AR123018A1 - Formulaciones del esteroide c21-n-pirazolilo 19-nor c3,3-disustituido y métodos de uso de este - Google Patents
Formulaciones del esteroide c21-n-pirazolilo 19-nor c3,3-disustituido y métodos de uso de esteInfo
- Publication number
- AR123018A1 AR123018A1 ARP210102037A ARP210102037A AR123018A1 AR 123018 A1 AR123018 A1 AR 123018A1 AR P210102037 A ARP210102037 A AR P210102037A AR P210102037 A ARP210102037 A AR P210102037A AR 123018 A1 AR123018 A1 AR 123018A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- compound
- disubstituted
- steroid
- pyrazolyl
- Prior art date
Links
Classifications
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- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1611—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1682—Processes
- A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/485—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
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- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Inorganic Chemistry (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
- Anesthesiology (AREA)
Abstract
Esta invención se relaciona con un esteroide C21-pirazolilo 19-nor C3,3-disustituido de fórmula (1) y composiciones farmacéuticas de este. También se divulgan en el presente documento para preparar las composiciones farmacéuticas del esteroide C21-pirazolilo 19-nor C3,3-disustituido de fórmula (1) y métodos de uso del esteroide C21-pirazolilo 19-nor C3,3-disustituido de fórmula (1) o formas sólidas cristalinas, sales farmacéuticamente aceptables y composiciones farmacéuticamente aceptables de este. Reivindicación 111: Un proceso para hacer una composición farmacéutica que comprende lo siguiente: (a) micronizar una forma cristalina del compuesto de la fórmula (1) para obtener una forma cristalina micronizada del compuesto de la fórmula (1), caracterizado por que la forma cristalina micronizada del compuesto de la fórmula (1) tiene una distribución de tamaño de partícula que se define por un D₉₀ de aproximadamente 1 mm a aproximadamente 100 mm; (b) mezclar la forma cristalina micronizada del compuesto de la fórmula (1) con uno o más excipientes farmacéuticamente aceptables para producir una mezcla; (c) granular la mezcla para producir gránulos; (d) moler los gránulos para producir una fase intragranular; y (e) mezclar la fase intragranular con uno o más excipientes farmacéuticos extragranulares para producir la composición farmacéutica. Reivindicación 115: El proceso de cualquiera de las reivindicaciones 111 - 113, caracterizado por que, en el paso (b), el compuesto cristalino micronizado de la fórmula (1) se mezcla con un relleno, un disgregante, un lubricante y un deslizante. Reivindicación 116: El proceso de la reivindicación 113 ó 115, caracterizado por que, en el paso (b), el relleno se selecciona del grupo que consiste en un relleno frágil, un relleno dúctil y combinaciones de estos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063054070P | 2020-07-20 | 2020-07-20 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR123018A1 true AR123018A1 (es) | 2022-10-26 |
Family
ID=77265332
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP210102037A AR123018A1 (es) | 2020-07-20 | 2021-07-20 | Formulaciones del esteroide c21-n-pirazolilo 19-nor c3,3-disustituido y métodos de uso de este |
Country Status (17)
Country | Link |
---|---|
US (2) | US20230285417A1 (es) |
EP (1) | EP4181884A1 (es) |
JP (1) | JP2023537240A (es) |
KR (1) | KR20230041049A (es) |
CN (1) | CN116367827A (es) |
AR (1) | AR123018A1 (es) |
AU (1) | AU2021312240A1 (es) |
BR (1) | BR112023000990A2 (es) |
CA (1) | CA3187178A1 (es) |
CL (1) | CL2023000176A1 (es) |
CO (1) | CO2023001579A2 (es) |
EC (1) | ECSP23012042A (es) |
IL (1) | IL299829A (es) |
MX (1) | MX2023000835A (es) |
PE (1) | PE20231301A1 (es) |
