JP6959268B2 - 第xa因子誘導体の調製 - Google Patents

第xa因子誘導体の調製 Download PDF

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JP6959268B2
JP6959268B2 JP2018565888A JP2018565888A JP6959268B2 JP 6959268 B2 JP6959268 B2 JP 6959268B2 JP 2018565888 A JP2018565888 A JP 2018565888A JP 2018565888 A JP2018565888 A JP 2018565888A JP 6959268 B2 JP6959268 B2 JP 6959268B2
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seq
acid sequence
amino acid
polypeptide
heavy chain
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JP2019528242A5 (enExample
JP2019528242A (ja
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マーク カーバーズ,
パメラ ビー. コンリー,
ゲンミン ルー,
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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
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Application filed by 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 filed Critical 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
Publication of JP2019528242A publication Critical patent/JP2019528242A/ja
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    • 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)
    • 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
    • A61K47/16Organic 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
    • A61K9/14Particulate 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
    • 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
    • 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
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14Extraction; Separation; Purification
    • C07K1/16Extraction; Separation; Purification by chromatography
    • C07K1/18Ion-exchange chromatography
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14Extraction; Separation; Purification
    • C07K1/16Extraction; Separation; Purification by chromatography
    • C07K1/20Partition-, reverse-phase or hydrophobic interaction chromatography
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14Extraction; Separation; Purification
    • C07K1/16Extraction; Separation; Purification by chromatography
    • C07K1/22Affinity chromatography or related techniques based upon selective absorption processes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745Blood coagulation or fibrinolysis factors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Wood Science & Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Hematology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Toxicology (AREA)
  • Peptides Or Proteins (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
JP2018565888A 2016-06-17 2017-06-19 第xa因子誘導体の調製 Active JP6959268B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2021165271A JP7273918B2 (ja) 2016-06-17 2021-10-07 第xa因子誘導体の調製
JP2023074627A JP2023086970A (ja) 2016-06-17 2023-04-28 第xa因子誘導体の調製

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662351841P 2016-06-17 2016-06-17
US62/351,841 2016-06-17
PCT/US2017/038169 WO2017219034A2 (en) 2016-06-17 2017-06-19 Preparation of factor xa derivatives

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2021165271A Division JP7273918B2 (ja) 2016-06-17 2021-10-07 第xa因子誘導体の調製

Publications (3)

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JP2019528242A JP2019528242A (ja) 2019-10-10
JP2019528242A5 JP2019528242A5 (enExample) 2020-06-11
JP6959268B2 true JP6959268B2 (ja) 2021-11-02

Family

ID=60663351

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Application Number Title Priority Date Filing Date
JP2018565888A Active JP6959268B2 (ja) 2016-06-17 2017-06-19 第xa因子誘導体の調製
JP2021165271A Active JP7273918B2 (ja) 2016-06-17 2021-10-07 第xa因子誘導体の調製
JP2023074627A Pending JP2023086970A (ja) 2016-06-17 2023-04-28 第xa因子誘導体の調製

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JP2021165271A Active JP7273918B2 (ja) 2016-06-17 2021-10-07 第xa因子誘導体の調製
JP2023074627A Pending JP2023086970A (ja) 2016-06-17 2023-04-28 第xa因子誘導体の調製

Country Status (22)

Country Link
US (4) US10604748B2 (enExample)
EP (3) EP3472314B1 (enExample)
JP (3) JP6959268B2 (enExample)
KR (1) KR102373215B1 (enExample)
CN (3) CN116425860B (enExample)
AU (2) AU2017283720C1 (enExample)
CA (1) CA3027457A1 (enExample)
CL (2) CL2018003654A1 (enExample)
CO (1) CO2019000120A2 (enExample)
DK (1) DK3472314T3 (enExample)
EA (1) EA037815B1 (enExample)
ES (2) ES3038834T3 (enExample)
HU (1) HUE054597T2 (enExample)
IL (1) IL263591B2 (enExample)
MX (1) MX2018015873A (enExample)
PE (1) PE20190661A1 (enExample)
PH (1) PH12018502614A1 (enExample)
PL (1) PL3472314T3 (enExample)
PT (1) PT3472314T (enExample)
SG (1) SG11201810915QA (enExample)
SI (1) SI3472314T1 (enExample)
WO (1) WO2017219034A2 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3604510B1 (en) * 2009-03-30 2025-03-26 Alexion Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same
SG10201705189XA (en) * 2013-01-24 2017-07-28 Portola Pharm Inc INHIBITION OF TISSUE FACTOR PATHWAY INHIBITOR WITH FACTOR Xa DERIVATIVES
EP3472314B1 (en) * 2016-06-17 2021-05-05 Alexion Pharmaceuticals, Inc. Preparation of factor xa derivatives
US12195774B2 (en) 2018-06-19 2025-01-14 Alexion Pharmaceuticals, Inc. Antidotes to factor XA inhibitors
KR102337683B1 (ko) * 2018-09-21 2021-12-13 주식회사 녹십자 고효율 항-tfpi 항체 조성물

