Inhibitors of bruton's tyrosine kinase

Irreversible Btk inhibitors forming covalent bonds with cysteine or serine residues effectively target Btk and its homologs, overcoming resistance and providing sustained inhibition for treating autoimmune diseases, cancers, and inflammatory conditions.

US20170015671A1Inactive Publication Date: 2017-01-19PHARMACYCLICS LLC
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Patent Information

Application Number
US15/268246
Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
Priority Date
2015-07-30
Filing Date
2016-09-16
Publication Date
2017-01-19
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

Current treatments for diseases related to aberrant tyrosine kinase activity, such as autoimmune diseases, cancers, and inflammatory conditions, often lack effective inhibitors that can specifically target Bruton's tyrosine kinase (Btk) and its homologs, particularly those that form covalent bonds with cysteine or serine residues, leading to incomplete inhibition and resistance mechanisms.

Method used

Development of irreversible inhibitors of Btk that form covalent bonds with cysteine or serine residues, including the C481S mutated form, which also target homologous tyrosine kinases, providing sustained inhibition and overcoming resistance mechanisms.

Benefits of technology

These irreversible inhibitors effectively inhibit Btk and its homologs, offering therapeutic benefits for diseases like autoimmune diseases, cancers, and inflammatory conditions by providing sustained kinase inhibition and addressing resistance issues.

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Abstract

Disclosed herein are amido compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
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