RU2766155C2 - Нейроактивные стероиды, их композиции и применения - Google Patents
Нейроактивные стероиды, их композиции и применения Download PDFInfo
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- RU2766155C2 RU2766155C2 RU2018135079A RU2018135079A RU2766155C2 RU 2766155 C2 RU2766155 C2 RU 2766155C2 RU 2018135079 A RU2018135079 A RU 2018135079A RU 2018135079 A RU2018135079 A RU 2018135079A RU 2766155 C2 RU2766155 C2 RU 2766155C2
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| KR102614507B1 (ko) | 2013-04-17 | 2023-12-19 | 세이지 테라퓨틱스, 인크. | 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법 |
| 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 |
| PL2986624T3 (pl) | 2013-04-17 | 2020-11-16 | Sage Therapeutics, Inc. | Neuroaktywne steroidy 19-NOR do stosowania w sposobach leczenia |
| WO2014169836A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| CA3199003A1 (en) | 2013-07-19 | 2015-01-22 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| HUE052308T2 (hu) | 2013-08-23 | 2021-04-28 | Sage Therapeutics Inc | Neuroaktív szteroidok, készítmények és alkalmazásuk |
| 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 |
| CN117024502A (zh) | 2014-10-16 | 2023-11-10 | 萨奇治疗股份有限公司 | 靶向cns障碍的组合物和方法 |
| EP3206493B1 (en) | 2014-10-16 | 2020-05-06 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
| EP3719029A1 (en) | 2014-11-27 | 2020-10-07 | Sage Therapeutics, Inc. | Compositions for inducing sedation |
| ES2857082T3 (es) | 2015-01-26 | 2021-09-28 | Sage Therapeutics Inc | Composiciones y métodos para el tratamiento de trastornos 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 |
| AU2017229656B2 (en) | 2016-03-08 | 2022-09-29 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| AU2017296295B2 (en) | 2016-07-11 | 2022-02-24 | Sage Therapeutics, Inc. | C7, C12, and C16 substituted neuroactive steroids and their methods of use |
| MA45599A (fr) | 2016-07-11 | 2019-05-15 | Sage Therapeutics Inc | Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation |
| KR20230079470A (ko) | 2016-08-23 | 2023-06-07 | 세이지 테라퓨틱스, 인크. | 결정질 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 |
| WO2018147791A1 (en) | 2017-02-10 | 2018-08-16 | Asarina Pharma Ab | 3-beta-hydroxy-5-alpha-pregnan-20-one for use in treatment of essential tremor |
| US20200281943A1 (en) * | 2017-09-07 | 2020-09-10 | Sage Therapeutics, Inc. | Neuroactive steroids and their methods of use |
| WO2019075362A1 (en) * | 2017-10-12 | 2019-04-18 | Sage Therapeutics, Inc. | METHOD OF TREATING CENTRAL NERVOUS SYSTEM DISORDERS WITH NEUROSTEROIDS AND GABAERGIC COMPOUNDS |
| US20190160078A1 (en) * | 2017-11-10 | 2019-05-30 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in treating genetic epileptic disorders |
| KR20200096596A (ko) | 2017-12-08 | 2020-08-12 | 세이지 테라퓨틱스, 인크. | Cns 장애의 치료를 위한 중수소화 21 -[4-시아노-피라졸-1 -일]-19-노르-프레간-3. 알파-올-20-온 유도체 |
| AU2019217320B2 (en) * | 2018-02-11 | 2023-12-21 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Steroid derivative regulators, method for preparing the same, and uses thereof |
| CN117959309A (zh) * | 2018-06-12 | 2024-05-03 | 萨奇治疗股份有限公司 | 19-去甲基c3,3-二取代的c21-n-吡唑基类固醇及其使用方法 |
| WO2020097045A1 (en) * | 2018-11-05 | 2020-05-14 | Ovid Therapeutics Inc. | Use of gaboxadol, ganaxolone and allopregnanolone to treat movement disorders |
