JP2019520417A5 - - Google Patents
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- JP2019520417A5 JP2019520417A5 JP2019500826A JP2019500826A JP2019520417A5 JP 2019520417 A5 JP2019520417 A5 JP 2019520417A5 JP 2019500826 A JP2019500826 A JP 2019500826A JP 2019500826 A JP2019500826 A JP 2019500826A JP 2019520417 A5 JP2019520417 A5 JP 2019520417A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutically acceptable
- acceptable salt
- formula
- alkyl
- 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 280
- 150000003839 salts Chemical class 0.000 claims description 112
- 229910052739 hydrogen Inorganic materials 0.000 claims description 86
- 239000001257 hydrogen Substances 0.000 claims description 86
- 125000000217 alkyl group Chemical group 0.000 claims description 63
- 125000001072 heteroaryl group Chemical group 0.000 claims description 48
- 229910052736 halogen Inorganic materials 0.000 claims description 46
- 150000002367 halogens Chemical group 0.000 claims description 46
- 150000002431 hydrogen Chemical group 0.000 claims description 46
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 44
- 125000003118 aryl group Chemical group 0.000 claims description 42
- 239000000203 mixture Substances 0.000 claims description 41
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 39
- 125000000623 heterocyclic group Chemical group 0.000 claims description 36
- 125000003545 alkoxy group Chemical group 0.000 claims description 34
- 125000003342 alkenyl group Chemical group 0.000 claims description 30
- 125000000304 alkynyl group Chemical group 0.000 claims description 30
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 30
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 22
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- -1 cyano-substituted pyrazolyl Chemical group 0.000 claims description 15
- 208000035475 disorder Diseases 0.000 claims description 14
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 12
- 206010002091 Anaesthesia Diseases 0.000 claims description 7
- 206010039897 Sedation Diseases 0.000 claims description 7
- 230000037005 anaesthesia Effects 0.000 claims description 7
- 230000036280 sedation Effects 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 6
- 125000002619 bicyclic group Chemical group 0.000 claims description 6
- 210000003169 central nervous system Anatomy 0.000 claims description 6
- 229910052757 nitrogen Inorganic materials 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 6
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 6
- 229910052717 sulfur Inorganic materials 0.000 claims description 6
- 239000011593 sulfur Substances 0.000 claims description 6
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 6
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 5
- 229910052731 fluorine Inorganic materials 0.000 claims description 5
- 239000011737 fluorine Substances 0.000 claims description 5
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 4
- 208000019022 Mood disease Diseases 0.000 claims description 4
- 208000016285 Movement disease Diseases 0.000 claims description 4
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical group NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 208000009575 Angelman syndrome Diseases 0.000 claims description 3
- 206010010904 Convulsion Diseases 0.000 claims description 3
- 208000001914 Fragile X syndrome Diseases 0.000 claims description 3
- 208000006289 Rett Syndrome 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
- 208000002193 Pain 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
- 206010044565 Tremor 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
- 239000003085 diluting agent Substances 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 230000004064 dysfunction Effects 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims description 2
- 230000001939 inductive effect Effects 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015706 neuroendocrine disease Diseases 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
- 239000008247 solid mixture Substances 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
