ES2772498T3 - Preparación de un inhibidor mek y formulación que comprende el mismo - Google Patents

Preparación de un inhibidor mek y formulación que comprende el mismo Download PDF

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Publication number
ES2772498T3
ES2772498T3 ES13847106T ES13847106T ES2772498T3 ES 2772498 T3 ES2772498 T3 ES 2772498T3 ES 13847106 T ES13847106 T ES 13847106T ES 13847106 T ES13847106 T ES 13847106T ES 2772498 T3 ES2772498 T3 ES 2772498T3
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Prior art keywords
compound
formula
mixture
acid
water
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ES13847106T
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English (en)
Spanish (es)
Inventor
Christoph Krell
Marian Misun
Daniel Niederer
Werner Pachinger
Marie-Christine Wolf
Daniel Zimmermann
Weidong Liu
Peter Stengel
Paul Nichols
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Array Biopharma Inc
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Array Biopharma Inc
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Application filed by Array Biopharma Inc filed Critical Array Biopharma Inc
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Publication of ES2772498T3 publication Critical patent/ES2772498T3/es
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Classifications

    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/06—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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • 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
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-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
    • C30B29/00—Single crystals or homogeneous polycrystalline material with defined structure characterised by the material or by their shape
    • C30B29/54—Organic compounds
    • C—CHEMISTRY; METALLURGY
    • C30—CRYSTAL GROWTH
    • C30B—SINGLE-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
    • C30B7/00—Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions
    • C30B7/08—Single-crystal growth from solutions using solvents which are liquid at normal temperature, e.g. aqueous solutions by cooling of the solution
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Materials Engineering (AREA)
  • Metallurgy (AREA)
  • Biochemistry (AREA)
  • Physiology (AREA)
  • Nutrition Science (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)
ES13847106T 2012-10-19 2013-10-18 Preparación de un inhibidor mek y formulación que comprende el mismo Active ES2772498T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201261716169P 2012-10-19 2012-10-19
PCT/US2013/065633 WO2014063024A1 (en) 2012-10-19 2013-10-18 Preparation of and formulation comprising a mek inhibitor

Publications (1)

Publication Number Publication Date
ES2772498T3 true ES2772498T3 (es) 2020-07-07

Family

ID=50488781

Family Applications (2)

Application Number Title Priority Date Filing Date
ES13847106T Active ES2772498T3 (es) 2012-10-19 2013-10-18 Preparación de un inhibidor mek y formulación que comprende el mismo
ES19211405T Active ES2971077T3 (es) 2012-10-19 2013-10-18 Formulación que comprende un inhibidor mek

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES19211405T Active ES2971077T3 (es) 2012-10-19 2013-10-18 Formulación que comprende un inhibidor mek

Country Status (23)

Country Link
US (7) US9238627B2 (enExample)
EP (3) EP3702351B1 (enExample)
JP (3) JP6385939B2 (enExample)
CN (3) CN109456272A (enExample)
AR (1) AR099630A1 (enExample)
BR (1) BR112015008623B1 (enExample)
CA (2) CA3079071C (enExample)
CY (1) CY1122670T1 (enExample)
DK (2) DK2909182T3 (enExample)
ES (2) ES2772498T3 (enExample)
FI (1) FI3702351T3 (enExample)
HR (1) HRP20240033T1 (enExample)
HU (2) HUE065433T2 (enExample)
JO (1) JOP20130304B1 (enExample)
LT (1) LT3702351T (enExample)
PL (2) PL3702351T3 (enExample)
PT (2) PT2909182T (enExample)
RS (1) RS65117B1 (enExample)
RU (2) RU2018127873A (enExample)
SI (2) SI2909182T1 (enExample)
SM (1) SMT202400044T1 (enExample)
TW (1) TWI650316B (enExample)
WO (1) WO2014063024A1 (enExample)

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WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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EP3702351B1 (en) 2023-11-22
SMT202400044T1 (it) 2024-03-13
RS65117B1 (sr) 2024-02-29
BR112015008623B1 (pt) 2022-10-25
DK3702351T3 (da) 2024-01-29
US10729678B2 (en) 2020-08-04
EP2909182A4 (en) 2016-07-06
US9382212B1 (en) 2016-07-05
HRP20240033T1 (hr) 2024-03-29
CY1122670T1 (el) 2021-03-12
WO2014063024A1 (en) 2014-04-24
TW201427956A (zh) 2014-07-16
FI3702351T3 (fi) 2024-01-24
JP2019194272A (ja) 2019-11-07
US20160168102A1 (en) 2016-06-16
US20200171002A1 (en) 2020-06-04
US20170231963A1 (en) 2017-08-17
JP2016503391A (ja) 2016-02-04
RU2018127873A (ru) 2019-03-14
US9562016B2 (en) 2017-02-07
PL2909182T3 (pl) 2020-06-01
US9980944B2 (en) 2018-05-29
AR099630A1 (es) 2016-08-10
EP2909182B1 (en) 2019-12-04
PT3702351T (pt) 2024-01-17
CN104870427B (zh) 2018-10-23
RU2015118572A (ru) 2016-12-20
DK2909182T3 (da) 2020-02-17
SI3702351T1 (sl) 2024-03-29
PL3702351T3 (pl) 2024-04-02
JOP20130304B1 (ar) 2021-08-17
US20180296533A1 (en) 2018-10-18
US20140128442A1 (en) 2014-05-08
HUE065433T2 (hu) 2024-05-28
EP4306171A3 (en) 2024-04-03
LT3702351T (lt) 2024-01-10
HUE047708T2 (hu) 2020-05-28
US20160168104A1 (en) 2016-06-16
SI2909182T1 (sl) 2020-03-31
CN109336824A (zh) 2019-02-15
CA2888474A1 (en) 2014-04-24
US10398683B2 (en) 2019-09-03
US20160168103A1 (en) 2016-06-16
JP2018135399A (ja) 2018-08-30
CN109336824B (zh) 2022-11-11
TWI650316B (zh) 2019-02-11
CA3079071A1 (en) 2014-04-24
CA2888474C (en) 2021-03-02
JP6385939B2 (ja) 2018-09-05
EP2909182A1 (en) 2015-08-26
HK1214254A1 (en) 2016-07-22
US9598376B2 (en) 2017-03-21
JP6737838B2 (ja) 2020-08-12
CN109456272A (zh) 2019-03-12
US9238627B2 (en) 2016-01-19
EP4306171A2 (en) 2024-01-17
CN104870427A (zh) 2015-08-26
PT2909182T (pt) 2020-03-02
BR112015008623A2 (pt) 2017-07-04
RU2669391C2 (ru) 2018-10-11
ES2971077T3 (es) 2024-06-03
EP3702351A1 (en) 2020-09-02
CA3079071C (en) 2022-06-07

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