Process for the manufacture of degarelix and its intermediates

作者: Jon Holbech Rasmussen , Palle Hedengran Rasmussen , Stefan Hansen , Wolfgang Oliver Wachs , Jens Fomsgaard

DOI:

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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. further polypeptides in solution-phase purification of Degarelix itself. can be obtained by subjecting precursor according formula (II): (P 1 )AA -AA 2 3 4 )-AA 5 6 7 8 9 10 -NH (II) or salt solvate thereof, treatment with cleaving agent an organic solvent, wherein P is amino protecting groups; preferably acetyl; hydrogen hydroxy! group, hydroxyl group; group.

参考文章(107)
Frans M J Debruyne, Gonadotropin-releasing hormone antagonist in the management of prostate cancer. Reviews in urology. ,vol. 6, ,(2004)
Ian M. Thompson, Eric J. Zeidman, Francisco R. Rodriguez, Sudden Death due to Disease Flare with Luteinizing Hormone-Releasing Hormone Agonist Therapy for Carcinoma of the Prostate Journal of Urology. ,vol. 144, pp. 1479- 1480 ,(1990) , 10.1016/S0022-5347(17)39774-4
Dieter Jocham, Christian Doehn, Martin Sommerauer, Drug evaluation: Degarelix--a potential new therapy for prostate cancer. IDrugs : the investigational drugs journal. ,vol. 9, pp. 565- 572 ,(2006)
R Persad, Leuprorelin acetate in prostate cancer: a European update. International Journal of Clinical Practice. ,vol. 56, pp. 389- 396 ,(2002)
Anders Nilsson, Guangcheng Jiang, Venkat Aravinda Potula, Atmakuri Venkata Dhanunjaya Rao, Dipak Kalita, Vikas Gajare, Mohosin Layek, Kesavan Balakumaran, Process for the manufacture of Degarelix and its intermediates ,(2011)
Bert Spilker, Guide to clinical trials ,(1991)
Morihiro Sudo, A medical instrument ,(1993)
H Lukka, T Waldron, L Klotz, E Winquist, J Trachtenberg, Genitourinary Cancer Disease Site Group of the Cancer Care Ontario Program in Evidence-Based Care, Maximal androgen blockade for the treatment of metastatic prostate cancer—a systematic review Current Oncology. ,vol. 13, pp. 81- 93 ,(2006) , 10.3747/CO.V13I3.85