BR112022012258A2 - Sal cristalino de bromidreto de um inibidor de ezh2, sua preparação e composição farmacêutica útil para o tratamento de câncer - Google Patents

Sal cristalino de bromidreto de um inibidor de ezh2, sua preparação e composição farmacêutica útil para o tratamento de câncer

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Publication number
BR112022012258A2
BR112022012258A2 BR112022012258A BR112022012258A BR112022012258A2 BR 112022012258 A2 BR112022012258 A2 BR 112022012258A2 BR 112022012258 A BR112022012258 A BR 112022012258A BR 112022012258 A BR112022012258 A BR 112022012258A BR 112022012258 A2 BR112022012258 A2 BR 112022012258A2
Authority
BR
Brazil
Prior art keywords
cancer
preparation
treatment
crystalline
hromydride
Prior art date
Application number
BR112022012258A
Other languages
English (en)
Inventor
Jacobus Verwijs Marinus
Jon Am Ende David
Richard Anderson Stephen
Paul George Beevers Andrew
Kenneth Breault Mark
Richard Tudhope Stephen
Ross Wolstenhulme Jamie
Original Assignee
Epizyme 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 Epizyme Inc filed Critical Epizyme Inc
Publication of BR112022012258A2 publication Critical patent/BR112022012258A2/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • 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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SAL CRISTALINO DE BROMIDRETO DE UM INIBIDOR DE EZH2, SUA PREPARAÇÃO E COMPOSIÇÃO FARMACÊUTICA ÚTIL PARA O TRATAMENTO DE CÂNCER. O pedido se refere a uma forma cristalina de bromidreto de N-((4,6-dimetil-2-oxo-1,2-di-hidropiridin-3-il)metil)-5-(etil(tetra-hidro-2H-piran-4-il)amino)-4-metil-4?-(morfolinometil)-[1,1?-bifenil]-3-carboxamida (Tazemetostat), aos métodos para a sua preparação e às composições farmacêuticas que a compreendem. O composto é conhecido por ser um inibidor eficaz de EZH2 (Intensificador de Zeste homólogo 2) útil para o tratamento de câncer.
BR112022012258A 2019-12-20 2020-12-18 Sal cristalino de bromidreto de um inibidor de ezh2, sua preparação e composição farmacêutica útil para o tratamento de câncer BR112022012258A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962951842P 2019-12-20 2019-12-20
PCT/US2020/066176 WO2021127539A1 (en) 2019-12-20 2020-12-18 Crystalline hydrobromide salt of a ezh2 inhibitor, its preparation and pharmaceutical composition useful for the treatment of cancer

Publications (1)

Publication Number Publication Date
BR112022012258A2 true BR112022012258A2 (pt) 2022-08-30

Family

ID=74191902

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112022012258A BR112022012258A2 (pt) 2019-12-20 2020-12-18 Sal cristalino de bromidreto de um inibidor de ezh2, sua preparação e composição farmacêutica útil para o tratamento de câncer

Country Status (10)

Country Link
US (2) US20210221800A1 (pt)
EP (1) EP4077314A1 (pt)
JP (1) JP2023509385A (pt)
KR (1) KR20220130698A (pt)
CN (1) CN115175904A (pt)
AU (1) AU2020408395A1 (pt)
BR (1) BR112022012258A2 (pt)
CA (1) CA3162315A1 (pt)
IL (1) IL294108A (pt)
WO (1) WO2021127539A1 (pt)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2692892A1 (en) * 2007-07-24 2009-01-29 Michael Malakhov Technology for the preparation of microparticles
RU2658911C2 (ru) * 2012-04-13 2018-06-26 Эпизайм, Инк. Солевая форма ингибитора гистон-метилтрансферазы ezh2 человека
ES2947819T3 (es) * 2014-11-17 2023-08-21 Epizyme Inc Método para el tratamiento del cáncer con N-((4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H-piran-4-il)amino)-4-metil-4'-(morfolinometil)-[1,1'-bifenil]-3-carboxamida

Also Published As

Publication number Publication date
EP4077314A1 (en) 2022-10-26
US20240166636A1 (en) 2024-05-23
IL294108A (en) 2022-08-01
AU2020408395A1 (en) 2022-07-07
JP2023509385A (ja) 2023-03-08
CN115175904A (zh) 2022-10-11
WO2021127539A1 (en) 2021-06-24
US20210221800A1 (en) 2021-07-22
KR20220130698A (ko) 2022-09-27
CA3162315A1 (en) 2021-06-24

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