JPWO2020077255A5 - - Google Patents
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- Publication number
- JPWO2020077255A5 JPWO2020077255A5 JP2021519712A JP2021519712A JPWO2020077255A5 JP WO2020077255 A5 JPWO2020077255 A5 JP WO2020077255A5 JP 2021519712 A JP2021519712 A JP 2021519712A JP 2021519712 A JP2021519712 A JP 2021519712A JP WO2020077255 A5 JPWO2020077255 A5 JP WO2020077255A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- compound
- pharmaceutically acceptable
- acceptable salt
- 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
Links
- 150000001875 compounds Chemical class 0.000 claims description 160
- 229910052739 hydrogen Inorganic materials 0.000 claims description 138
- 239000001257 hydrogen Substances 0.000 claims description 138
- 125000000217 alkyl group Chemical group 0.000 claims description 106
- 150000003839 salts Chemical class 0.000 claims description 96
- 125000000623 heterocyclic group Chemical group 0.000 claims description 94
- 150000002431 hydrogen Chemical class 0.000 claims description 86
- 125000000304 alkynyl group Chemical group 0.000 claims description 59
- 125000003342 alkenyl group Chemical group 0.000 claims description 58
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 54
- 125000003118 aryl group Chemical group 0.000 claims description 53
- 125000001072 heteroaryl group Chemical group 0.000 claims description 43
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 37
- 125000004429 atom Chemical group 0.000 claims description 36
- 229910052736 halogen Inorganic materials 0.000 claims description 36
- 150000002367 halogens Chemical group 0.000 claims description 36
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 34
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 32
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 32
- 229910052757 nitrogen Inorganic materials 0.000 claims description 19
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 17
- 239000008194 pharmaceutical composition Substances 0.000 claims description 17
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 229910052760 oxygen Inorganic materials 0.000 claims description 16
- 239000001301 oxygen Substances 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 15
- 208000035475 disorder Diseases 0.000 claims description 14
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 13
- 210000003169 central nervous system Anatomy 0.000 claims description 10
- 208000024714 major depressive disease Diseases 0.000 claims description 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 9
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 8
- 229910052717 sulfur Inorganic materials 0.000 claims description 8
- 239000011593 sulfur Substances 0.000 claims description 8
- 125000005843 halogen group Chemical group 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 4
- 125000003107 substituted aryl group Chemical group 0.000 claims description 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 2
- 208000026139 Memory disease Diseases 0.000 claims description 2
- 208000019022 Mood disease Diseases 0.000 claims description 2
- 208000016285 Movement disease Diseases 0.000 claims description 2
- 208000002193 Pain Diseases 0.000 claims description 2
- 201000009916 Postpartum depression Diseases 0.000 claims description 2
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims description 2
- 208000009205 Tinnitus Diseases 0.000 claims description 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 2
- 206010048010 Withdrawal syndrome Diseases 0.000 claims description 2
- 208000029560 autism spectrum disease Diseases 0.000 claims description 2
- 208000010877 cognitive disease Diseases 0.000 claims description 2
- -1 cyano, hydroxyl Chemical group 0.000 claims description 2
- 229910052805 deuterium Chemical group 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims description 2
- 229910052731 fluorine Inorganic materials 0.000 claims description 2
- 239000011737 fluorine Substances 0.000 claims description 2
- 230000036407 pain Effects 0.000 claims description 2
- 208000022821 personality disease Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- 208000019116 sleep disease Diseases 0.000 claims description 2
- 238000001228 spectrum Methods 0.000 claims description 2
- 208000005809 status epilepticus Diseases 0.000 claims description 2
- 201000009032 substance abuse Diseases 0.000 claims description 2
- 231100000736 substance abuse Toxicity 0.000 claims description 2
- 208000011117 substance-related disease Diseases 0.000 claims description 2
- 231100000886 tinnitus Toxicity 0.000 claims description 2
- 230000009529 traumatic brain injury Effects 0.000 claims description 2
- 230000002792 vascular Effects 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 18
- 239000000203 mixture Substances 0.000 claims 15
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 7
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 7
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 5
- 125000004122 cyclic group Chemical group 0.000 claims 5
- 206010002091 Anaesthesia Diseases 0.000 claims 2
- 206010039897 Sedation Diseases 0.000 claims 2
- 206010044565 Tremor Diseases 0.000 claims 2
- 230000037005 anaesthesia Effects 0.000 claims 2
