NOVEL DERIVATIVE OF PURINYLPYRIDINYLAMINO-2,4-DIFLUOROPHENYLSULPHONAMIDE, ITS PHARMACEUTICALLY ACCEPTABLE SALT, METHOD OF ITS OBTAINING AND PHARMACEUTICAL COMPOSITION, WHICH HAS INHIBITION ACTIVITY WITH RESPECT TO RAF-KINASE, CONTAINING CLAIMED COMPOUND AS ACTIVE INGREDIENT Russian patent published in 2015 - IPC C07D473/00 A61K31/52 A61P35/00 

Abstract RU 2550038 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel derivative of purinylpyridinylamino-2,4-difluorophenylsulphonamide of formula 1 and its pharmaceutically acceptable salt. Compounds have properties of inhibiting Raf-kinase super activity and can be applied for prevention and treatment of diseases, mediated by activity of Raf-kinase, such as cancer, in particular melanoma. In formula 1 R stands for methyl; ethyl; propyl; isopropyl, butyl, isobutyl; cyclopropyl; cyclobutyl; cyclopentyl; cyclohexyl; C5-C6aryl, unsubstituted or substituted with one or more substituents, selected from the group, which consists of chlorine, fluorine, bromine, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, trifluoromethoxy, fluoromethoxy, difluorimethoxy and trifluoroethoxy; C5-C12heteroaryl, which consists of one or two rings, non-substituted or substituted with one or more substituents, selected from the group, which consists of chlorine, fluorine, bromine, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, butoxycarbonyl, tret- butoxycarbonyl and dioxolanyl; C5-C6heterocycloalkyl, non-substituted or substituted with one or more substituents, selected from the group, which consists of chlorine, fluorine, bromine, methyl, ethyl, propyl, isopropyl, butyl, isobutyl; or C5-C6aryl-linear or branched C1-C6alkyl, non-substituted or substituted with one or more substituents, selected from the group, which consists of chlorine, fluorine, bromine, nitro, methyl, ethyl, propyl, isopropyl, butyl and isobutyl, and heteroaryl and heterocycloalkyl contain in ring one or more heteroatoms, selected from the group, which consists of N, O and S. Invention also relates to methods of obtaining formula 1 compounds.

EFFECT: improvement of characteristics.

15 cl, 3 tbl, 51 ex 1 dwg

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RU 2 550 038 C2

Authors

Shim Eun Kiong

Kim Nam Doo

Shim Tae Bo

Kim Seung Jong

Dates

2015-05-10Published

2011-11-25Filed