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SG10201809638YA - Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same - Google Patents

Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

Info

Publication number
SG10201809638YA
SG10201809638YA SG10201809638YA SG10201809638YA SG10201809638YA SG 10201809638Y A SG10201809638Y A SG 10201809638YA SG 10201809638Y A SG10201809638Y A SG 10201809638YA SG 10201809638Y A SG10201809638Y A SG 10201809638YA SG 10201809638Y A SG10201809638Y A SG 10201809638YA
Authority
SG
Singapore
Prior art keywords
neuroactive
alkoxy
treatment
prodrugs
methods
Prior art date
Application number
SG10201809638YA
Inventor
Douglas Covey
Albert Robichaud
Original Assignee
Univ Washington
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 Univ Washington, Sage Therapeutics Inc filed Critical Univ Washington
Publication of SG10201809638YA publication Critical patent/SG10201809638YA/en

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    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07J—STEROIDS
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    • 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
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
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    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
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    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/566—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol having an oxo group in position 17, e.g. estrone
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    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
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    • A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • 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
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    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C07J1/0022—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0029—Ethers
    • 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
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • C07J41/0016—Oximes
    • 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
    • C07J41/005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of only two carbon atoms, e.g. pregnane derivatives
    • 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
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0007—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
    • C07J5/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond 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
    • 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
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to 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
    • C07J21/006—Ketals at position 3
    • 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
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

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  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
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  • Psychiatry (AREA)
  • Anesthesiology (AREA)
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  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)

Abstract

NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds. [No Suitable Figure]
SG10201809638YA 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same SG10201809638YA (en)

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US201261738822P 2012-12-18 2012-12-18

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SG10201809638YA true SG10201809638YA (en) 2018-11-29

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SG11201504848QA SG11201504848QA (en) 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
SG10201809638YA SG10201809638YA (en) 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
SG10201706063UA SG10201706063UA (en) 2012-12-18 2013-12-18 Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

