JP2016517851A5 - - Google Patents
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- JP2016517851A5 JP2016517851A5 JP2016507995A JP2016507995A JP2016517851A5 JP 2016517851 A5 JP2016517851 A5 JP 2016517851A5 JP 2016507995 A JP2016507995 A JP 2016507995A JP 2016507995 A JP2016507995 A JP 2016507995A JP 2016517851 A5 JP2016517851 A5 JP 2016517851A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- substituted
- unsubstituted
- alkyl
- 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 108
- 125000000217 alkyl group Chemical group 0.000 claims description 53
- 239000001257 hydrogen Substances 0.000 claims description 41
- 229910052739 hydrogen Inorganic materials 0.000 claims description 41
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 27
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 19
- 150000002367 halogens Chemical class 0.000 claims description 19
- 150000003839 salts Chemical class 0.000 claims description 16
- 208000035475 disorder Diseases 0.000 claims description 15
- 125000001153 fluoro group Chemical group F* 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 125000006706 (C3-C6) carbocyclyl group Chemical group 0.000 claims description 10
- 125000001188 haloalkyl group Chemical group 0.000 claims description 9
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims description 8
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 6
- 210000003169 central nervous system Anatomy 0.000 claims description 6
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 6
- 125000005843 halogen group Chemical group 0.000 claims description 5
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 206010010904 Convulsion Diseases 0.000 claims description 2
- 208000026139 Memory 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
- 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
- 206010048010 Withdrawal syndrome Diseases 0.000 claims description 2
- 150000001336 alkenes Chemical class 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- 208000029560 autism spectrum disease Diseases 0.000 claims description 2
- 208000010877 cognitive disease Diseases 0.000 claims description 2
- 230000036461 convulsion Effects 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 230000036407 pain Effects 0.000 claims description 2
- 208000022821 personality disease Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 201000000980 schizophrenia Diseases 0.000 claims description 2
- 208000019116 sleep disease Diseases 0.000 claims description 2
- 208000020685 sleep-wake disease Diseases 0.000 claims description 2
- 238000001228 spectrum Methods 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
- 231100000886 tinnitus Toxicity 0.000 claims description 2
- 230000009529 traumatic brain injury Effects 0.000 claims description 2
- 238000011282 treatment Methods 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 238000007920 subcutaneous administration Methods 0.000 claims 1
- 208000019553 vascular disease Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 230000000069 prophylactic effect Effects 0.000 description 3
- 239000003795 chemical substances by application Substances 0.000 description 2
- 125000001072 heteroaryl group Chemical group 0.000 description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2013/074323 | 2013-04-17 | ||
| CN2013074323 | 2013-04-17 | ||
| PCT/CN2014/075594 WO2014169833A1 (en) | 2013-04-17 | 2014-04-17 | 19-nor c3,3-disubstituted c21-n-pyrazolyl steroids and methods of use thereof |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018164996A Division JP6710730B2 (ja) | 2013-04-17 | 2018-09-04 | 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 |
| JP2018164995A Division JP6784735B2 (ja) | 2013-04-17 | 2018-09-04 | 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016517851A JP2016517851A (ja) | 2016-06-20 |
| JP2016517851A5 true JP2016517851A5 (OSRAM) | 2017-06-01 |
| JP6470258B2 JP6470258B2 (ja) | 2019-02-13 |
Family
ID=51730809
Family Applications (7)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016507995A Active JP6470258B2 (ja) | 2013-04-17 | 2014-04-17 | 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 |
| JP2018164995A Active JP6784735B2 (ja) | 2013-04-17 | 2018-09-04 | 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 |
