KR102521573B1 - 옥시스테롤 및 그의 사용 방법 - Google Patents

옥시스테롤 및 그의 사용 방법 Download PDF

Info

Publication number
KR102521573B1
KR102521573B1 KR1020197014258A KR20197014258A KR102521573B1 KR 102521573 B1 KR102521573 B1 KR 102521573B1 KR 1020197014258 A KR1020197014258 A KR 1020197014258A KR 20197014258 A KR20197014258 A KR 20197014258A KR 102521573 B1 KR102521573 B1 KR 102521573B1
Authority
KR
South Korea
Prior art keywords
delete delete
alkyl
disorder
mmol
mixture
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
KR1020197014258A
Other languages
English (en)
Korean (ko)
Other versions
KR20190065429A (ko
Inventor
프란체스코 지. 살리투로
앨버트 제이. 로비쇼
가브리엘 마르티네즈 보텔라
보이드 엘. 해리슨
앤드류 그리핀
대니얼 라
Original Assignee
세이지 테라퓨틱스, 인크.
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 세이지 테라퓨틱스, 인크. filed Critical 세이지 테라퓨틱스, 인크.
Priority to KR1020237012221A priority Critical patent/KR20230051723A/ko
Publication of KR20190065429A publication Critical patent/KR20190065429A/ko
Application granted granted Critical
Publication of KR102521573B1 publication Critical patent/KR102521573B1/ko
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
    • A61K31/575—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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • 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
    • 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
    • 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
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Anesthesiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
KR1020197014258A 2016-10-18 2017-10-18 옥시스테롤 및 그의 사용 방법 Active KR102521573B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020237012221A KR20230051723A (ko) 2016-10-18 2017-10-18 옥시스테롤 및 그의 사용 방법

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662409768P 2016-10-18 2016-10-18
US201662409756P 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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020237012221A Division KR20230051723A (ko) 2016-10-18 2017-10-18 옥시스테롤 및 그의 사용 방법

Publications (2)

Publication Number Publication Date
KR20190065429A KR20190065429A (ko) 2019-06-11
KR102521573B1 true KR102521573B1 (ko) 2023-04-14

Family

ID=60263022

Family Applications (3)

Application Number Title Priority Date Filing Date
KR1020237012221A Ceased KR20230051723A (ko) 2016-10-18 2017-10-18 옥시스테롤 및 그의 사용 방법
KR1020197014258A Active KR102521573B1 (ko) 2016-10-18 2017-10-18 옥시스테롤 및 그의 사용 방법
KR1020257012306A Pending KR20250054838A (ko) 2016-10-18 2017-10-18 옥시스테롤 및 그의 사용 방법

Family Applications Before (1)

Application Number Title Priority Date Filing Date
KR1020237012221A Ceased KR20230051723A (ko) 2016-10-18 2017-10-18 옥시스테롤 및 그의 사용 방법

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020257012306A Pending KR20250054838A (ko) 2016-10-18 2017-10-18 옥시스테롤 및 그의 사용 방법

Country Status (14)

Country Link
US (4) US11111266B2 (enExample)
EP (3) EP4105223B1 (enExample)
JP (3) JP2019532079A (enExample)
KR (3) KR20230051723A (enExample)
CN (3) CN115322238A (enExample)
AU (3) AU2017345399B2 (enExample)
DK (1) DK4105223T3 (enExample)
ES (2) ES3038660T3 (enExample)
IL (3) IL293231B2 (enExample)
MA (1) MA46565A (enExample)
MX (2) MX2019004679A (enExample)
RU (1) RU2019115112A (enExample)
TW (3) TWI772331B (enExample)
WO (1) WO2018075698A1 (enExample)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2012304412A1 (en) 2011-09-08 2014-03-27 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
PT2968369T (pt) 2013-03-13 2018-12-05 Sage Therapeutics Inc Esteroides neuroativos e métodos para o seu uso
WO2015195967A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
CN113292623A (zh) 2015-07-06 2021-08-24 萨奇治疗股份有限公司 孕甾醇及其使用方法
PT3319612T (pt) 2015-07-06 2021-08-24 Sage Therapeutics Inc Oxisteróis e métodos de utilização dos mesmos
ES2921010T3 (es) 2016-04-01 2022-08-16 Sage Therapeutics Inc Oxisteroles y procedimientos de uso de los mismos
US10752653B2 (en) 2016-05-06 2020-08-25 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
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
BR112019008032A2 (pt) 2016-10-18 2019-09-03 Sage Therapeutics, Inc. oxiesteróis e métodos de uso dos mesmos
EP4105223B1 (en) 2016-10-18 2025-04-30 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
US10857163B1 (en) 2019-09-30 2020-12-08 Athenen Therapeutics, Inc. Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof
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
US20230347291A1 (en) 2022-03-30 2023-11-02 Donaldson Company, Inc. System and method for reclaiming solvent
WO2024006537A1 (en) * 2022-07-01 2024-01-04 Intercept Pharmaceuticals, Inc. Methods for ameliorating cognitive impairment using bile acid derivatives
EP4622987A1 (en) * 2022-11-21 2025-10-01 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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150158903A1 (en) * 2011-09-08 2015-06-11 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof

Family Cites Families (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2259698A (en) 1938-05-07 1941-10-21 Rare Chemicals Inc Physiologically effective substance and process of preparing same
US2594323A (en) 1948-07-22 1952-04-29 Upjohn Co 24-substituted delta 5-cholene-3, 24-diols
US3079385A (en) 1961-01-24 1963-02-26 Roussel Uclaf Novel process of preparation of polyhydroxylated pregnanes
US3206459A (en) 1962-10-19 1965-09-14 Syntex Corp 10alpha-pregnan-19-ol derivatives
JPS5324071B2 (enExample) 1974-04-30 1978-07-18
US4071625A (en) 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
JPS5840960B2 (ja) 1976-12-28 1983-09-08 帝人株式会社 ヒドロキシコレステロ−ル立体異性体間の相互変換法
JPS54163565A (en) 1978-06-09 1979-12-26 Teijin Ltd 24*255epoxyy3beta * 266 dihydroxyychlestoo55ene or protected derivative of hydroxyl group thereof and production
US4269777A (en) 1979-05-21 1981-05-26 Wisconsin Alumni Research Foundation Isotopically labeled vitamin D derivatives and processes for preparing same
JPS5735597A (en) 1980-08-13 1982-02-26 Teijin Ltd 25,26-epoxy-3beta,24-dihydroxycholest-5-ene or its hydroxyl- protected derivative and their preparation
JPS61254599A (ja) 1985-05-07 1986-11-12 Sumitomo Pharmaceut Co Ltd コレステロ−ルのフツ素誘導体
JPS62187485A (ja) 1986-02-13 1987-08-15 Teijin Ltd ２４，２５−エポキシコレステロ−ル類の製造法
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
EP0382790A4 (en) 1987-08-25 1991-03-27 Kelvin W. Gee Compositions and methods for alleviating stress, anxiety and seizure activity
US5376645A (en) 1990-01-23 1994-12-27 University Of Kansas Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof
EP0701444B1 (en) 1993-05-24 2010-04-07 Purdue Pharma Ltd. Methods and compositions for inducing sleep
IL110309A0 (en) 1993-07-15 1994-10-21 Univ Kentucky Res Found A method of protecting against neuron loss
DE4338316A1 (de) 1993-11-10 1995-05-11 Jenapharm Gmbh Neue Steroide mit radikophilen Substituenten, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
BR9506779A (pt) 1994-02-14 1997-10-14 Cocensys Inc Composto composição farmacéutica método para modular o complexo ionóforo receptor gaba-cloreto em um paciente animal pela ligação ao sitio neuroesteróide no dito complexo método para tratar ou evitar estresse ou ansiedade em um paciente animal método para aliviar ou evitar isônia pms ou pnd em um paciente animal método para tratar ou evitar perturbacões na disposicão de ánimo em um paciente animal e método para induzir anestesia em um paciente animal
TW385308B (en) 1994-03-04 2000-03-21 Merck & Co Inc Prodrugs of morpholine tachykinin receptor antagonists
US5595996A (en) 1994-10-25 1997-01-21 Merck & Co., Inc. 7-substituted 4-aza cholanic acid derivatives and their use
BR9509764A (pt) 1994-11-23 1998-07-07 Cocensys Inc Série androstano e pregnano para modulação alostérica de receptor de gaba
JPH08268917A (ja) 1995-03-31 1996-10-15 D D S Kenkyusho:Kk 癌組織への移行性の高い制癌剤
PL185523B1 (pl) 1995-06-06 2003-05-30 Cocensys Inc Neuroaktywne steroidy z grupy pochodnych androstanu i pregnanu oraz kompozycja farmaceutyczna
US5792635A (en) 1995-06-07 1998-08-11 Magainin Pharmaceuticals, Inc. Method of inhibiting the sodium/proton exchanger NHE3 and method of inhibiting growth by administering squalamine
