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

Links

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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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 (18)

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 (2) CL2023000176A1 (es)
CO (1) CO2023001579A2 (es)
EC (1) ECSP23012042A (es)
IL (1) IL299829A (es)
JO (1) JOP20220351A1 (es)
MX (1) MX2023000835A (es)
PE (1) PE20231301A1 (es)
TW (1) TW202220667A (es)
WO (1) WO2022020363A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2806877B2 (en) 2012-01-23 2025-01-29 Sage Therapeutics, Inc. Neuroactive steroid formulations comprising a complex of allopregnanolone and sulfobutyl ether beta-cyclodextrin
CA2882708A1 (en) 2012-08-21 2014-02-27 Sage Therapeutics, Inc. Methods of treating epilepsy or status epilepticus
KR102396328B1 (ko) 2013-04-17 2022-05-10 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
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
WO2016082789A1 (en) 2014-11-27 2016-06-02 Sage Therapeutics, Inc. Compositions and methods for treating cns disorders
EP3504189A1 (en) 2016-08-23 2019-07-03 Sage Therapeutics, Inc. A crystalline 19-nor c3, 3-disubstituted c21-n-pyrazolyl steroid
MA51046A (fr) 2017-12-08 2021-03-17 Sage Therapeutics Inc Dérivés de 21-[4-cyano-pyrazol-1-yl]-19-nor-pregan-3. alpha-ol-20-one deutérés pour le traitement de troubles du snc
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
WO2022232504A1 (en) 2021-04-29 2022-11-03 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21 -n-pyrazolyl steroid for use in treating major depressive disorder and postpartum depression
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
IL315023A (en) 2022-02-16 2024-10-01 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
WO2026055127A2 (en) 2024-09-04 2026-03-12 Sage Therapeutics, Inc., A Wholly Owned Subsidiary Of Supernus Pharmaceuticals, Inc. Process for producing a gaba receptor modulator

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3635B1 (ar) * 2009-05-18 2020-08-27 Millennium Pharm Inc مركبات صيدلانية صلبة وطرق لانتاجها
KR102396328B1 (ko) * 2013-04-17 2022-05-10 세이지 테라퓨틱스, 인크. 19-노르 c3,3-이치환된 c21-n-피라졸릴 스테로이드 및 그의 사용 방법
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
EP3504189A1 (en) * 2016-08-23 2019-07-03 Sage Therapeutics, Inc. A crystalline 19-nor c3, 3-disubstituted c21-n-pyrazolyl steroid
EP3612186A1 (en) * 2017-04-18 2020-02-26 Marinus Pharmaceuticals, Inc. Sustained release injectable neurosteroid formulations
WO2019051264A1 (en) * 2017-09-07 2019-03-14 Sage Therapeutics, Inc. NEUROACTIVE STEROIDS AND METHODS OF USE
CA3103421A1 (en) * 2018-06-12 2019-12-19 Sage Therapeutics, Inc. A 19-nor c3,3-disubstituted c21 -n-pyrazolyl steroid and methods of use thereof

Also Published As

Publication number Publication date
AU2021312240A1 (en) 2023-02-02
CA3187178A1 (en) 2022-01-27
BR112023000990A2 (pt) 2023-03-28
US20230057130A1 (en) 2023-02-23
KR20230041049A (ko) 2023-03-23
CO2023001579A2 (es) 2023-03-07
CL2023000176A1 (es) 2023-09-15
JP2023537240A (ja) 2023-08-31
AR123018A1 (es) 2022-10-26
US20230285417A1 (en) 2023-09-14
WO2022020363A9 (en) 2023-02-09
TW202220667A (zh) 2022-06-01
EP4181884A1 (en) 2023-05-24
WO2022020363A1 (en) 2022-01-27
PE20231301A1 (es) 2023-08-24
IL299829A (en) 2023-03-01
JOP20220351A1 (ar) 2022-12-27
MX2023000835A (es) 2023-04-10
CL2024000627A1 (es) 2024-09-13
CN116367827A (zh) 2023-06-30

Similar Documents

Publication Publication Date Title
ECSP23012042A (es) Formulaciones del esteroide c21-n-pirazolilo 19-nor c3,3-disustituido y métodos de uso de este
CL2019003610A1 (es) Un esteroide 19 nor-c21-n-pirazolilo c3,3-disustituido cristalino. (divisional solicitud 201900477).
NI202000078A (es) Compuestos heteroaril tetracíclicos
ECSP22047876A (es) Derivados de pirazolilo ?tiles como agentes anticancer?genos
MX2022001828A (es) Formas cristalinas de moduladores del regulador de conductancia transmembrana de la fibrosis quistica (cftr).
ECSP21004787A (es) Inhibidores de inflamasoma nlrp3
CO2019011762A2 (es) Compuestos que inhiben la proteína mcl-1
ECSP19048759A (es) Modulador del regulador de conductancia de transmembrana de fibrosis quística, composiciones farmacéuticas, y proceso para producir el modulador
NI202000099A (es) Compuestos de purinona y su uso en el tratamiento del cáncer
UY38001A (es) Compuestos que inhiben las proteínas ras mutantes g12c
MX2019015431A (es) Compuesto cíclico tipo cumarina como inhibidor de mek y su uso.
CL2022000955A1 (es) Aminas de heteroaril-bifenilo para el tratamiento de enfermedades pd-l1
MX2024003236A (es) Composiciones y metodos para el tratamiento de trastornos metabolicos y hepaticos.
AR119174A1 (es) Inhibidores de la replicación del virus de inmunodeficiencia humana
CO2020004977A2 (es) Compuestos bicíclicos para su uso como inhibidores de la ripi quinasa
CL2018002084A1 (es) Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1.
CR20220299A (es) Derivados de becimidazol
CL2024002379A1 (es) Composición farmacéutica y que comprende derivados de difenildiazol métodos de uso
CL2025000161A1 (es) Compuestos cíclicos y métodos de utilización de estos.
UY38488A (es) Derivados de pirazol y su uso en medicina
MX2025006719A (es) Análogos de nucleótidos, composiciones y usos de los mismos
MX2021014194A (es) Derivados de piridopirimidina y composiciones farmacéuticas, para su uso para prevenir o tratar enfermedades relacionadas con pi3 cinasa, que comprenden los mismos como principio activo.
PY2003748A (es) Inhibidores de inflamasoma nlrp3