Substituted [1,2,4]triazolo[4,3-a]pyrazines as BRD4 inhibitors

A method for inhibiting bromodomain protein 4 activity in a patient, comprising administering to the patient a therapeutically effective amount of a compound of the formula (I):

• wherein:
• R1 is —C1-3alkyl or —C1-3haloalkyl;
• R2 is —NHR4, —C1-5alkyl, —C1-5haloalkyl, halogen or —S—C1-3alkyl;
• R3 is 5-12 membered heteroaryl, substituted with —X—R10 and optionally further substituted with one or more groups independently selected from R9;
• R4 is —C1-5alkyl or 5-12 membered heterocycloalkyl, which heterocycloalkyl is optionally substituted with one or more groups independently selected from R5;
• R5 is —C1-5alkyl, —C1-5haloalkyl or —C1-3alkylene-O—C1-3alkyl;
• R9 is —C1-5alkyl, —O—C1-5alkyl, —N(C1-5alkyl)2, halogen, —C1-3alkylene-O—C1-3alkyl, —C1-5alkylene-N(C1-5alkyl)2 or 5-12 membered heterocycloalkyl, which heterocycloalkyl is optionally substituted with one or more groups independently selected from ═O and —C1-3alkyl, or
• R9 is —C6-10aryl or 5-12 membered heteroaryl, which aryl and heteroaryl are optionally and independently substituted with one or more groups selected from halogen, —C1-3alkyl, —O—C1-3alkyl, —C1-3haloalkyl, —O—C1-3haloalkyl, —N(C1-5alkyl)2 and —NH—C1-5alkyl;
• X is —C1-3alkylene- or —O—;
• and
• R10 is —C6-10aryl or 5-12 membered heteroaryl, each optionally substituted with one or more groups selected from halogen, —C1-3alkyl, —O—C1-3alkyl, —C1-3haloalkyl and —O—C1-3haloalkyl;
• or a pharmaceutically acceptable salt thereof, wherein the patient is treated for acute myeloid leukemia or multiple myeloma.