KR20210107050A - 3.알파.-히드록시-17.베타.-아미드 신경활성 스테로이드 및 그의 조성물 - Google Patents
3.알파.-히드록시-17.베타.-아미드 신경활성 스테로이드 및 그의 조성물 Download PDFInfo
- Publication number
- KR20210107050A KR20210107050A KR1020217022533A KR20217022533A KR20210107050A KR 20210107050 A KR20210107050 A KR 20210107050A KR 1020217022533 A KR1020217022533 A KR 1020217022533A KR 20217022533 A KR20217022533 A KR 20217022533A KR 20210107050 A KR20210107050 A KR 20210107050A
- Authority
- KR
- South Korea
- Prior art keywords
- substituted
- unsubstituted
- compound
- alkyl
- independently hydrogen
- 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.)
- Ceased
Links
- 0 *1N=Nc2ccccc12 Chemical compound *1N=Nc2ccccc12 0.000 description 5
- KECLSSZROFUBTD-WMKSVVDLSA-N CC[C@](CC1)([C@H](CC2)C[C@]1(COCC)O)[C@@H](CC1)[C@@H]2[C@H](CC2)[C@@]1(C)[C@H]2C(N)=O Chemical compound CC[C@](CC1)([C@H](CC2)C[C@]1(COCC)O)[C@@H](CC1)[C@@H]2[C@H](CC2)[C@@]1(C)[C@H]2C(N)=O KECLSSZROFUBTD-WMKSVVDLSA-N 0.000 description 1
- JZEQEXSRGBHBSC-KSTZIOMOSA-N CC[C@](CC1)([C@H](CC2)C[C@]1(COCC)O)[C@@H](CC1)[C@@H]2[C@H](CC2)[C@@]1(C)[C@H]2C(Nc1ncc(C#N)nc1)=O Chemical compound CC[C@](CC1)([C@H](CC2)C[C@]1(COCC)O)[C@@H](CC1)[C@@H]2[C@H](CC2)[C@@]1(C)[C@H]2C(Nc1ncc(C#N)nc1)=O JZEQEXSRGBHBSC-KSTZIOMOSA-N 0.000 description 1
- OALBKJHXMHYXBL-WMKSVVDLSA-N CC[C@](CC1)([C@H](CC2)C[C@]1(COCC)O)[C@@H](CC1)[C@@H]2[C@H](CC2)[C@@]1(C)[C@H]2C(O)=O Chemical compound CC[C@](CC1)([C@H](CC2)C[C@]1(COCC)O)[C@@H](CC1)[C@@H]2[C@H](CC2)[C@@]1(C)[C@H]2C(O)=O OALBKJHXMHYXBL-WMKSVVDLSA-N 0.000 description 1
- ZPBNABIKZKTQQH-UHFFFAOYSA-N N#Cc(cn1)ncc1Br Chemical compound N#Cc(cn1)ncc1Br ZPBNABIKZKTQQH-UHFFFAOYSA-N 0.000 description 1
- XSCHRSMBECNVNS-UHFFFAOYSA-N c1cc2nccnc2cc1 Chemical compound c1cc2nccnc2cc1 XSCHRSMBECNVNS-UHFFFAOYSA-N 0.000 description 1
- PBMFSQRYOILNGV-UHFFFAOYSA-N c1cnncc1 Chemical compound c1cnncc1 PBMFSQRYOILNGV-UHFFFAOYSA-N 0.000 description 1
- KYQCOXFCLRTKLS-UHFFFAOYSA-N c1nccnc1 Chemical compound c1nccnc1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 description 1
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
- A61P25/24—Antidepressants
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
- C07J1/0003—Androstane derivatives
- C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
- C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J21/005—Ketals
- C07J21/008—Ketals at position 17
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
- C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
-
- 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
- C07J41/0066—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 a carbon atom forming 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
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- 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
- C07J7/0005—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
- C07J7/0065—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 an OH group free esterified or etherified
- C07J7/007—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 an OH group free esterified or etherified not substituted in position 17 alfa
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)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Toxicology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862784222P | 2018-12-21 | 2018-12-21 | |
| US201862784229P | 2018-12-21 | 2018-12-21 | |
| US62/784,222 | 2018-12-21 | ||
| US62/784,229 | 2018-12-21 | ||
| PCT/US2019/067953 WO2020132504A1 (en) | 2018-12-21 | 2019-12-20 | 3.alpha.-hydroxy-17.beta.-amide neuroactive steroids and compositions thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20210107050A true KR20210107050A (ko) | 2021-08-31 |
Family
ID=69591712
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020217022533A Ceased KR20210107050A (ko) | 2018-12-21 | 2019-12-20 | 3.알파.-히드록시-17.베타.-아미드 신경활성 스테로이드 및 그의 조성물 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20220372067A1 (https=) |
| EP (1) | EP3898646B1 (https=) |
| JP (2) | JP7692830B2 (https=) |
| KR (1) | KR20210107050A (https=) |
| CN (1) | CN113195512A (https=) |
| AU (2) | AU2019403415B2 (https=) |
| BR (1) | BR112021012242A2 (https=) |
