INHIBITORS OF BRUTON'S TYROSINE KINASE
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Abstract
Disclosed herein are compounds that form covalent bonds with Bruton'"'"'s tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. 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.
99 Citations
37 Claims
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1-21. -21. (canceled)
- 22. A method of inhibiting Btk activity comprising administering a selective, covalent, Btk inhibitor, wherein the selective, covalent, Btk inhibitor selectively and covalently bonds to Bruton'"'"'s tyrosine kinase (Btk).
- 23. A method for inhibiting Btk activity comprising administering a Btk inhibitor, wherein the Btk inhibitor is a covalent drug that targets a cysteine residue of Bruton'"'"'s tyrosine kinase (Btk).
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24. A method for inhibiting Btk activity comprising administering an irreversible Btk inhibitor, wherein the irreversible Btk inhibitor forms a covalent bond to a Bruton'"'"'s tyrosine kinase (Btk).
- 25. A method for treating a B-cell proliferative disorder comprising administering to a subject in need thereof a selective, covalent, Btk inhibitor, wherein the selective, covalent, Btk inhibitor selectively and covalently bonds to Bruton'"'"'s tyrosine kinase (Btk).
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26. A method for treating a B-cell proliferative disorder comprising administering to a subject in need thereof a Btk inhibitor, wherein the Btk inhibitor is a covalent drug that targets a cysteine residue of Bruton'"'"'s tyrosine kinase (Btk).
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27. A method for treating a B-cell proliferative disorder comprising administering to a subject in need thereof an irreversible Btk inhibitor, wherein the irreversible Btk inhibitor forms a covalent bond to a Bruton'"'"'s tyrosine kinase (Btk).
Specification