TW (1) | TW202220667A (es) |
WO (1) | WO2022020363A1 (es) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN104736158A (zh) | 2012-01-23 | 2015-06-24 | 萨奇治疗股份有限公司 | 神经活性类固醇制剂和治疗中枢神经系统障碍的方法 |
RU2667010C2 (ru) | 2012-08-21 | 2018-09-13 | Сейдж Терапьютикс, Инк. | Способы лечения эпилепсии или эпилептического статуса |
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 |
PL3224269T3 (pl) | 2014-11-27 | 2020-08-24 | Sage Therapeutics, Inc. | Kompozycje i sposoby leczenia zaburzeń OUN |
CN115974955A (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 |
US20200291059A1 (en) | 2017-12-08 | 2020-09-17 | Sage Therapeutics, Inc. | Compositions and methods for treating cns disorders |
US20240245711A1 (en) | 2021-03-17 | 2024-07-25 | Sage Therapeutics, Inc. | A 19-nor c3,3-disubstituted c21-n-pyrazolyl steroid for the treatment of major depressive disorder |
WO2022232494A1 (en) | 2021-04-29 | 2022-11-03 | Sage Therapeutics, Inc. | Neuroactive steroid for use in treating major depressive disorder and postpartum depression in a lactating female |
JP2024515829A (ja) | 2021-04-29 | 2024-04-10 | セージ セラピューティクス, インコーポレイテッド | 大うつ病性障害および産後うつ病の処置における使用のための19-ノルc3,3-二置換c21-n-ピラゾリルステロイド |
AU2023220976A1 (en) | 2022-02-16 | 2024-09-05 | Sage Therapeutics, Inc. | Neuroactive steroids for treatment of cns-related disorders |
TW202341996A (zh) | 2022-02-28 | 2023-11-01 | 美商賽吉醫療公司 | 用於治療腸胃疾病或病狀之神經活性類固醇 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
KR102396328B1 (ko) * | 2013-04-17 | 2022-05-10 | 세이지 테라퓨틱스, 인크. | 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법 |
CN115974955A (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 |
IL303250A (en) * | 2017-09-07 | 2023-07-01 | Sage Therapeutics Inc | Neuroactive steroids and methods of using them |
TW202005653A (zh) * | 2018-06-12 | 2020-02-01 | 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 |
-
2021
- 2021-07-20 KR KR1020237005548A patent/KR20230041049A/ko unknown
- 2021-07-20 IL IL299829A patent/IL299829A/en unknown
- 2021-07-20 TW TW110126691A patent/TW202220667A/zh unknown
- 2021-07-20 CA CA3187178A patent/CA3187178A1/en active Pending
- 2021-07-20 PE PE2023000099A patent/PE20231301A1/es unknown
- 2021-07-20 AR ARP210102037A patent/AR123018A1/es unknown
- 2021-07-20 JP JP2023504021A patent/JP2023537240A/ja active Pending
- 2021-07-20 BR BR112023000990A patent/BR112023000990A2/pt unknown
- 2021-07-20 MX MX2023000835A patent/MX2023000835A/es unknown
- 2021-07-20 CN CN202180059412.0A patent/CN116367827A/zh active Pending
- 2021-07-20 AU AU2021312240A patent/AU2021312240A1/en active Pending
- 2021-07-20 WO PCT/US2021/042394 patent/WO2022020363A1/en active Application Filing
- 2021-07-20 US US18/006,141 patent/US20230285417A1/en active Pending
- 2021-07-20 EP EP21752441.2A patent/EP4181884A1/en active Pending
-
2022
- 2022-01-19 US US17/579,541 patent/US20230057130A1/en active Pending
-
2023
- 2023-01-19 CL CL2023000176A patent/CL2023000176A1/es unknown
- 2023-02-14 CO CONC2023/0001579A patent/CO2023001579A2/es unknown
- 2023-02-17 EC ECSENADI202312042A patent/ECSP23012042A/es unknown
Also Published As
Publication number | Publication date |
---|---|
CN116367827A (zh) | 2023-06-30 |
WO2022020363A9 (en) | 2022-03-10 |
ECSP23012042A (es) | 2023-03-31 |
MX2023000835A (es) | 2023-04-10 |
JP2023537240A (ja) | 2023-08-31 |
PE20231301A1 (es) | 2023-08-24 |
BR112023000990A2 (pt) | 2023-03-28 |
WO2022020363A1 (en) | 2022-01-27 |
CO2023001579A2 (es) | 2023-03-07 |
IL299829A (en) | 2023-03-01 |
KR20230041049A (ko) | 2023-03-23 |
US20230285417A1 (en) | 2023-09-14 |
CA3187178A1 (en) | 2022-01-27 |
TW202220667A (zh) | 2022-06-01 |
CL2023000176A1 (es) | 2023-09-15 |
EP4181884A1 (en) | 2023-05-24 |
AU2021312240A1 (en) | 2023-02-02 |
US20230057130A1 (en) | 2023-02-23 |
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