JPWO2019140272A5 - - Google Patents
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- Publication number
- JPWO2019140272A5 JPWO2019140272A5 JP2020538573A JP2020538573A JPWO2019140272A5 JP WO2019140272 A5 JPWO2019140272 A5 JP WO2019140272A5 JP 2020538573 A JP2020538573 A JP 2020538573A JP 2020538573 A JP2020538573 A JP 2020538573A JP WO2019140272 A5 JPWO2019140272 A5 JP WO2019140272A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- compound
- pharmaceutically acceptable
- alkyl
- 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.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims description 429
- 229910052739 hydrogen Inorganic materials 0.000 claims description 385
- 239000001257 hydrogen Substances 0.000 claims description 385
- 125000000217 alkyl group Chemical group 0.000 claims description 361
- 125000000623 heterocyclic group Chemical group 0.000 claims description 297
- 150000002431 hydrogen Chemical group 0.000 claims description 269
- 125000001072 heteroaryl group Chemical group 0.000 claims description 213
- 125000003342 alkenyl group Chemical group 0.000 claims description 211
- 150000003839 salts Chemical class 0.000 claims description 207
- 125000000304 alkynyl group Chemical group 0.000 claims description 191
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 187
- 125000003118 aryl group Chemical group 0.000 claims description 177
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 108
- 229910052736 halogen Inorganic materials 0.000 claims description 92
- 150000002367 halogens Chemical group 0.000 claims description 92
- -1 cyano, hydroxyl Chemical group 0.000 claims description 67
- 229910052757 nitrogen Inorganic materials 0.000 claims description 56
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 47
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 41
- 208000035475 disorder Diseases 0.000 claims description 38
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 36
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 36
- 125000004429 atom Chemical group 0.000 claims description 32
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 32
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 31
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 31
- 210000003169 central nervous system Anatomy 0.000 claims description 28
- 229910052760 oxygen Inorganic materials 0.000 claims description 26
- 239000001301 oxygen Substances 0.000 claims description 26
- 229910052717 sulfur Inorganic materials 0.000 claims description 26
- 125000004434 sulfur atom Chemical group 0.000 claims description 22
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 19
- 208000024714 major depressive disease Diseases 0.000 claims description 19
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 19
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 13
- 125000003545 alkoxy group Chemical group 0.000 claims description 13
- 125000001188 haloalkyl group Chemical group 0.000 claims description 13
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 13
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 10
- 125000003107 substituted aryl group Chemical group 0.000 claims description 8
- 230000017105 transposition Effects 0.000 claims description 8
- 206010015037 epilepsy Diseases 0.000 claims description 5
- 208000026139 Memory disease Diseases 0.000 claims description 4
- 208000019022 Mood disease Diseases 0.000 claims description 4
- 208000019430 Motor disease Diseases 0.000 claims description 4
- 208000002193 Pain Diseases 0.000 claims description 4
- 201000009916 Postpartum depression Diseases 0.000 claims description 4
- 208000005392 Spasm Diseases 0.000 claims description 4
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims description 4
- 208000009205 Tinnitus Diseases 0.000 claims description 4
- 206010048010 Withdrawal syndrome Diseases 0.000 claims description 4