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Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AP3071A (en) 2005-11-28 2014-12-31 Marinus Pharmaceuticals Ganaxolone formulations and methods for the makingand use thereof
PT2753632T (en) 2011-09-08 2023-08-17 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof
EP2766380B1 (en) 2011-10-14 2019-04-24 Sage Therapeutics, Inc. 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
BR112014018110B1 (en) 2012-01-23 2022-06-07 Sage Therapeutics, Inc Aqueous pharmaceutical compositions formulated for parenteral administration and use of allopregnanolone and sulfbutylether-b-cyclodextrin
ES2902684T3 (en) 2012-08-21 2022-03-29 Sage Therapeutics Inc Allopregnanolone for the treatment of refractory status epilepticus
NZ739760A (en) * 2012-12-18 2020-05-29 Univ Washington Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
CA3114062A1 (en) 2013-03-13 2014-10-02 Sage Therapeutics, Inc. Neuroactive steroids and methods of use thereof
PL3498725T3 (en) 2013-04-17 2021-11-08 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21-n-pyrazolyl steroid for use in therapy
CN112110976B (en) 2013-04-17 2023-08-29 萨奇治疗股份有限公司 19-nor steroids that stimulate neural activity 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
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
LT3021852T (en) * 2013-07-19 2021-04-12 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
DK3488852T3 (en) * 2013-08-23 2021-02-01 Sage Therapeutics Inc NEUROACTIVE STEROIDS, COMPOSITIONS AND USES
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
EP4306114A1 (en) * 2014-06-18 2024-01-17 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
JOP20200195A1 (en) 2014-09-08 2017-06-16 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof
CN118344424A (en) 2014-10-16 2024-07-16 萨奇治疗股份有限公司 Compositions and methods for targeting CNS disorders
EP3206493B1 (en) 2014-10-16 2020-05-06 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
JP6893173B2 (en) 2014-11-27 2021-06-23 セージ セラピューティクス， インコーポレイテッド Compositions and Methods for Treating CNS Disorders
RS61530B1 (en) 2015-01-26 2021-04-29 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
MA45276A (en) 2015-06-18 2018-04-25 Sage Therapeutics Inc NEUROACTIVE STEROID SOLUTIONS AND THEIR METHODS OF USE
AU2016289965B2 (en) 2015-07-06 2021-09-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
DK3319612T3 (en) 2015-07-06 2021-08-23 Sage Therapeutics Inc OXYSTEROLS AND METHODS FOR USE THEREOF
CN113292623A (en) 2015-07-06 2021-08-24 萨奇治疗股份有限公司 Pregnansterol and methods of use thereof
CA3001722A1 (en) 2015-10-16 2017-04-20 Marinus Pharmaceuticals, Inc. Injectable neurosteroid formulations containing nanoparticles
US20200306262A1 (en) * 2015-11-20 2020-10-01 Sage Therapeutics, Inc. Compounds and methods of their use
KR20220084418A (en) 2016-03-08 2022-06-21 세이지 테라퓨틱스, 인크. Neuroactive steroids, compositions, and uses thereof
JP7112331B2 (en) 2016-04-01 2022-08-03 セージ セラピューティクス， インコーポレイテッド Oxysterols and their uses
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
JP6966486B2 (en) 2016-07-07 2021-11-17 セージ セラピューティクス， インコーポレイテッド Oxysterols and how to use them
JP7065825B2 (en) 2016-07-11 2022-05-12 セージ セラピューティクス， インコーポレイテッド C7, C12, and C16 replacement neurostimulatory steroids and how to use them
EP4302764A3 (en) 2016-07-11 2024-06-26 Sage Therapeutics, Inc. C17, c20, and c21 substituted neuroactive steroids and their methods of use
KR20230050474A (en) 2016-08-11 2023-04-14 오비드 테라퓨틱스 인크. Methods and compositions for treatment of epileptic disorders
CN115974954A (en) 2016-08-23 2023-04-18 萨奇治疗股份有限公司 Crystal of 19-nor C3, 3-disubstituted C21-N-pyrazolylsterols
US10391105B2 (en) 2016-09-09 2019-08-27 Marinus Pharmaceuticals Inc. Methods of treating certain depressive disorders and delirium tremens
WO2018064649A1 (en) 2016-09-30 2018-04-05 Sage Therapeutics, Inc. C7 substituted oxysterols and methods as nmda modulators
ES2968140T3 (en) 2016-10-18 2024-05-08 Sage Therapeutics Inc Oxysterols and procedures for their use
JP7118957B2 (en) 2016-10-18 2022-08-16 セージ セラピューティクス， インコーポレイテッド Oxysterols and their uses
US20200291059A1 (en) 2017-12-08 2020-09-17 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
CN109988210B (en) * 2017-12-30 2022-05-17 天津药业研究院股份有限公司 Preparation method of progesterone and progesterone intermediate
CN113166193A (en) 2018-10-12 2021-07-23 萨奇治疗股份有限公司 Neuroactive steroids substituted at position 10 with a cyclic group for the treatment of CNS disorders
CN109289095B (en) * 2018-11-23 2021-03-26 淮海工学院 Enteroscope gel containing lidocaine hydrochloride and preparation method thereof
US11266662B2 (en) 2018-12-07 2022-03-08 Marinus Pharmaceuticals, Inc. Ganaxolone for use in prophylaxis and treatment of postpartum depression
CR20210629A (en) 2019-05-31 2022-03-22 Sage Therapeutics Inc Neuroactive steroids and compositions thereof
MX2022001553A (en) 2019-08-05 2022-04-18 Marinus Pharmaceuticals Inc Ganaxolone for use in treatment of status epilepticus.
US10857163B1 (en) 2019-09-30 2020-12-08 Athenen Therapeutics, Inc. Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof
WO2021113834A1 (en) 2019-12-06 2021-06-10 Marinus Pharmaceuticals, Inc. Ganaxolone for use in treating tuberous sclerosis complex
CN115551514A (en) 2020-03-25 2022-12-30 萨奇治疗股份有限公司 Use of a medicament for the treatment of respiratory disorders
CN117801047A (en) * 2023-01-19 2024-04-02 北京华睿鼎信科技有限公司 Neurosteroid derivative and use thereof

