BR112021017353A2 - Forma de composto com biodisponibilidade aprimorada e formulações da mesma - Google Patents

Forma de composto com biodisponibilidade aprimorada e formulações da mesma

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Publication number
BR112021017353A2
BR112021017353A2 BR112021017353A BR112021017353A BR112021017353A2 BR 112021017353 A2 BR112021017353 A2 BR 112021017353A2 BR 112021017353 A BR112021017353 A BR 112021017353A BR 112021017353 A BR112021017353 A BR 112021017353A BR 112021017353 A2 BR112021017353 A2 BR 112021017353A2
Authority
BR
Brazil
Prior art keywords
formulations
enhanced bioavailability
compound
fluoro
preparing
Prior art date
Application number
BR112021017353A
Other languages
English (en)
Inventor
Nasir Uddin Akm
Vasant DALI Mandar
Shripad Vaze Onkar
Original Assignee
Ptc 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 Ptc Therapeutics Inc filed Critical Ptc Therapeutics Inc
Publication of BR112021017353A2 publication Critical patent/BR112021017353A2/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular 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
    • A61K9/1629—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
    • A61K9/20—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
    • A61K9/205—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
    • 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)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

forma de composto com biodisponibilidade aprimorada e formulações da mesma. a presente invenção refere-se, em geral, a formas amorfas de compostos, tendo solubilidade aquosa e taxas de dissolução aprimoradas, e dispersões sólidas amorfas e formulações farmacêuticas orais das mesmas, e um processo para preparar as mesmas. a presente descrição refere-se especificamente a formas amorfas de 5-fluoro-2-(6-fluoro-2-metil-1h-benzimidazol-1-il)-n-[4-(trifluorometil)-fenil]pirimidina-4,6-diamina e dispersões sólidas amorfas e formulações farmacêuticas orais das mesmas, e um processo para preparar as mesmas.
BR112021017353A 2019-03-11 2020-03-09 Forma de composto com biodisponibilidade aprimorada e formulações da mesma BR112021017353A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962816402P 2019-03-11 2019-03-11
PCT/US2020/021648 WO2020185648A1 (en) 2019-03-11 2020-03-09 Compound form having enhanced bioavailability and formulations thereof

Publications (1)

Publication Number Publication Date
BR112021017353A2 true BR112021017353A2 (pt) 2021-11-16

Family

ID=70166162

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021017353A BR112021017353A2 (pt) 2019-03-11 2020-03-09 Forma de composto com biodisponibilidade aprimorada e formulações da mesma

Country Status (19)

Country Link
US (1) US20220185795A1 (pt)
EP (1) EP3938368B1 (pt)
JP (1) JP2022524424A (pt)
KR (1) KR20210151061A (pt)
CN (1) CN113853374A (pt)
AU (1) AU2020235825A1 (pt)
BR (1) BR112021017353A2 (pt)
CA (1) CA3131801A1 (pt)
CL (1) CL2021002365A1 (pt)
CO (1) CO2021011836A2 (pt)
EA (1) EA202192167A1 (pt)
EC (1) ECSP21067104A (pt)
HU (1) HUE062796T2 (pt)
IL (1) IL286163A (pt)
MX (1) MX2021010906A (pt)
PE (1) PE20212270A1 (pt)
PL (1) PL3938368T3 (pt)
SG (1) SG11202109503TA (pt)
WO (1) WO2020185648A1 (pt)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3931196A4 (en) * 2019-02-28 2022-12-14 PTC Therapeutics, Inc. METHODS OF TREATMENT OF MULTIPLE MYELOMA
MX2021011688A (es) * 2019-03-27 2022-01-24 Ptc Therapeutics Inc Combinaciones utiles en un metodo para tratar sarcoma.

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2892045C (en) 2012-11-21 2022-05-31 Ptc Therapeutics, Inc. Substituted reverse pyrimidine bmi-1 inhibitors

Also Published As

Publication number Publication date
WO2020185648A1 (en) 2020-09-17
CO2021011836A2 (es) 2021-12-10
IL286163A (en) 2021-10-31
PE20212270A1 (es) 2021-11-30
ECSP21067104A (es) 2021-11-18
EA202192167A1 (ru) 2022-01-12
JP2022524424A (ja) 2022-05-02
PL3938368T3 (pl) 2023-12-27
HUE062796T2 (hu) 2023-12-28
SG11202109503TA (en) 2021-09-29
CN113853374A (zh) 2021-12-28
EP3938368B1 (en) 2023-06-07
US20220185795A1 (en) 2022-06-16
CA3131801A1 (en) 2020-09-17
CL2021002365A1 (es) 2022-04-22
AU2020235825A1 (en) 2021-09-30
KR20210151061A (ko) 2021-12-13
EP3938368A1 (en) 2022-01-19
MX2021010906A (es) 2021-10-01

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