JP2005516962A5 - - Google Patents
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- Publication number
- JP2005516962A5 JP2005516962A5 JP2003556432A JP2003556432A JP2005516962A5 JP 2005516962 A5 JP2005516962 A5 JP 2005516962A5 JP 2003556432 A JP2003556432 A JP 2003556432A JP 2003556432 A JP2003556432 A JP 2003556432A JP 2005516962 A5 JP2005516962 A5 JP 2005516962A5
- Authority
- JP
- Japan
- Prior art keywords
- boc
- 4clphe
- lys
- heptapeptide
- 3pal
- 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.)
- Granted
Links
- 238000000034 method Methods 0.000 claims 16
- 125000006239 protecting group Chemical group 0.000 claims 7
- 238000004519 manufacturing process Methods 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 4
- 150000001413 amino acids Chemical class 0.000 claims 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 3
- -1 Boc group Chemical group 0.000 claims 2
- 229940124041 Luteinizing hormone releasing hormone (LHRH) antagonist Drugs 0.000 claims 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 2
- 125000002252 acyl group Chemical group 0.000 claims 2
- 238000012217 deletion Methods 0.000 claims 2
- 230000037430 deletion Effects 0.000 claims 2
- 239000002474 gonadorelin antagonist Substances 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- URKWHOVNPHQQTM-OAHLLOKOSA-N (2r)-2-[(2-methylpropan-2-yl)oxycarbonylamino]-3-naphthalen-2-ylpropanoic acid Chemical compound C1=CC=CC2=CC(C[C@@H](NC(=O)OC(C)(C)C)C(O)=O)=CC=C21 URKWHOVNPHQQTM-OAHLLOKOSA-N 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| SE0104463A SE0104463D0 (sv) | 2001-12-29 | 2001-12-29 | Mellanprodukter för syntes af LHRH-antagonister, sätt att framställa dem och sätt för framställning av LHRH-antagonister |
| PCT/IB2002/005583 WO2003055902A1 (en) | 2001-12-29 | 2002-12-23 | Intermediates for lhrh antagonist synthesis, process for their production, and process for lhrh antagonist production |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2005516962A JP2005516962A (ja) | 2005-06-09 |
| JP2005516962A5 true JP2005516962A5 (https=) | 2005-12-22 |
| JP4272529B2 JP4272529B2 (ja) | 2009-06-03 |
Family
ID=20286557
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003556432A Expired - Fee Related JP4272529B2 (ja) | 2001-12-29 | 2002-12-23 | Ｌｈｒｈ拮抗剤合成の中間体、その製造方法、およびｌｈｒｈ拮抗剤の製造方法 |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US20050124788A1 (https=) |
| EP (2) | EP1630169B1 (https=) |
| JP (1) | JP4272529B2 (https=) |
| KR (1) | KR100844520B1 (https=) |
| CN (1) | CN1304417C (https=) |
| AT (2) | ATE371666T1 (https=) |
| AU (1) | AU2002348749B2 (https=) |
| CA (1) | CA2471723C (https=) |
| CY (2) | CY1107580T1 (https=) |
| DE (2) | DE60215544T2 (https=) |
| DK (2) | DK1465917T3 (https=) |
| ES (2) | ES2296050T3 (https=) |
| IL (2) | IL162788A0 (https=) |
| NO (1) | NO330129B1 (https=) |
| NZ (1) | NZ534245A (https=) |
| PT (2) | PT1465917E (https=) |
| RU (1) | RU2307125C2 (https=) |
| SE (1) | SE0104463D0 (https=) |
| SI (1) | SI1630169T1 (https=) |
| WO (1) | WO2003055902A1 (https=) |
| ZA (1) | ZA200405136B (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4407322B2 (ja) * | 2004-03-09 | 2010-02-03 | 味の素株式会社 | ペプチドの製造方法 |
| CN101037472B (zh) * | 2006-03-14 | 2013-03-27 | 中国人民解放军军事医学科学院毒物药物研究所 | 具有低组胺释放作用的促黄体生成素释放激素拮抗剂 |
| 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 |
| PT2632934T (pt) * | 2010-10-27 | 2017-01-06 | Ferring Bv | Processo para o fabrico de degarelix e seus intermediários |
| EP2447276A1 (en) * | 2010-10-27 | 2012-05-02 | Ferring B.V. | Process for the manufacture of Degarelix and its intermediates |
