BR112013010360A2 - processo para a produção de degarealix e seus intermediários - Google Patents

processo para a produção de degarealix e seus intermediários

Info

Publication number
BR112013010360A2
BR112013010360A2 BR112013010360A BR112013010360A BR112013010360A2 BR 112013010360 A2 BR112013010360 A2 BR 112013010360A2 BR 112013010360 A BR112013010360 A BR 112013010360A BR 112013010360 A BR112013010360 A BR 112013010360A BR 112013010360 A2 BR112013010360 A2 BR 112013010360A2
Authority
BR
Brazil
Prior art keywords
protecting group
degarelix
amino protecting
intermediates
production
Prior art date
Application number
BR112013010360A
Other languages
English (en)
Other versions
BR112013010360B1 (pt
Inventor
Jens Fomsgaard
Jon Holbech Rasmussen
Palle Hedengran Rasmussen
Stefan Hansen
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 BR112013010360A2 publication Critical patent/BR112013010360A2/pt
Publication of BR112013010360B1 publication Critical patent/BR112013010360B1/pt

Links

Classifications

    • 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
    • C07K7/08—Linear peptides containing only normal peptide links having 12 to 20 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
    • C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides 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
    • 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
    • C07K1/023—General 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
    • 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
    • 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
    • C07K1/06—General 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
    • C07K1/061—General 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
    • 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
    • C07K1/06—General 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
    • C07K1/08—General 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
    • 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
    • C07K1/10—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length using coupling agents
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • 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
    • C07K5/0815—Tripeptides 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
    • 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
    • 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
    • C07K7/23—Luteinising hormone-releasing hormone [LHRH]; Related peptides
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

processo para a produção de degarealix e seus intermediários. a presente invenção refere-se a um processo de produção de fase líquida (ou solução) para preparação de decapeptídeo de degarelix, seu precursor protegido, e outros intermediários últeis. a invenção adicionalmente se refere a polipeptídeos úteis no processo de produção de fase de solução, e à purificação do próprio degarelix. o degarelix pode ser obtido pela sujeição de um precursor de degarelix, de acordo com a fómula (ii): (p~1~) aa~1~-aa~2~-aa~3ãa~4~(p~4~)-aa~5~-aa~6~(p~6~)-aa~7~-aa~8~(p~8~)-aa~9~-aa~10~nh~2~(ii), ou um sal ou solvato deste, a um tratamento com um agente de clivagem em um solvente orgânico, em que p~1~é um grupo de proteção de amino; preferivelmente acetila; p~4~é hidrogênio, ou um grupo de proteção de hidroxila, preferivelmente um grupo de proteção de hidroxila; p~6~é hidrogênio, ou um grupo de proteção de amino; preferivelmente um grupo de proteção de amino; e p~8~é um grupo de proteção de amino.
BR112013010360-4A 2010-10-27 2011-10-26 Processos para produção de polipeptídeos, processos para preparar degarelix, e compostos de polipeptídeo BR112013010360B1 (pt)

Applications Claiming Priority (3)

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
EP10189032.5 2010-10-27
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
BR112013010360A2 true BR112013010360A2 (pt) 2016-08-02
BR112013010360B1 BR112013010360B1 (pt) 2023-03-21

Family

ID=43531147

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112013010360-4A BR112013010360B1 (pt) 2010-10-27 2011-10-26 Processos para produção de polipeptídeos, processos para preparar degarelix, e compostos de polipeptídeo

Country Status (26)

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

Families Citing this family (14)

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GB0117057D0 (en) * 2001-07-12 2001-09-05 Ferring Bv Pharmaceutical composition
JOP20090061B1 (ar) 2008-02-11 2021-08-17 Ferring Int Center Sa طريقة معالجة سرطان البروستاتا بمضادات الهرمونات التناسلية GnRH
BRPI1010874A8 (pt) * 2009-05-01 2018-01-02 Ferring Bv composição para o tratamento de câncer de próstata
US20110039787A1 (en) * 2009-07-06 2011-02-17 Ferring International Center S.A. Compositions, kits and methods for treating benign prostate hyperplasia
WO2012055903A1 (en) 2010-10-27 2012-05-03 Ferring B.V. Process for the manufacture of degarelix and its intermediates
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
TWI580443B (zh) * 2012-06-01 2017-05-01 菲瑞茵公司 地蓋瑞利（ｄｅｇａｒｅｌｉｘ）之製備技術
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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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
PL2632935T3 (pl) 2017-01-31
EP2632935A1 (en) 2013-09-04
KR101904808B1 (ko) 2018-10-05
SI2632935T1 (sl) 2017-01-31
US9090656B2 (en) 2015-07-28
BR112013010360B1 (pt) 2023-03-21
WO2012055905A1 (en) 2012-05-03
AU2011322618B2 (en) 2015-05-21
CN103180335A (zh) 2013-06-26
NZ609064A (en) 2015-01-30
CA2815270A1 (en) 2012-05-03
TWI515201B (zh) 2016-01-01
EP2632935B1 (en) 2016-09-21
US20130281661A1 (en) 2013-10-24
ES2606753T3 (es) 2017-03-27
KR20130127443A (ko) 2013-11-22
US20160145301A1 (en) 2016-05-26
LT2632935T (lt) 2016-10-25
ZA201302670B (en) 2015-12-23
HUE030184T2 (en) 2017-04-28
MX343058B (es) 2016-10-24
DK2632935T3 (en) 2016-11-14
JP6007187B2 (ja) 2016-10-12
HRP20161315T1 (hr) 2016-12-02
EP2447276A1 (en) 2012-05-02
RS55193B1 (sr) 2017-01-31
RU2013118446A (ru) 2014-12-10
JO3243B1 (ar) 2018-03-08
MX2013004320A (es) 2013-12-02
PT2632935T (pt) 2016-11-02
IL225687A0 (en) 2013-06-27
AU2011322618A1 (en) 2013-05-02
CN103180335B (zh) 2016-04-06
SA111320880B1 (ar) 2015-03-30
RU2602042C2 (ru) 2016-11-10
US9822146B2 (en) 2017-11-21
TW201305186A (zh) 2013-02-01
JP2013540793A (ja) 2013-11-07
IL225687A (en) 2017-06-29

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