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RU2018118176A - Липосомы, содержащие проникающие в клетки пептиды и тетраэфирные липиды, для пероральной доставки макромолекул - Google Patents

Липосомы, содержащие проникающие в клетки пептиды и тетраэфирные липиды, для пероральной доставки макромолекул Download PDF

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RU2018118176A
RU2018118176A RU2018118176A RU2018118176A RU2018118176A RU 2018118176 A RU2018118176 A RU 2018118176A RU 2018118176 A RU2018118176 A RU 2018118176A RU 2018118176 A RU2018118176 A RU 2018118176A RU 2018118176 A RU2018118176 A RU 2018118176A
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liposome composition
composition according
paragraphs
seq
lipids
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RU2018118176A
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RU2743431C2 (ru
RU2018118176A3 (ru
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Филипп УЛЬ
Макс ЗАУТЕР
Уве Хаберкорн
Вальтер Мир
Герт ФРИККЕР
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Универзитет Хайдельберг
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
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    • 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
    • A61K47/69Medicinal 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6905Medicinal 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion
    • A61K47/6911Medicinal 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a liposome
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    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
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    • A61K38/22Hormones
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    • 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
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
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    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • AHUMAN NECESSITIES
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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
    • A61K47/42Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
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    • 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
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    • A61K47/543Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
    • A61K47/544Phospholipids
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    • A61K47/554Medicinal 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 compound the modifying agent being a steroid plant sterol, glycyrrhetic acid, enoxolone or bile acid
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    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions

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Claims (18)

1. Липосомная композиция, содержащая липосомы, причем указанные липосомы содержат
(a) тетраэфирные липиды (TEL) и
(b) проникающие в клетки пептиды (CPP),
где указанные CPP присоединены к соединению, которое является частью липидного бислоя липосомы.
2. Липосомная композиция по п.1, где указанные TEL получены из Sulfolobus sp.
3. Липосомная композиция по п.2, где указанные TEL получены из Sulfolobus acidocaldarius.
4. Липосомная композиция по любому из пп. 1-3, в которой указанные TEL выбраны из группы, состоящей из глицерилкалдитилтетраэфира (GCTE), диглицерилтетраэфира (DGTE) и их сочетаний.
5. Липосомная композиция по любому из пп. 1-4, в которой указанные липосомы содержат указанные TEL в количестве от 1 до 10 моль.% на основе общего количества липидов.
6. Липосомная композиция по любому из пп. 1-5, в которой указанные CPP выбраны из группы, состоящей из линейного или циклизованного пенетратина (SEQ ID № 1), пептида TAT (трансактиватор транскрипции) (SEQ ID № 2), MAP (модельный амфипатический пептид) (SEQ ID № 3), R9 (SEQ ID № 4), pVEC (SEQ ID № 5), транспортана (SEQ ID № 6) и MPG (SEQ ID № 7), их сочетаний и их димеров.
7. Липосомная композиция по любому из пп. 1-6, в которой указанные липосомы содержат указанные CPP в количестве от 0,1 до 1 моль.% на основе общего количества липидов.
8. Липосомная композиция по любому из пп. 1-7, в которой указанное соединение, к которому присоединены указанные CPP, выбраны из группы, состоящей из холестерина и его производных, фосфолипидов, лизофосфолипидов и тетраэфирных липидов.
9. Липосомная композиция по любому из пп. 1-8, в которой указанные CPP присоединены ковалентно.
10. Липосомная композиция по любому из пп. 1-9, в которой указанные CPP присоединены через линкер.
11. Липосомная композиция по п.10, в которой указанный линкер выбран из группы, состоящей из бифункциональных PEG-линкеров.
12. Липосомная композиция по любому из пп. 1-11, которая дополнительно содержит по меньшей мере одно терапевтическое средство и/или по меньшей мере одно диагностическое средство.
13. Липосомная композиция по любому из пп. 1-12 для применения в медицине.
14. Липосомная композиция для применения по п.13, где указанная композиция предназначена для перорального введения.
15. Применение липосомной композиции по любому из пп. 1-12 для пероральной доставки по меньшей мере одного терапевтического средства и/или по меньшей мере одного диагностического средства.
RU2018118176A 2015-10-21 2016-10-11 Липосомы, содержащие проникающие в клетки пептиды и тетраэфирные липиды, для пероральной доставки макромолекул RU2743431C2 (ru)

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Application Number Priority Date Filing Date Title
EP15003011.2 2015-10-21
EP15003011.2A EP3158992A1 (en) 2015-10-21 2015-10-21 Liposomes containing cell penetrating peptides and tetraetherlipids for the oral delivery of macromolecules
PCT/EP2016/001682 WO2017067642A1 (en) 2015-10-21 2016-10-11 Liposomes containing cell penetrating peptides and tetraetherlipids for the oral delivery of macromolecules

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RU2018118176A true RU2018118176A (ru) 2019-11-21
RU2018118176A3 RU2018118176A3 (ru) 2020-02-26
RU2743431C2 RU2743431C2 (ru) 2021-02-18

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US (1) US10653796B2 (ru)
EP (2) EP3158992A1 (ru)
JP (1) JP6689378B2 (ru)
CN (1) CN108135846B (ru)
ES (1) ES2870223T3 (ru)
RU (1) RU2743431C2 (ru)
WO (1) WO2017067642A1 (ru)
ZA (1) ZA201801514B (ru)

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RU2743431C2 (ru) 2021-02-18
EP3364952B1 (en) 2021-02-24
CN108135846B (zh) 2022-02-18
RU2018118176A3 (ru) 2020-02-26
EP3364952A1 (en) 2018-08-29
US20180303956A1 (en) 2018-10-25
WO2017067642A1 (en) 2017-04-27
CN108135846A (zh) 2018-06-08
US10653796B2 (en) 2020-05-19
ZA201801514B (en) 2019-07-31
JP6689378B2 (ja) 2020-04-28
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