CN110167575B - 因子xa衍生物的制备 - Google Patents

因子xa衍生物的制备 Download PDF

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Publication number
CN110167575B
CN110167575B CN201780041530.2A CN201780041530A CN110167575B CN 110167575 B CN110167575 B CN 110167575B CN 201780041530 A CN201780041530 A CN 201780041530A CN 110167575 B CN110167575 B CN 110167575B
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gly
glu
lys
thr
seq
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English (en)
Chinese (zh)
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CN110167575A (zh
Inventor
马克·卡巴兹
帕梅拉·B·康利
卢根民
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Alexion Pharmaceuticals Inc
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Alexion Pharmaceuticals Inc
Portola Pharmaceuticals LLC
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Application filed by Alexion Pharmaceuticals Inc, Portola Pharmaceuticals LLC filed Critical Alexion Pharmaceuticals Inc
Priority to CN202310427500.2A priority Critical patent/CN116425860B/zh
Priority to CN202410192888.7A priority patent/CN118271391A/zh
Publication of CN110167575A publication Critical patent/CN110167575A/zh
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/482—Serine endopeptidases (3.4.21)
    • A61K38/4846—Factor 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)
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14—Extraction; Separation; Purification
    • C07K1/16—Extraction; Separation; Purification by chromatography
    • C07K1/18—Ion-exchange chromatography
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14—Extraction; Separation; Purification
    • C07K1/16—Extraction; Separation; Purification by chromatography
    • C07K1/20—Partition-, reverse-phase or hydrophobic interaction chromatography
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/14—Extraction; Separation; Purification
    • C07K1/16—Extraction; Separation; Purification by chromatography
    • C07K1/22—Affinity chromatography or related techniques based upon selective absorption processes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/745—Blood coagulation or fibrinolysis factors
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6432—Coagulation factor Xa (3.4.21.6)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Zoology (AREA)
  • Biomedical Technology (AREA)
  • Wood Science & Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (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)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201780041530.2A 2016-06-17 2017-06-19 因子xa衍生物的制备 Active CN110167575B (zh)

Priority Applications (2)

Application Number Priority Date Filing Date Title
CN202310427500.2A CN116425860B (zh) 2016-06-17 2017-06-19 因子xa衍生物的制备
CN202410192888.7A CN118271391A (zh) 2016-06-17 2017-06-19 因子xa衍生物的制备

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 (2)

Application Number Title Priority Date Filing Date
CN202410192888.7A Division CN118271391A (zh) 2016-06-17 2017-06-19 因子xa衍生物的制备
CN202310427500.2A Division CN116425860B (zh) 2016-06-17 2017-06-19 因子xa衍生物的制备

Publications (2)

Publication Number Publication Date
CN110167575A CN110167575A (zh) 2019-08-23
CN110167575B true CN110167575B (zh) 2024-03-15

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CN201780041530.2A Active CN110167575B (zh) 2016-06-17 2017-06-19 因子xa衍生物的制备
CN202310427500.2A Active CN116425860B (zh) 2016-06-17 2017-06-19 因子xa衍生物的制备
CN202410192888.7A Pending CN118271391A (zh) 2016-06-17 2017-06-19 因子xa衍生物的制备

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CN202410192888.7A Pending CN118271391A (zh) 2016-06-17 2017-06-19 因子xa衍生物的制备

Country Status (21)

Country Link
US (4) US10604748B2 (enExample)
EP (3) EP3926044B1 (enExample)
JP (4) JP6959268B2 (enExample)
KR (1) KR102373215B1 (enExample)
CN (3) CN110167575B (enExample)
AU (3) AU2017283720C1 (enExample)
CL (2) CL2018003654A1 (enExample)
CO (1) CO2019000120A2 (enExample)
DK (1) DK3472314T3 (enExample)
EA (1) EA037815B1 (enExample)
ES (2) ES2875538T3 (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
PL3604510T3 (pl) * 2009-03-30 2025-07-28 Alexion Pharmaceuticals, Inc. Antidota na inhibitory czynnika xa i sposoby ich stosowania
EP2948168B1 (en) * 2013-01-24 2018-07-18 Portola Pharmaceuticals, Inc. Inhibition of tissue factor pathway inhibitor with factor xa derivatives
EP3926044B1 (en) * 2016-06-17 2025-06-04 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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101802188A (zh) * 2007-09-28 2010-08-11 普托拉制药有限公司 用于因子xa抑制剂的解毒剂和其使用方法
US20140346397A1 (en) * 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases
CN104379594A (zh) * 2012-06-14 2015-02-25 博尔托拉制药公司 用于纯化重组因子Xa衍生物的方法