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5189019A (en) * 1990-04-23 1993-02-23 Merck & Co., Inc. Antistasin derived anticoagulant protein
US5589571A (en) * 1994-10-28 1996-12-31 Cor Therapeutics, Inc. Process for production of inhibited forms of activated blood factors
JPH1066572A (ja) * 1996-08-29 1998-03-10 Showa Sangyo Co Ltd 高純度の大豆トリプシンインヒビターの製造方法
CA2401778C (en) 2000-02-29 2010-12-21 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
PT1948608E (pt) 2005-11-08 2012-05-24 Millennium Pharm Inc Novos sais farmacêuticos e polimorfos de um inibidor do fator xa
PT3078743T (pt) * 2007-09-28 2020-07-15 Portola Pharm Inc Antídotos para inibidores do fator xa e métodos de utilização dos mesmos
US8455439B2 (en) 2008-11-14 2013-06-04 Portola Pharmaceuticals, Inc. Antidotes for factor Xa inhibitors and methods of using the same in combination with blood coagulating agents
EP3604510B1 (en) * 2009-03-30 2025-03-26 Alexion Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same
WO2011008885A1 (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
CA2876361C (en) * 2012-06-14 2020-06-30 Portola Pharmaceuticals, Inc. Method for purification of recombinant factor xa derivatives
US20140346397A1 (en) * 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
SG10201705189XA (en) 2013-01-24 2017-07-28 Portola Pharm Inc INHIBITION OF TISSUE FACTOR PATHWAY INHIBITOR WITH FACTOR Xa DERIVATIVES
KR101988705B1 (ko) * 2013-09-24 2019-06-12 화이자 인코포레이티드 재조합 인간 응고 인자 Xa 단백질의 이질적 집단을 포함하는 조성물
AU2015305413B2 (en) * 2014-08-20 2020-09-24 Alexion Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
EP3472314B1 (en) * 2016-06-17 2021-05-05 Alexion Pharmaceuticals, Inc. Preparation of factor xa derivatives

Also Published As

Publication number Publication date
JP2022000477A (ja) 2022-01-04
KR20190019134A (ko) 2019-02-26
IL263591A (en) 2019-02-03
CN118271391A (zh) 2024-07-02
EA037815B1 (ru) 2021-05-25
US11845966B2 (en) 2023-12-19
AU2023200825A1 (en) 2023-03-16
ES3038834T3 (en) 2025-10-15
WO2017219034A2 (en) 2017-12-21
PE20190661A1 (es) 2019-05-08
CN110167575B (zh) 2024-03-15
US20170369862A1 (en) 2017-12-28
CL2020001733A1 (es) 2020-09-25
AU2017283720B2 (en) 2022-11-17
EP4588932A3 (en) 2025-10-01
US10604748B2 (en) 2020-03-31
KR102373215B1 (ko) 2022-03-10
US10954504B2 (en) 2021-03-23
JP7273918B2 (ja) 2023-05-15
US20200208131A1 (en) 2020-07-02
CO2019000120A2 (es) 2019-03-29
EP3472314B1 (en) 2021-05-05
AU2017283720A1 (en) 2019-01-03
ES2875538T3 (es) 2021-11-10
HUE054597T2 (hu) 2021-09-28
PH12018502614A1 (en) 2019-09-30
CL2018003654A1 (es) 2019-01-25
CN116425860B (zh) 2025-03-04
JP2023086970A (ja) 2023-06-22
SG11201810915QA (en) 2019-01-30
IL263591B2 (en) 2023-03-01
EP3472314A2 (en) 2019-04-24
EP4588932A2 (en) 2025-07-23
CA3027457A1 (en) 2017-12-21
AU2017283720C1 (en) 2024-07-25
EA201990052A1 (ru) 2019-05-31
MX2018015873A (es) 2019-08-12
PL3472314T3 (pl) 2021-11-22
EP3926044A1 (en) 2021-12-22
IL263591B (en) 2022-11-01
CN110167575A (zh) 2019-08-23
JP2019528242A (ja) 2019-10-10
US20240076642A1 (en) 2024-03-07
US20210348149A1 (en) 2021-11-11
EP3926044B1 (en) 2025-06-04
CN116425860A (zh) 2023-07-14
BR112018075964A2 (pt) 2019-04-02
WO2017219034A3 (en) 2019-03-14
SI3472314T1 (sl) 2021-11-30
EP3472314A4 (en) 2020-01-22
DK3472314T3 (da) 2021-07-26
PT3472314T (pt) 2021-06-18

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