JP2021502403A5 - - Google Patents
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- Publication number
- JP2021502403A5 JP2021502403A5 JP2020526304A JP2020526304A JP2021502403A5 JP 2021502403 A5 JP2021502403 A5 JP 2021502403A5 JP 2020526304 A JP2020526304 A JP 2020526304A JP 2020526304 A JP2020526304 A JP 2020526304A JP 2021502403 A5 JP2021502403 A5 JP 2021502403A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- syndrome
- substituted
- 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.)
- Granted
Links
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 12
- 208000011580 syndromic disease Diseases 0.000 claims 12
- 206010015037 epilepsy Diseases 0.000 claims 11
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 10
- 241000124008 Mammalia Species 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000004404 heteroalkyl group Chemical group 0.000 claims 8
- AURFZBICLPNKBZ-YZRLXODZSA-N 3alpha-hydroxy-5beta-pregnan-20-one Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-YZRLXODZSA-N 0.000 claims 7
- PGTVWKLGGCQMBR-FLBATMFCSA-N Ganaxolone Chemical compound C([C@@H]1CC2)[C@](C)(O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 PGTVWKLGGCQMBR-FLBATMFCSA-N 0.000 claims 7
- AURFZBICLPNKBZ-UHFFFAOYSA-N Pregnanolone Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(=O)C)C1(C)CC2 AURFZBICLPNKBZ-UHFFFAOYSA-N 0.000 claims 7
- ORNBQBCIOKFOEO-YQUGOWONSA-N Pregnenolone Natural products O=C(C)[C@@H]1[C@@]2(C)[C@H]([C@H]3[C@@H]([C@]4(C)C(=CC3)C[C@@H](O)CC4)CC2)CC1 ORNBQBCIOKFOEO-YQUGOWONSA-N 0.000 claims 7
- 229950006567 ganaxolone Drugs 0.000 claims 7
- ORNBQBCIOKFOEO-QGVNFLHTSA-N pregnenolone Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H](C(=O)C)[C@@]1(C)CC2 ORNBQBCIOKFOEO-QGVNFLHTSA-N 0.000 claims 7
- 229960000249 pregnenolone Drugs 0.000 claims 7
- 208000014644 Brain disease Diseases 0.000 claims 6
- 208000032274 Encephalopathy Diseases 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 208000035475 disorder Diseases 0.000 claims 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims 6
- 230000001037 epileptic effect Effects 0.000 claims 5
- 239000002858 neurotransmitter agent Substances 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 208000009575 Angelman syndrome Diseases 0.000 claims 2
- 102100034746 Cyclin-dependent kinase-like 5 Human genes 0.000 claims 2
- 101000945692 Homo sapiens Cyclin-dependent kinase-like 5 Proteins 0.000 claims 2
- 101001072243 Homo sapiens Protocadherin-19 Proteins 0.000 claims 2
- 102100036389 Protocadherin-19 Human genes 0.000 claims 2
- 208000006289 Rett Syndrome Diseases 0.000 claims 2
- 208000005392 Spasm Diseases 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- JLRGJRBPOGGCBT-UHFFFAOYSA-N Tolbutamide Chemical compound CCCCNC(=O)NS(=O)(=O)C1=CC=C(C)C=C1 JLRGJRBPOGGCBT-UHFFFAOYSA-N 0.000 claims 2
- MENQCIVHHONJLU-FZCSVUEKSA-N [(3s,5s,8r,9s,10s,13s,14s,17s)-17-acetyl-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate Chemical compound C([C@@H]1CC2)[C@@H](OS(O)(=O)=O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 MENQCIVHHONJLU-FZCSVUEKSA-N 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 238000003556 assay Methods 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000013500 continuous spikes and waves during sleep Diseases 0.000 claims 2
