CN108976272B - 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途 - Google Patents

3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途 Download PDF

Info

Publication number
CN108976272B
CN108976272B CN201810869360.3A CN201810869360A CN108976272B CN 108976272 B CN108976272 B CN 108976272B CN 201810869360 A CN201810869360 A CN 201810869360A CN 108976272 B CN108976272 B CN 108976272B
Authority
CN
China
Prior art keywords
substituted
unsubstituted
group
alkyl
compound
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
CN201810869360.3A
Other languages
English (en)
Chinese (zh)
Other versions
CN108976272A (zh
Inventor
R.B.尤帕萨尼
B.C.艾斯丘
B.L.哈里森
F.G.萨里特洛
A.J.罗比乔德
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 CN108976272A publication Critical patent/CN108976272A/zh
Application granted granted Critical
Publication of CN108976272B publication Critical patent/CN108976272B/zh
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
    • 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
    • A61P25/14—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
    • A61P27/16—Otologicals
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • 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
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • 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
    • 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)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Public Health (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Fats And Perfumes (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201810869360.3A 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途 Active CN108976272B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161547291P 2011-10-14 2011-10-14
US61/547,291 2011-10-14
US201261698204P 2012-09-07 2012-09-07
US61/698,204 2012-09-07
CN201280060883.4A CN104136452A (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201280060883.4A Division CN104136452A (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途

Publications (2)

Publication Number Publication Date
CN108976272A CN108976272A (zh) 2018-12-11
CN108976272B true CN108976272B (zh) 2021-05-25

Family

ID=47143295

Family Applications (4)

Application Number Title Priority Date Filing Date
CN202110494113.1A Pending CN113234114A (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
CN201280060883.4A Pending CN104136452A (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
CN202411226456.XA Pending CN119192266A (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
CN201810869360.3A Active CN108976272B (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途

Family Applications Before (3)

Application Number Title Priority Date Filing Date
CN202110494113.1A Pending CN113234114A (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
CN201280060883.4A Pending CN104136452A (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
CN202411226456.XA Pending CN119192266A (zh) 2011-10-14 2012-10-12 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途

Country Status (9)

