JP2014521662A - GABAA受容体のモジュレーターとしての新規な17β−ヘテロアリール置換ステロイド - Google Patents
GABAA受容体のモジュレーターとしての新規な17β−ヘテロアリール置換ステロイド Download PDFInfo
- Publication number
- JP2014521662A JP2014521662A JP2014523105A JP2014523105A JP2014521662A JP 2014521662 A JP2014521662 A JP 2014521662A JP 2014523105 A JP2014523105 A JP 2014523105A JP 2014523105 A JP2014523105 A JP 2014523105A JP 2014521662 A JP2014521662 A JP 2014521662A
- Authority
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- Japan
- Prior art keywords
- alkyl
- hydrogen
- heterocycloalkyl
- haloalkyl
- alkenyl
- 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.)
- Pending
Links
- 0 C[C@](CS)([C@@](*)CC(C)(CCC1)C(CC2)C1C(CC1)[C@@]2(C)[C@]1C#N)O Chemical compound C[C@](CS)([C@@](*)CC(C)(CCC1)C(CC2)C1C(CC1)[C@@]2(C)[C@]1C#N)O 0.000 description 6
- GDOPTJXRTPNYNR-UHFFFAOYSA-N CC1CCCC1 Chemical compound CC1CCCC1 GDOPTJXRTPNYNR-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/20—Hypnotics; Sedatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0044—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 with an estrane or gonane skeleton, including 18-substituted derivatives and derivatives where position 17-beta is substituted by a carbon atom not directly bonded to another carbon atom and not being part of an amide group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0094—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Anesthesiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161513059P | 2011-07-29 | 2011-07-29 | |
| US61/513,059 | 2011-07-29 | ||
| PCT/US2012/048816 WO2013019711A2 (en) | 2011-07-29 | 2012-07-30 | NOVEL 17β-HETEROARYL-SUBSTITUTED STEROIDS AS MODULATORS OF GABAA RECEPTORS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014521662A true JP2014521662A (ja) | 2014-08-28 |
| JP2014521662A5 JP2014521662A5 (enExample) | 2015-09-17 |
Family
ID=47629869
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014523105A Pending JP2014521662A (ja) | 2011-07-29 | 2012-07-30 | GABAA受容体のモジュレーターとしての新規な17β−ヘテロアリール置換ステロイド |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20140148412A1 (enExample) |
| EP (1) | EP2736919A4 (enExample) |
| JP (1) | JP2014521662A (enExample) |
| CA (1) | CA2843436A1 (enExample) |
| WO (1) | WO2013019711A2 (enExample) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018502891A (ja) * | 2015-01-26 | 2018-02-01 | 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 |
| JP2024114787A (ja) * | 2016-07-11 | 2024-08-23 | セージ セラピューティクス, インコーポレイテッド | C17、c20、およびc21置換神経刺激性ステロイドおよびそれらの使用方法 |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6205362B2 (ja) | 2011-09-08 | 2017-09-27 | セージ セラピューティクス, インコーポレイテッド | 神経刺激性のステロイド、組成物、およびそれらの使用 |
| CN104136452A (zh) | 2011-10-14 | 2014-11-05 | 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 |
| DK2806877T3 (da) | 2012-01-23 | 2019-11-04 | Sage Therapeutics Inc | Neuroaktive steroidformuleringer omfattende et kompleks af allopregnanolon og sulfobutylether beta-cyclodekstrin |
| CA2882708A1 (en) | 2012-08-21 | 2014-02-27 | Sage Therapeutics, Inc. | Methods of treating epilepsy or status epilepticus |
| JP2016501876A (ja) | 2012-11-30 | 2016-01-21 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | ステロイドの抗痙攣活性 |
| SMT201800657T1 (it) | 2013-03-13 | 2019-01-11 | Sage Therapeutics Inc | Steroidi neuroattivi e loro metodi di utilizzo |
| 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 |
| SI2986624T1 (sl) | 2013-04-17 | 2020-10-30 | Sage Therapeutics, Inc. | 19-nor nevroaktivni steroidi za metode zdravljenja |
| 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 |
| WO2014169836A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| SI3021852T1 (sl) | 2013-07-19 | 2021-07-30 | Sage Therapeutics, Inc. | Nevroaktivni steroidi, sestavki in uporabe le-teh |
| JP6466942B2 (ja) | 2013-08-23 | 2019-02-06 | セージ セラピューティクス, インコーポレイテッド | 向神経活性ステロイド、組成物、及びその使用 |
| ES2970222T3 (es) | 2014-06-18 | 2024-05-27 | Sage Therapeutics Inc | Oxiesteroles y procedimientos de uso de los mismos |
| WO2015195962A1 (en) | 2014-06-18 | 2015-12-23 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| WO2016036724A1 (en) | 2014-09-02 | 2016-03-10 | The Texas A&M University System | Method of treating organophosphate intoxication |
| JOP20200195A1 (ar) | 2014-09-08 | 2017-06-16 | Sage Therapeutics Inc | سترويدات وتركيبات نشطة عصبياً، واستخداماتها |
| RS60642B1 (sr) | 2014-10-16 | 2020-09-30 | Sage Therapeutics Inc | Kompozicije i postupci za lečenje poremećaja cns-a |
| EP4527461A3 (en) | 2014-10-16 | 2025-06-25 | Sage Therapeutics, Inc. | A compound, compositions thereof and this compound for use in methods of treating cns disorders |
| SMT202000276T1 (it) | 2014-11-27 | 2020-07-08 | Sage Therapeutics Inc | Composizioni e metodi per trattare disturbi del snc |
