Benzo [E] [1,3] oxazin-4-one derivatives as phosphoinositide 3-kinase inhibitors

摘要

Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)-alkyl. —C(O)—NH2, —C(O)—NH-alkyl, —SO2-alkyl, —SO2—NH2 or —SO2—NH-alkyl; R2 is aryl substituted with at least one nitrogen-containing group or R2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C1-C6 mono alkylamino, C1C6 bis alkylamino, C1C6 acylamino, C1-C6 aminoalkyl, mono (C1C6 alkyl)amino C1-C6 alkyl, bis (C1C6 alkyl)amino C1C6 alkyl, C1-C6-acylamino or C1 C6 alkynyl-NR11, R11 is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, halogen, O-alkyl, NH-alkyl, N-dialkyl, —C(O)—R7, —C(O)—NH2, —C(O)—NH—R7, —SO2—R7, —SO2—NH2, —SO2—NH—R7, NH-acyl, NH-sulfonyl, NR7-acyl, NR7-sulfonyl, N—C(O)—NH—R7, N—SO2—NH—R7, N—C(O)—NR7R7 or N—SO2—NR7R7; and R7 is alkyl, aryl or heteroaryl, are useful as PI3K inhibitors and are useful in therapy.;

主权项

1. A compound of formula (I):wherein:
W is O; each X is independently CH or N; R1 is R3 is H, alkyl, NH2, OH, ═O or halogen; R2 is aryl substituted with at least one nitrogen-containing group or R2 is a nitrogen-containing heteroaryl, cycloalkyl substituted with a nitrogen-containing group, nitrogen-containing cycloalkyl, C1-C6 mono alkylamino, C1-C6 bis alkylamino, C1-C6 acylamino, C1-C6 aminoalkyl, mono (C1-C6 alkyl)amino C1-C6 alkyl, bis (C1-C6 alkyl)amino C1-C6 alkyl, C1-C6-acylamino or C1-C6 alkynyl-NR11; wherein the nitrogen-containing group is amino, C1-C6 mono alkylamino, C1-C6 bis alkylamino, C1-C6 acylamino, C1-C6 aminoalkyl, mono (C1-C6 alkyl)amino C1-C6 alkyl, bis(C1-C6 alkyl)amino C1-C6 alkyl, C1-C6-acylamino, alkynyl-NR11 or NR6R6 wherein each R6 is independently selected from H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, —C(O)—R7, —C(O)—NH2, —C(O)—NH—R7, —SO2—R7, —SO2—NH2, —SO2—NH—R7, N—C(O)—NR7R7 or N—SO2—NR7 R7; R11 is H; and R7 is alkyl, aryl or heteroaryl.