公开(公告)号：EP4385517A2

公开(公告)日：2024-06-19

申请号：EP24172290.9

申请日：2013-05-31

申请人： Ferring B.V.

发明人： SCHWACH, Grégoire ,  NILSSON, Anders ,  GOTTSCHALK BOEVING, Tine Elisabeth ,  RASMUSSEN, Jon Holbech ,  MÖRNSTAM, Birgitta ,  TSIRK, Anders ,  ANNBY, Ulf ,  FOMSGAARD, Jens

IPC分类号： A61K38/09

CPC分类号： A61K38/25 ,  A61K9/0024 ,  A61K47/26 ,  A61K9/1623 ,  A61K9/19 ,  A61K38/08 ,  A61P35/00 ,  A61K47/12

摘要： The present invention provides methods for producing a lyophilized degarelix product which, upon reconstitution with water for injection in an amount of 20 mg/ml, shows a viscosity of up to 15 mPas.
The present invention also provides a lyophilized degarelix drug substance which shows, upon dissolution in water in an amount of 20 mg/ml, a viscosity of up to 3.2 mPas, and processes for providing this lyophilized degarelix drug substance.

公开(公告)号：EP4385517A3

公开(公告)日：2024-11-13

申请号：EP24172290.9

申请日：2013-05-31

申请人： Ferring B.V.

发明人： SCHWACH, Grégoire ,  NILSSON, Anders ,  GOTTSCHALK BOEVING, Tine Elisabeth ,  RASMUSSEN, Jon Holbech ,  MÖRNSTAM, Birgitta ,  TSIRK, Anders ,  ANNBY, Ulf ,  FOMSGAARD, Jens

IPC分类号： A61K38/09 ,  A61K47/12 ,  A61K9/00

摘要： The present invention provides methods for producing a lyophilized degarelix product which, upon reconstitution with water for injection in an amount of 20 mg/ml, shows a viscosity of up to 15 mPas.
The present invention also provides a lyophilized degarelix drug substance which shows, upon dissolution in water in an amount of 20 mg/ml, a viscosity of up to 3.2 mPas, and processes for providing this lyophilized degarelix drug substance.

公开(公告)号：EP2854831A2

公开(公告)日：2015-04-08

申请号：EP13726219.2

申请日：2013-05-31

申请人： Ferring B.V.

发明人： SCHWACH, Grégoire ,  NILSSON, Anders ,  GOTTSCHALK BOEVING, Tine Elisabeth ,  RASMUSSEN, Jon Holbech ,  MÖRNSTAM, Birgitta ,  TSIRK, Anders ,  ANNBY, Ulf ,  FOMSGAARD, Jens

IPC分类号： A61K38/09 ,  A61K47/12 ,  A61K9/00

CPC分类号： A61K38/08 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/1623 ,  A61K9/19 ,  A61K38/25 ,  A61K47/12 ,  A61K47/26 ,  C07K7/06

摘要： The present invention provides methods for producing a lyophilized degarelix product which, upon reconstitution with water for injection in an amount of 20 mg/ml, shows a viscosity of up to 15 mPas. The present invention also provides a lyophilized degarelix drug substance which shows, upon dissolution in water in an amount of 20 mg/ml, a viscosity of up to 3.2 mPas, and processes for providing this lyophilized degarelix drug substance.

摘要翻译： 本发明提供了制备冻干的地加瑞克产品的方法，该制剂在用20mg / ml的注射用水重建时，显示出高达15mPas的粘度。 本发明还提供一种冻干的地加瑞克氏药物，其溶解在水中的量为20mg / ml，粘度高达3.2mPas，以及提供该冻干的地加瑞克药物的方法。

公开(公告)号：EP2632935B1

公开(公告)日：2016-09-21

申请号：EP11776745.9

申请日：2011-10-26

申请人： Ferring B.V.

发明人： RASMUSSEN, Jon Holbech ,  FOMSGAARD, Jens ,  HANSEN, Stefan ,  RASMUSSEN, Palle Hedengran ,  WACHS, Wolfgang Oliver

IPC分类号： C07K5/083 ,  C07K5/087 ,  C07K5/09 ,  C07K7/23 ,  C07K1/02

CPC分类号： C07K7/06 ,  A61K38/04 ,  A61K38/08 ,  C07K1/00 ,  C07K1/02 ,  C07K1/023 ,  C07K1/026 ,  C07K1/08 ,  C07K1/10 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/0815 ,  C07K7/04 ,  C07K7/23 ,  Y02P20/55

摘要： The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula II: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ (P 1 )AA 1 -AA 2 -AA 3 -AA 4 (P 4 )-AA 5 -AA 6 (P 6 )-AA 7 -AA 8 (P 8 )-AA 9 -AA 10 -NH 2 €ƒ€ƒ€ƒ€ƒ€ƒ(II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P 1 is an amino protecting groups; preferably acetyl; P 4 is hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group; P 6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P 8 is an amino protecting group.

摘要翻译： 本发明涉及用于制备十肽Degarelix，其受保护的前体和其它有用的中间体的液体（或溶液）相制备方法。 本发明还涉及可用于溶液相制备方法和Degarelix本身纯化的多肽。 Degarelix可以通过使根据式II的Degarelix前体进行获得：€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ（P 1）AA 1 -AA 2 -AA 3 -AA 4（P 4） - AA 5 -AA 6（P 6）-AA 7 -AA 8（P 8）-AA 9 -AA 10 -NH 2€ƒ€ƒ€ƒ（II）或其盐或溶剂合物，至 在有机溶剂中用切割剂进行处理，其中P 1是氨基保护基; 优选乙酰; P 4是氢或羟基保护基，优选羟基保护基; P 6是氢或氨基保护基; 优选氨基保护基; 并且P 8是氨基保护基。

公开(公告)号：EP2632935A1

公开(公告)日：2013-09-04

申请号：EP11776745.9

申请日：2011-10-26

申请人： Ferring B.V.

发明人： RASMUSSEN, Jon Holbech ,  FOMSGAARD, Jens ,  HANSEN, Stefan ,  RASMUSSEN, Palle Hedengran ,  WACHS, Wolfgang Oliver

IPC分类号： C07K1/02 ,  C07K5/08 ,  C07K7/06

CPC分类号： C07K7/06 ,  A61K38/04 ,  A61K38/08 ,  C07K1/00 ,  C07K1/02 ,  C07K1/023 ,  C07K1/026 ,  C07K1/08 ,  C07K1/10 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/0815 ,  C07K7/04 ,  C07K7/23 ,  Y02P20/55

摘要： The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula II: €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ (P 1 )AA 1 -AA 2 -AA 3 -AA 4 (P 4 )-AA 5 -AA 6 (P 6 )-AA 7 -AA 8 (P 8 )-AA 9 -AA 10 -NH 2 €ƒ€ƒ€ƒ€ƒ€ƒ(II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P 1 is an amino protecting groups; preferably acetyl; P 4 is hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group; P 6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P 8 is an amino protecting group.

摘要翻译： 本发明涉及用于制备十肽Degarelix，其被保护的前体和其他有用的中间体的液体（或溶液）相制造方法。 本发明进一步涉及可用于溶液相制造过程和地加瑞克本身纯化的多肽。 地加瑞克可以通过使根据式（II）的地加瑞克前体进行获得：（P1） （II）化合物或其盐或溶剂化物在有机溶剂中用裂解剂处理，其中P 1是氨基保护基; 优选乙酰基; P 4是氢或羟基！ 保护基，优选羟基保护基; P 6是氢或氨基保护基; 优选氨基保护基团; P 8是氨基保护基。