Kezar Life Sciences has been granted a patent for a method to prepare compound “G” and its precursors. The claim specifically focuses on the preparation of compound “D”. GlobalData’s report on Kezar Life Sciences 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 Kezar Life Sciences, Cancer treatment biomarkers was a key innovation area identified from patents. Kezar Life Sciences's grant share as of May 2024 was 29%. Grant share is based on the ratio of number of grants to total number of patents.

Method for preparing compound "g" and precursors thereof

Source: United States Patent and Trademark Office (USPTO). Credit: Kezar Life Sciences Inc

A recently granted patent (Publication Number: US11976053B2) discloses a method for preparing benzyl (2S,3R)-3-hydroxy-3-(4-methoxyphenyl)-2-((S)-2-(2-morpholinoacetamido)propanamido)propanoate, referred to as compound "D". The method involves utilizing specific aprotic solvents such as acetonitrile and dichloromethane, along with tertiary amine bases like N,N-diisopropylethylamine and coupling agents like carbodiimide reagents. The molar ratio of the coupling agent to compound B is maintained at 1 to 1, and the temperature during the mixing steps is controlled between -5°C to 5°C. Additionally, the patent covers the preparation of compound B by mixing an acid with benzyl (2S,3R)-2-((tert-butoxycarbonyl)amino)-3-hydroxy-3-(4-methoxyphenyl)propanoate.

Furthermore, the patent includes claims for various crystalline compounds, such as a crystalline form of (2S,3R)-1-(benzyloxy)-3-hydroxy-3-(4-methoxyphenyl)-1-oxopropan-2-aminium chloride salt (compound "B-Cl"), compound E, and compound F tosylate. These crystalline compounds are essential intermediates in the synthesis of the final compound "D" and play a crucial role in the overall method described in the patent. The preparation of these crystalline compounds involves specific acids like p-toluenesulfonic acid and polar, aprotic solvents including ethyl acetate and N-methyl pyrrolidone. The stirring temperature during the admixing step for compound B preparation is maintained within a range of 15°C to 25°C, ensuring the desired crystalline form is obtained. Overall, the patent provides a detailed and systematic approach to synthesizing compound "D" and its intermediates, offering valuable insights for researchers and professionals in the pharmaceutical industry.

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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