- 230000036280 sedation Effects 0.000 claims 2
- 206010010904 Convulsion Diseases 0.000 claims 1
- 201000006517 essential tremor Diseases 0.000 claims 1
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 230000006698 induction Effects 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 description 5
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000017105 transposition Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024020461A JP2024040444A (ja) | 2018-10-12 | 2024-02-14 | Ｃｎｓ障害の処置において使用するための、１０位において環式基で置換された神経刺激性ステロイド |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862745109P | 2018-10-12 | 2018-10-12 | |
| US62/745,109 | 2018-10-12 | ||
| PCT/US2019/055926 WO2020077255A1 (en) | 2018-10-12 | 2019-10-11 | Neuroactive steroids substituted in position 10 with a cyclic group for use in the treatment of cns disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024020461A Division JP2024040444A (ja) | 2018-10-12 | 2024-02-14 | Ｃｎｓ障害の処置において使用するための、１０位において環式基で置換された神経刺激性ステロイド |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022504607A JP2022504607A (ja) | 2022-01-13 |
| JPWO2020077255A5 true JPWO2020077255A5 (https=) | 2022-10-11 |
| JP2022504607A5 JP2022504607A5 (https=) | 2022-10-11 |
| JP7671244B2 JP7671244B2 (ja) | 2025-05-01 |
Family
ID=68425315
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021519712A Active JP7671244B2 (ja) | 2018-10-12 | 2019-10-11 | Ｃｎｓ障害の処置において使用するための、１０位において環式基で置換された神経刺激性ステロイド |
| JP2024020461A Pending JP2024040444A (ja) | 2018-10-12 | 2024-02-14 | Ｃｎｓ障害の処置において使用するための、１０位において環式基で置換された神経刺激性ステロイド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024020461A Pending JP2024040444A (ja) | 2018-10-12 | 2024-02-14 | Ｃｎｓ障害の処置において使用するための、１０位において環式基で置換された神経刺激性ステロイド |
Country Status (14)
| Country | Link |
|---|---|
| US (2) | US11634453B2 (https=) |
| EP (2) | EP4321519B1 (https=) |
| JP (2) | JP7671244B2 (https=) |
| CN (2) | CN113166193B (https=) |
| AR (1) | AR116695A1 (https=) |
| AU (2) | AU2019357040B2 (https=) |
| BR (1) | BR112021009428A2 (https=) |
| CA (1) | CA3115805A1 (https=) |
| DK (1) | DK3864022T3 (https=) |
| ES (1) | ES2966055T3 (https=) |
| IL (1) | IL282183A (https=) |
| MX (2) | MX2021004159A (https=) |
| TW (2) | TWI835884B (https=) |
| WO (1) | WO2020077255A1 (https=) |
Families Citing this family (9)
| 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 |
| CN113166193B (zh) * | 2018-10-12 | 2025-08-19 | 萨奇治疗股份有限公司 | 用于治疗cns病症的在位置10处被环状基团取代的神经活性类固醇 |
Family Cites Families (14)
| 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 |
| KR100338287B1 (ko) * | 1994-02-14 | 2002-11-30 | 푸르듀 파머 리미티드 | 감마-아미노부티르산a수용체의알로오스테리조절용안드로스탄및프레그난 |
| 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 |
| FI972202L (fi) | 1994-11-23 | 1997-07-17 | Cocensys Inc | Androstaanit ja pregnaanit GABA-reseptoreiden allosteeriseen muunteluun |
| MX365644B (es) | 2012-12-18 | 2019-06-10 | Univ Washington | Esteroides neuroactivos sustituidos con 19-alcoxi-17, profarmacos de los mismos, y metodos de tratamiento usando los mismos. |
| US10577390B2 (en) * | 2014-10-16 | 2020-03-03 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| 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 |
| EP3728284B1 (en) | 2017-12-22 | 2024-08-21 | Sage Therapeutics, Inc. | 19-homo, 3.alpha.-hydroxy-steroid-20-one compounds for treating cns disorders |
| 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 |
| CN113166193B (zh) * | 2018-10-12 | 2025-08-19 | 萨奇治疗股份有限公司 | 用于治疗cns病症的在位置10处被环状基团取代的神经活性类固醇 |
| AU2020304673A1 (en) * | 2019-06-27 | 2022-01-20 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| US20230257415A1 (en) | 2019-06-27 | 2023-08-17 | Sage Therapeutics, Inc. | Compounds for treating cns disorders |
| 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 |
| 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 |
-
2019
- 2019-10-11 CN CN201980079330.5A patent/CN113166193B/zh active Active
- 2019-10-11 ES ES19797472T patent/ES2966055T3/es active Active
- 2019-10-11 EP EP23197779.4A patent/EP4321519B1/en active Active
- 2019-10-11 CN CN202511082220.8A patent/CN121045302A/zh active Pending
- 2019-10-11 MX MX2021004159A patent/MX2021004159A/es unknown
- 2019-10-11 BR BR112021009428-8A patent/BR112021009428A2/pt unknown
- 2019-10-11 JP JP2021519712A patent/JP7671244B2/ja active Active
- 2019-10-11 CA CA3115805A patent/CA3115805A1/en active Pending
- 2019-10-11 DK DK19797472.8T patent/DK3864022T3/da active
- 2019-10-11 AR ARP190102913A patent/AR116695A1/es unknown
- 2019-10-11 WO PCT/US2019/055926 patent/WO2020077255A1/en not_active Ceased
- 2019-10-11 US US17/284,206 patent/US11634453B2/en active Active
- 2019-10-11 AU AU2019357040A patent/AU2019357040B2/en active Active
- 2019-10-11 EP EP19797472.8A patent/EP3864022B1/en active Active
- 2019-10-14 TW TW108136955A patent/TWI835884B/zh active
- 2019-10-14 TW TW113106814A patent/TWI886813B/zh active
-
2021
- 2021-04-08 IL IL282183A patent/IL282183A/en unknown
- 2021-04-09 MX MX2024011494A patent/MX2024011494A/es unknown
-
2023
- 2023-02-21 US US18/171,798 patent/US20240376144A9/en active Pending
-
2024
- 2024-02-14 JP JP2024020461A patent/JP2024040444A/ja active Pending
-
2025
- 2025-01-22 AU AU2025200422A patent/AU2025200422A1/en active Pending