process for producing an aqueous solution comprising ferric chloride
YU77701A (sh) 1999-04-29 2005-07-19 Euro-Celtique S.A. 3-α-HIDROKSI-3Гџ-METOKSIMETIL-21-HETEROCIKLIČNO SUPSTITUISANI STEROIDI SA ANESTETIČKIM DEJSTVOM
US7018406B2 (en) 1999-11-17 2006-03-28 Corevalve Sa Prosthetic valve for transluminal delivery
DE60111304T2 (de) 2000-02-18 2005-11-10 Taiho Pharmaceutical Co. Ltd. Verfahren zur herstellung von steroid-derivaten
US6855836B2 (en) 2000-10-26 2005-02-15 Jenapharm Gmbh & Co. Kg 17-Methylene steroids, process for their production and pharmaceutical compositions that contain these compounds
US6844456B2 (en) 2000-11-03 2005-01-18 Washington University Modified, hydroxy-substituted aromatic structures having cytoprotective activity
GR1003861B (el) 2000-12-29 2002-04-11 Νεα νευροστεροειδη που αλληλεπιδρουν με τον υποδοχεα gabaa.
DK1608671T3 (da) 2003-03-24 2010-05-10 Sterix Ltd Østrogenderivater som inhibitorer af steroidsulfatase
WO2005000869A1 (en) 2003-05-29 2005-01-06 Washington University Neuroactive 13,24-cyclo-18,21-dinorcholanes and structurally-related pentacyclic steroids
AU2004292555A1 (en) 2003-11-24 2005-06-09 Merck & Co., Inc. Estrogen receptor modulators
WO2005105822A2 (en) * 2004-04-23 2005-11-10 Euro-Celtique S.A. 3-alpha-hydroxy 21-n- heteroaryl-pregnane derivatives for modulation of brain excitability and a process for the production thereof
US8604011B2 (en) 2004-09-27 2013-12-10 The Regents Of The University Of California Therapy for treatment of chronic degenerative brain diseases and nervous system injury
CA2582231A1 (en) 2004-09-29 2006-10-19 Hollis-Eden Pharmaceuticals, Inc. Steroid analogs and uses
KR20100095661A (ko) 2005-06-09 2010-08-31 유로-셀띠끄 소시에떼 아노님 신경 자극성 스테로이드의 약학적 조성물 및 그 용도
US20090203658A1 (en) 2007-01-08 2009-08-13 Duke University Neuroactive steroid compositions and methods of use therefor
DE102007027636A1 (de) 2007-06-12 2008-12-18 Bayer Schering Pharma Aktiengesellschaft 17ß-Cyano-18a-homo-19-nor-androst-4-en-Derivat, dessen Verwendung und das Derivat enthaltende Arzneimittel
US8575375B2 (en) 2007-06-15 2013-11-05 Research Triangle Institute Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties
GB0711948D0 (en) 2007-06-20 2007-08-01 Bionature E A Ltd Neurosteriod compounds
CN101412742B (zh) 2007-10-19 2013-07-31 天津金耀集团有限公司 一种抑制血管新生的硝酸酯药物
US20090264443A1 (en) 2008-04-18 2009-10-22 David Helton Treatment of organophosphate exposure with tetrahydroindolone arylpiperazine compounds
CN101624414B (zh) 2008-07-07 2013-02-13 天津金耀集团有限公司 一种抑制血管新生的硝酸酯药物
CZ2008434A3 (cs) 2008-07-10 2009-12-09 Ústav organické chemie a biochemie Akademie ved CR, v. v. i. Pregnanové anionické slouceniny, zpusob jejich výroby a jejich použití
WO2010054158A2 (en) 2008-11-07 2010-05-14 Auspex Pharmaceuticals, Inc. Steroid modulators of glucocorticoid receptor
WO2011079047A1 (en) 2009-12-23 2011-06-30 Drugtech Corporation Methods for reducing the occurrence of preterm delivery and other pregnancy-related conditions
WO2012013816A1 (en) 2010-07-30 2012-02-02 Medexis S.A. Compounds and methods for treating neoplasia
CN103347525A (zh) 2010-12-15 2013-10-09 哈博生物科学公司 制备3α-氧取代的甾族化合物的方法及化合物
WO2012109752A1 (en) 2011-02-15 2012-08-23 Socpra Sciences Et Génie, S.E.C. Steroid alkaloids and uses thereof as antimicrobial agents against electron transport-deficient microbes and as potentiators for antimicrobial agents against pathogenic bacteria
CZ201181A3 (cs) 2011-02-15 2012-09-12 Ústav organické chemie a biochemie Akademie ved CR, v.v.i. Deriváty pregnanolonu substituované v poloze 3alfa kationickou skupinou, zpusob jejich výroby, jejich použití a prostredek je obsahující
WO2012116290A2 (en) 2011-02-25 2012-08-30 Washington University Neuroactive 17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
EP2987866B1 (en) 2011-03-23 2017-12-06 Etsuro Ito Method and kit for super-high-sensitivity measurement of protein and nucleic acid, and novel enzyme substrate
CA2843436A1 (en) 2011-07-29 2013-02-07 The Regents Of The University Of California Novel 17.beta.-heteroaryl-substituted steroids as modulators of gaba a receptors
AU2012304412A1 (en) 2011-09-08 2014-03-27 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
WO2013188792A2 (en) * 2012-06-15 2013-12-19 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
CA2877122C (en) 2012-06-19 2020-04-28 Intercept Pharmaceuticals, Inc. Preparation, uses and solid forms of obeticholic acid