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 231100000886 tinnitus Toxicity 0.000 claims description 2
- 230000009529 traumatic brain injury Effects 0.000 claims description 2
- 210000005166 vasculature Anatomy 0.000 claims description 2
- 230000003444 anaesthetic effect Effects 0.000 claims 1
- 150000002222 fluorine compounds Chemical class 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 239000000932 sedative agent Substances 0.000 claims 1
- 230000001624 sedative effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 7
- 0 C[C@@](CC1(*)*)(C(*)[C@@](*)C2)[C@]2[C@@]2[C@]1[C@@](*)(CC(*)[C@](*)(C1*3)O)C13C(*)C2 Chemical compound C[C@@](CC1(*)*)(C(*)[C@@](*)C2)[C@]2[C@@]2[C@]1[C@@](*)(CC(*)[C@](*)(C1*3)O)C13C(*)C2 0.000 description 5
- AMNKRMGFSPVSTC-VASSRZOPSA-N CC([C@@H](CC1)C(CC2)[C@H](C3)C(C)(CC4)[C@@H]2C[C@]4(C)O)([C@H]1C(C[n]1nc(cncc2)c2c1)=O)[C@@H]3O Chemical compound CC([C@@H](CC1)C(CC2)[C@H](C3)C(C)(CC4)[C@@H]2C[C@]4(C)O)([C@H]1C(C[n]1nc(cncc2)c2c1)=O)[C@@H]3O AMNKRMGFSPVSTC-VASSRZOPSA-N 0.000 description 1
- NPKXZLGNJNLHHH-TZKILHFMSA-N C[C@]([C@@H](CC1)C(CC2)[C@H](C3)[C@@](C)(CC4)[C@@H]2C[C@]4(C)O)([C@H]1C(C[n]1ncc(C#N)c1)=O)C3=O Chemical compound C[C@]([C@@H](CC1)C(CC2)[C@H](C3)[C@@](C)(CC4)[C@@H]2C[C@]4(C)O)([C@H]1C(C[n]1ncc(C#N)c1)=O)C3=O NPKXZLGNJNLHHH-TZKILHFMSA-N 0.000 description 1
- NPYBYJIPAJWQBZ-CSQFSDRDSA-N C[C@]([C@@H](CC1)C(CC2)[C@H](C3)[C@@](C)(CC4)[C@@H]2C[C@]4(C)O)([C@H]1C(C[n]1ncc(C#N)c1)=O)C3O Chemical compound C[C@]([C@@H](CC1)C(CC2)[C@H](C3)[C@@](C)(CC4)[C@@H]2C[C@]4(C)O)([C@H]1C(C[n]1ncc(C#N)c1)=O)C3O NPYBYJIPAJWQBZ-CSQFSDRDSA-N 0.000 description 1
- JIVDAOKLFIWRHK-LEBVUOAQSA-N C[C@]([C@@H](CC1)[C@H](CC2)[C@H](C3)[C@@](C)(CC4)[C@@H]2C[C@]4(C)O)([C@H]1C(C[n]1ncc2c1cncc2)=O)[C@@H]3O Chemical compound C[C@]([C@@H](CC1)[C@H](CC2)[C@H](C3)[C@@](C)(CC4)[C@@H]2C[C@]4(C)O)([C@H]1C(C[n]1ncc2c1cncc2)=O)[C@@H]3O JIVDAOKLFIWRHK-LEBVUOAQSA-N 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022072338A JP7611186B2 (ja) | 2016-07-11 | 2022-04-26 | Ｃ７、ｃ１２、およびｃ１６置換神経刺激性ステロイドおよびそれらの使用方法 |
| JP2024226326A JP2025060778A (ja) | 2016-07-11 | 2024-12-23 | Ｃ７、ｃ１２、およびｃ１６置換神経刺激性ステロイドおよびそれらの使用方法 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662360876P | 2016-07-11 | 2016-07-11 | |
| US201662360884P | 2016-07-11 | 2016-07-11 | |
| US201662360887P | 2016-07-11 | 2016-07-11 | |
| US62/360,876 | 2016-07-11 | ||
| US62/360,884 | 2016-07-11 | ||
| US62/360,887 | 2016-07-11 | ||
| PCT/US2017/041605 WO2018013615A1 (en) | 2016-07-11 | 2017-07-11 | C7, c12, and c16 substituted neuroactive steroids and their methods of use |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022072338A Division JP7611186B2 (ja) | 2016-07-11 | 2022-04-26 | Ｃ７、ｃ１２、およびｃ１６置換神経刺激性ステロイドおよびそれらの使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019520417A JP2019520417A (ja) | 2019-07-18 |
| JP2019520417A5 true JP2019520417A5 (enExample) | 2020-08-13 |
| JP7065825B2 JP7065825B2 (ja) | 2022-05-12 |
Family
ID=59388162
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019500826A Active JP7065825B2 (ja) | 2016-07-11 | 2017-07-11 | Ｃ７、ｃ１２、およびｃ１６置換神経刺激性ステロイドおよびそれらの使用方法 |
| JP2022072338A Active JP7611186B2 (ja) | 2016-07-11 | 2022-04-26 | Ｃ７、ｃ１２、およびｃ１６置換神経刺激性ステロイドおよびそれらの使用方法 |
| JP2024226326A Pending JP2025060778A (ja) | 2016-07-11 | 2024-12-23 | Ｃ７、ｃ１２、およびｃ１６置換神経刺激性ステロイドおよびそれらの使用方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022072338A Active JP7611186B2 (ja) | 2016-07-11 | 2022-04-26 | Ｃ７、ｃ１２、およびｃ１６置換神経刺激性ステロイドおよびそれらの使用方法 |
| JP2024226326A Pending JP2025060778A (ja) | 2016-07-11 | 2024-12-23 | Ｃ７、ｃ１２、およびｃ１６置換神経刺激性ステロイドおよびそれらの使用方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US20190233465A1 (enExample) |
| EP (1) | EP3481844B1 (enExample) |
| JP (3) | JP7065825B2 (enExample) |
| AU (3) | AU2017296295B2 (enExample) |
| CA (2) | CA3279953A1 (enExample) |
| DK (1) | DK3481844T3 (enExample) |
| ES (1) | ES2992037T3 (enExample) |
| MA (1) | MA45600A (enExample) |
| WO (1) | WO2018013615A1 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20150158903A1 (en) | 2011-09-08 | 2015-06-11 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| ES2738526T3 (es) | 2011-10-14 | 2020-01-23 | Sage Therapeutics Inc | Compuestos 19-norpregnano 3,3-disustituidos, composiciones y usos de los mismos |
