Inhibitors of Bruton's tyrosine kinase
First Claim
Patent Images
1. A method of identifying an irreversible inhibitor of a Bruton'"'"'s tyrosine kinase (Btk) comprising:
- (1) contacting Btk with a compound of Formula VII;
(2) contacting at least one non-kinase molecule having at least one accessible SH group including glutathione and/or hemoglobin with the compound of Formula VII; and
(3) determining the covalent binding of the compound of Formula VII with Btk and the at least one non-kinase molecule; and
repeating steps (1), (2), and (3) for at least one other compound of Formula VII, wherein the compound of Formula (VII) has the structure;
5 Assignments
0 Petitions
Accused Products
Abstract
Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.
164 Citations
8 Claims
-
1. A method of identifying an irreversible inhibitor of a Bruton'"'"'s tyrosine kinase (Btk) comprising:
-
(1) contacting Btk with a compound of Formula VII; (2) contacting at least one non-kinase molecule having at least one accessible SH group including glutathione and/or hemoglobin with the compound of Formula VII; and (3) determining the covalent binding of the compound of Formula VII with Btk and the at least one non-kinase molecule; and repeating steps (1), (2), and (3) for at least one other compound of Formula VII, wherein the compound of Formula (VII) has the structure; - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
-
Specification