MX343058B - Proceso para la fabricacion de degarelix y sus intermedios. - Google Patents

Proceso para la fabricacion de degarelix y sus intermedios.

Info

Publication number
MX343058B
MX343058B MX2013004320A MX2013004320A MX343058B MX 343058 B MX343058 B MX 343058B MX 2013004320 A MX2013004320 A MX 2013004320A MX 2013004320 A MX2013004320 A MX 2013004320A MX 343058 B MX343058 B MX 343058B
Authority
MX
Mexico
Prior art keywords
degarelix
amino protecting
protecting group
protecting groups
hydrogen
Prior art date
Application number
MX2013004320A
Other languages
English (en)
Other versions
MX2013004320A (es
Inventor
Jon Holbech Rasmussen
Jens Fomsgaard
Stefan Hansen
Palle Hedengran Rasmussen
Wolfgang Oliver Wachs
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
Publication of MX2013004320A publication Critical patent/MX2013004320A/es
Publication of MX343058B publication Critical patent/MX343058B/es

Links

Classifications

    • 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

La presente invención se refiere a un proceso de fabricación de la fase líquida (o solución) para preparar el decapéptido Degarelix, su precursor protegido y otros productos intermedios útiles. La invención se refiere además a polipéptidos utilizados en el proceso de fabricación de la fase de solución y a la purificación de Degarelix en sí mismo. Degarelix puede obtenerse condicionando un precursor de Degarelix de acuerdo con la fórmula II: (P1) AA1-AA2 AA3-AA4 (P4) -AA5-AA6 (P6) -AA7-AA8 (P8) -AA9-AA10-NH2 (II) o una sal o solvato de la misma, a un tratamiento con un agente de escisión en un solvente Orgánico, donde P1 es un grupo protector amino; preferentemente acetilo; P4 es hidrógeno o un grupo protector hidroxilo, preferentemente un grupo protector hidroxilo; P6 es hidrógeno o un grupo protector amino; preferentemente un grupo protector amino; y P8 es un grupo protector amino.
MX2013004320A 2010-10-27 2011-10-26 Proceso para la fabricacion de degarelix y sus intermedios. MX343058B (es)

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
PCT/EP2011/068735 WO2012055905A1 (en) 2010-10-27 2011-10-26 Process for the manufacture of degarelix and its intermediates

Publications (2)

Publication Number Publication Date
MX2013004320A MX2013004320A (es) 2013-12-02
MX343058B true MX343058B (es) 2016-10-24

Family

ID=43531147

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013004320A MX343058B (es) 2010-10-27 2011-10-26 Proceso para la fabricacion de degarelix y sus intermedios.

Country Status (26)

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

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GB0117057D0 (en) * 2001-07-12 2001-09-05 Ferring Bv Pharmaceutical composition
TWI442932B (zh) 2008-02-11 2014-07-01 Ferring Int Ct Sa 以GnRH拮抗劑治療攝護腺癌的方法
CN105663059A (zh) * 2009-05-01 2016-06-15 辉凌公司 用于治疗前列腺癌的组合物
US20110039787A1 (en) * 2009-07-06 2011-02-17 Ferring International Center S.A. Compositions, kits and methods for treating benign prostate hyperplasia
RS55457B1 (sr) 2010-10-27 2017-04-28 Ferring Bv Postupak za proizvodnju degareliksa i njegovih intermedijara
EP2447276A1 (en) 2010-10-27 2012-05-02 Ferring B.V. Process for the manufacture of Degarelix and its intermediates
JO3755B1 (ar) 2011-01-26 2021-01-31 Ferring Bv تركيبات تستوستيرون
RU2657444C2 (ru) 2012-06-01 2018-06-13 Ферринг Б.В. Получение дегареликса
CN103992378A (zh) * 2013-11-01 2014-08-20 杭州诺泰制药技术有限公司 一种制备醋酸地加瑞克的方法
CN106589071B (zh) * 2016-12-12 2020-09-08 江苏诺泰澳赛诺生物制药股份有限公司 一种地加瑞克的合成方法
CN109748954B (zh) * 2017-11-06 2022-03-01 正大天晴药业集团股份有限公司 一种地加瑞克的纯化方法
CN107955061B (zh) * 2017-11-15 2021-07-30 连云港恒运药业有限公司 地加瑞克关键中间体的制备方法
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
CN110330552B (zh) * 2019-08-14 2021-03-16 凯莱英生命科学技术(天津)有限公司 醋酸地加瑞克的合成方法

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RS55457B1 (sr) 2010-10-27 2017-04-28 Ferring Bv Postupak za proizvodnju degareliksa i njegovih intermedijara
EP2447276A1 (en) 2010-10-27 2012-05-02 Ferring B.V. Process for the manufacture of Degarelix and its intermediates
JO3755B1 (ar) 2011-01-26 2021-01-31 Ferring Bv تركيبات تستوستيرون
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Also Published As

Publication number Publication date
IL225687A (en) 2017-06-29
EP2632935B1 (en) 2016-09-21
DK2632935T3 (en) 2016-11-14
JO3243B1 (ar) 2018-03-08
PT2632935T (pt) 2016-11-02
HUE030184T2 (en) 2017-04-28
ES2606753T3 (es) 2017-03-27
CA2815270A1 (en) 2012-05-03
AU2011322618B2 (en) 2015-05-21
TWI515201B (zh) 2016-01-01
SA111320880B1 (ar) 2015-03-30
US20160145301A1 (en) 2016-05-26
WO2012055905A1 (en) 2012-05-03
RS55193B1 (sr) 2017-01-31
US20130281661A1 (en) 2013-10-24
RU2602042C2 (ru) 2016-11-10
EP2632935A1 (en) 2013-09-04
CN103180335A (zh) 2013-06-26
BR112013010360A2 (pt) 2016-08-02
IL225687A0 (en) 2013-06-27
KR20130127443A (ko) 2013-11-22
US9822146B2 (en) 2017-11-21
BR112013010360B1 (pt) 2023-03-21
ZA201302670B (en) 2015-12-23
SI2632935T1 (sl) 2017-01-31
LT2632935T (lt) 2016-10-25
MX2013004320A (es) 2013-12-02
US9090656B2 (en) 2015-07-28
PL2632935T3 (pl) 2017-01-31
JP6007187B2 (ja) 2016-10-12
EP2447276A1 (en) 2012-05-02
KR101904808B1 (ko) 2018-10-05
TW201305186A (zh) 2013-02-01
HRP20161315T1 (hr) 2016-12-02
JP2013540793A (ja) 2013-11-07
AU2011322618A1 (en) 2013-05-02
NZ609064A (en) 2015-01-30
CN103180335B (zh) 2016-04-06
RU2013118446A (ru) 2014-12-10

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