NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES USEFUL AS PLASMA KALLIKREIN INHIBITOR

FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to a heterocyclic compound of formula (I), isomers thereof, stereoisomers and pharmaceutically acceptable salts thereof, where B is fused 6,5- or 6,6-heteroaromatic bicyclic ring containing N and optionally 1-2 nitro...

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Hauptverfasser: SMIT Elan Dzhon, MILLER Ien, STOKS Majkl Dzhon, EVANS Devid Majkl, DEJVI Rebekka Luiz, EDVARDS Khannakh Dzhoj, NOVAK Endryu Richard, KHODGSON Sajmon Tinbi
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry.SUBSTANCE: invention relates to organic chemistry and specifically to a heterocyclic compound of formula (I), isomers thereof, stereoisomers and pharmaceutically acceptable salts thereof, where B is fused 6,5- or 6,6-heteroaromatic bicyclic ring containing N and optionally 1-2 nitrogen atoms, which is optionally substituted with 1-2 substitutes selected from alkyl, alkoxy, halogen and NR8R9; where, when B is fused 6,5-heteroaromatic bicyclic ring, it is linked to -CONH-CH- through its 6-member ring component; W, X, Y and Z are independently selected from C, N and S, whereby ring is pyrazole, pyrrole or thiazole; where R5, R6 and R7 are absent or are selected from H, alkyl, halogen, aryl, heteroaryl, -NR8R9, CN, COOR8, CONR8R9, -NR8COR9, CFand R16; where at least one of R5, R6 and R7 is present and is selected from alkyl, halogen, aryl, heteroaryl, -NR8R9, CN, COOR8, CONR8R9, -NR8COR9, CFand R16; A is selected from aryl and heteroaryl; R8 and R9 are selected from H and alkyl; R16 is carbon-containing 3-6-member monocyclic ring which can be aromatic, saturated or unsaturated, optionally containing 2 heteroatoms selected from N and O, where ring R16, in its turn, is optionally substituted with 2 substitutes selected from alkyl and oxo; alkyl-linear saturated (C-C) hydrocarbon or branched saturated (C-C) hydrocarbon; alkyl is optionally substituted with 1-2 substitutes selected from (C-C)alkoxy, OH, CFand fluorine; alkoxy - linear O-linked (C-C) hydrocarbon or branched O-linked (C-C) hydrocarbon; alkoxy is optionally substituted with one CF; aryl is phenyl; aryl is optionally substituted with 1 substituent independently selected from ethylenedioxy, -(CH)-O-heteroaryl, -(CH)-heteroaryl and -(CH)-NR14R15; heteroaryl is 5- or 6-member monocyclic aromatic ring containing, when possible, 1-3 ring elements independently selected from N, NR8, S and O; heteroaryl is optionally substituted with 1-2 substitutes selected from alkyl, alkoxy, halogen, CN, aryl, -CONR10R11 and -NR10R11; R10 and R11 are selected from H and alkyl or R10 and R11 together with the nitrogen atom to which they are attached form carbon-containing 5-member heterocyclic ring which can be saturated or unsaturated with 2 double bonds and which is optionally substituted with 1-2 substitutes selected from alkyl and F; R14 and R15 together with the nitrogen atom to which they are attached form carbon-containing 5- or 6-member heterocyclic ring which is unsaturated with 2 double bonds and