FIELD: medicine technology.
SUBSTANCE: group of inventions includes a compound of formula (I), or its pharmaceutically acceptable salts or stereoisomers, a pharmaceutical composition and use. In the formula (I), each of X1, X2, X3 and X4 independently represents CR3 or N, and X1 X2, X3 and X4 do not simultaneously represent CR3 ; R3 at each occurrence is independently selected from the group consisting of hydrogen, amino, carboxyl, cyano, halogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylamino, (C-1-6 alkyl)2 amino , C2-8 alkenyl, C2-8 alkynyl, C1-6 alkylsulfonyl, C1-6 alkylthio, C3-6 cycloalkyl, 4-6 membered saturated nitrogen-containing heterocyclyl selected from azetidinyl, piperazinyl and morpholinyl, C1 -6 alkylcarbonyl, aminocarbonyl, C1-6 alkylaminocarbonyl, (C1-6 alkyl)2 aminocarbonyl, 4-6 membered heterocyclylcarbonyl selected from piperazinylcarbonyl and azetidinylcarbonyl, and pyrimidinyloxy, where C1-6 alkyl, C1-6 alkoxy , (C1-6 alkyl)2 amino, C2-8 alkynyl, 4-6 membered saturated nitrogen-containing heterocyclyl selected from azetidinyl, piperazinyl and morpholinyl, aminocarbonyl, C1-6 alkylaminocarbonyl and 4-6 membered heterocyclylcarbonyl, selected of piperazinylcarbonyl and azetidinylcarbonyl are unsubstituted or optionally substituted with one or two groups independently selected from a group consisting of hydroxy, amino, cyano, C1-6 alkyl, C1-6 alkoxy, (C1-6 alkyl)2 amino, C1-6 alkylcarbonyloxy, C3-6 cycloalkyl, halogenated C1-6 alkyl and a 4-6 membered saturated nitrogen-containing heterocyclyl selected from azetidinyl, pyrrolidinyl and piperidinyl which is unsubstituted or optionally substituted with C1-6 alkyl; L is a bond, -NH-(CH2)t -, and t is 0, 1, 2 or 3; ring A is selected from the group consisting of a 5-7 membered saturated monoheterocyclyl having an N atom as a heteroatom, a 7-11 membered saturated spiroheterocyclyl having 1 or 2 heteroatoms selected from O and N, and an aryl having from 6 to 14 carbon atoms; each R1 is independently selected from the group consisting of hydrogen, hydroxy, cyano, halogen, C1-6 alkyl optionally substituted with hydroxy, C1-6 alkoxy, and a 5-membered heteroaryl containing 1 to 3 heteroatoms selected from S and N; m is 0, 1, 2 or 3; and R2 is hydrogen; with the proviso that: when X1 is N and X2, X3 and X4 are each independently CR3, A is not phenyl; when X1 and X3 are each independently N and X2 and X4 are each independently CR3, A is not phenyl; and when X3 is N and X1, X2 and X4 are each independently CR3, A is not phenyl.
EFFECT: compound of formula (I) exhibiting the properties of a phosphodiesterase 9 (PDE9) inhibitor, which can be used to obtain a drug for the treatment or prevention of diseases mediated by PDE9.
18 cl, 8 tbl, 101 ex
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