Country Link
US (5) US20150291654A1 (enExample)
EP (2) EP2766380B1 (enExample)
JP (5) JP2014528485A (enExample)
CN (4) CN113234114A (enExample)
AU (5) AU2012323888A1 (enExample)
CA (2) CA3152410A1 (enExample)
ES (1) ES2738526T3 (enExample)
PT (1) PT2766380T (enExample)
WO (1) WO2013056181A1 (enExample)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1959966B1 (en) 2005-11-28 2020-06-03 Marinus Pharmaceuticals, Inc. Ganaxolone formulations and methods for the making and use thereof
WO2013036835A1 (en) 2011-09-08 2013-03-14 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
CN113234114A (zh) 2011-10-14 2021-08-10 萨奇治疗股份有限公司 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
CA2862076C (en) 2012-01-23 2020-04-21 Sage Therapeutics, Inc. Neuroactive steroid formulations and methods of treating cns disorders
PL2887944T3 (pl) 2012-08-21 2022-02-21 Sage Therapeutics, Inc. Allopregnanolon do leczenia lekoopornego stanu padaczkowego
JP2016501876A (ja) 2012-11-30 2016-01-21 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 ステロイドの抗痙攣活性
RS67266B1 (sr) 2013-03-13 2025-10-31 Sage Therapeutics Inc Neuroaktivni steroidi i postupci za njihovu upotrebu
WO2014169832A1 (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
WO2014169836A1 (en) * 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
MX362543B (es) 2013-04-17 2019-01-24 Sage Therapeutics Inc Esteroides c21-n-pirazolilo 19-nor c3,3- disustituidos y metodos de uso de los mismos.
HRP20210610T1 (hr) 2013-07-19 2021-05-28 Sage Therapeutics, Inc. Neuroaktivni steroidi, pripravci i njihove uporabe
PT3035940T (pt) * 2013-08-23 2019-01-28 Sage Therapeutics Inc Esteroides neuroativos, composições e seus usos
SG10201803812TA (en) * 2014-05-29 2018-06-28 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof
WO2015195962A1 (en) * 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
WO2015195967A1 (en) * 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
JOP20200195A1 (ar) 2014-09-08 2017-06-16 Sage Therapeutics Inc سترويدات وتركيبات نشطة عصبياً، واستخداماتها
US20160168190A1 (en) * 2014-09-17 2016-06-16 Prevacus, Inc. C-20 steroid compounds, compositions and uses thereof to treat traumatic brain injury (tbi), including concussions
EP3885352B1 (en) * 2014-10-16 2024-11-27 Sage Therapeutics, Inc. A compound, compositions thereof and this compound for use in methods of treating cns disorders
EP4275748A3 (en) * 2014-10-16 2024-01-03 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
RS60343B1 (sr) 2014-11-27 2020-07-31 Sage Therapeutics Inc Kompozicije i postupci za lečenje poremećaja cns-a
SMT202100113T1 (it) 2015-01-26 2021-05-07 Sage Therapeutics Inc Composizioni e metodi per trattare disturbi del snc
EP3258939B1 (en) 2015-02-20 2022-09-07 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
EP3280420B1 (en) * 2015-04-10 2024-03-27 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
MA45276A (fr) 2015-06-18 2018-04-25 Sage Therapeutics Inc Solutions de stéroïdes neuroactifs et leurs méthodes d'utilisation
BR112018000129B1 (pt) 2015-07-06 2024-01-09 Sage Therapeutics, Inc Compostos oxiesteróis, seus usos e composição farmacêutica
SMT202100476T1 (it) 2015-07-06 2021-09-14 Sage Therapeutics Inc Ossisteroli e metodi di uso degli stessi
JP6882996B2 (ja) 2015-07-06 2021-06-02 セージ セラピューティクス， インコーポレイテッド オキシステロールおよびそれらの使用の方法
CA3001722A1 (en) 2015-10-16 2017-04-20 Marinus Pharmaceuticals, Inc. Injectable neurosteroid formulations containing nanoparticles
CN113616661A (zh) 2016-03-08 2021-11-09 萨奇治疗股份有限公司 神经活性类固醇、其组合物及用途
