FIELD: pharmaceutics.
SUBSTANCE: group of inventions relates to the field of pharmaceutics and includes derivatives of 1H-pyrazolo[4,3-b]pyridine-7-amine of the formula (I), their pharmaceutically acceptable salts, application and pharmaceutical composition based on them. For compounds of the formula (I), L is selected from a group consisting of NH, CH2, S and O; R1 is selected from a group consisting of hydrogen, linear or branched C1-C5alkyl and C1-C5fluoroalkyl; R2 is selected from a group consisting of linear or branched C1-C8alkyl, saturated monocyclic C3-C8cycloalkyl and oxetanyl; R3 is methyl or ethyl substituted with phenyl, pyridonyl, pyridinyl, pyrimidinyl or pyrazinyl, all of which can optionally be substituted with one substituent selected from a group consisting of halogen, C1-C3alkyl, C1-C3fluoroalkyl and C1-C3alkoxy; or R3 is methyl or ethyl substituted with 5-element heteroaryl, which is selected from a group consisting of oxadiazolyl, thiazolyl, oxazolyl, isoxazolyl, triazolyl, pyrazolyl, tetrazolyl, imidazolyl, thiadiazolyl, thiophenyl, which is optionally substituted with one or two substituents selected from C1-C3alkyl and C1-C3fluoroalkyl; or L is CH2, and R3 is NH substituted with phenyl, pyridonyl, pyridinyl or triazolyl, all of which can optionally be substituted with one substituent selected from a group consisting of C1-C3alkyl and C1-C3alkoxy; R4 is phenyl, pyridinyl or pyridonyl, all of which can optionally be substituted with one substituent selected from a group consisting of C1-C4alkyl, C1-C4fluoroalkyl, C1-C3fluoroalkoxy, cyclopropyloxy, C1-C3alkoxy, C1-C3deutherioalkoxy and -N-R5R6, where each of R5 and R6 is independently selected from C1-C3alkyl; or R4 is 5-element heteroaryl, which is pyrazolyl, thiophenyl, thiazolyl, oxazolyl, isoxazolyl, triazolyl, optionally substituted with one or two substituents selected from C1-C4alkyl and -N-R5R6, where each of R5 and R6 is independently selected from H and C1-C3alkyl; or R4 is 4- or 5-element saturated heterocycle selected from a group consisting of oxazolidine-2-one, azetidine-2-one, imidazolidine-2-one, pyrrolidine-2-one, which in all cases can be optionally substituted with one or two substituents selected from oxo and C1-C4alkyl.
EFFECT: compounds of the formula (I) as PDE1 inhibitors.
(I)
16 cl, 1 tbl, 203 ex
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