| JP2018164996A Active JP6710730B2 (ja) | 2013-04-17 | 2018-09-04 | 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 |
| JP2020161921A Active JP7085601B2 (ja) | 2013-04-17 | 2020-09-28 | 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 |
| JP2022010037A Active JP7527318B2 (ja) | 2013-04-17 | 2022-01-26 | 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 |
| JP2023129979A Active JP7668850B2 (ja) | 2013-04-17 | 2023-08-09 | 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 |
| JP2024232815A Pending JP2025060975A (ja) | 2013-04-17 | 2024-12-27 | 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 |
Family Applications After (6)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018164995A Active JP6784735B2 (ja) | 2013-04-17 | 2018-09-04 | 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 |
| JP2018164996A Active JP6710730B2 (ja) | 2013-04-17 | 2018-09-04 | 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 |
| JP2020161921A Active JP7085601B2 (ja) | 2013-04-17 | 2020-09-28 | 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 |
| JP2022010037A Active JP7527318B2 (ja) | 2013-04-17 | 2022-01-26 | 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 |
| JP2023129979A Active JP7668850B2 (ja) | 2013-04-17 | 2023-08-09 | 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 |
| JP2024232815A Pending JP2025060975A (ja) | 2013-04-17 | 2024-12-27 | 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 |
Country Status (26)
| Country | Link |
|---|---|
| US (6) | US9512165B2 (OSRAM) |
| EP (4) | EP2986623B1 (OSRAM) |
| JP (7) | JP6470258B2 (OSRAM) |
| KR (4) | KR102239541B1 (OSRAM) |
| CN (4) | CN118754924A (OSRAM) |
| AU (5) | AU2014256229B2 (OSRAM) |
| BR (1) | BR112015026380A8 (OSRAM) |
| CA (1) | CA2909545A1 (OSRAM) |
| CY (2) | CY1121228T1 (OSRAM) |
| DK (3) | DK3909966T3 (OSRAM) |
| ES (3) | ES3044385T3 (OSRAM) |
| HR (2) | HRP20190232T1 (OSRAM) |
| HU (2) | HUE055554T2 (OSRAM) |
| IL (4) | IL310348A (OSRAM) |
| LT (2) | LT3498725T (OSRAM) |
| MX (3) | MX362543B (OSRAM) |
| PL (2) | PL2986623T3 (OSRAM) |
| PT (2) | PT3498725T (OSRAM) |
| RS (2) | RS58297B1 (OSRAM) |
| RU (1) | RU2675855C2 (OSRAM) |
| SG (2) | SG11201508550XA (OSRAM) |
| SI (2) | SI3498725T1 (OSRAM) |
| SM (2) | SMT201900066T1 (OSRAM) |
| TR (1) | TR201901745T4 (OSRAM) |
| WO (1) | WO2014169833A1 (OSRAM) |
| ZA (1) | ZA201507740B (OSRAM) |
Families Citing this family (71)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2631233C (en) | 2005-11-28 | 2011-11-08 | Marinus Pharmaceuticals | Ganaxolone formulations and methods for the making and use thereof |
| CN113234114A (zh) | 2011-10-14 | 2021-08-10 | 萨奇治疗股份有限公司 | 3,3-二取代的19-去甲孕甾烷化合物、组合物、及其用途 |
| WO2013112605A2 (en) | 2012-01-23 | 2013-08-01 | Sage Therapeutics, Inc. | Neuroactive steroid formulations and methods of treating cns disorders |
| US10039777B2 (en) | 2012-03-20 | 2018-08-07 | Neuro-Lm Sas | Methods and pharmaceutical compositions of the treatment of autistic syndrome disorders |
| HUE056838T2 (hu) | 2012-08-21 | 2022-04-28 | Sage Therapeutics Inc | Allopregnanolon makacs epileptikus állapot kezelésére |
| US20160068563A1 (en) | 2013-04-17 | 2016-03-10 | Boyd L. Harrison | 19-nor neuroactive steroids and methods of use thereof |
| US9725481B2 (en) | 2013-04-17 | 2017-08-08 | Sage Therapeutics, Inc. | 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof |
| TR201901745T4 (tr) | 2013-04-17 | 2019-03-21 | Sage Therapeutics Inc | 19-nor C3,3-disübstitüe edilmiş C21- n-pirazolil steroidleri ve bunların kullanım yöntemleri. |
| SI2986624T1 (sl) | 2013-04-17 | 2020-10-30 | Sage Therapeutics, Inc. | 19-nor nevroaktivni steroidi za metode zdravljenja |
| PL3021852T3 (pl) | 2013-07-19 | 2021-07-05 | Sage Therapeutics, Inc. | Neuroaktywne steroidy, kompozycje i ich zastosowania |
| PT3035940T (pt) | 2013-08-23 | 2019-01-28 | Sage Therapeutics Inc | Esteroides neuroativos, composições e seus usos |
| 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 |
| PT3206493T (pt) | 2014-10-16 | 2020-08-03 | Sage Therapeutics Inc | Composições e métodos para tratamento de transtornos do snc |
| KR20230170816A (ko) | 2014-10-16 | 2023-12-19 | 세이지 테라퓨틱스, 인크. | Cns 장애의 치료를 위한 조성물 및 방법 |
| JP6893173B2 (ja) | 2014-11-27 | 2021-06-23 | 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 |
| CN104558092B (zh) * | 2014-12-29 | 2017-01-18 | 北京理工大学 | 一种甾体皂苷化合物及其制备方法和用途 |
