TWI874337B - 神經活性類固醇及其使用方法 - Google Patents
神經活性類固醇及其使用方法 Download PDFInfo
- Publication number
- TWI874337B TWI874337B TW108144589A TW108144589A TWI874337B TW I874337 B TWI874337 B TW I874337B TW 108144589 A TW108144589 A TW 108144589A TW 108144589 A TW108144589 A TW 108144589A TW I874337 B TWI874337 B TW I874337B
- Authority
- TW
- Taiwan
- Prior art keywords
- compound
- substituted
- unsubstituted
- group
- pharmaceutically acceptable
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61P25/08—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
- A61P25/24—Antidepressants
-
- 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
- C07J41/0044—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group
-
- 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
- C07J41/0055—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 at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Toxicology (AREA)
- Biomedical Technology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862775470P | 2018-12-05 | 2018-12-05 | |
| US62/775,470 | 2018-12-05 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202039528A TW202039528A (zh) | 2020-11-01 |
| TWI874337B true TWI874337B (zh) | 2025-03-01 |
Family
ID=69006056
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108144589A TWI874337B (zh) | 2018-12-05 | 2019-12-05 | 神經活性類固醇及其使用方法 |
| TW114104450A TW202521127A (zh) | 2018-12-05 | 2019-12-05 | 神經活性類固醇及其使用方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW114104450A TW202521127A (zh) | 2018-12-05 | 2019-12-05 | 神經活性類固醇及其使用方法 |
Country Status (14)
| Country | Link |
|---|---|
| US (8) | US20230322846A9 (enExample) |
| EP (1) | EP3902818A1 (enExample) |
| JP (3) | JP7539378B2 (enExample) |
| KR (2) | KR20250174100A (enExample) |
| CN (1) | CN113383004A (enExample) |
| AR (1) | AR117264A1 (enExample) |
| AU (3) | AU2019392680B2 (enExample) |
| BR (1) | BR112021010996A2 (enExample) |
| CA (1) | CA3120872A1 (enExample) |
| IL (3) | IL312610B1 (enExample) |
| MA (1) | MA54594A (enExample) |
| MX (4) | MX2021006618A (enExample) |
| TW (2) | TWI874337B (enExample) |
| WO (1) | WO2020118060A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2806877B2 (en) | 2012-01-23 | 2025-01-29 | Sage Therapeutics, Inc. | Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin |
| CA2882708A1 (en) | 2012-08-21 | 2014-02-27 | Sage Therapeutics, Inc. | Methods of treating epilepsy or status epilepticus |
| KR102396328B1 (ko) | 2013-04-17 | 2022-05-10 | 세이지 테라퓨틱스, 인크. | 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법 |
| US10246482B2 (en) | 2014-06-18 | 2019-04-02 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| JOP20200195A1 (ar) | 2014-09-08 | 2017-06-16 | Sage Therapeutics Inc | سترويدات وتركيبات نشطة عصبياً، واستخداماتها |
| WO2016082789A1 (en) | 2014-11-27 | 2016-06-02 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| EP3504189A1 (en) | 2016-08-23 | 2019-07-03 | Sage Therapeutics, Inc. | A crystalline 19-nor c3, 3-disubstituted c21-n-pyrazolyl steroid |
| MA51046A (fr) | 2017-12-08 | 2021-03-17 | Sage Therapeutics Inc | Dérivés de 21-[4-cyano-pyrazol-1-yl]-19-nor-pregan-3. alpha-ol-20-one deutérés pour le traitement de troubles du snc |
| MX2020006599A (es) * | 2017-12-22 | 2020-11-06 | Sage Therapeutics Inc | Composiciones y metodos para el tratamiento de trastornos en el sistema nervioso central. |
| TW201930269A (zh) | 2018-01-12 | 2019-08-01 | 美商賽吉醫療公司 | 用於治療cns病症之組合物及方法 |
| WO2020132504A1 (en) * | 2018-12-21 | 2020-06-25 | Sage Therapeutics, Inc. | 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof |
| SG11202112391UA (en) | 2019-05-31 | 2021-12-30 | Sage Therapeutics Inc | Neuroactive steroids and compositions thereof |
| CN114729000A (zh) * | 2019-06-27 | 2022-07-08 | 萨奇治疗股份有限公司 | 用于治疗cns病症的化合物 |
| CA3143509A1 (en) * | 2019-06-27 | 2020-12-30 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| WO2021188778A2 (en) * | 2020-03-18 | 2021-09-23 | Sage Therapeutics, Inc. | Neuroactive steroids and their methods of use |
