NAPHTHYLAMIDE COMPOUND, PREPARATION METHOD AND USE THEREOF Russian patent published in 2018 - IPC C07D231/56 C07D491/48 C07D495/04 C07D261/20 A61K31/416 A61K31/4355 A61K31/4365 A61K31/519 A61K31/422 A61K31/4439 A61K31/423 A61P35/00 A61P17/06 A61P29/00 A61P27/02 

Abstract RU 2655607 C2

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound and a pharmaceutically acceptable salt thereof, wherein the compound is represented by the following general formula (II), wherein -C(O)NHR3 is located in any of the 1–4 positions of the naphthalene ring; R3 is selected from the group consisting of C1-C6 alkyl, C3-C6 cycloalkyl, substituted or unsubstituted phenyl and substituted or unsubstituted 5-6 member heteroaryl containing from 1 to 2 heteroatoms selected from N and O; in the case of substitution, the substituent is 1 to 3 substituents and each substituent is independently selected from the group consisting of C1-C3 alkyl, C1-C3 alkoxy, C1-C3 haloalkyl, C1-C3 haloalkoxy, hydroxy, amino, nitro and halogen; R2 is hydrogen or halogen; Z is C(R5)=CH, S or O; Y is NH, NMe, O, CH=C(R6) or CH=N; R5 is selected from the group consisting of hydrogen, halogen, C1-C3 alkyl and C1-C3 alkoxy, preferably from the group consisting of hydrogen, F, Cl, Br, methyl and methoxy; R6 is selected from the group consisting of hydrogen, pyrazolyl, C1-C3 alkyl substituted pyrazolyl and C1-C3 hydroxyalkyl-substituted pyrazolyl, preferably from the group consisting of hydrogen, pyrazolyl, methyl-substituted pyrazolyl and hydroxyethyl-substituted pyrazolyl. .

EFFECT: compounds of formula (II) are intended for the preparation of medicaments for the prevention and/or treatment of diseases associated with pathological angiogenesis, preferably as protein tyrosine kinase inhibitors, especially as VEGFR-2 (vascular endothelial growth factor receptor) inhibitors.

7 cl, 3 tbl, 46 ex

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RU 2 655 607 C2

Authors

Duan Venkhu

Din Tszyan

Lv Yuntsun

Se Khua

Dates

2018-05-29Published

2015-02-15Filed