CA2224866A1 (en) 1995-06-23 1997-01-09 Novo Nordisk A/S Meiosis regulating compounds
US6645953B2 (en) 1995-06-23 2003-11-11 Novo Nordisk A/S Meiosis regulating compounds
US5888996A (en) 1995-07-26 1999-03-30 Trustees Of Boston University Inhibition of NMDA receptor activity and modulation of glutamate-mediated synaptic activity
JP4313435B2 (ja) 1995-07-24 2009-08-12 トラスティーズ オブ ボストン ユニバーシティー プレグネノロンサルフェート誘導体によるｎｍｄａレセプター活性の抑制
WO1997042215A1 (en) 1996-05-06 1997-11-13 Bionumerik Pharmaceuticals, Inc. Process for preparing 27-hydroxy cholesterol and related derivatives
JPH09328498A (ja) 1996-06-10 1997-12-22 Teijin Ltd ２４，２５−ジヒドロキシコレステロールの製造法およびその合成中間体
WO1998005337A1 (en) 1996-08-01 1998-02-12 Cocensys, Inc. Use of gaba and nmda receptor ligands for the treatment of migraine headache
DE19635525A1 (de) 1996-08-20 1998-02-26 Schering Ag 7alpha-(xi-Aminoalkyl)-estratriene, Verfahren zu deren Herstellung, pharmazeutische Präparate, die diese 7alpha(xi-Aminoalkyl-estratriene enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln
WO1999058497A1 (en) 1998-05-11 1999-11-18 Novo Nordisk A/S Substituted guanidines and diaminonitroethenes, their preparation and use
KR20010043558A (ko) 1998-05-13 2001-05-25 한센 핀 베네드, 안네 제헤르, 웨이콥 마리안느 감수분열 조절 화합물
US8541600B2 (en) 1998-11-24 2013-09-24 Harbor Therapeutics, Inc. 11-aza, 11-thia and 11-oxa sterol compounds and compositions
DE19917930A1 (de) 1999-04-15 2000-10-19 Schering Ag Ent-Steroide als selektiv wirksame Estrogene
YU77701A (sh) 1999-04-29 2005-07-19 Euro-Celtique S.A. 3-α-HIDROKSI-3Гџ-METOKSIMETIL-21-HETEROCIKLIČNO SUPSTITUISANI STEROIDI SA ANESTETIČKIM DEJSTVOM
US6376530B1 (en) 1999-05-10 2002-04-23 Merck & Co., Inc. Cyclic amidines useful as NMDA NR2B antagonists
GB9910934D0 (en) 1999-05-11 1999-07-14 Res Inst Medicine Chem Chemical compounds
CN1098273C (zh) 1999-11-12 2003-01-08 中国科学院上海有机化学研究所 高立体选择性的合成24r,25－和24s,25－二羟基甾体化合物
GB0000228D0 (en) 2000-01-06 2000-03-01 Phytopharm Plc Fluoro substituted sapogenins and their use
GB0019290D0 (en) 2000-08-04 2000-09-27 Symphar Sa Methods for inducing apolipoprotein E secretion
GR1003861B (el) 2000-12-29 2002-04-11 Νεα νευροστεροειδη που αλληλεπιδρουν με τον υποδοχεα gabaa.
GB0107822D0 (en) 2001-03-28 2001-05-23 Phytopharm Plc Sapogenin derivatives their synthesis and use methods based upon their use
ATE375994T1 (de) 2001-05-03 2007-11-15 Univ Chicago Leber x rezeptoragonisten
US20070197484A1 (en) 2001-05-03 2007-08-23 Ching Song Method of treating disorder related to high cholesterol concentration
TW200300078A (en) 2001-11-08 2003-05-16 Univ Chicago Method of treating disorder related to high cholesterol concentration
EP1461028A4 (en) 2001-12-07 2007-07-25 Univ California TREATMENT FOR AGE-RELATED MACULAR AGENCY
ATE424211T1 (de) 2002-03-27 2009-03-15 Phytopharm Plc Therapeutische verwendung von sapogeninen
KR101130212B1 (ko) 2002-03-27 2012-04-13 파이토팜 피엘씨 사포게닌 및 그 유도체의 치료 방법 및 사용법
US6933312B2 (en) 2002-10-07 2005-08-23 Agouron Pharmaceuticals, Inc. Pyrazole derivatives
AU2003288231A1 (en) 2002-12-13 2004-07-09 Bayer Healthcare Ag Cholesterol 24-hydroxylase (cyp46) as therapeutic target for the treatment of alzheimer's disease
FR2850023B1 (fr) 2003-01-17 2007-04-06 Mapreg Medicaments pour le systeme nerveux
