VET PROTEIN DECOMPOSERS Russian patent published in 2021 - IPC C07D487/04 A61K31/4745 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound by the formula I, or a pharmaceutically acceptable salt or solvate thereof, wherein B constitutes B-1; R¹ constitutes -N(H)R³; Q¹ constitutes =N- and Q² constitutes -N =; R³ constitutes (a); X is selected from the group consisting of -C(=O)N(R^2a)-, -CH₂N(R^2b)-, -CH₂O-, -N(R^2c)-, -O- and -CH₂-; wherein the nitrogen atom from -C(=O)N(R^2a)- and -CH₂N(R^2b) is attached to L and the oxygen atom from -CH₂O- is attached to L; L is selected from the group consisting of -CH₂-, -CH₂CH₂-, -CH₂CH₂CH₂-, -CH₂(CH₂)₂CH₂-, -CH₂(CH₂)₃CH₂-, -CH₂(CH₂)₄CH₂-, -CH₂(CH₂)₅CH₂-, -CH₂(CH₂)₆CH₂-, -CH₂CH₂OCH₂CH₂-, -CH₂CH₂OCH₂CH₂OCH₂CH₂-, -CH₂CH₂O(CH₂CH₂O)₂CH₂CH₂-, -CH₂CH₂O(CH₂CH₂O)₂CH₂CH₂CH₂CH₂-, -CH₂CH₂O(CH₂CH₂O)₃CH₂CH₂-, -CH₂CH₂O(CH₂CH₂O)₄CH₂CH₂-, -CH₂CH₂O(CH₂CH₂O)₆CH₂CH₂-, -CH₂CH₂O(CH₂CH₂O)₆CH₂CH₂-, -CH₂CH₂CH₂OCH₂CH₂OCH₂CH₂-, -CH₂CH₂CH₂OCH₂CH₂OCH₂CH₂CH₂-, -CH₂CH₂CH₂O(CH₂CH₂O)₂CH₂-, -CH₂CH₂CH₂O(CH₂CH₂O)₂CH₂CH₂-, -CH₂CH₂CH₂O(CH₂CH₂O)₂CH₂CH₂CH₂-, -CH₂CH₂CH₂O(CH₂)₄OCH₂CH₂CH₂- and -(CH₂)_m-W-(CH₂)_n-; W constitutes unsubstituted or substituted 5-membered heteroarylenyl comprising 2 nitrogen atoms, wherein one or two substituents independently constitute C_1-4 alkyl; m equals 0, 1, 2, 3, 4, 5, 6, or 7; n equals 0, 1, 2, 3, 4, 5, 6, 7, or 8; Y is selected from the group consisting of -C≡C-, -CH₂-, -O-, -N(R^2d)-, -C(=O)N(R^2e)-, -N(R^2f)C(=O)CH₂O- and -N(R^2g)C(=O)CH₂N(R^2h)-; or Y is absent; wherein the nitrogen atom of carboxamide in-N(R^2f)C(=O)CH₂O- and -N(R^2g)C(=O)CH₂N(R^2h)- and the carbon atom in -C(=O)N(R^2e) - is attached to L; R^2a, R^2b, R^2c, R^2d, R^2e, R^2f, R^2g and R^2h are each independently selected from the group consisting of hydrogen and C_1-4 alkyl; Z is selected from the group consisting of -CH₂ and -C(=O)-; and R⁵ is selected from the group consisting of hydrogen and fluorine. The invention also relates to a compound by the formula XIV, or a pharmaceutically acceptable salt or solvate thereof, wherein R¹ constitutes -N(H)R³; Q¹ constitutes =N- and Q² constitutes -N=; R³ constitutes (a), R^7a is selected from the group consisting of chlorine and -OR^7b; and R^7b is selected from the group consisting of hydrogen and C_1-4 alkyl.

EFFECT: compound by the formula is intended to reduce the bromodomain protein BET in a cell of the patient during treatment of cancer.

21 cl, 16 dwg, 9 tbl, 27 ex