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AssigneeFerring B.V.
InventorsJon Holbech Rasmussen, Jens Fomsgaard, Stefan Hansen, Palle Hedengran Rasmussen, Wolfgang Oliver Wachs
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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): (P1)AA1-AA2-AA3-AA4(P4)-AA5-AA6(P6)-AA7-AA8(P8)-AA9-AA10-NH2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P1 is an amino protecting groups; preferably acetyl; P4 is hydrogen or a hydroxy! protecting group, preferably a hydroxyl protecting group; P6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P8 is an amino protecting group.
A process for preparing Degarelix having the formula Ac-AA1-AA10-NH2 or a pharmaceutically acceptable salt or solvate thereof, wherein AA1 is D-2Nal, AA2 is D-4Cpa, AA3 is D-3Pal, AA4 is Ser, AA5 is 4Aph(L-Hor), AA6 is D-Aph(Cbm), AA7 is Leu, AA8 is Lys(iPr), AA9 is Pro and AA10 is D-Ala, comprising:
A process for the manufacture of a decapeptide represented by formula (II)
A process for preparing a polypeptide represented by formula (IV):
A process for producing a compound of (PN)AA4(P4)-AA5-AA6(P6)-AA7, wherein AA4 is Ser, AA5 is 4Aph(L-Hor), AA6 is D-Aph(Cbm), AA7 is Leu, P4 is chosen from hydrogen and a hydroxyl protecting group, P6 is chosen from hydrogen and an amino protecting group, and PN is a protecting group that can be removed by hydrogenation, comprising the following steps:
Polypeptide compounds represented by the following formulae:
Dependencies are inferred from the claim text.