THIAZOLYLPHENYL-BENZENESULFONAMIDO DERIVATIVES AS KINASE INHIBITORS Russian patent published in 2017 - IPC C07D417/04 C07D417/14 A61K31/4427 A61P35/00 

Abstract RU 2606497 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula (I), where each of n and m independently equals 1; R1 is halogen or a group selected from a straight or branched (C1-C8)alkyl and heterocyclyl, selected from piperidinyl and tetrahydropyranyl, where piperidinyl is optionally substituted with (C1-C6)alkyl and (C3-C6)cycloalkyl; or R1 is NR7R8, where each R7 and R8 independently represents hydrogen or a group, selected from a straight or branched (C1-C8)alkyl, heterocyclyl, selected from piperidinyl and optionally substituted methyl; or, taken together with a nitrogen atom with which they are bonded, R7 and R8 can form optionally substituted 3-8-member heterocyclyl, optionally having one additional heteroatom or heteroatomic group selected from O, N and NH, optionally substituted with halogen; each of R2 and R3 independently represents hydrogen, halogen or optionally substituted group, selected from a straight or branched (C1-C8)alkyl and heterocyclyl, selected from imidazolidine, substituted -COCH3, -C=O, -CH2-OCH3, -CH3; or each of R2 and R3 independently represents NR17R18, where R17 and R18 independently denote hydrogen or optionally substituted group, selected from a straight or branched (C1-C8)alkyl, optionally substituted -NH-COCH3, -NHCOOCH3, -N(CH3)2; or R17 represents hydrogen and R18 represents COR22, where R22 denotes OR23 or optionally substituted group, selected from a straight or branched (C1-C8)alkyl, where R23 is straight or branched (C1-C8) alkyl, each of R4 and R5 is independently hydrogen or halogen; Rx is hydrogen; R6 denotes phenyl, optionally substituted with halogen; or a pharmaceutically acceptable salt thereof. Invention relates to a method of inhibiting activity in vitro of Raf, which involves bringing said receptor into contact with an effective amount of compound of formula (I). Compound of formula (I) or a pharmaceutically acceptable salt thereof are intended for use as a medicinal agent or in a pharmaceutical composition, with activity against a malignant tumour.

EFFECT: technical result is thiazolylphenyl-benzenesulfonamido derivatives as Raf kinase inhibitors.

10 cl, 1 tbl, 22 ex

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Authors

Pulichi Mauritsio

Trakvandi Gabriella

Markionni Kyara

Skolaro Alessandra

Kolombo Nikoletta

Dates

2017-01-10Published

2012-02-21Filed