AU2016238233B2 - Solution phase method for preparing etelcalcetide - Google Patents

Solution phase method for preparing etelcalcetide Download PDF

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Publication number
AU2016238233B2
AU2016238233B2 AU2016238233A AU2016238233A AU2016238233B2 AU 2016238233 B2 AU2016238233 B2 AU 2016238233B2 AU 2016238233 A AU2016238233 A AU 2016238233A AU 2016238233 A AU2016238233 A AU 2016238233A AU 2016238233 B2 AU2016238233 B2 AU 2016238233B2
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Australia
Prior art keywords
etelcalcetide
protected
arg
ala
coupling
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Active
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AU2016238233A
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English (en)
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AU2016238233A1 (en
Inventor
Ying Chen
Richard Crockett
Kevin CROSSLEY
Sheng CUI
Karel DECROOS
Etienne MONIOTTE
Krishnakumar Ranganathan
Yun SHI
Aleksander Swietlow
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Amgen Inc
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Amgen Inc
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Publication of AU2016238233A1 publication Critical patent/AU2016238233A1/en
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Publication of AU2016238233B2 publication Critical patent/AU2016238233B2/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
    • C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • C07K1/026—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution by fragment condensation in solution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid hormones
    • A61P5/20—Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
    • 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
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1019—Tetrapeptides with the first amino acid being basic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Endocrinology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Analytical Chemistry (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2016238233A 2015-03-26 2016-03-25 Solution phase method for preparing etelcalcetide Active AU2016238233B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562138903P 2015-03-26 2015-03-26
US62/138,903 2015-03-26
PCT/US2016/024308 WO2016154580A1 (en) 2015-03-26 2016-03-25 Solution phase method for preparing etelcalcetide

Publications (2)

Publication Number Publication Date
AU2016238233A1 AU2016238233A1 (en) 2017-10-19
AU2016238233B2 true AU2016238233B2 (en) 2019-11-21

Family

ID=55911037

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2016238233A Active AU2016238233B2 (en) 2015-03-26 2016-03-25 Solution phase method for preparing etelcalcetide

Country Status (7)

Country Link
US (1) US10858389B2 (enExample)
EP (1) EP3274360B1 (enExample)
JP (1) JP6783787B2 (enExample)
AU (1) AU2016238233B2 (enExample)
CA (1) CA2980960C (enExample)
ES (1) ES2806200T3 (enExample)
WO (1) WO2016154580A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10858389B2 (en) 2015-03-26 2020-12-08 Amgen Inc. Solution phase method for preparing etelcalcetide
CN106928321B (zh) * 2015-12-31 2019-07-26 深圳翰宇药业股份有限公司 一种合成Etelcalcetide的方法
CN108101959B (zh) * 2016-11-24 2021-07-09 四川科伦药物研究院有限公司 一种制备高纯度多肽或其类似物的方法
CN106967155B (zh) * 2017-03-17 2018-05-15 兰州凯博药业股份有限公司 一种多肽液相合成缩宫素的方法
CN110498835B (zh) * 2018-05-17 2021-06-08 深圳翰宇药业股份有限公司 一种合成etelcalcetide的方法
EP3613757A1 (en) 2018-08-20 2020-02-26 Wntresearch AB Solution phase routes for wnt hexapeptides
CN109280078B (zh) * 2018-10-30 2019-06-25 成都诺和晟泰生物科技有限公司 一种制备维拉卡肽的方法
CN109734778A (zh) * 2019-03-07 2019-05-10 苏州科技大学 一种维拉卡肽的制备方法
CN112175042B (zh) * 2019-07-03 2022-05-31 深圳翰宇药业股份有限公司 Etelcalcetide的合成方法
EP4021920A4 (en) * 2019-08-26 2023-08-16 Auro Peptides LTD IMPROVED PROCESS FOR PRODUCTION OF ETELCALCETIDE HYDROCHLORIDE
CN112521450A (zh) * 2019-09-19 2021-03-19 深圳市健翔生物制药有限公司 一种固液相结合制备维拉卡肽的方法
CN110668984B (zh) * 2019-12-03 2020-04-10 凯莱英医药集团（天津）股份有限公司 一种依特卡肽中间体及依特卡肽的合成方法
CN111925415A (zh) * 2020-08-10 2020-11-13 海南中和药业股份有限公司 一种维拉卡肽杂质的制备方法
US20230331778A1 (en) 2020-08-31 2023-10-19 Usv Private Limited An improved process for fmoc synthesis of etelcalcetide

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011014707A2 (en) * 2009-07-29 2011-02-03 Kai Pharmaceuticals, Inc. Therapeutic agents for reducing parathyroid hormone levels
WO2014210489A1 (en) * 2013-06-28 2014-12-31 Amgen Inc. Stable liquid formulation of amg 416 (velcalcetide)

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001005757A2 (en) 1999-07-19 2001-01-25 Nycomed Imaging As Process for the deprotection of protected thiols
US9409946B2 (en) 2008-06-17 2016-08-09 Peptisyntha Peptide manufacturing process
US8987377B2 (en) 2010-11-19 2015-03-24 Alnylam Pharmaceuticals, Inc. Poly(amide) polymers for the delivery of oligonucleotides
US10858389B2 (en) 2015-03-26 2020-12-08 Amgen Inc. Solution phase method for preparing etelcalcetide

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011014707A2 (en) * 2009-07-29 2011-02-03 Kai Pharmaceuticals, Inc. Therapeutic agents for reducing parathyroid hormone levels
WO2014210489A1 (en) * 2013-06-28 2014-12-31 Amgen Inc. Stable liquid formulation of amg 416 (velcalcetide)

Also Published As

Publication number Publication date
JP2018512415A (ja) 2018-05-17
WO2016154580A1 (en) 2016-09-29
JP6783787B2 (ja) 2020-11-11
EP3274360A1 (en) 2018-01-31
US10858389B2 (en) 2020-12-08
AU2016238233A1 (en) 2017-10-19
CA2980960C (en) 2024-05-28
EP3274360B1 (en) 2020-05-06
US20180079777A1 (en) 2018-03-22
CA2980960A1 (en) 2016-09-29
ES2806200T3 (es) 2021-02-16

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