| 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 |
| US11266662B2 (en) | 2018-12-07 | 2022-03-08 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in prophylaxis and treatment of postpartum depression |
| EP3911331A4 (en) * | 2019-01-14 | 2023-01-18 | Beijing Xuanyi Pharmasciences Co., Ltd. | TETRAZOLONE SUBSTITUTED STEROIDS AND USE THEREOF |
| US11497754B2 (en) | 2019-02-05 | 2022-11-15 | Washington University | Neurosteroids and enantiomers thereof for the prevention and treatment of neurodegenerative conditions |
| US20220125803A1 (en) * | 2019-03-04 | 2022-04-28 | Praxis Precision Medicines, Inc. | Methods for the treatment of perimenopause and menopause |
| MX2021013695A (es) | 2019-05-10 | 2022-01-26 | Brii Biosciences Inc | Composición farmacéutica que contiene brexanolona, ganaxolona y zuranolona y usos de esta. |
| WO2020243488A1 (en) | 2019-05-31 | 2020-12-03 | Sage Therapeutics, Inc. | Neuroactive steroids and compositions thereof |
| EP4009982A4 (en) | 2019-08-05 | 2023-08-09 | Marinus Pharmaceuticals, Inc. | GANAXOLONE FOR USE IN TREATMENT OF STATUS EPILEPTICUS |
| US10857163B1 (en) | 2019-09-30 | 2020-12-08 | Athenen Therapeutics, Inc. | Compositions that preferentially potentiate subtypes of GABAA receptors and methods of use thereof |
| MX2022006014A (es) * | 2019-12-06 | 2022-06-22 | Marinus Pharmaceuticals Inc | Ganaxolona para uso en el tratamiento del complejo de esclerosis tuberosa. |
| BR112022013585A2 (pt) * | 2020-01-12 | 2022-09-13 | Brii Biosciences Inc | Esteroides neuroativos e composição farmacêutica que contém os mesmos |
| EP4125921A1 (en) | 2020-03-25 | 2023-02-08 | Sage Therapeutics, Inc. | Use of agents for treatment of respiratory conditions |
| WO2022125408A1 (en) * | 2020-12-07 | 2022-06-16 | Marinus Pharmaceuticals, Inc | Use of ganaxolone in treating an epilepsy disorder |
| CN112516086B (zh) * | 2020-12-08 | 2022-05-20 | 武汉久安药物研究院有限公司 | 注射用布瑞诺龙脂肪乳及其制备方法 |
| JP2024507638A (ja) * | 2021-01-28 | 2024-02-21 | セージ セラピューティクス, インコーポレイテッド | 性機能障害処置のための神経刺激性ステロイドの使用 |
| CA3216542A1 (en) * | 2021-04-12 | 2022-10-20 | Sage Therapeutics, Inc. | Treatment of essential tremor |
| US11969434B1 (en) | 2022-08-29 | 2024-04-30 | Lipocine Inc. | Oral allopregnanolone compositions and methods of use |
| US12208103B1 (en) | 2021-05-07 | 2025-01-28 | Lipocine Inc. | Compositions and methods for treating CNS disorders |
| US11337987B1 (en) * | 2021-05-07 | 2022-05-24 | Lipocine Inc. | Compositions and methods for treating central nervous system disorders |
| KR20240037975A (ko) | 2021-07-28 | 2024-03-22 | 세이지 테라퓨틱스, 인크. | 신경활성 스테로이드의 결정질 형태 |
| WO2023146579A1 (en) * | 2022-01-27 | 2023-08-03 | Belnap Pharmaceuticals, Llc | Methods of treatment using oxytocin |
| WO2023164385A1 (en) * | 2022-02-28 | 2023-08-31 | Sage Therapeutics, Inc. | Neuroactive steroids for treatment of gastrointestinal diseases or conditions |
| WO2023211856A1 (en) * | 2022-04-26 | 2023-11-02 | Praxis Precision Medicines, Inc. | Methods for the treatment of neurological disorders |
| US12186327B2 (en) | 2022-08-29 | 2025-01-07 | Lipocine Inc. | Oral allopregnanolone compositions and methods of use |
| WO2024059608A1 (en) * | 2022-09-15 | 2024-03-21 | Sage Therapeutics, Inc. | Deuterated neuroactive steroids |
