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US 2026/0308145 A1Published application
Cdk2 inhibitors and methods of using same
AssigneeGuangdong Touchstone Translational Research Institute Co., Ltd.
InventorsHongjian Yang, Yexing Cao, Chang Bai, Jialiang Qin, Jing Su
Life of this patent
Estimating the term…
Abstract
The present invention provides novel compounds of Formula (I) as CDK2 inhibitors, which are useful for treating diseases or conditions mediated by CDK2, in particular, cancers and other diseases caused by abnormal cell proliferation. Preparation methods, pharmaceutical compositions and methods of use are also included.
Claims22
A compound of Formula (I),
- wherein
- X is CH or N;
- Z is CH or N;
- ring A is aryl, heteroaryl, cycloalkyl or heterocyclyl, or aryl-fused heterocyclyl, each of which is optionally and independently substituted with one R1 and one to four R2;
- wherein a carbon atom of the aryl-fused heterocyclyl is optionally substituted with one oxo, and a heteroatom of the aryl-fused heterocyclyl is optionally substituted with one or two oxo;
- R1 is —S(O)2—R10, —NH—S(O)2—R10 or —SF5;
- each R2 is independently H, alkyl, —CN, cyanoalkyl, amino, alkylamino, dialkylamino, —NO2, halo, haloalkyl, hydroxyl, hydroxyalkyl, alkoxyl, haloalkoxy, (haloalkoxy)alkyl, alkoxyalkyl, cycloalkyl or heterocyclyl;
- wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R7;
- R3 is H, halo, alkyl, haloalkyl, hydroxyl, hydroxyalkyl, alkoxyl, alkoxyalkyl, alkenyl, alkynyl, —CN or cyanoalkyl;
- R4 and R6 are each independently H, alkyl, halo, haloalkyl, hydroxyl, hydroxyalkyl, alkoxyl, haloalkoxy, (haloalkoxy)alkyl, alkoxyalkyl, amino, alkylamino, dialkylamino, -alk-N—R9R9, —CN, cyanoalkyl, cycloalkyl or heterocyclyl;
- wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R7;
- R5 is H, alkyl, halo, haloalkyl, hydroxyl, hydroxyalkyl, alkoxyl, haloalkoxy, (haloalkoxy)alkyl, alkoxyalkyl, —CN, cyanoalkyl, amino, alkylamino, dialkylamino, -alk-N—R9R9, aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocyclyl, -alk-cycloalkyl, -alk-heterocyclyl, —O-cycloalkyl, or —O— heterocyclyl, wherein the aryl, heteroaryl, cycloalkyl, cycloalkenyl, heterocyclyl, -alk-cycloalkyl, -alk-heterocyclyl, —O-cycloalkyl or —O-heterocyclyl is optionally substituted with one or more R7;
- each R7 is independently alkyl, halo, haloalkyl, hydroxyl, hydroxyalkyl, alkoxyl, haloalkoxy, (haloalkoxy)alkyl, alkoxyalkyl, amino, alkylamino, dialkylamino, —CN, cyanoalkyl, oxo (═O), R8—S(O)2—, R8—O—C(═O)—, R8—C(═O)—O—, R8—C(═O)—, cycloalkyl or heterocyclyl;
- wherein the cycloalkyl or heterocyclyl is optionally further substituted with one or more R7;
- each R8 is independently H, alkyl or —NR9R9;
- each R9 is independently H, cycloalkyl, -alk-cycloalkyl, or alkyl;
- R10 is H, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, heterocyclyl or —NR11R11;
- wherein the cycloalkyl or heterocyclyl is optionally substituted with one or more R7;
- each R11 is independently H, alkyl, cycloalkyl, heterocyclyl, -alk-cycloalkyl, -alk-heterocyclyl, hydroxyalkyl, -alk-O—R12, -alk-C(O)—OR9 or -alk-N—R9R9;
- wherein the cycloalkyl, -alk-cycloalkyl, -alk-heterocyclyl, or heterocyclyl is optionally substituted with one or more R7;
- each R12 is independently H, alkyl, cycloalkyl, haloalkyl, or heterocyclyl;
- the heteroaryl and heterocyclyl in each occurrence independently contain one or more ring-forming heteroatoms each of which is independently oxygen, sulfur or nitrogen;
- the heterocyclyl in each occurrence is saturated or partially unsaturated;
- and
- any H in each alkyl is optionally replaced with deuterium (D);
- or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof.
23 more elements
(canceled)
(canceled)
Dependencies are inferred from the claim text.