SI3436022T1 (sl) * 2016-04-01 2022-08-31 Sage Therapeutics, Inc. Oksisteroli in postopki za uporabo le-teh
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
ES2884071T3 (es) 2016-07-07 2021-12-10 Sage Therapeutics Inc 24-hidroxiesteroles sustituidos en 11 para el tratamiento de afecciones relacionadas con NMDA
AU2017296295B2 (en) 2016-07-11 2022-02-24 Sage Therapeutics, Inc. C7, C12, and C16 substituted neuroactive steroids and their methods of use
MA45599A (fr) * 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
US20180042903A1 (en) 2016-08-11 2018-02-15 Ovid Therapeutics Inc. Methods and compositions for treatment of epileptic disorders
JOP20190022B1 (ar) 2016-08-23 2023-03-28 Sage Therapeutics Inc ستيرويد 19- نور c3، 3- به استبدال ثنائي لـ c21-n بيرازوليل بلوري
US10391105B2 (en) 2016-09-09 2019-08-27 Marinus Pharmaceuticals Inc. Methods of treating certain depressive disorders and delirium tremens
MX392270B (es) 2016-09-30 2025-03-24 Sage Therapeutics Inc Oxisteroles sustituidos en c7 y metodos de uso de los mismos.
CN110267966B (zh) 2016-10-18 2022-07-08 萨奇治疗股份有限公司 氧甾醇及其使用方法
EP4105223B1 (en) * 2016-10-18 2025-04-30 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
WO2019075362A1 (en) * 2017-10-12 2019-04-18 Sage Therapeutics, Inc. METHOD OF TREATING CENTRAL NERVOUS SYSTEM DISORDERS WITH NEUROSTEROIDS AND GABAERGIC COMPOUNDS
US20200291059A1 (en) 2017-12-08 2020-09-17 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
CN118271387A (zh) 2017-12-22 2024-07-02 萨奇治疗股份有限公司 治疗cns疾病的组合物和方法
MX2020008422A (es) * 2018-02-11 2020-09-21 Jiangsu Hansoh Pharmaceutical Group Co Ltd Regulador derivado de esteroides, metodo para prepararlos y usos de los mismos.
CN114085260B (zh) 2018-02-11 2023-10-20 江苏豪森药业集团有限公司 甾族类衍生物调节剂、其制备方法和应用
TW202521129A (zh) 2018-12-05 2025-06-01 美商賽吉醫療公司 神經活性類固醇及其使用方法
WO2020118142A1 (en) 2018-12-07 2020-06-11 Marinus Pharmaceuticals, Inc. Ganaxolone for use in prophylaxis and treatment of pospartum depression
US20220372067A1 (en) 2018-12-21 2022-11-24 Sage Therapeutics, Inc. 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof
AR119047A1 (es) 2019-05-31 2021-11-17 Sage Therapeutics Inc Esteroides neuroactivos como moduladores de gabaa y su uso en el tratamiento de trastornos del snc
CA3145923A1 (en) 2019-08-05 2021-02-11 David Czekai Ganaxolone for use in treatment of status epilepticus
KR102890254B1 (ko) * 2019-08-07 2025-11-24 상하이 한서 바이오메디컬 컴퍼니 리미티드 스테로이드 유도체 조절제의 염 및 결정형
US10857163B1 (en) 2019-09-30 2020-12-08 Athenen Therapeutics, Inc. Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof
WO2021113068A1 (en) * 2019-12-05 2021-06-10 Sparx Therapeutics, Inc. Neuroactive steroids and compositions and methods thereof
IL293525A (en) 2019-12-06 2022-08-01 Marinus Pharmaceuticals Inc Ganaxolone for use in the treatment of multiple sclerosis complex
WO2021174205A1 (en) * 2020-02-27 2021-09-02 Brii Biosciences, Inc. Prodrugs of neuroactive steroids
EP4125921A1 (en) 2020-03-25 2023-02-08 Sage Therapeutics, Inc. Use of agents for treatment of respiratory conditions
EP4377327A1 (en) 2021-07-28 2024-06-05 Sage Therapeutics, Inc. Crystalline forms of a neuroactive steroid
WO2023237097A1 (zh) * 2022-06-09 2023-12-14 山东绿叶制药有限公司 19-去甲c3,3-二取代的c21-氮杂环取代类固醇及其使用方法
WO2024059608A1 (en) 2022-09-15 2024-03-21 Sage Therapeutics, Inc. Deuterated neuroactive steroids
KR20250162825A (ko) 2023-03-14 2025-11-19 쿠리아 스페인, 에스.에이.유. 3알파-하이드록시-3베타-알킬 스테로이드의 제조를 위한 방법 및 중간체
WO2025119319A1 (zh) * 2023-12-08 2025-06-12 山东绿叶制药有限公司 一种gabaa受体调节剂的晶型及其制备方法和应用

