CDK8/19 INHIBITORS
FIELD: pharmaceutics.SUBSTANCE: invention relates to a compound of the formula I or its pharmaceutically acceptable salt, which can be used as inhibitors of the activity of cyclin-dependent protein kinases CDK8/19. In the formula I, L is -[CH2]0-3-, - [CH2]0-2-C(O)-, -C(O)-[CH2]0-2-; R is -NR4R5, -O...
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Zusammenfassung: | FIELD: pharmaceutics.SUBSTANCE: invention relates to a compound of the formula I or its pharmaceutically acceptable salt, which can be used as inhibitors of the activity of cyclin-dependent protein kinases CDK8/19. In the formula I, L is -[CH2]0-3-, - [CH2]0-2-C(O)-, -C(O)-[CH2]0-2-; R is -NR4R5, -OR6; R1is -NR2R3; R2and R3are independently H; C1-6alkyl, unsubstituted or substituted with one or several substituents of R7; C3-7cycloalkyl, unsubstituted or substituted with one or several substituents of R8; or R2and R3, together with a nitrogen atom to which they are attached, form 4-7-element heterocyclic ring with 1-3 heteroatoms selected from N, where heterocyclic ring formed by R2and R3can be unsubstituted or substituted with one or several substituents of R9; R4and R5are independently H; C1-6alkyl, unsubstituted or substituted with one or several substituents of R12, or R4and R5, together with a nitrogen atom to which they are attached, form 4-7-element heterocyclic ring with 1-3 heteroatoms selected from N, where heterocyclic ring formed by R4and R5can be unsubstituted or substituted by one or several substituents of R14; R6is H; C1-6alkyl; R7and R12, each independently, is H, -OR18, C3-7cycloalkyl, unsubstituted or substituted by one or several radicals selected from C1-6alkyl, halogen; R8is H, Hal; R9and R14, each independently, is H, C1-6alkyl; R18is H, C1-C6alkyl. The invention also relates to a pharmaceutical composition containing therapeutically effective amount of a compound of the formula I and intended for the prevention or treatment of a disease or disorder mediated by the activation of cyclin-dependent protein kinases CDK8/19, and to a method for treating a disease or disorder mediated by the activation of cyclin-dependent protein kinases CDK8/19, including the injection of therapeutically effective amount of the specified compound.EFFECT: obtaining CDK8/19 inhibitors.11 cl, 6 tbl, 12 ex
Изобретение относится к соединению формулы I или его фармацевтически приемлемой соли, которые могут найти применение в качестве ингибиторов активности циклинзависимых протеинкиназ CDK8/19. В формуле I L представляет собой -[СН2]0-3-, -[СН2]0-2-C(O)-, -С(O)-[СН2]0-2-; R представляет собой -NR4R5, -OR6; R1представляет собой- NR2R3; R2и R3независимо представляет собой Н; C1-6алкил, незамещенный или замещенный одним или несколькими заместителями R7; С3-7циклоалкил, незамещенный или замещенный одним или несколькими заместителями R8; или R2и R3вместе с атомом азо |
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