EA201900246A1 - Ингибитор атф-зависимых обратных транспортеров клеток и способ его получения - Google Patents

Ингибитор атф-зависимых обратных транспортеров клеток и способ его получения

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Publication number
EA201900246A1
EA201900246A1 EA201900246A EA201900246A EA201900246A1 EA 201900246 A1 EA201900246 A1 EA 201900246A1 EA 201900246 A EA201900246 A EA 201900246A EA 201900246 A EA201900246 A EA 201900246A EA 201900246 A1 EA201900246 A1 EA 201900246A1
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EA
Eurasian Patent Office
Prior art keywords
glycol
inhibitor
oep
conjugate
polyoxypropylenehexol
Prior art date
Application number
EA201900246A
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English (en)
Other versions
EA034579B1 (ru
Inventor
Юрий Григорьевич ШТЫРЛИН
Альфия Габдулахатовна ИКСАНОВА
Юрий Владимирович БАДЕЕВ
Константин Валерьевич БАЛАКИН
Original Assignee
Акционерное Общество "Татхимфармпрепараты"
Федеральное Государственное Автономное Образовательное Учреждение Высшего Образования "Казанский (Приволжский) Федеральный Университет"
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Application filed by Акционерное Общество "Татхимфармпрепараты", Федеральное Государственное Автономное Образовательное Учреждение Высшего Образования "Казанский (Приволжский) Федеральный Университет" filed Critical Акционерное Общество "Татхимфармпрепараты"
Publication of EA201900246A1 publication Critical patent/EA201900246A1/ru
Publication of EA034579B1 publication Critical patent/EA034579B1/ru

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    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/25—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol
    • 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
    • A61K31/74—Synthetic polymeric materials
    • A61K31/765—Polymers containing oxygen
    • A61K31/77—Polymers containing oxygen of oxiranes
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • 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
    • A61K31/74—Synthetic polymeric materials
    • A61K31/765—Polymers containing oxygen
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—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 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/61—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 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/26—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring from cyclic ethers and other compounds
    • C08G65/2603—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring from cyclic ethers and other compounds the other compounds containing oxygen
    • C08G65/2606—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring from cyclic ethers and other compounds the other compounds containing oxygen containing hydroxyl groups
    • C08G65/2609—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring from cyclic ethers and other compounds the other compounds containing oxygen containing hydroxyl groups containing aliphatic hydroxyl groups
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G65/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G65/02—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring
    • C08G65/26—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring from cyclic ethers and other compounds
    • C08G65/2696—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule from cyclic ethers by opening of the heterocyclic ring from cyclic ethers and other compounds characterised by the process or apparatus used
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G2650/00—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule
    • C08G2650/28—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule characterised by the polymer type
    • C08G2650/30—Macromolecular compounds obtained by reactions forming an ether link in the main chain of the macromolecule characterised by the polymer type branched

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Furan Compounds (AREA)
  • Epoxy Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyrane Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Изобретение относится к химии лекарственных соединений, а именно к группе хиральных конъюгатов (оптически активных гибридных молекул) олигоэфирполиольной природы, являющихся ингибиторами АТФ-зависимых обратных транспортеров клеток (ОЭП-ингибитор). ОЭП-ингибитор представляет собой конъюгат с эквимольным соотношением оптически активного полиоксипропиленгексола и полиоксипропиленгликоля. Заявленный способ, по которому получается конъюгат, обеспечивает возможность получения препарата, увеличивающего эффективность действия лекарственных средств посредством ингибирования механизмов множественной лекарственной устойчивости клеток. Полученный препарат может быть использован в области биологии, фармакологии, фармацевтики, медицины, сельского хозяйства. ОЭП-ингибитор получают оксипропилированием смеси сорбита и бифункционального кислородсодержащего соединения в присутствии гидроокиси щелочного или щелочноземельного металла. Бифункциональное кислородсодержащее соединение может быть водой, пропиленгликолем, дипропиленгликолем, трипропиленгликолем, тетрапропиленгликолем, пентапропиленгликолем, гексапропиленгликолем, гептапропиленгликолем или их смесью. Ингибитор представляет собой коньюгат полиоксипропиленгликоля с молекулярной массой от 300 до 500 Да и полиоксипропиленгексола с молекулярной массой от 1000 до 1500 Да в эквимольном соотношении, с гидроксильным числом в пределах 215-240 мг KOH/г.
EA201900246A 2016-11-02 2017-10-31 Ингибитор атф-зависимых обратных транспортеров клеток и способ его получения EA034579B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
RU2016143074A RU2641304C1 (ru) 2016-11-02 2016-11-02 Ингибитор атф-зависимых обратных транспортеров клеток и способ его получения
PCT/RU2017/000809 WO2018084749A1 (ru) 2016-11-02 2017-10-31 Ингибитор атф-зависимых обратных транспортеров клеток и способ его получения

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EA201900246A1 true EA201900246A1 (ru) 2019-07-31
EA034579B1 EA034579B1 (ru) 2020-02-21

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US (1) US10987429B2 (ru)
EP (1) EP3536315B1 (ru)
JP (1) JP6861424B2 (ru)
CN (1) CN109890375B (ru)
EA (1) EA034579B1 (ru)
RU (1) RU2641304C1 (ru)
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RU2680834C1 (ru) * 2018-05-23 2019-02-28 федеральное государственное автономное образовательное учреждение высшего образования "Казанский (Приволжский) федеральный университет" (ФГАОУ ВО КФУ) Противоопухолевая композиция доксорубицина с ингибитором АТФ-зависимых обратных транспортеров клеток
AU2021366966A1 (en) * 2020-10-19 2023-03-02 Oxiteno S.A. Indústria E Comércio Composition, agrochemical formulation, methods for increasing water and nutrient availability and for improving pest control in plants and seeds, and uses of the composition and the agrochemical formulation

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SE523934C2 (sv) * 2001-09-24 2004-06-01 Perstorp Specialty Chem Ab Förfarande för av alkoxylering av di-, tri och polyalkoholer
CN101497559A (zh) * 2008-12-30 2009-08-05 浙江皇马科技股份有限公司 山梨醇和甘油混合醇聚氧丙烯醚的制备方法
RO127401B1 (ro) * 2010-10-06 2013-04-30 Oltchim S.A. Procedeu de obţinere a polieter poliolilor pe bază de sorbită
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CN102585201B (zh) * 2011-12-30 2014-04-02 高春青 一种用餐厨废弃物制备硬泡聚氨酯用多元醇的方法
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Publication number Publication date
EA034579B1 (ru) 2020-02-21
US10987429B2 (en) 2021-04-27
CN109890375B (zh) 2022-03-22
US20190255184A1 (en) 2019-08-22
JP6861424B2 (ja) 2021-04-21
EP3536315A4 (en) 2019-11-20
EP3536315A1 (en) 2019-09-11
EP3536315B1 (en) 2021-03-31
JP2020503370A (ja) 2020-01-30
WO2018084749A1 (ru) 2018-05-11
CN109890375A (zh) 2019-06-14
RU2641304C1 (ru) 2018-01-17

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