BICYCLIC INHIBITORS Russian patent published in 2018 - IPC C07D401/10 C07D413/14 C07D417/14 C07D471/04 C07D519/00 A61K31/5383 A61P27/00 

FIELD: chemistry.

SUBSTANCE: invention relates to compounds of formula (I)

Formula (I) in which W is selected from CH and N; X is selected from CH, CH₂-CH₂, CH = CH, N and NH; Y is selected from CH₂, CH, N, NH and O; in which the bond between X and Y is either saturated, unsaturated or aromatic; B is selected from: i) a radical of formula II (II) and ii) a condensed 6,5- or 6,6-heteroaromatic bicyclic ring structure containing N and, optionally, one or two additional heteroatoms, which are independently selected from N, which is optionally monosubstituted with NR8R9; P is H and Q is -C(R20)(R21)NH₂ or P is -C(R20)(R21)NH₂ and Q is H; U and V, independently of each other, are selected from C and N, thus the aromatic ring containing U and V is phenyl, pyridine or pyridazine; R1 is absent provided that U is N; R2 is absent provided that V is N; or, if present, R1 and R2, independently of one another, are selected from H and alkyl; R3 is selected from H, alkyl, alkoxy, CN, halogen and CF₃; A is selected from -(CH₂)_0-9-heteroaryl and -(CH₂)_0-9-aryl; R8 and R9 are H; R20 and R21, independently of each other, are selected from H and alkyl, which are directly related to plasma kallikrein activity.

EFFECT: these compounds are potentially useful in the treatment of impaired visual acuity, diabetic retinopathy, macular edema, hereditary angioedema, diabetes, pancreatitis, cerebral haemorrhage, nephropathy, cardiomyopathy, neuropathy, inflammatory bowel disease, arthritis, inflammation, septic shock, hypotension, cancer, adult respiratory distress syndrome, disseminated intravascular coagulation, cardiopulmonary bypass surgery and bleeding from post operative surgery.

22 cl, 5 tbl, 10 ex