JP2018502891A5 - - Google Patents
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- JP2018502891A5 JP2018502891A5 JP2017539021A JP2017539021A JP2018502891A5 JP 2018502891 A5 JP2018502891 A5 JP 2018502891A5 JP 2017539021 A JP2017539021 A JP 2017539021A JP 2017539021 A JP2017539021 A JP 2017539021A JP 2018502891 A5 JP2018502891 A5 JP 2018502891A5
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- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound according
- hydrogen
- composition
- 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 178
- 229910052739 hydrogen Inorganic materials 0.000 claims description 94
- 239000001257 hydrogen Substances 0.000 claims description 94
- 150000003839 salts Chemical class 0.000 claims description 90
- 125000003118 aryl group Chemical group 0.000 claims description 78
- 125000000217 alkyl group Chemical group 0.000 claims description 69
- 150000002431 hydrogen Chemical class 0.000 claims description 66
- 125000001072 heteroaryl group Chemical group 0.000 claims description 64
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 40
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 30
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims description 28
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 23
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 23
- 208000035475 disorder Diseases 0.000 claims description 23
- 208000005809 status epilepticus Diseases 0.000 claims description 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 14
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 12
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 12
- 125000002619 bicyclic group Chemical group 0.000 claims description 12
- 125000002950 monocyclic group Chemical group 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 201000009916 Postpartum depression Diseases 0.000 claims description 10
- 206010002091 Anaesthesia Diseases 0.000 claims description 9
- 206010039897 Sedation Diseases 0.000 claims description 9
- 230000037005 anaesthesia Effects 0.000 claims description 9
- 230000036280 sedation Effects 0.000 claims description 9
- 206010010904 Convulsion Diseases 0.000 claims description 7
- 210000003169 central nervous system Anatomy 0.000 claims description 7
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims description 6
- ZCQWOFVYLHDMMC-UHFFFAOYSA-N Oxazole Chemical compound C1=COC=N1 ZCQWOFVYLHDMMC-UHFFFAOYSA-N 0.000 claims description 6
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 claims description 6
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 6
- FZWLAAWBMGSTSO-UHFFFAOYSA-N Thiazole Chemical compound C1=CSC=N1 FZWLAAWBMGSTSO-UHFFFAOYSA-N 0.000 claims description 6
- 206010044565 Tremor Diseases 0.000 claims description 6
- 125000004429 atom Chemical group 0.000 claims description 6
- 229910052736 halogen Inorganic materials 0.000 claims description 6
- 150000002367 halogens Chemical class 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 6
- 229910052760 oxygen Inorganic materials 0.000 claims description 6
- 239000001301 oxygen Substances 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 125000004434 sulfur atom Chemical group 0.000 claims description 6
- 238000001990 intravenous administration Methods 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 4
- 206010015037 epilepsy Diseases 0.000 claims description 4
- 201000006517 essential tremor Diseases 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 208000009575 Angelman syndrome Diseases 0.000 claims description 3
- 208000001914 Fragile X syndrome Diseases 0.000 claims description 3
- 208000019022 Mood disease Diseases 0.000 claims description 3
- 208000016285 Movement disease Diseases 0.000 claims description 3
- 208000002193 Pain Diseases 0.000 claims description 3
- 208000006289 Rett Syndrome Diseases 0.000 claims description 3
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 claims description 3
