Process for the preparation of Degarelix acetate and Degarelix acetate-mannitol premix

US11332495B2 · kind B2 · utility

Assignee

• RK Pharma Solutions LLC · US

Inventors

• Ravishanker Kovi · Sparta, US
• Jayaraman Kannappan · Mahesana, IN
• Sai Saisuryanarayana Donthukurthi · Sayla, IN
• Shivam Saroj · Anand, IN
• Piyush Fadadu · Vadodara, IN
• Srikrishna Apar · Aurangabad, IN
• Sandeep Aher · Aurangabad, IN
• Veerabhadra Rao Bobbili · Darsi, IN

Key dates

• Filing date: Sep 15, 2020
• Grant date: May 17, 2022
• Expiry date: Sep 15, 2040

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07K1/061
• WIPO field: Biotechnology
• WIPO sector: Chemistry

Abstract

Methods for preparing degarelix acetate are provided that include the steps of providing a suitable resin; deprotecting the resin with a diethylenetriamine solution; reacting sequentially the deprotected resin with different Fmoc protected amino acids; deprotecting the amino acid in each sequence with a diethylenetriamine solution in a stepwise fashion to yield a degarelix crude compound; and purifying the degarelix crude compound to yield pharmaceutically acceptable degarelix acetate. Methods of preparing degarelix acetate-mannitol premix and the resulting degarelix acetate-mannitol premix are also provided.