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.)
- Granted
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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 (OSRAM) | 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 (OSRAM) |
| EP (4) | EP3932932B8 (OSRAM) |
| JP (6) | JP6255082B2 (OSRAM) |
| CN (3) | CN118702755A (OSRAM) |
| AU (5) | AU2014243773B2 (OSRAM) |
| BR (1) | BR112015022174B1 (OSRAM) |
| CA (2) | CA3114062A1 (OSRAM) |
| CY (2) | CY1120934T1 (OSRAM) |
| DK (3) | DK3932932T3 (OSRAM) |
| ES (3) | ES2699445T3 (OSRAM) |
| FI (1) | FI3932932T3 (OSRAM) |
| HR (3) | HRP20181994T1 (OSRAM) |
| HU (2) | HUE055668T2 (OSRAM) |
| IL (3) | IL280068B2 (OSRAM) |
| LT (3) | LT3932932T (OSRAM) |
| MX (2) | MX388210B (OSRAM) |
| PL (3) | PL3461834T3 (OSRAM) |
| PT (3) | PT2968369T (OSRAM) |
| RS (3) | RS58166B1 (OSRAM) |
| RU (1) | RU2684103C2 (OSRAM) |
| SI (3) | SI3461834T1 (OSRAM) |
| SM (3) | SMT202500336T1 (OSRAM) |
| TR (1) | TR201817995T4 (OSRAM) |
| WO (1) | WO2014160480A1 (OSRAM) |
| ZA (1) | ZA201506729B (OSRAM) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
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| EP1959966B1 (en) | 2005-11-28 | 2020-06-03 | Marinus Pharmaceuticals, Inc. | Ganaxolone formulations and methods for the making and use thereof |
| EP2633621B1 (en) | 2010-10-27 | 2017-08-30 | Merus Audio ApS | Audio amplifier using multi-level pulse width modulation |
| AU2012304412A1 (en) | 2011-09-08 | 2014-03-27 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| PT2968369T (pt) | 2013-03-13 | 2018-12-05 | Sage Therapeutics Inc | Esteroides neuroativos e métodos para o seu uso |
| WO2015195967A1 (en) | 2014-06-18 | 2015-12-23 | 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 |
| CA2963938C (en) | 2014-10-07 | 2023-10-24 | Sage Therapeutics, Inc. | Neuroactive compounds and methods of use thereof |
| CN113292623A (zh) | 2015-07-06 | 2021-08-24 | 萨奇治疗股份有限公司 | 孕甾醇及其使用方法 |
| PT3319612T (pt) | 2015-07-06 | 2021-08-24 | Sage Therapeutics Inc | Oxisteróis e métodos de utilização dos mesmos |
| EP3319610A4 (en) | 2015-07-06 | 2019-03-06 | Sage Therapeutics, Inc. | OXYSTEROLS AND METHOD OF USE THEREOF |
| EA036155B1 (ru) | 2015-10-16 | 2020-10-06 | Маринус Фармасьютикалс, Инк. | Инъекционные составы нейростероида, содержащие наночастицы |
| ES2921010T3 (es) * | 2016-04-01 | 2022-08-16 | Sage Therapeutics Inc | Oxisteroles y procedimientos de uso de los mismos |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| ES2884071T3 (es) * | 2016-07-07 | 2021-12-10 | Sage Therapeutics Inc | 24-hidroxiesteroles sustituidos en 11 para el tratamiento de afecciones relacionadas con NMDA |
| MX2019001669A (es) | 2016-08-11 | 2019-09-27 | Ovid Therapeutics Inc | Metodos y composiciones para el tratamiento de trastornos epilepticos. |
| US10391105B2 (en) | 2016-09-09 | 2019-08-27 | Marinus Pharmaceuticals Inc. | Methods of treating certain depressive disorders and delirium tremens |
| ES2935057T3 (es) * | 2016-09-30 | 2023-03-01 | Sage Therapeutics Inc | C7 oxisteroles sustituidos y estos compuestos para su uso como moduladores de la NMDA |
| EP4105223B1 (en) * | 2016-10-18 | 2025-04-30 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| BR112019008032A2 (pt) * | 2016-10-18 | 2019-09-03 | Sage Therapeutics, Inc. | oxiesteróis e métodos de uso dos mesmos |
| 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 |
| EP4009982A4 (en) | 2019-08-05 | 2023-08-09 | 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 |
| MX2022006014A (es) | 2019-12-06 | 2022-06-22 | Marinus Pharmaceuticals Inc | Ganaxolona para uso en el tratamiento del complejo de esclerosis tuberosa. |
| MX2023013072A (es) * | 2021-05-04 | 2024-03-19 | Sage Therapeutics Inc | Esteroide neuroactivo para el tratamiento del deterioro cognitivo leve asociado a la enfermedad de parkinson. |
| CA3223179A1 (en) | 2021-06-11 | 2022-12-15 | Sage Therapeutics, Inc. | Neuroactive steroid for the treatment of alzheimer's disease |
| WO2023028278A2 (en) * | 2021-08-25 | 2023-03-02 | Sage Therapeutics, Inc. | Positive nmda-modulating compounds and methods of use thereof |
| WO2023049295A1 (en) * | 2021-09-22 | 2023-03-30 | Sage Therapeutics, Inc. | Deuterated positive nmda-modulating compounds and methods of use thereof |
| WO2023083979A1 (en) * | 2021-11-10 | 2023-05-19 | 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 |
| EP4447953A1 (en) | 2021-12-13 | 2024-10-23 | 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 |
| AU2023287695A1 (en) | 2022-06-24 | 2025-02-06 | 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 |
| AR132567A1 (es) | 2023-05-02 | 2025-07-16 | Sage Therapeutics Inc | Formulaciones de esteroides neuroactivos y métodos de uso de estas |
| 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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