| CN115957332B (zh) * | 2022-11-01 | 2023-10-10 | 北京华睿鼎信科技有限公司 | 透明质酸酶稳定的布瑞诺龙纳米晶及其制备方法与应用 |
| CN120917034A (zh) * | 2023-05-11 | 2025-11-07 | 上海枢境生物科技有限公司 | 甾体类化合物、制备方法及其用途 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2445973C2 (ru) * | 2006-05-22 | 2012-03-27 | Ванда Фармасьютиклз, Инк. | Способ лечения глубокой депрессии у человека |
| WO2013043985A1 (en) * | 2011-09-23 | 2013-03-28 | The Regents Of The University Of California | Edible oils to enhance delivery of orally administered steroids |
| RU2488390C2 (ru) * | 2008-12-29 | 2013-07-27 | Тартуский Университет | Ингибиторы аргиназы для лечения депрессии |
| WO2014085668A1 (en) * | 2012-11-30 | 2014-06-05 | The Regents Of The University Of California | Anticonvulsant activity of steroids |
Family Cites Families (134)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3117142A (en) | 1961-03-01 | 1964-01-07 | Roussel Uclaf | Novel preparation of estradiol and estrone |
| US3169134A (en) | 1963-03-21 | 1965-02-09 | Searle & Co | 2, 3-oxygenated-17alpha-methyl-5alpha-androstan-17beta-ols |
| BE754111A (fr) | 1969-07-29 | 1971-01-29 | Upjohn Co | Nouveaux 7alpha- et 7beta-methyl-3alpha,5alpha- cycloandrostanes et composes analogues 19-nor et leur procede de preparation |
| US3943124A (en) | 1970-12-17 | 1976-03-09 | Gordon Hanley Phillipps | Chemical compounds |
| GB1430942A (en) | 1972-05-05 | 1976-04-07 | Glaxo Lab Ltd | 21-substituted 3alpha-hydroxy pregnanes |
| US3983111A (en) | 1972-05-05 | 1976-09-28 | Glaxo Laboratories Limited | Steroidal anaesthetics of the pregnane and 19-norpregnane series |
| US3865939A (en) | 1973-02-23 | 1975-02-11 | Procter & Gamble | Edible oils having hypocholesterolemic properties |
| US4071625A (en) | 1974-05-13 | 1978-01-31 | Richardson-Merrell Inc. | 19-Oxygenated-5α-androstanes for the enhancement of libido |
| GB1570394A (en) | 1976-01-06 | 1980-07-02 | Glaxo Lab Ltd | 11-acyloxy-3-hydroxy steroids |
| US4192871A (en) | 1976-01-06 | 1980-03-11 | Glaxo Laboratories Limited | Chemical compounds |
| GB1581234A (en) | 1976-04-05 | 1980-12-10 | Glaxo Operations Ltd | 11a - amino - 3a - hydroxysteroids |
| SE8600632D0 (sv) | 1986-02-13 | 1986-02-13 | Kabivitrum Ab | Novel pharmaceutical composition |
| US5120723A (en) * | 1987-08-25 | 1992-06-09 | University Of Southern California | Method, compositions, and compounds for modulating brain excitability |
| 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 |
| US5319115A (en) | 1987-08-25 | 1994-06-07 | Cocensys Inc. | Method for making 3α-hydroxy, 3β-substituted-pregnanes |
| US5719197A (en) | 1988-03-04 | 1998-02-17 | Noven Pharmaceuticals, Inc. | Compositions and methods for topical administration of pharmaceutically active agents |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| WO1993005786A1 (en) | 1991-09-13 | 1993-04-01 | Cocensys, Inc. | Novel gabaa receptor with steroid binding sites |
| EP0701444B1 (en) | 1993-05-24 | 2010-04-07 | Purdue Pharma Ltd. | Methods and compositions for inducing sleep |
| EP0656365B1 (en) | 1993-12-02 | 1997-04-09 | Akzo Nobel N.V. | Substituted 2beta-morpholinoandrostane derivatives |
| 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 |