- 230000007812 deficiency Effects 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 229950007402 eltanolone Drugs 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 230000003340 mental effect Effects 0.000 claims 2
- 125000001570 methylene group Chemical group [H]C([H])([*:1])[*:2] 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- XMRPGKVKISIQBV-UHFFFAOYSA-N (+-)-5- Pregnane-3,20-dione Natural products C1CC2CC(=O)CCC2(C)C2C1C1CCC(C(=O)C)C1(C)CC2 XMRPGKVKISIQBV-UHFFFAOYSA-N 0.000 claims 1
- XMRPGKVKISIQBV-BJMCWZGWSA-N 5alpha-pregnane-3,20-dione Chemical compound C([C@@H]1CC2)C(=O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 XMRPGKVKISIQBV-BJMCWZGWSA-N 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- FMGSKLZLMKYGDP-USOAJAOKSA-N dehydroepiandrosterone Chemical compound C1[C@@H](O)CC[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC=C21 FMGSKLZLMKYGDP-USOAJAOKSA-N 0.000 claims 1
- 238000002483 medication Methods 0.000 claims 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023112339A JP2023153783A (ja) | 2017-11-10 | 2023-07-07 | 遺伝性てんかん性障害の処置に使用するガナキソロン |
| JP2025067224A JP2025118661A (ja) | 2017-11-10 | 2025-04-16 | 遺伝性てんかん性障害の処置に使用するガナキソロン |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762584403P | 2017-11-10 | 2017-11-10 | |
| US62/584,403 | 2017-11-10 | ||
| PCT/US2018/060037 WO2019094724A1 (en) | 2017-11-10 | 2018-11-09 | Ganaxolone for use in treating genetic epileptic disoders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023112339A Division JP2023153783A (ja) | 2017-11-10 | 2023-07-07 | 遺伝性てんかん性障害の処置に使用するガナキソロン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021502403A JP2021502403A (ja) | 2021-01-28 |
| JP2021502403A5 true JP2021502403A5 (https=) | 2021-12-16 |
| JP7312169B2 JP7312169B2 (ja) | 2023-07-20 |
Family
ID=66438123
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020526304A Active JP7312169B2 (ja) | 2017-11-10 | 2018-11-09 | 遺伝性てんかん性障害の処置に使用するガナキソロン |
| JP2023112339A Pending JP2023153783A (ja) | 2017-11-10 | 2023-07-07 | 遺伝性てんかん性障害の処置に使用するガナキソロン |
| JP2025067224A Pending JP2025118661A (ja) | 2017-11-10 | 2025-04-16 | 遺伝性てんかん性障害の処置に使用するガナキソロン |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023112339A Pending JP2023153783A (ja) | 2017-11-10 | 2023-07-07 | 遺伝性てんかん性障害の処置に使用するガナキソロン |
| JP2025067224A Pending JP2025118661A (ja) | 2017-11-10 | 2025-04-16 | 遺伝性てんかん性障害の処置に使用するガナキソロン |
Country Status (11)
| Country | Link |
|---|---|
| US (3) | US20190160078A1 (https=) |
| EP (1) | EP3706755A4 (https=) |
| JP (3) | JP7312169B2 (https=) |
| KR (1) | KR20200085837A (https=) |
| CN (1) | CN111565724A (https=) |
| AU (2) | AU2018364659A1 (https=) |
| CA (1) | CA3079259A1 (https=) |
| EA (1) | EA202091144A1 (https=) |
| MY (1) | MY204493A (https=) |
| SG (2) | SG10202110563YA (https=) |
| WO (1) | WO2019094724A1 (https=) |
Families Citing this family (49)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HRP20230747T1 (hr) | 2011-09-08 | 2024-01-05 | Sage Therapeutics, Inc. | Neuroaktivni steroidi, pripravci i njihova uporaba |
| 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. |
| SMT201800657T1 (it) | 2013-03-13 | 2019-01-11 | Sage Therapeutics Inc | Steroidi neuroattivi e loro metodi di utilizzo |
| ES2807264T3 (es) | 2013-04-17 | 2021-02-22 | Sage Therapeutics Inc | Esteroides neuroactivos 19-nor para métodos de tratamiento |
| 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 |
| 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 |
