Ferring B.v.

Polypeptide Laboratories A/s

Stefan Hansen

Jon Holbech Rasmussen

Jens Fomsgaard

Palle Hedengran Rasmussen

Wolfgang Oliver Wachs

Palle H Rasmussen

Jens Fornsgaard

Wolfgang O Wachs

Jon Holbech Rasmusse

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: (P)AA-AA-AA-AA(P)-AA-AA(P)-AA-AA(P)-AA-AA-NH(II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein Pis an amino protecting groups; preferably acetyl; Pis hydrogen or a hydroxyl protecting group, preferably a hydroxyl protecting group; Pis hydrogen or an amino protecting groups; preferably an amino protecting groups; and Pis an amino protecting group.

Process for the manufacture of degarelix and its intermediates

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): (P)AA-AA-AA-AA(P)-AA-AA(P)-AA-AA(P)-AA-AA-NH(II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein Pis an amino protecting groups; preferably acetyl; Pis hydrogen or a hydroxy! protecting group, preferably a hydroxyl protecting group; Pis hydrogen or an amino protecting groups; preferably an amino protecting groups; and Pis an amino protecting group.

Process for the manufacture of Degarelix and its intermediates

The peptides Ac-D-2Nal-D-4ClPhe-D-3Pal-OH and Boc-D-2Nal-D-4ClPhe-D-3Pal-OH are intermediates useful in the synthesis of LHRH analogs by coupling with suitable heptapeptides, in particular with the heptapeptides P-Ser(P)-MMeTry(P)-D-Lys(Nic)-Leu-Lys(iPr,P)-Pro-D-AlaNHand P-Ser(P)-NMeTry(P)-D-Asn-Leu-Lys(iPr,P)-Pro-D-AlaNH.

Intermediates for LHRH antagonist synthesis, process for the production, and process for LHRH antagonist production

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Copenhagen, Denmark

Stefan Hansen