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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
WO2001064642A2 (en) 2000-02-29 2001-09-07 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor xa
CN101304971B (zh) 2005-11-08 2011-09-07 米伦纽姆医药公司 Xa因子抑制剂n-(5-氯-2-吡啶基)-2-[[4-[(二甲氨基)亚氨基甲基]苯甲酰基]氨基]-5-甲氧基-苯甲酰胺的医药盐和多晶型
CA2743496C (en) 2008-11-14 2018-03-27 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
EP2453910B1 (en) 2009-07-15 2016-08-31 Portola Pharmaceuticals, Inc. Unit dose formulation of antidote for factor xa inhibitors for use in preventing bleeding
EP2948168B1 (en) * 2013-01-24 2018-07-18 Portola Pharmaceuticals, Inc. Inhibition of tissue factor pathway inhibitor with factor xa derivatives
CN112195169A (zh) * 2013-09-24 2021-01-08 辉瑞大药厂 包含重组人凝血因子Xa蛋白的异质性群体的组合物
KR20250150675A (ko) * 2014-08-20 2025-10-20 포톨라 파마슈티컬스, 인코포레이티드 인자 xa 해독제용 동결건조된 제형
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Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
CN101802188A (zh) * 2007-09-28 2010-08-11 普托拉制药有限公司 用于因子xa抑制剂的解毒剂和其使用方法
CN104379594A (zh) * 2012-06-14 2015-02-25 博尔托拉制药公司 用于纯化重组因子Xa衍生物的方法
US20140346397A1 (en) * 2012-12-27 2014-11-27 Portola Pharmaceuticals, Inc. Compounds and methods for purification of serine proteases

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Hydroxyapatite Chromatography: Purification Strategies for Recombinant Proteins;Cummings et al.;《Methods in Enzymology》;20141231;第541卷;第67-83页 *
Manufacturing process used to produce long-acting recombinant factor VIII Fc fusion protein;McCue et al.;《Biologicals》;20150617;第213-219页 *
Purification of factor X by hydrophobic interaction chromatography;Husi et al.;《Journal of Chromatography B》;20011231;摘要和材料与方法部分 *

Also Published As

Publication number Publication date
MX2018015873A (es) 2019-08-12
CN116425860A (zh) 2023-07-14
CL2018003654A1 (es) 2019-01-25
JP6959268B2 (ja) 2021-11-02
DK3472314T3 (da) 2021-07-26
PE20190661A1 (es) 2019-05-08
JP2026010692A (ja) 2026-01-22
JP7273918B2 (ja) 2023-05-15
PH12018502614A1 (en) 2019-09-30
IL263591B (en) 2022-11-01
EA201990052A1 (ru) 2019-05-31
JP2019528242A (ja) 2019-10-10
US20200208131A1 (en) 2020-07-02
WO2017219034A2 (en) 2017-12-21
US20240076642A1 (en) 2024-03-07
JP2022000477A (ja) 2022-01-04
WO2017219034A3 (en) 2019-03-14
HUE054597T2 (hu) 2021-09-28
KR20190019134A (ko) 2019-02-26
CO2019000120A2 (es) 2019-03-29
ES3038834T3 (en) 2025-10-15
EP3472314A2 (en) 2019-04-24
CN116425860B (zh) 2025-03-04
CN118271391A (zh) 2024-07-02
IL263591A (en) 2019-02-03
PL3472314T3 (pl) 2021-11-22
CA3027457A1 (en) 2017-12-21
US11845966B2 (en) 2023-12-19
IL263591B2 (en) 2023-03-01
CN110167575A (zh) 2019-08-23
CL2020001733A1 (es) 2020-09-25
SG11201810915QA (en) 2019-01-30
JP2023086970A (ja) 2023-06-22
PT3472314T (pt) 2021-06-18
AU2017283720A1 (en) 2019-01-03
EP4588932A3 (en) 2025-10-01
KR102373215B1 (ko) 2022-03-10
US20170369862A1 (en) 2017-12-28
EP3926044A1 (en) 2021-12-22
SI3472314T1 (sl) 2021-11-30
EP4588932A2 (en) 2025-07-23
AU2023200825A1 (en) 2023-03-16
EP3472314A4 (en) 2020-01-22
US10954504B2 (en) 2021-03-23
EP3926044B1 (en) 2025-06-04
EA037815B1 (ru) 2021-05-25
AU2017283720C1 (en) 2024-07-25
US20210348149A1 (en) 2021-11-11
EP3472314B1 (en) 2021-05-05
ES2875538T3 (es) 2021-11-10
AU2026206233A1 (en) 2026-08-13
AU2023200825B2 (en) 2026-04-23
BR112018075964A2 (pt) 2019-04-02
AU2017283720B2 (en) 2022-11-17
US10604748B2 (en) 2020-03-31

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