DERIVATIVES OF 7-(HETEROARYL-AMINO)-6,7,8,9-TETRAHYDROPYRIDO[1,2-a]INDOLE-ACETIC ACID AND USE THEREOF AS PROSTAGLANDIN D2 RECEPTOR MODULATORS Russian patent published in 2016 - IPC C07D471/04 A61K31/437 A61P37/08 

Abstract RU 2596823 C2

FIELD: chemistry.

SUBSTANCE: invention relates to derivatives of 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indole-acetic acid with formula (I) or pharmaceutically acceptable salt of such compound, where R1 and R2 represent independently of each other hydrogen, (C1-C4)alkyl, (C1-C4)alkoxy group, halogen, trifluoromethoxy group or trifluoromethyl; R3 represents hydrogen, (C1-C4)alkyl, (C1-C2)alkoxy-(C2-C3)alkyl, (C1-C4)fluoroalkyl or (C3-C6)cycloalkyl-(C1-C2)alkyl; and R4 represents heteroaryl group, which is unsubstituted or mono-substituted, where substitutes are independently selected from group comprising halogen, (C1-C4)alkyl, (C3-C6)cycloalkyl, (C1-C4)alkoxy group, (C1-C4)fluoroalkyl and phenyl; where term "heteroaryl" denotes 5-10-member monocyclic or bicyclic aromatic ring containing one nitrogen atom and optionally one additional heteroatom selected from oxygen, nitrogen and sulphur. Invention also relates to the pharmaceutical composition based on compound with formula (I) and application of compound with formula (I).

EFFECT: obtaining new heterocyclic compounds having antagonistic activity in relation to CRTH2 receptor.

17 cl, 19 dwg, 51 ex

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Authors

Essaui Khamed

Boss Kristof

Gabije Zherom

Rishar-Bildshtajn Silviya

Zigrist Romen

Dates

2016-09-10Published

2012-04-13Filed