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:
R1 is benzyl or lower alkyl, each optionally substituted with one or more R1′; each R1′ is independently, lower alkyl, halo, or cyano; X is CH or NR4; R4 is C(═O)C(═O)nR4′; R4′ is lower alkyl or lower alkenyl; n is 0 or 1; represents either a single or double bond; m is 0 or 1; r is 0 or 1; Y is CN(R3)C(═O)R2, CH2, or N; R2 is lower alkyl, lower alkenyl, C(═O)H, or cycloalkyl, each optionally substituted independently with one or more R2′; each R2′ is independently lower alkyl, lower alkenyl, amino, alkyl amino, dialkyl amino, halo lower alkyl, phenyl or cyano; and R3 is H or lower alkyl; or a pharmaceutically acceptable salt thereof.