| CN112679571A (zh) * | 2020-12-24 | 2021-04-20 | 广西壮族自治区中国科学院广西植物研究所 | 一种罗汉果醇衍生物单体、其制备方法及应用 |
| JP2024532273A (ja) * | 2021-08-25 | 2024-09-05 | セージ セラピューティクス, インコーポレイテッド | ポジティブnmdaモジュレート化合物及びその使用方法 |
| 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 |
| JP2026509303A (ja) | 2023-03-14 | 2026-03-17 | キュリア、スペイン、エセ、ア、ウ | 3アルファ-ヒドロキシ-3ベータ-アルキルステロイドを調製するための方法および中間体 |
| WO2024197317A2 (en) * | 2023-03-23 | 2024-09-26 | Emory University | Neurosteroids and prodrugs thereof |
| CN119529013B (zh) * | 2024-11-25 | 2025-11-07 | 湖南新合新生物医药有限公司 | 一种祖拉诺龙中间体的合成方法 |
Citations (3)
| 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 |
| WO1998005337A1 (en) * | 1996-08-01 | 1998-02-12 | Cocensys, Inc. | Use of gaba and nmda receptor ligands for the treatment of migraine headache |
| WO2017049044A1 (en) * | 2015-09-16 | 2017-03-23 | Bartolucci Giampiero | Ursodeoxycholic acid and brain disorders |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2969M (fr) * | 1963-05-22 | 1964-11-30 | Roussel Uclaf | Nouveau médicament notamment pour le traitement des spasmes d'origine coronarienne on viscérale. |
| ES432106A1 (es) | 1973-11-30 | 1976-11-01 | Schering Ag | Procedimiento para la preparacion de d-homo-20-cetopregna- nos. |
| IL48628A0 (en) | 1974-12-23 | 1976-02-29 | Schering Ag | D-homo-20-keto-pregnanes and process for their manufactur |
| GB1570394A (en) | 1976-01-06 | 1980-07-02 | Glaxo Lab Ltd | 11-acyloxy-3-hydroxy steroids |
| US4060295A (en) | 1976-03-15 | 1977-11-29 | Molex Incorporated | Zero insertion force printed circuit board edge connector assembly |
| GB1581234A (en) | 1976-04-05 | 1980-12-10 | Glaxo Operations Ltd | 11a - amino - 3a - hydroxysteroids |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| US5939545A (en) | 1994-02-14 | 1999-08-17 | Cocensys, Inc. | Method, compositions, and compounds for allosteric modulation of the gaba receptor by members of the androstane and pregnane series |
| US8569275B2 (en) | 2002-08-28 | 2013-10-29 | Harbor Therapeutics, Inc. | Steroids having 7-oxgen and 17-heteroaryl substitution |
| FR2967914A1 (fr) | 2010-11-29 | 2012-06-01 | Centre Nat Rech Scient | Composes inhibiteurs d'interactions proteine-proteine ciblant les proteines kinases et leurs applications biologiques |
| EP3572417B1 (en) | 2011-10-14 | 2025-12-17 | Sage Therapeutics, LLC | 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof |
| KR102396328B1 (ko) | 2013-04-17 | 2022-05-10 | 세이지 테라퓨틱스, 인크. | 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법 |
| US9725481B2 (en) | 2013-04-17 | 2017-08-08 | Sage Therapeutics, Inc. | 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof |
| CN117024501A (zh) | 2014-10-16 | 2023-11-10 | 萨奇治疗股份有限公司 | 靶向cns障碍的组合物和方法 |
| WO2017187343A2 (en) | 2016-04-29 | 2017-11-02 | Thome Kreutz Fernando | Nanoemulsions and methods for cancer therapy |
| MA45599A (fr) | 2016-07-11 | 2019-05-15 | Sage Therapeutics Inc | Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation |
| EP3504189A1 (en) | 2016-08-23 | 2019-07-03 | Sage Therapeutics, Inc. | A crystalline 19-nor c3, 3-disubstituted c21-n-pyrazolyl steroid |
| CN108727453A (zh) | 2017-04-20 | 2018-11-02 | 华东理工大学 | 新型pd-1抑制剂及其应用 |
| BR112020012761A2 (pt) | 2017-12-22 | 2021-02-17 | Sage Therapeutics, Inc. | composições e métodos para o tratamento de distúrbios do snc |
| US20200384003A1 (en) | 2017-12-29 | 2020-12-10 | Shanghai Lanmu Chemicals Co., Ltd. | Triterpenoid-containing pharmaceutical composition and use thereof |
| WO2019154257A1 (zh) | 2018-02-11 | 2019-08-15 | 江苏豪森药业集团有限公司 | 一种甾族类衍生物调节剂及其制备方法和应用 |
| EP3852764A4 (en) | 2018-09-19 | 2022-06-15 | ModernaTX, Inc. | STEROL ANALOGUES AND USES THEREOF |
| WO2020132504A1 (en) | 2018-12-21 | 2020-06-25 | Sage Therapeutics, Inc. | 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof |
| WO2020210116A1 (en) | 2019-04-08 | 2020-10-15 | Athenen Therapeutics, Inc. | Steroids with altered pharmacokinetic properties and methods of use thereof |
| WO2020210117A1 (en) | 2019-04-08 | 2020-10-15 | Athenen Therapeutics, Inc. | Steroids with altered pharmacokinetic properties and methods of use thereof |
| SG11202113155XA (en) | 2019-05-30 | 2021-12-30 | Intercept Pharmaceuticals Inc | Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease |
| SG11202112391UA (en) | 2019-05-31 | 2021-12-30 | Sage Therapeutics Inc | Neuroactive steroids and compositions thereof |
| CN114729000A (zh) | 2019-06-27 | 2022-07-08 | 萨奇治疗股份有限公司 | 用于治疗cns病症的化合物 |
| WO2021080880A1 (en) | 2019-10-25 | 2021-04-29 | Covey Douglas | Nmdar inhibiting agents and gabaar potentiating agents and uses thereof |
| US20230250129A1 (en) | 2020-06-24 | 2023-08-10 | Sage Therapeutics, Inc. | Neuroactive steroids and compositions thereof |
-
2019
- 2019-12-05 KR KR1020257039569A patent/KR20250174100A/ko active Pending
- 2019-12-05 US US17/311,056 patent/US20230322846A9/en not_active Abandoned
- 2019-12-05 EP EP19828126.3A patent/EP3902818A1/en active Pending
- 2019-12-05 TW TW108144589A patent/TWI874337B/zh active
- 2019-12-05 JP JP2021531987A patent/JP7539378B2/ja active Active
- 2019-12-05 KR KR1020217020784A patent/KR102892974B1/ko active Active
- 2019-12-05 CA CA3120872A patent/CA3120872A1/en active Pending
- 2019-12-05 IL IL312610A patent/IL312610B1/en unknown
- 2019-12-05 IL IL312611A patent/IL312611B2/en unknown
- 2019-12-05 MA MA054594A patent/MA54594A/fr unknown
- 2019-12-05 TW TW114104450A patent/TW202521127A/zh unknown
- 2019-12-05 MX MX2021006618A patent/MX2021006618A/es unknown
- 2019-12-05 AU AU2019392680A patent/AU2019392680B2/en active Active
- 2019-12-05 IL IL283629A patent/IL283629B2/en unknown
- 2019-12-05 CN CN201980091069.0A patent/CN113383004A/zh active Pending
- 2019-12-05 WO PCT/US2019/064692 patent/WO2020118060A1/en not_active Ceased
- 2019-12-05 BR BR112021010996-0A patent/BR112021010996A2/pt unknown
- 2019-12-06 AR ARP190103566A patent/AR117264A1/es unknown
-
2021
- 2021-06-03 MX MX2024004789A patent/MX2024004789A/es unknown
- 2021-06-03 MX MX2024004788A patent/MX2024004788A/es unknown
- 2021-06-03 MX MX2024004790A patent/MX2024004790A/es unknown
-
2023
- 2023-06-13 US US18/334,209 patent/US11912738B2/en active Active
- 2023-06-13 US US18/334,124 patent/US11970514B2/en active Active
- 2023-06-13 US US18/334,189 patent/US11999765B2/en active Active
-
2024
- 2024-03-26 US US18/616,995 patent/US12410210B2/en active Active
- 2024-03-26 US US18/616,762 patent/US12264177B2/en active Active
- 2024-03-26 US US18/616,903 patent/US12252509B2/en active Active
- 2024-05-10 JP JP2024077572A patent/JP7720948B2/ja active Active
-
2025
- 2025-01-14 US US19/019,743 patent/US20250154194A1/en active Pending
- 2025-05-14 AU AU2025203487A patent/AU2025203487A1/en active Pending
- 2025-05-14 AU AU2025203485A patent/AU2025203485A1/en active Pending
- 2025-06-13 JP JP2025099700A patent/JP2025134803A/ja active Pending
Patent Citations (3)
| 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 |
| WO1998005337A1 (en) * | 1996-08-01 | 1998-02-12 | Cocensys, Inc. | Use of gaba and nmda receptor ligands for the treatment of migraine headache |
| WO2017049044A1 (en) * | 2015-09-16 | 2017-03-23 | Bartolucci Giampiero | Ursodeoxycholic acid and brain disorders |
Non-Patent Citations (1)
| Title |
|---|
| 網路文獻 ,Hong-Jin Shu, Lawrence N. Eisenman, Cunde Wang, Achintya K. Bandyopadhyaya,Kathiresan Krishnan, Amanda Taylor, Ann M. Benz, Brad Manion, Alex S. Evers,Douglas F. Covey, Charles F. Zorumski, and Steven Mennerick。 Photodynamic Effects of Steroid-Conjugated Fluorophores on GABAA Receptors Mol Pharmacol 76:754–765, 2009 2009年10月 https://pubmed.ncbi.nlm.nih.gov/19596835/ * |
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