| WO2015010054A2 (en) | 2013-07-19 | 2015-01-22 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| ES2848823T3 (es) | 2013-08-23 | 2021-08-12 | Sage Therapeutics Inc | Esteroides neuroactivos, composiciones y usos de los mismos |
| WO2015195967A1 (en) | 2014-06-18 | 2015-12-23 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| 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 |
| US10577390B2 (en) | 2014-10-16 | 2020-03-03 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| ME03809B (me) | 2014-10-16 | 2021-04-20 | Sage Therapeutics Inc | KOMPOZICIJE I POSTUPCI ZA LEČENJE POREMEĆAJA CNS-a |
| WO2016082789A1 (en) | 2014-11-27 | 2016-06-02 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| WO2016123056A1 (en) | 2015-01-26 | 2016-08-04 | 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 |
| MX382122B (es) | 2015-07-06 | 2025-03-13 | Sage Therapeutics Inc | Oxiesteroles y metodos de uso de los mismos. |
| PL3319611T3 (pl) | 2015-07-06 | 2021-07-12 | Sage Therapeutics, Inc. | Oksysterole i sposoby ich stosowania |
| AU2016289965B2 (en) | 2015-07-06 | 2021-09-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| HK1258616A1 (zh) | 2016-03-08 | 2019-11-15 | Sage Therapeutics, Inc. | 神经活性类固醇、组合物、及其用途 |
| EP3436022B1 (en) | 2016-04-01 | 2022-03-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| WO2018009867A1 (en) | 2016-07-07 | 2018-01-11 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| US20190233465A1 (en) | 2016-07-11 | 2019-08-01 | 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 |
| 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 |
| PT3519422T (pt) | 2016-09-30 | 2022-12-05 | Sage Therapeutics Inc | Oxisteróis substituídos em c7 e métodos como moduladores nmda |
| CA3041088C (en) | 2016-10-18 | 2024-05-21 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| DK4105223T3 (da) | 2016-10-18 | 2025-07-07 | Sage Therapeutics Inc | Oxysteroler og fremgangsmåder til anvendelse deraf |
| US10562930B1 (en) | 2018-08-31 | 2020-02-18 | Praxis Precision Medicines, Inc. | Salts and crystal forms of GABAA positive allosteric modulator |
| US11266662B2 (en) | 2018-12-07 | 2022-03-08 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in prophylaxis and treatment of postpartum depression |
| CN113939298A (zh) * | 2018-12-14 | 2022-01-14 | 普拉西斯精密医药公司 | 用于治疗抑郁症的方法 |
| 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 |
| CR20240234A (es) | 2019-05-31 | 2024-07-09 | Sage Therapeutics Inc | ESTEROIDES NEUROACTIVOS Y COMPOSICIONES DE ESTOS (Divisional 2021-629) |
| CN114340670B (zh) | 2019-07-11 | 2026-02-17 | 普拉克西斯精密药物股份有限公司 | T-型钙通道调节剂的制剂及其使用方法 |
| EP4041226A1 (en) * | 2019-10-02 | 2022-08-17 | Praxis Precision Medicines, Inc. | Combinations of gaba-a receptor positive allosteric modulators and nmda antagonists, nmda negative allosteric modulators or nmda partial agonists |
| JP7780431B2 (ja) | 2019-12-06 | 2025-12-04 | マリナス ファーマシューティカルズ， インコーポレイテッド | 結節性硬化症の治療での使用のためのガナキソロン |
| CN115776894A (zh) * | 2020-04-29 | 2023-03-10 | 普拉西斯精密医药公司 | T型钙通道调节剂的使用方法 |
| CN114304068B (zh) * | 2020-09-30 | 2025-07-18 | 中国科学院脑科学与智能技术卓越创新中心 | 癫痫动物模型的制备及其应用 |
| EP4255438A4 (en) * | 2020-12-07 | 2024-10-16 | Marinus Pharmaceuticals, Inc. | USE OF GANAXOLONE IN THE TREATMENT OF AN EPILEPTIC DISORDER |
| US20230321116A1 (en) * | 2022-02-16 | 2023-10-12 | Lipocine Inc. | 3Alpha-OH-5Beta-Pregnan-20-One Compositions and Methods for Treating Central Nervous System Disorders |