Family Cites Families (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB820779A (en) * 1954-12-08 1959-09-23 Syntex Sa Cyclopentanophenanthrene derivatives
US2856415A (en) * 1957-11-13 1958-10-14 Searle & Co 3,19-dihydroxy-5-androstene derivatives
BE632431A (en) * 1962-05-16
US3206459A (en) 1962-10-19 1965-09-14 Syntex Corp 10alpha-pregnan-19-ol derivatives
US4239681A (en) * 1974-04-15 1980-12-16 Richardson-Merrell Inc. Androst-4-en-19-ols
US4022769A (en) * 1974-05-13 1977-05-10 Richardson-Merrell Inc. Androst-4-en-19-ones
US4139617A (en) * 1974-05-13 1979-02-13 Richardson-Merrell Inc. 19-Oxygenated-androst-5-enes for the enhancement of libido
US4071625A (en) 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
DE2632677A1 (en) 1976-07-16 1978-01-26 Schering Ag PROCESS FOR THE MANUFACTURE OF ANDROSTANE-17-ONE DERIVATIVES AND THEIR USE
MA18433A1 (en) * 1978-05-26 1979-12-31 Ciba Geigy Ag PROCESS FOR THE SYNTHESIS OF THE HYDROXYACETYL SIDE CHAIN OF PREGNAGNE-TYPE STEROIDS, NEW 21-HYDROXY-20-OXO-17 ALPHA-PREGNAGNES AND PHARMACEUTICAL PRODUCTS CONTAINING
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
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
EP0656365B1 (en) 1993-12-02 1997-04-09 Akzo Nobel N.V. Substituted 2beta-morpholinoandrostane derivatives
US5661141A (en) * 1995-03-27 1997-08-26 Petrow; Vladimir 19-oxygenated steroids as therapeutic agents
ES2235187T3 (en) * 1995-06-06 2005-07-01 Euro-Celtique S.A. NEUROACTIVE STEROIDS OF THE ANDROSTAN AND PREGNAN SERIES.
WO1998005337A1 (en) * 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
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
DE60128251T2 (en) * 2000-11-03 2008-01-10 Washington University Oestrone derivatives with cell protective effect
GR1003861B (en) * 2000-12-29 2002-04-11 Novel gabaa modulating neurosteroids
CA2520142C (en) 2003-03-24 2011-01-04 Sterix Limited Oestrogen derivatives as inhibitors of steroid sulphatase
CN1281561C (en) * 2003-04-23 2006-10-25 中国科学院上海有机化学研究所 Compound with base skeleton of 1,6-methylene-[10]-annulene and use thereof
US7781421B2 (en) * 2003-05-29 2010-08-24 Washington University Neuroactive 13, 24-cyclo-18, 21-dinorcholanes and structurally related pentacyclic steriods
EP1689767A1 (en) * 2003-11-24 2006-08-16 Merck & Co., Inc. Estrogen receptor modulators
CN100376685C (en) * 2005-01-14 2008-03-26 天津科技大学 Preparation of theelin by microbial conversion
EP1868593A2 (en) * 2005-04-07 2007-12-26 Hythiam, Inc. Improved methods of and compositions for the prevention of anxiety, substance abuse, and dependence
DE102007027636A1 (en) 2007-06-12 2008-12-18 Bayer Schering Pharma Aktiengesellschaft 17β-Cyano-18α-homo-19-nor-androst-4-ene derivative, its use and the derivative-containing drug
AU2008265898B2 (en) 2007-06-15 2013-11-28 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
AU2011284606A1 (en) 2010-07-30 2013-03-14 Pharmacellion Ltd Compounds and methods for treating neoplasia
CN103347525A (en) 2010-12-15 2013-10-09 哈博生物科学公司 Methods and compounds for preparing 3alpha-oxygen substituted steroids
US9388210B2 (en) 2011-02-25 2016-07-12 Washington University Neuroactive 17(20)-Z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
ES2657986T3 (en) 2011-03-23 2018-03-07 Etsuro Ito Method and kit for measuring very high sensitivity of protein and nucleic acid and a novel enzyme substrate
WO2013188792A2 (en) * 2012-06-15 2013-12-19 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
US9765110B2 (en) * 2012-10-08 2017-09-19 Washington University Neuroactive 19-alkoxy-17(20)-Z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same
NZ739760A (en) 2012-12-18 2020-05-29 Univ Washington Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
US9562026B2 (en) * 2013-03-14 2017-02-07 Washington University Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors
DK3488852T3 (en) * 2013-08-23 2021-02-01 Sage Therapeutics Inc NEUROACTIVE STEROIDS, COMPOSITIONS AND USES

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