JP2010530004A5 - - Google Patents
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- Publication number
- JP2010530004A5 JP2010530004A5 JP2010512418A JP2010512418A JP2010530004A5 JP 2010530004 A5 JP2010530004 A5 JP 2010530004A5 JP 2010512418 A JP2010512418 A JP 2010512418A JP 2010512418 A JP2010512418 A JP 2010512418A JP 2010530004 A5 JP2010530004 A5 JP 2010530004A5
- Authority
- JP
- Japan
- Prior art keywords
- aryl
- alkyl
- substituted
- alkenyl
- cycloalkyl
- 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
Links
- 125000000217 alkyl group Chemical group 0.000 claims 85
- 125000003118 aryl group Chemical group 0.000 claims 64
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 61
- 125000003342 alkenyl group Chemical group 0.000 claims 57
- 125000000304 alkynyl group Chemical group 0.000 claims 49
- 125000000623 heterocyclic group Chemical class 0.000 claims 38
- 229920001577 copolymer Chemical group 0.000 claims 34
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 18
- 125000002534 ethynyl group Chemical class [H]C#C* 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- -1 triethylsilyl Chemical group 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 9
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- KWEDUNSJJZVRKR-UHFFFAOYSA-N carbononitridic azide Chemical compound [N-]=[N+]=NC#N KWEDUNSJJZVRKR-UHFFFAOYSA-N 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 150000001540 azides Chemical class 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 5
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 4
- 150000003242 quaternary ammonium salts Chemical class 0.000 claims 4
- BJSNHQAWNWHTOI-UHFFFAOYSA-N [N-]=[N+]=N[S+](C#N)C#N Chemical compound [N-]=[N+]=N[S+](C#N)C#N BJSNHQAWNWHTOI-UHFFFAOYSA-N 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000005031 thiocyano group Chemical group S(C#N)* 0.000 claims 3
- 229930194542 Keto Natural products 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000000468 ketone group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 claims 1
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 claims 1
- NENKKJDNYSKDBT-UHFFFAOYSA-N 1,3-dioxan-4-one Chemical compound O=C1CCOCO1 NENKKJDNYSKDBT-UHFFFAOYSA-N 0.000 claims 1
- GZTMCZAOQTVOJK-UHFFFAOYSA-N 1,3-dioxolan-4-one Chemical class O=C1COCO1 GZTMCZAOQTVOJK-UHFFFAOYSA-N 0.000 claims 1
- FYAVYWUBPQMCQN-UHFFFAOYSA-N 1,3-oxathiolan-5-one Chemical group O=C1CSCO1 FYAVYWUBPQMCQN-UHFFFAOYSA-N 0.000 claims 1
- 208000007848 Alcoholism Diseases 0.000 claims 1
- 208000019901 Anxiety disease Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000026139 Memory disease Diseases 0.000 claims 1
- 241001465754 Metazoa Species 0.000 claims 1
- 208000001738 Nervous System Trauma Diseases 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 125000003302 alkenyloxy group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004414 alkyl thio group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 230000036506 anxiety Effects 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 206010013663 drug dependence Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 1
- 208000028412 nervous system injury Diseases 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 208000011117 substance-related disease Diseases 0.000 claims 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical compound [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 claims 1
- 125000000475 sulfinyl group Chemical group [*:2]S([*:1])=O 0.000 claims 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 claims 1
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- DHCDFWKWKRSZHF-UHFFFAOYSA-N sulfurothioic S-acid Chemical compound OS(O)(=O)=S DHCDFWKWKRSZHF-UHFFFAOYSA-N 0.000 claims 1
- 0 C[C@](CC1)(C(CC2)C(CC3)C1[C@@](*)(CC1)C3C[C@]1(*)O)[C@]2S* Chemical compound C[C@](CC1)(C(CC2)C(CC3)C1[C@@](*)(CC1)C3C[C@]1(*)O)[C@]2S* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94425707P | 2007-06-15 | 2007-06-15 | |
| US60/944,257 | 2007-06-15 | ||
| PCT/US2008/067059 WO2008157460A1 (en) | 2007-06-15 | 2008-06-16 | Androstane and pregnane steroids with potent allosteric gaba receptor chloride ionophore modulating properties |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014202979A Division JP5990557B2 (ja) | 2007-06-15 | 2014-10-01 | Ｇａｂａレセプタークロライドイオノフォアの潜在的アロステリック調節特性を有するアンドロスタンステロイドおよびプレグナンステロイド |
