FIELD: pharmaceutics.
SUBSTANCE: invention relates to a CDK9 kinase inhibitor comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, which can be used to treat diseases associated with inhibition of CDK9 and/or with its activity caused by mutations. In formula (I), A is selected from the group consisting of cyclohexyl, phenyl and pyridinyl; X is CH or N; Z is -NH- or -NH-C(=O)-; n is 0 or 1; R1 is selected from the group consisting of hydrogen, halogen, cyano, (C1-C6)alkyl and (C1-C6)haloalkyl; R2 is selected from the group consisting of hydrogen and (C1-C6)alkyl, or two R2 together form (C3-C6)cycloalkyl; m is selected from integer of 1–3 and each R3 is independently selected from the group consisting of -NH-(C1-C3)alkyl(C1-C3)alkoxy, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)haloalkyl, (C1-C6)alkylacylamino, (C1-C6)alkylsulphonyl, (C1-C6)alkylsulphonamido, aminosulphonyl, (C1-C6)alkylaminosulphonyl, heterocyclylsulphonyl, in which heteroatom(s) is (are) optionally substituted with (C1-C6)alkyl, aminosulphonyl(C1-C3)alkyl, (C1-C3)alkylsulphonyl(C1-C3)alkyl, (C1-C3)alkylsulphonyl (C3-C6)cycloalkyl, heterocyclylaminoacyl, in which heteroatom(s) is (are) optionally substituted with (C1-C6)alkyl, heterocyclyl, in which heteroatom(s) is (are) optionally substituted with (C1-C6)alkyl, -S(=O)(=NH)(C1-C3)alkyl and -(C1-C3)alkyl-S(=O)(=NH)(C1-C3)alkyl, where heterocyclyl is independently a monocyclic non-aromatic ring formed by six or seven atoms, where one or two said ring atoms are a heteroatom selected from the group consisting of nitrogen and oxygen; R4 is selected from a group consisting of hydrogen and (C1-C6)alkyl. Invention also relates to a pharmaceutical composition containing said inhibitor, and use thereof for treating diseases, which carry CDK9 and/or CDK9 mutations, in particular hyperproliferative diseases, infectious diseases caused by a virus, and cardiovascular diseases.
EFFECT: dihydroisoquinolinone and isoindolinone derivatives and their use are disclosed.
10 cl, 6 tbl, 110 ex
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Authors
Dates
2025-01-21—Published
2021-10-21—Filed