| JP6875996B2 (ja) | 2015-02-20 | 2021-05-26 | セージ セラピューティクス, インコーポレイテッド | 神経刺激性ステロイド、組成物、およびその使用 |
| EP3319610A4 (en) | 2015-07-06 | 2019-03-06 | Sage Therapeutics, Inc. | OXYSTEROLS AND METHOD OF USE THEREOF |
| SG10202002655VA (en) | 2015-07-06 | 2020-05-28 | Sage Therapeutics Inc | Oxysterols and methods of use thereof |
| SMT202100226T1 (it) | 2015-07-06 | 2021-05-07 | Sage Therapeutics Inc | Ossisteroli e metodi di uso degli stessi |
| WO2017156103A1 (en) | 2016-03-08 | 2017-09-14 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| PL3436022T3 (pl) | 2016-04-01 | 2022-08-08 | Sage Therapeutics, Inc. | Oksysterole i sposoby ich stosowania |
| WO2017193046A1 (en) | 2016-05-06 | 2017-11-09 | Sage Therapeutics, Inc. | Oxysterols and methods of use thereof |
| HUE055263T2 (hu) | 2016-07-07 | 2021-11-29 | Sage Therapeutics Inc | 11-Szubsztituált 24-hidroxiszterolok NMDA-hoz kapcsolódó állapotok kezelésére |
| NZ790187A (en) | 2016-07-11 | 2025-08-29 | Sage Therapeutics Inc | C7, C12, and C16 substituted neuroactive steroids and their methods of use |
| TWI854445B (zh) | 2016-08-23 | 2024-09-01 | 美商賽吉醫療公司 | 結晶19-去甲c3,3-二取代之c21-n-吡唑類固醇 |
| 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 |
| CN119350419A (zh) | 2016-10-18 | 2025-01-24 | 萨奇治疗股份有限公司 | 氧甾醇及其使用方法 |
| ES3038660T3 (en) | 2016-10-18 | 2025-10-14 | Sage Therapeutics Inc | Oxysterols and methods of use thereof |
| CN114085260B (zh) * | 2018-02-11 | 2023-10-20 | 江苏豪森药业集团有限公司 | 甾族类衍生物调节剂、其制备方法和应用 |
| 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. |
| SG11202112391UA (en) | 2019-05-31 | 2021-12-30 | Sage Therapeutics Inc | Neuroactive steroids and compositions thereof |
| US12215126B2 (en) * | 2020-05-21 | 2025-02-04 | Brigham Young University | Cationic steroidal antimicrobial compounds with endogenous groups |
| WO2023060067A1 (en) | 2021-10-04 | 2023-04-13 | Marinus Pharmaceuticals, Inc. | Amorphous solid dispersion ganaxolone formulation |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3313809A (en) * | 1965-03-05 | 1967-04-11 | Sterling Drug Inc | Steroido[21, 20-d]isoxazoles |
| WO1996016076A1 (en) * | 1994-11-23 | 1996-05-30 | Cocensys, Inc. | Androstane and pregnane series for allosteric modulation of gaba receptor |
| WO1996040043A2 (en) * | 1995-06-06 | 1996-12-19 | Cocensys, Inc. | Neuroactive steroids of the androstane and pregnane series |
| WO1998005337A1 (en) * | 1996-08-01 | 1998-02-12 | Cocensys, Inc. | Use of gaba and nmda receptor ligands for the treatment of migraine headache |
| WO2007108002A2 (en) * | 2006-03-23 | 2007-09-27 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Use of digitalis-like compounds in the treatment of affective disorders |
-
2012
- 2012-07-30 EP EP12819773.8A patent/EP2736919A4/en not_active Withdrawn
- 2012-07-30 JP JP2014523105A patent/JP2014521662A/ja active Pending
- 2012-07-30 WO PCT/US2012/048816 patent/WO2013019711A2/en not_active Ceased
- 2012-07-30 CA CA2843436A patent/CA2843436A1/en not_active Abandoned
-
2014
- 2014-01-29 US US14/166,912 patent/US20140148412A1/en not_active Abandoned
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3313809A (en) * | 1965-03-05 | 1967-04-11 | Sterling Drug Inc | Steroido[21, 20-d]isoxazoles |
| WO1996016076A1 (en) * | 1994-11-23 | 1996-05-30 | Cocensys, Inc. | Androstane and pregnane series for allosteric modulation of gaba receptor |
| WO1996040043A2 (en) * | 1995-06-06 | 1996-12-19 | Cocensys, Inc. | Neuroactive steroids of the androstane and pregnane series |
| WO1998005337A1 (en) * | 1996-08-01 | 1998-02-12 | Cocensys, Inc. | Use of gaba and nmda receptor ligands for the treatment of migraine headache |
| WO2007108002A2 (en) * | 2006-03-23 | 2007-09-27 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | Use of digitalis-like compounds in the treatment of affective disorders |
Non-Patent Citations (1)
| Title |
|---|
| C.G.WERMUTH編, 『最新 創薬化学 上巻』, JPN6014041942, 15 August 1998 (1998-08-15), pages 235 - 271, ISSN: 0003360476 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2018502891A (ja) * | 2015-01-26 | 2018-02-01 | 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 |
| JP2020189848A (ja) * | 2015-01-26 | 2020-11-26 | 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 |
| JP2024114787A (ja) * | 2016-07-11 | 2024-08-23 | セージ セラピューティクス, インコーポレイテッド | C17、c20、およびc21置換神経刺激性ステロイドおよびそれらの使用方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2736919A4 (en) | 2015-01-14 |
| WO2013019711A3 (en) | 2013-04-04 |
| EP2736919A2 (en) | 2014-06-04 |
| WO2013019711A2 (en) | 2013-02-07 |
| CA2843436A1 (en) | 2013-02-07 |
| US20140148412A1 (en) | 2014-05-29 |
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