NITROGEN-CONTAINING HETEROCYCLIC DERIVATIVES AND USE THEREOF IN PHARMACEUTICAL PREPARATIONS Russian patent published in 2019 - IPC C07D239/36 C07D401/04 C07D401/14 C07D403/10 C07D413/10 C07D417/10 A61K31/496 A61K31/513 A61K31/5377 A61K31/541 A61P43/00 

Abstract RU 2701156 C2

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to a heterocyclic compound of formula (I), where V1 is CR1, V2 is N, V3 is CR3, and V4 is CR4; X is a bond or C1 alkylene; Y is O; A is

,

where each n independently takes values of 0, 1 or 2; and each R8a is independently H, F, Cl, Br, cyano or C1-4 haloalkyl; B is -NR7R7a; R1 is C1-3 alkyl, C6-10 aryl-C1-3-alkyl, C6-10 aryl-(CH2)p-G-(CH2)m-, pyridyl-(CH2)p-G-(CH2)m- or C6 cycloalkyl-(CH2)p-G-(CH2)m-, where each G is O or S, where each p is 0, and m is 1, 2 or 3; or where each of C6-10 aryl-(CH2)p-G-(CH2)m-, pyridyl-(CH2)p-G-(CH2)m- and C6 cycloalkyl-(CH2)p-G-(CH2)m- is optionally substituted with one or two F, Cl, Br, C2-6 alkynyl, C1-6 alkoxy or cyano; where C6-10 aryl-C1-3-alkyl is unsubstituted or substituted with F, Cl, Br; R3 is C1-3 alkyl; R4 is H; each R7 independently represents H, C1-6 alkyl or C1-6 alkoxy-C1-4-alkyl; and each R7a is independently C1-6 alkyl, C1-6 alkoxy-C1-4-alkyl, C6-10 aryl-C1-4-alkyl, C1-9 heteroaryl-C1-4-alkyl, C2-10 heterocyclyl-C1-4-alkyl or C3-10 cycloalkyl-C1-4-alkyl; where C1-9 heteroaryl is selected from imidazole, tetrazole and indole; and C2-10 heterocyclyl is selected from morpholine, piperidine and tetrahydrofuran; or R7 and R7a, together with the nitrogen atom to which they are bonded, optionally form a substituted or unsubstituted 3–8-member ring which is selected from morpholine, thiomorpholine, piperazine, piperidine, pyrrolidinyl, pyrrole and pyrazole; where substituted 3–8-member ring is substituted with 1 or 2 substitutes selected from oxo, C1-3 alkyl, hydroxyl and C2-3 alkynyl.

EFFECT: technical result is obtaining novel pyrimidinone derivatives, useful for preventing, regulating or treating tissue or organ fibrosis or for treating the severity of tissue or organ fibrosis in the patient's body.

10 cl, 2 tbl, 72 ex

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RU 2 701 156 C2

Authors

Chzhan Inzhun

Chzhan Tszyantsun

Van Syaotszyun

Lin Zhunfen

Tsao Shentyan

Van Chzhaokhe

Li Tszin

Dates

2019-09-25Published

2013-07-18Filed