JP2016513663A5 - - Google Patents
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- JP2016513663A5 JP2016513663A5 JP2016502244A JP2016502244A JP2016513663A5 JP 2016513663 A5 JP2016513663 A5 JP 2016513663A5 JP 2016502244 A JP2016502244 A JP 2016502244A JP 2016502244 A JP2016502244 A JP 2016502244A JP 2016513663 A5 JP2016513663 A5 JP 2016513663A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- pharmaceutically acceptable
- acceptable salt
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims description 96
- 229910052739 hydrogen Inorganic materials 0.000 claims description 46
- 239000001257 hydrogen Substances 0.000 claims description 46
- 150000003839 salts Chemical class 0.000 claims description 46
- 125000000217 alkyl group Chemical group 0.000 claims description 42
- 229910052731 fluorine Chemical group 0.000 claims description 30
- 239000011737 fluorine Chemical group 0.000 claims description 30
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 28
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 27
- 125000001153 fluoro group Chemical group F* 0.000 claims description 21
- 125000003342 alkenyl group Chemical group 0.000 claims description 14
- 125000000304 alkynyl group Chemical group 0.000 claims description 14
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 11
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 10
- 208000002193 Pain Diseases 0.000 claims description 6
- 210000003169 central nervous system Anatomy 0.000 claims description 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 4
- 206010015037 epilepsy Diseases 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 150000002367 halogens Chemical class 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000008958 Anti-N-Methyl-D-Aspartate Receptor Encephalitis Diseases 0.000 claims description 2
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 208000020925 Bipolar disease Diseases 0.000 claims description 2
- 208000000094 Chronic Pain Diseases 0.000 claims description 2
- 206010010904 Convulsion Diseases 0.000 claims description 2
- 206010012289 Dementia Diseases 0.000 claims description 2
- 208000030814 Eating disease Diseases 0.000 claims description 2
- 208000027534 Emotional disease Diseases 0.000 claims description 2
- 206010072378 Encephalitis autoimmune Diseases 0.000 claims description 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims description 2
- 208000023105 Huntington 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
- 208000032580 NMDA receptor encephalitis Diseases 0.000 claims description 2
- 208000029726 Neurodevelopmental disease Diseases 0.000 claims description 2
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000006289 Rett Syndrome Diseases 0.000 claims description 2
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 2
- 206010041247 Social fear Diseases 0.000 claims description 2
- 208000009205 Tinnitus Diseases 0.000 claims description 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 2
- 208000026911 Tuberous sclerosis complex Diseases 0.000 claims description 2
- 230000001154 acute effect Effects 0.000 claims description 2
- 208000005298 acute pain Diseases 0.000 claims description 2
- 208000012826 adjustment disease Diseases 0.000 claims description 2
- 125000001931 aliphatic group Chemical group 0.000 claims description 2
- 208000029188 anti-NMDA receptor encephalitis Diseases 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 208000029560 autism spectrum disease Diseases 0.000 claims description 2
- 230000006931 brain damage Effects 0.000 claims description 2
- 231100000874 brain damage Toxicity 0.000 claims description 2
- 208000029028 brain injury Diseases 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 208000010877 cognitive disease Diseases 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 235000014632 disordered eating Nutrition 0.000 claims description 2
- 208000018459 dissociative disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000024732 dysthymic disease Diseases 0.000 claims description 2
- 208000007386 hepatic encephalopathy Diseases 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 206010022437 insomnia Diseases 0.000 claims description 2
- 230000035772 mutation Effects 0.000 claims description 2
- 208000030459 obsessive-compulsive personality disease Diseases 0.000 claims description 2
- 208000022821 personality disease Diseases 0.000 claims description 2
- 208000028173 post-traumatic stress disease Diseases 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