| BR9506779A (pt) | 1994-02-14 | 1997-10-14 | Cocensys Inc | Composto composição farmacéutica método para modular o complexo ionóforo receptor gaba-cloreto em um paciente animal pela ligação ao sitio neuroesteróide no dito complexo método para tratar ou evitar estresse ou ansiedade em um paciente animal método para aliviar ou evitar isônia pms ou pnd em um paciente animal método para tratar ou evitar perturbacões na disposicão de ánimo em um paciente animal e método para induzir anestesia em um paciente animal |
| CA2186371A1 (en) | 1994-03-25 | 1995-10-05 | Robert T. Foster | Enhancement of the efficacy of dihydropyridines by deuteration |
| JP2002500616A (ja) | 1994-07-21 | 2002-01-08 | ファルマシア・アンド・アップジョン・カンパニー | 神経学的に活性なアミノステロイド |
| BR9509764A (pt) | 1994-11-23 | 1998-07-07 | Cocensys Inc | Série androstano e pregnano para modulação alostérica de receptor de gaba |
| US6780853B1 (en) | 1995-06-06 | 2004-08-24 | Euro-Celtique S.A. | Neuroactive steroids of the androstane and pregnane series |
| PL185523B1 (pl) | 1995-06-06 | 2003-05-30 | Cocensys Inc | Neuroaktywne steroidy z grupy pochodnych androstanu i pregnanu oraz kompozycja farmaceutyczna |
| JP4313435B2 (ja) | 1995-07-24 | 2009-08-12 | トラスティーズ オブ ボストン ユニバーシティー | プレグネノロンサルフェート誘導体によるnmdaレセプター活性の抑制 |
| WO1998005337A1 (en) | 1996-08-01 | 1998-02-12 | Cocensys, Inc. | Use of gaba and nmda receptor ligands for the treatment of migraine headache |
| US7630757B2 (en) | 1997-01-06 | 2009-12-08 | Flint Hills Scientific Llc | System for the prediction, rapid detection, warning, prevention, or control of changes in activity states in the brain of a subject |
| US6245757B1 (en) | 1997-10-03 | 2001-06-12 | Research Corporation Technologies, Inc. | Use of progestins to treat ischemic event |
| WO1999045931A1 (en) | 1998-03-11 | 1999-09-16 | Baeckstroem Torbjoern | Epiallopregnanolone in the treatment of cns disorders |
| US20020198174A1 (en) | 2001-05-07 | 2002-12-26 | Allergan Sales, Inc. | Disinfecting and solubilizing steroid compositions |
| US6376531B1 (en) | 1998-11-13 | 2002-04-23 | Rupert Charles Bell | Method of treatment using deuterium compounds |
| US20030236236A1 (en) | 1999-06-30 | 2003-12-25 | Feng-Jing Chen | Pharmaceutical compositions and dosage forms for administration of hydrophobic drugs |
| PT1104760E (pt) | 1999-12-03 | 2003-06-30 | Pfizer Prod Inc | Compostos de sulfamoil-heteroarilpirazole como agentes analgesicos e anti-inflamatorios |
| US6613308B2 (en) | 2000-09-19 | 2003-09-02 | Advanced Inhalation Research, Inc. | Pulmonary delivery in treating disorders of the central nervous system |
| US20020072509A1 (en) | 2000-10-11 | 2002-06-13 | Stein Donald Gerald | Methods for the treatment of a traumatic central nervous system injury |
| GR1003861B (el) | 2000-12-29 | 2002-04-11 | Νεα νευροστεροειδη που αλληλεπιδρουν με τον υποδοχεα gabaa. | |
| WO2002064804A2 (en) | 2001-02-13 | 2002-08-22 | University Of Florida | A bi-directional dual promoter complex with enhanced promoter activity for transgene expression in eukaryotes |
| US20030055026A1 (en) | 2001-04-17 | 2003-03-20 | Dey L.P. | Formoterol/steroid bronchodilating compositions and methods of use thereof |
| EP1392260A2 (en) | 2001-05-24 | 2004-03-03 | Alexza Molecular Delivery Corporation | Delivery of benzodiazepines through an inhalation route |