WO2014028398A2 (en) 2012-08-13 2014-02-20 The Regents Of The University Of California Mitigation of epileptic seizures by combination therapy using benzodiazepines and neurosteroids
WO2014058736A1 (en) 2012-10-08 2014-04-17 Washington University Neuroactive 19-alkoxy-17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
US9757391B2 (en) 2012-11-09 2017-09-12 Goodchild Investments Pty Ltd Neuroactive steroids and their use to facilitate neuroprotection
KR102400891B1 (ko) 2012-12-18 2022-05-20 워싱톤 유니버시티 신경활성 19-알콕시-17-치환된 스테로이드, 그의 전구약물, 및 그를 사용한 치료 방법
US8939545B2 (en) 2012-12-20 2015-01-27 Eastman Kodak Company Inkjet printing with managed airflow for condensation control
CA2831054C (en) 2013-01-09 2016-08-30 Sapna Life Sciences Corp. Formulations, and methods for their use in treatment of neuropathology and neurodegeneration as a result of traumatic injury
WO2014108808A2 (en) 2013-01-09 2014-07-17 Henry James Lorne Pharmaceutical formulations for the treatment and prevention of trauma-induced neuropathology and neurodegeneration
GB201302368D0 (en) 2013-02-11 2013-03-27 Univ Bath Compound
US9512170B2 (en) * 2013-03-01 2016-12-06 Washington University Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors
US9562026B2 (en) 2013-03-14 2017-02-07 Washington University Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors
PL2986624T3 (pl) 2013-04-17 2020-11-16 Sage Therapeutics, Inc. Neuroaktywne steroidy 19-NOR do stosowania w sposobach leczenia
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
KR102614507B1 (ko) 2013-04-17 2023-12-19 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
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
CA3199003A1 (en) 2013-07-19 2015-01-22 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
HUE052308T2 (hu) 2013-08-23 2021-04-28 Sage Therapeutics Inc Neuroaktív szteroidok, készítmények és alkalmazásuk
ES2927007T3 (es) 2014-05-29 2022-10-31 Sage Therapeutics Inc Esteroides neuroactivos, composiciones y usos de los mismos
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
EP3206493B1 (en) 2014-10-16 2020-05-06 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
CN117024502A (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
EP3719029A1 (en) * 2014-11-27 2020-10-07 Sage Therapeutics, Inc. Compositions for inducing sedation
ES2857082T3 (es) 2015-01-26 2021-09-28 Sage Therapeutics Inc Composiciones y métodos para el tratamiento de trastornos del SNC
CN105985396A (zh) 2015-02-16 2016-10-05 苏州泽璟生物制药有限公司 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物
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
UY36741A (es) 2015-06-21 2016-12-30 Prevacus Inc Compuesto de esteroide c-20, sus composiciones y usos para tratar la lesión cerebral traumática (tbi), que incluye las conmociones cerebrales
EP3347368A4 (en) 2015-09-08 2019-01-23 Viewpoint Therapeutics, Inc. COMPOUNDS AND FORMULATIONS FOR THE TREATMENT OF EYE DISEASES
EA036155B1 (ru) 2015-10-16 2020-10-06 Маринус Фармасьютикалс, Инк. Инъекционные составы нейростероида, содержащие наночастицы
WO2017087864A1 (en) 2015-11-20 2017-05-26 Sage Therapeutics, Inc. Compounds and methods of their use
AU2017229656B2 (en) 2016-03-08 2022-09-29 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
US10226550B2 (en) 2016-03-11 2019-03-12 Brigham Young University Cationic steroidal antimicrobial compositions for the treatment of dermal tissue
MA45599A (fr) 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
AU2017296295B2 (en) 2016-07-11 2022-02-24 Sage Therapeutics, Inc. C7, C12, and C16 substituted neuroactive steroids and their methods of use
KR20230079470A (ko) 2016-08-23 2023-06-07 세이지 테라퓨틱스, 인크. 결정질 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드
US10391105B2 (en) 2016-09-09 2019-08-27 Marinus Pharmaceuticals Inc. Methods of treating certain depressive disorders and delirium tremens
CN108727453A (zh) 2017-04-20 2018-11-02 华东理工大学 新型pd-1抑制剂及其应用
WO2019018119A1 (en) 2017-07-18 2019-01-24 Pairnomix, Llc METHODS FOR TREATING EPILEPSY AND DISORDERS ASSOCIATED WITH KCNTI
CA3073925A1 (en) 2017-08-31 2019-03-07 Takeda Pharmaceutical Company Limited Treatment of cns conditions
US20200281943A1 (en) 2017-09-07 2020-09-10 Sage Therapeutics, Inc. Neuroactive steroids and their methods of use
US20190160078A1 (en) 2017-11-10 2019-05-30 Marinus Pharmaceuticals, Inc. Ganaxolone for use in treating genetic epileptic disorders
CN112823164A (zh) 2018-05-04 2021-05-18 阿克罗斯制药公司 神经甾体衍生物和其用途

