DYRK1 inhibitors and uses thereof

摘要

The present invention relates to novel thiazolo[5,4-f]quinazoline compounds and methods that are useful in the amelioration, treatment or control of Down's syndrome or early Alzheimer's disease or in the amelioration, treatment or control of cancers, especially solid tumors. More specifically, the invention relates to DYRK1A and/or DYRK1B inhibitors and to methods for preparing such compounds.

主权项

1. A compound of formula (I): wherein: X is a nitrogen atom; Y is an oxygen atom, a sulfur atom, a NH group or a N—(C1-C3)alkyl group; R1 is a —C(=A)-B group, wherein:
A is NH or O andB is a OR5 or a NR5R6 group, wherein: R5 and R6 are independently chosen from a hydrogen atom and an unsubstituted or substituted C1-C8 alkyl group; A and B can alternatively independently be nitrogen and/or oxygen atoms and form, with the carbon atom to which they are bound, a heterocycloalkyl group; R2 is a hydrogen atom or an unsubstituted C1-C8 alkyl group; R3 is an unsubstituted or substituted C1-C8 alkyl or an unsubstituted or substituted aryl or heteroaryl group; R4 is a hydrogen atom, a halogen atom, an amino group, a cyano group or an unsubstituted or substituted C1-C5 alkyl group; R7 and R8 are independently chosen from a hydrogen atom, a halogen atom, a hydroxyl group, or an unsubstituted or substituted C1-C5 alkyl group or pharmaceutically acceptable salts thereof.