| HUE054092T2 (hu) | 2015-01-26 | 2021-08-30 | Sage Therapeutics Inc | Központi idegrendszeri zavarok kezelésére szolgáló kompozíciók és eljárások |
| US10329320B2 (en) | 2015-02-20 | 2019-06-25 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| MA45276A (fr) | 2015-06-18 | 2018-04-25 | Sage Therapeutics Inc | Solutions de stéroïdes neuroactifs et leurs méthodes d'utilisation |
| CN104910236B (zh) * | 2015-06-26 | 2016-08-17 | 西北农林科技大学农药研究所 | 吡唑基甾体衍生物及其制备方法、用途 |
| MX2018004376A (es) | 2015-10-16 | 2018-08-01 | Marinus Pharmaceuticals Inc | Formulaciones inyectables de neuroesteroides que contienen nanoparticulas. |
| RU2766155C2 (ru) | 2016-03-08 | 2022-02-08 | Сейдж Терапьютикс, Инк. | Нейроактивные стероиды, их композиции и применения |
| NZ790226A (en) | 2016-07-11 | 2025-08-29 | Sage Therapeutics Inc | C17, C20, and C21 substituted neuroactive steroids and their methods of use |
| CA3030420C (en) * | 2016-07-11 | 2025-11-18 | Sage Therapeutics, Inc. | C7, C12 AND C16 SUBSTITUTED NEUROACTIVE STEROIDS AND ASSOCIATED METHODS OF USE |
| JP2019524816A (ja) | 2016-08-11 | 2019-09-05 | オービッド・セラピューティクス・インコーポレイテッドＯｖｉｄ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | てんかん性障害の処置のための方法および組成物 |
| NZ791594A (en) * | 2016-08-23 | 2025-08-29 | Sage Therapeutics Inc | A crystalline 19-nor C3, 3-disubstituted C21-N-pyrazolyl steroid |
| US10391105B2 (en) | 2016-09-09 | 2019-08-27 | Marinus Pharmaceuticals Inc. | Methods of treating certain depressive disorders and delirium tremens |
| RU2019136361A (ru) * | 2017-04-18 | 2021-05-13 | Маринус Фармасьютикалс, Инк | Инъекционные составы нейростеорида с замедленным высвобождением |
| KR20200011946A (ko) * | 2017-06-01 | 2020-02-04 | 수미토모 케미칼 컴퍼니 리미티드 | 복소환 화합물 및 그것을 함유하는 조성물 |
| MX2020002652A (es) * | 2017-09-07 | 2020-09-25 | Sage Therapeutics Inc | Esteroides neuroactivos y su método de uso. |
| TW201919642A (zh) * | 2017-09-14 | 2019-06-01 | 美商賽吉醫療公司 | 19去甲c3,3-二取代之c21-n-吡唑類固醇及其使用方法 |
| WO2019075362A1 (en) * | 2017-10-12 | 2019-04-18 | Sage Therapeutics, Inc. | METHOD OF TREATING CENTRAL NERVOUS SYSTEM DISORDERS WITH NEUROSTEROIDS AND GABAERGIC COMPOUNDS |
| 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 |
| MX2020006608A (es) * | 2017-12-22 | 2020-11-06 | Sage Therapeutics Inc | Composiciones y metodos para el tratamiento de trastornos en el sistema nervioso central. |
| CN111770929B (zh) * | 2017-12-22 | 2023-12-26 | 萨奇治疗股份有限公司 | 治疗cns疾病的组合物和方法 |
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| MX2020008422A (es) | 2018-02-11 | 2020-09-21 | Jiangsu Hansoh Pharmaceutical Group Co Ltd | Regulador derivado de esteroides, metodo para prepararlos y usos de los mismos. |
| BR112020015131A2 (pt) * | 2018-02-11 | 2021-01-05 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Reguladores derivados de esteroide, método para preparar os mesmos, e usos dos mesmos |
| EP3806863A1 (en) * | 2018-06-12 | 2021-04-21 | Sage Therapeutics, Inc. | A 19-nor c3,3-disubstituted c21 -n-pyrazolyl steroid and methods of use thereof |
| 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 |
| CN109503694A (zh) * | 2018-11-21 | 2019-03-22 | 苏州闻天医药科技有限公司 | 一种新型gabaa受体调节剂及其用途 |
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| US11266662B2 (en) | 2018-12-07 | 2022-03-08 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in prophylaxis and treatment of postpartum depression |
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| CN116589521B (zh) * | 2019-01-08 | 2025-07-11 | 成都康弘药业集团股份有限公司 | 甾体类化合物、用途及其制备方法 |
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| EP4072559A4 (en) | 2019-12-06 | 2023-06-21 | Marinus Pharmaceuticals, Inc. | GANAXOLONE FOR USE IN THE TREATMENT OF TUBEROUS SCLEROSIS COMPLEX |
| JP2023519241A (ja) * | 2020-03-25 | 2023-05-10 | セージ セラピューティクス， インコーポレイテッド | 呼吸器状態の処置のための薬剤の使用 |
| JP2023537240A (ja) * | 2020-07-20 | 2023-08-31 | 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ｃ３，３－二置換ｃ２１－ｎ－ピラゾリルステロイドの製剤及びその使用方法 |
| US20240122945A1 (en) * | 2021-01-28 | 2024-04-18 | Sage Therapeutics, Inc. | Use of neuroactive steroids for treatment of sexual dysfunction |
| KR20230158033A (ko) | 2021-03-17 | 2023-11-17 | 세이지 테라퓨틱스, 인크. | 주요 우울 장애의 치료를 위한 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 |
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