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4071625A (en) * 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
WO1995021617A1 (en) * 1994-02-14 1995-08-17 Cocensys, Inc. Androstanes and pregnanes for allosteric modulation of gaba receptor
WO2013056181A1 (en) * 2011-10-14 2013-04-18 Sage Therapeutics, Inc. 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof

Also Published As

Publication number Publication date
RU2016110418A (ru) 2017-09-26
CN113750107B (zh) 2025-02-11
JP6826615B2 (ja) 2021-02-03
EP3035940B1 (en) 2018-10-17
DK3488852T3 (da) 2021-02-01
US20160229887A1 (en) 2016-08-11
US12071453B2 (en) 2024-08-27
WO2015027227A1 (en) 2015-02-26
EP3831387A1 (en) 2021-06-09
AU2014308621B2 (en) 2019-12-19
PT3488852T (pt) 2021-02-03
BR112016003862B1 (pt) 2022-09-06
EP3035940A1 (en) 2016-06-29
CN113750107A (zh) 2021-12-07
SI3488852T1 (sl) 2021-07-30
RU2016110418A3 (enExample) 2018-05-03
AU2014308621A1 (en) 2016-03-10
RU2696585C2 (ru) 2019-08-05
CN105579043A (zh) 2016-05-11
EP3488852B1 (en) 2020-10-28
JP7269911B2 (ja) 2023-05-09
US20210061848A1 (en) 2021-03-04
ES2706180T3 (es) 2019-03-27
AU2021290382B2 (en) 2024-02-22
AU2020201948B2 (en) 2021-09-30
PL3488852T3 (pl) 2021-06-28
EP3035940A4 (en) 2017-04-19
HK1225977B (en) 2017-09-22
CN105579043B (zh) 2021-09-14
CA2921512A1 (en) 2015-02-26
CA3235088A1 (en) 2015-02-26
EP3488852A1 (en) 2019-05-29
US20240239836A9 (en) 2024-07-18
RS61370B1 (sr) 2021-02-26
CA2921512C (en) 2024-05-28
CY1124112T1 (el) 2022-05-27
US20230279044A1 (en) 2023-09-07
LT3488852T (lt) 2021-02-25
JP2019070017A (ja) 2019-05-09
JP6466942B2 (ja) 2019-02-06
AU2021290382A1 (en) 2022-02-03
SMT202100048T1 (it) 2021-03-15
BR112016003862A2 (enExample) 2017-08-01
AU2020201948A1 (en) 2020-04-02
PT3035940T (pt) 2019-01-28
JP2021038248A (ja) 2021-03-11
ES2848823T3 (es) 2021-08-12
JP2016531134A (ja) 2016-10-06
HUE052308T2 (hu) 2021-04-28
US11498940B2 (en) 2022-11-15

Similar Documents

Publication Publication Date Title
AU2021290382B2 (en) Neuroactive steroids, compositions, and uses thereof
AU2021218132B2 (en) Compositions and methods for treating CNS disorders
AU2022203444B2 (en) Compositions and methods for treating CNS disorders
HK1225977A1 (en) Neuroactive steroids, compositions, and uses thereof
HK40052312A (en) Neuroactive steroids, compositions, and uses thereof
HK40009488A (en) Neuroactive steroids, compositions, and uses thereof
HK40009488B (en) Neuroactive steroids, compositions, and uses thereof

Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
DA2 Applications for amendment section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 19 AUG 2021

DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS AS SHOWN IN THE STATEMENT(S) FILED 19 AUG 2021