| CA (1) | CA3124371A1 (https=) |
| IL (1) | IL284183A (https=) |
| MX (2) | MX2021007504A (https=) |
| TW (2) | TWI848034B (https=) |
| WO (1) | WO2020132504A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG10201606063RA (en) | 2012-01-23 | 2016-09-29 | Sage Therapeutics Inc | Neuroactive steroid formulations and methods of treating cns disorders |
| MX2015002252A (es) | 2012-08-21 | 2015-07-21 | Sage Therapeutics Inc | Metodos para tratar epilepsia o estado de epilepsia. |
| JP6470258B2 (ja) | 2013-04-17 | 2019-02-13 | セージ セラピューティクス， インコーポレイテッド | １９−ノルｃ３，３−ジ置換ｃ２１−ｎ−ピラゾリルステロイドおよびその使用方法 |
| WO2015195962A1 (en) | 2014-06-18 | 2015-12-23 | 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 |
| TWI904593B (zh) | 2016-08-23 | 2025-11-11 | 美商賽吉醫療公司 | 結晶19-去甲c3,3-二取代之c21-n-吡唑類固醇 |
| EP3720867A1 (en) | 2017-12-08 | 2020-10-14 | Sage Therapeutics, Inc. | Deuterated 21 -[4-cyano-pyrazol-1 -yl]-19-nor-pregan-3. alpha-ol-20-one derivatives for treating cns disorders |
| IL283629B2 (en) | 2018-12-05 | 2026-03-01 | Sage Therapeutics Inc | Neuroactive steroids and methods of using them |
| CN113195512A (zh) * | 2018-12-21 | 2021-07-30 | 萨奇治疗股份有限公司 | 3.α.-羟基-17.β.-酰胺神经活性类固醇及其组合物 |
| IL299176A (en) * | 2020-06-24 | 2023-02-01 | Sage Therapeutics Inc | 3.alpha.-hydroxy, 17.beta.-c(o)-n-aryl substituted neuroactive steroids and compositions thereof |
| CN119192275B (zh) * | 2024-08-22 | 2025-05-30 | 湖南玉新药业有限公司 | 一种3-羰基-4-氮杂-5α-雄甾-17β-羧酸化合物的制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| CN119192266A (zh) | 2011-10-14 | 2024-12-27 | 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 |
| US9512170B2 (en) * | 2013-03-01 | 2016-12-06 | Washington University | Neuroactive 13, 17-substituted steroids as modulators for GABA type-A receptors |
| US10577390B2 (en) * | 2014-10-16 | 2020-03-03 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| EP4155314A1 (en) * | 2015-02-20 | 2023-03-29 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| MA45599A (fr) | 2016-07-11 | 2019-05-15 | Sage Therapeutics Inc | Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation |
| IL283629B2 (en) * | 2018-12-05 | 2026-03-01 | Sage Therapeutics Inc | Neuroactive steroids and methods of using them |
| CN113195512A (zh) * | 2018-12-21 | 2021-07-30 | 萨奇治疗股份有限公司 | 3.α.-羟基-17.β.-酰胺神经活性类固醇及其组合物 |
-
2019
- 2019-12-20 CN CN201980085054.3A patent/CN113195512A/zh active Pending
- 2019-12-20 US US17/416,367 patent/US20220372067A1/en active Pending
- 2019-12-20 TW TW108147086A patent/TWI848034B/zh active
- 2019-12-20 CA CA3124371A patent/CA3124371A1/en active Pending
- 2019-12-20 KR KR1020217022533A patent/KR20210107050A/ko not_active Ceased
- 2019-12-20 AU AU2019403415A patent/AU2019403415B2/en active Active
- 2019-12-20 WO PCT/US2019/067953 patent/WO2020132504A1/en not_active Ceased
- 2019-12-20 MX MX2021007504A patent/MX2021007504A/es unknown
- 2019-12-20 TW TW113121961A patent/TWI892697B/zh active
- 2019-12-20 EP EP19850836.8A patent/EP3898646B1/en active Active
- 2019-12-20 JP JP2021535679A patent/JP7692830B2/ja active Active
- 2019-12-20 BR BR112021012242-7A patent/BR112021012242A2/pt unknown
-
2021
- 2021-06-18 MX MX2025000126A patent/MX2025000126A/es unknown
- 2021-06-20 IL IL284183A patent/IL284183A/en unknown
-
2024
- 2024-06-11 JP JP2024094279A patent/JP2024107296A/ja active Pending
-
2025
- 2025-11-13 AU AU2025267433A patent/AU2025267433A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| US20220372067A1 (en) | 2022-11-24 |
| EP3898646A1 (en) | 2021-10-27 |
| TWI892697B (zh) | 2025-08-01 |
| MX2021007504A (es) | 2021-10-13 |
| WO2020132504A1 (en) | 2020-06-25 |
| TWI848034B (zh) | 2024-07-11 |
| AU2025267433A1 (en) | 2025-12-04 |
| EP3898646B1 (en) | 2026-02-18 |
| JP2024107296A (ja) | 2024-08-08 |
| JP2022514385A (ja) | 2022-02-10 |
| IL284183A (en) | 2021-08-31 |
| TW202438080A (zh) | 2024-10-01 |
| MX2025000126A (es) | 2025-02-10 |
| TW202038967A (zh) | 2020-11-01 |
| AU2019403415A1 (en) | 2021-07-08 |
| BR112021012242A2 (pt) | 2021-09-28 |
| AU2019403415B2 (en) | 2025-08-21 |
| CN113195512A (zh) | 2021-07-30 |
| CA3124371A1 (en) | 2020-06-25 |
| JP7692830B2 (ja) | 2025-06-16 |
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