EA036091B1 - ВОДНЫЕ СОСТАВЫ АНТИДОТОВ ФАКТОРА Xa (fXa) ДЛЯ ПРЕДУПРЕЖДЕНИЯ ИЛИ УМЕНЬШЕНИЯ КРОВОТЕЧЕНИЯ И ИХ ПРИМЕНЕНИЕ - Google Patents

ВОДНЫЕ СОСТАВЫ АНТИДОТОВ ФАКТОРА Xa (fXa) ДЛЯ ПРЕДУПРЕЖДЕНИЯ ИЛИ УМЕНЬШЕНИЯ КРОВОТЕЧЕНИЯ И ИХ ПРИМЕНЕНИЕ Download PDF

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Publication number
EA036091B1
EA036091B1 EA201790415A EA201790415A EA036091B1 EA 036091 B1 EA036091 B1 EA 036091B1 EA 201790415 A EA201790415 A EA 201790415A EA 201790415 A EA201790415 A EA 201790415A EA 036091 B1 EA036091 B1 EA 036091B1
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EA
Eurasian Patent Office
Prior art keywords
seq
arginine
mannitol
sucrose
composition
Prior art date
Application number
EA201790415A
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English (en)
Russian (ru)
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EA201790415A1 (ru
Inventor
Дзуан Вонг
Грегори А. Сача
Фуонг М. Нгуйен
Original Assignee
Портола Фармасьютикалз, Инк.
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Application filed by Портола Фармасьютикалз, Инк. filed Critical Портола Фармасьютикалз, Инк.
Publication of EA201790415A1 publication Critical patent/EA201790415A1/ru
Publication of EA036091B1 publication Critical patent/EA036091B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/36Blood coagulation or fibrinolysis factors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46Hydrolases (3)
    • A61K38/48Hydrolases (3) acting on peptide bonds (3.4)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46Hydrolases (3)
    • A61K38/48Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/482Serine endopeptidases (3.4.21)
    • A61K38/4846Factor VII (3.4.21.21); Factor IX (3.4.21.22); Factor Xa (3.4.21.6); Factor XI (3.4.21.27); Factor XII (3.4.21.38)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic 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
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183Amino acids, e.g. glycine, EDTA or aspartame
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14Hydrolases (3)
    • C12N9/48Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424Serine endopeptidases (3.4.21)
    • C12N9/6432Coagulation factor Xa (3.4.21.6)
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12YENZYMES
    • C12Y304/00Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21Serine endopeptidases (3.4.21)
    • C12Y304/21006Coagulation factor Xa (3.4.21.6)

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
EA201790415A 2014-08-20 2015-08-20 ВОДНЫЕ СОСТАВЫ АНТИДОТОВ ФАКТОРА Xa (fXa) ДЛЯ ПРЕДУПРЕЖДЕНИЯ ИЛИ УМЕНЬШЕНИЯ КРОВОТЕЧЕНИЯ И ИХ ПРИМЕНЕНИЕ EA036091B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462039809P 2014-08-20 2014-08-20
PCT/US2015/046173 WO2016029061A1 (en) 2014-08-20 2015-08-20 Lyophilized formulations for factor xa antidote

Publications (2)

Publication Number Publication Date
EA201790415A1 EA201790415A1 (ru) 2017-08-31
EA036091B1 true EA036091B1 (ru) 2020-09-25

Family

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Family Applications (2)

Application Number Title Priority Date Filing Date
EA201790415A EA036091B1 (ru) 2014-08-20 2015-08-20 ВОДНЫЕ СОСТАВЫ АНТИДОТОВ ФАКТОРА Xa (fXa) ДЛЯ ПРЕДУПРЕЖДЕНИЯ ИЛИ УМЕНЬШЕНИЯ КРОВОТЕЧЕНИЯ И ИХ ПРИМЕНЕНИЕ
EA202091385A EA202091385A3 (ru) 2014-08-20 2015-08-20 Лиофилизированные составы для антидота фактора ха

Family Applications After (1)

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EA202091385A EA202091385A3 (ru) 2014-08-20 2015-08-20 Лиофилизированные составы для антидота фактора ха

Country Status (14)