| IL275725B (en) | 2012-08-21 | 2022-08-01 | Sage Therapeutics Inc | Treatment methods for epilepsy and status epilepticus |
| LT2968369T (lt) | 2013-03-13 | 2018-12-27 | Sage Therapeutics, Inc. | Neuroaktyvūs steroidai ir jų panaudojimo būdai |
| US20160068563A1 (en) | 2013-04-17 | 2016-03-10 | Boyd L. Harrison | 19-nor neuroactive steroids and methods of use thereof |
| HRP20200995T1 (hr) | 2013-04-17 | 2020-11-27 | Sage Therapeutics, Inc. | 19-nor neuroaktivni steroidi za metode liječenja |
| HRP20190232T1 (hr) | 2013-04-17 | 2019-03-22 | Sage Therapeutics, Inc. | 19-nor c3,3-disupstituirani c21-n-pirazolil steroidi i postupci za njihovu upotrebu |
| 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 |
| SMT202100229T1 (it) | 2013-07-19 | 2021-05-07 | Sage Therapeutics Inc | Steroidi neuroattivi, composizioni e loro usi |
| SMT202100048T1 (it) | 2013-08-23 | 2021-03-15 | Sage Therapeutics Inc | Steroidi neuroattivi, composizioni e loro usi |
| 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 |
| JP6742308B2 (ja) | 2014-10-16 | 2020-08-19 | セージ セラピューティクス， インコーポレイテッド | Ｃｎｓ障害を処置するための組成物および方法 |
| AU2015331749A1 (en) | 2014-10-16 | 2017-05-04 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| ES2793237T3 (es) | 2014-11-27 | 2020-11-13 | Sage Therapeutics Inc | Composiciones y métodos para el tratamiento de trastornos del SNC |
| SI3250210T1 (sl) | 2015-01-26 | 2021-07-30 | Sage Therapeutics, Inc. | Sestavki in metode za zdravljenje CNS motenj |
| US10329320B2 (en) | 2015-02-20 | 2019-06-25 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| MX376833B (es) | 2015-07-06 | 2025-03-07 | Sage Therapeutics Inc | Oxiesteroles y metodos de uso de los mismos. |
| RS62220B1 (sr) | 2015-07-06 | 2021-09-30 | Sage Therapeutics Inc | Oksisteroli i postupci njihovog korišćenja |
| CN114272249A (zh) | 2016-04-01 | 2022-04-05 | 萨奇治疗股份有限公司 | 氧甾醇及其使用方法 |
| US10752653B2 (en) | 2016-05-06 | 2020-08-25 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| AU2017296295B2 (en) | 2016-07-11 | 2022-02-24 | Sage Therapeutics, Inc. | C7, C12, and C16 substituted neuroactive steroids and their methods of use |
| CN109689673B (zh) | 2016-07-11 | 2023-03-14 | 萨奇治疗股份有限公司 | C17、c20和c21取代的神经活性类固醇及其使用方法 |
| CN115974954A (zh) | 2016-08-23 | 2023-04-18 | 萨奇治疗股份有限公司 | 19-去甲c3,3-二取代的c21-n-吡唑基类固醇的晶体 |
| EP3519422B1 (en) | 2016-09-30 | 2022-08-31 | Sage Therapeutics, Inc. | C7 substituted oxysterols and these compounds for use as nmda modulators |
| KR20250054838A (ko) | 2016-10-18 | 2025-04-23 | 세이지 테라퓨틱스, 인크. | 옥시스테롤 및 그의 사용 방법 |
| ES2952106T3 (es) | 2016-10-18 | 2023-10-27 | Sage Therapeutics Inc | Oxisteroles y procedimientos de utilización de los mismos |
| 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 |
| 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 |
| CN111040015B (zh) * | 2018-10-15 | 2022-03-18 | 南京诺瑞特医药科技有限公司 | 19-去甲-c21取代类固醇衍生物 |
| 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 |
| CA3124703C (en) * | 2019-01-14 | 2023-10-17 | Beijing Xuanyi Pharmasciences Co., Ltd. | Tetrazolone substituted steroids and use thereof |
| 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 |
| AU2020302748A1 (en) * | 2019-06-27 | 2022-01-06 | Sage Therapeutics, Inc. | Compositions and methods for treating CNS disorders |
| WO2021023213A1 (zh) * | 2019-08-07 | 2021-02-11 | 上海翰森生物医药科技有限公司 | 一种甾族类衍生物调节剂的盐及其晶型 |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| US20230346801A1 (en) | 2020-03-25 | 2023-11-02 | Sage Therapeutics, Inc. | Use of agents for treatment of respiratory conditions |
| CN116606341A (zh) * | 2022-07-28 | 2023-08-18 | 上海醇健实业发展有限公司 | 治疗中枢神经系统疾病的甾体化合物及其制备方法、用途和药物组合物 |
| WO2025175304A2 (en) * | 2024-02-16 | 2025-08-21 | Sanofi Pasteur Inc. | Process for the preparation of deoxycholic acid |
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- 2017-07-11 EP EP17743137.6A patent/EP3481844B1/en active Active
- 2017-07-11 WO PCT/US2017/041605 patent/WO2018013615A1/en not_active Ceased
- 2017-07-11 US US16/316,851 patent/US20190233465A1/en not_active Abandoned
- 2017-07-11 CA CA3279953A patent/CA3279953A1/en active Pending
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