Inhibitors of bruton's tyrosine kinase
AssigneesHoffmann-La Roche Inc., Chugai Pharmaceutical Co., Ltd.
InventorsFrancisco Javier Lopez-Tapia, Sung-Sau So, Qi Qiao, Romyr Dominique
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Abstract
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 useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
Claims2
A method for treating an inflammatory and/or autoimmune condition, comprising a step of administering to a patient in need thereof a therapeutically effective amount of a compound of Formula I:
- wherein:
- R1 is H or halo;
- R2 is H, halo, or cyano;
- R3 is R4 or R5;
- R4 is halo or cyano;
- R5 is phenyl, heteroaryl, —C(═O)R5′, lower alkyl, or benzyl, optionally substituted with one or more R5′;
- R5′ is lower alkyl, cyano, hydroxyl, heterocycloalkyl, phenyl, amino, alkyl amino, dialkyl amino, or lower alkoxy;
- and
- X is lower alkyl or halo;
- or a pharmaceutically acceptable salt thereof.
A method for treating an inflammatory condition, comprising a step of administering to a patient in need thereof a therapeutically effective amount of a compound of Formula I:
- wherein:
- R1 is H or halo;
- R2 is H, halo, or cyano;
- R3 is R4 or R5;
- R4 is halo or cyano;
- R5 is phenyl, heteroaryl, —C(═O)R5′, lower alkyl, or benzyl, optionally substituted with one or more R5′;
- R5′ is lower alkyl, cyano, hydroxyl, heterocycloalkyl, phenyl, amino, alkyl amino, dialkyl amino, or lower alkoxy;
- and
- X is lower alkyl or halo;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.