CA3041077A1 - Oxysterols and methods of use thereof - Google Patents

Oxysterols and methods of use thereof Download PDF

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Publication number
CA3041077A1
CA3041077A1 CA3041077A CA3041077A CA3041077A1 CA 3041077 A1 CA3041077 A1 CA 3041077A1 CA 3041077 A CA3041077 A CA 3041077A CA 3041077 A CA3041077 A CA 3041077A CA 3041077 A1 CA3041077 A1 CA 3041077A1
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Prior art keywords
compound
alkyl
hydrogen
disorder
formula
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CA3041077A
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English (en)
French (fr)
Inventor
Francesco G. Salituro
Albert J. Robichaud
Gabriel Martinez Botella
Boyd L. Harrison
Andrew Griffin
Daniel La
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Sage Therapeutics Inc
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Sage Therapeutics Inc
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Publication of CA3041077A1 publication Critical patent/CA3041077A1/en
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    • 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
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • AHUMAN NECESSITIES
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    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P1/10Laxatives
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    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J17/00Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • C07J9/005Normal 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Anesthesiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
CA3041077A 2016-10-18 2017-10-18 Oxysterols and methods of use thereof Pending CA3041077A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662409756P 2016-10-18 2016-10-18
US201662409768P 2016-10-18 2016-10-18
US62/409,756 2016-10-18
US62/409,768 2016-10-18
PCT/US2017/057276 WO2018075698A1 (en) 2016-10-18 2017-10-18 Oxysterols and methods of use thereof

Publications (1)

Publication Number Publication Date
CA3041077A1 true CA3041077A1 (en) 2018-04-26

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Application Number Title Priority Date Filing Date
CA3041077A Pending CA3041077A1 (en) 2016-10-18 2017-10-18 Oxysterols and methods of use thereof

Country Status (15)

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US (4) US11111266B2 (enExample)
EP (3) EP4105223B1 (enExample)
JP (3) JP2019532079A (enExample)
KR (3) KR102521573B1 (enExample)
CN (3) CN110072874B (enExample)
AU (3) AU2017345399B2 (enExample)
CA (1) CA3041077A1 (enExample)
DK (1) DK4105223T3 (enExample)
ES (2) ES2968140T3 (enExample)
IL (3) IL320521A (enExample)
MA (1) MA46565A (enExample)
MX (2) MX2019004679A (enExample)
RU (1) RU2019115112A (enExample)
TW (3) TWI836485B (enExample)
WO (1) WO2018075698A1 (enExample)

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RS67266B1 (sr) 2013-03-13 2025-10-31 Sage Therapeutics Inc Neuroaktivni steroidi i postupci za njihovu upotrebu
WO2015195967A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
SMT202100476T1 (it) 2015-07-06 2021-09-14 Sage Therapeutics Inc Ossisteroli e metodi di uso degli stessi
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ES2884071T3 (es) 2016-07-07 2021-12-10 Sage Therapeutics Inc 24-hidroxiesteroles sustituidos en 11 para el tratamiento de afecciones relacionadas con NMDA
MX392270B (es) 2016-09-30 2025-03-24 Sage Therapeutics Inc Oxisteroles sustituidos en c7 y metodos de uso de los mismos.
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CN111560045A (zh) * 2020-06-23 2020-08-21 江苏佳尔科药业集团股份有限公司 一种以ba为原料合成石胆酸的方法
CN112375117A (zh) * 2020-11-14 2021-02-19 湖南科瑞生物制药股份有限公司 石胆酸及其中间体的制备方法
CN113651866B (zh) * 2021-08-02 2023-07-04 王涛 一种以21-羟基-20-甲基孕甾-4-烯-3-酮为原料合成胆固醇的新方法
WO2023083979A1 (en) * 2021-11-10 2023-05-19 Umecrine Ab 3.beta.-hydroxy, 3.alpha.-ethyl steroids for modulation of the alpha-3 subtype of the gaba-a receptor
JP2025512885A (ja) 2022-03-30 2025-04-22 ドナルドソン カンパニー,インコーポレイティド 溶媒を再利用するためのシステム及び方法
EP4547256A1 (en) * 2022-07-01 2025-05-07 Intercept Pharmaceuticals, Inc. Methods for ameliorating cognitive impairment using bile acid derivatives
AU2023385734A1 (en) * 2022-11-21 2025-06-26 Sage Therapeutics, Inc. Negative nmda-modulating compounds and methods of use thereof
CN115974950A (zh) * 2022-12-23 2023-04-18 上海彩迩文生化科技有限公司 一种3-烷基化的甾体中间体及其制备和应用
WO2025020191A1 (zh) * 2023-07-27 2025-01-30 珂阑(上海)医药科技有限公司 甾类化合物、其制备方法和应用
WO2025250816A1 (en) * 2024-05-29 2025-12-04 Sage Therapeutics, Inc. Agents for delivering nmda receptor modulating compounds and methods of use thereof

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