| JP2014202980A Division JP5828159B2 (ja) | 2007-06-15 | 2014-10-01 | Ｇａｂａレセプタークロライドイオノフォアの潜在的アロステリック調節特性を有するアンドロスタンステロイドおよびプレグナンステロイド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010530004A JP2010530004A (ja) | 2010-09-02 |
| JP2010530004A5 true JP2010530004A5 (enExample) | 2011-07-28 |
| JP5663303B2 JP5663303B2 (ja) | 2015-02-04 |
Family
ID=40156649
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010512418A Expired - Fee Related JP5663303B2 (ja) | 2007-06-15 | 2008-06-16 | Ｇａｂａレセプタークロライドイオノフォアの潜在的アロステリック調節特性を有するアンドロスタンステロイドおよびプレグナンステロイド |
| JP2014202979A Expired - Fee Related JP5990557B2 (ja) | 2007-06-15 | 2014-10-01 | Ｇａｂａレセプタークロライドイオノフォアの潜在的アロステリック調節特性を有するアンドロスタンステロイドおよびプレグナンステロイド |
| JP2014202980A Expired - Fee Related JP5828159B2 (ja) | 2007-06-15 | 2014-10-01 | Ｇａｂａレセプタークロライドイオノフォアの潜在的アロステリック調節特性を有するアンドロスタンステロイドおよびプレグナンステロイド |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014202979A Expired - Fee Related JP5990557B2 (ja) | 2007-06-15 | 2014-10-01 | Ｇａｂａレセプタークロライドイオノフォアの潜在的アロステリック調節特性を有するアンドロスタンステロイドおよびプレグナンステロイド |
| JP2014202980A Expired - Fee Related JP5828159B2 (ja) | 2007-06-15 | 2014-10-01 | Ｇａｂａレセプタークロライドイオノフォアの潜在的アロステリック調節特性を有するアンドロスタンステロイドおよびプレグナンステロイド |
Country Status (7)
| Country | Link |
|---|---|
| US (3) | US8575375B2 (enExample) |
| EP (1) | EP2155204B1 (enExample) |
| JP (3) | JP5663303B2 (enExample) |
| AU (1) | AU2008265898B2 (enExample) |
| CA (1) | CA2698172C (enExample) |
| ES (1) | ES2589139T3 (enExample) |
| WO (1) | WO2008157460A1 (enExample) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2698172C (en) * | 2007-06-15 | 2014-02-18 | Cook, Kevin M. | Androstane and pregnane steroids with potent allosteric gaba receptor chloride ionophore modulating properties |
| US20110086828A1 (en) * | 2009-10-07 | 2011-04-14 | Board Of Supervisors Of Louisiana State University And Agricultural And Mechanical College | Treatment of alcohol abuse and alcoholism using modulators of neurosteroid binding sites on gabaa receptors |
| US10478505B2 (en) | 2011-09-23 | 2019-11-19 | The Regents Of The University Of California | Edible oils to enhance delivery of orally administered steroids |
| CA3152410A1 (en) | 2011-10-14 | 2013-04-18 | Sage Therapeutics, Inc. | 3,3-disubstituted 19-nor pregnane compounds, compositions, and uses thereof for the treatment of cns related disorders |
| SMT202000008T1 (it) | 2012-01-23 | 2020-03-13 | Sage Therapeutics Inc | Formulazione di steroide neuroattivo comprendente un complesso di allopregnanolone e solfobutil eter beta-ciclodestrina |
| WO2014028398A2 (en) | 2012-08-13 | 2014-02-20 | The Regents Of The University Of California | Mitigation of epileptic seizures by combination therapy using benzodiazepines and neurosteroids |
| PL2887944T3 (pl) | 2012-08-21 | 2022-02-21 | Sage Therapeutics, Inc. | Allopregnanolon do leczenia lekoopornego stanu padaczkowego |
| ES2973320T3 (es) | 2012-11-30 | 2024-06-19 | Univ California | Alopregnanolona para tratar, reducir o mitigar los síntomas de la depresión posparto |
| TR201808616T4 (tr) | 2012-12-18 | 2018-07-23 | Sage Therapeutics Inc | Nöroaktif 19-alkoksi-17-ikameli steroidler, bunların ön ilaçları ve bunları kullanan tedavi yöntemleri. |
| CN113527400B (zh) | 2013-04-17 | 2024-06-28 | 萨奇治疗股份有限公司 | 19-去甲c3,3-二取代的c21-n-吡唑基类固醇及其使用方法 |
| RU2019126333A (ru) * | 2013-04-17 | 2019-10-08 | Сейдж Терапьютикс, Инк. | 19-нор нейроактивные стероиды и способы их применения |
| US20160068563A1 (en) | 2013-04-17 | 2016-03-10 | Boyd L. Harrison | 19-nor neuroactive 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 |
| WO2015010054A2 (en) | 2013-07-19 | 2015-01-22 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| AU2014308621C1 (en) | 2013-08-23 | 2022-01-06 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| WO2015195962A1 (en) | 2014-06-18 | 2015-12-23 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| EP3188734A4 (en) | 2014-09-02 | 2018-01-10 | 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 |
| SMT202000414T1 (it) | 2014-10-16 | 2020-09-10 | Sage Therapeutics Inc | Composizioni e metodi per trattare disturbi del snc |
| MX2021004492A (es) | 2014-10-16 | 2022-12-05 | Sage Therapeutics Inc | Composiciones para el tratamiento de trastornos del snc. |