| ES2316571T3 (es) | 2001-05-24 | 2009-04-16 | Alexza Pharmaceuticals, Inc. | Administracion de alprazolam, estazolam, midazolam o triazolam a traves de una via inhalatoria. |
| US7090830B2 (en) | 2001-05-24 | 2006-08-15 | Alexza Pharmaceuticals, Inc. | Drug condensation aerosols and kits |
| JP2003063965A (ja) | 2001-06-13 | 2003-03-05 | Otsuka Pharmaceut Factory Inc | 注射用シロスタゾール水性製剤 |
| CA2496867A1 (en) | 2002-08-28 | 2004-03-11 | Hollis-Eden Pharmaceuticals, Inc. | Therapeutic treatment methods |
| US9339508B2 (en) | 2003-01-17 | 2016-05-17 | Mapreg | Use of 3-methoxy-pregnenolone for the preparation of a drug for treating a traumatic brain injury |
| WO2005000869A1 (en) | 2003-05-29 | 2005-01-06 | Washington University | Neuroactive 13,24-cyclo-18,21-dinorcholanes and structurally-related pentacyclic steroids |
| US7816074B2 (en) | 2003-07-31 | 2010-10-19 | The Research Foundation Of State University Of New York | α4 β2 δGABA-A receptors as a strategy for PMS and alcoholism |
| GB0321607D0 (en) | 2003-09-15 | 2003-10-15 | Vectura Ltd | Manufacture of pharmaceutical compositions |
| US20070020299A1 (en) | 2003-12-31 | 2007-01-25 | Pipkin James D | Inhalant formulation containing sulfoalkyl ether cyclodextrin and corticosteroid |
| DE602005026225D1 (de) | 2004-03-12 | 2011-03-24 | Cipla Ltd | Sterilisationsprozess für Steroide |
| WO2005105822A2 (en) | 2004-04-23 | 2005-11-10 | Euro-Celtique S.A. | 3-alpha-hydroxy 21-n- heteroaryl-pregnane derivatives for modulation of brain excitability and a process for the production thereof |
| WO2006034196A1 (en) | 2004-09-17 | 2006-03-30 | Lifelike Biomatic Inc. | Compositions for enhancing memory and methods therefor |
| US8604011B2 (en) | 2004-09-27 | 2013-12-10 | The Regents Of The University Of California | Therapy for treatment of chronic degenerative brain diseases and nervous system injury |
| CA2582231A1 (en) | 2004-09-29 | 2006-10-19 | Hollis-Eden Pharmaceuticals, Inc. | Steroid analogs and uses |
| MX2007009915A (es) | 2005-02-15 | 2007-11-06 | Elan Pharma Int Ltd | Formulaciones en aerosol e inyectables de benzodiazepina nanoparticulada. |
| PL1868614T3 (pl) | 2005-03-24 | 2013-01-31 | Univ Emory | Schemat dawkowania do leczenia urazowego uszkodzenia mózgu progesteronem |
| EP1868593A2 (en) | 2005-04-07 | 2007-12-26 | Hythiam, Inc. | Improved methods of and compositions for the prevention of anxiety, substance abuse, and dependence |
| US20110319386A1 (en) | 2005-08-26 | 2011-12-29 | Braincells Inc. | Neurogenesis by muscarinic receptor modulation |
| EP1959966B1 (en) | 2005-11-28 | 2020-06-03 | Marinus Pharmaceuticals, Inc. | Ganaxolone formulations and methods for the making and use thereof |
| US20070287931A1 (en) | 2006-02-14 | 2007-12-13 | Dilorenzo Daniel J | Methods and systems for administering an appropriate pharmacological treatment to a patient for managing epilepsy and other neurological disorders |
| US7998971B2 (en) | 2006-09-08 | 2011-08-16 | Braincells Inc. | Combinations containing a 4-acylaminopyridine derivative |
| US20090239942A1 (en) | 2006-09-15 | 2009-09-24 | Cloyd James C | Topiramate Compositions and Methods of Making and Using the Same |
| US20090074677A1 (en) | 2007-01-08 | 2009-03-19 | Duke University | Neuroactive steroid compositions and methods of use therefor |
| US20090203658A1 (en) | 2007-01-08 | 2009-08-13 | Duke University | Neuroactive steroid compositions and methods of use therefor |
