INHIBITORS OF BRUTON'S TYROSINE KINASE

摘要

This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.;

主权项

1. A compound of Formula I, wherein: n is 1 or 2; R1 is —C(═O)R1′, —S(═O)2R1′, or —OC(R1′)2CH2OH; R1′ is methyl or morpholine; R2 is H or F; R3 is chloro or C(CH2)2R3′; R3′ is methyl, cyano, or hydroxymethyl; X is CH, CH2, or N; X2 is CH or N; X3 is CH or N; and Y is CH or O; with the proviso that when n is 2, both X are CH2; or a pharmaceutically acceptable salt thereof.