- 208000009205 Tinnitus Diseases 0.000 claims description 3
- 206010048010 Withdrawal syndrome Diseases 0.000 claims description 3
- 208000029560 autism spectrum disease Diseases 0.000 claims description 3
- 208000010877 cognitive disease Diseases 0.000 claims description 3
- 230000001939 inductive effect Effects 0.000 claims description 3
- 230000036407 pain Effects 0.000 claims description 3
- 208000022821 personality disease Diseases 0.000 claims description 3
- 201000000980 schizophrenia Diseases 0.000 claims description 3
- 208000019116 sleep disease Diseases 0.000 claims description 3
- 238000001228 spectrum Methods 0.000 claims description 3
- 201000009032 substance abuse Diseases 0.000 claims description 3
- 231100000736 substance abuse Toxicity 0.000 claims description 3
- 208000011117 substance-related disease Diseases 0.000 claims description 3
- 231100000886 tinnitus Toxicity 0.000 claims description 3
- 208000019553 vascular disease Diseases 0.000 claims description 3
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 241000124008 Mammalia Species 0.000 claims description 2
- 208000026139 Memory disease Diseases 0.000 claims description 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 2
- 230000036461 convulsion Effects 0.000 claims description 2
- 230000002920 convulsive effect Effects 0.000 claims description 2
- 208000028329 epileptic seizure Diseases 0.000 claims description 2
- 230000006870 function Effects 0.000 claims description 2
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims description 2
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical group NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims description 2
- 238000001802 infusion Methods 0.000 claims description 2
- 208000024714 major depressive disease Diseases 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 239000008247 solid mixture Substances 0.000 claims description 2
- 230000009529 traumatic brain injury Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 50
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims 6
- 238000000034 method Methods 0.000 description 48
- 208000028698 Cognitive impairment Diseases 0.000 description 1
- 239000003691 GABA modulator Substances 0.000 description 1
- 230000006931 brain damage Effects 0.000 description 1
- 231100000874 brain damage Toxicity 0.000 description 1
- 208000029028 brain injury Diseases 0.000 description 1
- 206010027175 memory impairment Diseases 0.000 description 1
- 208000020685 sleep-wake disease Diseases 0.000 description 1
- 150000003431 steroids Chemical class 0.000 description 1
- 230000000472 traumatic effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562107776P | 2015-01-26 | 2015-01-26 | |
| US62/107,776 | 2015-01-26 | ||
| US201562144789P | 2015-04-08 | 2015-04-08 | |
| US62/144,789 | 2015-04-08 | ||
| PCT/US2016/014835 WO2016123056A1 (en) | 2015-01-26 | 2016-01-26 | Compositions and methods for treating cns disorders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020131416A Division JP2020189848A (ja) | 2015-01-26 | 2020-08-03 | Ｃｎｓ障害を処置するための組成物および方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018502891A JP2018502891A (ja) | 2018-02-01 |
| JP2018502891A5 true JP2018502891A5 (enExample) | 2019-03-14 |
| JP6745274B2 JP6745274B2 (ja) | 2020-08-26 |
Family
ID=56544215
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017539021A Active JP6745274B2 (ja) | 2015-01-26 | 2016-01-26 | Ｃｎｓ障害を処置するための組成物および方法 |
| JP2020131416A Withdrawn JP2020189848A (ja) | 2015-01-26 | 2020-08-03 | Ｃｎｓ障害を処置するための組成物および方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020131416A Withdrawn JP2020189848A (ja) | 2015-01-26 | 2020-08-03 | Ｃｎｓ障害を処置するための組成物および方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US10426837B2 (enExample) |
| EP (1) | EP3250210B1 (enExample) |
| JP (2) | JP6745274B2 (enExample) |
| CY (1) | CY1124113T1 (enExample) |
| DK (1) | DK3250210T3 (enExample) |
| ES (1) | ES2857082T3 (enExample) |