- 208000029560 autism spectrum disease Diseases 0.000 claims description 4
- 208000010877 cognitive disease Diseases 0.000 claims description 4
- 208000022821 personality disease Diseases 0.000 claims description 4
- 201000000980 schizophrenia Diseases 0.000 claims description 4
- 208000019116 sleep disease Diseases 0.000 claims description 4
- 238000001228 spectrum Methods 0.000 claims description 4
- 201000009032 substance abuse Diseases 0.000 claims description 4
- 231100000736 substance abuse Toxicity 0.000 claims description 4
- 208000011117 substance-related disease Diseases 0.000 claims description 4
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 3
- 201000010099 disease Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 230000009529 traumatic brain injury Effects 0.000 claims description 3
- 239000000203 mixture Substances 0.000 claims 12
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 239000011593 sulfur Chemical group 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 3
- 206010044565 Tremor Diseases 0.000 claims 2
- 125000006193 alkinyl group Chemical group 0.000 claims 2
- 239000007789 gas Substances 0.000 claims 2
- 201000006517 essential tremor Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 208000005809 status epilepticus Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 description 19
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 description 13
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 description 9
- 125000000547 substituted alkyl group Chemical group 0.000 description 6
- 230000003455 independent Effects 0.000 description 5
- 125000005843 halogen group Chemical group 0.000 description 4
- 229960003692 gamma aminobutyric acid Drugs 0.000 description 2
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 description 2
- 206010001497 Agitation Diseases 0.000 description 1
- 208000029028 brain injury Diseases 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000001802 infusion Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 230000000472 traumatic effect Effects 0.000 description 1
- 208000019553 vascular disease Diseases 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023127398A JP7817214B2 (ja) | 2018-01-12 | 2023-08-03 | ＣＮＳ障害の処置における使用のためのアザ、オキサ、およびチア－プレグナン－２０－オン－３α－オール化合物 |
| JP2025061337A JP2025106370A (ja) | 2018-01-12 | 2025-04-02 | ＣＮＳ障害の処置における使用のためのアザ、オキサ、およびチア－プレグナン－２０－オン－３α－オール化合物 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862617134P | 2018-01-12 | 2018-01-12 | |
| US201862616768P | 2018-01-12 | 2018-01-12 | |
| US62/616,768 | 2018-01-12 | ||
| US62/617,134 | 2018-01-12 | ||
| US201862728514P | 2018-09-07 | 2018-09-07 | |
| US62/728,514 | 2018-09-07 | ||
| PCT/US2019/013315 WO2019140272A1 (en) | 2018-01-12 | 2019-01-11 | Aza-, oxa and thia-pregnan-20-one-3.alpha.-ol compounds for use in treating cns disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023127398A Division JP7817214B2 (ja) | 2018-01-12 | 2023-08-03 | ＣＮＳ障害の処置における使用のためのアザ、オキサ、およびチア－プレグナン－２０－オン－３α－オール化合物 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021510695A JP2021510695A (ja) | 2021-04-30 |
| JPWO2019140272A5 true JPWO2019140272A5 (https=) | 2022-01-18 |
| JP2021510695A5 JP2021510695A5 (https=) | 2022-01-18 |
| JP7538040B2 JP7538040B2 (ja) | 2024-08-21 |
Family
ID=65324563
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020538573A Active JP7538040B2 (ja) | 2018-01-12 | 2019-01-11 | ＣＮＳ障害の処置における使用のためのアザ、オキサ、およびチア－プレグナン－２０－オン－３α－オール化合物 |
| JP2023127398A Active JP7817214B2 (ja) | 2018-01-12 | 2023-08-03 | ＣＮＳ障害の処置における使用のためのアザ、オキサ、およびチア－プレグナン－２０－オン－３α－オール化合物 |
| JP2025061337A Pending JP2025106370A (ja) | 2018-01-12 | 2025-04-02 | ＣＮＳ障害の処置における使用のためのアザ、オキサ、およびチア－プレグナン－２０－オン－３α－オール化合物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023127398A Active JP7817214B2 (ja) | 2018-01-12 | 2023-08-03 | ＣＮＳ障害の処置における使用のためのアザ、オキサ、およびチア－プレグナン－２０－オン－３α－オール化合物 |
