330792-69-3Relevant articles and documents
PROCESSES AND INTERMEDIATES FOR PREPARING A BTK INHIBITOR
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Page/Page column 23; 24, (2020/12/07)
Disclosed is a process for the preparation of certain intermediates, e.g. process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof, in an enantioenriched form, which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.
Aminopyrazole Carboxamide Bruton's Tyrosine Kinase Inhibitors. Irreversible to Reversible Covalent Reactive Group Tuning
Schnute, Mark E.,Benoit, Stephen E.,Buchler, Ingrid P.,Caspers, Nicole,Grapperhaus, Margaret L.,Han, Seungil,Hotchandani, Rajeev,Huang, Nelson,Hughes, Robert O.,Juba, Brian M.,Kim, Kyung-Hee,Liu, Erica,McCarthy, Erin,Messing, Dean,Miyashiro, Joy S.,Mohan, Shashi,O'Connell, Thomas N.,Ohren, Jeffrey F.,Parikh, Mihir D.,Schmidt, Michelle,Selness, Shaun R.,Springer, John R.,Thanabal, Venkataraman,Trujillo, John I.,Walker, Daniel P.,Wan, Zhao-Kui,Withka, Jane M.,Wittwer, Arthur J.,Wood, Nancy L.,Xing, Li,Zapf, Christoph W.,Douhan, John
supporting information, p. 80 - 85 (2019/01/15)
Potent covalent inhibitors of Bruton's tyrosine kinase (BTK) based on an aminopyrazole carboxamide scaffold have been identified. Compared to acrylamide-based covalent reactive groups leading to irreversible protein adducts, cyanamide-based reversible-covalent inhibitors provided the highest combined BTK potency and EGFR selectivity. The cyanamide covalent mechanism with BTK was confirmed through enzyme kinetic, NMR, MS, and X-ray crystallographic studies. The lead cyanamide-based inhibitors demonstrated excellent kinome selectivity and rat pharmacokinetic properties.
Therapeutic Combinations of a Proteasome Inhibitor and a BTK Inhibitor
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Paragraph 0468-0469, (2019/07/23)
Therapeutic combinations of a proteasome inhibitor and a Bruton's tyrosine kinase (BTK) inhibitor are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of a proteasome inhibitor and a BTK inhibitor and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.