2-AMINOPYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION AND USE OF SAID COMPOUND Russian patent published in 2019 - IPC C07D239/48 C07D401/12 C07D403/12 A61K31/505 A61K31/506 A61K31/535 A61P35/00 

Abstract RU 2704129 C2

FIELD: chemistry.

SUBSTANCE: invention relates to organic chemistry and specifically to novel compounds of 2-aminopyrimidine of formula I, where R1 is selected from a group comprising halogen, cyano, substituted or unsubstituted C1-C6 alkyl or unsubstituted C1-C6 alkoxy; R2 is selected from a group comprising H, halogen, unsubstituted C1-C6 alkyl, unsubstituted C1-C6 alkoxy; R3 is H or -(CH2)mNR8R9; R4 and R5 each being H, unsubstituted C1-C6 alkyl, halogen, -(CH2)mNR8R9; wherein each m separately represents 0 or 1; each R8 and each R9 separately is selected from substituted and unsubstituted C1-C6 alkyl, or R8, R9 and bound N together form an unsubstituted or substituted 4–7 membered monocyclic ring containing 1 or 2 heteroatoms selected from O, N; W is NH, N(C1-C3 alkyl), O or S; X, Y, Z each separately is N or -CR10, where R10 is H; is unsubstituted 5-6-member aromatic ring containing 0, 1 heteroatoms selected from N; where each substituted element is separately substituted with 1 or 3 groups selected from halogen, C1-C3 alkyl, -NH(C1-C3 alkyl), -N(C1-C3 alkyl)(C1-C3 alkyl) and - C(= O)(C1-C3 alkyl). Also disclosed is a method of producing said compound, a pharmaceutical composition based on said compound, use of said compound for treating a tumour for preparing a medicament of a protease inhibitor EGFR or for preparing a medicinal agent of a protease inhibitor IGF1R. Also disclosed is an intermediate compound of formula III.

,

EFFECT: technical result is obtaining heterocyclic compounds useful as EGFR protease inhibitor or IGF1R protease inhibitor.

13 cl, 3 dwg, 2 tbl, 53 ex

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RU 2 704 129 C2

Authors

Ding Ke

Ding Dzhian

Chan Shingpan

Geng Meijyu

Ren Ksiaomei

Ksie Khua

Tu Zhengchao

Chen Ji

Dates

2019-10-24Published

2015-11-18Filed