| JP2025061337A Pending JP2025106370A (ja) | 2018-01-12 | 2025-04-02 | ＣＮＳ障害の処置における使用のためのアザ、オキサ、およびチア－プレグナン－２０－オン－３α－オール化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US11718642B2 (https=) |
| EP (2) | EP4706761A2 (https=) |
| JP (3) | JP7538040B2 (https=) |
| MA (1) | MA51568A (https=) |
| TW (1) | TW201930269A (https=) |
| WO (1) | WO2019140272A1 (https=) |
Families Citing this family (14)
| 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 |
| MA51568A (fr) | 2018-01-12 | 2021-04-21 | Sage Therapeutics Inc | Composés aza-, oxa et thia-pregnan-20-one-3.alpha.-ol s'utilisant dans le traitement de troubles du système nerveux central |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| US20230018765A1 (en) * | 2019-12-05 | 2023-01-19 | Sage Therapeutics, Inc. | A 19-nor c3,3-disubstituted c21-n-pyrazolyl steroid and methods of use thereof |
| CN111233815B (zh) * | 2020-01-21 | 2022-10-14 | 上海应用技术大学 | 一种异阿根廷蚁素的制备方法 |
| KR20220157426A (ko) | 2020-03-25 | 2022-11-29 | 세이지 테라퓨틱스, 인크. | 호흡기 병태의 치료를 위한 작용제의 용도 |
| WO2024118503A1 (en) | 2022-11-28 | 2024-06-06 | Hongene Biotech Corporation | Functionalized n-acetylgalactosamine analogs |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL48628A0 (en) * | 1974-12-23 | 1976-02-29 | Schering Ag | D-homo-20-keto-pregnanes and process for their manufactur |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| AU698834B2 (en) | 1993-05-24 | 1998-11-12 | Purdue Pharma Ltd. | Methods and compositions for inducing sleep |
| FI972202L (fi) * | 1994-11-23 | 1997-07-17 | Cocensys Inc | Androstaanit ja pregnaanit GABA-reseptoreiden allosteeriseen muunteluun |
| RU2194712C2 (ru) | 1995-06-06 | 2002-12-20 | Коукенсис, Инк. | НЕЙРОАКТИВНЫЕ СТЕРОИДЫ, ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ, СПОСОБ ЛЕЧЕНИЯ ИЛИ ПРОФИЛАКТИКИ РАЗЛИЧНЫХ НАРУШЕНИЙ, СПОСОБ ИНДУКЦИИ СНА И СПОСОБ ИНДУКЦИИ АНЕСТЕЗИИ С ИХ ИСПОЛЬЗОВАНИЕМ, СПОСОБ МОДУЛИРОВАНИЯ КОМПЛЕКСА РЕЦЕПТОР ГАМКa-ХЛОРИДНЫЙ ИОНОФОР |
| AU3967297A (en) | 1996-08-01 | 1998-02-25 | Cocensys, Inc. | Use of gaba and nmda receptor ligands for the treatment of migraine headache |
| 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 |
| ME03809B (me) | 2014-10-16 | 2021-04-20 | Sage Therapeutics Inc | KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a |
| CN111741965B (zh) | 2017-12-22 | 2024-06-25 | 萨奇治疗股份有限公司 | 治疗中枢神经系统疾病的组合物和方法 |
| MA51568A (fr) | 2018-01-12 | 2021-04-21 | Sage Therapeutics Inc | Composés aza-, oxa et thia-pregnan-20-one-3.alpha.-ol s'utilisant dans le traitement de troubles du système nerveux central |
| CN114656514B (zh) | 2018-02-11 | 2024-05-14 | 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 |
| CN109503694A (zh) | 2018-11-21 | 2019-03-22 | 苏州闻天医药科技有限公司 | 一种新型gabaa受体调节剂及其用途 |
| IL283629B2 (en) | 2018-12-05 | 2026-03-01 | Sage Therapeutics Inc | Neuroactive steroids and methods of using them |
| WO2020135454A1 (zh) | 2018-12-26 | 2020-07-02 | 张家口华健致远生物科技有限公司 | 一类类固醇化合物及其用途 |
| TW202143976A (zh) | 2020-03-18 | 2021-12-01 | 美商賽吉醫療公司 | 神經活性類固醇及其使用方法 |
-
2019
- 2019-01-11 MA MA051568A patent/MA51568A/fr unknown
- 2019-01-11 JP JP2020538573A patent/JP7538040B2/ja active Active
- 2019-01-11 EP EP25209494.1A patent/EP4706761A2/en active Pending
- 2019-01-11 US US16/961,097 patent/US11718642B2/en active Active
- 2019-01-11 WO PCT/US2019/013315 patent/WO2019140272A1/en not_active Ceased
- 2019-01-11 TW TW108101261A patent/TW201930269A/zh unknown
- 2019-01-11 EP EP19703816.9A patent/EP3737687B1/en active Active
-
2023
- 2023-06-05 US US18/328,865 patent/US12421275B2/en active Active
- 2023-08-03 JP JP2023127398A patent/JP7817214B2/ja active Active
-
2025
- 2025-04-02 JP JP2025061337A patent/JP2025106370A/ja active Pending
- 2025-08-06 US US19/291,992 patent/US20260078143A1/en active Pending
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