| ME03749B (me) | 2014-11-27 | 2021-04-20 | Sage Therapeutics Inc | KOMPOZICIJE I POSTUPCIZA LEČENJE POREMEĆAJA CNS-a |
| DK3250210T3 (da) | 2015-01-26 | 2021-03-08 | Sage Therapeutics Inc | Sammensætninger og fremgangsmåder til behandling af cns-forstyrrelser |
| 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 |
| AR105044A1 (es) | 2015-06-18 | 2017-08-30 | Sage Therapeutics Inc | Soluciones de esteroides neuroactivos y sus métodos de uso, recipiente |
| RU2766155C2 (ru) | 2016-03-08 | 2022-02-08 | Сейдж Терапьютикс, Инк. | Нейроактивные стероиды, их композиции и применения |
| WO2018013613A1 (en) | 2016-07-11 | 2018-01-18 | 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 |
| EP3507093A4 (en) * | 2016-08-30 | 2020-04-08 | Rize Inc. | Method of fabricating a three-dimensional object with removable support structure |
| CA3075038A1 (en) * | 2017-09-07 | 2019-03-14 | Sage Therapeutics, Inc. | Neuroactive steroids and their methods of use |
| JP7648538B2 (ja) | 2019-04-27 | 2025-03-18 | ヘルス リサーチ インコーポレイテッド | 前立腺癌の治療のためのクマリン修飾アンドロゲン |
| 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 |
| CN111057120B (zh) * | 2019-12-27 | 2021-04-27 | 苏州翔实医药发展有限公司 | 一种依托孕烯衍生物a及其制备方法和用途 |
| JP2023527288A (ja) * | 2020-05-18 | 2023-06-28 | ヴィスタゲン セラピューティクス、インコーポレイテッド | 適応障害の治療 |
| WO2023060067A1 (en) | 2021-10-04 | 2023-04-13 | Marinus Pharmaceuticals, Inc. | Amorphous solid dispersion ganaxolone formulation |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2753361A (en) * | 1955-02-01 | 1956-07-03 | Searle & Co | 17-thio-5-androstene-3-ols |
| US2763669A (en) * | 1955-03-01 | 1956-09-18 | Searle & Co | delta-17-thio-androsten-3-ones |
| US2847427A (en) * | 1957-09-09 | 1958-08-12 | Searle & Co | Delta or 5,16 androstadien-17-alkylsulfones and sulfoxides |
| US3001986A (en) * | 1960-07-14 | 1961-09-26 | Searle & Co | 3-oxygenated 17 - amino - 17 - carboxyethylandrostane lactams and delta4 compounds corresponding |
| US3094522A (en) * | 1961-07-25 | 1963-06-18 | Merck & Co Inc | Alkanoylthio and pyrazolo androstane derivatives |
| US3094521A (en) | 1961-07-25 | 1963-06-18 | Merck & Co Inc | Alkanoylthio and pyrazolo androstane derivatives |
| US4891367A (en) * | 1987-04-22 | 1990-01-02 | Merrell Dow Pharmaceuticals Inc. | 17β-(cyclopropyloxy)androst-5-en-3β-ol and related compounds useful as C17-20 lyase inhibitors |
| US5232917A (en) | 1987-08-25 | 1993-08-03 | University Of Southern California | Methods, compositions, and compounds for allosteric modulation of the GABA receptor by members of the androstane and pregnane series |
| DK0752860T3 (da) | 1994-02-14 | 2000-11-13 | Euro Celtique Sa | Androstaner og pregnaner til allosterisk modulering af GABA-receptor |
| US5939545A (en) * | 1994-02-14 | 1999-08-17 | Cocensys, Inc. | Method, compositions, and compounds for allosteric modulation of the gaba receptor by members of the androstane and pregnane series |
| CN1187053C (zh) * | 1997-10-06 | 2005-02-02 | 利兰·斯坦福青年大学托管委员会 | 糖皮质素受体拮抗剂用于制造治疗精神病药物的用途 |
| US5962444A (en) * | 1998-05-29 | 1999-10-05 | Research Triangle Institute | 17β-nitro-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties |
| CA2698172C (en) | 2007-06-15 | 2014-02-18 | Cook, Kevin M. | Androstane and pregnane steroids with potent allosteric gaba receptor chloride ionophore modulating properties |
-
2008
- 2008-06-16 CA CA2698172A patent/CA2698172C/en not_active Expired - Fee Related
- 2008-06-16 ES ES08771137.0T patent/ES2589139T3/es active Active
- 2008-06-16 JP JP2010512418A patent/JP5663303B2/ja not_active Expired - Fee Related
- 2008-06-16 AU AU2008265898A patent/AU2008265898B2/en not_active Ceased
- 2008-06-16 WO PCT/US2008/067059 patent/WO2008157460A1/en not_active Ceased
- 2008-06-16 US US12/664,470 patent/US8575375B2/en not_active Expired - Fee Related
- 2008-06-16 EP EP08771137.0A patent/EP2155204B1/en not_active Not-in-force
-
2013
- 2013-08-23 US US13/974,633 patent/US9518080B2/en not_active Expired - Fee Related
-
2014
- 2014-10-01 JP JP2014202979A patent/JP5990557B2/ja not_active Expired - Fee Related
- 2014-10-01 JP JP2014202980A patent/JP5828159B2/ja not_active Expired - Fee Related
-
2016
- 2016-11-02 US US15/341,573 patent/US10087211B2/en not_active Expired - Fee Related
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