FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to compounds of formula (I),
(III) and
(VI), possessing properties of TNF-α inhibitors, and their pharmaceutical salts and stereoisomers, as well as to a based on them pharmaceutical composition and a method of treatment with their application. In the general formulae (I), (II), (III) and (VI) X stands for C=O or CH2; R1 stands for -Y-R3; R2 stands for H or (C1-C6)alkyl; Y stands for a 6-10-membered aryl, heteroaryl or heterocycle, each of which can be substituted with one or more halogens; R3 stands for -(CH2)n-aryl, -O-(CH2)n-aryl or -(CH2)n-O-aryl, in which the aryl can be substituted with one or more of the following substituents: (C1-C6)alkyl, which itself can be substituted with one or more halogens; (C1-C6)alkoxy, which itself is substituted with one or more halogens; oxo; amino; carboxyl; cyano; hydroxyl; halogen; deuterium; 6-10-membered aryl or heteroaryl, in case of necessity substituted with one or more (C1-C6)alkyls, (C1-C6)alkoxy or halogens; -CONH2; or -COO-(C1-C6)alkyl, where the alkyl can be substituted with one or more halogens; -(CH2)n-heterocycle; -O-(CH2)n-heterocycle or -(CH2)n-O-heterocycle, where the heterocycle can be substituted with one or more of the following substituents: (C1-C6)alkyl, itself in case of necessity substituted with one or more halogens; (C1-C6)alkoxy, itself substituted with one or more halogens; oxo; amino; carboxyl; cyano; hydroxyl, halogen; deuterium; 6-10-membered aryl or heteroaryl, in case of necessity substituted with one or more (C1-C6)alkyls, (C1-C6)alkoxy or halogens; -CONH2; or -COO-(C1-C6)alkyl, where the alkyl can be substituted with one or more halogens; or -(CH2)n-heteroaryl, -O-(CH2)n-heteroaryl or -(CH2)n-O-heteroaryl, where the heteroaryl can be substituted with one or more of the following substituents: (C1-C6)alkyl, itself in case of necessity substituted with one or more halogens; (C1-C6)alkoxy, itself substituted with one or more halogens; oxo; amino; carboxyl; cyano; hydroxyl; halogen; deuterium; 6-10-membered aryl or heteroaryl, in case of necessity substituted with one or more (C1-C6)alkyls, (C1-C6)alkoxy or halogens; -CONH2; or -COO-(C1-C6)alkyl, where the alkyl can be substituted with one or more halogens; and n=0, 1, 2 or 3.
EFFECT: obtaining the compounds, possessing the properties of the TNF-α inhibitor.
18 cl, 1 tbl, 309 ex
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Authors
Dates
2015-11-10—Published
2011-02-10—Filed