- 208000020016 psychiatric disease Diseases 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- 230000000698 schizophrenic effect Effects 0.000 claims description 2
- 208000019116 sleep disease Diseases 0.000 claims description 2
- 239000000126 substance Substances 0.000 claims description 2
- 231100000886 tinnitus Toxicity 0.000 claims description 2
- 230000009529 traumatic brain injury Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 2
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 description 5
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 description 5
- HOKKHZGPKSLGJE-GSVOUGTGSA-N N-Methyl-D-aspartic acid Chemical compound CN[C@@H](C(O)=O)CC(O)=O HOKKHZGPKSLGJE-GSVOUGTGSA-N 0.000 description 3
- 238000000034 method Methods 0.000 description 2
- 0 C[C@](C*(*)C(*)(*)O)C(CC1)C(C)(CC2)C1C1C2[C@@](C)(CC[C@@](C)(C2)O)C2=CC1 Chemical compound C[C@](C*(*)C(*)(*)O)C(CC1)C(C)(CC2)C1C1C2[C@@](C)(CC[C@@](C)(C2)O)C2=CC1 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- 206010029350 Neurotoxicity Diseases 0.000 description 1
- 206010039897 Sedation Diseases 0.000 description 1
- 206010044221 Toxic encephalopathy Diseases 0.000 description 1
- 150000001298 alcohols Chemical group 0.000 description 1
- 230000003444 anaesthetic effect Effects 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 229930195712 glutamate Natural products 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 230000002503 metabolic effect Effects 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 231100000228 neurotoxicity Toxicity 0.000 description 1
- 230000007135 neurotoxicity Effects 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361779735P | 2013-03-13 | 2013-03-13 | |
| US61/779,735 | 2013-03-13 | ||
| PCT/US2014/026784 WO2014160480A1 (en) | 2013-03-13 | 2014-03-13 | Neuroactive steroids and methods of use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017231660A Division JP6530804B2 (ja) | 2013-03-13 | 2017-12-01 | 神経刺激性ステロイドおよびその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016513663A JP2016513663A (ja) | 2016-05-16 |
| JP2016513663A5 true JP2016513663A5 (enExample) | 2017-04-13 |
| JP6255082B2 JP6255082B2 (ja) | 2017-12-27 |
Family
ID=51625437
Family Applications (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016502244A Active JP6255082B2 (ja) | 2013-03-13 | 2014-03-13 | 神経刺激性ステロイドおよびその使用方法 |
| JP2017231660A Active JP6530804B2 (ja) | 2013-03-13 | 2017-12-01 | 神経刺激性ステロイドおよびその使用方法 |
| JP2019093816A Withdrawn JP2019135261A (ja) | 2013-03-13 | 2019-05-17 | 神経刺激性ステロイドおよびその使用方法 |
| JP2021111379A Active JP7317898B2 (ja) | 2013-03-13 | 2021-07-05 | 神経刺激性ステロイドおよびその使用方法 |
| JP2022159468A Active JP7715692B2 (ja) | 2013-03-13 | 2022-10-03 | 神経刺激性ステロイドおよびその使用方法 |
| JP2025094024A Pending JP2025120299A (ja) | 2013-03-13 | 2025-06-05 | 神経刺激性ステロイドおよびその使用方法 |
Family Applications After (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017231660A Active JP6530804B2 (ja) | 2013-03-13 | 2017-12-01 | 神経刺激性ステロイドおよびその使用方法 |
| JP2019093816A Withdrawn JP2019135261A (ja) | 2013-03-13 | 2019-05-17 | 神経刺激性ステロイドおよびその使用方法 |
| JP2021111379A Active JP7317898B2 (ja) | 2013-03-13 | 2021-07-05 | 神経刺激性ステロイドおよびその使用方法 |
| JP2022159468A Active JP7715692B2 (ja) | 2013-03-13 | 2022-10-03 | 神経刺激性ステロイドおよびその使用方法 |
| JP2025094024A Pending JP2025120299A (ja) | 2013-03-13 | 2025-06-05 | 神経刺激性ステロイドおよびその使用方法 |
Country Status (25)
| Country | Link |
|---|---|
| US (6) | US20160031930A1 (enExample) |
| EP (4) | EP4643945A3 (enExample) |
| JP (6) | JP6255082B2 (enExample) |
| CN (3) | CN118702755A (enExample) |
| AU (5) | AU2014243773B2 (enExample) |
| BR (1) | BR112015022174B1 (enExample) |
| CA (2) | CA3114062A1 (enExample) |
| CY (2) | CY1120934T1 (enExample) |
| DK (3) | DK3932932T3 (enExample) |
| ES (3) | ES2699445T3 (enExample) |
| FI (1) | FI3932932T3 (enExample) |
| HR (3) | HRP20181994T1 (enExample) |
| HU (2) | HUE072324T2 (enExample) |
| IL (3) | IL318314A (enExample) |
| LT (3) | LT3461834T (enExample) |
| MX (2) | MX362544B (enExample) |
| PL (3) | PL2968369T3 (enExample) |
| PT (3) | PT3932932T (enExample) |
| RS (3) | RS67266B1 (enExample) |
| RU (1) | RU2684103C2 (enExample) |
| SI (3) | SI3932932T1 (enExample) |
| SM (3) | SMT201800657T1 (enExample) |
| TR (1) | TR201817995T4 (enExample) |
| WO (1) | WO2014160480A1 (enExample) |
| ZA (1) | ZA201506729B (enExample) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20120107533A (ko) | 2005-11-28 | 2012-10-02 | 마리누스 파마슈티컬스 | ｇａｎａｘｏｌｏｎｅ 제형, 이의 제조방법 및 용도 |