Country Link
US (6) US20160237420A1 (https=)
EP (2) EP3750556A1 (https=)
JP (4) JP6742986B2 (https=)
KR (3) KR20250150675A (https=)
CN (2) CN113171447B (https=)
AU (3) AU2015305413B2 (https=)
CA (1) CA2961739C (https=)
DK (1) DK3182993T3 (https=)
EA (2) EA036091B1 (https=)
ES (1) ES2814157T3 (https=)
IL (2) IL250413B (https=)
SG (1) SG11201701247RA (https=)
WO (1) WO2016029061A1 (https=)
ZA (1) ZA201701764B (https=)

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PL3604510T3 (pl) * 2009-03-30 2025-07-28 Alexion Pharmaceuticals, Inc. Antidota na inhibitory czynnika xa i sposoby ich stosowania
KR20250150675A (ko) * 2014-08-20 2025-10-20 포톨라 파마슈티컬스, 인코포레이티드 인자 xa 해독제용 동결건조된 제형
CN108883160B (zh) * 2016-02-24 2022-06-28 博尔托拉制药公司 因子xa解毒剂的冻干制剂
JP6959268B2 (ja) 2016-06-17 2021-11-02 ポートラ ファーマシューティカルズ, インコーポレイテッド 第xa因子誘導体の調製
WO2018213151A1 (en) * 2017-05-18 2018-11-22 Merck Sharp & Dohme Corp. Pharmaceutical formulation comprising incretin-insulin conjugates
CN112512480B (zh) * 2018-05-21 2024-10-01 中外制药株式会社 被封入玻璃容器的冷冻干燥制剂
CN110760479A (zh) * 2019-05-17 2020-02-07 上海交通大学医学院附属瑞金医院 靶向血小板表达的凝血因子Xa及其应用

Citations (6)

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WO2000048635A1 (en) * 1999-02-22 2000-08-24 Baxter International Inc. Novel albumin-free factor viii formulations
US20040180827A1 (en) * 2003-01-08 2004-09-16 Chiron Corporation Stabilized lyophilized compositions comprising tissue factor pathway inhibitor or tissue factor pathway inhibitor variants
US20110015128A1 (en) * 2009-07-15 2011-01-20 Portola Pharmaceuticals, Inc. Unit dose formulation of antidotes for factor xa inhibitors and methods of using the same
WO2011088152A1 (en) * 2010-01-12 2011-07-21 Portola Pharmaceuticals, Inc. Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof
WO2011131720A1 (en) * 2010-04-20 2011-10-27 Octapharma Ag New stabilizing agent for pharmaceutical proteins
US20130252979A1 (en) * 2010-12-03 2013-09-26 Portola Pharmaceuticals, Inc. Pharmaceutical compositions, dosage forms and new forms of the compound of mula (i), and methods of use thereof

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CA2151044A1 (en) 1992-12-15 1994-06-23 Terence K. Brunck Novel inhibitors for factor xa
US6586574B1 (en) * 1999-08-17 2003-07-01 Nn A/S Stabilization of freeze-dried cake
AU2001250783A1 (en) 2000-02-29 2001-09-12 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
US6586584B2 (en) * 2001-01-29 2003-07-01 Becton, Dickinson And Company Sequences and methods for detection of Hepatitis C virus
NZ592533A (en) 2005-11-08 2012-08-31 Millennium Pharm Inc METHOD FOR THE PREPARATION OF N-(5-CHLORO-2-PYRIDINYL)-2-[[4-[(DIMETHYLAMINO) IMINOMETHYL] BENZOYL] AMINO]-5-METHOXY-BENZAMIDE, A FACTOR Xa INHIBITOR
US9283260B2 (en) * 2006-04-21 2016-03-15 Amgen Inc. Lyophilized therapeutic peptibody formulations
KR102069498B1 (ko) * 2007-09-28 2020-01-23 포톨라 파마슈티컬스, 인코포레이티드 인자 Xa 저해제에 대한 안티도트 및 그것을 사용하는 방법
US20110178019A1 (en) 2008-09-03 2011-07-21 Brita Rippner New protecting compositions for recombinantly produced factor viii
EP2364165B1 (en) 2008-11-14 2018-01-03 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents
PL3604510T3 (pl) * 2009-03-30 2025-07-28 Alexion Pharmaceuticals, Inc. Antidota na inhibitory czynnika xa i sposoby ich stosowania
US20120121580A1 (en) * 2009-07-28 2012-05-17 Merck Sharp & Dohme Corp. Methods for producing high concentration lyophilized pharmaceutical formulations
US9683020B2 (en) * 2011-08-01 2017-06-20 Emory University VLPS containing ligands and methods related thereto
JP6514893B2 (ja) * 2011-09-30 2019-05-15 ザ・チルドレンズ・ホスピタル・オブ・フィラデルフィアThe Children’S Hospital Of Philadelphia 止血を調節するための組成物および方法
GB201310946D0 (en) * 2013-06-19 2013-07-31 Cambridge Entpr Ltd Antidote
KR20250150675A (ko) * 2014-08-20 2025-10-20 포톨라 파마슈티컬스, 인코포레이티드 인자 xa 해독제용 동결건조된 제형

