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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Hauptverfasser: Kasatkina Mariya Andreevna, Evdokimov Anton Aleksandrovich, Smirnov Evgenij Yurevich, Maksimenko Elena Aleksandrovna, Gavrilov Aleksej Sergeevich, Morozov Dmitrij Valentinovich, Lenshmidt Liliana Vyacheslavovna, Mishina Mariya Sergeevna, Alafinov Andrej Ivanovich, Chestnova Anna Yurevna, Mindich Aleksej Leonidovich, Silonov Sergej Aleksandrovich, Yakovlev Pavel Andreevich
Format: Patent
Sprache:eng ; rus
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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