| WO2023060024A1 (en) * | 2021-10-04 | 2023-04-13 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in treating tuberous sclerosis complex and seizure disorders |
| WO2023060067A1 (en) * | 2021-10-04 | 2023-04-13 | Marinus Pharmaceuticals, Inc. | Amorphous solid dispersion ganaxolone formulation |
| CN119604281A (zh) * | 2022-06-02 | 2025-03-11 | 来普卡公司 | 治疗癫痫的方法和组合物 |
| KR20250136397A (ko) * | 2023-01-27 | 2025-09-16 | 하이로리스 디벨롭먼츠 에스에이 | 쓴맛 약물을 위한 맛 차폐제로서 비타민 e tpgs 의 용도 |
| WO2024257008A1 (en) * | 2023-06-13 | 2024-12-19 | Biostrike Unipessoal Lda | Compounds for diagnosing and treating epilepsy syndromes, methods and uses thereof |
| WO2025248486A1 (en) * | 2024-05-29 | 2025-12-04 | Biostrike Unipessoal Lda | Compounds for preventing sudden death in epilepsy (sudep), methods and uses thereof |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5556847A (en) * | 1994-10-27 | 1996-09-17 | Duquesne University Of The Holy Ghost | Methods of effecting memory enhancement mediated by steroid sulfatase inhibitors |
| US5888996A (en) * | 1995-07-26 | 1999-03-30 | Trustees Of Boston University | Inhibition of NMDA receptor activity and modulation of glutamate-mediated synaptic activity |
| 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. |
| US9629853B2 (en) * | 2014-05-21 | 2017-04-25 | Wisconsin Alumni Research Foundation | Uses of ganaxolone |
| EP4059522A1 (en) * | 2015-02-06 | 2022-09-21 | Marinus Pharmaceuticals, Inc. | Intravenous ganaxolone formulations and their use in treating status epilepticus and other seizure disorders |
| EA036155B1 (ru) * | 2015-10-16 | 2020-10-06 | Маринус Фармасьютикалс, Инк. | Инъекционные составы нейростероида, содержащие наночастицы |
| HK1258616A1 (zh) | 2016-03-08 | 2019-11-15 | Sage Therapeutics, Inc. | 神经活性类固醇、组合物、及其用途 |
| EP4233861A3 (en) * | 2016-08-11 | 2023-10-11 | Ovid Therapeutics, Inc. | Compositions for treatment of essential tremor |
| EP3612186A1 (en) * | 2017-04-18 | 2020-02-26 | Marinus Pharmaceuticals, Inc. | Sustained release injectable neurosteroid formulations |
-
2018
- 2018-11-09 AU AU2018364659A patent/AU2018364659A1/en not_active Abandoned
- 2018-11-09 SG SG10202110563YA patent/SG10202110563YA/en unknown
- 2018-11-09 EA EA202091144A patent/EA202091144A1/ru unknown
- 2018-11-09 CA CA3079259A patent/CA3079259A1/en active Pending
- 2018-11-09 JP JP2020526304A patent/JP7312169B2/ja active Active
- 2018-11-09 EP EP18876989.7A patent/EP3706755A4/en active Pending
- 2018-11-09 WO PCT/US2018/060037 patent/WO2019094724A1/en not_active Ceased
- 2018-11-09 US US16/185,677 patent/US20190160078A1/en not_active Abandoned
- 2018-11-09 SG SG11202004329TA patent/SG11202004329TA/en unknown
- 2018-11-09 KR KR1020207016409A patent/KR20200085837A/ko not_active Ceased
- 2018-11-09 CN CN201880085880.3A patent/CN111565724A/zh active Pending
- 2018-11-09 MY MYPI2020002311A patent/MY204493A/en unknown
-
2022
- 2022-03-24 US US17/703,331 patent/US20220249515A1/en not_active Abandoned
-
2023
- 2023-07-07 JP JP2023112339A patent/JP2023153783A/ja active Pending
-
2024
- 2024-03-21 US US18/612,277 patent/US20250082651A1/en active Pending
- 2024-10-15 AU AU2024227357A patent/AU2024227357A1/en not_active Abandoned
-
2025
- 2025-04-16 JP JP2025067224A patent/JP2025118661A/ja active Pending
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