| US7813811B2 (en) | 2007-02-08 | 2010-10-12 | Neuropace, Inc. | Refillable reservoir lead systems |
| JP2010523708A (ja) | 2007-04-11 | 2010-07-15 | バイオマリン ファーマシューティカル インコーポレイテッド | テトラヒドロビオプテリンを投与する方法、関連する組成物および測定方法 |
| US8530463B2 (en) | 2007-05-07 | 2013-09-10 | Hale Biopharma Ventures Llc | Multimodal particulate formulations |
| JP2010530371A (ja) | 2007-06-11 | 2010-09-09 | ユニバーシティ オブ サザン カリフォルニア | 神経学的機能を増強するための作用物質、組成物および方法 |
| US8575375B2 (en) | 2007-06-15 | 2013-11-05 | Research Triangle Institute | Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties |
| GB0711948D0 (en) | 2007-06-20 | 2007-08-01 | Bionature E A Ltd | Neurosteriod compounds |
| EP2175886A1 (en) | 2007-06-28 | 2010-04-21 | CNSBio Pty Ltd | Combination methods and compositions for treatment of neuropathic pain |
| US20100297181A1 (en) | 2007-12-26 | 2010-11-25 | Eisai R&D Management Co., Ltd. | AMPA Receptor Antagonists for Epilepsy, Mental Disorders or Deficits in Sensory Organ |
| MX2010006025A (es) | 2008-01-03 | 2010-06-30 | Biomarin Pharm Inc | Analogo de pterina para tratar afeccion sensible a bh4. |
| US20090198145A1 (en) | 2008-02-06 | 2009-08-06 | Chow Harrison | Compositions, methods, and systems for rapid induction and maintenance of continuous rem sleep |
| US8729070B2 (en) | 2008-02-20 | 2014-05-20 | Targia Pharmaceuticals | CNS pharmaceutical compositions and methods of use |
| WO2010063030A2 (en) | 2008-11-30 | 2010-06-03 | Feigelson, Daniel | Dermal application of vasoconstrictors |
| CZ2008434A3 (cs) | 2008-07-10 | 2009-12-09 | Ústav organické chemie a biochemie Akademie ved CR, v. v. i. | Pregnanové anionické slouceniny, zpusob jejich výroby a jejich použití |
| EP3135672B9 (en) | 2008-10-10 | 2020-05-20 | VM Discovery, Inc. | Compositions and methods for treating alcohol use disorders, pain and other diseases |
| WO2010088409A2 (en) | 2009-01-30 | 2010-08-05 | Emory University | Methods of neuroprotection using neuroprotective steroids and a vitamin d |
| US20120142645A1 (en) | 2009-03-17 | 2012-06-07 | Marx Christine E | Neuroactive steroid compositions and methods of use for lowering cholesterol |
| CZ303037B6 (cs) * | 2009-05-28 | 2012-03-07 | Ústav organické chemie a biochemie, Akademie ved CR, v. v. i. | Deriváty pregnanolonu substituované v poloze 3alfa, zpusob jejich výroby a jejich použití |
| WO2011079047A1 (en) * | 2009-12-23 | 2011-06-30 | Drugtech Corporation | Methods for reducing the occurrence of preterm delivery and other pregnancy-related conditions |
| DK2525798T3 (da) | 2010-01-21 | 2017-11-20 | Drawbridge Pharmaceuticals Pty Ltd | Anæstetisk formulering |
| DK2635333T3 (en) | 2010-11-03 | 2014-12-08 | Sanofi Aventis Deutschland | Needle containing drug |
| WO2012075286A2 (en) | 2010-12-01 | 2012-06-07 | The Regents Of The University Of California | Intrapulmonary benzodiazepine for the treatment and prevention of seizures |
| CZ201181A3 (cs) | 2011-02-15 | 2012-09-12 | Ústav organické chemie a biochemie Akademie ved CR, v.v.i. | Deriváty pregnanolonu substituované v poloze 3alfa kationickou skupinou, zpusob jejich výroby, jejich použití a prostredek je obsahující |
| WO2012116290A2 (en) | 2011-02-25 | 2012-08-30 | Washington University | Neuroactive 17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same |
