JP7591504B2 - B-rafキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用 - Google Patents

B-rafキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用 Download PDF

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JP7591504B2
JP7591504B2 JP2021542104A JP2021542104A JP7591504B2 JP 7591504 B2 JP7591504 B2 JP 7591504B2 JP 2021542104 A JP2021542104 A JP 2021542104A JP 2021542104 A JP2021542104 A JP 2021542104A JP 7591504 B2 JP7591504 B2 JP 7591504B2
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compound
hpmcas
solid dispersion
amorphous solid
cancer
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JP2022517675A (ja
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チャン、グオリャン
チョウ、チャンヨウ
スン、ファンビン
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BeOne Medicines Ltd
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Beigene Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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
    • A61K47/61Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate 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
    • A61K9/146Intimate 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
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    • A61K9/20Pills, tablets, discs, rods
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    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
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  • 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)
JP2021542104A 2019-01-25 2020-01-23 B-rafキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用 Active JP7591504B2 (ja)

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JP2024200421A JP2025017374A (ja) 2019-01-25 2024-11-18 B-rafキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用

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CN2019073254 2019-01-25
CNPCT/CN2019/073254 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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JP2022517675A JP2022517675A (ja) 2022-03-09
JPWO2020151756A5 JPWO2020151756A5 (https=) 2023-01-27
JP2022517675A5 JP2022517675A5 (https=) 2023-01-27
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JP2024200421A Pending JP2025017374A (ja) 2019-01-25 2024-11-18 B-rafキナーゼ二量体阻害剤の安定な固体分散体、その調製方法及び使用

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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) TWI909513B (https=)
WO (1) WO2020151756A1 (https=)
ZA (1) ZA202104032B (https=)

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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
TWI909513B (zh) 2019-01-25 2025-12-21 英屬開曼群島商百濟神州有限公司 作為b-raf激酶二聚體抑制劑之化合物及其製備方法
WO2022146022A1 (ko) * 2020-12-29 2022-07-07 주식회사 티씨노바이오사이언스 엑토뉴클레오티드 피로포스파타아제-포스포디에스터라아제의 저해 활성을 갖는 신규한 나프티리딘온 유도체 및 이들의 용도
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
WO2023240178A1 (en) * 2022-06-08 2023-12-14 Mapkure, Llc Methods of treating cancer with a b-raf inhibitor
KR20250069903A (ko) * 2022-09-26 2025-05-20 맵큐어, 엘엘씨 암 치료를 위한 B-Raf 저해제와 항-EGFR 항체의 조합물
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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US12582604B2 (en) 2026-03-24
BR112021014563A2 (pt) 2021-10-05
ZA202104032B (en) 2022-08-31
EP3914591A1 (en) 2021-12-01
IL284636A (en) 2021-08-31
SG11202107849RA (en) 2021-08-30
CA3123476A1 (en) 2020-07-30
EP3914591A4 (en) 2022-11-09
TWI849043B (zh) 2024-07-21
CN113330011A (zh) 2021-08-31
WO2020151756A1 (en) 2020-07-30
MX2021008884A (es) 2021-08-19
US20220105033A1 (en) 2022-04-07
TWI909513B (zh) 2025-12-21
TW202444718A (zh) 2024-11-16
KR20210120039A (ko) 2021-10-06
AU2020211000A1 (en) 2021-08-12
JP2025017374A (ja) 2025-02-05
TW202043225A (zh) 2020-12-01
JP2022517675A (ja) 2022-03-09
AU2020211000B2 (en) 2025-11-06

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