| SG11201407679PA (en) | 2012-06-01 | 2014-12-30 | Ferring Bv | Manufacture of degarelix |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4098777A (en) * | 1977-03-14 | 1978-07-04 | Merck & Co., Inc. | Process for the preparation of pyroglutamyl-Ala-Lys-Ser-Gln-Gly-Gly-Ser-Asn |
| SU1623166A1 (ru) * | 1989-04-03 | 1994-02-15 | Институт биоорганической химии АН БССР | Нейтропептиды, обладающие поведенческой активностью |
| US5225598A (en) * | 1990-03-30 | 1993-07-06 | Union Carbide Chemicals & Plastics Technology Corporation | Selective production of linear pentaethylenehexamine and hydroxyethyldiethylenetriamine |
| EP0540626A1 (en) * | 1990-07-24 | 1993-05-12 | Eastman Chemical Company | Process for synthesizing peptides |
| US5710246A (en) * | 1996-03-19 | 1998-01-20 | Abbott Laboratories | Process for intermediates for the synthesis of LHRH antagonists |
| WO1998018798A1 (en) * | 1996-10-30 | 1998-05-07 | Pfizer Inc. | Pyridone-fused azabicyclic- or cytisine derivatives, their preparation and their use in addiction therapy |
| US5968895A (en) * | 1996-12-11 | 1999-10-19 | Praecis Pharmaceuticals, Inc. | Pharmaceutical formulations for sustained drug delivery |
| DE19941248A1 (de) | 1998-09-01 | 2000-03-02 | Asta Medica Ag | Peptide mit N-substituierten Glycingruppen sowie diese enthaltende Arzneimittel zur Behandlung hormonabhängiger Tumore |
-
2001
- 2001-12-29 SE SE0104463A patent/SE0104463D0/xx unknown
-
2002
- 2002-12-23 PT PT02781699T patent/PT1465917E/pt unknown
- 2002-12-23 JP JP2003556432A patent/JP4272529B2/ja not_active Expired - Fee Related
- 2002-12-23 DK DK02781699T patent/DK1465917T3/da active
- 2002-12-23 RU RU2004119964/04A patent/RU2307125C2/ru not_active IP Right Cessation
- 2002-12-23 EP EP05025717A patent/EP1630169B1/en not_active Expired - Lifetime
- 2002-12-23 PT PT05025717T patent/PT1630169E/pt unknown
- 2002-12-23 AT AT05025717T patent/ATE371666T1/de active
- 2002-12-23 ES ES05025717T patent/ES2296050T3/es not_active Expired - Lifetime
- 2002-12-23 CA CA2471723A patent/CA2471723C/en not_active Expired - Fee Related
- 2002-12-23 IL IL16278802A patent/IL162788A0/xx unknown
- 2002-12-23 EP EP02781699A patent/EP1465917B1/en not_active Expired - Lifetime
- 2002-12-23 WO PCT/IB2002/005583 patent/WO2003055902A1/en not_active Ceased
- 2002-12-23 DE DE60215544T patent/DE60215544T2/de not_active Expired - Lifetime
- 2002-12-23 AU AU2002348749A patent/AU2002348749B2/en not_active Ceased
- 2002-12-23 NZ NZ534245A patent/NZ534245A/en not_active IP Right Cessation
- 2002-12-23 DK DK05025717T patent/DK1630169T3/da active
- 2002-12-23 KR KR1020047010267A patent/KR100844520B1/ko not_active Expired - Fee Related
- 2002-12-23 CN CNB028283813A patent/CN1304417C/zh not_active Expired - Fee Related
- 2002-12-23 DE DE60222189T patent/DE60222189T2/de not_active Expired - Lifetime
- 2002-12-23 AT AT02781699T patent/ATE342913T1/de active
- 2002-12-23 US US10/500,047 patent/US20050124788A1/en not_active Abandoned
- 2002-12-23 SI SI200230642T patent/SI1630169T1/sl unknown
- 2002-12-23 ES ES02781699T patent/ES2275012T3/es not_active Expired - Lifetime
-
2004
- 2004-06-28 ZA ZA2004/05136A patent/ZA200405136B/en unknown
- 2004-06-29 IL IL162788A patent/IL162788A/en not_active IP Right Cessation
- 2004-07-16 NO NO20043047A patent/NO330129B1/no not_active IP Right Cessation
-
2007
- 2007-01-18 CY CY20071100070T patent/CY1107580T1/el unknown
- 2007-11-27 CY CY20071101513T patent/CY1107025T1/el unknown
-
2008
- 2008-08-12 US US12/189,925 patent/US8173770B2/en not_active Expired - Lifetime
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