GB0403889D0 (en) 2004-02-21 2004-03-24 Univ Edinburgh Uses of er-beta modulators
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
US20070032464A1 (en) 2004-10-08 2007-02-08 Shutsung Liao Methods of treating cancers
DE602005025391D1 (de) 2004-11-01 2011-01-27 Seo Hong Yoo Verfahren und zusammensetzungen zur verringerung der neurodegeneration bei amyotrophischer lateralsklerose
JP2009528291A (ja) 2006-02-27 2009-08-06 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア オキシステロール化合物及びヘッジホッグ経路
CN101164540A (zh) 2006-08-03 2008-04-23 中山大学 海洋甾体化合物在制备治疗神经元损伤药物中的应用
GB0619860D0 (en) 2006-10-06 2006-11-15 Birkeland Innovasjon As Treatment of insulin resistance and disorders associated therewith
WO2008057468A1 (en) 2006-11-02 2008-05-15 Curis, Inc. Small organic molecule regulators of cell proliferation
HUE036410T2 (hu) 2006-11-21 2018-07-30 Asarina Pharma Ab Pregnán és androsztán szteroidok alkalmazása CNS rendellenességek kezelésére szolgáló gyógyszerkészítmény elõállítására
AU2008331808B2 (en) 2007-03-16 2014-08-21 The Regents Of The University Of California Oxysterols for activation of hedgehog signaling, osteoinduction, antiadipogenesis, and Wnt signaling
CN101842355A (zh) 2007-06-20 2010-09-22 奥斯拜客斯制药有限公司 作为纤维化抑制剂的取代的n-芳基吡啶酮
GB0712494D0 (en) 2007-06-27 2007-08-08 Isis Innovation Substrate reduction therapy
EP2207542A2 (en) 2007-11-06 2010-07-21 N.V. Organon A method of hormone suppression in humans
WO2009090063A1 (en) 2008-01-16 2009-07-23 Jado Technologies Gmbh Steroid sapogenin, androstane and triterpenoid sapogenin derivatives for the treatment and prevention of infectious diseases
WO2009137843A2 (en) 2008-05-09 2009-11-12 Emory University Nmda receptor antagonists for the treatment of neuropsychiatric disorders
WO2010065709A2 (en) 2008-12-03 2010-06-10 Amin Khan Hydroxamic acid derivatives, preparation and therapeutic uses thereof
WO2010075282A1 (en) 2008-12-22 2010-07-01 University Of Washington Molecular inhibitors of the wnt/beta-catenin pathway
WO2010088408A2 (en) 2009-01-28 2010-08-05 Emory University Subunit selective nmda receptor antagonists for the treatment of neurological conditions
US8829213B2 (en) 2009-07-29 2014-09-09 The University Of Chicago Liver X receptor agonists
WO2011028794A2 (en) 2009-09-01 2011-03-10 Lazarus Therapeutics, Inc. Treatment of huntington's disease with cycloserine and an nmda receptor antagonist
FR2953138B1 (fr) 2009-12-02 2015-10-16 Assist Publ Hopitaux Marseille Composes aminosteroidiens pour une application topique locale pour la decolonisation cutaneo-muqueuse de staphylococcus aureus
WO2011092127A1 (en) 2010-01-26 2011-08-04 Bayer Schering Pharma Aktiengesellschaft 14,17-bridged estratriene derivatives comprising heterocyclic bioisosteres for the phenolic a-ring
KR101692275B1 (ko) 2010-02-11 2017-01-04 노오쓰웨스턴 유니버시티 ２차 구조 안정화된 ｎｍｄａ 수용체 조절제 및 그의 용도
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
US20120035156A1 (en) 2010-08-09 2012-02-09 Daniela Alberati Combination of glyt1 compound with antipsychotics
US8969525B2 (en) 2010-11-09 2015-03-03 Enzo Life Sciences, Inc. Hydroxycholesterol immunoassay
US20150031655A1 (en) 2011-04-15 2015-01-29 University Of North Dakota Combination of liver x receptor modulator and estrogen receptor modulator for the treatment of age-related diseases