| FR2973031B1 (fr) | 2011-03-23 | 2013-11-29 | Univ Strasbourg | Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique |
| US9084797B2 (en) | 2011-05-23 | 2015-07-21 | Besins Healthcare Luxembourg Sarl | Progesterone treatment for improving sleep quality |
| EP2727473A4 (en) | 2011-06-28 | 2015-05-06 | Vivozon Inc | COMBINATION OF EFFICIENT SUBSTANCES WITH SYNERGISTIC EFFECTS OF MULTIPLE TARGETING AND USE THEREOF |
| CA2843436A1 (en) * | 2011-07-29 | 2013-02-07 | The Regents Of The University Of California | Novel 17.beta.-heteroaryl-substituted steroids as modulators of gaba a receptors |
| AU2012304412A1 (en) | 2011-09-08 | 2014-03-27 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| PT2766380T (pt) | 2011-10-14 | 2019-07-29 | Sage Therapeutics Inc | Compostos de 19-nor pregnano 3,3-dissubstituídos, composições e seus usos |
| US9125926B2 (en) | 2011-11-29 | 2015-09-08 | Amino Up Chemical Co. Ltd | Vicenin 2 and analogues thereof for use as an antispasmodic and/or prokinetic agent |
| RS59734B1 (sr) | 2012-01-23 | 2020-02-28 | Sage Therapeutics Inc | Formulacije neuroaktivnog steroida koje uključuju kompleks alopregnanolona i sulfobutil etar beta-ciklodekstrina |
| WO2013188792A2 (en) | 2012-06-15 | 2013-12-19 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| 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 |
| EP2887944B1 (en) | 2012-08-21 | 2021-10-06 | Sage Therapeutics, Inc. | Allopregnanolone for treating refractory status epilepticus |
| WO2014058736A1 (en) | 2012-10-08 | 2014-04-17 | Washington University | Neuroactive 19-alkoxy-17(20)-z-vinylcyano-substituted steroids, prodrugs thereof, and methods of treatment using same |
| US9757391B2 (en) | 2012-11-09 | 2017-09-12 | Goodchild Investments Pty Ltd | Neuroactive steroids and their use to facilitate neuroprotection |
| KR102400891B1 (ko) | 2012-12-18 | 2022-05-20 | 워싱톤 유니버시티 | 신경활성 19-알콕시-17-치환된 스테로이드, 그의 전구약물, 및 그를 사용한 치료 방법 |
| WO2014108808A2 (en) | 2013-01-09 | 2014-07-17 | Henry James Lorne | Pharmaceutical formulations for the treatment and prevention of trauma-induced neuropathology and neurodegeneration |
| WO2014169836A1 (en) | 2013-04-17 | 2014-10-23 | Sage Therapeutics, Inc. | 19-nor neuroactive steroids and methods of use thereof |
| KR102614507B1 (ko) | 2013-04-17 | 2023-12-19 | 세이지 테라퓨틱스, 인크. | 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법 |
| PL2986624T3 (pl) | 2013-04-17 | 2020-11-16 | Sage Therapeutics, Inc. | Neuroaktywne steroidy 19-NOR do stosowania w sposobach leczenia |
| 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 |
| CA3199003A1 (en) | 2013-07-19 | 2015-01-22 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| HUE052308T2 (hu) | 2013-08-23 | 2021-04-28 | Sage Therapeutics Inc | Neuroaktív szteroidok, készítmények és alkalmazásuk |
| ES2927007T3 (es) * | 2014-05-29 | 2022-10-31 | Sage Therapeutics Inc | Esteroides neuroactivos, composiciones y usos de los mismos |
| 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 |
| EP4059522A1 (en) | 2015-02-06 | 2022-09-21 | Marinus Pharmaceuticals, Inc. | Intravenous ganaxolone formulations and their use in treating status epilepticus and other seizure disorders |
| GB2541015A (en) | 2015-08-06 | 2017-02-08 | Ge Oil & Gas Uk Ltd | Subsea flying lead |
