Substituted [1,2,4]triazolo[4,3-A]pyrazines that are BRD4 inhibitors

摘要

Disclosed are compounds of the formula (I);
wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.

主权项

1. A compound of formula (I) wherein, R1 is —C1-3alkyl or —C1-3haloalkyl; R2 is selected from —NHR4, —C1-5alkyl, —C1-5haloalkyl, halogen and —S—C1-3alkyl; R3 is a 5-12 membered heteroaryl, which group is substituted with —X—R10 and optionally further substituted with one or more groups independently selected from R9; R4 is selected from —C1-5alkyl and 5-12 membered heterocycloalkyl, which heterocycloalkyl can be optionally substituted with one or more groups independently selected from R5; R5 is selected from —C1-5alkyl, —C1-5haloalkyl and —C1-3alkylene-O—C1-3alkyl; R9 is selected from —C1-5alkyl, —O—C1-5alkyl, —N(C1-5alkyl)2, halogen, —C1-3alkylene-O—C1-3alkyl, —C1-5alkylene-N(C1-5alkyl)2 and 5-12 membered heterocycloalkyl, wherein the heterocycloalkyl group can be optionally substituted with one or more groups independently selected from ═O and —C1-3alkyl, or R9 is selected from —C6-10aryl and 5-12 membered heteroaryl, wherein the aryl and heteroaryl groups can be 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—; R10 is —C6-10aryl or 5-12 membered heteroaryl, each of which groups can be 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.