| HR (1) | HRP20210344T1 (enExample) |
| HU (1) | HUE054092T2 (enExample) |
| LT (1) | LT3250210T (enExample) |
| PL (1) | PL3250210T3 (enExample) |
| PT (1) | PT3250210T (enExample) |
| RS (1) | RS61530B1 (enExample) |
| SI (1) | SI3250210T1 (enExample) |
| SM (1) | SMT202100113T1 (enExample) |
| WO (1) | WO2016123056A1 (enExample) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2012323888A1 (en) | 2011-10-14 | 2014-05-29 | Sage Therapeutics, Inc. | 3,3 disubstituted 19-nor pregnane compounds, compositions, and uses thereof |
| KR102121633B1 (ko) | 2012-08-21 | 2020-06-10 | 세이지 테라퓨틱스, 인크. | 간질 또는 간질지속 상태를 치료하는 방법 |
| EP2986623B1 (en) | 2013-04-17 | 2018-11-07 | Sage Therapeutics, Inc. | 19-nor c3,3-disubstituted c21-n-pyrazolyl 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 |
| US20160068563A1 (en) | 2013-04-17 | 2016-03-10 | Boyd L. Harrison | 19-nor neuroactive steroids and methods of use thereof |
| HUE051403T2 (hu) | 2013-04-17 | 2021-03-01 | Sage Therapeutics Inc | Neuroaktív 19-nor-szteroidok kezelési eljárásokhoz |
| LT3021852T (lt) | 2013-07-19 | 2021-04-12 | Sage Therapeutics, Inc. | Neuroaktyvūs steroidai, jų kompozicijos ir panaudojimas |
| EP3035940B1 (en) | 2013-08-23 | 2018-10-17 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| US10246482B2 (en) | 2014-06-18 | 2019-04-02 | 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 |
| EP3206493B1 (en) | 2014-10-16 | 2020-05-06 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| CN112961206A (zh) | 2014-10-16 | 2021-06-15 | 萨奇治疗股份有限公司 | 靶向cns障碍的组合物和方法 |
| HUE049014T2 (hu) | 2014-11-27 | 2020-09-28 | Sage Therapeutics Inc | Készítmények és módszerek a központi idegrendszer rendellenességeinek kezelésére |
| ES2857082T3 (es) | 2015-01-26 | 2021-09-28 | Sage Therapeutics Inc | Composiciones y métodos para el tratamiento de trastornos del SNC |
| US10329320B2 (en) | 2015-02-20 | 2019-06-25 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| NZ790187A (en) | 2016-07-11 | 2025-08-29 | Sage Therapeutics Inc | C7, C12, and C16 substituted neuroactive steroids and their methods of use |
| NZ790225A (en) | 2016-07-11 | 2025-08-29 | Sage Therapeutics Inc | C17, C20, and C21 substituted neuroactive steroids and their methods of use |
| IL315950A (en) | 2016-08-23 | 2024-11-01 | Sage Therapeutics Inc | 19-NOR C3, 3-Dimuter C21-N-Pyrazolyl Steroid Crystalline |
| MA51046A (fr) | 2017-12-08 | 2021-03-17 | Sage Therapeutics Inc | Dérivés de 21-[4-cyano-pyrazol-1-yl]-19-nor-pregan-3. alpha-ol-20-one deutérés pour le traitement de troubles du snc |
| CN114206900A (zh) | 2019-05-31 | 2022-03-18 | 萨奇治疗股份有限公司 | 神经活性类固醇及其组合物 |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| PE20221911A1 (es) | 2020-03-25 | 2022-12-23 | Sage Therapeutics Inc | Uso de agentes para el tratamiento de condiciones respiratorias |
| CN113968886B (zh) * | 2021-11-15 | 2022-12-13 | 湖南科瑞生物制药股份有限公司 | 一种17-甲酸甾体化合物的制备方法 |
| WO2024197317A2 (en) * | 2023-03-23 | 2024-09-26 | Emory University | Neurosteroids and prodrugs thereof |
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2016
- 2016-01-26 ES ES16743932T patent/ES2857082T3/es active Active
- 2016-01-26 HU HUE16743932A patent/HUE054092T2/hu unknown
- 2016-01-26 HR HRP20210344TT patent/HRP20210344T1/hr unknown
- 2016-01-26 PL PL16743932T patent/PL3250210T3/pl unknown
- 2016-01-26 LT LTEP16743932.2T patent/LT3250210T/lt unknown
- 2016-01-26 SM SM20210113T patent/SMT202100113T1/it unknown
- 2016-01-26 SI SI201631107T patent/SI3250210T1/sl unknown
- 2016-01-26 EP EP16743932.2A patent/EP3250210B1/en active Active
- 2016-01-26 PT PT167439322T patent/PT3250210T/pt unknown
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- 2016-01-26 JP JP2017539021A patent/JP6745274B2/ja active Active
- 2016-01-26 WO PCT/US2016/014835 patent/WO2016123056A1/en not_active Ceased
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2019
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