Substituted azaindole compounds, salts, pharmaceutical compositions thereof and methods of use

摘要

The present invention provides substituted azaindole prodrugs, methods of making said prodrugs, pharmaceutical compositions of said prodrugs and methods of using said prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as cancer.

主权项

1. A compound of Formula (I): or a racemic mixture, a stereoisomer, a geometric isomer, a tautomer, a solvate, an N-oxide, a metabolite or a pharmaceutically acceptable salt thereof, wherein:
each of X and Y is independently H, —C(═O)R3, —C(═O)OR4, —C(R1R2)OC(═O)R3, —C(R1R2)OC(═O)OR4 or —C(R1R2)OP(═O)(OR4)(OR4a), with the proviso that when Y is H, X is not —C(═O)CH3 or H; each R1 and R2 is independently H, D, C1-6alkyl, C1-6haloalkyl, C3-6cycloalkyl, —(C1-4 alkylene)-(C3-6cycloalkyl), C3-6heterocyclyl or —(C1-4alkylene)-(C3-6heterocyclyl); or R1 and R2, together with the carbon atom they are attached to, form an unsubstituted or substituted 3-8 membered carbocyclic or heterocyclic ring; each R3 is independently H, D, C1-10haloalkyl, C3-8cycloalkyl, —(C1-6 alkylene)-(C3-8cycloalkyl), C3-8heterocyclyl, —(C1-6alkylene)-(C3-8heterocyclyl), C6-10aryl, —(C1-6alkylene)-(C6-10aryl), 5-10 membered heteroaryl or —(C1-6alkylene)-(5-10 membered heteroaryl), wherein each of the C1-10alkyl, C1-10haloalkyl, C3-8cycloalkyl, —(C1-6alkylene)-(C3-8cycloalkyl), C3-8heterocyclyl, —(C1-6alkylene)-(C3-8heterocyclyl), C6-10aryl, —(C1-6 alkylene)-(C6-10aryl), 5-10 membered heteroaryl and —(C1-6alkylene)-(5-10 membered heteroaryl) is unsubstituted or optionally substituted with 1, 2, 3 or 4 substituents independently selected from D, F, Br, I, C1-6alkyl, C1-6haloalkyl, OH, NH2, C1-6 alkoxy and C1-6alkylamino; and each R4 and R4a is independently H, C1-10haloalkyl, C3-8cycloalkyl, —(C1-6 alkylene)-(C3-8cycloalkyl), C3-8heterocyclyl, —(C1-6alkylene)-(C3-8heterocyclyl), C6-10aryl, —(C1-6alkylene)-(C6-10aryl), 5-10 membered heteroaryl or —(C1-6alkylene)-(5-10 membered heteroaryl), wherein each of the C1-10alkyl, C3-8cycloalkyl, —(C1-6alkylene)-(C3-8cycloalkyl), C3-8heterocyclyl, —(C1-6alkylene)-(C3-8heterocyclyl), C6-10aryl, —(C1-6 alkylene)-(C6-10aryl), 5-10 membered heteroaryl and —(C1-6alkylene)-(5-10 membered heteroaryl) is unsubstituted or optionally substituted with 1, 2, 3 or 4 substituents independently selected from D, F, Cl, OH, NH2, oxo (═O), C1-6haloalkyl, C1-6 alkoxy and C1-6alkylamino.