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996016076A1 (en) * 1994-11-23 1996-05-30 Cocensys, Inc. Androstane and pregnane series for allosteric modulation of gaba receptor
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

Family Cites Families (95)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1994E (fr) 1902-11-20 1903-11-24 Jules Bernard Dispositif de suspension élastique amortisseur de chocs pour chassis, caisses de véhicules, sièges et sommiers élastiques
US2856415A (en) 1957-11-13 1958-10-14 Searle & Co 3,19-dihydroxy-5-androstene derivatives
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
GB1380246A (en) 1970-12-17 1975-01-08 Glaxo Lab Ltd 3alpha-hydroxy-androstanes and esters thereof
US3983111A (en) 1972-05-05 1976-09-28 Glaxo Laboratories Limited Steroidal anaesthetics of the pregnane and 19-norpregnane series
GB1430942A (en) 1972-05-05 1976-04-07 Glaxo Lab Ltd 21-substituted 3alpha-hydroxy pregnanes
GB1436324A (en) 1972-05-12 1976-05-19 Glaxo Lab Ltd Anaesthetic 3alpha-hydroxy pregnanes
US4071625A (en) 1974-05-13 1978-01-31 Richardson-Merrell Inc. 19-Oxygenated-5α-androstanes for the enhancement of libido
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
GB1570394A (en) 1976-01-06 1980-07-02 Glaxo Lab Ltd 11-acyloxy-3-hydroxy steroids
US4192871A (en) * 1976-01-06 1980-03-11 Glaxo Laboratories Limited Chemical compounds
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
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
WO1989002272A1 (en) * 1987-08-25 1989-03-23 Gee Kelvin W 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
EP0603312A4 (en) 1991-09-13 1995-06-07 Cocensys Inc NEW GABA A RECEPTOR WITH STEROID BINDING POINTS.
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
JP4008024B2 (ja) * 1993-05-24 2007-11-14 パーデュー、ファーマ、リミテッド、パートナーシップ Ｇａｂａａレセプター複合体と相互作用させるための化合物
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
EP0656365B1 (en) 1993-12-02 1997-04-09 Akzo Nobel N.V. Substituted 2beta-morpholinoandrostane derivatives
DK1038880T3 (da) * 1994-02-14 2008-03-03 Euro Celtique Sa Androstaner og pregnaner til allosterisk modulering af GABA-receptor
WO1996003421A1 (en) 1994-07-21 1996-02-08 Pharmacia & Upjohn Company Neurologically active aminosteroids
CA2223996A1 (en) 1995-06-06 1996-12-19 Cocensys, Inc. Neuroactive steroids of the androstane and pregnane series
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
HUP0201818A3 (en) 1999-04-29 2004-04-28 Euro Celtique Sa 3alpha-hydroxy-3beta-methoxymethyl-21-heterocycle substituted steroids with anesthetic activity and pharmaceutical compositions containing the same
US7018406B2 (en) 1999-11-17 2006-03-28 Corevalve Sa Prosthetic valve for transluminal delivery
ATE297406T1 (de) 2000-02-18 2005-06-15 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
EP1330467B1 (en) 2000-11-03 2007-05-02 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.
AU2004224053B2 (en) 2003-03-24 2011-06-09 Sterix Limited Oestrogen derivatives as inhibitors of steroid sulphatase
US7781421B2 (en) 2003-05-29 2010-08-24 Washington University Neuroactive 13, 24-cyclo-18, 21-dinorcholanes and structurally related pentacyclic steriods
JP2007512344A (ja) 2003-11-24 2007-05-17 メルク　エンド　カムパニー　インコーポレーテッド エストロゲン受容体調節剤
US20090118248A1 (en) 2004-04-23 2009-05-07 Euro-Celtique S.A. 3-Alpha-hydroxy 21-n-heteroaryl-pregnane derivatives for modulation of brain excitability and a process for the production thereof
WO2006037016A2 (en) 2004-09-27 2006-04-06 The Regents Of The University Of California Novel therapy for treatment of chronic degenerative brain diseases and nervous system injury
EP2471536A1 (en) 2004-09-29 2012-07-04 Harbor BioSciences, Inc. Steroid analogs and characterization and treatment methods
DE602006013622D1 (de) 2005-06-09 2010-05-27 Euro Celtique Sa Steroids und anwendungen davon
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
CA2698172C (en) 2007-06-15 2014-02-18 Cook, Kevin M. 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
CZ301216B6 (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
US20110152840A1 (en) 2009-12-23 2011-06-23 Drugtech Corporation Methods for reducing the occurrence of preterm delivery and other pregnancy-related conditions
EP2598513A1 (en) 2010-07-30 2013-06-05 Medexis S.A. Compounds and methods for treating neoplasia
EP2667876A2 (en) 2010-12-15 2013-12-04 Harbor BioSciences, Inc. Methods and compounds for preparing 3alpha-oxygen substituted steroids
CZ303443B6 (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
CA2828047C (en) 2011-02-15 2020-03-10 Socpra Sciences Et Genie, 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
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
US9851309B2 (en) 2011-03-23 2017-12-26 Satoshi Watabe Ultra-high-sensitive assay of protein and nucleic acid and kit, 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
WO2013036835A1 (en) 2011-09-08 2013-03-14 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
CN113234114A (zh) 2011-10-14 2021-08-10 萨奇治疗股份有限公司 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
WO2013188792A2 (en) 2012-06-15 2013-12-19 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
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
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
US9757391B2 (en) 2012-11-09 2017-09-12 Goodchild Investments Pty Ltd Neuroactive steroids and their use to facilitate neuroprotection
SG10201706063UA (en) 2012-12-18 2017-09-28 Univ Washington Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same
US8939545B2 (en) 2012-12-20 2015-01-27 Eastman Kodak Company Inkjet printing with managed airflow for condensation control
US9562026B2 (en) 2013-03-14 2017-02-07 Washington University Neuroactive substituted cyclopent[a]anthracenes as modulators for GABA type-A receptors
MX362543B (es) 2013-04-17 2019-01-24 Sage Therapeutics Inc Esteroides c21-n-pirazolilo 19-nor c3,3- disustituidos y metodos de uso de los mismos.
WO2014169832A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive 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
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
HRP20210610T1 (hr) 2013-07-19 2021-05-28 Sage Therapeutics, Inc. Neuroaktivni steroidi, pripravci i njihove uporabe
PT3035940T (pt) 2013-08-23 2019-01-28 Sage Therapeutics Inc Esteroides neuroativos, composições e seus usos
SG10201803812TA (en) 2014-05-29 2018-06-28 Sage Therapeutics Inc Neuroactive steroids, compositions, and uses thereof
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
EP3885352B1 (en) 2014-10-16 2024-11-27 Sage Therapeutics, Inc. A compound, compositions thereof and this compound for use in methods of treating cns disorders
EP4275748A3 (en) 2014-10-16 2024-01-03 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
RS60343B1 (sr) 2014-11-27 2020-07-31 Sage Therapeutics Inc Kompozicije i postupci za lečenje poremećaja cns-a
SMT202100113T1 (it) 2015-01-26 2021-05-07 Sage Therapeutics Inc Composizioni e metodi per trattare disturbi del snc
EP3258939B1 (en) 2015-02-20 2022-09-07 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
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
WO2017044659A1 (en) 2015-09-08 2017-03-16 Viewpoint Therapeutics, Inc. Compounds and formulations for treating ophthalmic diseases
CA3001722A1 (en) 2015-10-16 2017-04-20 Marinus Pharmaceuticals, Inc. Injectable neurosteroid formulations containing nanoparticles
MA43284A (fr) 2015-11-20 2018-09-26 Sage Therapeutics Inc Composés et leurs méthodes d'utilisation
CN113616661A (zh) 2016-03-08 2021-11-09 萨奇治疗股份有限公司 神经活性类固醇、其组合物及用途
US10226550B2 (en) 2016-03-11 2019-03-12 Brigham Young University Cationic steroidal antimicrobial compositions for the treatment of dermal tissue
AU2017296295B2 (en) 2016-07-11 2022-02-24 Sage Therapeutics, Inc. C7, C12, and C16 substituted neuroactive steroids and their methods of use
MA45599A (fr) 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
JOP20190022B1 (ar) 2016-08-23 2023-03-28 Sage Therapeutics Inc ستيرويد 19- نور c3، 3- به استبدال ثنائي لـ c21-n بيرازوليل بلوري
US11285139B2 (en) 2017-08-31 2022-03-29 Takeda Pharmaceutical Company Limited Treatment of CNS conditions

