CN109336824B - Mek抑制剂的制备和包含mek抑制剂的制剂 - Google Patents

Mek抑制剂的制备和包含mek抑制剂的制剂 Download PDF

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CN109336824B
CN109336824B CN201811124073.6A CN201811124073A CN109336824B CN 109336824 B CN109336824 B CN 109336824B CN 201811124073 A CN201811124073 A CN 201811124073A CN 109336824 B CN109336824 B CN 109336824B
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compound
crystalline
formula
mixture
methyl
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CN109336824A (zh
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C.M.克雷尔
M.米森
D.A.尼德尔
W.H.帕钦格
M-c.沃尔夫
D.齐默尔曼
W.刘
P.J.斯滕格尔
P.尼科尔斯
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Array Biopharma Inc
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Novartis AG
Array Biopharma Inc
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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
    • A61K31/41Heterocyclic 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
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/02Inorganic compounds
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    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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    • 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
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/00Medicinal preparations characterised by special physical form
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    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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    • C30BSINGLE-CRYSTAL GROWTH; UNIDIRECTIONAL SOLIDIFICATION OF EUTECTIC MATERIAL OR UNIDIRECTIONAL DEMIXING OF EUTECTOID MATERIAL; REFINING BY ZONE-MELTING OF MATERIAL; PRODUCTION OF A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; SINGLE CRYSTALS OR HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; AFTER-TREATMENT OF SINGLE CRYSTALS OR A HOMOGENEOUS POLYCRYSTALLINE MATERIAL WITH DEFINED STRUCTURE; APPARATUS THEREFOR
    • C30B29/00Single crystals or homogeneous polycrystalline material with defined structure characterised by the material or by their shape
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    • C30B7/00Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions
    • C30B7/08Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions by cooling of the solution
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    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
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  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Materials Engineering (AREA)
  • Metallurgy (AREA)
  • Biochemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN201811124073.6A 2012-10-19 2013-10-18 Mek抑制剂的制备和包含mek抑制剂的制剂 Active CN109336824B (zh)

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Application Number Priority Date Filing Date Title
US201261716169P 2012-10-19 2012-10-19
US61/716,169 2012-10-19
PCT/US2013/065633 WO2014063024A1 (en) 2012-10-19 2013-10-18 Preparation of and formulation comprising a mek inhibitor
CN201380063271.5A CN104870427B (zh) 2012-10-19 2013-10-18 Mek抑制剂的制备和包含mek抑制剂的制剂

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CN109336824A CN109336824A (zh) 2019-02-15
CN109336824B true CN109336824B (zh) 2022-11-11

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CN201810684986.7A Pending CN109456272A (zh) 2012-10-19 2013-10-18 Mek抑制剂的制备和包含mek抑制剂的制剂
CN201380063271.5A Active CN104870427B (zh) 2012-10-19 2013-10-18 Mek抑制剂的制备和包含mek抑制剂的制剂
CN201811124073.6A Active CN109336824B (zh) 2012-10-19 2013-10-18 Mek抑制剂的制备和包含mek抑制剂的制剂

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CN201380063271.5A Active CN104870427B (zh) 2012-10-19 2013-10-18 Mek抑制剂的制备和包含mek抑制剂的制剂

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EP (3) EP4306171A3 (enExample)
JP (3) JP6385939B2 (enExample)
CN (3) CN109456272A (enExample)
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WO2021116901A1 (en) * 2019-12-09 2021-06-17 Biocon Limited Forms of binimetinib and process for preparation thereof
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CN112679438A (zh) * 2020-12-31 2021-04-20 武汉九州钰民医药科技有限公司 制备司美替尼的方法
JP2024521788A (ja) 2021-05-27 2024-06-04 ミラティ セラピューティクス, インコーポレイテッド 併用療法
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WO2024003942A1 (en) * 2022-07-01 2024-01-04 Natco Pharma Limited An improved process for the preparation of selumetinib sulfate
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WO2025034702A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 for use in the treatment of ras protein-related disease or disorder
WO2025080946A2 (en) 2023-10-12 2025-04-17 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
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US20160168102A1 (en) 2016-06-16
US10729678B2 (en) 2020-08-04
LT3702351T (lt) 2024-01-10
BR112015008623B1 (pt) 2022-10-25
HK1214254A1 (en) 2016-07-22
FI3702351T3 (fi) 2024-01-24
JP2016503391A (ja) 2016-02-04
PT3702351T (pt) 2024-01-17
US20200171002A1 (en) 2020-06-04
US9562016B2 (en) 2017-02-07
US20160168104A1 (en) 2016-06-16
JP6385939B2 (ja) 2018-09-05
WO2014063024A1 (en) 2014-04-24
EP4306171A2 (en) 2024-01-17
TW201427956A (zh) 2014-07-16
RU2015118572A (ru) 2016-12-20
CA2888474A1 (en) 2014-04-24
CA3079071A1 (en) 2014-04-24
US10398683B2 (en) 2019-09-03
JP2018135399A (ja) 2018-08-30
EP3702351A1 (en) 2020-09-02
DK3702351T3 (da) 2024-01-29
JP6737838B2 (ja) 2020-08-12
CY1122670T1 (el) 2021-03-12
ES2971077T3 (es) 2024-06-03
SI2909182T1 (sl) 2020-03-31
EP2909182A1 (en) 2015-08-26
EP2909182A4 (en) 2016-07-06
US9598376B2 (en) 2017-03-21
CN104870427A (zh) 2015-08-26
BR112015008623A2 (pt) 2017-07-04
DK2909182T3 (da) 2020-02-17
US9382212B1 (en) 2016-07-05
US20170231963A1 (en) 2017-08-17
CN104870427B (zh) 2018-10-23
US20140128442A1 (en) 2014-05-08
CN109456272A (zh) 2019-03-12
RS65117B1 (sr) 2024-02-29
CA2888474C (en) 2021-03-02
PL3702351T3 (pl) 2024-04-02
CA3079071C (en) 2022-06-07
US20180296533A1 (en) 2018-10-18
EP2909182B1 (en) 2019-12-04
US20160168103A1 (en) 2016-06-16
CN109336824A (zh) 2019-02-15
JOP20130304B1 (ar) 2021-08-17
RU2018127873A (ru) 2019-03-14
SI3702351T1 (sl) 2024-03-29
US9980944B2 (en) 2018-05-29
SMT202400044T1 (it) 2024-03-13
AR099630A1 (es) 2016-08-10
ES2772498T3 (es) 2020-07-07
US9238627B2 (en) 2016-01-19
EP3702351B1 (en) 2023-11-22
HUE047708T2 (hu) 2020-05-28
TWI650316B (zh) 2019-02-11
JP2019194272A (ja) 2019-11-07
RU2669391C2 (ru) 2018-10-11
PL2909182T3 (pl) 2020-06-01
PT2909182T (pt) 2020-03-02
HUE065433T2 (hu) 2024-05-28
HRP20240033T1 (hr) 2024-03-29
EP4306171A3 (en) 2024-04-03

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