| JP5866369B2 (ja) | 2010-10-27 | 2016-02-17 | メルス オーディオ アンパーツゼルスカブ | マルチレベルのパルス幅変調を使用するオーディオアンプ |
| HRP20230747T1 (hr) | 2011-09-08 | 2024-01-05 | Sage Therapeutics, Inc. | Neuroaktivni steroidi, pripravci i njihova uporaba |
| RS67266B1 (sr) | 2013-03-13 | 2025-10-31 | Sage Therapeutics Inc | Neuroaktivni steroidi i postupci za njihovu upotrebu |
| US10259840B2 (en) | 2014-06-18 | 2019-04-16 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| EP3166613A4 (en) * | 2014-07-09 | 2018-02-21 | Duke University | Compositions and methods for the repair of myelin |
| PE20170907A1 (es) | 2014-10-07 | 2017-07-12 | Sage Therapeutics Inc | Compuestos neuroactivos y metodos de uso de los mismos |
| MD3319611T2 (ro) | 2015-07-06 | 2021-06-30 | Sage Therapeutics Inc | Oxisteroli și metode de utilizare a acestora |
| HUE055199T2 (hu) * | 2015-07-06 | 2021-11-29 | Sage Therapeutics Inc | Oxiszterolok és alkalmazási eljárásaik |
| JP6882996B2 (ja) * | 2015-07-06 | 2021-06-02 | セージ セラピューティクス， インコーポレイテッド | オキシステロールおよびそれらの使用の方法 |
| EP3362042A1 (en) | 2015-10-16 | 2018-08-22 | Marinus Pharmaceuticals, Inc. | Injectable neurosteroid formulations containing nanoparticles |
| PT3436022T (pt) | 2016-04-01 | 2022-07-04 | Sage Therapeutics Inc | Oxisteróis e métodos de utilização dos mesmos |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| MD3481846T2 (ro) * | 2016-07-07 | 2021-11-30 | Sage Therapeutics Inc | 24-Hidroxisteroli 11-substituiți pentru utilizare în tratamentul stărilor legate de NMDA |
| EP3586845A1 (en) | 2016-08-11 | 2020-01-01 | Ovid Therapeutics, Inc. | Compositions for treatment of essential tremor |
| US10391105B2 (en) | 2016-09-09 | 2019-08-27 | Marinus Pharmaceuticals Inc. | Methods of treating certain depressive disorders and delirium tremens |
| US11149056B2 (en) | 2016-09-30 | 2021-10-19 | Sage Therapeutics, Inc. | C7 substituted oxysterols and methods of use thereof |
| EP4105223B1 (en) * | 2016-10-18 | 2025-04-30 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| RU2019115113A (ru) * | 2016-10-18 | 2020-11-24 | Сейдж Терапьютикс, Инк. | Оксистеролы и способы их применения |
| CN106632565A (zh) * | 2016-11-07 | 2017-05-10 | 湖南科瑞生物制药股份有限公司 | 一种合成胆固醇的新方法 |
| US11266662B2 (en) | 2018-12-07 | 2022-03-08 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in prophylaxis and treatment of postpartum depression |
| WO2020260558A1 (en) | 2019-06-27 | 2020-12-30 | Phenex Pharmaceuticals Ag | 3-modified iso-/isoallo-lithocholic acid derivatives or their homo-analogs for preventing and treating clostridioides difficile-associated diseases |
| WO2021026124A1 (en) | 2019-08-05 | 2021-02-11 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in treatment of status epilepticus |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| WO2021113834A1 (en) | 2019-12-06 | 2021-06-10 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in treating tuberous sclerosis complex |
| JP2024517282A (ja) * | 2021-05-04 | 2024-04-19 | セージ セラピューティクス， インコーポレイテッド | パーキンソン病に関連する軽度認知障害の治療のための神経活性ステロイド |
| EP4351588A1 (en) | 2021-06-11 | 2024-04-17 | Sage Therapeutics, Inc. | Neuroactive steroid for the treatment of alzheimer's disease |
| US20240368214A1 (en) * | 2021-08-25 | 2024-11-07 | Sage Therapeutics, Inc. | Positive nmda-modulating compounds and methods of use thereof |
| JP2024534558A (ja) * | 2021-09-22 | 2024-09-20 | セージ セラピューティクス， インコーポレイテッド | 重水素化ｎｍｄａ正調節化合物及びその使用方法 |
| EP4430056A1 (en) * | 2021-11-10 | 2024-09-18 | Umecrine AB | 3.beta.-hydroxy, 3.alpha.-ethyl steroids for modulation of the alpha-3 subtype of the gaba-a receptor |
| AU2022409329A1 (en) * | 2021-12-13 | 2024-07-11 | Sage Therapeutics, Inc. | Neuroactive steroid for the treatment of huntington's disease |
| WO2023114224A1 (en) | 2021-12-13 | 2023-06-22 | Sage Therapeutics, Inc. | Combination of muscarinic receptor positive modulators and nmda positive allosteric modulators |
| CN114478672B (zh) * | 2022-01-27 | 2024-06-14 | 浙江仙居君业药业有限公司 | 一种he3286的合成方法 |
| WO2023250185A1 (en) | 2022-06-24 | 2023-12-28 | Sage Therapeutics, Inc. | Crystalline forms of a neuroactive steroid |
| JP2025523826A (ja) | 2022-07-12 | 2025-07-25 | セージ セラピューティクス， インコーポレイテッド | 神経活性ステロイドの結晶形態 |
| WO2024229290A1 (en) | 2023-05-02 | 2024-11-07 | Sage Therapeutics, Inc. | Neuroactive steroid formulations and methods of use thereof |
| WO2025227053A1 (en) * | 2024-04-25 | 2025-10-30 | Sage Therapeutics, Inc. | Nmda receptor positive allosteric modulatory compositions and methods of use thereof |
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