US20140335050A1 (en) 2011-05-27 2014-11-13 The General Hospital Corporation Methods, compositions, and kits for the treatment of cancer
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
PT2766380T (pt) 2011-10-14 2019-07-29 Sage Therapeutics Inc Compostos de 19-nor pregnano 3,3-dissubstituídos, composições e seus usos
US20150119327A1 (en) 2012-04-25 2015-04-30 The Regents Of The University Of California Drug screening platform for rett syndrome
WO2014025942A1 (en) 2012-08-09 2014-02-13 Emory University Nmda receptor modulators and uses related thereto
WO2014028942A2 (en) 2012-08-17 2014-02-20 Trueex Group Llc Interoffice bank offered rate financial product and implementation
KR102400891B1 (ko) 2012-12-18 2022-05-20 워싱톤 유니버시티 신경활성 19-알콕시-17-치환된 스테로이드, 그의 전구약물, 및 그를 사용한 치료 방법
CN105073119A (zh) 2013-01-23 2015-11-18 司菲埃拉制药私人有限公司 用于线粒体生物发生和与线粒体功能障碍或耗竭相关的疾病的新颖11β-羟基类固醇化合物
WO2014120786A1 (en) 2013-01-29 2014-08-07 Naurex, Inc. Spiro-lactam nmda receptor modulators and uses thereof
HK1220472A1 (zh) * 2013-03-13 2017-05-05 萨奇治疗股份有限公司 神经活性类固醇、组合物、及其用途
PT2968369T (pt) 2013-03-13 2018-12-05 Sage Therapeutics Inc Esteroides neuroativos e métodos para o seu uso
PL2986624T3 (pl) * 2013-04-17 2020-11-16 Sage Therapeutics, Inc. Neuroaktywne steroidy 19-NOR do stosowania w sposobach leczenia
HK1222565A1 (zh) 2013-09-25 2017-07-07 范安德尔研究所 高效糖皮質激素
MX388168B (es) 2014-02-08 2025-03-19 Genentech Inc Un anticuerpo anti-amiloide beta (a?) monoclonal humanizado para usarse en el tratamiento de enfermedad de alzheimer.
WO2015195967A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
EP3166613A4 (en) 2014-07-09 2018-02-21 Duke University Compositions and methods for the repair of myelin
CA2963938C (en) 2014-10-07 2023-10-24 Sage Therapeutics, Inc. Neuroactive compounds and methods of use thereof
CN113292623A (zh) 2015-07-06 2021-08-24 萨奇治疗股份有限公司 孕甾醇及其使用方法
PT3319612T (pt) 2015-07-06 2021-08-24 Sage Therapeutics Inc Oxisteróis e métodos de utilização dos mesmos
EP3319610A4 (en) 2015-07-06 2019-03-06 Sage Therapeutics, Inc. OXYSTEROLS AND METHOD OF USE THEREOF
GB2557875A (en) 2015-09-02 2018-07-04 Univ Swansea Diagnostic methods and kits
ES2921010T3 (es) 2016-04-01 2022-08-16 Sage Therapeutics Inc Oxisteroles y procedimientos de uso de los mismos
US10752653B2 (en) 2016-05-06 2020-08-25 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
AU2017296295B2 (en) 2016-07-11 2022-02-24 Sage Therapeutics, Inc. C7, C12, and C16 substituted neuroactive steroids and their methods of use
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
BR112019008032A2 (pt) 2016-10-18 2019-09-03 Sage Therapeutics, Inc. oxiesteróis e métodos de uso dos mesmos
EP4105223B1 (en) 2016-10-18 2025-04-30 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
AU2018234828A1 (en) 2017-03-15 2019-09-19 Modernatx, Inc. Lipid nanoparticle formulation
BR112019027458A2 (pt) 2017-06-23 2020-07-07 Intercept Pharmaceuticals, Inc. métodos e intermediários para a preparação de derivados de ácidos biliares
US20190160078A1 (en) 2017-11-10 2019-05-30 Marinus Pharmaceuticals, Inc. Ganaxolone for use in treating genetic epileptic disorders

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20150158903A1 (en) * 2011-09-08 2015-06-11 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof

Also Published As

Publication number Publication date
MA46565A (fr) 2019-08-28
US20230331768A1 (en) 2023-10-19
IL293231B2 (en) 2025-10-01
AU2024202773A1 (en) 2024-05-16
TWI772331B (zh) 2022-08-01
AU2022200810A1 (en) 2022-02-24
CN114891056A (zh) 2022-08-12
IL266092B2 (en) 2023-08-01
IL266092A (en) 2019-06-30
ES3038660T3 (en) 2025-10-14
JP2023063535A (ja) 2023-05-09
JP2019532079A (ja) 2019-11-07
MX2022005160A (es) 2022-06-08
US11111266B2 (en) 2021-09-07
WO2018075698A1 (en) 2018-04-26
TW201827057A (zh) 2018-08-01
ES2968140T3 (es) 2024-05-08
AU2017345399B2 (en) 2022-02-24
KR20250054838A (ko) 2025-04-23
RU2019115112A3 (enExample) 2020-12-15
CN110072874A (zh) 2019-07-30
CA3041077A1 (en) 2018-04-26
BR112019008069A2 (pt) 2019-09-03
TW202446399A (zh) 2024-12-01
KR20230051723A (ko) 2023-04-18
JP7304444B2 (ja) 2023-07-06
CN115322238A (zh) 2022-11-11
RU2019115112A (ru) 2020-11-24
CN110072874B (zh) 2022-08-12
US20220024968A1 (en) 2022-01-27
EP4105223B1 (en) 2025-04-30
AU2022200810B2 (en) 2024-02-01
DK4105223T3 (da) 2025-07-07
IL293231B1 (en) 2025-06-01
MX2019004679A (es) 2019-10-15
EP3529256A1 (en) 2019-08-28
IL293231A (en) 2022-07-01
EP4616908A3 (en) 2025-11-26
KR20190065429A (ko) 2019-06-11
EP4616908A2 (en) 2025-09-17
NZ752728A (en) 2024-08-30
TWI836485B (zh) 2024-03-21
JP2022033255A (ja) 2022-02-28
IL266092B1 (en) 2023-04-01
US11613556B2 (en) 2023-03-28
US20250179112A1 (en) 2025-06-05
US12180247B2 (en) 2024-12-31
EP4105223A1 (en) 2022-12-21
US20200123195A1 (en) 2020-04-23
AU2017345399A1 (en) 2019-05-09
IL320521A (en) 2025-06-01
EP3529256B1 (en) 2023-08-09
TW202317138A (zh) 2023-05-01

Similar Documents

Publication Publication Date Title
KR102521573B1 (ko) 옥시스테롤 및 그의 사용 방법
KR102583278B1 (ko) 옥시스테롤 및 그의 사용 방법
CN121085986A (zh) C7取代的氧固醇及其作为nmda调节剂的方法
JP2025184962A (ja) オキシステロールおよびその使用方法
HK40102021A (en) Oxysterols and methods of use thereof
HK40083913A (en) Oxysterols and methods of use thereof
HK40006309B (en) Oxysterols and methods of use thereof
HK40006309A (en) Oxysterols and methods of use thereof
HK40006820A (en) Oxysterols and methods of use thereof
HK40006820B (en) Oxysterols and methods of use thereof

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20190517

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20201016

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20220930

Patent event code: PE09021S01D

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

Patent event code: PE07011S01D

Comment text: Decision to Grant Registration

Patent event date: 20230109

A107 Divisional application of patent
GRNT Written decision to grant
PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20230410

PR0701 Registration of establishment

Comment text: Registration of Establishment

Patent event date: 20230410

Patent event code: PR07011E01D

PR1002 Payment of registration fee

Payment date: 20230411

End annual number: 3

Start annual number: 1

PG1601 Publication of registration