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000048635A1 (en) * 1999-02-22 2000-08-24 Baxter International Inc. Novel albumin-free factor viii formulations
US20040180827A1 (en) * 2003-01-08 2004-09-16 Chiron Corporation Stabilized lyophilized compositions comprising tissue factor pathway inhibitor or tissue factor pathway inhibitor variants
US20110015128A1 (en) * 2009-07-15 2011-01-20 Portola Pharmaceuticals, Inc. Unit dose formulation of antidotes for factor xa inhibitors and methods of using the same
WO2011088152A1 (en) * 2010-01-12 2011-07-21 Portola Pharmaceuticals, Inc. Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof
WO2011131720A1 (en) * 2010-04-20 2011-10-27 Octapharma Ag New stabilizing agent for pharmaceutical proteins
US20130252979A1 (en) * 2010-12-03 2013-09-26 Portola Pharmaceuticals, Inc. Pharmaceutical compositions, dosage forms and new forms of the compound of mula (i), and methods of use thereof

Also Published As

Publication number Publication date
DK3182993T3 (da) 2020-09-21
CN113171447B (zh) 2024-05-17
JP7416549B2 (ja) 2024-01-17
AU2015305413A1 (en) 2017-03-23
US11028382B2 (en) 2021-06-08
ZA201701764B (en) 2020-10-28
IL276960A (en) 2020-10-29
JP2017525704A (ja) 2017-09-07
AU2020289768A1 (en) 2021-01-21
JP2019206595A (ja) 2019-12-05
US20180320160A1 (en) 2018-11-08
US20250163399A1 (en) 2025-05-22
EA202091385A2 (ru) 2021-03-31
ES2814157T3 (es) 2021-03-26
JP6742986B2 (ja) 2020-08-19
IL250413B (en) 2020-09-30
KR102482517B1 (ko) 2022-12-28
IL250413A0 (en) 2017-03-30
EA201790415A1 (ru) 2017-08-31
KR20230007550A (ko) 2023-01-12
CA2961739A1 (en) 2016-02-25
JP2023158199A (ja) 2023-10-26
CN107073082A (zh) 2017-08-18
AU2020289768B2 (en) 2024-06-13
KR102867491B1 (ko) 2025-10-01
CN113171447A (zh) 2021-07-27
US20200299667A1 (en) 2020-09-24
AU2015305413B2 (en) 2020-09-24
US20210284986A1 (en) 2021-09-16
US20160237420A1 (en) 2016-08-18
WO2016029061A1 (en) 2016-02-25
CN107073082B (zh) 2021-04-30
US20200299668A1 (en) 2020-09-24
AU2024219698A1 (en) 2024-10-03
SG11201701247RA (en) 2017-03-30
JP2022003101A (ja) 2022-01-11
KR20170042776A (ko) 2017-04-19
KR20250150675A (ko) 2025-10-20
EA202091385A3 (ru) 2021-06-30
EP3750556A1 (en) 2020-12-16
CA2961739C (en) 2024-04-30
IL276960B (en) 2022-04-01
EP3182993A4 (en) 2018-01-17
EP3182993B1 (en) 2020-07-01
EP3182993A1 (en) 2017-06-28

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