SG11202107849RA - Stable solid dispersions of b-raf kinase dimer inhibitor, methods of preparation, and uses therefor - Google Patents

Stable solid dispersions of b-raf kinase dimer inhibitor, methods of preparation, and uses therefor

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Publication number
SG11202107849RA
SG11202107849RA SG11202107849RA SG11202107849RA SG11202107849RA SG 11202107849R A SG11202107849R A SG 11202107849RA SG 11202107849R A SG11202107849R A SG 11202107849RA SG 11202107849R A SG11202107849R A SG 11202107849RA SG 11202107849R A SG11202107849R A SG 11202107849RA
Authority
SG
Singapore
Prior art keywords
compound
hpmcas
weight ratio
freebase
solid dispersion
Prior art date
Application number
SG11202107849RA
Other languages
English (en)
Inventor
Changyou Zhou
Huangbin Sun
Guoliang Zhang
Original Assignee
Beigene Ltd
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 Beigene Ltd filed Critical Beigene Ltd
Publication of SG11202107849RA publication Critical patent/SG11202107849RA/en

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Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/61—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Dispersion Chemistry (AREA)
SG11202107849RA 2019-01-25 2020-01-23 Stable solid dispersions of b-raf kinase dimer inhibitor, methods of preparation, and uses therefor SG11202107849RA (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2019073254 2019-01-25
CN2019095227 2019-07-09
PCT/CN2020/073944 WO2020151756A1 (en) 2019-01-25 2020-01-23 Stable solid dispersions of b-raf kinase dimer inhibitor, methods of preparation, and uses therefor

Publications (1)

Publication Number Publication Date
SG11202107849RA true SG11202107849RA (en) 2021-08-30

Family

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Family Applications (1)

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SG11202107849RA SG11202107849RA (en) 2019-01-25 2020-01-23 Stable solid dispersions of b-raf kinase dimer inhibitor, methods of preparation, and uses therefor

Country Status (14)

Country Link
US (1) US12582604B2 (enExample)
EP (1) EP3914591A4 (enExample)
JP (2) JP7591504B2 (enExample)
KR (1) KR20210120039A (enExample)
CN (1) CN113330011A (enExample)
AU (1) AU2020211000B2 (enExample)
BR (1) BR112021014563A2 (enExample)
CA (1) CA3123476A1 (enExample)
IL (1) IL284636A (enExample)
MX (1) MX2021008884A (enExample)
SG (1) SG11202107849RA (enExample)
TW (2) TWI849043B (enExample)
WO (1) WO2020151756A1 (enExample)
ZA (1) ZA202104032B (enExample)

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TWI849043B (zh) 2019-01-25 2024-07-21 英屬開曼群島商百濟神州有限公司 B-raf激酶二聚體抑制劑之穩定固體分散體、製備方法及其用途
AU2021412688B2 (en) * 2020-12-29 2025-06-12 Txinno Bioscience Inc. Novel naphthyridinone derivative having inhibitory activity against ectonucleotide pyrophosphatase-phosphodiesterase and use thereof
KR102889693B1 (ko) 2021-09-08 2025-11-20 주식회사 엘지에너지솔루션 배터리 진단 장치, 배터리 관리 시스템, 배터리 팩, 전기 차량 및 배터리 진단 방법
CN114366717B (zh) * 2022-01-11 2023-06-09 四川农业大学 一种基于egcg纳米粒的肠溶固体分散体颗粒、制备方法及其应用
JP2025519981A (ja) * 2022-06-08 2025-06-30 マップキュア,エルエルシー B-raf阻害剤によるがんの治療方法
JP2025532826A (ja) * 2022-09-26 2025-10-03 マップキュア,エルエルシー がんの処置のためのb-raf阻害剤と、抗egfr抗体との組み合わせ
JP2026507361A (ja) * 2023-03-10 2026-03-02 エスティー ファーム カンパニー リミテッド 新規固体分散体およびその製造方法
TW202515875A (zh) 2023-10-12 2025-04-16 瑞士商百濟神州瑞士有限責任公司 包含b-raf激酶二聚體抑制劑之固體形式、其製備方法及用途
WO2025252204A1 (en) * 2024-06-07 2025-12-11 Beigene (Suzhou) Co., Ltd. Amorphous solid dispersions of a braf inhibitor

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Also Published As

Publication number Publication date
EP3914591A1 (en) 2021-12-01
AU2020211000A1 (en) 2021-08-12
TW202444718A (zh) 2024-11-16
AU2020211000B2 (en) 2025-11-06
JP2025017374A (ja) 2025-02-05
CA3123476A1 (en) 2020-07-30
US20220105033A1 (en) 2022-04-07
KR20210120039A (ko) 2021-10-06
TW202043225A (zh) 2020-12-01
WO2020151756A1 (en) 2020-07-30
CN113330011A (zh) 2021-08-31
EP3914591A4 (en) 2022-11-09
TWI849043B (zh) 2024-07-21
ZA202104032B (en) 2022-08-31
TWI909513B (zh) 2025-12-21
JP2022517675A (ja) 2022-03-09
BR112021014563A2 (pt) 2021-10-05
JP7591504B2 (ja) 2024-11-28
IL284636A (en) 2021-08-31
MX2021008884A (es) 2021-08-19
US12582604B2 (en) 2026-03-24

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