JO3243B1 - عملية لتصنيع الديغارليكس ومركباته الوسيطة - Google Patents

عملية لتصنيع الديغارليكس ومركباته الوسيطة

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Publication number
JO3243B1
JO3243B1 JOP/2011/0318A JOP20110318A JO3243B1 JO 3243 B1 JO3243 B1 JO 3243B1 JO P20110318 A JOP20110318 A JO P20110318A JO 3243 B1 JO3243 B1 JO 3243B1
Authority
JO
Jordan
Prior art keywords
degarelix
amino protecting
protecting group
protecting groups
hydrogen
Prior art date
Application number
JOP/2011/0318A
Other languages
English (en)
Inventor
Hedengran Rasmussen Palle
Holbech Rasmussen Jon
Fomsgaard Jens
Hansen Stefan
Oliver Wachs Wolfgang
Original Assignee
Ferring Bv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ferring Bv filed Critical Ferring Bv
Application granted granted Critical
Publication of JO3243B1 publication Critical patent/JO3243B1/ar

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/08Linear peptides containing only normal peptide links having 12 to 20 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • 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
    • 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
    • C07K1/02General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • 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
    • C07K1/02General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • C07K1/023General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution using racemisation inhibiting 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
    • C07K1/02General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • C07K1/026General 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
    • 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
    • C07K1/06General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • C07K1/061General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents using protecting groups
    • 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
    • C07K1/06General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents
    • C07K1/08General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using protecting groups or activating agents using activating 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
    • C07K1/10General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using coupling agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0812Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0815Tripeptides with the first amino acid being basic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/23Luteinising hormone-releasing hormone [LHRH]; Related peptides
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Analytical Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Peptides Or Proteins (AREA)
  • Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

يتعلق الاختراع الحالي بعملية تصنيع في الطور السائل (أو محلول) لتحضير الديكا ببتيد دِجاريليكس، والمادة المُنتجة المحمية الخاصة به، ومركبات وسيطة أخرى مفيدة. يتعلق الاختراع أيضاً ببولي ببتيدات مفيدة في عملية التصنيع في الطور السائل وبتنقية الدِجاريليكس نفسه. يمكن الحصول على الدِجاريليكس بواسطة إخضاع مادة منتجة للدِجاريليكس وفقاً للصيغة II: أو ملح أو ذوابة منه، إلى عملية معالجة بعامل انشطار في مذيب عضوي، حيث تكونP1 عبارة عن مجموعات حماية من الأمينو؛ يفضل الأسيتيل؛ تكون P4 عبارة عن مجموعات حماية من الهيدروجين أو الهيدروكسيل، يفضل مجموعة حماية من الهيدروكسيل؛ تكون P6 عبارة عن مجموعات حماية من الهيدروجين أو الأمينو؛ يفضل مجموعات حماية من الأمينو؛ وتكون P8 عبارة عن مجموعة حماية من الأمينو.
JOP/2011/0318A 2010-10-27 2011-10-24 عملية لتصنيع الديغارليكس ومركباته الوسيطة JO3243B1 (ar)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP10189032A EP2447276A1 (en) 2010-10-27 2010-10-27 Process for the manufacture of Degarelix and its intermediates
US40930410P 2010-11-02 2010-11-02

Publications (1)

Publication Number Publication Date
JO3243B1 true JO3243B1 (ar) 2018-03-08

Family

ID=43531147

Family Applications (1)

Application Number Title Priority Date Filing Date
JOP/2011/0318A JO3243B1 (ar) 2010-10-27 2011-10-24 عملية لتصنيع الديغارليكس ومركباته الوسيطة

Country Status (26)

Country Link
US (2) US9090656B2 (ar)
EP (2) EP2447276A1 (ar)
JP (1) JP6007187B2 (ar)
KR (1) KR101904808B1 (ar)
CN (1) CN103180335B (ar)
AU (1) AU2011322618B2 (ar)
BR (1) BR112013010360B1 (ar)
CA (1) CA2815270A1 (ar)
DK (1) DK2632935T3 (ar)
ES (1) ES2606753T3 (ar)
HR (1) HRP20161315T1 (ar)
HU (1) HUE030184T2 (ar)
IL (1) IL225687A (ar)
JO (1) JO3243B1 (ar)
LT (1) LT2632935T (ar)
MX (1) MX343058B (ar)
NZ (1) NZ609064A (ar)
PL (1) PL2632935T3 (ar)
PT (1) PT2632935T (ar)
RS (1) RS55193B1 (ar)
RU (1) RU2602042C2 (ar)
SA (1) SA111320880B1 (ar)
SI (1) SI2632935T1 (ar)
TW (1) TWI515201B (ar)
WO (1) WO2012055905A1 (ar)
ZA (1) ZA201302670B (ar)

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EP2447276A1 (en) 2010-10-27 2012-05-02 Ferring B.V. Process for the manufacture of Degarelix and its intermediates
PT2632934T (pt) 2010-10-27 2017-01-06 Ferring Bv Processo para o fabrico de degarelix e seus intermediários
JO3755B1 (ar) 2011-01-26 2021-01-31 Ferring Bv تركيبات تستوستيرون
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CN109929007B (zh) * 2017-12-15 2023-07-28 连云港恒运药业有限公司 地加瑞克关键二肽中间体的制备方法
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PT2632934T (pt) 2010-10-27 2017-01-06 Ferring Bv Processo para o fabrico de degarelix e seus intermediários
JO3755B1 (ar) 2011-01-26 2021-01-31 Ferring Bv تركيبات تستوستيرون
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Also Published As

Publication number Publication date
HUE030184T2 (en) 2017-04-28
ZA201302670B (en) 2015-12-23
JP6007187B2 (ja) 2016-10-12
RS55193B1 (sr) 2017-01-31
IL225687A (en) 2017-06-29
DK2632935T3 (en) 2016-11-14
KR20130127443A (ko) 2013-11-22
US9822146B2 (en) 2017-11-21
CN103180335A (zh) 2013-06-26
MX343058B (es) 2016-10-24
EP2447276A1 (en) 2012-05-02
BR112013010360B1 (pt) 2023-03-21
MX2013004320A (es) 2013-12-02
SI2632935T1 (sl) 2017-01-31
JP2013540793A (ja) 2013-11-07
PL2632935T3 (pl) 2017-01-31
EP2632935B1 (en) 2016-09-21
WO2012055905A1 (en) 2012-05-03
US20130281661A1 (en) 2013-10-24
HRP20161315T1 (hr) 2016-12-02
IL225687A0 (en) 2013-06-27
NZ609064A (en) 2015-01-30
LT2632935T (lt) 2016-10-25
TWI515201B (zh) 2016-01-01
CN103180335B (zh) 2016-04-06
ES2606753T3 (es) 2017-03-27
PT2632935T (pt) 2016-11-02
BR112013010360A2 (pt) 2016-08-02
RU2602042C2 (ru) 2016-11-10
TW201305186A (zh) 2013-02-01
SA111320880B1 (ar) 2015-03-30
EP2632935A1 (en) 2013-09-04
CA2815270A1 (en) 2012-05-03
AU2011322618A1 (en) 2013-05-02
US20160145301A1 (en) 2016-05-26
KR101904808B1 (ko) 2018-10-05
US9090656B2 (en) 2015-07-28
AU2011322618B2 (en) 2015-05-21
RU2013118446A (ru) 2014-12-10

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