ECSP23012042A - 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 este

Info

Publication number
ECSP23012042A
ECSP23012042A ECSENADI202312042A ECDI202312042A ECSP23012042A EC SP23012042 A ECSP23012042 A EC SP23012042A EC SENADI202312042 A ECSENADI202312042 A EC SENADI202312042A EC DI202312042 A ECDI202312042 A EC DI202312042A EC SP23012042 A ECSP23012042 A EC SP23012042A
Authority
EC
Ecuador
Prior art keywords
disubstituted
steroid
pyrazolyl
methods
formulations
Prior art date
Application number
ECSENADI202312042A
Other languages
English (en)
Inventor
Raj Jain
Padma Narayan
Jianing Meng
Carolyn Wilkerson
Todd Stutzman
Paul Watson
Bret Berner
Xiaoxia Chen
Original Assignee
Sage Therapeutics Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Sage Therapeutics Inc filed Critical Sage Therapeutics Inc
Publication of ECSP23012042A publication Critical patent/ECSP23012042A/es

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Classifications

    • 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
    • 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
    • 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
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (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 refiere a un esteroide C21-pirazolilo 19-nor C3,3-disustituido de fórmula (I) y composiciones farmacéuticas de este. También se divulgan en el presente documento métodos para preparar las composiciones farmacéuticas del esteroide C21-pirazolilo 19-nor C3,3-disustituido de fórmula (I) y métodos de uso del esteroide C21-pirazolilo 19-nor C3,3-disustituido de fórmula (I) o formas sólidas cristalinas, sales farmacéuticamente aceptables y composiciones farmacéuticamente aceptables de este.
ECSENADI202312042A 2020-07-20 2023-02-17 Formulaciones del esteroide c21-n-pirazolilo 19-nor c3,3-disustituido y métodos de uso de este ECSP23012042A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US202063054070P 2020-07-20 2020-07-20

Publications (1)

Publication Number Publication Date
ECSP23012042A true ECSP23012042A (es) 2023-03-31

Family

ID=77265332

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSENADI202312042A ECSP23012042A (es) 2020-07-20 2023-02-17 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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ627781A (en) 2012-01-23 2016-10-28 Sage Therapeutics Inc Neuroactive steroid formulations and methods of treating cns disorders
IL275725B (en) 2012-08-21 2022-08-01 Sage Therapeutics Inc Treatment methods for epilepsy and status epilepticus
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
EP3719029A1 (en) 2014-11-27 2020-10-07 Sage Therapeutics, Inc. Compositions for inducing sedation
AR109393A1 (es) 2016-08-23 2018-11-28 Sage Therapeutics Inc Un esteroide 19-nor-c21-pirazolilo c3,3-disustituido cristalino
JP2021505608A (ja) 2017-12-08 2021-02-18 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ジュウテリウム化された２１−［４−シアノ−ピラゾール−１−イル］−１９−ノル−プレガン−３．α−オール−２０−オン誘導体
JP2024510436A (ja) 2021-03-17 2024-03-07 セージ セラピューティクス， インコーポレイテッド 大うつ病性障害の処置のための１９－ノルｃ３，３－２置換ｃ２１－ｎ－ピラゾリルステロイド
BR112023022264A2 (pt) 2021-04-29 2024-01-23 Sage Therapeutics Inc Esteroide c21-n-pirazolil 19-nor c3,3-dissubstituído e métodos de uso do mesmo
EP4329769A1 (en) 2021-04-29 2024-03-06 Sage Therapeutics, Inc. Neuroactive steroid for use in treating major depressive disorder and postpartum depression in a lactating female
AU2023220976A1 (en) 2022-02-16 2024-09-05 Sage Therapeutics, Inc. Neuroactive steroids for treatment of cns-related disorders
WO2023163879A1 (en) 2022-02-28 2023-08-31 Sage Therapeutics, Inc. Neuroactive steroids for treatment of gastrointestinal diseases or conditions

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
HUE041369T2 (hu) * 2013-04-17 2019-05-28 Sage Therapeutics Inc 19-nor C3,3-diszubsztituált C21-N-pirazolil-szteroidok és eljárás ezek alkalmazására
AR109393A1 (es) 2016-08-23 2018-11-28 Sage Therapeutics Inc Un esteroide 19-nor-c21-pirazolilo c3,3-disustituido cristalino
WO2019051264A1 (en) * 2017-09-07 2019-03-14 Sage Therapeutics, Inc. NEUROACTIVE STEROIDS AND METHODS OF USE
KR20210021005A (ko) * 2018-06-12 2021-02-24 세이지 테라퓨틱스, 인크. 19-nor c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법

Also Published As

Publication number Publication date
PE20231301A1 (es) 2023-08-24
CO2023001579A2 (es) 2023-03-07
WO2022020363A1 (en) 2022-01-27
IL299829A (en) 2023-03-01
KR20230041049A (ko) 2023-03-23
MX2023000835A (es) 2023-04-10
JP2023537240A (ja) 2023-08-31
US20230285417A1 (en) 2023-09-14
CN116367827A (zh) 2023-06-30
BR112023000990A2 (pt) 2023-03-28
US20230057130A1 (en) 2023-02-23
EP4181884A1 (en) 2023-05-24
WO2022020363A9 (en) 2022-03-10
AU2021312240A1 (en) 2023-02-02
CA3187178A1 (en) 2022-01-27
TW202220667A (zh) 2022-06-01
CL2023000176A1 (es) 2023-09-15
AR123018A1 (es) 2022-10-26

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