EA201291280A1 - Новая полиморфная форма основания иматиниба и получение её солей - Google Patents

Новая полиморфная форма основания иматиниба и получение её солей

Info

Publication number
EA201291280A1
EA201291280A1 EA201291280A EA201291280A EA201291280A1 EA 201291280 A1 EA201291280 A1 EA 201291280A1 EA 201291280 A EA201291280 A EA 201291280A EA 201291280 A EA201291280 A EA 201291280A EA 201291280 A1 EA201291280 A1 EA 201291280A1
Authority
EA
Eurasian Patent Office
Prior art keywords
imatinibe
foundation
salts
obtaining
polymorphic form
Prior art date
Application number
EA201291280A
Other languages
English (en)
Other versions
EA024088B1 (ru
Inventor
Примоз Бенкиц
Ярослав Тихи
Аница Пецавар
Тамара Герман
Франц Врецер
Анамария Вайс
Вида Шкрабаня
Original Assignee
КРКА, д.д., НОВО МЕСТО
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by КРКА, д.д., НОВО МЕСТО filed Critical КРКА, д.д., НОВО МЕСТО
Publication of EA201291280A1 publication Critical patent/EA201291280A1/ru
Publication of EA024088B1 publication Critical patent/EA024088B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/16—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
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • 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
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Abstract

Изобретение относится к способу получения нового полиморфа основания иматиниба, способу получения его соли мезилата и их включению в фармацевтические композиции, которые имеют улучшенную стабильность и чистоту, а также к способам их получения.
EA201291280A 2010-06-18 2011-06-17 α-ФОРМА МЕЗИЛАТА ИМАТИНИБА, СПОСОБЫ ЕЕ ПОЛУЧЕНИЯ И СОДЕРЖАЩАЯ ЕЁ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ EA024088B1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
SI201000181 2010-06-18
SI201000348 2010-10-27
SI201000398 2010-11-19
SI201100054 2011-02-22
PCT/EP2011/003025 WO2011157450A1 (en) 2010-06-18 2011-06-17 New polymorphic form of imatinib base and preparation of salts thereof

Publications (2)

Publication Number Publication Date
EA201291280A1 true EA201291280A1 (ru) 2013-04-30
EA024088B1 EA024088B1 (ru) 2016-08-31

Family

ID=44259640

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201291280A EA024088B1 (ru) 2010-06-18 2011-06-17 α-ФОРМА МЕЗИЛАТА ИМАТИНИБА, СПОСОБЫ ЕЕ ПОЛУЧЕНИЯ И СОДЕРЖАЩАЯ ЕЁ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Country Status (4)

Country Link
EP (1) EP2582689B1 (ru)
EA (1) EA024088B1 (ru)
SI (1) SI2582689T1 (ru)
WO (1) WO2011157450A1 (ru)

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JP5928159B2 (ja) * 2012-05-28 2016-06-01 ニプロ株式会社 医薬組成物
KR101242955B1 (ko) * 2012-06-25 2013-03-12 제일약품주식회사 이마티닙 메실레이트 결정형 α의 제조 방법
WO2014016848A2 (en) * 2012-07-24 2014-01-30 Laurus Labs Private Limited Solid forms of tyrosine kinase inhibitors, process for the preparation and their pharmaceutical composition thereof
EP3007699A4 (en) * 2013-06-12 2017-01-18 Shilpa Medicare Limited Crystalline imatinib mesylate process
US20150044288A1 (en) * 2013-07-31 2015-02-12 Windward Pharma, Inc. Aerosol tyrosine kinase inhibitor compounds and uses thereof
CN104974134B (zh) * 2015-05-19 2017-01-18 江苏豪森药业集团有限公司 甲磺酸伊马替尼的精制方法
EA035891B1 (ru) 2016-01-25 2020-08-27 КРКА, д.д., НОВО МЕСТО Быстродиспергируемая фармацевтическая композиция, включающая ингибитор тирозинкиназы
US11464776B2 (en) 2019-05-16 2022-10-11 Aerovate Therapeutics, Inc. Inhalable imatinib formulations, manufacture, and uses thereof
EP3969111A4 (en) 2019-05-16 2023-08-16 Aerovate Therapeutics, Inc. INHALABLE FORMULATIONS FOR KINASE INHIBITION

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Also Published As

Publication number Publication date
EP2582689A1 (en) 2013-04-24
EP2582689B1 (en) 2017-03-01
SI2582689T1 (sl) 2017-05-31
EA024088B1 (ru) 2016-08-31
WO2011157450A1 (en) 2011-12-22

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM