CN113490492B - 吡唑酰胺化合物的非晶质固体分散体 - Google Patents

吡唑酰胺化合物的非晶质固体分散体 Download PDF

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CN113490492B
CN113490492B CN202080018640.9A CN202080018640A CN113490492B CN 113490492 B CN113490492 B CN 113490492B CN 202080018640 A CN202080018640 A CN 202080018640A CN 113490492 B CN113490492 B CN 113490492B
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pharmaceutically acceptable
formula
solid dispersion
hydrate
compound
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CN113490492A (zh
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中岛由博
中岛骏
森由匡
野泽智司
石川嘉昭
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Japan Tobacco Inc
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Japan Tobacco Inc
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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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
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    • 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
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    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
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    • 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
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    • A61K9/1682—Processes
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    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • 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
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN202080018640.9A 2019-03-04 2020-03-03 吡唑酰胺化合物的非晶质固体分散体 Active CN113490492B (zh)

Applications Claiming Priority (3)

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JP2019-038327 2019-03-04
JP2019038327 2019-03-04
PCT/JP2020/008840 WO2020179770A1 (ja) 2019-03-04 2020-03-03 ピラゾール－アミド化合物の非晶質固体分散体

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CN113490492B true CN113490492B (zh) 2024-09-27

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US (1) US20220409548A1 (https=)
EP (1) EP3936127B1 (https=)
JP (1) JP7489370B2 (https=)
KR (1) KR20210135266A (https=)
CN (1) CN113490492B (https=)
AU (1) AU2020232630A1 (https=)
BR (1) BR112021016815A2 (https=)
CA (1) CA3132296A1 (https=)
MX (1) MX2021010692A (https=)
WO (1) WO2020179770A1 (https=)

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AU2022337617A1 (en) * 2021-09-01 2024-04-18 Japan Tobacco Inc. Nitrogen-containing tricyclic compound and pharmaceutical use thereof
AU2022381641A1 (en) * 2021-11-03 2024-06-20 Beijing Innocare Pharma Tech Co., Ltd. Amorphous solid dispersion comprising (s) -1- (1-acryloylpyrrolidin-3-yl) -3- ( (3, 5-dimethoxyphenyl) ethynyl) -5- (methylamino) -1h-pyrazole-4-carboxamide
KR102769218B1 (ko) * 2022-09-28 2025-02-24 주식회사 제이디바이오사이언스 신규한 플루오렌 유도체 및 이의 용도
JP2024091760A (ja) * 2024-04-15 2024-07-05 信越化学工業株式会社 非晶質固体分散体を含む複合物
US20250332105A1 (en) * 2024-04-25 2025-10-30 Beijing Innocare Pharma Tech Co., Ltd. Amorphous solid dispersion comprising (s)-1-(1-acryloylpyrrolidin-3-yl)-3-((3,5-dimethoxyphenyl)ethynyl)-5-(methylamino)-1h-pyrazole-4-carboxamide

Citations (1)

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WO2018021508A1 (ja) * 2016-07-29 2018-02-01 日本たばこ産業株式会社 ピラゾール－アミド化合物の製造方法

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CA2645566A1 (en) 2006-03-20 2007-09-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
BR112012031516A2 (pt) 2010-06-09 2016-11-08 Abbott Lab dispersões sólidas contendo inibidores de quinase
JP5475561B2 (ja) * 2010-06-14 2014-04-16 ポリプラスチックス株式会社 充填材の配向解析方法
JP2014521745A (ja) 2011-08-16 2014-08-28 メルク・シャープ・アンド・ドーム・コーポレーション 安定した非晶質分散体を調製するための無機マトリックスと有機ポリマーの組み合わせの使用
BR112015022077A2 (pt) 2013-03-15 2017-07-18 Japan Tobacco Inc composto de pirazol-amida e usos medicinais do mesmo
WO2018013693A1 (en) * 2016-07-13 2018-01-18 Celgene Corporation Solid dispersions and cocrystals comprising 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione compositions and methods of use thereof
CN108785256B (zh) * 2017-04-28 2021-06-29 江苏恒瑞医药股份有限公司 一种固体分散体及其制备方法

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2018021508A1 (ja) * 2016-07-29 2018-02-01 日本たばこ産業株式会社 ピラゾール－アミド化合物の製造方法

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CN113490492A (zh) 2021-10-08
BR112021016815A2 (pt) 2021-11-16
EP3936127A1 (en) 2022-01-12
MX2021010692A (es) 2021-10-01
AU2020232630A1 (en) 2021-09-16
WO2020179770A1 (ja) 2020-09-10
JP7489370B2 (ja) 2024-05-23
US20220409548A1 (en) 2022-12-29
JPWO2020179770A1 (https=) 2020-09-10
EP3936127A4 (en) 2022-12-14
EP3936127B1 (en) 2025-04-30
KR20210135266A (ko) 2021-11-12
CA3132296A1 (en) 2020-09-10

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