Methods for preparing tyk2 inhibitors

By optimizing the synthetic route of Tyk2 inhibitors and utilizing a combination of transition metal catalysts and ligands, the problems of low yield and unstable product quality in existing technologies have been solved, achieving efficient preparation of high-purity Tyk2 inhibitors to meet the needs of clinical trials.

CN116813561BActive Publication Date: 2026-06-16BRISTOL MYERS SQUIBB CO
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
BRISTOL MYERS SQUIBB CO
Filing Date
2018-03-29
Publication Date
2026-06-16

AI Technical Summary

⚠Technical Problem

Existing technologies for preparing Tyk2 inhibitors suffer from complex chemical steps, low yields, and unstable product quality, making it difficult to meet the needs of clinical trials.

⚗Method used

An improved synthetic route was adopted, which involved the use of specific transition metal catalysts, ligands and bases, through a series of precise chemical reaction steps to optimize the conversion process of compounds, thereby improving yield and product purity.

🎯Benefits of technology

The chemical steps were simplified, significantly improving yield and overall productivity, ensuring high quality of compound I, and making it suitable for the preparation of pharmaceutical APIs.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present invention relates to processes for the preparation of Tyk2 inhibitors. In particular, the present invention relates to improved processes for the synthesis of 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide, Compound I, which is currently in clinical trials for the treatment of autoimmune and autoinflammatory diseases such as psoriasis.
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