BioLineRx has been granted a patent for a large-scale process to prepare a cyclic peptide, involving solid phase peptide synthesis, oxidation of cysteine residues, and isolation techniques. The process includes specific coupling, cleaving, and isolating steps, ensuring efficient production of the desired cyclic peptide. GlobalData’s report on BioLineRx gives a 360-degree view of the company including its patenting strategy. Buy the report here.
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According to GlobalData’s company profile on BioLineRx, Peptide pharmacophores was a key innovation area identified from patents. BioLineRx's grant share as of May 2024 was 23%. Grant share is based on the ratio of number of grants to total number of patents.
Large-scale process for preparing cyclic peptide
A recently granted patent (Publication Number: US11993631B2) outlines a large-scale process for preparing a cyclic peptide with a specific sequence ID or a pharmaceutically acceptable salt. The process involves sequentially coupling amino acids and 4-fluorobenzoic acid to a resin through solid-phase peptide synthesis, followed by cleaving the linear peptide from the resin and oxidizing cysteine residues to form an intramolecular disulfide bond, resulting in the desired cyclic peptide. Key steps include using specific reagents like diisopropylcarbodiimide (DIC) and ethyl cyanohydroxyiminoacetate/N-hydroxybenzotriazole for coupling, trifluoroacetic acid (TFA) with scavengers like dithioerythritol (DTE) or dithiothreitol (DTT) for cleaving, and hydrogen peroxide for oxidation. The process also involves isolating the cyclic peptide through reverse-phase chromatography and lyophilization, with resin specifications and post-lyophilization grinding detailed for optimal results.
Furthermore, the patent includes specific variations and concentrations for the reagents used in the process, such as a two-fold molar excess of DIC and ethyl cyanohydroxyiminoacetate/N-hydroxybenzotriazole for coupling, a scavenger concentration range of 10 mg/mL to 500 mg/mL for cleaving, and a dithiothreitol concentration of about 50 mg/mL. The process also details the precipitation of the free linear peptide without concentration by evaporation, using a mixture of tert-butyl methyl ether (MTBE) and hexane. Additionally, the isolation of the cyclic peptide on a C18 column with elution using a triethylammonium phosphate solution is specified, along with the post-lyophilization grinding step. The patent emphasizes resin specifications of at least 0.3 milliequivalents per gram and the use of a Rink aminomethylstyrene resin for optimal outcomes in the preparation of the cyclic peptide.
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GlobalData Patent Analytics tracks bibliographic data, legal events data, point in time patent ownerships, and backward and forward citations from global patenting offices. Textual analysis and official patent classifications are used to group patents into key thematic areas and link them to specific companies
