KR20210120039A - B-raf 키나제 이합체 억제제의 안정적인 고체 분산액, 이의 제조 방법 및 용도 - Google Patents

B-raf 키나제 이합체 억제제의 안정적인 고체 분산액, 이의 제조 방법 및 용도 Download PDF

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KR20210120039A
KR20210120039A KR1020217026908A KR20217026908A KR20210120039A KR 20210120039 A KR20210120039 A KR 20210120039A KR 1020217026908 A KR1020217026908 A KR 1020217026908A KR 20217026908 A KR20217026908 A KR 20217026908A KR 20210120039 A KR20210120039 A KR 20210120039A
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compound
hpmcas
free base
solid dispersion
weight ratio
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구오리앙 장
창유 조우
황빈 선
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베이진 엘티디
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    • 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
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    • 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

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  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • 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)
KR1020217026908A 2019-01-25 2020-01-23 B-raf 키나제 이합체 억제제의 안정적인 고체 분산액, 이의 제조 방법 및 용도 Pending KR20210120039A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CNPCT/CN2019/073254 2019-01-25
CN2019073254 2019-01-25
CN2019095227 2019-07-09
CNPCT/CN2019/095227 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

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KR20210120039A true KR20210120039A (ko) 2021-10-06

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KR1020217026908A Pending KR20210120039A (ko) 2019-01-25 2020-01-23 B-raf 키나제 이합체 억제제의 안정적인 고체 분산액, 이의 제조 방법 및 용도

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

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WO2023038398A1 (ko) 2021-09-08 2023-03-16 주식회사 엘지에너지솔루션 배터리 진단 장치, 배터리 관리 시스템, 배터리 팩, 전기 차량 및 배터리 진단 방법
WO2024191137A1 (ko) * 2023-03-10 2024-09-19 에스티팜 주식회사 신규 고체분산체 및 이의 제조방법

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CN111484490B (zh) * 2019-01-25 2024-07-09 百济神州有限公司 适合大规模生产b-raf激酶二聚体抑制剂的方法
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
JP2024504285A (ja) * 2020-12-29 2024-01-31 ティーエックスイノ バイオサイエンス インコーポレイテッド エクトヌクレオチドピロホスファターゼ－ホスホジエステラーゼの阻害活性を有する新規のナフチリジノン誘導体及びこれらの用途
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
WO2023240178A1 (en) * 2022-06-08 2023-12-14 Mapkure, Llc Methods of treating cancer with a b-raf inhibitor
EP4593831A1 (en) * 2022-09-26 2025-08-06 Mapkure, LLC Combinations of a b-raf inhibitor, and an anti-egfr antibody for the treatment of cancer
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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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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2023038398A1 (ko) 2021-09-08 2023-03-16 주식회사 엘지에너지솔루션 배터리 진단 장치, 배터리 관리 시스템, 배터리 팩, 전기 차량 및 배터리 진단 방법
WO2024191137A1 (ko) * 2023-03-10 2024-09-19 에스티팜 주식회사 신규 고체분산체 및 이의 제조방법

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AU2020211000A1 (en) 2021-08-12
US12582604B2 (en) 2026-03-24
IL284636A (en) 2021-08-31
AU2020211000B2 (en) 2025-11-06
SG11202107849RA (en) 2021-08-30
US20220105033A1 (en) 2022-04-07
TW202444718A (zh) 2024-11-16
MX2021008884A (es) 2021-08-19
CA3123476A1 (en) 2020-07-30
JP2025017374A (ja) 2025-02-05
TW202043225A (zh) 2020-12-01
CN113330011A (zh) 2021-08-31
JP7591504B2 (ja) 2024-11-28
EP3914591A4 (en) 2022-11-09
JP2022517675A (ja) 2022-03-09
WO2020151756A1 (en) 2020-07-30
ZA202104032B (en) 2022-08-31
EP3914591A1 (en) 2021-12-01
TWI849043B (zh) 2024-07-21
TWI909513B (zh) 2025-12-21
BR112021014563A2 (pt) 2021-10-05

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