RU2017138283A - Сложные эфиры гликозаминогликана, способы их получения и их применение в композициях офтальмического назначения - Google Patents

Сложные эфиры гликозаминогликана, способы их получения и их применение в композициях офтальмического назначения Download PDF

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RU2017138283A
RU2017138283A RU2017138283A RU2017138283A RU2017138283A RU 2017138283 A RU2017138283 A RU 2017138283A RU 2017138283 A RU2017138283 A RU 2017138283A RU 2017138283 A RU2017138283 A RU 2017138283A RU 2017138283 A RU2017138283 A RU 2017138283A
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Prior art keywords
esters
glycosiminoglican
optalmic
reception
compositions
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RU2017138283A
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RU2017138283A3 (ru
RU2726192C2 (ru
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Никла БАРИКОРДИ
Роберто МЕРИГИ
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Иальблю С.Р.Л.
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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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/727—Heparin; Heparan
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/006—Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
    • C08B37/0063—Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
    • 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
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • 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
    • A61K31/715—Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
    • A61K31/726—Glycosaminoglycans, i.e. mucopolysaccharides
    • A61K31/728—Hyaluronic acid
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • 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
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/006—Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
    • C08B37/0063—Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
    • C08B37/0069—Chondroitin-4-sulfate, i.e. chondroitin sulfate A; Dermatan sulfate, i.e. chondroitin sulfate B or beta-heparin; Chondroitin-6-sulfate, i.e. chondroitin sulfate C; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/006—Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
    • C08B37/0063—Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
    • C08B37/0072—Hyaluronic acid, i.e. HA or hyaluronan; Derivatives thereof, e.g. crosslinked hyaluronic acid (hylan) or hyaluronates
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08B—POLYSACCHARIDES; DERIVATIVES THEREOF
    • C08B37/00—Preparation of polysaccharides not provided for in groups C08B1/00 - C08B35/00; Derivatives thereof
    • C08B37/006—Heteroglycans, i.e. polysaccharides having more than one sugar residue in the main chain in either alternating or less regular sequence; Gellans; Succinoglycans; Arabinogalactans; Tragacanth or gum tragacanth or traganth from Astragalus; Gum Karaya from Sterculia urens; Gum Ghatti from Anogeissus latifolia; Derivatives thereof
    • C08B37/0063—Glycosaminoglycans or mucopolysaccharides, e.g. keratan sulfate; Derivatives thereof, e.g. fucoidan
    • C08B37/0075—Heparin; Heparan sulfate; Derivatives thereof, e.g. heparosan; Purification or extraction methods thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/03—Monocarboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Biochemistry (AREA)
  • Materials Engineering (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)

Claims (5)

1. Сложные эфиры гликозаминогликана, в которых по меньшей мере часть гидроксильных групп, присутствующих на остатке N-ацетилглюкозамина, этерифицирована с апокаротиноидом, где указанный гликозаминогликан является гиалуроновой кислотой, а указанный апокаротиноид выбран из кроцетина, биксина.
2. Сложные эфиры по п. 1, в которых степень замещения апокаротиноидами в сложных эфирах составляет от 0,1 до 5%, а молекулярная масса указанных сложных эфиров составляет от 350000 до 2000000 Дальтон.
3. Сложные эфиры гликозаминогликана по п. 1 или 2, предназначенные для использования для защиты глаз от синего света.
4. Композиция для защиты глаз от синего света, содержащая по меньшей мере один сложный эфир по п. 1 или 2.
5. Композиция по п. 4, имеющая форму 0,1-1% раствора соединения в очищенной воде, необязательно в присутствии полиэтиленгликолей, бензалкония хлорида или хлоргексидина.
RU2017138283A 2015-04-07 2016-04-07 Сложные эфиры гликозаминогликана, способы их получения и их применение в композициях офтальмического назначения RU2726192C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ITFI20150102 2015-04-07
ITFI2015A000102 2015-04-07
PCT/IB2016/051960 WO2016162809A1 (en) 2015-04-07 2016-04-07 Glycosaminoglycan esters, processes for their preparation and their use in formulations for ophthalmic use

Publications (3)