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO1996016076A1 (en) * 1994-11-23 1996-05-30 Cocensys, Inc. Androstane and pregnane series for allosteric modulation of gaba receptor

Also Published As

Publication number Publication date
AU2019203046A1 (en) 2019-05-23
AU2019203046B2 (en) 2021-04-08
JP2022130546A (ja) 2022-09-06
US20150291654A1 (en) 2015-10-15
CN104136452A (zh) 2014-11-05
US20230287037A1 (en) 2023-09-14
JP7617057B2 (ja) 2025-01-17
US20200223884A1 (en) 2020-07-16
EP3572417B1 (en) 2025-12-17
AU2023204015A1 (en) 2023-07-13
AU2017208284B2 (en) 2019-01-31
JP7096864B2 (ja) 2022-07-06
CA2852057A1 (en) 2013-04-18
JP2025061026A (ja) 2025-04-10
CA2852057C (en) 2022-06-07
AU2017208284A1 (en) 2017-08-10
JP6745783B2 (ja) 2020-08-26
HK1201274A1 (en) 2015-08-28
CN119192266A (zh) 2024-12-27
WO2013056181A1 (en) 2013-04-18
JP2014528485A (ja) 2014-10-27
ES2738526T3 (es) 2020-01-23
AU2021204782B2 (en) 2023-04-13
US10435431B2 (en) 2019-10-08
EP2766380A1 (en) 2014-08-20
US20210040141A1 (en) 2021-02-11
AU2012323888A1 (en) 2014-05-29
JP2018058888A (ja) 2018-04-12
CN113234114A (zh) 2021-08-10
JP2020189851A (ja) 2020-11-26
PT2766380T (pt) 2019-07-29
EP3572417A3 (en) 2020-03-25
CN108976272A (zh) 2018-12-11
EP3572417A2 (en) 2019-11-27
AU2021204782A1 (en) 2021-08-05
EP2766380B1 (en) 2019-04-24
US20170342103A1 (en) 2017-11-30
AU2023204015B2 (en) 2025-09-11
CA3152410A1 (en) 2013-04-18

Similar Documents

Publication Publication Date Title
CN108976272B (zh) 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
AU2025203873A1 (en) Neuroactive steroids, compositions, and uses thereof
HK40001824A (en) 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
HK40001824B (zh) 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途
HK40018206A (en) 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof
HK1201274B (en) 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40001824

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant