ES2538828T3 - Método para la fabricación de degarelix - Google Patents
Método para la fabricación de degarelix Download PDFInfo
- Publication number
- ES2538828T3 ES2538828T3 ES10720343.2T ES10720343T ES2538828T3 ES 2538828 T3 ES2538828 T3 ES 2538828T3 ES 10720343 T ES10720343 T ES 10720343T ES 2538828 T3 ES2538828 T3 ES 2538828T3
- Authority
- ES
- Spain
- Prior art keywords
- support
- dialkylpiperidine
- 4aph
- degarelix
- weight
- Prior art date
- Legal status (The legal status 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 status listed.)
- Active
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
- C07K7/06—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
-
- 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
- A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
-
- 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
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
Abstract
Un método de fabricación de degarelix, Ac-D-2Nal-DPhe(4Cl)-D-3Pal-Ser-4Aph(Hor)-D-4Aph(Cbm)-Leu-ILys-Pro- D-Ala-NH2, en donde el degarelix comprende 0,3% en peso o menos, en particular 0,1% en peso o menos, lo más particularmente 0,01% en peso o menos, de Ac-D-2Nal-D-Phe(4Cl)-D-3Pal-Ser-X-D-4Aph(Cbm)-Leu-ILys-Pro-D-Ala- NH2, en donde X es 4-([2-(5-hidantoil)]-acetilamino)-fenilalanina, comprendiendo el método la síntesis por etapas sobre un soporte sólido que comprende un grupo amino conectado al soporte, en donde las etapas comprenden proporcionar una solución de un aminoácido o péptido del que el grupo amino en α se protege mediante Fmoc; poner en contacto el soporte con la solución en presencia de un reactivo para formar un enlace peptídico entre un grupo carboxilo del aminoácido o péptido disuelto y el grupo amino conectado al soporte durante un tiempo suficiente para formar dicho enlace peptídico; retirar el Fmoc poniendo en contacto el soporte con una base orgánica seleccionada de piperidina y piperidina sustituida con alquilo en C, en particular 2-alquilpiperidina, 3-alquilpiperidina, 2,4-dialquilpiperidina, 2,5-dialquilpiperidina, 2,6-dialquilpiperidina, en donde el alquilo es una cadena ramificada o lineal de 1 a 6 carbonos, en particular metilo o etilo, lo más particularmente metilo, en un disolvente orgánico.
Description
Claims (1)
-
imagen1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0900558 | 2009-04-24 | ||
| SE0900558 | 2009-04-24 | ||
| PCT/EP2010/002550 WO2010121835A1 (en) | 2009-04-24 | 2010-04-26 | Method for the manufacture of degarelix |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2538828T3 true ES2538828T3 (es) | 2015-06-24 |
Family
ID=42494847
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES10720343.2T Active ES2538828T3 (es) | 2009-04-24 | 2010-04-26 | Método para la fabricación de degarelix |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US8828938B2 (es) |
| EP (1) | EP2421887B1 (es) |
| JP (1) | JP5850458B2 (es) |
| KR (1) | KR101621725B1 (es) |
| CN (1) | CN102428097B (es) |
| AU (1) | AU2010241171B2 (es) |
| CA (1) | CA2759255C (es) |
| DK (1) | DK2421887T3 (es) |
| ES (1) | ES2538828T3 (es) |
| HK (1) | HK1167865A1 (es) |
| HU (1) | HUE025732T2 (es) |
| IL (1) | IL215846A (es) |
| NZ (1) | NZ595888A (es) |
| PL (1) | PL2421887T3 (es) |
| RU (1) | RU2515555C2 (es) |
| SG (1) | SG175744A1 (es) |
| WO (1) | WO2010121835A1 (es) |
| ZA (1) | ZA201107709B (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2011066386A1 (en) | 2009-11-25 | 2011-06-03 | Novetide, Ltd. | Process for production of degarelix |
| EP2447276A1 (en) * | 2010-10-27 | 2012-05-02 | Ferring B.V. | Process for the manufacture of Degarelix and its intermediates |
| ES2617336T3 (es) * | 2010-10-27 | 2017-06-16 | Ferring B.V. | Procedimiento para la fabricación de degarelix y sus productos intermedios |
| CN102329373B (zh) * | 2011-09-29 | 2014-10-22 | 深圳翰宇药业股份有限公司 | 地加瑞克的固相合成工艺 |
| AR092840A1 (es) * | 2012-06-01 | 2015-05-06 | Ferring Bv | Elaboracion de degarelix |
| CN102952174A (zh) * | 2012-11-16 | 2013-03-06 | 济南环肽医药科技有限公司 | 一种地加瑞克的合成方法 |
| CN103351428B (zh) * | 2013-08-05 | 2016-09-07 | 海南双成药业股份有限公司 | 一种固相片段法合成地加瑞克 |
| CN103992392B (zh) * | 2014-05-19 | 2017-05-31 | 泰州启瑞医药科技有限公司 | 一种地加瑞克的固相合成方法 |
| CN104177478B (zh) * | 2014-08-27 | 2018-04-03 | 成都圣诺生物制药有限公司 | 一种合成地加瑞克的方法 |
| CN104292394B (zh) * | 2014-09-19 | 2017-02-08 | 深圳微球科技有限公司 | 一种Rink酰胺树脂的制备方法 |
| CN105085634A (zh) * | 2015-08-29 | 2015-11-25 | 中肽生化有限公司 | 一种地加瑞克的制备方法 |
| DK3390427T3 (da) | 2015-12-17 | 2021-09-27 | Fresenius Kabi Ipsum S R L | Fremgangsmåde til fremstilling af degarelix og dets mellemprodukter |
| CN105524143B (zh) * | 2016-03-10 | 2019-01-22 | 成都圣诺生物制药有限公司 | 一种合成地加瑞克的方法 |
| CN109929012B (zh) * | 2017-12-15 | 2023-07-28 | 连云港恒运药业有限公司 | 地加瑞克关键四肽中间体的制备方法 |
| CN109575109B (zh) * | 2018-12-27 | 2022-03-25 | 兰州大学 | 片段缩合制备地加瑞克的方法 |
| US20220177521A1 (en) | 2019-03-07 | 2022-06-09 | Fresenius Kabi Ipsum S.R.L. | Process for the preparation of degarelix |
| US11332495B2 (en) | 2019-09-21 | 2022-05-17 | RK Pharma Solutions LLC | Process for the preparation of Degarelix acetate and Degarelix acetate-mannitol premix |
| CA3159716A1 (en) * | 2019-12-05 | 2021-06-10 | Fresenius Kabi Usa, Llc | Method for analyzing degarelix and associated products |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5925730A (en) * | 1997-04-11 | 1999-07-20 | Ferring Bv | GnRH antagonists |
| GB0307777D0 (en) * | 2003-04-04 | 2003-05-07 | Medical Res Council | Conjugate compounds |
| US7968080B2 (en) * | 2003-08-20 | 2011-06-28 | The Regents Of The University Of California | Somatostatin analogs with inhibitory activity to growth hormone release |
-
2010
- 2010-04-26 WO PCT/EP2010/002550 patent/WO2010121835A1/en active Application Filing
- 2010-04-26 ES ES10720343.2T patent/ES2538828T3/es active Active
- 2010-04-26 CA CA2759255A patent/CA2759255C/en active Active
- 2010-04-26 PL PL10720343T patent/PL2421887T3/pl unknown
- 2010-04-26 AU AU2010241171A patent/AU2010241171B2/en active Active
- 2010-04-26 SG SG2011076296A patent/SG175744A1/en unknown
- 2010-04-26 DK DK10720343.2T patent/DK2421887T3/en active
- 2010-04-26 CN CN201080018334.1A patent/CN102428097B/zh active Active
- 2010-04-26 KR KR1020117027921A patent/KR101621725B1/ko active IP Right Grant
- 2010-04-26 EP EP10720343.2A patent/EP2421887B1/en not_active Revoked
- 2010-04-26 US US13/265,402 patent/US8828938B2/en active Active
- 2010-04-26 HU HUE10720343A patent/HUE025732T2/en unknown
- 2010-04-26 NZ NZ595888A patent/NZ595888A/xx unknown
- 2010-04-26 RU RU2011142266/04A patent/RU2515555C2/ru active
- 2010-04-26 JP JP2012506406A patent/JP5850458B2/ja active Active
-
2011
- 2011-10-20 ZA ZA2011/07709A patent/ZA201107709B/en unknown
- 2011-10-23 IL IL215846A patent/IL215846A/en active IP Right Grant
-
2012
- 2012-08-30 HK HK12108504.8A patent/HK1167865A1/xx unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR101621725B1 (ko) | 2016-05-17 |
| NZ595888A (en) | 2013-05-31 |
| AU2010241171A1 (en) | 2011-11-10 |
| HK1167865A1 (en) | 2012-12-14 |
| EP2421887A1 (en) | 2012-02-29 |
| HUE025732T2 (en) | 2016-04-28 |
| SG175744A1 (en) | 2011-12-29 |
| DK2421887T3 (en) | 2015-07-27 |
| PL2421887T3 (pl) | 2015-11-30 |
| EP2421887B1 (en) | 2015-04-22 |
| WO2010121835A1 (en) | 2010-10-28 |
| ZA201107709B (en) | 2012-06-27 |
| JP2012529425A (ja) | 2012-11-22 |
| RU2515555C2 (ru) | 2014-05-10 |
| JP5850458B2 (ja) | 2016-02-03 |
| CA2759255A1 (en) | 2010-10-28 |
| IL215846A (en) | 2016-07-31 |
| CN102428097B (zh) | 2014-10-29 |
| CA2759255C (en) | 2018-03-27 |
| KR20120030385A (ko) | 2012-03-28 |
| RU2011142266A (ru) | 2013-05-27 |
| IL215846A0 (en) | 2012-01-31 |
| AU2010241171B2 (en) | 2014-01-09 |
| US8828938B2 (en) | 2014-09-09 |
| CN102428097A (zh) | 2012-04-25 |
| US20120041172A1 (en) | 2012-02-16 |
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