Publication Number Publication Date
RU2017138283A true RU2017138283A (ru) 2019-05-07
RU2017138283A3 RU2017138283A3 (ru) 2019-09-30
RU2726192C2 RU2726192C2 (ru) 2020-07-09

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RU2017138283A RU2726192C2 (ru) 2015-04-07 2016-04-07 Сложные эфиры гликозаминогликана, способы их получения и их применение в композициях офтальмического назначения

Country Status (12)

Country Link
US (1) US10328097B2 (ru)
EP (1) EP3280396B1 (ru)
JP (1) JP6847091B2 (ru)
KR (1) KR20180002674A (ru)
CN (1) CN107636020A (ru)
AU (1) AU2016244391B2 (ru)
BR (1) BR112017021608A2 (ru)
CA (1) CA2981861A1 (ru)
ES (1) ES2888648T3 (ru)
MA (1) MA41912A (ru)
RU (1) RU2726192C2 (ru)
WO (1) WO2016162809A1 (ru)

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Publication number Priority date Publication date Assignee Title
IT202000012535A1 (it) * 2020-05-27 2021-11-27 Stefano Colombo Composizione oftalmica a base di acido ialuronico per la protezione dai danni causati dall’inquinamento ambientale
CN116284495A (zh) * 2023-03-20 2023-06-23 润辉生物技术（威海）有限公司 全反式维甲酸低分子透明质酸酯衍生物及其制备方法和应用

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4851521A (en) * 1985-07-08 1989-07-25 Fidia, S.P.A. Esters of hyaluronic acid
IT1281877B1 (it) * 1995-05-10 1998-03-03 Fidia Advanced Biopolymers Srl Sali di metalli pesanti di succinil derivati dell'acido ialuronico e loro impiego come potenziali agenti terapeutici
ITTS20010017A1 (it) * 2001-07-17 2003-01-17 Ct Ricerche Polytech Soc Coop Esteri polisaccaridici di acido retinoico.
ITMI20022745A1 (it) * 2002-12-23 2004-06-24 Coimex Scrl United Companies Esteri misti dell'acido ialuronico ad attivita' citostatica e prodifferenziante e procedimento per la loro produzione.
ITMI20030043A1 (it) 2003-01-14 2004-07-15 Coimex S C R L United Companies Uso di esteri retinoici dell'acido ialuronico in cellule
WO2005077176A1 (en) * 2004-02-11 2005-08-25 The Trustees Of Columbia University In The City Of New York Anthocyanin compounds and methods of use thereof
ITMI20040347A1 (it) * 2004-02-26 2004-05-26 Pharma Medical Ltd Nuovo farmaco di associazione
US20070207116A1 (en) * 2006-03-01 2007-09-06 Brown David C Antioxidant compositions for the eye
ITMI20062134A1 (it) * 2006-11-08 2008-05-09 Cbb Net S A Preparaziobne di esteri della diacereina con acido ialuronico e loro formulazioni per l'impiego farmaceutico
US8865685B2 (en) * 2011-06-30 2014-10-21 Johnson & Johnson Vision Care, Inc. Esters for treatment of ocular inflammatory conditions
EP2903588B1 (en) * 2012-10-02 2020-02-19 Allergan, Inc. Dermal filler hydrogels with vitamin a/cyclodextrin inclusion complexes

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Publication number Publication date
EP3280396A1 (en) 2018-02-14
RU2017138283A3 (ru) 2019-09-30
CN107636020A (zh) 2018-01-26
JP6847091B2 (ja) 2021-03-24
WO2016162809A1 (en) 2016-10-13
US10328097B2 (en) 2019-06-25
CA2981861A1 (en) 2016-10-13
AU2016244391A1 (en) 2017-11-23
RU2726192C2 (ru) 2020-07-09
US20180117077A1 (en) 2018-05-03
JP2018510962A (ja) 2018-04-19
BR112017021608A2 (pt) 2018-07-03
AU2016244391B2 (en) 2020-11-19
EP3280396B1 (en) 2021-06-23
MA41912A (fr) 2018-02-13
KR20180002674A (ko) 2018-01-08
ES2888648T3 (es) 2022-01-05

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