| AU2016338916B2 (en) | 2015-10-14 | 2021-12-23 | The Regents Of The University Of California | Enhancing beta cell replication and/or survival |
| AU2017229656B2 (en) | 2016-03-08 | 2022-09-29 | Sage Therapeutics, Inc. | Neuroactive steroids, compositions, and uses thereof |
| MX2019001669A (es) | 2016-08-11 | 2019-09-27 | Ovid Therapeutics Inc | Metodos y composiciones para el tratamiento de trastornos epilepticos. |
| US20180050005A1 (en) | 2016-08-16 | 2018-02-22 | Janssen Pharmaceutica Nv | Concentrated Solution of 17-Hydroxydocosahexaenoic Acid |
| US20180050107A1 (en) | 2016-08-16 | 2018-02-22 | Janssen Pharmaceutica Nv | Neurosteroid compositions and methods of use thereof |
| JP7378781B2 (ja) | 2016-09-07 | 2023-11-14 | グリア エルエルシー | 脳神経の薬理学的な経皮活性化による神経変性障害に関連する症状の治療 |
| US10391105B2 (en) | 2016-09-09 | 2019-08-27 | Marinus Pharmaceuticals Inc. | Methods of treating certain depressive disorders and delirium tremens |
| WO2018169798A1 (en) | 2017-03-11 | 2018-09-20 | The Regents Of The University Of California | Mitigation of cns disorders by combination therapy using neurosteroids, and ampa blockers |
| KR20190137839A (ko) | 2017-04-18 | 2019-12-11 | 마리누스 파마슈티컬스 인코포레이티드 | 지속 방출 주사용 뉴로스테로이드 제제 |
| US20180338959A1 (en) | 2017-05-24 | 2018-11-29 | Ovid Therapeutics Inc. | Treatment of depressive disorders |
| US11752115B2 (en) | 2017-06-21 | 2023-09-12 | The Board Of Trustees Of The University Of Illinois | PPAR-alpha agonist treatment of neuropsychiatric disorders |
| US11992495B2 (en) | 2017-06-23 | 2024-05-28 | The Regents Of The University Of California | Enhancing GABA's ability to modulate immune responses |
| EP3641779B1 (en) | 2017-06-23 | 2024-02-28 | The Board of Trustees of the University of Illinois | Treatment of neuropsychiatric disorders with neurosteroids and analogues thereof |
| US20190160078A1 (en) | 2017-11-10 | 2019-05-30 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in treating genetic epileptic disorders |
| CN112823164A (zh) | 2018-05-04 | 2021-05-18 | 阿克罗斯制药公司 | 神经甾体衍生物和其用途 |
| US11311529B2 (en) | 2018-11-08 | 2022-04-26 | Varsona Therapeutics, Inc. | Topical formulations of 5-α-reductase inhibitors and uses thereof |
| CN113395962A (zh) | 2018-11-21 | 2021-09-14 | Certego治疗公司 | 加波沙朵用于降低自杀风险和快速缓解抑郁症 |
| US11266662B2 (en) | 2018-12-07 | 2022-03-08 | Marinus Pharmaceuticals, Inc. | Ganaxolone for use in prophylaxis and treatment of postpartum depression |
| AU2019396139A1 (en) | 2018-12-14 | 2021-07-15 | Acerus Biopharma Inc. | Active ester derivatives of testosterone, compositions and uses thereof |
-
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Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2445973C2 (ru) * | 2006-05-22 | 2012-03-27 | Ванда Фармасьютиклз, Инк. | Способ лечения глубокой депрессии у человека |
| RU2488390C2 (ru) * | 2008-12-29 | 2013-07-27 | Тартуский Университет | Ингибиторы аргиназы для лечения депрессии |
| WO2013043985A1 (en) * | 2011-09-23 | 2013-03-28 | The Regents Of The University Of California | Edible oils to enhance delivery of orally administered steroids |
| WO2014085668A1 (en) * | 2012-11-30 | 2014-06-05 | The Regents Of The University Of California | Anticonvulsant activity of steroids |
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